Unit 3- Cholinergic Agonists Flashcards
Ach
Cholinergic agonist, nonselective, short duration of action before degradation by cholinesterases
Ach Receptor Specificity
Susceptible to colinesterase, cardiovascular, GI, bladder, eye, and nicotinic action
Methacholine Receptor Specificity
Susceptible to cholinesterase, cardiovascular, GI, bladder, eye, and nicotinic action
Carbachol Receptor Specificity
Cardiovascular, GI, bladder, eye, and nicotinic action
Bethanechol Receptor Specificity
Cardiovascular, GI, bladder, and eye action
Pharmacologic Effects of Choline Derivatives
Similar to Ach administration
Physiological Response of Choline Derivatives
Not identical and varying in selectivity for organ systems
Bethanechol
Resistant to cholinesterase, promotes bladder contraction, contracts detrusor muscle
Carbachol
Topically induces miosis after cataract surgery
Pilocarpine
Stimulates exocrine secretion, GI contraction, constricts pupil, treats glaucoma, keratoconjunctivitis
Arecoline
Targets glands, smooth muscle, and myocardium,
Pilocarpine Adverse Effects
Local irritation and inflammation, can cause systemic vomiting/diarrhe
Indirect Acting Cholinergic Agonists
Inhibits acetylcholinesterase, enhances Ach effects at all cholinergic receptors in the body
AChE Function
Anionic region and esteratic site to bind Ach
Reversible AchE Inhibitors
Physostigmine, neostigmine, edrophonium, pyridostigmine
Physostigmine
GI movement, pupillary constriction, may cause twitching, no cardiovascular effects at therapeutic doses, bladder contraction, bronchiole contraction
Neostigmine
GI movement, stimulates nicotinic receptors, may cause twitching, no cardiovascular effects at therapeutic doses, bladder contraction and bronchiole contraction
Reversible Inhibitors Use
Reverse nondepolarizing neuromuscular blockign drugs, therapy of myasthenia gravis
Reversible Inhibitors Adverse Effects
Excess muscarinic action, increased GI motility, diarrhea, salivation, bradycardia
Irreversible AchE Inhibitors
Organophosphates phosphorylate AchE, preventing Ach inactivation
Organophosphate Posioning
Salivation, vomiting, defecation, GI motility, urination, bradycardia, hypotension, bronchoconstriction, twitching, paralysis
Pralidoxime
Reactivates AchE by removing phosphate group