Azithromycin Granules Instructions

Main ingredient: Azithromycin.
Chemical name: (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-xylo-hexopyranosyl]oxy]-1-oxacyclohexadecan-15-one.
Molecular formula: C38H72N2O12
Molecular weight: 749.00

 

This product is white or off-white granules.

 

1. Acute pharyngitis and acute tonsillitis caused by pyogenic streptococci.
2. Sinusitis, 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-multidrug-resistant Neisseria gonorrhoeae.
5. Skin and soft tissue infections caused by sensitive bacteria.

 

0.1g (100,000 units).

 

Pour this product into a cup, add an appropriate amount of cooled boiled water, dissolve and shake well before oral administration. Take 1 hour before meals or 2 hours after meals.
Adult dosage:
1. For sexually transmitted diseases caused by Chlamydia trachomatis or sensitive Neisseria gonorrhoeae, a single oral dose of 1.0g is sufficient;
2. For treatment of other infections: total dose 1.5g, taken in three doses, 0.5g once daily; or the same total dose of 1.5g, with 0.5g on the first day, then 0.25g once daily from day 2 to 5. Pediatric dosage: 1. For treatment of otitis media and pneumonia, on day 1, single oral dose of 10mg/kg body weight (maximum 0.5g per day), days 2-5, single oral dose of 5mg/kg body weight daily (maximum 0.25g per day) or administered as follows: Weight (kg) Day 1 (once daily) Days 2-5 (once daily) 15-25 0.2g 0.1g 26-35 0.3g 0.15g 36-45 0.4g 0.2g 2. For treatment of pediatric pharyngitis and tonsillitis, single oral dose of 12mg/kg body weight daily (maximum 0.5g per day) for 5 consecutive days, or as directed by a physician.

 

This product is generally well tolerated, with a low incidence of adverse reactions, mostly mild to moderate and reversible.
1. Common adverse reactions include: (1) Gastrointestinal reactions: diarrhea, nausea, abdominal pain, loose stools, vomiting, etc.; (2) Skin reactions: rash, itching, etc.; (3) Other reactions: such as anorexia, vaginitis, dizziness, or dyspnea.
2. Clinical observations have also noted the following adverse reactions occurring in less than 1% of cases: (1) Digestive system: indigestion, gastrointestinal bloating, mucositis, oral candidiasis, gastritis, etc.; (2) Nervous system: headache, drowsiness, etc.; (3) Allergic reactions: bronchospasm, etc.; (4) Other reactions: taste disturbances, etc.
3. Post-marketing oral formulations have also reported the following adverse reactions, with unclear association to this product: (1) Allergic reactions: joint pain, angioneurotic edema, urticaria, photosensitivity; (2) Cardiovascular system: arrhythmia, ventricular tachycardia; (3) Gastrointestinal: rare pseudomembranous colitis, tongue discoloration; (4) Genitourinary system: interstitial nephritis, acute renal failure; (5) Hematopoietic system: thrombocytopenia; (6) Hepatobiliary system: reports of azithromycin-induced hepatitis and cholestatic jaundice, occasionally liver necrosis and liver failure, rarely fatal, causality not established; (7) Psychiatric and nervous system: aggressive behavior, nervousness, anxiety, worry, headache, drowsiness, dizziness, vertigo, convulsions, hyperactivity; (8) Skin and appendages: rare severe skin reactions such as erythema multiforme, Stevens-Johnson syndrome, and toxic epidermal necrolysis have been reported; (9) Sensory organs: macrolide antibiotics have been reported to impair hearing in patients. Some patients taking azithromycin have experienced hearing impairment including hearing loss, tinnitus, and/or deafness. Studies indicate this is related to prolonged high-dose use, with most patients recovering hearing upon follow-up. Rare reports of azithromycin-induced taste changes.
4. Laboratory abnormalities: elevated serum ALT, AST, creatinine, LDH, bilirubin, and alkaline phosphatase; decreased white blood cells, neutrophils, and platelet counts.

 

Contraindicated in patients allergic to azithromycin, erythromycin, or any other macrolide antibiotics.

 

1. Food intake can affect the absorption of azithromycin, so it should be taken 1 hour before or 2 hours after meals.
2. Patients with mild renal impairment (creatinine clearance ≥40 ml/min) do not require dose adjustment, but there is no data on the use of azithromycin in patients with more severe renal impairment, so caution should be exercised when using azithromycin in these patients.
3. Since the hepatobiliary system is the main route of azithromycin excretion, use with caution in patients with hepatic impairment; it should not be used in patients with severe liver disease. Liver function should be regularly monitored during treatment.
4. If allergic reactions occur during treatment (such as angioneurotic edema, skin reactions, Stevens-Johnson syndrome, and toxic epidermal necrolysis), the medication should be stopped immediately and appropriate measures taken.
5. During treatment, if the patient develops diarrhea, pseudomembranous colitis should be considered. If diagnosed, appropriate treatment measures should be taken, including maintaining water and electrolyte balance and supplementing protein.
6. If any adverse events and/or adverse reactions occur during the use of this product, please consult a doctor.
7. Please inform your doctor if you are using other medications concurrently.
8. Keep out of reach of children.

