Term
What are the classes and subclasses of Cholinergic drugs? |
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Definition
Cholinomimetics/parasympathomimetics: 1. Direct acting ones - Cholinergic agonists 2. Indirect acting ones - acetylcholinesterase inhibitors Cholinergic antagonists/parasympatholytics 1. Muscarinic Antagonists 2. Nictoinic antagonists (ganglionic blockers and neuromuscular blockers) |
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Term
Name 1 choline ester and the receptor it targets. |
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Definition
Bethanechol - MUSCARINIC (bladder and GI hypotonia) |
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Term
What is a new M3 specific agonist? WHen is it used? |
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Definition
Cevimeline...to treat dry mouth in Sjorgen's syndrome patients |
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Term
Name 2 natural alkaloids that are choinergic agonists and the receptor they target. |
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Definition
Muscarine - from mushroom; obvi muscarinic receptor (that's how they discovered the diff. receptors) Pilocarpine - muscarinic (glaucoma) |
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Term
When do we use bethanechol? |
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Definition
WITH PATIENTS THAT HAVE DECREASED PARASYMPATHETIC TONE: Postoperative/postpartum - urinary retention and/or inadequate emptying of bladder Postoperative abdominal distension or GI tract atony or paresis. |
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Term
Where does bethanechol work? |
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Definition
M3's in urinary bladder, GI |
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Term
When do we use pilocarpine? |
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Definition
Glaucoma or xerostomia (dry mouth) |
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Term
What reverses the effect of atropine after an eye exam? |
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Definition
Pilocarpine - activates sphincter pupillae to constrict pupil (M3) |
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Term
What does the eye tolerate better: pilocarpine or AChE inhibitors? |
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Definition
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Term
How does pilocarpine decrease IOP? |
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Definition
constricts pupil , which reduces the angle block???? via M3 |
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Term
What is a warning with pilocarpine use? |
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Definition
Its a tertiary amine, therefore is kinda hydrophobic, therefore can get into the systemic system more easily....so we can see some parasym. responses nearby like runny nose |
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Term
How does pilocarpine work on the salivary gland? |
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Definition
AChR agonist acts on M3 on salivary gland to increase secretion |
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Term
Which one of these drugs is preferred for xerostomia? Pilcarpine, bethanechol, or cevimeline? |
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Definition
Cevimeline - greatest affinity for M3 on the salivary gland than the other 2. Less side effects |
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Term
When do we use cevimeline? |
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Definition
Irradiation of head/neck (destroys salivary gland and we need to get out as much as possible) Xerostomia assoicated with Sjogren's syndrome |
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Term
What is the special features of the MOA of cevimeline? |
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Definition
M3 agonist which is more selective, potent in action at the salivary and lacrimal glands than others. |
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Term
What the side effects of muscarinic agonists? |
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Definition
Diarrhea, Diaphoresis (sweat glands have muscarinic receptors), Miosis, Nausea, salivation, urinary urgency, CNS disturbances (for substances that can cross BBB - like pilocarpine) |
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Term
What are the 2 contraindications for muscarinic agonists? |
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Definition
ASTHMA (increases bronchoconstriction and increased mucous secretion) HEART DISEASE (slow conductivity of heart - M2's but still agonized by agonists designed to target M3's - arrhythmias can develop) |
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Term
What are pseudo cholinesterases? |
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Definition
non-specific, circulating esterases that cleave any ester bond. This is why we cannot clinically use ACh |
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Term
Where can AChE inhibitots work? |
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Definition
Anywhere pretty much - All visceral parasympathetics NMJ ALL autonomic ganglia |
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Term
-stigmine drugs are usually what? What other one with this too? |
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Definition
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Term
Where does neostigmine work? Can it X BBB? |
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Definition
Neuromuscular junction mostly! No, cannot X BBB. |
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Term
What drug is the best for treating myasthenia gravis? Why? |
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Definition
Neostigmine....greatest effects at NMJ (better than physostigmine) |
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Term
What are some adverse effects of Neostigmine? |
