2011年12月19日，美国食品药品管理局FDA已批准Prezista(达如那韦)的口服混悬液制剂。Prezista现有100mg/ml的口服混悬液出售，作为处方药，该药用于治疗感染人类免疫缺陷病毒(HIV)的患者。
另外，Prezista的药品说明书也进行了更新，提供了针对儿科患者及难以吞咽Prezista片剂的成人患者的口服混悬液用药说明。
对于初治的成人及曾接受过治疗且未使用与达如那韦耐药有关的替代药物的成人，可采用Prezista 8 ml、每日用药1次联合利托那韦1.25ml、每日用药1次(与餐同服)进行治疗。8ml剂量应借助配备的口服注射器平分为2次服用。对于曾接受过治疗且至少使用过1种与达如那韦耐药有关的替代药物的成人，以6ml剂量的口服混悬液、每日用药2次联合利托那韦1.25ml、每日用药2次(与餐同服)进行治疗。
PREZISTA（达芦那韦）口服混悬液，口服使用
PREZISTA（达芦那韦）片剂，薄膜包衣口服使用
美国首次批准 - 2006年
适应症和用法
PREZISTA是人类免疫缺陷病毒（HIV-1）蛋白酶抑制剂表明对HIV-1感染成年患者的治疗。 PREZISTA也表示对HIV-1感染的患儿3岁及以上的治疗。 PREZISTA必须共同施用利托那韦（PREZISTA /利托那韦），并与其它抗逆转录病毒药物。
用法用量
治疗过的成年患者和治疗经验的成人患者无关联的达芦那韦耐换人：800毫克（一次800毫克片剂）与利托那韦100毫克，每天一次，并与食物一起服用。
治疗经验成年患者中的至少一个地瑞那韦抗性相关替代：600毫克（1600毫克片剂）与利托那韦100mg的每日食物服用两次。
小儿患者（3至小于18岁，体重至少10千克）：PREZISTA的剂量和利托那韦是基于体重和不应超过成人剂量。 PREZISTA应采取与利托那韦与食物。
PREZISTA /利托那韦不推荐用于治疗重度肝功能损害的使用。
包装规格
口服混悬液：100mg/mL*1瓶

薄膜包衣片：75mg*480片、 150mg*240片 600mg*60片 800mg*30片
PREZISTA ORAL SUSPENSION Rx
Generic Name and Formulations:
Darunavir (as ethanolate) 100mg/mL; strawberry-cream flavor.
Company:
Janssen Therapeutics
Indications for PREZISTA ORAL SUSPENSION:
Treatment of HIV infection in combination with ritonavir and with other antiretroviral agents.
Adult:
Take with food. Use oral susp if unable to swallow tabs. ≥18yrs: Treatment-naive and treatment-experienced with no darunavir resistance associated substitutions: 800mg once daily with ritonavir 100mg once daily. Treatment-experienced with at least one darunavir resistance associated substitution: 600mg twice daily with ritonavir 100mg twice daily. Severe hepatic impairment: not recommended.
Children:
<3yrs: not recommended. Take with food. Use oral susp if unable to swallow tabs. Treatment-naive and treatment-experienced with no darunavir resistance associated substitutions: ≥3yrs to <18yrs: ≥10kg–<11kg: 350mg once daily with ritonavir 64mg once daily; ≥11kg–<12kg: 385mg once daily with ritonavir 64mg once daily; ≥12kg–<13kg: 420mg once daily with ritonavir 80mg once daily; ≥13kg–<14kg: 455mg once daily with ritonavir 80mg once daily; ≥14kg–<15kg: 490mg once daily with ritonavir 96mg once daily ≥15–<30kg: 600mg (6mL of susp) once daily with ritonavir 100mg once daily; ≥30kg–<40kg: 675mg (6.8mL of susp) once daily with ritonavir 100mg once daily; ≥40kg: 800mg once daily with ritonavir 100mg once daily. Treatment-experienced with at least one darunavir resistance associated substitution: ≥3yrs to <18yrs: ≥10kg–<11kg: 200mg twice daily with ritonavir 32mg twice daily; ≥11kg–<12kg: 220mg twice daily with ritonavir 32mg twice daily; ≥12kg–<13kg: 240mg twice daily with ritonavir 40mg twice daily; ≥13kg–<14kg: 260mg twice daily with ritonavir 40mg twice daily; ≥14kg–<15kg: 280mg twice daily with ritonavir 48mg twice daily ≥15–<30kg: 375mg (3.8mL of susp) twice daily with ritonavir 48 mg twice daily; ≥30kg–<40kg: 450mg (4.6mL of susp) twice daily with ritonavir 60mg twice daily; ≥40kg: 600mg twice daily with ritonavir 100mg twice daily. Severe hepatic impairment: not recommended.
