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Darunavir

    Brands

    DEA Class; Rx

    Common Brand Names; Prezista

    • HIV, Protease Inhibitors

    Protease inhibitor (PI)
    For human immunodeficiency virus (HIV) infection when used in combination with other antiretroviral agents
    HIV strains resistant to other PIs are responsive to darunavir

    Coadministered with ritonavir and in combination with other antiretroviral agents for HIV infection

    Treatment-naive or antiretroviral treatment-experienced (with no darunavir resistance associated substitutions): 800 mg + ritonavir 100 mg PO qDay with food

    Hypersensitivity

    Coadministration of darunavir/ritonavir

    • Concomitant CYP3A4 substrates that are toxic in excess
    • Concurrent strong CYP3A4 inducers (eg, St John’s wort, rifampin)
    • Alpha-1 antagonist: Alfuzosin
    • Cardiovascular agents: Ranolazine, ivabradine, dronedarone
    • Antigout: Colchicine (in patients with renal/and or hepatic impairment)
    • Antimycobacterial: Rifampin
    • Antipsychotics: Lurasidone, pimozide
    • Ergot derivatives (eg, dihydroergotamine, ergotamine, methylergonovine)
    • GI motility agent: Cisapride
    • Herbal product: St. John’s wort (Hypericum perforatum)
    • Hepatitis C direct acting antiviral: Elbasvir/grazoprevir
    • Lipid modifying agents: Lomitapide, lovastatin, simvastatin
    • PDE-5 inhibitor: Sildenafil (used for treatment of pulmonary arterial hypertension)
    • Sedatives/hypnotics: PO midazolam, triazolam
    • Opioid antagonist: Naloxegol
    • Increased total cholesterol (10-25%)
    • Increased triglycerides (3-10%)
    • Diarrhea (9%)
    • Headache (7%)
    • Rash (6%)
    • Abdominal pain (6%)
    • Nausea (4%)
    • Vomiting (2%)
    • Anorexia (2%)
    • Fatigue

    Must be taken with ritonavir and food, since dose is based on the fact that darunavir is metabolized by CYP3A4 and ritonavir is a potent CYP3A4 inhibitor

    Severe skin reactions, accompanied by fever and/or elevations of transaminases reported (0.4%); Stevens-Johnson Syndrome (<0.1%), toxic epidermal necrolysis, drug rash with eosinophilia and systemic symptoms, and acute generalized exanthematous pustulosis also reported

    Caution with elderly patients

    Caution with hepatic impairment (not recommended if severe)

    Contains a sulfa moiety; monitor patients with a known sulfonamide allergy

    Increase in total cholesterol and triglycerides reported; screen before therapy and throughout treatment

    Pancreatitis reported; use caution in patients at risk for pancreatitis (those with elevated triglycerids, history of pancreatitis, or advanced HIV disease

    Risk of immune reconstitution syndrome

    Redistribution/accumulation of body fat, including central obesity, dorsocervical fat enlargement (buffalo hump), peripheral wasting, facial wasting, breast enlargement, and “cushingoid appearance” have been observed in patients receiving antiretroviral therapy

    Patients may develop new onset diabetes mellitus or hyperglycemia; initiation or dose adjustments of insulin or oral hypoglycemic agents may be required

    Patients with hemophilia may develop increased bleeding events

    Not for use in patients < 3 years of age; toxicity may occur

    The recommended dosage in pregnant patients is 600 mg taken with ritonavir 100 mg twice daily with food

    There are no data on the presence of darunavir in human milk, the effects on the breastfed infant, or the effects on milk production

    Adults

    1200 mg/day PO.

    Geriatric

    1200 mg/day PO.

    Adolescents

    weighing 40 kg or more: 1200 mg/day PO.
    weighing 30 to 39 kg: 900 mg/day PO.

    Children

    3 to 12 years weighing 40 kg or more: 1200 mg/day PO.
    3 to 12 years weighing 30 to 39 kg: 900 mg/day PO.
    3 to 12 years weighing 15 to 29 kg: 750 mg/day PO.
    3 to 12 years weighing 14 to 14.9 kg: 560 mg/day PO.
    3 to 12 years weighing 13 to 13.9 kg: 520 mg/day PO.
    3 to 12 years weighing 12 to 12.9 kg: 480 mg/day PO.
    3 to 12 years weighing 11 to 11.9 kg: 440 mg/day PO.
    3 to 12 years weighing 10 to 10.9 kg: 400 mg/day PO.
    3 to 12 years weighing less than 10 kg: Not recommended.
    younger than 3 years: Not recommended.

    Infants

    Not recommended.

    Neonates

    Not recommended.

    Darunavir 

    tablet

    • 75mg
    • 150mg
    • 400mg
    • 600mg
    • 800mg

    oral suspension

    • 100mg/mL