Drug Index

Entecavir

 
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Mechanism :

By competing with the natural substrate deoxyguanosine triphosphate, entecavir functionally inhibits all three activities of the HBV polymerase (reverse transcriptase, rt): (1) base priming, (2) reverse transcription of the negative strand from the pregenomic messenger RNA, and (3) synthesis of the positive strand of HBV DNA. Upon activation by kinases, the drug can be incorporated into the DNA which has the ultimate effect of inhibiting the HBV polymerase activity.


Indication :

• Chronic hepatitis B virus infection


Contraindications :

Hypersensitivity, Patients with HIV who are not receiving HAART.


Dosing :

<2 years: Safety and efficacy not established. To be taken on an empty stomach.

>2 years: Nucleoside-naive: 0.5 mg orally every day. In lamivudine or telbivudine known resistant mutation: 1 mg orally every day.


Adverse Effect :

Fatigue, headache, dizziness, nausea, diarrhea, dyspepsia, vomiting, somnolence, insomnia, lactic acidosis, increased transaminases.


Interaction :

Drugs that reduce Renal Function or Compete for Active Tubular Secretion: Coadministration with entecavir may increase serum concentrations of either entecavir or the co administered drug.

Lamivudine, Adefovir Dipivoxil, or Tenofovir Disoproxil Fumarate: Coadministration with entecavir did not result in significant drug interactions.



Renal Dose :

Dose in Renal Impairment GFR (mL/min)
30-50250 mcg daily; 500 mcg daily in lamivudine-refractory patients
10-30150 mcg daily; 300 mcg daily in lamivudine-refractory patients
<1050 mcg daily; 100 mcg daily in lamivudine-refractory patients

Dose in Patients undergoing Renal Replacement Therapies
CAPD0.3% dialysed. Dose as in GFR<10 mL/min
HD13% dialysed. Dose as in GFR<10 mL/min
HDF/High fluxDialysed. Dose as in GFR<10 mL/ min
CAV/VVHDLikely to be dialysed. Dose as in GFR=10–30 mL/min

Hepatic Dose :

No dosage adjustments are recommended.
06/01/2020 08:14:32 Entecavir
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