Trade Names:Truvada- Tablets emtricitabine 200 mg/tenofovir disoproxil fumarate 300 mg (equiv. to tenofovir disoproxil 245 mg)
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.Tenofovir disoproxil fumarate
Tenofovir disoproxil fumarate is a prodrug of tenofovir, which inhibits the activity of HIV-1 reverse transcriptase by competing with deoxyadenosine 5-triphosphate and by DNA chain termination after incorporation into DNA.
Treatment of HIV-1 infection in combination with other antiretroviral agents.
PO Emtricitabine 200 mg/tenofovir disoproxil fumarate 300 mg once daily.Renal Function ImpairmentAdults
POCrCl 50 mL/min or more
Give dose every 24 h.CrCl 30 to 49 mL/min
Give dose every 48 h.CrCl less than 30 mL/min
Do not administer.
Store tablets at controlled room temperature (59° to 86°F).
Tenofovir concentrations may be elevated, increasing the risk of adverse reactions. The AUC and C min of atazanavir may be decreased.Didanosine
AUC and C max of didanosine may be elevated, increasing the risk of adverse reactions (eg, neuropathy, pancreatitis).Drugs that reduce renal function or compete for active tubular secretion (eg, acyclovir, cidofovir, ganciclovir, valacyclovir)
May increase serum concentrations of emtricitabine or tenofovir.Lamivudine
Because of similarities between emtricitabine and lamivudine, drugs containing lamivudine should not be coadministered.
None well documented.
Incidences of the following adverse reactions were reported with combined use of emtricitabine/tenofovir disoproxil fumarate plus efavirenz.
Depression, fatigue (9%); dizziness (8%); headache (6%); insomnia (5%); asthenia (postmarketing).
Diarrhea, nausea (9%); vomiting (2%); abdominal pain, increased amylase, pancreatitis (postmarketing).
Acute renal failure, acute tubular necrosis, Fanconi syndrome, increased creatinine, interstitial nephritis, nephrogenic diabetes insipidus, polyuria, proteinuria, proximal renal tubulopathy, renal failure, renal insufficiency (postmarketing).
Hepatic steatosis, hepatitis, increased liver enzymes (postmarketing).
Allergic reactions (postmarketing).
Increased fasting cholesterol (22%); increased creatine kinase (9%); increased serum amylase (8%); elevated fasting triglycerides (4%); decreased neutrophils, hematuria, increased AST (3%); hyperglycemia, increased ALT (2%); increased alkaline phosphatase (1%).
Hypokalemia, hypophosphatemia, lactic acidosis (postmarketing).
Muscular weakness, myopathy, osteomalacia, rhabdomyolysis (postmarketing).
Sinusitis, upper respiratory tract infections (8%); dyspnea (postmarketing).
Lactic acidosis and hepatomegaly with steatosis (including fatal cases) have been reported with use of nucleoside analogues alone and in combination with other antiretroviral agents. Truvada is not indicated for the treatment of chronic hepatitis B virus (HBV) infection and the safety and efficacy have not been established in patients co-infected with HBV and HIV.
Monitor patient for signs of lactic acidosis. Withhold drug and notify health care provider immediately if any of the following occur: feeling cold, dizzy, or light-headed; profound weakness or tiredness; slow or irregular heartbeat; unexpected stomach discomfort; unusual muscle pain.
Calculate CrCl prior to starting therapy and as appropriate during therapy.
Category B .
Undetermined. Advise HIV-infected mothers not to breast-feed infants.
Safety and efficacy not established.
Use with caution because of greater frequency of decreased hepatic, renal, or cardiac function, and concomitant diseases or other drug therapy.
Dosage adjustments are recommended. Do not administer to patients with CrCl less than 30 mL/min or to patients with end-stage renal disease requiring dialysis.
Decreases from baseline bone mineral density at the lumbar spine and hip have been seen. Ensure that bone density monitoring is performed in HIV-infected patients with history of pathologic bone fracture or at substantial risk for osteopenia. Ensure that supplementation with calcium and vitamin D has been considered in patients with HIV-associated osteopenia or osteoporosis.
Redistribution and accumulation of body fat, including central obesity, dorsocervical fat enlargement (buffalo hump), peripheral wasting, facial wasting, breast enlargement, and cushingoid appearance, may occur.
Exacerbations of hepatitis B have been reported after discontinuation of emtricitabine. It is recommended that all patients with HIV be tested for chronic HBV before initiating antiretroviral therapy. Closely monitor patients who are coinfected with HIV and HBV with both clinical and laboratory follow-up for at least several months after stopping treatment.
Dosage adjustment is recommended.
During initial phase of treatment, patients may develop an inflammatory response to indolent or residual opportunistic infections.
Renal function impairment, including acute renal failure and Fanconi syndrome, can occur.
Limited clinical experience is available.
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