Clarithromycin extended-release tablets

Clarithromycin belongs to the class of semisynthetic macrolide antibiotics. Clarithromycin can bind to the bacterial ribosome 5OS subunit, thereby inhibiting its protein synthesis and producing an antibacterial effect. In vitro, it has good antibacterial activity against both standard strains and clinical isolates, and has good antibacterial effects against a variety of aerobic and anaerobic Gram-positive or Gram-negative bacteria. Generally, the minimum inhibitory concentration (MIC) of clarithromycin is the logarithmic dilution of the minimum inhibitory concentration of erythromycin. The results of in vitro pharmacodynamic studies have shown that clarithromycin can inhibit Legionella pneumophila and Mycoplasma pneumoniae, and kill Helicobacter pylori, and its activity under neutral conditions is stronger than that under acidic conditions. In vitro and in vivo data show that it has a significant clinical effect on mycobacteria. In vivo data show that Enterobacter, Pseudomonas and other non-lactose metabolizing Gram-negative bacteria are not sensitive to clarithromycin. In vitro pharmacodynamic studies and clinical observations have confirmed that clarithromycin has antibacterial activity against the following bacteria and is effective against infections caused by them: Gram-positive bacteria: Staphylococcus aureus, Streptococcus pneumoniae, Streptococcus pyogenes, and Listeria monocytogenes. Gram-negative bacteria: Haemophilus influenzae, Haemophilus parainfluenzae, Moraxella catarrhalis, Neisseria gonorrhoeae, Legionella pneumophila. Others: Mycoplasma pneumoniae, Chlamydia pneumoniae. Mycobacterium: Mycobacterium leprae, Mycobacterium kansasii, Mycobacterium chelonae, Mycobacterium fortuitum, Mycobacterium avium, and Mycobacterium intracellulare. The production of beta-lactamase does not affect the activity of clarithromycin. Note: Most strains resistant to penicillin I and II are resistant to clarithromycin. Helicobacter pylori: Helicobacter pylori. 104 patients were isolated and cultured before treatment and were treated with clarithromycin at the MIC level. Among them, 4 had resistant strains, 2 had moderately susceptible strains, and 98 had susceptible strains. In vitro pharmacodynamic studies have confirmed that clarithromycin has antibacterial activity against the following bacteria, but due to the lack of sufficient clinical trials, its safety and effectiveness in the treatment of clinical infections remain to be determined: Aerobic Gram-positive bacteria: Streptococcus agalactiae, Streptococcus (C, F, G groups), Streptococcus viridans. Aerobic Gram-negative bacteria: Bordetella pertussis, Pasteurella multiflora. Anaerobic Gram-positive bacteria: Clostridium, Pseudomonas niger, Propionibacterium acnes. Anaerobic Gram-negative bacteria: Bacteroides melanogaster. Spirochete: Borrelia burgdorferi, Treponema pallidum. Campylobacter: Campylobacter jejuni. Clarithromycin is mainly metabolized to biologically active 14-OH clarithromycin in humans and other primates. The activity of the metabolite against most microorganisms is the same as that of clarithromycin or only 1/2 or 1/4 of that of clarithromycin, but the activity against Haemophilus parainfluenzae is twice that of clarithromycin. In vitro or in vivo, clarithromycin and 14-OH clarithromycin have additive or synergistic effects on different strains of Haemophilus influenzae. In multiple animal infection models, it was found that clarithromycin is 2-10 times more active than erythromycin. For example, in systemic infection in mice, subcutaneous abscesses in mice, and respiratory tract infections in mice caused by Streptococcus, Staphylococcus aureus, Streptococcus pyogenes, and Haemophilus influenzae, clarithromycin is more active than erythromycin, and is more significant in Legionella infection in guinea pigs, that is, clarithromycin administered intraperitoneally at a dose of 1.6 mg/kg/day is more effective than erythromycin at a dose of 50 mg/kg/day.

The main ingredient is clarithromycin.

This product is a yellow film-coated tablet, which appears white or off-white after removing the coating.

Clarithromycin sustained-release tablets are indicated for infections caused by microorganisms that are sensitive to clarithromycin: 1. Lower respiratory tract infections: such as bronchitis, pneumonia, etc.; 2. Upper respiratory tract infections: such as pharyngitis, sinusitis, etc.; 3. Mild to moderate infections of the skin and soft tissues: such as folliculitis, cellulitis, erysipelas, etc.

Oral administration, the commonly recommended adult dose is one tablet (0.5g) once a day. Take with meals. Do not crush or chew clarithromycin extended-release tablets. Children over 12 years old, same as adults. Children under 12 years old, please use other appropriate dosage forms. In more serious infections, the dose can be increased to once a day, 2 tablets (1g) each time. The treatment cycle is usually 7-14 days. Clarithromycin extended-release tablets are contraindicated in patients with severe renal impairment (creatinine clearance < 30ml/min). Clarithromycin tablets may be used in this patient group. Patients with moderate renal impairment (creatinine clearance 30-60ml/min) should reduce the dose by 50%, and the maximum dose is 1 tablet (0.5g) of clarithromycin extended-release tablet per day.

