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Pharm Test 6
Antimicrobials
57
Pharmacology
Graduate
03/24/2010

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Term
An example of a post therapy superinfection
Definition
Clostridium difficile-Associated Diarrhea CDAD
Term
Antimicrobial mechanisms of action (General)
Definition
1) Antifolates (sulfonamides, trimethoprim)
2) Inhibitors of cell wall synthesis (penicillins, cephalosporins, bacitracin, and vancomycin)
3) altering permeability of cell membrane (miconazole, nystatin, clotrimazole)
4) inhibitors of protein synthesis (chloramphenicol, aminoglycosides, tetracyclines, macrolides)
5) inhibitors of nucleic acid synthesis (fluoroquinolones, metrondizaole)
Term
Prophylactic Antimicrobial drugs used in what 3 settings?
Definition
1) protect against specific organisms that they have been or will be exposed
2) prevention of secondary infections
3) prevent infections from various surgical procedures
Term
bactericidal antibiotics
Definition
1) penicillins
2) chephalosporins
3) aminoglycosides
4) vancomycin
Term
bacteriostatic antimicrobials
Definition
1) tetracyclines
2) clindamycin
3) macrolides
4) chloramphenicol
5) sulfonamides
Term
rifampin causes what interaction with OTC
Definition
induces hepatic CYP 450 enzymes
Term
tetracycline causes what OTC interaction?
Definition
interferes with enterohepatic circulation of estrogen
Term
Sulfonamide mechanism of action
Definition
competitive antagonist of PABA (necessary for folic acid synthesis)- this inhibits cell growth
Term
1-2) suflonamide Action
3) contraindicated in?
Definition
1) bacteriostatic
2) Broad Spectrum of Activity
3) pregnancy/infants
Term
sulfonamides compete with what protein?
Definition
Bilirubin a plasma protein, decrease in folic acid can cause high levels in infants causing neural tube defects
Term
sulfonamide excretion
Definition
excreted unchanged in glomerular filtration-good to treat UTI's
Term
1) serious side effects of Sulfonamides
2) how is it overcome?
Definition
1) crystalline aggregates in urine
2) introduction of more acid-soluable form (sulfisoxazole (Gantrisin))
Term
Sulfmethoxazole-Trimethoprim Combination
-Co-trimoxazole (Bactrim, Spetra)
Definition
effect is additive and synergistic, blocks PABA conversion into DNA at two points
Term
co-trimoxazole therapeutic uses (broader then sulfonamides)
Definition
1) chronic/reccurent UTIs
2) Penumocystis
3) Otitis Media
4) bacterial respiratory tract infections
5) prostate infections
Term
nitrofurantoin (Macrodantin, Furadantin)
Definition
Urinary Tract Antiseptic that is effective in sulfonamides are not
Term
Antibacterial spectrums of Pen G, Pen V, and penicillinase-resistant penicillins. What organisms do they affect?
Definition
narrow spectrum, effect mainly gram-positive organisms
Term
Pencillin mechanism of action
Definition
blocks cell wall synthesis by inhibiting step in cross-linking of peptidoglycan strands.
Term
primary basis for pencillin resistance?
Definition
production of penicillinase (beta lactamase)
Term
1) Pen G -administered?
2) Pen V - administered?
3) Amoxicillin -spectrum?
Definition
1) parentally, food/gastric acid interferes w/absorption
2) administered orally
3) extended spectrum
Term
effect of probenecid on penicillin?
Definition
blocks kidney tubular secretory mechanisms and prolongs duration of action of penicillin
Term
dicloxacillin (Methocillin)
1) resistance?
Definition
Penicillin family, MRSA (penicillinase resistant)
Term
common penicillin toxicity?
Definition
cation intoxication, hypersensitivity, safe in pregnancy
Term
Cephalosporin generations
Definition
1) 1st generation-similar to penicillinase resistant penicicllins but provides slight gram-negative protection
2) 2nd-best anaerobe coverage of all cephalosporins
3) 3rd-oral provide no anaerobe coverage
4) 4th-some gram-positive activity, value unknown
Term
cephalosporin mechanism of action
Definition
same as penicillin
Term
cephalosporin toxicities
Definition
1) Hypersenstivity similar to penicillin-some cross rxn does occur-1st gen.
2) gastrointestional complaints (superinfections)
3) disulfram-like rxn
Term
Gonorrhea drug of choice?
Definition
ceftriaxone (Rocephin)
Term
Clavulanic Acid
Definition
1) Beta-lactamase inhibitor
2) Extends spectrum of activity for penicillin
3) Combined w/amoxicillin as oral preperation (Augmentin)
Term
Vancomycin (Vancocin)
1) use
2) Mechanism of Action
3) Toxicities
Definition
1) for severe infections, use should be limited, oral-clostridium
2) inhibits cell wall synthesis (bactericidal)
3) red Neck, Red Man- rapid IV infusion-histamine release
Term
Erythromycin
1) class
2) Spectrum
Definition
1) Macrolide Antibiotic
2) primarily bacteriostatic, limited spectrum similar to penicillin, active against chlamydia, mycoplasm, and legionella
Term
1) erythromycin that causes live toxicities?
2) Erythromycin that is not affected by food?
