近日，德国勃林格殷格翰制药公司的研制的aptivus(替拉那韦)胶囊通过了美国FDA的加速批准。加速批准即加快某类药品的审批过程，获加速批准的药品必须用于治疗严重疾病或危及生命的不治之症，且相对现有药品能够使患者显著受益。aptivus是一种非肽类蛋白酶抑制剂，通过抑制蛋白酶(一种在HIV复制过程中必需的酶)发挥作用。aptivus能进入被感染的免疫细胞，并抑制多种其他蛋白酶抑制剂(PI)药物耐受的HIV病毒的复制。哈佛医学院医学副教授，aptivus的批准剂量为500毫克，与利托那韦(aptivus/r)200毫克合用，每日服用两次。aptivus必须与利托那韦共同使用，以使aptivus达到治疗水平。否则，aptivus的水平将不足以抑制HIV的复制。
同时，aptivus/r必须与其他抗HIV药品同时服用。
aptivus250毫克软胶囊将在获得FDA批准的两周内在美国上市。
Generic Name for APTIVUS
Tipranavir 250mg; soft gel caps; contains alcohol.
Legal Classification:
Rx
Pharmacological Class for APTIVUS
HIV-1 protease inhibitor.
Manufacturer of APTIVUS
Boehringer Ingelheim Pharmaceuticals
Indications for APTIVUS
HIV-1 infection in treatment-experienced patients or in those with HIV strains resistant to multiple protease inhibitors (PIs) in combination with ritonavir.
Adult dose for APTIVUS
Swallow caps whole. Tipranavir 500mg + ritonavir 200mg twice daily.
Children's dosing for APTIVUS
<2 years: not recommended. Use soln if unable to swallow caps. Calculate dose based on body wt. (kg) or BSA (m2). 2–18 years: 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.
Also:
APTIVUS ORAL SOLUTION
Contraindications for APTIVUS
Moderate to severe hepatic insufficiency (Child-Pugh B–C). Concomitant potent CYP3A inducers or substrates (eg, alfuzosin, amiodarone, bepridil, flecainide, propafenone, quinidine, rifampin, ergots, cisapride, St. John's wort, lovastatin, simvastatin, pimozide, sildenafil, oral midazolam, triazolam).
Warnings/Precautions for APTIVUS
Not for use in treatment-naive patients. Sulfa allergy. Mild hepatic impairment (Child-Pugh A). Hepatitis. Monitor lipids, liver function (baseline and periodically); discontinue if asymptomatic increase in AST/ALT >10xULN, or AST/ALT 5–10xULN and total bilirubin >2.5xULN. Diabetes. Risk of increased bleeding. Hemophilia: monitor for spontaneous bleeding. Pregnancy (Cat.C). Nursing mothers: not recommended.
Interactions for APTIVUS
See Contraindications. Concomitant salmeterol, fluticasone, amprenavir, lopinavir, saquinavir, or fluconazole, ketoconazole, itraconazole ≥200mg/day: not recommended. Caps: avoid metronidazole, disulfiram. May be synergistic with enfuvirtide. Potentiates PDE5 inhibitors (eg, sildenafil, tadalafil, vardenafil), trazodone, desipramine; reduce dose: see literature. Avoid concomitant colchicine if renal or hepatic impairment; otherwise: reduce dose: see literature. Reduce rifabutin dose by 75%. Antagonizes estrogens (use non-hormonal contraceptives), methadone, valproic acid, omeprazole. Antagonized by carbamazepine, phenobarbital, phenytoin. Potentiates atorvastatin, rosuvastatin: use lowest possible dose. Monitor hypoglycemics, immunosuppressants, tricyclics, SSRIs, warfarin, drugs that affect or are affected by CYP3A4 (eg, azole antifungals, calcium channel blockers, clarithromycin, NNRTIs, PIs, statins). Increased risk of bleeding with concomitant anticoagulants, antiplatelet agents, high-dose Vit.E. Separate dosing of didanosine, antacids. Oral soln: avoid high-dose Vit.E supplements.
Adverse Reactions for APTIVUS
GI upset, abdominal pain, pyrexia, fatigue, headache, rash (discontinue if severe), fat redistribution, severe liver disease, hepatitis (discontinue if symptomatic), hypertriglyceridemia, hyperlipidemia, hyperglycemia, immune reconstitution syndrome, intracranial hemorrhage (may be fatal), others; children: also cough.
Notes for APTIVUS
Register pregnant patients exposed to tipranavir by calling (800) 258-4263.
How is APTIVUS supplied?
Caps—120; Soln—95mL (w. dispensing syringe)