Term
*****
Remember that Cholingergic simply refers to Acetylcholine
Cholinergic receptors include Nicotinic and Muscarinic receptors
-Muscarinic receptors are located on smooth mm, and their stimulation resembles that of PNS activation
-Nicotinic receptors are located on autonomic ganglia (NN) and on skeletal muscle (NM)
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Definition
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Term
****
Cholinergic drugs that BIND to and activate N or M receptors are direct acting agonists
Cholingergic drugs that do NOT stimulate the receptor but instead amplify the effects of ACh are indirect-acting agonists |
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Definition
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Term
What are the are the Direct Acting Cholingergic Agonists I need to know?
(7 drugs) |
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Definition
-Bethanechol
-Pilocarpine
-Carbachol
-Civimeline
-Nicotine
-Varenicline (Chantix)
-Methacholine
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Term
Bethanechol
-Clincial Applications
-Action |
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Definition
-Cholinergic Direct Agonist, that is selective for Muscarinic Receptors
-ACTION: activates Bowel and Bladder smooth mm
Clinical Applications:
postoperative ileus, neurogenic ileus and urinary retention (ileus = lack of peristalsis) |
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Term
Pilocarpine
-Action
-clinical applications |
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Definition
Pilocarpine is a Direct Acting Cholinergic Agonist
ACTION:
-Contracts ciliary mm of eye (M3 stimulated, contraction of the ciliary mm then causes trabecular meshwork to open up, which increases the drainage of aqueous humor, wihc decreases intraocular pressure
-contracts pupillary sphincter
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Term
What is Pilocarpine used to treat?
What are its side effects? |
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Definition
Remember that Pilocarpine is a Direct Actining Cholinergic Agonist, that is relatively selective for Muscarinic receptors
-It is used to treat open and closed angle glaucoma
(remember that pilo causes the contraction of ciliary mm and pupillary shconter, which helps relief intraocular pressure)
-Side effects are blurred vision (causes contractin of ciliary mm, which affects accomodation, causing blurred vision) |
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Term
"you cry, drool, and sweat on your pilow"
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Definition
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Term
Carbachol
-Action
-Clinical Applications |
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Definition
-direct acting cholinergic agonist
-used to treat:
glaucoma
pupillary constriction
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Term
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Definition
-direct acting cholinergic agonist
-selective for M3 receptors, thus causes salivation but NOT sweating
-Thus is used to increase salivation |
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Term
What is Methacholine?
-Action
-Clinical Application |
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Definition
-direct acting cholinergic agonist
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Term
| This drug stimulates muscarinic receptors in the airway and thus is used as a challenge test for diagnosis of asthma |
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Definition
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Term
| What are the Indirect Agonists (cholinesterase inhibitors) I need to know? |
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Definition
-Neostigmine
-Pyridostigmine
-Physostigmine
-Donepezil
-Rivastigmine
-Galantamine
-Edrophonium
-Pralidoxime |
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Term
What is Neostigmine?
-ACTION
-Clinical Application? |
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Definition
Neostigmine is an indirect agonist cholinergic drug
-IE it is a cholinesterase inhibitor, which increases endogenous ACh
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Term
| What drug is used to treat myasthenia gravis and reverse neuromuscular juntion blockade postop? |
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Definition
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Term
Pyridostigmine
-Action
-clinical Application |
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Definition
Pyridostigmine is a indirect acting cholingergic agonist
ACtION:
-increase endogenous ACh (
-used to treat Myasthenia gravis
clinical application:
-myasthenia gravis
-no CNS penetration |
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Term
Physostigmine
-action
-clinical application |
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Definition
-indirect agonist, cholingergic drug
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Term
What drug is used to treat anticholinergic toxicity, IE an atropine overdose
(atropine is a muscarinic antagonist) |
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Definition
Physostigmine
rememer that "physostigmine phyxes atropione overdose" |
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Term
What is Edrophonium?
ACTION
CLINICAL APPLICATION |
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Definition
Edrophonium is an indirect agonist,
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Term
| What drug was used to diagnose Myasthenia gravis (except now that is done by an antibody acytlcholine test) |
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Definition
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Term
Echothiophate
action
clinical application |
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Definition
Echothiophate is indirect agonist, cholinesterase inhibitor
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Term
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Definition
-increases endogenous ACh by inhibiting AChE
-used to teat Alzheimer's disease |
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Term
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Definition
increases endogenous ACh by inhibiting AChE
-used to teat Alzheimer's disease |
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Term
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Definition
increases endogenous ACh by inhibiting AChE
-used to teat Alzheimer's disease |
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Term
| What are the 3 AChE inhibitors that are used to treat Alzheimer's that I need to know? |
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Definition
Donepezil
Rivastigmine
Galantamine |
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Term
| What is Pralidoxime (2 PAM)? |
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Definition
-used in EARLY treatment of organophosphate poisoning (causes regeneration of AChE if given early)
**remember that organophosphates phosphorylate cholinesterase, causing AChE inhibition, which will lead to the accumulation of ACh |
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Term
Organophosphates can bind and inhibiti AChE.
What are the symptoms of Organophosphate poisoning or Cholinesterase inhibitor poisoning? |
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Definition
DUMBBELSS
D = diarrhea
U = urination
M = miosis
B = bronchospasm
E = excitation of skeletal mm and CNS
L = Lacrimation
S = sweating
S = salivation |
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