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160 Cards in this Set
- Front
- Back
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What form of penicillin is admin IV?
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Penicillin G
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What form of penicillin is admin orally?
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Penicillin V
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What is the mechanism of bacteria killing with penciillin?
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1. Bind pencillin-binding proteins (transpeptidase) 2. Block transpeptidase corss-linking of cell wall 3. Activate autolytic enzymes
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What is penicillin used for?
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Bactericidal for G+ cocci, G+ rods, G-cocci, and spirochetes.
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Is penicillin resistant to penicillinase?
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No
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What are the toxicities of penicillin?
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Hypersensitivity rxns, hemolytic anemia
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What are the penicillinase resistant penicillins that work the same way as penicillin?
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Methicillin, nafcillin, dicloxacillin
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What antibiotics are used to primarily target S. aureus?
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Methicillin, nafcillin, dicloxacillin
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What is the toxicity of methicillin?
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Interstitial nephritis
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What is the main toxicity of methicillin, nafcillin, and dicloxacillin?
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Hypersensitivity rxns
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What are the aminopenicillins and how do they differ from penicillins?
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Ampicillin, amoxicillin - wider spectrum, Amoxicillin has greater oral availability than ampicillin
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Which bacteria do ampicillin/amoxicillin cover?
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Haemophilus influenzae, E. coli, Listeria monocytogenes, Proteus, Salmonella, entterococci. (Ampicillin/amoxicillin HELPS kill enterococci.
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What are the toxicicities of ampicillin and amoxicillin?
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Hypersensitivities reactions; ampicillin rash; pseudomembranous colitis
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What beta lactams can be used against Pseudomonas?
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Ticarcillin, carbenicillin, piperacillin (TCP: Takes Care of Pseudomonas)
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What bacteria can Ticarcillin, carbenicillin, piperacillin be used against?
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Pseudomonas spp. and G- rods
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What beta lactams are penicillinase resistant?
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Methicillin, nafcillin, dicloxacillin
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What does clauvulanic acid do?
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Beta-lactamase inhibitor
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What are the toxicities of ticarcillin, carbenicillin, piperacillin?
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hypersensitivity reaction
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How do cephalosporins work?
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B-lactam drugs that inhibit cell walls ynthesis but are less susceptible to penicillinases
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What bacteria do 1st generation cephalosporins cover?
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Gram positive cocci, Proteus mirabilis, E. coli, Klebsiella pneumoiae (PEcK)
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What generation cephalosporin are cefazolin and cephalexin?
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1st generation
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What bacteria do 2nd generation cephalosporins cover?
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Gram + cocci, Haemophilus, Enterobacter aerogenes, Neisseria spp., Proteus mirabilis, E. coli, Klebsiella pneumoniae, Serratia marescens (HEN PEcKS)
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What generation cephalosporin are ceftriaxone, cefotaxime, and ceftazidime
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3rd generation
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What generation cephalosporin are cefoxitin, cefaclor, cefuroxime?
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2nd generation
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What bacteria do 3rd generation cephalosporins cover?
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Serious G- infections resistant to other B-lactams, meningitis (ceftriaxone)
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What are ceftazidime and cefoperazone typically used for
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Pseudomonas
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What is ceftriaxone typically used for?
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Gonorrhea and meningitis (good CSF penetration)
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What is the name of the fourth generation cephalosporin?
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Cefepime
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What is the use for cefepine?
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Increased activity against Pseudomonas and G+ organism, otherwise same as 3rd generation
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What are the toxicities of cephalosporins?
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Hypersensitivity reactions. Cross-hypersensitivity with penicillins occur in 5-10% of patients. Increased nephrotoxicitiy of aminoglycosides; Disulfiram like rxn with ethanol
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What are aztreonams and how do they work?
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Monobactam resistant to B-lactamases. Inhibit cell wall synthesis by binding to pencillin binding protein.
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How are aztreonams different from cephalosporins int erms of toxicity
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No cross-allergenicitiy with penicillins
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What are aztreonams used for?
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G- rods: Klebsiella, Pseudomonas, Serratia (magic bullet for G- aerobic bacteria)
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What monobactam has no activity against G+ or anaerobes?
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Aztreonam
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What are the toxicities associated with aztreonam use?
