Adefovir Dipivoxil Tablets

Adefovir is an acyclic phosphorylated nucleoside analog of adenosine monophosphate. It is phosphorylated to an active metabolite, adefovir diphosphate, under the action of cellular kinases. Adefovir diphosphate inhibits HBV DNA polymerase (reverse transcriptase) in the following two ways: one is to compete with the natural substrate deoxyadenosine triphosphate, and the other is to cause the termination of DNA chain extension after integration into viral DNA. The inhibition constant (Ki) of adefovir diphosphate on HBV DNA polymerase is 0.1μM. However, the inhibitory effect on human DNA polymerase α and γ is weak, with Ki values of 1.18μM and 0.97μM, respectively.

The main ingredients of this product: Adefovir dipivoxil, chemical name: 9-{2-[di-(pivaloyloxymethoxy)phosphorylmethoxy]ethyl}adenine. Molecular weight: C20H32N5O8

This product is off-white tablets.

This product is suitable for the treatment of adult patients with chronic hepatitis B with active replication of hepatitis B virus and compensated liver function with persistent elevation of serum amino acid transferase.

Adults (18-65 years old): The recommended dose of this product is 10 mg once a day, either orally before or after meals.

Common adverse reactions in foreign clinical studies are weakness, headache, abdominal pain, nausea, (gastrointestinal) flatulence, diarrhea and indigestion. Adverse reactions in domestic clinical studies include leukopenia (mild), diarrhea (mild) and alopecia (moderate). One serious adverse event occurred in the clinical study, which was a case of acute myeloid leukemia type M3 after 29 weeks of treatment with this product. The researcher judged that it was not related to this product. The main adverse reaction is that the use of adefovir dipivoxil has strong potential nephrotoxicity, and once the drug is discontinued, the patient is likely to experience an exacerbation of hepatitis.

This product is contraindicated in patients with known hypersensitivity to adefovir, adefovir dipivoxil, or any excipients in adefovir dipivoxil tablets.

Precautions for children: The efficacy and safety of Hevili in patients under 18 years of age have not been determined (see [Precautions] - Others). Adefovir dipivoxil should not be used in children and adolescents. Precautions for pregnancy and lactation: Pregnancy: There is insufficient data on the use of adefovir dipivoxil in pregnant women. Animal studies of intravenous adefovir have shown reproductive toxicity (see [Pharmacology and Toxicology] - Clinical Safety Data). Pregnant women should avoid using adefovir dipivoxil as much as possible. If it is necessary to use it, the pros and cons should be weighed. The use of adefovir dipivoxil during pregnancy can only be considered when the potential benefits definitely outweigh the risks to the fetus. There is currently no data on the effect of adefovir dipivoxil on mother-to-child transmission of HBV. Therefore, infants should be immunized according to standard recommendations to prevent neonatal HBV infection. Because the potential risk to the developing human embryo is not clear, it is recommended that women of childbearing age treated with adefovir dipivoxil take effective contraceptive measures. Lactation: It is not yet known whether adefovir is secreted into human breast milk. Therefore, mothers who are taking adefovir dipivoxil should be warned not to breastfeed their babies. Precautions for the elderly: The efficacy and safety of Hevily in elderly patients over 65 years old have not been clearly established (see [Precautions] - Others).

Adefovir dipivoxil is rapidly converted to adefovir in the body. At concentrations significantly higher than those observed in vivo (4000 times), adefovir has no inhibitory effect on any of the following common human CYP450 enzymes: CYP1A2, CYP2C9, CYP2C19, CYP2D6 and CYP3A4. Adefovir dipivoxil is not a substrate for these enzymes. However, it is not clear whether adefovir can induce CYP450 enzymes. Based on the results of in vitro experiments and the renal elimination pathway of adefovir, the possibility of adefovir interacting with other drugs mediated by CYP450 as an inhibitor or substrate is very small. Adefovir is excreted through the kidneys by glomerular filtration and active tubular secretion (see [Pharmacokinetics] - Elimination). The combined use of 10 mg of adefovir dipivoxil with other drugs secreted by the renal tubules or drugs that change the renal tubular secretion function can increase the serum concentration of adefovir dipivoxil or the combined drug (see [Precautions] - Renal Function). Caution should be exercised when 10 mg of adefovir dipivoxil is used in combination with drugs that are actively secreted by the renal tubules, because the two drugs compete for the same elimination pathway, which may cause an increase in the serum concentration of adefovir or the co-administered drug. Adefovir dipivoxil does not change the pharmacokinetics of lamivudine, trimethoprim/sulfamethoxazole, acetaminophen, and ibuprofen. When adefovir dipivoxil is used simultaneously with lamivudine, trimethoprim/sulfamethoxazole, and acetaminophen, the pharmacokinetics of adefovir dipivoxil are not changed. When adefovir dipivoxil is used simultaneously with ibuprofen (800 g, 3 times a day), adefovir dipivoxil Cmax (33%), AUC (23%), and urinary recovery increase, which appears to be due to increased oral bioavailability rather than decreased renal clearance.

seal.

10mg

Tentatively 24 months.

Star Lake Bioscience Co., Inc. Zhaoqing Guangdong

• Founded in:

  2006-12-11

• Address:

  No. 64, Heping Road, Zhaoqing City

• Tax NO.:

  91441200796261264M

• Registered Funds:

  -

• Email:

  Log in to view