 

Animal studies have shown no effect on the fetus, but there is a lack of experience in human pregnant women; therefore, the use in pregnant women must carefully weigh the benefits and risks. There is no data indicating whether this product is excreted in breast milk, so use in lactating women should be considered with caution.

 

Regardless of the type of infection, the total recommended dose of azithromycin in children should not exceed 1500 mg. Azithromycin dry suspension is used for children weighing more than 45 kg, with the same dosage as adults. The efficacy and safety of treating otitis media in children under 6 months, community-acquired pneumonia, and pharyngitis or tonsillitis in children under 2 years old have not been established.

 

No studies have been conducted and there are no reliable references.

 

According to foreign drug interaction study data, the following information about this product has been obtained:
Antacids: In pharmacokinetic studies exploring the simultaneous administration of antacids and azithromycin, the peak concentration of azithromycin decreased by approximately 25%, with no observed effect on total bioavailability. Patients who need to take both azithromycin and antacids should not take these medications at the same time. Cetirizine: In healthy volunteers, co-administration of azithromycin and cetirizine (20 mg) for 5 days showed no pharmacokinetic interaction at steady-state concentrations, nor was there a significant change in the QT interval. Deoxyinosine (2'-deoxyinosine): Compared to placebo, six HIV-positive patients taking 1200 mg azithromycin and 400 mg deoxyinosine daily showed no effect on the steady-state pharmacokinetics of deoxyinosine. Digoxin: There have been reports that some macrolide antibiotics affect the intestinal metabolism of digoxin in certain patients. Therefore, patients taking both azithromycin and digoxin should be monitored for potential increases in digoxin blood levels. Zidovudine: Single doses of 1000 mg and multiple doses of 1200 mg or 600 mg azithromycin have little effect on the plasma pharmacokinetics or urinary excretion of zidovudine or its glucuronide metabolite. However, oral azithromycin can increase the concentration of phosphorylated zidovudine in peripheral blood mononuclear cells, which is the clinically active metabolite. The clinical significance of these findings is unclear but may be beneficial to patients. Azithromycin has no significant effect on the hepatic cytochrome P450 system. Unlike other macrolide antibiotics such as erythromycin, azithromycin does not affect the pharmacokinetics of other drugs and does not lose activity by inducing hepatic cytochrome P450 or forming cytochrome metabolic complexes. Ergot: Due to the theoretical possibility of ergot toxicity, the concurrent use of azithromycin and ergot derivatives is not recommended. Pharmacokinetic studies have been conducted between azithromycin and the following drugs primarily metabolized by the hepatic cytochrome P450 system. Atorvastatin: Daily co-administration of atorvastatin 10 mg and azithromycin 500 mg has no effect on atorvastatin blood concentrations (HMG CoA-reductase inhibition assay). Carbamazepine: Pharmacokinetic studies in healthy volunteers show no significant effect on the blood concentrations of carbamazepine and its active metabolites when co-administered with azithromycin. Cimetidine: In single-dose pharmacokinetic studies of cimetidine, administration two hours before azithromycin showed no change in azithromycin pharmacokinetics. Coumarin oral anticoagulants: Pharmacokinetic studies in healthy volunteers show that azithromycin does not affect the anticoagulant effect of a single 15 mg dose of warfarin. Post-marketing reports indicate that concurrent use of azithromycin and coumarin oral anticoagulants may enhance anticoagulant effects. Although causality is not established, patients using coumarin oral anticoagulants concurrently should have their prothrombin time monitored regularly. Cyclosporine: Pharmacokinetic studies in healthy volunteers show that after daily oral administration of azithromycin 500 mg for 3 days, a single oral dose of cyclosporine 10 mg/kg results in significantly increased peak concentration and 5-hour AUC of cyclosporine. Therefore, caution is required when co-administering these drugs. If co-administration is necessary, cyclosporine blood levels should be monitored to adjust dosage accordingly. Efavirenz: Co-administration of azithromycin (single dose 600 mg) and efavirenz (400 mg daily for 7 days) showed no clinically significant pharmacokinetic changes. Fluconazole: Co-administration of a single dose of fluconazole 800 mg and azithromycin 1200 mg showed no significant change in fluconazole pharmacokinetics; azithromycin's total exposure and half-life were unchanged, though peak blood concentration decreased by 18%, without clinical significance. Indinavir: Co-administration of a single 1200 mg dose of azithromycin had no significant effect on the pharmacokinetics of indinavir (800 mg three times daily for 5 days). Methylprednisolone: Drug interaction studies in healthy volunteers showed no significant effect of azithromycin on methylprednisolone pharmacokinetic parameters. Midazolam: Healthy volunteers co-administered azithromycin (500 mg/day for 3 days) and a single 15 mg dose of midazolam showed no significant changes in midazolam pharmacokinetics or pharmacodynamics. Nelfinavir: Co-administration of azithromycin 1200 mg and nelfinavir (750 mg three times daily until steady-state blood levels) showed no clinically significant drug interactions, so no dose adjustment is necessary. Rifabutin: Co-administration of this product with rifabutin does not affect serum concentrations of either drug. However, neutropenia has been reported when azithromycin is combined with rifabutin. Although neutropenia is associated with rifabutin use, it is unclear whether azithromycin contributes. Sildenafil: Studies in healthy male volunteers show no evidence that azithromycin (500 mg daily for 3 days) affects the peak blood concentration or AUC of sildenafil or its main N-desmethyl metabolite. Terfenadine: Pharmacokinetic studies indicate no drug interaction between azithromycin and terfenadine. Although rare cases of interaction have been reported and cannot be completely ruled out, there is no specific evidence that such interaction occurs. Theophylline: No interaction between azithromycin and theophylline was observed in healthy volunteers. Triazolam: Compared to placebo, 14 healthy volunteers co-administered azithromycin (500 mg on day 1, 250 mg on day 2) and triazolam (0.125 mg on day 2) showed no significant effect on triazolam pharmacokinetics. TMP/SMZ: Daily administration of TMP/SMZ 160 mg/800 mg for 7 days with a single 1200 mg dose of azithromycin on day 7 showed no significant changes in TMP/SMZ blood concentration, total exposure, or urinary clearance. Azithromycin blood concentrations were consistent with other studies.

