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Tipranavir

    Brands

    DEA Class; Rx

    Common Brand Names; Aptivus

    • HIV, Protease Inhibitors

    Non-peptidic protease inhibitor (PI); must be “boosted” with ritonavir
    Used to treat HIV-1 infection in treatment-experienced patients with strains resistant to more than 1 PI
    Black Box Warnings regarding fatal and non-fatal hepatotoxicity and intracranial hemorrhage

    Indicated for the treatment of human immunodeficiency virus (HIV) infection in combination with other antiretroviral agents in patients with evidence of HIV replication despite ongoing antiretroviral therapy who are either treatment-experienced or have HIV-1 strains resistant to multiple protease inhibitors.

     

    Hypersensitivity

    Moderate-severe hepatic impairment (Child-Pugh Class B & C)

    Drugs that are contraindicated with tipranavir (when coadministered ‘boosted’ with ritonavir) include alpha1-adrenoreptor agonists (eg, alfuzosin), antiarrhythmics (amiodarone, bepridil, flecainide, propafenone, quinidine), rifampin, voriconazole, ergot derivatives (dihydroergotamine, ergonovine, ergotamine, methylergonovine), cisapride, St. John’s wort, lovastatin, simvastatin, lurasidone, pimozide, sildenafil (when used for PAH), midazolam, and triazolam

    • Diarrhea (15%)
    • Rash (3-21%)
    • Hypertriglyceridemia (61%)
    • Increased transaminases (26-32%)
    • 1-10%
    • Abdominal pain (4%)
    • Dyspnea (2%)
    • Epistaxis (4%)
    • Dehydration (2%)
    • Fatigue (6%)
    • Headache (5%)
    • Weight loss (3%)
    • Nausea (5-9%)
    • Pyrexia (6%)
    • Anemia (3%)
    • Vomiting (6%)
    • Myalgia (2%)

    Caution in mild hepatic impairment

    Risk of severe, potentially fatal hepatotoxicity

    Not recommended in treatment-naive patients

    May have antiplatelet/anticoagulant action

    Risk of potentially fatal intracranial hemorrhage

    Risk of immune reconstitution syndrome if used in combination with other antiretroviral drugs

    Fat redistribution with “cushingoid appearance” and “buffalo hump” may occur

    Autoimmune disorders (such as Graves’ disease, polymyositis, and Guillain-Barré syndrome) have also been reported to occur in the setting of immune reconstitution; however, the time to onset is more variable, and can occur many months after initiation of treatment

    Must be coadministered with ritonavir

    Sulfonamide allergy

    Coadministration with other CYP3A4 substrates (ritonavir inhibits CYP3A4 and increases toxicity risk for drugs metabolized by CYP3A4)

    Increased risk of rash, especially with hormonal contraceptives

    Use of drug may reduce efficacy of estrogen-based oral contraceptives; advise patients to use alternative methods of nonhormonal contraception

    Risk of large increase in total cholesterol and triglycerides

    Contains 116 IU/mL vitamin E (>RDA); limit supplemented vitamin E

    Prospective pregnancy data from the APR and an Expanded Access program are not sufficient to adequately assess risk of major birth defects, miscarriage, or adverse maternal or fetal outcomes

    there is no information regarding presence of tipranavir in human milk, effects on breastfed infant, or on milk production

    Adults

    1000 mg/day PO.

    Geriatric

    1000 mg/day PO.

    Adolescents

    28 mg/kg/day or 750 mg/m2/day, not to exceed 1000 mg/day PO.

    Children

     >= 2 years: 28 mg/kg/day or 750 mg/m2/day, not to exceed 1000 mg/day PO.
     < 2 years: Safety and efficacy have not been established.

    Infants

    Safety and efficacy have not been established.

    Neonates

    Safety and efficacy have not been established.

    Tipranavir

    capsule

    • 250mg

    oral solution

    • 100mg/mL