Neuro Pharm (Kruse) Flashcards
Methacholine
cholinergic agonist (used to diagnose bronchial airway hyperreactivity)
Carbachol
cholinergic agonist (used to treat glaucoma or produce miosis)
Bethanechol
cholinergic agonist (used to treat urinary retention and heartburn)f
Cevimeline
cholinergic agonist (used to treat xerostomia) metabolized via P450 >> excreted in urine
Pilocarpine
cholinergic agonist (used to treat head/neck cancer, glaucoma and produces miosis and salivation)
Varenicline
cholinergic partial agonist (used for smoking cessation and binds nicotinic receptors)
What are the 3 groups of AChE inhibitors and which ones can be used therapeutically (reversible)?
1) alcohols *
2) carbamic acid esters *
3) organophosphates
What is commonly used in a drug overdose and what is it combined with?
atropine (cholinergic antagonist) in conjunction with pralidoxime because it pulls organophosphates that are covalent/irreversible away from atropine
What are some CNS disorders that anticholinergics can treat?
1) Parkinson (benztropine, trihexyphenidyl and procyclidine)
2) motion sickness (scopolamine)
3) anesthesia (atropine, glycopyrrolate are paired with neostigmine)
Benztropine
anticholinergic (to treat Parkinson Disease)
Trihexyphenidyl
anticholinergic (to treat Parkinson Disease)
Procyclidine
anticholinergic (to treat Parkinson Disease)
Scopolamine
anticholinergic (to treat motion sickness)
What 2 drugs can treat uveitis and iritis?
ophthamologic disorders
homatropine and atropine (anticholinergics)
Homatropine
anticholinergic (to prevent synechia formation in uveitis and iritis)
What 2 drugs can be used to treat COPD?
ipratropium and tiotropium
What anticholinergic is used to treat common traveler’s diarrhea and what is it combined with?
diphenoxylate and atropine (added to reduce risk of abuse since diphenoxylate is an opiate)
What anticholinergic is used for GU disorders but has profound side effects?
oxybutynin
What anticholinergics are preferred for GU disorders because of their minimal side effects?
darifenacin, solifenacin, tolterodine
What are 3 contraindications for anticholinergics?
glaucoma, prostatic hyperplasia, acid peptic disease
What is glycopyrrolate and how does it work?
antimuscarinic in GI disorders and after anesthesia as it stimulate skeletal muscle by increasing the levels of ACh in the body
What are some charged AChE inhibitors?
neostigmine, edrophonium, pyridostigmine, echothiophate, ambenonium
What are some neutral AChE inhibitors and what can they do that charged ones cannot?
physostigmine, donepezil, galantamine, rivastigmine, tacrine –> they can cross the BBB
Major NT of sympathetic nervous system
norepinephrine
Contraindication for varenicline use
suicidal ideation or changes in mood
What are 3 big uses of direct-acting cholinergic agonists?
glaucoma, accommodative esotropia, GI/GU disorders
Contraindications for muscarinic stimulants?
asthma, hyperthyroidism, coronary insufficiency, acid peptic disease
Compare alpha adrenergic receptor agonists with mAChR antagonists in treatment of ophthalmologic disorders
alpha adrenergic agonists are shorter acting and produce less adverse effects, while mAChR antagonists are used when cycloplegia or prolonged mydriasis is required (LASIK)
What can cause cholinergic poisoning?
cholinesterase inhibitor insecticides, wild mushrooms, chemical warfare nerve gases
What are some acute symptoms of nicotinic agonist toxicity?
CNS stimulation, respiratory paralysis, HTN, cardiac arrhythmias
How do you treat acute toxicity from nicotinic stimulants?
Atropine (for excess muscarinic stim) and diazepam (for CNS stimulation)
