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177 Cards in this Set
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Difference between Bactericidal and Bacteriostatic?
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Bactericidal kills bacteria
Bacteriostatic screws up their cell metabolism--->slowed growth and reproduction |
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Who are the bacteriostatic antibiotics?
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They're ECSTaTiC!
Erythromycin Clindamycin Sulfamethoxazole Trimethoprim Tetracyclines Chloramphenicol |
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Who are the Bactericidal antibiotics?
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Very Finely Proficient At Cell Murder
Vancomycin Fluoroquinolones Penicillin Aminoglycosides Cephalosporins Metronidazole |
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IV vs Oral Penicillin?
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IV = Penicillin G
oral = Penicillin V |
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MOA for Penicillin?
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Bind penicillin binding proteins
Block transpeptidase cross-linking of cell wall Activate autolytic enzymes |
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Clinical uses for Penicillin?
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Gram-Pos Cocci
Gram-Pos Rods Gram-Neg Cocci Spirochetes as long as they aren't penicillinase resistant |
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Penicillin toxicity?
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Hypersensitivity Rxns
Hemolytic anemia |
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Who are the penicillinase-resistant penicillins?
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Methicillin
Nafcillin Dicloxacillin |
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Why are they penicillinase resistant?
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They have a bulkier R group
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Clinical Use for Penicillinase Resistant penicillins?
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Staph aureus (except MRSA)
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Why is MRSA resistant?
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Altered penicillin-binding protein target site
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Adverse effects of Methicillin, nafcillin, dicloxacillin?
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Hypersensitivity rxn
Methicillin can ---> Interstitial nephritis |
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Who are the aminopenicillins?
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Ampicillin
Amoxicillin |
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What's the benefit of Ampicillin/Amoxicillin?
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Same mechanism as penicillin, but Wider spectrum.
Amoxicillin has greater oral bioavailability than ampicillin |
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How can you make Ampicillin/Amoxicillin better?
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Add clavulanic acid (penicillinase inhibitor)
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Clinical Uses for Ampicillin/Amoxicillin?
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Extended Spectrum
Picks up certain Gram Positive's and Negative's: HELPS Haemophilus influenzae E. coli Listeria monocytogenes Proteus mirabilis Salmonella and enterococci |
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Adverse effects of Ampicillin/Amoxicillin?
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hypersensitivity rxn
Ampicillin rash Pseudomembranous colitis |
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Who are the anti-pseudomonals?
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Ticarcillin
Carbenicillin Piperacillin |
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Clinical uses of Ticarcillin, Carbenicillin, Piperacillin>
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Pseudomonas and gram-neg rods
Susceptible to penicillinase so combo w/ Clav |
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Adverse Effects of Ticarcillin, Carbenicillin, Piperacillin
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Hypersensitivity rxn
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What is the point of the Cephalosporins?
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Beta-lactam drugs that inhibit cell wall synthesis but are less susceptible to penicillinases
Bactericidal |
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Who are the 1st gen cephalosporins?
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Cefazolin
Cephalexin |
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Who do cefazolin and cephalexin (1st gen) go after?
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PEcK
Proteus E. coli Klebsiella and Gram Pos Cocci |
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Who are the 2nd Gen Cephalosporins?
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Cefoxitin
Cefaclor Cefuroxime |
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Who do the 2nd gen guys go after?
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HEN PEcKS
H. influenzae Enterobacter aerogenes Neisseria spp Proteus E. coli Klebsiella Serratia marcescens |
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Who are the 3rd Gen Cephalosporins?
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Ceftriaxone
Cefotaxime Ceftazidime |
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Who do the 3rd gen guys go after?
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Serious Gram-Neg infections resistant to the other Beta-Lactams
MENINGITIS: these guys can get through BBB |
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Who are the 4th Gen Cephalosporins?
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Cefepime
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Who do the 4th Gen guys go after?
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Inc activity against Pseudomonas and Gram-Pos organisms
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Adverse Effects of Cephalosporins?
