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102 Cards in this Set

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drug
bethanechol
parasympathetic that promotes GI and urinary tract mobility, mAChR agonist
atropine
parasympathetic antagonist dilates pupils (locally) or increases heart rate (systemically)
ipratroprium
parasympathetic antagonist dilates bronchioles
pancuronium
antagonist of neuromuscular junction activity used to induce paralysis in surgery
edrophonium
increase NMJ activity used in diagnosis and treatment of myasthenia gravis (if administration mitigates muscle weakness then postive for MG, if it makes the weakness worse then there is a depolarizing antagonist of nAChR present) via inhibition of AChEsterase (simple alcohol, reversible inhibition)
neostigmine
increase NMJ activity used in diagnosis and treatment of myasthenia gravis via inhibition of AChEsterase and direct activation of nAChR, quaternary ammonium, also used to increase GI motility
barbituates
activate GABA neurons in cortex (sedative and hypnotic)
benzodiazepenes
activate GABA neurons in cortex (sedative and hypnotic)
clonidine
partail agonist that acts on presynaptic alpha-2 receptors
tricyclic antidepressants
block NE and serotonin reuptake
monoamine oxidase inhibitors
block NE degradation
ssri
block serotonin reuptake (antidepressant)
carbidopa
inhibitor of dopamine decarboxylase (Ldopa-->dopamine)
vesamicol
inhibits the H+/Ach antiporter into the vesicles
hemicholinium-3
inhibits sodium-dependent transport of choline into neurons
hexamthonium
selective blockage of presynaptic cholinergic receptor that prevents facilitation and causes rapid tetanic fade
botulinum toxin
degrades synaptobrevin and blocks Ach synaptic vesicle fusion; ;used for achalasia, strabismus (eye misalignment due to ocular imbalance, esotropia=cross-eyed, exotropia=wall-eyed), blepharospasm (involuntary closing of the eyelids), cosmetic
pralidoxime
strong nucleophile that prevents aging of AChE
diisopropyl fluorophosphate
organophosphate that inhibits AChE shows property of aging
physostigmine
increase NMJ activity used in diagnosis and treatment of myasthenia gravis via inhibition of AChEsterase, quaternary ammonium
ambenonium
treatment of myasthenia gravis via inhibition of AChE
Meds to treat alzheimers
tacrine, donepezil, rivastigmine, galantamine
three uses of AChE inhibitors
increase transmission at NMJ, increase parasympathetic tone, increase cholinergic activity in CNS in Alzheimer's Dz
methacholine
used for diagnosis of asthma (mAChR agonist)
Carbachol
mAChR agonist, used as a miotic agent, treatment of glaucoma
pilocarpine
alkaloid mAChR agonist used for drymouth secondary to decreased salivary secretion (xerostomia) treatment as it induces saliva
succinylcholine
nAChR agonist, used to induce depolarizing paralysis (see fasciculations at onset)
uses of atropine
induce mydriasis (pupil dilation), to reverse sinus bradycardia caused by excessive vagal tone in the context of MI or asystole, inhibit excessive salivary and mucus secretion during surgery, to prevent vagal reflexes induced by surgical trauma of visceral organs, counteract the effects of muscarine poisoning from certain mushrooms
atropine
alkaloid mAChR antagonist, must be used in high doses
scopolamine
mAChR antagonist used for motion sickness (CNS effects)
pirenzepine
mAChR antagonist selective for M1 and M4, alternative peptic ulcer treatment to H2 receptor blockers
ipratropium
mAChR antagonist. Quaternary ammonium, COPD (better than beta-adrenergic agonists)
d-tubocurarine
long lasting nAChR antagonist
pancuronium
long lasting nAChR antagonist
vecuronium
intermediate lasting nAChR antagonist
rocuronium
intermediate lasting nAChR antagonist
mivacurium
short lasting nAChR antagonist
mecamylamine
nAChR antagonist used to treat HTN in patients with acute dissecting aortic aneurysms (lower BP and blunt sympathtic reflexes that would normally cause rise in BP)
