Zidolamil and davidin tablets

1. Lamivudine and zidovudine are effective selective inhibitors of HIV-1 and HIV-2. Both have strong synergistic effects and can inhibit HIV replication in cell culture. They can be gradually metabolized to 5-triphosphate (TP) by intracellular kinases. 2. Lamivudine-TP and zidovudine-TP are substrate competitive inhibitors of HIV reverse transcriptase. However, their main antiviral activity is incorporation into the viral DNA chain in the form of monophosphate, resulting in the termination of the viral DNA chain. 3. The triphosphate hydrochloride of lamivudine and zidovudine has a much lower affinity for host cell DNA polymerase than for viral DNA. In in vitro tests, the relationship between the sensitivity of lamivudine and/or zidovudine to HIV and the clinical treatment response is still under study. Because in vitro sensitivity tests have not yet been standardized, different methodologies may have different results. 4. Clinical trials have shown that the combination of lamivudine and zidovudine can reduce HIV viral load and increase CD4 cell counts. Data from terminal clinical trials indicate that the use of lamivudine alone or in combination with zidovudine, or when zidovudine is included in the treatment regimen, significantly reduces the risk of disease progression and death. Zidovudine-resistant strains can become zidovudine-susceptible strains while acquiring lamivudine resistance. In addition, in vitro studies have demonstrated that the combination of the two drugs can delay the emergence of zidovudine-resistant strains. Clinical isolates of HIV virus that have been treated with lamivudine and zidovudine, respectively, have been shown to become less sensitive in vitro to nucleoside analogs to which they have been exposed. However, in vitro studies have also demonstrated that zidovudine-resistant isolates can become zidovudine-susceptible strains while simultaneously acquiring lamivudine resistance. Furthermore, clinical observations have demonstrated that in vivo studies of patients who have never been treated with antiretroviral drugs can delay the development of zidovudine resistance by combining lamivudine and zidovudine. 5. There is no synergistic toxic effect when lamivudine and zidovudine are used together. The clinically relevant toxic reactions of the combination of the two are anemia, low neutrophils and leukopenia. 6. Mutagenicity: In bacterial experiments, lamivudine and zidovudine have no mutagenic effect. However, in mammalian in vitro experiments, such as mouse lymphoma experiments, they are as active as other nucleoside analogs. In vivo studies have shown that lamivudine has no genetic toxicity when the blood concentration reaches 40-50 times the clinical blood concentration. In vitro mutagenicity cannot be confirmed in in vivo experiments, so there is no risk of genetic toxicity when receiving lamivudine for treatment. Zidovudine's induction of chromosomes was observed in the micronucleus test of mice with multiple oral doses of zidovudine. After AIDS patients were treated with zidovudine, many chromosome fragments were also seen in the peripheral blood lymphocytes. The clinical significance of the above findings is still unclear. 7. Carcinogenicity: In long-term oral carcinogenicity tests in rats and mice, no carcinogenicity of lamivudine was found. In oral carcinogenicity studies of zidovudine in mice and rats, late-stage vaginal epithelial cancers were observed, but no other zidovudine-related tumors were observed in either sex of the two species. Subsequent intravaginal carcinogenicity studies confirmed that the occurrence of vaginal cancer was caused by long-term local exposure of the vaginal epithelial of rodents to high concentrations of zidovudine that were not metabolized in the urine. It is not certain whether the above predictions of the carcinogenicity of zidovudine in rodents are meaningful for humans, and it is not clear whether the above findings have clinical significance. In addition, two transplacental carcinogenicity studies were conducted in mice. In one of the studies conducted by the National Cancer Institute of the United States, pregnant mice were given the maximum tolerated dose of zidovudine from day 12 to day 18 of pregnancy. One year after birth, the incidence of tumors in the lungs, livers, and reproductive organs of female mice that had been exposed to the highest dose group (420 mg/kg body weight) increased. In the second study, zidovudine was given continuously for 24 months from day 10 of pregnancy at a dose of 40 mg/kg. Treatment-related findings were limited to late-stage vaginal epithelial tumors, with an incidence and timing similar to those observed in the standard oral dose carcinogenicity study. Thus, the second study showed that zidovudine is not a transplacental carcinogen. It can be concluded that the transplacental carcinogenicity data in the first study represent a hypothetical risk and that the use of zidovudine in pregnant women infected with HIV reduces the risk of mother-to-child transmission of HIV to uninfected children. 8. Reproductive toxicity: In animal reproduction studies, both lamivudine and zidovudine cross the placenta, as has been demonstrated in human studies. At relatively low systemic drug exposures, lamivudine increased early embryonic lethality in rabbits, consistent with human findings. However, this was not the case in rat studies at very high systemic drug exposures. Zidovudine had similar effects in both species, but only at very high systemic drug exposures. Lamivudine was not teratogenic in animal studies. Obstetrically toxic doses given to rats during organogenesis resulted in an increased incidence of malformations, but no evidence of fetal malformations was observed at low doses. 9. Fertility: Lamivudine and zidovudine did not impair male and female fertility in rat studies.

