Antibiotic, Macrolide: Inhibits RNA-dependent protein synthesis at the chain elongation step; binds to the 50S ribosomal subunit resulting in blockage of transpeptidation
藥動學
Absorption: rapid from the GI tract. Distribution: extensive tissue; distributes well into skin, lungs, sputum, tonsils, and cervix; penetration into CSF is poor; Vd: 31 to 33 L/kg. Protein binding: 7% to 51%. Metabolism: hepatic to inactive metabolites. Bioavailability: 34% to 52%; variable effect with food. Half-life elimination: Infants and Children 4 months to 15 years: 54.5 hours; Adults: 68 to 72 hours. Time to peak, serum: ~2 to 3 hours. Excretion: biliary (major route 50%, unchanged); urine (6% to 14% unchanged).
禁忌症
Hypersensitivity to azithromycin, erythromycin, other macrolide (eg, azalide or ketolide) antibiotics, or any component of the formulation; history of cholestatic jaundice/hepatic dysfunction associated with prior azithromycin use
懷孕分類
B
1. Azithromycin crosses the placenta.
2. Azithromycin is recommended for the treatment of several infections, including chlamydia, and granuloma inguinale, and prophylaxis of Mycobacterium avium complex in select pregnant patients.
哺乳分類
1. Azithromycin is present in breast milk. 2. azithromycin is one of the recommended agents for the treatment of granuloma inguinale in lactating patients.
副作用
Altered cardiac conduction: prolonged QT interval on ECG (Ref) and polymorphic ventricular tachycardia. Clostridioides difficile infection (CDI) : Clostridioides difficile associated diarrhea and Clostridioides difficile colitis. Drug-induced liver injury: cholestatic hepatitis, hepatocellular hepatitis, and mixed cholestatic/hepatocellular hepatitis. Hypersensitivity reactions (delayed) : skin rash, severe cutaneous adverse reactions (SCARs). Hypersensitivity reactions (immediate) : angioedema, urticaria and anaphylaxis. Ototoxicity: hearing loss and tinnitus.
劑量和給藥方法
Adult: upper respiratory tract infections, lower respiratory tract infections, skin and soft tissue infections and oral disease: 500mg once daily for 3 days. Older adult: the same dose as adults; the elderly are more likely to develop arrhythmias and the risk of torsades de points, use with caution.<20231009>Acne vulgaris, inflammatory, moderate to severe (alternative agent) (off-label use): 500 mg once daily for 4 consecutive days per month for 3 months or 500 mg once daily for 3 days in the first week, followed by 500 mg once weekly until week 10 or 500 mg once daily for 3 consecutive days each week in month 1, followed by 500 mg once daily for 2 consecutive days each week in month 2, then 500 mg once daily for 1 day each week in month 3. Sexually transmitted infections (Chlamydia trachomatis) : 1 g as a single dose, preferably under direct observation; give in combination with ceftriaxone if the patient is at high risk for gonorrhea. Pertussis (off-label use) : 500 mg on day 1, followed by 250 mg once daily on days 2 to 5. Bronchiectasis (noncystic fibrosis), prevention of pulmonary exacerbations (off-label use) : 500 mg 3 times weekly or 250 mg once daily. Bronchiolitis obliterans (off-label use) : 250 mg 3 times weekly; some experts recommend an initial dose of 250 mg daily for the first 5 days. Chronic obstructive pulmonary disease, acute exacerbation (treatment) : 500 mg in a single loading dose on day 1, followed by 250 mg once daily on days 2 to 5 or 500 mg once daily for 3 days. Cystic fibrosis, anti-inflammatory (off-label use) : 250 mg (<40 kg) or 500 mg (≥40 kg) 3 times weekly or 250 mg once daily. Pneumonia, community-acquired: Outpatient: 500 mg on day 1, followed by 250 mg once daily for 4 days or 500 mg once daily for 3 days. Inpatient: 500 mg once daily for a minimum of 3 days. Rhinosinusitis, acute bacterial: 500 mg once daily for 3 days.
小兒調整劑量
10 mg/kg once daily for 3 days; maximum dose: 500 mg/dose. Children≥45 kg are given the same dose as adults (500 mg per day for 3 days).<20231009>
腎功能調整劑量
No dosage adjustment necessary
肝功能調整劑量
1.There is no dosage adjustment provided in the manufacturer's labeling. 2.Use with caution due to potential for hepatotoxicity (rare); discontinue immediately for signs or symptoms of hepatitis.