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tetracaine

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Description

Tetracaine: A potent local anesthetic of the ester type used for surface and spinal anesthesia. [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

tetracaine : A benzoate ester in which 4-N-butylbenzoic acid and 2-(dimethylamino)ethanol have combined to form the ester bond; a local ester anaesthetic (ester caine) used for surface and spinal anaesthesia. [Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]

Cross-References

ID SourceID
PubMed CID5411
CHEMBL ID698
CHEBI ID9468
SCHEMBL ID34714
MeSH IDM0021210

Synonyms (157)

Synonym
diaethylaminoaethanol ester der p-butylaminobenzoesaeure
tetracainum
tetracaina
p-(butylamino)benzoic acid beta-(dimethylamino)ethyl ester
AC-3480
AB00053549-11
BRD-K45071273-003-05-8
benzoic acid, p-(butylamino)-, 2-(dimethylamino)ethyl ester
KBIO1_000607
DIVK1C_000607
anetain
einecs 202-316-6
brn 2216051
tetracainum [inn-latin]
fissucain
2-dimethylaminoethylester kyseliny p-butylaminobenzoove [czech]
dikain
medicaine
p-butylaminobenzoyl-2-dimethylaminoethanol
metraspray
contralgin
laudocaine
tetrakain [czech]
mucaesthin
pontocaine
meethobalm
dimethylaminoethyl p-butyl-aminobenzoate
intercain
2-(dimethylamino)ethyl p-(butylamino)benzoate
diaethylaminoaethanol ester der p-butylaminobenzoesaeure [german]
p-(butylamino)benzoic acid, 2-(dimethylamino)ethyl ester
rexocaine
niphanoid
medihaler-tetracaine
tetrakain
dicain
tetracaina [inn-spanish]
dicaine
uromucaesthin
SPECTRUM_001032
BSPBIO_000382
NCGC00016049-02
lopac-t-7508
cas-136-47-0
NCGC00016049-01
PRESTWICK2_000571
IDI1_000607
PRESTWICK3_000571
BSPBIO_001944
SPECTRUM5_001072
benzoic acid, 4-(butylamino)-, 2-(dimethylamino)ethyl ester
inchi=1/c15h24n2o2/c1-4-5-10-16-14-8-6-13(7-9-14)15(18)19-12-11-17(2)3/h6-9,16h,4-5,10-12h2,1-3h
2-(dimethylamino)ethyl 4-(butylamino)benzoate
benzoic acid,4-butylamino,2-dimethylaminoethyl ester pantocain base
AB00053549
94-24-6
C07526
amethocaine
tetracaine
tetracaine, meets usp testing specifications
D00551
tetracaine (usp/inn)
amethocaine (tn)
KBIOGR_000781
KBIOSS_001512
KBIO2_001512
KBIO3_001444
KBIO2_004080
KBIO2_006648
PRESTWICK1_000571
SPECTRUM3_000562
NINDS_000607
SPECTRUM4_000351
PRESTWICK0_000571
SPECTRUM2_001328
SPBIO_002601
SPBIO_001455
BPBIO1_000422
LOPAC0_001211
NCGC00162367-01
tetracaine, >=98% (tlc)
NCGC00016049-04
chebi:9468 ,
CHEMBL698 ,
FT-0656378
bdbm50017659
tetracaine base
100311-22-6
T2789
CCG-205285
NCGC00016049-03
4-(butylamino)benzoic acid 2-(dimethylamino)ethyl ester
BCPP000048
BCP0726000001
2-dimethylaminoethylester kyseliny p-butylaminobenzoove
unii-0619f35cgv
tetracaine [usp:inn:ban]
0619f35cgv ,
4-14-00-01172 (beilstein handbook reference)
EPITOPE ID:174843
AKOS015889234
STL483844
tetracaine [inn]
synera component tetracaine
tetracaine [usp-rs]
tetracaine [green book]
tetracaine [vandf]
tetracaine component of synera
tetracaine [mart.]
tetracaine [orange book]
tetracaine [who-dd]
tetracaine [usp monograph]
tetracaine [ep monograph]
TE4 ,
SCHEMBL34714
landocaine
pantocaine (salt/mix)
2-(dimethylamino)ethyl 4-(butylamino)benzoate #
.beta.-dimethylaminoethyl p-butylaminobenzoate
DTXSID1043883 ,
Q-201805
HY-A0079
2-(dimethylamino)ethyl4-(n-butylamino)benzoate
AB00053549_12
AB00053549_13
mfcd00053787
DB09085
amethocaine hcl
tetracaine, united states pharmacopeia (usp) reference standard
tetracain
SBI-0051178.P004
BCP04777
Q419608
SY066710
BRD-K45071273-003-15-7
SDCCGSBI-0051178.P005
NCGC00016049-14
AS-81743
EN300-6748839
blt 3
tetracainum (inn-latin)
tetracaine (usp monograph)
s01ha03
tetracaine (usp:inn:ban)
c05ad02
diathylaminoathanol ester der p-butylaminobenzosaure
numfast tetracaine green
tetracaine (usp-rs)
dtxcid9023883
n01ba03
tetracaine (ep monograph)
d04ab06
tetracaine (mart.)
franklynumb 3
tetracaina (inn-spanish)
burn solution cream
tetracaine cream

Research Excerpts

Overview

Tetracaine is a local anesthetic widely used in ocular diagnosis and ophthalmic surgery. Tetracaine inhibits ryanodine receptors (RyRs), the calcium release channels of the sarcoplasmic reticulum.

ExcerptReferenceRelevance
"Tetracaine is a local anesthetic drug used in the clinical setting as an ointment during urinary catheterization."( Tetracaine from urethral ointment causes false positive amphetamine results by immunoassay.
Brunet, M; Escalante, A; González-de-la-Presa, B; Marés, L; Parra-Robert, M; Salgado, E; To-Figueras, J; Wijngaard, R, 2021
)
2.79
"Tetracaine is a local anesthetic widely used in ocular diagnosis and ophthalmic surgery and may lead to some adverse effects and complications at a clinical dose. "( Tetracaine induces apoptosis through a mitochondrion-dependent pathway in human corneal stromal cells in vitro.
Fan, TJ; Song, Z, 2018
)
3.37
"Tetracaine is a tertiary amine local anaesthetic which inhibits ryanodine receptors (RyRs), the calcium release channels of the sarcoplasmic reticulum (SR). "( Three independent mechanisms contribute to tetracaine inhibition of cardiac calcium release channels.
Laver, DR; van Helden, DF, 2011
)
2.07
"Tetracaine is a good alternative to bupivacaine, currently controversial for intrathecal use."( [Isobaric spinal anaesthesia with bupivacaine and tetracaine (author's transl)].
Lanz, E; Schellenberg, B; Theiss, D, 1979
)
1.23
"Tetracaine, which is an inhibitor of protein kinase C, inhibited the TPA-induced secretion of [3H]phosphatidylcholine from alveolar type II cells in a dose-dependent manner."( Involvement of protein kinase C in pulmonary surfactant secretion from alveolar type II cells.
Mason, RJ; Sano, K; Voelker, DR, 1985
)
0.99

Effects

ExcerptReferenceRelevance
"Tetracaine has been extensively used to study the role of the SR Ca(2+) fluxes in muscle cells, yet a detailed understanding of tetracaine action on RyR channels is lacking."( Three independent mechanisms contribute to tetracaine inhibition of cardiac calcium release channels.
Laver, DR; van Helden, DF, 2011
)
1.35

Actions

Tetracaine appears to inhibit the saturable component whilst leaving the non-saturable component relatively unaffected. Tetracaine will enhance cocaine toxicity.

ExcerptReferenceRelevance
"Tetracaine appears to inhibit the saturable component whilst leaving the non-saturable component relatively unaffected."( Alpha-aminoisobutyric acid transport in rat soleus muscle and its modification by membrane stabilizers and insulin.
Cooper, GJ; Kohn, PG, 1980
)
0.98
"Tetracaine will enhance cocaine toxicity."( Tetracaine protects against cocaine lethality in mice.
Goldfrank, LR; Grant, SA; Hoffman, RS, 1993
)
3.17

Treatment

Tetracaine inhibited the extension of McTNs and their ability to promote tumor cell aggregation and reattachment. Tetracaine has no effect at 0 degrees C, a temperature at which there is only limited partitioning of the anesthetic into the bilayer.

ExcerptReferenceRelevance
"Tetracaine hydrochloride treatment resulted in translocation of hnRNPA1 from the nucleoplasm to the nuclear envelope and reduced the protein stability of hnRNPA1 possibly by disrupting the dynamic balance of ubiquitination and neddylation."( Tetracaine hydrochloride induces cell cycle arrest in melanoma by downregulating hnRNPA1.
Chen, Y; Feng, J; Huang, X; Jia, J; Jiang, X; Liao, Y; Yi, J; Yi, P, 2022
)
2.89
"Tetracaine treatment also significantly decreased the expression and activity levels of MMP-2 and MMP-9, whilst increasing TIMP-2 expression in MDA-MB-231 cells."( Tetracaine downregulates matrix metalloproteinase activity and inhibits invasiveness of strongly metastatic MDA-MB-231 human breast cancer cells.
Djamgoz, MB; İnanç-Sürer, Ş; Keleş, D; Oktay, G; Sipahi, M, 2023
)
3.07
"Tetracaine-treated females had accumulation patterns similar to courted but unmated females and to females exposed only to other females."( Differential effects of courtship and mating on receptivity and brain metabolism in female red-sided garter snakes (Thamnophis sirtalis parietalis).
Crews, D; Daniels, D; Faro, C; Mendonça, MT, 2003
)
1.04
"Tetracaine-pretreated rats showed equivalent or significantly greater decreases in licking behavior, suggesting that local anesthetic pretreatment either did not alter or enhanced development of desensitization to RTX."( Tetracaine attenuates irritancy without attenuating desensitization produced by intravesical resiniferatoxin in the rat.
Craft, RM; Porreca, F, 1994
)
2.45
"Treatment with Tetracaine inhibited the extension of McTNs and their ability to promote tumor cell aggregation and reattachment."( Local anesthetics inhibit kinesin motility and microtentacle protrusions in human epithelial and breast tumor cells.
Balzer, EM; Cho, EH; Martin, SS; Matrone, MA; Peckham, M; Whipple, RA; Yoon, JR, 2011
)
0.71
"Treatment with tetracaine has no effect at 0 degrees C, a temperature at which there is only limited partitioning of the anesthetic into the bilayer."( Trinitrobenzenesulfonic acid and fluorodinitrobenzene: probes to study local anesthetic effects in cell membranes.
Bradford, P; Marinetti, GV, 1981
)
0.6
"Rats treated with tetracaine at 10% or 20% developed lesions in the posterior white matter and posterior roots. "( Neurotoxicity of intrathecally administered tetracaine commences at the posterior roots near entry into the spinal cord.
Asato, F; Hoka, S; Takenami, T; Yagishita, S,
)
0.73
"Pretreatment with tetracaine or bupivacaine significantly prolonged the latency of rapid depolarization."( Bupivacaine, but not tetracaine, protects against the in vitro ischemic insult of rat hippocampal CA1 neurons.
Higashi, H; Kano, T; Niiyama, S; Tanaka, E; Yamamoto, S; Yasumoto, S, 2002
)
0.96

Toxicity

The objective of this study was to test the hypothesis that topical tetracaine would be safe to use for 24 hours and would not affect corneal healing. There were no serious complications or uncommon adverse e.

ExcerptReferenceRelevance
" We conclude that central nervous system toxic effects of amide/amide or amide/ester anesthetic combinations, such as might occur during accidental intravascular injection, are no more than when the drugs are administered alone."( Central nervous system toxicity of local anesthetic mixtures in the rat.
Baker, MT; Dexter, F; Spiegel, DA; Todd, MM; Warner, DS, 1992
)
0.28
" Dose-response curves were constructed from the data obtained, and the CD50 and LD50 values for each local anesthetic alone and in combination with each of the vasoconstrictors were calculated by probit analysis."( Modification of local anesthetic toxicity by vasoconstrictors.
Dorris, RL; Taylor, SE,
)
0.13
" These results suggest that the CNS is the primary target organ for the toxic effects of both highly lipid-soluble and highly protein-bound local anesthetics (i."( Comparative CNS toxicity of lidocaine, etidocaine, bupivacaine, and tetracaine in awake dogs following rapid intravenous administration.
Covino, BG; Feldman, HS; Giasi, R; Liu, PL; Patterson, MK, 1983
)
0.5
" No other adverse features were evident."( Evaluation of the efficacy and safety of amethocaine gel applied topically before venous cannulation in adults.
O'Connor, B; Tomlinson, AA, 1995
)
0.29
" It appears that spinal anesthesia is safe and effective for major operative procedures in high-risk infants."( Spinal anesthesia for primary repair of gastroschisis: a new and safe technique for selected patients.
Abajian, JC; Hong, AR; Vane, DW, 1994
)
0.29
" Synthetic local anesthetics such as tetracaine and proparacaine were developed which were more potent and less toxic than cocaine, but still produced corneal epithelium defects if used chronically."( Comparative toxicity of tetracaine, proparacaine and cocaine evaluated with primary cultures of rabbit corneal epithelial cells.
Acosta, D; Grant, RL, 1994
)
0.87
" No patient exhibited an adverse reaction related to TAC."( Safe and effective method for application of tetracaine, adrenaline, and cocaine to oral lacerations.
Bonadio, WA, 1996
)
0.55
"This TAC application technique was safe and highly effective in providing anesthesia for minor oral lacerations."( Safe and effective method for application of tetracaine, adrenaline, and cocaine to oral lacerations.
Bonadio, WA, 1996
)
0.55
" Proparacaine was statistically more toxic than were the others."( Corneal endothelial toxicity of topical anesthesia.
Judge, AJ; Lee, DA; Miller, KM; Najafi, K, 1997
)
0.3
"Sub-Tenon's anaesthesia is an efficient and safe anaesthetic technique."( Sub-Tenon's anaesthesia: an efficient and safe technique.
Auclin, FX; Boureau, CM; Chong Sit, DA; Roman, SJ; Ullern, MM, 1997
)
0.3
"Both tetracaine and proparacaine had toxic effects on stromal keratocytes related not only to drug concentrations but also to time exposure."( Toxicity of topical anesthetic agents to human keratocytes in vivo.
Kasetsuwan, N; LaBree, L; McDonnell, PJ; Moreira, LB; Sanchez, D; Shah, SS, 1999
)
0.82
" ischiadicus as a first sign of toxic side effects indicated that low effect is combined with short paresis."( Local anaesthetic effects and toxicity of seven new diethanolamine and morpholine derivatives of fomocaine. Testing in rats compared with procaine and tetracaine.
Fleck, C; Karge, E; Listing, M; Loy, S; Oelschläger, H; Wennek-Klose, J, 2003
)
0.52
" Immediately following the procedure, the subjects, the investigator, and an independent observer rated pain intensity and adverse events were recorded."( Self-warming lidocaine/tetracaine patch effectively and safely induces local anesthesia during minor dermatologic procedures.
Berman, B; de Araujo, T; Flores, J; Pariser, D; Pariser, R; Ramirez, CC, 2005
)
0.64
"The current study was conducted to determine whether topical anesthesia with oral sedation and without an anesthetist present in the operating room is a safe and cost-effective strategy for low-risk patients undergoing cataract surgery."( Safety of cataract surgery under topical anesthesia with oral sedation without anesthetic monitoring.
Rocha, G; Turner, C, 2007
)
0.34
" Oral sedation was provided by lorazepam, and an anesthetist was available to manage any medical adverse events."( Safety of cataract surgery under topical anesthesia with oral sedation without anesthetic monitoring.
Rocha, G; Turner, C, 2007
)
0.34
" No medical adverse events were reported in 454 cases (84."( Safety of cataract surgery under topical anesthesia with oral sedation without anesthetic monitoring.
Rocha, G; Turner, C, 2007
)
0.34
"Topical anesthesia appears to be a safe alternative to injection anesthesia without many of the disadvantages of the latter and may be preferable in carefully selected patients."( Safety of cataract surgery under topical anesthesia with oral sedation without anesthetic monitoring.
Rocha, G; Turner, C, 2007
)
0.34
" Specular microscopy performed at 30 days postoperatively showed a significantly greater loss of endothelial cells with the use of VisThesia, suggesting that the 1% lidocaine concentration used in VisThesia may be toxic to corneal endothelial cells."( Safety and efficacy of two ocular anesthetic methods for phacoemulsification: topical anesthesia and viscoanesthesia (VisThesia).
Herasymyuk, O; Ouled-Moussa, R; Perone, JM; Popovici, A; Reynders, S,
)
0.13
" Secondary outcomes included vital sign changes, soft-tissue anesthesia, and treatment-emergent adverse events."( Safety and efficacy of a novel nasal spray for maxillary dental anesthesia.
Almubarak, SA; Ayoub, F; Ciancio, SG; Garlapo, DA; Hutcheson, MC; Pantera, CT; Pantera, EA; Sobieraj, BD, 2013
)
0.39
"Data from this study demonstrate that topical anesthetic for facial rejuvenation can be enhanced with laser pretreatment while maintaining safe blood serum levels."( Topical lidocaine enhanced by laser pretreatment: a safe and effective method of analgesia for facial rejuvenation.
Kenkel, J; Oni, G; Rasko, Y, 2013
)
0.39
"The objective of this study was to test the hypothesis that topical tetracaine would be safe to use for 24 hours and would not affect corneal healing, that patients would experience more pain relief, and that patients would perceive tetracaine to be more effective than saline eye drops for the treatment of pain caused by corneal abrasions."( Topical tetracaine used for 24 hours is safe and rated highly effective by patients for the treatment of pain caused by corneal abrasions: a double-blind, randomized clinical trial.
Densie, IK; Herbison, P; Waldman, N, 2014
)
1.07
" Due to the lack of appreciable benefits and the presence of notable adverse effects, using vapocoolants or Cetacaine for this tail biopsy procedure in laboratory mice is unadvisable and we encourage the removal of these agents from institutional tail biopsy guidelines."( Adverse effects of vapocoolant and topical anesthesia for tail biopsy of preweanling mice.
Braden, GC; Brice, AK; Hankenson, FC, 2015
)
0.42
" All six studies demonstrated that a short course of dilute topical anesthetic provided efficacious analgesia without adverse effects or delayed epithelial healing."( The Safety of Topical Anesthetics in the Treatment of Corneal Abrasions: A Review.
Milne, K; Otterness, K; Rezaie, S; Swaminathan, A, 2015
)
0.42
"Systemic reactions from local tetracaine use are often an anomaly - not only is tetracaine short-acting and quickly metabolized by the pseudocholinesterase system leading to very limited systemic uptake, but most adverse reactions are usually associated with dental or spinal anesthesia."( Neurotoxicity secondary to local tetracaine use.
Adeleye, A; Rech, MA; Sharp, L, 2020
)
1.13

Pharmacokinetics

ExcerptReferenceRelevance
" The potential exists for the use of multiple heated patches for longer application times, but the pharmacokinetic properties and tolerability of these multiple and/or longer applications have not been assessed."( Effects of application durations and heat on the pharmacokinetic properties of drug delivered by a lidocaine/tetracaine patch: a randomized, open-label, controlled study in healthy volunteers.
Charney, MR; Marriott, TB; Stanworth, S, 2012
)
0.59
"The aim of this study was to assess the effects of heat and application time on the pharmacokinetic properties and tolerability of the patch after the application of 4 lidocaine/tetracaine (70/70 mg) heated patches applied at the same time in healthy volunteers for up to 12 hours."( Effects of application durations and heat on the pharmacokinetic properties of drug delivered by a lidocaine/tetracaine patch: a randomized, open-label, controlled study in healthy volunteers.
Charney, MR; Marriott, TB; Stanworth, S, 2012
)
0.78

Compound-Compound Interactions

Compound lidocaine/prilocaine cream combined with tetracaine may be a more effective approach for preventing coughing and stabilising circulation during extubation following general anaesthesia.

ExcerptReferenceRelevance
"The analgesic effect of subarachnoid administration of tetracaine combined with low dose morphine or nalbuphine for spinal anesthesia was evaluated in 60 ASA physical status class I or II patients."( [The analgesic effect of subarachnoid administration of tetracaine combined with low dose morphine or nalbuphine for spinal anesthesia].
Lin, ML, 1992
)
0.78
"A simple liquid-phase microextraction (LPME) device combined with high-performance liquid chromatography (HPLC) is presented for the simultaneous analysis of local anaesthetics, lidocaine, bupivacaine, and tetracaine, from human urine sample."( Liquid-phase microextraction combined with high-performance liquid chromatography for the determination of local anaesthetics in human urine.
Chen, B; Kang, S; Ma, M; Yao, S; Zhao, Q, 2006
)
0.52
" This study explored the safety and satisfaction of patients who received egg retrieval under vaginal topical tetracaine anesthesia combined with intravenous propofol anesthesia."( Tetracaine combined with propofol for painless oocyte retrieval: from a single center study.
Cheng, J; Cheng, Z; Guo, L; Li, C; Lu, Y; Qin, J; Shao, X; Zhou, L, 2020
)
2.21
"Results showed that tetracaine combined with propofol anesthesia could effectively reduce the dose of propofol during surgery, ensure the quality of follicles, effectively reduce the postoperative pain and improve the operational satisfaction without affecting the prognosis."( Tetracaine combined with propofol for painless oocyte retrieval: from a single center study.
Cheng, J; Cheng, Z; Guo, L; Li, C; Lu, Y; Qin, J; Shao, X; Zhou, L, 2020
)
2.32
" We speculated that the application of compound lidocaine/prilocaine combined with tetracaine spray would better prevent coughing caused by tracheal extubation."( Compound lidocaine/prilocaine cream combined with tetracaine prevents cough caused by extubation after general anaesthesia: a randomised controlled trial.
Gao, J; Li, T; Li, Y; Wang, M; Zhang, E; Zhang, H; Zhang, L; Zhao, X, 2023
)
1.39
"Patients scheduled for laparoscopic cholecystectomy or cholecystectomy combined with common bile duct exploration under general anaesthesia were randomly assigned to Group C (saline spray), Group L (2 g compound lidocaine/prilocaine cream contains 5 mg of lidocaine and 5 mg prilocaine)), Group T (tetracaine) and Group F (compound lidocaine/prilocaine cream combined with tetracaine)."( Compound lidocaine/prilocaine cream combined with tetracaine prevents cough caused by extubation after general anaesthesia: a randomised controlled trial.
Gao, J; Li, T; Li, Y; Wang, M; Zhang, E; Zhang, H; Zhang, L; Zhao, X, 2023
)
1.34
"Compound lidocaine/prilocaine cream combined with tetracaine may be a more effective approach for preventing coughing and stabilising circulation during extubation following general anaesthesia."( Compound lidocaine/prilocaine cream combined with tetracaine prevents cough caused by extubation after general anaesthesia: a randomised controlled trial.
Gao, J; Li, T; Li, Y; Wang, M; Zhang, E; Zhang, H; Zhang, L; Zhao, X, 2023
)
1.42

Bioavailability

ExcerptReferenceRelevance
" absorption rate is nearly a third of that of lidocaine or tetracaine."( Comparative subcutaneous absorption of local anesthetics: lidocaine, procaine and tetracaine.
Lustig, A; Menczel, E; Paran, I; Yacobi, A, 1977
)
0.73
"The bioavailability of topically applied ocular drugs is very poor, due largely to drug loss through drainage and tear turnover."( Influence of topical anesthesia on tear dynamics and ocular drug bioavailability in albino rabbits.
Patton, TF; Robinson, JR, 1975
)
0.25
"The choice of vehicle for patch test materials is important for the bioavailability and stability of the allergens."( Aspects of pharmaceutical and chemical standardization of patch test materials.
Hansen, J; Kreilgård, B, 1989
)
0.28
" Bioavailability was determined by area under the curve of the dose-response relationship with varying drop volumes."( Exponential Decay Metrics of Topical Tetracaine Hydrochloride Administration Describe Corneal Anesthesia Properties Mechanistically.
Ethington, J; Gaynes, BI; Goldmeier, D, 2017
)
0.73

Dosage Studied

The incidence of intraoperative supplemental analgesic and hypotension and the dosage of ephedrine used to treat hypotension were greater in the patients anesthetized with tetracaine 10 mg. The study was undertaken to define a dose-response relationship for clonidine in prolonging canine Tetracaine spinal anesthesia.

ExcerptRelevanceReference
"From a study on the interrelationship between electroshock-induced convulsions, autonomic function, catecholamines, and cardiovascular homeostasis in dogs, the authors found that: (1) the asystole of electroshock (ES) was significnatly prolonged by high spinal anesthesia but not by relative alpha- or beta-adrenergic blockade; (2) increased levels of circulating catecholamines were solely responsible for the marked hypertensive response to ES, since the pressor effect could be blocked by preventing the release of catecholamines with high spinal anesthesia or by inhibiting alpha-adrenergic receptors with phenoxybenzamine; (3) the adrenal medulla appeared to be the source of most of the ES-induced increase in circulating catecholamines; (4) the asystole and arrhythmias of ES were a cholinergic effect, since they were blocked by atropine; (5) there was a dose-response relationship between the coulombs of electricity administered and the catecholamine and cardiovascular responses; and (6) that the adverse cardiovascular effects of ES therapy could be ameliorated pharmacologically."( Autonomic blockade and the cardiovascular and catecholamine response to electroshock.
Anton, AH; Redderson, CL; Uy, DS,
)
0.13
" All the drugs caused rapid retraction of the neurites, which was reversible in all cases but for sodium dodecyl sulphate, and showed a sigmoid dose-response relationship."( Reversal of morphological differentiation of mouse neuroblastoma cells by mitosis-inhibitors and anesthetics.
Edström, A; Erkell, LJ; Hansson, HA, 1975
)
0.25
" For example, intermittent application of a particular dosage results in lower blood levels, and allowing sufficient time between doses reduces the amount necessary to obtain the desired anesthesia."( Local anesthesia in otolaryngology. A re-evaluation.
Schenck, NL,
)
0.13
" Dose-response curves were constructed from the data obtained, and the CD50 and LD50 values for each local anesthetic alone and in combination with each of the vasoconstrictors were calculated by probit analysis."( Modification of local anesthetic toxicity by vasoconstrictors.
Dorris, RL; Taylor, SE,
)
0.13
" In addition, the Ca2+ dose-response curves of both activities in intact platelets, obtained by stimulation with A23187 in the presence of Ca2+/HEDTA-buffers, were compared."( Correlation between calpain-mediated cytoskeletal degradation and expression of platelet procoagulant activity. A role for the platelet membrane-skeleton in the regulation of membrane lipid asymmetry?
Bevers, EM; Comfurius, P; Verhallen, PF; Zwaal, RF, 1987
)
0.27
"The study was undertaken to define a dose-response relationship for clonidine in prolonging canine tetracaine spinal anesthesia."( Dose-response relationship of clonidine in tetracaine spinal anesthesia.
Kehler, CH; Kozody, R; Mensink, FJ; Wade, JG, 1987
)
0.75
" The diffusion of 14-18% of the epidurally injected dosage of morphine and 18-27% of dikain through the dura mater takes place depending on the segmentary level."( [Experimental evaluation of dura mater permeability on a model of peridural analgesia with morphine and dikain].
Vitenbek, IA, 1987
)
0.27
" Dose-response curves for lignocaine, mepivacaine, bupivacaine, amethocaine and cinchocaine were obtained after single intrathecal injection to the mouse."( A methodological study of spinal (subarachnoid) anaesthesia in the rat and the mouse.
Akerman, SB, 1985
)
0.27
" Dose-response curves for the relaxation of muscle to these drugs were all in parallel."( Mechanisms of slow contracture induced by potassium and caffeine in skeletal muscle of the dog.
Aoyama, T; Ono, H; Sato, T, 1984
)
0.27
" Duration of activity of the compounds was greater than that of lidocaine, but less than that of tetracaine, with comparable dosage levels."( Local anesthetics: 2-N,N-dialkylaminoacyl-2'-methyl (or 2',6'-dimethyl)-4'-butylaminoanilides.
Foye, WO; Jan, CM; Takman, BH, 1982
)
0.48
" 3 The log dose-response curve for the contractile response of longitudinal muscle strips from guinea-pig intestine to carbachol was shifted in a parallel fashion by low concentrations of tetracaine, but flattened by higher doses."( The interaction of amine local anaesthetics with muscarinic receptors.
Taylor, WJ; Wolf, A; Young, JM, 1980
)
0.45
" Enhanced inactivation of BTX-modified Na+ channels by tetracaine was determined by steady-state inactivation measurement and by the dose-response curve."( Charged tetracaine as an inactivation enhancer in batrachotoxin-modified Na+ channels.
Mok, WM; Wang, GK; Wang, SY, 1994
)
0.97
" The rate of delivery of radiolabelled tetracaine from two different liposome formulas (1F2 and 23C2) and two conventional dosage forms (PEG Ointment USP and Glaxal base) was investigated in Flow-thru diffusion cells using human breast skin from mammoplasty."( In vitro cutaneous and percutaneous delivery and in vivo efficacy of tetracaine from liposomal and conventional vehicles.
Foldvari, M, 1994
)
0.79
" A tetracaine dose-response curve for HVA-ICa indicated an apparent dissociation constant of 79."( Local anesthetics depress the calcium current of rat sensory neurons in culture.
Muteki, T; Sugiyama, K, 1994
)
0.91
" Dose-response curves were plotted for each drug."( Duration of spinal anaesthesia is determined by the partition coefficient of local anaesthetic.
Benita, S; Golomb, E; Grant, GJ; Langerman, L, 1994
)
0.29
" Dose-response studies indicate that the optimum formulation for the diffusion of tetracaine in vivo is 60% free base and 40% acid salt (w/w) in 40% propylene glycol and 60% saline (v/v)."( Evaluation of local anesthesia provided by transdermal patches containing different formulations of tetracaine.
Goodwin, SR; Miller, KJ; Shah, DO; Westermann-Clark, GB, 1993
)
0.73
"9 (w/w) ratios, provided a stable, dermatologically acceptable dosage form, in which the liposomes were uniformly distributed and their structures were preserved."( Effect of vehicle on topical liposomal drug delivery: petrolatum bases.
Foldvari, M,
)
0.13
" Dose-response curves for tetracaine in the presence of saturating cGMP are well fit with a Michaelis-Menten binding scheme indicating that a single tetracaine molecule is sufficient to produce block."( Mechanism of tetracaine block of cyclic nucleotide-gated channels.
Fodor, AA; Gordon, SE; Zagotta, WN, 1997
)
0.97
" In another five cochleae an accumulated dose-response relationship was determined by increasing the tetracaine concentration in steps (50, 100, 300, 500, 1000 and 2000 microM), measuring the difference in amplitude of the receptor potentials."( Effects of local anaesthetics on the gross receptor potentials in the guinea pig cochlea.
Brundin, L; Flock, A; Idrizbegovic, E; Jäger, W, 1997
)
0.51
" Physicians must adhere to recommendations to avoid mucous membrane contact and ensure appropriate dosing with these agents."( Topical anesthesia.
Keyes, PD; Rizos, J; Tallon, JM, 1998
)
0.3
" There were no significant differences between the two groups with respect to ease of intubation, procedure performance, procedure duration, and dosing of midazolam or meperidine."( Topical pharyngeal anesthesia does not improve upper gastrointestinal endoscopy in conscious sedated patients.
Davis, DE; Jones, MP; Kubik, CM, 1999
)
0.3
" The results of this study indicate therefore that the novel bioadhesive patch provides clinically comparable anaesthesia to the established gel formulation in a more defined dosage form."( Novel bioadhesive delivery system for percutaneous local anaesthesia.
McCafferty, DF; Moss, GP; Woolfson, AD, 2000
)
0.31
"Successful spinal anesthesia in premature and former premature infants depends on close attention to preoperative assessment, patient positioning during and immediately after anesthetic induction, drug dosing and perioperative monitoring."( [Spinal anesthesia in premature infants--indications, technical aspects and results].
Erez, I; Freud, E; Gutermacher, M; Jedeikin, R; Lazar, L; Litmanowitz, I; Shenkman, Z; Shorer, S, 2002
)
0.31
" The incidence of intraoperative supplemental analgesic and hypotension and the dosage of ephedrine used to treat hypotension were greater in the patients anesthetized with tetracaine 10 mg than in those anesthetized with bupivacaine 10 mg, which is equipotent to tetracaine 10 mg."( [Spinal anesthesia using hyperbaric bupivacaine HCl for cesarean section].
Fukumitsu, K; Haruna, J; Hirao, O; Kawaraguchi, Y; Kinouchi, K; Kitamura, S; Matsuda, Y; Miyamoto, Y; Nakao, F; Taniguchi, A, 2003
)
0.51
" Lowering the dosage of local anesthetics is one of the methods to mitigate the side effects."( Minimal dosage of tetracaine supplemented with epinephrine for spinal anesthesia in anorectal surgery.
Huang, HW; Shiau, JM; Su, HP; Tseng, CC; Wang, KR, 2004
)
0.66
" Therefore, we undertook a dose-response study of hypobaric tetracaine for THR."( Hypobaric spinal anesthesia with 0.2% tetracaine for total joint hip arthroplasy.
Ahn, HJ; Kim, JA, 2005
)
0.84
"To compare a surgically adjusted dose of strabismus surgery using topical anesthesia in cooperative patients with dosage guidelines adapted to the surgeon's personal technique using sub-Tenon's anesthesia."( Surgery for esotropia under topical anesthesia.
Ogallar, C; Rodríguez, JM; Tejedor, J, 2010
)
0.36
" This information will help to guide dosing regimens for in vivo topical cross-linking studies."( Aliphatic β-nitroalcohols for therapeutic corneoscleral cross-linking: corneal permeability considerations.
Kim, M; Paik, DC; Trokel, SL; Wen, Q, 2013
)
0.39
" In this article, patient selection, lidocaine dosing and safety, and patient monitoring are reviewed."( Anesthesia for office procedures.
Simpson, CB; Wang, SX, 2013
)
0.39
" Patients continued prescribed analgesic dosing regimens."( Effectiveness of a heated lidocaine/tetracaine topical patch for pain associated with myofascial trigger points: results of an open-label pilot study.
Busch, M; Marriott, T; Rauck, R, 2013
)
0.66
" Both 27 and 48 demonstrated robust activity in the acute rat monoiodoacetate-induced osteoarthritis model of pain, and subchronic dosing of 48 showed a shift to a lower EC50 over 7 days."( Substituted Indazoles as Nav1.7 Blockers for the Treatment of Pain.
Daanen, JF; DeGoey, DA; El-Kouhen, OF; Fricano, MM; Frost, JM; Ghoreishi-Haack, N; Gum, RJ; Hsieh, GC; Kort, ME; Lundgaard, GL; Matulenko, MA; Neelands, T; Pai, M; Shi, L; Zhan, C; Zhang, XF, 2016
)
0.43
"To identify pharmacodynamic (PD) and pharmacokinetic (PK) metrics that aid in mechanistic understanding of dosage considerations for prolonged corneal anesthesia."( Exponential Decay Metrics of Topical Tetracaine Hydrochloride Administration Describe Corneal Anesthesia Properties Mechanistically.
Ethington, J; Gaynes, BI; Goldmeier, D, 2017
)
0.73
" Bioavailability was determined by area under the curve of the dose-response relationship with varying drop volumes."( Exponential Decay Metrics of Topical Tetracaine Hydrochloride Administration Describe Corneal Anesthesia Properties Mechanistically.
Ethington, J; Gaynes, BI; Goldmeier, D, 2017
)
0.73
"Use of a small drop volume of a topical anesthetic (as low as 11 μL) is bioequivalent to conventional drop size and seems to optimize dosing regiments with a little effect on ke."( Exponential Decay Metrics of Topical Tetracaine Hydrochloride Administration Describe Corneal Anesthesia Properties Mechanistically.
Ethington, J; Gaynes, BI; Goldmeier, D, 2017
)
0.73
" Methemoglobin and oxygen saturation levels did not change compared with baseline after dosing with either treatment."( A Proof-of-concept Study Using Quantitative Sensory Threshold Analysis to Compare Two Intraoral Topical Anesthetics.
Cooper, SA; Doyle, G; Farrar, JT; Giannakopoulos, H; Hersh, EV; Hutcheson, MC; Lesavoy, B; Mousavian, M; Secreto, S; Wang, P; Wang, S, 2019
)
0.51
" Myocytes superfused with 3-morpholinosydnonimine N-ethylcarbamide (SIN-1), an ONOO- donor, decreased the amplitude of Ca2+ transients and contraction in a dose-response (1-200 μM) manner."( Peroxynitrite-Induced Intracellular Ca2+ Depression in Cardiac Myocytes: Role of Sarco/Endoplasmic Reticulum Ca2+ Pump.
Escalante, B; Flores-Tamez, V; Rios, A, 2019
)
0.51
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Roles (1)

