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Spring Exam #1 - Penicillins
n/a
32
Pharmacology
Graduate
03/25/2010

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Term
natural penicillins
Definition
penicillin G, penicillin V potassium, penicillin G procaine, penicillin G benzathine
Term
penicillinase resistant penicillins - antistaphylococcal penicillins
Definition
methicillin, nafcillin, oxacillin
Term
extended spectrum penicillins (aminopenicillins)
Definition
ampicillin, amoxicillin
Term
antipseudomonal penicillins
Definition
ticarcillin + clavulanate potassium (Timentin), piperacillin + tazobactam (Zosyn)
Term
Other beta-lactam drugs
Definition
aztreonam, imipenem + cilastatin, clavulanic acid, tazobactam
Term
Mechanism of Action of Penicillins
Definition
inhibits bacterial cell wall synthesis by inhibiting transpeptidase enzyme & subsequent production of highly cross-linked peptidoglycan cell wall;
bactericidal effect only on actively dividing cells that are producing cell wall;
little or no effect on dormant bacteria or on bacteria that lack cell walls
Term
aminoglycosides (gentamycin, etc)
Definition
penicillins are often used in combo with these antibiotics for a SYNERGISTIC killing effect
Term
increase concentration of penicillins
Definition
to overcome resistance due to structural differencesin PBPs - high molecular weight PBPs w/ low affinity for antibiotic
Term
enzymatic destruction of penicillins
Definition
most important form of resistance; use beta-lactamase inhibitors to overcome
Term
mycoplasma
Definition
bacteria without cell walls are NOT killed by penicllins
Term
amoxicillin
Definition
only penicillin that does not impair oral absorption
Term
Administration of Penicillins
Definition
food impairs oral absorption, so administer 1-2 hrs before or after a meal
Term
probenecid
Definition
drug that blocks tubular secretion of penicillins, causing an increase in penicillin concentration
Term
nafcillin, oxacillin, dicloxacillin
Definition
eliminated by biliary excretion mostly, some kidney excretion; DON'T need to adjust dose in renal failure
Term
Symptoms of Type I Hypersensitivity to Penicillins
Definition
skin rxns - rash, angioedema, urticaria, pruritus;
GI - nausea, abdominal pain, vomiting, & diarrhea;
dyspnea, wheezing;
hypotension, tachycardia, arrhythmias;
Fatality due to laryngeal edema, cardiovascular collapse
Term
1-72 hrs
Definition
time it may take for a Type 1 Hypersensitivity rxn to penicillins
Term
methicillin
Definition
most common cause of acute allergic interstitial nephritis
Term
Skin test
Definition
used to determine if pt will have Type 1 hypersensitivity rxn to penicillins; DOES NOT detect for Type II, III, or IV type rxns
Term
Side Effects of Penicillins
Definition
non-allergic skin rashes;
GI - upset, nausea, vomiting, diarrhea;
CNS toxicity - seizures;
excess Na & K - cardiac & renal toxicity;
Term
Penicillin G
Definition
PK: oral absorption is only 33%, available for IV or IM;
Used w/ aminoglycosides for SYNERGISTIC effect;
Probenecid increases plasma levels;
DRUG OF CHOICE - IM or IV for syphillis (Treponema pallidum);
Used for: non-resistant Staph & Strep infections, use w/ aminoglycoside against Enterococcal infections,
Term
Third gen. cephalosporin (ceftriaxone)
Definition
DRUG of CHOICE for Gram-negatives such as Neisseria meningitidis
Term
penicillin G procaine & pencillin G benzathine
Definition
slow release forms; give IM in gluteus maximus or midlateral thigh area;
Used for:
strep. pyogenes infections, strep. pharyngitis, prophylaxis for rheumatic fever, and for treating syphilis
Term
IV nafcillin, oxacillin
Definition
for serious systemic STAPH infections; do NOT need to adjust dose in renal failure
Term
nafcillin, methicillin, oxacillin
Definition
DRUG of CHOICE for penicillinase-producing Staph. aureaus: skin infections, soft tissue infections, osteomyelitis, acute endocarditis;

NOT EFFECTIVE against Gram (-) aerobes (E.coli, klebsiella, enterobacter)
Term
vancomycin
Definition
drug of choice for pts w/ MRSA
Term
ampicillin, amoxicillin
Definition
extended spectrum penicillins that treat:
Haemophilus influenzae - URTIs (sinusitis, otitis);
E. Coli - UTIs
Listeria monocytogenes - MENINGITIS in immunocompromised & in kids <2 months, bacteremia;
Proteus mirabilis - UTIs;
Salmonella, Strep. pyogenes & pneumoniae - URTIs;
Moraxella - RTIs
Enterococcus
Term
piperacillin + tazobactam (Zosyn)
Definition
use in combo with a fluoroquinolone (cipro or levo) to treat Community-Acquired Pneumonia (CAP)
Term
piperacillin + tazobactam (Zosyn)
Definition
used to treat:
higher dose used to treat nosocomial pneumonia;
septicemia by gram (-)'s;
UTIs - may use aminoglycoside with to treat;
gynecologic & obstetric infections;
intra-abdominal infections
Term
ticarcillin + clavulanate potassium (Tiementin)
Definition
used to treat susceptible Psuedomonas aeuruginosa infections such as septicemia & UTIs
Term
aztreonam
Definition
highly resistant to enzymatic inactivation by beta-lactamases produced by gram (-) bacteria;
ONLY active against GRAM (-) RODS;
use with gram (-) infections that have previous allergic rxns to beta-lactam antibiotics (penicillins, cephalosporins);
NO CROSS-REACTIVITY with penicillin or cephalosporin allergies
Term
imipenem + cilastatin (Primaxin)
Definition
extremely BROAD spectrum & activity and VERY POWERFUL antibiotic; SHOULD NOT BE ROUTINELY USED to prevent resistance;
Reserved for SERIOUS HOSPITAL ACQUIRED (nosocomial) INFECTIONS that include: resistant microorgansims or infections with multiple microorganisms
Term
amoxicillin + clavulanic acid (Augmentin)
Definition
DRUG CHOICE for acute otitis media and sinusitis and for human & animal bite wounds;
also used to treat: RTIs, UTIs, Skin & Skin structure infections
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