beta-lactam inhibitors - others Flashcards
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
• Eliminated unchanged in urine
VANCOMYCIN
RoA of vancomycin
IV
penetrates most tissues
VANCOMYCIN
• Toxic effects of vancomycin
Chills Fever Phlebitis Ototoxicity Nephrotoxicity
• Toxic effects of vancomycin
Chills Fever Phlebitis Ototoxicity Nephrotoxicity
Antimetabolite inhibitor of cytosolic enolpyruvate transferase
B. FOSFOMYCIN
Prevents the formation of N- acetylmuramic acid which is essential in peptidoglycan chain formation
B. FOSFOMYCIN
Resistance occurs via decreased intracellular accumulation of the drug
B. FOSFOMYCIN
Excreted in the kidney with urinary levels exceeding the minimum inhibitory concentration (MIC) for many urinary tract pathogens
B. FOSFOMYCIN
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
Diarrhea is common
Synergistic with beta-lactam and quinolones in specific infections
B. FOSFOMYCIN
Peptide antibiotic
Interferes with a late stage in cell wall synthesis in gram (+) organisms
Marked toxicity
Limited to topical use only
C. BACITRACIN
RoA of bacitracin
Topical
Antimetabolite
D. CYLCOSERINE
Blocks the incorporation of D-Ala into the pentapeptide side chain of the peptidoglycan
D. CYLCOSERINE
Used only in TB caused by organisms resistant to first-line antituberculous drugs
D. CYLCOSERINE
Potentially neurotoxic
Tremors
Seizure
Psychosis
D. CYLCOSERINE