beta-lactam: other drugs Flashcards
Is vancomycin absorbed orally?
no
Bactericidal glycoprotein
A. VANCOMYCIN
Binds to the D-Ala-D-Ala terminal of the nascent peptidoglycan pentapeptide side chain
A. VANCOMYCIN
Inhibits transglycosylation
A. VANCOMYCIN
Prevents elongation of peptidoglycan chain
A. VANCOMYCIN
Interferes with cross-linking
A. VANCOMYCIN
Spectrum of activity of VANCOMYCIN
Narrow
what is the tissue penetration of vancomycin when given IV?
Wide:Penetrates most tissues
Drug that is eliminated unchanged in urine
vancomycin
• Rapid IV infusion of vancomycin may cause diffuse blushing called
“Red man syndrome”
Cause of “Red man syndrome”
Rapid IV infusion of vancomycin
Toxic effects of vancomycin
Chills Fever Phlebitis Ototoxicity Nephrotoxicity
Antimetabolite inhibitor of cytosolic enolpyruvate transferase
fosfomycin
Prevents the formation of N- acetylmuramic acid which is essential in peptidoglycan chain formation
fosfomycin
fosfomycin Prevents the formation of ————– which is essential in peptidoglycan chain formation
N- acetylmuramic acid
essential in peptidoglycan chain formation
N- acetylmuramic acid
In a single dose, drug is less effective than the 7-day course of treatment with fluoroquinolones
fosfomycin
Multiple dosing of this drug can result to resistance rapidly
fosfomycin
Diarrhea is common with this drug
fosfomycin
common toxicity of fosfomycin
diarrhea
fosfomycin is synergistic with (2) drugs in specific infections
beta-lactam and quinolones
Excreted in the kidney with urinary levels exceeding the minimum inhibitory concentration (MIC) for many urinary tract pathogens
fosfomycin
mode of excretion for fosfomycin
kidney
Resistance to this drug occurs via decreased intracellular accumulation of the drug
fosfomycin
Peptide antibiotic
C. BACITRACIN
Interferes with a late stage in cell wall synthesis in gram (+) organisms
C. BACITRACIN
Limited to topical use only
C. BACITRACIN
toxicity of bacitracin
nephrotoxicity
Antimetabolite
cycloserine
Blocks the incorporation of D-Ala into the pentapeptide side chain of the peptidoglycan
cycloserine
Used only in TB caused by organisms resistant to first-line antituberculous drugs
cycloserine
2nd line anti-TB drugs
cycloserine
Potentially neurotoxic
Tremors
Seizure
Psychosis
cycloserine
Used in fixed combination with certain hydrolyzable penicillins
Effective against plasmid-encoded beta-lactamases
CLAVULANIC ACID, SULBACTAM, and TAZOBACTAM
carbapenem with
Long half-life
Less active against pseudomonas
IM injection causes pain and irritation
ERTAPENEM
Similar to imipenem
Not metabolized by renal dehydropeptidases
Less likely to cause seizure
MEROPENEM
advantage of meropenem to imipenem
Not metabolized by renal dehydropeptidases
Less likely to cause seizure
Rapidly inactivated by renal dehydropeptidases I
imipenem
enzyme that inactivates imipenem
renal dehydropeptidases I
Administered in combination imipenem
Inhibits formation of nephrotoxic metabolites
Cilastatin
Inhibitor of the enzyme renal dehydropeptidases I
cilastatin
Increases the half-life of imipenem
Cilastatin
Adverse effects of imipenem-cilastatin
GI distress
Skin rash
At very high plasma levels, CNS toxicity
Confusion, encephalopathy, seizures
drug of choice for enterobacter
imipenem
Chemically different from penicillins
Retain the beta-lactam ring
carbapenems
Low susceptibility to beta-lactamases
carbapenems
Wide activity against
Gram(+) cocci
Gram (-) rods
Anaerobes
carbapenems
For pseudomonal infections
Combined with aminoglycosides
carbapenems
Useful for infections caused by organisms resistant to other antibiotics
carbapenems
RoA of carbapenems
IV
Monobactam
ASTREONAM
Resistant to beta-lactamases produced by certain gram (-) rods
ASTREONAM
No activity against gram (+) and anaerobes
ASTREONAM
An inhibitor of cell wall synthesis binding to PBP3
ASTREONAM
Synergistic with aminoglycosides
ASTREONAM
Adverse effects of astreonam
GI upset with possible superinfection Vertigo Headache Rare hepatotoxicity Skin rash
is astreonam bactericidal or bacteriostatic
?
is astreonam synergistic with aminoglycosides
yes
is astreonam nephrotoxic
no
RoA of astreonam
IV
Does astreonam have cross-allergenicity with penicillin?
none
Does imipenem have cross-allergenicity with penicillin?
yes but PARTIAL only
elimination of astreonam
renal tubular secretion
half-life of astreonam is prolonged when
if person has renal failure