Fosamprenavir
- Atc Codes:J05AE07
- CAS Codes:226700-81-8
- PHARMGKB ID:226700-81-8
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
- Induces
- Drug Interactions
- Nutrition/Nutraceutical Interactions
- Dosage
- Pharmacokinetics and Pharmacodynamics
- Special Considerations
Brand Names
Europe
Austria: Telzir; Belgium: Telzir; Bulgaria: Telzir; Czech Republic: Telzir; Denmark: Telzir; Estonia: Telzir; Finland: Telzir; France: Telzir; Germany: Telzir; Greece: Telzir; Hungary: Telzir; Italy: Telzir; Latvia: Telzir; Lithuania: Telzir; Malta: Telzir; Netherlands: Telzir; Poland: Telzir; Portugal: Telzir; Romania: Telzir; Slovakia: Telzir; Slovenia: Telzir; Spain: Telzir; Sweden: Telzir; UK: Telzir.
North America
Canada: Telzir; USA: Lexiva.
Latin America
Argentina: Telzir; Mexico: Telzer.
Asia
Japan: Lexiva.
Drug combinations
Chemistry
Fosamprenavir Calcium: C~25~H~36~CaN~3~O~9~PS. Mw: 625.68. (1) Carbamic acid, [(1S,2R)-3-[[(4-aminophenyl)sulfonyl](2-methylpropyl)amino]-1-(phenylmethyl)-2-(phosphonooxy)propyl]-, C-[(3S)-tetrahydro-3-furanyl] ester, calcium salt (1:1); (2)(3S)-Tetrahydro-3-furyl [(αS)-α-[(1R)-1-hydroxy-2-(N^1^-isobutylsulfanilamido)ethyl]phenethyl]carbamate, calcium phosphate (ester)(1:1). CAS-226700-81-8 (2000).
Pharmacologic Category
Antiretrovirals; HIV Protease Inhibitors. (ATC-Code: J05AE07).
Mechanism of action
Fosamprenavir calcium is a prodrug of amprenavir and has little or no antiviral activity until hydrolyzed to amprenavir in vivo by cellular phosphatases. Amprenavir is an inhibitor of human immunodeficiency virus (HIV) protease. By interfering with formation of essential proteins and enzymes, amprenavir blocks maturation of the virus and causes formation of nonfunctional, immature, noninfectious virions.
Therapeutic use
Treatment of HIV infections in combination with at least two other antiretroviral agents.
Pregnancy and lactiation implications
Caution if administered during pregnancy. HIV-infected women should not breast-feed due to risk of HIV transmission and risk of adverse effects in the infant.
Unlabeled use
Contraindications
Hypersensitivity to fosamprenavir, amprenavir, or any component of the formulation. Concurrent therapy with CYP3A4 substrates with narrow therapeutic window. Concomitant use with cisapride, delavirdine, ergot derivatives, lovastatin, midazolam, pimozide, rifampin, simvastatin, St. John’s wort, or triazolam. Use of flecainide and propafenone with concomitant ritonavir therapy.
Warnings and precautions
Protease inhibitors have been associated with a variety of hypersensitivity events (some severe), including rash, anaphylaxis (rare), angioedema, bronchospasm, erythema multiforme, and/or Stevens-Johnson syndrome (rare). Patients may develop immune reconstitution syndrome. Increases in total cholesterol and triglycerides reported. Use with caution in sulfonamide allergy. Hyperglycemia, exacerbation of diabetes, DKA, and new-onset diabetes mellitus reported in patients receiving protease inhibitors. Use with caution in hemophilia A or B, and in underlying hepatic disease, such as hepatitis B or C or cirrhosis. Potential for CYP-mediated interactions. Avoid use with hormonal contraceptives (e.g. ethinyl estradiol/norethindrone). Estrogen/progestin levels may be reduced with concomitant use. May cause fat redistribution. Acute hemolytic anemia reported.