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102 Cards in this Set
- Front
- Back
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bactericidal antibiotics
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penicillin, cephalosporins, vancomycin, aminoglycosides, floroquines, metronidazole
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penicillin G
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IV form of penicillin
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penicillin V
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oral form of penicillin
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MOA of penicillin
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1. bind penicillin binding protein (aka tranpepsidase)
2. block transpepsidase cross-lining of cell wall 3. activate autolytic enzymes - (works on dividing bacteria) |
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clinical use of penicillin?
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Bactericidal
Gram-positive cocci/rods: Streptococci, Pneumococci Gram-negative cocci: Meningococci Enterococci Spirochetes: Treponema pallidum |
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Is penicillin penicillinase resistant?
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No
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toxixity of penicillin
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hypersensitivity reactions, drug-induced coombs positive-hemolytic anemia
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how do gram negative bacteria protect themselves from penicillin?
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1.prevent penicillin from penetrating cell layers by altering porins
2. beta-lactase enzyme 3.alter molecular structure of transpepsidase so beta-lactam antibiotic (penicillin) no bind to it |
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example of a bacteria that uses: altered molecular structure of transpepsidase so beta-lactam antibiotic (penicillin) no bind to it
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MRSA
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How do gram positive bacteria protect themselves from penicillin?
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1. Secrete beta-lactamase = penicillinase (S aureus)
2. Try to intercept antibiotic outside the cell wall |
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Name the penicillinase resistant penicillin? MOA?
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methicillin, nafcillin, dicloxacillin
MOA same as penicillin: 1. Bind penicillin-binding proteins 2. Block transpeptidase cross-linking of cell wall 3. Activate autolytic enzymes Penicillinase Resistant (Beta-lactamase resistant) - bulkier R group - acts to hinder B-lactamase access to the B-lactam ring |
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clinical use of penicillinase resistant penicillin?
why? |
s. Aureus but not MRSA
MRSA is resistant b/c of altered penicillin-binding protein target site |
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TOXICITY of all penicillinase resistant penicillin
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HYPERSENSITIVITY reactions
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Which penicillinase resistant penicillin causes intersitial nephritis?
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Methicillin
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aminopenicillins - names and clinical use?
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ampicillin, amoxicillin
Gram-negative Rods: H. influenzae, E coli, L. monocytogenes, Proteus mirabilis, Salmonella, Enterococci |
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Are anti-pseudomonals susceptible to penillinase?
What can use to help with? Names? |
Yes,
Give with clavulanic acid - which is a beta-lactamase inhibitor Piperacillin, Ticarcillin, Carbenicillin |
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toxicity of anti-pseudomonals?
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hypersensitivity reactions
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Cephalosprins MOA
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B-lactam drug that inhibit cell wall synthesis
Less susceptible to penicilinase Bactericidal |
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what are the first generation cephalosporins?
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Cefazolin, Cephalexin
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clinical use of 1st generation cephalosporins?
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Gram positive cocci: Pneumococci, Streptococci, Staphylococci
Proteus mirabilis E. coil Klebsiella pneumoniae PEcK |
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what are the 2nd generation cephalosporins?
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cefoxitin, cefaclor,cefuroxime - furry fox is fat
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clinical use of 2nd generation cephalosporins?
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Gram positive cocci
H. influenza Enterobacter aerogenes Neiseseria spp Proteus mirabilis E. coil Klebsiella pneumoniae Serratia marcescens HEN PEcKS |
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what are the 3rd generation cephalosporins?
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cetriaxone, cefotaxime, ceftazidime
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clinical use of 3rd generation cephalosporins?
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Serious Gram Negative: Serratia, Pseudomonas, Enterobacter, H. influenzae, Neisseria - infections resistant to oteher B lactams - meningitis (most penetrate BBB)
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ceftazidime used for what?
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pseudomonas
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ceftriaxone used for what?
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gonorrhea
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what are 4th generation cephalosporins?
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Cefepime and Cefpiramide - pime mide
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Clinical use of 4th generation cephalosporins?
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Gram Negative: Pseudomonas, Serratia, Enterobacter, H. influenzae, Neisseria
Gram positive: S. aureus, S. pneumoniae |
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toxicities of all cephs?
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Hypersensitivity reactions,
Cross hypersensitivity with penicillins, Increased nephro tox of aminoglycosides, Disulfiram like reaciton w/ ethanol |
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What is aztreonam?
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Monocyclic B-lactam ring that act to inhibit peptidoglycan cross linking
Resistant to Beta lactamase |
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what is the moa of aztreonam?
