Lectures 13 - 14: Cholinergic System 1 and 2 Flashcards
Treatment of anticholinesterase overdoses.
Atropine
Can cause prolonged/excessive skeletal muscle paralysis
Gentamycin (aka aminoglycosides)
Treatment of Parkinson’s disease and tardive dyskinesia.
Benztropine
Block of choline uptake
Hemicholinium
Is also an antiemetic.
Scopolamine (Hyoscine)
Oxime Compounds (cholinesterase re-activators)
Pralidoxime
Antispasmodic: relax GI tract and bladder.
Atropine
Direct acting cholinergic agonists
Pilocarpine
High dose: excitation effect such as restlessness, disorientation and hallucinations.
Atropine
Actions of Muscarinic Antagonists (atropine, Benztropine, Ipratropium, Scopolamine (Hyoscine))
-Peripheral
● Block secretions (saliva, bronchial, GIT, etc.).
● Dilates pupil (mydriasis).
● Mydriasis can precipitate narrow angle glaucoma in the predisposed.
● Relaxes ciliary muscle to cause cycloplegia (lens fixed for far vision).
● Tachycardia (block of vagal influence).
● Blocks GIT motility (constipation).
● Relaxes bronchial smooth muscles.
Choline esters (longer duration than Ach)
Bethanechol
Blocks the rate-limiting step (uptake of choline into the neuron)
Hemicholinium
Muscarinic antagonists (no action on nicotinic receptors)
Atropine
Blocks nicotinic receptors on skeletal muscles
Gentamycin (aka aminoglycosides)
Antisecretory: block secretions in the upper and lower respiratory tracts prior to surgery.
Atropine
Long-acting reversible anticholinesterases
Neostigmine, Physostigmine
Block of Ach storage
Vesamicol
Induce reactivation of enzymes inactivated by phosphorylation.
Pralidoxime
Adverse Effects of Muscarinic Agonists (Acetylcholine, Pilocarpine, Bethanechol)
-Hypotension:
● Due to vasodilation :
Caused by the muscarinic receptor mediated release of NO from endothelium.
● Also due to decreased cardiac output:
due to decreased heart rate and force of contraction.
● Reflex tachycardia often overrides bradycardia.
-Bronchospasm:
● No significance in normal individuals, but may precipitate asthma in asthmatics.
-Others:
● Nausea, vomiting, GIT cramps, and diarrhea.
Actions of Acetylcholine
-Heart: decreases heart rate and cardiac output.
-Blood vessels: vasodilation and decrease in blood
pressure.
-GI tract: increases salivary secretion and stimulates
intestinal secretion and motility.
-Lungs: enhanced bronchiolar secretions and
bronchoconstriction.
-Genitourinary tract: increased tone of the detrusor
urinae muscle causing the expulsion of urine.
-Eye: muscle contraction for near vision and pupil
constriction (miosis).
Irreversible (Long-acting) Anticholinesterases:
Organophosphates
War gases and pesticides.
Ecothiophate
Treatment of paralytic ileus and bladder atony
Neostigmine