Names and pronunciation
(en-te′ka-veer) Baraclude
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Individual generic drug information
Extracted information for entecavir only.
(en-te′ka-veer) Baraclude
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Func. class.: Antiviral
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Chem. class.: Nucleoside analog
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ACTION: Inhibits hepatitis B virus DNA polymerase by competing with natu- ral substrates and by causing DNA termi- nation after its incorporation into viral DNA; causes viral DNA death
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USES: Chronic hepatitis B (HBV)
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Extracted information for entecavir only.
CONTRAINDICATIONS: Hyper- sensitivity Precautions: Pregnancy, breastfeeding, children, geriatric patients, severe renal disease, liver transplant
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Black Box Warning: Hepatic disease, hepatitis, HIV, lactic acidosis Black Box Warning: For HIV prior to be- ginning treatment because HIV resistance may occur in chronic hepatitis B patients; monitor HIV RNA; don’t use in those with HIV and HBV unless receiving antiretroviral treatment for both Black Box Warning: For lactic acido- sis and severe hepatomegaly with stenosis; increased serum lactate, in- creased hepatic enzymes; discontinue if present, discontinue if signs occur; may be fatal • Geriatric patients more carefully; may develop renal, cardiac symptoms more rapidly Black Box Warning: For exacerbations of hepatitis (jaundice, pruritus, fatigue), anorexia after discontinuing treatment, and for several months monitor LFTs • Pregnancy/breastfeeding: use if clearly needed; register pregnant women at the Antiretroviral Pregnancy Registry at 800- 258-4263; to reduce risk of postnatal transmission, HIV-infected mothers are advised to avoid breastfeeding Black Box Warning: Symptoms of lactic acidosis: muscle pain, severe tiredness, weakness, trouble breathing, stomach pain with nausea/vomiting, coldness in arms/ legs, fast/irregular heartbeat, dizziness Black Box Warning: Symptoms of hepato- toxicity: eyes/skin turning yellow, dark urine, light-colored bowel movements, no appetite for days, nausea, stomach pain; may be worsened after discontinuing treatment • That product does not cure but lowers amount of HBV in body • That product does not stop spread of HBV to others by sex, sharing needles, or being exposed to blood • Not to breastfeed; to notify prescriber if pregnancy is planned or suspected • Not to operate machinery until effect is known, dizziness may occur • That regular follow-up and lab tests will be needed HIGH ALERT
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SIDE EFFECTS CNS: Headache, fatigue, dizziness, insomnia ENDO: Hyperglycemia GI: Dyspepsia, nausea, vomiting, diar- rhea, elevated liver function enzymes INTEG: Alopecia, rash SYST: Lactic acidosis, severe hepato- megaly with steatosis
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INTERACTIONS Drug/Food Decrease: absorption—high-fat meal Drug/Lab Test Increase: ALT, AST, total bilirubin, amylase, lipase, creatinine, blood glucose, urine glucose Decrease: platelets, albumin
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Extracted information for entecavir only.
DOSAGE AND ROUTES Chronic hepatitis B (nucleoside treatment naive) • Adult and adolescent ≥16 yr: PO tablet 0.5 mg/day • Adult: PO (solution) 0.5 mg daily; Child/adolescent ≥2 yr >30 kg: 0.5 mg (10 mL) daily; Child ≥2 yr, 27 to 30 kg: 0.45 mg (9 mL) daily; Child ≥2 yr, 24 to 26 kg: 0.4 mg (8 mL) daily; Child ≥2 yr, 21 to 23 kg: 0.35 mg (7 mL) daily; Child ≥2 yr, 18 to 20 kg: 0.3 mg (6 mL) daily; Child ≥2 yr, 15 to 17 kg: 0.25 mg (5 mL) daily; Child ≥2 yr, 12 to 14 kg: 0.2 mg (4 mL) daily; Child ≥2 yr, 0.15 mg (3 mL) daily Chronic hepatitis B with compensated liver disease • Adult/adolescent ≥16 yr: PO tablet 1 mg/day • Adult: PO (solution) 1 mg/day; Child/ adolescent ≥2 yr, >30 kg: 1 mg (20 E mL) daily; Child ≥2 yr, 27 to 30 kg: 0.9 mg (18 mL) daily; Child ≥2 yr, 24 to 26 kg: 0.8 mg (16 mL) daily; Child ≥2 yr, 21 to 23 kg: 0.7 mg (14 mL) daily; Child ≥2 yr, 18 to 20 kg: 0.6 mg (12 mL) daily; Child ≥2 yr, 15 to 17 kg: 0.5 mg (10 mL) daily; Child ≥2 yr, 12 to 14 kg: 0.4 mg (8 mL) daily; Child ≥2 yr, 10 to 11 kg: 0.3 mg (6 mL) daily Renal dose • Adult/child >16 yr: PO CCr ≥50 mL/ min, 0.5 mg/day; CCr 30-49 mL/min, 0.25 mg/day, 0.5 mg/day or 1 mg q48hr for lamiVUDine-refractory patient; CCr 10-29 mL/min, 0.15/day or 1 mg q72hr for lami- VUDine-refractory patient; CCr <10 mL/ min, 0.05 mg/day, 0.1 mg/day or 1 mg q7day for lamiVUDine-refractory patient • Child 2-<16 yr: PO (dosage based on weight) 10-11 kg: 0.15 mg once daily (0.3 mg once daily if history of lami VUDine resistance) >11-14 kg: 0.2 mg once daily (0.4 mg once daily if history of lamiVUDine resistance) >14-17 kg: 0.25 mg once daily (0.5 mg once daily if history of lamiVUDine resistance) >17-20 kg: 0.3 mg once daily (0.6 mg once daily if history of lamiVUDine resistance) >20-23 kg: 0.35 mg once daily (0.7 mg once daily if history of lamiVUDine resistance) >23-26 kg: 0.4 mg once daily (0.8 mg once daily if history of lamiVUDine resistance) >26-30 kg: 0.45 mg once daily (0.9 mg once daily if history of lamiVUDine resistance) >30 kg: 0.5 mg once daily (1 mg once daily if history of lamiVUDine resistance)
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Available forms: Tablets, film coated 0.5, 1 mg; oral solution 0.05 mg/mL
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Administer: • After hemodialysis • By mouth on empty stomach 2 hr prior to or after food • Store at room temperature • Oral solution: use calibrated oral dos- ing spoon provided; may be used inter- changeably with tablets, do not dilute
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Extracted information for entecavir only.