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Definition
generalized cholinergic stimulation and drop in BP Overdose: cholinergic crisis and muscle paralysis (via densitization from too much ACh) |
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Term
What is physostigmine used for? Can it X BBB? |
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Definition
Antidote for atropine overdose (and other anticholinergics) Reduces intraoccular pressure in glucoma (same mech. as pilocarpine) Hypotonia of bladder and GI YES can X BBB cuz its tertiary amine |
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Term
What are some adverse side effects of physostigmine? What about super high doses? |
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Definition
Diarrhea, nausea, sweating, miosis, urinary urgency High doses: convulsions (its Xed BBB), bradycardia and hypotension |
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Term
What are the symptoms of organophosphate poisoning? pneumonic? others not in pneumonic? |
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Definition
SLUD - salivation, lacrimation, urination, defecation Others: miosis, GI motility, emesis/vomitting and MAYBE confusion/halucinations if Xed BBB |
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Term
What do organophosphates do? |
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Definition
Irreversible, long-lasting AChE inhibitor They phosphorylate AChE...which will be degraded over time (called "aging"). Therefore it is considered an IRREVERSIBLE drug (after the point of aging) Aging can be 2 mins to hours, depends |
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Term
How do we treat organophosphate or nerve gas poisoning prophylactically and post-exposure? |
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Definition
Prophylaxis: Pyridostigmine if in danger of chemical warfare...this drug will block the site the poison is attempting to phosphorylate Post exposure: Use of muscarinic antagonists (atropine or scopolamine). This will inhibit all those extra ACh activity the organophosphates caused. An injection of PRALIDOXIME can chemically dephosphorylate AChE (rendering it active again) but ONLY before the "aging" process has occured. |
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Term
Edrophonium is a ____-acting ______ (rev./irrev.) AChE inhibitor |
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Definition
SHORT (the only short), therefore REVERSIBLE |
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Term
Physostigmine is a ____-acting ______ (rev./irrev.) AChE inhibitor |
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Definition
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Term
Neostigmine is a ____-acting ______ (rev./irrev.) AChE inhibitor |
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Definition
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Term
Pyridostigmine is a ____-acting ______ (rev./irrev.) AChE inhibitor |
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Definition
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Term
Rivastigmine is a ____-acting ______ (rev./irrev.) AChE inhibitor |
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Definition
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Term
Galantamine is a ____-acting ______ (rev./irrev.) AChE inhibitor |
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Definition
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Term
Ambenonium is a ____-acting ______ (rev./irrev.) AChE inhibitor |
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Definition
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Term
Donepezil is a ____-acting ______ (rev./irrev.) AChE inhibitor |
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Definition
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Term
Tacrine is a ____-acting ______ (rev./irrev.) AChE inhibitor |
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Definition
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Term
Name 2 synthetic organophosphates. What is their mode of inhibition and time frame |
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Definition
BOTH are long-lasting IRREVERSIBLE inhbitors of AChE Ecothiophate Isofluorophate |
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Term
Name 2 nerve gases. What is their mode of inhibition and time frame |
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Definition
Both are long-term and irreversible to AChE. Sarin and Soman |
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Term
Name 4 AChE inhibitors that treat myasthenia gravis. |
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Definition
Edrophonium (short - diagnostic test only) Neostigmine Pyridostigmine Ambenonium |
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Term
What AChE inhibitor treats hypotonia of bladder and GI? |
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Definition
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Term
What 2 AChE inhibitors treat Glaucoma? |
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Definition
Physostigmine and Ecothiophate |
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Term
What 4 drugs treat alzherimers? What is the MOA? What is their unique characteristics? |
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Definition
They ALL must X the BBB They are all AChE inhibitors Donepezil, Rivastigmine, Tacrine, Galantamine |
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Term
Name 2 belladona alkaloids? What do they do? |
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Definition
Atropine Scopolamine Muscarinic ANTAGONISTS |
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Term
Name 3 muscarinic antagonists that are synthetic. |
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Definition
Ipratropium Tiotropium Tolterodine |
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Term
What is the clinical use of atropine? |
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Definition
