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102 Cards in this Set

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bactericidal antibiotics
penicillin, cephalosporins, vancomycin, aminoglycosides, floroquines, metronidazole
penicillin G
IV form of penicillin
penicillin V
oral form of penicillin
MOA of penicillin
1. bind penicillin binding protein (aka tranpepsidase)
2. block transpepsidase cross-lining of cell wall
3. activate autolytic enzymes - (works on dividing bacteria)
clinical use of penicillin?
Bactericidal
Gram-positive cocci/rods: Streptococci, Pneumococci
Gram-negative cocci: Meningococci
Enterococci
Spirochetes: Treponema pallidum
Is penicillin penicillinase resistant?
No
toxixity of penicillin
hypersensitivity reactions, drug-induced coombs positive-hemolytic anemia
how do gram negative bacteria protect themselves from penicillin?
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
example of a bacteria that uses: altered molecular structure of transpepsidase so beta-lactam antibiotic (penicillin) no bind to it
MRSA
How do gram positive bacteria protect themselves from penicillin?
1. Secrete beta-lactamase = penicillinase (S aureus)
2. Try to intercept antibiotic outside the cell wall
Name the penicillinase resistant penicillin? MOA?
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
clinical use of penicillinase resistant penicillin?
why?
s. Aureus but not MRSA

MRSA is resistant b/c of altered penicillin-binding protein target site
TOXICITY of all penicillinase resistant penicillin
HYPERSENSITIVITY reactions
Which penicillinase resistant penicillin causes intersitial nephritis?
Methicillin
aminopenicillins - names and clinical use?
ampicillin, amoxicillin

