Azithromycin Tablets

Pharmacological action Azithromycin is an azalide antibiotic. Its mechanism of action is to interfere with the synthesis of proteins (without affecting the synthesis of nucleic acids) by binding to the subunits of the 50S ribosomes of sensitive microorganisms. In vitro tests and clinical studies have shown that azithromycin is effective against the following pathogens: Gram-positive aerobic microorganisms: Staphylococcus aureus, Streptococcus pyogenes, Streptococcus pneumoniae, and hemolytic Streptococci. Azithromycin has cross-resistance to erythromycin-resistant Gram-positive bacteria. Most fecal streptococci (enterococci) and methicillin-resistant Staphylococci are resistant to this product. Gram-negative aerobic microorganisms: Haemophilus influenzae, Moraxella catarrhalis, and Mycoplasma trachomatis. In vitro tests and clinical studies suggest that this product can prevent diseases caused by the avian intracellular mycobacterium complex (composed of avian intracellular mycobacterium and intracellular mycobacterium). This product is ineffective against strains that produce beta-lactamase. In vitro research results have been obtained for the following microorganisms, but their clinical significance is still unclear, including Streptococcus (C, F, G), Streptococcus viridans, Bordetella pertussis, Haemophilus dukei, Legionella pneumophila, Bacteroides, Peptostreptococcus, Borrelia burgdorferi, Chlamydia pneumoniae, Treponema pallidum, Ureaplasma urealyticum, etc. Toxicological studies Genetic toxicity: The results of human lymphocyte test, mouse bone marrow micronucleus test and mouse in vitro lymphoma cell test all confirmed that this product has no mutagenic effect. Reproductive toxicity: Reproductive toxicity tests in rats and mice showed that when the dosage reached the dose level that produced moderate maternal toxicity (i.e. 200 mg/kg/day, calculated by body surface area, about 2 to 4 times the human dosage of 500 mg/kg/day), no teratogenic effect was found. No damage to fertility and fetus has been found. Carcinogenicity: There is no research data on the carcinogenicity of this product in animals for long-term use.

The main ingredient of this product is azithromycin, and its chemical name is: (2R, 3S, 4R, 5R, 8R, 10R, 11R, 12S, 13S, 14R)-13-[(2,6-dideoxy-3-C-methyl-3-O-methyl-α-L-ribo-hexopyranosyl)oxy]-2-ethyl-3,4,10-trihydroxy-3,5,6,8,10,12,14-heptamethyl-11-[[3,4,6-trideoxy-3-(dimethylamino)-β-D-xyl-hexopyranosyl]oxy]-1-oxa-6-azacyclopentadecan-15-one. Chemical structure: Molecular formula: C38H72N2O12 (anhydrous) Molecular weight: 749.00

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

1. Acute pharyngitis and acute tonsillitis caused by Streptococcus pyogenes. 2. Sinusitis, acute otitis media, acute bronchitis, and acute exacerbation of chronic bronchitis caused by sensitive bacteria. 3. Pneumonia caused by Streptococcus pneumoniae, Haemophilus influenzae, and Mycoplasma pneumoniae. 4. Urethritis and cervicitis caused by Chlamydia trachomatis and non-multi-drug resistant Neisseria gonorrhoeae. 5. Skin and soft tissue infections caused by sensitive bacteria.

Oral administration, 1 hour before or 2 hours after meals. Adult dosage: 1. For sexually transmitted diseases caused by Chlamydia trachomatis or sensitive Neisseria gonorrhoeae, only 1.0g of this product needs to be taken orally at a single time. 2. For the treatment of other infections: 0.5g on the first day, 0.25g on the second to fifth day; or 0.5g on the first day for 3 consecutive days. Pediatric dosage: 1. For the treatment of otitis media and pneumonia, 10mg/kg of body weight is taken on the first day (the maximum amount per day does not exceed 0.5g), 5mg/kg of body weight is taken on the second to fifth day (the maximum amount per day does not exceed 0.25g) or the following method of administration: 0.2g on the first day for body weight 15-25 (kg), 0.1g on the second to fifth day. 0.3g on the first day for body weight 26-35 (kg), 0.15g on the second to fifth day. For children weighing 36-45 kg, take 0.4 g at a time on the first day, and 0.2 g at a time on the 2nd to 5th day. 2. For the treatment of pharyngitis and tonsillitis in children, take 12 mg/kg of body weight at a time (maximum daily dose not exceeding 0.5 g) for 5 consecutive days.

