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54 Cards in this Set

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this drug prevents the uptake of choline into the presynaptic terminal of a cholinergic neuron
hemicholinium
this drug inhibits ACH release into the synapse?
botulinum toxin
these drugs inhibit acetylcholine breakdown by acetylcholine esterase into --> choline and acetate
ACHE inhibitors
Choline acetyl transferase does what ?
takes CHOLINE and ACETYL COA and forms ACETYLCHOLINE
BOTULISM toxin interacts w/ what protein to prevent ACH release?
synaptobrevin
what conditions are drugs that prevent ACH release used for?
- blepharospasm
- strabismus/hyperhydrosis
- dystonia
-cosmetics
this muscarinic receptor is located -->
- eye (sphincter/ciliary muscle)
- lungs (bronchioles/glands)
- gi tract (stomach/intestines)
- bladder
- sphincters, glands, endothelium of blood vessels
M3 muscarinic receptor
stimulation of pupillary sphincter and ciliary muscle in the eye via the m3 receptor does what?
- sphincter contraction --> miosis (pinpoint pupils)
- contraction of ciliary muscle --> accomodation for near vision
these muscarinic receptors are located on the heart ?
M2 receptors
- sa node
- av node
M2 stimulation in heart causes what?
- enhances parasympathetic tone on the heart
--> Sa node --> dcrse heart rate
--> av node --> dcrse condctn velocity
does m2 receptor stimulation have any effect on the ventricles of the heart?
no effects on the ventricles or the purkinje system of the heart
M3 receptor stimulation of the lungs causes what?
bronchioles contract --> bronchospasm
+secretions from the glands in the lungs (incrsd edema)
M1 receptors are responsible for what affects in the gi?
- m1 stimulation --> increases GI secretion
m3 stimluation in the stomach and intestines causes what?
stomach --> increase motlity and cramps
- contraction of intestines --> diarrhea and involuntary defecation
M3 bladder stimulation?
-contraction of detrusor
- relaxation of trigone/sphincter
- --> causes voiding and urinary incontinence
m3 receptor stimulation of sphincters?
all RELAX except for the Lower esophageal sphincter (contracts)
m3 stimulation of glands?
increased sweating , salivation and lacrimation
m3 stimulation of the blood vessels (endothelial cells)
dilation of the blood vessels via NO release
Nn stimulation in the adrenal medulla produces what catecholamines?
NE and E
autonomic ganglia stimulation does what ?
Nn Receptor --> net fx depends on overall combined fx of sympathetic and parasympathetic dominance
neuromuscular junction has what types of receptors? and respond to which stimulatory molecules?
- Nicotinic muscle receptors
- respond to NE and E
--> twitches --> hyperactive skeletal muscle
M1 and M3 are coupled with what g-protein?
Gq --> incrse IP3, DAG, Ca2+
M2 coupled to which g-protein?
Gi-inhibitory protein
- dcrses a.cyclase --> dcrse cAMP
NN and NM...any second messengers?
no second messengers... activation and opening of Na/K channels
name 4 muscarinic agonists
Ach, Betanechol, metacholine, pilocarpine
this drug has only MUSCARINIC activity, and is used for
- post op ileus
- urinary retention
BETHANECOL
this drug prefers M>N and stimulates AChE hydrolysis...used in the diagnosis of BRONCHIAL HYPERACTIVITY
Methacholine
this drug stimulates the M RECEPTORS only, and does NOT cause any ACHE hydrolysis... used topically for glaucoma and xerostomia
Pilocarpine
acetylcholinesterase inhibitors cause what to happen in the synapse?
increases levels of ACh due to inhibition of the enzyme that breaks down ACh (acetylcholinesterase)
- dx of myasthenia gravis
- differentiate from myasthenia and cholinergic crisis
Edrophonium - short acting
Rx of glaucoma, and is antidote for atropine overdose
Physostigmine (enters the cns)
Rx of ileus, urinary retention and myasthenia
- used to reverse the fx of NON-DEPOLARIZING NM blockers
Neostigmine, pyridostigmine
- no cns entry b/c quaternary amine
rx of alzheimers disease
Donepezil, tacrine
- lipid solube = cns entrance
rx of glaucoma and often used as insecticides
organophosphates
- ecothiophate (glaucoma)
- malathion,parathion (insecticides)
- sarin (nerve gas)
DUMBBELSS ?
ACHE inhibitor overdose --> poisoning effects seen in someone who overdosed
--> fx of having too much ACh in the synpase --> overload of muscarinic effects
DUMBBELSS?
D= DIARRHEA
u= urination
m=miosis
b= bradycardia
b= bronchoconstriction
e= excitation (mscle and cns) --> leads to paralysis
l= lacrimation
s= salivation
s= sweating
antidote for ache overdose? regeneration of ache?
atropine (muscarinic receptor antagonist)
- pralidoxime
name the prototype drug for MUSCARINIC RECEPTOR ANTAGONISTS
Atropine
what type of amine must atropine be in order to enter the cns?
tertiary amine
atropine fx on the body?
- dcrsed secretion
- mydriasis and cycloplegia (paralysis of accomodation)
- hyperthermia (via vasodilation = red face)
- tachycardia (incrsd risk for arrythmias)
- sedation --> sleepppy
- urnry retention and constipation (dcrsd gi motility )
what is a major sidefx of atropine?
dry mouth due to dcrsd gland secretion
what is the hallmark side effect of muscarinic blockade?
- tachycardia
give 6 other drugs that have atropine like fx in their pharm?
-antihistamines - all of them have some atropine like fx
- tca's
- antipsychotics
- quinidine
- amantadine (antiviral y parks rx)
- meperidine
tca's and antipsychotic overdose can lead to ?
the 3 c's...
- coma
- convulsions
- cardiotoxicity
what do u use to treat an overdose of atropine?
if symptomatic --> physostigmine
- 3* amine that blocks AChE --> thus increasing the breakdown of Ach in the cleft and causing a dcrse --> less Muscarinic stimulation
clinical uses of this drug are --> antispasmodic, antisecretory prior to intubation, management of ACHE overdose, antidarrheal, mydriasis of the eye (long acting 36-48 hours)
Atropine
this drug is a opthamological topical M-blocker with a few hours of fx
Tropicamide
used in asthma and COPD
- no cns entry and causes no change in mucus viscosity
Ipratropium
- causes bronchodilation via blockage of the Muscarinic M3 receptors in the lung
muscarinic blocker used in motion sickness
- causes sedation and short term memory loss
Scopolamine
these m-blockers are lipid soluble, and used in parks
- also used to manage the EPS symptoms caused by antipsychotics
Benztropine
- trihexyphenidyl
when is the SANS dominant in the body?
- vascular tone
- thermoregulatory sweat glands
when is PANS dominant in the body?
sa node
av node
pupil
gi/ gu muscles
sphincters
name 2 drugs that are used as Ganglion blocking agents (Nicotinic receptor antagonists)
hexamethonium
mecamylamine
moa of hexamethonium or mecamylamine?
reduce predominant autonomic tone
- prevent baroreceptor changes in heart rate