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All about: Emtricitabine

Big Image Pronouncation: (em-trye-SYE-ta-been)
Class: NNRT inhibitor

Trade Names:
Emtriva
- Capsules 200 mg
- Oral solution 10 mg/mL

Mechanism of Action

Pharmacology

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%. Postdose C 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 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%).

Indications and Usage

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

Unlabeled Uses

Hepatitis B virus (HBV) treatment.

Contraindications

Standard considerations.

Dosage and Administration

Adults

PO 200 mg capsules 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 who can swallow an intact capsule, or 6 mg/kg oral solution up to a max of 240 mg (24 mL) once daily.

Renal function impairment
Adults

PO Ccr at least 50 mL/min, administer 200 mg capsules every 24 h or 240 mg (24 mL) oral solution every 24 h. Ccr 30 to 49 mL/min, administer 200 mg capsules every 48 h or 120 mg (12 mL) oral solution every 24 h. Ccr 15 to 29 mL/min, administer 200 mg capsules every 72 h or 80 mg (8 mL) oral solution every 24 h. Ccr less than 15 mL/min or hemodialysis, administer 200 mg capsules every 96 h or 60 mg (6 mL) oral solution every 24 h.

General Advice

  • May be administered without regard to meals. Administer with food if GI upset occurs.
  • Although data are insufficient to recommend a specific dose adjustment in children with renal function impairment, consider a reduction in dose and or increase in dosing interval similar to adjustments for adults.

Storage/Stability

Store capsules at controlled room temperature (59° to 86°F). Store oral solution under refrigeration at 36° to 46°F. Use oral solution within 3 mo if stored at 77°F.

Drug Interactions

None well documented.

Laboratory Test Interactions

None well documented.

Adverse Reactions

CNS

Adults

Headache (13%); insomnia (7%); depressive disorders (6%); paresthesia (5%); dizziness, neuropathy/peripheral neuritis (4%); abnormal dreams (2%).

Dermatologic

Adults

Rash event (17%; including allergic reaction, maculopapular rash, pruritus, pustular rash, rash, urticaria, vesiculobullous rash); skin discoloration (hyperpigmentation on palms and/or soles).

Children

Hyperpigmentation (32%); rash (21%).

EENT

Adults

Rhinitis (18%).

Children

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

GI

Adults

Diarrhea (23%); nausea (18%); vomiting (9%); dyspepsia (4%).

Children

Vomiting (23%); diarrhea (20%); gastroenteritis (11%).

Hematologic-Lymphatic

Children

Anemia (7%).

Lab Tests

Children

Decreased neutrophils, elevated CPK, increased ALT, increased amylase (9%).

Respiratory

Adults

Increased cough (14%).

Children

Increased cough (28%); pneumonia (15%).

Miscellaneous

Adults

Asthenia (16%); abdominal pain (8%); myalgia (4%); arthralgia (3%).

Children

Infection (44%); fever (18%); abdominal pain (10%).

Precautions

Warnings

Lactic acidosis/severe hepatomegaly with stenosis

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.


Monitor

Monitor patient for signs of lactic acidosis. If patient develops profound weakness or tiredness; unexpected stomach discomfort; feeling cold, dizzy, or light-headed; or fast or irregular heartbeat, withhold drug.


Pregnancy

Category B .

Lactation

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

Children

Safety and efficacy not established in children younger than 3 mo of age.

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.

Hepatitis B

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 coinfected with HIV and HBV using clinical and laboratory follow-up for at least several months after stopping treatment.

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.

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