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Responsible for increased gland secretion (Salivary, gastric) |
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Responsible for Ganglionic potnetiation, slow EPSP |
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Stimulatory muscarinic receptors (Gq) |
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Definition
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Inhibitory muscarinic receptors (Gi) |
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Definition
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Pertussis sensitive muscarinic receptor (inhibitory) |
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Definition
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muscarinic receptor
increases secretion and contraction of smooth muscle |
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Definition
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hyperpolarization through opening of K channels is important for which receptors (muscarinic)? |
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ACH, Methacholine, bethanecol, carbachol |
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muscarine, nicotine, pilocarpine |
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All of these have a longer effect than Ach because they are not hydrolyzed as rapdily or at all |
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causes vasodilation and drop in BP leads to reflex w/ tachycardia |
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causes vasodilation and drop in BP reflex tachycardia is over come: bradycardia |
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no parasympathetic innervation of blood vessels, however circulating muscarinic agents can cause vasodilation due to what receptors on endothelial cells that stimulates production of EDRF (NO) |
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disease can remove endothelium from BV leading to what when muscarinic agonists hit em |
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lungs: bronchoconstriction, increased seretion |
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contradicted in asthma patients |
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myenteric plexus receptor (^ activity) |
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increased peristalsis smooth mm relaxation of sphincter increases secretion |
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Definition
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eccrine (thermogregulatory) are only sweat glands controlled by muscarinic what are receptors for em |
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in cns involved in controlling voluntary movements |
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in cns involved in regulating actions of other nT like dopamine |
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Definition
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eser of choline, slightly sensitive to achesterase |
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Definition
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ester of choline; resistant to Acetylcholine esteras |
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Definition
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contraindication my cause hypotension w/ choline ester |
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Definition
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contraindication may cuase increased gastric secretions w/ choline ester |
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Definition
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Contraindications to choline esters |
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Definition
Hyperthryoidism (atrial fib), asthma, CAD (hypotension), acid-peptic disorders (increases gastric secretions), obstructive urinary retention |
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Only high IV doses lead to short term effects |
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Ocular surgery: distilled to anterior chamber lasts 20 min |
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Definition
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Sweat spot test for autonomic neuropathy in diabetic patients (subdermal injection w/. iodine -> black spots) |
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Definition
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Inhalation to diagnose bronchial airway hypersensitivity |
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Definition
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Significant nicotinic activity (seen in prsence of atropine) Ester of choline |
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Definition
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limited to opthalmic applications (reduction in IOP) but severe side effects CV and GI (due to nicotinic activity also) |
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Definition
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No nicotinic acitivyt ester |
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emptying of bladder in cases of acute postoperative and postpartum NONOBSTRUCTIVE urinary retension also hypotonic, myotonic, neurogenic bladder |
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Definition
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orally or Subq injection ester (only one given systemically!!!) |
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Definition
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Which ester is most likely to produce systemic side effects |
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crosses BBB longer acting than choline esters but less potent |
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Definition
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Very active on eye and sweat glands: miosis and acommodation last 4-8 hrs |
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Definition
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Initial treatment for open angle glaucoma (contracts ciliar mm )
Acute treatment of angle closure glacoma |
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Do not use if IOP higher htan 45mmHg can reduce angle further |
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Can overcome mydriatic actions of atropine used alternatively to break up lesions |
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Orally causes increase in salivation (xerostomia treatment ) from radiation/ Sjogrens |
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Definition
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M3 and M1 selective muscarinic agonist |
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Definition
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can be used for Xerstomia in Sjogrens syndrome works M3 and m1 only |
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can both activate and inhibit nicotinic receptors |
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acutely: increases HR and BP from symnpathetic ganglia stimulation and secretion of epi at adrenal medulla |
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partial agonist at neuronal nicotinic receptors stimulates receptors while blocking at same time |
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functionally similar to acetylcholinesterase but found in plasma |
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Definition
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simple alcohol w/ quaternary ammonium group (less solubility in CNS) reversible short acting |
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Definition
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Carbanic acid esters of alcohols w/ quaternary ammonium |
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Definition
cargbamates, eg neostigmine |
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In addition to the muscarinic effects of over activation (DUMBELS) you may see vasodilation w/ systemic agent such as this |
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Definition
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treatment for cholinergic overactivation |
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Definition
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treatment for nicotinic overactivation |
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Definition
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200x more potent than morphine for pain from frog(alkaloid) |
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carbamic acid esters and simple alcohols are cholinesterase inhibitors (indirect agents) that are |
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organic derivatives of phosphoric acid are _____ inihbitors of cholinesterase
(phosphorylate serine residue) |
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used to treat patients of organophosphate poisoining. PRevents "aging" by displacing phosphorus group |
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low doses lipophilic agents: increase alertness in CNS high : convulsions followed by respiratory failure |
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Definition
acetylcholinesterase inhibitors |
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moderate doses REDUCE CO INCREASE BP
might be bad for alzheimers pts that are hypertensive |
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Definition
acetylcholinesterase inhibitors |
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large/toxic doses can result in marked bradycardia decrease in CO (large) hypotension |
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Definition
acetylcholinesterase inhibitors |
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10% of MG patients will not beneifit from anticholinesterase inhibitor because it is not autoimmune disease it is |
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DOC for anticholinergic drug poisoning (scopolamine etc) |
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Carbamate w/ intermediate duration 30 min- 6 hrs |
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Decreases IOP for 2 hrs pilocarpine more effective |
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synthetic carbamate that cant go through CNS
postoperative urinary retention/paralytic ileus |
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Used to reverse NM blockade by copetative neuromuscular blocers like tubocurarine
sometimes used to lower IOP in management of glaucoma or after opthalmic surgery though others are usually used |
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Definition
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Neostigmine analog used for MG (longer duration of action) 3-6 hrs |
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Definition
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Used for Mg duration of action 4-8 hrs (no cns effects) |
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quaternary ammonium, no CNS used for glaucoma |
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high lipid solubility used exclusively as insecticide (Lice)
carbamate |
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Definition
Carbaryl (Sevin, Carbacide) |
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first piperidine type reversible anticholesterase used |
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Definition
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selective for AChE low for butyrylcholinesterase |
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Similar to donepezil but also approved for parkinsons w/ dementia transdermal patch |
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derived from daffodils (AChE inhibitor) no hepatotoxicity mild ot moderate Alzheimer disease |
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Rarely used due to hepato toxicity |
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Irreversible inhibitor of AChE but low lipid solubility so can be topical only used for glaucoma that doesnt work with other stuff 100 hr duration*** |
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administered at low concentrations prophalaxis to nerve agents reversible and can lock irreversible nerve agents from binding
gives them time to get treated w/ atropine (cholinergic antagonist) or Pralidoxime (2-PAM) also get benzo as anticonvuslant |
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toxic dose of nicotine found in |
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