Cholinergics Flashcards
What direct cholinergic agonists are sensitive to cholinesterase
Acetylcholine ++++, methacoline +
What drugs are direct pure mAChR agonists
Methacoline, bethanechol, pilocarpine
What direct cholinergic agonists can cross the membrane
Alkaloids
What direct cholinergic agonists are used to cause miosis in intraocular surgery
ACh, carbachol, pilocarpine
What direct cholinergic agonists is used to treat urinary retention
Bethanechol
What direct cholinergic agonist is used to treat heart burn
Bethanechol
What direct cholinergic agonists are used to treat glaucoma
Carbachol, pilocarpine
What direct cholinergic agonists is used to treat sjogrens/xerostomia
Pilocarpine
What direct cholinergic agonist is used to treat smoking
Varenicline
What are the side effects of varenicline
Nausea, neuropsychiatric
What are the symptoms of a muscarinic toxicity
Sludge. Salivation, lacrimation, urination, defecation, GI, emesis
What are the contraindications for direct cholinergic agonists
Asthma, hyperthyroidism, coronary insufficiency, acid peptic disease
What are the symptoms of nicotinic toxicity
CNS stimulation, skeletal m end plate depolarization, respiratory paralysis, hypertension, Arrhythmias
Tx for nicotinic toxicity
Atropine and diazepam
What are the 3 types of AChE inhibitors and what about their binding
Alcohols - reversible
Carbamic acid esters - reversible and longer lasting
Organophosphates - irreversible
What are the charged AChE inhibitors
Edrophonium, pyridostigmine, neostigmine, echothiophate, ambenonium
What are the neutral AChE inhibitors
Physostigmine, donepezil, galantamine, rivastigmine, tacrine
What are the uses for AChE inhibitors
Glaucoma, dementia, antidote to anticholinergics, reversal of neuromuscular paralysis, myasthenia gravis
What can cause anticholinergics poisoning
Atropine, antihistamine, TCAs, sleep aids, cold preparations
What are the symptoms of anticholinergics poisoning
Cutaneous vasodilation, anhidrosis, anhydrotic HTN, nonreactive mydriasis, delirium, hallucinations, reduced desire to urinate
What are the symptoms of AChE inhibitor poisoning
Sludge plus muscle fasciculations
Treatment for AChE inhibitor toxicity
Atropine and pralidoxine
Do choline esters cross membranes? Why?
No because they are permanently charged
Drugs used for cholinergic poisoning?
Atropine + pralidoxine
What are the anticholinergics used to treat parkinson disease
Tertiary amines - benzotropine, trihexyphenidyl, and procyclidine. This is used in combination with dopaminergic therapy.
What is the anticholinergic used to treat motion sickness
Scopolamine - PO,injection, transdermal
What are the role of anticholinergics in anesthesia? Ex?
Atropine is given to block responses to vagal reflexes induced by surgical manipulation of viscera.
Atropine or glycopryrrolate is paired with the cholinesterase inhibitor neostigmine to block its parasympathetic effects
What anticholinergics are used to prevent synechia formation in uveitis and irits (iris adhering to lens or cornea)?
Homatropine or atropine
What anticholinergics are used to treat asthma and COPD?
Ipratropium and tiotropium
What mAChR antagonists are used to treat GI hypermotility?
Lomotil - combination of atropine and diphenoxylate
What specific receptor is targeted for symptomatic relief in Tx of urinary urgency
M3
What are the selective M3 antagonists?
Oxybutynin, darifenacin, solifenacin, and tolterodine
What are the side effects of oxybutynin
dry mouth/eyes, dizziness, constipation, blurred vision
What are the adverse effects of antimuscarinic agents used to reduce GI secretion
Mydriasis (pupillary dilation) & cycloplega (paralysis of ciliary m - loss of accomodation)
What are the contraindications for anticholinergics?
Glaucoma, prostatic hyperplasiam acid-peptic disease
What are the symptoms of anticholinergic overdose?
Dry as a bone, blind as a bat, red as a beet, mad as a hatter, hot as a hare. Tx with AChE inhibitors