Clarithromycin is well tolerated. Transient central nervous system side effects that have been reported include: dizziness, lightheadedness, anxiety, insomnia, nightmares, tinnitus, confusion, disorientation, hallucinations, mental disorders, and personality disorders. A patient with a history of bipolar disorder developed changes in mental status, paranoid behavior, hypokalemia, and hypoxemia after taking 8g of clarithromycin. Changes in the sense of smell have also been reported, usually associated with taste inversion. Cases of hearing loss after medication have been reported, which recovered after discontinuation of the drug. Other side effects include: headache, arthralgia, myalgia, and allergic reactions, ranging from urticaria, mild rash, and angioedema to anaphylaxis and rarely Stevens-Johnson syndrome/toxic skin necrolysis. As with other macrolides, rare reports of

It is contraindicated for patients who are allergic to macrolide antibiotics. Since the dose of clarithromycin extended-release tablets cannot be reduced to less than 0.5g per day, it is contraindicated for patients with a creatinine clearance of less than 30ml/min. Clarithromycin is contraindicated for use with the following drugs: astemizole, cisapride, pimozide, and terfenadine.

Precautions for children: Children over 12 years old are the same as adults. For children under 12 years old, please use other suitable dosage forms. Precautions for pregnancy and lactation: The safety of clarithromycin for pregnant and lactating women has not been fully clarified. Pregnant women should use clarithromycin with caution, especially in the first 3 months of pregnancy. Clarithromycin can be excreted from breast milk. Precautions for the elderly: The researchers conducted a trial to evaluate and compare the safety and pharmacokinetics of 0.5g clarithromycin tablets after multiple oral administration of 0.5g in healthy elderly male and female subjects and healthy young adult male subjects. Compared with the young group, the circulating plasma concentrations of the parent drug and 14-hydroxy metabolites in the elderly group were higher and eliminated more slowly. However, when renal clearance was correlated with creatinine clearance, there was no difference between the two groups. It can be seen that the in vivo disposition of clarithromycin is related to renal function, but not to age.

Interaction with cytochrome P450 Data indicate that clarithromycin is metabolized primarily by the hepatic cytochrome P4503A (CYP3A) isozyme, which is an important mechanism for many drug interactions. Under this mechanism, the metabolism of other drugs used concomitantly with clarithromycin is inhibited, resulting in increased drug concentrations in serum. The following drugs or classes of drugs are known or suspected to be metabolized by the same CYP3A isozyme: alprazolam, astemizole, carbamazepine, cilostazol, cisapride, cyclosporine, disopyramide, ergot alkaloids, lovastatin, methylprednisolone, midazolam, omeprazole, oral anticoagulants (e.g., warfarin), pimozide, quinidine, levofloxacin, sildenafil, simvastatin, tacrolimus, terfenadine, triazolam, and vinblastine. Other drugs that interact with other isozymes in the cytochrome P450 system by similar mechanisms include phenytoin, theophylline, and valproate. Clinical studies have shown that when theophylline or carbamazepine is used in combination with clarithromycin, its circulating concentration increases slightly but statistically significantly (Ple; 0.05). There are rare reports of rhabdomyolysis when clarithromycin is used in combination with HMG-CoA reductase inhibitors (such as lovastatin and simvastatin). The combination of cisapride and clarithromycin will increase the patient's cisapride blood concentration, leading to Q-T interval prolongation and arrhythmias such as ventricular tachycardia, ventricular fibrillation and peak torsades de pointes. The combination of clarithromycin and pimozide will also have this effect (see [Contraindications]). Macrolide drugs can change the metabolism of terfenadine and increase its blood concentration, which is sometimes accompanied by arrhythmias such as Q-T interval prolongation, ventricular tachycardia, ventricular fibrillation and peak torsades de pointes (see [Contraindications]). In a study of 14 healthy subjects, co-administration of clarithromycin with terfenadine resulted in a 2- to 3-fold increase in the plasma concentration of the acid metabolite of terfenadine, leading to a prolongation of the Q-T interval, but without any clinical symptoms. Similar reactions have been observed when astemizole is co-administered with other macrolides. There have been post-marketing reports of torsional peaks when clarithromycin is co-administered with quinidine or disopyramide. The plasma concentrations of these drugs should be monitored during treatment with clarithromycin. Interactions with Other Drugs Co-administration of clarithromycin with digoxin can result in an increase in the plasma concentration of digoxin, so blood concentration monitoring should be considered. Interactions with Antiretroviral Drugs Concomitant oral administration of clarithromycin tablets with zidovudine in HIV-infected adults may result in a decrease in the steady-state plasma concentration of zidovudine. This is because clarithromycin appears to interfere with the absorption of co-administered oral zidovudine. To date, no such interactions have been reported in HIV-infected pediatric patients. Similar interaction studies of clarithromycin extended-release tablets with zidovudine have not been conducted. Pharmacokinetic studies have shown that the combined use of ritonavir (0.2g, once every 8 hours) and clarithromycin (0.5g, once every 12 hours) will lead to significant inhibition of clarithromycin metabolites, with Cmax, Cmin and AUC of clarithromycin increased by 31%, 182% and 77% respectively, and the formation of 14-(R) hydroxyclarithromycin was significantly inhibited. Due to the large therapeutic window of clarithromycin, when the patient's renal function is normal, there is no need to reduce the dose, but for patients with renal impairment, the dose should be adjusted as follows: for patients with ClCR of 30-60ml/min, the clarithromycin dose is reduced by 50%, that is, the maximum dose is 1 clarithromycin sustained-release tablet per day. Patients with severe renal impairment (ClCR less than 30ml/min) should not use clarithromycin sustained-release tablets because this product cannot be reduced in dose. Clarithromycin tablets can be used in this population. When the daily dose of clarithromycin is greater than 1g, it should not be used in combination with ritonavir.

Store in a dry place at room temperature (10-30°C).

0.5g

Tentatively 24 months.

Jiangsu Hengrui Pharmaceuticals Co., Ltd.

• Founded in:

  1997-04-28

• Address:

  No. 38 Huanghe Road, Lianyungang Economic and Technological Development Zone

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  9132070070404786XB

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  6,379,002,274 yuan

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