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tizanidine

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Description

tizanidine: RN given refers to parent cpd; structure [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

tizanidine : 2,1,3-Benzothiadiazole substituted at C-4 by a Delta(1)-imidazolin-2-ylamino group and at C-4 by a chloro group. It is an agonist at alpha2-adrenergic receptor sites. [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 CID5487
CHEMBL ID1079
CHEBI ID63629
SCHEMBL ID60334
MeSH IDM0081344

Synonyms (77)

Synonym
BIDD:GT0580
chebi:63629 ,
CHEMBL1079 ,
ternelin
sirdalud
5-chloro-n-(4,5-dihydro-1h-imidazol-2-yl)-2,1,3-benzothiadiazol-4-amine
tizanidinum [inn-latin]
2,1,3-benzothiadiazole, 5-chloro-4-(2-imidazolin-2-ylamino)-
tizanidine [inn:ban]
2,1,3-benzothiadiazole-4-amine, 5-chloro-n-(4,5-dihydro-1h-imidazol-2-yl)-
tizanidina [inn-spanish]
brn 0618691
2,1,3-benzothiadiazol-4-amine, 5-chloro-n-(4,5-dihydro-1h-imidazol-2-yl)-
5-chloro-4-(2-imidazolin-2-yl-amino)-2,1,3-benzothiadiazole
51322-75-9
tizanidine
C07452
DB00697
NCGC00160529-01
5-chloro-4-(2-imidazolin-2-ylamino)-2,1,3-benzothiadiazole
NCGC00160529-03
NCGC00160529-02
NCGC00160529-04
HMS2089B03
(5-chloro-benzo[1,2,5]thiadiazol-4-yl)-(4,5-dihydro-1h-imidazol-2-yl)-amine
bdbm50240671
NCGC00160529-05
L001084
sirdalud (tn)
tizanidine (inn)
D08611
FT-0639985
STK711168
tox21_111876
dtxsid9023679 ,
dtxcid203679
cas-51322-75-9
A828535
AKOS005530682
unii-6ai06c00gw
tizanidina
6ai06c00gw ,
tizanidinum
tizanidine [mi]
tizanidine [who-dd]
tizanidine [vandf]
tizanidine [inn]
S5537
gtpl7308
HY-B0194
SCHEMBL60334
AB00698468-04
tox21_111876_1
NCGC00160529-06
AB00698468-06
MLS006011763
smr000857268
n-(5-chloro-2,1,3-benzothiadiazol-4-yl)-n-(4,5-dihydro-1h-imidazol-2-yl)amine #
AB00698468_07
SR-01000765392-2
5-chloro-4-(2-imidazolin-4-on-2-ylamino)-2,1,3-benzothiadiazole
Q423538
F20799
5-chloro-n-(4,5-dihydro-1h-imidazol-2-yl)-benzo[c][1,2,5]thiadiazol-4-amine
BCP12884
BRD-K06335600-003-16-5
5-chloro-4-(2-imidazolin-2-ylamino)benzo-2,1,3-thiadiazole
SDCCGSBI-0633792.P001
NCGC00160529-14
HMS3886K10
HMS3743M03
CCG-266992
tizanidin
tizanidinum (inn-latin)
tizanidina (inn-spanish)
m03bx02
EN300-27019999

Research Excerpts

Overview

Tizanidine is an alpha2-adrenergic agonist, used to treat spasticity associated with multiple sclerosis and spinal injury. The effect mechanism of tizanids in neuropathic pain remains largely unknown. Tizanidine has antispasmodic and antispastic effects.

ExcerptReferenceRelevance
"Tizanidine (TND) is a muscle relaxant having antispasmodic and antispastic effects."( A biophysical approach to study the impact of muscle relaxant drug tizanidine on stability and activity of serum albumins.
Al-Thabaiti, SA; Anand, A; Khan, I; Malik, MA; Patel, R; Sharma, A; Siddiquee, MA; Singh, B; Wani, FA, 2023
)
1.87
"Tizanidine hydrochloride is a skeletal muscle relaxant used for the treatment of spasm, a sudden involuntary muscle contraction leading to pain. "( Microneedle-Mediated Transdermal Delivery of Tizanidine Hydrochloride.
Pandya, K; Patel, B; Thakkar, H, 2020
)
2.26
"Tizanidine hydrochloride is a centrally acting skeletal muscle relaxant used in the treatment of spasticity. "( Development and Stability Control of Pediatric Oral Tizanidine Hydrochloride Formulations for Hospital Use.
Ayres, MV; Balsan, ME; de Almeida, SHO; de Saldanha Simon, E; Garcia, CV; Gobetti, C; Oppe, TP; Wingert, NR, 2020
)
2.25
"Tizanidine is an alpha2-adrenergic agonist, used to treat spasticity associated with multiple sclerosis and spinal injury. "( Physiologically based pharmacokinetic modeling of altered tizanidine systemic exposure by CYP1A2 modulation: Impact of drug-drug interactions and cigarette consumption.
Heimbach, T; Jogiraju, VK; Taft, DR; Toderika, Y, 2021
)
2.31
"Tizanidine is an alpha2 agonist with central action whose myorelaxant effects are often used off-label against primary backpain in clinical practice. "( [Focus on tizanidine in primary care medecine].
Frascarolo, S; Moutinot, B; Sartori, C, 2021
)
2.47
"tizanidine is a highly selective α2-AR agonist, but the effect mechanism of tizanidine in neuropathic pain remains largely unknown."( Tizanidine exerts anti-nociceptive effects in spared nerve injury model of neuropathic pain through inhibition of TLR4/NF-κB pathway.
Li, L; Pei, W; Wang, W; Wei, L; Zhao, Y; Zou, Y, 2018
)
2.64
"Tizanidine HCl is a skeletal muscle relaxant that suffers from extensive hepatic metabolism resulting in 34-40% oral bioavailability. "( Chitosan lactate wafer as a platform for the buccal delivery of tizanidine HCl: in vitro and in vivo performance.
Aboelwafa, AA; El-Gazayerly, ON; El-Mahrouk, GM; Taha, MS, 2014
)
2.08
"Tizanidine is a centrally acting α2-agonist with muscle relaxant properties."( Tizanidine for the management of acute postoperative pain after inguinal hernia repair: A placebo-controlled double-blind trial.
Akkaya, T; Caparlar, C; Kulaçoğlu, H; Mercan, U; Yazicioğlu, D, 2016
)
2.6
"Tizanidine hydrochloride is an α2-adrenergic agonist used for the symptomatic relief of spasticity associated with multiple sclerosis or with spinal cord injury or disease. "( A UHPLC-UV Method to Quantify Skin Deposition and Transdermal Permeation of Tizanidine Hydrochloride.
del Río-Sancho, S; Kalia, YN; López-Castellano, A; Merino, V,
)
1.8
"Tizanidine hydrochloride is a very useful medication in patients suffering from spasticity caused by MS, acquired brain injury or spinal cord injury. "( Update on tizanidine for muscle spasticity and emerging indications.
Garay, E; Malanga, G; Reiter, RD, 2008
)
2.19
"Tizanidine is an imidazoline with central alpha(2)-adrenoceptor agonist activity at both spinal and supraspinal levels, which is indicated as a short-acting drug for the management of spasticity. "( Pediatric safety of tizanidine: clinical adverse event database and retrospective chart assessment.
Chez, M; Henney, HR, 2009
)
2.12
"Tizanidine HCl is an alpha2 adrenergic agonist indicated for treating spasticity due to MS or spinal cord injury."( Nightly sublingual tizanidine HCl in multiple sclerosis: clinical efficacy and safety.
Auriel, E; Karni, A; Vakhapova, V, 2010
)
1.41
"Tizanidine (Zanaflex) is a centrally acting imidazoline muscle relaxant that is structurally similar to clonidine (α(2)-adrenergic agonist) but not to other myorelaxants such as baclofen or benzodiazepines. "( Tizanidine (Zanaflex): a muscle relaxant that may prolong the QT interval by blocking IKr.
Drolet, B; Kaddar, N; Patoine, D; Pilote, S; Simard, C; Vigneault, P, 2012
)
3.26
"Tizanidine hydrochloride is an orally administered prokinetic agent that facilitates or restores motility through-out the length of the gastrointestinal tract. "( Formulation and evaluation of effervescent floating tablets of tizanidine hydrochloride.
Chithaluru, K; Kumar, KK; Ramarao, T; Someshwar, K, 2011
)
2.05
"Tizanidine is an α2-adrenoreceptor agonist that inhibits noradrenaline release and binds to imidazoline receptors."( Tizanidine for alcohol withdrawal treatment.
Bou Khalil, R, 2011
)
2.53
"Tizanidine is an alpha2-adrenergic agonist that inhibits the release of norepinephrine at both the spinal cord and brain, with antinociceptive effects that are independent of the endogenous opioid system. "( Chronic daily headache prophylaxis with tizanidine: a double-blind, placebo-controlled, multicenter outcome study.
Cantrell, DT; Lake, AE; Saper, JR; White, JR; Winner, PK, 2002
)
2.02
"Tizanidine is a clonidine derivative and has the same effects, such as sedation, anxiolysis and analgesic response. "( Effect of oral tizanidine on local-anesthetic infiltration pain during epidural catheterization.
Imanaga, K; Inoue, T; Ogawa, R; Wajima, Z, 2004
)
2.12
"Tizanidine is a centrally acting muscle relaxant with a novel mechanism of action and structurally related to clonidine. "( Retrospective review of Tizanidine (Zanaflex) overdose.
Adamson, LA; Bosse, GM; Spiller, HA, 2004
)
2.07
"Tizanidine is a centrally acting alpha-2 adrenoreceptor agonist widely used in the treatment of spasticity in patients with cerebral or spinal injury, and it is causing drawsiness in some of them. "( [Effects of tizanidine for refractory sleep disturbance in disabled children with spastic quadriplegia].
Cho, K; Fujieda, K; Fukuda, I; Miyamoto, A; Oka, R; Tanaka, H, 2004
)
2.15
"Tizanidine seems to be a useful probe drug for measuring presystemic metabolism by CYP1A2."( Ciprofloxacin greatly increases concentrations and hypotensive effect of tizanidine by inhibiting its cytochrome P450 1A2-mediated presystemic metabolism.
Backman, JT; Granfors, MT; Neuvonen, M; Neuvonen, PJ, 2004
)
1.28
"Tizanidine is an imidazoline central alpha(2)-adrenoceptor agonist widely used to manage spasticity secondary to conditions such as multiple sclerosis (MS), stroke, and spinal cord injury (SCI). "( A practical overview of tizanidine use for spasticity secondary to multiple sclerosis, stroke, and spinal cord injury.
Henney, HR; Kamen, L; Runyan, JD, 2008
)
2.1
"Tizanidine is a well-tolerated and effective drug for symptomatic treatment of spasticity."( A double-blind, placebo-controlled trial of tizanidine in the treatment of spasticity caused by multiple sclerosis. United Kingdom Tizanidine Trial Group.
, 1994
)
1.27
"Tizanidine (TZD) is an alpha-2-adrenergic drug with potential spinal analgesic action and could be a substitute or additive for intrathecal (i.t.) opiates in chronic pain treatment. "( Distribution, tolerability and tissue compatibility of intrathecal tizanidine in the sheep.
Loew, M; Ochs, G; Tonn, J; Toyka, K, 1998
)
1.98
"Tizanidine hydrochloride is an alpha2-adrenergic agonist that inhibits the release and effectiveness of norepinephrine at both central sites (eg, the locus ceruleus) and the spinal cord. "( An open-label dose-titration study of the efficacy and tolerability of tizanidine hydrochloride tablets in the prophylaxis of chronic daily headache.
Lake, AE; Saper, JR; Winner, PK, 2001
)
1.99
"Tizanidine appears to be a promising non-opiate analgesic for intrathecal usage."( Effect of intrathecal tizanidine on antinociception and blood pressure in the rat.
Ivankovich, AD; Kroin, JS; Lubenow, TR; McCarthy, RJ; Penn, RD, 1990
)
1.32

Effects

Tizanidine (TIZ) has long been known to be an alpha 2-adrenoceptor agonist and inhibitor of ASP and GLU release. Early experience with this agent appears to be favourable.

ExcerptReferenceRelevance
"Tizanidine (TIZ) has long been known to be an alpha 2-adrenoceptor agonist and inhibitor of ASP and GLU release."( Effects of tizanidine on morphine physical dependence: attenuation and intensification.
Ariciŏglu, F; Dizdar, Y; Esin, Y; Koyuncuŏglu, H; Uresin, Y, 1992
)
1.39
"Tizanidine has been recently introduced, and early experience with this agent appears to be favourable."( Pharmacotherapy of spasticity: some theoretical and practical considerations.
Rice, GP, 1987
)
0.99

Actions

ExcerptReferenceRelevance
"Tizanidine can cause sedation, which is minimized by dose titration."( Tizanidine in the management of spasticity and musculoskeletal complaints in the palliative care population.
Barton, AE; Smith, HS,
)
2.3

Treatment

Treatment with tizanidine reduced muscle tone significantly, as shown by improved Ashworth scores and increased knee swing amplitude recorded by the pendulum test. Treatment was effective in 60% of the patients.

