Drug/Small Molecule:
triazolam

PharmGKB contains no dosing guidelines for this drug/small molecule. 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 drug/small molecule. 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.

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.

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This is a non-comprehensive list of genetic tests with pharmacogenetics relevance, typically submitted by the manufacturer and manually curated by PharmGKB. The information listed is provided for educational purposes only and does not constitute an endorsement of any listed test or manufacturer.

A more complete listing of genetic tests is found at the Genetic Testing Registry (GTR).

PGx Test Variants Assayed Gene?

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 triazolam variant annotations

Gene ? Variant?
(142)
Alternate Names ? Drugs ? Alleles ?
(+ chr strand)
Function ? Amino Acid?
Translation
VIP No Clinical Annotations available No Variant Annotations available
rs776746 12083G>A, 219-237G>A, 321-1G>A, 37303382C>T, 581-237G>A, 689-1G>A, 99270539C>T, CYP3A5*1, CYP3A5*3, CYP3A5*3C, CYP3A5:6986A>G, g.6986A>G, intron 3 splicing defect, rs776746 A>G
C > T
Acceptor
Alleles, Functions, and Amino Acid Translations are all sourced from dbSNP 142
2D structure from PubChem
provided by PubChem

Overview

Generic Names
  • DEA No. 2887
  • Triazolamum [INN-Latin]
Trade Names
  • Alti-Triazolam
  • Apo-Triazo
  • Clorazolam
  • Gen-Triazolam
  • Halcion
  • Novidorm
  • Novo-Triolam
  • Novodorm
  • Songar
Brand Mixture Names

PharmGKB Accession Id:
PA451753

Description

Withdrawn in the United Kingdom due to risk of psychiatric adverse drug reactions. This drug continues to be available in the U.S. Internationally, triazolam is a Schedule IV drug under the Convention on Psychotropic Substances.

Source: Drug Bank

Indication

For the short-term treatment of insomnia.

Source: Drug Bank

Other Vocabularies

Information pulled from DrugBank has not been reviewed by PharmGKB.

Pharmacology, Interactions, and Contraindications

Mechanism of Action

Benzodiazepines bind nonspecifically to bezodiazepine receptors BNZ1, which mediates sleep, and BNZ2, which affects affects muscle relaxation, anticonvulsant activity, motor coordination, and memory. As benzodiazepine receptors are thought to be coupled to gamma-aminobutyric acid-A (GABA A) receptors, this enhances the effects of GABA by increasing GABA affinity for the GABA receptor. Binding of GABA to the site opens the chloride channel, resulting in a hyperpolarized cell membrane that prevents further excitation of the cell.

Source: Drug Bank

Pharmacology

A short-acting benzodiazepine used as a hypnotic agent in the treatment of insomnia. Some countries temporarily withdrew triazolam from the market because of concerns about adverse reactions, mostly psychological, associated with higher dose ranges. Its use at lower doses with appropriate care and labeling has been reaffirmed by the FDA and most other countries. Triazolam has a shorter half-life than chlordiazepoxide, flurazepam, and prazepam and does not generate active metabolites.

Source: Drug Bank

Absorption, Distribution, Metabolism, Elimination & Toxicity

Biotransformation

Hepatic. Small amounts of unmetabolized triazolam appear in the urine.

Source: Drug Bank

Absorption

Bioavailability is 44% (oral) and 53% (sublingual).

Source: Drug Bank

Half-Life

1.5-5.5 hours

Source: Drug Bank

Toxicity

Symptoms of overdose include drowsiness, slurred speech, motor inco-ordination, coma, and respiratory depression.

Source: Drug Bank

Route of Elimination

Triazolam and its metabolites, principally as conjugated glucuronides, which are presumably inactive, are excreted primarily in the urine. Only small amounts of unmetabolized triazolam appear in the urine. The two primary metabolites accounted for 79.9% of urinary excretion.

Source: Drug Bank

Chemical Properties

Chemical Formula

C17H12Cl2N4

Source: Drug Bank

Isomeric SMILES

Cc1nnc2n1-c3ccc(cc3C(=NC2)c4ccccc4Cl)Cl

Source: OpenEye

Canonical SMILES

CC1=NN=C2CN=C(C3=CC=CC=C3Cl)C3=C(C=CC(Cl)=C3)N12

Source: Drug Bank

Average Molecular Weight

343.21

Source: Drug Bank

Monoisotopic Molecular Weight

342.043901818

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 ?