RoleDescription
local anaestheticAny member of a group of drugs that reversibly inhibit the propagation of signals along nerves. Wide variations in potency, stability, toxicity, water-solubility and duration of action determine the route used for administration, e.g. topical, intravenous, epidural or spinal block.
[role information is derived from Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]

Drug Classes (2)

ClassDescription
benzoate esterEsters of benzoic acid or substituted benzoic acids.
tertiary amino compoundA compound formally derived from ammonia by replacing three hydrogen atoms by organyl groups.
[compound class information is derived from Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]

Protein Targets (21)

Potency Measurements

ProteinTaxonomyMeasurementAverage (µ)Min (ref.)Avg (ref.)Max (ref.)Bioassay(s)
regulator of G-protein signaling 4Homo sapiens (human)Potency3.35870.531815.435837.6858AID504845
arylsulfatase AHomo sapiens (human)Potency0.15101.069113.955137.9330AID720538
euchromatic histone-lysine N-methyltransferase 2Homo sapiens (human)Potency4.74440.035520.977089.1251AID504332
mitogen-activated protein kinase 1Homo sapiens (human)Potency11.07920.039816.784239.8107AID995
histone acetyltransferase KAT2A isoform 1Homo sapiens (human)Potency2.23870.251215.843239.8107AID504327
muscarinic acetylcholine receptor M1Rattus norvegicus (Norway rat)Potency21.15460.00106.000935.4813AID943; AID944
lamin isoform A-delta10Homo sapiens (human)Potency12.58930.891312.067628.1838AID1487
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Inhibition Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Potassium channel subfamily K member 3Homo sapiens (human)IC50 (µMol)668.00000.00700.89855.1000AID1525553
5-hydroxytryptamine receptor 4Cavia porcellus (domestic guinea pig)IC50 (µMol)3.26800.00011.00768.7800AID625218
5-hydroxytryptamine receptor 4Cavia porcellus (domestic guinea pig)Ki1.71200.00000.887110.0000AID625218
Bile salt export pumpHomo sapiens (human)IC50 (µMol)512.90000.11007.190310.0000AID1449628
Amine oxidase [flavin-containing] AHomo sapiens (human)IC50 (µMol)0.31700.00002.37899.7700AID625150
5-hydroxytryptamine receptor 2AHomo sapiens (human)IC50 (µMol)3.41500.00010.88018.8500AID625192
5-hydroxytryptamine receptor 2AHomo sapiens (human)Ki0.97600.00000.385510.0000AID625192
5-hydroxytryptamine receptor 2CHomo sapiens (human)IC50 (µMol)3.26800.00011.03029.0000AID625218
5-hydroxytryptamine receptor 2CHomo sapiens (human)Ki1.71200.00010.954910.0000AID625218
Sodium channel protein type 7 subunit alphaHomo sapiens (human)IC50 (µMol)0.05600.03603.73359.0000AID1891560
Sodium channel protein type 5 subunit alphaHomo sapiens (human)IC50 (µMol)0.50750.00033.64849.2000AID1296888; AID1366271; AID1891570; AID700026
Sodium channel protein type 9 subunit alphaHomo sapiens (human)IC50 (µMol)1.46930.00602.77499.0000AID1296884; AID1296885; AID1366216; AID599097; AID700027; AID700028
Sodium channel protein type 9 subunit alphaHomo sapiens (human)Ki6.25000.36000.43000.5000AID611515; AID611516
Sodium channel protein type 2 subunit alphaHomo sapiens (human)IC50 (µMol)0.79500.00003.740110.0000AID1296896; AID700020
Sigma non-opioid intracellular receptor 1Homo sapiens (human)IC50 (µMol)1.67300.00030.70285.3660AID625223
Sigma non-opioid intracellular receptor 1Homo sapiens (human)Ki0.70300.00000.490110.0000AID625223
Sodium channel protein type 3 subunit alphaHomo sapiens (human)IC50 (µMol)0.74000.00532.80859.0000AID1296897
Sodium channel protein type 8 subunit alphaHomo sapiens (human)IC50 (µMol)0.52000.00113.47059.0000AID1296898
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Activation Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
cGMP-gated cation channel alpha-1Bos taurus (cattle)Kd9.40006.80006.80006.8000AID254235; AID254236
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (149)

Processvia Protein(s)Taxonomy
potassium ion transportPotassium channel subfamily K member 3Homo sapiens (human)
chemical synaptic transmissionPotassium channel subfamily K member 3Homo sapiens (human)
response to xenobiotic stimulusPotassium channel subfamily K member 3Homo sapiens (human)
monoatomic ion transmembrane transportPotassium channel subfamily K member 3Homo sapiens (human)
negative regulation of cytosolic calcium ion concentrationPotassium channel subfamily K member 3Homo sapiens (human)
regulation of resting membrane potentialPotassium channel subfamily K member 3Homo sapiens (human)
cellular response to zinc ionPotassium channel subfamily K member 3Homo sapiens (human)
cellular response to hypoxiaPotassium channel subfamily K member 3Homo sapiens (human)
cochlea developmentPotassium channel subfamily K member 3Homo sapiens (human)
potassium ion transmembrane transportPotassium channel subfamily K member 3Homo sapiens (human)
stabilization of membrane potentialPotassium channel subfamily K member 3Homo sapiens (human)
fatty acid metabolic processBile salt export pumpHomo sapiens (human)
bile acid biosynthetic processBile salt export pumpHomo sapiens (human)
xenobiotic metabolic processBile salt export pumpHomo sapiens (human)
xenobiotic transmembrane transportBile salt export pumpHomo sapiens (human)
response to oxidative stressBile salt export pumpHomo sapiens (human)
bile acid metabolic processBile salt export pumpHomo sapiens (human)
response to organic cyclic compoundBile salt export pumpHomo sapiens (human)
bile acid and bile salt transportBile salt export pumpHomo sapiens (human)
canalicular bile acid transportBile salt export pumpHomo sapiens (human)
protein ubiquitinationBile salt export pumpHomo sapiens (human)
regulation of fatty acid beta-oxidationBile salt export pumpHomo sapiens (human)
carbohydrate transmembrane transportBile salt export pumpHomo sapiens (human)
bile acid signaling pathwayBile salt export pumpHomo sapiens (human)
cholesterol homeostasisBile salt export pumpHomo sapiens (human)
response to estrogenBile salt export pumpHomo sapiens (human)
response to ethanolBile salt export pumpHomo sapiens (human)
xenobiotic export from cellBile salt export pumpHomo sapiens (human)
lipid homeostasisBile salt export pumpHomo sapiens (human)
phospholipid homeostasisBile salt export pumpHomo sapiens (human)
positive regulation of bile acid secretionBile salt export pumpHomo sapiens (human)
regulation of bile acid metabolic processBile salt export pumpHomo sapiens (human)
transmembrane transportBile salt export pumpHomo sapiens (human)
biogenic amine metabolic processAmine oxidase [flavin-containing] AHomo sapiens (human)
positive regulation of signal transductionAmine oxidase [flavin-containing] AHomo sapiens (human)
dopamine catabolic processAmine oxidase [flavin-containing] AHomo sapiens (human)
temperature homeostasis5-hydroxytryptamine receptor 2AHomo sapiens (human)
positive regulation of cytokine production involved in immune response5-hydroxytryptamine receptor 2AHomo sapiens (human)
glycolytic process5-hydroxytryptamine receptor 2AHomo sapiens (human)
intracellular calcium ion homeostasis5-hydroxytryptamine receptor 2AHomo sapiens (human)
activation of phospholipase C activity5-hydroxytryptamine receptor 2AHomo sapiens (human)
positive regulation of cytosolic calcium ion concentration5-hydroxytryptamine receptor 2AHomo sapiens (human)
memory5-hydroxytryptamine receptor 2AHomo sapiens (human)
positive regulation of cell population proliferation5-hydroxytryptamine receptor 2AHomo sapiens (human)
response to xenobiotic stimulus5-hydroxytryptamine receptor 2AHomo sapiens (human)
positive regulation of phosphatidylinositol biosynthetic process5-hydroxytryptamine receptor 2AHomo sapiens (human)
regulation of dopamine secretion5-hydroxytryptamine receptor 2AHomo sapiens (human)
artery smooth muscle contraction5-hydroxytryptamine receptor 2AHomo sapiens (human)
urinary bladder smooth muscle contraction5-hydroxytryptamine receptor 2AHomo sapiens (human)
positive regulation of heat generation5-hydroxytryptamine receptor 2AHomo sapiens (human)
negative regulation of potassium ion transport5-hydroxytryptamine receptor 2AHomo sapiens (human)
phosphatidylinositol 3-kinase/protein kinase B signal transduction5-hydroxytryptamine receptor 2AHomo sapiens (human)
positive regulation of neuron apoptotic process5-hydroxytryptamine receptor 2AHomo sapiens (human)
protein localization to cytoskeleton5-hydroxytryptamine receptor 2AHomo sapiens (human)
positive regulation of fat cell differentiation5-hydroxytryptamine receptor 2AHomo sapiens (human)
positive regulation of glycolytic process5-hydroxytryptamine receptor 2AHomo sapiens (human)
positive regulation of vasoconstriction5-hydroxytryptamine receptor 2AHomo sapiens (human)
symbiont entry into host cell5-hydroxytryptamine receptor 2AHomo sapiens (human)
sensitization5-hydroxytryptamine receptor 2AHomo sapiens (human)
behavioral response to cocaine5-hydroxytryptamine receptor 2AHomo sapiens (human)
positive regulation of inflammatory response5-hydroxytryptamine receptor 2AHomo sapiens (human)
positive regulation of peptidyl-tyrosine phosphorylation5-hydroxytryptamine receptor 2AHomo sapiens (human)
detection of temperature stimulus involved in sensory perception of pain5-hydroxytryptamine receptor 2AHomo sapiens (human)
detection of mechanical stimulus involved in sensory perception of pain5-hydroxytryptamine receptor 2AHomo sapiens (human)
release of sequestered calcium ion into cytosol5-hydroxytryptamine receptor 2AHomo sapiens (human)
negative regulation of synaptic transmission, glutamatergic5-hydroxytryptamine receptor 2AHomo sapiens (human)
positive regulation of ERK1 and ERK2 cascade5-hydroxytryptamine receptor 2AHomo sapiens (human)
G protein-coupled serotonin receptor signaling pathway5-hydroxytryptamine receptor 2AHomo sapiens (human)
presynaptic modulation of chemical synaptic transmission5-hydroxytryptamine receptor 2AHomo sapiens (human)
positive regulation of execution phase of apoptosis5-hydroxytryptamine receptor 2AHomo sapiens (human)
positive regulation of platelet aggregation5-hydroxytryptamine receptor 2AHomo sapiens (human)
positive regulation of DNA biosynthetic process5-hydroxytryptamine receptor 2AHomo sapiens (human)
G protein-coupled receptor signaling pathway, coupled to cyclic nucleotide second messenger5-hydroxytryptamine receptor 2AHomo sapiens (human)
phospholipase C-activating serotonin receptor signaling pathway5-hydroxytryptamine receptor 2AHomo sapiens (human)
serotonin receptor signaling pathway5-hydroxytryptamine receptor 2AHomo sapiens (human)
chemical synaptic transmission5-hydroxytryptamine receptor 2AHomo sapiens (human)
behavioral fear response5-hydroxytryptamine receptor 2CHomo sapiens (human)
intracellular calcium ion homeostasis5-hydroxytryptamine receptor 2CHomo sapiens (human)
phospholipase C-activating G protein-coupled receptor signaling pathway5-hydroxytryptamine receptor 2CHomo sapiens (human)
phospholipase C-activating serotonin receptor signaling pathway5-hydroxytryptamine receptor 2CHomo sapiens (human)
locomotory behavior5-hydroxytryptamine receptor 2CHomo sapiens (human)
feeding behavior5-hydroxytryptamine receptor 2CHomo sapiens (human)
positive regulation of phosphatidylinositol biosynthetic process5-hydroxytryptamine receptor 2CHomo sapiens (human)
cGMP-mediated signaling5-hydroxytryptamine receptor 2CHomo sapiens (human)
regulation of nervous system process5-hydroxytryptamine receptor 2CHomo sapiens (human)
regulation of appetite5-hydroxytryptamine receptor 2CHomo sapiens (human)
regulation of corticotropin-releasing hormone secretion5-hydroxytryptamine receptor 2CHomo sapiens (human)
positive regulation of fat cell differentiation5-hydroxytryptamine receptor 2CHomo sapiens (human)
positive regulation of calcium-mediated signaling5-hydroxytryptamine receptor 2CHomo sapiens (human)
release of sequestered calcium ion into cytosol5-hydroxytryptamine receptor 2CHomo sapiens (human)
positive regulation of ERK1 and ERK2 cascade5-hydroxytryptamine receptor 2CHomo sapiens (human)
G protein-coupled serotonin receptor signaling pathway5-hydroxytryptamine receptor 2CHomo sapiens (human)
serotonin receptor signaling pathway5-hydroxytryptamine receptor 2CHomo sapiens (human)
G protein-coupled receptor signaling pathway, coupled to cyclic nucleotide second messenger5-hydroxytryptamine receptor 2CHomo sapiens (human)
chemical synaptic transmission5-hydroxytryptamine receptor 2CHomo sapiens (human)
monoatomic cation transportcGMP-gated cation channel alpha-1Bos taurus (cattle)
sodium ion transportcGMP-gated cation channel alpha-1Bos taurus (cattle)
calcium ion transportcGMP-gated cation channel alpha-1Bos taurus (cattle)
visual perceptioncGMP-gated cation channel alpha-1Bos taurus (cattle)
sodium ion transmembrane transportcGMP-gated cation channel alpha-1Bos taurus (cattle)
calcium ion transmembrane transportcGMP-gated cation channel alpha-1Bos taurus (cattle)
osmosensory signaling pathwaySodium channel protein type 7 subunit alphaHomo sapiens (human)
response to bacteriumSodium channel protein type 7 subunit alphaHomo sapiens (human)
cellular homeostasisSodium channel protein type 7 subunit alphaHomo sapiens (human)
sodium ion homeostasisSodium channel protein type 7 subunit alphaHomo sapiens (human)
cardiac muscle cell action potential involved in contractionSodium channel protein type 7 subunit alphaHomo sapiens (human)
sodium ion transmembrane transportSodium channel protein type 7 subunit alphaHomo sapiens (human)
regulation of heart rateSodium channel protein type 5 subunit alphaHomo sapiens (human)
cardiac conduction system developmentSodium channel protein type 5 subunit alphaHomo sapiens (human)
cardiac ventricle developmentSodium channel protein type 5 subunit alphaHomo sapiens (human)
brainstem developmentSodium channel protein type 5 subunit alphaHomo sapiens (human)
sodium ion transportSodium channel protein type 5 subunit alphaHomo sapiens (human)
positive regulation of sodium ion transportSodium channel protein type 5 subunit alphaHomo sapiens (human)
response to denervation involved in regulation of muscle adaptationSodium channel protein type 5 subunit alphaHomo sapiens (human)
telencephalon developmentSodium channel protein type 5 subunit alphaHomo sapiens (human)
cerebellum developmentSodium channel protein type 5 subunit alphaHomo sapiens (human)
sodium ion transmembrane transportSodium channel protein type 5 subunit alphaHomo sapiens (human)
odontogenesis of dentin-containing toothSodium channel protein type 5 subunit alphaHomo sapiens (human)
positive regulation of action potentialSodium channel protein type 5 subunit alphaHomo sapiens (human)
positive regulation of epithelial cell proliferationSodium channel protein type 5 subunit alphaHomo sapiens (human)
membrane depolarizationSodium channel protein type 5 subunit alphaHomo sapiens (human)
cardiac muscle contractionSodium channel protein type 5 subunit alphaHomo sapiens (human)
regulation of ventricular cardiac muscle cell membrane repolarizationSodium channel protein type 5 subunit alphaHomo sapiens (human)
regulation of atrial cardiac muscle cell membrane depolarizationSodium channel protein type 5 subunit alphaHomo sapiens (human)
regulation of atrial cardiac muscle cell membrane repolarizationSodium channel protein type 5 subunit alphaHomo sapiens (human)
regulation of ventricular cardiac muscle cell membrane depolarizationSodium channel protein type 5 subunit alphaHomo sapiens (human)
cellular response to calcium ionSodium channel protein type 5 subunit alphaHomo sapiens (human)
cardiac muscle cell action potential involved in contractionSodium channel protein type 5 subunit alphaHomo sapiens (human)
regulation of cardiac muscle cell contractionSodium channel protein type 5 subunit alphaHomo sapiens (human)
ventricular cardiac muscle cell action potentialSodium channel protein type 5 subunit alphaHomo sapiens (human)
membrane depolarization during action potentialSodium channel protein type 5 subunit alphaHomo sapiens (human)
membrane depolarization during cardiac muscle cell action potentialSodium channel protein type 5 subunit alphaHomo sapiens (human)
atrial cardiac muscle cell action potentialSodium channel protein type 5 subunit alphaHomo sapiens (human)
SA node cell action potentialSodium channel protein type 5 subunit alphaHomo sapiens (human)
AV node cell action potentialSodium channel protein type 5 subunit alphaHomo sapiens (human)
bundle of His cell action potentialSodium channel protein type 5 subunit alphaHomo sapiens (human)
membrane depolarization during AV node cell action potentialSodium channel protein type 5 subunit alphaHomo sapiens (human)
membrane depolarization during SA node cell action potentialSodium channel protein type 5 subunit alphaHomo sapiens (human)
membrane depolarization during Purkinje myocyte cell action potentialSodium channel protein type 5 subunit alphaHomo sapiens (human)
membrane depolarization during bundle of His cell action potentialSodium channel protein type 5 subunit alphaHomo sapiens (human)
AV node cell to bundle of His cell communicationSodium channel protein type 5 subunit alphaHomo sapiens (human)
regulation of heart rate by cardiac conductionSodium channel protein type 5 subunit alphaHomo sapiens (human)
membrane depolarization during atrial cardiac muscle cell action potentialSodium channel protein type 5 subunit alphaHomo sapiens (human)
regulation of sodium ion transmembrane transportSodium channel protein type 5 subunit alphaHomo sapiens (human)
sodium ion transportSodium channel protein type 9 subunit alphaHomo sapiens (human)
inflammatory responseSodium channel protein type 9 subunit alphaHomo sapiens (human)
circadian rhythmSodium channel protein type 9 subunit alphaHomo sapiens (human)
response to toxic substanceSodium channel protein type 9 subunit alphaHomo sapiens (human)
post-embryonic developmentSodium channel protein type 9 subunit alphaHomo sapiens (human)
sensory perception of painSodium channel protein type 9 subunit alphaHomo sapiens (human)
sodium ion transmembrane transportSodium channel protein type 9 subunit alphaHomo sapiens (human)
behavioral response to painSodium channel protein type 9 subunit alphaHomo sapiens (human)
detection of temperature stimulus involved in sensory perception of painSodium channel protein type 9 subunit alphaHomo sapiens (human)
detection of mechanical stimulus involved in sensory perceptionSodium channel protein type 9 subunit alphaHomo sapiens (human)
cardiac muscle cell action potential involved in contractionSodium channel protein type 9 subunit alphaHomo sapiens (human)
sodium ion transportSodium channel protein type 2 subunit alphaHomo sapiens (human)
nervous system developmentSodium channel protein type 2 subunit alphaHomo sapiens (human)
intrinsic apoptotic signaling pathway in response to osmotic stressSodium channel protein type 2 subunit alphaHomo sapiens (human)
neuron apoptotic processSodium channel protein type 2 subunit alphaHomo sapiens (human)
memorySodium channel protein type 2 subunit alphaHomo sapiens (human)
determination of adult lifespanSodium channel protein type 2 subunit alphaHomo sapiens (human)
neuronal action potentialSodium channel protein type 2 subunit alphaHomo sapiens (human)
dentate gyrus developmentSodium channel protein type 2 subunit alphaHomo sapiens (human)
nerve developmentSodium channel protein type 2 subunit alphaHomo sapiens (human)
myelinationSodium channel protein type 2 subunit alphaHomo sapiens (human)
cellular response to hypoxiaSodium channel protein type 2 subunit alphaHomo sapiens (human)
cardiac muscle cell action potential involved in contractionSodium channel protein type 2 subunit alphaHomo sapiens (human)
sodium ion transmembrane transportSodium channel protein type 2 subunit alphaHomo sapiens (human)
lipid transportSigma non-opioid intracellular receptor 1Homo sapiens (human)
nervous system developmentSigma non-opioid intracellular receptor 1Homo sapiens (human)
G protein-coupled opioid receptor signaling pathwaySigma non-opioid intracellular receptor 1Homo sapiens (human)
regulation of neuron apoptotic processSigma non-opioid intracellular receptor 1Homo sapiens (human)
protein homotrimerizationSigma non-opioid intracellular receptor 1Homo sapiens (human)
sodium ion transportSodium channel protein type 3 subunit alphaHomo sapiens (human)
behavioral response to painSodium channel protein type 3 subunit alphaHomo sapiens (human)
cardiac muscle cell action potential involved in contractionSodium channel protein type 3 subunit alphaHomo sapiens (human)
sodium ion transmembrane transportSodium channel protein type 3 subunit alphaHomo sapiens (human)
sodium ion transportSodium channel protein type 8 subunit alphaHomo sapiens (human)
nervous system developmentSodium channel protein type 8 subunit alphaHomo sapiens (human)
peripheral nervous system developmentSodium channel protein type 8 subunit alphaHomo sapiens (human)
neuronal action potentialSodium channel protein type 8 subunit alphaHomo sapiens (human)
optic nerve developmentSodium channel protein type 8 subunit alphaHomo sapiens (human)
myelinationSodium channel protein type 8 subunit alphaHomo sapiens (human)
sodium ion transmembrane transportSodium channel protein type 8 subunit alphaHomo sapiens (human)
cardiac muscle cell action potential involved in contractionSodium channel protein type 8 subunit alphaHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (52)

Processvia Protein(s)Taxonomy
monoatomic ion channel activityPotassium channel subfamily K member 3Homo sapiens (human)
open rectifier potassium channel activityPotassium channel subfamily K member 3Homo sapiens (human)
potassium channel activityPotassium channel subfamily K member 3Homo sapiens (human)
potassium ion leak channel activityPotassium channel subfamily K member 3Homo sapiens (human)
S100 protein bindingPotassium channel subfamily K member 3Homo sapiens (human)
outward rectifier potassium channel activityPotassium channel subfamily K member 3Homo sapiens (human)
protein bindingBile salt export pumpHomo sapiens (human)
ATP bindingBile salt export pumpHomo sapiens (human)
ABC-type xenobiotic transporter activityBile salt export pumpHomo sapiens (human)
bile acid transmembrane transporter activityBile salt export pumpHomo sapiens (human)
canalicular bile acid transmembrane transporter activityBile salt export pumpHomo sapiens (human)
carbohydrate transmembrane transporter activityBile salt export pumpHomo sapiens (human)
ABC-type bile acid transporter activityBile salt export pumpHomo sapiens (human)
ATP hydrolysis activityBile salt export pumpHomo sapiens (human)
protein bindingAmine oxidase [flavin-containing] AHomo sapiens (human)
primary amine oxidase activityAmine oxidase [flavin-containing] AHomo sapiens (human)
aliphatic amine oxidase activityAmine oxidase [flavin-containing] AHomo sapiens (human)
monoamine oxidase activityAmine oxidase [flavin-containing] AHomo sapiens (human)
flavin adenine dinucleotide bindingAmine oxidase [flavin-containing] AHomo sapiens (human)
Gq/11-coupled serotonin receptor activity5-hydroxytryptamine receptor 2AHomo sapiens (human)
virus receptor activity5-hydroxytryptamine receptor 2AHomo sapiens (human)
G protein-coupled serotonin receptor activity5-hydroxytryptamine receptor 2AHomo sapiens (human)
protein binding5-hydroxytryptamine receptor 2AHomo sapiens (human)
protein tyrosine kinase activator activity5-hydroxytryptamine receptor 2AHomo sapiens (human)
identical protein binding5-hydroxytryptamine receptor 2AHomo sapiens (human)
protein-containing complex binding5-hydroxytryptamine receptor 2AHomo sapiens (human)
serotonin binding5-hydroxytryptamine receptor 2AHomo sapiens (human)
1-(4-iodo-2,5-dimethoxyphenyl)propan-2-amine binding5-hydroxytryptamine receptor 2AHomo sapiens (human)
neurotransmitter receptor activity5-hydroxytryptamine receptor 2AHomo sapiens (human)
Gq/11-coupled serotonin receptor activity5-hydroxytryptamine receptor 2CHomo sapiens (human)
G protein-coupled serotonin receptor activity5-hydroxytryptamine receptor 2CHomo sapiens (human)
protein binding5-hydroxytryptamine receptor 2CHomo sapiens (human)
identical protein binding5-hydroxytryptamine receptor 2CHomo sapiens (human)
serotonin binding5-hydroxytryptamine receptor 2CHomo sapiens (human)
1-(4-iodo-2,5-dimethoxyphenyl)propan-2-amine binding5-hydroxytryptamine receptor 2CHomo sapiens (human)
neurotransmitter receptor activity5-hydroxytryptamine receptor 2CHomo sapiens (human)
intracellularly cAMP-activated cation channel activitycGMP-gated cation channel alpha-1Bos taurus (cattle)
intracellularly cGMP-activated cation channel activitycGMP-gated cation channel alpha-1Bos taurus (cattle)
calcium channel activitycGMP-gated cation channel alpha-1Bos taurus (cattle)
sodium channel activitycGMP-gated cation channel alpha-1Bos taurus (cattle)
cAMP bindingcGMP-gated cation channel alpha-1Bos taurus (cattle)
cGMP bindingcGMP-gated cation channel alpha-1Bos taurus (cattle)
sodium channel activitySodium channel protein type 7 subunit alphaHomo sapiens (human)
transmembrane transporter bindingSodium channel protein type 7 subunit alphaHomo sapiens (human)
osmolarity-sensing monoatomic cation channel activitySodium channel protein type 7 subunit alphaHomo sapiens (human)
voltage-gated sodium channel activitySodium channel protein type 7 subunit alphaHomo sapiens (human)
voltage-gated sodium channel activitySodium channel protein type 5 subunit alphaHomo sapiens (human)
protein bindingSodium channel protein type 5 subunit alphaHomo sapiens (human)
calmodulin bindingSodium channel protein type 5 subunit alphaHomo sapiens (human)
fibroblast growth factor bindingSodium channel protein type 5 subunit alphaHomo sapiens (human)
enzyme bindingSodium channel protein type 5 subunit alphaHomo sapiens (human)
protein kinase bindingSodium channel protein type 5 subunit alphaHomo sapiens (human)
protein domain specific bindingSodium channel protein type 5 subunit alphaHomo sapiens (human)
ankyrin bindingSodium channel protein type 5 subunit alphaHomo sapiens (human)
ubiquitin protein ligase bindingSodium channel protein type 5 subunit alphaHomo sapiens (human)
transmembrane transporter bindingSodium channel protein type 5 subunit alphaHomo sapiens (human)
nitric-oxide synthase bindingSodium channel protein type 5 subunit alphaHomo sapiens (human)
voltage-gated sodium channel activity involved in cardiac muscle cell action potentialSodium channel protein type 5 subunit alphaHomo sapiens (human)
voltage-gated sodium channel activity involved in AV node cell action potentialSodium channel protein type 5 subunit alphaHomo sapiens (human)
voltage-gated sodium channel activity involved in bundle of His cell action potentialSodium channel protein type 5 subunit alphaHomo sapiens (human)
voltage-gated sodium channel activity involved in Purkinje myocyte action potentialSodium channel protein type 5 subunit alphaHomo sapiens (human)
voltage-gated sodium channel activity involved in SA node cell action potentialSodium channel protein type 5 subunit alphaHomo sapiens (human)
scaffold protein bindingSodium channel protein type 5 subunit alphaHomo sapiens (human)
voltage-gated sodium channel activitySodium channel protein type 9 subunit alphaHomo sapiens (human)
protein bindingSodium channel protein type 9 subunit alphaHomo sapiens (human)
voltage-gated sodium channel activitySodium channel protein type 2 subunit alphaHomo sapiens (human)
protein bindingSodium channel protein type 2 subunit alphaHomo sapiens (human)
calmodulin bindingSodium channel protein type 2 subunit alphaHomo sapiens (human)
G protein-coupled opioid receptor activitySigma non-opioid intracellular receptor 1Homo sapiens (human)
protein bindingSigma non-opioid intracellular receptor 1Homo sapiens (human)
voltage-gated sodium channel activitySodium channel protein type 3 subunit alphaHomo sapiens (human)
voltage-gated sodium channel activitySodium channel protein type 8 subunit alphaHomo sapiens (human)
protein bindingSodium channel protein type 8 subunit alphaHomo sapiens (human)
ATP bindingSodium channel protein type 8 subunit alphaHomo sapiens (human)
sodium ion bindingSodium channel protein type 8 subunit alphaHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (58)

Processvia Protein(s)Taxonomy
plasma membranePotassium channel subfamily K member 3Homo sapiens (human)
synapsePotassium channel subfamily K member 3Homo sapiens (human)
plasma membranePotassium channel subfamily K member 3Homo sapiens (human)
basolateral plasma membraneBile salt export pumpHomo sapiens (human)
Golgi membraneBile salt export pumpHomo sapiens (human)
endosomeBile salt export pumpHomo sapiens (human)
plasma membraneBile salt export pumpHomo sapiens (human)
cell surfaceBile salt export pumpHomo sapiens (human)
apical plasma membraneBile salt export pumpHomo sapiens (human)
intercellular canaliculusBile salt export pumpHomo sapiens (human)
intracellular canaliculusBile salt export pumpHomo sapiens (human)
recycling endosomeBile salt export pumpHomo sapiens (human)
recycling endosome membraneBile salt export pumpHomo sapiens (human)
extracellular exosomeBile salt export pumpHomo sapiens (human)
membraneBile salt export pumpHomo sapiens (human)
mitochondrionAmine oxidase [flavin-containing] AHomo sapiens (human)
mitochondrial outer membraneAmine oxidase [flavin-containing] AHomo sapiens (human)
cytosolAmine oxidase [flavin-containing] AHomo sapiens (human)
mitochondrionAmine oxidase [flavin-containing] AHomo sapiens (human)
neurofilament5-hydroxytryptamine receptor 2AHomo sapiens (human)
plasma membrane5-hydroxytryptamine receptor 2AHomo sapiens (human)
caveola5-hydroxytryptamine receptor 2AHomo sapiens (human)
axon5-hydroxytryptamine receptor 2AHomo sapiens (human)
cytoplasmic vesicle5-hydroxytryptamine receptor 2AHomo sapiens (human)
presynaptic membrane5-hydroxytryptamine receptor 2AHomo sapiens (human)
neuronal cell body5-hydroxytryptamine receptor 2AHomo sapiens (human)
dendritic shaft5-hydroxytryptamine receptor 2AHomo sapiens (human)
postsynaptic membrane5-hydroxytryptamine receptor 2AHomo sapiens (human)
cell body fiber5-hydroxytryptamine receptor 2AHomo sapiens (human)
glutamatergic synapse5-hydroxytryptamine receptor 2AHomo sapiens (human)
G protein-coupled serotonin receptor complex5-hydroxytryptamine receptor 2AHomo sapiens (human)
plasma membrane5-hydroxytryptamine receptor 2AHomo sapiens (human)
dendrite5-hydroxytryptamine receptor 2AHomo sapiens (human)
plasma membrane5-hydroxytryptamine receptor 2CHomo sapiens (human)
synapse5-hydroxytryptamine receptor 2CHomo sapiens (human)
G protein-coupled serotonin receptor complex5-hydroxytryptamine receptor 2CHomo sapiens (human)
plasma membrane5-hydroxytryptamine receptor 2CHomo sapiens (human)
dendrite5-hydroxytryptamine receptor 2CHomo sapiens (human)
photoreceptor outer segmentcGMP-gated cation channel alpha-1Bos taurus (cattle)
rod photoreceptor outer segmentcGMP-gated cation channel alpha-1Bos taurus (cattle)
transmembrane transporter complexcGMP-gated cation channel alpha-1Bos taurus (cattle)
plasma membraneSodium channel protein type 7 subunit alphaHomo sapiens (human)
glial cell projectionSodium channel protein type 7 subunit alphaHomo sapiens (human)
voltage-gated sodium channel complexSodium channel protein type 7 subunit alphaHomo sapiens (human)
caveolaSodium channel protein type 5 subunit alphaHomo sapiens (human)
nucleoplasmSodium channel protein type 5 subunit alphaHomo sapiens (human)
nucleolusSodium channel protein type 5 subunit alphaHomo sapiens (human)
endoplasmic reticulumSodium channel protein type 5 subunit alphaHomo sapiens (human)
plasma membraneSodium channel protein type 5 subunit alphaHomo sapiens (human)
caveolaSodium channel protein type 5 subunit alphaHomo sapiens (human)
cell surfaceSodium channel protein type 5 subunit alphaHomo sapiens (human)
intercalated discSodium channel protein type 5 subunit alphaHomo sapiens (human)
membraneSodium channel protein type 5 subunit alphaHomo sapiens (human)
lateral plasma membraneSodium channel protein type 5 subunit alphaHomo sapiens (human)
Z discSodium channel protein type 5 subunit alphaHomo sapiens (human)
T-tubuleSodium channel protein type 5 subunit alphaHomo sapiens (human)
sarcolemmaSodium channel protein type 5 subunit alphaHomo sapiens (human)
perinuclear region of cytoplasmSodium channel protein type 5 subunit alphaHomo sapiens (human)
voltage-gated sodium channel complexSodium channel protein type 5 subunit alphaHomo sapiens (human)
plasma membraneSodium channel protein type 9 subunit alphaHomo sapiens (human)
axonSodium channel protein type 9 subunit alphaHomo sapiens (human)
voltage-gated sodium channel complexSodium channel protein type 9 subunit alphaHomo sapiens (human)
plasma membraneSodium channel protein type 2 subunit alphaHomo sapiens (human)
plasma membraneSodium channel protein type 2 subunit alphaHomo sapiens (human)
intercalated discSodium channel protein type 2 subunit alphaHomo sapiens (human)
T-tubuleSodium channel protein type 2 subunit alphaHomo sapiens (human)
axonSodium channel protein type 2 subunit alphaHomo sapiens (human)
node of RanvierSodium channel protein type 2 subunit alphaHomo sapiens (human)
paranode region of axonSodium channel protein type 2 subunit alphaHomo sapiens (human)
presynaptic membraneSodium channel protein type 2 subunit alphaHomo sapiens (human)
glutamatergic synapseSodium channel protein type 2 subunit alphaHomo sapiens (human)
voltage-gated sodium channel complexSodium channel protein type 2 subunit alphaHomo sapiens (human)
membraneSodium channel protein type 2 subunit alphaHomo sapiens (human)
nuclear envelopeSigma non-opioid intracellular receptor 1Homo sapiens (human)
nuclear inner membraneSigma non-opioid intracellular receptor 1Homo sapiens (human)
nuclear outer membraneSigma non-opioid intracellular receptor 1Homo sapiens (human)
endoplasmic reticulumSigma non-opioid intracellular receptor 1Homo sapiens (human)
endoplasmic reticulum membraneSigma non-opioid intracellular receptor 1Homo sapiens (human)
lipid dropletSigma non-opioid intracellular receptor 1Homo sapiens (human)
cytosolSigma non-opioid intracellular receptor 1Homo sapiens (human)
postsynaptic densitySigma non-opioid intracellular receptor 1Homo sapiens (human)
membraneSigma non-opioid intracellular receptor 1Homo sapiens (human)
growth coneSigma non-opioid intracellular receptor 1Homo sapiens (human)
cytoplasmic vesicleSigma non-opioid intracellular receptor 1Homo sapiens (human)
anchoring junctionSigma non-opioid intracellular receptor 1Homo sapiens (human)
postsynaptic density membraneSigma non-opioid intracellular receptor 1Homo sapiens (human)
endoplasmic reticulumSigma non-opioid intracellular receptor 1Homo sapiens (human)
sarcoplasmSodium channel protein type 3 subunit alphaHomo sapiens (human)
voltage-gated sodium channel complexSodium channel protein type 3 subunit alphaHomo sapiens (human)
plasma membraneSodium channel protein type 8 subunit alphaHomo sapiens (human)
membraneSodium channel protein type 8 subunit alphaHomo sapiens (human)
Z discSodium channel protein type 8 subunit alphaHomo sapiens (human)
cell junctionSodium channel protein type 8 subunit alphaHomo sapiens (human)
axonSodium channel protein type 8 subunit alphaHomo sapiens (human)
cytoplasmic vesicleSodium channel protein type 8 subunit alphaHomo sapiens (human)
node of RanvierSodium channel protein type 8 subunit alphaHomo sapiens (human)
axon initial segmentSodium channel protein type 8 subunit alphaHomo sapiens (human)
presynaptic active zone membraneSodium channel protein type 8 subunit alphaHomo sapiens (human)
parallel fiber to Purkinje cell synapseSodium channel protein type 8 subunit alphaHomo sapiens (human)
postsynaptic density membraneSodium channel protein type 8 subunit alphaHomo sapiens (human)
glutamatergic synapseSodium channel protein type 8 subunit alphaHomo sapiens (human)
voltage-gated sodium channel complexSodium channel protein type 8 subunit alphaHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (98)

