PREZISTA Rx

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PREZISTA

Viral infections
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Generic Name and Formulations:

Darunavir (as ethanolate) 75mg, 150mg, 600mg, 800mg; tabs.

Select therapeutic use:

Indications for PREZISTA:

Treatment of HIV-1 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 or 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 or with no baseline resistance information: 600mg twice daily with ritonavir 100mg twice daily. Pregnancy: 600mg twice daily with ritonavir 100mg twice daily; may consider 800mg once daily with ritonavir 100mg once daily only if stable on dose prior to pregnancy and virologically suppressed (HIV-1 RNA <50copies/mL). Severe hepatic impairment: not recommended.

Children:

<3yrs: not recommended. Take with food. Use oral susp if unable to swallow tabs. Treatment-naive or 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 once daily with ritonavir 100mg once daily; ≥30kg–<40kg: 675mg 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 twice daily with ritonavir 48 mg twice daily; ≥30kg–<40kg: 450mg twice daily with ritonavir 60mg twice daily; ≥40kg: 600mg twice daily with ritonavir 100mg twice daily. Severe hepatic impairment: not recommended.

Contraindications:

Concomitant alfuzosin, dronedarone, colchicine (in renal and/or hepatic impairment), ranolazine, pimozide, ergots, cisapride, oral midazolam, triazolam, St. John's wort, lovastatin, simvastatin, rifampin, sildenafil (Revatio; only when used to treat PAH).

Warnings/Precautions:

Perform genotypic/phenotypic testing, treatment history in treatment-experienced patients prior to initiation. Sulfonamide allergy. Hepatic impairment (eg, chronic hepatitis, cirrhosis, pre-treatment elevated transaminases): monitor liver enzymes esp. during 1st few weeks; 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. Nursing mothers: not recommended.

Interactions:

See Contraindications. Voriconazole, salmeterol, boceprevir, simeprevir, apixaban, rivaroxaban, dabigatran (in renal impairment), rifapentine, everolimus, avanafil, not studied protease inhibitors (eg, lopinavir/ritonavir, saquinavir): not recommended. Potentiates carbamazepine, risperidone, thioridazine, TCAs, trazodone, 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), sedatives/hypnotics, budesonide, prednisolone, fluticasone, bosentan (see full labeling), maraviroc (max 150mg twice daily), colchicine (dose adjustments: see full labeling), quetiapine (reduce dose by ⅙ or consider alternative antiretrovirals). Potentiates, and is potentiated by, indinavir, ketoconazole, itraconazole. Antagonizes sertraline, paroxetine, phenytoin, phenobarbital (monitor levels), ethinyl estradiol, norethindrone (use backup contraception). Antagonized by dexamethasone. 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. Reduce concomitant clarithromycin dose in renal impairment. Separate dosing of didanosine.

See Also:

PREZISTA ORAL SUSPENSION

Pharmacological Class:

Protease inhibitor.

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.

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)

PREZISTA 800mg tablets (Qty:30)

appx. price $1369.00