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Usually nontoxic; occasional GI uspet. No cross-allergenicitiy with penicillins.
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Patients who cannot tolerate what drugs for what reasons use aztreonam?
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Penicillin-allergic; Renal insufficiency = cannot tolerate aminoglycosides
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What are the carbapenems?
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Imipenem/cilastatin and Meropenem
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What is the function of cilastatin?
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Inhibitor of renal dihydropeptidase I which inactivates imipenem
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What is the drug of choice for Enterobacter?
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Imipenem/cilastatin, meropenem
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What bacteria do the carbapenems (imipenem/cilastin, meropenem) cover?
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Broadest coverage! Gram + cocci, G- rods, and anaerobes
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What are the toxicities of the carbapenems? Name the carbapenems
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Imipenem/cilastin, meropenem. GI distress, skin rash, and CNS toxicity (seizures - lowers seizure threshold; Meropenem has a reduced risk of seizures)
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When would it be appropriate to use imipenem/cilastin or meropenem?
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Only with life-threatening infections or after other drugs have failed - because of significant side effects
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How does vancomycin work?
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Inhibits cell wall mucopeptide formation by binding D-ala D-ala portion of cell wall precursors.
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How does vancomycin resistance occur?
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Amino acid change of D-ala D-ala to D-ala D-lac
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What is vancomycin used for?
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Serious, gram positive multidurg-resistant organisms, including S. aureus, MRSA, enterococci and C. difficile (pseudomembranous colitis)
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What are the toxicities of vancomycin?
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Nephrotoxicity, ototoxicity, thrombophlebitis, diffuse flushing - "red man syndrome" (can largely be prevented by pretreatment with antihistaqmines and slow infusion rate) Well tolerated in general - does NOT have many problems
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What are the names of the aminoglycosides?
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Gentamicin, Neomycin, Amikacin, Tobramycin, Streptomycin "Mean" GNATS canNOT kill anaerobes (NOT = toxicities)
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Are aminoglycosides bactericidal or bacterialstatic?
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bactericidal
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How do aminoglycosides work and what do they require to work?
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Inhibit the formation of initiation complex at 30s and cause misreading of mRNA. Requires O2 for uptake so ineffective against anaerobes
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What is Amikacin, Gentamicin and the res tof the drugs in its class used for? What class of drugs are these?
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Aminoglycosides. Used for severe gram-negative rod infections. Ineffective against anaerobes
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What class of drugs is Tobramycin and the rest of the drugs in its class synergistic with?
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B-lactam antibiotic
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What is used in bowel surgery?
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Neomycin
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Aminoglycosides are nephrotoxic esp. when used with what? Aminoglycosides are ototoxic esp. when used with what?
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Cephalosporins; loop diuretics
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What are the toxicities of Gentamicin, Tobramycin and the rest of the drugs in this class?
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Nephrotoxicity (esp. with cephalosporins), Ototoxicity (esp. with loop diuretics), Teratogen
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What are the names of the main tetracyclines?
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Tetracycline, doxycycline, demeclocycline, minocycline
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Besides being an antibiotic, what other role does demeclocycline play?
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ADH antagonist; acts as a diuretic in SIADH
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How is doxycycline eliminated and what is special about this?
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Fecally eliminated and can be used in pts with renal failure; Also chelates cations poorly so can be taken with food
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How do tetracyclines work?
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Bind to 30s and prevent attachment of aminoacyl-tRNA
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Tetracyclines must not be taken with what and why
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NOT with milk, antacids, or iron-containing preparations because divalent cations inhibit its absorption in the gut
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What organisms are tetracyclines used for?
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Sexually transmitted to animal transmitted! Vibrio cholerae, Acne (doxycycline). Chlamydia, Ureaplasma Urealyticum (family Mycoplasmatacae - normal genital flora), Mycoplasma penumoniae, Tularemia, H. pyloria, Borrelia burgdorferi, Rickettsia (VACUUM THe BedRoom)
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What are the toxicities of tetracyclines?
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GI distress, discoloration of teeth and inhibition of bone growth in children, photosensitivity (chelation of Ca++), contraindicated in pregnancy
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What are the macrolides?
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Erythromycin, Azithromycin, Clarithromycin
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How does erythromycin and the rest of the antibiotics in its class work? what are these other antibiotics?
