Cholinomimetics Flashcards
Pilocarpine (Salagen) Class
Direct Acting non-ester
Pilocarpine MOA
Direct acting muscarinic cholinomimetic
Pilocarpine (Salagen) Treatments
Glaucoma
ACh activates sphincter and ciliary muscle constriction to increase drainage of aqueous humor and decrease IO pressure
Pilocarpine (Salagen) Side Effects
SLUDGE
Cevimeline (Evoxac) Class
Direct Acting non-ester
Cevimeline (Evoxac) MOA
Direct acting muscarinic cholinomimetic
Cevimeline (Evoxac) Treatments
Dry mouth (ex. Sjogen’s, post radiation therapy; via increased salivation)
Nicotine (NRT) Class
Direct Acting non-ester
Nicotine (NRT) MOA
Direct acting nicotinic cholinomimetic, reduces cravings
Nicotine (NRT) Treatment
Smoking cessation
Cevimeline (Evoxac) Side effects
SLUDGE
Neostigmine Class
Indirect Acting
Neostigmine MOA
AChE Inhibitor (Short Acting)
Neostigmine Treatment
Post-operative and neurogenic ileus, urinary retention, myasthenia gravis (increasesmuscle strength for 0.5-2 hrs), reversal of neuromuscular blockade
Donepezil (Aricept) Class
Indirect Acting non-ester
Donepezil (Aricept) MOA
AChE Inhibitor
Donepezil (Aricept) Treatment
Alzheimer’s (amplifies endogenous ACh in brain)
Edrophonium (Enlon) Class
Indirect acting non-ester
Edrophonium (Enlon) MOA
AChE inhibitor
Edrophonium (Enlon) Treatment
Myasthenia gravis
Direct Acting Cholinergic Agonists MOA
Bind directly to nicotinic or muscarinic cholinoreceptors. May be esters or non-esters of choline
Physiologic effects of direct acting Cholinergic agonists
Decrease HR and CO
Decrease BP via vasodilation
Increase salivation, sweat, and lacrimal production
Stimulate intestinal secretions and motility
Increase bronchial secretions
Contract detrussor muscle of bladder
Pupilary constriction
Primary clinical uses of direct acting cholinergic agonists
- Diseases of the eye (Glaucoma)
- Decreased secretions
- GI and urinary tract disorders esp. post operative
Indirect Acting Cholinergic Agonists MOA
Prolong the life of ACh in synapse by inhibiting ACHesterase. This increases the effect of ACh
Pralidoxime PAM (Protopam) Class
Strong nucleophile
Pralidoxime PAM (Protopam) MOA
Regenerates phosphorylated AChE
Pralidoxime Treatment
Antidote to poisoning by nerve gas or insecticide
Sarin Class
Indirect acting organophosphate
Sarin MOA
AChE inhibitor
Sarin Treatment
Volatile nerve gas
Antidote to indirect acting cholinergic agonists
PAM and atropine
Toxic effects of cholinergic receptor activating drugs
SLUDGE Salivation Lacrimation Urination Defecation GI Distress Emesis
Antidote to direct acting cholinergic agonists
Atropine
Muscarinic receptors that lead to excitation
M1, M3, M5
Muscarinic receptors that lead to inhibition
M2, M4
Location of M1 receptors
Gastric parietal cells
Location of M2 receptors
Cardiac cells and smooth muscle
Location of M3 receptors
bladder, exocrine glands, smooth muscle
Location of nicotinic receptors
CNS, adrenal medulla, autonomic ganglia, NMJ
Physostigmine (Esterine) Class
Indirect acting carbamate
Physostigmine (Esterine) MOA
AChE inhibitor (short acting)
Physostigmine (Esterine) Therapeutics
Glaucoma (ACh activates papillary sphincter and ciliary muscles of the eyes)
Physostigmine (Esterine) SE
SLUDGE and general increase in cholinergic neurtotransmission, paralysis
Direct acting cholimimetics MOA
Bind directly to cholinergic receptors
Indirect acting cholimimetics MOA
Inhibit acetylchloinesterase, therefore ACh is not broken down in the synaptic cleft and more is available to send signals