Page last updated: 2024-12-06

zolazepam

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Description

Zolazepam: A pyrazolodiazepinone with pharmacological actions similar to ANTI-ANXIETY AGENTS. It is commonly used in combination with TILETAMINE to obtain immobilization and anesthesia in animals. [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID35775
CHEMBL ID2111144
SCHEMBL ID114155
MeSH IDM0023149

Synonyms (24)

Synonym
4-(2-fluorophenyl)-6,8-dihydro-1,3,8-trimethylpyrazolo-(3,4-e)(1,4)diazepin-7(1h)-one
zolazepam [inn:ban]
flupyrazapon
zolazepam
zolazepamum [inn-latin]
pyrazolo(3,4-e)(1,4)diazepin-7(1h)-one, 4-(2-fluorophenyl)-6,8-dihydro-1,3,8-trimethyl-
4-(2-fluorophenyl)-1,3,8-trimethyl-6h-pyrazolo[3,4-e][1,4]diazepin-7-one
ci 716
zolazepamum
unii-g1r474u58u
31352-82-6
g1r474u58u ,
zolazepam [who-dd]
4-(o-fluorophenyl)-6,8-dihydro-1,3,8-trimethylpyrazolo(3,4-e)(1,4)diazepin-7(1h)-one
zolazepam [mi]
zolazepam [inn]
SCHEMBL114155
CHEMBL2111144
DTXSID30185278
Q4024647
4-(2-fluorophenyl)-1,3,8-trimethyl-6,8-dihydropyrazolo[3,4-e][1,4]diazepin-7(1h)-one
DB11555
NCGC00522014-01
AKOS040754575

Research Excerpts

Overview

Zolazepam is a widely used benzodiazepine known for its muscle relaxant and anticonvulsant properties.

ExcerptReferenceRelevance
"Zolazepam is a widely used benzodiazepine known for its muscle relaxant and anticonvulsant properties."( Dissociative anaesthesia in dogs and cats with use of tiletamine and zolazepam combination. What we already know about it.
Kiełbowicz, Z; Kucharski, P, 2021
)
1.58

Treatment

ExcerptReferenceRelevance
"Treatment with zolazepam and Telazol increased microsomal benzyloxyresorufin O-dealkylase (BROD) activity by approximately 9- and 15-fold, respectively, and increased microsomal testosterone 16 beta-hydroxylase activity by 5- and 8-fold, respectively."( Induction of hepatic cytochrome P450 2B and P450 3A isozymes in rats by zolazepam, a constituent of Telazol.
Bandiera, SM; Wong, A, 1998
)
0.87

Toxicity

ExcerptReferenceRelevance
"The goals of the study were to find a safe intraperitoneal injection anesthesia protocol for medium-duration surgery in mice (e."( Optimization of intraperitoneal injection anesthesia in mice: drugs, dosages, adverse effects, and anesthesia depth.
Arras, M; Autenried, P; Rettich, A; Rülicke, T; Spaeni, D, 2001
)
0.31

Pharmacokinetics

ExcerptReferenceRelevance
"A pharmacokinetic and tissue residue study was conducted to assess the risks associated with human consumption of polar bears in arctic Canada that have been exposed to the immobilizing drug Telazol, a mixture of tiletamine hydrochloride and zolazepam hydrochloride."( Pharmacokinetics and tissue residues of Telazol in free-ranging polar bears.
Farley, SD; Gorecki, DK; Ramsay, MA; Semple, HA, 2000
)
0.49
" These results collectively point to major pharmacokinetic and metabolic differences between the two components of this fixed-dose anesthetic combination."( Pharmacokinetic study in pigs and in vitro metabolic characterization in pig- and human-liver microsomes reveal marked differences in disposition and metabolism of tiletamine and zolazepam (Telazol).
Beilman, GJ; Kaila, N; Kumar, A; Mann, HJ; Remmel, RP, 2014
)
0.59

Compound-Compound Interactions

Low dose tiletamine-zolazepam combined with methadone provided superior sedation to ACE.