Assay IDTitleYearJournalArticle
AID1449628Inhibition of human BSEP expressed in baculovirus transfected fall armyworm Sf21 cell membranes vesicles assessed as reduction in ATP-dependent [3H]-taurocholate transport into vesicles incubated for 5 mins by Topcount based rapid filtration method2012Drug metabolism and disposition: the biological fate of chemicals, Dec, Volume: 40, Issue:12
Mitigating the inhibition of human bile salt export pump by drugs: opportunities provided by physicochemical property modulation, in silico modeling, and structural modification.
AID680274TP_TRANSPORTER: increase in Calcein-AM intracellular accumulation (Calcein-AM: 0.5 uM, Tetracaine: 320 uM) in MDR1-expressing NIH-3T3 cells2004Biochemical and biophysical research communications, Mar-19, Volume: 315, Issue:4
Distinct groups of multidrug resistance modulating agents are distinguished by competition of P-glycoprotein-specific antibodies.
AID1366216Inhibition of human Nav1.7 expressed in CHO-K1 cells at -120 mV holding potential incubated over 5 mins measured at 15 secs interval by Qpatch clamp assay2017Bioorganic & medicinal chemistry letters, 11-15, Volume: 27, Issue:22
Discovery of aminocyclohexene analogues as selective and orally bioavailable hNav1.7 inhibitors for analgesia.
AID204252Duration of spinal anesthesia at the digits of the hind limbs was measured in sheep at dose 10(mg/kg)1981Journal of medicinal chemistry, Jan, Volume: 24, Issue:1
New antiarrhythmic agents. 5. alpha-Aminoaceto-2,6-xylidides with functionalized amide alkyl substituents.
AID700026Inhibition of human NaV1.5 alpha subunit expressed in CHOK1 cells at -90 mV holding potential by patch clamp electrophysiological assay2012Journal of medicinal chemistry, Aug-09, Volume: 55, Issue:15
3-Oxoisoindoline-1-carboxamides: potent, state-dependent blockers of voltage-gated sodium channel Na(V)1.7 with efficacy in rat pain models.
AID1891570Inhibition of human Nav 1.5 expressed in HEK293 cells at -90 mV holding potential by Whole cell voltage clamp electrophysiology assay2022Bioorganic & medicinal chemistry, 06-01, Volume: 63Discovery of (R)-(3-fluoropyrrolidin-1-yl)(6-((5-(trifluoromethyl)pyridin-2-yl)oxy)quinolin-2-yl)methanone (ABBV-318) and analogs as small molecule Na
AID1366271Inhibition of human Nav1.5 expressed in HEK293 cells at -120 mV holding potential incubated over 5 mins measured at 15 secs interval by Qpatch clamp assay2017Bioorganic & medicinal chemistry letters, 11-15, Volume: 27, Issue:22
Discovery of aminocyclohexene analogues as selective and orally bioavailable hNav1.7 inhibitors for analgesia.
AID700027Inhibition of recombinant human NaV1.7 alpha subunit expressed in HEK293 cells at -90 mV holding potential by patch clamp electrophysiological assay2012Journal of medicinal chemistry, Aug-09, Volume: 55, Issue:15
3-Oxoisoindoline-1-carboxamides: potent, state-dependent blockers of voltage-gated sodium channel Na(V)1.7 with efficacy in rat pain models.
AID781330pKa (acid-base dissociation constant) as determined by potentiometric titration2014Pharmaceutical research, Apr, Volume: 31, Issue:4
Comparison of the accuracy of experimental and predicted pKa values of basic and acidic compounds.
AID204246Duration of spinal anesthesia at the anal region was measured in sheep at dose 10(mg/kg)1981Journal of medicinal chemistry, Jan, Volume: 24, Issue:1
New antiarrhythmic agents. 5. alpha-Aminoaceto-2,6-xylidides with functionalized amide alkyl substituents.
AID23271Partition coefficient (logD7.4)1990Journal of medicinal chemistry, Jul, Volume: 33, Issue:7
Structure-activity relationships of antineoplastic agents in multidrug resistance.
AID19006Calculated membrane partition coefficient (Kmemb)2004Journal of medicinal chemistry, Mar-25, Volume: 47, Issue:7
Surface activity profiling of drugs applied to the prediction of blood-brain barrier permeability.
AID205268Inhibition of binding of Batrachotoxinin [3H]BTX-B to high affinity sites on voltage dependent sodium channels in a vesicular preparation from guinea pig cerebral cortex at 10 uM1985Journal of medicinal chemistry, Mar, Volume: 28, Issue:3
[3H]Batrachotoxinin A 20 alpha-benzoate binding to voltage-sensitive sodium channels: a rapid and quantitative assay for local anesthetic activity in a variety of drugs.
AID701019Binding affinity to Xenopus laevis oocyte CNGA1/CNGB1 assessed as inhibition of 2 mM cGMP-induced currents at +50 mV potential at 5 uM by patch-clamp method2011Journal of medicinal chemistry, Jul-14, Volume: 54, Issue:13
Cyclic nucleotide-gated channel block by hydrolysis-resistant tetracaine derivatives.
AID204257Duration of spinal anesthesia at the weight support was measured in sheep at dose 10(mg/kg)1981Journal of medicinal chemistry, Jan, Volume: 24, Issue:1
New antiarrhythmic agents. 5. alpha-Aminoaceto-2,6-xylidides with functionalized amide alkyl substituents.
AID611515Displacement of [3H]BTX from human Nav1.7 expressed in human HEK293 cells after 1 hr by MicroBeta analyzer2011Journal of medicinal chemistry, Jul-14, Volume: 54, Issue:13
Identification of a potent, state-dependent inhibitor of Nav1.7 with oral efficacy in the formalin model of persistent pain.
AID588213Literature-mined compound from Fourches et al multi-species drug-induced liver injury (DILI) dataset, effect in non-rodents2010Chemical research in toxicology, Jan, Volume: 23, Issue:1
Cheminformatics analysis of assertions mined from literature that describe drug-induced liver injury in different species.
AID392049Cardiotoxicity in Dunkin-Hartley guinea pig assessed as maximal QTc prolongation time at 10 mg/kg, iv administered as 3 fold cumulative doses measured every 10 seconds at end of every 20 mins follow up period of individual dose by ECG2008European journal of medicinal chemistry, Nov, Volume: 43, Issue:11
Identification of "toxicophoric" features for predicting drug-induced QT interval prolongation.
AID701012Binding affinity to Xenopus oocyte CNGA1/CNGB1 assessed as not corrected for ion accumulation at +40 mV potential by electrophysiological assay2011Journal of medicinal chemistry, Jul-14, Volume: 54, Issue:13
Cyclic nucleotide-gated channel block by hydrolysis-resistant tetracaine derivatives.
AID1296884Inhibition of recombinant human Nav1.7 expressed in HEK293F cells preincubated for 40 mins followed by DiSBAC2 substrate addition measured after 90 mins by FRET assay2016Journal of medicinal chemistry, Apr-14, Volume: 59, Issue:7
Substituted Indazoles as Nav1.7 Blockers for the Treatment of Pain.
AID1061889Displacement of [3H]BTX-B from neuronal voltage-gated sodium channel in rat cerebral cortex synaptoneurosomes after 60 mins by scintillation counting2014Bioorganic & medicinal chemistry, Jan-01, Volume: 22, Issue:1
A highly predictive 3D-QSAR model for binding to the voltage-gated sodium channel: design of potent new ligands.
AID588211Literature-mined compound from Fourches et al multi-species drug-induced liver injury (DILI) dataset, effect in humans2010Chemical research in toxicology, Jan, Volume: 23, Issue:1
Cheminformatics analysis of assertions mined from literature that describe drug-induced liver injury in different species.
AID1296886Inhibition of human Nav1.7 expressed in HEK293F cells measured at -100 mV holding potential by voltage-patch clamp method2016Journal of medicinal chemistry, Apr-14, Volume: 59, Issue:7
Substituted Indazoles as Nav1.7 Blockers for the Treatment of Pain.
AID701015Inhibition of Xenopus laevis oocyte CNGA1/CNGB1 assessed as inhibition of cGMP-induced currents at +50 mV potential at 1 uM by patch-clamp method in presence of 100 uM cGMP2011Journal of medicinal chemistry, Jul-14, Volume: 54, Issue:13
Cyclic nucleotide-gated channel block by hydrolysis-resistant tetracaine derivatives.
AID599097Inhibition of human NaV1.7 expressed in HEK293 cells by [14C]guanidinium influx assay2011Bioorganic & medicinal chemistry letters, Jun-15, Volume: 21, Issue:12
Discovery of XEN907, a spirooxindole blocker of NaV1.7 for the treatment of pain.
AID781326pKa (acid-base dissociation constant) as determined by Avdeef ref: DOI: 10.1002/047145026X2014Pharmaceutical research, Apr, Volume: 31, Issue:4
Comparison of the accuracy of experimental and predicted pKa values of basic and acidic compounds.
AID450269Displacement of [3H]-BTX-B from neuronal voltage-gated sodium channel in rat cerebral cortex synaptoneurosomes2009Bioorganic & medicinal chemistry, Oct-01, Volume: 17, Issue:19
Ligand-based design and synthesis of novel sodium channel blockers from a combined phenytoin-lidocaine pharmacophore.
AID700028Inhibition of recombinant human NaV1.7 alpha subunit expressed in HEK293 cells at -65 mV holding potential by patch clamp electrophysiological assay2012Journal of medicinal chemistry, Aug-09, Volume: 55, Issue:15
3-Oxoisoindoline-1-carboxamides: potent, state-dependent blockers of voltage-gated sodium channel Na(V)1.7 with efficacy in rat pain models.
AID588212Literature-mined compound from Fourches et al multi-species drug-induced liver injury (DILI) dataset, effect in rodents2010Chemical research in toxicology, Jan, Volume: 23, Issue:1
Cheminformatics analysis of assertions mined from literature that describe drug-induced liver injury in different species.
AID254236Apparent dissociation constant against Cyclic nucleotide gated channel alpha 1 at +40 mV2005Journal of medicinal chemistry, Sep-08, Volume: 48, Issue:18
Modifications to the tetracaine scaffold produce cyclic nucleotide-gated channel blockers with widely varying efficacies.
AID395328Lipophilicity, log P of the compound2009Journal of medicinal chemistry, Mar-26, Volume: 52, Issue:6
Relationship between brain tissue partitioning and microemulsion retention factors of CNS drugs.
AID701016Inhibition of Xenopus laevis oocyte CNGA1/CNGB1 assessed as inhibition of currents at +50 mV potential at 2 uM by patch-clamp method in presence of 100 uM cGMP2011Journal of medicinal chemistry, Jul-14, Volume: 54, Issue:13
Cyclic nucleotide-gated channel block by hydrolysis-resistant tetracaine derivatives.
AID1296896Inhibition of recombinant human Nav1.2 expressed in HEK293 cells preincubated for 40 mins followed by DiSBAC2 substrate addition measured after 90 mins by FRET assay2016Journal of medicinal chemistry, Apr-14, Volume: 59, Issue:7
Substituted Indazoles as Nav1.7 Blockers for the Treatment of Pain.
AID71803Tonic inhibition of compound action potential by 50% was determined in the absence of avidin in desheathed frog sciatic nerves1987Journal of medicinal chemistry, Aug, Volume: 30, Issue:8
Limited nerve impulse blockade by "leashed" local anesthetics.
AID204569Onset of spinal anesthesia at the anal region was measured in sheep at dose 10(mg/kg)1981Journal of medicinal chemistry, Jan, Volume: 24, Issue:1
New antiarrhythmic agents. 5. alpha-Aminoaceto-2,6-xylidides with functionalized amide alkyl substituents.
AID1296898Inhibition of recombinant human Nav1.6 expressed in HEK293 cells preincubated for 40 mins followed by DiSBAC2 substrate addition measured after 90 mins by FRET assay2016Journal of medicinal chemistry, Apr-14, Volume: 59, Issue:7
Substituted Indazoles as Nav1.7 Blockers for the Treatment of Pain.
AID395325Lipophilicity, log P by microemulsion electrokinetic chromatography2009Journal of medicinal chemistry, Mar-26, Volume: 52, Issue:6
Relationship between brain tissue partitioning and microemulsion retention factors of CNS drugs.
AID1891560Inhibition of recombinant human Nav 1.7 expressed in HEK293F cells incubated for 3 mins by FRET based membrane potential assay2022Bioorganic & medicinal chemistry, 06-01, Volume: 63Discovery of (R)-(3-fluoropyrrolidin-1-yl)(6-((5-(trifluoromethyl)pyridin-2-yl)oxy)quinolin-2-yl)methanone (ABBV-318) and analogs as small molecule Na
AID701020Binding affinity to Xenopus laevis oocyte CNGA1/CNGB1 assessed as inhibition of 2 mM cGMP-induced currents at -50 mV potential at 5 uM by patch-clamp method2011Journal of medicinal chemistry, Jul-14, Volume: 54, Issue:13
Cyclic nucleotide-gated channel block by hydrolysis-resistant tetracaine derivatives.
AID1525553Inhibition of human TASK1 expressed in Xenopus oocytes by whole cell voltage clamp assay2019Journal of medicinal chemistry, 11-27, Volume: 62, Issue:22
TASK Channels Pharmacology: New Challenges in Drug Design.
AID1296888Inhibition of human Nav1.5 expressed in HEK293 cells by whole cell-patch clamp method2016Journal of medicinal chemistry, Apr-14, Volume: 59, Issue:7
Substituted Indazoles as Nav1.7 Blockers for the Treatment of Pain.
AID311932Inhibition of ASM in human H4 cells assessed as residual activity at 10 uM2008Journal of medicinal chemistry, Jan-24, Volume: 51, Issue:2
Identification of new functional inhibitors of acid sphingomyelinase using a structure-property-activity relation model.
AID313728Blockade of CNGA1/CNGB1 expressed in Xenopus oocyte by electrophysiological method2008Bioorganic & medicinal chemistry letters, Jan-15, Volume: 18, Issue:2
Block of cyclic nucleotide-gated channels by tetracaine derivatives: role of apolar interactions at two distinct locations.
AID630203Inhibition of retinal rod CNGA1/CNGB1 expressed in Xenopus laevis oocytes assessed as blockade of cGMP-induced current at -50 mV holding potential by patch-clamp electrophysiology2011Bioorganic & medicinal chemistry letters, Nov-01, Volume: 21, Issue:21
Halogen substituents on the aromatic moiety of the tetracaine scaffold improve potency of cyclic nucleotide-gated channel block.
AID781329pKa (acid-base dissociation constant) as determined by other workers2014Pharmaceutical research, Apr, Volume: 31, Issue:4
Comparison of the accuracy of experimental and predicted pKa values of basic and acidic compounds.
AID450273Lipophilicity, log P of the compound2009Bioorganic & medicinal chemistry, Oct-01, Volume: 17, Issue:19
Ligand-based design and synthesis of novel sodium channel blockers from a combined phenytoin-lidocaine pharmacophore.
AID204578Onset of spinal anesthesia at the digits of the hind limbs was measured in sheep at dose 10 (mg/kg)1981Journal of medicinal chemistry, Jan, Volume: 24, Issue:1
New antiarrhythmic agents. 5. alpha-Aminoaceto-2,6-xylidides with functionalized amide alkyl substituents.
AID19424Partition coefficient (logD7.4)2001Journal of medicinal chemistry, Jul-19, Volume: 44, Issue:15
ElogD(oct): a tool for lipophilicity determination in drug discovery. 2. Basic and neutral compounds.
AID701013Binding affinity to Xenopus oocyte CNGA1/CNGB1 assessed as corrected for ion accumulation at +40 mV potential by electrophysiological assay2011Journal of medicinal chemistry, Jul-14, Volume: 54, Issue:13
Cyclic nucleotide-gated channel block by hydrolysis-resistant tetracaine derivatives.
AID409951Inhibition of human liver MAOB2008Journal of medicinal chemistry, Nov-13, Volume: 51, Issue:21
Quantitative structure-activity relationship and complex network approach to monoamine oxidase A and B inhibitors.
AID1296885Inhibition of human Nav1.7 expressed in HEK293F cells measured at -65 mV holding potential by voltage-patch clamp method2016Journal of medicinal chemistry, Apr-14, Volume: 59, Issue:7
Substituted Indazoles as Nav1.7 Blockers for the Treatment of Pain.
AID1918126Stability in human plasma assessed as degradation at measured after 4 hrs by HPLC-MS analysis2022Journal of medicinal chemistry, 11-10, Volume: 65, Issue:21
Identification and Biochemical Characterization of Pyrrolidinediones as Novel Inhibitors of the Bacterial Enzyme MurA.
AID701018Inhibition of Xenopus laevis oocyte CNGA1/CNGB1 assessed as inhibition of currents at +50 mV potential at 2 uM by patch-clamp method in presence of 50 uM cGMP2011Journal of medicinal chemistry, Jul-14, Volume: 54, Issue:13
Cyclic nucleotide-gated channel block by hydrolysis-resistant tetracaine derivatives.
AID1296897Inhibition of recombinant human Nav1.3 expressed in HEK293 cells preincubated for 40 mins followed by DiSBAC2 substrate addition measured after 90 mins by FRET assay2016Journal of medicinal chemistry, Apr-14, Volume: 59, Issue:7
Substituted Indazoles as Nav1.7 Blockers for the Treatment of Pain.
AID700021Inhibition of human NaV1.7 F1737A mutant expressed in HEK293 cells at -65 mV holding potential by patch clamp electrophysiological assay2012Journal of medicinal chemistry, Aug-09, Volume: 55, Issue:15
3-Oxoisoindoline-1-carboxamides: potent, state-dependent blockers of voltage-gated sodium channel Na(V)1.7 with efficacy in rat pain models.
AID1918127Stability in human plasma assessed as half life at by HPLC-MS analysis2022Journal of medicinal chemistry, 11-10, Volume: 65, Issue:21
Identification and Biochemical Characterization of Pyrrolidinediones as Novel Inhibitors of the Bacterial Enzyme MurA.
AID312896Partition coefficient, log P by UPLC method2008Journal of medicinal chemistry, Feb-14, Volume: 51, Issue:3
High-throughput log P determination by ultraperformance liquid chromatography: a convenient tool for medicinal chemists.
AID45741Collateral sensitivity of CHRC5 cells to local anesthetics/steroids as log of ratio of molar concentration of drug inducing 50% growth inhibition in CHO AUXB1 cells to that of CHRC5 cells1990Journal of medicinal chemistry, Jul, Volume: 33, Issue:7
Structure-activity relationships of antineoplastic agents in multidrug resistance.
AID237685Lipophilicity determined as logarithm of the partition coefficient in the alkane/water system2005Journal of medicinal chemistry, May-05, Volume: 48, Issue:9
Calculating virtual log P in the alkane/water system (log P(N)(alk)) and its derived parameters deltalog P(N)(oct-alk) and log D(pH)(alk).
AID630202Inhibition of retinal rod CNGA1/CNGB1 expressed in Xenopus laevis oocytes assessed as blockade of cGMP-induced current at +50 mV holding potential by patch-clamp electrophysiology2011Bioorganic & medicinal chemistry letters, Nov-01, Volume: 21, Issue:21
Halogen substituents on the aromatic moiety of the tetracaine scaffold improve potency of cyclic nucleotide-gated channel block.
AID699984Selectivity ratio of IC50 for human NaV1.7 F1737A mutant at -65 mV holding potential to IC50 for recombinant human NaV1.7 alpha subunit at -65 mV holding potential2012Journal of medicinal chemistry, Aug-09, Volume: 55, Issue:15
3-Oxoisoindoline-1-carboxamides: potent, state-dependent blockers of voltage-gated sodium channel Na(V)1.7 with efficacy in rat pain models.
AID700020Inhibition of human NaV1.2 alpha subunit expressed in CHOK1 cells at -65 mV holding potential by patch clamp electrophysiological assay2012Journal of medicinal chemistry, Aug-09, Volume: 55, Issue:15
3-Oxoisoindoline-1-carboxamides: potent, state-dependent blockers of voltage-gated sodium channel Na(V)1.7 with efficacy in rat pain models.
AID392048Cardiotoxicity in iv dosed Dunkin-Hartley guinea pig assessed as drug level required to evoke 50 ms QTc prolongation administered as 3 fold cumulative doses measured every 10 seconds at end of every 20 mins follow up period of individual dose by ECG2008European journal of medicinal chemistry, Nov, Volume: 43, Issue:11
Identification of "toxicophoric" features for predicting drug-induced QT interval prolongation.
AID311934Dissociation constant, pKa of the compound2008Journal of medicinal chemistry, Jan-24, Volume: 51, Issue:2
Identification of new functional inhibitors of acid sphingomyelinase using a structure-property-activity relation model.
AID409949Inhibition of human liver MAOA2008Journal of medicinal chemistry, Nov-13, Volume: 51, Issue:21
Quantitative structure-activity relationship and complex network approach to monoamine oxidase A and B inhibitors.
AID312895Partition coefficient, log P of the compound2008Journal of medicinal chemistry, Feb-14, Volume: 51, Issue:3
High-throughput log P determination by ultraperformance liquid chromatography: a convenient tool for medicinal chemists.
AID700008Selectivity ratio of IC50 for human NaV1.5 alpha subunit at -90 mV holding potential to IC50 for recombinant human NaV1.7 alpha subunit at -65 mV holding potential2012Journal of medicinal chemistry, Aug-09, Volume: 55, Issue:15
3-Oxoisoindoline-1-carboxamides: potent, state-dependent blockers of voltage-gated sodium channel Na(V)1.7 with efficacy in rat pain models.
AID701014Drug degradation in 0.1 M phosphate buffer at pH 7.4 assessed as human butyrylcholinestase-mediated compound hydrolysis rate at 50 uM after 24 hrs by HPLC analysis2011Journal of medicinal chemistry, Jul-14, Volume: 54, Issue:13
Cyclic nucleotide-gated channel block by hydrolysis-resistant tetracaine derivatives.
AID701017Inhibition of Xenopus laevis oocyte CNGA1/CNGB1 assessed as inhibition of cGMP-induced currents at +50 mV potential at 1 uM by patch-clamp method in presence of 50 uM cGMP2011Journal of medicinal chemistry, Jul-14, Volume: 54, Issue:13
Cyclic nucleotide-gated channel block by hydrolysis-resistant tetracaine derivatives.
AID91481Binding constant against human serum albumin (HSA)2001Journal of medicinal chemistry, Dec-06, Volume: 44, Issue:25
Cheminformatic models to predict binding affinities to human serum albumin.
AID611516Displacement of [3H]N-(3-(4-(4-(Benzyloxy)piperidin-1-yl)-1,3,5-triazin-2-ylamino)-phenyl)acetamide from human Nav1.7 expressed in human HEK293 cells after 1 hr by MicroBeta analyzer2011Journal of medicinal chemistry, Jul-14, Volume: 54, Issue:13
Identification of a potent, state-dependent inhibitor of Nav1.7 with oral efficacy in the formalin model of persistent pain.
AID515780Intrinsic solubility of the compound in water2010Bioorganic & medicinal chemistry, Oct-01, Volume: 18, Issue:19
QSAR-based solubility model for drug-like compounds.
AID205267Inhibition of binding of Batrachotoxinin [3H]BTX-B to high affinity sites on voltage dependent sodium channels in a vesicular preparation from guinea pig cerebral cortex1985Journal of medicinal chemistry, Mar, Volume: 28, Issue:3
[3H]Batrachotoxinin A 20 alpha-benzoate binding to voltage-sensitive sodium channels: a rapid and quantitative assay for local anesthetic activity in a variety of drugs.
AID311935Partition coefficient, log P of the compound2008Journal of medicinal chemistry, Jan-24, Volume: 51, Issue:2
Identification of new functional inhibitors of acid sphingomyelinase using a structure-property-activity relation model.
AID254235Apparent dissociation constant against Cyclic nucleotide gated channel alpha 1 at 0 mV2005Journal of medicinal chemistry, Sep-08, Volume: 48, Issue:18
Modifications to the tetracaine scaffold produce cyclic nucleotide-gated channel blockers with widely varying efficacies.
AID1508630Primary qHTS for small molecule stabilizers of the endoplasmic reticulum resident proteome: Secreted ER Calcium Modulated Protein (SERCaMP) assay2021Cell reports, 04-27, Volume: 35, Issue:4
A target-agnostic screen identifies approved drugs to stabilize the endoplasmic reticulum-resident proteome.
AID504812Inverse Agonists of the Thyroid Stimulating Hormone Receptor: HTS campaign2010Endocrinology, Jul, Volume: 151, Issue:7
A small molecule inverse agonist for the human thyroid-stimulating hormone receptor.
AID1508627Counterscreen qHTS for small molecule stabilizers of the endoplasmic reticulum resident proteome: GLuc-NoTag assay2021Cell reports, 04-27, Volume: 35, Issue:4
A target-agnostic screen identifies approved drugs to stabilize the endoplasmic reticulum-resident proteome.
AID1508628Confirmatory qHTS for small molecule stabilizers of the endoplasmic reticulum resident proteome: Secreted ER Calcium Modulated Protein (SERCaMP) assay2021Cell reports, 04-27, Volume: 35, Issue:4
A target-agnostic screen identifies approved drugs to stabilize the endoplasmic reticulum-resident proteome.
AID1347049Natriuretic polypeptide receptor (hNpr1) antagonism - Pilot screen2019Science translational medicine, 07-10, Volume: 11, Issue:500
Inhibition of natriuretic peptide receptor 1 reduces itch in mice.
AID1347058CD47-SIRPalpha protein protein interaction - HTRF assay qHTS validation2019PloS one, , Volume: 14, Issue:7
Quantitative high-throughput screening assays for the discovery and development of SIRPα-CD47 interaction inhibitors.
AID1347151Optimization of GU AMC qHTS for Zika virus inhibitors: Unlinked NS2B-NS3 protease assay2020Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49
Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors.
AID1347059CD47-SIRPalpha protein protein interaction - Alpha assay qHTS validation2019PloS one, , Volume: 14, Issue:7
Quantitative high-throughput screening assays for the discovery and development of SIRPα-CD47 interaction inhibitors.
AID1347405qHTS to identify inhibitors of the type 1 interferon - major histocompatibility complex class I in skeletal muscle: primary screen against the NCATS LOPAC collection2020ACS chemical biology, 07-17, Volume: 15, Issue:7
High-Throughput Screening to Identify Inhibitors of the Type I Interferon-Major Histocompatibility Complex Class I Pathway in Skeletal Muscle.
AID588378qHTS for Inhibitors of ATXN expression: Validation
AID1508629Cell Viability qHTS for small molecule stabilizers of the endoplasmic reticulum resident proteome2021Cell reports, 04-27, Volume: 35, Issue:4
A target-agnostic screen identifies approved drugs to stabilize the endoplasmic reticulum-resident proteome.
AID1347050Natriuretic polypeptide receptor (hNpr2) antagonism - Pilot subtype selectivity assay2019Science translational medicine, 07-10, Volume: 11, Issue:500
Inhibition of natriuretic peptide receptor 1 reduces itch in mice.
AID1347086qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lymphocytic Choriomeningitis Arenaviruses (LCMV): LCMV Primary Screen - GLuc reporter signal2020Antiviral research, 01, Volume: 173A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity.
AID1347410qHTS for inhibitors of adenylyl cyclases using a fission yeast platform: a pilot screen against the NCATS LOPAC library2019Cellular signalling, 08, Volume: 60A fission yeast platform for heterologous expression of mammalian adenylyl cyclases and high throughput screening.
AID1347057CD47-SIRPalpha protein protein interaction - LANCE assay qHTS validation2019PloS one, , Volume: 14, Issue:7
Quantitative high-throughput screening assays for the discovery and development of SIRPα-CD47 interaction inhibitors.
AID1347082qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lassa (LASV) Arenavirus: LASV Primary Screen - GLuc reporter signal2020Antiviral research, 01, Volume: 173A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity.
AID1347083qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lassa (LASV) Arenavirus: Viability assay - alamar blue signal for LASV Primary Screen2020Antiviral research, 01, Volume: 173A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity.
AID1347045Natriuretic polypeptide receptor (hNpr1) antagonism - Pilot counterscreen GloSensor control cell line2019Science translational medicine, 07-10, Volume: 11, Issue:500
Inhibition of natriuretic peptide receptor 1 reduces itch in mice.
AID504836Inducers of the Endoplasmic Reticulum Stress Response (ERSR) in human glioma: Validation2002The Journal of biological chemistry, Apr-19, Volume: 277, Issue:16
Sustained ER Ca2+ depletion suppresses protein synthesis and induces activation-enhanced cell death in mast cells.
AID504810Antagonists of the Thyroid Stimulating Hormone Receptor: HTS campaign2010Endocrinology, Jul, Volume: 151, Issue:7
A small molecule inverse agonist for the human thyroid-stimulating hormone receptor.
AID588349qHTS for Inhibitors of ATXN expression: Validation of Cytotoxic Assay
AID504749qHTS profiling for inhibitors of Plasmodium falciparum proliferation2011Science (New York, N.Y.), Aug-05, Volume: 333, Issue:6043
Chemical genomic profiling for antimalarial therapies, response signatures, and molecular targets.
AID1159607Screen for inhibitors of RMI FANCM (MM2) intereaction2016Journal of biomolecular screening, Jul, Volume: 21, Issue:6
A High-Throughput Screening Strategy to Identify Protein-Protein Interaction Inhibitors That Block the Fanconi Anemia DNA Repair Pathway.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (2,431)

TimeframeStudies, This Drug (%)All Drugs %
pre-19901288 (52.98)18.7374
1990's463 (19.05)18.2507
2000's379 (15.59)29.6817
2010's247 (10.16)24.3611
2020's54 (2.22)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 64.35

According to the monthly volume, diversity, and competition of internet searches for this compound, as well the volume and growth of publications, there is estimated to be very strong demand-to-supply ratio for research on this compound.

