Table of contents

  • Brand Names
  • Chemistry
  • Pharmacologic Category
  • Mechanism of Action
  • Therapeutic Use
  • Pregnancy and Lactation Implications
  • Contraindications
  • Warnings and Precautions
  • Adverse Reactions
  • Substrate of
  • Inhibits
  • Induces
  • Drug Interactions
  • Nutrition/Nutraceutical Interactions
  • Dosage
  • Pharmacokinetics and Pharmacodynamics
  • Special Considerations

Brand Names


Austria: Aptivus; Belgium: Aptivus; Bulgaria: Aptivus; Cyprus: Aptivus; Czech Republic: Aptivus; Denmark: Aptivus; Estonia: Aptivus; Finland: Aptivus; France: Aptivus; Germany: Aptivus; Greece: Aptivus; Hungary: Aptivus; Ireland: Aptivus; Italy: Aptivus; Latvia: Aptivus; Lithuania: Aptivus; Luxembourg: Aptivus; Malta: Aptivus; Netherlands: Aptivus; Poland: Aptivus; Portugal: Aptivus; Romania: Aptivus; Slovakia: Aptivus; Spain: Aptivus; Sweden: Aptivus; UK: Aptivus.

North America

Canada: Aptivus; USA: Aptivus.

Latin America

Argentina: Aptivus; Mexico: Aptivus.

Drug combinations


Tipranavir Disodium: C~31~H~31~F~3~N~2~Na~2~O~5~S. Mw: 646.63. (1) [R-(R*,R*)]-N-[3-[1-[5,6-Dihydro-4-hydroxy-2-oxo-6-(2-phenylethyl)-6-propyl-2H-pyran-3-yl]propyl]phenyl]-5-(trifluoromethyl)-2-pyridinesulfonamide disodium salt; (2) 3′-[(1R)-1-[(6R)-5,6-Dihydro-4-hydroxy-2-oxo-6-phenethyl-6-propyl-2H-pyran-3-yl]propyl]-5-(trifluoromethyl)-2-pyridinesulfonanilide, disodium salt. CAS-191150-83-1 (1998).

Pharmacologic Category

Antiretrovirals; HIV Protease Inhibitors. (ATC-Code: J05AE09).

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-1 infections in combination with ritonavir and other antiretroviral agents. Limited to highly treatment-experienced or multiprotease inhibitor-resistant patients.

Pregnancy and lactiation implications

Unnown if tipranavir crosses human placenta. Pregnancy and protease inhibitors both associated with increased risk of hyperglycemia. Women receiving estrogens have increased incidence of rash. Excretion in breast milk unknown (contraindicated in nursing women).

Unlabeled use


Concurrent therapy of tipranavir/ritonavir with amiodarone, cisapride, ergot derivatives, flecainide, lovastatin, midazolam, pimozide, propafenone, quinidine, rifampin, simvastatin, St. John’s wort, and triazolam. Moderate-to-severe hepatic impairment.

Warnings and precautions

May cause fat redistribution. In combination with ritonavir, may cause hepatitis and/or exacerbate pre-existing hepatic dysfunction (patients with chronic hepatitis B or C at increased risk). Protease inhibitors associated with a variety of hypersensitivity events, including rash, anaphylaxis, angioedema, bronchospasm, erythema multiforme, and/or Stevens-Johnson syndrome. 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. Use in combination with ritonavir associated with rare reports of fatal and nonfatal intracranial hemorrhage (causal relationship not established). Use with caution in sulfonamide allergy. 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 during protease inhibitor therapy reported), and in mild hepatic impairment (contraindicated in moderate-to-severe impairment). May impair platelet aggregation, resulting in bleeding (use with caution in patients who may be at risk for increased bleeding (trauma, surgery or other medical conditions)). Anticoagulant and antiplatelet agent co-administration may increase risk of bleeding. Use with caution in patients taking strong CYP3A4 inhibitors and moderate CYP3A4 inducers. Concomitant use with selected major CYP3A4 substrates and strong CYP3A4 inducers contraindicated. Women receiving estrogens have increased incidence of rash. Co-administration with ritonavir required. Oral solution formulation contains vitamin E.



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