This product is generally well tolerated, with a low incidence of adverse reactions, most of which are mild to moderate reversible reactions. (I) Clinical trial experience Because clinical trials are completed under different conditions, the adverse reaction rate of a drug observed in clinical trials cannot be directly compared with the adverse reaction rate of other drugs in clinical trials, and may not reflect the adverse reaction rate in actual application. In clinical trials of intravenous azithromycin for the treatment of community-acquired pneumonia, 2 to 5 doses were administered intravenously, and most of the adverse reactions reported were mild to moderate and recovered after discontinuation of the drug. Most patients in these clinical trials had more than one comorbidity and required the use of other drugs. About 1.2% of patients using intravenous preparations of this product discontinued the drug, and 2.4% of patients treated with intravenous or oral azithromycin discontinued the drug due to adverse reaction symptoms or abnormal laboratory tests. In clinical trials conducted in patients with pelvic inflammatory disease, 2% of female patients receiving azithromycin monotherapy discontinued the drug due to clinical adverse reactions after 1 to 2 doses were administered intravenously, and 4% of patients using azithromycin in combination with metronidazole discontinued treatment due to adverse reactions. In the above studies, the most common adverse reactions leading to discontinuation of the drug were gastrointestinal reactions (abdominal pain, nausea, vomiting, diarrhea, etc.) and rash, and the laboratory abnormalities leading to discontinuation of the drug were mainly elevated aminotransferases and/or alkaline phosphatase. In the study of community-acquired pneumonia, the most common adverse reactions in adult patients treated with intravenous/oral preparations of this product were gastrointestinal reactions, including diarrhea or loose stools (4.3%), nausea (3.9%), abdominal pain (2.7%), and vomiting (1.4%). About 12% of patients experienced adverse reactions related to intravenous injection, the most common of which were injection site pain (6.5%) and local inflammatory reactions (3.1%). In clinical trials of patients with pelvic inflammatory disease, adult female patients received intravenous/oral preparations of this product, and the most common adverse reactions related to treatment were also gastrointestinal reactions, among which diarrhea (8.5%) and nausea (6.6%) were the most common, followed by vaginitis (2.8%), abdominal pain (1.9%), anorexia (1.9%), rash and itching (1.9%). In these studies, a higher proportion of female patients experienced nausea (10.3%), abdominal pain (3.7%), vomiting (2.8%), administration site reactions, stomatitis, dizziness, and dyspnea (total 1.9%) when azithromycin was coadministered with metronidazole. Other adverse reactions caused by the multiple-dose intravenous/oral azithromycin regimen did not exceed 1%. Adverse reactions with an incidence of less than 1% were: Gastrointestinal reactions: dyspepsia, abdominal distension, mucositis, oral candidiasis, and gastritis. Nervous system: headache, somnolence. Allergic reactions: bronchospasm. Special senses: taste perversion. (II) Post-marketing experience The following adverse events have been reported in adults and/or children with oral azithromycin preparations after marketing, but it is not certain whether they were caused by azithromycin: Allergic reactions: arthralgia, edema, urticaria, angioneurotic edema. Cardiovascular: Arrhythmias including ventricular tachycardia, hypotension, rare QT prolongation, and torsade de pointes. Gastrointestinal: Anorexia, constipation, dyspepsia, abdominal distention, vomiting/diarrhea but rarely dehydration, pseudomembranous colitis, pancreatitis, oral candidiasis, pyloric stenosis and, rarely, tongue discoloration. Systemic: Asthenia, paresthesia, fatigue, malaise and anaphylactic shock reactions. Genitourinary: Interstitial nephritis, acute renal failure, vaginitis. Hematopoietic: Thrombocytopenia. Hepatic/biliary: Adverse reactions related to hepatic dysfunction have been reported in post-marketing experience with azithromycin. Nervous: Convulsions, dizziness/vertigo, headache, somnolence, hyperactivity, nervousness, agitation and syncope. Ear and labyrinth disorders: Deafness, tinnitus, hearing loss, vertigo. Psychiatric: Aggressive reactions and anxiety. Skin and appendages: Itching. Rare severe skin reactions include erythema multiforme, Stevens-Johnson syndrome and toxic epidermolytic necrolysis. Special senses: Hearing impairment includes hearing loss, deafness and/or tinnitus, and there have also been reports of abnormal taste/smell and/or loss. Laboratory abnormalities: Significant abnormal laboratory tests seen in clinical trials (regardless of whether they are drug-related) are: Incidence 4% to 6%: Alanine aminotransferase (ALT), aspartate aminotransferase (AST), creatinine increased. Incidence 1% to 3%: Lactate dehydrogenase (LDH), bilirubin increased. Incidence less than 1%: Leukopenia, neutropenia, decreased platelet count, increased serum alkaline phosphatase. Follow-up found that the above laboratory abnormalities were reversible. In clinical trials of multiple doses of azithromycin (intravenous/oral) in more than 750 patients, no more than 2% of patients discontinued azithromycin due to treatment-related liver enzyme abnormalities.

