Generic Name and Formulations:
Darunavir (as ethanolate) 75mg, 150mg, 600mg, 800mg; tabs.

Company:
Janssen Therapeutics

Indications for PREZISTA:
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 ORAL SUSPENSION

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)