MetricThis Compound (vs All)
Research Demand Index64.35 (24.57)
Research Supply Index8.02 (2.92)
Research Growth Index4.30 (4.65)
Search Engine Demand Index123.39 (26.88)
Search Engine Supply Index2.14 (0.95)

This Compound (64.35)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials349 (12.98%)5.53%
Reviews76 (2.83%)6.00%
Case Studies149 (5.54%)4.05%
Observational1 (0.04%)0.25%
Other2,113 (78.61%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Clinical Trials (94)

Trial Overview

TrialPhaseEnrollmentStudy TypeStart DateStatus
Role of Pupil Centroid Shift Compensation on Lower and Higher Order Aberrations During Photorefractive Keratectomy: An Eye-to-Eye Study [NCT03844178]Phase 2104 participants (Anticipated)Interventional2019-02-10Recruiting
Cardiovascular Changes and Tetracaine Pharmacokinetics Following Intranasal Administration of Standard and High Doses of Kovacaine Mist (Tetracaine Hydrochloride With Oxymetazoline Hydrochloride) in Healthy Volunteers [NCT01304316]Phase 212 participants (Actual)Interventional2010-09-30Completed
Pretreatment of Lacerations With Topical LET (Lidocaine-Epinephrine-Tetracaine) Reduces Pain During Tissue Adhesive Repair in Children: Double-blind, Randomized, Controlled Trial of Efficacy [NCT01202487]Phase 2222 participants (Actual)Interventional2011-04-30Completed
A Single Blinded Observational Study of the Effectiveness of a Pain Ease Local Anesthetic Spray, Combined With Ametop Gel, to Reduce the Discomfort of Intravenous Insertion [NCT03749915]240 participants (Anticipated)Interventional2018-11-20Not yet recruiting
Pilot Study: Measurement of Plasma Levels of Lidocaine/Tetracaine and Adverse Effects Derived From a New Topical Formulation for Treatment of Neuropathic Pain [NCT06171243]20 participants (Anticipated)Observational2023-03-17Recruiting
Comparison Between 2% Lidocaine Gel and 5% Tetracaine Eye Drop as Topical Anesthesia in Phacoemulsification [NCT03143452]72 participants (Actual)Interventional2016-12-01Completed
Injectable Lidocaine Provides Similar Analgesia Compared to Transdermal Lidocaine/Tetracaine Patch for the Incision and Drainage of Skin Abscesses: A Randomized Controlled Trial [NCT02066818]Early Phase 120 participants (Actual)Interventional2008-01-31Completed
Evaluation of Deep Topical Fornix Nerve Block Versus Topical Anaesthesia in Patients Undergoing Implantable Contact Lens Procedure [NCT02196441]102 participants (Anticipated)Interventional2014-08-31Not yet recruiting
An Open-label Pilot Study Evaluating Synera® in the Treatment of Patients With Patellar Tendinopathy [NCT01111773]Phase 213 participants (Actual)Interventional2010-06-30Completed
Phase 1, Randomized, Double-Blind, Placebo-Controlled, 4-Period, Complete Cross-Over Comparison of the Anesthetic Efficacy of Bilateral and Unilateral Application of Kovacaine Mist in Healthy Volunteers [NCT02457806]Phase 148 participants (Actual)Interventional2011-08-31Completed
A Double Blind Randomized Controlled Trial Comparing the Efficacy of 7% Lidocaine / 7% Tetracaine Cream Versus 2,5% Lidocaine / 2,5% Prilocaine Cream for Local Anaesthesia During Laser Treatment of Acne Keloidalis Nuchae and Tattoo Removal [NCT02372786]Phase 430 participants (Actual)Interventional2014-11-30Completed
Pulpal Blood Flow With the Use of Intra-nasal Anesthetic: a Randomized Double-blind Crossover Study [NCT03368391]Phase 425 participants (Anticipated)Interventional2018-01-03Not yet recruiting
Painless Sharp Wound Debridement With Lidocaine-23%-Tetra-caine-7% Gel Versus EMLA 5% Cream: a Single-blind, Crossover, Randomised, Controlled Trial [NCT05890703]Phase 240 participants (Anticipated)Interventional2023-06-01Recruiting
An Open-Label Pilot Study Evaluating Synera® in the Treatment of Patients With Carpal Tunnel Syndrome [NCT00991068]Phase 224 participants (Actual)Interventional2009-09-30Completed
Lidocaine/Tetracaine Patch (Ralydan) vs Lidocaine/Prilocaine Cream (EMLA) for Needle Related Procedures in Children: a Multicenter, Randomized Controlled Trial [NCT02519660]Phase 3339 participants (Actual)Interventional2015-04-30Completed
Intravitreal Injection Anesthesia - Comparison of Different Topical Agents. [NCT01224847]92 participants (Actual)Interventional2009-10-31Completed
Topical Anesthesia of Tetracaine Hydrochloride Jelly on Cervix After Hysteroscopic Uterine Stent Insertion [NCT02863679]84 participants (Actual)Interventional2016-05-31Completed
An Open-label Pilot Study Evaluating Synera® in the Treatment of Patients With Pain Associated With Myofascial Trigger Points [NCT01106989]Phase 220 participants (Actual)Interventional2010-06-30Completed
Comparing Topical Tetracaine Drops to Topical Focal Phenol for Local Anesthesia During Intratympanic Steroid Injection [NCT04794842]Early Phase 180 participants (Actual)Interventional2021-08-01Active, not recruiting
A Randomized, Double-Blind, Two-Period, Crossover Study to Evaluate the Depth and Duration of Anesthesia of Synera™ Patches Compared to Placebo Patches Applied to Healthy Adult Volunteers [NCT00891163]Phase 425 participants (Actual)Interventional2006-12-31Completed
Kovanaze Vs. Articaine in Achieving Pulpal Anesthesia of Maxillary Teeth: A Randomized Clinical Trial [NCT04104789]Phase 20 participants (Actual)Interventional2020-09-30Withdrawn(stopped due to Manufacture of drug discontinued before any participants could be enrolled.)
Short Term Topical Tetracaine is Safe and Highly Efficacious for the Treatment of Pain Caused by Corneal Abrasions: a Double-blind Randomized Clinical Trial [NCT04187417]118 participants (Actual)Interventional2015-01-01Completed
Does Rapydan Influence Routine Clinical Chemistry and Hematology Measurements? [NCT00765934]25 participants (Anticipated)Interventional2009-11-30Completed
Kovanaze Vs. Articaine in Achieving Pulpal Anesthesia of Maxillary Teeth: A Randomized Clinical Trial [NCT04105985]Phase 20 participants (Actual)Interventional2020-08-31Withdrawn(stopped due to Manufacturer discontinued drug before any participants could be enrolled.)
A Pharmacokinetic Study of Synera™ (Lidocaine 70 mg and Tetracaine 70 mg Topical Patch) to Evaluate the Systemic Exposure to Lidocaine and Tetracaine in Neonates and Infants [NCT00747669]Phase 411 participants (Anticipated)Interventional2008-09-30Suspended(stopped due to Difficulty with enrollment)
An Open Label, Placebo and Positive Controlled, Randomised, Cross-over Study in Healthy Male Volunteers to Determine the Effect on Penile Skin Sensation of a Newly Formulated Tetracaine Product PET500 [NCT04247230]Phase 120 participants (Actual)Interventional2008-09-03Completed
The Efficacy of the Eutectic Mixture of Local Anesthetics (EMLA) Cream Versus the Synera Patch for Pain Reduction During Venipuncture in Children [NCT00530803]Phase 2100 participants (Actual)Interventional2007-06-30Completed
Tetracaine (Ametop®) Compared to Placebo for Reducing Pain Associated With Intramuscular Injection of Palivizumab (Synagis®) - A Pilot Study [NCT00484393]Phase 47 participants (Actual)Interventional2007-11-30Completed
A Phase III, Multi-Center, Randomized, Double-Blind, Parallel-Groups Clinical Trial Comparing the Efficacy and Safety of Intranasally Administered Kovacaine Mist to Tetracaine Alone and to Placebo for Anesthetizing Maxillary Teeth in Adults [NCT01710787]Phase 3110 participants (Actual)Interventional2012-10-31Completed
A Randomized, Double-blind, Placebo Controlled, Parallel Study Evaluating the Efficacy of S-Caine™ Peel (Lidocaine 7% and Tetracaine 7% Cream) for Induction of Local Dermal Anesthesia Before Vascular Access Procedures in Children [NCT00125255]Phase 381 participants (Actual)Interventional2005-06-30Completed
[NCT01914250]40 participants (Anticipated)Interventional2013-01-31Completed
Systemic Analgesia and Local Anaesthesia for Percutaneous Venous Catheter Placement in Preterm Neonates [NCT00213200]Phase 3108 participants Interventional2003-07-31Completed
Ametop - Friend or Foe A Prospective Observational Study of the Incidence of Adverse Reactions With Ametop [NCT02750137]192 participants (Actual)Observational2014-08-31Completed
Conventional Sedation Compaired With THRIVE Under General Anesthesia in Endotracheal Intubation by Fiberbronchoscope in Patients With Difficult Airways,A Randomized Controlled Study [NCT04924621]42 participants (Anticipated)Interventional2021-06-10Recruiting
Treatment of Corneal Abrasions With Topical Tetracaine: an Evaluation of Safety and Efficacy [NCT02771392]Phase 2/Phase 3120 participants (Anticipated)Interventional2016-06-30Not yet recruiting
A Randomised, Controlled, Single-blinded, Cross Over Comparison Study to Compare the Efficacy of the Rapydan Medicated Plaster Versus Tetracaine Gel [NCT00670696]Phase 40 participants (Actual)Interventional2008-04-30Withdrawn(stopped due to No longer sponsor of trial)
A Single-Center, Study Evaluating The Pharmacokinetics Of Tetracaine, Para-Butylaminobenzoic Acid, And Oxymetazoline After Intranasal Administration Of Kovacaine Mist To Healthy Pediatric Subjects [NCT01952990]Phase 218 participants (Actual)Interventional2013-09-30Completed
The Efficacy of Topical Amethocaine Gel in Reducing the Pain of Local Anesthetic Infiltration Prior to Neuraxial Anesthesia in Non-labouring Pregnant Women: A Randomized Controlled Trial [NCT01864213]Phase 178 participants (Actual)Interventional2013-05-31Completed
Kovanaze Vs. Articaine in Achieving Pulpal Anesthesia of Maxillary Teeth: A Randomized Clinical Trial [NCT03962634]Phase 23 participants (Actual)Interventional2019-08-28Terminated(stopped due to Drug is no longer being manufactured)
Lidocaine/Tetracaine Patch (Rapydan) for Topical Anaesthesia Before Arterial Access: A Double-blind, Randomized Trial [NCT01494311]Phase 490 participants (Actual)Interventional2011-03-31Completed
An Open-Label Pilot Study Evaluating Synera® in the Treatment of Patients With Shoulder Impingement Syndrome [NCT01055444]Phase 220 participants (Actual)Interventional2010-03-31Completed
Topical Anesthesia to Decrease the Trigeminal-Cardiac Reflex During Intra-arterial Injection of Chemotherapy for Retinoblastoma in Children. [NCT02955524]Early Phase 10 participants (Actual)Interventional2018-03-31Withdrawn(stopped due to I discontinued this study because I transferred to another institution.)
The Effects on Betadine 5% Penetration When Using Lidocaine 2% Jelly Versus Topical Tetracaine 0.5% for Topical Phacoemulsification Cataract Surgery. [NCT00827073]40 participants (Actual)Interventional2008-11-30Completed
Comparison of Spinal Tetracaine With Fentanyl and Epinephrine Versus Bupivacaine With Fentanyl and Epinephrine for Combined Spinal Epidural Labor Analgesia [NCT01005459]Phase 446 participants (Actual)Interventional2009-08-31Terminated(stopped due to feasibility /drug availability issues - No study drug sources available)
A Double-blind, Partial Cross-over, Incomplete Factorial Study to Assess the Local Anesthetic Efficacy and Safety of CTY-5339 Anesthetic Spray (CTY-5339-A) When Applied to the Cheek Mucosal Tissue in Normal Volunteers [NCT02908620]Phase 240 participants (Actual)Interventional2016-12-07Completed
An Open-Label Safety Study to Evaluate the Use of S-Caine™ Peel (Lidocaine 7% and Tetracaine 7% Cream) in Adult Patients Undergoing a Minor or Major Dermal Procedure [NCT00107835]Phase 3408 participants (Actual)Interventional2005-05-31Completed
A Randomized, Double-Blind, Paired, Placebo Controlled Study Evaluating the Duration of Anesthetic Effect Produced by the S-Caine™ Peel (Lidocaine 7% and Tetracaine 7% Cream) When Applied for 30 and 60 Minutes [NCT00110253]Phase 340 participants (Actual)Interventional2005-06-30Completed
Randomized, Double-Blind, Placebo Controlled, Paired Study Evaluating S-Caine™ Peel (Lidocaine 7% and Tetracaine 7% Cream)for Induction of Local Dermal Anesthesia for Dermal Filler Injection on the Face of Adults [NCT00110760]Phase 370 participants (Actual)Interventional2005-06-30Completed
Parameters in Fractional Laser Assisted Delivery of Topical Anesthetics: Role of Anesthetic and Application Time [NCT03279757]Phase 415 participants (Actual)Interventional2016-10-01Completed
An Open-Label Safety Study to Evaluate the Use of S-Caine™ Peel (Lidocaine 7% and Tetracaine 7% Cream) in Pediatric Patients Undergoing a Minor or Major Dermal Procedure [NCT00107822]Phase 380 participants Interventional2005-04-30Completed
A Randomized, Double-Blind, Placebo Controlled, Paired Study Evaluating the Efficacy of S-Caine™ Peel (Lidocaine 7% and Tetracaine 7% Cream) in Providing Local Dermal Anesthesia for Non-Ablative Facial Laser Resurfacing in Adults [NCT00110747]Phase 354 participants (Actual)Interventional2005-06-30Completed
A Comparison of Amethocaine Creams Versus Liposomal Lidocaine Cream as Pain Reliever Prior to Venipuncture in Children at the Paediatric Emergency Department. [NCT00353002]0 participants (Actual)Interventional2006-07-31Withdrawn
Pilot Study: A Randomized Trial Of Anesthetic Agents For Intravitreal Injection [NCT00769392]28 participants (Actual)Interventional2008-09-30Completed
Effect of Intra-cuff Lidocaine and Tetracaine on Tracheal Tube-induced Emergence Phenomena [NCT00798018]100 participants (Actual)Interventional2008-10-31Completed
Heated Lidocaine Patch Compared to Subacromial Injections in the Treatment of Pain Associated With Shoulder Impingement Syndrome, A Pilot [NCT01544283]Phase 260 participants (Anticipated)Interventional2012-03-31Recruiting
A Randomized, Double-Blind, Placebo Controlled, Paired Study Evaluating S-Caine™ Peel (Lidocaine 7% and Tetracaine 7% Cream) for Induction of Local Dermal Anesthesia for Laser-Assisted Tattoo Removal in Adults [NCT00110734]Phase 360 participants InterventionalCompleted
A Randomized, Double-Blind, Placebo Controlled, Parallel Study Evaluating the Efficacy of S-Caine™ Peel (Lidocaine 7% and Tetracaine 7% Cream) to Provide Local Dermal Anesthesia for Pulsed Dye Laser Therapy in Adults [NCT00110773]Phase 380 participants (Actual)Interventional2005-06-30Completed
Comparative Efficacy of 20% Benzocaine Versus TAC Alternate Gel for Control of Pain of Dental Needle Insertion in the Palate [NCT00846690]Phase 420 participants (Anticipated)Interventional2009-01-31Recruiting
A Prospective, Observer-masked, Randomized Clinical Trial to Investigate and Compare the Clinical Efficacy of Chloroprocaine 3% Gel and Tetracaine 0.5% Eye Drop as Topical Anestheticsin Phacoemulsification. [NCT04685538]Phase 3338 participants (Actual)Interventional2020-09-09Completed
Prospective, Randomized, Double-blinded, Split-face Study Comparing Efficacy of Lidocaine 2.5%/Prilocaine 2.5% Cream Under Occlusion, and Lidocaine 23% /Tetracaine 7% Ointment for Anesthesia Prior to 1927nm Fractional Laser Treatment [NCT04523961]Phase 2/Phase 332 participants (Anticipated)Interventional2021-01-08Recruiting
Phase II Study of Lidoderm Patches Prior to Intravenous Catheter Insertion. [NCT00552695]Phase 245 participants (Actual)Interventional2007-08-31Completed
Decision Support for Intraoperative Low Blood Pressure [NCT02726620]22,435 participants (Actual)Interventional2017-01-05Completed
A Double-Blind, Randomized, Split-Face Comparison Trial on Topical Anesthetic Agents Prior to Fractional Skin Resurfacing [NCT01842373]0 participants (Actual)Interventional2013-07-31Withdrawn(stopped due to Funding not secured)
Comparison of 2 Application Techniques for LET (Lidocaine 4%; Epinephrine 0.1%; Tetracaine 0.5%) Gel Used Prior to Simple Laceration Repair [NCT04536493]Phase 448 participants (Actual)Interventional2019-06-19Completed
Evaluation of the Depth and Duration of Anesthesia From Heated Lidocaine/Tetracaine (Synera®) Patches Compared With 5% Lidocaine (Lidoderm®) Patches Applied to Healthy Adult Volunteers [NCT01688518]Phase 122 participants (Actual)Interventional2012-09-30Completed
An Open-Label Pharmacokinetic Study of the Synera Patch Applied for 2-, 4-, and 12-hours and a Lidocaine/Tetracaine Patch Without Heat Applied for 4 Hours in Healthy Adult Volunteers [NCT01602757]Phase 112 participants (Actual)Interventional2010-02-28Completed
A Randomized, Double-Blind, Crossover Study Comparing Pliaglis™ (Lidocaine and Tetracaine) Cream 7%/7% to Placebo Cream When Applied for 60 Minutes in the Treatment of Patients With Postherpetic Neuralgia [NCT00609323]Phase 223 participants (Actual)Interventional2008-01-31Completed
Comparison of 0.5% Tetracaine Drops Versus 2% Lidocaine Gel for Anesthetic Efficacy and Comfort in Patients Undergoing LASIK [NCT01383200]Phase 411 participants (Actual)Interventional2011-06-30Terminated(stopped due to eyes that received gel had slightly thinner than intended flaps)
Comparison of 2 Application Techniques for LET (Lidocaine 4%; Epinephrine 0.1%; Tetracaine 0.5%) Gel Used Prior to Simple Laceration Repair in Children [NCT04203225]Phase 448 participants (Actual)Interventional2017-05-22Completed
Comparison of Efficacy of Two Topical Anesthetics: Benzocaine Versus Pliaglis for Control of Pain Associated With Dental Needle Insertion in the Palate, A Double Blind Study [NCT01951820]Phase 464 participants (Actual)Interventional2013-08-31Completed
A Phase 2, Single-Center, Open-Label, Randomized, Parallel-Groups, Dose-Ranging Study to Assess the Efficacy and Safety of Intranasally Administered Kovacaine Mist for Anesthetizing Maxillary Teeth in Pediatric Subjects [NCT01701505]Phase 248 participants (Actual)Interventional2012-10-31Completed
A Phase II, Single-Center, Randomized, Double-Blind, Active-Treatment-Controlled, Parallel-Group Study of the Efficacy of Kovacaine Nasal Spray for Anesthetizing Maxillary Teeth in Healthy Dental Patients [NCT01302483]Phase 245 participants (Actual)Interventional2008-12-31Completed
A Phase III Clinical Study of the Efficacy and Safety of Lidocaine and Tetracaine Cream (CU-30101) in a Multicenter, Randomized, Double-Blind, Active-Controlled, Paired Design for Facial Laser Aesthetics in Chinese Adults [NCT05793892]Phase 3286 participants (Anticipated)Interventional2023-03-31Not yet recruiting
Anesthetic Effect Duration Produced by Lidocaine 7% + Tetracaine 7% Cream on 2 Different Body Areas [NCT01545765]Phase 430 participants (Actual)Interventional2012-05-31Completed
Open-Label, Randomized, Split-Face Study to Evaluate the Efficacy, Safety and Subject Satisfaction of Pain Management During and After Restylane® Dermal Filler Injections for the Correction of Nasolabial Folds [NCT00716443]Phase 451 participants (Actual)Interventional2008-07-31Terminated(stopped due to Sponsor decision)
A Phase III, Multi-Center, Randomized, Double-Blind, Parallel-Groups Clinical Trial Comparing the Efficacy and Safety of Intranasally Administered Kovacaine Mist to Tetracaine Alone and to Placebo for Anesthetizing Maxillary Teeth in Adults [NCT01660893]Phase 326 participants (Actual)Interventional2012-08-31Terminated
Topical Analgesia Before Inhalational Anaesthesia: A Retrospective Observational Study [NCT04959409]500 participants (Actual)Observational2020-08-01Completed
Prospective Evaluation of Topical Anesthesia in Children [NCT04378283]99 participants (Actual)Interventional2016-05-31Completed
In Children, Does the Use of Synera Patch for Local Analgesia Before Vascular Access Reduce Pain Associated With Propofol Injection for Anesthesia Induction? [NCT01576770]Phase 480 participants (Anticipated)Interventional2012-04-30Recruiting
Dorsal Penile Nerve Block for Rigid Cystoscopy in Men: a Single-center, Randomized, Double-blind and Placebo-controlled Study [NCT02502487]258 participants (Actual)Interventional2015-06-30Completed
In Children, Placing a Synera Patch for Intravenous Access Combined With Administration of a Propofol-Lidocaine Mixture Decreases Pain Associated With Propofol Intravenous Injection. [NCT02240628]Phase 476 participants (Actual)Interventional2014-08-31Completed
A Double-blind, Cross-over, Incomplete Factorial Study to Assess the Local Anesthetic Efficacy and Safety of CTY-5339 Anesthetic Spray (CTY-5339A) When Applied to the Gingival Mucosal Tissue in Normal Volunteers [NCT03233737]Phase 275 participants (Actual)Interventional2017-06-15Completed
Local Anaesthesia [Topical Amethocaine Gel (Ametop)] for Intramuscular Injection in Term Neonates: A Randomized Controlled Trial. [NCT00267111]Phase 2110 participants (Actual)Interventional2003-07-31Completed
Effect of Tetracaine on Pain Management and Corneal Healing in Patients With Acute Corneal Abrasion [NCT02483897]Phase 30 participants (Actual)Interventional2015-06-30Withdrawn(stopped due to inabililty to recruit at required rate)
Preoperative Education With Image Illustrations Enhances the Effect of Tetracaine Mucilage in Alleviating Postoperative Catheter-related Bladder Discomfort: a Prospective, Randomized, Controlled Study [NCT03199105]64 participants (Anticipated)Interventional2017-07-01Recruiting
A Phase II, Single-Site, Open-Label Clinical Trial To Evaluate The Efficacy And Recommended Dosing Regimen Of Kovacaine Mist Administered Unilaterally For Anesthetizing Maxillary Teeth In Healthy Dental Patients [NCT01479517]Phase 230 participants (Actual)Interventional2012-01-31Completed
Efficacy and Safety of Synera in OA Pain [NCT01654302]Phase 1/Phase 240 participants (Actual)Interventional2013-09-30Completed
Effect of Synera in Reducing Pain Associated With Venipuncture and Superficial Dermatologic Procedures [NCT01744197]Phase 261 participants (Actual)Interventional2013-01-31Completed
The Pharmacokinetics Of Tetracaine, Para-Butylaminobenzoic Acid, And Oxymetazoline After Intranasal Administration Of The Highest Phase 3 Dose Of Kovacaine™ Mist To Healthy Volunteers [NCT01807624]Phase 224 participants (Actual)Interventional2013-03-31Completed
The Effect of Topical Anesthetic Using Lidocaine 2.5%/Prilocaine 2.5% Versus Lidocaine 7%/Tetracaine 7% Cream on Patients' Pain and Operative Experience During Treatment With QSwitched 532nm Laser [NCT02427724]48 participants (Anticipated)Interventional2015-04-30Active, not recruiting
Efficacy of Tetracaine/Oxymetazoline Nasal Spray for Endodontic Treatment [NCT03502135]Phase 40 participants (Actual)Interventional2018-09-30Withdrawn(stopped due to study drug not available in time)
Efficacy and Safety Assessment of Intracameral Injection of T2380 in Cataract Surgery Versus Reference Group (Topical Mydriatics and Anaesthetic) [NCT02101359]Phase 3609 participants (Actual)Interventional2011-06-30Completed
A Phase 3, Multi-Center, Randomized, Double-Blind, Parallel-Groups Clinical Trial Comparing The Efficacy And Safety Of Intranasally Administered Kovacaine Mist To Placebo For Anesthetizing Maxillary Teeth In Pediatric Patients [NCT01844830]Phase 390 participants (Actual)Interventional2013-05-31Completed
A Phase 3, Multi-Center, Randomized, Double-Blind, Parallel-Groups Clinical Trial Comparing the Efficacy and Safety of Intranasally Administered Kovacaine Mist to Placebo for Anesthetizing Maxillary Teeth in Adults [NCT01745380]Phase 3150 participants (Actual)Interventional2013-02-28Completed
[information is prepared from clinicaltrials.gov, extracted Sep-2024]

Trial Outcomes

TrialOutcome
NCT00267111 (2) [back to overview]Visual Analogue Scale
NCT00267111 (2) [back to overview]Pain Scores Assessed by Neonatal Facial Action
NCT00484393 (1) [back to overview]To Determine if a Difference in Pain Scale Ratings is Detectable Following Intramuscular Palivizumab Injection That Was Pre-treated With Placebo or Tetracaine.
NCT00530803 (5) [back to overview]Blinded Observer's Subjective Ratings of the Participant's Pain Level at Needle Insertion, Using a 6-point NRS
NCT00530803 (5) [back to overview]Parent Rating of Child's Pain Using a 6-point NRS
NCT00530803 (5) [back to overview]Participants Self-rating of Pain Using the Wong-Baker FACES Pain Rating Scale.
NCT00530803 (5) [back to overview]Blinded Observer's Subjective Ratings of the Participant's Pain Level at 5 Minutes Post Venipuncture Procedure, Using a 6-point NRS
NCT00530803 (5) [back to overview]Blinded Observer's Subjective Ratings of Participants' Pain Level at Tourniquet Placement, Using a 6-point NRS
NCT00552695 (2) [back to overview]Success of Intravenous (IV) Insertion
NCT00552695 (2) [back to overview]Pain on Visual Analog Scale (VAS)
NCT00716443 (15) [back to overview]"Number of Participants Who Answered the Question If it Was Different Than What You Expected, Was it? Three Hours After Injection of Restylane® Into the Nasolabial Folds"
NCT00716443 (15) [back to overview]"Number of Participants Who Answered the Question If You Experienced Pain, Was it What You Expected From the Injection Procedure? Three Hours After Injection of Restylane® Into the Nasolabial Folds"
NCT00716443 (15) [back to overview]"Number of Participants Who Answered the Question Still Speaking to the Topical Anesthetic You Had on the Right/Left Side of Your Face, Would You Recommend it to Your Friend or Family Member? 3 Hours After Injection of Restylane® Into Nasolabial Folds"
NCT00716443 (15) [back to overview]"Number of Participants Who Answered the Question What Level of Pain Did You Experience When You Were Injected? Three Hours After Injection of Restylane® Into the Nasolabial Folds"
NCT00716443 (15) [back to overview]"Number of Participants With Yes/no Answers to Question to Investigator Did the Topical Anesthetics Provide Adequate Anesthesia for the Injections of Restylane® Into the Nasolabial Folds Procedure? Day of Injection of Restylane® Into Nasolabial Folds"
NCT00716443 (15) [back to overview]Number of Participants in Each Category of the Blinded Evaluator's Evaluation of Subject's Pain Scale Immediately After Injection of Restylane® Into the Nasolabial Folds
NCT00716443 (15) [back to overview]Number of Participants in Each Category of the Blinded Evaluator's Evaluation of Subject's Pain Scale One Hour After Injection of Restylane® Into the Nasolabial Folds
NCT00716443 (15) [back to overview]Number of Participants in Each Category of the Blinded Evaluator's Evaluation of Subject's Pain Scale Upon First Needle Stick of Injection of Restylane® Into the Nasolabial Folds
NCT00716443 (15) [back to overview]Number of Participants in Each Category of the Investigator Evaluation of the Subject's Post Procedure Pain Assessment Scale Immediately After Injection of Restylane® Into the Nasolabial Folds
NCT00716443 (15) [back to overview]Number of Participants in Each Category of the Investigator Evaluation of the Subject's Post Procedure Pain Assessment Scale Upon First Needle Stick of Injection of Restylane® Into the Nasolabial Folds
NCT00716443 (15) [back to overview]Number of Participants in Each Category of the Investigator's Evaluation of Subject's Pain Scale One Hour After Injection of Restylane® Into the Nasolabial Folds
NCT00716443 (15) [back to overview]Subject's Pain Evaluation by Visual Analog Scale (VAS)Upon First Needlestick, Immediately After Injection, One Hour After Injection and Three Hours After Injection of Restylane® Into the Nasolabial Folds
NCT00716443 (15) [back to overview]Number of Participants in Each Category of the Blinded Evaluator's Evaluation of Subject's Pain Scale Three Hours After Injection of Restylane® Into the Nasolabial Folds
NCT00716443 (15) [back to overview]Number of Participants in Each Category of the Investigator's Evaluation of Subject's Pain Scale Three Hours After Injection of Restylane® Into the Nasolabial Folds
NCT00716443 (15) [back to overview]Number of Participants With Tolerability Assessments Resulting in Adverse Events From Baseline to Two Days After Injection of Restylane® Into the Nasolabial Folds
NCT00769392 (2) [back to overview]Discomfort From Anesthesia Used Prior to Intravitreal Injections
NCT00769392 (2) [back to overview]Discomfort Associated With the Intravitreal Injection
NCT00798018 (1) [back to overview]Visual Analogue Scale(0-100mm) by the Subject.
NCT00827073 (2) [back to overview]Change in Ln(Bacterial Colony Count) From Pre-antibiotic Administration to Post Study Medication Swabs
NCT00827073 (2) [back to overview]Number of Bacterial Species in Pre-antibiotic Administration and in Post Study Medication Swabs
NCT01005459 (1) [back to overview]Spinal Analgesic Duration
NCT01302483 (5) [back to overview]Maximum Change in Pulse From Baseline
NCT01302483 (5) [back to overview]Pulpal Anesthesia
NCT01302483 (5) [back to overview]Maximum Change in Blood Pressure From Baseline
NCT01302483 (5) [back to overview]Soft Tissue Anesthesia Duration
NCT01302483 (5) [back to overview]Maximum Change in Pulse Oximetry From Baseline
NCT01304316 (9) [back to overview]Cmax of PBBA
NCT01304316 (9) [back to overview]Cmax of Tetracaine
NCT01304316 (9) [back to overview]Diastolic BP Maximum Change From Baseline
NCT01304316 (9) [back to overview]Half Life of Oxymetazoline
NCT01304316 (9) [back to overview]Pulse Oximetry Maximum Change From Baseline
NCT01304316 (9) [back to overview]Pulse Rate Maximum Change From Baseline
NCT01304316 (9) [back to overview]Systolic BP Maximum Change From Baseline
NCT01304316 (9) [back to overview]Half Life of PBBA
NCT01304316 (9) [back to overview]Cmax of Oxymetazoline
NCT01383200 (1) [back to overview]Participants Score on Pain Scale
NCT01479517 (4) [back to overview]The Proportion of Subjects Receiving Kovacaine Mist Who do Not Require Rescue Anesthesia During the Operative Dental Procedure
NCT01479517 (4) [back to overview]Naris Examination
NCT01479517 (4) [back to overview]The Incidence of Subjects Receiving Kovacaine Mist With Changes in Systolic and Diastolic Blood Pressure Exceeding +/- 25% of Preoperative Measurements Values.
NCT01479517 (4) [back to overview]The Proportion of Subjects Giving a Positive Response to Evaluation Question for Subjective Numbness Assessment (SNA) After the Procedure is Completed.
NCT01545765 (2) [back to overview]Duration of Anesthesia(Minutes)
NCT01545765 (2) [back to overview]Adverse Events
NCT01654302 (1) [back to overview]Index Knee Pain Scores on a Numeric Rating Scale (NRS)
NCT01660893 (14) [back to overview]Absolute Maximum Change From Baseline in Heart Rate
NCT01660893 (14) [back to overview]Number of Participants With a Decrease From Baseline in Diastolic Blood Pressure Greater Than or Equal to 15 mm Hg and to a Value Lower Than 90 mm Hg
NCT01660893 (14) [back to overview]Number of Participants With a Decrease From Baseline in Systolic Blood Pressure Greater Than or Equal to 15 mm Hg and to a Value Lower Than 90 mm Hg
NCT01660893 (14) [back to overview]Number of Participants With an Increase From Baseline in Diastolic Blood Pressure Greater Than or Equal to 15 mm Hg and to a Value Higher Than 90 mm Hg
NCT01660893 (14) [back to overview]Number of Participants With an Increase From Baseline in Systolic Blood Pressure Greater Than or Equal to 25 mm Hg and to a Value Higher Than 160 mm Hg
NCT01660893 (14) [back to overview]Alcohol Sniff Test
NCT01660893 (14) [back to overview]Absolute Maximum Change From Baseline in Systolic Blood Pressure and Diastolic Blood Pressure
NCT01660893 (14) [back to overview]Number of Participants With Heart Rate Lower Than 50 Bpm
NCT01660893 (14) [back to overview]The Profile Over Time of Systolic Blood Pressure
NCT01660893 (14) [back to overview]The Profile Over Time of Heart Rate
NCT01660893 (14) [back to overview]The Profile Over Time of Diastolic Blood Pressure
NCT01660893 (14) [back to overview]Intraoral Soft-tissue Anesthesia (Yes/no)
NCT01660893 (14) [back to overview]Completion of the Study Dental Procedure Without Need for Rescue by Injection of Local Anesthetic (Yes/no).
NCT01660893 (14) [back to overview]Number of Participants With Heart Rate Higher Than 125 Bpm
NCT01701505 (10) [back to overview]Incidence of Adverse Events by Dose Level Regardless of Age
NCT01701505 (10) [back to overview]Number of Participants Who Completed the Study Dental Procedure Without Need for Rescue by Injection of Local Anesthetic.
NCT01701505 (10) [back to overview]Diastolic Blood Pressure
NCT01701505 (10) [back to overview]Heart Rate
NCT01701505 (10) [back to overview]Naris Examination (NE) to Assess Reactions to the Study Drug.
NCT01701505 (10) [back to overview]Systolic Blood Pressure
NCT01701505 (10) [back to overview]Oxygen Saturation
NCT01701505 (10) [back to overview]Number of Participants With Adverse Events by Dose Level and Age
NCT01701505 (10) [back to overview]Number of Participants With Adverse Events by Dose Level and Age
NCT01701505 (10) [back to overview]Number of Participants With Adverse Events by Dose Level and Age
NCT01710787 (16) [back to overview]Absolute Maximum Change From Baseline in Diastolic Blood Pressure
NCT01710787 (16) [back to overview]Absolute Maximum Change From Baseline in Heart Rate
NCT01710787 (16) [back to overview]Absolute Maximum Change From Baseline in Systolic Blood Pressure
NCT01710787 (16) [back to overview]Number of Participants Who Completed the Study Dental Procedure After Without Need for Rescue by Injection of Local Anesthetic.
NCT01710787 (16) [back to overview]Number of Participants With a Decrease From Baseline in Diastolic Blood Pressure Greater Than or Equal to 10 mm Hg and to a Value Lower Than 50 mm Hg
NCT01710787 (16) [back to overview]Number of Participants With a Decrease From Baseline in Systolic Blood Pressure Greater Than or Equal to 15 mm Hg and to a Value Lower Than 90 mm Hg
NCT01710787 (16) [back to overview]Number of Participants With a Heart Rate Higher Than 125 Bpm
NCT01710787 (16) [back to overview]Number of Participants With an Increase From Baseline in Diastolic Blood Pressure Greater Than or Equal to 15 mm Hg and to a Value Higher Than 105 mm Hg
NCT01710787 (16) [back to overview]Number of Participants With an Increase From Baseline in Systolic Blood Pressure Greater Than or Equal to 25 mm Hg and to a Value Higher Than 160 mm Hg
NCT01710787 (16) [back to overview]Alcohol Sniff Test
NCT01710787 (16) [back to overview]Intraoral Soft-tissue Anesthesia (Yes/no)
NCT01710787 (16) [back to overview]The Profile Over Time of Systolic Blood Pressure
NCT01710787 (16) [back to overview]The Profile Over Time of Heart Rate
NCT01710787 (16) [back to overview]The Profile Over Time of Diastolic Blood Pressure
NCT01710787 (16) [back to overview]Number of Participants With a Heart Rate Lower Than 50 Bpm
NCT01710787 (16) [back to overview]Intraoral Soft-tissue Anesthesia (Onset and Duration)
NCT01744197 (3) [back to overview]Global Assessment of Satisfaction With Venipuncture
NCT01744197 (3) [back to overview]Percentage of Patients With No Pain (VAS=0)
NCT01744197 (3) [back to overview]Percentage of Patients With No or Minor Pain (VAS<3)
NCT01745380 (16) [back to overview]Number of Participants Who Completed the Study Dental Procedure Without Need for Rescue by Injection of Local Anesthetic.
NCT01745380 (16) [back to overview]Maximum Change From Baseline in Systolic Blood Pressure
NCT01745380 (16) [back to overview]Maximum Change From Baseline in Heart Rate
NCT01745380 (16) [back to overview]Maximum Change From Baseline in Diastolic Blood Pressure
NCT01745380 (16) [back to overview]Alcohol Sniff Test
NCT01745380 (16) [back to overview]The Profile Over Time of Diastolic Blood Pressure
NCT01745380 (16) [back to overview]The Profile Over Time of Heart Rate
NCT01745380 (16) [back to overview]The Profile Over Time of Systolic Blood Pressure
NCT01745380 (16) [back to overview]Number of Participants With an Increase From Baseline in Systolic Blood Pressure Greater Than or Equal to 25 mm Hg and/or to a Value Higher Than 160 mm Hg
NCT01745380 (16) [back to overview]Number of Participants With a Heart Rate Lower Than 50 Bpm
NCT01745380 (16) [back to overview]Number of Participants With a Heart Rate Higher Than 125 Bpm
NCT01745380 (16) [back to overview]Number of Participants With a Decrease From Baseline in Systolic Blood Pressure Greater Than or Equal to 15 mm Hg and/or to a Value Lower Than 90 mm Hg
NCT01745380 (16) [back to overview]Number of Participants With a Decrease From Baseline in Diastolic Blood Pressure Greater Than or Equal to 10 mm Hg and/or to a Value Lower Than 50 mm Hg
NCT01745380 (16) [back to overview]Number of Participants With an Increase From Baseline in Diastolic Blood Pressure Greater Than or Equal to 15 mm Hg and/or to a Value Higher Than 105 mm Hg
NCT01745380 (16) [back to overview]Number of Participants Who Received Three Sprays and Completed the Study Dental Procedure Without Need for Rescue by Injection of Local Anesthetic.
NCT01745380 (16) [back to overview]Number of Participants Who Completed the Study Dental Procedure Without Need for Rescue by Injection of Local Anesthetic by Age Group (≤50 and >50 Years)
NCT01807624 (13) [back to overview]Decrease in Pulse Rate > 20 Bpm on 2 Consecutive Measurements After Administration of Study Medication
NCT01807624 (13) [back to overview]Decrease in SBP > 20 mmHg on 2 Consecutive Measurements After Administration of Study Medication
NCT01807624 (13) [back to overview]Increase in DBP > 20 mmHg on 2 Consecutive Measurements After Administration of Study Medication
NCT01807624 (13) [back to overview]Increase in Pulse Rate > 20 Bpm on 2 Consecutive Measurements After Administration of Study Medication
NCT01807624 (13) [back to overview]Increase in SBP > 20 mmHg on 2 Consecutive Measurements After Administration of Study Medication
NCT01807624 (13) [back to overview]SpO2 Decrease of > 5% on 2 Consecutive Measurements After Administration of Study Medication
NCT01807624 (13) [back to overview]SpO2 Increase of > 5% on 2 Consecutive Measurements After Administration of Study Medication
NCT01807624 (13) [back to overview]AUC0-t of Oxymetazoline and PBBA
NCT01807624 (13) [back to overview]Cmax of Oxymetazoline and PBBA
NCT01807624 (13) [back to overview]Half-life of Oxymetazoline and PBBA
NCT01807624 (13) [back to overview]Tmax of Oxymetazoline and PBBA
NCT01807624 (13) [back to overview]AUC0-infinity of Oxymetazoline and PBBA
NCT01807624 (13) [back to overview]Decrease in DBP > 20 mmHg on 2 Consecutive Measurements After Administration of Study Medication
NCT01844830 (9) [back to overview]Results of Naris Examination (NE) - Patency and Ulcerations
NCT01844830 (9) [back to overview]Number of Participants Who Completed the Study Dental Procedure Without Need for Rescue by Injection of Local Anesthetic. by Age Group (3-5, 6-11, and 12-17 Years Old, Inclusive).
NCT01844830 (9) [back to overview]Incidence of Adverse Events (AEs) by Dosage Cohort
NCT01844830 (9) [back to overview]Incidence of Adverse Events (AEs) by Age Group
NCT01844830 (9) [back to overview]Number of Participants Who Completed the Study Dental Procedure Without Need for Rescue by Injection of Local Anesthetic.
NCT01844830 (9) [back to overview]Maximum Change From Baseline in Systolic Blood Pressure
NCT01844830 (9) [back to overview]Maximum Change From Baseline in Heart Rate
NCT01844830 (9) [back to overview]Maximum Change From Baseline in Diastolic Blood Pressure
NCT01844830 (9) [back to overview]Number of Participants Who Completed the Study Dental Procedure Without Need for Rescue by Injection of Local Anesthetic.by Dosage Cohort.
NCT01951820 (1) [back to overview]Measurement of Pain Associated With Injection, in Millimeters, According to Visual Analog Scale
NCT02101359 (1) [back to overview]The Primary Efficacy Variable is Response Based on the Realisation of the Capsulorhexis Without Use of Any Additive Mydriatic Treatment.
NCT02240628 (2) [back to overview]Number of Children in Each Group Who Don't Feel Pain or Have Mild Pain on Propofol Injection.
NCT02240628 (2) [back to overview]Pain Intensity
NCT02502487 (21) [back to overview]Visual Analog Scale (VAS) for Pain
NCT02502487 (21) [back to overview]Visual Analog Scale (VAS) for Pain
NCT02502487 (21) [back to overview]Visual Analog Scale (VAS) for Pain
NCT02502487 (21) [back to overview]Visual Analog Scale (VAS) for Pain
NCT02502487 (21) [back to overview]Breath Rate at Cystoscopic Inspection of Penile and Bulbar Urthra
NCT02502487 (21) [back to overview]Heart Rate at Cystoscopic Inspection of Penile and Bulbar Urthra
NCT02502487 (21) [back to overview]Heart Rate Before Gel Administration
NCT02502487 (21) [back to overview]Mean Arterial Pressure After Withdrawal of Cystoscope
NCT02502487 (21) [back to overview]Mean Arterial Pressure at Cystoscopic Inspection of External Sphincter
NCT02502487 (21) [back to overview]Mean Arterial Pressure at Cystoscopic Inspection of Penile and Bulbar Urthra
NCT02502487 (21) [back to overview]Mean Arterial Pressure Before Gel Administration
NCT02502487 (21) [back to overview]Oxygen Saturation by Pulse After Withdrawal of Cystoscope
NCT02502487 (21) [back to overview]Oxygen Saturation by Pulse at Cystoscopic Inspection of External Sphincter
NCT02502487 (21) [back to overview]Oxygen Saturation by Pulse at Cystoscopic Inspection of Penile and Bulbar Urthra
NCT02502487 (21) [back to overview]Breath Rate After Withdrawal of Cystoscope
NCT02502487 (21) [back to overview]Oxygen Saturation by Pulse Before Gel Administration
NCT02502487 (21) [back to overview]Breath Rate at Cystoscopic Inspection of External Sphincter
NCT02502487 (21) [back to overview]Visual Analog Scale (VAS) for Pain
NCT02502487 (21) [back to overview]Breath Rate Before Gel Administration
NCT02502487 (21) [back to overview]Heart Rate After Withdrawal of Cystoscope
NCT02502487 (21) [back to overview]Heart Rate at Cystoscopic Inspection of External Sphincter
NCT02726620 (43) [back to overview]Usage Frequency of Cardiovascular Drugs: Norepinephrine
NCT02726620 (43) [back to overview]Usage Frequency of Cardiovascular Drugs: Glycopyrrolate
NCT02726620 (43) [back to overview]Usage Frequency of Cardiovascular Drugs: Ephinephrine
NCT02726620 (43) [back to overview]Usage Frequency of Cardiovascular Drugs: Ephedrine
NCT02726620 (43) [back to overview]Average Use of Cardiovascular Drugs: Norepinephrine
NCT02726620 (43) [back to overview]Average Use of Cardiovascular Drugs: Glycopyrrolate
NCT02726620 (43) [back to overview]Average Use of Cardiovascular Drugs: Epinephrine
NCT02726620 (43) [back to overview]Average Use of Cardiovascular Drugs: Ephedrine
NCT02726620 (43) [back to overview]30-day Mortality
NCT02726620 (43) [back to overview]Timing of Cardiovascular Drugs for MAP < 60 mmHg
NCT02726620 (43) [back to overview]Timing of Cardiovascular Drugs for MAP < 55 mmHg
NCT02726620 (43) [back to overview]Timing of Cardiovascular Drugs for MAP < 50 mmHg
NCT02726620 (43) [back to overview]Time to Discharge Readiness at the Postanesthesia Care Unit (PACU)
NCT02726620 (43) [back to overview]Postoperative Rise in Creatinine Levels
NCT02726620 (43) [back to overview]Intravenous Anesthetic Drug Use During Intraoperative Hypotension: MAP < 65 mmHg
NCT02726620 (43) [back to overview]Intravenous Anesthetic Drug Use During Intraoperative Hypotension: MAP < 60 mmHg
NCT02726620 (43) [back to overview]Intravenous Anesthetic Drug Use During Intraoperative Hypotension: MAP < 55 mmHg
NCT02726620 (43) [back to overview]Intravenous Anesthetic Drug Use During Intraoperative Hypotension: MAP < 50 mmHg
NCT02726620 (43) [back to overview]Intraoperative Administration of Intravenous Fluids
NCT02726620 (43) [back to overview]Incidence of a MAP < 60 mmHg for > 20 Minutes
NCT02726620 (43) [back to overview]Incidence of a MAP < 60 mmHg for > 10 Minutes
NCT02726620 (43) [back to overview]Incidence of a MAP < 60 mmHg
NCT02726620 (43) [back to overview]Incidence of a MAP < 55 mmHg for > 20 Minutes
NCT02726620 (43) [back to overview]Incidence of a MAP < 55 mmHg for > 10 Minutes
NCT02726620 (43) [back to overview]Incidence of a MAP < 55 mmHg
NCT02726620 (43) [back to overview]Incidence of a MAP < 50 mmHg for > 20 Minutes
NCT02726620 (43) [back to overview]Timing of Cardiovascular Drugs for MAP < 65 mmHg
NCT02726620 (43) [back to overview]Incidence of a MAP < 50 mmHg for > 10 Minutes
NCT02726620 (43) [back to overview]Incidence of a MAP < 50 mmHg
NCT02726620 (43) [back to overview]In-hospital Mortality
NCT02726620 (43) [back to overview]Estimated Intraoperative Blood Loss
NCT02726620 (43) [back to overview]Depth and Duration of Intraoperative Hypotension - Threshold MAP 75 mmHg
NCT02726620 (43) [back to overview]Depth and Duration of Intraoperative Hypotension - Threshold MAP 70 mmHg
NCT02726620 (43) [back to overview]Depth and Duration of Intraoperative Hypotension - Threshold MAP 65 mmHg
NCT02726620 (43) [back to overview]Depth and Duration of Intraoperative Hypotension - Threshold MAP 60 mmHg
NCT02726620 (43) [back to overview]Depth and Duration of Intraoperative Hypotension - Threshold MAP 55 mmHg
NCT02726620 (43) [back to overview]Depth and Duration of Intraoperative Hypotension - Threshold MAP 50 mmHg
NCT02726620 (43) [back to overview]Average Use of Cardiovascular Drugs: Phenylephrine
NCT02726620 (43) [back to overview]Inhaled Anesthetic Drug Use During Intraoperative Hypotension: MAP < 65 mmHg
NCT02726620 (43) [back to overview]Inhaled Anesthetic Drug Use During Intraoperative Hypotension: MAP < 60 mmHg
NCT02726620 (43) [back to overview]Inhaled Anesthetic Drug Use During Intraoperative Hypotension: MAP < 55 mmHg
NCT02726620 (43) [back to overview]Inhaled Anesthetic Drug Use During Intraoperative Hypotension: MAP < 50 mmHg
NCT02726620 (43) [back to overview]Usage Frequency of Cardiovascular Drugs: Phenylephrine
NCT02908620 (10) [back to overview]Duration of Anesthesia as Measured by Pin Prick Test (PPT) for One Spray CTY-5339-A Compared to One Spray CTY-5339-CB
NCT02908620 (10) [back to overview]Duration of Anesthesia as Measured by Pin Prick Test (PPT) for Two Sprays CTY-5339-A Compared to One Spray CTY-5339-CB in Combination With One Spray CTY-5339-P (Placebo)
NCT02908620 (10) [back to overview]Duration of Anesthesia as Measured by PPT for One Spray CTY-5339-A Compared to Two Sprays CTY-5339-A
NCT02908620 (10) [back to overview]Duration of Anesthesia as Measured by QST Heat for One Spray CTY-5339-A Compared to Two Sprays CTY-5339-A
NCT02908620 (10) [back to overview]Duration of Anesthesia as Measured by QST Heat for Two Sprays CTY-5339-A Compared to One Spray CTY-5339-CB in Combination With One Spray CTY-5339-P (Placebo)
NCT02908620 (10) [back to overview]Onset of Anesthesia for PPT
NCT02908620 (10) [back to overview]Onset of Anesthesia for QST Heat
NCT02908620 (10) [back to overview]Percentage of Responders for PPT at Each Time Point
NCT02908620 (10) [back to overview]Percentage of Responders for QST Heat at Each Time Point
NCT02908620 (10) [back to overview]Duration of Anesthesia as Measured by Heat Sensation Threshold (QST Heat) for One Spray CTY-5339-A Compared to One Spray CTY-5339-CB
NCT03233737 (22) [back to overview]Stage II: Sum of Temperature Differences (STID) for Heat Sensation Threshold (QST Heat) (Post-hoc)
NCT03233737 (22) [back to overview]Stage II: Onset of Anesthesia for Pin Prick Test (PPT)
NCT03233737 (22) [back to overview]Stage II: Percentage of Subjects Reaching Maximum Heat for Heat Sensation Threshold (QST Heat)
NCT03233737 (22) [back to overview]Stage II: Percentage of Subjects Reaching Minimal Pain on Pin Prick Test (PPT) (≤2 on Numerical Rating Scale Pain Scale)
NCT03233737 (22) [back to overview]Stage I: Percentage of Responders for Heat Sensation Threshold (QST Heat) at Each Time Point
NCT03233737 (22) [back to overview]Stage II: Duration of Anesthesia as Measured by Pin Prick Test (PPT) for One Spray CTY-5339-A Compared to One Spray CTY-5339-CB
NCT03233737 (22) [back to overview]Stage I: Percentage of Responders for Pin Prick Test (PPT) at Each Time Point
NCT03233737 (22) [back to overview]Stage I: Sum of Pain Intensity Differences (SPID) for Pin Prick Test (PPT) (Post-hoc)
NCT03233737 (22) [back to overview]Stage II: Percentage of Responders for Heat Sensation Threshold (QST Heat) at Each Time Point
NCT03233737 (22) [back to overview]Stage II: Duration of Anesthesia as Measured by Heat Sensation Threshold (QST Heat) for One Spray CTY-5339-A Compared to One Spray CTY-5339-CB
NCT03233737 (22) [back to overview]Stage I: Percentage of Subjects Reaching Minimal Pain on Pin Prick Test (PPT) (≤2 on Numerical Rating Scale Pain Scale)
NCT03233737 (22) [back to overview]Stage I: Percentage of Subjects Reaching Maximum Heat for Heat Sensation Threshold (QST Heat)
NCT03233737 (22) [back to overview]Stage I: Sum of Temperature Differences (STID) for Heat Sensation Threshold (QST Heat) (Post-hoc)
NCT03233737 (22) [back to overview]Stage I: Onset of Anesthesia for Heat Sensation Threshold (QST Heat)
NCT03233737 (22) [back to overview]Stage I: Duration of Minimal Pain for Pin Prick Test (PPT) (≤2 on Numerical Rating Scale Pain Scale)
NCT03233737 (22) [back to overview]Stage I: Duration of Anesthesia as Measured by Pin Prick Test (PPT) for One Spray CTY-5339-A Compared to One Spray CTY-5339-CB Compared to One Spray CTY-5339-P (Placebo: Vehicle Control)
NCT03233737 (22) [back to overview]Stage I: Duration of Anesthesia as Measured by Heat Sensation Threshold (QST Heat) for One Spray CTY-5339-A Compared to One Spray CTY-5339-CB Compared to One Spray CTY-5339-P (Placebo: Vehicle Control)
NCT03233737 (22) [back to overview]Stage I: Onset of Anesthesia for Pin Prick Test (PPT)
NCT03233737 (22) [back to overview]Stage II: Percentage of Responders for Pin Prick Test (PPT) at Each Time Point
NCT03233737 (22) [back to overview]Stage II: Sum of Pain Intensity Differences (SPID) for Pin Prick Test (PPT) (Post-hoc)
NCT03233737 (22) [back to overview]Stage II: Duration of Minimal Pain for Pin Prick Test (PPT) (≤2 on Numerical Rating Scale Pain Scale)
NCT03233737 (22) [back to overview]Stage II: Onset of Anesthesia for Heat Sensation Threshold (QST Heat)
NCT04203225 (2) [back to overview]Visual Analog Scale Pain Score
NCT04203225 (2) [back to overview]Need for Additional Local Anesthetic
NCT04685538 (11) [back to overview]Patient Global Satisfaction
NCT04685538 (11) [back to overview]Number of Participants With Abnormalities of the Retina, Macula, or Optic Nerve by Fundoscopy
NCT04685538 (11) [back to overview]Number of Participants in Each Treatment Group With a Successful Surface Anesthesia
NCT04685538 (11) [back to overview]Intra-ocular Pressure
NCT04685538 (11) [back to overview]Fluoresceine
NCT04685538 (11) [back to overview]Objective Ocular Signs
NCT04685538 (11) [back to overview]Corneal Thickness
NCT04685538 (11) [back to overview]Changes in Ocular Symptoms
NCT04685538 (11) [back to overview]Best Far Corrected Visual Acuity
NCT04685538 (11) [back to overview]Surgeon Satisfaction
NCT04685538 (11) [back to overview]Endothelial Cell Counts