ExcerptReferenceRelevance
"To evaluate anesthetic effects of tiletamine-zolazepam (TZ), alone or in combination with butorphanol, in goats undergoing laparotomy for embryo collection."( Anesthetic effects of tiletamine-zolazepam, alone or in combination with butorphanol, in goats.
Carroll, GL; Hambleton, R; Hartsfield, SM, 1997
)
0.84
"To evaluate antinociceptive and selected effects associated with IM administration of xylazine hydrochloride in combination with tiletamine-zolazepam in llamas."( Physiologic and antinociceptive effects following intramuscular administration of xylazine hydrochloride in combination with tiletamine-zolazepam in llamas.
Doherty, TJ; Egger, CM; Elliot, SB; Seddighi, R; Whitlock, BK, 2013
)
0.79
" Procedures-Each llama received tiletamine-zolazepam (2 mg/kg) combined with either xylazine (0."( Physiologic and antinociceptive effects following intramuscular administration of xylazine hydrochloride in combination with tiletamine-zolazepam in llamas.
Doherty, TJ; Egger, CM; Elliot, SB; Seddighi, R; Whitlock, BK, 2013
)
0.86
"Low dose tiletamine-zolazepam combined with methadone provided superior sedation to ACE."( A comparison of low dose tiletamine-zolazepam or acepromazine combined with methadone for pre-anaesthetic medication in cats.
Kloeppel, H; Mair, A; Ticehurst, K, 2014
)
1
"The goal of this study was to determine whether a drug combination using nalbuphine with dexmedetomidine and tiletamine/zolazepam is non-inferior to one that uses butorphanol."( Use of nalbuphine as a substitute for butorphanol in combination with dexmedetomidine and tiletamine/zolazepam: a randomized non-inferiority trial.
Cornell, HN; Hofmeister, EH; Kelsey, SE; Kreisler, RE; Smith, VA, 2020
)
0.98
" Each animal was randomly assigned to receive either 80 µg/kg (group L) or 100 µg/kg (group H) medetomidine, combined with 3 mg/kg tiletamine-zolazepam administered intramuscularly."( Comparison of the Cardiovascular Effects of Two Medetomidine Doses Combined with Tiletamine-Zolazepam for the Immobilization of Red Deer Hinds (Cervus elaphus).
Einwaller, J; Habe, M; Painer, J; Pohlin, F; Rauch, H; Stalder, G, 2022
)
1.14

Dosage Studied

A tiletamine/zolazepam combination was used to immobilize 24 captive giant Chacoan peccaries (Catagonus wagneri) at a mean dosage rate of 2. The drug was administered intramuscularly in ten dogs at a dosage of 10 mg/kg bwt of tiletamines.

