This drug entry is a stub and has not been fully annotated. It is scheduled to be annotated soon.

Identification

Generic Name
Zolazepam
DrugBank Accession Number
DB11555
Background

Zolazepam is a pyrazolodiazepinone derivative used as an anaesthetic in veterinary medicine. Zolazepam is typically used in combination with the NMDA antagonist tiletamine or the α2 adrenoceptor agonist xylazine. It is around four times the potency of diazepam but it is both water-soluble and un-ionized at physiological pH meaning that its onset is very fast.

Type
Small Molecule
Groups
Vet approved
Structure
Weight
Average: 286.31
Monoisotopic: 286.122989282
Chemical Formula
C15H15FN4O
Synonyms
  • Zolazepam
  • Zolazepamum
External IDs
  • CI 716
  • CI-716
  • DEA No. 7295

Pharmacology

Indication

Not Available

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Contraindications & Blackbox Warnings
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Pharmacodynamics

Not Available

Mechanism of action
Not Available
Absorption

Not Available

Volume of distribution

Not Available

Protein binding

Not Available

Metabolism
Not Available
Route of elimination

Not Available

Half-life

Not Available

Clearance

Not Available

Adverse Effects
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Toxicity

Not Available

Pathways
Not Available
Pharmacogenomic Effects/ADRs
Not Available

Interactions

Drug Interactions
This information should not be interpreted without the help of a healthcare provider. If you believe you are experiencing an interaction, contact a healthcare provider immediately. The absence of an interaction does not necessarily mean no interactions exist.
DrugInteraction
1,2-BenzodiazepineThe risk or severity of adverse effects can be increased when Zolazepam is combined with 1,2-Benzodiazepine.
AcetazolamideThe risk or severity of adverse effects can be increased when Acetazolamide is combined with Zolazepam.
AcetophenazineThe risk or severity of adverse effects can be increased when Acetophenazine is combined with Zolazepam.
AclidiniumZolazepam may increase the central nervous system depressant (CNS depressant) activities of Aclidinium.
AgomelatineThe risk or severity of adverse effects can be increased when Agomelatine is combined with Zolazepam.
AlfentanilThe risk or severity of adverse effects can be increased when Alfentanil is combined with Zolazepam.
AlimemazineThe risk or severity of adverse effects can be increased when Alimemazine is combined with Zolazepam.
AlmotriptanThe risk or severity of adverse effects can be increased when Almotriptan is combined with Zolazepam.
AlosetronThe risk or severity of adverse effects can be increased when Alosetron is combined with Zolazepam.
AlprazolamThe risk or severity of adverse effects can be increased when Alprazolam is combined with Zolazepam.
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Food Interactions
Not Available

Products

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Product Ingredients
IngredientUNIICASInChI Key
Zolazepam hydrochloride45SJ093Q1N33754-49-3NJERAXSSDSHLGE-UHFFFAOYSA-N

Categories

Drug Categories
Chemical TaxonomyProvided by Classyfire
Description
This compound belongs to the class of organic compounds known as alpha amino acids and derivatives. These are amino acids in which the amino group is attached to the carbon atom immediately adjacent to the carboxylate group (alpha carbon), or a derivative thereof.
Kingdom
Organic compounds
Super Class
Organic acids and derivatives
Class
Carboxylic acids and derivatives
Sub Class
Amino acids, peptides, and analogues
Direct Parent
Alpha amino acids and derivatives
Alternative Parents
Fluorobenzenes / Aryl fluorides / Tertiary carboxylic acid amides / Pyrazoles / Heteroaromatic compounds / Lactams / Ketimines / Propargyl-type 1,3-dipolar organic compounds / Azacyclic compounds / Organopnictogen compounds
show 4 more
Substituents
Alpha-amino acid or derivatives / Aromatic heteropolycyclic compound / Aryl fluoride / Aryl halide / Azacycle / Azole / Benzenoid / Carbonyl group / Carboxamide group / Fluorobenzene
show 20 more
Molecular Framework
Aromatic heteropolycyclic compounds
External Descriptors
Not Available
Affected organisms
Not Available

Chemical Identifiers

UNII
G1R474U58U
CAS number
31352-82-6
InChI Key
GDSCFOSHSOWNDL-UHFFFAOYSA-N
InChI
InChI=1S/C15H15FN4O/c1-9-13-14(10-6-4-5-7-11(10)16)17-8-12(21)19(2)15(13)20(3)18-9/h4-7H,8H2,1-3H3
IUPAC Name
4-(2-fluorophenyl)-1,3,8-trimethyl-1H,6H,7H,8H-pyrazolo[3,4-e][1,4]diazepin-7-one
SMILES
CN1N=C(C)C2=C1N(C)C(=O)CN=C2C1=CC=CC=C1F

