Acetylcholine is:
2. The neurotransmitter at the skeletal neuromuscular junction
How do autonomic cholinergic drugs affect synaptic activity?
by interacting with the acetylcholine receptor
Types of Cholinergic receptors
Muscarinic - found on peripheral tissues
Nicotinic- located at skeletal neuromuscular junction
Two categories of cholinergic drugs
Cholinergic Stimulants
Direct acting and Indirect acting (anticholinesterase) agents
Direct Acting Cholinergic drugs
MOA: bind directly to cholinergic receptor to activate it initiating a response
Drugs by condition:
Gastrointestinal and urinary bladder: Bethanechol
Glaucoma: Carbachol, Pilocarpine
Side effects: GI (nausea, vomiting, diarrhea), increase salivation, bradycardia, increased sweating, flushing
Indirect acting cholinergic stimulants
MOA: inhibit acetylcholinesterase enzyme found at all cholinergic synapses
Drugs by condition:
Alzheimer’s Disease (Aricept, Remingl, Exelon, Cognex)
Reversal of Neuromuscular Blockage
Myasthenia gravis
Reversal of Anticholinergic induced CNS toxicity
Side effects: GI (Nausea, vomiting, diarrhea), increase salivation, bradycardia, increased sweating, flushing.
Antimuscarinic anticholinergic drugs
MOA: block the postsynaptic cholinergic muscarinic receptor.
Drugs by condition/disease:
Multi-use (atropine)
GI ( Bentyl, hyoscyamine, homatropine) aka antispasmodics
Parkinson Disease (Benztropine, trihexyphenidyl)
Motion sickness (Scopolamine)
Urinary Tract (Detrol)
Respiratory Tract (Ipratropium, Tiotropium)
Side effects: dryness of mouth, blurred vision, urinary retention, constipation, tachycardia
Anticholinergic Drugs
Antimuscarinic anticholinergic drugs