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darunavir Indications HIV infection (must be used with ritonavir and with other antiretrovirals).

Action Inhibits HIV-1 protease, selectively inhibiting the cleavage of HIV-encoded specific polyproteins in infected cells. This prevents the formation of mature virus particles. Therapeutic Effects: Increased CD4 cell counts and decreased viral load with subsequent slowed progression of HIV infection and its sequelae. Pharmacokinetics Absorption: Without ritonavir37% absorbed following oral administration; with ritonavir 82%. Foodqabsorption by 30%. Distribution: Unknown. Protein Binding: 95% bound to plasma proteins. Metabolism and Excretion: Extensively metabolized by CYP3A enzyme system. 41% eliminated unchanged in feces, 8% in urine. Half-life: 15 hr. TIME/ACTION PROFILE
ROUTE ONSET PEAK DURATION PO unknown 2.54 hr 12 hr

Contraindications/Precautions Contraindicated in: Concurrent dihydroergotamine, ergonovine, ergotamine, methylergonovine, midazolam, pimozide, triazolam, lovastatin, simvastatin, rifampin, or St. Johns wort; Lactation: HIV may be transmitted in human milk; Pedi: Children _3 yr. Use Cautiously in: Hepatic impairment; Sulfa allergy; Geri: Consider age-related impairment in hepatic function, concurrent chronic disease states and drug therapy; OB: Use in pregnancy only if maternal benefit outweighs fetal risk; Pedi: Children 36 yr (safety not established). Adverse Reactions/Side Effects Based on concurrent use with ritonavir. GI: HEPATOTOXICITY, constipation, diarrhea, nausea, vomiting. Endo: hyperglycemia. Metab: body fat redistribution. Derm: rash. Interactions Drug-Drug: Darunavir and ritonavir are both inhibitors of CYP3A and are metabolized by CYP3A. Multiple drug-drug interactions can be expected with drugs that share, inhibit, or induce these pathways. Consult product information for more specific details. Rifampinqmetabolism and maypantiretroviral effectiveness, concurrent use is contraindicated.pmetabolism of and may qrisk of ergot toxicity with dihydroergotamine, ergonovine, ergotamine, or methylergonovine; concurrent use is contraindicated.p metabolism of and mayqrisk of myopathy with lovastatin and simvastatin; concurrent use is contraindicated.qlevels and risk of cardiotoxicity with pimozide; concurrent use is contraindicated. qlevels and risk of excess CNS depression with midazolam or triazolam; concurrent use is contraindicated. Concurrent use with indinavir mayqdarunavir and indinavir levels.qlevels

and risk of myopathy from atorvastatin, rosuvastatin, or pravastatin (use lowest dose of these agents or consider fluvastatin). Concurrent use with efavirenz results inpdarunavir levels andqefavirenz levels; use combination cautiously. Lopivavir/ritonavir mayplevels; although concurrent use is not recommended, additional ritonavir may be required. Saquinavir mayplevels; concurrent use is not recommended. qlevels of lidocaine, quinidine, propafenone, flecainide, and amiodarone; use cautiously and with available blood level monitoring. qdigoxin levels; blood level monitoring recommended. Mayqcarbamazepine levels; blood level monitoring recommended. Mayp phenytoin or phenobarbital levels; blood level monitoring recommended.plevels of warfarin; monitor INR.qlevels of trazodone and desipramine; use cautiously andpdose if necessary. qlevels of clarithromycin;pdose of clarithromycin if CCr _60 mL/min. Ketoconazole and itraconazole may levels.qlevels of ketoconazole and itraconazole

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