Visual Analogue Scale

"Parents and nurses were asked to assess the infant's pain response during the procedure using Visual analogue scale (VAS) on an unmarked horizontal 10 cm continuous line where 0=no pain on the left side and 10=worst possible pain on the right side. Parents and nurses were trained to use the VAS prior to the IM injection." (NCT00267111)
Timeframe: During the entire procedure

,
InterventionCms (Mean)
Parents VAS ratingNurses VAS rating
Amethocaine Gel 4% Group4.65.0
Placebo Group4.64.9

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Pain Scores Assessed by Neonatal Facial Action

The presence or absence of 3 facial actions (brow bulge, eyes squeeze and deepening of the nasolabial furrow) were scored in 2 second intervals for the first 20 seconds (or less if the phase lasted < 20 seconds) of each procedure phase from the videotapes by a trained research assistant. The data were then collapsed for each facial action into the percentage of time the infant expressed the action. An overall pain score was computed by summing the percentage scores for the three facial actions and then dividing by three. The score ranged from 0% to 100% with higher values suggesting more pain. (NCT00267111)
Timeframe: For the purpose of analysis IM injection procedure was divided into 4 phases: baseline , cleansing, injection and recovery phases.. For each phase facial actions were scored for the first 20 seconds or less if the phase lasted < 20 seconds.

,
InterventionPercentage of time (Mean)
BaselineCleaningInjectionRecovery
1 g Amethocaine Gel 4%14307079
Placebo Group18447576

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To Determine if a Difference in Pain Scale Ratings is Detectable Following Intramuscular Palivizumab Injection That Was Pre-treated With Placebo or Tetracaine.

Parent score 1-10 (1 representing no pain and 10 representing extreme pain) FLACC (Face, Legs, Activity, Cry, Consolability) Score 0-10 (at baseline and post injection) (0 representing no pain and 10 representing extreme pain) Change in FLACC score (NCT00484393)
Timeframe: 2 visits, 1 month apart

,
Interventionunits on a scale (Mean)
Parent scoreFLACC at baselineFLACC post injectionChange in FLACC
Placebo7.31.69.37.7
Tetracaine7.31.78.46.7

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Blinded Observer's Subjective Ratings of the Participant's Pain Level at Needle Insertion, Using a 6-point NRS

The NRS (Numerical Rating Scale) is a 6-point rating scale where 0= no pain and 5 = worst pain. Blinded observers reported their own subjective evaluation of the level of pain experienced by the participants at needle insertion. Total number of participants subjectively evaluated as experiencing each pain level is reported. (NCT00530803)
Timeframe: during needle insertion

,
InterventionParticipants (Count of Participants)
Participants evaluated at NRS = 0 (No pain)Participants evaluated at NRS = 1Participants evaluated at NRS = 2Participants evaluated at NRS = 3Participants evaluated at NRS = 4Participants evaluated at NRS = 5
EMLA Cream32142200
Synera Patch25129220

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Parent Rating of Child's Pain Using a 6-point NRS

The Numerical Rating Scale (NRS) is a 6-point rating scale where 0= no pain and 5 = worst pain. Parents reported their own subjective evaluation of participants pain level. Each participant had only one parental assessment. Total number of parental assessment for each pain level on the 6-point NRS is reported as total number of participants experiencing that pain level. (NCT00530803)
Timeframe: immediately after venipuncture is completed

,
InterventionParticipants (Count of Participants)
number of participants with NRS=0 (no pain)number of participants with NRS=1number of participants with NRS=2number of participants with NRS=3number of participants with NRS=4number of participants with NRS=5
EMLA Cream4261100
Synera Patch4151201

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Participants Self-rating of Pain Using the Wong-Baker FACES Pain Rating Scale.

"Participants were asked to report their level of pain using a 6-point Wong-Baker FACES Pain Rating Scale ranging from 0, no pain, to 5, the most pain you can have. The Wong-Baker FACES Pain Rating Scale is a validated tool for measuring pain in patients as young as 3 years old. A FACES pain score less than or equal to 2 is considered no pain to mild pain, and is clinically acceptable. Studies have shown average FACES pain scores for children receiving vascular access with placebo to be 2.2 to 3.5." (NCT00530803)
Timeframe: immediately after completion of venipuncture

,
InterventionParticipants (Count of Participants)
Participants with FACES Score = 0 (No pain)Participants with FACES Score = 1Participants with FACES Score = 2Participants with FACES Score = 3Participants with FACES Score = 4Participants with FACES Score = 5
EMLA Cream4262000
Synera Patch3883100

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Blinded Observer's Subjective Ratings of the Participant's Pain Level at 5 Minutes Post Venipuncture Procedure, Using a 6-point NRS

The NRS (Numerical Rating Scale) is a 6-point rating scale where 0= no pain and 5 = worst pain. Blinded observers reported their own subjective evaluation of the level of pain participants were experiencing 5 minutes after the venipuncture was completed. Total number of participants subjectively evaluated as experiencing each pain level is reported. (NCT00530803)
Timeframe: 5 minutes post venipuncture

,
InterventionParticipants (Count of Participants)
Participants evaluated at NRS = 0 (No pain)Participants evaluated at NRS = 1Participants evaluated at NRS = 2Participants evaluated at NRS = 3Participants evaluated at NRS = 4Participants evaluated at NRS = 5
EMLA Cream4531100
Synera Patch4541000

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Blinded Observer's Subjective Ratings of Participants' Pain Level at Tourniquet Placement, Using a 6-point NRS

The NRS (Numerical Rating Scale) is a 6-point rating scale where 0= no pain and 5 = worst pain. Blinded observers reported their own subjective evaluation of the level of pain experienced by the participants at tourniquet placement. Total number of participants subjectively evaluated as experiencing each pain level is reported. (NCT00530803)
Timeframe: before venipuncture

,
InterventionParticipants (Count of Participants)
Participants evaluated at NRS = 0 (No pain)Participants evaluated at NRS = 1Participants evaluated at NRS = 2Participants evaluated at NRS = 3Participants evaluated at NRS = 4Participants evaluated at NRS = 5
EMLA Cream4162100
Synera Patch3765110

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Success of Intravenous (IV) Insertion

Percentage of patients in whom intravenous catheter was inserted successfully (NCT00552695)
Timeframe: After first attempt of catheter insertion

InterventionPercentage of participants (Number)
LIDODERM Patch18
Control Patch17

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Pain on Visual Analog Scale (VAS)

Pain on 100 mm Visual Aanalog Scale from 0 (no pain) to 100 (most pain). (NCT00552695)
Timeframe: 0 MINUTES

Interventionmm (Median)
LIDODERM Patch18
Control Patch35

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"Number of Participants Who Answered the Question If it Was Different Than What You Expected, Was it? Three Hours After Injection of Restylane® Into the Nasolabial Folds"

"Number of participants who answered the question If it was different than what you expected, was it? (More pain, Less pain or No response) three hours after injection of Restylane® into the nasolabial folds" (NCT00716443)
Timeframe: three hours after injection of Restylane® into the nasolabial folds

,
Interventionparticipants (Number)
More painLess painNo response
Compounded Topical Anesthetic Ointment91428
Pliaglis® Cream101427

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"Number of Participants Who Answered the Question If You Experienced Pain, Was it What You Expected From the Injection Procedure? Three Hours After Injection of Restylane® Into the Nasolabial Folds"

"Number of participants who answered No, Yes, Had no expectations or No response to the question If you experienced pain, was it what you expected from the injection procedure? three hours after injection of Restylane® into the nasolabial folds" (NCT00716443)
Timeframe: three hours after injection of Restylane® into the nasolabial folds

,
Interventionparticipants (Number)
NoYesHad no expectationsNo response
Compounded Topical Anesthetic Ointment829131
Pliaglis® Cream1027122

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"Number of Participants Who Answered the Question Still Speaking to the Topical Anesthetic You Had on the Right/Left Side of Your Face, Would You Recommend it to Your Friend or Family Member? 3 Hours After Injection of Restylane® Into Nasolabial Folds"

"Number of participants who answered No, Yes or No response to the question Still speaking to the topical anesthetic you had on the right/left side of your face, would you recommend it to your friend or family member? three hours after injection of Restylane® into the nasolabial folds" (NCT00716443)
Timeframe: three hours after injection of Restylane® into the nasolabial folds

,
Interventionparticipants (Number)
NoYesNo response
Compounded Topical Anesthetic Ointment12390
Pliaglis® Cream13380

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"Number of Participants Who Answered the Question What Level of Pain Did You Experience When You Were Injected? Three Hours After Injection of Restylane® Into the Nasolabial Folds"

"Number of participants who answered according to a scale of None, Minimal, Mild, Moderate, Severe, or No response to the question What level of pain did you experience when you were injected? three hours after injection of Restylane® into the nasolabial folds" (NCT00716443)
Timeframe: three hours after injection of Restylane® into the nasolabial folds

,
Interventionparticipants (Number)
NoneMinimalMildModerateSevereNo response
Compounded Topical Anesthetic Ointment22415910
Pliaglis® Cream42315810

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"Number of Participants With Yes/no Answers to Question to Investigator Did the Topical Anesthetics Provide Adequate Anesthesia for the Injections of Restylane® Into the Nasolabial Folds Procedure? Day of Injection of Restylane® Into Nasolabial Folds"

"Number of participants with yes or no answers to question asked to investigator on the day of injection of Restylane® into the nasolabial folds Did the topical anesthetics provided adequate anesthesia for the injections of Restylane® into the nasolabial folds procedure?" (NCT00716443)
Timeframe: Day of injection of Restylane® into the nasolabial folds

,
Interventionparticipants (Number)
YesNo
Compounded Topical Anesthetic Ointment447
Pliaglis® Cream447

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Number of Participants in Each Category of the Blinded Evaluator's Evaluation of Subject's Pain Scale Immediately After Injection of Restylane® Into the Nasolabial Folds

Number of participants in each category of the Blinded Evaluator's Evaluation of Subject's Pain scale (0 = No pain; 1 = Slight pain; 2 = Moderate pain; 3 = Severe pain) immediately after injection of Restylane® into the nasolabial folds (NCT00716443)
Timeframe: immediately after injection of Restylane® into the nasolabial folds

,
Interventionparticipants (Number)
No painSlight painModerate painSevere pain
Compounded Topical Anesthetic Ointment281841
Pliaglis® Cream351150

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Number of Participants in Each Category of the Blinded Evaluator's Evaluation of Subject's Pain Scale One Hour After Injection of Restylane® Into the Nasolabial Folds

Number of participants in each category of the Blinded Evaluator's Evaluation of Subject's Pain scale (0 = No pain; 1 = Slight pain; 2 = Moderate pain; 3 = Severe pain) one hour after an injection of Restylane® into the nasolabial folds (NCT00716443)
Timeframe: one hour after injection of Restylane® into the nasolabial folds

,
Interventionparticipants (Number)
No painSlight painModerate painSevere pain
Compounded Topical Anesthetic Ointment49200
Pliaglis® Cream49200

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Number of Participants in Each Category of the Blinded Evaluator's Evaluation of Subject's Pain Scale Upon First Needle Stick of Injection of Restylane® Into the Nasolabial Folds

Number of participants in each category of the Blinded Evaluator's Evaluation of Subject's Pain scale (0 = No pain; 1 = Slight pain; 2 = Moderate pain; 3 = Severe pain) upon first needle stick of an injection of Restylane® into the nasolabial folds (NCT00716443)
Timeframe: upon first needle stick of injection of Restylane® into the nasolabial folds

,
Interventionparticipants (Number)
No painMild painModerate painSevere pain
Compounded Topical Anesthetic Ointment929130
Pliaglis® Cream143160

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Number of Participants in Each Category of the Investigator Evaluation of the Subject's Post Procedure Pain Assessment Scale Immediately After Injection of Restylane® Into the Nasolabial Folds

Number of participants in each category of the Investigator Evaluation of the Subject's Post Procedure Pain Assessment scale (0 = No pain; 1 = Slight pain; 2 = Moderate pain; 3 = Severe pain) immediately after injection of Restylane® into the nasolabial folds immediately after injection of Restylane® into the nasolabial folds (NCT00716443)
Timeframe: immediately after injection of Restylane® into the nasolabial folds

,
Interventionparticipants (Number)
No painSlight painModerate painSevere pain
Compounded Topical Anesthetic Ointment291570
Pliaglis® Cream351060

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Number of Participants in Each Category of the Investigator Evaluation of the Subject's Post Procedure Pain Assessment Scale Upon First Needle Stick of Injection of Restylane® Into the Nasolabial Folds

Number of participants in each category of the Investigator Evaluation of the Subject's Post Procedure Pain Assessment scale (0 = No pain; 1 = Slight pain; 2 = Moderate pain; 3 = Severe pain) upon first needle stick of an injection of Restylane® into the nasolabial folds (NCT00716443)
Timeframe: Upon first needle stick of injection of Restylane® into the nasolabial folds

,
Interventionparticipants (Number)
No painSlight painModerate painSevere pain
Compounded Topical Anesthetic Ointment1325121
Pliaglis® Cream172860

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Number of Participants in Each Category of the Investigator's Evaluation of Subject's Pain Scale One Hour After Injection of Restylane® Into the Nasolabial Folds

Number of participants in each category of the Investigator's Evaluation of Subject's Pain scale (0 = No pain; 1 = Slight pain; 2 = Moderate pain; 3 = Severe pain) one hour after injection of Restylane® into the nasolabial folds (NCT00716443)
Timeframe: one hour after injection of Restylane® into the nasolabial folds

,
Interventionparticipants (Number)
No painSlight painModerate painSevere pain
Compounded Topical Anesthetic Ointment49200
Pliaglis® Cream49200

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Subject's Pain Evaluation by Visual Analog Scale (VAS)Upon First Needlestick, Immediately After Injection, One Hour After Injection and Three Hours After Injection of Restylane® Into the Nasolabial Folds

Subject's pain as evaluated using a VAS scale from 0 - 10 cm (centimeters) with 0 cm being no pain and 10 cm being the worst pain imaginable upon first needlestick, immediately after injection, one hour after injection and three hours after injection of Restylane® into the nasolabial folds (NCT00716443)
Timeframe: upon first needlestick, immediately after injection, one hour after injection and three hours after injection of Restylane® into the nasolabial folds

,
Interventioncentimeters (Mean)
upon first needle stickimmediately after injectionone hour after injectionthree hours after injection
Compounded Topical Anesthetic Ointment2.82.80.60.5
Pliaglis® Cream2.32.70.80.5

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Number of Participants in Each Category of the Blinded Evaluator's Evaluation of Subject's Pain Scale Three Hours After Injection of Restylane® Into the Nasolabial Folds

Number of participants in each category of the Blinded Evaluator's Evaluation of Subject's Pain scale (0 = No pain; 1 = Slight pain; 2 = Moderate pain; 3 = Severe pain) three hours after injection of Restylane® into the nasolabial folds (NCT00716443)
Timeframe: three hours after injection of Restylane® into the nasolabial folds

,
Interventionparticipants (Number)
No painMild painModerate painSevere pain
Compounded Topical Anesthetic Ointment50100
Pliaglis® Cream50100

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Number of Participants in Each Category of the Investigator's Evaluation of Subject's Pain Scale Three Hours After Injection of Restylane® Into the Nasolabial Folds

Number of participants in each category of the Investigator's Evaluation of Subject's Pain scale (0 = No pain; 1 = Slight pain; 2 = Moderate pain; 3 = Severe pain) three hours after injection of Restylane® into the nasolabial folds (NCT00716443)
Timeframe: three hours after injection of Restylane® into the nasolabial folds

,
Interventionparticipants (Number)
No painMild painModerate painSevere pain
Compounded Topical Anesthetic Ointment49200
Pliaglis® Cream50100

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Number of Participants With Tolerability Assessments Resulting in Adverse Events From Baseline to Two Days After Injection of Restylane® Into the Nasolabial Folds

Number of participants w/ tolerability assessments (erythema, edema, blanching) resulting in adverse events from Baseline to two days after injection of Restylane® into the nasolabial folds (NCT00716443)
Timeframe: Baseline to two days after injection of Restylane® into the nasolabial folds

Interventionparticipants (Number)
Pliaglis® Cream0
Compounded Topical Anesthetic Ointment0

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Discomfort From Anesthesia Used Prior to Intravitreal Injections

Discomfort from Anesthesia used prior to Intravitreal Injections using a Subjective Analog Pain Scale (0-10); no pain (0) and severe pain (10). (NCT00769392)
Timeframe: 16 weeks

Interventionunits on a scale (Mean)
Lidocaine 4%Lidocaine 2% Injectable SolutionProparacaine OphthalmicTetracaine Ophthalmic
All Participants1.41.60.71.0

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Discomfort Associated With the Intravitreal Injection

Discomfort Associated With the Intravitreal Injection using a Subjective Analog Pain Scale (0-10); no pain (0) and severe pain (10) (NCT00769392)
Timeframe: 16 weeks

Interventionunits on a scale (Mean)
Lidocaine 4%Lidocaine 2% Injectable SolutionProparacaine OphthalmicTetracaine Ophthalmic
All Participants32.32.83.1

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Visual Analogue Scale(0-100mm) by the Subject.

visual analogue scale (VAS) was used to evaluate the post-intubation sore throat. The VAS was a well-recongnized standard tool for rating of pain. The VAS measures exactly 100 mm. 0 means no pain and 100 means the worst pain that one can image. Patient marks a point on the line that matches the amount of pain he or she feels. (NCT00798018)
Timeframe: 6 hours, 12 hours, 24 hours, 48 hours after extubation

,,,
Interventionmm (Mean)
6h12h24h48h
Air Alone51504345
Lidocaine22252023
Normal Saline40384143
Tetracaine91379

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Change in Ln(Bacterial Colony Count) From Pre-antibiotic Administration to Post Study Medication Swabs

Within 3 hours from time of culture acquisition, the samples will be vortexed for 30 seconds and 100µl aliquots will be plated onto 5% sheep blood and chocolate agar plates. These plates will be incubated with 5% carbon dioxide at 35˚ C for 72 hours. After 72 hours all plates will be read for colony count and identification of all isolates will be performed using routine microbiological methods. The natural log of bacterial bacterial colony count will be used for the outcome measure. (NCT00827073)
Timeframe: (1) Pre-antibiotics swab, and (2) Post-study medication (pre surgery)

InterventionLn(bacterial colony count) (Mean)
Tetracaine 0.5% Drop-0.14
Lidocaine 2% Jelly-0.52

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Number of Bacterial Species in Pre-antibiotic Administration and in Post Study Medication Swabs

(NCT00827073)
Timeframe: (1) Pre-antibiotics swab and (2) Post-study medication (pre surgery)

,
Interventionbacterial spceies (Mean)
pre number of bacterial spicespost surgery number of bacterial speices
Lidocaine 2% Jelly11
Tetracaine 0.5% Drop11

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Spinal Analgesic Duration

duration of time in minutes from the time the combined spinal epidural is placed until the participant requests additional analgesia; at that time the epidural was dosed and study participation was complete (NCT01005459)
Timeframe: 1-2 hrs

Interventionminutes (Mean)
Tetracaine 2mg92.68
Bupivacaine 2 mg89.61

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Maximum Change in Pulse From Baseline

Maximum change from Baseline at any time point. (NCT01302483)
Timeframe: Baseline, 15, 20, 30, 40, 50, 60, 120 minutes

Interventionbeats per minute (Mean)
Kovacaine Nasal Spray-11.13
Lidocaine Injection-6.60

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Pulpal Anesthesia

Number of participants who did not need rescue anesthesia to complete the study dental procedure, i.e. Kovacaine provided enough pulpal anesthesia to complete a dental procedure. (NCT01302483)
Timeframe: Continuous throughout dental treatment period (up to 60 minutes)

Interventionparticipants (Number)
Kovacaine Nasal Spray25
Lidocaine Injection14

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Maximum Change in Blood Pressure From Baseline

Maximum change from Baseline at any time point. (NCT01302483)
Timeframe: Baseline, 15, 20, 30, 40 50, 60, 120 minutes

,
InterventionmmHG (Mean)
Systolic blood pressureDiastolic blood pressure
Kovacaine Nasal Spray4.50-2.67
Lidocaine Injection3.43-5.07

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Soft Tissue Anesthesia Duration

"Assessment of pain using a Rotadent sensor probe, applying up to 20 grams/cm^2 at the tissue site. At each time point, participants were asked if they felt pain from the sensor probe at each site location in the mouth. The four sites were:~Site 1: Distal to the apex of the tooth in the position of the maxillary first premolar at the deepest point in the buccal vestibule~Site 2: Apical to the maxillary lateral incisor at the deepest point in the labial vestibule~Site 3: Incisive papilla~Site 4: At the confluence of the alveolar process and hard palate medial to the maxillary second premolar (near the greater palatine foramen)" (NCT01302483)
Timeframe: Baseline, 15, 20, 30, 40, 50, 60, 80, 100, 120 minutes

,
InterventionMinutes (Mean)
Site 1 DurationSite 2 DurationSite 3 DurationSite 4 Duration
Kovacaine Nasal Spray21.116.131.831.4
Lidocaine Injection34.232.125.029.3

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Maximum Change in Pulse Oximetry From Baseline

Maximum change from Baseline at any time point (NCT01302483)
Timeframe: Baseline, 15, 20, 30, 40, 50, 60, 120 minutes

InterventionSpO2 (Mean)
Kovacaine Nasal Spray0.17
Lidocaine Injection-0.80

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Cmax of PBBA

Extra-vascular, non-compartmental analysis is used to derive pharmacokinetic parameters; estimated from observed plasma concentration values, the dose administered, the AUCs, and the terminal elimination phase rate constant for each dose group (NCT01304316)
Timeframe: Baseline, 5, 10, 15, 20, 25, 30, 40, 50, 60, 70, 80, 90, 100, 110, 120 minutes

Interventionng/mL (Mean)
Standard DoseHigh Dose
Kovacaine Nasal Spray492886

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Cmax of Tetracaine

Extra-vascular, non-compartmental analysis is used to derive pharmacokinetic parameters; estimated from observed plasma concentration values, the dose administered, the AUCs, and the terminal elimination phase rate constant for each dose group (NCT01304316)
Timeframe: Baseline, 5, 10, 15, 20, 25, 30, 40, 50, 60, 70, 80, 90, 100, 110, 120 minutes

Interventionng/mL (Mean)
18 mg36 mg
Kovacaine Nasal Spray0.2431.15

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Diastolic BP Maximum Change From Baseline

(NCT01304316)
Timeframe: Baseline, 5, 10, 15, 20, 25, 30, 40, 50, 60, 70, 80, 90, 100, 110, 120 minutes

InterventionmmHg (Mean)
Standard K305 DoseHigh K305 Dose
Kovacaine Nasal Spray10.811.7

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Half Life of Oxymetazoline

Extra-vascular, non-compartmental analysis is used to derive pharmacokinetic parameters; estimated from observed plasma concentration values, the dose administered, the AUCs, and the terminal elimination phase rate constant for each dose group (NCT01304316)
Timeframe: Baseline, 5, 10, 15, 20, 25, 30, 40, 50, 60, 70, 80, 90, 100, 110, 120 minutes

Interventionh (Mean)
0.3 mg0.6 mg
Kovacaine Nasal Spray2.321.72

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Pulse Oximetry Maximum Change From Baseline

(NCT01304316)
Timeframe: Baseline, 5, 10, 15, 20, 25, 30, 40, 50, 60, 70, 80, 90, 100, 110, 120 minutes

Intervention% oxygen (Mean)
Standard K305 DoseHigh K305 Dose
Kovacaine Nasal Spray0.90.3

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Pulse Rate Maximum Change From Baseline

(NCT01304316)
Timeframe: Baseline, 5, 10, 15, 20, 25, 30, 40, 50, 60, 70, 80, 90, 100, 110, 120 minutes

Interventionbpm (Mean)
Standard K305 DoseHigh K305 Dose
Kovacaine Nasal Spray5.28.5

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Systolic BP Maximum Change From Baseline

(NCT01304316)
Timeframe: Baseline, 5, 10, 15, 20, 25, 30, 40, 50, 60, 70, 80, 90, 100, 110, 120 minutes

InterventionmmHg (Mean)
Standard K305 DoseHigh K305 Dose
Kovacaine Nasal Spray10.714.7

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Half Life of PBBA

Extra-vascular, non-compartmental analysis is used to derive pharmacokinetic parameters; estimated from observed plasma concentration values, the dose administered, the AUCs, and the terminal elimination phase rate constant for each dose group (NCT01304316)
Timeframe: Baseline, 5, 10, 15, 20, 25, 30, 40, 50, 60, 70, 80, 90, 100, 110, 120 minutes

Interventionh (Mean)
Standard doseHigh dose
Kovacaine Nasal Spray1.001.01

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Cmax of Oxymetazoline

Extra-vascular, non-compartmental analysis is used to derive pharmacokinetic parameters; estimated from observed plasma concentration values, the dose administered, the AUCs, and the terminal elimination phase rate constant for each dose group (NCT01304316)
Timeframe: Baseline, 5, 10, 15, 20, 25, 30, 40, 50, 60, 70, 80, 90, 100, 110, 120 minutes

Interventionng/mL (Mean)
0.3 mg0.6 mg
Kovacaine Nasal Spray1.452.05

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Participants Score on Pain Scale

Do you have sharp pain in your eye? Pain will be assessed by units on a scale of 1-5: 1 means no symptoms, 2 means slight discomfort, 3 means mild discomfort, 4 means moderate discomfort, and 5 means severe discomfort (NCT01383200)
Timeframe: 1 hour (60minutes) post LASIK operation

InterventionScore on scale (Mean)
Tetracaine1.95
Lidocaine2.01

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The Proportion of Subjects Receiving Kovacaine Mist Who do Not Require Rescue Anesthesia During the Operative Dental Procedure

(NCT01479517)
Timeframe: at 15 minutes, with +10 minute window

Interventionparticipants (Number)
Kovacaine Mist 0.1 mL x 4 Sprays10
Kovacaine Mist 0.2 mL x 2 Sprays7
Kovacaine Mist, 0.2 mL x 1 Spray8

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Naris Examination

Number of patients with an abnormal naris examination finding. (NCT01479517)
Timeframe: 60 minutes post drug administration

InterventionParticipants (Count of Participants)
Kovacaine Mist 0.1 mL x 4 Sprays0
Kovacaine Mist 0.2 mL x 2 Sprays0
Kovacaine Mist, 0.2 mL x 1 Spray0

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The Incidence of Subjects Receiving Kovacaine Mist With Changes in Systolic and Diastolic Blood Pressure Exceeding +/- 25% of Preoperative Measurements Values.