ExcerptReferenceRelevance
"Tizanidine treatment reduced muscle tone significantly, as shown by improved Ashworth scores and increased knee swing amplitude recorded by the pendulum test, both of which correlated significantly with plasma concentration. "( Relationship of the antispasticity effect of tizanidine to plasma concentration in patients with multiple sclerosis.
Cohen, JA; Francis, GS; Hudson, S; Lindsey, JW; Lynch, SG; Mass, MK; Nance, PW; O'Connor, P; Schapiro, RT; Shellenberger, K; Sheremata, WA; Vollmer, T; Whitham, R, 1997
)
2
"Treatment with tizanidine was carried out with 1 mg/ day in 18 mo-7 yr old children, 2 mg/day in 7-12 yr old children as initial doses, and for those older than 12 yr similar dosing to that in adults. "( [Protocol for tizanidine use in infantile cerebral palsy].
Arroyo Riaño, O; Benavente Valdepeñas, A; Palazón García, R, 2008
)
1.06
"Treatment with tizanidine resulted in a significant improvement in pain intensity (P=0.0375), quality of life (P=0.0001), and physician assessment of disability (P=0.0001)."( Open-label dose-titration safety and efficacy study of tizanidine hydrochloride in the treatment of spasticity associated with chronic stroke.
Dromerick, A; Gelber, DA; Good, DC; Richardson, M; Sergay, S, 2001
)
0.9
"Treatment with tizanidine was effective in 60% of the patients; there were high correlations between spasticity before and after tizanidine administration and the severity of symptoms and also between the degree of improvement in spasticity and in that of the symptoms."( Development of a simple spasticity quantification method: effects of tizanidine on spasticity in patients with sequelae of cerebrovascular disease.
Asanuma, M; Hirata, H; Ogawa, N; Ota, Z; Yamamoto, M; Yamawaki, Y, 1992
)
0.86
"Treatment with tizanidine produced an apparent improvement of mobility in some patients suffering from moderate or marked paresis associated with a marked spasticity of their legs."( Tizanidine versus baclofen in the treatment of spasticity in multiple sclerosis patients.
Hoogstraten, MC; Minderhoud, JM; van der Ploeg, RJ; van Marle, S; vd Burg, W; Vreeling, A, 1988
)
2.06

Toxicity

Tizanidine is primarily metabolized via cytochrome P450 (CYP) 1A2. Medications that inhibit the enzyme will affect the clearance of tizanidine. This could lead to increased plasma concentrations of the drug and potentially serious adverse events.

ExcerptReferenceRelevance
" No serious drug-related adverse events or abnormal biochemistry or haematology were observed in either group."( A multicentre placebo-controlled study in general practice to evaluate the efficacy and safety of tizanidine in acute low-back pain.
Berry, H; Hutchinson, DR,
)
0.35
" The most common adverse events during tizanidine treatment were somnolence, xerostomia, and fatigue."( Efficacy and safety of tizanidine in the treatment of spasticity in patients with spinal cord injury. North American Tizanidine Study Group.
Bugaresti, J; Martinez-Arizala, A; Nance, PW; Shellenberger, K; Sheremata, W, 1994
)
0.87
" No serious adverse events were considered to be drug related."( Open-label dose-titration safety and efficacy study of tizanidine hydrochloride in the treatment of spasticity associated with chronic stroke.
Dromerick, A; Gelber, DA; Good, DC; Richardson, M; Sergay, S, 2001
)
0.56
"Overall, the data suggest that tizanidine is safe and efficacious in the treatment of stroke-related spasticity, preserving muscle strength while reducing muscle tone and painful spasms in affected patients."( Open-label dose-titration safety and efficacy study of tizanidine hydrochloride in the treatment of spasticity associated with chronic stroke.
Dromerick, A; Gelber, DA; Good, DC; Richardson, M; Sergay, S, 2001
)
0.84
"5 million adverse drug reaction (ADR) reports for 8620 drugs/biologics that are listed for 1191 Coding Symbols for Thesaurus of Adverse Reaction (COSTAR) terms of adverse effects."( Assessment of the health effects of chemicals in humans: II. Construction of an adverse effects database for QSAR modeling.
Benz, RD; Contrera, JF; Kruhlak, NL; Matthews, EJ; Weaver, JL, 2004
)
0.32
" The most common adverse events and pharmacodynamic effects are related to plasma concentrations."( A clinically relevant review of tizanidine hydrochloride dose relationships to pharmacokinetics, drug safety and effectiveness in healthy subjects and patients.
Henney, HR; Runyan, JD, 2008
)
0.63
" We compared spontaneous adverse event reports in the Acorda Therapeutics worldwide clinical adverse event database for children (< or = 16 years; n = 99) and adults (>16 years; n = 1153) who had received tizanidine and for whom at least one adverse event was reported, and performed a retrospective chart review of the safety of tizanidine in children (< or = 16 years; n = 76) at a large US pediatric neurology practice."( Pediatric safety of tizanidine: clinical adverse event database and retrospective chart assessment.
Chez, M; Henney, HR, 2009
)
0.86
"The overall safety of tizanidine in the pediatric group appeared good; however, the adverse event profile differed from that in adults."( Pediatric safety of tizanidine: clinical adverse event database and retrospective chart assessment.
Chez, M; Henney, HR, 2009
)
0.99
" Tizanidine-induced adverse effects were examined in 100 patients treated with coadministration of tizanidine and 8 CYP1A2 inhibitors."( [Clinical survey of tizanidine-induced adverse effects--impact of concomitant drugs providing cytochrome P450 1A2 modification--].
Homma, M; Kohda, Y; Matsumoto, S; Momo, K; Sasaki, T, 2013
)
1.62
" We aimed to quantify co-administration of MQAB with interacting drugs and associated adverse drug reactions."( Drug safety of macrolide and quinolone antibiotics in a tertiary care hospital: administration of interacting co-medication and QT prolongation.
Corti, N; Hoppe, L; Kovari, H; Maechler, S; Niedrig, D; Russmann, S, 2016
)
0.43
" Electrocardiographic (ECG) monitoring and associated adverse events were validated in medical records."( Drug safety of macrolide and quinolone antibiotics in a tertiary care hospital: administration of interacting co-medication and QT prolongation.
Corti, N; Hoppe, L; Kovari, H; Maechler, S; Niedrig, D; Russmann, S, 2016
)
0.43
" Forty-four MQAB users had contraindicated co-administrations of simvastatin, atorvastatin, or tizanidine and three of those related adverse drug reactions."( Drug safety of macrolide and quinolone antibiotics in a tertiary care hospital: administration of interacting co-medication and QT prolongation.
Corti, N; Hoppe, L; Kovari, H; Maechler, S; Niedrig, D; Russmann, S, 2016
)
0.65
" However, adverse drug reactions were rarely found, and costs vs."( Drug safety of macrolide and quinolone antibiotics in a tertiary care hospital: administration of interacting co-medication and QT prolongation.
Corti, N; Hoppe, L; Kovari, H; Maechler, S; Niedrig, D; Russmann, S, 2016
)
0.43
" Percentages of improved patients' spasticity scale, mild adverse effect and severe adverse effect were extracted as outcomes."( A mixed treatment comparison on efficacy and safety of treatments for spasticity caused by multiple sclerosis: a systematic review and network meta-analysis.
Fu, X; Li, J; Li, M; Ma, Q; Wang, C; Wang, Y; Wu, H; Yang, W, 2018
)
0.48
" Cannabinoids, tizanidine and diazepam had significantly more mild adverse effect reports than placebo."( A mixed treatment comparison on efficacy and safety of treatments for spasticity caused by multiple sclerosis: a systematic review and network meta-analysis.
Fu, X; Li, J; Li, M; Ma, Q; Wang, C; Wang, Y; Wu, H; Yang, W, 2018
)
0.83
" However, concomitant use of tizanidine with ciprofloxacin, a strong inhibitor of the P450-CYP1A2 cytochrome metabolic pathway of tizanidine, can result in increased tizanidine plasma levels and associated adverse outcomes, particularly hypotension."( Risk of tizanidine-induced adverse events after concomitant exposure to ciprofloxacin: A cohort study in the U.S.
Giannouchos, TV; Gómez-Lumbreras, A; Malone, DC, 2022
)
1.45
" The prevalence of co-administration of drugs with a documented interaction highlights the need for continuous education across providers to avoid the incidence of DDI related adverse events and further complications and to improve patient outcomes."( Risk of tizanidine-induced adverse events after concomitant exposure to ciprofloxacin: A cohort study in the U.S.
Giannouchos, TV; Gómez-Lumbreras, A; Malone, DC, 2022
)
1.16
"Tizanidine is primarily metabolized via cytochrome P450 (CYP) 1A2 and therefore medications that inhibit the enzyme will affect the clearance of tizanidine, leading to increased plasma concentrations of tizanidine and potentially serious adverse events."( A Disproportionality Analysis of Drug-Drug Interactions of Tizanidine and CYP1A2 Inhibitors from the FDA Adverse Event Reporting System (FAERS).
Boyce, RD; Gómez-Lumbreras, A; Horn, J; Malone, DC; Tan, MS; Villa-Zapata, L, 2022
)
2.41
"Our aim was to study the occurrence of adverse events reported in the FDA Adverse Event Reporting System (FAERS) involving the combination of tizanidine and drugs that inhibit the metabolic activity of CYP1A2."( A Disproportionality Analysis of Drug-Drug Interactions of Tizanidine and CYP1A2 Inhibitors from the FDA Adverse Event Reporting System (FAERS).
Boyce, RD; Gómez-Lumbreras, A; Horn, J; Malone, DC; Tan, MS; Villa-Zapata, L, 2022
)
1.17
"A disproportionality analysis of FAERS reports from 2004 quarter 1 through 2020 quarter 3 was conducted to calculate the reporting odds ratio (ROR) of reports mentioning tizanidine in a suspect or interacting role or having any role, a CYP1A2 inhibitor, and the following adverse events: hypotension, bradycardia, syncope, shock, cardiorespiratory arrest, and fall or fracture."( A Disproportionality Analysis of Drug-Drug Interactions of Tizanidine and CYP1A2 Inhibitors from the FDA Adverse Event Reporting System (FAERS).
Boyce, RD; Gómez-Lumbreras, A; Horn, J; Malone, DC; Tan, MS; Villa-Zapata, L, 2022
)
1.16
"A total of 89 reports were identified mentioning tizanidine, at least one CYP1A2 inhibitor, and one of the adverse events of interest."( A Disproportionality Analysis of Drug-Drug Interactions of Tizanidine and CYP1A2 Inhibitors from the FDA Adverse Event Reporting System (FAERS).
Boyce, RD; Gómez-Lumbreras, A; Horn, J; Malone, DC; Tan, MS; Villa-Zapata, L, 2022
)
1.22

Pharmacokinetics

Among nonsmokers, the peak concentration (C(max) and area under concentration-time curve from 0 to infinity [AUC(0-infinity)] of tizanidine did not differ significantly between females and males. The efficiency and duration of action of a single oral dose (8 mg) of tzanidine in patients with spinal cord injuries were determined by studying its antispastic, cardiovascular and sedative effects.

ExcerptReferenceRelevance
"The efficiency and duration of action of a single oral dose (8 mg) of tizanidine in patients with spinal cord injuries were determined by studying its antispastic, cardiovascular and sedative effects along with its pharmacokinetic profile in five tetraplegic and five paraplegic patients."( Pharmacodynamics and pharmacokinetics of the oral antispastic agent tizanidine in patients with spinal cord injury.
Baker, H; Desai, P; el Masri, W; Frankel, HL; Luckitt, J; Mathias, CJ, 1989
)
0.75
" Repeated administration of [14C]tizanidine resulted in no apparent change in pharmacokinetic characteristics."( Pharmacokinetics of orally administered tizanidine in healthy volunteers.
Bhuta, S; Jaffe, JM; Tse, FL, 1987
)
0.82
" All of the calculated steady-state pharmacokinetic parameter changes for baclofen, tizanidine, and its major metabolites were within the 30% criterion."( A controlled pharmacokinetic evaluation of tizanidine and baclofen at steady state.
Groves, L; Novack, GD; Shah, J; Shellenberger, MK, 1999
)
0.79
" Blood samples were collected to determine plasma tizanidine pharmacokinetic profiles, and computerized cognitive function tests were performed that yielded a validated composite score, Power of Attention, an index of sedation."( Effects of food on the single-dose pharmacokinetics/pharmacodynamics of tizanidine capsules and tablets in healthy volunteers.
Henney, HR; Kovelesky, RA; Shah, J; Wesnes, KA, 2006
)
0.82
" A pharmacokinetic mechanism for the cranberry juice-warfarin interaction seems unlikely."( Effects of daily ingestion of cranberry juice on the pharmacokinetics of warfarin, tizanidine, and midazolam--probes of CYP2C9, CYP1A2, and CYP3A4.
Backman, JT; Lilja, JJ; Neuvonen, PJ, 2007
)
0.56
"Among nonsmokers, the peak concentration (C(max)) and area under concentration-time curve from 0 to infinity [AUC(0-infinity)] of tizanidine did not differ significantly between females and males."( Effects of gender and moderate smoking on the pharmacokinetics and effects of the CYP1A2 substrate tizanidine.
Backman, JT; Neuvonen, PJ; Schröder, MT, 2008
)
0.77
" The most common adverse events and pharmacodynamic effects are related to plasma concentrations."( A clinically relevant review of tizanidine hydrochloride dose relationships to pharmacokinetics, drug safety and effectiveness in healthy subjects and patients.
Henney, HR; Runyan, JD, 2008
)
0.63
" pharmacokinetic data on 670 drugs representing, to our knowledge, the largest publicly available set of human clinical pharmacokinetic data."( Trend analysis of a database of intravenous pharmacokinetic parameters in humans for 670 drug compounds.
Lombardo, F; Obach, RS; Waters, NJ, 2008
)
0.35
"5 ng x h/mL), and the half-life (1."( Effects of mexiletine, a CYP1A2 inhibitor, on tizanidine pharmacokinetics and pharmacodynamics.
Homma, M; Inomata, S; Kohda, Y; Momo, K; Osaka, Y; Tanaka, M, 2010
)
0.62
"Based on the pharmacokinetic and statistical results, it was concluded that; Tizanidine PIC® 4 mg tablets is bioequivalent to Sirdalud® 4 mg tablets of Novartis and smoking decreases Cmax and AUC of tizanidine."( Pharmacokinetic comparison of two 4 mg tablet formulations of tizanidine.
Al-Ghazawi, M; Alzoubi, M; Faidi, B, 2013
)
0.86
" The objective of this study was to evaluate the pharmacokinetic profile of tizanidine nasal spray and compare it to the profile of tizanidine oral tablets."( Pharmacokinetic characterization of tizanidine nasal spray, a novel intranasal delivery method for the treatment of skeletal muscle spasm.
Cardì, F; Drago, F; Piazza, C; Salomone, S; Sinagra, T; Urso, V; Vitale, DC, 2013
)
0.89
" The pharmacokinetic parameters of tizanidine in 9 healthy male Japanese subjects were compared with those of Caucasians in previous studies."( Lower metabolic clearance of tizanidine in Japanese subjects.
Homma, M; Kohda, Y; Momo, K, 2013
)
0.96
" The physiologically based pharmacokinetic (PBPK) modeling platform Simcyp® was used to evaluate the impact of CYP1A2 modulation on tizanidine exposure through drug-drug interactions (DDIs) and host-dependent habits (cigarette smoking)."( Physiologically based pharmacokinetic modeling of altered tizanidine systemic exposure by CYP1A2 modulation: Impact of drug-drug interactions and cigarette consumption.
Heimbach, T; Jogiraju, VK; Taft, DR; Toderika, Y, 2021
)
1.07
" Physiologically based pharmacokinetic models were developed for tizanidine, incorporating the PerMCL model and the WSM, respectively, to simulate the interaction of tizanidine with a range of CYP1A2 inhibitors and inducers."( Understanding Interindividual Variability in the Drug Interaction of a Highly Extracted CYP1A2 Substrate Tizanidine: Application of a Permeability-Limited Multicompartment Liver Model in a Population Based Physiologically Based Pharmacokinetic Framework.
Bois, FY; Fisher, C; Gardner, I; Jamei, M; Kilford, P; Pan, X; Zhang, M, 2022
)
1.17