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Hypersensitivity Rxns
Inc nephrotoxicity of aminoglycosides Disulfiram-like rxn w/ booze (in those w/ methylthiotetrazole group) |
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MOA for Aztreonam?
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Monobactam resistant to Beta-Lactamases
Inhibits cell wall synthesis by binding to PBP3 Synergistic w/ aminoglycosides No cross-allergenicity w/ PCN's |
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Clinical uses of Aztreonam?
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Gram Neg Rods (kleb, pseudo, serratia)
No use on gram pos or anaerobes Use for PCN allergies and pts w/ renal insufficiency that can't tolerate aminoglycosides |
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Adverse effects of Aztreonam?
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Usually safe
Occasionally GI upset |
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Who is always given w/ Imipenem? why?
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Cilastatin
its an inhibitor of renal dihydropeptidase I --> decreased inactivation of imipenam in renal tubules |
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Mechanism of Imipenam?
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Broad spectrum, beta-lactamase resistant carbapenam
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Clinical uses of imipenam?
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Gram Pos Cocci
Gram Neg Rods Anaerobes Drug of Choice for Enterobacter Serious SE's limit use to life-threatening infections or after other drugs have failed |
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What's up w/ Meropenem?
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Reduced risk of seizures and is stable to dihydropeptidase I (so no need for cilastatin)
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Adverse Effects of Imipenem?
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GI distress
Skin Rash CNS Toxicity (seizures) at high plasma levels |
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MOA of Vancomycin?
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Inhibits cell wall mucopeptide formation by binding D-ala D-ala part of cell wall precursors
Bactericidal |
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How do you get Vancomycin resistant bugs?
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Mutation of D-ala D-ala ---> D-ala D-lac
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Uses of Vancomycin?
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Serious, Gram Pos Multidrug-resistant bugs
S. aureus C. difficile (pseudomembranous colitis) |
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Adverse Effects of Vancomycin?
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usually well tolerated
Nephrotoxic Ototoxic Thrombophlebitis Diffuse flushing = red man syndrome |
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How to prevent Red Man Syndrome?
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Slow infusion rate
PreRx w/ Antihistamines |
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Who are the Protein Synthesis Inhibitors?
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buy AT 30, CCELL at 50
30S INHIBITORS Aminoglycosides Tetracyclines 50S INHIBITORS Clindamycin, Chloramphenicol Erythromycin Lincomycin Linezolid |
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Who are the Aminoglycosides? bacteriostatic or cidal?
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GNATS
Gentamycin Neomycin Amikacin Tobramycin Streptomycin Bactericidal |
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Bacteriostatic vs Bactericidal
for the rest of the Protein synthesis inhibitors? |
Tetracyclines (static)
Clindamycin, Chloramphenicol (static) Erythromycin (static) Lincomycin (static) Linezolid (variable) |
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MOA for Aminoglycosides?
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Inhibit formation of initiation complex --->misread mRNA
Require O2 = ineffective against anaerobes |
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Indications for aminoglycosides?
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Severe Gram Neg Rods
Synergistic w/ beta-lactams Neomycin for bowel surgery |
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Adverse Effects of Aminoglycosides?
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Nephrotoxic (esp when combo'd w/ cephalosporins)
Ototoxic (esp when combo'd w/ loop diuretics) Teratogen! |
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Who are the Tetracyclines?
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Tetracycline
Doxycycline Demeclocycline Minocycline |
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MOA for Tetracyclines?
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Bind 30S and prevent attachment of aminoacyl-tRNA
Limited CNS penetration |
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Special use for Doxycycline?
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Its fecally eliminated so good for renal failure pts
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Special use of Demeclocycline?
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ADH Antagonist, so its a diuretic in SIADH
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Indications for Tetracyclines?
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VACUUM THe BedRoom
Vibrio cholerae Acne Chlamydia Ureaplasma Urealyticum Mycoplasma pneumoniae Tularemia H. pylori Borrelia burgdorferi (Lyme) Rickettsia |
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Adverse Effects of Tetracyclines?
