beta-lactam inhibitors - others Flashcards by Carmina Mislang

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OTHER BETA-LACTAM DRUGS
monobactam

astreonam

 Resistant to beta-lactamases produced by certain gram (-) rods
 Klebsiella
 Pseudomonas
 Serratia
 No activity against gram (+) and anaerobes

astreonam

astreonam RoA

IV

Elimination of astreonam

 Eliminated via renal tubular secretion

w/ or w/o cross-allergenicity with penicillin?

none

adverse effects of astreonam

 Adverse effects
 GI upset with possible superinfection
 Vertigo
 Headache
 Rare hepatotoxicity
 Skin rash

 An inhibitor of cell wall synthesis binding to PBP3
 Synergistic with aminoglycosides

astreonam

 Chemically different from penicillins
 Retain the beta-lactam ring

carbapenems

the carbapenems are (3)

B. IMIPENEM, MEROPENEM, and ERTAPENEM

 Low susceptibility to beta-lactamases

carbapenems

 Wide activity against
 Gram(+) cocci
 Gram (-) rods
 Anaerobes

carbapenems

RoA of carbapenems

IV

 Useful for infections caused by organisms resistant to other antibiotics


CARBAPENEMS

Drug of choice for enterobacter

CARBAPENEMS

Inactivates impinem

renal dehydropeptidase I

 Administered in combination w/impinen

cilastatin

 Increases the half-life of impinem
 Inhibits formation of nephrotoxic metabolites

cilastatin

 Inhibitor of the renal dehydropeptidase I

cilastatin

 Adverse effects of imipenem-cilastatin

GI distress
 Skin rash
 At very high plasma levels, CNS toxicity
 Confusion, encephalopathy, seizures

cross-allergenicity with penicillins (C, INC, Par)

Partial

 Similar to imipenem
 Not metabolized by renal dehydropeptidases
 Less likely to cause seizure

MEROPENEM

 Long half-life
 Less active against pseudomonas
 IM injection causes pain and irritation

ERTAPENEM

 Used in fixed combination with certain hydrolyzable penicillins
 Effective against plasmid-encoded beta-lactamases
 Gonococci
 Streptococci
 E. coli
 H. influenzae

beta-lactam inihibitors: CLAVULANIC ACID, SULBACTAM, and TAZOBACTAM

Bactericidal glycoprotein

VANCOMYCIN

Binds to the D-Ala-D-Ala terminal of the nascent peptidoglycan pentapeptide side chain

VANCOMYCIN

Inhibits transglycosylation

VANCOMYCIN

Prevents elongation of peptidoglycan chain

VANCOMYCIN

Interferes with cross-linking

VANCOMYCIN

spectrum of activity of vancomycin

Narrow spectrum of activity

• Rapid IV infusion of this drug may cause diffuse blushing
 “Red man syndrome”

VANCOMYCIN

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OTHER BETA-LACTAM DRUGSmonobactam

astreonam

 Resistant to beta-lactamases produced by certain gram (-) rods  Klebsiella Pseudomonas Serratia No activity against gram (+) and anaerobes

astreonam

astreonam RoA

IV

Elimination of astreonam

 Eliminated via renal tubular secretion

w/ or w/o cross-allergenicity with penicillin?

none

adverse effects of astreonam

 Adverse effects  GI upset with possible superinfection Vertigo Headache Rare hepatotoxicity Skin rash

 An inhibitor of cell wall synthesis binding to PBP3 Synergistic with aminoglycosides

astreonam

 Chemically different from penicillins  Retain the beta-lactam ring

carbapenems

the carbapenems are (3)

B. IMIPENEM, MEROPENEM, and ERTAPENEM

 Low susceptibility to beta-lactamases

carbapenems

 Wide activity against  Gram(+) cocci Gram (-) rods Anaerobes

carbapenems

RoA of carbapenems

IV

 Useful for infections caused by organisms resistant to other antibiotics

CARBAPENEMS

Drug of choice for enterobacter

CARBAPENEMS

Inactivates impinem

renal dehydropeptidase I

 Administered in combination w/impinen

cilastatin

 Increases the half-life of impinem  Inhibits formation of nephrotoxic metabolites

cilastatin

 Inhibitor of the renal dehydropeptidase I

cilastatin

 Adverse effects of imipenem-cilastatin

GI distress Skin rash At very high plasma levels, CNS toxicity Confusion, encephalopathy, seizures

cross-allergenicity with penicillins (C, INC, Par)

Partial

 Similar to imipenem Not metabolized by renal dehydropeptidases Less likely to cause seizure

MEROPENEM

 Long half-life Less active against pseudomonas IM injection causes pain and irritation

ERTAPENEM

 Used in fixed combination with certain hydrolyzable penicillins Effective against plasmid-encoded beta-lactamases  Gonococci Streptococci E. coli  H. influenzae

beta-lactam inihibitors: CLAVULANIC ACID, SULBACTAM, and TAZOBACTAM

Bactericidal glycoprotein

VANCOMYCIN

Binds to the D-Ala-D-Ala terminal of the nascent peptidoglycan pentapeptide side chain

VANCOMYCIN

Inhibits transglycosylation

VANCOMYCIN

Prevents elongation of peptidoglycan chain

VANCOMYCIN

Interferes with cross-linking

VANCOMYCIN

spectrum of activity of vancomycin

Narrow spectrum of activity

• Rapid IV infusion of this drug may cause diffuse blushing “Red man syndrome”

VANCOMYCIN

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OTHER BETA-LACTAM DRUGS
monobactam

 Resistant to beta-lactamases produced by certain gram (-) rods
 Klebsiella
 Pseudomonas
 Serratia
 No activity against gram (+) and anaerobes

 Adverse effects
 GI upset with possible superinfection
 Vertigo
 Headache
 Rare hepatotoxicity
 Skin rash

 An inhibitor of cell wall synthesis binding to PBP3
 Synergistic with aminoglycosides

 Chemically different from penicillins
 Retain the beta-lactam ring

 Wide activity against
 Gram(+) cocci
 Gram (-) rods
 Anaerobes

 Useful for infections caused by organisms resistant to other antibiotics


 Increases the half-life of impinem
 Inhibits formation of nephrotoxic metabolites

GI distress
 Skin rash
 At very high plasma levels, CNS toxicity
 Confusion, encephalopathy, seizures

 Similar to imipenem
 Not metabolized by renal dehydropeptidases
 Less likely to cause seizure

 Long half-life
 Less active against pseudomonas
 IM injection causes pain and irritation

 Used in fixed combination with certain hydrolyzable penicillins
 Effective against plasmid-encoded beta-lactamases
 Gonococci
 Streptococci
 E. coli
 H. influenzae

• Rapid IV infusion of this drug may cause diffuse blushing
 “Red man syndrome”