Gram-negative Rods: H. influenzae, E coli, L. monocytogenes, Proteus mirabilis, Salmonella, Enterococci
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
toxicity of anti-pseudomonals?
hypersensitivity reactions
Cephalosprins MOA
B-lactam drug that inhibit cell wall synthesis
Less susceptible to penicilinase
Bactericidal
what are the first generation cephalosporins?
Cefazolin, Cephalexin
clinical use of 1st generation cephalosporins?
Gram positive cocci: Pneumococci, Streptococci, Staphylococci
Proteus mirabilis
E. coil
Klebsiella pneumoniae
PEcK
what are the 2nd generation cephalosporins?
cefoxitin, cefaclor,cefuroxime - furry fox is fat
clinical use of 2nd generation cephalosporins?
Gram positive cocci
H. influenza
Enterobacter aerogenes
Neiseseria spp
Proteus mirabilis
E. coil
Klebsiella pneumoniae
Serratia marcescens
HEN PEcKS
what are the 3rd generation cephalosporins?
cetriaxone, cefotaxime, ceftazidime
clinical use of 3rd generation cephalosporins?
Serious Gram Negative: Serratia, Pseudomonas, Enterobacter, H. influenzae, Neisseria - infections resistant to oteher B lactams - meningitis (most penetrate BBB)
ceftazidime used for what?
pseudomonas
ceftriaxone used for what?
gonorrhea
what are 4th generation cephalosporins?
Cefepime and Cefpiramide - pime mide
Clinical use of 4th generation cephalosporins?
Gram Negative: Pseudomonas, Serratia, Enterobacter, H. influenzae, Neisseria
Gram positive: S. aureus, S. pneumoniae
toxicities of all cephs?
Hypersensitivity reactions,
Cross hypersensitivity with penicillins,
Increased nephro tox of aminoglycosides,
Disulfiram like reaciton w/ ethanol
What is aztreonam?
Monocyclic B-lactam ring that act to inhibit peptidoglycan cross linking
Resistant to Beta lactamase
what is the moa of aztreonam?
inhibits cell wall synthesis (binds to PBP3)
synergistic with aminoglycosides,
no cross-allergy with penicillin
what is the clinical use of aztreonam?
Gram negative rods: Klebiella spp, Pseudomonas spp, Serratia spp
NO activity against gram positive gram positives or anerobes
toxicity of aztreonam?
usually nontoxic, occasional GI upset
What is Imipenem and Meropenem?
Broad spectrum
B lactamase resistant carbapenem
Imipenem is always administered with Cilastatin
what is cilastatin and why is it administered with imipenem?
it is a renal dihydropeptidase inhibitor that inactivates imipenem in the renal tubules
clinical use of imipenem/cilastatin, meropenem
Enterobactor - Drug of choice
Gram poitive cocci
Gram negative rods
Anerobes
Pseudomonas
Drug of choice for Enterobacter?
Imipenem/Cilastatin, Meropenem
what is tox of imipenem/cilastatin, meropenem?
GI distress , skin rash, seizures at high plasma levels
Vancomycin MOA
Inhibits cell wall mucopeptide formation by binding D-ala D ala of cell wall precursors
how does vancomycin resistance occur?
D-ALA D-ALA TO D-ALA D-LAC
is vacomycin bactericidal or static?
bactericidal
what is the clinical use of vancomycin?
Gram positive multidrug resistant organisms including S. aureus, Enterococci, Streptococci, and C. difficile
What causes nephrotoxicity, ototoxicity, thrombophlebitis and diffuse flushing?
Vancomycin
What causes red man syndrome?
vancomycin
How prevent red man syndrome?
Pretreat with antihistamines and slow infusion rate.
30 S Inhibitors
AT 30 - Aminoglycosides (bacteriocidal), Tetracyclines (bacteristatic)
50 S Inhibitors
cell at 50 - Chloamphenicol, Erythromycin, Lincomycin, cLindamycin (all bacteriostatic)
examples of aminoglycosides
streptomycin, gentamycin, tobramycin, amikacin
Aminoglycosides MOA
Bactericidal,
Inhibit ormaltion of initiation complex and cause misreading of mRNA
Requires o2 for uptake, therfore ineffective angainst anaerobes
Aminoglycosides clinical use
Severe gram negative infections
Synergistic with B-lactam antibiotics
Use in bowel surgery.
Neomycin
Aminoglycosides toxicity
Nephrotoxicity (with cephalosporins)
Ototoxicity (especially with loop diuretics)
Teratogen
Clinical use of tetracyclines:
Vibrio cholerae, Acne, Chlamydia, Ureaplasma, Urealyticum, Mycoplasma pneumoniae, Tularemia, H. pylori, Borrelia burgdorferi (Lyme Disease), Rickettsia - VACUUM THe BedRoom
Tetracycline toxicity and contradiction.
Tox:
GI distress
Discoloration of teeth
Inhibition of bone growth in children
Photosensitivity
Contradiction in Pregnancy
MOA of Tetracyclines?
Bacteriostatic
Bind to 30S and prevent attachment of aminoacyl-tRNA
Limited to CNS penetration
Doxycycline: elimination, use with renal failure, contridiction with what meds/food and why?
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
What are the tetracyclines?
Tetracyclines, doxycycline, demeclocycline, minocycline
What are the Macrolides:
Erythromycin, azithromycin, clarithromycin
Macrolides MOA
Inhibit protein synthesis by blocking translocation, bind to the 23S rRNA of the 50S ribosomal subunit, bacteriostatic
Clinical use of macrolides
URIs, pneumonias, STDs
Gram positive cocci (streptococcal infections in patients allegic to penicillin), Mycoplasma, Legionella, Chlamydia, Neisseria
Macrolides toxicity
GI discomfort (most common cause of noncompliance)
Acute cholestatic hepatitis
Eosinophilia
Skin rashes
What drug increases serum concentration of theophyllines and oral anticoagulants?
Macrolides
What is the MOA of Chloamphenicol?
Inhibits 50S peptidyltransferase, bacteriostatic
Clinical use of chlorophenicol?
Meningitis: Haemophilus influenzae, Neisseria meningitidis, Streptococcus pneumoniae
Toxicity of chloroamphenicol
Anemia (dose dependent)
Aplastic anemia (dose independent)
Gray baby syndrome (in premature infants b/c they lack liver UDP-glycuronyl transferase)
Clindamycin MOA
Blocks peptide bond formation at 50s ribosomal subunit.
Bacteriostatic
treats anaerobes above the diaphram
clindamycin
treat anaerobic infections (Bacteroides fragalis, clostridium perfringens)
clindamycin
What drug causes pseudomembranous colitis (C. difficile overgrowth. fever , diarrhea)?
clindamycin
types of sulfonamides
sulfamethoxazole (SMX) sulfisoxazole, triple sulfas, sulfadiazine
sulfonamides MOA
PABA antimetabolites inhibit dihydropteroate synthase. bacteriostatic
clinical use of sulfonamides
gram-positive, gram-negative, Nocaria, Chlamydia. Triple sulfas or SMX for simple UTI
Sulfonamides Toxicity
Hypersensitivity reactions
Hemolysis if G6PD deficient
Nephrotoxicity (tubulointerstitial nephritis)
What do Sulfonamides cause in infants?
Kernicterus in infants
What drug displace other drugs from albumin (e.g. warfarin)?
Sulfonamides
What are Trimethoprim toxicities? What may alleviate symptoms?
Megaloblastic anemia
Leukopenia
Granulocytopenia

