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PENICILLIN - CELL WALL BIOSYNTHESIS INHIBITOR - BETA LACTAM USE: gram +, gram - cocci, spirochaetes like gonorrhea and syphilis (s. pneumo, non-lactamase staph, n. meningitidis, clostridium, treponema - NOT against gram - rods and anaerobes Mechanism: inhibits transpeptidase, bactericidal Other: ORAL ROUTE INEFFECTIVE, IV, or IM, 2 membered ring with side chains, most excreted in urine, not good for topical applications, widely distributed excet in CNS, spectrum of action varies, - lactamase sensistive Side Effects: allergy, rash, anaphylactic shock, low toxicity, seizures at high doses, nausea, vomiting, diarrhea (if oral) |
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PENICILLIN- CELL WALL BIOSYNTHESIS INHIBITOR - BETA LACTAM USE: gram +, gram - cocci, spirochaetes like gonorrhea and syphilis (s. pneumo, non-lactamase staph, n. meningitidis, clostridium, treponema - NOT against gram - rods and anaerobes Mechanism: inhibits transpeptidase, bactericidal Other: ORAL absorption better than Pen G but NOT For serious infections, 2 membered ring with side chains, most excreted in urin, not good for topical applications, widely distributed except in CNS, spectrum of action varies Side Effects: allergy, rash, anaphylactic shock, low toxicity, seizures at high doses, nausea, vomiting, diarrhea (if oral) |
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BETA-LACATAMASE RESISTANT- CELL WALL BIOSYNTHESIS INHIBITOR USE: against penicillinase producing Staphylococci and streptococci except MRSA and enterococci Mechanism: inhibits transpeptidase but has resistance against lactamase Side Effects: more than penicillins |
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EXTENDED SPECTRUM - CELL WALL BIOSYNTHESIS INHIBITOR USE: non-lactamase gram - bacilli such as E. Coli, H. influenza, Salmonella, Shigella Mechanism: inhibit transpeptidase Other: ORAL absorption reduced by food, not a substitute for Pen G or V Side Effects: FREQUENTLY PRODUCES RASHES |
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EXTENDED SPECTRUM - CELL WALL BIOSYNTHESIS INHIBITOR USE: non-lactamase gram - bacilli such as E. Coli, H. influenza, Salmonella, Shigella Mechanism: inhibit transpeptidase Other: ORAL absorption reduced by food, not a substitute for Pen G or V Side Effects: FREQUENTLY PRODUCES RASHES |
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EXTENDED SPECTRUM- CELL WALL BIOSYNTHESIS INHIBITOR USE: acinetobacter, pseudomonas community acquired Mechanism: inhibits transpeptidase Other: NOT PENICILLINASE RESISTANT, IV ADMIN for serious hospital infections |
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EXTENDED SPECTRUM- CELL WALL BIOSYNTHESIS INHIBITOR USE: acinetobacter, pseudomonas community acquired Mechanism: inhibits transpeptidase Other: NOT PENICILLINASE RESISTANT, IV ADMIN for serious hospital infections |
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BETA LACTAMASE INHIBITORS- CELL WALL BIOSYNTHESIS INHIBITOR USE: compound pill with other B-lactamase sensisitive drugs and is a B-lactamase suicide inhibitor Mechanism: prevents lactamase from breaking down the B lactams Other: structurally related to penicillin, synergistic with Amoxicillin, no antimicrobial activity on own Side Effects: may cause allergic reaction |
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BETA LACTAMASE INHIBITORS- CELL WALL BIOSYNTHESIS INHIBITOR USE: compound pill with other B-lactamase sensisitive drugs and is a B-lactamase suicide inhibitor Mechanism: prevents lactamase from breaking down the B lactams Other: structurally related to penicillin, synergistic with Amoxicillin, no antimicrobial activity on own Side Effects: may cause allergic reactions |
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BETA LACTAMASE INHIBITORS- CELL WALL BIOSYNTHESIS INHIBITOR USE: compound pill with other B-lactamase sensisitive drugs and is a B-lactamase suicide inhibitor Mechanism: prevents lactamase from breaking down the B lactams Other: structurally related to penicillin, synergistic with Amoxicillin, no antimicrobial activity on own Side EFffects: may cause allergic reactions |
