内酰胺酶抑制剂抗生素(英文ppt)lactam

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1、Miscellaneous Antibiotics,Polymyxins Active against gram-negative including pseudomonas. Polymyxin B is only available. Bactericidal inhibits cell wall synthesis. Used only topically . Highly nephrotoxic.,Spectinomycin,Bactericidal ,inhibits protein synthesis by binding to 30S ribosomal subunits. Ac

2、tive against gram positive & gram negative organisms. Rapidly absorbed after intramuscular injection. Excreted through kidney .,Clinical uses,As an alternative treatment for drug- resistant gonorrhea or gonorrhea in penicillin allergic patients. No cross-resistance with other drugs used in gonorrhea

3、.A single intramuscular dose is given,Adverse effects,Pain at the site of injection Fever And nausea Nephrotoxicity ( rare ),Clindamycin,Active against gram-positive cocci Gram negative anaerobic organisms Inhibits protein synthesis by binding to 50S ribosomal subunits.,Pharmacokinetics,Given orally

4、 or intravenously Highly bound to plasma proteins Distributes well into all body fluids & tissues except brain &CSF. Penetrates well into abscess & is taken up by phagocytic cells.,Metabolized by the liver.Both active drug & active metabolites are excreted in bile & urineNo dosage adjustment is need

5、ed for renal failure.,Clinical uses,Severe anaerobic infections ( bones and joints) . Conjunctivitis. In combination with aminoglycoside or cephalosporin to treat penetrating wounds of the abdomen & the gut. Infections in female genital tract ( septic abortion ,pelvis abscess ).,For prophylaxis of e

6、ndocarditis in patients with valvular heart disease Plus primaquine is an effective alternative to co-trimoxazole for moderate or severe pneumocystis jiroveci pneumonia in AIDS patients,Adverse Effects,Diarrhea , nausea, Skin rash Antibiotic-associated colitis Impaired liver function Neutropenia ( n

7、ot common ),Vancomycin,BactericidalInhibits bacterial cell wall synthesisActive on gram-positive bacteria including -lactamase producer & those resistant to methicillin.,Pharmacokinetics,Poorly absorbed from GIT Slow IVI is used for treatment of systemic infections. Widely distributed Cerebrospinal

8、fluid levels are achieved in meningeal inflammation Excreted mainly through renal route,Clinical uses,Endocarditis or sepsis mainly caused by methicillin resistant staphylococci. Alternative to penicillin in enterococcal endocarditis( in combination with gentamicin). Meningitis( in combination with

9、cephalosporin) Orally only for the treatment of antibiotic -associated enterocolitis,Adverse effects,Phlebitis at the site of infusion Fever Ototoxicity & nephrotoxicity ( not common). Red man or red neck syndrome. Hypotension,Bacitracin,Bactericidal Inhibits cell wall synthesis Active against gram

10、+ve organismsUsed only topically in skin ,eye ,nose infections .As ointment in combination with polymyxin or neomycin for mixed bacterial infections. As solution in saline for irrigation of joints, wounds or pleural cavity.,Adverse Effects,Highly nephrotoxic producing proteinuria, hematuriaHypersens

11、itivity reactions,Teicoplanin,Similar to vancomycin in :Mechanism of actionAntibacterial activity Given I.M. or I.V.long half-life(45-70 h).once daily.,Cycloserine,Bactericidal Inhibits bacterial cell wall Effective on gram- positive & gram- negative organisms as well as M.tuberculosis.Rapidly absorbed orally Widely distributed in body tissues & fluids. Excreted as active form in urineUsed in treatment of pulmonary & extrapulmonary tuberculosisC.N.S. toxicity ( headaches, tremors, acute psychosis, convulsions) Contraindicated in epileptic & psychotic patients,

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