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GI distress
Discolor teeth Inhibit bone growth in kids Photosensitivity Bad for pregnancy |
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Who are the Macrolides?
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Erythromycin
Azithromycin Clarithromycin |
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MOA for the macrolides?
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Inhibit protein synthesis by blocking translocation by binding 23S rRNA of 50S
Bacteriostatic |
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Indications for Macrolides?
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URI's
Pneumonias STDs Gram Pos Cocci for PCN allergies Mycoplasma Legionella Chlamydia Neisseria |
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Adverse Effects of Macrolides?
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GI discomfort-->noncompliance
Acute Cholestatic hepatitis Eosinophilia Skin Rashes Inc serum [ ] of theophyllines and oral anticoagulants |
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MOA of Chloramphenicol?
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Inhibit 50S peptidyltransferase activity
Bacteriostatic |
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Indications for Chloramphenicol?
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Meningitis (H. influenzae, N. meningitidis, Strep pneumoniae)
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Adverse Effects of Chloramphenicol?
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Anemia (dose dep)
Aplastic Anemia (dose indep) Gray Baby Syndrome |
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What's up w/ Gray Baby Syndrome?
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happens in premature infants b/c they lack liver UDP-glucuronyl transferase
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MOA for Clindamycin?
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Blocks peptide formation at 50S
Bacteriostatic |
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Indications for Clinadmycin?
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Rx's Anaerobe Infections (above diaphragm)
Bacteroides fragilis C. perfringens |
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Adverse Effects of Clindamycin?
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Pseudomembranous colitis (C. difficile)
Fever Diarrhea |
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Who are the Sulfonamides?
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Sulfamethoxazole (SMX, made famous by TMP)
Sulfisoxazole Sulfadiazine |
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MOA for Sulfonamides?
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PABA antimetabolites inhibit dihydropteroate synthetase
Bacteriostatic |
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Indications for Sulfonamides?
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Gram Pos
Gram Neg Nocardia Chlamydia Triple Sulfas or SMX for UTI's |
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Adverse Effects of Sulfonamides?
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Hypersensitivity Rxns
Hemolysis if G6PD def Nephrotoxic (tubulointerstitial nephritis) Photosensitivity Kernicterus in infants Displace other drugs from albumin (e.g. warfarin) |
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MOA of Trimethoprim? why's this good w/ sulfonamides?
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Inhibits Bacterial DIhydrofolate Reductase.
Its blocks another step in the same chain of rxns that is necessary for bacterial production folate needed for DNA, RNA, Proteins, etc |
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Adverse Effects of Trimethoprim?
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Megaloblastic Anemia
leukopenia Granulocytopenia may be able to alleviate these effects w/ supplemental folic acid |
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Sulfa allergies = contraindications of ?
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Sulfonamides
Sulfonylureas Sulfasalazine Thiazide Diuretics Acetazolamide Furosemide |
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Who are the Fluoroquinolones?
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Ciprofloxacin and all the other floxacin's
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MOA of Fluoroquinolones?
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Inhibit DNA Gyrase (topo II)
Bactericidal |
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Harmful Drug Interaction of Fluoroquinolones?
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DON'T TAKE W/ ANTACIDS
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Indications for Fluoroquinolones?
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Gram Neg Rods of Urinary and GI Tracts (including Pseudomonas)
Neisseria Some gram-pos's |
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Adverse Effects of Fluoroquinolones?
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GI upset
Superinfections Skin rashes HA Dizzy Not for preggers and kids b/c of cartilage damage Tendonitis and Tendon rupture in adults Leg cramps and myalgias in kids |
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MOA for Metronidazole?
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Forms toxic metabolies in bacterial cell --> DNA Damage
Bactericidal and Antiprotozoal |
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Clinical Uses for Metronidazole?
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GET GAP
Giardia Entamoeba Trichomonas Gardnererlla vaginalis Anaerobes (bacteroides, clostridium) h. Pylori |
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What else is given w/ Metronidazole for H. pylori therapy?