Compound-Compound Interactions

Simcyp was used to evaluate the impact of CYP1A2 modulation on tizanidine exposure through drug-drug interactions (DDIs) and host-dependent habits (cigarette smoking)

ExcerptReferenceRelevance
"Potential drug-drug interactions (pDDIs) are described in various case reports, but few studies have evaluated the impact of specific combinations on a population level."( Analysis of Drug-Drug Interactions in Swiss Claims Data Using Tizanidine and Ciprofloxacin as a Prototypical Contraindicated Combination.
Curkovic, I; Egbring, M; Jödicke, AM; Kullak-Ublick, GA; Neuer, T; Roos, M; Tomka, IT; Zellweger, U, 2018
)
0.72
"To compare extracorporeal shock wave therapy combined with oral medication and an exercise program vs sham treatment with medication and exercise for the treatment of chronic low back pain (CLBP)."( Extracorporeal Shock Wave Therapy Combined With Oral Medication and Exercise for Chronic Low Back Pain: A Randomized Controlled Trial.
Khosrawi, S; Ramezani, M; Taheri, P, 2021
)
0.62
"Extracorporeal shock wave therapy combined with oral medication and exercise was safe and effective in the short-term treatment of chronic low back pain."( Extracorporeal Shock Wave Therapy Combined With Oral Medication and Exercise for Chronic Low Back Pain: A Randomized Controlled Trial.
Khosrawi, S; Ramezani, M; Taheri, P, 2021
)
0.62
" The physiologically based pharmacokinetic (PBPK) modeling platform Simcyp® was used to evaluate the impact of CYP1A2 modulation on tizanidine exposure through drug-drug interactions (DDIs) and host-dependent habits (cigarette smoking)."( Physiologically based pharmacokinetic modeling of altered tizanidine systemic exposure by CYP1A2 modulation: Impact of drug-drug interactions and cigarette consumption.
Heimbach, T; Jogiraju, VK; Taft, DR; Toderika, Y, 2021
)
1.07
" The aim of the current study was to compare the performance of a permeability-limited multicompartment liver (PerMCL) model, which operates as an approximation of the dispersion model, and the well stirred model (WSM) for predicting tizanidine drug-drug interactions (DDIs)."( Understanding Interindividual Variability in the Drug Interaction of a Highly Extracted CYP1A2 Substrate Tizanidine: Application of a Permeability-Limited Multicompartment Liver Model in a Population Based Physiologically Based Pharmacokinetic Framework.
Bois, FY; Fisher, C; Gardner, I; Jamei, M; Kilford, P; Pan, X; Zhang, M, 2022
)
1.12

Bioavailability

The main limitations of the therapeutic effectiveness of tizanidine hydrochloride (TNZ) are its low bioavailability due to its tendency to undergo first-pass metabolism and short biological half-life. The aim of the present investigation was to formulate self-microemulsifying drug delivery system (SMEDDS) tablets to enhance oral bioavailability.

ExcerptReferenceRelevance
" Sirdalud was well absorbed and almost completely metabolized in the five species."( Biological fate of sirdalud in animals and man.
Hirst, DR; Koch, P; von Wartburg, BR, 1989
)
0.28
" Single- and multiple-dose pharmacokinetic studies in healthy volunteers have shown that the relative bioavailability of the modified release formulation is similar to that of conventional tablets and is unaffected by food."( Modified release tizanidine: a review.
Hutchinson, DR,
)
0.47
" Similarly, clinical myotonolytic activity of eperisone would only be expected at high doses unless its functional bioavailability were to be much better in man than in either the mouse or rabbit."( Comparison of the myotonolytic activity of tizanidine, eperisone and afloqualone in mouse and rabbit.
Coward, DM; White, TG,
)
0.39
" Tizanidine was rapidly and almost completely absorbed from the gastrointestinal tract, although the estimated bioavailability was only 21% due to extensive first-pass metabolism."( Pharmacokinetics of orally administered tizanidine in healthy volunteers.
Bhuta, S; Jaffe, JM; Tse, FL, 1987
)
1.45
" Calculated values of clearance and apparent volume of distribution were almost certainly overestimates as it seems probable that the orally-administered drug undergoes significant presystemic elimination (its bioavailability was not determined in the investigation here reported)."( Tizanidine--initial pharmacokinetic studies in patients with spasticity.
Eadie, MJ; Heazlewood, V; Maruff, P; Symoniw, P, 1983
)
1.71
"The quantitative structure-bioavailability relationship of 232 structurally diverse drugs was studied to evaluate the feasibility of constructing a predictive model for the human oral bioavailability of prospective new medicinal agents."( QSAR model for drug human oral bioavailability.
Topliss, JG; Yoshida, F, 2000
)
0.31
" The validated method has been successfully used to analyze human plasma samples for application in pharmacokinetic, bioavailability or bioequivalence studies."( Quantification of tizanidine in human plasma by liquid chromatography coupled to tandem mass spectrometry.
Kandikere, VN; Maurya, S; Mudigonda, K; Nirogi, RV; Shukla, M, 2006
)
0.67
"Oral bioavailability (F) is a product of fraction absorbed (Fa), fraction escaping gut-wall elimination (Fg), and fraction escaping hepatic elimination (Fh)."( Physicochemical space for optimum oral bioavailability: contribution of human intestinal absorption and first-pass elimination.
Chang, G; El-Kattan, A; Miller, HR; Obach, RS; Rotter, C; Steyn, SJ; Troutman, MD; Varma, MV, 2010
)
0.36
" The objective of the present investigation was to develop effervescent floating matrix tablets of tizanidine hydrochloride for prolongation of gastric residence time in order to overcome its low bioavailability (34-40 %) and short biological half life (4."( Formulation and evaluation of effervescent floating tablets of tizanidine hydrochloride.
Chithaluru, K; Kumar, KK; Ramarao, T; Someshwar, K, 2011
)
0.83
" Therefore, the nasal route of administration, which bypasses portal circulation, may increase the bioavailability of tizanidine and, possibly, reduce the time to peak plasma concentration, thereby shorting the latency of therapeutic effect."( Pharmacokinetic characterization of tizanidine nasal spray, a novel intranasal delivery method for the treatment of skeletal muscle spasm.
Cardì, F; Drago, F; Piazza, C; Salomone, S; Sinagra, T; Urso, V; Vitale, DC, 2013
)
0.87
"The bioavailability of the tizanidine intranasal formulation was higher than that of tizanidine oral tablets."( Pharmacokinetic characterization of tizanidine nasal spray, a novel intranasal delivery method for the treatment of skeletal muscle spasm.
Cardì, F; Drago, F; Piazza, C; Salomone, S; Sinagra, T; Urso, V; Vitale, DC, 2013
)
0.96
"A strong need exists for the development of transdermal patch having improved bioavailability at the site of action with fewer side effects at off-target organs."( Fabrication and characterization of matrix type transdermal patches loaded with tizanidine hydrochloride: potential sustained release delivery system.
Katas, H; Rahman, KU; Razzaq, Z; Shahid, N; Siddique, MI; Waqas, MK, 2018
)
0.71
" It has low oral bioavailability and short halflife."( Optimization of Microemulgel for Tizanidine Hydrochloride.
Brahmane, S; Chabukswar, A; Jagdale, S, 2020
)
0.84
"The ATP-binding cassette transporter P-glycoprotein (P-gp) is known to limit both brain penetration and oral bioavailability of many chemotherapy drugs."( A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
Ambudkar, SV; Brimacombe, KR; Chen, L; Gottesman, MM; Guha, R; Hall, MD; Klumpp-Thomas, C; Lee, OW; Lee, TD; Lusvarghi, S; Robey, RW; Shen, M; Tebase, BG, 2019
)
0.51
"The aim of the present investigation was to formulate self-microemulsifying drug delivery system (SMEDDS) tablets to enhance the oral bioavailability of tizanidine hydrochloride."( Development of Solid Self-Microemulsifying System of Tizanidine Hydrochloride for Oral Bioavailability Enhancement: In Vitro and In Vivo Evaluation.
Pramanik, S; Thakkar, H, 2020
)
1.01
" The currently available oral dosage forms exhibit low oral bioavailability due to high first-pass metabolism."( Derma roller mediated transdermal delivery of tizanidine invasomes for the management of skeletal muscle spasms.
Brahmam, B; Chaudhari, P; Dsouza, L; Lewis, SA, 2021
)
0.88
"The main limitations of the therapeutic effectiveness of tizanidine hydrochloride (TNZ) are its low bioavailability due to its tendency to undergo first-pass metabolism and short biological half-life."( Development of Biocompatible Nanoparticles of Tizanidine Hydrochloride in Orodispersible Films:
Dutt, R; Kaushik, D; Mittal, V; Pandey, P; Rahman, MH; Singh, S; Sinha, S; Thapa, S; Verma, R, 2022
)
1.22
" TZN has low oral bioavailability due to extensive first-pass metabolism and is used orally at a dose of 6-24 mg per day."( Chitosan-based buccal mucoadhesive patches to enhance the systemic bioavailability of tizanidine.
Arpa, MD; Cevher, E; Gök, MK; Okur, NÜ; Özgümüş, S, 2023
)
1.13

Dosage Studied

Tizanidine, an alpha(2)-adrenoceptor agonist, is a short-acting drug with larger interpatient variability, and linear pharmacokinetics that is dosage form-dependent. Results suggest that similar to clonidine, a high dosage of tizanalid influences gastric acid secretion and gastric ulcers.

