Chemical: Drug
oxazepam

PharmGKB contains no dosing guidelines for this . To report known genotype-based dosing guidelines, or if you are interested in developing guidelines, click here.

PharmGKB has no annotated drug labels with pharmacogenomic information for this . If you know of a drug label with PGx, send us a message.

PharmGKB contains no Clinical Variants that meet the highest level of criteria.

To see more Clinical Variants with lower levels of criteria, click the button at the bottom of the page.

Disclaimer: The PharmGKB's clinical annotations reflect expert consensus based on clinical evidence and peer-reviewed literature available at the time they are written and are intended only to assist clinicians in decision-making and to identify questions for further research. New evidence may have emerged since the time an annotation was submitted to the PharmGKB. The annotations are limited in scope and are not applicable to interventions or diseases that are not specifically identified.

The annotations do not account for individual variations among patients, and cannot be considered inclusive of all proper methods of care or exclusive of other treatments. It remains the responsibility of the health-care provider to determine the best course of treatment for a patient. Adherence to any guideline is voluntary, with the ultimate determination regarding its application to be made solely by the clinician and the patient. PharmGKB assumes no responsibility for any injury or damage to persons or property arising out of or related to any use of the PharmGKB clinical annotations, or for any errors or omissions.

? = Mouse-over for quick help

The table below contains information about pharmacogenomic variants on PharmGKB. Please follow the link in the "Variant" column for more information about a particular variant. Each link in the "Variant" column leads to the corresponding PharmGKB Variant Page. The Variant Page contains summary data, including PharmGKB manually curated information about variant-drug pairs based on individual PubMed publications. The PMIDs for these PubMed publications can be found on the Variant Page.

The tags in the first column of the table indicate what type of information can be found on the corresponding Variant Page.

Links in the "Gene" column lead to PharmGKB Gene Pages.

List of all variant annotations for oxazepam

Gene ? Variant?
(147)
Alternate Names ? Chemicals ? Alleles ?
(+ chr strand)
Function ? Amino Acid?
Translation
No VIP available CA VA
rs1902023 NC_000004.11:g.69536084A=, NC_000004.11:g.69536084A>C, NC_000004.12:g.68670366A=, NC_000004.12:g.68670366A>C, NM_001076.3:c.253T=, NM_001076.3:c.253T>G, NP_001067.2:p.Tyr85=, NP_001067.2:p.Tyr85Asp, NT_167250.1:g.248671C=, NT_167250.1:g.248671C>A, NT_167250.2:g.246721C=, NT_167250.2:g.246721C>A, rs141137354, rs52823570, rs57851547
A > C
SNP
Y85D
Alleles, Functions, and Amino Acid Translations are all sourced from dbSNP 147

Overview

Generic Names
  • Oxazipam
  • Oxozepam
  • d-Oxazepam hemisuccinate
Trade Names
  • Adumbran
  • Ansioxacepam
  • Anxiolit
  • Aplakil
  • Astress
  • Azutranquil
  • Bonare
  • Drimuel
  • Droxacepam
  • Durazepam
  • Enidrel
  • Hi-Long
  • Isodin
  • Lederpam
  • Limbial
  • Murelax
  • Nesontil
  • Noctazepam
  • Notaral
  • Oxa-puren
  • Oxanid
  • Pacienx
  • Praxiten
  • Propax
  • Psiquiwas
  • QUEN
  • Quilibrex
  • Rondar
  • Sedigoa
  • Serax
  • Serenal
  • Serenid
  • Serenid-D
  • Serepax
  • Seresta
  • Serpax
  • Sigacalm
  • Sobril
  • Tacepam
  • Tazepam
  • Uskan
  • Vaben
  • Wy-3498 stic
  • Zaxopam
Brand Mixture Names

PharmGKB Accession Id

PA450731

Type(s):

Drug

Description

Oxazepam is an intermediate-acting benzodiazepine used to treat alcohol withdrawal and anxiety disorders.

Source: Drug Bank

Indication

For the treatment of anxiety disorders and alcohol withdrawal.

Source: Drug Bank

Other Vocabularies

Information pulled from DrugBank has not been reviewed by PharmGKB.

