Product Overview
[Drug Name]
Generic Name: Entecavir Dispersible Tablets
Trade Name: Bei Shuang Ding
English Name: Entecavir Tablets
Chinese Pinyin: EnTiKaWeiFenSanPian (BeiShuangDing)
[Ingredients]
Entecavir. Chemical Name: 2-Amino-9-[(1S,3R,4S)-4-hydroxy-3-hydroxymethyl-2-methylenecyclopentyl]-1,9-dihydro-6H-purin-6-one monohydrate.
[Properties]
This product is a white or off-white tablet.
[Indications]
This product 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]
Adults and adolescents aged 16 years and above should take 0.5 mg (1 tablet) orally once daily. Patients who develop viremia or lamivudine-resistant mutations during lamivudine treatment should receive 1 mg (two 0.5 mg tablets) once daily. This product should be taken on an empty stomach (at least 2 hours before or after a meal). See the inner package insert for details.
[Adverse Reactions]
1. The evaluation of adverse reactions was based on four global clinical trials: AI463014, AI463022, AI463026, and AI463027, as well as three clinical trials conducted in China (AI463012, AI463023, and AI463056). A total of 2,596 patients with chronic hepatitis B were enrolled in these seven studies. In studies comparing entecavir to lamivudine, adverse events and laboratory abnormalities were similar between entecavir and lamivudine. 2. In studies conducted internationally, the most common adverse events with this product were headache, fatigue, dizziness, and nausea. Common adverse events in patients treated with lamivudine include headache, fatigue, and dizziness. In these four studies, 1% of entecavir-treated patients and 4% of lamivudine-treated patients withdrew from the study due to adverse events and abnormal laboratory test values. See the inner package insert for details.
[Contraindications]
Entecavir is contraindicated in patients with allergies to entecavir or any of the ingredients in the formulation.
[Precautions]
1. For patients with a creatinine clearance <50 ml/min, including those on hemodialysis or CAPD, an adjustment in the entecavir dose is recommended. 2. The safety and efficacy of entecavir in liver transplant recipients are unknown. If a liver transplant recipient is considered for entecavir treatment and has been or is currently receiving immunosuppressive medications that may affect renal function, such as cyclosporine or tacrolimus, renal function should be closely monitored before and during entecavir administration. 3. Patients should take entecavir under the guidance of a physician and inform their physician of any new symptoms and concomitant medications. Patients should be informed that discontinuation of entecavir may lead to worsening of liver disease, and therefore should consider changing their treatment under the guidance of their physician. 4. Patients should undergo HIV antibody testing before starting entecavir treatment. Patients should be informed that if they are infected with HIV and not receiving effective HIV medication, entecavir may increase the risk of developing resistance to HIV medication. For details, see the inner package insert. Please read the package insert carefully and use as directed by your doctor.
[Special Population Use]
Precautions for Children:
Safety and efficacy data for this drug in children under 16 years of age have not been established.
Precautions for Pregnancy and Breastfeeding:
Studies on the effects of entecavir on pregnant women are inadequate. This drug should only be used after a thorough balance of potential risks and benefits has been made.
Precautions for Elderly Patients:
Due to the lack of sufficient clinical studies involving patients aged 65 years and older, it is unclear whether elderly patients respond differently to this drug compared to younger patients. Other clinical trial reports have not found differences between elderly and younger patients. Entecavir is primarily excreted by the kidneys, and the risk of toxic reactions may be higher in patients with impaired renal function. Because elderly patients often have decreased renal function, careful attention should be paid to dosage selection and renal function monitoring.
[Drug Interactions]
The metabolism of entecavir was evaluated in vitro and in vivo. 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 did 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 did not induce the following human CYP450 enzymes: 1A2, 2C9, 2C19, 3A4, 3A5, and 2B6. Concomitant administration of drugs that are metabolized by CYP450 inhibitors or inducers did not affect the pharmacokinetics of entecavir. Furthermore, concomitant administration of entecavir did not affect the pharmacokinetics of known CYP substrates.
[Pharmacological Action]
In human HepG2 cells transfected with wild-type hepatitis B virus, the concentration required for 50% inhibition of viral DNA synthesis (EC50) of entecavir was 0.004 μM. The median EC50 for entecavir against lamivudine-resistant viral strains (rtL180M, rtM204V) was 0.026 μM (range, 0.01 to 0.059 μM). Coadministration of entecavir with HIV nucleoside reverse transcriptase inhibitors (NRTIs) is unlikely to reduce the anti-HBV efficacy of entecavir or any of the other agents in this class. In testing HBV combination therapy in cell culture, abacavir, didanosine, lamivudine, stavudine, tenofovir, or zidovudine did not antagonize the anti-HBV activity of entecavir over a wide range of concentrations. In HIV antiviral activity studies, entecavir showed no antagonistic effect on the anti-HIV activity of six NRTIs in cell culture at concentrations four times greater than the peak in vivo concentration. See the inner package insert for details.
[Storage] Sealed.
[Strength] 0.5 mg
[Packaging] 7 tablets/box
[Expiry Date] 24 months
[Approval Number] National Medicine Standard H20140037
[Manufacturer] Anhui Baker Biopharmaceutical Co., Ltd.