Severe bradycardia To produce mydriasis and cycloplegia (loss of accomodation) for exam of eye Suppress respiratory secretions prior to surgery Treat organophosphate (AChE inhibitors) poisoning & mushroom poisoning |
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Term
What is cyloplegia and what causes it? |
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Definition
Loss of accomodation of the eye...used during eye exams via ATROPINE |
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Term
What gets thru the BBB: atropine or scopolamine? |
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Definition
Both, but only scopolamine to a therapeutic level |
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Term
What is atropine used for? |
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Definition
Mydriasis, cycloplegia, reduction in GI motility and reduction of salivary,sweat, and lacrimal secretions |
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Term
What are the side effects of atropine? |
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Definition
Dry mouth, constipation, dilated pupils, blurred vision, hot/dry/flushed skin, tachycardia, fever, CNS disturbances (at very very high levels) |
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Term
What is the lowest amount of atropine we give? Why? |
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Definition
2.0 mg...anything under will actually decrease HR even more (complicated explaination) |
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Term
When is scopolamine used? |
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Definition
Sea sickness, opthalmic use, adjunct drug in anesthesia to produce sedation/amnesia |
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Term
What are the side effects of scopolamine? |
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Definition
much greater CNS side effects: drowsiness, amnesia, fatigue, loss of REM sleep |
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Term
What is ipratropium bromide used for? |
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Definition
Asthma and COPD as a bronchodilator in adjunct to albuterol OR just ipratropium Br by itself if patient cannot tolerate adrenergic agonists |
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Term
What is the MOA of ipratropium bromide? |
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Definition
Blockage of muscarinic receptors causing bronchodilation (but not very much decrease in mucocilliary clearance) |
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Term
What is tiotropium bromide |
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Definition
Muscarinic antagonist that has a GREATER ACTIVITY for M3 vs M2, therefore used in Asthma and COPD, with selective action toward the bronchioles |
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Term
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Definition
Muscarinic antagonist. Used to treat overactive bladder (reduce incontinence, frequecy, urge, and increase the amt of urine bladder can hold) |
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Term
What is the MOA of tolterodine? |
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Definition
Muscarinic antagonist...blocks M3 receptors on bladder and sphincter and calms down an overactive bladder |
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Term
WHat is the contraindication of M3 antagonists? |
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Definition
Slow voiding (urinary retention) EX - BPH |
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Term
What are the contraindications for giving muscarinic antagonists? |
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Definition
Glaucoma, BPH or any urinary/kidney condidtion, excessive constipation, myasthenia gravis (cuz when used with AChE inhibitor will MASK the symptoms of cholinergic crisis, which is something you NEED to be able to detect) |
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Term
Name some ganglionic blockers (nicotinic antagonists) |
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Definition
There are no nicotinic antagonists that act on the ganglions...at least none we need to know cuz they're never used |
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Term
Name the non-depolarizing NMJ blockers |
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Definition
Atracurium, cistracurium, vecuronium, rocuronium, pancuronium, tubocurarine |
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Term
Name the depolarizing NMJ blockers |
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Definition
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Term
What is succinyl choline? How is it broken down? |
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Definition
2 ACh's linked at one end Plasma cholinesterases degrade and NOT AChE's |
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Term
Succinylcholines have a ____ onset and ____ duration |
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Definition
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Term
Contrast Phase I and Phase II of depolarizing blockers MOA. |
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Definition
Phase I: SuCh acts as ACh and causes muscle fasiculation via depolarization, etc until receptors are desensitized. During phase 1, addition of AChE inhibitor will WORSEN the paralysis effects in the end. Phase II: SuCh might be blocking the nicotinic ion channels but either way receptors are desenstized by phase I and not even huge amounts of ACh can cause contraction, therefore AChE inhibitiors (which increase ACh at NMJ) would be worthless) |
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Term
What are some side effects of succinylcholine? |
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Definition
Muscle pain, hyperkalemia, blockage of ganglionic nictoinic receptors (decreased HR, increased IOP), MALIGNANT HYPERTHERMIA |
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