Drug/Small Molecule:
lorazepam

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.

Links to Unannotated Labels

These links are to labels associated with lorazepam that have not been annotated by PharmGKB.

  1. DailyMed - DrugLabel PA166105181

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.

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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.

Gene ? Variant?
(138)
Alternate Names / Tag SNPs ? Drugs ? Alleles ?
(+ chr strand)
Function ? Amino Acid?
Translation
No VIP available No Clinical Annotations available VA
rs1902023 248671C>C, 253T>G, 291G/T, 69536084A>C, 9746751A>C, D85Y, Tyr85Asp, UGT2B15*2, UGT2B15:D85Y, UGT2B15:Y85D
C > A
Missense
Tyr85Asp
No VIP available No Clinical Annotations available VA
rs7438284 10175004A>T, 69964337A>T, 801A>T, Pro267=
A > T
Synonymous
Pro267Pro
No VIP available CA VA
rs7439366 10175005T>C, 69964338T>C, 802T>C, Tyr268His, UGT2B7*2, UGT2B7:802C>T, UGT2B7:H268Y, UGT2B7Y
T > C
Missense
Tyr268His
Alleles, Functions, and Amino Acid Translations are all sourced from dbSNP 138
2D structure from PubChem
provided by PubChem

Overview

Generic Names
  • (+/-)-Lorazepam
  • L-Lorazepam Acetate
  • O-Chlorooxazepam
  • O-Chloroxazepam
Trade Names
  • Almazine
  • Alzapam
  • Anxiedin
  • Aplacassee
  • Ativan
  • Bonatranquan
  • Delormetazepam
  • Emotival
  • Idalprem
  • Lorabenz
  • Lorax
  • Loraz
  • Lorazepam Intensol
  • Lorsilan
  • Pro Dorm
  • Psicopax
  • Punktyl
  • Quait
  • Securit
  • Sedatival
  • Sedazin
  • Somagerol
  • Tavor
  • Temesta
  • Wypax
Brand Mixture Names

PharmGKB Accession Id:
PA450267

Description

A benzodiazepine used as an anti-anxiety agent with few side effects. It also has hypnotic, anticonvulsant, and considerable sedative properties and has been proposed as a preanesthetic agent.

Source: Drug Bank

Indication

For the management of anxiety disorders, and for treatment of status epilepticus.

Source: Drug Bank

Other Vocabularies

Information pulled from DrugBank has not been reviewed by PharmGKB.

Pharmacology, Interactions, and Contraindications

Mechanism of Action

Lorazepam binds to an allosteric site on GABA-A receptors, which are pentameric ionotropic receptors in the CNS. Binding potentiates the effects of the inhibitory neurotransmitter GABA, which upon binding opens the chloride channel in the receptor, allowing chloride influx and causing hyperpolerization of the neuron.

Source: Drug Bank

Pharmacology

Lorazepam, a benzodiazepine not transformed to active metabolites, is used to treat anxiety, status epilepticus, and for sedation induction and anterograde amnesia.

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

Hepatic

Source: Drug Bank

Protein Binding

85%

Source: Drug Bank

Absorption

Readily absorbed with an absolute bioavailability of 90%.

Source: Drug Bank

Half-Life

12 hours

Source: Drug Bank

Toxicity

Somnolence, confusion, and coma, LD 50=3178mg/kg (orally in mice).

Source: Drug Bank

Route of Elimination

Lorazepam is rapidly conjugated at its 3-hydroxy group into lorazepam glucuronide which is then excreted in the urine.

Source: Drug Bank

Chemical Properties

Chemical Formula

C15H10Cl2N2O2

Source: Drug Bank

Isomeric SMILES

c1ccc(c(c1)C2=NC(C(=O)Nc3c2cc(cc3)Cl)O)Cl

Source: OpenEye

Canonical SMILES

OC1N=C(C2=CC=CC=C2Cl)C2=C(NC1=O)C=CC(Cl)=C2

Source: Drug Bank

Average Molecular Weight

321.158

Source: Drug Bank

Monoisotopic Molecular Weight

320.011932988

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 VA No VIP available No VIP available
UGT2B15
No Dosing Guideline available No Drug Label available CA VA No VIP available No VIP available
UGT2B7

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
lorazepam Increased risk of toxicity (source: Drug Bank)
lorazepam Increased risk of toxicity (source: Drug Bank)
clozapine Increased risk of toxicity (source: Drug Bank)
clozapine Increased risk of toxicity (source: Drug Bank)
mephenytoin 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)
lorazepam Possible increased levels of the hydantoin, decrease of benzodiazepine (source: Drug Bank)
lorazepam Possible increased levels of the hydantoin, decrease of benzodiazepine (source: Drug Bank)
lorazepam The CNS depressants, Triprolidine and Lorazepam, may increase adverse/toxic effects due to additivity. Monitor for increased CNS depressant effects during concomitant therapy. (source: Drug Bank)
lorazepam The CNS depressants, Triprolidine and Lorazepam, may increase adverse/toxic effects due to additivity. Monitor for increased CNS depressant effects during concomitant therapy. (source: Drug Bank)
lorazepam Valproic acid may increase the serum concentration of Lorazepam by reducing Lorazepam metabolism. The Lorazepam dose should be reduced by 50% during concomitant therapy. Monitor for increased Lorazepam effects and toxicity. (source: Drug Bank)

Publications related to lorazepam: 8

No Dosing Guideline available No Drug Label available CA VA No VIP available No VIP available
Pharmacokinetic and pharmacodynamic interaction of lorazepam and valproic acid in relation to UGT2B7 genetic polymorphism in healthy subjects. Clinical pharmacology and therapeutics. 2008. Chung J-Y, et al. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available VA 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 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
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
Inhibitory effect of azole antifungal agents on the glucuronidation of lorazepam using rabbit liver microsomes in vitro. Biological & pharmaceutical bulletin. 2000. Sawamura R, 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:
0054-3532-44
DrugBank:
DB00186
KEGG Drug:
D00365
PubChem Compound:
3958
PubChem Substance:
156663
46508468
Drugs Product Database (DPD):
2243278
ChemSpider:
3821
Therapeutic Targets Database:
DAP000237
FDA Drug Label at DailyMed:
5ff82103-cc57-4af9-9362-82a7c686271d

Clinical Trials

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

Common Searches

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