Indications for APTIVUS ORAL SOLUTION:
In combination with ritonavir to treat HIV-1 infection in patients who are treatment-experienced and infected with HIV-1 strains resistant to more than one protease inhibitor. Not for use in treatment-naive patients.
Swallow caps whole. Tipranavir 500mg + ritonavir 200mg twice daily.
<2yrs: not established. Use soln if unable to swallow caps. Calculate dose based on body wt. (kg) or BSA (m2). 2–18yrs: Tipranavir 14mg/kg + ritonavir 6mg/kg (or 375mg/m2 + ritonavir 150mg/m2) twice daily; max tipranavir 500mg + ritonavir 200mg twice daily. May consider reducing dose to tipranavir 12mg/kg + ritonavir 5mg/kg (or 290mg/m2 + ritonavir 115mg/m2) twice daily if intolerance or toxicity occurs provided their virus is not resistant to multiple PIs.
Moderate or severe hepatic impairment (Child-Pugh B or C). Concomitant potent CYP3A inducers or substrates (eg, alfuzosin, amiodarone, bepridil, flecainide, propafenone, quinidine, rifampin, ergots, cisapride, St. John's wort, lovastatin, simvastatin, pimozide, lurasidone, sildenafil [Revatio; for PAH], oral midazolam, triazolam). Concomitant colchicine (in renal or hepatic impairment).
Hepatotoxicity. Intracranial hemorrhage.
Increased risk of hepatotoxicity esp. in patients with chronic hepatitis B or C co-infection. Monitor liver function, lipids at baseline and periodically; discontinue if symptomatic hepatitis, asymptomatic increase in AST/ALT >10×ULN, or AST/ALT 5–10×ULN and total bilirubin >2.5×ULN. Mild hepatic impairment (Child-Pugh A). Risk of intracranial hemorrhage (may be fatal). Increased bleeding risk. Hemophilia: monitor for spontaneous bleeding. Sulfa allergy. Diabetes. Elderly. Advise females and males of reproductive potential to use nonhormonal contraception. Pregnancy. Nursing mothers: not recommended.
HIV-1 protease inhibitor.
See Contraindications. Concomitant etravirine, fosamprenavir, lopinavir, saquinavir, atazanavir, salmeterol, fluticasone, atorvastatin, or fluconazole, ketoconazole, itraconazole >200mg/day: not recommended. May be potentiated by enfuvirtide. Antagonized by carbamazepine, phenobarbital, phenytoin, buprenorphine/naloxone. Potentiates sildenafil, tadalafil, vardenafil, IV midazolam, trazodone, colchicine, desipramine (monitor), SSRIs, clarithromycin (in renal impairment); reduce dose: see full labeling. Antagonizes abacavir, didanosine, zidovudine, estrogens (as HRT; monitor for deficiency), methadone, meperidine, omeprazole, dolutegravir, raltegravir, valproic acid. Reduce rifabutin dose by 75%, quetiapine to ⅙ of current dose (if no alternative). Monitor hypoglycemics, immunosuppressants, CCBs, warfarin. Increased risk of bleeding with concomitant anticoagulants, antiplatelet agents, high-dose Vit.E. Separate dosing of didanosine by ≥2hrs. Bosentan: adjust dose (see full labeling). Caps: avoid metronidazole, disulfiram. Oral soln: avoid high-dose Vit.E supplements.
Diarrhea, nausea, pyrexia, vomiting, fatigue, abdominal pain, headache, rash (discontinue if severe); fat redistribution, hepatitis, hepatic decompensation, hypertriglyceridemia, hyperlipidemia, hyperglycemia, immune reconstitution syndrome, intracranial hemorrhage; children: also cough.
Register pregnant patients exposed to tipranavir by calling (800) 258-4263.
Caps—120; Soln—95mL (w. dispensing syringe)