Names and pronunciation
(ti-pran′a-veer) Aptivus
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Drug reference
(ti-pran′a-veer) Aptivus
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Func. class.: Antiretroviral
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Chem. class.: Protease inhibitor
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ACTION: Inhibits human immuno- deficiency virus (HIV) protease, thereby preventing the maturation of the virus
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USES: HIV in combination with other antiretrovirals
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CONTRAINDICATIONS: Hyper- sensitivity Precautions: Pregnancy, breastfeeding, children, renal disease, history of renal stones, sulfa allergy, hemophilia, diabetes mellitus, pancreatitis, alcoholism, immune reconstitution syndrome, surgery, trauma, infection
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Black Box Warning: Intracranial bleed- ing, hepatitis, hepatic disease (Child- Pugh B, C) Black Box Warning: Hepatitis, pancre- atitis: ALT, AST; total bilirubin, amylase; all may be elevated, discontinue in those with hepatic insufficiency or hepatitis or AST/ALT 10 × upper limit or AST/ALT 5-10 × ULN and total bilirubin 2.5 × ULN; assess for anorexia, nausea, jaundice, hepatomegaly, clay-colored stools • HIV: Viral load, CD4, plasma HIV RNA, serum cholesterol profile, serum triglyc- erides during treatment • Bowel pattern before, during treat- ment; if severe abdominal pain with bleeding occurs, product should be dis- continued; monitor hydration • Serious rash: if serious rash occurs, product should be discontinued • Immune reconstitution syndrome: has been reported with combination anti retroviral therapy, patients may develop pain (MAC, CMV, PcP, TB) and autoimmune disease months after treatment Black Box Warning: Intracranial bleed- ing: more common in those with trauma, surgery, or those taking antiplatelets or anticoagulants; assess for headache, nausea, vomiting, seizures, confusion, in- ability to speak, can be fatal • Cushingoid symptoms: buffalo hump, facial/peripheral wasting, breast enlarge- ment, central obesity • Pregnancy/breastfeeding: use only if benefits outweigh fetal risk; enroll preg nant women in the Antiretroviral Preg nancy Registry, 1-800-258-4263; do not breastfeed
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SIDE EFFECTS CNS: Headache, insomnia, dizziness, somnolence, fatigue, fever, intracranial bleeding GI: Diarrhea, abdominal pain, nausea, vomiting, anorexia, dry mouth, hepatitis B or C, pancreatitis, fatalities when given with ritonavir GU: Nephrolithiasis INTEG: Rash, urticaria, lipodystrophy, serious rash MS: Pain OTHER: Asthenia, insulin-resistant hyper glycemia, hyperlipidemia, ketoacidosis
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INTERACTIONS Life-threatening dysrhythmias: amioda rone, astemizole, cisapride, ergots, fle cainide, midazolam, pimozide, propafe none, quiNIDine, rifabutin, rifAMPin, terfenadine, triazolam Increase: myopathy, rhabdomyolysis— HMG-CoA reductase inhibitors (lovastatin, simvastatin) Increase: tipranavir levels—ketocon- azole, delavirdine, itraconazole Increase: levels of both products—cla rithromycin, zidovudine Increase: levels of tipranavir—oral contraception Decrease: tipranavir levels—rifamycins, fluconazole, nevirapine, efavirenz Drug/Herb Decrease: tipranavir levels—St. John’s wort; avoid concurrent use Drug/Food Decrease: tipranavir absorption—grape- fruit juice; high-fat, high-protein foods Drug/Lab Test Increase: AST/ALT, cholesterol, blood glucose, amylase, lipase, triglycerides
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DOSAGE AND ROUTES • Adult: PO 500 mg coadministered with ritonavir 200 mg bid with food • Adolescent and child ≥2 yr: PO 14 mg/kg given with ritonavir 6 mg/kg bid or 375 mg/m2 given with ritonavir 150 mg/m2 bid, max 500 mg with ritonavir 200 mg bid
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Available forms: Caps 250 mg; oral solution 100 mg/mL
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Administer: • Not to be used in those who are treatment-naive • Swallow cap whole; do not break, crush, chew; store caps in refrigerator before use; after opening, store at room temperature; use within 60 days • After meals • In equal intervals around the clock to maintain blood levels
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Assess: • Signs of infection, anemia; presence of other sexually transmitted diseases
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Evaluate: • Therapeutic response: improving CD4 counts, viral load
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CLINICAL CONSIDERATIONS
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Patient and caregiver information: • To take as prescribed; if dose is missed, to take as soon as remembered up to 1 hr before next dose; not to dou- ble dose; that this product must be taken with other antivirals • That product must be taken in equal intervals around the clock to maintain blood levels for duration of therapy • That hyperglycemia may occur; to watch for increased thirst, weight loss, hunger, dry, itchy skin; to notify prescriber • That product does not cure AIDS, only controls symptoms; not to donate blood • That redistribution of body fat may occur • Not to use with other products unless approved by prescriber, many drug inter- actions • That product must be taken in combi- nation with ritonavir • To stop product and notify prescriber if anorexia, nausea, vomiting, yellowing of skin or eyes, clay-colored stools, fatigue, pain in upper abdomen HIGH ALERT
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PHARMACOKINETICS Terminal half-life 6 hr, peak 3 hr, plasma protein binding 99.9%, steady state 7-10 days, metabolism CYP3A4, 80% fecal excretion
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• Adolescent and child ≥2 yr: PO 14 mg/kg given with ritonavir 6 mg/kg bid or 375 mg/m2 given with ritonavir 150 mg/m2 bid, max 500 mg with ritonavir 200 mg bid
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