1. Chapter 36 Macrolides Clarithromycin Azithromycin Erythromycin
[‘mækrəlaid]
大环内脂类
Clarithromycin
Azithromycin
Erythromycin
Semisynthetic derivatives of Erythromycin
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2. Erythromycin 1. Pharmacokinetics
Oral absorption: be destroyed at acid pH and is therefore given as an enteric-coated tablet or as an acid-stable ester prodrug (erythromycin ethyl succinate).
Distribution: widely except brain and cerebrospinal fluid;
Excretion: be metabolized in the liver and have short half-lives (1–3 h).
琥乙红霉素
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3. 2. Antibacterial activity:
Erythromycin usually is bacteriostatic, but may be bactericidal in high concentrations against very susceptible organisms;
3. Spectrum of activity
Similar spectrum of activity to broad spectrum penicillins
(1) Gram-positive bacteria and gut anaerobes;
(2) Others: Legionella, Mycoplasma, Chlamydia, Mycobacterium, Campylobacter species, and Bordetella pertussis
[,li:dʒə'nelə]军团菌
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4. 4. Mechanism of action
Inhibit protein synthesis by binding reversibly to 50S ribosomal subunits of sensitive bacteria.
Inhibit the translocation step wherein the nascent peptide chain temporarily residing at the A site of the transferase reaction fails to move to the P, or donor, site.
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5. 5. Clinical uses
1. Mycoplasma pneumoniae infections; 2. Legionnaires' disease (first-line); 3. Chlamydial infections; 4. Diphtheria; 5. Pertussis; 6. Treating individuals who are allergic to penicillins: Streptococcal, Staphylococcal infections, tetanus, syphilis, etc.
支原体肺炎
衣原体感染
[dif‘θiəriə] 白喉
[pə‘tʌsis]百日咳
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6. 6. Adverse effects
1. Gastrointestinal effects: anorexia, nausea, vomiting, and diarrhea; 2. Liver toxicity: acute cholestatic hepatitis; 3. Cardiac toxicity: arrhythmias, including QT prolongation with ventricular tachycardia; 4. Allergic reactions.
急性胆汁淤积型肝炎
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