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FIU -Antibacterial Drugs 2
FIU -Antibacterial Drugs 2
24
Pharmacology
Professional
01/11/2012

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Term
Protein synthesis inhibitors
Definition
Tetracyclins; aminoglycosides; macrolides/ketolides (erythromycin); chloramphenicol; clindamycin; quinopristin and dalfopristin; linezolid
Term
Antibacterial drugs acting on 30S subunit of ribosome
Definition
aminoglycosides and tetracyclins (AT 30 years old in CEL(c)L #50)
Term
Antibacterial drugs acting on 50S subunit of ribosome
Definition
chloramphenicol; erthyromycin (macrolides); linezolid; clindamycin (AT 30 years old in CEL(c)L #50) also: quinopristin and dalfopristin
Term
PO (oral) bacterial protein synthesis inhibitors
Definition
Chloramphenicol, clindamycin, erthyromycin (macrolides), tetracyclin (NOT: aminoglycosides - large and polar)
Term
Bacterial protein synthesis inhibitors excreted through bile
Definition
azithromycin, doxycyclin, erythromycin (LiverADE)
Term
Bacterial protein synthesis inhibitors that interfere with hepatic CYP450 metabolism
Definition
Macrolides (NOT: telithromycin), chloramphenicol, fluoroquinolones
(Have a MCFlurry with your McLiver)
Term
Antibacterial drugs contraindicated with pregnancy
Definition
fluoroquinolones (cartilage damage); chloramphenicol (Gray Baby); aminoglycosides (ototoxicity); tetracclines (bone growth inhibition); sulfonamides (kernicterus)
Term
Antibacterial drugs causing photosensitivity
Definition
tetracyclins, sulfonamides and quinolones (QUeST for sun)
Term
tetracyclin cidal/static, broad/narrow, mode of action, oral?, excretion (exception), resistance, tx, SE (3)?
Definition
static; broad, at 30S: blocks A site/aminoacyl-tRNA attachment; PO; renal excretion (doxycyclin: bile), don't use if renal compromised px; resistance: active efflux, altered target (blocks tetracyclin binding site; tx: acne, rosacea (propionibacterium acnes), atypicals (mycoplasma pneumonia, chlamydia), rocky mountain spotted fever, Lyme disease, cholera; SE: 1) chelation (No milk, Ca, Mg etc - attaches to cations and can't be absorbed 2) Pregnancy Cat. D: stunted growth, permanent discoloration of teeth (also not for child < 8 or breastfeeding moms) 3)photosensitivity
Term
Demeclocyclin category, side effect, off label indication
Definition
tetracyclin; causes nephrogenic diabetes insipidus (disrupts ADH receptors); tx of SIADH (syndrome of inappropriate release of ADH), caused by some cancer tumors ilke small cell lung cancer
Term
aminoglycosides cidal/static, broad/narrow (requirement), mode of action, oral?, excretion (exception), resistance, use with?, tx, SE (5)?
Definition
cidal; aerobic gram - (require O2); at 30S: blocks association with 50S subunit, if binds after association, risrupts mRNA reading leading to toxic proteins and cell death; NOT PO (very big/polar; renal excretion; resistance: antibiotic altering/conjugating enzyme (acetyl-, nucleotidyl and phospho-transferases); synergy with beta lactan cell wall inhibitors (lets aminoglycosides in); tx: topical antibiotic (Neosporin): bacitracin (cel wall inhib.), neomycin, polymixin (cell wall more permeable); SE: amiNOglycosides 1)nephrotoxic 2) irreversible ototoxicity (cochlear and vestibular: can't perceive termination of movement) 3)paralysis (blocks NMJ, no ACh released like botulin toxin, bad for myasthenia gravis px 4) contat dermititis (neomycin only) 5) pregnancy Cat. D
Term
aminoglycoside examples
Definition
amikacin, gentamicin, netilmicin, neomycin, streptomycin, tobramycin (GNNATS! A mean guy likes!)
Term
macrolides/ketolides (erythromycin) cidal/static, broad/narrow, mode of action, oral?, excretion, resistance, tx, SE (3)?
