Cholinergic Agonists and Antagonists Flashcards
Muscarinic Receptors
GPCR receptors M1,M2,M3
M1 Receptors
Increases IP3, DAG and therefore Calcium
Activated myenteric plexus for GI motility and secretions
M2 Receptors
Open potassium channels to decrease heart rate and contractility
Decrease cAMP and Calcium at sympathetic nerves to decrease NE release
M3
Increase Ip3, DAG and calcium
Contract ciliary muscles for accomodation and AH drain
Contract GI, bladder and bronchiolar muscle
Secretions at GI, sweat, tear, salivary glands
Nicotinic Receptors
Ligand gated ion channels
Pentameric structures that open upon ACH binding and cause flow into the cell to initiate downstream effects
Nn
Postganglionic sympathetic and parasympathetic cells
Nm
Neuromuscular junction
Direct Acting Nicotinic
Nicotinic- nicotine, succinylcholine
Competitive Muscarinic Antagonists
Atropine, Scopalamine, Glycopyrrolate
Organophosphate Poisoning
SLUDGE or DUMBBELS
Treat with 2-PAM
SLUDGE and DUMBBELS
Sweating, LAcrimation, Urination, Diarrhea, Gastric Distress, Emesis
Diarrhea, Urination, Miosis, Bronchorrea, Bradycardia, Emesis, Lacrimation, Salivation
Atropine Poisoning
Blind as a bat (dilated, blurred vision) Mad as a hatter (Nervous, confused, hallucinate) Red as a beet (Flushed skin) Hot as a hare (hot skin) Dry as a bone (dry mouth, skin) Bowel and bladder lose their tone And the heart runs alone (tachycardia) Treat with physostigmine, lavage, lower temp, cathertization, barbituates
Nicotine
Activates neuronal nictoinic receptors and is used clinically to help with smoking cessation
Sucinylcholine
Depolarizing block of Nm receptors
Eliminated by butyryl cholinesterase
Used as a neuromuscular block during shock therapy or emergency intubation
Acetylcholine
Quartenary Nitrogen Analog
RAPID half life and is a nicotinic/muscarinic agonst
Eliminated by acetylcholinesterase
No therapeutic use