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Macrolides
| Question | Answer |
|---|---|
| 1.Macrolides | Bacteriostatic and ahows time dependant killing |
| Examples | Erythromycin , Clarithromycin, Azithromycin |
| Mechanism of action | Inhibit protein synthesis, Peptide chain elongation prevented. |
| Spectrum of antibacterial activity | Simillar to penicillin . Effective against gram + organisms. Pneumococci , streptococci, staphylococci, corynebacteria. Gram - bacteria. Legionella, bordetella, pertussis, campylobacter jejuni. |
| Erythromycin | Prototype. More effective against gram +, Bacteriostatic but may be at high concerntrations bactericidal, |
| Elimination | Bile and feces |
| Dosage | 250-500 mg 4 times a day |
| Indications | Mycoplasma pneumonia, Legionnaires disease, Diphtheria, Alternative for penicillin allergic patients for infections with streptococcus aureus, atreptococcus puogenes, streptococcus pneumoniae, trepnima pallidum. |
| Adverse effects | Less toxic. Anorexia,nausea, diarrhea . Cholestatic hepatitis. |
| Clarithromycin | Simillar spectrum of antibacterial activity as erythromycin. More active against H. Influenza. Completely absorbed from GIT, |
| Half life | 6 hours |
| Available as | Modified release preparations, Oral suspension, IV form |
| Indications | RTI including atypical pneumonia , Otitis media, Atypical mycobacterial infections , H.pylori eradication |
| Azithromycin | Less active than erythromycin |
| Route | Orally, Food interferes the absorption |
| Half life | 50 hours |
| Excretion | Bile |
| Adverse effects | Gi effects are less than erythromycin |
| 2. Ketolides | Telithromycin |
| Telithromycin | First ketolide, a semisynthetic derivatives of macrolides. Spectrum is simillar to macrolides. Effective against erythromycin resistant streptococcus pneumoniae. |
| Route | Orally |
| Half life | 10 hours |
| Uses | Oral treatment of upper and lower RTi |
| Adverse effects | Diarrhea, transient visual disturbances and rarely hepatotoxicity |
| 3. Lincosamidea | Clindamycin |
| Clindamycin | Derivative of lincosamides. Spectrum simillar to erythromycin and flucoxacillin. |
| Route | Orally |
| Available as | Oral capsule, oral solution . Clindamycin phosphate for IM and IV use. Topical preparation |
| Indications | Staphylococcal bone and joint infections, Serious intra abdominal infection , Skin and aoft tissue infection , Acne vulgaricus |