ExcerptRelevanceReference
"Five anesthetic agents (C1744, etorphine, fentanyl, ketamine hydrochloride, and halothane) were tested to establish the dosage of a safe, effective, short-acting anesthetic for use in the sea otter."( Comparison of anesthetic agents in the sea otter.
Kocher, FH; Williams, TD, 1978
)
0.26
"001) positive linear relationship between duration of anesthesia and dosage for all animals in which the duration was recorded (n = 36)."( Tiletamine and zolazepam for immobilization of wild lions and leopards.
Bertram, BC; Hamilton, PH; King, JM, 1977
)
0.61
" The drug was administered intramuscularly in ten dogs at a dosage of 10 mg/kg bwt of tiletamine and 10 mg/kg bwt of zolazepam and tested for its effects on hemodynamics, respiration, and the antagonistic effect of flumazenil."( [Anesthesia in dogs with the combination preparation Tilest 500].
Hess, L, 1991
)
0.49
" Neither dosing regimen caused significant changes in right atrial pressure, heart rate, pulmonary vascular resistance, or pulmonary capillary wedge pressure."( The cardiovascular response of sheep to tiletamine-zolazepam and butorphanol tartrate anesthesia.
Howard, BW; Januszkiewicz, AJ; Lagutchik, MS; Martin, DG,
)
0.38
" Two dosage levels of 12 mg/kg and 22 mg/kg were evaluated."( Evaluation of a combination of tiletamine and zolazepam as an anesthetic for ferrets.
Payton, AJ; Pick, JR, 1989
)
0.54
" Results showed Telazol to be a safe anesthetic and when dosed at 60 mg/kg to be suitable for major surgical procedures."( A new anesthetic agent for use in the gerbil.
Hrapkiewicz, KL; Smiler, KL; Stein, S, 1989
)
0.28
" A dosage of 5 mg/kg of body weight, administered IM, resulted in variable weak tranquilization."( Evaluation of use of tiletamine/zolazepam for anesthesia of bullfrogs and leopard frogs.
Durante, R; Letcher, J, 1995
)
0.57
" Thirteen animals were given an additional dosage of ketamine hydrochloride manually when they recovered from the first injection of TEL."( Field application of Telazol (tiletamine hydrochloride and zolazepam hydrochloride) to immobilize wild red howler monkeys (Alouatta seniculus) in Venezuela.
Agoramoorthy, G; Rudran, R, 1994
)
0.53
" Recovery time varied with weight and dosage of yohimbine."( Immobilization of Rocky Mountain elk with Telazol and xylazine hydrochloride, and antagonism by yohimbine hydrochloride.
Brundige, GC; Hustead, DR; Jenks, JA; Millspaugh, JJ; Tyner, CL, 1995
)
0.29
" The addition of methoxyflurane significantly potentiated the anaesthetic and analgesic properties of the high dosage ketamine-xylazine combination."( Evaluation of anaesthetic regimens in guineapigs.
Crenshaw, D; Hinson, A; Radde, GR; Toth, LA, 1996
)
0.29
" A secondary goal was to compare the effects produced by Telazol and its constituents with those elicited by sodium phenobarbital (PB) using the same dosing regimen."( Induction of hepatic cytochrome P450 2B and P450 3A isozymes in rats by zolazepam, a constituent of Telazol.
Bandiera, SM; Wong, A, 1998
)
0.53
"Of the 5,766 cats for which dosing records were complete, 4,584 (79."( Use of the anesthetic combination of tiletamine, zolazepam, ketamine, and xylazine for neutering feral cats.
Centonze, LA; Cistola, AM; Levy, JK; Robertson, SA; Williams, LS, 2002
)
0.57
" The dosage required to achieve a satisfactory level of anesthesia was smaller for subantarctic fur seals than for most other species of seals and was less for animals in better body condition."( Response of wild subantarctic fur seal (Arctocephalus tropicalis) females to ketamine and tiletamine-zolazepam anesthesia.
Beauplet, G; Dabin, W; Guinet, C, 2002
)
0.53
" The mean dosage (0."( Tiletamine-zolazepam, ketamine, and xylazine anesthesia of captive cheetah (Acinonyx jubatus).
Bonar, CJ; Evans, SE; Lewandowski, AH, 2002
)
0.7
" Although induction time was similar between drugs, induction dosage and volume were less with XZT."( Anesthesia of polar bears using xylazine-zolazepam-tiletamine or zolazepam-tiletamine.
Cattet, MR; Caulkett, NA; Lunn, NJ, 2003
)
0.58
" A combination of 500 mg zolazepam, 500 mg tiletamine, 500 mg xylazine, and 1000 mg (10 ml) ketamine, administered in a dosage of 1 ml per 100-150 kg bodyweight (depending on the species), proved to be most reliable and effective."( [Immobilization of cattle and bison with a combination of xylazine, zolazepam-tiletamine and ketamine].
Hofkes, LM; Hoyer, MJ; Overgaauw, PA; van Dijk, P, 2005
)
0.87
" A fixed ratio of 1 mg CAR:10 mg XYL intramuscularly was used, increasing or decreasing the dosage until the optimal dosage (defined by an induction time < 3 min and PaCO(2)< 60 mmHg) was reached for each animal."( Determination and evaluation of an optimal dosage of carfentanil and xylazine for the immobilization of white-tailed deer (Odocoileus virginianus).
Miller, KV; Osborn, DA; Ramsay, EC; Schumacher, J; Storms, TN; Zagaya, N, 2005
)
0.33
"01) between dosage and time to first effect of immobilants."( Tiletamine-zolazepam-xylazine immobilization of American marten (Martes americana).
Belant, JL, 2005
)
0.72
" There was no relationship between the amount (mg/kg) of Telazol-xylazine injected and time to first effect of immobilants, dosage and time to induction, or between dosage and time to recovery."( Tiletamine-zolazepam-xylazine immobilization of fishers (Martes pennanti).
Belant, JL, 2007
)
0.73
" The total Telazol dosage was also significantly different between young lemurs (33 +/- 15 mg/kg) and mature lemurs (18 +/- 9 mg/kg)."( Field anesthesia of wild ring-tailed lemurs (Lemur catta) using tiletamine-zolazepam, medetomidine, and butorphanol.
Cuozzo, FP; Larsen, RS; Moresco, A; Sauther, ML, 2011
)
0.6
"The objectives of our study were to investigate the dose-response relationship of the TASER X26 discharge duration in an anesthetized swine model."( Repetitive TASER X26 discharge resulted in adverse physiologic events with a dose-response relationship related to the duration of discharge in anesthetized swine model.
Ahn, JH; Choi, SC; Min, YG; Park, EJ, 2013
)
0.39
" In the main trial (romifidine combinations) mean time (minutes) to standing increased with increasing dosage (R40TZ1 13; R80TZ2 32)."( Romifidine and low doses of tiletamine-zolazepam in dogs.
Domínguez, JM; Fernández, A; Gómez-Villamandos, RJ; Granados, MM; López, I; Martínez, C; Morgaz, J; Muñoz, P; Navarrete, R, 2013
)
0.66
" The dosage and drug combination used was effective for immobilization of ABBs with minimal adverse effects on vital signs and can be recommended in most clinical applications."( Immobilization of Asiatic Black Bears ( Ursus thibetanus ) with Medetomidine-Zolazepam-Tiletamine in South Korea.
Jeong, DH; Seok, SH; Song, BC; Yang, JJ; Yeon, SC, 2017
)
0.68
"To determine the effective dosage of the combination tiletamine-zolazepam-ketamine-xylazine (TKX), with or without methadone, in dogs."( Determination of the effective dosage of tiletamine-zolazepam-ketamine-xylazine, with or without methadone, in dogs.
Baier, ME; Herrera Becerra, JR; Martins, LGB; Monteiro, ER; Souza, MJ, 2022
)
1.21
" The consistency of respiratory parameters during the entire exposure time is paramount to ensuring dosing accuracy."( Comparison of Alfaxalone-Midazolam, Tiletamine-Zolazepam, and KetamineAcepromazine Anesthesia during Plethysmography in Cynomolgus Macaques (
Astleford, SM; Bowling, PA; Casselman, AM; Dixon, BC; Ghering, JM; Marion, BM; White, CE, 2022
)
0.98
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Protein Targets (1)