May be alleviate with supplimental folinic acid
When Trimethoprim-Sulfamethoxazole (TMP-SMX) is used in combination which causes sequential block of what? Used for what infections/organisms?
Sequential block of folate synthesis.
Used for recurrent UTIs, Shigella, Salmonella, Pneumocystis carinii pneumonia (PCP)
Trimethoprim MOA
inhibits bacterial dihydrofolate reductase, bacteriostatic
Name the fluoroquinolones.
Ciprofloxacin
Norfloxacin
Ofloxacin
Sparfloxacin
Moxifloxacin
Gatifloxacin
Enoxacin
Nalidixic acid (a quinolone)
Fluoroquinolones MOA?
inhibit DNA gyrase (topoisomerase II), bacericidal
clinical use of fluoroquinolones
Gram-negative rods of urinary and GI tracts (including Pseudomonas), Neisseria, Some gram-positive organisms
Fluoroquinolones toxicity.
GI upset, superinfections, skin rashes, headache, dizziness.
Fluoroquinolones contradicted in who and why?
Contradicted in pregnant women and children because animal studies show damage to cartilage.
Fluoroquinolones toxicity.
Tendonitis and tendon rupture in adults
Leg cramps and myalgias in kids.
Metronidazole MOA
Forms toxic metabolites in the bacterial cell
Bactericidal
Antiprotozoal
Metronidazole clinical use
Metronidazole clinical use
Antiprotozal: Giardia, Entamoeba, Trichomonas, Gardnerella vaginalis, Anaerobes (bacteriodes, clostridium)
'Triple therapy" against H. pylori contains what drugs.
Metronidazole
Bismuth
Amoxicillin (or tetracycline)
Polymyxin B and polymyxin E are examples of what type of drug?
Polymyxins
Polymixins MOA
Bind to cell membranes of bacteria and disrupt their osmotic properties

Cationic, basic proteins act like detergents.

Myxins mix up membranes
Polymixins clinical use
Used for resistant gram negative infections
Polymixins toxicity
Neurotoxicity
Acute renal tubular necrosis
List Anti-TB Drugs
Streptomycin
Pyrazinamide
Isoniazid(INH)
Rifampin
Ethambutol
Cycloserine (2nd line therapy)
TB prophylazxis?
Isoniazid (INH)
Isoniazid MOA
Deacerased synthesis of mycolic acid
Isoniazid (INH) toxicity
Hemolysis if G6PD deficincy
Neurotoxicity
Hepatotoxicity
SLE-like syndrome
What can prevent neurotoxicity in Isoniazid (INH)?
Pyridoxine (Vit B6)
Common toxicity to all anti-tb drugs.
Hepatotoxic
Rifampin MOA
Inhibits DNA-dependent RNA polymerase
Rifampin clinical uses
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
Rifampin toxicity
Minor heptotoxicity
Drug interaction (increased P 450)
Rifampin has when effect on body fluids?
Turn body fluids red/organge