Pharmacology, Interactions, and Contraindications

Mechanism of Action

Similar to other benzodiazepines, oxazepam exerts its anxiolytic effects by potentiating the effect of gamma-aminobutyric acid (GABA) on GABA-A receptors through a cooperative mechanism of action. GABA receptors are ionotropic chloride-linked channel receptors that produce inhibitory postsynaptic potentials. When activated by GABA, the GABA receptor/chloride ionophore complex undergoes a conformational change that allows the passage of chloride ions through the channel. Benzodiazepines are believed to exert their effect by increasing the effect of GABA at its receptor. Benzodiazepine binding increases chloride conductance in the presence of GABA by increasing the frequency at which the channel opens. In contrast, barbiturates increase chloride conductance in the presence of GABA by prolonging the time in which the channel remains open. There are 18 subtypes of the GABA receptor subunits. The alpha 2 subunit of the alpha ~2~beta ~3~gamma 2 receptor complex is thought to mediate anxiolytic effects while the alpha 1 subunit of the alpha ~1~beta ~2~gamma 2 receptor complex is thought to mediate sedative, anticonvulsant and anterograde amnesia effects.

Source: Drug Bank

Pharmacology

Oxazepam is believed to stimulate GABA receptors in the ascending reticular activating system. Since GABA is inhibitory, receptor stimulation increases inhibition and blocks both cortical and limbic arousal following stimulation of the brain stem reticular formation.

Source: Drug Bank

Food Interaction

Avoid alcohol.|Avoid excessive quantities of coffee or tea (Caffeine).|Take with food.

Source: Drug Bank

Absorption, Distribution, Metabolism, Elimination & Toxicity

Biotransformation

No active metabolites. Metabolized via conjugation prior to elimination.

Source: Drug Bank

Protein Binding

80-99%

Source: Drug Bank

Absorption

Well absorbed from the gastrointestinal tract following oral administration. Time to peak concentration = 2-4 hours. Onset of action is slow, > 3 hours, following oral administration.

Source: Drug Bank

Half-Life

5-15 hours

Source: Drug Bank

Toxicity

Symptoms of overdose include confusion, drowsiness, and lethargy.

Source: Drug Bank

Route of Elimination

This product has a single, major inactive metabolite in man, a glucuronide excreted in the urine.

Source: Drug Bank

Chemical Properties

Chemical Formula

C15H11ClN2O2

Source: Drug Bank

Isomeric SMILES

c1ccc(cc1)C2=NC(C(=O)Nc3c2cc(cc3)Cl)O

Source: OpenEye

Canonical SMILES

OC1N=C(C2=CC=CC=C2)C2=C(NC1=O)C=CC(Cl)=C2

Source: Drug Bank

Average Molecular Weight

286.713

Source: Drug Bank

Monoisotopic Molecular Weight

286.050905313

Source: Drug Bank

SMILES

OC1N=C(C2=CC=CC=C2)C2=C(NC1=O)C=CC(Cl)=C2

Source: Drug Bank

InChI String

InChI=1S/C15H11ClN2O2/c16-10-6-7-12-11(8-10)13(9-4-2-1-3-5-9)18-15(20)14(19)17-12/h1-8,15,20H,(H,17,19)

Source: Drug Bank

PharmGKB Curated Pathways

Pathways created internally by PharmGKB based primarily on literature evidence.

External Pathways

Links to non-PharmGKB pathways.

PharmGKB contains no links to external pathways for this drug. To report a pathway, click here.

Genes that are associated with this drug in PharmGKB's database based on (1) variant annotations, (2) literature review, (3) pathways or (4) information automatically retrieved from DrugBank, depending on the "evidence" and "source" listed below.

Curated Information ?

Drug Targets

Gene Description
ALB (source: Drug Bank)
GABRA1 (source: Drug Bank)
GABRA2 (source: Drug Bank)
GABRA3 (source: Drug Bank)
GABRA4 (source: Drug Bank)
GABRA5 (source: Drug Bank)
GABRA6 (source: Drug Bank)
GABRB1 (source: Drug Bank)
GABRB2 (source: Drug Bank)
GABRB3 (source: Drug Bank)
GABRD (source: Drug Bank)
GABRE (source: Drug Bank)
GABRG1 (source: Drug Bank)
GABRG2 (source: Drug Bank)
GABRG3 (source: Drug Bank)
GABRP (source: Drug Bank)
GABRQ (source: Drug Bank)
GABRR1 (source: Drug Bank)
GABRR2 (source: Drug Bank)
GABRR3 (source: Drug Bank)

