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Flashcards in beta-lactam inhibitors - others Deck (47):
1

OTHER BETA-LACTAM DRUGS
monobactam

astreonam

2

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

astreonam

3

astreonam RoA

IV

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Elimination of astreonam

 Eliminated via renal tubular secretion

5

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

none

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adverse effects of astreonam

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

7

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

astreonam

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

carbapenems

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the carbapenems are (3)

B. IMIPENEM, MEROPENEM, and ERTAPENEM

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 Low susceptibility to beta-lactamases

carbapenems

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

carbapenems

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RoA of carbapenems

IV

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 Useful for infections caused by organisms resistant to other antibiotics

CARBAPENEMS

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Drug of choice for enterobacter

CARBAPENEMS

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Inactivates impinem

renal dehydropeptidase I

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 Administered in combination w/impinen

cilastatin

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

cilastatin

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 Inhibitor of the renal dehydropeptidase I

cilastatin

19

 Adverse effects of imipenem-cilastatin

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

20

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

Partial

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

MEROPENEM

22


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

ERTAPENEM

23


 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

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Bactericidal glycoprotein

VANCOMYCIN

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

VANCOMYCIN

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Inhibits transglycosylation

VANCOMYCIN

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Prevents elongation of peptidoglycan chain

VANCOMYCIN

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Interferes with cross-linking

VANCOMYCIN

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spectrum of activity of vancomycin

Narrow spectrum of activity

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

VANCOMYCIN

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• Eliminated unchanged in urine

VANCOMYCIN

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RoA of vancomycin

IV

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penetrates most tissues

VANCOMYCIN

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• Toxic effects of vancomycin

 Chills
 Fever
 Phlebitis
 Ototoxicity
 Nephrotoxicity

35

• Toxic effects of vancomycin

 Chills
 Fever
 Phlebitis
 Ototoxicity
 Nephrotoxicity

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 Antimetabolite inhibitor of cytosolic enolpyruvate transferase


B. FOSFOMYCIN

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 Prevents the formation of N- acetylmuramic acid which is essential in peptidoglycan chain formation


B. FOSFOMYCIN

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 Resistance occurs via decreased intracellular accumulation of the drug


B. FOSFOMYCIN

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 Excreted in the kidney with urinary levels exceeding the minimum inhibitory concentration (MIC) for many urinary tract pathogens


B. FOSFOMYCIN

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 In a single dose
 Drug is less effective than the 7-day course of treatment with fluoroquinolones
 Multiple dosing can result to resistance rapidly


B. FOSFOMYCIN

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 Diarrhea is common
 Synergistic with beta-lactam and quinolones in specific infections


B. FOSFOMYCIN

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 Peptide antibiotic
 Interferes with a late stage in cell wall synthesis in gram (+) organisms
 Marked toxicity
 Limited to topical use only

C. BACITRACIN

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RoA of bacitracin

Topical

44


 Antimetabolite

D. CYLCOSERINE

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Blocks the incorporation of D-Ala into the pentapeptide side chain of the peptidoglycan

D. CYLCOSERINE

46

Used only in TB caused by organisms resistant to first-line antituberculous drugs

D. CYLCOSERINE

47

Potentially neurotoxic
 Tremors
 Seizure
 Psychosis

D. CYLCOSERINE

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