Entecavir Dispersible Tablets

This product is a guanine nucleoside analog that has an inhibitory effect on hepatitis B virus (HBV) polymerase. It can be converted into an active triphosphate through phosphorylation, and the half-life of the triphosphate in the cell is 15 hours. By competing with the natural substrate of HBV polymerase, deoxyguanosine triphosphate, entecavir triphosphate can inhibit all three activities of viral polymerase (reverse transcriptase): (1) HBV polymerase initiation; (2) formation of pregenomic mRNA reverse transcription negative strand; (3) synthesis of HBVDNA positive strand. The inhibition constant (Ki) of entecavir triphosphate on HBVDNA polymerase is 0.0012μM. Entecavir triphosphate has a weak inhibitory effect on cellular α, β, δDNA polymerase and mitochondrial γDNA polymerase, with Ki values ranging from 18 to 160μM.

Entecavir

This product is white to off-white tablets

It is suitable for the treatment of chronic hepatitis B in adults with active viral replication, persistent elevation of serum transaminase ALT, or active lesions shown in liver histology.

1. Adults and adolescents over 16 years old should take this product orally, once a day, 0.5 mg each time. 2. Patients who develop viremia or lamivudine-resistant mutations during lamivudine treatment should take it once a day, 1 mg each time. 3. This product should be taken on an empty stomach (at least 2 hours before or after a meal).

ALT increase, fatigue, dizziness, nausea, abdominal pain, abdominal discomfort, upper abdominal pain, liver discomfort, myalgia, insomnia and urticaria. These adverse events are mostly mild to moderate. In the trial compared with lamivudine, the incidence of adverse events of this product is comparable to that of lamivudine.

The metabolism of entecavir was evaluated in vivo and in vitro. Entecavir is not a substrate, inhibitor, or inducer of the cytochrome P450 (CYP450) enzyme system. At concentrations approximately 10,000 times the human concentration, entecavir does not inhibit any of the major human CYP450 enzymes: 1A2, 2C9, 2C19, 2D6, 3A4, 2B6, and 2E1. At concentrations approximately 340 times the human concentration, entecavir does not induce human CYP450 enzymes: 1A2, 2C9, 2C19, 3A4, 3A5, and 2B6. Concomitant administration of drugs that are metabolized by inhibiting or inducing the CYP450 system has no effect on the pharmacokinetics of entecavir. In addition, concomitant administration of entecavir has no effect on the pharmacokinetics of known CYP substrates. When studying the interaction of entecavir with lamivudine, adefovir, and tenofovir, it was found that the steady-state pharmacokinetics of entecavir and the interacting drugs were not altered. Because entecavir is primarily cleared by the kidneys, taking entecavir with drugs that reduce renal function or compete for active glomerular secretion may increase the plasma concentrations of these two drugs. Concomitant use of entecavir with lamivudine, adefovir, and tenofovir does not cause significant drug interactions. The interaction of concomitant use of entecavir with other drugs that are cleared by the kidneys or are known to affect renal function has not been studied. Patients should be closely monitored for the occurrence of adverse reactions when taking entecavir and such drugs at the same time.

Seal tightly and store in a dry place below 25℃.

0.5 mg

36 months

Hunan Qianjin Xieli Pharmaceutical Co., Ltd.

• Founded in:

  2003-06-26

• Address:

  No. 1361, Huanghe North Road, Tianyuan District, Zhuzhou City

• Tax NO.:

  9143020075336479XF

• Registered Funds:

  32 million yuan

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