ExcerptRelevanceReference
" Plasma tizanidine levels rose within half an hour after dosing and peaked at one hour."( Pharmacodynamics and pharmacokinetics of the oral antispastic agent tizanidine in patients with spinal cord injury.
Baker, H; Desai, P; el Masri, W; Frankel, HL; Luckitt, J; Mathias, CJ, 1989
)
0.95
" The dosage was optimized corresponding to the clinical symptoms."( [Comparative double-blind study of the effectiveness and tolerance of baclofen, tetrazepam and tizanidine in spastic movement disorders of the lower extremities].
Paulig, M; Pellkofer, M, 1989
)
0.5
" The dosage of tizanidine used ranged from 6 to 18 mg/day."( Modified release tizanidine in the treatment of spasticity.
Chantraine, A; Van Ouwenaller, C,
)
0.82
" Dosage was increased progressively, if tolerated, to a maximum of 24 mg tizanidine or 30 mg diazepam per day at the end of 2 weeks."( A multi-centre, double-blind trial of tizanidine, a new antispastic agent, in spasticity associated with hemiplegia.
Bes, A; Eyssette, M; Pierrot-Deseilligny, E; Rohmer, F; Warter, JM, 1988
)
0.78
" Neither the maximal clinical dosage of tizanidine (3 mg) nor twice that dosage (6 mg) induced any marked somatic or psychic symptoms compared with the placebo."( Effects of tizanidine in healthy volunteers: double-blind study compared with diazepam and a placebo.
Igarashi, S; Yamamura, H; Yanagita, T, 1988
)
0.93
" Relief of spasticity, from the dosage used, was relatively slight and appeared greatest at the time of peak plasma levels of the drug."( Tizanidine--initial pharmacokinetic studies in patients with spasticity.
Eadie, MJ; Heazlewood, V; Maruff, P; Symoniw, P, 1983
)
1.71
" These results suggest that similar to clonidine, a high dosage of tizanidine influences gastric acid secretion and gastric ulcers, although the activity is lower than that of clonidine."( [Influence of a muscle relaxant, tizanidine, on gastric acid secretion and gastric ulcer in rats].
Kanaoka, R; Maeda-Hagiwara, M; Watanabe, H; Watanabe, K, 1983
)
0.78
" The study consisted of 4 parts: I, double-blind cross-over trial at maximal dosage 10 mg/day in 13 patients; II, open trial at maximal dosage 32 mg/day in 10 patients; III, long-term medication at dosage 32 mg/day for 6-15 months in 4 patients; IV, single dose (12 mg) administration in 3 patients."( Antiparetic and antispastic effects induced by tizanidine in patients with spastic paresis.
Gransberg, L; Knutsson, E; Mårtensson, A, 1982
)
0.52
"0123) linear dose-response relation between single doses and antispastic action of tizanidine."( Correlations between dose, plasma concentrations, and antispastic action of tizanidine (Sirdalud).
Emre, M; Leslie, GC; Muir, C; Part, NJ; Pokorny, R; Roberts, RC, 1994
)
0.74
" All efficacy parameters were evaluated by the physician/assessor, and the physician/prescriber was responsible for all dosage adjustments."( Tizanidine treatment of spasticity caused by multiple sclerosis: results of a double-blind, placebo-controlled trial. US Tizanidine Study Group.
Birnbaum, G; Carter, JL; Greenstein, J; Lublin, FD; Smith, C, 1994
)
1.73
" Tizanidine was titrated to an optimized dosage in each patient to a maximum of 36 mg/d."( Efficacy and safety of tizanidine in the treatment of spasticity in patients with spinal cord injury. North American Tizanidine Study Group.
Bugaresti, J; Martinez-Arizala, A; Nance, PW; Shellenberger, K; Sheremata, W, 1994
)
1.51
" Dose-response curves were plotted for suppression of paw withdrawal 30 minutes after intrathecal injection of various doses of tizanidine, clonidine, and octreotide."( Effects of intrathecal nonnarcotic analgesics on chronic tactile allodynia in rats: alpha 2-agonists versus somatostatin analog.
Kroin, JS; Ono, N; Paice, JA; Penn, RD, 1997
)
0.5
" Wide interpatient variability in the effective plasma concentrations of tizanidine means that the optimal dosage must be titrated over 2 to 4 weeks for each patient (dosages of 2 to 36 mg/day have been used in clinical trials)."( Tizanidine. A review of its pharmacology, clinical efficacy and tolerability in the management of spasticity associated with cerebral and spinal disorders.
Bryson, HM; Wagstaff, AJ, 1997
)
1.97
"A randomized, double-blind, placebo-controlled, dose-response study of tizanidine hydrochloride (8 or 16 mg)."( Relationship of the antispasticity effect of tizanidine to plasma concentration in patients with multiple sclerosis.
Cohen, JA; Francis, GS; Hudson, S; Lindsey, JW; Lynch, SG; Mass, MK; Nance, PW; O'Connor, P; Schapiro, RT; Shellenberger, K; Sheremata, WA; Vollmer, T; Whitham, R, 1997
)
0.79
" Concentrations of tizanidine and baclofen were nearly identical during the single and concomitant dosing periods."( A controlled pharmacokinetic evaluation of tizanidine and baclofen at steady state.
Groves, L; Novack, GD; Shah, J; Shellenberger, MK, 1999
)
0.89
" Dosing was titrated from 2 mg at bedtime to a median daily dose of 14 mg (mean, 13."( An open-label dose-titration study of the efficacy and tolerability of tizanidine hydrochloride tablets in the prophylaxis of chronic daily headache.
Lake, AE; Saper, JR; Winner, PK, 2001
)
0.54
" Ten of 47 patients (21%) were able to reach the maximum daily dosage of 36 mg."( Open-label dose-titration safety and efficacy study of tizanidine hydrochloride in the treatment of spasticity associated with chronic stroke.
Dromerick, A; Gelber, DA; Good, DC; Richardson, M; Sergay, S, 2001
)
0.56
" The average dosage at 4 weeks was 25."( Prospective assessment of tizanidine for spasticity due to acquired brain injury.
Brunner, RM; Guin-Renfroe, S; Johnson, A; Meythaler, JM, 2001
)
0.61
" The analysis of variance (ANOVA) and Student's t-test were applied to correlate the results of tizanidine and rofecoxib determination in dosage form by means of HPTLC and HPLC method."( Application of HPLC and HPTLC for the simultaneous determination of tizanidine and rofecoxib in pharmaceutical dosage form.
Agrawal, H; Dhaneshwar, SR; Kakad, A; Kaul, N; Patil, B, 2005
)
0.78
" The designed system is able to maintain plasma concentration without the need of frequent dosing and reduce side effects unlike in case of conventional dosage form."( In-vitro studies of tizanidine controlled-release microcapsular matrices.
Dashora, K; Saraf, S, 2006
)
0.66
" Careful dosing of tizanidine is warranted in small females, whereas male smokers can require higher than average doses."( Effects of gender and moderate smoking on the pharmacokinetics and effects of the CYP1A2 substrate tizanidine.
Backman, JT; Neuvonen, PJ; Schröder, MT, 2008
)
0.89
"Tizanidine, an alpha(2)-adrenoceptor agonist, is a short-acting drug with larger interpatient variability, and linear pharmacokinetics that is dosage form-dependent."( A practical overview of tizanidine use for spasticity secondary to multiple sclerosis, stroke, and spinal cord injury.
Henney, HR; Kamen, L; Runyan, JD, 2008
)
2.1
"Tizanidine, one of the few oral antispastic therapies approved for use in the USA, has a narrow therapeutic index that can often make optimal patient dosing difficult."( A clinically relevant review of tizanidine hydrochloride dose relationships to pharmacokinetics, drug safety and effectiveness in healthy subjects and patients.
Henney, HR; Runyan, JD, 2008
)
2.07
" Practical advice on tizanidine dosing and/or switching between formulations is provided."( A clinically relevant review of tizanidine hydrochloride dose relationships to pharmacokinetics, drug safety and effectiveness in healthy subjects and patients.
Henney, HR; Runyan, JD, 2008
)
0.95
"Scheduled medical uses and dosing of tizanidine in our hospital are shown."( [Protocol for tizanidine use in infantile cerebral palsy].
Arroyo Riaño, O; Benavente Valdepeñas, A; Palazón García, R, 2008
)
0.98
"Treatment with tizanidine was carried out with 1 mg/ day in 18 mo-7 yr old children, 2 mg/day in 7-12 yr old children as initial doses, and for those older than 12 yr similar dosing to that in adults."( [Protocol for tizanidine use in infantile cerebral palsy].
Arroyo Riaño, O; Benavente Valdepeñas, A; Palazón García, R, 2008
)
1.06
"The objective of this study was to formulate stable and controlled release microparticles for simultaneous delivery and UV spectrophotometric detection in combined dosage of an non-steroidal anti-inflammatory drug (NSAID) (nimesulide, NMS) and a spasmolytic agent (tizanidine, TZN) to maintain plasma concentration that may increase patients compliance, improved therapeutic efficacy, The aim was also to reduce severity of upper GI side effects of NMS because of alteration in delivery pattern via slow release of drug from microparticles and to increase the benefits of spasticity and disability for spastic patients by administering TZN in a modified release formulation as these two drugs are often prescribed in combination for the management of pain associated with muscles spasm."( Formulation of two-drug controlled release non-biodegradable microparticles for potential treatment of muscles pain and spasm and their simultaneous spectrophotometeric estimation.
Aamir, MN; Ahmad, M; Akhtar, N; Khan, SA; Kousar, R; Murtaza, G,
)
0.31
" To reduce muscle tension, 34 patients of the main group received tizanidine with the modified release of active substance (sirdalud MR) in dosage one capsule (6 mg) per day."( [The use of sirdalud MR in patients with multiple sclerosis].
Batysheva, TT; Boĭko, AN; Kamchatnov, PR; Petrov, SV; Popova, NF; Zaĭtsev, KA, 2010
)
0.6
"This study was conducted to assess the effects of various excipients in 10 different Tizanidine hydrochloride tablet dosage forms that were prepared by direct compression method (DC)."( Effects of various excipients on tizanidine hydrochloride tablets prepared by direct compression.
Anjum, F; Ghayas, S; Khan, LG; Razvi, N; Siddiqui, SA, 2014
)
0.91
" The drug should be gradually reduced in dosage under observation by a psychiatrist."( [Tizanidine withdrawal symptoms in stress cardiomyopathy].
Bayer, D; Bengesser, SA; Kapfhammer, HP; Mörkl, S; Schöggl, H, 2015
)
1.33
" Following botulinum toxin A treatment, clinical improvement led to the gradual reduction of baclofen or tizanidine dosing to one-third of the former dose."( Comparison of Efficacy and Side Effects of Oral Baclofen Versus Tizanidine Therapy with Adjuvant Botulinum Toxin Type A in Children With Cerebral Palsy and Spastic Equinus Foot Deformity.
Aksoy, SN; Dai, AI; Demiryürek, AT, 2016
)
0.89
" The proposed method was validated according to the ICH guidelines and was successfully applied to the analysis of these drugs in their tablet dosage forms with high accuracy."( Simultaneous Determination of Tizanidine, Nimesulide, Aceclofenac and Paracetamol in Tablets and Biological Fluids Using Micellar Liquid Chromatography.
Belal, F; Derayea, S; Hammad, MA; Omar, MA; Saleh, SF; Zayed, S, 2018
)
0.77
" The presently available oral dosage form has limitations such as high first pass metabolism resulting in low oral bioavailability."( Microneedle-Mediated Transdermal Delivery of Tizanidine Hydrochloride.
Pandya, K; Patel, B; Thakkar, H, 2020
)
0.82
" The currently available oral dosage forms exhibit low oral bioavailability due to high first-pass metabolism."( Derma roller mediated transdermal delivery of tizanidine invasomes for the management of skeletal muscle spasms.
Brahmam, B; Chaudhari, P; Dsouza, L; Lewis, SA, 2021
)
0.88
"The fast-dissolving film of TNZ HCl was prepared by the solvent-casting method and characterized using scanning electron microscopy, FTIR, and XRD, and evaluated for critical quality attributes for this type of dosage form such as disintegration time, tensile strength, drug content, dissolution, and ex vivo permeability."( Development of Biocompatible Nanoparticles of Tizanidine Hydrochloride in Orodispersible Films:
Dutt, R; Kaushik, D; Mittal, V; Pandey, P; Rahman, MH; Singh, S; Sinha, S; Thapa, S; Verma, R, 2022
)
0.98
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Roles (2)

RoleDescription
alpha-adrenergic agonistAn agent that selectively binds to and activates alpha-adrenergic receptors.
muscle relaxantA drug used to produce muscle relaxation (excepting neuromuscular blocking agents). Its primary clinical and therapeutic use is the treatment of muscle spasm and immobility associated with strains, sprains, and injuries of the back and, to a lesser degree, injuries to the neck. Also used for the treatment of a variety of clinical conditions that have in common only the presence of skeletal muscle hyperactivity, for example, the muscle spasms that can occur in multiple sclerosis.
[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
benzothiadiazole
imidazolesA five-membered organic heterocycle containing two nitrogen atoms at positions 1 and 3, or any of its derivatives; compounds containing an imidazole skeleton.
[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 (27)

Potency Measurements

ProteinTaxonomyMeasurementAverage (µ)Min (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Chain A, MAJOR APURINIC/APYRIMIDINIC ENDONUCLEASEHomo sapiens (human)Potency15.84890.003245.467312,589.2998AID2517
RAR-related orphan receptor gammaMus musculus (house mouse)Potency1.49600.006038.004119,952.5996AID1159521
ATAD5 protein, partialHomo sapiens (human)Potency8.75560.004110.890331.5287AID493106; AID493107
AR proteinHomo sapiens (human)Potency26.60320.000221.22318,912.5098AID743040
regulator of G-protein signaling 4Homo sapiens (human)Potency21.37920.531815.435837.6858AID504845
EWS/FLI fusion proteinHomo sapiens (human)Potency0.52580.001310.157742.8575AID1259252
glucocorticoid receptor [Homo sapiens]Homo sapiens (human)Potency8.48520.000214.376460.0339AID720691
retinoic acid nuclear receptor alpha variant 1Homo sapiens (human)Potency15.84650.003041.611522,387.1992AID1159555
cytochrome P450 2D6Homo sapiens (human)Potency17.37680.00108.379861.1304AID1645840
arylsulfatase AHomo sapiens (human)Potency37.93301.069113.955137.9330AID720538
euchromatic histone-lysine N-methyltransferase 2Homo sapiens (human)Potency22.38720.035520.977089.1251AID504332
activating transcription factor 6Homo sapiens (human)Potency13.44810.143427.612159.8106AID1159516
chromobox protein homolog 1Homo sapiens (human)Potency31.62280.006026.168889.1251AID488953
nuclear factor erythroid 2-related factor 2 isoform 1Homo sapiens (human)Potency37.57510.000627.21521,122.0200AID743202
nuclear receptor ROR-gamma isoform 1Mus musculus (house mouse)Potency35.48130.00798.23321,122.0200AID2546
peripheral myelin protein 22Rattus norvegicus (Norway rat)Potency12.57970.005612.367736.1254AID624044
lamin isoform A-delta10Homo sapiens (human)Potency25.11890.891312.067628.1838AID1487
ATP-dependent phosphofructokinaseTrypanosoma brucei brucei TREU927Potency0.75690.060110.745337.9330AID485368
[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)
ATP-binding cassette sub-family C member 3Homo sapiens (human)IC50 (µMol)133.00000.63154.45319.3000AID1473740
Multidrug resistance-associated protein 4Homo sapiens (human)IC50 (µMol)133.00000.20005.677410.0000AID1473741
Bile salt export pumpHomo sapiens (human)IC50 (µMol)134.00000.11007.190310.0000AID1443980; AID1473738
Canalicular multispecific organic anion transporter 1Homo sapiens (human)IC50 (µMol)133.00002.41006.343310.0000AID1473739
NischarinHomo sapiens (human)Ki0.02830.00420.21923.8019AID342861
[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)
Alpha-1B adrenergic receptor Cricetulus griseus (Chinese hamster)EC50 (µMol)0.32200.01000.34440.9430AID1342011
Alpha-2A adrenergic receptorHomo sapiens (human)EC50 (µMol)0.08600.00080.37336.7100AID1342005
Alpha-1A adrenergic receptorBos taurus (cattle)EC50 (µMol)0.26400.00900.37401.1320AID1342009
Alpha-2C adrenergic receptorHomo sapiens (human)EC50 (µMol)1.23100.00050.55416.7100AID1342007
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (91)

