Drug Mechanisms Of Action - Antimicrobials

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competitive inhibitors of dihydropteroate synthetase (PABA to dihydropteroate)

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sulfonamides

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these are polypeptide antibiotics that form pores

(bind to phosphatidyl ethanolamine-rich arease of membrane)

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polymyxins (colistin)

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inhibits DNA dependent RNA polymerase and RNA synthesis

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rifampin

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block DNA gyrase

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quinolones (e.g. ciprofloxacin)

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metronidazole inhibits ______

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nucleic acid synthesis

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antibiotics to avoid in pregnancy

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Streptomycin may damage eighth cranial nerve (Vestibulocochlear)
and cause skeletal defects in the fetus

Aminoglycosides - ototoxicity

Fluroquinolones - cartilage damage

Tetracyclines - discolored teeth, inhibition of bone growth, cartaracts

Sulfonamides - kernicterus

chloramphenicol - "gray baby"

Metronidazole - mutagenesis

Griseofulvin - teratogenic

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cause liver damage

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tetracyclines and isoniazid

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inhibits P450

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Chloramphenicol

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cause nephrotoxicity

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sulfonamides, aminoglycosides, outdated tetracyclines

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cuase neurotoxicty

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massive dose of penicillin G, aminoglycosides, tetracyclines (in infants)

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toxic to bone marrow

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Chloramphenicol

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cause hemolysis of red cells in paitnets deficient in glucose-6-phosphate dehydrogenase

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sulfonamides, chloramphenicol, nitrofurantoin

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rifampin interferes with _____ and other drugs by enhancing breakdown

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birth control pills

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Chloramphenicol interferes with ___ and ___ by inhibiting breakdown.

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with phenytoin (antiepileptic) and coumadin (warfarin)

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drug interaction with seldane (terfenadine)

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erythromycin

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____ are not effective against dormant bacteria

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penicillins

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elimination time of penicillin

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30-60 min

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Methicillin (no longer available in the US)
Nafcillin
Oxacillin
Cloxacillin
Dicloxacillin

Are what kind of drugs?

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Penicillinase-resistant penicillins

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Penicillin G and penicillin V NOT effective against

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Bacteroides fragilis

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used in surgical prophylaxis

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cefazolin

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Major problem - metabolized in renal tubule. Used in conjunction with cilastatin, an inhibitor of renal dehydropeptidase - combination is known as Primaxin™.

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carbapenems (e.g. imipenem)

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major toxicity of carbapenems

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seizures

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amoxicillin + clavulanic acid =

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Augmentin

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drug that is inactivated to glucuronic acid derivative in liver

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chloramphenicol

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Chloramphenicol is given by

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oral or parenteral; rapidly absorbed from GI tract

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causes "gray baby" syndrome

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Chloramphenicol
(infants lack glucuronic acidd conjugation detoxification mechanism)

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Chloramphenicol inhibits ______; therefore, contraindication with

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P450
phenytoin and coumarin (warfarin)

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rapidly decompose at elevated temperature or pH

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tetracycline

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____ and ____ are tetracyclines that have low renal clearance

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doxcycline and minocycline

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tetracycline is given by

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mouth

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doxycycline is excreted in

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feces

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lipid soluble forms of tetracycline

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doxycycline and minocycline

(thus have longer half lives of 16-20 hours; other tetracyclines are 6-10 hrs)

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major route of elimination of tetracyclines

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urinary excretion

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Should not be given during pregnancy and up to 8 years old

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tetracyclines

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causes Phototoxic reaction: photosensitization & severe sunburn

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tetracyclines

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aminoglycosides are given _____

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parenterally (Negligible GI absorption)

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Mainly excreted as active drug through glomerular filtration

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aminoglycosides (kanamycin, amikacin, tobramycin, gentamicin, streptomycin, neomycin)

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adverse effect of aminoglycoside (esp. Neomycin)

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nephrotxicity

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causes flushing due to histamine release

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vancomycin

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adverse reactions of vancomycin

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ototoxicity and nephrotoxicity

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should not be used to treat pneumonia

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daptomycine (Pulmonary surfactant antagonizes daptomycin)

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Spectrum similar but not identical to penicillin G

Never use as sole drug to treat severe staphylococcal infections

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macrolides

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erythromycin + ______ = fatal arrythmias

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Seldane (Terfenadine) (an antihistamine)

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binds to dihydrofolate reductase

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Trimethoprim

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a PEP analog that inhibits the synthesis of NAM from NAG.

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Phosphomycin/Fosfomycin

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an analog of D-Ala and inhibits the racemase reaction and addition of D-Ala to the AA1-AA2-AA3 chain

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D-cycloserine

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binds undecaprenyl-PP and inhibits recycling of the carrier.

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Bacitracin

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binds D-Ala-D-Ala and sterically hinders PBPs from carrying out transpeptidation and transglycosylation reactions

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Vancomycin

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structurally related to D-Ala and tightly bind PBPs inhibiting their transglycosylation and transpeptidation activity.

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beta-lactams

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Polymyxins (colistin) have higher binding affinity for Gram-negative / Gram-positive bacteria

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gram negative

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novobiocin and ciprofloxacin are ___ antibiotics

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quinolones

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induces breaks in DNA

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metronidazole

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prevent the assembly of the ribosome.

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oxazolidinones Zyvox (linezolid)

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block the P-site of the ribosome

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Streptogramins

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requires a strong proton motive force to be transported (can only be used against aerobes)

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aminoglycosides

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1. N-acetylation
2. O-phosphorylation
3. O-adenylation

modifications will inactivate _____

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aminoglycosides

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can be inactivated by acetylation (acetyl transferase)

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Chloramphenicol

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MRSA (methicillin resistant S. aureus) contains a ____ gene that encodes a new beta-lactam resistant PBP (PBP2a)

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mecA