Rifapentine Capsules
Function and Efficacy
Rifapentine is a semi-synthetic broad-spectrum bactericidal agent with strong antibacterial activity against Mycobacterium tuberculosis in vitro, with a minimum inhibitory concentration (MIC) of 0.12-0.25 mg/L, 2-10 times stronger than rifampicin; its anti-tuberculosis infection effect in mice is also better than rifampicin. Mycobacterium leprae and other mycobacteria such as Mycobacterium kansasii and Mycobacterium toad are also sensitive to this product, but Mycobacterium avium is resistant. In addition, this product has high antibacterial activity against most Gram-positive cocci, with a MIC of 0.025 mg/L; it has poor effect on Gram-negative bacteria. Its effect on Chlamydia is similar to that of erythromycin and doxycycline, but worse than rifampicin; it has poor effect on methicillin-resistant Staphylococcus. According to in vitro test results, Chlamydia, Staphylococcus aureus and Neisseria gonorrhoeae will develop resistance to this product. Combined with doxycycline, it has a synergistic effect on Neisseria gonorrhoeae; combined with isoniazid, its effect on tuberculosis bacteria far exceeds that of rifampicin and isoniazid combined. Its mechanism of action is the same as that of rifampicin, which is to firmly bind to the subunits of DNA-dependent RNA polymerase, inhibit the synthesis of bacterial RNA, prevent the enzyme from connecting to DNA, thereby blocking the RNA transcription process and stopping the synthesis of DNA and protein. Animal experiments have shown that this product has certain liver toxicity and teratogenic effects on the fetus.
Ingredients
The main ingredient of this product is rifapentine, whose chemical name is 3-[[(4-cyclopentyl-1-piperazinyl)imino]methyl]-rifamycin. Molecular formula: C47H64N4O12, molecular weight: 877.04.
| Name | Description | Content | CAS NO. | Manufacturer |
|---|---|---|---|---|
| RifapentineIngredients |
It is a semi-synthetic broad-spectrum bactericidal agent. It has strong antibacterial activity against Mycobacterium tuberculosis in vitro, with a minimum inhibitory concentration (MIC) of 0.12-0.25 mg/L, which is 2-10 times stronger than rifampicin; its anti-tuberculosis infection effect in mice is also better than rifampicin. Mycobacterium leprae and other mycobacteria such as Mycobacterium kansasii and Mycobacterium toad are also sensitive to this product, but Mycobacterium avium is resistant. In addition, this product has high antibacterial activity against most Gram-positive cocci, with a MIC of 0.025 mg/L; it has poor effect on Gram-negative bacteria. Its effect on Chlamydia is similar to that of erythromycin and doxycycline, which is worse than rifampicin; it has poor effect on methicillin-resistant Staphylococcus. According to the results of in vitro tests, Chlamydia, Staphylococcus aureus and Neisseria gonorrhoeae will develop resistance to this product. Combined with doxycycline, it has a synergistic effect on Neisseria gonorrhoeae; combined with isoniazid, its effect on Mycobacterium tuberculosis far exceeds that of rifampicin and isoniazid. Its mechanism of action is the same as that of rifampicin, which is to firmly bind to the subunit of DNA-dependent RNA polymerase, inhibit the synthesis of bacterial RNA, prevent the enzyme from connecting to DNA, thereby blocking the RNA transcription process and stopping the synthesis of DNA and protein. Animal experiments have shown that this product has certain liver toxicity and teratogenic effects on the fetus. More |
61379-65-5 | 5 |
Appearance
This product is in the form of capsules.
Indication
1. This product is used in combination with other anti-tuberculosis drugs for the initial and retreatment treatment of various tuberculosis, but it is not suitable for the treatment of tuberculous meningitis. 2. It is suitable for short-term chemotherapy under direct observation by medical staff. 3. It can also be used for the treatment of non-tuberculous mycobacterial infections. 4. It may be effective in the treatment of leprosy in combination with other anti-leprosy drugs;
Usage and Dosage
Oral, anti-tuberculosis. Adults take 0.6g at a time (those weighing less than 55kg should take less), once a day, on an empty stomach (1 hour before meals) with water; take 1-2 times a week. It needs to be used in combination with other anti-tuberculosis drugs. The treatment course for initial pulmonary tuberculosis patients is generally 6-9 months.
