Classes
DEA Class; Rx
Common Brand Names; Prezista
- HIV, Protease Inhibitors
Description
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
Indications
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
Contraindications
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
Adverse Effects
- 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
Warnings
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
Pregnancy and Lactation
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
Maximum Dosage
1200 mg/day PO.
1200 mg/day PO.
weighing 40 kg or more: 1200 mg/day PO.
weighing 30 to 39 kg: 900 mg/day PO.
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.
Not recommended.
Not recommended.
How supplied
Darunavir
tablet
- 75mg
- 150mg
- 400mg
- 600mg
- 800mg
oral suspension
- 100mg/mL
