Cholinergics and Anticholinergics Flashcards
What aids in the release and Acetycholine?
ChAT- choline acetyltranferase
VAMP- vescicle- associated membrane proteins
SNAP- synaptasome-associated proteins
AchE- Acetylcholinesterase
Cholinergic agents
AKA cholinergic agonists, parasympathomimetics, cholinomimetics
Mimics Acetylecholine (ACh)
Cholinoceptors
Mediates the parasympathetic activity
Muscarinic and nicotonic receptors
M1 receptor
Nerves, CNS, ENS
Pirenzepine and telezepine
Pirenzepine
Inhibits gastric acid secretion and reduces muscle spasm
Treatment of peptic ulcers
Chronic obstructive pulmonary disease
Telezepine
More potent inhibitor of gastric acid than pirenzepine
Treating peptic ulcers in humans
M2 receptor
Heart, nerves, smooth muscle (cardiac M2)
Tripitramine and methoctramine
Tripitramine
Selective antagonist for M2 receptors
Blocks cholinergic bradycardia
Methoctramine
Cardiac M2 muscarinic receptor antagonist
M3 receptor
Other visceral organs: bladder constriction, bronchoconstriction, increases exocrine gland secretion, increases gut motility, miosis via pupillary sphincter
Darifenacin and solifenacin
Darifenacin
Selective antagonist of M3 receptor
Treatment of overactive bladder
Solifenacin
Selective M3 receptor antagonist
Urinary antispasmodic, treatment of overactive bladder
Direct acting cholingeric stimulants
Acts directly on cholinergic receptors
Cholingeric (muscaneric) agonists
Includes cholinesters (acetylcholine, methacholine, bethanechol, carbachol) and alkaloids (muscarine and pilocarpine)
Indirect acting cholinergic stimulants
Inhibits the breakdown of AcH by inhibiting cholinesterase
Includes carbamates (reversible) and phosphates (irreversible)
Why is ACh administration difficult in clinics?
Non selective (acts everywhere)
Rapidly deactivated (AChE and short half-life)
Cholinesters and natural alkaloids
Absorption: polarity dependent, IV IM and SQ for local effects
Metabolism: AChE dependent
Therapeutic uses for muscarinic agonists
Treatment of urinary bladder disorders, xerostomia (dry mouth), diagnosis of bronchial hyperreactivity, opthalmology , glaucoma treatment
Pharmacological effects that AcH has on the cardiovascular system
Inhibitory effects:
Vasodilation
Decrease in HR, conduction velocity in AV node and force of cardiac contraction
Pharmacological effects that AcH/ cholinergic drugs has on the GI tract
Excite the smooth muscles of the GI tract
Increased activity, motility, secretion and urinary frequency
Pharmacological effects that AcH/ cholinergic drugs has on the eye
Miosis (constriction) and decreased intraocular pressure
What overall effects does does AcH/ cholinergic drugs have on the body
Increased secretion from every body system
Increased salivation and sweating