Glossary of Antimicrobials3 4-16-06

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Trimethoprim How does it work?
inhibits folic acid pathway by blocking dihydrofolate reductase which humans have as well
Trimethoprim What are its uses?
used in combo with Sulfamethoxazole (TMP-SMX) causing a sequential block of folate synthesis. Used for recurrent UTIs, Shigella, Salmonella, and prophylaxis for PCP in AIDS patients
Trimethoprim Toxicities?
Megaloblastic anemia, pancytopenia (may be alleviated with supplemental folinic acid)
Fluoroquinolones What the most famous floroquinolone?
Ciprofloxacin (treatment for Anthrax)
Fluoroquinolones How does it work?
inhibits DNA gyrase (topoisomerase II)
Fluoroquinolones What are its uses?
Gram neg rods or urinary and GI tract (incl. pseudomonas), Neisseria, some gram pos spp
Fluoroquinolones What population is contraindicated for use?
pregnancy and children
Fluoroquinolones What are its toxicities?
GI upset, superinfection, skin rashes, headache, dizziness and tendonitis and tendon rupture in adults. FluoroquinoLONES hurt attachment to BONES.
Metronidazole How does it work?
forms toxic metabolites in the bacteria. Bactericidal.
Metronidazole What are its uses?
Giardia, Entamoeba, Trichomonas
GET on the Metro

gardnerella vaginalis, Bacteroides, clostridium

Used with bismuth and amoxicillin (or tetracycline) for triple therapy against H pylori
What is the role of Metronidazole in H. pylori infection?
Used as part of triple therapy: bismuth, amoxicillin and metronidazole

Metronidazole Main toxicity?
disulfiram-like (antabuse) reaction to alcohol and headache
Which drug do you use to treat anaerobic infections above the diaphram and which for below the diaphram
anaerobes above diaphram: Clindamycin, and anaerobes below diaphram: metronidazole
Polymyxins How does it work?
disrupts osmotic properties of bacteria, acts like a detergent
Polymyxins What is it used for?
resistant gram negative infections
Polymyxins Toxicities?
neurotoxicity, acute renal tubular necrosis
Isoniazid How does it work?
decreases synthesis of mycolic acid
Isoniazid What is it used for?
MTB (mycobacterium tuberculosis). The only agent used as solo prophylaxis against TB
Isoniazid Toxicities?
Hemolysis if G6PD deficient, neurotoxicity, hepatotoxicitiy, drug induced SLE. INH, Injures Neurons and Hepatocytes
Isoniazid What vitamin prevents neurotoxicity
Vitamin B6 (pyridoxine)
Isoniazid Why are toxicities particularly important to monitor in patients taking INH?
INH half-lives are different in fast versus slow acetylators!
Rifampin How does it work?
inhibits DNA-dependent RNA polymerase
Rifampin What is it used for?
Mycobacterium tuberculosis, delays resistance to dapsone when used for leprosy, meningococcal prophylaxis
Rifampin Toxicities?
Minor hepatotoxicity and increases P-450
Rifampin How can it be used for leprosy?
rifampin delays resistance to dapsone when used for leprosy
Rifampin What would happen if you used rifampin alone?
get rapid resistance
Rifampin What does it do to bodily fluids?
makes them red/orange in color
Rifampin What are the 4 R's of Rifampin
RNA polymerase inhibitor, Revs up microsomal p-450, Red/Orange body fluids, Resistance is rapid if used alone
Anti-TB Drugs What are the anti-TB drugs?
Rifampin, Ethambutol, Streptomycin, Pyrazinamide, Isoniazid (INH) -- RESPIre
Anti-TB Drugs What do you use for TB prophylaxis?
Anti-TB Drugs What toxicity is common to all?
Most common resistance mechanism for penicillins / cephalosporins.
Beta-lactamase cleavage of beta-lactam ring.
Most common resistance mechanism for aminoglycosides.
Modification via acetylation, adenylation, or phosphorylation.
Most common resistance mechanism for vancomycin.
Terminal D-ala of cell wall component replaced with D-lac; decrease affinity.
Most common resistance mechanism for Chlorampenicol.
Modification via acetylation.
Most common resistance mechanism for macrolides.
Methylation of rRNA near erythromycin's ribosome-binding site.
Most common resistance mechanism for tetracycline.
Decrease uptake or increase transport out of cell.
Most common resistance mechanism for sulfonamides.
Altered enzyme (bacterial dihydropteroate synthetase), decrease uptake, or increase PABA synthesis.
drug of choice for prophylaxis of meningococcal infection.
Rifampin (drug of choice)
Drug of choice for gonorrhea.
Ceftriaxone. 3rd generation cephalosporin.
Drug of choice for syphilis.
Benzathine penicillin G.
Drug of choice for meningococcal infection. Drug of choice for history of recurrent UTIs.
Drug of choice for Pneumocystis carinii pneumonia.
TMP-SMX (drug of choice), aerosolized pentamindine

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