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inhibits cell wall synthesis (binds to PBP3)
synergistic with aminoglycosides, no cross-allergy with penicillin |
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what is the clinical use of aztreonam?
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Gram negative rods: Klebiella spp, Pseudomonas spp, Serratia spp
NO activity against gram positive gram positives or anerobes |
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toxicity of aztreonam?
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usually nontoxic, occasional GI upset
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What is Imipenem and Meropenem?
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Broad spectrum
B lactamase resistant carbapenem Imipenem is always administered with Cilastatin |
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what is cilastatin and why is it administered with imipenem?
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it is a renal dihydropeptidase inhibitor that inactivates imipenem in the renal tubules
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clinical use of imipenem/cilastatin, meropenem
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Enterobactor - Drug of choice
Gram poitive cocci Gram negative rods Anerobes Pseudomonas |
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Drug of choice for Enterobacter?
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Imipenem/Cilastatin, Meropenem
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what is tox of imipenem/cilastatin, meropenem?
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GI distress , skin rash, seizures at high plasma levels
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Vancomycin MOA
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Inhibits cell wall mucopeptide formation by binding D-ala D ala of cell wall precursors
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how does vancomycin resistance occur?
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D-ALA D-ALA TO D-ALA D-LAC
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is vacomycin bactericidal or static?
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bactericidal
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what is the clinical use of vancomycin?
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Gram positive multidrug resistant organisms including S. aureus, Enterococci, Streptococci, and C. difficile
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What causes nephrotoxicity, ototoxicity, thrombophlebitis and diffuse flushing?
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Vancomycin
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What causes red man syndrome?
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vancomycin
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How prevent red man syndrome?
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Pretreat with antihistamines and slow infusion rate.
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30 S Inhibitors
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AT 30 - Aminoglycosides (bacteriocidal), Tetracyclines (bacteristatic)
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50 S Inhibitors
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cell at 50 - Chloamphenicol, Erythromycin, Lincomycin, cLindamycin (all bacteriostatic)
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examples of aminoglycosides
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streptomycin, gentamycin, tobramycin, amikacin
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Aminoglycosides MOA
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Bactericidal,
Inhibit ormaltion of initiation complex and cause misreading of mRNA Requires o2 for uptake, therfore ineffective angainst anaerobes |
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Aminoglycosides clinical use
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Severe gram negative infections
Synergistic with B-lactam antibiotics |
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Use in bowel surgery.
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Neomycin
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Aminoglycosides toxicity
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Nephrotoxicity (with cephalosporins)
Ototoxicity (especially with loop diuretics) Teratogen |
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Clinical use of tetracyclines:
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Vibrio cholerae, Acne, Chlamydia, Ureaplasma, Urealyticum, Mycoplasma pneumoniae, Tularemia, H. pylori, Borrelia burgdorferi (Lyme Disease), Rickettsia - VACUUM THe BedRoom
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Tetracycline toxicity and contradiction.
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Tox:
GI distress Discoloration of teeth Inhibition of bone growth in children Photosensitivity Contradiction in Pregnancy |
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MOA of Tetracyclines?
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Bacteriostatic
Bind to 30S and prevent attachment of aminoacyl-tRNA Limited to CNS penetration |
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Doxycycline: elimination, use with renal failure, contridiction with what meds/food and why?
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Fecally eliminated
Can be used in pts with renal failure Not take with milk, antacids, or iron-containtaing preparations because divalent cations inhibit its absorbtion in the gut |
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What are the tetracyclines?
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Tetracyclines, doxycycline, demeclocycline, minocycline
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What are the Macrolides:
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Erythromycin, azithromycin, clarithromycin
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Macrolides MOA
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Inhibit protein synthesis by blocking translocation, bind to the 23S rRNA of the 50S ribosomal subunit, bacteriostatic
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Clinical use of macrolides
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URIs, pneumonias, STDs
Gram positive cocci (streptococcal infections in patients allegic to penicillin), Mycoplasma, Legionella, Chlamydia, Neisseria |
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Macrolides toxicity
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GI discomfort (most common cause of noncompliance)
Acute cholestatic hepatitis Eosinophilia Skin rashes |
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What drug increases serum concentration of theophyllines and oral anticoagulants?
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Macrolides
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What is the MOA of Chloamphenicol?
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Inhibits 50S peptidyltransferase, bacteriostatic
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Clinical use of chlorophenicol?
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Meningitis: Haemophilus influenzae, Neisseria meningitidis, Streptococcus pneumoniae
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Toxicity of chloroamphenicol
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Anemia (dose dependent)
Aplastic anemia (dose independent) Gray baby syndrome (in premature infants b/c they lack liver UDP-glycuronyl transferase) |
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Clindamycin MOA
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Blocks peptide bond formation at 50s ribosomal subunit.
