Classes
DEA Class; Rx
Common Brand Names; Aptivus
- HIV, Protease Inhibitors
Description
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
Indications
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.
Contraindications
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
Adverse Effects
- 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%)
Warnings
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
Pregnancy and Lactation
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
Maximum Dosage
1000 mg/day PO.
1000 mg/day PO.
28 mg/kg/day or 750 mg/m2/day, not to exceed 1000 mg/day PO.
>= 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.
Safety and efficacy have not been established.
Safety and efficacy have not been established.
How supplied
Tipranavir
capsule
- 250mg
oral solution
- 100mg/mL