Processvia Protein(s)Taxonomy
xenobiotic metabolic processATP-binding cassette sub-family C member 3Homo sapiens (human)
xenobiotic transmembrane transportATP-binding cassette sub-family C member 3Homo sapiens (human)
bile acid and bile salt transportATP-binding cassette sub-family C member 3Homo sapiens (human)
glucuronoside transportATP-binding cassette sub-family C member 3Homo sapiens (human)
xenobiotic transportATP-binding cassette sub-family C member 3Homo sapiens (human)
transmembrane transportATP-binding cassette sub-family C member 3Homo sapiens (human)
leukotriene transportATP-binding cassette sub-family C member 3Homo sapiens (human)
monoatomic anion transmembrane transportATP-binding cassette sub-family C member 3Homo sapiens (human)
transport across blood-brain barrierATP-binding cassette sub-family C member 3Homo sapiens (human)
prostaglandin secretionMultidrug resistance-associated protein 4Homo sapiens (human)
cilium assemblyMultidrug resistance-associated protein 4Homo sapiens (human)
platelet degranulationMultidrug resistance-associated protein 4Homo sapiens (human)
xenobiotic metabolic processMultidrug resistance-associated protein 4Homo sapiens (human)
xenobiotic transmembrane transportMultidrug resistance-associated protein 4Homo sapiens (human)
bile acid and bile salt transportMultidrug resistance-associated protein 4Homo sapiens (human)
prostaglandin transportMultidrug resistance-associated protein 4Homo sapiens (human)
urate transportMultidrug resistance-associated protein 4Homo sapiens (human)
glutathione transmembrane transportMultidrug resistance-associated protein 4Homo sapiens (human)
transmembrane transportMultidrug resistance-associated protein 4Homo sapiens (human)
cAMP transportMultidrug resistance-associated protein 4Homo sapiens (human)
leukotriene transportMultidrug resistance-associated protein 4Homo sapiens (human)
monoatomic anion transmembrane transportMultidrug resistance-associated protein 4Homo sapiens (human)
export across plasma membraneMultidrug resistance-associated protein 4Homo sapiens (human)
transport across blood-brain barrierMultidrug resistance-associated protein 4Homo sapiens (human)
guanine nucleotide transmembrane transportMultidrug resistance-associated protein 4Homo 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)
positive regulation of cytokine productionAlpha-2A adrenergic receptorHomo sapiens (human)
DNA replicationAlpha-2A adrenergic receptorHomo sapiens (human)
G protein-coupled receptor signaling pathwayAlpha-2A adrenergic receptorHomo sapiens (human)
adenylate cyclase-activating G protein-coupled receptor signaling pathwayAlpha-2A adrenergic receptorHomo sapiens (human)
adenylate cyclase-inhibiting G protein-coupled receptor signaling pathwayAlpha-2A adrenergic receptorHomo sapiens (human)
Ras protein signal transductionAlpha-2A adrenergic receptorHomo sapiens (human)
Rho protein signal transductionAlpha-2A adrenergic receptorHomo sapiens (human)
female pregnancyAlpha-2A adrenergic receptorHomo sapiens (human)
positive regulation of cell population proliferationAlpha-2A adrenergic receptorHomo sapiens (human)
negative regulation of norepinephrine secretionAlpha-2A adrenergic receptorHomo sapiens (human)
regulation of vasoconstrictionAlpha-2A adrenergic receptorHomo sapiens (human)
actin cytoskeleton organizationAlpha-2A adrenergic receptorHomo sapiens (human)
platelet activationAlpha-2A adrenergic receptorHomo sapiens (human)
positive regulation of cell migrationAlpha-2A adrenergic receptorHomo sapiens (human)
activation of protein kinase activityAlpha-2A adrenergic receptorHomo sapiens (human)
activation of protein kinase B activityAlpha-2A adrenergic receptorHomo sapiens (human)
negative regulation of epinephrine secretionAlpha-2A adrenergic receptorHomo sapiens (human)
cellular response to hormone stimulusAlpha-2A adrenergic receptorHomo sapiens (human)
receptor transactivationAlpha-2A adrenergic receptorHomo sapiens (human)
vasodilationAlpha-2A adrenergic receptorHomo sapiens (human)
glucose homeostasisAlpha-2A adrenergic receptorHomo sapiens (human)
fear responseAlpha-2A adrenergic receptorHomo sapiens (human)
positive regulation of potassium ion transportAlpha-2A adrenergic receptorHomo sapiens (human)
positive regulation of MAP kinase activityAlpha-2A adrenergic receptorHomo sapiens (human)
positive regulation of MAPK cascadeAlpha-2A adrenergic receptorHomo sapiens (human)
positive regulation of epidermal growth factor receptor signaling pathwayAlpha-2A adrenergic receptorHomo sapiens (human)
negative regulation of calcium ion-dependent exocytosisAlpha-2A adrenergic receptorHomo sapiens (human)
negative regulation of insulin secretionAlpha-2A adrenergic receptorHomo sapiens (human)
intestinal absorptionAlpha-2A adrenergic receptorHomo sapiens (human)
thermoceptionAlpha-2A adrenergic receptorHomo sapiens (human)
negative regulation of lipid catabolic processAlpha-2A adrenergic receptorHomo sapiens (human)
positive regulation of membrane protein ectodomain proteolysisAlpha-2A adrenergic receptorHomo sapiens (human)
negative regulation of calcium ion transportAlpha-2A adrenergic receptorHomo sapiens (human)
negative regulation of insulin secretion involved in cellular response to glucose stimulusAlpha-2A adrenergic receptorHomo sapiens (human)
negative regulation of uterine smooth muscle contractionAlpha-2A adrenergic receptorHomo sapiens (human)
adrenergic receptor signaling pathwayAlpha-2A adrenergic receptorHomo sapiens (human)
adenylate cyclase-activating adrenergic receptor signaling pathwayAlpha-2A adrenergic receptorHomo sapiens (human)
adenylate cyclase-inhibiting adrenergic receptor signaling pathwayAlpha-2A adrenergic receptorHomo sapiens (human)
phospholipase C-activating adrenergic receptor signaling pathwayAlpha-2A adrenergic receptorHomo sapiens (human)
positive regulation of wound healingAlpha-2A adrenergic receptorHomo sapiens (human)
presynaptic modulation of chemical synaptic transmissionAlpha-2A adrenergic receptorHomo sapiens (human)
negative regulation of calcium ion transmembrane transporter activityAlpha-2A adrenergic receptorHomo sapiens (human)
regulation of vasoconstrictionAlpha-1A adrenergic receptorBos taurus (cattle)
positive regulation of MAPK cascadeAlpha-1A adrenergic receptorBos taurus (cattle)
regulation of cardiac muscle contractionAlpha-1A adrenergic receptorBos taurus (cattle)
regulation of smooth muscle contractionAlpha-2C adrenergic receptorHomo sapiens (human)
G protein-coupled receptor signaling pathwayAlpha-2C adrenergic receptorHomo sapiens (human)
cell-cell signalingAlpha-2C adrenergic receptorHomo sapiens (human)
negative regulation of norepinephrine secretionAlpha-2C adrenergic receptorHomo sapiens (human)
regulation of vasoconstrictionAlpha-2C adrenergic receptorHomo sapiens (human)
platelet activationAlpha-2C adrenergic receptorHomo sapiens (human)
activation of protein kinase B activityAlpha-2C adrenergic receptorHomo sapiens (human)
negative regulation of epinephrine secretionAlpha-2C adrenergic receptorHomo sapiens (human)
receptor transactivationAlpha-2C adrenergic receptorHomo sapiens (human)
positive regulation of MAPK cascadeAlpha-2C adrenergic receptorHomo sapiens (human)
positive regulation of neuron differentiationAlpha-2C adrenergic receptorHomo sapiens (human)
adrenergic receptor signaling pathwayAlpha-2C adrenergic receptorHomo sapiens (human)
adenylate cyclase-activating adrenergic receptor signaling pathwayAlpha-2C adrenergic receptorHomo sapiens (human)
negative regulation of insulin secretionAlpha-2C adrenergic receptorHomo sapiens (human)
xenobiotic metabolic processCanalicular multispecific organic anion transporter 1Homo sapiens (human)
xenobiotic transmembrane transportCanalicular multispecific organic anion transporter 1Homo sapiens (human)
negative regulation of gene expressionCanalicular multispecific organic anion transporter 1Homo sapiens (human)
bile acid and bile salt transportCanalicular multispecific organic anion transporter 1Homo sapiens (human)
bilirubin transportCanalicular multispecific organic anion transporter 1Homo sapiens (human)
heme catabolic processCanalicular multispecific organic anion transporter 1Homo sapiens (human)
xenobiotic export from cellCanalicular multispecific organic anion transporter 1Homo sapiens (human)
transmembrane transportCanalicular multispecific organic anion transporter 1Homo sapiens (human)
transepithelial transportCanalicular multispecific organic anion transporter 1Homo sapiens (human)
leukotriene transportCanalicular multispecific organic anion transporter 1Homo sapiens (human)
monoatomic anion transmembrane transportCanalicular multispecific organic anion transporter 1Homo sapiens (human)
transport across blood-brain barrierCanalicular multispecific organic anion transporter 1Homo sapiens (human)
xenobiotic transport across blood-brain barrierCanalicular multispecific organic anion transporter 1Homo sapiens (human)
apoptotic processNischarinHomo sapiens (human)
Rac protein signal transductionNischarinHomo sapiens (human)
actin cytoskeleton organizationNischarinHomo sapiens (human)
negative regulation of cell migrationNischarinHomo sapiens (human)
outer dynein arm assemblyNischarinHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (41)