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Triple Therapy
Metro Bismuth Amoxicillin (or tetracycline) |
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Adverse Effects of Metronidazole?
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Disulfiram-like rxn w/ alcohol
HA Metallic taste |
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Who are the Polymyxins?
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Polymyxin B and E
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MOA for Polymyxins?
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Bind to bacterial cell membranes and disrupt osmotic properties
Act like detergents |
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Indications for Polymyxins?
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Resistant Gram-Neg Infections
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Toxicity for Polymyxins?
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Neurotoxic
Acute Renal Tubular Necrosis |
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Who are the Mycobacteria?
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M. tuberculosis
M. avium-intracellulare M. leprae |
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Prophylaxis for M. tuberculosis?
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Isoniazid
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Rx for M. tuberculosis?
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RIPE
Rifampin Isoniazid Pyrazinamide Ethambutol |
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Prophylaxis for M. avium-intracellulare?
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Azithromycin
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Rx for M. avium-intracellulare?
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Azithromycin
Rifampin Ethambutol Streptomycin |
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Prophylaxis for M. leprae?
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N/A
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Rx for M. leprae?
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Dapsone
Rifampin Clofazimine |
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2nd line therapy for TB?
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Cycloserine
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Important SE of Ethambutol?
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Optic Neuropathy (red-green color blindness)
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General SE's of other TB drugs
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hepatotoxic
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MOA for Isoniazid?
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Dec Synthesis of Mycolic Acids
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SE's of Isoniazid?
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Neurotoxic
Hepatotoxic |
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How can you prevent Isoniazid neurotoxicity?
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Pyridoxine (B6)
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MOA for Rifampin?
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Inhibits DNA-Dep RNA polymerase
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Besides TB, what else is Rifampin used for?
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Delays resistance to dapsone in leprosy
Meningococcal prophylaxis and chemoprophylaxis in contacts of kids w/ H. influenzae type B |
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Adverse Effects of Rifampin?
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Minor hepatoxicity and drug interactions (Inc P-450)
Orange Body fluids (benign) |
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Four R's 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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Mechanisms of Resitance
PCN/Cephalosporins? |
1. Beta-Lactamases cleave beta-lactam ring
2. Altered PBP (MRSA) |
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Mechanisms of Resitance
Aminoglycosides? |
Modification via acetylation, adenylation, or phosphorylation
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Mechanisms of Resitance
Vancomycin? |
Terminal D-ala replaced w/ D-lac
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Who are the Nonsurgical Antimicrobial Prophylaxis for Menigococcal infection?
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Rifampin (#1)
maybe minocycline |
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Who are the Nonsurgical Antimicrobial Prophylaxis for Gonorrhea?
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Ceftriaxone
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Who are the Nonsurgical Antimicrobial Prophylaxis for Syphilis?
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Benzathine PCN G
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Who are the Nonsurgical Antimicrobial Prophylaxis for recurrent UTI's?
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TMP-SMX
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Pneumocystis jiroveci pneumonia?
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TMP-SMX
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Who are the Nonsurgical Antimicrobial Prophylaxis for endocarditis w/ surgical or dental procedures?
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PCN's
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Rx for MRSA?
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Vancomycin
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Rx for VRE?
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Linezolid and Streptogramins (quinupristin/dalfopristin)
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MOA for Amphotericin B?
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Binds Ergosterol (unique to fungi)--->membrane pores allowing leakage of electrolytes
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Clinical uses of Amp B?
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SYSTEMIC MYCOSES
Cryptococcus Blastomyces Coccidioides Aspergillus Histoplasma Candida Mucor Intrathecally for meningitis b/c it doesn't cross BBB |
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Adverse Effects of Amp B?
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Fever/Chills
Hypotension Nephrotoxic Arrhythmias Anemia IV phlebitis |
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Ways to reduce toxicities of Amp B?
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hydration reduces nephrotoxicity
Liposomal amphotericin reduces toxicity |
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MOA of Nystatin?