Definition
1) erythromycin estolate (llosone)
2) erythromycin ethylsuccinate (E.E.S.)
Term
Erythromycin toxcities
Definition
1) cardiac arythmias
2) epigastric distres (30%)- most common in children
3) inhibits CYP450
4) drug interactions w/viagra, warfrin, and theophylline
Term
clarithromycin (Biaxin)
1) SE
Definition
Macrolide
1) same drug interactions as erythromycin, GI/abnormal taste most common complaints
Term
azithromycin (Zithromax, Z-pack)
1) SE
Definition
macrolide with long T1/2- 1 dose regimen available
1) GI discomfort, does not inactivate CYP450
Term
Clindamycin (Cleocin)
1) toxcities
Definition
Alternative to penicillin, has GI SE, widely distributed-including bone, no CNS penetration,
1) GI-colitis -with black box warning- caused by clindamycin resistant Clostiridium, treated with vancomycin
Term
tetracyclines
1) spectrum
2) Phamracokinetics
3) Toxcities
Definition
1) broadest available
2) chelation-chelates with Calcium-cannot be taken with dairy products, excreted in urine and bile
3) hepatic toxicity-pregnancy highly suceptible, Renal toxicity
Term
Doxycycline (Vibramycin)
Definition
Tetracycline, oral agent
Term
Aminoglycosides
1) Spectrum
2) Mechanism of Action
3) Toxcities
Definition
1) Broad Spectrum
2) inhibits protein synthesis, ribsomal S30 subunit
3) Ototoxicities-CNVIII, dose/time/pt related, neuromuscular blockade, nephrotoxicity
Term
fluroquinolone
1) class/spectrum
2) mechanism of action
3) Black Box Warning
Definition
1) synthetic, broad spectrum, bactericidal
2) interferes enzyme DNA gyrase
3) associated with tendinitis and tendon rupture
Term
Ciproflaxacin (Cipro)
1) Toxicities
Definition
fluroquinolone, widespread use
1) may damage growing cartilage, contraindicated in children <18 and pregnant women, increased risk for photosenstivity/photoxicity
Term
levofloxacin (Levaquin)
Definition
fluoroquinolone, respiratory fluoroquinolone, effective against streptococcus penumoniae
Term
Neomycin
1) class
2) toxicity
Definition
1) OTC topical aminoglycoside antibiotic, broad spectrum
2) if given systemic-sever toxicities, deafness, renal tubular necrosis
Term
Polymyxin B
1) class
2) Toxicity
Definition
1) OTC topical antimicrobial, limited spectrum-gram negative
2) tubular necrosis, neurotoxicities
Term
Bacitracin
1) class
2) toxicities
Definition
1) OTC topical antimicrobial, limited spectrum for gram-positive
2) severe nephrotoxicity
Term
Rx topical antibiotics
Definition
-sulfacetamide, erythromycin-opthalmic
-Mupirocin (Bactroban)
-Retapamulin (Altabax)
Term
Metronidazole (Flagyl)
1) spectrum
2) Toxicities
3) Drug Interactions
Definition
1) obligate anaerobic bacteria, bactericidal
2) Oral (Stomatitis, black tongue, metallic taste), disulfram like rxns
3) alcohol, metabolism of warfrin is inhibited, avoid w/pts on lithium
Term
isoniazid (Nydrazid)
1) use
2) Mechanism of action
3) Toxicities
Definition
1) TB treatment
2) inhibits cell wall synthesis
3) neurotoxic-give Vit. B6 to prevent, hepatotoxic
Term
Rifampin (Rifadin)
1) use
2) Mechanism of action
3) adverse rxns
Definition
1) TB treatment
2) inhibits bacterial DNA-dependent RNA polymerase
3) hepatoxicity, orange-pink color to saliva, tears, urine, and sweat
Term
One of the most common fungal infections in the US
Definition
Candida albicans
Term
Amphotericin B (Fungizone)
1) class
2) SE
Definition
1) Polyene Antifunal Agent
2) renal damage
Term
nystatin (Mycostatin)
1) class
2) SE
Definition
1) Polyene Antifunal Antibiotic, effective against candida albicans
2) bitter/foul taste
Term
Azole Antifunal mechanism of action
Definition
broad spectrum of fungi, bind to CYP-450 and inhibit formation of ergosterol
Term
miconazole (Monistat)
Definition
Azole Antifunal, imidazole group,
Term
ketoconazole (Nizoral)
Definition
Azole antifungal, imidzole group, oral use-once a day dosing
Term
clotrimazole (Mycelex, Lotrimin)
1) class
2) spectrum
Definition
1) Azole antifungal,
2) topical broad spectrum-candidiasis
Term
fluconazole (Diflucan)
Definition
trizole group, synthetic w/broad spectrum, once-a-day dosing
Term
griseofulvin (Fulvicin)
1) uses
2) long use
Definition
1) dermatomycoses, no effect on candida species
2) deposited into keratin precursor cells, keratin becomes resistant to fungal infections
Term
terbinafine (Lamisil)
1) mechanism of action
2) CYP-450 action
Definition
1) prevents ergosterol synthesis-membrane dysfunction, accumulates in keratin
2) no CYP-450 effects
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