Therapeutic Class
Antiretroviral Agent, Protease Inhibitor

Treatment of HIV-1 infections in combination with ritonavir and other antiretroviral agents.

Adult Doses

Treatment of HIV infection: Oral:

Therapy-naive: 800 mg once daily; coadministration with ritonavir 100 mg once daily is required. Note: Recommended (with ritonavir) as a first-line therapy with tenofovir/emtricitabine in antiretroviral naïve patients

Therapy-experienced: Note: If genotypic testing is not possible, 600 mg twice daily, coadministered with ritonavir 100 mg twice daily, is recommended.

With no resistance-associated substitutions: 800 mg once daily; coadministration with ritonavir 100 mg once daily is required

With ≥1 resistance-associated substitution: 600 mg twice daily; coadministration with ritonavir 100 mg twice daily is required

Pediatric Doses

Treatment of HIV infection: Oral: 

Children ≥6 years:

≥20 kg to <30 kg: 375 mg twice daily; coadministration with ritonavir 50 mg twice daily is required

≥30 kg to <40 kg: 450 mg twice daily; coadministration with ritonavir 60 mg twice daily is required

≥40 kg: 600 mg twice daily; coadministration with ritonavir 100 mg twice daily is required

Note: Do not use once-daily dosing in pediatric patients; maximum dose: 600 mg darunavir/100 mg ritonavir twice daily.

Doses in Renal impairment

No adjustment required for mild-to-moderate impairment.

Doses in Hepatic impairment

No adjustment for mild-to-moderate impairment (Child-Pugh classes A and B). Not recommended for patients with severe impairment


Coadministration with medications highly dependent upon CYP3A4 for clearance and for which increased levels are associated with serious and/or life-threatening events e.g. alfuzosin, cisapride, ergot alkaloids [eg, dihydroergotamine, ergonovine, ergotamine, methylergonovine], lovastatin, midazolam [oral], pimozide, rifampin, sildenafil (when used for pulmonary artery hypertension ) , simvastatin, St John's wort, triazolam.

Warnings / Precautions

Fat redistribution: May cause redistribution of fat (eg, buffalo hump, peripheral wasting with increased abdominal girth, cushingoid appearance).

Hepatotoxicity: Infrequent cases of drug-induced hepatitis (including acute and cytolytic) have been reported. May exacerbate pre-existing hepatic dysfunction.

Hypersensitivity reactions:

Immune reconstitution syndrome: Patients may develop immune reconstitution syndrome resulting in the occurrence of an inflammatory response to an indolent or residual opportunistic infection; further evaluation and treatment may be required.

Increased cholesterol: Increases in total cholesterol and triglycerides have been reported;

Pancreatitis: use caution in patients at risk for pancreatitis including those with elevated triglycerides, advanced HIV disease, or history of pancreatitis.

Sulfonamide allergy: contains sulfa moiety

Diabetes: Changes in glucose tolerance, hyperglycemia, exacerbation of diabetes, DKA, and new-onset diabetes mellitus have been reported in patients receiving protease inhibitors.

Hemophilia A or B: increased bleeding during protease inhibitor therapy

Colchicine: Do not coadminister in patients with renal or hepatic impairment.

High potential for interactions: Use with caution in patients taking strong CYP3A4 inhibitors, moderate or strong CYP3A4 inducers and major CYP3A4 substrates ;

Salmeterol: Concomitant use not recommended due to increased risk of cardiovascular adverse events, including QTc prolongation.

Adverse Reactions

As a class, protease inhibitors potentially cause dyslipidemias which includes elevated cholesterol and triglycerides and a redistribution of body fat centrally to cause increased abdominal girth, buffalo hump, facial atrophy, and breast enlargement. These agents also cause hyperglycemia.

Endocrine & metabolic: Hypercholesterolemia, LDL increased, Hyperglycemia, triglycerides increased, diabetes mellitus

Gastrointestinal: Vomiting, diarrhea, Abdominal pain, nausea, amylase increased, lipase increased, abdominal distention, anorexia, dyspepsia

Central nervous system: Headache, fatigue

Dermatologic: Rash

Hepatic: ALT increased, AST increased, alkaline phosphatase

Neuromuscular & skeletal: Weakness

Food Interactions

Food: Bioavailability is increased when administered with food.

Herb/nutraceutical: St John’s wort may decrease the plasma levels of darunavir; concomitant use is contraindicated

Mechanism of Actions

Binds to the site of HIV-1 protease activity and inhibits cleavage of viral Gag-Pol polyprotein precursors into individual functional proteins required for infectious HIV. This results in the formation of immature, noninfectious viral particles.


Substrate of CYP3A4 (major); Inhibits P-glycoprotein


Absorption: Increased 30% with food

Protein binding: ~95%; primarily to alpha1 acid glycoprotein (AAG)

Metabolism: Hepatic, via CYP3A4 to minimally-active metabolites

Bioavailability: 82%

Half-life elimination: ~15 hours

Time to peak, plasma: 2.5-4 hours

Excretion: Feces (~80%, 41% as unchanged drug); urine (~14%, 8% as unchanged drug)

NOTE: All kinetic parameters derived in the presence of ritonavir coadministration.


Coadministration with ritonavir and food is required (bioavailability is increased). Take with meals.

Pregnancy Category

C: Drug Pregnancy Category Animal reproduction studies have shown an adverse effect on the fetus and there are no adequate and well-controlled studies in humans, but potential benefits may warrant use of the drug in pregnant women despite potential risks.


Excretion in breast milk unknown/not recommended

ATC Classification
GenericPedia Classification
  • Available As
  • Darunavir 300 mg
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