The main ingredient is lamivudine.

This product is a white to off-white capsule-shaped film-coated tablet with GXFC3 printed on one side.

It is suitable for HIV-infected adults and children over 12 years old who have progressive immunodeficiency. This product can reduce the viral load of HIV-1 and increase the number of CD4 cells.

Adults and children over 12 years old: The recommended dose is 1 tablet twice a day, with or without food. If the dose of this drug needs to be reduced clinically, or one of the ingredients in this drug (lamivudine or zidovudine) needs to be reduced or discontinued, use separate tablets/capsules and oral solutions of lamivudine (Epivir) and zidovudine (Retrovir).

1. In the treatment of HIV infection, side effects of lamivudine and zidovudine alone or in combination have been reported, most of which are still unclear. These side effects may be related to lamivudine, zidovudine, or the use of a large number of drugs in the treatment of HIV infection, or they may be caused by underlying disease progression. 2. Because this drug contains lamivudine and zidovudine, the type and severity of adverse reactions are expected to be related to the two components it contains. Routine combined use of lamivudine and zidovudine has not been found to increase toxicity significantly. 3. Lamivudine: Its common side effects include headache, malaise, fatigue, nausea, diarrhea, vomiting, upper abdominal pain, fever and rash. There have been reports of pancreatitis and peripheral neuropathy (or paresthesia), but these have not been found to be related to the dose of lamivudine.

Patients with known allergies to lamivudine, zidovudine, or any excipients in the formulation should not use this drug. Zidovudine is contraindicated in patients with neutrophil counts of 0.75x109/L or hemoglobin levels of 7.5g/dL or (4.65mmol/L), so this drug should also be contraindicated in such patients. There is not much data on the use of lamivudine in children, so lamivudine is contraindicated in children under 12 years of age.

Precautions for children: This product is contraindicated for children under 12 years old, because the dosage of the drug cannot be accurately reduced according to the weight of the child. Precautions for pregnancy and lactation: 1. Animal reproduction studies have shown that both lamivudine and zidovudine can pass the placenta and increase early fetal death. Lamivudine can cause an increase in the silk screen of early rabbit embryos, while zidovudine has an effect on rats and rabbits. Lamivudine is not teratogenic in animal experiments. Zidovudine given to rats during organ formation increases the incidence of teratogenesis, while low doses have been found to produce teratogenesis. Animal reproduction experiments cannot fully predict human reactions, so it is recommended not to take this drug in the first 3 months of pregnancy unless the benefits of treatment to the mother outweigh the risks to the fetus. Zidovudine can reduce the chance of mother-to-child transmission of HIV when used in pregnant women and newborns. However, there is no such data available for lamivudine, and the safety of using lamivudine during human pregnancy has not yet been confirmed. In short, during pregnancy, this drug can only be considered when the expected benefits of the drug outweigh the possible risks. Based on the carcinogenic effects and mutations found in animal experiments, the risk of carcinogenicity of this drug to humans cannot be ruled out. It is uncertain whether the results of the carcinogenicity study of zidovudine in rodents can be applied to humans, but late vaginal tumors have been found in rodents taking zidovudine for life (occurring after 19 consecutive months of daily oral doses of zidovudine). The relevance of these findings to infants infected and uninfected with HIV treated with zidovudine is unclear. However, these findings should be informed to pregnant women who are considering using this drug. In studies of female and male rats, no effects of lamivudine and zidovudine on fertility were found. There is currently no information on the effects of drugs on female fertility, and no effects of zidovudine on the number, morphology and motility of male sperm have been found. 2. Lactation: Lamivudine and zidovudine were found in the milk of lactating rats treated orally. It is not clear whether the same is true in human milk. Given the possibility that these drugs are secreted into the milk, mothers taking this drug are advised not to breastfeed their newborns. Elderly precautions: No specific data are available for this age group, but special attention is recommended for this group of patients because of changes that occur with age, such as decreased renal function and changes in hematological parameters.

