Entecavir Capsules, nickname entecavir hydrate and entecavir hydrate, is the latest anti hepatitis B virus first-line drug. In addition to entecavir capsule, there are entecavir dispersible tablets. Entecavir capsule is suitable for the treatment of chronic adult hepatitis B with active virus replication, continuous increase of serum transaminase ALT or active liver histology.
The main ingredient is entecavir. Chemical name: 2-amino-9 – [(1s, 3R, 4S) – 4-hydroxy-3-hydroxymethyl-2-methylene cyclopentyl] – 1,9-dihydro-6h-purine-6-one monohydrate.
Properties: This product is white or almost white tablets.
Indications: chronic hepatitis B, gastroenterology.
This product is suitable for the treatment of chronic adult hepatitis B with active virus replication, continuous increase of serum transaminase ALT or active liver histology
It is prohibited for those allergic to entecavir or any ingredient in the preparation.
When nucleoside drugs are used alone or in combination with other antiretroviral drugs, lactic acidosis and severe fatty hepatomegaly, including death cases, have been reported.
When chronic hepatitis B patients stopped anti HBV treatment, severe acute exacerbation of hepatitis B has been reported, including entecavir. The liver function of those who stopped anti HBV treatment should be closely monitored in clinical and laboratory examinations, and at least for several months. If necessary, the treatment of anti HBV can be resumed.
Limited clinical experience suggests that if Entecavir Capsules is used in the treatment of chronic hepatitis B virus (HBV) with human immunodeficiency virus (HIV) infection and without anti HIV therapy, there may be resistance to HIV nucleoside reverse transcriptase inhibitors. Entecavir is not recommended in patients with HBV complicated with HIV infection and not receiving highly active antiretroviral therapy (HAART).
Medication for pregnant women: the study on the effect of entecavir on pregnant women is insufficient. This product can only be used after fully weighing the potential risks and benefits of the fetus. At present, there is no data suggesting that this product can affect the mother to child transmission of HBV. Therefore, appropriate intervention measures should be taken to prevent neonatal infection with HBV. Entecavir Capsules can be secreted from rat milk. However, it is still unclear whether there is secretion in human milk, so mothers taking this product are not recommended to breastfeed.
Medication for children: the safety and efficacy data of this product for children under 16 years old have not been established
Geriatric medication: since there are not enough elderly patients aged 65 and over to participate in the clinical study of this product, it is unclear how the reactions of elderly patients and young patients to this product are different. Other clinical trial reports also did not find the difference between elderly patients and young patients. Entecavir Capsules is mainly excreted by the kidney. In patients with renal function injury, the risk of toxic reaction may be higher. Because most of the elderly patients have decreased renal function, we should pay attention to the choice of drug dose and monitor renal function.
The metabolism of Entecavir Capsules was evaluated in vivo and in vitro. Entecavir is not a substrate, inhibitor or inducer of cytochrome P450 (CYP450) enzyme system. Entecavir did not inhibit any major human CYP450 enzymes: 1A2, 2C9, 2c19, 2d6, 3A4, 2b6 and 2E1 when the concentration reached about 10000 times that in human body. When the concentration reached about 340 times that in human body, Entecavir Capsules did not induce human CYP450 enzymes: 1A2, 2C9, 2c19, 3A4, 3A5 and 2b6. Simultaneous administration of drugs metabolized by inhibiting or inducing CYP450 system had no effect on the pharmacokinetics of entecavir. Moreover, simultaneous administration of entecavir had no effect on the pharmacokinetics of known CYP substrates.
When studying the interaction of Entecavir Capsules with lamivudine, adefovir and tenofovir, it was found that the steady-state pharmacokinetics of entecavir and its interacting drugs did not change. Since entecavir is mainly cleared through the kidney, taking drugs that reduce renal function or competitive secretion through the active glomerulus may increase the blood concentration of these two drugs. There was no obvious drug interaction between entecavir and lamivudine, adefovir and tenofovir. The interaction of concomitant Entecavir Capsules with other drugs known to affect renal function through renal clearance has not been studied. Patients should closely monitor the occurrence of adverse reactions when taking entecavir and such drugs at the same time.