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Erythromycin, azithromycin, clarithromycin. Inhibit protein synthesis by blocking translocation; bind to the 23S rRNA of the 50S ribosomal subunit
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What is the clinical use of the macrolides?
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URIs, pneumonias, STDs - G+ cocci (strept infections in patients allergic to penicillin), Mycoplasma, Legionella, Chlamydia, Neisseria
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What are the toxicities of the macrolides?
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GI discomfort (most common cause of noncompliance),. acute cholestatic hepatitis (rare), eosinophilia, skin rashes. Increases serum concentration of theophyllines, oral anticoagulants
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What is the mechanism of chloramphenicol? Bacteriostatic or bacteriocidal
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Inhibits 50S peptidyltransferase activity. Bacteriostatic
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What are the clinical uses of chloramphenicol?
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Meningitis (H. influenze, N. meningitidis, Strept pneumoniae - good penetration of CNS), young children and prenant women with Rocky Mtn. Fever who can't use tetracyclines
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What are the toxicities of chloramphenicol?
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Anemia (dose dependent), aplastic anemia (dose independent), gray baby syndrome (in premature infants because they lack liver UDP-glucuronyl transferase)
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What drug is responsible for grey baby syndrome and what are its signs?
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Chloramphenicol. Vasomotor collapse (shock), abdominal distention, and cyanosis (grey)
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What is the mechanism of clindamycin?
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Blocks peptide bond formation at 50S ribosomal subunit. Bacteriostatic
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What is the clinical use of clindamycin?
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Treat anaerobic infections (Bacteroides fragilis, Clostridium perfringens)
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What are the toxicities of clindamycin?
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Pseudomembranous colitis (C. difficile overgrowth), fever, diarrhea
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Name three common sulfonamides used
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Sulfamethoxazole (SMX), sulfisoxazole, sulfadiazine
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What is the mechanism of Sulfonamides?
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PABA antimetabolites inhibit DIHYDROPTEROATE SYNTHASE
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Are sulfonamides bacteriocidal or bacteriostaic?
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Bacteriostatic
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What bacteria is sulfisoxazole used for?
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G+, G-, Nocardia, Chlamydia
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What is used for simple UTI from sulfonamide class?
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Triple sulfas or SMX for simple UTI
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What are the toxicities for the class of drugs sulfamethoxazole is in?
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Hypersensitivity rxns, hemolysis if G6PD deficient, nephrotoxicity, (tubulointerstitial nephritis), photosensitivity, kernicterus in infants, displace other drugs from albumin (warfarin)
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What is kernicterus?
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Displacement of bilirubin from binding sites on serum albumin so deposits and damage to brain centers of infants
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What class of antibiotics inhibits dihydropteroate synthase?
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Sulfonamides
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What class of drugs inhibits dihydrofolate reductase?
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Trimethoprim
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How does trimethoprim work?
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Inhibits dihydrofolate reductase. DNA/RNA cannot be formed
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What class of drugs is often used in combination with trimethoprim?
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Sulfonamides (trimethoprim-sulfamethoxazole [TMP-SMX]), causing sequential block of folate synthesis.
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What is the combination of TMP-SMX used for?
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Recurrent UTIs, Shigella, Salmonella, Pneumocystis jiroveci pneumonia
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What are the toxicities of Trimethoprim and what can they be alleviated by?
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megaloblastic anemia, leukopenia, granulocytopenia. Supplemental folinic acid
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Name typical sulfa drugs
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Sulfasalazine (GI drug for UC and Crohn's), Sulfonylureas, Thiazides, Acetazolamide, or Furosemide
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Name some common fluoroquinolones?
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Ciprofloxacin, norfloxacin, ofloxacin, sparfloxacin, moxifloxacin, gatifloxacin, enoxacin
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Name a common quinolone
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Nalidixic acid
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What is the mechanism of floroquinolones
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Inhibits DNA gyrase (topoisomerase II).
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Are ciprofloxacin and gatifloxacin and the restof the drugs in its class bactericidal or bacteriostatic
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Bacteriacidal
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What must fluoroquinolones not be taken with?
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Antacids
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What two class of antibiotics should nOT be taken with antacids?