Processvia Protein(s)Taxonomy
ATP bindingATP-binding cassette sub-family C member 3Homo sapiens (human)
ABC-type xenobiotic transporter activityATP-binding cassette sub-family C member 3Homo sapiens (human)
glucuronoside transmembrane transporter activityATP-binding cassette sub-family C member 3Homo sapiens (human)
ABC-type glutathione S-conjugate transporter activityATP-binding cassette sub-family C member 3Homo sapiens (human)
ABC-type bile acid transporter activityATP-binding cassette sub-family C member 3Homo sapiens (human)
ATP hydrolysis activityATP-binding cassette sub-family C member 3Homo sapiens (human)
ATPase-coupled transmembrane transporter activityATP-binding cassette sub-family C member 3Homo sapiens (human)
xenobiotic transmembrane transporter activityATP-binding cassette sub-family C member 3Homo sapiens (human)
ATPase-coupled inorganic anion transmembrane transporter activityATP-binding cassette sub-family C member 3Homo sapiens (human)
icosanoid transmembrane transporter activityATP-binding cassette sub-family C member 3Homo sapiens (human)
ABC-type transporter activityATP-binding cassette sub-family C member 3Homo sapiens (human)
guanine nucleotide transmembrane transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
protein bindingMultidrug resistance-associated protein 4Homo sapiens (human)
ATP bindingMultidrug resistance-associated protein 4Homo sapiens (human)
ABC-type xenobiotic transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
prostaglandin transmembrane transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
urate transmembrane transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
purine nucleotide transmembrane transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
ABC-type glutathione S-conjugate transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
ABC-type bile acid transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
efflux transmembrane transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
15-hydroxyprostaglandin dehydrogenase (NAD+) activityMultidrug resistance-associated protein 4Homo sapiens (human)
ATP hydrolysis activityMultidrug resistance-associated protein 4Homo sapiens (human)
glutathione transmembrane transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
ATPase-coupled transmembrane transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
xenobiotic transmembrane transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
ATPase-coupled inorganic anion transmembrane transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
ABC-type transporter activityMultidrug resistance-associated protein 4Homo 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)
alpha2-adrenergic receptor activityAlpha-2A adrenergic receptorHomo sapiens (human)
protein bindingAlpha-2A adrenergic receptorHomo sapiens (human)
protein kinase bindingAlpha-2A adrenergic receptorHomo sapiens (human)
alpha-1B adrenergic receptor bindingAlpha-2A adrenergic receptorHomo sapiens (human)
alpha-2C adrenergic receptor bindingAlpha-2A adrenergic receptorHomo sapiens (human)
thioesterase bindingAlpha-2A adrenergic receptorHomo sapiens (human)
heterotrimeric G-protein bindingAlpha-2A adrenergic receptorHomo sapiens (human)
protein homodimerization activityAlpha-2A adrenergic receptorHomo sapiens (human)
protein heterodimerization activityAlpha-2A adrenergic receptorHomo sapiens (human)
epinephrine bindingAlpha-2A adrenergic receptorHomo sapiens (human)
norepinephrine bindingAlpha-2A adrenergic receptorHomo sapiens (human)
guanyl-nucleotide exchange factor activityAlpha-2A adrenergic receptorHomo sapiens (human)
protein heterodimerization activityAlpha-1A adrenergic receptorBos taurus (cattle)
alpha2-adrenergic receptor activityAlpha-2C adrenergic receptorHomo sapiens (human)
protein bindingAlpha-2C adrenergic receptorHomo sapiens (human)
alpha-2A adrenergic receptor bindingAlpha-2C adrenergic receptorHomo sapiens (human)
protein homodimerization activityAlpha-2C adrenergic receptorHomo sapiens (human)
protein heterodimerization activityAlpha-2C adrenergic receptorHomo sapiens (human)
epinephrine bindingAlpha-2C adrenergic receptorHomo sapiens (human)
guanyl-nucleotide exchange factor activityAlpha-2C adrenergic receptorHomo sapiens (human)
protein bindingCanalicular multispecific organic anion transporter 1Homo sapiens (human)
ATP bindingCanalicular multispecific organic anion transporter 1Homo sapiens (human)
organic anion transmembrane transporter activityCanalicular multispecific organic anion transporter 1Homo sapiens (human)
ABC-type xenobiotic transporter activityCanalicular multispecific organic anion transporter 1Homo sapiens (human)
bilirubin transmembrane transporter activityCanalicular multispecific organic anion transporter 1Homo sapiens (human)
ABC-type glutathione S-conjugate transporter activityCanalicular multispecific organic anion transporter 1Homo sapiens (human)
ATP hydrolysis activityCanalicular multispecific organic anion transporter 1Homo sapiens (human)
ATPase-coupled transmembrane transporter activityCanalicular multispecific organic anion transporter 1Homo sapiens (human)
xenobiotic transmembrane transporter activityCanalicular multispecific organic anion transporter 1Homo sapiens (human)
ATPase-coupled inorganic anion transmembrane transporter activityCanalicular multispecific organic anion transporter 1Homo sapiens (human)
ABC-type transporter activityCanalicular multispecific organic anion transporter 1Homo sapiens (human)
integrin bindingNischarinHomo sapiens (human)
protein bindingNischarinHomo sapiens (human)
phosphatidylinositol bindingNischarinHomo sapiens (human)
identical protein bindingNischarinHomo sapiens (human)
dynein heavy chain bindingNischarinHomo sapiens (human)
alpha-tubulin bindingNischarinHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (35)

Processvia Protein(s)Taxonomy
plasma membraneATP-binding cassette sub-family C member 3Homo sapiens (human)
basal plasma membraneATP-binding cassette sub-family C member 3Homo sapiens (human)
basolateral plasma membraneATP-binding cassette sub-family C member 3Homo sapiens (human)
membraneATP-binding cassette sub-family C member 3Homo sapiens (human)
nucleolusMultidrug resistance-associated protein 4Homo sapiens (human)
Golgi apparatusMultidrug resistance-associated protein 4Homo sapiens (human)
plasma membraneMultidrug resistance-associated protein 4Homo sapiens (human)
membraneMultidrug resistance-associated protein 4Homo sapiens (human)
basolateral plasma membraneMultidrug resistance-associated protein 4Homo sapiens (human)
apical plasma membraneMultidrug resistance-associated protein 4Homo sapiens (human)
platelet dense granule membraneMultidrug resistance-associated protein 4Homo sapiens (human)
external side of apical plasma membraneMultidrug resistance-associated protein 4Homo sapiens (human)
plasma membraneMultidrug resistance-associated protein 4Homo 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)
cytoplasmAlpha-2A adrenergic receptorHomo sapiens (human)
plasma membraneAlpha-2A adrenergic receptorHomo sapiens (human)
basolateral plasma membraneAlpha-2A adrenergic receptorHomo sapiens (human)
neuronal cell bodyAlpha-2A adrenergic receptorHomo sapiens (human)
axon terminusAlpha-2A adrenergic receptorHomo sapiens (human)
presynaptic active zone membraneAlpha-2A adrenergic receptorHomo sapiens (human)
dopaminergic synapseAlpha-2A adrenergic receptorHomo sapiens (human)
postsynaptic density membraneAlpha-2A adrenergic receptorHomo sapiens (human)
glutamatergic synapseAlpha-2A adrenergic receptorHomo sapiens (human)
GABA-ergic synapseAlpha-2A adrenergic receptorHomo sapiens (human)
receptor complexAlpha-2A adrenergic receptorHomo sapiens (human)
plasma membraneAlpha-2A adrenergic receptorHomo sapiens (human)
nucleusAlpha-1A adrenergic receptorBos taurus (cattle)
cytoplasmAlpha-1A adrenergic receptorBos taurus (cattle)
plasma membraneAlpha-1A adrenergic receptorBos taurus (cattle)
caveolaAlpha-1A adrenergic receptorBos taurus (cattle)
nuclear membraneAlpha-1A adrenergic receptorBos taurus (cattle)
cytoplasmAlpha-2C adrenergic receptorHomo sapiens (human)
endosomeAlpha-2C adrenergic receptorHomo sapiens (human)
plasma membraneAlpha-2C adrenergic receptorHomo sapiens (human)
plasma membraneAlpha-2C adrenergic receptorHomo sapiens (human)
plasma membraneCanalicular multispecific organic anion transporter 1Homo sapiens (human)
cell surfaceCanalicular multispecific organic anion transporter 1Homo sapiens (human)
apical plasma membraneCanalicular multispecific organic anion transporter 1Homo sapiens (human)
intercellular canaliculusCanalicular multispecific organic anion transporter 1Homo sapiens (human)
apical plasma membraneCanalicular multispecific organic anion transporter 1Homo sapiens (human)
nucleoplasmNischarinHomo sapiens (human)
early endosomeNischarinHomo sapiens (human)
cytosolNischarinHomo sapiens (human)
plasma membraneNischarinHomo sapiens (human)
microtubule cytoskeletonNischarinHomo sapiens (human)
membraneNischarinHomo sapiens (human)
intracellular membrane-bounded organelleNischarinHomo sapiens (human)
intercellular bridgeNischarinHomo sapiens (human)
recycling endosomeNischarinHomo sapiens (human)
cytoplasmNischarinHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (146)