Potency Measurements

ProteinTaxonomyMeasurementAverage (µ)Min (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Spike glycoproteinSevere acute respiratory syndrome-related coronavirusPotency16.04610.009610.525035.4813AID1479145; AID1479148
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Ceullar Components (1)

Processvia Protein(s)Taxonomy
virion membraneSpike glycoproteinSevere acute respiratory syndrome-related coronavirus
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (3)

Assay IDTitleYearJournalArticle
AID1146339Antianxiety activity in Holtzman rat assessed as dose required to elicit increase in milk consumption1977Journal of medicinal chemistry, Dec, Volume: 20, Issue:12
Pyrazolodiazepines. 2. 4-Aryl-1,3-dialkyl-6,8-dihydropyrazolo[3,4-e] [1,4]diazepin-7(1H)-ones as antianxiety and anticonvulsant agents.
AID1146338Anticonvulsant activity in rat assessed as protection against pentylenetetrazole-induced clonic seizures1977Journal of medicinal chemistry, Dec, Volume: 20, Issue:12
Pyrazolodiazepines. 2. 4-Aryl-1,3-dialkyl-6,8-dihydropyrazolo[3,4-e] [1,4]diazepin-7(1H)-ones as antianxiety and anticonvulsant agents.
AID1146340Ratio of diazepam MED to compound MED for antianxiety activity in Holtzman rat1977Journal of medicinal chemistry, Dec, Volume: 20, Issue:12
Pyrazolodiazepines. 2. 4-Aryl-1,3-dialkyl-6,8-dihydropyrazolo[3,4-e] [1,4]diazepin-7(1H)-ones as antianxiety and anticonvulsant agents.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (311)

TimeframeStudies, This Drug (%)All Drugs %
pre-199023 (7.40)18.7374
1990's94 (30.23)18.2507
2000's88 (28.30)29.6817
2010's80 (25.72)24.3611
2020's26 (8.36)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 48.07

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 strong demand-to-supply ratio for research on this compound.

MetricThis Compound (vs All)
Research Demand Index48.07 (24.57)
Research Supply Index5.95 (2.92)
Research Growth Index5.02 (4.65)
Search Engine Demand Index75.81 (26.88)
Search Engine Supply Index2.00 (0.95)

This Compound (48.07)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials61 (18.89%)5.53%
Reviews7 (2.17%)6.00%
Case Studies12 (3.72%)4.05%
Observational1 (0.31%)0.25%
Other242 (74.92%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]