Emtricitabine

Trade Names:
Emtriva
- Capsules 200 mg
- Solution, oral 10 mg/mL

Pharmacology

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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.

Pharmacokinetics

Absorption

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.

Elimination

Plasma t _½ is approximately 10 h. Eliminated in the urine (86% with 13% as putative metabolites) and feces (14%).

Special Populations

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.

Emtricitabine is not metabolized by liver enzymes, so the impact of hepatic impairment should be limited.

Not fully evaluated.

Exposure is similar to adults.

Indications and Usage

In combination with other antiretroviral agents for the treatment of HIV-1 infection.

Unlabeled Uses

Hepatitis B virus (HBV) treatment.

Contraindications

Standard considerations.

Dosage and Administration

PO 200 mg capsule once daily or 240 mg (24 mL) oral solution once daily.

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.

PO 3 mg/kg once daily.

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.

PO Consider a reduction in dose and/or increase in dosing interval similar to adjustments for adults.

General Advice

• May be administered without regard to meals. Administer with food if GI upset occurs.

Storage/Stability

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.

Drug Interactions

Do not coadminister with Atripla or Truvada , or drugs containing lamivudine.

Laboratory Test Interactions

None well documented.

Adverse Reactions

CNS

Dizziness (25%); headache (22%); insomnia (16%); abnormal dreams (11%); depression, depressive disorders, fatigue (9%); paresthesia (6%); neuropathy/peripheral neuritis (4%).

Dermatologic

Hyperpigmentation (32%); rash event, including allergic reaction, maculopapular rash, pruritus, pustular rash, rash, urticaria, and vesiculobullous rash (30%).

EENT

Otitis media (23%); rhinitis (20%).

GI

Diarrhea, vomiting (23%); nausea (18%); abdominal pain (14%); gastroenteritis (11%); dyspepsia (8%).

Lab Tests

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%).

Respiratory

Increased cough (28%); pneumonia (15%); sinusitis, upper respiratory tract infection (8%); nasopharyngitis (5%).

Miscellaneous

Infection (44%); fever (18%); asthenia (16%); anemia (7%); myalgia (6%); arthralgia (5%).

Precautions

Pregnancy

Category B .

Lactation

Undetermined. HIV-infected mothers should not breast-feed their infants.

Elderly

Use with caution because of the greater frequency of decreased hepatic, renal, or cardiac function, and concomitant diseases or other drug therapy.

Renal Function

Dosage adjustment is recommended.

Fat redistribution

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.

Immune reconstitution syndrome

During the initial phase of treatment, patients may develop an inflammatory response to indolent or residual opportunistic infections.

Overdosage

Symptoms

No severe reactions were reported with a single dose of 1,200 mg.

Patient Information

• Advise patient to read the patient information leaflet before starting therapy and with each refill.
• Warn patient that this drug is not to be used by itself but is combined with other antiviral agents and not to change the dose or stop taking any of the antiviral agents unless advised by health care provider.
• Advise patient to take prescribed dose daily without regard to meals but to take with food if stomach upset occurs.
• Advise patient that if a dose is missed to take the dose as soon as possible and then return to the normal schedule. However, if it is within 6 h of the next dose, skip the dose and take the next dose at the regular time. If a dose is skipped, caution patient not to double the dose to catch up but to continue with the normal schedule unless advised by health care provider.
• Instruct patient to report these symptoms immediately to health care provider: difficulty breathing; persistent nausea or vomiting; profound weakness or tiredness; unexpected stomach discomfort; fast or irregular heartbeat; feeling cold, dizzy, or light-headed.
• Inform patient that drug does not completely eliminate HIV virus and, therefore, does not reduce risk of transmitting HIV to others. Appropriate precautions must still be followed.
• Advise patient that the drug is not a cure for HIV infection and illnesses associated with HIV infection, including opportunistic infections, as they may continue to be acquired. Patient should remain under the care of health care provider.
• Caution HIV-infected mother that breast-feeding could cause HIV infection in the baby.
• Advise patients coinfected with HBV and HIV that severe acute exacerbations of hepatitis B have been reported when emtricitabine has been discontinued.
• Advise patients not to coadminister with other drugs containing lamivudine.
• Advise patients redistribution or accumulation of body fat may occur.

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