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1ST GENERATION CEPHALOSPORIN- CELL WALL BIOSYNTHESIS INHIBITOR - BETA LACTAM USE: gram positive and some community acquired gram negative NOT anaerobes, surgical prophylaxis, staph and strep infections Mechanism: inhibits cell wall synthesis and contains a B lactam Other: DO NOT penetrate the CNS, excreted in urine with some partially metabolized, NOT topical due to allergeniity, give ORALLY Resistance: cephalosporinase, penicillinase, low-affinity penicillin binding proteins Side Effects: nausea, vomit, pain, stomatitis, nephrotoxicity, superinfection due to gram negative inhibition, allergy and cross-reactivity iwth penicillin - anaphylaxis |
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1ST GENERATION CEPHALOSPORIN- CELL WALL BIOSYNTHESIS INHIBITOR - BETA LACTAM USE: gram positive and some community acquired gram negative NOT anaerobes, surgical prophylaxis, staph and strep infections Mechanism: inhibits cell wall synthesis and contains a B lactam Other: DO NOT penetrate the CNS, excreted in urine with some partially metabolized, NOT topical due to allergeniity, give IV Resistance: cephalosporinase, penicillinase, low-affinity penicillin binding proteins Side Effects: nausea, vomit, pain, stomatitis, nephrotoxicity, superinfection due to gram negative inhibition, allergy and cross-reactivity iwth penicillin - anaphylaxis |
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2ND GENERATION CEPHALOSPORIN- CELL WALL BIOSYNTHESIS INHIBITOR - BETA LACTAM USE: extended gram negative spectru, with some efficacy agagint oral and bowel anaerobes Mechanism: inhibits cell wall synthesis and contains a B lactam Other: DO NOT penetrate the CNS, excreted in urine with some partially metabolized, NOT topical due to allergeniity, give ORALLY Resistance: cephalosporinase, penicillinase, low-affinity penicillin binding proteins Side Effects: nausea, vomit, pain, stomatitis, nephrotoxicity, superinfection due to gram negative inhibition, allergy and cross-reactivity iwth penicillin - anaphylaxis **Less effective v. gram positive than 1st generation |
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3RD GENERATION CEPHALOSPORIN- CELL WALL BIOSYNTHESIS INHIBITOR - BETA LACTAM USE: extended gram negative spectrum and PENETRATES THE CNS for meningitis causes by pneumococci and meningococci, influenza, susceptible E.COli and Klebsiella, penicillin resistant N. gonorrhea Mechanism: inhibits cell wall synthesis and contains a B lactam Other: excreted in urine with some partially metabolized, NOT topical due to allergeniity, give ORALLY Resistance: cephalosporinase, penicillinase, low-affinity penicillin binding proteins Side Effects: nausea, vomit, pain, stomatitis, nephrotoxicity, superinfection due to gram negative inhibition, allergy and cross-reactivity iwth penicillin - anaphylaxis **Less effective v. gram positive than 1st generation |
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4TH GENERATION CEPHALOSPORIN- CELL WALL BIOSYNTHESIS INHIBITOR - BETA LACTAM USE: enhanced resistance against beta-lactamase, PENETRATES THE CNS, extended against gram - such as enterobacteriacea and pseudomonas, extended activity v. gram positive Mechanism: inhibits cell wall synthesis and contains a B lactam Other: excreted in urine with some partially metabolized, NOT topical due to allergeniity, give IV Resistance: cephalosporinase, penicillinase, low-affinity penicillin binding proteins Side Effects: nausea, vomit, pain, stomatitis, nephrotoxicity, superinfection due to gram negative inhibition, allergy and cross-reactivity iwth penicillin - anaphylaxis |