EvidenceGene
No Dosing Guideline available No Drug Label available No Clinical Annotation available No Variant Annotation available VIP No VIP available
CYP3A4
No Dosing Guideline available No Drug Label available No Clinical Annotation available No Variant Annotation available VIP No VIP available
CYP3A5

Drug Targets

Gene Description
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)
TSPO (source: Drug Bank)

Drug Interactions

Drug Description
triazolam Increases the effect and toxicity of benzodiazepine (source: Drug Bank)
triazolam Increases the effect and toxicity of benzodiazepine (source: Drug Bank)
triazolam Increases the effect and toxicity of benzodiazepine (source: Drug Bank)
triazolam Increases the effect and toxicity of benzodiazepine (source: Drug Bank)
triazolam Increases the effect and toxicity of benzodiazepine (source: Drug Bank)
triazolam Increases the effect of the benzodiazepine (source: Drug Bank)
triazolam Increases the effect of the benzodiazepine (source: Drug Bank)
triazolam The macrolide increases the effect of the benzodiazepine (source: Drug Bank)
triazolam The macrolide increases the effect of the benzodiazepine (source: Drug Bank)
triazolam Increased risk of toxicity (source: Drug Bank)
triazolam Increased risk of toxicity (source: Drug Bank)
triazolam The antiviral agent increases the effect and toxicity of benzodiazepine (source: Drug Bank)
triazolam The antiviral agent increases the effect and toxicity of benzodiazepine (source: Drug Bank)
triazolam The calcium channel blocker increases the effect and toxicity of the benzodiazepine (source: Drug Bank)
triazolam The calcium channel blocker increases the effect and toxicity of the benzodiazepine (source: Drug Bank)
triazolam The antiviral agent increases the effect and toxicity of benzodiazepine (source: Drug Bank)
triazolam The antiviral agent increases the effect and toxicity of benzodiazepine (source: Drug Bank)
triazolam The macrolide increases the effect of the benzodiazepine (source: Drug Bank)
triazolam The macrolide increases the effect of the benzodiazepine (source: Drug Bank)
triazolam Increases the effect of the benzodiazepine (source: Drug Bank)
triazolam Increases the effect of the benzodiazepine (source: Drug Bank)
triazolam Amprenavir increases the effect and toxicity of benzodiazepine (source: Drug Bank)
triazolam Amprenavir increases the effect and toxicity of benzodiazepine (source: Drug Bank)
triazolam Possible increased levels of the hydantoin, decrease of benzodiazepine (source: Drug Bank)
triazolam The protease inhibitor increases the effect of the benzodiazepine (source: Drug Bank)
triazolam The protease inhibitor increases the effect of the benzodiazepine (source: Drug Bank)
triazolam The imidazole increases the effect of the benzodiazepine (source: Drug Bank)
triazolam The imidazole increases the effect of the benzodiazepine (source: Drug Bank)
triazolam The imidazole increases the effect of the benzodiazepine (source: Drug Bank)
triazolam The imidazole increases the effect of the benzodiazepine (source: Drug Bank)
triazolam Modafinil decreases the effect of triazolam (source: Drug Bank)
triazolam Modafinil decreases the effect of triazolam (source: Drug Bank)
triazolam Nefazodone increases the effect of triazolam (source: Drug Bank)
triazolam Nefazodone increases the effect of triazolam (source: Drug Bank)
triazolam The protease inhibitor increases the effect of the benzodiazepine (source: Drug Bank)
triazolam The protease inhibitor increases the effect of the benzodiazepine (source: Drug Bank)
triazolam Omeprazole increases the effect of benzodiazepine (source: Drug Bank)
triazolam Omeprazole increases the effect of benzodiazepine (source: Drug Bank)
triazolam Possible increased levels of the hydantoin, decrease of benzodiazepine (source: Drug Bank)
triazolam Possible increased levels of the hydantoin, decrease of benzodiazepine (source: Drug Bank)
triazolam Rifampin decreases the effect of benzodiazepine (source: Drug Bank)
triazolam Rifampin decreases the effect of benzodiazepine (source: Drug Bank)
triazolam Telithromycin increases the effect/toxicity of the benzodiazepine (source: Drug Bank)
triazolam Telithromycin may reduce clearance of Triazolam. Consider alternate therapy or monitor for changes in the therapeutic/adverse effects of Triazolam if Telithromycin is initiated, discontinued or dose changed. (source: Drug Bank)
triazolam Tipranavir, co-administered with Ritonavir, may increase the plasma concentration of Triazolam. Concomitant therapy is contraindicated. (source: Drug Bank)
amprenavir Amprenavir increases the effect and toxicity of benzodiazepine (source: Drug Bank)
amprenavir Amprenavir increases the effect and toxicity of benzodiazepine (source: Drug Bank)
aprepitant Aprepitant increases the effect and toxicity of benzodiazepine (source: Drug Bank)
atazanavir Atazanavir increases the effect and toxicity of benzodiazepine (source: Drug Bank)
atazanavir Atazanavir increases the effect and toxicity of benzodiazepine (source: Drug Bank)
cimetidine Cimetidine increases the effect and toxicity of benzodiazepine (source: Drug Bank)
cimetidine Cimetidine increases the effect and toxicity of benzodiazepine (source: Drug Bank)
clarithromycin The macrolide increases the effect of the benzodiazepine (source: Drug Bank)
