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antimicrobial drugs
antimicrobial drugs
24
Health Care
Professional
11/29/2010

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Term
penicillin G
Definition
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)
Term
Penicillin V
Definition
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)
Term
oxacillin
Definition
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
Term
amoxicillin
Definition
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
Term
ampicillin
Definition
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
Term
piperacillin
Definition
EXTENDED SPECTRUM- CELL WALL BIOSYNTHESIS INHIBITOR
USE: acinetobacter, pseudomonas community acquired
Mechanism: inhibits transpeptidase
Other: NOT PENICILLINASE RESISTANT, IV ADMIN for serious hospital infections
Term
ticarcillin
Definition
EXTENDED SPECTRUM- CELL WALL BIOSYNTHESIS INHIBITOR
USE: acinetobacter, pseudomonas community acquired
Mechanism: inhibits transpeptidase
Other: NOT PENICILLINASE RESISTANT, IV ADMIN for serious hospital infections
Term
clavulanic acid
Definition
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
Term
sulbactam
Definition
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
Term
tazobactam
Definition
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
Term
cephalexin
Definition
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
Term
cefazolin
Definition
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
Term
cefaclor
Definition
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
Term
cefixime
Definition
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
Term
cefepime
Definition
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
Term
imipenem
Definition
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
Term
meropenem
Definition
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
Term
cilstatin
Definition
CARBAPENEMS- CELL WALL BIOSYNTHESIS INHIBITOR
USE; inhibitor of renal dehydropeptidase
- co administered with imipenem for synergy and to prevent imipenem from being degraded.
Term
aztreonam
Definition
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
Term
bacitracin
Definition
Use: treat gut infections
Mechanism: Interferes with cell wall biosynthesis
Side Effects: nephrotoxicity, rare hypersensitivity
Other: NOT topical, ORAL for gut infections
Term
daptomycin
Definition
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
Term
fosfomycin
Definition
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
Term
vancomycin
Definition
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
Term
Beta Lactam methods of resistance
Definition
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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