 

No studies have been conducted and there are no reliable references.

 

Pharmacological Action Azithromycin is a nitrogen-containing macrolide antibiotic. Its mechanism of action is through binding to the 50S ribosomal subunit of susceptible microorganisms, thereby interfering with protein synthesis (without affecting nucleic acid synthesis).
In vitro tests and clinical studies have shown that azithromycin is effective against the following pathogenic bacteria: Gram-positive aerobic microorganisms: Staphylococcus aureus, pyogenic streptococci, Streptococcus pneumoniae, hemolytic streptococci. Azithromycin exhibits cross-resistance with erythromycin-resistant Gram-positive bacteria. Most fecal streptococci (enterococci) and methicillin-resistant Staphylococcus aureus are resistant to this drug. Gram-negative aerobic microorganisms: Haemophilus influenzae, Moraxella catarrhalis. Other microorganisms: Chlamydia trachomatis. In vitro tests and clinical studies suggest that this drug can prevent diseases caused by the Mycobacterium avium complex (composed of Mycobacterium avium and Mycobacterium intracellulare). The β-lactamase produced by bacteria does not affect the activity of azithromycin. In vitro studies have been conducted on the following microorganisms, but their clinical significance is unclear, including streptococci (groups C, F, G), viridans streptococci, Bordetella pertussis, Haemophilus ducreyi, Legionella pneumophila, Bacteroides species, Enterococcus species, Borrelia, Mycoplasma pneumoniae, Treponema pallidum, Ureaplasma urealyticum, etc. Toxicological effects: Genetic toxicity: Results from human lymphocyte tests, mouse bone marrow micronucleus tests, and mouse in vitro lymphoma cell tests show that azithromycin does not exhibit mutagenic effects. Reproductive toxicity: Reproductive toxicity tests in rats and mice indicate that when azithromycin (administered orally) is given at doses causing moderate maternal toxicity (i.e., 200 mg/kg/day, calculated by body surface area, approximately 2-4 times the human dose of 500 mg/kg/day), no teratogenic effects were observed. No damage to fertility or fetuses has been found. There are currently no adequate and well-controlled clinical trials in pregnant women. Since animal reproductive studies do not always predict human outcomes, azithromycin should only be used during pregnancy if clearly necessary. It is unknown whether this drug is secreted in human milk; since many drugs are secreted in breast milk, caution should be exercised when used by nursing women. Carcinogenicity: There is no data on the carcinogenicity of long-term use of this drug in animals.

 

Rapidly absorbed after oral administration, with a bioavailability of 37%. After a single oral dose of 0.5 g, the peak time is 2.5 to 2.6 hours, and the peak blood concentration (Cmax) is 0.4 to 0.45 mg/L. The drug is widely distributed in the body, with tissue concentrations reaching 10 to 100 times the concurrent blood concentration. Concentrations are high in macrophages and fibroblasts, with the former able to transport azithromycin to sites of inflammation. The blood elimination half-life (t1/2β) after a single dose is 35 to 48 hours. More than 50% of the dose is excreted unchanged via the bile, and about 4.5% is excreted unchanged in the urine within 72 hours after administration. The serum protein binding rate decreases as blood drug concentration increases; at a blood concentration of 0.02 μg/ml, the serum protein binding rate is 15%, and at 2 μg/ml, it is 7%. Foreign data show that pharmacokinetic parameters do not significantly change in patients with mild to moderate renal impairment (glomerular filtration rate 10–80 ml/min), but there are significant differences in patients with severe renal impairment (glomerular filtration rate less than 10 ml/min) compared to normal individuals, with systemic exposure increased by 33%.

 

Keep sealed and store in a dry place.

 

Blister pack with paper-aluminum composite film bags, 9 bags per box.

 

24 months.

 

Chinese Pharmacopoeia 2005 Edition, Volume II. ^[1]