Drugs That Affect Acetylcholine Flashcards
Are there any therapeutic applications for acetylcholine? why or why not?
no, effects would be widespread and the metabolism of Ach by acetylcholinesterase happens rapidly
What is the acronym to remember Ach cholinergic agonist effects?
DUMBBELLS
- Diarrhea
- Urination
- Miosis/muscle weakness
- Bradycardia
- Bronchoconstriction
- Excitation or emesis
- Lacrimation
- Lethargy
- Salivation
What are the side effects of anticholinergic antagonists?
anti-DUMBBELLS (side effect in the (parentheses)
- Diarrhea (Constipation)
- Urination (Urinary retention)
- Miosis (Mydriasis/blurry vision)
- Bradycardia (Tachycardia)
- Bronchoconstriction (Bronchodilation)
- Excitation (Paralysis)
- Lacrimation (Dry eyes)
- Lethargy (Stimulated)
- Salivation (Dry mouth)
can’t see, can’t pee, can’t spit, can’t shit
What do M1 receptors do?
found in CNS and GI tract
what do M2 receptors do?
decreased heart rate and decreased atrial contraction
what do M3 receptors do?
- activates sweat glands
- increases GI motility
- increases bladder contraction
- bronchoconstriction
what drugs are muscarinic agonists that are choline esters?
- Acetylcholine
- Methacholine
- Carbachol
- Bethanechol
what drugs are muscarinic agonist that are naturally occurring cholinomimetic alkaloids?
- Pilocarpine
- Cevimeline
- Adenosine
what are therapeutic uses of muscarinic agonists?
- urinary bladder disorders
- xerostomia
- ophthalmology: miotic agents and glaucoma
- supraventricular tachycardia (SVT) - adenosine - stops heart and resets
when is Pilocarpine indicated? What is the SE
I:xerostomia, topically for glaucoma
SE: sweating (DUMBBELLS)
what is the advantage of cevimeline?
- longer acting than pilocarpine
*stimulates the salivary gland longer than pilocarpine
*less side effects than pilocarpine
what does cevimeline activate?
- Preferentially activates M1 and M3 receptors on lacrimal and salivary gland epithelia so also used for xerostomia
what does adenosine do?
Slows and “stops” conduction through the AV node
when is adenosine indicated?
treatment of SVT
what is the dosing of adenosine?
6 mg push, then 12 mg push x2
*half life is less then 10 secs
what do acetylcholinesterase inhibitors do?
prevent breakdown of acetylcholine
what are the acetylcholinesterase inhibitors?
- Donepezil (alz)
- Galantamine (alz)
- Physostigmine (myasethenia gravis)
- Neostigmine (Mg)
- Pyridostigmine (Mg)
- Rivastigmine (alz)
what is Donepezil used for?
approved for clinical use and treatment of Alzheimer’s disease
*Primary agent
what is the SE of Donepezil
DUMBBELLS
what is Rivastigmine used for?
- Indicated for treatment of Alzheimer’s disease
- Much more lipophilic and has longer duration of action
what IS Pyridostigmine used for
myasthenia gravis
* less lipophilic than Alzheimer’s drugs
when is atropine indicated?
Symptomatic bradycardia in the ACLS algorithm
What is the SE of atropine
ANTI-DUMBBELLS
what is a use of muscarinic antagonist?
COPD/asthma
how are muscarinic antagonists used for COPD/asthma?
- inhalation
*Will limit side effects
what drugs are a short acting muscarinic antagonist?
Ipratropium (Atrovent)
what drugs are a long acting muscarinic antagonist?
Tiotropium (Spiriva)
how are muscarinic antagonists used in overactive bladder?
block muscarinic receptors in the urinary tract leading to decreased bladder contraction and a decrease in urination
- more selectivity and few side effects
what muscarinic antagonists are used in overactive bladder?
Oxybutynin (Ditropan)
what muscarinic antagonists are used for motion sickness, post-op n/v?
Scopolamine
what are the depolarizing neuromuscular agents?
Succinylcholine
what are the nondepolarizing neuromuscular agents?
- Rocuronium
- Vecuronium
- Cisatracurium
What are the indications for neuromuscular blockers
- Muscle relaxation in rapid sequential/endotracheal tube
- Muscle relaxation during surgery
- Control of muscle tone following cardiac arrest
what drug is used for nicotine replacement therapy?
Varenicline (Chantix)
*partial nicotinic agonist
what are contraindications of atropine?
Tachycardia
what are contraindications of amitriptyline?
patients with urinary retention issues
