Darunavir
- Atc Codes:J05AE10
- CAS Codes:206361-99-1
- PHARMGKB ID:206361-99-1
Table of contents
- Brand Names
- Chemistry
- Pharmacologic Category
- Therapeutic Use
- Pregnancy and Lactation Implications
- Contraindications
- Warnings and Precautions
- Adverse Reactions
- Caution and personalized dose adjustment in patients with the following genotypes
- Other genes that may be involved
- Substrate of
- Inhibits
- Induces
- Drug Interactions
- Nutrition/Nutraceutical Interactions
- Dosage
- Pharmacokinetics and Pharmacodynamics
- Special Considerations
Brand Names
Europe
Austria: Prezista; Belgium: Prezista; Bulgaria: Prezista; Czech Republic: Prezista; Denmark: Prezista; Estonia: Prezista; Finland: Prezista; France: Prezista; Germany: Prezista; Greece: Prezista; Hungary: Prezista; Ireland: Impaqtiv, Prezista; Italy: Prezista; Latvia: Prezista; Lithuania: Prezista; Luxembourg: Prezista; Malta: Prezista; Netherlands: Prezista; Poland: Prezista; Portugal: Prezista; Romania: Prezista; Slovakia: Prezista; Slovenia: Prezista; Spain: Prezista; Sweden: Prezista; UK: Prezista.
North America
Canada: Prezista; USA: Prezista.
Latin America
Argentina: Prezista.
Asia
Japan: Prezista.
Drug combinations
Chemistry
Darunavir: C~27~H~37~N~3~O~7~S. Mw: 547.66. (1) [(1S,2R)-3-[[(4-Aminophenyl)sulfonyl](2-methylpropyl)amino]-2-hydroxy-1-(phenylmethyl)propyl]-carbamic acid (3R,3aS,6aR)-hexahydrofuro[2,3-b]furan-3-yl ester; (2) Carbamic acid, [(1S,2R)-3-[[(4-aminophenyl)sulfonyl](2-methylpropyl)amino]-2-hydroxy-1-(phenylmethyl)propyl]-, (3R,3aS,6aR)-hexahydrofuro[2,3-b]furan-3-yl ester. CAS-206361-99-1 (2005).
Pharmacologic Category
Antiretrovirals; HIV Protease Inhibitors. (ATC-Code: J05AE10).
Mechanism of action
Binds to the HIV-1 protease activity site and inhibits activity of enzyme. Inhibition prevents cleavage of viral polyproteins, resulting in formation of immature, noninfectious viral particles.
Mechanism of action
Therapeutic use
Treatment of HIV-1 infections in combination with ritonavir and other antiretroviral agents in previously treated or multiprotease inhibitor-resistant patients.
Pregnancy and lactiation implications
No teratogenicity demonstrated in animal studies. Not known whether the drug is distributed into human milk. HIV-infected mothers are discouraged from breast-feeding.
Unlabeled use
Contraindications
Hypersensitivity to darunavir or any component of the formulation. Concurrent therapy with cisapride, dihydroergotamine, ergonovine, ergotamine, methylergonovine, midazolam, pimozide, triazolam or any other major CYP3A4 substrates.
Warnings and precautions
May cause fat redistribution. May cause hepatitis or liver injury (risk factors include multiple medications, HIV disease, hepatitis B/C coinfection, and/or immune reconstitution syndrome). Hypersensitivity reactions may occur (rash, anaphylaxis (rare), angioedema, bronchospasm, erythema multiforme, and/or Stevens-Johnson syndrome). Immune reconstitution syndrome may be developed in patients who respond to antiretroviral therapy. Increases in total cholesterol and triglycerides reported. Caution in sulfonamide allergy (contains a sulfonamide moiety), hemophilia A or B (increased bleeding), or hepatic dysfunction (may be exacerbated). May cause diabetogenic effects (i.e. changes in glucose tolerance, hyperglycemia, exacerbation of diabetes, diabetic ketoacidosis, and new-onset diabetes mellitus). Beware of possible CYP-mediated interactions. Should be co-administered with ritonavir.