clarithromycin The macrolide increases the effect of the benzodiazepine (source: Drug Bank)
clozapine Increased risk of toxicity (source: Drug Bank)
clozapine Increased risk of toxicity (source: Drug Bank)
delavirdine The antiviral agent increases the effect and toxicity of benzodiazepine (source: Drug Bank)
delavirdine The antiviral agent increases the effect and toxicity of benzodiazepine (source: Drug Bank)
diltiazem The calcium channel blocker increases the effect and toxicity of the benzodiazepine (source: Drug Bank)
diltiazem The calcium channel blocker increases the effect and toxicity of the benzodiazepine (source: Drug Bank)
efavirenz The antiviral agent increases the effect and toxicity of benzodiazepine (source: Drug Bank)
efavirenz The antiviral agent increases the effect and toxicity of benzodiazepine (source: Drug Bank)
erythromycin The macrolide increases the effect of the benzodiazepine (source: Drug Bank)
erythromycin The macrolide increases the effect of the benzodiazepine (source: Drug Bank)
ethotoin Possible increased levels of the hydantoin, decrease of benzodiazepine (source: Drug Bank)
fluconazole Fluconazole increases the effect of the benzodiazepine (source: Drug Bank)
fluconazole Fluconazole increases the effect of the benzodiazepine (source: Drug Bank)
fosamprenavir Amprenavir increases the effect and toxicity of benzodiazepine (source: Drug Bank)
fosamprenavir Amprenavir increases the effect and toxicity of benzodiazepine (source: Drug Bank)
fosphenytoin Possible increased levels of the hydantoin, decrease of benzodiazepine (source: Drug Bank)
indinavir The protease inhibitor increases the effect of the benzodiazepine (source: Drug Bank)
indinavir The protease inhibitor increases the effect of the benzodiazepine (source: Drug Bank)
itraconazole The imidazole increases the effect of the benzodiazepine (source: Drug Bank)
itraconazole The imidazole increases the effect of the benzodiazepine (source: Drug Bank)
josamycin The macrolide increases the effect of the benzodiazepine (source: Drug Bank)
ketoconazole The imidazole increases the effect of the benzodiazepine (source: Drug Bank)
ketoconazole The imidazole increases the effect of the benzodiazepine (source: Drug Bank)
mephenytoin Possible increased levels of the hydantoin, decrease of benzodiazepine (source: Drug Bank)
mephenytoin Possible increased levels of the hydantoin, decrease of benzodiazepine (source: Drug Bank)
modafinil Modafinil decreases the effect of triazolam (source: Drug Bank)
modafinil Modafinil decreases the effect of triazolam (source: Drug Bank)
nefazodone Nefazodone increases the effect of triazolam (source: Drug Bank)
nefazodone Nefazodone increases the effect of triazolam (source: Drug Bank)
nelfinavir The protease inhibitor increases the effect of the benzodiazepine (source: Drug Bank)
nelfinavir The protease inhibitor increases the effect of the benzodiazepine (source: Drug Bank)
omeprazole Omeprazole increases the effect of the benzodiazepine (source: Drug Bank)
omeprazole Omeprazole increases the effect of the benzodiazepine (source: Drug Bank)
phenytoin Possible increased levels of the hydantoin, decrease of benzodiazepine (source: Drug Bank)
phenytoin Possible increased levels of the hydantoin, decrease of benzodiazepine (source: Drug Bank)
rifampin Rifampin decreases the effect of the benzodiazepine (source: Drug Bank)
rifampin Rifampin decreases the effect of the benzodiazepine (source: Drug Bank)
ritonavir The protease inhibitor increases the effect of the benzodiazepine (source: Drug Bank)
ritonavir The protease inhibitor increases the effect of the benzodiazepine (source: Drug Bank)
saquinavir The protease inhibitor increases the effect of the benzodiazepine (source: Drug Bank)
saquinavir The protease inhibitor increases the effect of the benzodiazepine (source: Drug Bank)
telithromycin Telithromycin increases the effect/toxicity of the benzodiazepine (source: Drug Bank)
telithromycin Telithromycin increases the effect/toxicity of the benzodiazepine (source: Drug Bank)
verapamil The calcium channel blocker increases the effect and toxicity of the benzodiazepine (source: Drug Bank)
verapamil The calcium channel blocker increases the effect and toxicity of the benzodiazepine (source: Drug Bank)
voriconazole The imidazole increases the effect of the benzodiazepine (source: Drug Bank)
voriconazole The imidazole increases the effect of the benzodiazepine (source: Drug Bank)
triazolam The CNS depressants, Triprolidine and Triazolam, may increase adverse/toxic effects due to additivity. Monitor for increased CNS depressant effects during concomitant therapy. (source: Drug Bank)
triazolam The CNS depressants, Triprolidine and Triazolam, may increase adverse/toxic effects due to additivity. Monitor for increased CNS depressant effects during concomitant therapy. (source: Drug Bank)
triazolam Verapamil may increase the serum concentration of Triazolam by decreasing its metabolism. Avoid concomitant therapy if possible or consider a dose reduction in the initial dose of Triazolam. (source: Drug Bank)
triazolam Voriconazole may increase the serum concentration of triazolam by decreasing its metabolism. Monitor for triazolam toxicity if voriconazole is initiated or dose increased. (source: Drug Bank)

