is a derivative of erythromycin. It was successfully developed by the Japanese Taisho Corporation in the early 1990s and registered under the trade name Clarith.
Appearance and properties: This product is white or off-white crystalline powder; odorless and bitter. This product is easily soluble in chloroform, soluble in acetone or ethyl acetate, slightly soluble in methanol or ethanol, and insoluble in water.
Clarithromycin mechanism of action
Clarithromycin belongs to the class of macrolide antibiotics. Its mechanism is to inhibit the synthesis of the 50S subunit of the nuclear protein and inhibit protein synthesis to produce bacteriostatic effects. This medicine has an inhibitory effect on Gram-positive bacteria such as Staphylococcus aureus, Streptococcus, and Pneumococcus, and some Gram-negative bacteria such as Haemophilus influenzae, Pertussis, Gonorrhea, Legionella Anaerobic bacteria such as Bacteroides fragilis, Peptostreptococcus, Propionibacterium acnes, etc. also have inhibitory effects. In addition, it has an inhibitory effect on mycoplasma. This medicine is characterized by its antibacterial activity similar to erythromycin in vitro, but its antibacterial activity against some bacteria such as Staphylococcus aureus, streptococcus, Haemophilus influenzae, etc. in vivo is stronger than erythromycin. There is cross-resistance with erythromycin.
Using erythromycin as the raw material, hydrolyze to remove a methyl group on the amino group, and then react with benzyl chloroformate to protect the hydroxyl group and amino group on the 5-position side chain tetrahydropyran ring, and then in dimethyl sulfoxide and Tetrahydrofuran neutralizes the methyl iodide reaction, methylates the hydroxyl group at the 6-position, then catalyzes the hydrogenolysis to remove the protective group, reacts with formaldehyde to hydroxymethylate the amino group, and finally reduces to methyl, which is clarithromycin.
Clarithromycin and its tablets, currently produced dosage forms also include granules, dispersible tablets, sustained-release tablets, injections and dry suspensions.
Mainly used for upper and lower respiratory tract caused by sensitive bacteria, including tonsillitis, pharyngitis, sinusitis, bronchitis, pneumonia, skin, soft tissue infection, pus, erysipelas, folliculitis, wound infection, etc. The cyclic lactones are similar. The product can also be used for genitourinary infections caused by Chlamydia trachomatis or ureaplasma urealyticum, atypical mycobacterial infections of AIDS patients, etc.
Clarithromycin how to take and Clarithromycin dosage
Adults take 250 mg every 12h, the dose of severe patients can be increased to 500 mg every 12h; the course of treatment depends on the degree of infection, usually 7 to 14 days. If the creatinine clearance rate is less than 0.501ml / 1.73 square meters per second, the dose will be halved. Children's dose: 7.5 mg / kg each time, twice a day, the highest dose does not exceed 500 mg per day. Mild: 250 mg each time, 500 mg each time for severe, once every 12 hours, course of treatment 7-14 days. Children over 12 years old are counted as adults. Children under 12 years of age should not use this medicine.
Clarithromycin side effects
Clarithromycin adverse effects
1. There are mainly oral odor, gastrointestinal reactions such as abdominal pain, diarrhea, nausea, vomiting, headache, and serum aminotransferase transiently increased.
2. Allergic reactions may occur. The mild cases are drug eruption and urticaria, and the severe cases are allergy and Stevens-Johnson disease.
3. Occasionally hepatic toxicity, pseudomembranous enteritis caused by Clostridium difficile.
4. There have been reports of transient side effects of the central nervous system, including anxiety, dizziness, insomnia, hallucinations, nightmares or confusion, but the relationship between the cause and the drug is still unclear.
Clarithromycin can interfere with the metabolism of carbamazepine, so that the latter's blood concentration is significantly increased. When the two are used together, the blood concentration should be monitored, and if necessary, the dosage should be adjusted. Combined with theophylline can increase theophylline blood concentration, but generally do not need to adjust the dosage of theophylline. This product can change the blood concentration of the following combined drugs.
The mild cases are drug eruptions and urticaria, and the severe cases are allergies. There have been reports of transient central nervous system side effects, such as anxiety, dizziness, insomnia, hallucinations, nightmares, and confusion.
Allergic to macrolides, pregnant women, nursing women, severe liver and kidney dysfunction, arrhythmia, bradycardia, prolonged QT interval, iron deficiency heart disease, congestive heart failure and water and electrolyte disorders are prohibited or use with caution. The product is mainly metabolized and excreted in the liver, so people with liver insufficiency, severe renal insufficiency, and elderly people over 65 years of age should pay special attention to adverse reactions. Gastrointestinal dysfunction and systemic symptoms may occur when overdose is taken, gastric lavage and supportive therapy may be given. Neither hemodialysis nor peritoneal dialysis can remove the product, so drugs that have not been absorbed (such as gastric lavage) should be excluded as soon as possible and symptomatic treatment should be given. Pregnant women are prohibited (the concentration of this product in animal embryos is 2-17 times that of human serum). Breastfeeding women should be used with caution (feeding should be suspended).
Clarithromycin is a veterinary drug that people often use in bee breeding, but excessive or frequent use will cause the bees themselves and the honey produced by bees to contain residual clarithromycin.
Clarithromycin Rapid Test Dipsticks can quickly detect whether the honey contains residual Clarithromycin. It is not only simple to operate, but also has short detection time and high accuracy, and the test results comply with EU standards.