Drug Interactions

Interaction Description
clozapine - oxazepam Increased risk of toxicity (source: Drug Bank)
clozapine - oxazepam Increased risk of toxicity (source: Drug Bank)
oxazepam - clozapine Increased risk of toxicity (source: Drug Bank)
oxazepam - clozapine Increased risk of toxicity (source: Drug Bank)
oxazepam - mephenytoin Possible increased levels of the hydantoin, decrease of benzodiazepine (source: Drug Bank)
oxazepam - phenytoin Possible increased levels of the hydantoin, decrease of benzodiazepine (source: Drug Bank)
phenytoin - oxazepam Possible increased levels of the hydantoin, decrease of benzodiazepine (source: Drug Bank)
phenytoin - oxazepam Possible increased levels of the hydantoin, decrease of benzodiazepine (source: Drug Bank)
triprolidine - oxazepam The CNS depressants, Triprolidine and Oxazepam, may increase adverse/toxic effects due to additivity. Monitor for increased CNS depressant effects during concomitant therapy. (source: Drug Bank)
triprolidine - oxazepam The CNS depressants, Triprolidine and Oxazepam, may increase adverse/toxic effects due to additivity. Monitor for increased CNS depressant effects during concomitant therapy. (source: Drug Bank)

Curated Information ?

Relationships from National Drug File - Reference Terminology (NDF-RT)

May Treat
Contraindicated With

Publications related to oxazepam: 10

No Dosing Guideline available No Drug Label available CA VA No VIP available No VIP available
Evidence for oxazepam as an in vivo probe of UGT2B15: oxazepam clearance is reduced by UGT2B15 D85Y polymorphism but unaffected by UGT2B17 deletion. British journal of clinical pharmacology. 2009. He Xi, et al. PubMed
No Dosing Guideline available No Drug Label available CA No Variant Annotation available No VIP available No VIP available
Effect of the UGT2B15 genotype on the pharmacokinetics, pharmacodynamics, and drug interactions of intravenous lorazepam in healthy volunteers. Clinical pharmacology and therapeutics. 2005. Chung Jae-Yong, et al. PubMed
No Dosing Guideline available No Drug Label available CA VA No VIP available No VIP available
UDP-glucuronosyltransferase (UGT) 2B15 pharmacogenetics: UGT2B15 D85Y genotype and gender are major determinants of oxazepam glucuronidation by human liver. The Journal of pharmacology and experimental therapeutics. 2004. Court Michael H, et al. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available No Variant Annotation available No VIP available No VIP available
The benzodiazepine site of the GABAA receptor: an old target with new potential?. Sleep medicine. 2004. Bateson Alan N. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available No Variant Annotation available No VIP available No VIP available
Stereoselective conjugation of oxazepam by human UDP-glucuronosyltransferases (UGTs): S-oxazepam is glucuronidated by UGT2B15, while R-oxazepam is glucuronidated by UGT2B7 and UGT1A9. Drug metabolism and disposition: the biological fate of chemicals. 2002. Court Michael H, et al. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available No Variant Annotation available No VIP available No VIP available
Mapping of the benzodiazepine recognition site on GABA(A) receptors. Current topics in medicinal chemistry. 2002. Sigel Erwin. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available No Variant Annotation available No VIP available No VIP available
Med-psych drug-drug interactions update. Psychosomatics. 2002. Armstrong Scott C, et al. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available No Variant Annotation available No VIP available No VIP available
New insights into the role of the GABA(A)-benzodiazepine receptor in psychiatric disorder. The British journal of psychiatry : the journal of mental science. 2001. Nutt D J, et al. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available No Variant Annotation available No VIP available No VIP available
The glucuronidation of opioids, other xenobiotics, and androgens by human UGT2B7Y(268) and UGT2B7H(268). Drug metabolism and disposition: the biological fate of chemicals. 1998. Coffman B L, et al. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available No Variant Annotation available No VIP available No VIP available
The benzodiazepine binding site of GABAA receptors. Trends in pharmacological sciences. 1997. Sigel E, et al. PubMed

LinkOuts

Web Resource:
Wikipedia
National Drug Code Directory:
0228-2067-10
DrugBank:
DB00842
ChEBI:
7823
KEGG Compound:
C07359
KEGG Drug:
D00464
PubChem Compound:
4616
PubChem Substance:
46506031
9563
Drugs Product Database (DPD):
726370
ChemSpider:
4455
Therapeutic Targets Database:
DAP000243
FDA Drug Label at DailyMed:
a0d5a4c1-ec79-42e6-8e8f-ae4d144edb43

Clinical Trials

These are trials that mention oxazepam and are related to either pharmacogenetics or pharmacogenomics.

No trials loaded.

NURSA Datasets

provided by nursa.org

No NURSA datasets available.

Common Searches

Search PubMed
Search Medline Plus
Search PubChem
Search CTD

Sources for PharmGKB drug information: DrugBank, PubChem.