Delavirdine

Table of contents

  • Brand Names
  • Chemistry
  • Pharmacologic Category
  • Mechanism of Action
  • Therapeutic Use
  • Pregnancy and Lactation Implications
  • Contraindications
  • Warnings and Precautions
  • Adverse Reactions
  • Caution and personalized dose adjustment in patients with the following genotypes
  • Substrate of
  • Inhibits
  • Drug Interactions
  • Nutrition/Nutraceutical Interactions
  • Dosage
  • Pharmacokinetics and Pharmacodynamics
  • Special Considerations

Brand Names

Europe

Greece: Rescriptor.

North America

Canada: Rescriptor; USA: Rescriptor.

Asia

Japan: Rescriptor.

Drug combinations

Chemistry

Delavirdine Mesylate: C~22~H~28~N~6~O~3~S CH~4~O~3~S. Mw: 552.67. (1) Piperazine, 1-[3-[(1-methylethyl)amino]-2-pyridinyl]-4-[[5-[(methylsulfonyl)amino]-1H-indol-2-yl]carbonyl]-, monomethanesulfonate; (2) 1-[3-(Isopropylamino)-2-pyridyl]-4-[(5-methanesulfonamidoindol-2-yl)carbonyl]piperazine monomethanesulfonate. CAS-147221-93-0; CAS-136817-59-9 (delavirdine)(1994).

Pharmacologic Category

Antiretrovirals; Non-nucleoside Reverse Transcriptase Inhibitors. (ATC-Code: J05AG02).

Mechanism of action

Binds directly to reverse transcriptase, blocking RNA-dependent and DNA-dependent DNA polymerase activities.

Therapeutic use

Treatment of human immunodeficiency virus type 1 (HIV-1) infection in combination with at least two additional antiretroviral agents.

Pregnancy and lactiation implications

Teratogenic in animals. There are no adequate, controlled studies to date using delavirdine in pregnant women, and the drug should be used during pregnancy only if potential benefits justify potential risks to the fetus or unless other alternatives are unavailable. Women should not breast-feed while they are receiving delavirdine.

Unlabeled use

Contraindications

Hypersensitivity to delavirdine or any component of the formulation. Concurrent use of alprazolam, cisapride, ergot alkaloids, midazolam, pimozide, rifampin, or triazolam.

Warnings and precautions

Redistribution or accumulation of body fat may occur. Patients who respond to antiretroviral therapy may develop an inflammatory response to indolent or residual opportunistic infections, during initial treatment. Rash may develop, mainly on the upper body and proximal arms. Severe and life-threatening skin reactions, including Stevens-Johnson syndrome and erythema multiforme, reported rarely. Hepatic and acute renal failure reported after treatment. Avoid use as monotherapy in HIV (should always be administered in conjunction with other antiretroviral agents and should not be used alone in the treatment of HIV infection). Caution in patients taking strong CYP3A4 inhibitors, moderate or strong CYP3A4 inducers and major CYP3A4 substrates.

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