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Fluoroquinolones and Tetracyclines
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Why is ciprofloxacin contraindicated in pregnant women and children?
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Causes damage to cartilage
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What are the toxicities of ofloxacin and norfloxacin
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GI upset, superinfections, skin rashes, headache, dizziness. Tendonitis and tendon rupture in adults; leg cramps and myalgias in kids (fluroquinoLONES hurt attachments to your BONES)
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How does metronidazole work?
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Forms toxic metabolites in the bacterial cell that damages DNA
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What bactericidal and antiprotozoal agent forms toxic emtabolites in bacteria that damage DNA?
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Metronidazole
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What organisms is metronadazole used with?
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Giardia, Entamoeba, Trichomonas, Gardnerella vaginalis, Anerobes (Bacterioides, Clostridium). Used with bismuth and amoxicillin (or tetracycline) for "triple therapy" against H. Pylori
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What agent is used with bismuth and amoxicillin (or tetracycline) for "triple therapy" against H. Pylori
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Metronidazole
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What antibacterial agents are cationic, basic proteins that act like detergents, binding to cell membranes and disrupting bacteria's osmotic properties?
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Polymyxins
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What are polymixin B and polymixin E used for?
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Resistant G- infections
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What are the toxicities of polymyxins?
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Neurotoxicity, acute renal tubular necrosis
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What drug can be used prophylaxtically against M. tuberculosis?
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Isoniazid
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What are the toxicities of metronidazole?
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Disulfiram-like rxn with alcohol; headache, metallic taste. Contra: pregnancy --> mutagenesis
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What drug can be used prophylactically against M. avium-intracellulare?
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Azithromycin
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What are the first line anti-TB drugs?
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Streptamycin, Pyrazinamide, Isoniazid (INH), Rifampin, Ethambutol (INH-SPIRE)
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What is a second line drug for TB?
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Cycloserine
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What is an important side effect of Ethambutol?
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Optic neuropathy (red-green color blindness)
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What is an important side effect for Pyrazinamide, Isoniazid, and Rifampin?
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Hepatotoxicity
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How does isoniazid work?
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Decreased synthesis of mycolic acids.
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What are the toxicities of isoniazid and how can they be prevented?
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Neurotoxicity, Hepatotoxicity. Pyridoxiine (vit B6) can help prevent neurotoxicity
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How does Rifampin work?
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Inhibits DNA dependent RNA polymerase
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What are the clinical uses for rifampin?
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Mycobacterium tuberculosis, delays resistance to dapsone when used for leprosy. Used for meningococcal prophylaxis and chemprophylaxis in contacts of children with Haemophilus influenzae type B
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What are the toxicities of Rifampin?
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Minor hepatotoxicity and drug interactions (inc. P-450); orange body fluids (nonhazardous side effect)
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4 Rs of Rifampin?
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RNA polymerase inhibitor, Revs up microsomal P-450, Red/orange body fluids, Rapid resistance if used alone
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What is the most common mechnism of penicillin or cephalosporin resistance?
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B-lactamase cleavage of B-lactam ring, or altered PBP in cases of MRSA or penicillin resistance S. pneumoniae
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What is the most common mechnism of aminoglycoside resistance?
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Modification via acetylation, adenylation, or phosphorylation
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What is the most common mechanism of vancomycin resistance?
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Terminal D-ala of cell wall component replaced with D-lac; decreased affinity
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What is the most common mechanism of chloramphenicol resistance?
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Modification via acetylation
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What is the most common mechanism of macrolide resistance?
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Methylation of rRNA near erythromycin's ribosome-binding site
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What is the most common mechanism of tetracycline resistance?
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Decreased uptake or increased transport out of cell
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What is the most common mechanism of sulfonamide resistance?
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Altered enzyme (bacterial dihydropteroate synthase), decreased uptake, or increased PABA synthesis
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What is the most common mechanism of resistance to quinolones?
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Altered gyrase or reduced uptake
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What is used for prophylaxis against meningococcal infection?
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Rifampin (rx of choice), minocycline
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What is used for prophylaxis against gonorrhea?
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Ceftriaxone
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What is used for prophylaxis against syphilis?
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Benzathine penicillin G
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What is used for prophylaxis against history of recurrent UTIs?