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Binds ergosterol, disrupting membrane
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Clinical uses for Nystatin?
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Too toxic for systemic use
Swish and swallow for oral Candidiasis Topical for diaper rash or vaginal candidiasis |
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Who are the Azoles?
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Fluconazole
Ketoconazole Clotrimazole Miconazole Itraconazole Voriconazole |
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MOA for Azoles?
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Inhibit fungal sterol (ergosterol) synthesis
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General Clinical uses for Azoles?
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Systemic Mycoses
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Clinical uses for Fluconazole?
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Cryptococcal meningitis in AIDS pts (it can cross BBB)
Candidal infections of all types |
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Clinical uses for Ketoconazole?
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Blastomyces
Coccidioides Histoplasma Candida Hypercortisolism |
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What are Clotrimazole and Miconazole used for?
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Topical Fungal Infections
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Toxicity of Azoles?
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Hormone Synthesis Inhibition (gynecomastia)
Liver Dysfunction (inhibit P-450) Fever Chills |
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MOA for Flucytosine?
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Inhibits DNA synthesis by conversion of 5-fluorouracil
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Uses for Flucytosine?
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Systemic fungal infections (candida, cryptococcus) in combo w/ Amp B
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Adverse Effects of Flucytosine?
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N&V
Diarrhea Bone Marrow Suppression |
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MOA for Caspofungin?
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Inhibits cell wall synthesis by inhibiting synthesis of Beta-glucan
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Uses for Caspofungin?
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Invasive aspergillosis
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Toxicity for Caspofungin?
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GI Upset
Flushing |
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MOA for Terbinafine?
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Inhibits fungal enzyme squalene epoxidase
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Uses for Terbinafine?
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Rx Dermatophytes (esp onychomycosis)
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MOA for Griseofulvin?
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Interferes w/ microtubule fxn
Disrupts mitosis Deposits in keratin-containing tissues (nails) |
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Uses for Griseofulvin?
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Oral Rx for superficial infections
Inhibits growth of dermatophytes (tinea, ringworm) |
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Toxicity of Griseofulvin?
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Teratogen
Carciogenic Confusion HA Inc P-450 and warfarin metabolism don't ever prescribe... |
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MOA for Amantadine?
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Blocks viral penetration and UNCOATING (M2 protein)
May buffer pH of endosome Causes dopamine release from intact nerve terminals |
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Clinical uses for Amantadine?
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Prophylaxis and Rx for Influenza A
Parkinson's Disease |
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Toxicity of Amantadine?
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Ataxia
Dizziness Slurred Speech i.e. drunk or cerebellar... |
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Mech or resistance for amantadine?
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Mutated M2 protein
90% of Influenza A strains are resistant |
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Alternate to Amantadine? usefulness?
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Rimantidine
Derivative w/ fewer CNS SE's b/c it doesn't cross BBB |
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MOA for Oseltamivir and Zanamivir?
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Inhibit influenza neuraminidase--->dec release of progeny
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Clinical uses for Oseltamivir and Zanamivir?
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Influenza A and B
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MOA for Ribavirin?
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Inhibits synthesis of guanine nucleotides by competitively inhibiting IMP dehydrogenase
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Clinical uses for Ribavirin?
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RSV
Chronic Hep C |
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Toxicity of Ribavirin?
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Hemolytic Anemia
Severe Teratogen |
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MOA for Acyclovir?
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Monophosphorylated by HSV/VZV thymidine kinase
Guanosine analog Triphosphate formed by cellular enzymes ***Preferentially inhibits DNA Polymerase by chain termination |
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Clinical uses for Acyclovir?
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HSV (lesions and encephalopathy)
VZV (use famciclovir) EBV Prophylaxis for immunocomp No effect on latent HSV or VZV |
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Toxicity of Acyclovir
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well tolerated
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Mech of resistance to Acyclovir?
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Lack of Thymidine kinase
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MOA for Ganciclovir?
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5'-monophosphate formed by CMV viral kinase or HSV/VZV thymidine kinase.
