Pharm ANS drugs

Description:	Pharm: ANS drugs
Category:	USMLE
Created by:	jsad on 2009-08-10

Question	Answer
which adrenergic receptors AREN'T innervated?	Beta-2
receptors causing miosis vs mydriasis in eye	miosis=M3, mydriasis=a1
how to tell if it is a1 or M3 being affected in pupil?	check for cycloplegia (M3)
this drug blocks Choline uptake into nerve terminal	Hemicholinium
ACh release blocking agent	Botulinum toxin
How does Botulinum toxin work?	interacts w/ synaptobrevin to prevent ACh release
Muscarinic receptors in Heart: Which type and what function?	type is M2. function is slows heart rate (SA node) and conduction (AV node). NO MUSCLE AFFECTS
Where are M1 receptors located?	GIT glands
Muscarinic affect on sphincters of GIT	relaxes all but lower esophageal sphincter
Do indirect agonists work on blood vessel muscarinic receptors?	NO b/c these receptors (M3) aren't innervated. Function via EDRF.
Are muscarinic agonists used in glaucoma?	Yes. ciliary muscle contraction assists in lowering IOP.
are there specific agonists/antagonists drugs for M1,M2,M3	NO. Muscarinic drugs (ag/antag) are nonspecific
Locations of nicotinic receptors (3)?	Adrenal medulla (release NE/Epi) Nn, Autonomic Ganglia Nn, Neuromuscular junction (Nm)
which are Gq coupled Muscarinic receptors?	M1, M3 (Gq=IP3/DAG/Ca2+)
Which are Gi coupled Muscarinic receptors?	M2 (Gi= decreased cAMP)
Which are Gs coupled Muscarinic receptors?	NONE. no cAMP producing M receptors.
Nicotinic receptor mechanism?	Na/K ion channel coupled.
Name the Muscarinic agonists (4)	ACh (duh), BethaneCHOL, MethaCHOLine, Pilocarpine
Use of Bethanechol?	Urinary retention/post op ileus
Use of Pilocarpine?	glaucoma, xerostomia (dry mouth)
Name AChE inhibitors (5 'groups')	Edrophonium, Physostigmine, Neostigmine/Pyridostigmine, Donepezil, Organophosphates (echoTHIOphate, malaTHIOn, paraTHIOn, sarin)
Use of Edrophonium?	distinguish between myasthenic crisis and cholinergic crisis
what's the difference btwn myasthenic crisis and cholinergic crisis?	myasthenic crisis = not enough ACh, cholinergic crisis= too much ACh
Which of the following AChE inh's enters CNS: neostigmin, physostigmine, pyridostigmine?	Physostigmine (tertiary Amine)
What AChE inh is used to treat Alzheimers?	Donepezil (CNS entry<--Lipid soluble)
ACHE inh poisoning?	DUMBBELSS diarrhea, urination, miosis, bradycardia, bronchoconstrxn, excitation (muscle/cns), lacrimation, salivation, sweating
If given atropine for AChE inh poisoning, where will affect of reversal bot be seen?	muscle...requires Pralidoxime
can atropine enter CNS?	yes, it's a tertiary amine
List of anti-muscarinics (6)	aTROPine, TROPicamide, ipraTROPium, scopolamine, benzTROPine, trihexyphenydyl
Use of ipratropium	Asthma/COPD
use of scopolamine	motion sickness
use of benztropine/trihexyphenidyl?	Parkinsonism and EPS of anti-psychotics
What are the only 3 locations that have naturally predominant SANS stimulation	arterioles, veins, sweat glands. If Nn are blocked, this is impt.
Antidote for atropine poisoning?	physostigmine
in adrenegric neurons, what is role of reserpine?	Blocks vesicle formation (Dopamine entry into vesicle for subsequent formation of NE)
function of guanethedine?	blocks NE vesicle release (exocytosis)
are a1 receptors present on arterioles or veins?	BOTH. arteriole contraction = increased TPR (afterload), venous contraction = increased preload
Renin release control is through which adrenergic receptors?	a1 and B1
which receptor stim causes decreased Renin	a1
which rec stim causes increased renin	B1
Which receptors control insulin release?	a2, B2
which rec stim causes increased insulin	B2
which rec stim causes decreased insulin	a2
affect of B2 stim in Uterus?	relaxation
affect of B2 stim in blood vessels?	vasodilation!! (un innervated)
effect of D1 rec in kidney?	vasodilation
Gq coupled adrenergic rec?	a1 (M1,M3)
Gi coupled?	a2, (M2)
Gs coupled?	B1, B2, D1
what are the a1 agonists?	Phenylephrine, Methoxamine
how will a1 stim affect BP/HR?	increased TPR= incr BP....leads to reflex bradycardia. No change in total pulse pressure
what are the a2 agonists?	methyldopa, clonidine
uses of a2 agonists?	methyldopa, clonidine used in mild-moderate HTN (cause decr. NE release)
which adrenergic agonists stimulates B1=B2?	isoproterenol
B1>B2?	dobutamine
B2 agonists?	salmeterol, albuterol, terbutaline
BP/HR affects of B1 and B2	B1= incr HR, incr stroke volume, incr CO, incr pulse pressure B2= decr BP (vasodilation)
norepinephrine affects what receptors?	a1,a2,B1 (NOT B2!!! therefore NEVER lowers BP)
which adrenergic rec causes lower BP?	B2!!!!!!!!!!!!
Epinephrine at low, med, high dose	low= isproteranol (B1=B2) med= dobutamine (B1>B2) high= norepinephrine (a1, B1)
how to differentiate high dose Epi from NE?	Epi has B2 affects, so if you give a1-block..BP will drop with Epi but not with NE.
why Epi given instead of NE during anaphylaxis?	B2 affect of Epi causes bronchodilation!
indirect adrenergic agonists mech of action?	Release NE from mobile pool
name 3 indirect adrenergic agonists	tyramine (wine/cheese), amphetamines, ephedrine
tyramine is metabolized by what enzyme	MAO-A (so if you take MAOi's, your tyramine levels go up and cause hypertensive crisis)
what are the non selective alpha blockers?	phentolamine, phenoxybenzamine
which non selective alpha blocker is comp inh, which is non comp inh?	comp= phentolamine, noncomp=phenoxybenzamine
selective a1 blockers?	prazocin, doxazocin, terazocin, tamsulosin
a2 blockers?	yohimbine, mirtazapine
which B blockers have B1 selectivity	A-M (acebutolol-->Metoprolol)
Which B blocker causes CNS depression	Propranolol
Which 2 B blockers have intrinsic sympathomimetic activity	Acebutolol, Pindolol
which B blockers have K+ blockade	sotAlol
which have combined a1 and B blockade	labetAlol, carvedIlol
what opens the angle of glaucoma: miosis or mydriasis?	miosis
what types of drugs can be used to cause miosis for closed angle glaucoma?	M agonists, AChE inh's
how can aqeous humor produxn be decreased	B blockers
what does B1 rec do to Myocyte	cAMP causes phosphorylation of Na+, K+, Ca2+ channels. M2 does opposite.