Amprenavir
- Atc Codes:J05AE05
- CAS Codes:161814-49-9
- PHARMGKB ID:161814-49-9
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
- Other genes that may be involved
- Substrate of
- Inhibits
- Drug Interactions
- Nutrition/Nutraceutical Interactions
- Dosage
- Pharmacokinetics and Pharmacodynamics
- Special Considerations
Brand Names
Europe
Austria: Agenerase; Bulgaria: Agenerase; Cyprus: Agenerase; Czech Republic: Agenerase; Estonia: Agenerase; Finland: Agenerase; Germany: Agenerase; Greece: Agenerase; Hungary: Agenerase; Ireland: Agenerase; Latvia: Agenerase; Luxembourg: Agenerase; Malta: Agenerase; Netherlands: Agenerase; Poland: Agenerase; Portugal: Agenerase; Romania: Agenerase; Slovakia: Agenerase; Sweden: Agenerase; UK: Agenerase.
North America
USA: Agenerase (d).
Latin America
Argentina: Agenerase (d); Brazil: Agenerase.
Drug combinations
Chemistry
Amprenavir: C~25~H~35~N~3~O~6~S. Mw: 505.63. (1) [3S-[3R*(1R*,2S*)]]-[3-[[(4-Aminophenyl)sulfonyl](2-methylpropyl)amino]-2-hydroxy-1-(phenylmethyl)propyl] tetrahydro-3-furanyl carbamate; (2)(3S)-Tetrahydro-3-furyl [(αS)-α-[(1R-1-hydroxy-2-(N^1^-isobutylsulfanilamido)ethyl]phenethyl]carbamate. CAS-161814-49-9 (1997).
Pharmacologic Category
Antiretrovirals; HIV Protease Inhibitors. (ATC-Code: J05AE05).
Mechanism of action
Binds to the protease activity site and inhibits the activity of the enzyme.
Therapeutic use
Treatment of HIV infections.
Pregnancy and lactiation implications
Use of oral solution is contraindicated during pregnancy. Risk of hyperglycemia. Contraindicated during lactation.
Unlabeled use
Contraindications
Hypersensitivity to amprenavir or any component of the formulation. Concurrent therapy with cisapride, ergot derivatives, midazolam, pimozide, and triazolam. Severe previous allergic reaction to sulfonamides. Oral solution is contraindicated in infants or children <4 years of age, pregnant women, patients with renal or hepatic failure, and patients receiving concurrent metronidazole or disulfiram.
Warnings and precautions
May cause fat redistribution. Hypersensitivity reactions may occur (including rash, anaphylaxis (rare), angioedema, bronchospasm, erythema multiforme, and/or Stevens-Johnson syndrome (rare)). Immune reconstitution syndrome may develop. Use with caution in sulfonamide allergy. Changes in glucose tolerance, hyperglycemia, exacerbation of diabetes, diabetic ketoacidosis, and new-onset diabetes mellitus reported. Use with caution in hemophilia A or B (risk of increased bleeding). Use with caution in hepatic impairment (may cause hepatitis and/or exacerbate pre-existing hepatic dysfunction). High potential for CYP-mediated interactions exists (CYP3A4 inhibitors, moderate or strong CYP3A4 inducers and major CYP3A4 substrates). Use of oral solution should be avoided (increased risk of propylene glycol-associated adverse effects, especially in certain ethnic populations (Asians, Eskimos, Native Americans)).