.
Found on postganlionic neurons of the parasympathetic nervous system
Ligand gated ion channels
Also found at neuromuscular junctions of the somatic nervous system
Gate for Na+
All are true
M1,3,5 are mainly stimulatory, couple to Gq
M2,4 are mainly inhibitory, couple to Gi
GPCRs found at sympathetic and parasympathetic sites
All are true
Blood pressure and flow
Metabolism
Blood glucose levels
Micturition and defecation
Pupillary light and accommodation reflexes
Glandular secretions
Bronchial dilation
Body temperature
Gastrointestinal movements and secretions
Compete with ACh for a common binding site on muscarinic receptors
Inhibit with ACh for a common binding site on muscarinic receptors
Compete with NE for a common binding site on muscarinic receptors
Inhibit with NE for a common binding site on muscarinic receptors
A. Direct is by parasympathetic fiber activation; decreases cardiac output
B. Indirect is by inhibition of NE secretion
C. Indirect is by inhibition of ACh secretion
A and b
A and c
Decrease in cardiac force of contraction
Decreased heart rate
Vasodilation
Decreased conduction rate in SA and AV nodes
Vasoconstriction
Increased heart rate
Carbechol
Arecoline
Pilocarpine
Muscarine
Bethanechol
Methacholine
Carbechol
Arecoline
Pilocarpine
Muscarine
Bethanechol
Methacholine
Smooth muscle
Vascular muscle
Cardiac muscle
Gland cell
Peripheral ganglia
CNS
Increase tone and motility of GI
Decrease tone and motility of GI
Actions are comparable to homotropine
Actions are not comparable to atropine
Tiotropium
Homatropine
Ipratropium
Tropicamide
Methylatropine
Cause euphoria; can also cause hallucination, delirium
Cause CNS depression (drowsiness, fatigue, amnesia, dreamless sleep, etc..)
Used in Parkinson’s disease as adjuncts to levodopa; also used to treat tardive dyskinesia
Cause mild vagus nerve inhibition by inhibiting medulla and higher brain centers
Cause mild vagus nerve excitation by stimulating medulla and higher brain centers
Phenothiazines
Histamine H1 antagonists
Tricyclic antidepressants
Beta blockers
Newer antipsychotic drugs
Calcium channel blockers
Some have high affinity for the anionic site of AChE (edrophonium is prototype)
Acid transforming inhibitors bind to AChE and form an intermediate acid-enzyme compound
Carbamated AChE cannot hydrolyze ACh
Bind AChE at the esteratic site
Form a stable but inactive compound
Some have high affinity for the anionic site of AChE (edrophonium is prototype)
Acid transforming inhibitors bind to AChE and form an intermediate acid-enzyme compound
Carbamated AChE cannot hydrolyze ACh
Bind AChE at the esteratic site
Form a stable but inactive compound
Carbamates and acridines
Nerve gases (sarin, tabun, soman
Tacrine
Carbaryl
Phystostigmine
Carbamates and acridines
Nerve gases (sarin, tabun, soman
Tacrine
Carbaryl
Phystostigmine
Edrophonium
Physostigmine
Neostigmine
Diazinon
Edrophonium
Physostigmine
Neostigmine
Diazinon
Edrophonium
Physostigmine
Neostigmine
Diazinon
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