entecavir (en-tek-aveer) Baraclude

 Indications

Chronic hepatitis B infection with evidence of active viral

replication and either persistent elevations in AST or

ALT or histologically active disease.

Action

Phosphorylated intracellularly to active form which acts

as an analogue of guanosine, interfering with viral DNA

synthesis. Therapeutic Effects: Decreased hepatic

damage due to chronic hepatitis B infection.

Pharmacokinetics

Absorption: Well absorbed following oral administration.

Distribution: Extensive tissue distribution.

Metabolism and Excretion: 62–73% excreted

unchanged by kidneys.

Half-life: Plasma—128–149 hr; intracellular—15

hr.

TIME/ACTION PROFILE (blood levels)

ROUTE ONSET PEAK DURATION

PO rapid 0.5–1 hr 24 hr

Contraindications/Precautions

Contraindicated in: Hypersensitivity; Lactation: Potential

for serious adverse effects in infant.

Use Cautiously in: Renal impairment (doseprecommended

if CCr 50 mL/min; Liver transplant recipients

(careful monitoring of renal function recommended);

Patients coinfected with HIV (unless

receiving highly active antiretroviral therapy; atqrisk

for resistance); OB: Use only if clearly needed, considering

benefits and risks; Pedi: Children 2 yr (safety

not established); Geri:qrisk of toxicity due to age-relatedpin

renal function.

Adverse Reactions/Side Effects

CNS: dizziness, fatigue, headache. GI: HEPATOMEGALY

(WITH STEATOSIS), dyspepsia, nausea. F and E: LACTIC

ACIDOSIS. Derm: alopecia, rash.

Interactions

Drug-Drug: Concurrent use of drugs which may impair

renal function mayqblood levels and risk of toxicity.

Route/Dosage

PO (Adults and Children 16 yr): Compensated

liver disease—0.5 mg once daily (1 mg once daily if

history of lamivudine or telbivudine resistance); Decompensated

liver disease—1 mg once daily.

Renal Impairment

PO (Adults and Children 16 yr): CCr 30–50

mL/min—0.25 mg once daily or 0.5 mg q 48 hr (0.5

mg once daily or 1 mg q 48 hr if history of lamivudine

resistance) CCr 10–30 mL/min—0.15 mg once

daily or 0.5 mg q 72 hr (0.3 mg once daily or 1 mg q

72 hr if history of lamivudine resistance); CCr 10 mL/

min—0.05 mg once daily or 0.5 mg q 7 days (0.1 mg

once daily or 1 mg q 7 days if history of lamivudine resistance).

PO (Children 2–16 yr and 10–11 kg): 0.15 mg

once daily (0.3 mg once daily if history of lamivudine

resistance).

PO (Children 2–16 yr and 11–14 kg): 0.2 mg

once daily (0.4 mg once daily if history of lamivudine

resistance).

PO (Children 2–16 yr and 14–17 kg): 0.25 mg

once daily (0.5 mg once daily if history of lamivudine

resistance).

PO (Children 2–16 yr and 17–20 kg): 0.3 mg

once daily (0.6 mg once daily if history of lamivudine

resistance).

PO (Children 2–16 yr and 20–23 kg): 0.35 mg

once daily (0.7 mg once daily if history of lamivudine

resistance).

PO (Children 2–16 yr and 23–26 kg): 0.4 mg

once daily (0.8 mg once daily if history of lamivudine

resistance).

PO (Children 2–16 yr and 26–30 kg): 0.45 mg

once daily (0.9 mg once daily if history of lamivudine

resistance).

PO (Children 2–16 yr and 30 kg): 0.5 mg once

daily (1 mg once daily if history of lamivudine resistance).

Availability (generic available)

Tablets: 0.5 mg, 1 mg. Oral solution (orange flavor):

0.05 mg/mL.