Assess: • For nephrotoxicity: increasing CCr, BUN
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Evaluate: • Therapeutic response: decreased symptoms of chronic hepatitis B, improv- ing LFTs
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CLINICAL CONSIDERATIONS
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Patient and caregiver information: • Not to take with food; to take 2 hr prior to or after meals • To take exactly as prescribed, to read the “Patient Information,” to take missed dose when remembered unless close to time of next dose; that compliance with dosage schedule is required; not to share product • Not to stop medication without ap- proval of prescriber • That optimal duration of treatment is unknown • To avoid use with other medications, supplements unless approved by pre- scriber • To notify prescriber of decreased uri- nary output, blood in urine
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Extracted information for entecavir only.
PHARMACOKINETICS Peak 0.5-1.5 hr, steady-state 6-10 days, 100% bioavailability, extensively dis- tributed to tissues, protein binding 13%, terminal half-life 128-149 hr duration up to 24 hr, excreted unchanged (62%-73%) via kidneys
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Filter the extracted dose blocks for this individual drug.
Chronic hepatitis B (nucleoside treatment naive)
• Adult and adolescent ≥16 yr: PO tablet 0.5 mg/day
Candidate age grouping · source page 473
Chronic hepatitis B (nucleoside treatment naive)
• Adult: PO (solution) 0.5 mg daily; Child/adolescent ≥2 yr >30 kg: 0.5 mg (10 mL) daily; Child ≥2 yr, 27 to 30 kg: 0.45 mg (9 mL) daily; Child ≥2 yr, 24 to 26 kg: 0.4 mg (8 mL) daily; Child ≥2 yr, 21 to 23 kg: 0.35 mg (7 mL) daily; Child ≥2 yr, 18 to 20 kg: 0.3 mg (6 mL) daily; Child ≥2 yr, 15 to 17 kg: 0.25 mg (5 mL) daily; Child ≥2 yr, 12 to 14 kg: 0.2 mg (4 mL) daily; Child ≥2 yr, 0.15 mg (3 mL) daily Chronic hepatitis B with compensated liver disease
Candidate age grouping · source page 473
Chronic hepatitis B (nucleoside treatment naive)
• Adult/adolescent ≥16 yr: PO tablet 1 mg/day
Candidate age grouping · source page 473
Chronic hepatitis B (nucleoside treatment naive)
• Adult: PO (solution) 1 mg/day; Child/ adolescent ≥2 yr, >30 kg: 1 mg (20 E mL) daily; Child ≥2 yr, 27 to 30 kg: 0.9 mg (18 mL) daily; Child ≥2 yr, 24 to 26 kg: 0.8 mg (16 mL) daily; Child ≥2 yr, 21 to 23 kg: 0.7 mg (14 mL) daily; Child ≥2 yr, 18 to 20 kg: 0.6 mg (12 mL) daily; Child ≥2 yr, 15 to 17 kg: 0.5 mg (10 mL) daily; Child ≥2 yr, 12 to 14 kg: 0.4 mg (8 mL) daily; Child ≥2 yr, 10 to 11 kg: 0.3 mg (6 mL) daily Renal dose
Candidate age grouping · source page 473
Chronic hepatitis B (nucleoside treatment naive)
• Adult/child >16 yr: PO CCr ≥50 mL/ min, 0.5 mg/day; CCr 30-49 mL/min, 0.25 mg/day, 0.5 mg/day or 1 mg q48hr for lamiVUDine-refractory patient; CCr 10-29 mL/min, 0.15/day or 1 mg q72hr for lami- VUDine-refractory patient; CCr <10 mL/ min, 0.05 mg/day, 0.1 mg/day or 1 mg q7day for lamiVUDine-refractory patient
Candidate age grouping · source page 473