(NCT01479517)
Timeframe: 60 minutes

,,
Interventionparticipants (Number)
Increased systolic BP >25%Decreased systolic BP >25%Increased diastolic BP >25%Decreased diastolic BP >25%
Kovacaine Mist 0.1 mL x 4 Sprays0000
Kovacaine Mist 0.2 mL x 2 Sprays1000
Kovacaine Mist, 0.2 mL x 1 Spray1000

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The Proportion of Subjects Giving a Positive Response to Evaluation Question for Subjective Numbness Assessment (SNA) After the Procedure is Completed.

(NCT01479517)
Timeframe: 60 minutes

,,
Interventionparticipants (Number)
Lip numbSide of nose numbLower eyelid numbCheek numbAbnormal sensation tapping front teethAbnormal sensation in roof of mouth
Kovacaine Mist 0.1 mL x 4 Sprays69361010
Kovacaine Mist 0.2 mL x 2 Sprays550286
Kovacaine Mist, 0.2 mL x 1 Spray350157

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Duration of Anesthesia(Minutes)

Onset and end of anesthesia are evaluated by Pinprick tests. Duration of anesthesia is calculated as: difference between onset and end of anesthesia (minutes). (NCT01545765)
Timeframe: From T0 (product removal) up to T8 hours after product removal

InterventionMinutes (Median)
Lidocaine 7% + Tetracaine 7% Face - First Application Time80
Lidocaine 7% + Tetracaine 7% Face - Second Application Time140
Lidocaine 7% + Tetracaine 7% Thigh - First Application Time0
Lidocaine 7% + Tetracaine 7% Thigh - Second Application Time400

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Adverse Events

Incidence of adverse events was to be reported during the study period (NCT01545765)
Timeframe: During the study

Interventionparticipants (Number)
Lidocaine 7% + Tetracaine 7% Face - First Application Time2
Lidocaine 7% + Tetracaine 7% Face - Second Application Time2
Lidocaine 7% + Tetracaine 7% Thigh - First Application Time2
Lidocaine 7% + Tetracaine 7% Thigh - Second Application Time2

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Index Knee Pain Scores on a Numeric Rating Scale (NRS)

Subject rated index knee pain 5 minutes after stopped experimental exercise (with intervention). Index knee pain was reported using the Numeric Rating Scale, a scale from 0 to 10 where 0 = no pain and 10 = the worst pain possible. (NCT01654302)
Timeframe: 5 minutes after stopped exercise, performed 1 hour after intervention (patch application)

Interventionunits on a scale (Mean)
Synera4.167
Inactive Patch4.703

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Absolute Maximum Change From Baseline in Heart Rate

(NCT01660893)
Timeframe: from baseline to 120 minutes following drug administration

Interventionbpm (Mean)
Kovacaine Mist, 3 Sprays Unilateral3.4
Tetracaine Only, 3 Sprays Unilateral3.5
Placebo, 3 Sprays Unilateral2.3

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Number of Participants With a Decrease From Baseline in Diastolic Blood Pressure Greater Than or Equal to 15 mm Hg and to a Value Lower Than 90 mm Hg

(NCT01660893)
Timeframe: at any time within 120 minutes following drug administration

InterventionParticipants (Count of Participants)
Kovacaine Mist, 3 Sprays Unilateral0
Tetracaine Only, 3 Sprays Unilateral0
Placebo, 3 Sprays Unilateral0

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Number of Participants With a Decrease From Baseline in Systolic Blood Pressure Greater Than or Equal to 15 mm Hg and to a Value Lower Than 90 mm Hg

(NCT01660893)
Timeframe: at any time within 120 minutes following drug administration

InterventionParticipants (Count of Participants)
Kovacaine Mist, 3 Sprays Unilateral0
Tetracaine Only, 3 Sprays Unilateral0
Placebo, 3 Sprays Unilateral0

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Number of Participants With an Increase From Baseline in Diastolic Blood Pressure Greater Than or Equal to 15 mm Hg and to a Value Higher Than 90 mm Hg

(NCT01660893)
Timeframe: at any time within 120 minutes following drug administration

InterventionParticipants (Count of Participants)
Kovacaine Mist, 3 Sprays Unilateral0
Tetracaine Only, 3 Sprays Unilateral0
Placebo, 3 Sprays Unilateral0

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Number of Participants With an Increase From Baseline in Systolic Blood Pressure Greater Than or Equal to 25 mm Hg and to a Value Higher Than 160 mm Hg

(NCT01660893)
Timeframe: at any time within 120 minutes following drug administration

InterventionParticipants (Count of Participants)
Kovacaine Mist, 3 Sprays Unilateral0
Tetracaine Only, 3 Sprays Unilateral0
Placebo, 3 Sprays Unilateral0

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Alcohol Sniff Test

The change from screening in the the distance from the nose (in centimeters) that a patient is able to detect the smell of an alcohol swab. (NCT01660893)
Timeframe: administered at approximately 24 hours after drug administration

Interventioncm (Mean)
Kovacaine Mist, 3 Sprays Unilateral0.4
Tetracaine Only, 3 Sprays Unilateral0.8
Placebo, 3 Sprays Unilateral2.1

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Absolute Maximum Change From Baseline in Systolic Blood Pressure and Diastolic Blood Pressure

(NCT01660893)
Timeframe: from baseline to 120 minutes following drug administration

,,
InterventionmmHg (Mean)
Systolic Blood PressureDiastolic Blood Pressure
Kovacaine Mist, 3 Sprays Unilateral12.811.2
Placebo, 3 Sprays Unilateral1.26.2
Tetracaine Only, 3 Sprays Unilateral3.54.5

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Number of Participants With Heart Rate Lower Than 50 Bpm

(NCT01660893)
Timeframe: at any time within 120 minutes following drug administration

InterventionParticipants (Count of Participants)
Kovacaine Mist, 3 Sprays Unilateral0
Tetracaine Only, 3 Sprays Unilateral0
Placebo, 3 Sprays Unilateral0

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The Profile Over Time of Systolic Blood Pressure

(NCT01660893)
Timeframe: from baseline to 120 minutes following drug administration

,,
InterventionmmHg (Mean)
Pre-Study10 Minutes30 Minutes45 Minutes60 Minutes90 Minutes120 Minutes
Kovacaine Mist, 3 Sprays Unilateral113.0116.5123.0118.5116.1117.7119.5
Placebo, 3 Sprays Unilateral125.5118.8NA118.8121.7119.7119.2
Tetracaine Only, 3 Sprays Unilateral116.1114.2110.0113.6113.3112.0113.7

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The Profile Over Time of Heart Rate

(NCT01660893)
Timeframe: from baseline to 120 minutes following drug administration

,,
Interventionbpm (Mean)
Pre-Study10 Minutes30 Minutes45 Minutes60 Minutes90 Minutes120 Minutes
Kovacaine Mist, 3 Sprays Unilateral76.969.664.669.667.367.168.4
Placebo, 3 Sprays Unilateral81.075.8NA73.870.272.070.8
Tetracaine Only, 3 Sprays Unilateral69.167.164.564.365.364.365.0

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The Profile Over Time of Diastolic Blood Pressure

(NCT01660893)
Timeframe: from baseline to 120 minutes following drug administration

,,
InterventionmmHg (Mean)
Pre-Study10 Minutes30 Minutes45 Minutes60 Minutes90 Minutes120 Minutes
Kovacaine Mist, 3 Sprays Unilateral74.177.981.076.476.180.579.1
Placebo, 3 Sprays Unilateral77.775.5NA74.277.878.877.7
Tetracaine Only, 3 Sprays Unilateral73.073.870.072.275.973.172.1

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Intraoral Soft-tissue Anesthesia (Yes/no)

Number of patients who reported no pain when incisive papilla and greater palatine foramen soft-tissue was tested with a probe (NCT01660893)
Timeframe: at 15 minutes with a 3 minute window

,,
InterventionParticipants (Count of Participants)
Incisive PapillaGreater Palatine Foramen
Kovacaine Mist, 3 Sprays Unilateral72
Placebo, 3 Sprays Unilateral21
Tetracaine Only, 3 Sprays Unilateral51

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Completion of the Study Dental Procedure Without Need for Rescue by Injection of Local Anesthetic (Yes/no).

(NCT01660893)
Timeframe: at 15 minutes with a 3 minute window

,,
InterventionParticipants (Count of Participants)
SuccessFailure
Kovacaine Mist, 3 Sprays Unilateral55
Placebo, 3 Sprays Unilateral06
Tetracaine Only, 3 Sprays Unilateral28

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Number of Participants With Heart Rate Higher Than 125 Bpm

(NCT01660893)
Timeframe: at any time within 120 minutes following drug administration

InterventionParticipants (Count of Participants)
Kovacaine Mist, 3 Sprays Unilateral0
Tetracaine Only, 3 Sprays Unilateral0
Placebo, 3 Sprays Unilateral0

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Incidence of Adverse Events by Dose Level Regardless of Age

(NCT01701505)
Timeframe: from baseline to 24 hours following drug administration

InterventionParticipants (Count of Participants)
Kovacaine Mist High Dose8
Kovacaine Mist Mid Dose12
Kovacaine Mist Low Dose20

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Number of Participants Who Completed the Study Dental Procedure Without Need for Rescue by Injection of Local Anesthetic.

If the participant does not have sufficient anesthesia to complete the Study Dental Procedure, the participant is given a rescue injection of local anesthetic and is considered a failure for this outcome. (NCT01701505)
Timeframe: at 14 minutes with a 3 minute window

InterventionParticipants (Count of Participants)
Cohort A: 12-17 Years Low Dose (120uL Kovacaine Mist)6
Cohort A: 12-17 Years Med Dose (200 uL Kovacaine Mist)7
Cohort A: 12-17 High Dose (400uL Kovacaine Mist)8
Cohort B: 7-11 Years Low Dose (120uL Kovacaine Mist)5
Cohort B: 7-11 Years Med Dose (200 uL Kovacaine Mist)7
Cohort C: 3-6 Years Low Dose (120uL Kovacaine Mist)4

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Diastolic Blood Pressure

(NCT01701505)
Timeframe: At Baseline, 12 minutes, and 120 minutes

,,,,,
InterventionmmHg (Mean)
Baseline12 mins120 mins
Cohort A: 12-17 High Dose (400uL Kovacaine Mist)62.166.170.1
Cohort A: 12-17 Years Low Dose (120uL Kovacaine Mist)64.663.964.3
Cohort A: 12-17 Years Med Dose (200 uL Kovacaine Mist)70.968.469.0
Cohort B: 7-11 Years Low Dose (120uL Kovacaine Mist)65.062.065.0
Cohort B: 7-11 Years Med Dose (200 uL Kovacaine Mist)63.864.661.6
Cohort C: 3-6 Years Low Dose (120uL Kovacaine Mist)61.060.466.1

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Heart Rate

(NCT01701505)
Timeframe: At Baseline, 12 minutes, and 120 minutes

,,,,,
Interventionbpm (Mean)
Baseline12 mins120 mins
Cohort A: 12-17 High Dose (400uL Kovacaine Mist)75.577.376.1
Cohort A: 12-17 Years Low Dose (120uL Kovacaine Mist)72.975.478.4
Cohort A: 12-17 Years Med Dose (200 uL Kovacaine Mist)83.680.984.3
Cohort B: 7-11 Years Low Dose (120uL Kovacaine Mist)90.391.691.9
Cohort B: 7-11 Years Med Dose (200 uL Kovacaine Mist)80.682.586.9
Cohort C: 3-6 Years Low Dose (120uL Kovacaine Mist)90.189.395.0

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Naris Examination (NE) to Assess Reactions to the Study Drug.

The principal investigator will perform a visual inspection to note number of participants at post-dose that have a ulceration, inflammation or minor bleeding. (NCT01701505)
Timeframe: At Baseline and 120 Minutes

,,,,,
InterventionParticipants (Count of Participants)
Post-dose ulceration (not present at baselinePost-dose inflammation (not present at baseliPost-dose minor bleeding (not present at baseline)
Cohort A: 12-17 High Dose (400uL Kovacaine Mist)000
Cohort A: 12-17 Years Low Dose (120uL Kovacaine Mist)001
Cohort A: 12-17 Years Med Dose (200 uL Kovacaine Mist)011
Cohort B: 7-11 Years Low Dose (120uL Kovacaine Mist)000
Cohort B: 7-11 Years Med Dose (200 uL Kovacaine Mist)000
Cohort C: 3-6 Years Low Dose (120uL Kovacaine Mist)000

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Systolic Blood Pressure

(NCT01701505)
Timeframe: At Baseline, 12 minutes, and 120 minutes

,,,,,
InterventionmmHg (Mean)
Baseline12 mins120 mins
Cohort A: 12-17 High Dose (400uL Kovacaine Mist)115.4121.0116.4
Cohort A: 12-17 Years Low Dose (120uL Kovacaine Mist)113.1119.1120.5
Cohort A: 12-17 Years Med Dose (200 uL Kovacaine Mist)122.5122.3120.1
Cohort B: 7-11 Years Low Dose (120uL Kovacaine Mist)111.3105.5106.3
Cohort B: 7-11 Years Med Dose (200 uL Kovacaine Mist)106.5109.9102.3
Cohort C: 3-6 Years Low Dose (120uL Kovacaine Mist)97.8101.9101.9

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Oxygen Saturation

(NCT01701505)
Timeframe: At Baseline, 12 minutes, and 120 minutes

,,,,,
Interventionpercent (Mean)
Baseline12 mins120 mins
Cohort A: 12-17 High Dose (400uL Kovacaine Mist)98.397.996.9
Cohort A: 12-17 Years Low Dose (120uL Kovacaine Mist)97.397.397.0
Cohort A: 12-17 Years Med Dose (200 uL Kovacaine Mist)98.898.397.4
Cohort B: 7-11 Years Low Dose (120uL Kovacaine Mist)97.397.496.0
Cohort B: 7-11 Years Med Dose (200 uL Kovacaine Mist)97.496.397.5
Cohort C: 3-6 Years Low Dose (120uL Kovacaine Mist)97.696.497.5

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Number of Participants With Adverse Events by Dose Level and Age

(NCT01701505)
Timeframe: from baseline to 24 hours following drug administration

InterventionParticipants (Count of Participants)
3-6 Years7-11 Years12-17 Years
Kovacaine Mist Low Dose866

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Number of Participants With Adverse Events by Dose Level and Age

(NCT01701505)
Timeframe: from baseline to 24 hours following drug administration

InterventionParticipants (Count of Participants)
7-11 Years12-17 Years
Kovacaine Mist Mid Dose75

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Number of Participants With Adverse Events by Dose Level and Age

(NCT01701505)
Timeframe: from baseline to 24 hours following drug administration

InterventionParticipants (Count of Participants)
12-17 Years
Kovacaine Mist High Dose8

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Absolute Maximum Change From Baseline in Diastolic Blood Pressure

(NCT01710787)
Timeframe: from baseline to 120 minutes following drug administration

InterventionmmHg (Mean)
Kovacaine Mist, 3 Sprays Unilateral10.5
Tetracaine Only, 3 Sprays Unilateral7.3
Placebo, 3 Sprays Unilateral6.7

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Absolute Maximum Change From Baseline in Heart Rate

(NCT01710787)
Timeframe: from baseline to 120 minutes following drug administration

Interventionbpm (Mean)
Kovacaine Mist, 3 Sprays Unilateral9.4
Tetracaine Only, 3 Sprays Unilateral10.5
Placebo, 3 Sprays Unilateral7.0

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Absolute Maximum Change From Baseline in Systolic Blood Pressure

(NCT01710787)
Timeframe: from baseline to 120 minutes following drug administration

Interventionmm Hg (Mean)
Kovacaine Mist, 3 Sprays Unilateral13.7
Tetracaine Only, 3 Sprays Unilateral10.8
Placebo, 3 Sprays Unilateral5.1

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Number of Participants Who Completed the Study Dental Procedure After Without Need for Rescue by Injection of Local Anesthetic.

If the participant does not have sufficient anesthesia to complete the Study Dental Procedure, the participant is given a rescue injection of local anesthetic and is considered a failure for this outcome. (NCT01710787)
Timeframe: at 15 minutes with a 3 minute window

Interventionpercentage of patients (Number)
Kovacaine Mist, 3 Sprays Unilateral84.1
Tetracaine Only, 3 Sprays Unilateral27.3
Placebo, 3 Sprays Unilateral27.3

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Number of Participants With a Decrease From Baseline in Diastolic Blood Pressure Greater Than or Equal to 10 mm Hg and to a Value Lower Than 50 mm Hg

(NCT01710787)
Timeframe: at any time within 120 minutes following drug administration

Interventionparticipants (Number)
Kovacaine Mist, 3 Sprays Unilateral1
Tetracaine Only, 3 Sprays Unilateral0
Placebo, 3 Sprays Unilateral0

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Number of Participants With a Decrease From Baseline in Systolic Blood Pressure Greater Than or Equal to 15 mm Hg and to a Value Lower Than 90 mm Hg

(NCT01710787)
Timeframe: at any time within 120 minutes following drug administration

InterventionParticipants (Count of Participants)
Kovacaine Mist, 3 Sprays Unilateral0
Tetracaine Only, 3 Sprays Unilateral0
Placebo, 3 Sprays Unilateral0

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Number of Participants With a Heart Rate Higher Than 125 Bpm

(NCT01710787)
Timeframe: at any time within 120 minutes following drug administration

InterventionParticipants (Count of Participants)
Kovacaine Mist, 3 Sprays Unilateral1
Tetracaine Only, 3 Sprays Unilateral0
Placebo, 3 Sprays Unilateral0

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Number of Participants With an Increase From Baseline in Diastolic Blood Pressure Greater Than or Equal to 15 mm Hg and to a Value Higher Than 105 mm Hg

(NCT01710787)
Timeframe: at any time within 120 minutes following drug administration

InterventionParticipants (Count of Participants)
Kovacaine Mist, 3 Sprays Unilateral1
Tetracaine Only, 3 Sprays Unilateral0
Placebo, 3 Sprays Unilateral0

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Number of Participants With an Increase From Baseline in Systolic Blood Pressure Greater Than or Equal to 25 mm Hg and to a Value Higher Than 160 mm Hg

(NCT01710787)
Timeframe: at any time within 120 minutes following drug administration

InterventionParticipants (Count of Participants)
Kovacaine Mist, 3 Sprays Unilateral2
Tetracaine Only, 3 Sprays Unilateral1
Placebo, 3 Sprays Unilateral0

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Alcohol Sniff Test

The distance from the nose (in centimeters) that a patient is able to detect the smell of alcohol on an alcohol swab. (NCT01710787)
Timeframe: administered at baseline, 120 minutes and approximately 24 hours after drug administration

,,
Interventioncm (Mean)
Pre-Study (Baseline)120 Minutes24 Hours
Kovacaine Mist, 3 Sprays Unilateral19.21818.2
Placebo, 3 Sprays Unilateral21.220.920.4
Tetracaine Only, 3 Sprays Unilateral18.817.716.1

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Intraoral Soft-tissue Anesthesia (Yes/no)

Number of patients who reported no pain when incisive papilla soft-tissue was tested with a probe at designated timepoints (NCT01710787)
Timeframe: at Baseline, 15, 30, 45, 60, 90, and 120 minutes with a 3 minute window

,,
InterventionParticipants (Count of Participants)
Baseline15 mins30 mins45 mins60 mins90 mins120 mins
Kovacaine Mist, 3 Sprays Unilateral019172117105
Placebo, 3 Sprays Unilateral0003100
Tetracaine Only, 3 Sprays Unilateral0835210

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The Profile Over Time of Systolic Blood Pressure

(NCT01710787)
Timeframe: from baseline to 120 minutes following drug administration

,,
InterventionmmHg (Mean)
Pre-Study (Baseline)10 mins30 mins45 mins60 mins90 mins120 mins
Kovacaine Mist, 3 Sprays Unilateral121.3125.0123.5121.7123.1124.3125.0
Placebo, 3 Sprays Unilateral118.5121.5130.5118.7117.5116.6115.7
Tetracaine Only, 3 Sprays Unilateral118.6122.0122.2125.1121.7122.1121.1

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The Profile Over Time of Heart Rate

(NCT01710787)
Timeframe: from baseline to 120 minutes following drug administration

,,
Interventionbeats per minute (Mean)
Pre-Study (Baseline)10 mins30 mins45 mins60 mins90 mins120 mins
Kovacaine Mist, 3 Sprays Unilateral76.575.369.872.871.373.171.4
Placebo, 3 Sprays Unilateral74.876.376.073.173.072.173.7
Tetracaine Only, 3 Sprays Unilateral75.17682.674.173.272.073.8

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The Profile Over Time of Diastolic Blood Pressure

(NCT01710787)
Timeframe: from baseline to 120 minutes following drug administration

,,
InterventionmmHg (Mean)
Pre-Study (Baseline)10 mins30 mins45 mins60 mins90 mins120 mins
Kovacaine Mist, 3 Sprays Unilateral75.079.681.777.179.079.377.8
Placebo, 3 Sprays Unilateral74.877.384.575.476.674.175.7
Tetracaine Only, 3 Sprays Unilateral75.377.779.678.776.875.776.9

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Number of Participants With a Heart Rate Lower Than 50 Bpm

(NCT01710787)
Timeframe: at any time within 120 minutes following drug administration

InterventionParticipants (Count of Participants)
Kovacaine Mist, 3 Sprays Unilateral1
Tetracaine Only, 3 Sprays Unilateral2
Placebo, 3 Sprays Unilateral0

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Intraoral Soft-tissue Anesthesia (Onset and Duration)

Mean onset and duration of incisive papilla anesthesia based on number of patients who reported no pain when soft-tissue was tested with a probe at designated timepoints (NCT01710787)
Timeframe: up to 120 mins post-dose

,,
Interventionminutes (Mean)
OnsetDuration
Kovacaine Mist, 3 Sprays Unilateral9.779.2
Placebo, 3 Sprays Unilateral37.026.0
Tetracaine Only, 3 Sprays Unilateral19.532.1

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Global Assessment of Satisfaction With Venipuncture

Rates of Satisfied and very satisfied are used to be compared between two groups. (NCT01744197)
Timeframe: 30 minutes after the venipuncture.

Interventionpercentage of participants (Number)
Synera74.0
Placebo53.7

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Percentage of Patients With No Pain (VAS=0)

The primary efficacy endpoint is the subject's report of pain intensity regarding the venipuncture using a 0-10 VAS. The VAS =0 is considered as patients with no pain and would also be compared between 2 groups. (NCT01744197)
Timeframe: 30 minutes after the venipuncture.

Interventionpercentage of participants (Number)
Synera19.4
Placebo8.3

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Percentage of Patients With No or Minor Pain (VAS<3)

The primary efficacy endpoint is the subject's report of pain intensity regarding the venipuncture using a 0-10 VAS. The VAS <3 is considered as patients with no or minor pain and would be compared between 2 groups. (NCT01744197)
Timeframe: 30 minutes after the venipuncture.

Interventionpercentage of participants (Number)
Synera38.0
Placebo21.3

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Number of Participants Who Completed the Study Dental Procedure Without Need for Rescue by Injection of Local Anesthetic.

If the participant does not have sufficient anesthesia to complete the Study Dental Procedure, the participant is given a rescue injection of local anesthetic and is considered a failure for this outcome. (NCT01745380)
Timeframe: at 15 minutes, +3 minute window

Interventionparticipants (Number)
Kovacaine Mist88
Placebo14

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Maximum Change From Baseline in Systolic Blood Pressure

(NCT01745380)
Timeframe: from baseline to 120 minutes following drug administration

InterventionmmHg (Mean)
Kovacaine Mist13.8
Placebo9.2

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Maximum Change From Baseline in Heart Rate

(NCT01745380)
Timeframe: from baseline to 120 minutes following drug administration

Interventionbpm (Mean)
Kovacaine Mist5.3
Placebo5.1

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Maximum Change From Baseline in Diastolic Blood Pressure

(NCT01745380)
Timeframe: from baseline to 120 minutes following drug administration

InterventionmmHg (Mean)
Kovacaine Mist11.1
Placebo6.4

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Alcohol Sniff Test

The change from screening in the the distance from the nose (in centimeters) that a patient is able to detect the smell of alcohol on a cotton ball. (NCT01745380)
Timeframe: administered at approximately 24 hours after drug administration

Interventioncm (Mean)
Kovacaine Mist-0.8
Placebo1.3

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The Profile Over Time of Diastolic Blood Pressure

(NCT01745380)
Timeframe: from baseline to 120 minutes following drug administration

,
InterventionmmHg (Mean)
pre-study10 mins30 mins45 mins60 mins90 mins120 mins
Kovacaine Mist73.578.574.476.476.677.879.3
Placebo74.775.267.074.776.775.475.4

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The Profile Over Time of Heart Rate

(NCT01745380)
Timeframe: from baseline to 120 minutes following drug administration

,
Interventionbeats per minute (Mean)
pre-study10 mins30 mins45 mins60 mins90 mins120 mins
Kovacaine Mist71.068.067.566.465.865.665.6
Placebo73.672.666.370.969.267.768.9

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The Profile Over Time of Systolic Blood Pressure

(NCT01745380)
Timeframe: from baseline to 120 minutes following drug administration

,
InterventionmmHg (Mean)
pre-study10 mins30 mins45 mins60 mins90 mins120 mins
Kovacaine Mist123.1128.6117.3125.0127.1128.8129.5
Placebo124.0125.4116.3124.8126.7126.1124.9

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Number of Participants With an Increase From Baseline in Systolic Blood Pressure Greater Than or Equal to 25 mm Hg and/or to a Value Higher Than 160 mm Hg

(NCT01745380)
Timeframe: at any time within 120 minutes following drug administration

Interventionparticipants (Number)
Kovacaine Mist5
Placebo2

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Number of Participants With a Heart Rate Lower Than 50 Bpm

(NCT01745380)
Timeframe: at any time within 120 minutes following drug administration

Interventionparticipants (Number)
Kovacaine Mist4
Placebo1

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Number of Participants With a Heart Rate Higher Than 125 Bpm

(NCT01745380)
Timeframe: at any time within 120 minutes following drug administration

Interventionparticipants (Number)
Kovacaine Mist0
Placebo0

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Number of Participants With a Decrease From Baseline in Systolic Blood Pressure Greater Than or Equal to 15 mm Hg and/or to a Value Lower Than 90 mm Hg

(NCT01745380)
Timeframe: at any time within 120 minutes following study drug administration

Interventionparticipants (Number)
Kovacaine Mist1
Placebo1

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Number of Participants With a Decrease From Baseline in Diastolic Blood Pressure Greater Than or Equal to 10 mm Hg and/or to a Value Lower Than 50 mm Hg

(NCT01745380)
Timeframe: at any time within 120 minutes following study drug administration

Interventionparticipants (Number)
Kovacaine Mist1
Placebo0

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Number of Participants With an Increase From Baseline in Diastolic Blood Pressure Greater Than or Equal to 15 mm Hg and/or to a Value Higher Than 105 mm Hg

(NCT01745380)
Timeframe: at any time within 120 minutes following study drug administration

Interventionparticipants (Number)
Kovacaine Mist1
Placebo1

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Number of Participants Who Received Three Sprays and Completed the Study Dental Procedure Without Need for Rescue by Injection of Local Anesthetic.

A participant will receive two sprays and Study Dental Procedure will begin. If the participant does not have sufficient anesthesia a third sprays will be given. If after the third spray, the participant does not have sufficient anesthesia to complete the Study Dental Procedure, the participant is given a rescue injection of local anesthetic. This outcome analyzes just the participants who received the third spray and whether or not they completed the Study Dental Procedure without need for rescue by injection of local anesthesia. (NCT01745380)
Timeframe: at 25 minutes, +3 minute window

Interventionparticipants (Number)
Kovacaine Mist16
Placebo0

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Number of Participants Who Completed the Study Dental Procedure Without Need for Rescue by Injection of Local Anesthetic by Age Group (≤50 and >50 Years)

If the participant does not have sufficient anesthesia to complete the Study Dental Procedure, the participant is given a rescue injection of local anesthetic and is considered a failure for this outcome. This outcome is broken down by age group, 1) less than 50 years of age and 2) 50 years of age and older. (NCT01745380)
Timeframe: at 15 minutes (+3 minute window) or 25 minutes (+3 minute window) if third intranasal spray is used

,
Interventionpercentage of participants (Number)
less or = to 50greater than 50
Kovacaine Mist8790.3
Placebo20.643.8

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Decrease in Pulse Rate > 20 Bpm on 2 Consecutive Measurements After Administration of Study Medication

(NCT01807624)
Timeframe: 0, 5, 10, 15, 20, 25, 30, 40, 50 minutes, and 1, 1.25, 1.5, 1.75, 2, 3, 4, 6, 8, 12, 16 and 24 hours after completion of the last nasal spray

Interventionparticipants (Number)
Kovacaine Nasal Spray2

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Decrease in SBP > 20 mmHg on 2 Consecutive Measurements After Administration of Study Medication

(NCT01807624)
Timeframe: 0, 5, 10, 15, 20, 25, 30, 40, 50 minutes, and 1, 1.25, 1.5, 1.75, 2, 3, 4, 6, 8, 12, 16 and 24 hours after completion of the last nasal spray

Interventionparticipants (Number)
Kovacaine Nasal Spray0

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Increase in DBP > 20 mmHg on 2 Consecutive Measurements After Administration of Study Medication

(NCT01807624)
Timeframe: 0, 5, 10, 15, 20, 25, 30, 40, 50 minutes, and 1, 1.25, 1.5, 1.75, 2, 3, 4, 6, 8, 12, 16 and 24 hours after completion of the last nasal spray

Interventionparticipants (Number)
Kovacaine Nasal Spray1

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Increase in Pulse Rate > 20 Bpm on 2 Consecutive Measurements After Administration of Study Medication

(NCT01807624)
Timeframe: 0, 5, 10, 15, 20, 25, 30, 40, 50 minutes, and 1, 1.25, 1.5, 1.75, 2, 3, 4, 6, 8, 12, 16 and 24 hours after completion of the last nasal spray

Interventionparticipants (Number)
Kovacaine Nasal Spray2

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Increase in SBP > 20 mmHg on 2 Consecutive Measurements After Administration of Study Medication

(NCT01807624)
Timeframe: 0, 5, 10, 15, 20, 25, 30, 40, 50 minutes, and 1, 1.25, 1.5, 1.75, 2, 3, 4, 6, 8, 12, 16 and 24 hours after completion of the last nasal spray

Interventionparticipants (Number)
Kovacaine Nasal Spray3

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SpO2 Decrease of > 5% on 2 Consecutive Measurements After Administration of Study Medication

(NCT01807624)
Timeframe: 0, 5, 10, 15, 20, 25, 30, 40, 50 minutes, and 1, 1.25, 1.5, 1.75, 2, 3, 4, 6, 8, 12, 16 and 24 hours after completion of the last nasal spray

Interventionparticipants (Number)
Kovacaine Nasal Spray0

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SpO2 Increase of > 5% on 2 Consecutive Measurements After Administration of Study Medication

(NCT01807624)
Timeframe: 0, 5, 10, 15, 20, 25, 30, 40, 50 minutes, and 1, 1.25, 1.5, 1.75, 2, 3, 4, 6, 8, 12, 16 and 24 hours after completion of the last nasal spray

Interventionparticipants (Number)
Kovacaine Nasal Spray0

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AUC0-t of Oxymetazoline and PBBA

(NCT01807624)
Timeframe: 0, 5, 10, 15, 20, 25, 30, 40, 50 minutes, and 1, 1.25, 1.5, 1.75, 2, 3, 4, 6, 8, 12, 16 and 24 hours after completion of the last nasal spray

Interventionng*h/mL (Mean)
OxymetazolinePBBA
Kovacaine Nasal Spray3.67960

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Cmax of Oxymetazoline and PBBA

(NCT01807624)
Timeframe: 0, 5, 10, 15, 20, 25, 30, 40, 50 minutes, and 1, 1.25, 1.5, 1.75, 2, 3, 4, 6, 8, 12, 16 and 24 hours after completion of the last nasal spray

Interventionng/mL (Mean)
OxymetazolinePBBA
Kovacaine Nasal Spray1.79465

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Half-life of Oxymetazoline and PBBA

(NCT01807624)
Timeframe: 0, 5, 10, 15, 20, 25, 30, 40, 50 minutes, and 1, 1.25, 1.5, 1.75, 2, 3, 4, 6, 8, 12, 16 and 24 hours after completion of the last nasal spray

Interventionminutes (Mean)
OxymetazolinePBBA
Kovacaine Nasal Spray5.232.6

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Tmax of Oxymetazoline and PBBA

(NCT01807624)
Timeframe: 0, 5, 10, 15, 20, 25, 30, 40, 50 minutes, and 1, 1.25, 1.5, 1.75, 2, 3, 4, 6, 8, 12, 16 and 24 hours after completion of the last nasal spray

Interventionminutes (Mean)
OxymetazolinePBBA
Kovacaine Nasal Spray5.822

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AUC0-infinity of Oxymetazoline and PBBA

(NCT01807624)
Timeframe: 0, 5, 10, 15, 20, 25, 30, 40, 50 minutes, and 1, 1.25, 1.5, 1.75, 2, 3, 4, 6, 8, 12, 16 and 24 hours after completion of the last nasal spray

Interventionng*h/mL (Mean)
OxymetazolinePBBA
Kovacaine Nasal Spray4.24973

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Decrease in DBP > 20 mmHg on 2 Consecutive Measurements After Administration of Study Medication

(NCT01807624)
Timeframe: 0, 5, 10, 15, 20, 25, 30, 40, 50 minutes, and 1, 1.25, 1.5, 1.75, 2, 3, 4, 6, 8, 12, 16 and 24 hours after completion of the last nasal spray

Interventionparticipants (Number)
Kovacaine Nasal Spray0

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Results of Naris Examination (NE) - Patency and Ulcerations

"The investigators evaluated the treatment naris for patency and ulcerations.~Patency was evaluated as followed: The nostril not used for dosing study drug was manually occluded and the subject was asked to sniff gently. Airflow in the naris was used to determine if it was patent (yes) or not (no).~For ulcers, the investigators performed a visual examination for the presence of ulcers and recorded if they were present (yes) or not (no)." (NCT01844830)
Timeframe: 120 minutes post drug administration

,
InterventionParticipants (Count of Participants)
Patency (yes)Ulcerations (yes)
Kovacaine Mist590
Placebo300

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Number of Participants Who Completed the Study Dental Procedure Without Need for Rescue by Injection of Local Anesthetic. by Age Group (3-5, 6-11, and 12-17 Years Old, Inclusive).

