Product Overview
[Drug Name]
Generic Name: Entecavir Dispersible Tablets
Trade Name: Aipuding
English Name: Entecavir Dispersible Tablets
Chinese Pinyin: EnTiKaWeiFenSanPian
[Ingredients]
Entecavir
[Properties]
This product is a white to off-white tablet.
[Indications]
It is indicated for the treatment of chronic hepatitis B in adults with active viral replication, persistently elevated serum ALT, or active liver histological lesions.
[Dosage and Administration]
1. Adults and adolescents aged 16 years and over, take 0.5 mg orally once daily.
2. For patients who develop viremia or lamivudine-resistant mutations during lamivudine treatment, take 1 mg once daily.
3. This product should be taken on an empty stomach (at least 2 hours before or after a meal).
[Adverse Reactions]
ALT elevation, fatigue, dizziness, nausea, abdominal pain, abdominal discomfort, upper abdominal pain, liver discomfort, myalgia, insomnia, and urticaria. These adverse events were mostly mild to moderate. In studies comparing this product to lamivudine, the incidence of adverse events was comparable to that of lamivudine.
[Precautions]
1. Patients with renal impairment
2. Liver transplant recipients
3. Pregnant and lactating women
4. Pediatrics
5. Elderly patients. See package insert for details.
[Drug Interactions]
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 any of the human CYP450 enzymes: 1A2, 2C9, 2C19, 3A4, 3A5, and 2B6. Concomitant administration of drugs metabolized by CYP450 inhibitors or inducers has no effect on the pharmacokinetics of entecavir. Furthermore, concomitant administration of entecavir has no effect on the pharmacokinetics of known CYP substrates. Studies of the interaction of entecavir with lamivudine, adefovir, and tenofovir revealed no alterations in the steady-state pharmacokinetics of either entecavir or the interacting drugs. Because entecavir is primarily eliminated by the kidneys, concurrent administration of entecavir with drugs that reduce renal function or compete for active glomerular secretion may increase the plasma concentrations of these drugs. Concomitant administration of entecavir with lamivudine, adefovir, or tenofovir does not result in significant drug interactions. The interaction of entecavir with other drugs that are eliminated by the kidneys or are known to affect renal function has not been studied. Patients taking entecavir with these drugs should be closely monitored for adverse reactions.
[Pharmacology]
This product is a guanine nucleoside analog that inhibits hepatitis B virus (HBV) polymerase. It can be phosphorylated to form an active triphosphate, which has a half-life of 15 hours in cells. By competing with the natural substrate of HBV polymerase, deoxyguanosine triphosphate, entecavir triphosphate can inhibit all three activities of viral polymerase (reverse transcriptase): (1) initiation of HBV polymerase; (2) formation of the negative strand of pregenomic mRNA reverse transcription; and (3) synthesis of the positive strand of HBV DNA. The inhibition constant (Ki) of entecavir triphosphate on HBV DNA polymerase is 0.0012 μM. Entecavir triphosphate has a weak inhibitory effect on cellular α, β, δ DNA polymerase and mitochondrial γ DNA polymerase, with Ki values of 18 to 160 μM.
[Storage]Sealed and stored in a dry place below 25°C.
[Specification] 0.5mg x 7 tablets
[Packaging] Box
[Expiration Period] 24 months
[Approval Number] National Medicine Standard H20140093
[Manufacturer] Company Name: Hunan Qianjin Xieli Pharmaceutical Co., Ltd.