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TMP-SMX
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What is used for prophylaxis against Pneumocystis jiroveci pneumonia?
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TMP-SMX (rx of choice), aerosolized pentamidine
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What is used for prophylaxis against endocarditis with surgical or dental procedures?
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Penicillins
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What is used for MRSA?
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Vancomycin
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What is used for VRE?
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Linezolid and streptogramins (quinupristin/dalfopristin)
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What components make up streptogramins and what are their functions?
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Quinupristin - binds to 50s, prevents elongation of polypeptide. Dalfopristin - changes conformation of 50s, enhancing binding of Quinupristin
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What is the mechanism of Amphotericin B?
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Binds ergosterol (unique to fungi)'; forms membrane pores that allow leakage of electrolytes
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What two antifungals bind to ergosterol, disrupting fungal membranes?
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Amphotericin B and Nystatin
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What is Amphotericin B used for?
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Wide spectrum of systemic mycoses: Cryptococcus, Blastomyces, Coccidioides, Aspergillus, histoplasma, Candida, Mucor (systemic mycoses).
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How is amphotericin used for fungal meningitis?
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Injected intrathecally - does not cross blood-brain barrier
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What are the toxicities of amphotericin B? What cna reduce toxicities?
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Fever/chills ("shake and bake"), hypotension, nephrotoxicity, arrhythmias, anemia, IV phlembitis. Hydration and liposomal amphotericin reduce toxicity
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What is the mechanism of nystatin?
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Binds to ergosterol, disrupting fungal membranes. Too toxic for systemic use.
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What is the clinical use of nystatin?
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"Swish and swallow" for oral candidais; topical for diaper rash or vaginal candidiasis
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What are the most common azoles?
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Fluconazole, ketoconazole, clotrimazole, miconazole, itraconazole, voriconazole
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What is the mechanism of azoles?
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Inhibits fungal sterol (ergosterol) synthesis from lanosterol.
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What is fluconazole used for?
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Systemic mycoses. Cryptococcal meningitis in AIDS ptients (can cross blood-brain barrier) and candidal infections of all types (yeast infections)
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What azoles are used primarily for topical fungal infections?
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Clotrimazole and miconazole
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What endocrine effect does Ketoconazole have? What can ketoconazole used for clinically because of this?
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Ketoconazole blocks human gonadal and adrenal steroid synthesis leading to decreased testosterone and cortisol production. can be used for hypercortisolism (Cushing's)
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What are the toxicities of ketoconazole?
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Hormone synthesis inhibition (gynecomastia), liver dysfunction (inhibits cytochrome P-450), fever, chills
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What are the benefits of fluconazole comapred to ketoconazole?
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Fluconazole has no endocrine effects and penetrates into the CSF well
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How does flucytosine work?
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It is converted to 5-fluorouracil, inhibits thymidylate synthase and inhibits DNA synthesis
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What is flucytosine used for clinically?
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Systemic fungal infections (Candida, Cryptococcus) in combo with amphotericin B
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What are the toxicities of flucytosine
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Nausea, vomiting, diarrhea, bone marrow suppression - reversible neutropenia and TCP
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What is the mechanism of caspofungin?
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Inhbits cell wall synthesis by inhibiting synthesis of B-glucan
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What is the clinical use of caspofungin?
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Invasive aspergillosis
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What are the toxicities of caspofungin?
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GI upset, flushing
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What is the mechanism of terbinafine?
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Inhibits the fungal enzyme squalene epoxide
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What antifungal inhbits the enzyme squalene epoxide?
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Terbinafine
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Clinical use of terbinafine
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Used to treat dermatophytoses (esp. onychomycosis)
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What is the mechanism of griseofulvin?
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Interferes with microtubule function; disrupts mitosis.
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Griseofulvin forms deposits in
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Keratin containing tissues
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What antifungal interferes with microtubule function and disrupts mitosis?
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Griseofulvin
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What is griseofulvin used for?
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Oral treatment of superficial infections; inhibits growth of dermatophytes (tinea, ringworm)
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What antifungal is an oral treatment for superficial infections and inhibits the growth of drmatophytes?
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Griseofulvin
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What are the toxicities of griseofulvin?
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Teratogenic, carcinogenic, confusion, headaches, Increased P-450, and Increased warfarin metabolism
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