Mechanis - Bacteriostatic - Bacteriostatic - Bacteriostatic - Bacteriostatic - Bacteriostatic - Bactericial m - Effective against G+ - Actively against many - Protein synthesis inhibitors - Act as competitive - Chemotherapeutic agent - Inhibit DNA replication & G- G+ - Active against bacterial cause inhibitors of enzyme (dihydrofolate reductase & transcription - Act by inhibiting protein meningitis (N. meningitides, S. DHPS (needed for folate inhibitor) - Enter cells via porin synthesis of bacteria by pneumonia, H. influenza) synthesis – folate for cell - Act by interfering with the binding to the 50S - Excellent CSF penetration) division) action of DHFR – inhibit ribosomal element synthesis of tetrahydrofolate reductase - Precursor in DNA nucleotide & thymidine Indication - Treat mild to moderate - Typhoid - Pneumonia - Prophylaxis - Pt with infection of infections - Multi-drug resistant salmonella - Urinary tract infection - Urinary tract infections intracellular pathogen typhi - Shigellosis such as Mycoplasma - 2nd line agent in treatment of - Certain protozoa pneumonia tetracyclin-resistant chorela infections - Brain abscess (staphylococcal or mixed organism) - Meningitis (for pt with severe penicillin & cephalosporin allergy) Contra- 1) Pregnant women - Interaction with digoxin Control the dosage for 1) Neonates Enchance toxicity indication 2) Breast feeding may occur in some pt. 1) Neonates 2) Infant <2 months 1) Caffeine / women 2) Pt with abnormal liver function 3) Pregnant women 2) NSAID interaction 3) Children <8 yrs old 3) Thephylline 4) Renal impairment Monitor plasma level for 4) Corticosteroid pt. 1) Children <4 yrs old Drug interacton: 2) Elderly Antacid, cimetidine, 3) Pt with renal failure warfarin, phenytoin, cyclosporine & rifampin Adverse Serious effect on - Cholestatic jaundice - Aplastic anaemia - Crystalluria effect calcified tissues, it - Ototoxicity - Bone marrow suppression - Hypersensitivity can be deposit in - Accumulate in liver - Leukemia - Hemolytic anemia bone, cause (inhibit hepatic - Gray baby syndrome discoloration & metabolism) hypoplasia of the teeth Dosage 750mg (4x daily) Resistance 1) Reduced membrane permeability 2) Mutation of 50S ribosomal unit 3) Elaboration of chloramphenicol acetyltransferase Example / Erythromycin, types Azithromycin, Chlarithromycin