Macrolides Antibiotics PDF

MACROLIDES MACROLIDE ANTIBIOTICS  Mechanism of action Bacteriostatic Inhibit protein synthesis, by binding with 50s ribosome.  Resistance Modification of ribosomal binding site. Production of esterases. Reduced permeability. Cross resistance Between Macrolides, C...

MACROLIDES MACROLIDE ANTIBIOTICS  Mechanism of action Bacteriostatic Inhibit protein synthesis, by binding with 50s ribosome.  Resistance Modification of ribosomal binding site. Production of esterases. Reduced permeability. Cross resistance Between Macrolides, Clindamycin & Chloramphenicol  Erythromycin Antimicrobial spectrum: Similar to Penicillin G G+ve, G-ve, Mycoplasma spp, Chlamydia spp, Ricketsiae spp, Spirochetes spp.  Routes of administration & preparations Erythromycin base Enteric coated or film coated - Oral – tab, suspension, ointment Erythromycin estolate - - Oral – tab, suspension Erythromycin stearate - - Oral – tab, suspension Erythromycin ethyl succinate - - Oral – tab, suspension Erythromycin lactobionate – iv infusion Erythromycin gluceptate - iv infusion Dose – 250 – 500 mg -qid USES- Dental uses- alternative to Penicillins who are allergic to it – Periodontal & Periapical abscesses, ANUG, post extraction infections Pertussis - Bordetella pertussis - Choice drug Diptheria – antitoxin + drug Treatment & Prophylaxis Corynebacterium diphtheriae Chancroid – Haemophilus ducreyi Chlamydial infections a. Pneumonia – Chlamydial pneumoniae & Chlamydial psittaci  b. Epididymitis, nongonococcal urethritis (NGU), Lymphogranuloma venerium, pelvic inflammatory disease, trachoma, inclusion conjunctivits, neonatal conjunctivitis Neonatal conjunctivits – Neisseria gonorrhoea Cholera - Vibrio cholerae Donavanosis/ Granuloma inguinale - Calymmatobacterium granulomatis  Legionnaire’ s disease – Legionella pneumophila Acne - Propionibacterium acnes Prophylaxis of surgical infections in patients undergoing bowel surgery Eryhtromycin + Neomycin  Alternative to Penicillins Subacute bacterial endocarditis - prophylaxis Rheumatic fever – prophylaxis Respiratory tract infections Skin & soft tissue infections  Gonnorrhoea - Neisseria gonorrhoea Syphilis – Treponema pallidum Actinomycosis Anthrax Leptospirosis NON ANTIMICROBIAL USE Diabetic gastroparesis - prokinetic  Adverse drug reactions Gastrointestinal tract – Mild to severe epigastric pain, anorexia, abdominal cramps, nausea, vomiting & diarrhoea. Hepatotoxicity cholestatic hepatitis – fever, jaundice as a hypersensitivity reaction.  Rare – allergic reactions,fever, eosinophilia, rashes, pruritis & urticaria. Reversible sensory neural deafness. Iv – thrombophlebitis IV - QT prolongation / Torsades de pointes  Drug interaction Hepatic microsomal enzyme inhibitor - QT prolongation / Torsades de pointes – serious ventricular arrhythmias & death have been reported when given along with terfenadine, astemizole & Cisapride. Increases the serum concentration of Theophylline, warfarin, Valproate, Digoxin  ROXITHROMYCIN Long acting Acid stable Twice daily dosing Antimicrobial spectrum: Similar to Erythromycin  Routes of adminstration oral DOSE – 150 mg bid – before meals  Uses Orodental infections Respiratory tract infections ENT infections Skin & soft tissue infections Genital tract infections  ADR Nausea, vomiting, diarrhoea, abdominal cramps, anorexia, constipation, flatulence Weakness, ataxia, malaise, dizziness, headache & vertigo  CLARITHROMYCIN Antimicrobial spectrum: Resembles Erythromycin + H pylori, Mycobacterium avium intracellulare, Mycobacterium leprae Protozoa- Toxoplasma gondii, Cryptosporidium spp.  Routes of administration: oral, iv infusion DOSE: 250mg – bid for 7 days 500mg bid – 14days – severe cases  USES Orodental infections Legionnairre’s disease – choice drug Pertussis Atypical pneumonia H pylori – Peptic ulcer disease MAC in HIV+ve patients - first line drug in combination- prophylaxis & treatment  Pulmonary disease – M kansasii Lepromatous leprosy – Mycobacterium leprae Sub acute bacterial endocarditis- prophylaxis -alternative to Penicillins Pharyngitis, tonsilitis, sinusitis, otitis media. Skin & soft tissue infections.  Campylobacter enteritis Toxoplasmosis diarrhoea Cryptosporidium diarrhoea  Adverse drug reactions Taste disturbances, stomatitis, glossitis GIT- same as Erythromycin but less frequent Aggravate muscle weakness in myasthenia gravis patients. Contraindications Pregnancy Drug interaction Same as that of Erythromycin  AZITHROMYCIN Very long acting - once daily dosing Antimicrobial spectrum ROA: Oral, IV, eyedrops Dose – 500mg OD  USES Legionnaire’s pneumonia Chlamydial infections - Epididymitis, nongonococcal urethritis (NGU), Lymphogranuloma venerium, Pelvic inflammatory disease, Trachoma - 1g Single dose Chancroid – 1g Single dose Pertussis  MAC - prophylaxis & treatment – one of the component in the combination regimen Sub acute bacterial endocarditis- prophylaxis -alternative to Penicillins Meningococcal meningitis – chemoprophylaxis Malaria  Campylobacter enteritis Toxoplasmosis diarrhoea Cryptosporidium diarrhoea  Alternative to Penicillins Pharyngitis, tonsillitis, sinusitis, otitis media. Skin & soft tissue infections Syphilis Gonorrhoea Typhoid  Adverse drug reactions GIT- same as Erythromycin but less frequent Aggravate muscle weakness myasthenia gravis patients. Drug interaction Same as that of Erythromycin  SPIRAMYCIN Synergistic with metronidazole against anerobic organisms ROA - ORAL USES TOXOPLASMOSIS CRYPTOSPORIDIOSIS CHLAMYDIAL & GONOCOCCAL INFECTIONS  MENINGOCOCCAL MENINGITIS – PROPHYLAXIS ADR Nausea, Vomiting,diarrhea & abdominal pain  TELITHROMYCIN - KETOLIDE ROA – oral – once daily dosing Use Respiratory tract infections ADR: Nausea, vomiting, Diarrhoea & abdominal pain. Reversible hepatic dysfunction