Classifications: antiretroviral agent; hiv protease inhibitor; Therapeutic:antiretroviral; protease inhibitor
Pregnancy Category: B
300 mg tablets
Darunavir is an inhibitor of HIV-1 protease that selectively inhibits the cleavage of HIV polyproteins in infected cells,
thereby preventing the maturation of virus particles.
Darunavir reduces the viral load (decreases the number of RNA copies) and increases the number of T helper CD4 cells.
Treatment of HIV infection, usually in combination with two nucleoside reverse transcriptase inhibitors, such as lamivudine
Hypersensitivity to darunavir or protease inhibitors, ritonavir; pancreatitis; lactation. Safety and efficacy in children
have not been established.
Hepatic function impairment, hepatitis; severe renal impairment, chronic renal failure; hemophilia A or B; diabetes mellitus;
diabetes ketoacidosis; hyperglycemia; elderly; pregnancy (category B).
Route & Dosage
Adult: PO 600 mg b.i.d. with 100 mg ritonavir PO
CNS: Headache. GI:
- Give with food and coadminister with 100 mg ritonavir.
- Tablets must be swallowed whole.
- Store at 15°30° C (59°86° F). Protect from light and moisture.
Abdominal pain, constipation
, diarrhea, vomiting. Skin:
InteractionsDrug: azole antifungals
increase the levels of darunavir. Coadministration of other inhibitors of CYP3A4 may also increase darunavir. anticonvulsants
(e.g., carbamazepine, phenobarbital, phenytoin
), efavirenz, rifamycins
(e.g., rifampin, rifabutin
), and saquinavir
may decrease darunavir levels. Darunavir may increase the levels of azole antifungals
, efavirenz, indinavir, rifamycins
, amiodarone, bepridil, lidocaine, quinidine, calcium channel blockers
(e.g., nifedipine, nicardipine, felodipine
), clarithromycin, immunosuppressants
(e.g., cyclosporine, sirolimus, tacrolimus
), phosphodiesterase type 5 inhibitors
(e.g., sildenafil, tadalafil, vardenafil
), and trazodone, due in part to its ability to inhibit CYP3A4. Darunavir decreases the levels of the lopinavir
combination, oral contraceptives
(e.g., ethinyl estradiol, norethindrone
), methadone, selective serotonin reuptake inhibitors
(e.g., paroxetine, sertraline
)], and warfarin.
Coadministration of darunavir with benzodiazepines
(e.g., midazolam, triazolam
) increases the risk of prolonged or increased sedation or respiratory depression
. Coadministration of darunavir with ergot alkaloids
may increase ergot toxicity
. Coadministration of darunavir with hmg coa reductase inhibitors
increases the risk of myopathy. Combination use of darunavir with pimozide
increases the risk of cardiac arrhythmias. Food:
Food enhances the bioavailability of darunavir. Herbal: St. John's wort
decreases the level of darunavir.
82% absorbed (in combination with ritonavir). Peak:
2.54 h. Distribution:
95% protein bound. Metabolism:
In the liver. Elimination:
Primarily fecal (80%) with minor elimination in urine. Half-Life:
Assessment & Drug Effects
- Monitor for and report S&S of pancreatitis, as this may be an indication for discontinuation of darunavir.
- Monitor for S&S of skin rash. Notify physician immediately if a severe rash appears.
- Monitor diabetics for loss of glycemic control.
- Lab tests: Periodic CD4+ cell count, plasma HIV-RNA, lipid profile, LFTs; and plasma glucose.
- Increase monitoring of INR with concurrent warfarin therapy.
- Monitor for adverse effects or loss of efficacy of concurrent medications, as many drug interactions occur with darunavir.
Patient & Family Education
- Follow directions for taking the drug (see Administration). If a dose is missed by more than 6 h, wait until the next regularly
scheduled dose. If a dose is missed by less than 6 h, take a dose and continue with the next regularly scheduled dose.
- Tell your health care professional about all medications you are taking, including non-prescription drugs, nutritional supplements,
or herbal products.
- Ensure that you know which medicines should NOT be taken with darunavir, as serious consequences could occur.
- Report any of the following to a health care provider: blistering, redness, or peeling skin or mucus membranes; severe skin
- Use or add a barrier contraceptive if using an estrogen-containing oral contraceptive in order to prevent pregnancy.