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25 Cards in this Set

  • Front
  • Back

Acetylcholine (ACh)

Muscarinic Agonist - Choline ester

- quaternary - no CNS

- sensitive to cholinesterase

- M receptors and N receptors

- topical on conjunctiva - local


Muscarinic Agonist - Choline ester

- quaternary - no CNS

- not sensitive to cholinesterase

- M3 > M1 > M1

- affect N receptors

- topical on conjunctiva - local


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


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


Muscarinic agonist - nature alkaloid (mushrooms)

- quaternary amonium - still can enter CNS

- M receptors only

- no therapeutic uses

Nicotine (carbachol)

Nicotinic agonist


Reversible cholinesterase inhibitor

- short acting 10-20min

- diagnose MG (diff MG from cholinergic crisis)

- if muscle power improve = MG


reversible cholinesterase inhibitor

- tert amine = CNS -> convulsion in high dose

- glaucoma

- bladder/intestinal atony

**antidote in atropine poisioning**


reversible cholinesterase inhibitor

- last 0.5-2hr

- quat amine -> no CNS action

- poor oral absorption

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


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


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)


- 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**


- general vasodilation (M3 -> NO release)

Pharmacodynamics of Choline esters on the GI and endocrine


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

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

- contract lower esophageal sphincter


- 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


- 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


- bronchial sm muscle contract

- +tracheobronchial secretions


- +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


- 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


- 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