trimethaphan
nAChR antagonist used to treat HTN in patients with acute dissecting aortic aneurysms (lower BP and blunt sympathtic reflexes that would normally cause rise in BP)
alpha-1 receptor antagonists
hypertension and prostatic hypertrophy therapies
alpha-2 receptor agonists
act at CNS sites to decreases sympathetic outflow to perifery and decrease SMC contraction, tx for hypertension
beta-1 receptor antagonists
decrease heart rate, AV-nodal conduction velocity, and contractility, used to treat MI, hypertension, supraventricular tachycardia, and mild-moderate CHF
beta-2 receptor agonists
vasodilate, decrease bronchiolar constriction (asthma tx), act on kidney to catabolize glycogen (increase blood sugar)
systemic dopamine treatment
for shock (high doses [>10ug/kg per min]activates alpha 1 adrenergic receptor to induce vasoconstriction)
alpha-methyltyrosine
treatment of HTN associated with pheochromocytomas, analogue of tyrosine that blocks catecholamine synthesis
reserpine
irreversible inhibits VMAT (uptake 2) which prevents formation of catecholamine vesicles, was used for HTN tx, no longer really used
indirect sympathomimetics
act to displace NE from vesicles
mixed sympathomimetics
displace NE from vesicles and direct effect on adrenoreceptors
tyramine
dietary amine that when taken with MAOI can get into vesicles and cause an acute displacement of NE out of the vesicles --> HTN crisis (wine has a high concentration of tyramine)
guanethidine
displaces NE from vesicles, used for uncontrolled HTN
guanadrel
displaces NE from vesicles, used for HTN, not used much anymore.
amphetamine
displaces endogenous catecholamines, inhibits MAO, acts as an agonist to peripheral Beta and Alpha-receptors, potent adrenoceptor agonist in the CNS, increased alertness, decreased fatigue, depressed appetite, insomnia; side fx: fatigue and depression
ephedrine
similar yet less potent than amphetamine
pseudoephedrine
similar yet less potent than amphetamine
phenylpropanolamine
similar yet less potent than amphetamine
methamphetamine
similar and more potent than amphetamine, also known as crystal meth or crank
cocaine
inhibits NET (type 1 Uptake) of catecholamines nearly completely, significant risk of abuse
imipramine
tricyclic antidepressent that inhibits NET mediated reuptake of NE, also inhibit seratonin and block serotonergic, alpha-adrenergic, histaminergic, and muscarinic receptors; lots of side effects; used for depression (NE and serotonin reuptake inhibition); latency period of several weeks
None
amitriptyline
tricyclic antidepressent that inhibits NEW mediated reuptake of NE, also inhibit seratonin and block serotonergic, alpha-adrenergic, histaminergic, and muscarinic receptors; lots of side effects; used for depression (NE and serotonin reuptake inhibition); latency period of several weeks
phenelzine
nonselective MAOI (MOA-A and MOA-B)
iproniazid
nonselective MAOI (MOA-A and MOA-B)
tranylcypromine
nonselective MAOI (MOA-A and MOA-B)
clorgyline
selective MOA-A inhibition
selegiline
selective MOA-B inhibition
brofaromine
reversible MOA-A inhibitor
befloxatone
reversible MOA-A inhibitor
moclobemide
reversible MOA-A inhibitor
uses of MOAIs
depression, parkinson's dz (selegiline), avoid eating fermented foods with lots of tyramine, do not take with SSRI - can precipitate "serotonin syndrome" (restlessness, tremors, seizures, possibly coma and death)
"serotonin syndrome"
concommitant use of SSRIs and MOAIs; restlessness, tremors, seizures, possibly coma and death
methoxamine
alpha-1 agonist for hyptotension or shock treatment
phenylephrine
topical alpha-1 agonist, also used for shock
oxymetazoline
topical alpha-1 agonist
tetrahydrazoline
topical alpha-1 agonist
clonidine
