Lamivudine CAS: 134678-17-4
CAS Registry Number
475.4°C at 760 mmHg
4.91E-11mmHg at 25°C
New antiviral medicine
Lamivudine is a new antiviral drug, belonging to the nucleoside reverse transcriptase inhibitors, both in vitro and in experimental infected animals in hepatitis B virus (HBV) has strong inhibitory effect, can inhibit the synthesis of HIV virus, the drug by GlaxoSmithKline group. In the 1990s by some countries of Europe and North America used to treatment of AIDS medicine, the 1990s mid medical experts for the discovery of the DNA of hepatitis B virus inhibition, in 1998 the United States Food and Drug Administration (FDA) first approved as a medicine for treating hepatitis B treatment. China's State Food and Drug Administration approved the drug import is mainly used as a medicine for treating hepatitis B and Chinese goods were as lamivudine, 1999 officially began in domestic sales in mainland China. After 10 years of clinical validation, lamivudine is currently the only confirmed can delay the progression of liver cirrhosis, less side effects, less expensive medicine, at present, the 200 million hepatitis B patients are using.
Lamivudine in HBV infected cells and normal cells metabolism generates lamivudine triphosphate, which is the active form of lamivudine, both HBV polymerase inhibitor is also the polymerase substrate. Lamivudine triphosphate is incorporated into viral DNA chain, blocking viral DNA synthesis without disturbing the normal cells deoxynucleoside metabolism, weak inhibition of mammalian DNA polymerase alpha and beta, has almost no effect on the DNA content in mammalian cells. The structure, DNA content and function of mitochondria were not obvious. HBV-DNA test results showed that lamivudine can quickly inhibit HBV replication, and its inhibitory effect on the whole treatment process. At the same time, the serum levels of serum aminotransferase were decreased to normal. The long-term application of liver necrosis and inflammatory changes could be significantly improved.
Chronic hepatitis B virus replication of hepatitis B virus.
After oral administration of lamivudine, the absorption is good, and the concentration of 1hr in the adult oral 0.1g is about Cmax, and the concentration of 1.1-1.5 g/mL is 80-85%. With food at the same time, can make Tmax delay HR 0.25-2.5, Cmax 10-40%, but the biological use of the same. Intravenous dosing studies results show that lamivudine average distribution capacity of 1.3 L/Kg, system average clearance rate of 0.3 L / h / kg, percent seventy by organic cation transport system by renal clearance and elimination half-life 5-7hr. In the dose range, the pharmacokinetics of lamivudine was linear, and the plasma protein binding rate was low. In vitro studies showed that the binding rate of serum albumin was <16-36%. Can pass through the blood brain barrier to enter the cerebrospinal fluid. The drug was excreted by the kidney, and the excretion of the kidney was about 70% of the total, and only 5-10% was the derivative of the trans - sulfur oxide. The patient's renal function is not affected by the excretion of lamivudine, the creatinine clearance rate in patients with <30mL/, not recommended to use this product. Liver damage does not affect the metabolism of medicine, due to increased age and decreased renal excretory function in elderly patients, lamivudine metabolism without significant changes, only in the creatinine clearance rate <30mL/ points, to have effect.