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37 Cards in this Set
- Front
- Back
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Name the two types of cholinergic receptors and describe their functional difference.
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Muscarinic - G protein receptors
Nicotinic - Ion channel receptors |
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What is the function of an M1 receptor?
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Activates myenteric plexus
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What is the function of an M2 receptor?
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Decreases heart rate, and NE release from sympathetic nerves
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What is the function of an M3 receptor?
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Contracts ciliary muscle, bronchiolar muscle, GI smooth muscle, detrusor muscle
Stimulates secretion from GI, eccrine sweat glands, and salivary glands. |
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Name two nicotinic receptor agonists and their medical uses.
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Nicotine (smoking cessation aid)
Succyinylcholine (muscle relaxant) |
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Can quaternary nitrogen analogs cross the BBB?
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No.
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What is methacholine? What are its primary effects?
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It is a quaternary N chonlinergic drug. It prefers M type receptors and is non selective. So its effects are bronchoconstriction, secretions, sweating, etc
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What is the clinical indication of methylcholine?
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Diagnostic for sub clinical asthema
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What are the toxicities and contraindications of methylcholine?
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The toxicicity is bronchoconstriction.
The contraindication is B blockade (this would exacerbate what...) |
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What is carbacol? What are its receptor selectivities?
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Carbacol is a non-selective cholinergic drug with a quaternary nitrogen.
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What are the indications of carbacol? Describe its function in these indications.
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Glaucoma and ocular surgery. It constricts the ciliary muscles causing pupilary dilation. This opens the tribecular meshwork accommodating the exit of aqueous humor.
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What is Bethanechol? What are its receptor selectivities?
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Bethanechol is a muscarinic selective cholinergic drug. Its primary action is on M1 and M3 receptors at clinical levels.
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What are the indications of bethanechol?
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Bladder atony, post operative urinary retention.
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What are the contraindications and toxicities of bethanechol?
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Toxicity: Bradycardia (only in OD)
Contraindications: Ulcers, asthma, bradycardia |
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What is Muscarine and where does it come from?
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Muscarine is a quaternary purely muscrinic cholinergic agonist. It is a degradation resistant toxin.
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What is Pilocarpine and what receptor affinity does it have?
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Pilocarpine is a non-selective muscarinic agonist. It has a tertiary nitrogen and can cross the BBB.
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What are the indications of Pilocarpine?
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Dry mouth and neck from radiotherapy, Sjogren's syndrome, (an autoimmune disease affecting salivary glands) and narrow angle glaucoma (obstruction at the lens/cornea interface)
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What are the toxicities of Pilocarpine
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Generally excess muscarinic stimulation (bradycardia, bronchoconstriction, hypotension, excessive salivation)
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How do indirectly acting cholinomimetics work? (give general and specific answers)
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By inhibiting AChE and butrylcholinesterase (a variant in plasma, liver, glia)
Specifically by preventing or slowing the enzyme from going back into its active form after it catalyzes a reaction. |
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What is neostigmine? What are its effects?
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It is an indirect cholinomemetic with a quatinary nitrogen. It increases the amount of Ach at the NM junction.
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What are the indications of neostigmine?
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Myasthenia gravis, reversal of NM blockade in reversal of anesthesia.
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What are the toxicities and contraindications of neostigmine?
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Toxicity: Excess muscarinic and nicotinic stimulation
Contraindications: Intestinal obstruction (increased peristalsis would be painful) |
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What is edrophonium? What does it effect?
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It is a direct acting cholinomimetic. It stimulates cholinergic receptors directly.
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What are the indications of edrphonium?
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Excessive AChE inhibitor (MG PT will get better if this is the case), diagnosis of myasthenia gravis
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What is Physostigmine? What are its effects?
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It is a muscarinic agonist which has a tertiary nitrogen. It functions to cause pupilary dilation and salivation.
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What are the indications of physostigmine?
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It is used in narrow angle glaucoma, dry mouth, and to reverse the CNS effects of a muscarinic antagonist.
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What are the toxicities and contraindications of physostigimine?
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Toxicities: Convulsions, CV depression, respiratory depression
Contraindications: Asthema, heart disease, intestinal obstruction. |
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What is donepezil? What is its only indication?
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It is an exclusive inhibitor of AChE used in Alzheimer's Disease
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What to organophosphates do?
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They are IRREVERSIBLE AChE inhibitors.
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What is the acronym used in organophosphate poisoning?
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S - salivation
L - lacrimation U - urination D - defication |
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How do you treat organophosphate poisoning?
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Ventilation, gastric suction, atropine (anti muscarinic agent), 2-PAM
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What is Echothiophate? What is is it used in?
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It is an irreversible AChE inhibitor used in open angle glaucoma treatment via intraocular injection.
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What is atropine?
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It is a competitive muscarinic antagonist
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What are the indications of atropine?
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Organophosphate poisoning, induction of long term mydriasis, bradycardia due to vagal stimulation, GI hypermotility, bladder spasms
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What is scopalamine? What is its use?
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It is a muscatinic antagonist similar to atropine.
It is used in patch form for as an anti motion sickness drug. |
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What is glycopyrrolate? Cite an important point about its structure.
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It is a quaternary nitrogen muscarinic antagonist.
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What are the indications of glycopyrrolate?
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Used to protect against the muscarinic effects of many AChE inhibitors used to reverse anesthesia
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