alpha-2 agonist used for HTN and drug withdrawal symptoms, acts on presynaptic receptors to decrease sympathetic outflow, common side fx include bradycardia (decreased sympathetic activity and increased parasympathetic activity) and dry mouth
guanabenz
similar to clonidine more selective for alpha-2 receptors, less side effects
guanfacine
similar to clonidine
methyldopa
precursor to methylnorepinephrine, alpha-2 receptor agonist, decreases sympathetic outflow by activating presynaptic receptors, used for hypertension, especially in pregnant women (safer in pregnancy), has potential rare side effects of hepatotoxicity and autoimmune hemolytic anemia
dobutamine
beta-1 receptor agonist, used for acute management of decompensated heart failure (really a racemic mixture that has different effects depending on the stereoisomer)
isoproterenol
beta-1 and beta-2 receptor agonist, good for asthma but has cardiac side effect (beta-1 mediated), supplanted by newer selective drugs
metaproterenol
beta-2 selective agonist, used to treat obstructive airway disease and acute asthma via beta-2 receptor-mediated bronchodilation
terbutaline
beta-2 selective agonist, used to treat obstructive airway disease and acute asthma via beta-2 receptor-mediated bronchodilation
albuterol
beta-2 selective agonist, used to treat obstructive airway disease and acute asthma via beta-2 receptor-mediated bronchodilation
salmeterol
long-acting (12hr) beta-2 receptor agonist, bad for acute bronchoconstriction, may be good for prophylaxis
phenoxybenzamine
alpha-1 and alpha-2 receptor antagonist, used predominantly for pheochromocytomas and benign prostatic obstruction and HTN, many potential side effects and inductions of compensatory responses
phentolamine
reversibe, nonselective alpha-adrenoceptor antagonist, used for preoperative management of pheochromocytomas and HTN; many potential side effects and inductions of compensatory responses
prazosin
alpha-1 receptor antagonist, decreases peripheral resistance and preload, used to treat HTN and CHF; may have marked hypotension so first dose is given in small quantities
terazpsom
alpha-1 receptor antagonist, decreases peripheral resistance and preload, used to treat HTN and CHF; may have marked hypotension so first dose is given in small quantities, longer halflife than prazosin
doxazosin
alpha-1 receptor antagonist, decreases peripheral resistance and preload, used to treat HTN and CHF; may have marked hypotension so first dose is given in small quantities, longer halflife than prazosin
tamsulosin
alpha-1A receptor antagonist (found on prostate), used to treat BPH
yohimbine
alpha2 receptor antagonist, was used for ED, not used really anymore
propanolol
beta1 and beta2 antagonist, used to treat HTN and angina, may have decreased libido side effect (CNS effect)
nadolol
beta1 and beta2 antagonist, used to treat HTN and angina, may have decreased libido side effect (CNS effect)
timolol
beta1 and beta2 antagonist, used to treat HTN and angina, may have decreased libido side effect (CNS effect), ocular formulation used to treat glaucoma
labetalol
blocks alpha1 beta1 and beta2 receptors, used for HTN treatment, potential hepatoxicity requires close monitoring
carvedilol
blocks alpha1 beta1 and beta2 receptors, used for HTN treatment,
pindolol
partial agonist at beta1 and beta2, blocks action of NE at beta1 receptor, useful for hypertension but agonistic effect on beta1 causes less of a decrease in HR, therefore better to be used in people with bradycardia and HTN
acebutolol
partial agonist of beta-1 adrenoceptors, no effect on beta2, used for HTN
esmolol
beta1 selective antagonist, 3-4 minute halflife, used for emergency beta-blockade (as in thyroid storm)
metoprolol
beta1 selective antagonist, 4-8 hour halflife, prolongs life expectancy in people with moderate to mild CHF and patients who have survived a first MI
atenolol
beta1 selective antagonist, 4-8 hour halflife
celiprolol
beta1 selective antagonist and beta2 selective agonist