Product Overview
[Drug Name]
Generic Name: Rifapentine Capsules
Trade Name: Shanjiang
English Name: Rifapentin Capsules
Chinese Pinyin: LifupendingJiaonang
[Ingredients]
The main ingredient of this product is rifapentine, whose chemical name is 3-[[(4-cyclopentyl-1-piperazinyl)imino]methyl]-rifamycin. Chemical Structure: Molecular Formula: C47H64N4O12 Molecular Weight: 877.04
[Properties]
This product is a capsule.
[Indications]
1. This product is used in combination with other anti-tuberculosis drugs for the initial and retreatment treatment of various tuberculosis conditions, but is not suitable for the treatment of tuberculous meningitis.
2. It is suitable for short-term chemotherapy under direct medical observation.
3. It can also be used to treat non-tuberculous mycobacterial infections.
4. It may be effective in combination with other anti-leprosy drugs for the treatment of leprosy.
[Dosage and Administration]
Oral, anti-tuberculosis. Adults: 0.6g (reduced dosage for those weighing <55kg), once daily, on an empty stomach (one hour before meals) with water; take 1-2 times a week. It should be used in combination with other anti-tuberculosis drugs. The typical course of treatment for initial pulmonary tuberculosis is 6-9 months.
[Adverse Reactions]
Adverse reactions are milder than those of rifampin. In a few cases, leukopenia and thrombocytopenia; elevated alanine aminotransferase; rash, dizziness, and insomnia may occur. Gastrointestinal reactions are rare. No flu-like symptoms, immune thrombocytopenia, or anaphylactic shock-like reactions have been observed with this drug. If these adverse reactions occur, discontinue the drug immediately.
[Contraindications]
1. This drug is contraindicated in patients with allergies to this drug or rifamycins.
2. This drug is contraindicated in patients with severe hepatic insufficiency, biliary obstruction, or pregnant women.
[Precautions]
1. This drug has cross-sensitivity reactions with other rifamycins. 2. Use with caution in patients with alcoholism or impaired liver function. Patients with impaired liver function must be closely monitored for changes in liver function.
3. Patients who develop leukopenia and thrombocytopenia after taking this product should avoid surgical procedures such as tooth extraction and maintain good oral hygiene, flossing with caution until blood counts return to normal.
4. Interference with Diagnosis: May cause a positive direct antiglobulin test (Coombs test); interfere with the determination of serum folate and vitamin B12 concentrations; may cause a false positive in the sodium sulfonamide retention test; may interfere with the results of various urinalysis tests performed using a spectrophotometer or color changes; and may increase the results of blood urea nitrogen, serum alkaline phosphatase, serum alanine aminotransferase, aspartate aminotransferase, serum bilirubin, and serum uric acid concentrations.
5. During the use of this product, changes in blood counts and liver function should be frequently monitored.
6. This product should not be used again if a patient has experienced an allergic reaction due to circulating antibodies after intermittent rifampicin use, such as hypotension or shock, acute hemolytic anemia, thrombocytopenia, or acute interstitial tubulonephritis.
7. This product should be taken with water on an empty stomach (one hour before meals); internationally, it is recommended to take this product after a high-fat and low-carbohydrate breakfast to improve bioavailability. If gastrointestinal irritation symptoms occur after taking rifampicin, this product can be taken instead.
8. This product may rapidly develop bacterial resistance when used alone to treat tuberculosis, and must be combined with other anti-TB drugs.
9. After taking this product, urine, feces, saliva, sputum, and tears may appear orange-red.
[Use in Special Populations]
Precautions for Children:
The safety of this product in children under 5 years of age has not been established.
Precautions for Pregnancy and Lactation:
This product is contraindicated in pregnant women. This product is excreted in breast milk. Lactating women should carefully weigh the risks and benefits before taking this product. If this product is necessary, breastfeeding should be discontinued.
Precautions for the Elderly:
Elderly patients may have decreased liver function, so the dosage should be reduced as appropriate.
[Drug Interactions]
1. Daily alcohol consumption while taking this product may increase its hepatotoxicity. Therefore, alcohol should be abstained from while taking this product.
2. Para-aminosalicylates may affect the absorption of this product, resulting in decreased blood concentrations. If coadministration is necessary, the two drugs should be taken at least 6 hours apart.
3. Phenobarbital drugs may affect the absorption of this product and should not be taken concomitantly with this product.