Assay IDTitleYearJournalArticle
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.
AID588217FDA HLAED, serum glutamic pyruvic transaminase (SGPT) increase2004Current drug discovery technologies, Dec, Volume: 1, Issue:4
Assessment of the health effects of chemicals in humans: II. Construction of an adverse effects database for QSAR modeling.
AID1443980Inhibition of human BSEP expressed in fall armyworm sf9 cell plasma membrane vesicles assessed as reduction in vesicle-associated [3H]-taurocholate transport preincubated for 10 mins prior to ATP addition measured after 15 mins in presence of [3H]-tauroch2010Toxicological sciences : an official journal of the Society of Toxicology, Dec, Volume: 118, Issue:2
Interference with bile salt export pump function is a susceptibility factor for human liver injury in drug development.
AID1474167Liver toxicity in human assessed as induction of drug-induced liver injury by measuring verified drug-induced liver injury concern status2016Drug discovery today, Apr, Volume: 21, Issue:4
DILIrank: the largest reference drug list ranked by the risk for developing drug-induced liver injury in humans.
AID588214FDA HLAED, liver enzyme composite activity2004Current drug discovery technologies, Dec, Volume: 1, Issue:4
Assessment of the health effects of chemicals in humans: II. Construction of an adverse effects database for QSAR modeling.
AID625289Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for liver disease2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID625288Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for jaundice2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID1473740Inhibition of human MRP3 overexpressed in Sf9 insect cell membrane vesicles assessed as uptake of [3H]-estradiol-17beta-D-glucuronide in presence of ATP and GSH measured after 10 mins by membrane vesicle transport assay2013Toxicological sciences : an official journal of the Society of Toxicology, Nov, Volume: 136, Issue:1
A multifactorial approach to hepatobiliary transporter assessment enables improved therapeutic compound development.
AID444050Fraction unbound in human plasma2010Journal of medicinal chemistry, Feb-11, Volume: 53, Issue:3
Physicochemical space for optimum oral bioavailability: contribution of human intestinal absorption and first-pass elimination.
AID444055Fraction absorbed in human2010Journal of medicinal chemistry, Feb-11, Volume: 53, Issue:3
Physicochemical space for optimum oral bioavailability: contribution of human intestinal absorption and first-pass elimination.
AID625281Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for cholelithiasis2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID625279Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for bilirubinemia2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID1079946Presence of at least one case with successful reintroduction. [column 'REINT' in source]
AID342860Displacement of [125I]PIC from human alpha2 adrenoceptors expressed in CHO cells2008Bioorganic & medicinal chemistry, Aug-01, Volume: 16, Issue:15
QSAR study of imidazoline antihypertensive drugs.
AID1473738Inhibition of human BSEP overexpressed in Sf9 cell membrane vesicles assessed as uptake of [3H]-taurocholate in presence of ATP measured after 15 to 20 mins by membrane vesicle transport assay2013Toxicological sciences : an official journal of the Society of Toxicology, Nov, Volume: 136, Issue:1
A multifactorial approach to hepatobiliary transporter assessment enables improved therapeutic compound development.
AID625283Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for elevated liver function tests2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID539464Solubility of the compound in 0.1 M phosphate buffer at 600 uM at pH 7.4 after 24 hrs by LC/MS/MS analysis2010Bioorganic & medicinal chemistry letters, Dec-15, Volume: 20, Issue:24
Experimental solubility profiling of marketed CNS drugs, exploring solubility limit of CNS discovery candidate.
AID425652Total body clearance in human2009Journal of medicinal chemistry, Aug-13, Volume: 52, Issue:15
Physicochemical determinants of human renal clearance.
AID444053Renal clearance in human2010Journal of medicinal chemistry, Feb-11, Volume: 53, Issue:3
Physicochemical space for optimum oral bioavailability: contribution of human intestinal absorption and first-pass elimination.
AID1079944Benign tumor, proven histopathologically. Value is number of references indexed. [column 'T.BEN' in source]
AID425653Renal clearance in human2009Journal of medicinal chemistry, Aug-13, Volume: 52, Issue:15
Physicochemical determinants of human renal clearance.
AID468443Inhibition of human FAAH at 1 uM2009Bioorganic & medicinal chemistry letters, Dec-01, Volume: 19, Issue:23
Mining biologically-active molecules for inhibitors of fatty acid amide hydrolase (FAAH): identification of phenmedipham and amperozide as FAAH inhibitors.
AID588218FDA HLAED, lactate dehydrogenase (LDH) increase2004Current drug discovery technologies, Dec, Volume: 1, Issue:4
Assessment of the health effects of chemicals in humans: II. Construction of an adverse effects database for QSAR modeling.
AID1079945Animal toxicity known. [column 'TOXIC' in source]
AID342863Selectivity ratio of pKi for human imidazoline receptor 1 to pKi for human alpha2 adrenoceptors2008Bioorganic & medicinal chemistry, Aug-01, Volume: 16, Issue:15
QSAR study of imidazoline antihypertensive drugs.
AID588215FDA HLAED, alkaline phosphatase increase2004Current drug discovery technologies, Dec, Volume: 1, Issue:4
Assessment of the health effects of chemicals in humans: II. Construction of an adverse effects database for QSAR modeling.
AID625287Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for hepatomegaly2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID29812Oral bioavailability in human2000Journal of medicinal chemistry, Jun-29, Volume: 43, Issue:13
QSAR model for drug human oral bioavailability.
AID27167Delta logD (logD6.5 - logD7.4)2000Journal of medicinal chemistry, Jun-29, Volume: 43, Issue:13
QSAR model for drug human oral bioavailability.
AID588219FDA HLAED, gamma-glutamyl transferase (GGT) increase2004Current drug discovery technologies, Dec, Volume: 1, Issue:4
Assessment of the health effects of chemicals in humans: II. Construction of an adverse effects database for QSAR modeling.
AID29359Ionization constant (pKa)2000Journal of medicinal chemistry, Jun-29, Volume: 43, Issue:13
QSAR model for drug human oral bioavailability.
AID1079943Malignant tumor, proven histopathologically. Value is number of references indexed. [column 'T.MAL' in source]
AID1079939Cirrhosis, proven histopathologically. Value is number of references indexed. [column 'CIRRH' in source]
AID625291Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for liver function tests abnormal2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID1474166Liver toxicity in human assessed as induction of drug-induced liver injury by measuring severity class index2016Drug discovery today, Apr, Volume: 21, Issue:4
DILIrank: the largest reference drug list ranked by the risk for developing drug-induced liver injury in humans.
AID342861Displacement of [125I]PIC from human imidazoline receptor 1 in human platelets analyzed under norepinephrine mask of alpha 2AR2008Bioorganic & medicinal chemistry, Aug-01, Volume: 16, Issue:15
QSAR study of imidazoline antihypertensive drugs.
AID588216FDA HLAED, serum glutamic oxaloacetic transaminase (SGOT) increase2004Current drug discovery technologies, Dec, Volume: 1, Issue:4
Assessment of the health effects of chemicals in humans: II. Construction of an adverse effects database for QSAR modeling.
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.
AID1079949Proposed mechanism(s) of liver damage. [column 'MEC' in source]
AID539476Solubility of the compound at pH 7.22010Bioorganic & medicinal chemistry letters, Dec-15, Volume: 20, Issue:24
Experimental solubility profiling of marketed CNS drugs, exploring solubility limit of CNS discovery candidate.
AID625280Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for cholecystitis2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
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.
AID1079931Moderate liver toxicity, defined via clinical-chemistry results: ALT or AST serum activity 6 times the normal upper limit (N) or alkaline phosphatase serum activity of 1.7 N. Value is number of references indexed. [column 'BIOL' in source]
AID540213Half life in human after iv administration2008Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 36, Issue:7
Trend analysis of a database of intravenous pharmacokinetic parameters in humans for 670 drug compounds.
AID540211Fraction unbound in human after iv administration2008Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 36, Issue:7
Trend analysis of a database of intravenous pharmacokinetic parameters in humans for 670 drug compounds.
AID625286Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for hepatitis2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID1079932Highest frequency of moderate liver toxicity observed during clinical trials, expressed as a percentage. [column '% BIOL' in source]
AID1079938Chronic liver disease either proven histopathologically, or through a chonic elevation of serum amino-transferase activity after 6 months. Value is number of references indexed. [column 'CHRON' in source]
AID1079933Acute liver toxicity defined via clinical observations and clear clinical-chemistry results: serum ALT or AST activity > 6 N or serum alkaline phosphatases activity > 1.7 N. This category includes cytolytic, choleostatic and mixed liver toxicity. Value is
AID540212Mean residence time in human after iv administration2008Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 36, Issue:7
Trend analysis of a database of intravenous pharmacokinetic parameters in humans for 670 drug compounds.
AID444058Volume of distribution at steady state in human2010Journal of medicinal chemistry, Feb-11, Volume: 53, Issue:3
Physicochemical space for optimum oral bioavailability: contribution of human intestinal absorption and first-pass elimination.
AID1079940Granulomatous liver disease, proven histopathologically. Value is number of references indexed. [column 'GRAN' in source]
AID444054Oral bioavailability in human2010Journal of medicinal chemistry, Feb-11, Volume: 53, Issue:3
Physicochemical space for optimum oral bioavailability: contribution of human intestinal absorption and first-pass elimination.
AID1473741Inhibition of human MRP4 overexpressed in Sf9 cell membrane vesicles assessed as uptake of [3H]-estradiol-17beta-D-glucuronide in presence of ATP and GSH measured after 20 mins by membrane vesicle transport assay2013Toxicological sciences : an official journal of the Society of Toxicology, Nov, Volume: 136, Issue:1
A multifactorial approach to hepatobiliary transporter assessment enables improved therapeutic compound development.
AID444052Hepatic clearance in human2010Journal of medicinal chemistry, Feb-11, Volume: 53, Issue:3
Physicochemical space for optimum oral bioavailability: contribution of human intestinal absorption and first-pass elimination.
AID588220Literature-mined public compounds from Kruhlak et al phospholipidosis modelling dataset2008Toxicology mechanisms and methods, , Volume: 18, Issue:2-3
Development of a phospholipidosis database and predictive quantitative structure-activity relationship (QSAR) models.
AID1079947Comments (NB not yet translated). [column 'COMMENTAIRES' in source]
AID540210Clearance in human after iv administration2008Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 36, Issue:7
Trend analysis of a database of intravenous pharmacokinetic parameters in humans for 670 drug compounds.
AID625292Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) combined score2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID1079935Cytolytic liver toxicity, either proven histopathologically or where the ratio of maximal ALT or AST activity above normal to that of Alkaline Phosphatase is > 5 (see ACUTE). Value is number of references indexed. [column 'CYTOL' in source]
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.
AID625284Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for hepatic failure2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID1079937Severe hepatitis, defined as possibly life-threatening liver failure or through clinical observations. Value is number of references indexed. [column 'MASS' in source]
AID625282Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for cirrhosis2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID1473739Inhibition of human MRP2 overexpressed in Sf9 cell membrane vesicles assessed as uptake of [3H]-estradiol-17beta-D-glucuronide in presence of ATP and GSH measured after 20 mins by membrane vesicle transport assay2013Toxicological sciences : an official journal of the Society of Toxicology, Nov, Volume: 136, Issue:1
A multifactorial approach to hepatobiliary transporter assessment enables improved therapeutic compound development.
AID444051Total clearance in human2010Journal of medicinal chemistry, Feb-11, Volume: 53, Issue:3
Physicochemical space for optimum oral bioavailability: contribution of human intestinal absorption and first-pass elimination.
AID1079934Highest frequency of acute liver toxicity observed during clinical trials, expressed as a percentage. [column '% AIGUE' in source]
AID1079942Steatosis, proven histopathologically. Value is number of references indexed. [column 'STEAT' in source]
AID444056Fraction escaping gut-wall elimination in human2010Journal of medicinal chemistry, Feb-11, Volume: 53, Issue:3
Physicochemical space for optimum oral bioavailability: contribution of human intestinal absorption and first-pass elimination.
AID28681Partition coefficient (logD6.5)2000Journal of medicinal chemistry, Jun-29, Volume: 43, Issue:13
QSAR model for drug human oral bioavailability.
AID1079936Choleostatic liver toxicity, either proven histopathologically or where the ratio of maximal ALT or AST activity above normal to that of Alkaline Phosphatase is < 2 (see ACUTE). Value is number of references indexed. [column 'CHOLE' in source]
AID625290Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for liver fatty2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID1079948Times to onset, minimal and maximal, observed in the indexed observations. [column 'DELAI' in source]
AID625285Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for hepatic necrosis2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID1079941Liver damage due to vascular disease: peliosis hepatitis, hepatic veno-occlusive disease, Budd-Chiari syndrome. Value is number of references indexed. [column 'VASC' in source]
AID444057Fraction escaping hepatic elimination in human2010Journal of medicinal chemistry, Feb-11, Volume: 53, Issue:3
Physicochemical space for optimum oral bioavailability: contribution of human intestinal absorption and first-pass elimination.
AID540209Volume of distribution at steady state in human after iv administration2008Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 36, Issue:7
Trend analysis of a database of intravenous pharmacokinetic parameters in humans for 670 drug compounds.
AID1296008Cytotoxic Profiling of Annotated Libraries Using Quantitative High-Throughput Screening2020SLAS discovery : advancing life sciences R & D, 01, Volume: 25, Issue:1
Cytotoxic Profiling of Annotated and Diverse Chemical Libraries Using Quantitative High-Throughput Screening.
AID1346986P-glycoprotein substrates identified in KB-3-1 adenocarcinoma cell line, qHTS therapeutic library screen2019Molecular pharmacology, 11, Volume: 96, Issue:5
A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
AID1346987P-glycoprotein substrates identified in KB-8-5-11 adenocarcinoma cell line, qHTS therapeutic library screen2019Molecular pharmacology, 11, Volume: 96, Issue:5
A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
AID1347154Primary screen GU AMC qHTS for Zika virus inhibitors2020Proceedings 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.
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.
AID1347105qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for MG 63 (6-TG R) cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347121qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for control Hh wild type fibroblast cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347093qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-MC cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347094qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-37 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347089qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for TC32 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347103qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for OHS-50 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347111qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for SK-N-MC cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347118qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for TC32 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347424RapidFire Mass Spectrometry qHTS Assay for Modulators of WT P53-Induced Phosphatase 1 (WIP1)2019The Journal of biological chemistry, 11-15, Volume: 294, Issue:46
Physiologically relevant orthogonal assays for the discovery of small-molecule modulators of WIP1 phosphatase in high-throughput screens.
AID1347425Rhodamine-PBP qHTS Assay for Modulators of WT P53-Induced Phosphatase 1 (WIP1)2019The Journal of biological chemistry, 11-15, Volume: 294, Issue:46
Physiologically relevant orthogonal assays for the discovery of small-molecule modulators of WIP1 phosphatase in high-throughput screens.
AID1347123qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for Rh41 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347112qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for BT-12 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
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.
AID1347115qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for NB-EBc1 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1745845Primary qHTS for Inhibitors of ATXN expression
AID1347407qHTS to identify inhibitors of the type 1 interferon - major histocompatibility complex class I in skeletal muscle: primary screen against the NCATS Pharmaceutical 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.
AID1347116qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for SJ-GBM2 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347124qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for RD cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347125qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for Rh18 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347108qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh41 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347092qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for A673 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347127qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for Saos-2 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347096qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for U-2 OS cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347091qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SJ-GBM2 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID651635Viability Counterscreen for Primary qHTS for Inhibitors of ATXN expression
AID1347126qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for Rh30 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347097qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Saos-2 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347101qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-12 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347117qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for BT-37 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347128qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for OHS-50 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347095qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB-EBc1 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
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.
AID1347102qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh18 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347107qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh30 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347129qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for SK-N-SH cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
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.
AID1347090qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for DAOY cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347099qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB1643 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347114qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for DAOY cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347106qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for control Hh wild type fibroblast cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347122qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for U-2 OS cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347113qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for LAN-5 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347119qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for MG 63 (6-TG R) cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347100qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for LAN-5 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347109qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for NB1643 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347104qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for RD cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347110qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for A673 cells)2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347098qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-SH cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
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.
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.
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.
AID588378qHTS for Inhibitors of ATXN expression: Validation
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.
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.
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.
AID588349qHTS for Inhibitors of ATXN expression: Validation of Cytotoxic Assay
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.
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.
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.
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.
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.
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.
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.
AID1347411qHTS to identify inhibitors of the type 1 interferon - major histocompatibility complex class I in skeletal muscle: primary screen against the NCATS Mechanism Interrogation Plate v5.0 (MIPE) Libary2020ACS 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.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (415)

TimeframeStudies, This Drug (%)All Drugs %
pre-199063 (15.18)18.7374
1990's82 (19.76)18.2507
2000's114 (27.47)29.6817
2010's118 (28.43)24.3611
2020's38 (9.16)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 125.22

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 Index125.22 (24.57)
Research Supply Index6.30 (2.92)
Research Growth Index4.68 (4.65)
Search Engine Demand Index232.91 (26.88)
Search Engine Supply Index2.00 (0.95)

This Compound (125.22)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials101 (22.95%)5.53%
Reviews49 (11.14%)6.00%
Case Studies46 (10.45%)4.05%
Observational2 (0.45%)0.25%
Other242 (55.00%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Clinical Trials (25)

