Ritonavir
- Atc Codes:J05AE03
- CAS Codes:155213-67-5
- PHARMGKB ID:155213-67-5
Table of contents
- Brand Names
- Drug Combinations
- Chemistry
- Pharmacologic Category
- Mechanism of Action
- Therapeutic Use
- Pregnancy and Lactation Implications
- Contraindications
- Warnings and Precautions
- Adverse Reactions
- 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: Norvir; Belgium: Norvir; Bulgaria: Norvir; Czech Republic: Norvir; Denmark: Norvir; Estonia: Norvir; Finland: Norvir; France: Norvir; Germany: Norvir; Greece: Norvir; Hungary: Norvir; Ireland: Norvir; Italy: Norvir; Latvia: Norvir; Lithuania: Norvir; Luxembourg: Norvir; Malta: Norvir; Netherlands: Norvir; Poland: Norvir; Portugal: Norvir; Romania: Norvir; Slovakia: Norvir; Slovenia: Norvir; Spain: Norvir; Sweden: Norvir; UK: Norvir.
North America
Canada: Norvir; USA: Norvir.
Latin America
Argentina: Busvir, Rifaxi, Ritonavir; Mexico: Norvir.
Asia
Japan: Norvir.
Drug combinations
Ritonavir and Lopinavir
Chemistry
Ritonavir: C~37~H~48~N~6~O~5~S~2~. Mw: 720.94. (1) 2,4,7,12-Tetraazatridecan-13-oic acid, 10-hydroxy-2-methyl-5-(1-methylethyl)-1-[2-(1-methylethyl)-4-thiazolyl]-3,6-dioxo-8,11-bis(phenylmethyl)-5-thiazolylmethyl ester [5S-(5R*,8R*,10R*,11R*)]-; (2) 5-Thiazolylmethyl [(αS)-α-[(1S,3S)-1-hydroxy-3-[(2S)-2-[3-[(2-isopropyl-4-thiazolyl)methyl]-3-methylureido]-3-methylbutyramido]-4-phenylbutyl]phenethyl]carbamate. CAS-155213-67-5 (1995).
Pharmacologic Category
Antiretrovirals; HIV Protease Inhibitors. (ATC-Code: J05AE03).
Mechanism of action
Binds to site of HIV-1 protease activity and inhibits cleavage of viral Gag-Pol polyprotein precursors into individual functional proteins required for infectious HIV. This results in formation of immature, noninfectious viral particles.
Therapeutic use
Treatment of HIV infection, as part of multidrug regimen (at least 3 antiretroviral agents). May be used as pharmacokinetic «booster» for other protease inhibitors.
Pregnancy and lactiation implications
No increased risk of overall birth defects observed following 1^st^ trimester exposure. If needed during pregnancy, use in combination with another PI to boost levels of 2^nd^ PI. Contraindicated in nursing women.
Unlabeled use
Contraindications
Hypersensitivity to ritonavir or any component of the formulation. Concurrent alfuzosin, amiodarone, cisapride, dihydroergotamine, ergonovine, ergotamine, flecainide, methylergonovine, midazolam, pimozide, propafenone, quinidine, triazolam, voriconazole (when ritonavir ≥800 mg/day).
Warnings and precautions
Protease inhibitors associated with a variety of hypersensitivity events (some severe), including rash, anaphylaxis (rare), angioedema, bronchospasm, erythema multiforme, and/or Stevens-Johnson syndrome (rare). Generally recommended to discontinue treatment if severe rash or moderate symptoms accompanied by other systemic symptoms occur. May cause fat redistribution. Patients may develop immune reconstitution syndrome resulting in occurrence of inflammatory response to indolent or residual opportunistic infection. Increases in total cholesterol and triglycerides reported. Ritonavir associated with AV block due to prolongation of PR interval (use caution with drugs which prolong the PR interval). Use with caution in cardiomyopathy, ischemic heart disease, pre-existing conduction abnormalities, or structural heart disease (may be at increased risk of conduction abnormalities (e.g. second- or third-degree AV block)). Changes in glucose tolerance, hyperglycemia, exacerbation of diabetes, DKA, and new-onset diabetes mellitus reported in patients receiving protease inhibitors. Use with caution in hemophilia A or B (increased bleeding events, including spontaneous skin hematoma and hemarthrosis, reported during protease inhibitor therapy). May cause hepatitis, jaundice, and/or exacerbation of pre-existing hepatic dysfunction (use with caution in underlying hepatic disease, such as hepatitis B or C or cirrhosis). Use with caution in increased triglycerides (pancreatitis observed). Ritonavir may interact with many medications, resulting in potentially serious and/or life-threatening adverse events. Use with caution in patients taking strong CYP3A4 inhibitors, moderate or strong CYP3A4 inducers and major CYP3A4 substrates. Not recommended for use with alfuzosin, amiodarone, cisapride, ergot derivatives, flecainide, lovastatin, midazolam, pimozide, propafenone quinidine, simvastatin, St. John’s wort, triazolam, or voriconazole.