Bacteriostatic |
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treats anaerobes above the diaphram
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clindamycin
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treat anaerobic infections (Bacteroides fragalis, clostridium perfringens)
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clindamycin
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What drug causes pseudomembranous colitis (C. difficile overgrowth. fever , diarrhea)?
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clindamycin
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types of sulfonamides
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sulfamethoxazole (SMX) sulfisoxazole, triple sulfas, sulfadiazine
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sulfonamides MOA
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PABA antimetabolites inhibit dihydropteroate synthase. bacteriostatic
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clinical use of sulfonamides
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gram-positive, gram-negative, Nocaria, Chlamydia. Triple sulfas or SMX for simple UTI
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Sulfonamides Toxicity
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Hypersensitivity reactions
Hemolysis if G6PD deficient Nephrotoxicity (tubulointerstitial nephritis) |
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What do Sulfonamides cause in infants?
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Kernicterus in infants
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What drug displace other drugs from albumin (e.g. warfarin)?
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Sulfonamides
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What are Trimethoprim toxicities? What may alleviate symptoms?
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Megaloblastic anemia
Leukopenia Granulocytopenia May be alleviate with supplimental folinic acid |
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When Trimethoprim-Sulfamethoxazole (TMP-SMX) is used in combination which causes sequential block of what? Used for what infections/organisms?
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Sequential block of folate synthesis.
Used for recurrent UTIs, Shigella, Salmonella, Pneumocystis carinii pneumonia (PCP) |
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Trimethoprim MOA
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inhibits bacterial dihydrofolate reductase, bacteriostatic
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Name the fluoroquinolones.
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Ciprofloxacin
Norfloxacin Ofloxacin Sparfloxacin Moxifloxacin Gatifloxacin Enoxacin Nalidixic acid (a quinolone) |
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Fluoroquinolones MOA?
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inhibit DNA gyrase (topoisomerase II), bacericidal
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clinical use of fluoroquinolones
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Gram-negative rods of urinary and GI tracts (including Pseudomonas), Neisseria, Some gram-positive organisms
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Fluoroquinolones toxicity.
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GI upset, superinfections, skin rashes, headache, dizziness.
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Fluoroquinolones contradicted in who and why?
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Contradicted in pregnant women and children because animal studies show damage to cartilage.
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Fluoroquinolones toxicity.
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Tendonitis and tendon rupture in adults
Leg cramps and myalgias in kids. |
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Metronidazole MOA
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Forms toxic metabolites in the bacterial cell
Bactericidal |
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Antiprotozoal
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Metronidazole clinical use
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Metronidazole clinical use
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Antiprotozal: Giardia, Entamoeba, Trichomonas, Gardnerella vaginalis, Anaerobes (bacteriodes, clostridium)
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'Triple therapy" against H. pylori contains what drugs.
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Metronidazole
Bismuth Amoxicillin (or tetracycline) |
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Polymyxin B and polymyxin E are examples of what type of drug?
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Polymyxins
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Polymixins MOA
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Bind to cell membranes of bacteria and disrupt their osmotic properties
Cationic, basic proteins act like detergents. Myxins mix up membranes |
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Polymixins clinical use
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Used for resistant gram negative infections
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Polymixins toxicity
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Neurotoxicity
Acute renal tubular necrosis |
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List Anti-TB Drugs
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Streptomycin
Pyrazinamide Isoniazid(INH) Rifampin Ethambutol Cycloserine (2nd line therapy) |
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TB prophylazxis?
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Isoniazid (INH)
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Isoniazid MOA
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Deacerased synthesis of mycolic acid
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Isoniazid (INH) toxicity
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Hemolysis if G6PD deficincy
Neurotoxicity Hepatotoxicity SLE-like syndrome |
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What can prevent neurotoxicity in Isoniazid (INH)?
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Pyridoxine (Vit B6)
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Common toxicity to all anti-tb drugs.
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Hepatotoxic
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Rifampin MOA
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Inhibits DNA-dependent RNA polymerase
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Rifampin clinical uses
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Used against TB (Mycobacterium tuberculosis)
Delays resistance to dapsone when used for leprosy Used for meningococcal prophylaxis and chemoprophylaxis in contacts of childeren with H. influenza type B |
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Rifampin toxicity
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Minor heptotoxicity
Drug interaction (increased P 450) |
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Rifampin has when effect on body fluids?
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Turn body fluids red/organge
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