Guanosine analog Triphosphate formed by cellular enz's Preferentially inhibits DNA polymerase |
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Uses for Ganciclovir?
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CMV (esp in immunocomp)
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Toxicity of Ganciclovir?
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Leukopenia
Neutropenia Thrombocytopenia Renal Toxicity i.e. worse than acyclovir |
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Mech of resistance to ganciclovir?
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Mutated CMV DNA polymerase or lack of viral kinase
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MOA for Foscarnet?
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Viral DNA Polymerase inhibitor that binds pyrophosphate binding site of enzyme
Doesn't require activation by viral kinase |
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Uses for Foscarnet?
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CMV Retinitis in immunocomp when ganciclovir fails
Acyclovir-resistant HSV |
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Toxicity of Foscarnet?
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Nephrotoxicity
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Mechanism of Resistance to Foscarnet?
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Mutated DNA polymerase
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Types of drugs for HIV Therapy?
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Protease Inhibitors
Reverse Transcriptase Inhibitors Fusion Inhibitors |
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Who are the Protease Inhibitors?
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NAVIR's
saquinavir ritonavir indinavir nelfinavir amprenavir |
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MOA of Protease Inhibitors?
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Inhibit maturation of new virus by blocking protease in progeny
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Toxicity of Protease Inhibitors?
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GI intolerance (N&D)
Hyperglycemia Lipodystrophy Thrombocytopenia (indinavir) |
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Who are the Reverse Transcriptase Inhibitors?
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NUCLEOSIDES
**Zidovudine (ZDV formerly AZT) didanosine (ddI) zalcitabine (ddC) stavudine (d4T) lamivudine (3TC) abacavir NON-NUCLEOSIDES Nevirapine Efavirenz Delavirdine |
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MOA for Reverse Transciptase Inhibitors
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Preferentially inhibit reverse transcriptase of HIV
Prevent incorporation of DNA copy of viral genome into host DNA |
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Toxicity of Reverse Transciptase Inhibitors?
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Bone Marrow Suppression
Peripheral neuropathy Lactic Acidosis (nucleosides) Rash (non-nucleosides) Megaloblastic Anemia (ZDV azt) |
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what is HAART? when is it used?
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Highly Active Antiretroviral Therapy (HAART) usually means a combo of protease inhibitors and Reverse Transciptase Inhibitors.
Started when CD4 count drops below 500 or w/ a high viral load |
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When else is ZDV used?
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Prophylaxis
in pregnancy for prevention of Tx |
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Who are the Fusion Inhibitors?
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Enfuvirtide
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MOA of fusion inhibitors?
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Bind viral gp41 subunit--->inhibit conformational change required for fusion w/ CD4 cells--->blocked entry and subsequent replication
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Toxicity of fusion inhibitors?
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Hypersensitivity Rxns
Rxns to subcu injection site Inc risk of bacterial pneumonia |
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Clincal uses for fusion inhibitors?
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Pts w/ persistent viral replication in spite of antiretroviral therapy.
Combo w/ other drugs |
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MOA of Interferons?
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Glycoproteins from human leukocytes that block various stages of viral RNA and DNA synthesis.
Induce ribonuclease that degrades viral mRNA |
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Clinical uses of Interferons?
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IFN-alpha:
Chronic Hep B and C Kaposi's Sarcoma IFN-Beta: MS IFN-Gamma: NADPH Oxidase Def |
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Toxicity of Interferons?
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Neutropenia
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Antibiotics to avoid in Pregnancy and what they cause? Mnemonic?
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SAFE Moms Take Really Good Care.
Sulfonamides (kernicterus) Aminoglycosides (ototoxic) Fluoroquinolones (cartilage damage) Erythromycin (acute cholestatic hepatitis in mom; clarithromycin is also embryotoxic) Metronidazole (mutagenesis) Tetracyclines (discolored teeth, inhibit bone growth) Ribavirin (teratogenic) Griseofulvin (teratogenic) Chloramphenicol (gray baby) |
