Pharm NBDE II Flashcards
what local anesthetics are esters
procaine, tetracaine, cocaine
where are amides metabolized?
liver
where are esters metabolized?
MAINLY esterase’s in the plasma
which class of drugs has the most consistency in structure?
local anesthetics
they differ only in their immediate chains (ester or amide) that connects the aromatic group to the tertiary amino terminus
what causes methemoglobinemia?
prilocaine and acetominophen at high doses
what does high systemic levels of local anesthetic lead to?
cardiovascular collapse due to DIRECT myocardial depression and hypotensive shock
how do local anesthetics work?
prevent the generation of nerve impulses by interfering with sodium transport into the neuron
what form of LA can penetrate tissue membrane?
non-ionized, free-base form
the duration of lidocaine is increased in the presence of what drug? and why?
propranolol
propranolol is a beta blower, slows heart, slows blood delivery to liver so that lido is not metabolized and remains in systemic circulation for longer also they compete for the same enzyme site
do esters or amides have longer half lives?
amides
what is the most probable cause of a serious severe LA toxic reaction?
excessive blood levels due to intravascular injection
initially high levels of LA lead to what?
depression of inhibitory neurons on the CNS ** aka cns stimulation (which can lead to convulsion) –> higher levels depress inhibitory and excitatory neurons which leads to overall cans depression which can lead to respiratory depression and death
what disease would make the patient most sensitive to epinephrine in LA?
Graves- hyperthyroidism results in high levels of circulating thyroid hormone which causes a hyper metabolic state and increases sympathetic activity which would lead to a hypertensive crisis
what is the only anesthetic that predictably produces vasoconstriction?
cocaine
given the pKa of a drug, if the pH of body tissue is less (more acidic from inflammation), which form of the drug will predominate?
the ionized (charged) form of the drug. This makes it harder for the drug to penetrate the membrane.
what form of LA blocks nerve conduction?
positively charged - LA penetrate as unionized into the neuron and then re-equibrilate back to charged and uncharged inside to block conduction
what are the AHA limits (in mg) of epi in cardiovascular disease vs. regular patients
0.04 mg for cardiovascular disease vs. 0.2 mg in healthy
why is penicillin G injected rather than take orally?
sensitive to acid degradation
which penicillin has the best gram negative spectrum?
ampicillin
hat drugs are cross-reactive with penicillin?
cephalosporin and ampicillin
which penicillin is useful against penicillanse-producing bugs like staph?
dicloxacillin
what Ab is good for pseudomonas infections?
carbenicillin because its extended spectrum
what is given prophylactically for dental procedures to prevent bacterial endocarditis?
2g of amoxicillin - clindamycin if allergies
how do bactericidal agents work?
kill bacteria through inhibiting rapidly growing cell wall synthesis