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25 Cards in this Set

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Acetylcholine (ACh)

Muscarinic Agonist - Choline ester


- quaternary - no CNS


- sensitive to cholinesterase


- M receptors and N receptors


- topical on conjunctiva - local

Carbachol

Muscarinic Agonist - Choline ester


- quaternary - no CNS


- not sensitive to cholinesterase


- M3 > M1 > M1


- affect N receptors


- topical on conjunctiva - local

Bethanecol

Muscarinic Agonist - Choline ester


- quaternary - no CNS


- not sensitive to Cholinesterase


- M3 > M1 > M2


- No N activity


- PO, SC administer ** avoid IV/IM admin**


- systemic effects

Pilocarpine

Muscarinic agonist - natural alkaloid


- tertiary amine - enter CNS


- M receptors only


- glaucoma treatment


**drug of choice for emergency IOC reduction


- xerostomia (dry mouth from radiation or Sjogren) - oral

Muscarine

Muscarinic agonist - nature alkaloid (mushrooms)


- quaternary amonium - still can enter CNS


- M receptors only


- no therapeutic uses

Nicotine (carbachol)

Nicotinic agonist

Edrophonium

Reversible cholinesterase inhibitor


- short acting 10-20min


- diagnose MG (diff MG from cholinergic crisis)


- if muscle power improve = MG

Physostigmine

reversible cholinesterase inhibitor


- tert amine = CNS -> convulsion in high dose


- glaucoma


- bladder/intestinal atony


**antidote in atropine poisioning**

Neostigmine

reversible cholinesterase inhibitor


- last 0.5-2hr


- quat amine -> no CNS action


- poor oral absorption


- treat paralytic ileus, urinary retention, treat symptoms of MG

Donepezil

reversible cholinesterase inhibitor


- lipid soluble


- treat Alzheimer's

Organophosphates (parathion, etc)

irreversible cholinesterase inhibitor


- bind covalently to AChE -OH in active site


- need to make new


- nerve gas agents


- can be used for glaucoma


**atropine is antidote

Pralidoxime

AKA PAM = Cholinesterase reactivators


- oxime ->


** give as soon as possible to -aging**

MOA of Cholinergic agonists

all Choline esters and natural alkaloids activate M1, M2, M3 receptors


- postsynaptic -> alter function of effector organ


- presynaptic -> inhib release of NT

choline esters and nicotinic receptors

some choline esters -> activation ->


- initial => depolarize postjunction mem -> AP -> response in effector organ


- depolarization blockade = prolonged activation of N receptors -> no depol -> no further AP -> response of organ is blocked

Pharm effects of Cholinergic agonists

effects = that of postganglionic parasymp nerve impulses

Pharmacodynamics of Choline esters on the CVS (heart/vessels)

heart


- SA node -> -HR (M2 open K+ channels)


- atria -> -refractoriness, -contractility


- AV node -> -conduction, -automaticity, +refractoriness


- vent -> few recep -> few effects (-NE release)


**low dose -> direct effect counter by relfex tachy from vasodilation, high dose -> direct effect > relfex**




vessels


- general vasodilation (M3 -> NO release)

Pharmacodynamics of Choline esters on the GI and endocrine

GI


- +tone, +contract (peristaltic), +secretions of GI


- relax sphincters (N stim in ganglionic peptidergic neurons), pure M agonist -> -effect


- contract lower esophageal sphincter


Endocrine


- mild insulin secretion

Pharmacodynamics of Choline esters on the GU system

GU = Micturition


- +uretal peristalsis


- contract detrusor


- relax trigone and internal sphincter (decr effect if pure M agonist)


- erection (negligible on uterus)

Pharmacodynamics of Choline esters on the eye

Eye


- contr sphinter of iris


- contract ciliary muscle ->


- +lens curve -> near vision focus


- +aq humor outflow schlem cannal


- incr secretion of lacrimal glad

Pharmacodynamics of Choline esters on the respiratory system

Repiratory


- bronchial sm muscle contract


- +tracheobronchial secretions


skin


- +sweat gland secretions

Pharmacokinetics of choline esters

absorption - oral = low (hydrophilic, hydrolized in GI)


Dist = in periph tissue only (quaternary amines dont cross BBB to CNS)


biotransform - ACh by acetylcholinesterase


excretion - kidney

choline esters


- adverse effects when locally admin (eye)

ACh and carbachol


- vision problem (far and dim light)


- reddening stinging of the conjunctiva


- cataract - long term


- retinal detachment - long term

choline esters


- adverse effects when systemic admin

bethanechol


- nausea (GI activity) & vomit (CTZ M receptor)


- abdominal pain, diarrhea


- cough (bronchospasm and +secretions)


- sweating, acrimation, salivation


- flushing


- urinary urgency


- low BP

choline esters


- contraindication

local (eye)


- iritis, cataract, previous retinal detachment


systemic


- asthma/COPD


- cardiac arrhythmia, miocardial disease, CAD


- peptic ulcer, GI obstruct, IBD


- urinary tract obstruction


- hyperthyroidism

natural alkaloids


- MOA, Pharm effects, adverse effects, and contraindications

effects similar to choline esters except:


** greater for sweating and salivation**


- can enter CNS


- mycetism = mushroom poisoning