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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