4. Concomitant use of this product with oral anticoagulants may reduce the anticoagulant effect of the latter. Caution should be exercised.
5. Concomitant use of this product with isoniazid may increase the risk of hepatotoxicity, especially in patients with pre-existing liver impairment and those with rapid acetylation of isoniazid.
6. Concomitant use of this product with ethionamide may aggravate its adverse reactions.
7. Concomitant use of antacids can significantly reduce the bioavailability of this product.
8. Concomitant use of adrenocortical hormones (glucocorticoids, mineralocorticoids), aminophylline, theophylline, chloramphenicol, clofibrate, cyclosporine, verapamil (Isapamil), tocainide, propafenone, trimethoprim, coumarin or indandione derivatives, oral hypoglycemic agents, corticotropin, dapsone, digitalis glycosides, disopyramide, quinidine, etc. with this product can reduce the efficacy of these drugs due to the latter inducing hepatic microsomal enzyme activity. Therefore, with the exception of digoxin and dapsone, the dosage of these drugs should be adjusted before and during treatment with this product. When used concomitantly with coumarins or indandiones, the prothrombin time should be measured daily or periodically and the dosage adjusted accordingly.
9. This product can induce hepatic microsomal enzymes, increasing the metabolism of the anti-tumor drugs dacarbazine and cyclophosphamide, forming alkylated metabolites, which can promote leukopenia, thus requiring dosage adjustment.
10. Co-administration with diazepam (Valium) may increase the latter's elimination, resulting in a decrease in its blood concentration, necessitating dosage adjustment.
11. This product may increase the metabolism of phenytoin in the liver, so phenytoin blood concentrations should be measured and dosage adjusted when the two are used together.
12. This product may increase the degradation of levothyroxine in the liver, so the levothyroxine dose should be increased when the two are used together.
13. This product may also increase the metabolism of methadone and mexiletine in the liver, causing methadone withdrawal symptoms and a decrease in mexiletine blood concentrations, so the latter two require dosage adjustment when used together.
14. Probenecid may compete with this product for uptake by hepatocytes, increasing its blood concentration and producing toxic reactions. However, this effect is unstable, so adding probenecid to increase this product's blood concentration is generally not advisable.
15. Chlorophenazine may reduce this product's absorption, delaying peak time and prolonging its half-life.
16. Combination with miconazole or ketoconazole can reduce the blood concentrations of the latter drugs. Therefore, this drug should not be used in combination with imidazoles.
[Pharmacological Actions]
Rifapentine is a semisynthetic broad-spectrum bactericidal agent with strong in vitro antibacterial activity against Mycobacterium tuberculosis, with a minimum inhibitory concentration (MIC) of 0.12-0.25 mg/L, 2-10 times more potent than rifampin. It also demonstrates superior anti-TB activity in mice. Mycobacterium leprae and other mycobacteria, such as Mycobacterium kansasii and Mycobacterium xenopus, are also susceptible to this drug, but Mycobacterium avium is resistant. Furthermore, this drug exhibits high antibacterial activity against most Gram-positive cocci, with an MIC of 0.025 mg/L. Its activity against Gram-negative bacteria is poor. Its activity against Chlamydia spp. is similar to that of erythromycin and doxycycline, but weaker than that of rifampin. It is also less effective against methicillin-resistant Staphylococci. In vitro testing has shown that Chlamydia, Staphylococcus aureus, and Neisseria gonorrhoeae can develop resistance to this drug. Combining it with doxycycline, it exhibits synergistic effects against Neisseria gonorrhoeae. Combining it with isoniazid, it is far more effective against Mycobacterium tuberculosis than the combined effect of rifampicin and isoniazid. Its mechanism of action is similar to that of rifampicin: it binds firmly to subunits of DNA-dependent RNA polymerase, inhibiting bacterial RNA synthesis and preventing the enzyme from ligating to DNA, thereby blocking RNA transcription and halting DNA and protein synthesis. Animal studies have demonstrated that this drug has some hepatotoxicity and fetal teratogenicity.
[Storage]
Keep in a dark, sealed container.
[Specifications]
0.15g
[Packaging]
0.15g x 20s
[Expiry Date]
24 months
[Approval Number]
National Medicine Standard H10940211
[Manufacturer]
Sichuan Changzheng Pharmaceutical Co., Ltd.