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CARBAPENEMS- CELL WALL BIOSYNTHESIS INHIBITOR USE: gram negative rods, gram positives and anaerobes, resistant to many beta lactamases, serious nosocomial infections, mixed infections, NOT for MRSA or VRE unless absolutely necessary Mechanism: Inhibits transpeptidase Other: IV admin, renal metabolism and excretiON, distributes well in CNS ***CO-ADMIN WITH INHIBITOR OF RENTAL DEHYDROPEPTIDASE- CILASTATIN or it will be rapidly metabolized Side Effects: neurotoxicity, sizures, nausea, vomit, superinfection, cross-allergic reaction to penicillin |
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CARBAPENEMS- CELL WALL BIOSYNTHESIS INHIBITOR USE: gram negative rods, gram positives and anaerobes, resistant to many beta lactamases, serious nosocomial infections, mixed infections, NOT for MRSA or VRE unless absolutely necessary Mechanism: Inhibits transpeptidase Other: IV admin, renal metabolism and excretiON, distributes well in CNS Side Effects: neurotoxicity, sizures, nausea, vomit, superinfection, cross-allergic reaction to penicillin |
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CARBAPENEMS- CELL WALL BIOSYNTHESIS INHIBITOR USE; inhibitor of renal dehydropeptidase - co administered with imipenem for synergy and to prevent imipenem from being degraded. |
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MONOBACTAM- CELL WALL BIOSYNTHESIS INHIBITOR USE:gram negative rods (may replace aminoglycosides) NOT against gram positives or anaerobes Mechanism: inhibits transpeptidase Other: monocyclic lactam, poor oral absorption, IM or IV admin, rapid renal elim, drug penetrates an inflamed CNS Side Effects: mild, plebitis, pain at injection site, less toxic than aminoglycosides |
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Use: treat gut infections Mechanism: Interferes with cell wall biosynthesis Side Effects: nephrotoxicity, rare hypersensitivity Other: NOT topical, ORAL for gut infections |
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cyclic lipopeptide from Streptomyces USE: complicated skin and soft tissue infectiion caused by gram + like s. aureus (MRSA), streptococcus, vancomycin snesitive enterococcus faecalis, MRSA bacteremia Mechanism: depolarizes gram positive bacteria, bactericidal Other: IV admin, renal elimination - ADJUST DOSE IN RENAL INSUFFICIENCY, resistance observed and some cross resistance Side Effects: mild muscle pain or weakness elevated with creatine phosphokinase |
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CELL WALL BIOSYNTHESIS INHIBITOR USE: single dose oral treatment of un-complicated UTI's in women caused by E. faecalis and E coli Other: well absorbed, distributes well, low levels in CNS except in inflamed meninges, excreted unchanged in the urine, resistance if multiple doses given in monotherapy Side Effects: well tolerated, diarrhea, vaginitis Mechanism: inhibits cell wall biosynthesis by blocking peptidogloycan synthesis - different step than vancomycin and penicillins |
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CELL WALL BIOSYNTHESIS INHIBITOR USE: most gram positive cocci and bacilli, NOT gram negative, effective v. MOST MRSA, penicillin-resistant strep penumo coag negative staph OTER: combo therapy with aminoglycosides is synergistic NOT recommeded for antibiotic associated colitis by C. dificile. Mechanism: inhibits synthesis of bacterial cell wall upstream of penicillin, blocks cell wall precursor formation, bactericidal except bacteriostatic in enterococci Other: poorly absorbed orally but can be used for gut infections, not IM, distributes in CNS if meninges inflamed, excreted by the idney with dose adjustments needed for renal insufficiency resistance is a concern with VRSA due to plasmid encoded resistance units SIde effects: hypersensitivity, flushing, tachycardia, low BP, phlebitis and pain at injection site, ototoxicity and nephrotoxicity |
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Beta Lactam methods of resistance |
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1. penicillinase - common 2. altered penicillin binding proteins 3. decreased uptake by gram negatives 4. under certain considitions, protoplasts can survive and divide 5. both inherent and acquired resistance common |
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