See Also:
PREZISTA
Pharmacological Class:
Protease inhibitor.
Contraindications:
Concomitant rifampin, alfuzosin, ergots, cisapride, St. John's wort, lovastatin, simvastatin, pimozide, oral midazolam, triazolam, sildenafil (Revatio; only when used to treat PAH).
Warnings/Precautions:
Sulfonamide allergy. Hepatic impairment (eg, chronic hepatitis, cirrhosis, pre-treatment elevated transaminases): monitor liver enzymes; interrupt or discontinue therapy if liver dysfunction occurs or worsens. Severe renal impairment. Diabetes (may need insulin or oral hypoglycemics dose adjusted). Hemophilia: monitor for spontaneous bleeding. Elderly. Pregnancy (Cat.C). Nursing mothers: not recommended.
Interactions:
See Contraindications. Voriconazole, salmeterol, boceprevir, telaprevir: not recommended. Avoid protease inhibitors other than those studied (lopinavir/ritonavir, saquinavir, indinavir, atazanavir), dexamethasone, fluticasone. Potentiates carbamazepine, risperidone, thioridazine, trazodone, desipramine, IV midazolam, rifabutin, digoxin, HMG-CoA reductase inhibitors (eg, pravastatin, atorvastatin, rosuvastatin; use lowest dose necessary; max atorvastatin dose is 20mg/day), sildenafil, vardenafil, tadalafil (reduce their doses). Potentiates, and is potentiated by, indinavir, ketoconazole, itraconazole. Increases bosentan (see full labeling), maraviroc, nevirapine, tenofovir, efavirenz, colchicine (dose adjustments: see full labeling) levels. Antagonizes sertraline, paroxetine, phenytoin, phenobarbital (monitor levels), ethinyl estradiol, norethindrone (use backup contraception). Caution with antimalarials (artemether, lumefantrine). Monitor carbamazepine, antiarrhythmics (eg, bepridil, systemic lidocaine, quinidine, amiodarone, flecainide, propafenone), calcium channel blockers, β-blockers, warfarin, digoxin, immunosuppressants (eg, tacrolimus, sirolimus, cyclosporine), buprenorphine, buprenorphine/naloxone, methadone (possible opiate withdrawal syndrome). Reduce concomitant clarithromycin dose in renal impairment. Separate dosing of didanosine. Others.
Adverse Reactions:
Diarrhea, nausea, vomiting, abdominal pain, headache; skin reactions (may be severe; discontinue if occurs), drug-induced hepatitis, new onset diabetes, hyperglycemia, fat redistribution, immune reconstitution syndrome, others.
Note:
Note: See Norvir entry for more information on ritonavir. To register pregnant patients exposed to darunavir/ritonavir call (800) 258-4263.
Metabolism:
Hepatic (CYP3A); 95% protein bound.
Elimination:
Fecal (primary), renal.
Generic Availability:
NO
How Supplied:
Tabs 75mg—480; 150mg—240; 600mg—60; 800mg—30; Oral susp—200mL (w. dosing syringe)
http://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?setid=814301F9-C990-46A5-B481-2879A521A16F