Probenecid

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Name: Probenecid

Class:

Mech.: Interferes w/renal excretion of drugs that undergo tubular secretion. Inhib. glucuronide conjugation of other drugs.

Absorption:

Distribution:

Metab.:

Excretion, t½:

Toxicity/S.E.s:

Utility:

Special Features: Decreases renal excretion of methotrexate — possible toxicity. Decreases renal excretion of penicillin.

 

Sulbactam

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Name: Sulbactam

Class: b-Lactamase Inhibitor

Mech.: inhibits some b-lactamases

Absorption:

Distribution:

Metab.:

Excretion, t½:

Toxicity/S.E.s:

Utility: Combined with ampicillin (Unasyn-sulbactam) to increase efficacy against penicillinase-producing bacteria (i.e., staph).

Special Features:

 

Clavulanic acid

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Name: Clavulanic acid

Class: b-Lactamase Inhibitor

Mech.: inhibits some b-lactamases

Absorption:

Distribution:

Metab.:

Excretion, t½:

Toxicity/S.E.s:

Utility: Combined with amoxicillin (Augmentin) to increase efficacy against penicillinase-producing bacteria (i.e., staph.)

Special Features:

 

Ticarcillin (Ticar)

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Name: Ticarcillin (Ticar)

Class: Penicillin (Extended spectrum)

Mech.: Binds to PBPs, blocks activity of transpeptidases in terminal stages of cell wall formation. Bactericidal.

Absorption: IM, IV.

Distribution: Widely distributed, little CSF unless meninges inflamed.

Metab.:

Excretion, t½: Rapidly elim. by kidneys (probenecid blocks excretion), small amt. in bile.

Toxicity/S.E.s: hypersensitivity (1-10%), superinfection., coagulation disorders.

Utility: Gram -. Effective against Pseudomonas, Proteus mirabilus, often used w/aminoglyc.

Special Features: Narrow spectrum. Resistance develops quickly.

 

Cephalothin (Keflin)

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Name: Cephalothin (Keflin)

Class: First Gen. Cephalosporin

Mech.: Binds to PBPs, blocks activity of transpeptidases in terminal stages of cell wall formation. Bactericidal.

Absorption: IV. IM rarely used due to pain.

Distribution: Poor CSF.

Metab.:

Excretion, t½:

Toxicity/S.E.s: Hypersensitivity (some cross-sensitivity to pen.), superinfection, renal damage (worse if comb. w/aminoglycs.)

Utility: Usu not DOC. Serious Klebsiella infects., strep/staph infects, some penicillinase-producing bacteria.

Special Features: Narrow spectrum. Greater gram - activity than pen. G. More gram+ activity than gram - activity. Less susceptible to b-lactamase than most penicillins.