Cholinergic Drugs Flashcards
4 choline esters
Acetylcholine
Methacholine
Carbachol
Bethanechol
Choline ester properties
Charged
Poorly distributed to CNS
Metabolized by acetylcholinesterase (to some degree)
Muscarinic or nicotinic:
Acetylcholine
Both
Muscarinic or nicotinic:
Methacholine
Muscarinic
Muscarinic or nicotinic:
Carbachol
Both, more nicotinic
Muscarinic or nicotinic:
Bethanechol
What about it?
Muscarinic
Specifically affects urinary/GU system
4 alkaloids
Nicotine
Muscarine
Pilocarpine
Lobeline
Are alkaloids charged or uncharged?
Uncharged (absorbed into CNS) EXCEPT muscarine
Muscarinic or nicotinic:
Pilocarpine?
Muscarinic
Muscarinic or nicotinic:
Lobeline
Nicotinic
Danger of muscarine
Can cross BBB and be highly toxic (poison mushrooms)
MoA of indirect cholinergic agonists
AChE inhibitors
3 groups of AChE inhibitors
- Alcohols - reversible
- Carbamic acid esters - reversible but longer
- Organophosphates - irreversible (covalent)
Miosis during surgery
Acetylcholine, Carbachol, Pilocarpine
Urinary retention treatment
Bethanechol
Glaucoma treatment
Does what?
Carbachol, Pilocarpine
Contraction of ciliary body, fascilitating outflow of aqueous humor
Xerostomia treatment (dry mouth)
Cevimeline, Pilocarpine
Varenicline
Smoking cessation
Partial agonist for neuronal nicotinic receptors
Reduced but not eliminated dopamine release
Reduce cravings and withdrawal
Side effects of Varenicline
Neuropsychiatric symptoms - suicide
GI uses for cholinergic agonists
Post-operative ileus
Congenital megacolon
Esophageal reflux
SLUDGE
Muscarinic stimulant toxicity
Salivation, Lacrimation, Urination, Dehydration, GI issues (diarrhea), Emesis (vomiting)
Use for anti-nicotinic antagonists
Skeletal muscle relaxants
Uses for anti-muscarinic antagonists
Block parasympathetic effects of CNS, heart, nerves, SM, glands, endothelium
Prototypical muscarinic antagonist
Atropine
General function of anticholinergics
Increase sympathetics
Parkinson’s disease (CNS disorders)
Tertiary amines - benztropine, trihexyphenidyl, procyclidine
Antimuscarinics - reduce tremors due to loss of dopaminergic neurons in substantia nigra
Motion sickness
Scopolamine
Anesthesia
Atropine - block vagal responses for visceral surgery
W/ neostigmine to block parasympathetic effects
Must dilate eye for surgery. What to use?
Alpha-1 agonist rather than anticholinergic - shorter-acting with less side effects
Asthma, COPD
Ipratropium, Tiotropium Muscarinic antagonists (inhalation)
Lomotil
Atropine + opiate (diphenoxylate)
Antidiarrheal, discourages abuse of opiate
Urinary urgency treatment
Darifenacin, solifenacin, tolterodine
Selective M3 antagonists w/o major side effects
Treatment for cholinergic poisoning (insecticides, wild mushrooms, nerve gasses)
Atropine + pralidoxime (cholinesterase regenerator)
Contraindications for anticholinergics
Glaucoma
Prostatic hyperplasia
Acid-peptic disease
Contraindications for muscarinic agonists
Asthma
Hyperthyroid
Coronary insufficiency
Acid-peptic disease
Nicotinic poisoning causes
Tobacco
Insecticides
Acute nicotinic toxicity
Convulsions, skeletal muscle depolarization blockade (paralysis), respiratory paralysis, HTN, cardiac arrhythmias
Treating nicotinic toxicity
Atropine + Diazepam (anti-convulsant)
Charged AChE inhibitors
Edrophonium, pyridostigmine, neostigmine, echothiophate, ambenonium
Uncharged AChE inhibitors
Physostigmine, donepezil, galantamine, rivastigmine, tacrine
3 classes of cholinesterase inhibitors (+ examples)
- Alcohols (edrophonium)
- Carbamic acid esters (neostigmine, pysostigmine, pyridostigmine)
- Organophosphates (Echothiophate, parathion, malathion, sarin, soman, tabun)
Oxybutynin
M3 selective antagonist (w/ bad side effects)
Better to use Darifenacin, Solifenacin, Tolterodine
Fixing depolarized skeletal muscle block
Neostigmine (AChE inhibitor) + atropine/glycopyrrolate