If the participant does not have sufficient anesthesia to complete the Study Dental Procedure, the participant is given a rescue injection of local anesthetic and is considered a failure for this outcome. (NCT01844830)
Timeframe: 100µL dose - at 10 minutes, +3 minute window; for subjects who receive the 200µL or 400µL dose - at 15 minutes, +3 minute window

,
InterventionParticipants (Count of Participants)
3 to 5 years6 to 11 years12 to 17 years
Kovacaine Mist171415
Placebo862

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Incidence of Adverse Events (AEs) by Dosage Cohort

Patients with AEs (NCT01844830)
Timeframe: from baseline to 24 hours following drug administration

,
InterventionCount of participants (Number)
100 µL200 µL400 µL
Kovacaine Mist122215
Placebo697

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Incidence of Adverse Events (AEs) by Age Group

Patients with AEs (NCT01844830)
Timeframe: from baseline to 24 hours following drug administration

,
InterventionCount of participants (Number)
3 to 5 years6 to 11 years12 to 17 years
Kovacaine Mist171913
Placebo7114

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Number of Participants Who Completed the Study Dental Procedure Without Need for Rescue by Injection of Local Anesthetic.

If the participant does not have sufficient anesthesia to complete the Study Dental Procedure, the participant is given a rescue injection of local anesthetic and is considered a failure for this outcome. (NCT01844830)
Timeframe: 100µL dose - at 10 minutes, +3 minute window; for subjects who receive the 200µL or 400µL dose - at 15 minutes, +3 minute window

InterventionParticipants (Count of Participants)
Kovacaine Mist46
Placebo16

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Maximum Change From Baseline in Systolic Blood Pressure

(NCT01844830)
Timeframe: from baseline to 24 hours following drug administration

InterventionmmHg (Mean)
Kovacaine Mist5.4
Placebo1.0

[back to top]

Maximum Change From Baseline in Heart Rate

(NCT01844830)
Timeframe: from baseline to 24 hours following drug administration

Interventionbpm (Mean)
Kovacaine Mist5.6
Placebo6.9

[back to top]

Maximum Change From Baseline in Diastolic Blood Pressure

(NCT01844830)
Timeframe: from baseline to 24 hours following drug administration

InterventionmmHg (Mean)
Kovacaine Mist8.3
Placebo2.4

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Number of Participants Who Completed the Study Dental Procedure Without Need for Rescue by Injection of Local Anesthetic.by Dosage Cohort.

If the participant does not have sufficient anesthesia to complete the Study Dental Procedure, the participant is given a rescue injection of local anesthetic and is considered a failure for this outcome. (NCT01844830)
Timeframe: 100µL dose - at 10 minutes, +3 minute window; for subjects who receive the 200µL or 400µL dose - at 15 minutes, +3 minute window

,
InterventionParticipants (Count of Participants)
100 µL200 µL400 µL
Kovacaine Mist141418
Placebo754

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Measurement of Pain Associated With Injection, in Millimeters, According to Visual Analog Scale

The investigation is trying to determine if the compounded topical anesthetic (Pliaglis) is more effective than the active control (benzocaine) in numbing the gums before needle penetration. The effectiveness of the topical anesthetics will be determined by the patient indicating their level of discomfort felt upon needle stick by using a Heft-Parker visual analog pain scale (scale of 0 - 170mm with 0mm equating to no pain and 170mm equating to maximum pain). (NCT01951820)
Timeframe: 2.5 minutes

Interventionmm (Mean)
Benzocaine38.5
Pliaglis26.9

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The Primary Efficacy Variable is Response Based on the Realisation of the Capsulorhexis Without Use of Any Additive Mydriatic Treatment.

(NCT02101359)
Timeframe: Day 0

Interventionpercentage of responders (Number)
T238098.9
Reference Group94.7

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Number of Children in Each Group Who Don't Feel Pain or Have Mild Pain on Propofol Injection.

(NCT02240628)
Timeframe: During propofol injection.

Interventionparticipants (Number)
Propofol-Lidocaine Mixture29
Propofol -Saline Mixture19

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Pain Intensity

"A blinded independent observer will rate pain on Propofol injection according to a pain scale.~No pain.~Mild pain(associated with facial expression of pain).~Moderate Pain(Pulling/withdrawal of arm).~Severe Pain(Screaming)." (NCT02240628)
Timeframe: During Propofol injection.

,
Interventionparticipants (Number)
1234
Propofol -Saline Mixture61368
Propofol-Lidocaine Mixture20912

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Visual Analog Scale (VAS) for Pain

A visual analog scale (VAS) ranging from 0 to 10 was used to assess the patients' pain during the procedure. 0 means no pain, 1 to 3 means mild pain, 4 to 7 means moderate pain, and 8 to 10 means severe pain. Patients were asked the VAS score to express the degree of pain at each time point. (NCT02502487)
Timeframe: at cystoscopic inspection of external sphincter

Interventionunits on a scale (Median)
Tetracaine Gel Group6
Dorsal Penile Nerve Block Group4
Combination Group4

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Visual Analog Scale (VAS) for Pain

A visual analog scale (VAS) ranging from 0 to 10 was used to assess the patients' pain during the procedure. 0 means no pain, 1 to 3 means mild pain, 4 to 7 means moderate pain, and 8 to 10 means severe pain. Patients were asked the VAS score to express the degree of pain at each time point. (NCT02502487)
Timeframe: at cystoscopic inspection of penile and bulbar urethra

Interventionunits on a scale (Median)
Tetracaine Gel Group1
Dorsal Penile Nerve Block Group1
Combination Group1

[back to top]

Visual Analog Scale (VAS) for Pain

A visual analog scale (VAS) ranging from 0 to 10 was used to assess the patients' pain during the procedure. 0 means no pain, 1 to 3 means mild pain, 4 to 7 means moderate pain, and 8 to 10 means severe pain. Patients were asked the VAS score to express the degree of pain at each time point. (NCT02502487)
Timeframe: at cystoscopic inspection of prostate and bladder

Interventionunits on a scale (Median)
Tetracaine Gel Group2
Dorsal Penile Nerve Block Group0
Combination Group0

[back to top]

Visual Analog Scale (VAS) for Pain

A visual analog scale (VAS) ranging from 0 to 10 was used to assess the patients' pain during the procedure. 0 means no pain, 1 to 3 means mild pain, 4 to 7 means moderate pain, and 8 to 10 means severe pain. Patients were asked the VAS score to express the degree of pain at each time point. (NCT02502487)
Timeframe: before gel administration

Interventionunits on a scale (Median)
Tetracaine Gel Group0
Dorsal Penile Nerve Block Group0
Combination Group0

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Breath Rate at Cystoscopic Inspection of Penile and Bulbar Urthra

(NCT02502487)
Timeframe: at cystoscopic inspection of penile and bulbar Urthra

Interventiontimes per minute (Mean)
Tetracaine Gel Group20.0
Dorsal Penile Nerve Block Group19.8
Combination Group19.6

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Heart Rate at Cystoscopic Inspection of Penile and Bulbar Urthra

(NCT02502487)
Timeframe: at cystoscopic inspection of penile and bulbar urethra

InterventionBeats per minute (Mean)
Tetracaine Gel Group84.8
Dorsal Penile Nerve Block Group83.8
Combination Group81.1

[back to top]

Heart Rate Before Gel Administration

(NCT02502487)
Timeframe: before gel administration

InterventionBeats per minute (Mean)
Tetracaine Gel Group75.0
Dorsal Penile Nerve Block Group75.9
Combination Group73.6

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Mean Arterial Pressure After Withdrawal of Cystoscope

(NCT02502487)
Timeframe: after withdrawal of cystoscope

InterventionmmHg (Mean)
Tetracaine Gel Group99.3
Dorsal Penile Nerve Block Group95.7
Combination Group95.2

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Mean Arterial Pressure at Cystoscopic Inspection of External Sphincter

(NCT02502487)
Timeframe: at cystoscopic inspection of external sphincter

InterventionmmHg (Mean)
Tetracaine Gel Group113.7
Dorsal Penile Nerve Block Group105.8
Combination Group104.8

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Mean Arterial Pressure at Cystoscopic Inspection of Penile and Bulbar Urthra

(NCT02502487)
Timeframe: at cystoscopic inspection of penile and bulbar urthra

InterventionmmHg (Mean)
Tetracaine Gel Group100
Dorsal Penile Nerve Block Group99.8
Combination Group98.2

[back to top]

Mean Arterial Pressure Before Gel Administration

(NCT02502487)
Timeframe: before gel administration

InterventionmmHg (Mean)
Tetracaine Gel Group95.3
Dorsal Penile Nerve Block Group96.6
Combination Group95.1

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Oxygen Saturation by Pulse After Withdrawal of Cystoscope

(NCT02502487)
Timeframe: after withdrawal of cystoscope

Interventionpercentage (Median)
Tetracaine Gel Group99
Dorsal Penile Nerve Block Group98
Combination Group99

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Oxygen Saturation by Pulse at Cystoscopic Inspection of External Sphincter

(NCT02502487)
Timeframe: at cystoscopic inspection of external sphincter

Interventionpercentage (Median)
Tetracaine Gel Group99
Dorsal Penile Nerve Block Group98
Combination Group99

[back to top]

Oxygen Saturation by Pulse at Cystoscopic Inspection of Penile and Bulbar Urthra

(NCT02502487)
Timeframe: at cystoscopic inspection of penile and bulbar urthra

Interventionpercentage (Median)
Tetracaine Gel Group99
Dorsal Penile Nerve Block Group98
Combination Group99

[back to top]

Breath Rate After Withdrawal of Cystoscope

(NCT02502487)
Timeframe: after withdrawal of cystoscope

Interventiontimes per minute (Mean)
Tetracaine Gel Group19.7
Dorsal Penile Nerve Block Group19.4
Combination Group19.4

[back to top]

Oxygen Saturation by Pulse Before Gel Administration

(NCT02502487)
Timeframe: before gel administration

Interventionpercentage (Median)
Tetracaine Gel Group99
Dorsal Penile Nerve Block Group98
Combination Group99

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Breath Rate at Cystoscopic Inspection of External Sphincter

(NCT02502487)
Timeframe: at cystoscopic inspection of external sphincter

Interventiontimes per minute (Mean)
Tetracaine Gel Group20.1
Dorsal Penile Nerve Block Group19.8
Combination Group19.8

[back to top]

Visual Analog Scale (VAS) for Pain

A visual analog scale (VAS) ranging from 0 to 10 was used to assess the patients' pain during the procedure. 0 means no pain, 1 to 3 means mild pain, 4 to 7 means moderate pain, and 8 to 10 means severe pain. Patients were asked the VAS score to express the degree of pain at each time point. (NCT02502487)
Timeframe: after withdrawal of cystoscope

Interventionunits on a scale (Median)
Tetracaine Gel Group0
Dorsal Penile Nerve Block Group0
Combination Group0

[back to top]

Breath Rate Before Gel Administration

(NCT02502487)
Timeframe: before gel administration

Interventiontimes per minute (Mean)
Tetracaine Gel Group19.8
Dorsal Penile Nerve Block Group19.6
Combination Group19.5

[back to top]

Heart Rate After Withdrawal of Cystoscope

(NCT02502487)
Timeframe: after withdrawal of cystoscope

InterventionBeats per minute (Mean)
Tetracaine Gel Group76.7
Dorsal Penile Nerve Block Group72.3
Combination Group71.6

[back to top]

Heart Rate at Cystoscopic Inspection of External Sphincter

(NCT02502487)
Timeframe: at cystoscopic inspection of external sphincter

InterventionBeats per minute (Mean)
Tetracaine Gel Group96.7
Dorsal Penile Nerve Block Group90.2
Combination Group86.2

[back to top]

Usage Frequency of Cardiovascular Drugs: Norepinephrine

Cardiovascular drugs as defined under interventions. Frequency of patients receiving the drug. Cardiovascular drugs that were given in <1% of cases are not reported. (NCT02726620)
Timeframe: During the anesthetic phase of the surgical procedure: an expected average of 2.5 hours

InterventionParticipants (Count of Participants)
Usual Care Group762
Hypotension Decision Support233

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Usage Frequency of Cardiovascular Drugs: Glycopyrrolate

Cardiovascular drugs as defined under interventions. Frequency of patients receiving the drug. Cardiovascular drugs that were given in <1% of cases are not reported. (NCT02726620)
Timeframe: During the anesthetic phase of the surgical procedure: an expected average of 2.5 hours

InterventionParticipants (Count of Participants)
Usual Care Group11093
Hypotension Decision Support1257

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Usage Frequency of Cardiovascular Drugs: Ephinephrine

Cardiovascular drugs as defined under interventions. Frequency of patients receiving the drug. Cardiovascular drugs that were given in <1% of cases are not reported. (NCT02726620)
Timeframe: During the anesthetic phase of the surgical procedure: an expected average of 2.5 hours

InterventionParticipants (Count of Participants)
Usual Care Group1215
Hypotension Decision Support409

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Usage Frequency of Cardiovascular Drugs: Ephedrine

Cardiovascular drugs as defined under interventions. Frequency of patients receiving the drug. Cardiovascular drugs that were given in <1% of cases are not reported. (NCT02726620)
Timeframe: During the anesthetic phase of the surgical procedure: an expected average of 2.5 hours

InterventionParticipants (Count of Participants)
Usual Care Group9310
Hypotension Decision Support2718

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Average Use of Cardiovascular Drugs: Norepinephrine

Cardiovascular drugs as defined under interventions. Average use for each drug will be calculated. Cardiovascular drugs that were given in <1% of cases are not reported, as the average dosage would be meaningless. (NCT02726620)
Timeframe: During the anesthetic phase of the surgical procedure: an expected average of 2.5 hours

Interventionmg (Median)
Usual Care Group0.62
Hypotension Decision Support0.70

[back to top]

Average Use of Cardiovascular Drugs: Glycopyrrolate

Cardiovascular drugs as defined under interventions. Average use for each drug will be calculated. Cardiovascular drugs that were given in <1% of cases are not reported, as the average dosage would be meaningless. (NCT02726620)
Timeframe: During the anesthetic phase of the surgical procedure: an expected average of 2.5 hours

Interventionmg (Median)
Usual Care Group0.40
Hypotension Decision Support0.40

[back to top]

Average Use of Cardiovascular Drugs: Epinephrine

Cardiovascular drugs as defined under interventions. Average use for each drug will be calculated. Cardiovascular drugs that were given in <1% of cases are not reported, as the average dosage would be meaningless. (NCT02726620)
Timeframe: During the anesthetic phase of the surgical procedure: an expected average of 2.5 hours

Interventionmg (Median)
Usual Care Group1.00
Hypotension Decision Support0.70

[back to top]

Average Use of Cardiovascular Drugs: Ephedrine

Cardiovascular drugs as defined under interventions. Average use for each drug will be calculated. Cardiovascular drugs that were given in <1% of cases are not reported, as the average dosages would be meaningless. (NCT02726620)
Timeframe: During the anesthetic phase of the surgical procedure: an expected average of 2.5 hours

Interventionmg (Median)
Usual Care Group20
Hypotension Decision Support15

[back to top]

30-day Mortality

Vanderbilt University Medical Center: combination of in-hospital mortality and 'alive-index' (which checks for visits to the hospital in the electronic healthcare record as indication of being alive at 30 days) (NCT02726620)
Timeframe: 30 days after surgery

InterventionParticipants (Count of Participants)
Usual Care Group511
Hypotension Decision Support143

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Timing of Cardiovascular Drugs for MAP < 60 mmHg

Cardiovascular drugs as defined under interventions. Time of first administration of cardiovascular drug relative to the time at which the mean arterial pressure (MAP) drops below 60 mmHg. Per patient the average time to first administration of all hypotensive episodes was calculated. That average time is used as the outcome variable. A negative value indicates that administration occurred before the drop in MAP. (NCT02726620)
Timeframe: During the anesthetic phase of the surgical procedure: an expected average of 2.5 hours

Interventionminutes (Median)
Usual Care Group0.8
Hypotension Decision Support1.5

[back to top]

Timing of Cardiovascular Drugs for MAP < 55 mmHg

Cardiovascular drugs as defined under interventions. Time of first administration of cardiovascular drug relative to the time at which the mean arterial pressure (MAP) drops below 55 mmHg. Per patient the average time to first administration of all hypotensive episodes was calculated. That average time is used as the outcome variable. A negative value indicates that administration occurred before the drop in MAP. (NCT02726620)
Timeframe: During the anesthetic phase of the surgical procedure: an expected average of 2.5 hours

Interventionminutes (Median)
Usual Care Group1
Hypotension Decision Support0.5

[back to top]

Timing of Cardiovascular Drugs for MAP < 50 mmHg

Cardiovascular drugs as defined under interventions. Time of first administration of cardiovascular drug relative to the time at which the mean arterial pressure (MAP) drops below 50 mmHg. Per patient the average time to first administration of all hypotensive episodes was calculated. That average time is used as the outcome variable. A negative value indicates that administration occurred before the drop in MAP. (NCT02726620)
Timeframe: During the anesthetic phase of the surgical procedure: an expected average of 2.5 hours

Interventionminutes (Median)
Usual Care Group1
Hypotension Decision Support0

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Time to Discharge Readiness at the Postanesthesia Care Unit (PACU)

The time from arriving at the postanesthesia care unit (PACU) until the time the patient is considered ready for discharge (in minutes). (NCT02726620)
Timeframe: A specific time frame on the day of surgery: from the start of admission to the PACU to discharge from the PACU, an expected average of 4 hours

Interventionminutes (Median)
Usual Care Group67
Hypotension Decision Support60

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Postoperative Rise in Creatinine Levels

Absolute values for serum creatinine before and after surgery will be compared. When multiple postoperative creatinine measurements are made, the maximum difference is reported. (NCT02726620)
Timeframe: Within 7 days after surgery

Interventionmg/dL (Median)
Usual Care Group0.00
Hypotension Decision Support0.00

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Intravenous Anesthetic Drug Use During Intraoperative Hypotension: MAP < 65 mmHg

Average concentrations of propofol infusion rates during MAP < 65 mmHg episodes (NCT02726620)
Timeframe: During the anesthetic phase of the surgical procedure: an expected average of 2.5 hours

Interventionmcg/kg/min (propofol) (Median)
Usual Care Group60.10
Hypotension Decision Support48.59

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Intravenous Anesthetic Drug Use During Intraoperative Hypotension: MAP < 60 mmHg

Average concentrations of propofol infusion rates during MAP < 60 mmHg episodes (NCT02726620)
Timeframe: During the anesthetic phase of the surgical procedure: an expected average of 2.5 hours

Interventionmcg/kg/min (propofol) (Median)
Usual Care Group61.07
Hypotension Decision Support50.00

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Intravenous Anesthetic Drug Use During Intraoperative Hypotension: MAP < 55 mmHg

Average concentrations of propofol infusion rates during MAP < 55 mmHg episodes (NCT02726620)
Timeframe: During the anesthetic phase of the surgical procedure: an expected average of 2.5 hours

Interventionmcg/kg/min (propofol) (Median)
Usual Care Group63.95
Hypotension Decision Support50.00

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Intravenous Anesthetic Drug Use During Intraoperative Hypotension: MAP < 50 mmHg

Average concentrations of propofol infusion rates during MAP < 50 mmHg episodes (NCT02726620)
Timeframe: During the anesthetic phase of the surgical procedure: an expected average of 2.5 hours

Interventionmcg/kg/min (propofol) (Median)
Usual Care Group65.00
Hypotension Decision Support50.00

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Intraoperative Administration of Intravenous Fluids

Total amount (mL) of intravenous fluids (as defined under interventions) administered during the surgical procedure. (NCT02726620)
Timeframe: During the anesthetic phase of the surgical procedure: an expected average of 2.5 hours

InterventionmL (Median)
Usual Care Group1500.00
Hypotension Decision Support1400.00

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Incidence of a MAP < 60 mmHg for > 20 Minutes

Incidence of a mean arterial pressure (MAP) < 60 mmHg for a cumulative duration of all hypotensive episodes of more than 20 minutes during the anesthetic phase of the procedure. (NCT02726620)
Timeframe: During the anesthetic phase of the surgical procedure: an expected average of 2.5 hours

InterventionParticipants (Count of Participants)
Usual Care Group3632
Hypotension Decision Support792

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Incidence of a MAP < 60 mmHg for > 10 Minutes

Incidence of a mean arterial pressure (MAP) < 60 mmHg for a cumulative duration of all hypotensive episodes of more than 10 minutes during the anesthetic phase of the procedure. (NCT02726620)
Timeframe: During the anesthetic phase of the surgical procedure: an expected average of 2.5 hours

InterventionParticipants (Count of Participants)
Usual Care Group6989
Hypotension Decision Support1723

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Incidence of a MAP < 60 mmHg

Incidence of a mean arterial pressure (MAP) < 60 mmHg during anesthesia for 1 minute or more. (NCT02726620)
Timeframe: During the anesthetic phase of the surgical procedure: an expected average of 2.5 hours

InterventionParticipants (Count of Participants)
Usual Care Group13779
Hypotension Decision Support3798

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Incidence of a MAP < 55 mmHg for > 20 Minutes

Incidence of a mean arterial pressure (MAP) < 55 mmHg for a cumulative duration of all hypotensive episodes of more than 20 minutes during the anesthetic phase of the procedure. (NCT02726620)
Timeframe: During the anesthetic phase of the surgical procedure: an expected average of 2.5 hours

InterventionParticipants (Count of Participants)
Usual Care Group1223
Hypotension Decision Support284

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Incidence of a MAP < 55 mmHg for > 10 Minutes

Incidence of a mean arterial pressure (MAP) < 55 mmHg for a cumulative duration of all hypotensive episodes of more than 10 minutes during the anesthetic phase of the procedure. (NCT02726620)
Timeframe: During the anesthetic phase of the surgical procedure: an expected average of 2.5 hours

InterventionParticipants (Count of Participants)
Usual Care Group3181
Hypotension Decision Support759

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Incidence of a MAP < 55 mmHg

Incidence of a mean arterial pressure (MAP) < 55 mmHg during anesthesia for 1 minute or more. (NCT02726620)
Timeframe: During the anesthetic phase of the surgical procedure: an expected average of 2.5 hours

InterventionParticipants (Count of Participants)
Usual Care Group10991
Hypotension Decision Support3045

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Incidence of a MAP < 50 mmHg for > 20 Minutes

Incidence of a mean arterial pressure (MAP) < 50 mmHg for a cumulative duration of all hypotensive episodes of more than 20 minutes during the anesthetic phase of the procedure. (NCT02726620)
Timeframe: During the anesthetic phase of the surgical procedure: an expected average of 2.5 hours

InterventionParticipants (Count of Participants)
Usual Care Group304
Hypotension Decision Support85

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Timing of Cardiovascular Drugs for MAP < 65 mmHg

Cardiovascular drugs as defined under interventions. Time of first administration of cardiovascular drug relative to the time at which the mean arterial pressure (MAP) drops below 60 mmHg. Per patient the average time to first administration of all hypotensive episodes was calculated. That average time is used as the outcome variable. A negative value indicates that administration occurred before the drop in MAP. (NCT02726620)
Timeframe: During the anesthetic phase of the surgical procedure: an expected average of 2.5 hours

Interventionminutes (Median)
Usual Care Group2
Hypotension Decision Support1.14

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Incidence of a MAP < 50 mmHg for > 10 Minutes

Incidence of a mean arterial pressure (MAP) < 50 mmHg for a cumulative duration of all hypotensive episodes of more than 10 minutes during the anesthetic phase of the procedure. (NCT02726620)
Timeframe: During the anesthetic phase of the surgical procedure: an expected average of 2.5 hours

InterventionParticipants (Count of Participants)
Usual Care Group1159
Hypotension Decision Support326

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Incidence of a MAP < 50 mmHg

Incidence of a mean arterial pressure (MAP) < 50 mmHg during anesthesia for 1 minute or more. (NCT02726620)
Timeframe: During the anesthetic phase of the surgical procedure: an expected average of 2.5 hours

InterventionParticipants (Count of Participants)
Usual Care Group7781
Hypotension Decision Support2196

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In-hospital Mortality

Hospital mortality rate during a single hospital admission after the surgery (NCT02726620)
Timeframe: All postoperative days during a single hospital admission, expected median of 5 days

InterventionParticipants (Count of Participants)
Usual Care Group487
Hypotension Decision Support137

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Estimated Intraoperative Blood Loss

The estimated blood loss in mL during the surgical procedure (NCT02726620)
Timeframe: During the surgical procedure: an expected average of 2 hours

InterventionmL (Median)
Usual Care Group100
Hypotension Decision Support75

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Depth and Duration of Intraoperative Hypotension - Threshold MAP 75 mmHg

Depth and duration of intraoperative hypotension will be modeled by calculating areas under the threshold for mean arterial pressures (MAPs). Thresholds will vary from 75 mmHg to 50 mmHg in 5 mmHg decrements. Together these variables represent the depth and duration of intraoperative hypotension. To optimize goodness of fit of these variables, the decremental steps may be increased to 10 mmHg and more restrictive lowest and highest thresholds may be chosen for the statistical analysis. (NCT02726620)
Timeframe: During the anesthetic phase of the surgical procedure: an expected average of 2.5 hours

InterventionmmHg*minute (Median)
Usual Care Group485
Hypotension Decision Support417

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Depth and Duration of Intraoperative Hypotension - Threshold MAP 70 mmHg

Depth and duration of intraoperative hypotension will be modeled by calculating areas under the threshold for mean arterial pressures (MAPs). Thresholds will vary from 75 mmHg to 50 mmHg in 5 mmHg decrements. Together these variables represent the depth and duration of intraoperative hypotension. To optimize goodness of fit of these variables, the decremental steps may be increased to 10 mmHg and more restrictive lowest and highest thresholds may be chosen for the statistical analysis. (NCT02726620)
Timeframe: During the anesthetic phase of the surgical procedure: an expected average of 2.5 hours

InterventionmmHg*minute (Median)
Usual Care Group273
Hypotension Decision Support235

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Depth and Duration of Intraoperative Hypotension - Threshold MAP 65 mmHg

Depth and duration of intraoperative hypotension will be modeled by calculating areas under the threshold for mean arterial pressures (MAPs). Thresholds will vary from 75 mmHg to 50 mmHg in 5 mmHg decrements. Together these variables represent the depth and duration of intraoperative hypotension. To optimize goodness of fit of these variables, the decremental steps may be increased to 10 mmHg and more restrictive lowest and highest thresholds may be chosen for the statistical analysis. (NCT02726620)
Timeframe: During the anesthetic phase of the surgical procedure: an expected average of 2.5 hours

InterventionmmHg*minute (Median)
Usual Care Group96
Hypotension Decision Support86

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Depth and Duration of Intraoperative Hypotension - Threshold MAP 60 mmHg

Depth and duration of intraoperative hypotension will be modeled by calculating areas under the threshold for mean arterial pressures (MAPs). Thresholds will vary from 75 mmHg to 50 mmHg in 5 mmHg decrements. Together these variables represent the depth and duration of intraoperative hypotension. To optimize goodness of fit of these variables, the decremental steps may be increased to 10 mmHg and more restrictive lowest and highest thresholds may be chosen for the statistical analysis. (NCT02726620)
Timeframe: During the anesthetic phase of the surgical procedure: an expected average of 2.5 hours

InterventionmmHg*minute (Median)
Usual Care Group57
Hypotension Decision Support52

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Depth and Duration of Intraoperative Hypotension - Threshold MAP 55 mmHg

Depth and duration of intraoperative hypotension will be modeled by calculating areas under the threshold for mean arterial pressures (MAPs). Thresholds will vary from 75 mmHg to 50 mmHg in 5 mmHg decrements. Together these variables represent the depth and duration of intraoperative hypotension. To optimize goodness of fit of these variables, the decremental steps may be increased to 10 mmHg and more restrictive lowest and highest thresholds may be chosen for the statistical analysis. (NCT02726620)
Timeframe: During the anesthetic phase of the surgical procedure: an expected average of 2.5 hours

InterventionmmHg*minute (Median)
Usual Care Group23
Hypotension Decision Support23

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Depth and Duration of Intraoperative Hypotension - Threshold MAP 50 mmHg

Depth and duration of intraoperative hypotension will be modeled by calculating areas under the threshold for mean arterial pressures (MAPs). Thresholds will vary from 75 mmHg to 50 mmHg in 5 mmHg decrements. Together these variables represent the depth and duration of intraoperative hypotension. To optimize goodness of fit of these variables, the decremental steps may be increased to 10 mmHg and more restrictive lowest and highest thresholds may be chosen for the statistical analysis. (NCT02726620)
Timeframe: During the anesthetic phase of the surgical procedure: an expected average of 2.5 hours

InterventionmmHg*minute (Median)
Usual Care Group19
Hypotension Decision Support19

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Average Use of Cardiovascular Drugs: Phenylephrine

Cardiovascular drugs as defined under interventions. Average use for each drug will be calculated. Cardiovascular drugs that were given in <1% of cases are not reported, as the average dosage would be meaningless. (NCT02726620)
Timeframe: During the anesthetic phase of the surgical procedure: an expected average of 2.5 hours

Interventionmg (Median)
Usual Care Group0.90
Hypotension Decision Support1.30

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Inhaled Anesthetic Drug Use During Intraoperative Hypotension: MAP < 65 mmHg

Average concentrations of inhalational anesthesia during MAP < 65 mmHg episodes (NCT02726620)
Timeframe: During the anesthetic phase of the surgical procedure: an expected average of 2.5 hours

,
InterventionEndTidal% (other) (Median)
Sevoflurane (EndTidal %)Isoflurane (EndTidal %)Desflurane (EndTidal %)
Hypotension Decision Support1.270.682.31
Usual Care Group1.350.684.10

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Inhaled Anesthetic Drug Use During Intraoperative Hypotension: MAP < 60 mmHg

Average concentrations of inhalational anesthesia during MAP < 60 mmHg episodes (NCT02726620)
Timeframe: During the anesthetic phase of the surgical procedure: an expected average of 2.5 hours

,
InterventionEndTidal% (other) (Median)
Sevoflurane (EndTidal %)Isoflurane (EndTidal %)Desflurane (EndTidal %)
Hypotension Decision Support1.250.672.33
Usual Care Group1.350.684.36

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Inhaled Anesthetic Drug Use During Intraoperative Hypotension: MAP < 55 mmHg

Average concentrations of inhalational anesthesia during MAP < 55 mmHg episodes (NCT02726620)
Timeframe: During the anesthetic phase of the surgical procedure: an expected average of 2.5 hours

,
InterventionEndTidal% (other) (Median)
Sevoflurane (EndTidal %)Isoflurane (EndTidal %)Desflurane (EndTidal %)
Hypotension Decision Support1.250.674.65
Usual Care Group1.340.684.60

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Inhaled Anesthetic Drug Use During Intraoperative Hypotension: MAP < 50 mmHg

Average concentrations of inhalational anesthesia during MAP < 50 mmHg episodes (NCT02726620)
Timeframe: During the anesthetic phase of the surgical procedure: an expected average of 2.5 hours

,
InterventionEndTidal% (other) (Median)
Sevoflurane (EndTidal %)Isoflurane (EndTidal %)Desflurane (EndTidal %)
Hypotension Decision Support1.230.654.70
Usual Care Group1.320.654.28

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Usage Frequency of Cardiovascular Drugs: Phenylephrine

Cardiovascular drugs as defined under interventions. Frequency of patients receiving the drug. Cardiovascular drugs that were given in <1% of cases are not reported. (NCT02726620)
Timeframe: During the anesthetic phase of the surgical procedure: an expected average of 2.5 hours

InterventionParticipants (Count of Participants)
Usual Care Group12211
Hypotension Decision Support3685

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Duration of Anesthesia as Measured by Pin Prick Test (PPT) for One Spray CTY-5339-A Compared to One Spray CTY-5339-CB

"Evaluations were completed at 1-minute intervals for the first 5 minutes to capture onset of anesthesia. Starting at 5 minutes after drug administration, the PPT was done at 5 minute intervals up to the one hour time point. If there was no indication of anesthesia by 10 minutes, the subject was considered a treatment failure and the assessment of PPT was discontinued. In addition, once onset of anesthesia had occurred, if there was no longer any anesthesia at two consecutive evaluation time points from 10 minutes onward, the assessment of PPT was discontinued.~The PPT was assessed using a 90-mm, 26-gauge pencil-point spinal needle. At screening, 3 pin pricks were performed on each cheek. Pin pricks were assessed using a 0 (no pain) to 10 (severe pain) Numerical Rating Scale (NRS). In order to be eligible for the study, for each cheek, subjects must have had a minimum score of 3 for the last 2 pin pricks, and one of those scores had to be 4 or higher." (NCT02908620)
Timeframe: Change in pain assessment from baseline (time of application) up to one hour post-application

Interventionminutes (Mean)
One Spray CTY-5339-A17.9
One Spray CTY-5339-CB16.4

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Duration of Anesthesia as Measured by Pin Prick Test (PPT) for Two Sprays CTY-5339-A Compared to One Spray CTY-5339-CB in Combination With One Spray CTY-5339-P (Placebo)

"Assessments will be made over a period of one hour, with assessments at 1 minute intervals for the first 5 minutes and then every 5 minutes after that. Duration of effect was defined as the time (in minutes) from onset to treatment failure (i.e., for PPT, an assessment of Same/More pain, and for QST, the average heat temperature was greater than the average heat temperature at Baseline (non-treated cheek), up to the 60-minute time point (at two consecutive time points)." (NCT02908620)
Timeframe: Time of application up to one hour post-application

InterventionMinutes (Mean)
Two Sprays CTY-5339-A17.3
One Spray CTY-5339-CB in Combination With One Spray CTY-5339-P13.5

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Duration of Anesthesia as Measured by PPT for One Spray CTY-5339-A Compared to Two Sprays CTY-5339-A

Assessments will be made over a period of one hour, with assessments at 1 minute intervals for the first 5 minutes and then every 5 minutes after that. (NCT02908620)
Timeframe: Time of application up to one hour post-application

