Cholinergic agonists And AChe Inhibitors Flashcards
What are the muscarinic agonists?
BCAP
Bethanechol ( Uricholine)
Cevimeline ( Evoxac)
Acetylcholine ( Michol - E)
Pilocarpine (Salagen)
What are Organophosphates?
Malathion
Sarin
What are reversible AchE inhibitors?
PEND
Pyridostigmine ( Mestinon)
Edrophonium ( Tensilon)
Neostigmine ( prostigmin)
Donepezil ( Aricept)
What are Cholinesterase reactivators
Pralidoxime (protopam)
What are the main drug strategies to intensify ACh neurotransmission?
Direct activation of ACh receptors
- nicotinic cholinergic receptor agonists
- increase cognition in dementia
- Smoking cessation - Muscarinic cholinergic receptor agonists
- enhance parasympathetic function to treat urinary retention, glaucoma and xerostomia
What are the main drug strategies to intensify ACh neurotransmission.
(2) AchE inhibitors increase the lifespan of ACh in the synapse.
- Myasthenia gravis, dimentia
- Chemical warfare insecticides
Nicotinic receptor facts
Excitatory ligand gated ion channels
Nn
Nm
Activated by nicotine
Muscarinic receptor facts
Mushroom
M1- M5
Glycoprotein- Coupled Receptors
Excite or Inhibit
Why does exogenous ACh not have widespread cholinergic activation?
Rapid plasma breakdown
Does not reach peripheral synapse
Does not penetrate BBB
How does peripheral mAchR agonist affect the heart?
It lowers BP and Heart workload
Decreased heart rate (M2)
Decreased conduction velocity
Vasodilation ( M3)
How does increased mAchR agonist affect the lungs
Respiratory tract - Bronchoconstriction
Smooth muscle
How does increase mAchR agonism affect the bladder
Bladder voiding
How does mAchR affect the GI
Increased GI motility and secretion
How does maAchR agonist affect the salivary and sweat glands?
Stimulate secretion of salivary, nasalpharyngeal, lacrimal and sweat glands
How does mAchR agonism affect the eyes?
Pupillary contraction accommodation of lens for near vision.