Drugs used for Cholinomimetic Drugs Flashcards
Direct Acting Choline Ester
MOA:
- Muscarinic agonist
- negligible effect at nicotinic receptors
C/A:
Postoperative and neurogenic ileus and urinary retention
Bethanechol
Direct Acting Choline Esters
MOA: Nonselective muscarinic and nicotinic agonist; otherwise similar to bethanechol; C/A: used topically almost exclusively for glaucoma
Carbachol
Direct Acting Muscarinic Alkaloid or Synthetics
MOA: Like bethanechol, partial agonist
C/A : Glaucoma; Sjögren’s syndrome
Pilocarpine
Direct Acting Muscarinic Alkaloids or Synthetics
MOA: Synthetic M3-selective;similar to pilocarpine
Cevimeline
Direct Acting Muscarinic Alkaloids or Synthetics
MOA: Synthetic M3-selective;similar to pilocarpine
Cevimeline
Direct Acting Nicotinic Agonists
MOA: Agonist at both Nn and Nm receptors
C/A:
- Medical use in smoking cessation
- nonmedical use in smoking and in insecticides
Nicotine
Direct Acting Nicotinic Agonist
MOA: Selective partial agonist at α4β2 nicotinic receptors;
C/A: used exclusively for smoking cessation
Varenicline
Short Acting Cholinesterase Inhibitor
MOA: Alcohol, binds briefly to active site of acetylcholinesterase (AChE) and prevents access of acetylcholine (ACh)
C/A: Diagnosis and acute treatment of myasthenia gravis
Edrophonium
Intermediate - Acting Cholinesterase Inhibitor (Carbamates)
MOA: Forms covalent bond with AChE, but hydrolyzed and released
C/A:
- Myasthenia gravis
- postoperative and neurogenic ileus and urinary retention
Neostigmine
Intermediate - Acting Cholinesterase Inhibitor (Carbamates)
MOA: Forms covalent bond with AChE, but hydrolyzed and released
C/A:
- Myasthenia gravis
- postoperative and neurogenic ileus and urinary retention
Neostigmine
Intermediate - Acting Cholinesterase Inhibitor (Carbamates)
MOA: Like neostigmine, but longer-acting (4–6 h)
C/A: used in myasthenia
Pyridostigmine
Intermediate - Acting Cholinesterase Inhibitor (Carbamates)
MOA: Like neostigmine, but natural alkaloid tertiary amine
C/A : enters CNS
Physostigmine
Long Acting Cholinesterase Inhibitors (Organophosphates)
MOA: Like neostigmine but released more slowly
C/A: Obsolete: was used in glaucoma
Echothiopate
Long Acting Cholinesterase Inhibitors (Organophosphates)
Insecticide, relatively safe for mammals and birds because metabolized by other enzymes to inactive products; some medical use as ectoparasiticide
Malathion
Long Acting Cholinesterase Inhibitors (Organophosphates)
Insecticide, dangerous for all animals; toxicity important because of agricultural use and exposure of farm workers
Parathion
Long Acting Cholinesterase Inhibitors (Organophosphates)
“Nerve gas,” used exclusively in warfare and terrorism
Sarin