Trial Overview

TrialPhaseEnrollmentStudy TypeStart DateStatus
Multimodal Nonopioid Pain Protocol Following Shoulder Arthroplasty Surgery [NCT05488847]Phase 480 participants (Anticipated)Interventional2022-06-25Recruiting
Randomized, 2-way Crossover, Bioequivalence Study of Tizanidine Hydrochloride 4mg Tablets and Zanaflex® 4mg Tablets Administered As 1 x 4mg Tablet in Healthy Adult Subjects Under Fasting Conditions [NCT01146028]Phase 142 participants (Actual)Interventional2001-09-30Completed
Prospective Analgesic Compound Efficacy (PACE) Study [NCT02403687]300 participants (Actual)Observational [Patient Registry]2015-06-30Completed
Integrating Tailored Postoperative Opioid Tapering and Pain Management Support for Patients on Long-Term Opioid Use Presenting for Spine Surgery [NCT06027099]Phase 3375 participants (Anticipated)Interventional2024-02-29Not yet recruiting
Preemptive Single Dose Tizanidine and Ultrasound Guided Superficial Cervical Block on Pain After Thyroidectomy [NCT02725359]Phase 460 participants (Actual)Interventional2016-04-30Completed
Drug Discrimination in Methadone-Maintained Humans Study 3 [NCT01068847]Phase 19 participants (Actual)Interventional2010-02-28Completed
Randomized, 2-way Crossover, Bioequivalence Study of Tizanidine Hydrochloride 4mg Tablets and Zanaflex® 4mg Tablets Administered As 1 x 4mg Tablet in Healthy Adult Subjects Under Fed Conditions [NCT01065987]Phase 124 participants (Actual)Interventional2001-09-30Completed
Investigation of the Effectiveness of Tizanidine on Pain After Herniorrhaphy [NCT02016443]Phase 430 participants (Actual)Interventional2013-11-30Completed
A Randomized, Double-blind, Active and Placebo-controlled, Study of SPARC1401 in Subjects With Moderate to Severe Acute Low Back Pain [NCT02887534]Phase 20 participants (Actual)Interventional2016-11-30Withdrawn
Effect of CYP2B6 Genotype and Efavirenz on the Disposition and Pharmacodynamic of Methadone and Tizanidine in Healthy Volunteers [NCT05789173]Early Phase 160 participants (Anticipated)Interventional2023-10-06Recruiting
Safety and Efficacy of Oral Tizanidine Hydrochloride in Preventing Migraine Attacks in Adult Migraine Patients: a Multicenter, Randomized, Double Blind, Placebo Controlled Clinical Study [NCT05484349]Phase 3189 participants (Anticipated)Interventional2023-08-31Not yet recruiting
Addition of Muscle Relaxants in a Multimodal Analgesic Regimen for Analgesia After Primary Total Knee Arthroplasty [NCT04574791]240 participants (Actual)Interventional2020-09-03Enrolling by invitation
A Multicenter, Open-Label, Randomized, 4-Way Crossover Trial of the Safety and Efficacy of Tizanidine Hydrochloride Capsules Versus Zanaflex (Tizanidine Hydrochloride) Tablets Taken Under Fed and Fasted Conditions in Patients With Moderate to Severe Spast [NCT00047580]Phase 3120 participants Interventional2002-06-30Completed
Clinical Study on the Effect of Tizanidine on the Function and Pain of Patients After Shoulder Arthroscopy [NCT05852093]Early Phase 1100 participants (Anticipated)Interventional2023-06-01Not yet recruiting
Placebo-Controlled Trial of BOTOX® Versus Zanaflex® for the Treatment of Subjects With Post Stroke Upper Limb Spasticity [NCT00430196]Phase 4135 participants Interventional2003-12-31Completed
Long Term Clinical Efficacy and Safety of Novel Sublingual Tizanidine HCl (12 mg) for the Treatment of Spasticity in Patients With Multiple Sclerosis - Open Label Extension Study [NCT00464958]Phase 1/Phase 210 participants (Actual)Interventional2008-01-31Terminated(stopped due to Study was stopped as the sponsor is no longer funding this project)
A Phase III, Multicenter, Randomized Study to Assess the Efficacy and Safety of 0,5 mg Tizaspray® Administered Intranasally Versus Sirdalud® 2 mg Tablets, in Patients With Acute Low Back Pain [NCT02934061]Phase 3117 participants (Actual)Interventional2016-10-31Completed
A Double-Blind, Randomized, Two-Way Crossover, Comparative Study to Evaluate the Clinical Efficacy and Safety of Novel Sublingual Tizanidine HCl Versus Placebo in Children With Chronic Traumatic Brain Injury [NCT00287157]Phase 15 participants (Actual)Interventional2006-12-31Completed
A Phase I, Open-Label, Multicenter, 3- Period, Fixed-Sequence Study to Investigate the Effect of Vemurafenib on the Pharmacokinetics of a Single Dose of Tizanidine (a CYP1A2 Substrate) in Patients With BRAFV600 Mutation-Positive Metastatic Malignancy [NCT01844674]Phase 118 participants (Actual)Interventional2013-09-02Completed
A Double-Blind, Randomized, Crossover Study to Evaluate the Clinical Efficacy and Safety of Oral Tizanidine HCl (12 mg) Versus Novel Sublingual Tizanidine HCl (12 mg) for the Treatment of Spasticity in MS Patients [NCT00358293]Phase 1/Phase 220 participants Interventional2006-12-31Completed
Ibuprofen Plus Metaxolone, Tizanidine, or Baclofen for Low Back Pain: A Randomized Trial [NCT03068897]Phase 4320 participants (Actual)Interventional2017-05-03Completed
Effect of Gabapentin and Tizanidine on Insomnia in Chronic Pain Patients: A Randomized, Double-blind, Placebo-controlled Crossover Trial. [NCT04429347]Phase 224 participants (Anticipated)Interventional2020-07-29Enrolling by invitation
Single-Dose, Phase 1b Study to Assess Pharmacokinetics, Safety and Tolerability, and Pharmacodynamics of Tizanidine at 4 Different Oral Dose Levels in Pediatric Subjects With Mild to Moderate Spasticity Due to Cerebral Palsy [NCT01405950]Phase 110 participants (Actual)Interventional2011-05-31Terminated(stopped due to Please see 'Further study details as provided by Acorda Therapeutics' for explanation of why study stopped.)
A Partial-Blind, Randomized, Parallel Design Study With a Nested Crossover Comparison to Define the ECG Effects of Tizanidine Compared to Placebo and the Positive Control, Moxifloxacin, in Healthy Men and Women Using a Blinded ECG Evaluator: A Thorough EC [NCT01839279]Phase 2136 participants (Actual)Interventional2013-04-30Completed
Open Randomised Comparative Study of the Efficacy and Safety of Neuromultivit (Solution for Injections, 2 ml) in Patients With Vertebrogenic Radiculopathy [NCT02508805]Phase 3100 participants (Actual)Interventional2015-05-31Completed
[information is prepared from clinicaltrials.gov, extracted Sep-2024]

Trial Outcomes

TrialOutcome
NCT01405950 (2) [back to overview]Pharmacokinetic (PK) Parameter AUC0-8 (Area Under the Concentration-time Curve From Time 0 to 8 Hours) of a Single Dose of Tizanidine at 4 Different Dose Levels in Children and Adolescents With Cerebral Palsy and Mild to Moderate Spasticity.
NCT01405950 (2) [back to overview]Pharmacokinetic (PK) Parameter Cmax (Maximum Observed Drug Concentration in Plasma) of a Single Dose of Tizanidine at 4 Different Dose Levels in Children and Adolescents With Cerebral Palsy and Mild to Moderate Spasticity.
NCT01839279 (6) [back to overview]Area Under the Plasma Concentration-time Curve During a Dosing Interval (AUCt) of Single Doses of 8 and 24 mg Tizanidine After Reaching Steady State.
NCT01839279 (6) [back to overview]Assessing the Relationship Between Changes in the QTc Interval and Plasma Levels of Tizanidine Using Concentration-effect Modeling
NCT01839279 (6) [back to overview]Maximum Plasma Concentration (Cmax) of Single Doses of 8 and 24 mg Tizanidine After Reaching Steady State.
NCT01839279 (6) [back to overview]Time to Reach Maximum Plasma Concentration (Tmax) of Single Doses of 8 and 24 mg Tizanidine After Reaching Steady State.
NCT01839279 (6) [back to overview]The Baseline-adjusted, Placebo-corrected (ΔΔQTc) on QTc Method Not Selected as Primary Endpoint.
NCT01839279 (6) [back to overview]The Primary Endpoint Will be the Baseline-adjusted, Placebo-corrected Effect on QTc (ΔΔQTc) on Day 14.
NCT03068897 (4) [back to overview]Change in Functional Impairment as Measured by the Roland Morris Disability Questionnaire (RMDQ)
NCT03068897 (4) [back to overview]Levels of Disability
NCT03068897 (4) [back to overview]Number of Participants Who Experience Change in Low Back Pain
NCT03068897 (4) [back to overview]Number of Participants With Need for Medication for Low Back Pain

Pharmacokinetic (PK) Parameter AUC0-8 (Area Under the Concentration-time Curve From Time 0 to 8 Hours) of a Single Dose of Tizanidine at 4 Different Dose Levels in Children and Adolescents With Cerebral Palsy and Mild to Moderate Spasticity.

"Baseline: immediately before the standardized meal (i.e., before administration of tizanidine) on dosing day~0.25, 0.5, 1, 1.5, 2, 3, 4, 6, and 8 hours after administration of tizanidine~PK parameters will be derived by using WinNonlin Pro (version 5.0.1 or later, Pharsight Corp)." (NCT01405950)
Timeframe: Baseline and 0.25, 0.5, 1, 1.5, 2, 3, 4, 6, and 8 hours

Interventionhour*nanogram/mililiter (Mean)
Dose Level 15.60
Dose Level 26.11

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Pharmacokinetic (PK) Parameter Cmax (Maximum Observed Drug Concentration in Plasma) of a Single Dose of Tizanidine at 4 Different Dose Levels in Children and Adolescents With Cerebral Palsy and Mild to Moderate Spasticity.

"Baseline: immediately before the standardized meal (i.e., before administration of tizanidine) on dosing day~0.25, 0.5, 1, 1.5, 2, 3, 4, 6, and 8 hours after administration of tizanidine~PK parameters will be derived by using WinNonlin Pro (version 5.0.1 or later, Pharsight Corp)." (NCT01405950)
Timeframe: Baseline and 0.25, 0.5, 1, 1.5, 2, 3, 4, 6, and 8 hours

Interventionnanogram/mililiter (Mean)
Dose Level 11.87
Dose Level 25.29

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Area Under the Plasma Concentration-time Curve During a Dosing Interval (AUCt) of Single Doses of 8 and 24 mg Tizanidine After Reaching Steady State.

(NCT01839279)
Timeframe: 0.5, 1, 1.5, 2, 4, 8, 12 & 24 hours post dose on Days 5 (8 mg) and 14 (24 mg)

Interventionng*hr/mL (Geometric Mean)
Day 5 (Tizanidine 8 mg)32.4
Day 14 (Tizanidine 24 mg)115

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Assessing the Relationship Between Changes in the QTc Interval and Plasma Levels of Tizanidine Using Concentration-effect Modeling

The relationship will be quantified using a linear mixed effects model with an intercept. Data from Day 5 and Day 14 were fitted into regression model to obtain a slope of change. The measure type 'Number' followed by (90% Confidence Interval) shown in results is the slope from the linear fit. (NCT01839279)
Timeframe: Day 5, Day 14

Interventionmsec per ng/mL (Number)
Tizanidine-0.1209

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Maximum Plasma Concentration (Cmax) of Single Doses of 8 and 24 mg Tizanidine After Reaching Steady State.

(NCT01839279)
Timeframe: 0.5, 1, 1.5, 2, 4, 8, 12 & 24 hours post dose on Days 5 (8 mg) and 14 (24 mg)

Interventionng/mL (Geometric Mean)
Day 5 (Tizanidine 8 mg)11.7
Day 14 (Tizanidine 24 mg)27.4

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Time to Reach Maximum Plasma Concentration (Tmax) of Single Doses of 8 and 24 mg Tizanidine After Reaching Steady State.

(NCT01839279)
Timeframe: 0.5, 1, 1.5, 2, 4, 8, 12 & 24 hours post dose on Days 5 (8 mg) and 14 (24 mg)

Interventionhour (Median)
Day 5 (Tizanidine 8 mg)1.35
Day 14 (Tizanidine 24 mg)2.10

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The Baseline-adjusted, Placebo-corrected (ΔΔQTc) on QTc Method Not Selected as Primary Endpoint.

Change from baseline in Cardiac Repolarization (QTc Interval) at Day 5 (Tizanidine 8 mg). Moxifloxacin was not investigational drug, it was used to assess the sensitivity of the study. (NCT01839279)
Timeframe: Baseline and Day 5

,,
Interventionmsec (Least Squares Mean)
Timepoint (Hour) 00.511.52481224
Tizanidine 8 mg-0.8-0.40.01.1-0.42.6-1.5-0.1-0.5
Tizanidine 8 mg Placebo-corrected0.1-0.8-2.3-0.1-0.71.6-2.2-0.8-1.9
Tizanidine Placebo 8 mg-0.90.42.31.30.41.00.60.71.4

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The Primary Endpoint Will be the Baseline-adjusted, Placebo-corrected Effect on QTc (ΔΔQTc) on Day 14.

Change from baseline in Cardiac Repolarization (QTc Interval) at Day 14 (Tizanidine 24 mg). Moxifloxacin was not investigational drug, it was used to assess the sensitivity of the study. (NCT01839279)
Timeframe: Baseline and Day 14

,,
Interventionmilliseconds (msec) (Least Squares Mean)
Timepoint (Hour) 00.511.52481224
Tizanidine 24 mg-4.3-2.0-4.0-4.7-3.61.6-2.4-2.00.4
Tizanidine 24 mg Placebo-corrected-3.7-3.2-6.6-7.4-6.4-1.8-5.5-3.0-2.2
Tizanidine Placebo 24 mg-0.51.22.62.72.93.43.11.02.6

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Change in Functional Impairment as Measured by the Roland Morris Disability Questionnaire (RMDQ)

"The Roland Morris Disability Questionnaire (RMDQ) is a 24 item instrument that evaluates the impact of low back pain on one's daily life. It is most sensitive for patients with mild to moderate disability due to acute, sub-acute or chronic low back pain. Each question can be answered as either a yes or no. The score ranges from 0 to 24 where a higher score reflects greater impairment and, therefore, worsening in the quality of life. The change in RMDQ is obtained by subtracting the RMDQ score at one week after discharge from the baseline score." (NCT03068897)
Timeframe: Baseline and 7 days

Interventionunits on a scale (Mean)
Metaxalone10.1
Tizanidine11.2
Baclofen10.6
Placebo11.1

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Levels of Disability

Disability will be assessed with the Roland-Morris Disability Questionnaire (RMDQ) where patients are asked to tick a box if they agree with 24 statements regarding their ability to perform certain activities (dressing, housework, walking). If the don't agree with the statement (able to perform those activities) they need to leave the tick-box blank or unchecked. Every agreement (tick) counts as a point and an absolute value is formed (min: 0, max: 24). The higher the value the higher the disability level. (NCT03068897)
Timeframe: 7 days

Interventionunits on a scale (Median)
Metaxalone5
Tizanidine3
Baclofen6
Placebo3

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Number of Participants Who Experience Change in Low Back Pain

Change is assessed by verbal numerical scale of which 0 represents no pain and 10 represents the worst pain imaginable between the baseline ED visit and the one week follow-up (baseline - 1 week ). The baseline questions will refer to the time period immediately prior to ED presentation (Before you came to the ER today, were you able to…..) (NCT03068897)
Timeframe: Baseline and 7 days

InterventionParticipants (Count of Participants)
Metaxalone28
Tizanidine25
Baclofen26
Placebo22

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Number of Participants With Need for Medication for Low Back Pain

Patients will be asked what medications they have used for low back pain (NCT03068897)
Timeframe: 7 days

InterventionParticipants (Count of Participants)
Metaxalone49
Tizanidine48
Baclofen49
Placebo46

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