1. Since this drug contains lamivudine and zidovudine, all interactions that can occur with these two drugs can also occur with Shuangtaizhi. Since lamivudine has limited metabolism and limited plasma protein binding, and is completely excreted by the kidneys, it is unlikely to interact with other drugs. Zidovudine is similar to it, and is also limited in plasma protein binding, but it is mainly excreted in the liver after being combined into an inactive glucuronidated metabolite. The drug interactions listed below are not complete, and they only represent the types of drugs that should be paid attention to when using. 1. Interactions related to lamivudine: TMP is a component of co-trimoxazole, which can increase the effective concentration of lamivudine at a therapeutic dose by 40%. Unless the patient has renal impairment, there is generally no need to adjust the dose (see Dosage and Administration). Lamivudine does not affect the pharmacokinetics of co-trimoxazole. When co-trimoxazole and lamivudine are used to treat patients with renal impairment, it should be considered with caution. At present, when lamivudine is used in combination with other drugs, the interactions between them should be considered, especially some drugs that are mainly cleared by the kidneys. 2. Interactions with zidovudine: The combined use of zidovudine and lamivudine can increase the effect of zidovudine by 13% and the peak plasma level by 28%. This has no effect on the safety of patients, so there is no need to adjust its dosage. Zidovudine has no effect on the pharmacokinetics of lamivudine. There are reports showing that the blood concentration of phenytoin in some patients is reduced when receiving combined treatment with zidovudine and phenytoin. However, there was one case in which the blood concentration of phenytoin increased. These findings suggest that the level of phenytoin should be closely monitored for patients receiving combined treatment with this drug and phenytoin. In placebo-controlled trials of paracetamol combined with zidovudine, especially when used for a long time, the incidence of neutropenia is increased. However, the pharmacokinetic data obtained show that this dose of paracetamol does not increase the plasma concentration of zidovudine and its glucuronic acid metabolites. 3. Other drugs, including aspirin, codeine, morphine, indomethacin, ketoprofen, naproxen, oxazepam, cimetidine, clofibrate, dapsone and isoprinosine and other drugs can change the metabolism of zidovudine by competitively inhibiting glucuronidation or directly inhibiting liver microsomal metabolism. Before these drugs are used in combination with this drug, especially for long-term treatment, the possibility of drug interaction should be considered. 4. Combined treatment, especially in acute treatment, if the medication contains drugs that may cause nephrotoxicity or bone marrow suppression (such as systemic pentamidine, dapsone, pyrimethamine, co-trimoxazole, amphotericin B, flucytosine, guanidine, interferon, vincristine, vinblastine and doxorubicin), it may also increase the risk of interaction with zidovudine. If it is necessary to use this drug in combination with these drugs, special attention should be paid to monitoring the patient's renal function and blood changes. If necessary, the dose of one or more of the drugs should be reduced. 5. In in vitro tests, since the nucleoside drug ribavirin antagonizes the antiviral activity of zidovudine, the combination of the two should be avoided. Some patients treated with this drug may continue to have opportunistic infections, so it is advisable to use antimicrobial drugs for prevention at the same time. Preventive drugs include co-trimoxazole, pentamidine aerosol, pyrimethamine and acyclovir. A few clinical trials have shown that these drugs do not increase side effects when used in combination with zidovudine. Limited data suggest that propanesulfonic acid reduces glucuronidation and reduces the excretion of glucuronic acid compounds (which may also be zidovudine) by the kidneys, thereby prolonging the half-life of zidovudine and expanding the area under the drug-time curve.

Store below 30°C.

Each tablet contains 150 mg of lamivudine and 300 mg of zidovudine

24 months