Patients with known hypersensitivity to azithromycin, erythromycin, other macrolides or ketolides are contraindicated. Patients with a history of cholestatic jaundice/hepatic insufficiency after previous use of azithromycin are contraindicated. Warning Allergic reactions There are very rare reports of severe allergic reactions caused by azithromycin treatment, including angioedema, anaphylactic shock reactions, skin reactions, including Stevens-Johnson syndrome and toxic epidermal necrolysis. Although rare, there have been reports of death. When some patients develop allergic symptoms, symptomatic treatment is initially effective. If treatment is stopped prematurely, allergic symptoms can recur rapidly even without azithromycin. Such patients require extended symptomatic treatment and observation. It is not known whether the occurrence of these events is related to the long half-life of azithromycin in tissues and the body's longer exposure to antigens. If an allergic reaction occurs, the drug should be discontinued immediately and appropriate treatment should be given. Physicians should be aware that allergic symptoms may reappear after symptomatic treatment is stopped. Hepatotoxicity: Abnormal liver function, hepatitis, cholestatic jaundice, hepatic necrosis, and liver failure have been reported, some of which may be fatal. If signs and symptoms of hepatitis occur, discontinue use of this medicine immediately. Clostridium difficile-associated diarrhea (CDAD) has been reported with nearly all antimicrobial agents, including this medicine, and can range in severity from mild diarrhea to fatal colitis. Antimicrobial therapy can cause changes in the normal flora of the colon, leading to overgrowth of C. difficile. Toxins A and B produced by C. difficile have been implicated in the pathogenesis of CDAD. Highly toxin-producing C. difficile causes increased morbidity and mortality, and these infections may be difficult to treat with antimicrobial agents and may require colectomy. CDAD must be considered in all patients who develop diarrhea after taking antibiotics. A careful history is warranted, as CDAD has been reported after more than 2 months of antimicrobial therapy. If CDAD is suspected or confirmed, it may be necessary to discontinue antibiotics that are not directed against C. difficile. Water, electrolytes, and protein must be appropriately supplemented according to clinical needs, and antibiotics effective against Clostridium difficile must be given, and surgical evaluation must be performed if necessary.

Precautions for children: Regardless of the type of infection, the recommended total dose of azithromycin in children is no more than 1500 mg. Azithromycin tablets are used for children weighing more than 45 kg, and the dosage and usage are the same as for adults. The efficacy and safety of treating otitis media, community-acquired pneumonia, and pharyngitis or tonsillitis in children under 6 months of age and under 2 years of age have not yet been determined. Precautions for pregnancy and lactation: There are currently no adequate and strictly controlled clinical trials in pregnant women. Since the results of animal reproduction studies do not always predict the situation in humans, the use of this drug in pregnant women must be fully weighed. It is not known whether this product is secreted in human milk. Since many drugs are secreted in human milk, breastfeeding women must consider carefully when using it. Precautions for the elderly: Not yet clear.

When nelfinavir is in steady state, coadministration of a single oral dose of azithromycin may increase azithromycin serum concentrations. Although no dose adjustment of azithromycin is required when coadministered with nelfinavir, close monitoring for known adverse effects of azithromycin, such as liver enzyme abnormalities and hearing loss, is necessary. Spontaneous postmarketing reports suggest that coadministration of azithromycin may enhance the effects of oral anticoagulants. Close monitoring of prothrombin time is required when patients are taking azithromycin and oral anticoagulants concomitantly. When used at therapeutic doses, azithromycin has little effect on the pharmacokinetics of atorvastatin, carbamazepine, cetirizine, didanosine, efavirenz, fluconazole, indinavir, midazolam, rifabutin, sildenafil, theophylline (IV and oral), triazolam, trimethoprim/sulfamethoxazole, or zidovudine. Efavirenz or fluconazole have little effect on the pharmacokinetics of azithromycin when coadministered. No dose adjustment of either drug is required when azithromycin is coadministered with any of the above drugs. In clinical trials, no interactions have been reported between azithromycin and the following drugs. However, no specific studies have been conducted to date to evaluate the potential for interactions between azithromycin and these drugs. However, these situations have occurred with the use of other macrolides. Therefore, in the absence of new research data, patients should be closely observed when azithromycin is used in combination with the following drugs: Digoxin - increased blood concentrations of digoxin. Ergotamine or dihydroergotamine - acute ergot poisoning, manifested by severe peripheral vasospasm and dysesthesia. Increased concentrations of terfenadine, cyclosporine, hexobacterial, and phenytoin. Effects on laboratory tests: No effects on laboratory test results have been reported.

Sealed, store in a dry place.

0.25 g

24 months

Sinopharm Shantou Jinshi Pharmaceutical Co., Ltd.

• Founded in:

  1987-09-10

• Address:

  No. 36, Taishan Road, Shantou City

• Tax NO.:

  91440500192729292G

• Registered Funds:

  83.98 million yuan

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