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

May Treat
Contraindicated With

Publications related to triazolam: 9

No Dosing Guideline available No Drug Label available No Clinical Annotation available No Variant Annotation available VIP No VIP available
PharmGKB summary: very important pharmacogene information for CYP3A5. Pharmacogenetics and genomics. 2012. Lamba Jatinder, 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
Machine learning methods and docking for predicting human pregnane X receptor activation. Chemical research in toxicology. 2008. Khandelwal Akash, 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
Effects of genetic polymorphism of cytochrome P450 enzymes on the pharmacokinetics of benzodiazepines. Journal of clinical pharmacy and therapeutics. 2007. Fukasawa T, 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
In vitro metabolism of midazolam, triazolam, nifedipine, and testosterone by human liver microsomes and recombinant cytochromes p450: role of cyp3a4 and cyp3a5. Drug metabolism and disposition: the biological fate of chemicals. 2003. Patki Kiran 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
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
Effect of modafinil on the pharmacokinetics of ethinyl estradiol and triazolam in healthy volunteers. Clinical pharmacology and therapeutics. 2002. Robertson Philmore, 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 benzodiazepine binding site of GABAA receptors. Trends in pharmacological sciences. 1997. Sigel E, et al. PubMed

LinkOuts

Web Resource:
Wikipedia
National Drug Code Directory:
0054-4858-51
DrugBank:
DB00897
ChEBI:
9674
KEGG Drug:
D00387
PubChem Compound:
5556
PubChem Substance:
46509147
7847453
Drugs Product Database (DPD):
2230024
ChemSpider:
5355
Therapeutic Targets Database:
DAP000244
FDA Drug Label at DailyMed:
db564864-17fc-4ba5-a438-a467ef57a0ca

Clinical Trials

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

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Sources for PharmGKB drug information: DrugBank, Open Eye Scientific Software.