Drug/Small Molecule:
delavirdine

2D structure

Overview

Generic Names: DLV; SPP
Trade Names: Bhap Der; Rescriptor
PharmGKB Accession Id: PA449223

Description

A potent, non-nucleoside reverse transcriptase inhibitor with activity specific for HIV-1. PubChem (source: Drug Bank)

Indication

For the treatment of HIV-1 infection in combination with appropriate antiretroviral agents when therapy is warranted (source: Drug Bank)

ATC Therapeutic Category

  • J05AG:Non-nucleoside reverse transcriptase inhibitors

Pharmacology, Interactions, and Contraindications

Mechanism Of Action

Delavirdine binds directly to viral reverse transcriptase (RT) and blocks the RNA-dependent and DNA-dependent DNA polymerase activities by disrupting the enzyme's catalytic site. (source: Drug Bank)

Pharmacology

Delavirdine is a non-nucleoside reverse transcriptase inhibitor (nNRTI) with activity against Human Immunodeficiency Virus Type 1 (HIV-1). Delavirdine binds directly to reverse transcriptase (RT) and blocks the RNA-dependent and DNA-dependent DNA polymerase activities by causing a disruption of the enzyme's catalytic site. The activity of Delavirdine does not compete with template or nucleoside triphosphates. HIV-2 RT and eukaryotic DNA polymerases (such as human DNA polymerases alpha, beta, or sigma) are not inhibited by Delavirdine. (source: Drug Bank)

Food Interactions

Take without regard to meals. (source: Drug Bank)

Absorption, Distribution, Metabolism, Elimination & Toxicity

Biotransformation

Hepatic (source: Drug Bank)

Protein Binding

98% (source: Drug Bank)

Absorption

Rapidly absorbed (source: Drug Bank)

Toxicity

Major toxicity of delavirdine is rash and should be advised to promptly notify their physician should rash occur. The majority of rashes associated with delavirdine occur within 1 to 3 weeks after initiating treatment with delavirdine. The rash normally resolves in 3 to 14 days and may be treated symptomatically while therapy with delavirdine is continued. Any patient experiencing severe rash or rash accompanied by symptoms such as fever, blistering, oral lesions, conjunctivitis, swelling, muscle or joint aches should discontinue medication and consult a physician. (source: Drug Bank)

Isomeric SMILES Code:

CC(C)NC1=C(N=CC=C1)N2CCN(CC2)C(=O)C3=CC4=C(N3)C=CC(=C4)NS(=O)(=O)C (source: Drug Bank)

The following genes are in curated knowledge about this drug.

  Gene Relationship Evidence
Phenotype data available Genotype Data Available Literature annotations available Has annotations
CYP2D6
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  • PK
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Publications

A list of non-curated publications that mention this drug along with other genes is available.

Drug Targets

Gene Description
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The following drugs are in curated knowledge about this drug.

  Drug Relationship Evidence
Phenotype data available Genotype Data Available Literature annotations available Not annotated
tamoxifen
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Publications

A list of non-curated publications that mention this drug along with other drugs is available.

Drug Interactions

Drug Description
alprazolam Uncurated Annotation The antiviral agent increases the effect and toxicity of benzodiazepine (source: Drug Bank)
amprenavir Uncurated Annotation Decreased levels of delavirdine with increased levels of amprenavir (source: Drug Bank)
astemizole Uncurated Annotation Increased risk of cardiotoxicity and arrhythmias (source: Drug Bank)
atorvastatin Uncurated Annotation The NNRT inhibitor increases the effect and toxicity of the statin (source: Drug Bank)
calcium Uncurated Annotation The antiacid decreases the effect of delavirdine (source: Drug Bank)
carbamazepine Uncurated Annotation The anticonvulsant decreases the effect of delavirdine (source: Drug Bank)
cisapride Uncurated Annotation Increased risk of cardiotoxicity adn arrhythmias (source: Drug Bank)
ergonovine Uncurated Annotation The antiretroviral agent may increase the ergot derivative toxicity (source: Drug Bank)
fosamprenavir Uncurated Annotation Decreased levels of delavirdine with increased levels of amprenavir (source: Drug Bank)
indinavir Uncurated Annotation Increases the effect of indinavir (source: Drug Bank)
lovastatin Uncurated Annotation The NNRT inhibitor increases the effect and toxicity of the statin (source: Drug Bank)
magnesium Uncurated Annotation The antiacid decreases the effect of delavirdine (source: Drug Bank)
magnesium oxide Uncurated Annotation The antiacid decreases the effect of delavirdine (source: Drug Bank)
methylergonovine Uncurated Annotation The antiretroviral agent may increase the ergot derivative toxicity (source: Drug Bank)
methylphenobarbital Uncurated Annotation The anticonvulsant decreases the effect of delavirdine (source: Drug Bank)
midazolam Uncurated Annotation The antiviral agent increases the effect and toxicity of benzodiazepine (source: Drug Bank)
phenobarbital Uncurated Annotation The anticonvulsant decreases the effect of delavirdine (source: Drug Bank)
phenytoin Uncurated Annotation The anticonvulsant decreases the effect of delavirdine (source: Drug Bank)
rifabutin Uncurated Annotation Rifabutin decreases the effect of delavirdine (source: Drug Bank)
rifampin Uncurated Annotation Rifampin decreases the effect of delavirdine (source: Drug Bank)
ritonavir Uncurated Annotation Increases the effect of ritonavir (source: Drug Bank)
saquinavir Uncurated Annotation Increases the effect of saquinavir and hepatic toxicity (source: Drug Bank)
simvastatin Uncurated Annotation The NNRT inhibitor increases the effect and toxicity of the statin (source: Drug Bank)
terfenadine Uncurated Annotation Increased risk of cardiotoxicity and arrhythmias (source: Drug Bank)
triazolam Uncurated Annotation The antiviral agent increases the effect and toxicity of benzodiazepine (source: Drug Bank)

Non-Curated Information

A list of non-curated publications that mention this drug along with other diseases is available.

LinkOuts

Web Resource:
Wikipedia
DrugBank:
DB00705
KEGG Compound ID:
C06941
PubChem Compound ID:
5625
PubChem Substance ID:
206947

Common Searches

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Non-Curated Publications

A list of non-curated publications that mention this drug is available.

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