Interventionminutes (Mean)
One Spray CTY-5339-A17.9
Two Sprays CTY-5339-A17.3

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Duration of Anesthesia as Measured by QST Heat for One Spray CTY-5339-A Compared to Two Sprays CTY-5339-A

Assessments will be made over a period of one hour, with assessments at 1 minute intervals for the first 5 minutes and then every 5 minutes after that. (NCT02908620)
Timeframe: Time of application up to one hour post-application

Interventionminutes (Mean)
One Spray CTY-5339-A44.6
Two Sprays CTY-5339-A46.8

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Duration of Anesthesia as Measured by QST Heat for Two Sprays CTY-5339-A Compared to One Spray CTY-5339-CB in Combination With One Spray CTY-5339-P (Placebo)

"Assessments will be made over a period of one hour, with assessments at 1 minute intervals for the first 5 minutes and then every 5 minutes after that. Duration of effect was defined as the time (in minutes) from onset to treatment failure (i.e., for PPT, an assessment of Same/More pain, and for QST, the average heat temperature was greater than the average heat temperature at Baseline (non-treated cheek), up to the 60-minute time point (at two consecutive time points)." (NCT02908620)
Timeframe: Time of application up to one hour post-application

Interventionminutes (Mean)
Two Sprays CTY-5339-A46.8
One Spray CTY-5339-CB in Combination With One Spray CTY-5339-P38.9

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Onset of Anesthesia for PPT

Assessments will be made over a period of one hour, with assessments at 1 minute intervals for the first 5 minutes and then every 5 minutes after that. (NCT02908620)
Timeframe: Time of application up to one hour post-application

InterventionMinutes (Mean)
One Spray CTY-5339-A1.2
Two Sprays CTY-5339-A1.5
One Spray CTY-5339-CB1.7
One Spray CTY-5339-CB in Combination With One Spray CTY-5339-P1.7

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Onset of Anesthesia for QST Heat

Assessments will be made over a period of one hour, with assessments at 1 minute intervals for the first 5 minutes and then every 5 minutes after that. (NCT02908620)
Timeframe: Time of application up to one hour post-application

InterventionMinutes (Mean)
One Spray CTY-5339-A3.1
Two Sprays CTY-5339-A1.9
One Spray CTY-5339-CB1.7
CTY-5339-CB 1 Spray + Placebo 1 Spray4.2

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Percentage of Responders for PPT at Each Time Point

Assessments will be made over a period of one hour, with assessments at 1 minute intervals for the first 5 minutes and then every 5 minutes after that. (NCT02908620)
Timeframe: Time of application up to one hour post-application

,,,
InterventionParticipants (Count of Participants)
Responded to treatment at the 1 minute time pointResponded to treatment at the 2 minute time pointResponded to treatment at the 3 minute time pointResponded to treatment at the 4 minute time pointResponded to treatment at the 5 minute time pointResponded to treatment at the 10 minute time pointResponded to treatment at the 15 minute time pointResponded to treatment at the 20 minute time pointResponded to treatment at the 25 minute time pointResponded to treatment at the 30 minute time pointResponded to treatment at the 35 minute time pointResponded to treatment at the 40 minute time pointResponded to treatment at the 45 minute time pointResponded to treatment at the 50 minute time pointResponded to treatment at the 55 minute time pointResponded to treatment at the 60 minute time point
One Spray CTY-5339-A121312121058433110000
One Spray CTY-5339-CB1414128786442101010
One Spray CTY-5339-CB in Combination With One Spray CTY-5339-P1013108964212111111
Two Sprays CTY-5339-A1291112765656301100

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Percentage of Responders for QST Heat at Each Time Point

Assessments will be made over a period of one hour, with assessments at 1 minute intervals for the first 5 minutes and then every 5 minutes after that. (NCT02908620)
Timeframe: Time of application up to one hour post-application

,,,
InterventionParticipants (Count of Participants)
Responded to treatment at the 5 minute time pointResponded to treatment at the 10 minute time pointResponded to treatment at the 15 minute time pointResponded to treatment at the 20 minute time pointResponded to treatment at the 25 minute time pointResponded to treatment at the 30 minute time pointResponded to treatment at the 35 minute time pointResponded to treatment at the 40 minute time pointResponded to treatment at the 45 minute time pointResponded to treatment at the 50 minute time pointResponded to treatment at the 55 minute time pointResponded to treatment at the 60 minute time point
One Spray CTY-5339-A1617151715141312139910
One Spray CTY-5339-CB18171817151417161210910
One Spray CTY-5339-CB in Combination With One Spray CTY-5339-P1513151414131212111098
Two Sprays CTY-5339-A181717151514121111121111

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Duration of Anesthesia as Measured by Heat Sensation Threshold (QST Heat) for One Spray CTY-5339-A Compared to One Spray CTY-5339-CB

"Starting at 5 minutes after drug administration, the QST was done at 5 minute intervals up to the one hour time point. If there was no indication of anesthesia by 10 minutes, the subject was considered a treatment failure and the assessment of PPT was discontinued. In addition, once onset of anesthesia had occurred, if there was no longer any anesthesia at two consecutive evaluation time points from 10 minutes onward, the assessment of QST was discontinued.~The heat stimuli were delivered in 3 repetitions, with inter-stimulus intervals of 30s. The basal thermode temperature was set at a comfortable 35ºC. The rate at which the thermode heated up was set at 0.5ºC/s, while the rate at which it cooled down was set at 8ºC/s. The maximum thermode temperature was set at 51ºC. Heat sensation threshold was defined as the temperature at which the subjects first felt tingling, warmth, heat, or pain." (NCT02908620)
Timeframe: Change in temperature from baseline (time of application) up to one hour post-application

Interventionminutes (Mean)
One Spray CTY-5339-A44.6
One Spray CTY-5339-CB51.1

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Stage II: Sum of Temperature Differences (STID) for Heat Sensation Threshold (QST Heat) (Post-hoc)

"STID was calculated as a sum of the delta QST Heat scores at each time point until the designated time point. The delta QST Heat score is defined as the change in QST Heat score from baseline. QST Heat scores were the temperature where the sensation of a heat stimuli was felt: ranging from 35 ºC to a maximum of 50.5 ºC with intervals of 0.5 ºC, at a frequency of every 1 minute for the first 5 minutes and then every 5 minutes thereafter until the final 60 minute time point.~The total possible scale range was from -155 ºC (best) to +155 ºC (worst) for STID at the 30 minute time point, and from -248 ºC (best) to +248 ºC (worst) for SPID at the 60 minute time point Lower scores signify a better outcome (less sensitive to pain than at baseline = less pain with therapy = therapy was more effective).~Stage II outcome." (NCT03233737)
Timeframe: Up to one hour post-application

,
InterventionDegrees Celcius (ºC) (Mean)
STID at the 30 minute time pointSTID at the 60 minute time point
One Spray CTY-5339-A136.5214
One Spray CTY-5339-CB96.6149.1

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Stage II: Onset of Anesthesia for Pin Prick Test (PPT)

"Onset of anesthesia was the time point at which the PPT average pain score was less than the Baseline PPT average score by any amount. Also, in 10 minutes or less, the subject must have had a lower PPT average pain score of ≥ 1 unit than the Baseline PPT. Onset was expected to be between 1 and 5 minutes. PPT scores were assessed using a 0 (no pain) to 10 (severe pain) Numerical Rating Scale at a frequency of every 1 minute for the first 5 minutes and then every 5 minutes thereafter until the final 60 minute time point.~Stage II outcome." (NCT03233737)
Timeframe: Up to one hour post-application

Interventionminutes (Mean)
One Spray CTY-5339-A1.1
One Spray CTY-5339-CB1.1

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Stage II: Percentage of Subjects Reaching Maximum Heat for Heat Sensation Threshold (QST Heat)

"QST Heat scores were the temperature where the sensation of a heat stimuli was felt: ranging from 35 ºC to a maximum of 50.5 ºC with intervals of 0.5 ºC, at a frequency of every 1 minute for the first 5 minutes and then every 5 minutes thereafter until the final 60 minute time point. Reaching maximum heat for QST Heat was defined as subjects reaching the maximum temperature without reporting pain at one or more time points.~Stage II outcome." (NCT03233737)
Timeframe: Any time within one hour post-application

InterventionParticipants (Count of Participants)
One Spray CTY-5339-A7
One Spray CTY-5339-CB5

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Stage II: Percentage of Subjects Reaching Minimal Pain on Pin Prick Test (PPT) (≤2 on Numerical Rating Scale Pain Scale)

"Response is defined as a subject having a PPT average pain score of ≤2 recorded at any single time point where PPT was performed. PPT scores were assessed using a 0 (no pain) to 10 (severe pain) Numerical Rating Scale at a frequency of every 1 minute for the first 5 minutes and then every 5 minutes thereafter until the final 60 minute time point.~Stage II outcome." (NCT03233737)
Timeframe: Any time within one hour post-application

InterventionParticipants (Count of Participants)
One Spray CTY-5339-A50
One Spray CTY-5339-CB50

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Stage I: Percentage of Responders for Heat Sensation Threshold (QST Heat) at Each Time Point

"Response at a time point is defined as an increase of QST heat pain temperature by ≥ 3 degrees C compared to the Baseline QST. QST Heat scores were the temperature where the sensation of a heat stimuli was felt: ranging from 35 ºC to a maximum of 50.5 ºC with intervals of 0.5 ºC, at a frequency of every 1 minute for the first 5 minutes and then every 5 minutes thereafter until the final 60 minute time point.~Stage I outcome." (NCT03233737)
Timeframe: Time of application up to one hour post-application

,,
InterventionParticipants (Count of Participants)
Responded to treatment at the 1 minute time pointResponded to treatment at the 2 minute time pointResponded to treatment at the 3 minute time pointResponded to treatment at the 4 minute time pointResponded to treatment at the 5 minute time pointResponded to treatment at the 10 minute time pointResponded to treatment at the 15 minute time pointResponded to treatment at the 20 minute time pointResponded to treatment at the 25 minute time pointResponded to treatment at the 30 minute time pointResponded to treatment at the 35 minute time pointResponded to treatment at the 40 minute time pointResponded to treatment at the 45 minute time pointResponded to treatment at the 50 minute time pointResponded to treatment at the 55 minute time pointResponded to treatment at the 60 minute time point
Stage I: One Spray CTY-5339-A7788899998666666
Stage I: One Spray CTY-5339-CB2333332211100000
Stage I: One Spray CTY-5339-P4444444410000000

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Stage II: Duration of Anesthesia as Measured by Pin Prick Test (PPT) for One Spray CTY-5339-A Compared to One Spray CTY-5339-CB

"The duration of effect, was defined as the length of time in minutes from onset of anesthesia to the absence of anesthesia.Onset was the time point at which the PPT average pain score was less than the Baseline PPT average score by any amount. Also, in 10 minutes or less, the subject must have had a lower PPT average pain score of ≥ 1 unit than Baseline. Absence of anesthesia was defined as follows: After Onset had been established, absence was the first of two time points with consecutive occurrences of regression of absence of analgesia. Reports of less pain by ≥1 unit than Baseline indicated analgesia; while a report of similar (< 1 unit) or more pain than Baseline indicated regression or absence of analgesia. The minimum onset time was 1 minute. PPT scores were assessed using a 0 (no pain) to 10 (severe pain) Numerical Rating Scale at a frequency of every 1 minute for the first 5 minutes and then every 5 minutes thereafter until the final 60 minute time point.~Stage II outcome." (NCT03233737)
Timeframe: Up to one hour post-application

Interventionminutes (Mean)
One Spray CTY-5339-A14.6
One Spray CTY-5339-CB7.4

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Stage I: Percentage of Responders for Pin Prick Test (PPT) at Each Time Point

"Response at at time point is defined as when the PPT average pain score was less than the Baseline PPT average score by any amount. PPT scores were assessed using a 0 (no pain) to 10 (severe pain) Numerical Rating Scale at a frequency of every 1 minute for the first 5 minutes and then every 5 minutes thereafter until the final 60 minute time point.~Stage I outcome." (NCT03233737)
Timeframe: Time of application up to one hour post-application

,,
InterventionParticipants (Count of Participants)
Responded to treatment at the 1 minute time pointResponded to treatment at the 2 minute time pointResponded to treatment at the 3 minute time pointResponded to treatment at the 4 minute time pointResponded to treatment at the 5 minute time pointResponded to treatment at the 10 minute time pointResponded to treatment at the 15 minute time pointResponded to treatment at the 20 minute time pointResponded to treatment at the 25 minute time pointResponded to treatment at the 30 minute time pointResponded to treatment at the 35 minute time pointResponded to treatment at the 40 minute time pointResponded to treatment at the 45 minute time pointResponded to treatment at the 50 minute time pointResponded to treatment at the 55 minute time pointResponded to treatment at the 60 minute time point
Stage I: One Spray CTY-5339-A8910101010101099987766
Stage I: One Spray CTY-5339-CB810101010108442211111
Stage I: One Spray CTY-5339-P4333233222222222

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Stage I: Sum of Pain Intensity Differences (SPID) for Pin Prick Test (PPT) (Post-hoc)

"SPID was calculated as a sum of the delta PPT scores at each time point until the designated time point. The delta PPT score is defined as the change in PPT score from baseline. PPT scores were assessed using a 0 (no pain) to 10 (severe pain) Numerical Rating Scale at a frequency of every 1 minute for the first 5 minutes and then every 5 minutes thereafter until the final 60 minute time point.~The total possible scale range was from -100 (best) to +100 (worst) for SPID at the 30 minute time point, and from -160 (best) to +160 (worst) for SPID at the 60 minute time point Lower scores signify a better outcome (less sensitive to pain than at baseline = less pain with therapy = therapy was more effective).~Stage I outcome." (NCT03233737)
Timeframe: Up to one hour post-application

,,
Interventionscore (Mean)
SPID at the 30 minute time pointSPID at the 60 minute time point
Stage I: One Spray CTY-5339-A-82.1-128.1
Stage I: One Spray CTY-5339-CB-37.8-44.0
Stage I: One Spray CTY-5339-P-29.3-53.3

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Stage II: Percentage of Responders for Heat Sensation Threshold (QST Heat) at Each Time Point

"Response at a time point is defined as an increase of QST heat pain temperature by ≥ 3 degrees C compared to the Baseline QST.~QST Heat scores were the temperature where the sensation of a heat stimuli was felt: ranging from 35 ºC to a maximum of 50.5 ºC with intervals of 0.5 ºC, at a frequency of every 1 minute for the first 5 minutes and then every 5 minutes thereafter until the final 60 minute time point.~Stage II outcome." (NCT03233737)
Timeframe: Up to one hour post-application

,
InterventionParticipants (Count of Participants)
Responded to treatment at the 1 minute time pointResponded to treatment at the 2 minute time pointResponded to treatment at the 3 minute time pointResponded to treatment at the 4 minute time pointResponded to treatment at the 5 minute time pointResponded to treatment at the 10 minute time pointResponded to treatment at the 15 minute time pointResponded to treatment at the 20 minute time pointResponded to treatment at the 25 minute time pointResponded to treatment at the 30 minute time pointResponded to treatment at the 35 minute time pointResponded to treatment at the 40 minute time pointResponded to treatment at the 45 minute time pointResponded to treatment at the 50 minute time pointResponded to treatment at the 55 minute time pointResponded to treatment at the 60 minute time point
One Spray CTY-5339-A36373737373838363228242219171413
One Spray CTY-5339-CB2930303031343129241915151212119

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Stage II: Duration of Anesthesia as Measured by Heat Sensation Threshold (QST Heat) for One Spray CTY-5339-A Compared to One Spray CTY-5339-CB

"The duration of effect, was defined as the time from onset to treatment failure, as measured by QST Heat score. QST Heat scores were the temperature where the sensation of a heat stimuli was felt: ranging from 35 ºC to a maximum of 50.5 ºC with intervals of 0.5 ºC, at a frequency of every 1 minute for the first 5 minutes and then every 5 minutes thereafter until the final 60 minute time point. The QST Heat-based Duration of effect was calculated by the length of time in minutes from onset of anesthesia to the absence of anesthesia where Onset of anesthesia was defined by PPT unless specific QST thresholds were not met. After Onset had been established, absence of analgesia or offset was the first of two time points with consecutive occurrences of regression or absence of analgesia. Reports of QST heat pain temperature by ≥ 3 °C of the Baseline QST indicated analgesia; while a report of similar (<3 °C) than Baseline indicated regression or absence of analgesia. Stage" (NCT03233737)
Timeframe: Up to one hour post-application

Interventionminutes (Mean)
One Spray CTY-5339-A45.5
One Spray CTY-5339-CB40.8

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Stage I: Percentage of Subjects Reaching Minimal Pain on Pin Prick Test (PPT) (≤2 on Numerical Rating Scale Pain Scale)

"Response is defined as a subject having a PPT average pain score of ≤2 recorded at any single time point where PPT was performed. PPT scores were assessed using a 0 (no pain) to 10 (severe pain) Numerical Rating Scale at a frequency of every 1 minute for the first 5 minutes and then every 5 minutes thereafter until the final 60 minute time point.~Stage I outcome." (NCT03233737)
Timeframe: Any time within one hour post-application

InterventionParticipants (Count of Participants)
Stage I: One Spray CTY-5339-A10
Stage I: One Spray CTY-5339-CB9
Stage I: One Spray CTY-5339-P2

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Stage I: Percentage of Subjects Reaching Maximum Heat for Heat Sensation Threshold (QST Heat)

"QST Heat scores were the temperature where the sensation of a heat stimuli was felt: ranging from 35 ºC to a maximum of 50.5 ºC with intervals of 0.5 ºC, at a frequency of every 1 minute for the first 5 minutes and then every 5 minutes thereafter until the final 60 minute time point. Reaching maximum heat for QST Heat was defined as subjects reaching the maximum temperature without reporting pain at one or more time points.~Stage I outcome." (NCT03233737)
Timeframe: Any time within one hour post-application

InterventionParticipants (Count of Participants)
Stage I: One Spray CTY-5339-A5
Stage I: One Spray CTY-5339-CB0
Stage I: One Spray CTY-5339-P0

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Stage I: Sum of Temperature Differences (STID) for Heat Sensation Threshold (QST Heat) (Post-hoc)

"STID was calculated as a sum of the delta QST Heat scores at each time point until the designated time point. The delta QST Heat score is defined as the change in QST Heat score from baseline. QST Heat scores were the temperature where the sensation of a heat stimuli was felt: ranging from 35 ºC to a maximum of 50.5 ºC with intervals of 0.5 ºC, at a frequency of every 1 minute for the first 5 minutes and then every 5 minutes thereafter until the final 60 minute time point.~The total possible scale range was from -155 ºC (best) to +155 ºC (worst) for STID at the 30 minute time point, and from -248 ºC (best) to +248 ºC (worst) for SPID at the 60 minute time point Lower scores signify a better outcome (less sensitive to pain than at baseline = less pain with therapy = therapy was more effective).~Stage I outcome." (NCT03233737)
Timeframe: Up to one hour post-application

,,
InterventionDegrees Celcius (ºC) (Mean)
STID at the 30 minute time pointSTID at the 60 minute time point
Stage I: One Spray CTY-5339-A153.0320.2
Stage I: One Spray CTY-5339-CB10.426.1
Stage I: One Spray CTY-5339-P72.5134.6

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Stage I: Onset of Anesthesia for Heat Sensation Threshold (QST Heat)

"Onset of anesthesia was defined by Pin Prick Test (PPT) unless specific QST thresholds were not met.~If the PPT Onset was 5 minutes or less, then QST must have been greater than the Baseline QST temperature at 5 minutes by any amount and QST must have been ≥ 3 °C of the Baseline QST at 5 or 10 minutes.~If the PPT Onset was 10 minutes, then QST must have been ≥ 3 °C of the Baseline QST temperature at 10 minutes.~If PPT did not achieve Onset, then QST alone could have achieved onset at either 5 or 10 minutes if QST was greater than the Baseline QST temperature at 5 or 10 minutes by any amount and the QST was ≥ 3 °C of the Baseline QST at 5 or 10 minutes.~QST Heat scores were the temperature where the sensation of a heat stimuli was felt: ranging from 35 ºC to a maximum of 50.5 ºC with intervals of 0.5 ºC, at a frequency of every 1 minute for the first 5 minutes and then every 5 minutes thereafter until the final 60 minute time point.~Stage I outcome." (NCT03233737)
Timeframe: Up to one hour post-application

Interventionminutes (Mean)
Stage I: One Spray CTY-5339-A2.0
Stage I: One Spray CTY-5339-CB0.4
Stage I: One Spray CTY-5339-P0.8

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Stage I: Duration of Minimal Pain for Pin Prick Test (PPT) (≤2 on Numerical Rating Scale Pain Scale)

"Response at a time point is defined as having the PPT average pain score of ≤2. PPT scores were assessed using a 0 (no pain) to 10 (severe pain) Numerical Rating Scale at a frequency of every 1 minute for the first 5 minutes and then every 5 minutes thereafter until the final 60 minute time point.~Stage I outcome." (NCT03233737)
Timeframe: Up to one hour post-application

Interventionminutes (Mean)
Stage I: One Spray CTY-5339-A14.5
Stage I: One Spray CTY-5339-CB2.9
Stage I: One Spray CTY-5339-P0.2

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Stage I: Duration of Anesthesia as Measured by Pin Prick Test (PPT) for One Spray CTY-5339-A Compared to One Spray CTY-5339-CB Compared to One Spray CTY-5339-P (Placebo: Vehicle Control)

"The duration of effect, was defined as the length of time in minutes from onset of anesthesia to the absence of anesthesia.Onset was the time point at which the PPT average pain score was less than the Baseline PPT average score by any amount. Also, in 10 minutes or less, the subject must have had a lower PPT average pain score of ≥ 1 unit than Baseline. Absence of anesthesia was defined as follows: After Onset had been established, absence was the first of two time points with consecutive occurrences of regression of absence of analgesia. Reports of less pain by ≥1 unit than Baseline indicated analgesia; while a report of similar (< 1 unit) or more pain than Baseline indicated regression or absence of analgesia. The minimum onset time was 1 minute. PPT scores were assessed using a 0 (no pain) to 10 (severe pain) Numerical Rating Scale at a frequency of every 1 minute for the first 5 minutes and then every 5 minutes thereafter until the final 60 minute time point.~Stage I outcome." (NCT03233737)
Timeframe: Up to one hour post-application

Interventionminutes (Mean)
Stage I: One Spray CTY-5339-A49.2
Stage I: One Spray CTY-5339-CB21.3
Stage I: One Spray CTY-5339-P25.2

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Stage I: Duration of Anesthesia as Measured by Heat Sensation Threshold (QST Heat) for One Spray CTY-5339-A Compared to One Spray CTY-5339-CB Compared to One Spray CTY-5339-P (Placebo: Vehicle Control)

"The duration of effect, was defined as the time from onset to treatment failure, as measured by QST Heat score. QST Heat scores were the temperature where the sensation of a heat stimuli was felt: ranging from 35 ºC to a maximum of 50.5 ºC with intervals of 0.5 ºC, at a frequency of every 1 minute for the first 5 minutes and then every 5 minutes thereafter until the final 60 minute time point. The QST Heat-based Duration of effect was calculated by the length of time in minutes from onset of anesthesia to the absence of anesthesia where Onset of anesthesia was defined by PPT unless specific QST thresholds were not met. After Onset had been established, absence of analgesia or offset was the first of two time points with consecutive occurrences of regression or absence of analgesia. Reports of QST heat pain temperature by ≥ 3 °C of the Baseline QST indicated analgesia; while a report of similar (<3 °C) than Baseline indicated regression or absence of analgesia. Stage I outcome." (NCT03233737)
Timeframe: Up to one hour post-application

Interventionminutes (Mean)
Stage I: One Spray CTY-5339-A42.5
Stage I: One Spray CTY-5339-CB6.1
Stage I: One Spray CTY-5339-P5

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Stage I: Onset of Anesthesia for Pin Prick Test (PPT)

"Onset of anesthesia was the time point at which the PPT average pain score was less than the Baseline PPT average score by any amount. Also, in 10 minutes or less, the subject must have had a lower PPT average pain score of ≥ 1 unit than the Baseline PPT. Onset was expected to be between 1 and 5 minutes. PPT scores were assessed using a 0 (no pain) to 10 (severe pain) Numerical Rating Scale at a frequency of every 1 minute for the first 5 minutes and then every 5 minutes thereafter until the final 60 minute time point.~Stage I outcome." (NCT03233737)
Timeframe: Up to one hour post-application

Interventionminutes (Mean)
Stage I: One Spray CTY-5339-A1.3
Stage I: One Spray CTY-5339-CB1.2
Stage I: One Spray CTY-5339-P2.8

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Stage II: Percentage of Responders for Pin Prick Test (PPT) at Each Time Point

"Response at at time point is defined as when the PPT average pain score was less than the Baseline PPT average score by any amount. PPT scores were assessed using a 0 (no pain) to 10 (severe pain) Numerical Rating Scale at a frequency of every 1 minute for the first 5 minutes and then every 5 minutes thereafter until the final 60 minute time point.~Stage II outcome." (NCT03233737)
Timeframe: Up to one hour post-application

,
InterventionParticipants (Count of Participants)
Responded to treatment at the 1 minute time pointResponded to treatment at the 2 minute time pointResponded to treatment at the 3 minute time pointResponded to treatment at the 4 minute time pointResponded to treatment at the 5 minute time pointResponded to treatment at the 10 minute time pointResponded to treatment at the 15 minute time pointResponded to treatment at the 20 minute time pointResponded to treatment at the 25 minute time pointResponded to treatment at the 30 minute time pointResponded to treatment at the 35 minute time pointResponded to treatment at the 40 minute time pointResponded to treatment at the 45 minute time pointResponded to treatment at the 50 minute time pointResponded to treatment at the 55 minute time pointResponded to treatment at the 60 minute time point
One Spray CTY-5339-A47505049494949494846433632252019
One Spray CTY-5339-CB46484848494948464542342721202018

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Stage II: Sum of Pain Intensity Differences (SPID) for Pin Prick Test (PPT) (Post-hoc)

"SPID was calculated as a sum of the delta PPT scores at each time point until the designated time point. The delta PPT score is defined as the change in PPT score from baseline. PPT scores were assessed using a 0 (no pain) to 10 (severe pain) Numerical Rating Scale at a frequency of every 1 minute for the first 5 minutes and then every 5 minutes thereafter until the final 60 minute time point.~The total possible scale range was from -100 (best) to +100 (worst) for SPID at the 30 minute time point, and from -160 (best) to +160 (worst) for SPID at the 60 minute time point Lower scores signify a better outcome (less sensitive to pain than at baseline = less pain with therapy = therapy was more effective).~Stage II outcome." (NCT03233737)
Timeframe: Up to one hour post-application

,
Interventionscore (Mean)
SPID at the 30 minute time pointSPID at the 60 minute time point
One Spray CTY-5339-A-85.2-122.6
One Spray CTY-5339-CB-63.2-86.6

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Stage II: Duration of Minimal Pain for Pin Prick Test (PPT) (≤2 on Numerical Rating Scale Pain Scale)

"Response at a time point is defined as having the PPT average pain score of ≤2. PPT scores were assessed using a 0 (no pain) to 10 (severe pain) Numerical Rating Scale at a frequency of every 1 minute for the first 5 minutes and then every 5 minutes thereafter until the final 60 minute time point.~Stage II outcome." (NCT03233737)
Timeframe: Up to one hour post-application

Interventionminutes (Mean)
One Spray CTY-5339-A14.6
One Spray CTY-5339-CB7.4

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Stage II: Onset of Anesthesia for Heat Sensation Threshold (QST Heat)

"Onset of anesthesia was defined by Pin Prick Test (PPT) unless specific QST thresholds were not met.~If the PPT Onset was 5 minutes or less, then QST must have been greater than the Baseline QST temperature at 5 minutes by any amount and QST must have been ≥ 3 °C of the Baseline QST at 5 or 10 minutes.~If the PPT Onset was 10 minutes, then QST must have been ≥ 3 °C of the Baseline QST temperature at 10 minutes.~If PPT did not achieve Onset, then QST alone could have achieved onset at either 5 or 10 minutes if QST was greater than the Baseline QST temperature at 5 or 10 minutes by any amount and the QST was ≥ 3 °C of the Baseline QST at 5 or 10 minutes.~QST Heat scores were the temperature where the sensation of a heat stimuli was felt: ranging from 35 ºC to a maximum of 50.5 ºC with intervals of 0.5 ºC, at a frequency of every 1 minute for the first 5 minutes and then every 5 minutes thereafter until the final 60 minute time point.~Stage II outcome." (NCT03233737)
Timeframe: Up to one hour post-application

Interventionminutes (Mean)
One Spray CTY-5339-A1
One Spray CTY-5339-CB1.3

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Visual Analog Scale Pain Score

Pain score self-rated by patient on 100m Visual Analog Pain scale, minimum value 0, maximum value 100, higher scores equal more pain (worse outcome) (NCT04203225)
Timeframe: Immediately on placement or attempt at placement of first suture

Interventionmm (Mean)
Single LET16
Triple LET16

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Need for Additional Local Anesthetic

Need for additional infiltrated local anesthetic (lidocaine) (NCT04203225)
Timeframe: At any time during suturing procedure, time frame is duration of procedure, generally 10-20 minutes, less than one hour. Determined by chart review immediately after procedure completion.

InterventionParticipants (Count of Participants)
Single LET4
Triple LET5

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Patient Global Satisfaction

"Patient global satisfaction at D1 based on a 5-question questionnaire read by a masked observer.~A question read by a masked observer assessed the patient satisfaction about the overall anesthesia during the surgery: Overall, how satisfied are you with the topical study product used for your local anesthesia during your cataract surgery? It was measured with 5 possible answers (Likert satisfaction scale): Very satisfied (0), Globally satisfied (1), Neither satisfied nor Unsatisfied (2), Globally unsatisfied (3), Very unsatisfied (4). It was measured at Visit 3." (NCT04685538)
Timeframe: day 1 - visit2 (Inclusion visit/Surgery) after the treatment

Interventionscore on a scale (Mean)
Chloroprocaine 3%1.35
Tetracaine 0.5%1.27

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Number of Participants With Abnormalities of the Retina, Macula, or Optic Nerve by Fundoscopy

Modification of the basal status of the assesment. Dilated fundus examination on retina, macula, optic nerve. (NCT04685538)
Timeframe: Visit 1 (Day -90/Day -1) and Visit 4 (Day 8 ± 1 day), up to approximately 102 days

,
InterventionParticipants (Count of Participants)
macula abnormal V1macula abnormal V4optic nerve abnormal V1optic nerve abnormal V4retina abnormal V1retina abnormal V4
Chloroprocaine 3%151316121313
Tetracaine 0.5%161016101112

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Number of Participants in Each Treatment Group With a Successful Surface Anesthesia

Τhe primary endpoint is the number of partecipants in each treatment group with a successful surface anesthesia, without any supplementation at the time point T4 (1 minute after the 3rd drop installation) (NCT04685538)
Timeframe: Before Intra Ocular Lens (IOL) implantation surgery.

,
Interventionparticipants (Number)
Anesthesia SuccessAnesthesia NO Success
Chloroprocaine 3%15314
Tetracaine 0.5%15219

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Intra-ocular Pressure

Modification of the basal status of the assesment. Intraocular pressure (in mmHg) was assessed according to site current practice (air puff or applanation tonometer). (NCT04685538)
Timeframe: Visit 1 (Day -90/Day -1) and Visit 4 (Day 8 ± 1 day), up to approximately 102 days

,
InterventionmmHg (Mean)
visit 1 Selectionvisit 4 Final
Chloroprocaine 3%1514.7
Tetracaine 0.5%1514.88

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Fluoresceine

Modification of the basal status evaluated with fluorescein test Approximately 2-3 minutes following fluorescein instillation, corneal staining was to be evaluated in both eyes, using a slit lamp, based on the Oxford scale (grades of 0-5: 0 is normal, 5 is severe abnormal). (NCT04685538)
Timeframe: Visit 1 (Day -90/Day -1) and Visit 4 (Day 8 ± 1 day), up to approximately 102 days

,
Interventionscore on a scale (Mean)
Corneal Fluorescein Staining visit1Corneal Fluorescein Staining visit4
Chloroprocaine 3%0.210.32
Tetracaine 0.5%0.160.25

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Objective Ocular Signs

- Objective ocular signs assessed by slit lamp examination, flare, and other objective ocular signs will be graded according to the following scale: 0 = none, 1 = mild, 2 = moderate, 3 = severe. The minimum value is 0 and maximum value is 3 (NCT04685538)
Timeframe: Visit 1 (Day -90/Day -1) and Visit 4 (Day 8 ± 1 day), up to approximately 102 days

,
Interventionscore on a scale (Mean)
Anterior Chamber Cells and Flare visit1Anterior Chamber Cells and Flare visit4Chemosis visit1Chemosis visit4
Chloroprocaine 3%00.040.030.09
Tetracaine 0.5%00.030.040.09

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Corneal Thickness

Modification of the basal status of the assesment (Corneal thickness). Measurement of the central corneal thickness was to be performed with a pachymeter (NCT04685538)
Timeframe: Visit 1 (Day -90/Day -1) and Visit 4 (Day 8 ± 1 day), up to approximately 102 days

,
Interventionum (Mean)
visit 1 (Day -90/Day -1)visit 4 (Day 8 ± 1 day)
Chloroprocaine 3%539.59557.8
Tetracaine 0.5%536.59546.54

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Changes in Ocular Symptoms

Changes in ocular symptoms (pain, irritation/burning/stinging, foreign body sensation) will be graded by the patients according to the following scale (0 is the minimum value and 3 is tha maximum value) (0 = absent, 1 = mild, 2 = moderate, 3 = severe) during the study on Visit 1-selection and on visit 4-final (NCT04685538)
Timeframe: Visit 1 (Day -90/Day -1) and Visit 4 (Day 8 ± 1 day), up to approximately 102 days

,
Interventionscore on a scale (Mean)
Foreign Body Sensation visit1Foreign Body Sensation visit4Irritation/Burning/Stinging visit1Irritation/Burning/Stinging visit4pain visit1pain visit4
Chloroprocaine 3%0.080.190.110.110.010.05
Tetracaine 0.5%0.060.170.110.150.010.05

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Best Far Corrected Visual Acuity

Modification of the basal status of the assesment evaluated by LogMAR (Logarithm of the Minimum Angle of Resolution). When using a LogMAR chart, visual acuity is scored with reference to the logarithm of the minimum angle of resolution, as the chart's name suggests. An observer who can resolve details as small as 1 minute of visual angle scores LogMAR 0, since the base-10 logarithm of 1 is 0; an observer who can resolve details as small as 2 minutes of visual angle (i.e., reduced acuity) scores LogMAR 0.3, since the base-10 logarithm of 2 is near-approximately 0.3; and so on. (NCT04685538)
Timeframe: Visit 1 (Day -90/Day -1) and Visit 4 (Day 8 ± 1 day), up to approximately 102 days

,
InterventionLogMAR (Mean)
Best Corrected Visual Acuity LogMAR visit1Best Corrected Visual Acuity LogMAR visit4
Chloroprocaine 3%0.490.12
Tetracaine 0.5%0.470.08

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Surgeon Satisfaction

"Evaluation of surgeon satisfaction. Surgeon satisfaction was assessed through the question How do you consider the study product global tolerance?, at a scale (a score of 0 is the minimum value with the best outcome and 3 is the maximum value with the worst outcome): (0) Very satisfactory, (1) Satisfactory, (2) Not very satisfactory, (3) Unsatisfactory. It is recorded at V2 and filled in by the surgeon who had performed the study. It is measured at Visit 2." (NCT04685538)
Timeframe: day 1 - visit2 (Inclusion visit/Surgery)

Interventionscore on a scale (Mean)
Chloroprocaine 3%0.17
Tetracaine 0.5%0.17

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Endothelial Cell Counts

Modification of the basal status of the Endothelial cell counts evaluated with the specular microscopy (NCT04685538)
Timeframe: Visit 1 (Day -90/Day -1) and Visit 4 (Day 8 ± 1 day), up to approximately 102 days

,
Interventioncell/mm^2 (Mean)
Endothelial Cells Count [cell/mm2] visit1Endothelial Cells Count [cell/mm2] visit4
Chloroprocaine 3%2440.762049.88
Tetracaine 0.5%2511.892166.96

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