Trade Names:Emtriva- Capsules 200 mg- Solution, oral 10 mg/mL
Inhibits activity of HIV-1 reverse transcriptase by competing with the natural substrate deoxycytidine 5′-triphosphate and by being incorporated into nascent viral DNA, resulting in chain termination.
Rapidly and extensively absorbed after oral administration. Absolute bioavailability is about 93% (capsules) and 75% (solution). Postdose T max about 1 to 2 h. Steady-state C max is about 1.8 mcg/mL. AUC is about 10 mcg/mL•h. Mean steady-state trough plasma concentration at 24 h postdose is 0.09 mcg/mL.
Plasma t ½ is approximately 10 h. Eliminated in the urine (86% with 13% as putative metabolites) and feces (14%).
C max and AUC are increased in patients with CrCl less than 50 mL/min or end-stage renal disease requiring dialysis. Dosage reduction required.Hepatic Function Impairment
Emtricitabine is not metabolized by liver enzymes, so the impact of hepatic impairment should be limited.Elderly
Not fully evaluated.Children
Exposure is similar to adults.
In combination with other antiretroviral agents for the treatment of HIV-1 infection.
Hepatitis B virus (HBV) treatment.
PO 200 mg capsule once daily or 240 mg (24 mL) oral solution once daily.Children 3 mo through 17 yr of age
PO 200 mg capsules once daily for children weighing more than 33 kg or 6 mg/kg oral solution up to a max of 240 mg (24 mL) once daily.Children 0 to 3 mo of age
PO 3 mg/kg once daily.Renal Function ImpairmentAdults
PO CrCl at least 50 mL/min, administer 200 mg capsules every 24 h or 240 mg (24 mL) oral solution every 24 h. CrCl 30 to 49 mL/min, administer 200 mg capsules every 48 h or 120 mg (12 mL) oral solution every 24 h. CrCl 15 to 29 mL/min, administer 200 mg capsules every 72 h or 80 mg (8 mL) oral solution every 24 h. CrCl less than 15 mL/min or hemodialysis, administer 200 mg capsules every 96 h or 60 mg (6 mL) oral solution every 24 h.Children
PO Consider a reduction in dose and/or increase in dosing interval similar to adjustments for adults.
Store capsules at 59° to 86°F. Store solution under refrigeration at 36° to 46°F. Use solution within 3 mo if stored at 59° to 86°F.
Do not coadminister with Atripla or Truvada , or drugs containing lamivudine.
None well documented.
Dizziness (25%); headache (22%); insomnia (16%); abnormal dreams (11%); depression, depressive disorders, fatigue (9%); paresthesia (6%); neuropathy/peripheral neuritis (4%).
Hyperpigmentation (32%); rash event, including allergic reaction, maculopapular rash, pruritus, pustular rash, rash, urticaria, and vesiculobullous rash (30%).
Otitis media (23%); rhinitis (20%).
Diarrhea, vomiting (23%); nausea (18%); abdominal pain (14%); gastroenteritis (11%); dyspepsia (8%).
Elevated cholesterol (22%); elevated creatinine kinase (12%); elevated triglycerides (10%); increased amylase (8%); elevated AST (6%); decreased neutrophils, elevated CPK, elevated gamma-glutamyl transferase, increased ALT (5%); decreased hemoglobin (4%); hematuria, hyperglycemia, hypoglycemia (3%); elevated pancreatic amylase (2%); elevated alkaline phosphatase, elevated bilirubin, elevated lipase (1%).
Increased cough (28%); pneumonia (15%); sinusitis, upper respiratory tract infection (8%); nasopharyngitis (5%).
Infection (44%); fever (18%); asthenia (16%); anemia (7%); myalgia (6%); arthralgia (5%).
Lactic acidosis and severe hepatomegaly with stenosis, including fatal cases, have been reported with use of nucleoside analogs alone and in combination with other antiretroviral agents.
Emtricitabine is not indicated for the treatment of chronic HBV infection. Severe acute exacerbations of HBV have been reported in patients who have discontinued emtricitabine.
Monitor patient for signs of lactic acidosis. Closely monitor hepatic function for at least several months in patients who discontinue emtricitabine or are coinfected with HIV-1 and HBV. HBV testing is recommended prior to initiation of therapy. Closely monitor clinical response to treatment and renal function in patients with baseline CrCl less than 50 mL/min.
Category B .
Undetermined. HIV-infected mothers should not breast-feed their infants.
Use with caution because of the greater frequency of decreased hepatic, renal, or cardiac function, and concomitant diseases or other drug therapy.
Dosage adjustment is recommended.
Redistribution and accumulation of body fat, including central obesity, dorsocervical fat enlargement (buffalo hump), peripheral wasting, facial wasting, breast enlargement, and cushingoid appearance, have occurred in patients receiving antiretroviral therapy.
During the initial phase of treatment, patients may develop an inflammatory response to indolent or residual opportunistic infections.
No severe reactions were reported with a single dose of 1,200 mg.
Copyright © 2009 Wolters Kluwer Health.