Adverse Reactions
The adverse reactions of this product are milder than those of rifampicin. In a few cases, leukopenia and thrombocytopenia, elevated alanine aminotransferase, rash, dizziness, insomnia, etc. are seen. Gastrointestinal reactions are rare. No influenza syndrome, immune thrombocytopenia, or anaphylactic shock-like reactions were found in the use of this product. If such adverse reactions occur, the drug must be discontinued immediately.
Precautions
1. Patients who are allergic to this product or rifamycin antibiotics are contraindicated. 2. Patients with severe liver dysfunction, biliary obstruction and pregnant women are contraindicated.
Special Population Medication
Precautions for children: The safety of this product in children under 5 years old has not been determined. Precautions for pregnancy and lactation: Pregnant women are prohibited from using this product. This product can be excreted through breast milk. Lactating women should fully weigh the pros and cons before deciding whether to use the drug. If this product is needed, breastfeeding should be suspended. Precautions for the elderly: Elderly patients have decreased liver function, and the dosage should be reduced as appropriate.
Drug Interactions
1 Drinking alcohol every day while taking this product may increase the hepatotoxicity of this product, so you should abstain from alcohol while taking this product. 2 Para-aminosalicylate may affect the absorption of this product, resulting in a decrease in its blood concentration; if it must be used together, the interval between taking the two should be at least 6 hours. 3 Phenobarbital drugs may affect the absorption of this product, so it is not suitable to be taken with this product at the same time. 4 When this product is used simultaneously with oral anticoagulants, the latter's anticoagulant effect will be reduced, so attention should be paid. 5 The combination of this product with isoniazid may increase the risk of hepatotoxicity, especially in patients with existing liver damage and patients with rapid acetylation of isoniazid. 6 The combination of this product with ethionamide may aggravate its adverse reactions. 7 The combination of antacids will significantly reduce the bioavailability of this product. 8. When adrenocortical hormones (glucocorticoids, mineralocorticoids), aminophylline, theophylline, chloramphenicol, clofibrate, cyclosporine, verapamil (Isopamine), tocainide, propafenone, trimethoprim, coumarin or indandione derivatives, oral hypoglycemic drugs, corticotropin, dapsone, digitalis glycosides, disopyramide, quinidine, etc. are used in combination with this product, the latter can induce the activity of liver microsomal enzymes, which can weaken the efficacy of the above drugs. Therefore, except for digoxin and dapsone, the above drugs need to adjust the dosage before and during the treatment of this product. When used in combination with coumarin or indandione, the prothrombin time should be measured daily or regularly to adjust the dosage accordingly. 9. This product can induce liver microsomal enzymes, increase the metabolism of anti-tumor drugs dacarbazine (dacarbazine) and cyclophosphamide, form alkylated metabolites, and promote leukopenia, so the dosage needs to be adjusted. 10 When used in combination with diazepam (Valium), the latter's elimination can be increased, causing its blood concentration to decrease, so the dosage needs to be adjusted. 11 This product can increase the metabolism of phenytoin in the liver, so when the two are used together, the blood concentration of phenytoin should be measured and the dosage adjusted. 12 This product can increase the degradation of levothyroxine in the liver, so the dose of levothyroxine should be increased when the two are used together. 13 This product can also increase the metabolism of methadone and mexiletine in the liver, causing methadone withdrawal symptoms and reduced mexiletine blood concentration, so the latter two need to adjust the dose when used together. 14 Probenecid can compete with this product for uptake by liver cells, increasing the blood concentration of this product and producing toxic reactions. However, this effect is unstable, so it is usually not appropriate to add probenecid to increase the blood concentration of this product. 15 Chlorophenazone can reduce the absorption of this product, delay the peak time and prolong the half-life. 16. When used in combination with miconazole or ketoconazole, the blood concentrations of the latter two drugs may be reduced. Therefore, this product should not be used in combination with imidazoles.
Storage
Keep away from light and store in sealed container.
Packaging Specification
0.15g
Validity Period
24 months
Manufacturer
Sichuan MED-SHINE Pharmaceutical Co., Ltd.
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Founded in:
1998-09-15 -
Address:
No. 1069, Tsingtao Beer Avenue, Chengdu Cross-Strait Science and Technology Industrial Development Park, Wenjiang District, Chengdu -
Tax NO.:
9151011570915754XK -
Registered Funds:
50 million yuan -
Website:
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Email: