Prezista

Darunavir

HIV-1 infection in adults & childn ≥6 yr, & weighing ≥40 kg, in combination w/ ritonavir & other antiretroviral agents.

Treatment-naïve adult & ped patient Prezista 800 mg w/ ritonavir 100 mg once daily. Treatment-experienced adult & ped patient w/ no darunavir resistance associated substitutions Prezista 800 mg once daily w/ ritonavir 100 mg once daily. Treatment-experienced adult patient w/ at least 1 darunavir resistance associated substitution, or w/ no baseline resistance information Prezista 600 mg bd w/ ritonavir 100 mg bd. Treatment-experienced ped patient w/ at least 1 darunavir resistance associated substitutions Prezista 600 mg w/ ritonavir 100 mg bd. Childn 6 to <18 yr, & weighing ≥40 kg Do not exceed the recommended adult dose.

Should be taken with food.

Hypersensitivity. Co-administration w/ drugs that are highly dependent on CYP3A for clearance & for which elevated plasma conc are associated w/ serious &/or life-threatening events (narrow therapeutic index) eg, alfuzosin, colchicine (in patients w/ renal &/or hepatic impairment), rifampin, lurasidone, pimozide, dronedarone, ivabradine, ranolazine, ergot derivatives, cisapride, St. John's wort (Hypericum perforatum), elbasvir/grazoprevir, lomitapide, lovastatin, simvastatin, naloxegol, sildenafil when used for treatment of pulmonary arterial HTN, orally administered midazolam/triazolam.

Discontinue immediately if signs or symptoms of severe skin reactions develop. Failure to administer w/ ritonavir & food may result in loss of efficacy of darunavir. Reports of drug-induced hepatitis. Increased risk for liver function abnormalities in patients w/ pre-existing liver dysfunction, including chronic active hepatitis B or C. Conduct appropriate lab testing eg, serum liver biochemistries prior to initiating therapy, & monitor during treatment. Patients w/ underlying chronic hepatitis, cirrhosis, or in patients who have pre-treatment elevations of transaminases should be monitored for elevation in serum liver biochemistries, especially during the 1st several mth of treatment. Contains a sulfonamide moiety; caution in patients w/ known sulfonamide allergy. Reports of new onset DM, exacerbation of pre-existing DM, hyperglycemia; redistribution/accumulation of body fat; immune reconstitution syndrome. Reports of increased bleeding, including spontaneous skin hematomas & hemarthrosis in patients w/ hemophilia type A & B treated w/ PIs. Co-administration w/ CYP3A substrates, inhibitors or inducers. Not recommended in patients w/ severe hepatic impairment. Advise patients to use an effective alternative (non-hormonal) contraceptive method or add a barrier method of contraception. Clinical monitoring is recommended when co-administered w/ drospirenone. Use only during pregnancy if potential benefit justifies potential risk. Do not breastfeed while on treatment. Not recommended in childn <6 yr. Caution in elderly patients.

Treatment-naïve adults: Diarrhea, headache, abdominal pain, rash, nausea, vomiting, anorexia; lab abnormalities (increased ALT, AST, triglycerides, total cholesterol, LDL-C, glucose levels, pancreatic lipase, pancreatic amylase). Treatment-experienced adults: Diarrhea, nausea, rash, abdominal pain, vomiting, asthenia, headache, abdominal distension, dyspepsia, fatigue, anorexia, DM; lab abnormalities (increased ALT, AST, triglycerides, total cholesterol, LDL-C, glucose levels, pancreatic lipase, pancreatic amylase). Treatment-experienced ped subject 6 to <18 yr, weighing at least 20 kg: Vomiting, diarrhea, abdominal pain, headache, rash, nausea, fatigue; lab abnormalities (increased ALT, AST, pancreatic amylase, pancreatic lipase, total cholesterol, LDL). Treatment-experienced ped subject 3 to <6 yr, weighing at least 10 kg: Diarrhea, vomiting, rash, abdominal pain, anorexia. Treatment‑naïve ped patients 12 to <18 yr, weighing at least 40 kg: Vomiting, nausea, diarrhea, abdominal pain, decreased appetite, pruritus, rash.

Increased plasma conc of drugs that are primarily metabolized by CYP3A & CYP2D6 or are transported by P-gp. Prezista/ritonavir co-administered w/ drugs that have active metabolite(s) formed by CYP3A may result in reduced plasma conc of these active metabolite(s). Lowered plasma conc w/ CYP3A inducers. Increased plasma conc w/ CYP3A or P-gp inhibitors. Didanosine should be administered 1 hr before or 2 hr after Prezista/ritonavir (administered w/ food). Increased conc of both darunavir & indinavir when co-administered. Not recommended to co-administer w/ lopinavir or saquinavir w/ or w/o ritonavir. Increased conc of darunavir & the co-administered antifungals (itraconazole, isavuconazole, ketoconazole). Increased conc of darunavir & the co-administered rifabutin & its active metabolite. Increased conc of maraviroc; alfuzosin; clarithromycin (adjust clarithromycin dose in patients w/ renal impairment); apixaban, rivaroxaban; carbamazepine; clonazepam; amitriptyline, desipramine, imipramine, nortriptyline, trazodone; colchicine; lumefantrine; antineoplastics (eg, dasatinib, nilotinib, vinblastine, vincristine); lurasidone, pimozide, quetiapine, antipsychotics (eg, perphenazine, risperidone, thioridazine); β-blockers; Ca-channel blockers; ranolazine, ivabradine, dronedarone, antiarrhythmics, digoxin; systemic corticosteroid primarily metabolized by CYP3A; bosentan; ergot derivatives; cisapride; elbasvir/grazoprevir, glecaprevir/pibrentasvir; immunosuppressants; salmeterol; HMG-CoA reductase inhibitors; lomitapide; fentanyl, oxycodone, tramadol; norbuprenorphine; naloxegol; PDE-5 inhibitors; ticagrelor; orally administered midazolam/triazolam, sedatives/hypnotics; fesoterodine, solifenacin. Decreased conc of warfarin; phenytoin, phenobarb; paroxetine, sertraline; voriconazole; ethinyl estradiol, norethindrone; methadone; clopidogrel active metabolite; omeprazole. Decreased conc w/ rifampin, rifapentine; systemic dexamethasone; St. John's wort. Potential for hyperkalemia w/ drospirenone.

Antivirals

J05AE10 - darunavir ; Belongs to the class of protease inhibitors. Used in the systemic treatment of viral infections.

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