How to use rifapentine

  Pharmacology: The nature of the antibacterial spectrum is the same as that of rifampicin. It has antibacterial effects on Mycobacterium tuberculosis, Mycobacterium lepra, Staphylococcus aureus, certain viruses, Chlamydia and other microorganisms, and its anti-tuberculosis effect is 2 to 10 times stronger than that of rifampicin. The peak blood concentration is about 16.8μg/ml when the product (fine crystal) is taken once on an empty stomach; it can be maintained at 15.35~16.89μg/ml for 4~12 hours; 5.4μg/ml for 48 hours. There are also considerable concentrations in bone and brain tissues. The product is mainly excreted from the feces in its original form and as metabolites. t1/2 is 18 hours on average. [Rifapentine has high antibacterial activity against Mycobacterium tuberculosis, and the minimum inhibitory concentration (MIC) against human type Mycobacterium tuberculosis (H37Rv) is 0.195-0.39mg/L. Its antibacterial effect is 2-4 times stronger than that of rifampin. The minimum bactericidal concentration (MBC) for multiplying Mycobacterium tuberculosis was 0.195-0.78mg/L. The efficacy on infected tuberculosis mice was 4-6 times higher than that of rifampicin. It also has high antibacterial activity against gram-positive bacteria, and its effect on Chlamydia is better than erythromycin and tetracycline, but not as good as rifampicin; the antibacterial effect on Mycobacterium leprae is stronger, and the bactericidal dose of rifapentine is 1/8 of rifampicin in mice infected with Mycobacterium leprae.The mechanism of action is to inhibit DNA synthesis of bacteria. There is cross-resistance among bacteria to rifamycin antibiotics.  Pharmacokinetics of this product is well absorbed orally. After oral administration of rifapentine 400mg in normal people, the time to reach the bee is 6-12h, and the peak blood concentration can reach 16.9mg/L, and 1.3mg/L can still be measured after 72h. Taking the drug after eating can reduce the absorption of the drug in the stomach and intestines, and make the blood concentration decrease obviously. The plasma protein binding rate of this product is 98%, and the half-reduction period is 30.7h. This product is mainly metabolized in the liver and excreted by the feces through bile, and 13.3% of the dose is excreted in the urine within 72h after taking the drug. It is widely distributed in the body after oral absorption, with the liver being the most abundant, followed by the kidney, lung, tears, saliva and chest and abdominal fluids.  Indications: Mainly used for the treatment of tuberculosis (often in combination with other anti-tuberculosis drugs). Rifapentine is used for the treatment of pulmonary tuberculosis and various extrapulmonary tuberculosis, such as genitourinary tuberculosis, bone and joint tuberculosis and lymphatic tuberculosis. Several units in China have used rifapentine (administered twice a week) in combination with other drugs to treat tuberculosis cases, and have made randomized control with rifampin (administered daily) combination therapy. After 3 years of follow-up, it was concluded that rifapentine administered twice a week had the same treatment results as rifampin administered daily, with fewer adverse effects. In addition, it can also be used for the treatment of leprosy.  Dosage: Adult dose: 600 mg orally once or twice a week on an empty stomach. The duration of treatment and treatment regimen (in combination with other anti-tuberculosis drugs) will depend on the condition.  [Dosage: Capsules: 150mg/capsule, 300mg/capsule.  Contraindications: This product is contraindicated in women with a history of allergy or toxicity to rifamycins and in women within 3 months of pregnancy. Patients with cirrhosis, hepatic insufficiency, chronic alcoholism should use with caution or reduce the dosage appropriately. Regular liver function and blood tests are required for long-term users.  Dosing Instructions: Complete cross-resistance with rifampin. Must be taken on an empty stomach. Cross-allergic reactions with other rifamycins. The bioavailability of the crude crystals is only 1/3-1/4 of that of the fine crystals. Adverse Reactions: Individual cases may cause allergic reactions: rash, drug fever, facial flushing or pallor, shortness of breath, palpitations, chest tightness, abdominal pain, anaphylaxis. Leukopenia and elevated transaminases may also be observed.  The toxicity of this product is mild and easy to be tolerated by patients. Gastrointestinal reactions are not obvious, and asymptomatic transient elevation of transaminases is occasionally seen during the course of treatment. Patients’ urine and stool, saliva, tears and sputum may appear red during the course of drug administration.  Interaction: Bacteria are prone to develop resistance to this product alone, so it should be combined with other anti-tuberculosis drugs or other antibacterial drugs to prevent or delay the development of bacterial resistance.