References

General References
  1. Natalini CC, Alves SD, Guedes AG, Polydoro AS, Brondani JT, Bopp S: Epidural administration of tiletamine/zolazepam in horses. Vet Anaesth Analg. 2004 Apr;31(2):79-85. [Article]
  2. Hubbell JA, Bednarski RM, Muir WW: Xylazine and tiletamine-zolazepam anesthesia in horses. Am J Vet Res. 1989 May;50(5):737-42. [Article]
  3. Hong WH, Szulczewski DH: Characteristics of equilibrium reaction of zolazepam. J Pharm Sci. 1981 Jun;70(6):691-3. [Article]
  4. Wilson RP, Zagon IS, Larach DR, Lang CM: Cardiovascular and respiratory effects of tiletamine-zolazepam. Pharmacol Biochem Behav. 1993 Jan;44(1):1-8. [Article]
  5. Cattet MR, Caulkett NA, Lunn NJ: Anesthesia of polar bears using xylazine-zolazepam-tiletamine or zolazepam-tiletamine. J Wildl Dis. 2003 Jul;39(3):655-64. [Article]
  6. Lin HC, Wallace SS, Tyler JW, Robbins RL, Thurmon JC, Wolfe DF: Comparison of tiletamine-zolazepam-ketamine and tiletamine-zolazepam-ketamine-xylazine anaesthesia in sheep. Aust Vet J. 1994 Aug;71(8):239-42. [Article]
  7. Fernandez-Moran J, Palomeque J, Peinado VI: Medetomidine/tiletamine/zolazepam and xylazine/tiletamine/zolazepam combinations for immobilization of fallow deer (Cervus dama). J Zoo Wildl Med. 2000 Mar;31(1):62-4. [Article]
  8. Caulkett NA, Cattet MR, Cantwell S, Cool N, Olsen W: Anesthesia of wood bison with medetomidine-zolazepam/tiletamine and xylazine-zolazepam/tiletamine combinations. Can Vet J. 2000 Jan;41(1):49-53. [Article]
  9. Selmi AL, Mendes GM, Figueiredo JP, Guimaraes FB, Selmi GR, Bernal FE, McMannus C, Paludo GR: Chemical restraint of peccaries with tiletamine/zolazepam and xylazine or tiletamine/zolazepam and butorphanol. Vet Anaesth Analg. 2003 Jan;30(1):24-9. [Article]
  10. Cattet MR, Caulkett NA, Polischuk SC, Ramsay MA: Anesthesia of polar bears (Ursus maritimus) with zolazepam-tiletamine, medetomidine-ketamine, and medetomidine-zolazepam-tiletamine. J Zoo Wildl Med. 1999 Sep;30(3):354-60. [Article]
ChemSpider
32907
RxNav
1535252
ChEMBL
CHEMBL2111144
ZINC
ZINC000000002259
Wikipedia
Zolazepam

Clinical Trials

Clinical Trials
PhaseStatusPurposeConditionsCount

Pharmacoeconomics

Manufacturers
Not Available
Packagers
Not Available
Dosage Forms
FormRouteStrength
InjectionIntramuscular; Intravenous
Prices
Not Available
Patents
Not Available

Properties

State
Not Available
Experimental Properties
Not Available
Predicted Properties
PropertyValueSource
Water Solubility0.269 mg/mLALOGPS
logP1.76ALOGPS
logP1.26ChemAxon
logS-3ALOGPS
pKa (Strongest Basic)2.38ChemAxon
Physiological Charge0ChemAxon
Hydrogen Acceptor Count3ChemAxon
Hydrogen Donor Count0ChemAxon
Polar Surface Area50.49 Å2ChemAxon
Rotatable Bond Count1ChemAxon
Refractivity87.97 m3·mol-1ChemAxon
Polarizability28.9 Å3ChemAxon
Number of Rings3ChemAxon
Bioavailability1ChemAxon
Rule of FiveYesChemAxon
Ghose FilterYesChemAxon
Veber's RuleNoChemAxon
MDDR-like RuleNoChemAxon
Predicted ADMET Features
Not Available

Spectra

Mass Spec (NIST)
Not Available
Spectra
SpectrumSpectrum TypeSplash Key
Predicted GC-MS Spectrum - GC-MSPredicted GC-MSNot Available
Predicted MS/MS Spectrum - 10V, Positive (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 20V, Positive (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 40V, Positive (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 10V, Negative (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 20V, Negative (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 40V, Negative (Annotated)Predicted LC-MS/MSNot Available

Drug created at February 26, 2016 17:46 / Updated at February 21, 2021 18:53