Definition
static; broad; at 50S: inhibits translocation of peptidyl-tRNA from A to P site; PO; renal excretion - don't use if renal compromised e.g. clarithromycin (except azithromycin and erythromycin: excreted in bile, don't use if liver dysfunction); resistance: antibiotic altering (methylation) except telithromycin; tx: outpatients (lower/upper respiratory tract infections: tissue penetration good/for intracellular pathogens) also least penetration E->C->A->T most; SE: 1) Motilin agonist = GI distress 2) reversible ototoxicity 3) Interferes with hepatic metabolism (esp. 2C9 increasing warfarin action...but not telithromycin)
Term
macrolide examples
Definition
erythromycin, clarithromycin, azithromycin, telithromycin (macrolides ECAT: mad crows lie and Eat CATs).
Term
chloramphenicol cidal/static, broad/narrow, mode of action, oral?, metabolism, resistance, tx, SE (5)?
Definition
static; broad; at 50 S: inhibits peptididyl transferase and stops formation of peptide bonds (transpeptidation); PO/IV; metabolized extensively by liver (glucoronyl transferase -> makes water soluble, normally very lipid soluble and passes BBB); resistance: antibiotic altering (acetyl CoA transferase); tx: for life threatening infections like meningitis only (toxicity); SE: 1) interferes with hepatic CYP450 drug metabolism (esp. 2C9 -> increases warfarin action) 2) GI distress; 3) anemia (bone marrow toxicity) 4) Gray Baby Syndrome (because undeveloped glucoronyl transferase system -> high serum levels leading to respiratory and circulatory problems like hypothermia and cyanosis also: bbb crossed affecting CNS causing hypotonia "throw baby in pool with chlorine" 5) pregnancy cat. D and not for children
Term
clindamycin cidal/static, broad/narrow, mode of action, oral?, tx, SE?
Definition
static; anaerobic bacteria; at 50S: inhibits translocation of peptidyl-tRNA from A to P site; PO; tx: anaerobic bacteria (esp. bacteriolides fraglis); also for osteomyelitis; SE: pseudomembranous colitic caused by C. difficile (use metronidazole, vancoycin)
Term
Quinupristin and dalfopristin mode of action; tx
Definition
at 50S: blocks A site and aminoacyl-tRNA attachment; tx: VRSA, VRE (vancomycin resistant bacteria: staph/entercocci)
Term
linezolid static/cidal, mode of action, tx
Definition
static; at 50S: blocks association of 50S subunit with 30S subunit; tx: VRSA, VRE (vancomycin resistant bacteria: staph/entercocci)
Term
Inhibitors of folic acid synthesis
Definition
sulfonamides, trimethoprim
Term
purpose of folic acid
Definition
needed for DNA, RNA and protein synthesis (purine, thymine production)
Term
sulfonamides mode of action, side effects (7)
Definition
inhibits dihydropteroate synthetase conversion of pteridine/PABA to dihydropteroic acid which becomes DHF (dihydrofolic acid)...enzyme exists in bacteria only; SE: 1) Steven Johnson syndrom/skin rash (sulfur groups increase hypersensitivity) 2) crystalluria 3) phototoxicity 4) kernicterus (displaces bilirubin from serum proteins 5) bleeding (displaces warfarin from serum proteins 6) hypoglycemia (displaces K+ channel blocker/diabetes drug tolbutamide from serum proteins 7) hemolytic anemia due to oxidative stress if px deficient in glucose 6-phosphate dehydrogenase
Term
trimethoprim mode of action, other drugs with same effect, side effect
Definition
inhibition of dihydrofolate reductase conversion of DHF to THF (tetrahydrofolic acid)...in both humans and bacteria; can use pyrimethamine or methotrexate to interfere with DHF reductase for high metabolizers; SE: folate deficiency -> megaloblastic anemia (use supplement that auto converts to THF but can't enter bacteria)
Term
co-trimoxazole drugs? use? Why co-administered?
Definition
sulfonamide + trimethoprim (SMX + TMP); inhibitors of bacteria folate synthesis; 1) reduce resistance 2) synergistic effect
Term
DNA gyrase inhibitors category, ending, cidal/static, broad/narrow, mode of action; resistance; side effects (6)
Definition
fluoroquinolones, -floxacin; cidal; broad; interfere with topoisomerase II (DNA gyrase) which creates gram - negative supercoils during DNA replication and Topoisomerase IV which decatenates (separates replicated loops) by cutting, unwinding and re-ligating DNA ... "topple queen"; resistance: altered target (DNA), decreased accumulation (altered porin); SE: 1)chelation 2) NO: if pregnant (cartilage erosion) 3) tendon rupture 4) photosensitivity 5) NO: if arrthymias (QT longer) 6) interacts with hepatic drug metabolism
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