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Stribild(埃替拉韦+恩曲他滨+富马酸替诺福韦酯)

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STRIBILD(elvitegravir,cobicistat,恩曲他滨 emtricitabine,富马酸替诺福韦酯 tenofovir disoproxil fumarate)片,为口服的新组方药丸

STRIBILD is a one-pill, once-a-day prescription medicine used as a complete HIV-1 treatment. STRIBILD is used to treat HIV-1 in adults who have never taken HIV-1 medicines before. STRIBILD does not cure HIV-1 or AIDS.

Pharmacological Class:

Integrase strand transfer inhibitor + pharmacokinetic enhancer + nucleos(t)ide analog HIV-1 reverse transcriptase inhibitors.

Active Ingredient(s):

Elvitegravir 150mg, cobicistat 150mg, emtricitabine 200mg, tenofovir disoproxil fumarate (DF) 300mg; tablets.

Company

Gilead Sciences, Inc.

Indication(s):

Treatment of HIV-1 infection in adults who are antiretroviral treatment-na?ve.

Pharmacology:

Stribild is a fixed-dose combination tablet containing elvitegravir, cobicistat, emtricit?abine, and tenofovir DF. Elvitegravir is a HIV-1 integrase strand transfer inhibitor. Cobicistat is a mechanism-based inhibitor of CYP450 enzymes of the CYP3A family. Tenofovir DF, an acyclic nucleoside phosphonate diester analog of adeno?sine monophosphate, is converted in vivo to ?tenofovir. Emtricitabine is a synthetic nucleoside analog of cytidine.

Clinical Trials:

The approval of Stribild is supported by 48-week data from two Phase 3 studies in which the single tablet regimen met its primary objective of non-inferiority compared to Atripla (efavirenz 600mg/emtricitabine 200mg/tenofovir disoproxil fumarate 300mg) (Study 102) and to a regimen containing ritonavir-boosted atazanavir plus Truvada (emtricitabine 200mg/tenofovir disoproxil fumarate 300mg) (Study 103).

Legal Classification:

Rx

Adults:

1 tablet once daily with food. Renal impairment (CrCl <70mL/min): do not initiate; if CrCl declines to <50mL/min during therapy discontinue. Severe hepatic impairment: not recommended.

Children:

<18 years: not established.

Contraindication(s):

Concomitant alfuzosin, rifampin, ergots, cisapride, St. John’s wort, lova?statin, simvastatin, pimozide, sildenafil (when dosed for PAH), triazolam, oral midazolam.

Warnings/Precautions:

Suspend therapy if lactic acidosis or hepatotoxicity (eg, hepatomegaly, steatosis) occurs. Not for treating chronic hepatitis B; test for HBV before starting therapy and closely monitor patients co-infected with HBV and HIV during and for several months after stopping treatment (discontinuing therapy may exacerbate HBV infection). Monitor creatinine clearance, urine glucose, urine protein, serum phosphorus (for patients at risk for renal impairment). History of pathologic fracture or risk factors of osteoporosis or bone loss: consider monitoring bone mineral density (BMD). Pregnancy (Cat. B). Nursing mothers: not recommended.

Interaction(s)

See Contraindications. Avoid with concurrent or recent use of nephrotoxic agents. Do not administer with other antiretroviral agents. May be potentiated by CYP3A inhibitors, antagonized by CYP3A inducers. May potentiate drugs metabolized by CYP3A or CYP2D6, or are substrates of P-gp, BCRP, OATP1B1 or OATP1B3. May antagonize CYP2C9 substrates. Separate antacids by at least 2 hours. May potentiate antiarrhythmics, digoxin, clarithromycin (reduce dose by 50% if CrCl 50–60mL/min), telithromycin, carbamaze?pine, clonazepam, ethosuximide, SSRIs, TCAs, trazodone, ketoconazole (max 200mg/day), itraconazole (max 200mg/day), voriconazole, beta-blockers, calcium channel blockers, fluticasone (use alternative corticosteroid), atorvastatin, immunosuppressants, (monitor), neuroleptics, sedatives/hypnotics, PDE5 inhibitors (see literature for dose adjustments). Antagonized by carbamazepine, oxcarbazepine, phenobarbital, phenytoin, rifabutin, rifapentine, systemic dexamethasone. Con?com?itant colchicine (see literature); do not coadminister to patients with renal or hepatic impairment. Dis?continue use of bosentan at least 36 hours prior to initiation of Stribild; after at least 10 days following initiation, resume bosentan. Concomitant salmet?erol: not recommended; increased risk of cardiovascular events. Use alternative non-hormonal methods of contraception. Monitor INR.

Adverse Reaction(s)

Nausea, diarrhea; decreased BMD, fat redistribution, immune reconstitution syndrome.

How Supplied:

Tabs—30

LAST UPDATED:

12/1/2012

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