pharm exam 3 Flashcards
dopamine blockade at mesolimbic-mesocortical pathway
antipsychotic efficacy
DA blockade at nigrostriatal pathway
parkinsonian side effects
DA blockade at tuberoinfundibular pathway
hyperprolactinemia (weight gain, sexual dysfunction)
DA blockade at medullary-periventricular pathway
anti-emetic effects
DA hypothesis
excess DA @ mesolimbic –> + symptoms
deficit DA @ mesocortical –> - symptoms
antipsychotics mechanism
DA D2 receptor antagonists!!
EXCEPT atypical higher affinity for 5-HT2A than D2 (why it’s better at treating - symptoms)
what is the neuroleptic malignant syndrome tetrad?
- mental status change (confusion, stupor)
- hyperthermia
- extreme muscle rigidity (increase CK)
- autonomic dysfunction (tachycardia, HTN, sweating)
high potency antipsychotic characteristics
higher risk EPSE but less sedating
high potency antipsychotic prototype
haloperidol
low potency antipsychotic characteristics
lower risk of EPSE but more sedating
low potency antipsychotic prototype
chlorpromazine
second generation antipsychotic protoype
clozapine
what’s unique about clozapine?
efficacy for recalcitrant schizophrenia & suicidal behavior; reserved for cases where other antipsychotics have failed due to agranulocytosis; nearly absent risk of EPSE/TD
list the four 5-HT2A > D2 antagonists
risperidone
olanzapine
quetiapine
ziprasidone
the partial D2 receptor agonist
aripiprazole (abilify); its partial agonism of D2 receptors blocks full agonist effect of DA
atypical vs typical antipsychotics
atypical better at treating NEGATIVE symptoms, have lower risk EPSE/TD, but higher risk of weight gain & more expensive
MIC definition
lowest conc. of an agent that PREVENTS VISIBLE BACTERIAL GROWTH in 24 hrs
what are innately resistant to aminoglycosides?
anaerobes
what are innately resistant to metronidazole?
aerobes
what are gram negative innately resistant to?
LIPOPHILIC– standard penicillins & high MW hydrophilic– vancomycin
ways a bug can ACQUIRE resistance?
- inactivation of the antibiotic
- decreased uptake of the antibiotic
- increased efflux of the antibiotic
- altered target site (so it can’t bind)
- bypass target process
mechanisms of acquiring resistance
enzyme induction (increasing expression of existing resistance genes), vertical transfer (spontaneous mutation), horizontal transfer (conjugation)
do abx cause mutations?
NO! they promote resistance by exerting selective pressure
classic mech. of MDR
gram neg. doing horizontal transfer (conjugation, plasmid transferring R factor)
highest risk for c dif
clindamycin, cephalosporins (broad spectrum), fluoroquinolones, carbapenems
tx c dif
NOT antidiarrheal agents. abx: metronidazole, vancomycin, fidaxomicin)
downside of bacteriostatics
reliant on competent host immune system (so don’t use in immunocompromised)
what agent would you use for locations that are difficult for abx to penetrate?
bactericidal! esp. in endocarditis, meningitis, osteomyelitis
ideal or actual body weight for aminoglycosides
ideal! bc hydrophilic
abx whose dose should be reduced in pts with decreased kidney fxn
Cephalosporins (1 & 2 gen) Aminoglycosides Vancomycin Ethambutol Sulfonamides/trimethoprim Carbapenems Extended spectrum penicillins
abx whose dose should be reduced in pts with decreased liver fxn
Clindamycin Chloramphenicol Metronidazole Macrolides Rifampin Isoniazid Tetracylclines
category D abx
DON’T USE IN PREGNANT! Aminoglycosides & tetracyclines (and sulfonamide-induced kernicterus during nursing)
most common abx that provoke sensitivity rxn’s
beta lactams
sulfonamides
trimethoprim
erythromycin
significance of gram neg. OM
hinders transport of many abx; small hydrophilic drugs can cross via transport through porins
list the bactericidal agents
aminoglycosides, beta-lactams, daptomycin, fluoroquinolones, isoniazid, metronidazole, polymyxins, pyrazinamide, rifampin, vancomycin
list the bacteriostatic agents
(the CCEMOSTT ones!)
chloramphenicol, clindamycin, ethambutol, macrolides, oxazolidinones, sulfonamides, tetracyclines, trimethoprim
what class inhibits cell wall synthesis?
beta lactams! & glycopeptides (vancomycin), fosfomycin (treats uncomplicated UTIs in women)