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109 Cards in this Set
- Front
- Back
where is nicotinic-g receptor
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ACh receptor at parasympathetic/sympathetic ganglia
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type of receptor at parasympathetic organ?
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muscarinic
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neurotransmitter at alpha/beta receptors
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NE
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neurotransmitter at muscarinic receptors
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ACh
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for the most part, nicotic actions create _____ :(
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side-effects
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For the most part, indirect acting cholinomimetic drugs inhibit ______
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Ach-esterase
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examples of direct acting cholinomimetic drugs
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Ach
Bethanechol Pilocarpine |
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examples of indirect acting cholinomimetic drugs
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Physostigmine
Neostigmine Edrophonium |
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Acetylcholine is
a) specific b)nonspecific |
nonspecific (muscarinic/nicotinic)
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Why does ACh have a short duration of action?
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ACh-esterase
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ACh has nicotinic action: describe its side-effect profile.
a) poor b) rich c) no side-effects |
poor = side-effect prone
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initial effect of IV Ach on Heart rate and BP
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increase both initially
(subsequent decrease in both) |
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Direct acting cholinergic drugs
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Ach (Miochol-E)
Bethanechol (Urecholine) Carbachol Cevimeline (Evoxac) Pilocarpine |
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Side effect of Pilocarpine
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diarrhea
Pile o' crap-ine |
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cholinergic agonists are more resistant to _______
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ACh-esterase
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Cholinergic Agonist directly stimulate ___________receptor
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muscarinic
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Cholinergic Agonist effect on the eye
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miosis
improved near vision |
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Cholinergic Agonist effect on the heart
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decreased HR
decreased CF decreased conduction |
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Cholinergic Agonist effect on the lung
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bronchoconstriction
increased secretion |
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Cholinergic Agonist effect on GI
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increased motility
relaxed sphincters increased secretion |
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Cholinergic Agonist effect on urinary bladder
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contraction
relaxed spinchters |
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Cholinergic Agonist effect on glands
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secretion
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Cholinergic agonist used as a test for asthma
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methanacol (provocholine)
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Bethanechol is selective for ________and _______
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GI and urinary tracts
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Bethanechol is the DOC for postoperative, postpartum, neurogenic _____________
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urinary retention
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Bethanechol is used for reflux_________
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esophagitis
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Bethanechol is used for postoperative abdominal ________
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distension
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Carbachol has a poor side effect profile b/c ________
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has muscarinic and NICOTINIC actions
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main usage for carbachol
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1- treatment of glaucoma
2- for cataract surgery: to reduce intraocular pressure and produc miosis |
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pilocarpine is specific for _______ receptors
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muscarinic
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pilocarpine has minimal ________ actions
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nicotinic
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Pilocarpine is used to reverse _________
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mydriasis
and effects of cyclopegic agents |
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pilocarpine is most commonly used cholinergic agonist to treat _________
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glaucoma
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pilocarpine used to treat dry mouth by increasing _______
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salivation
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Muscarine is specific for _______ receptors
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muscarinic
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side effects of direct acting cholinergic agonists
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sweating, salivation,
cutaneous vasodilation with flushing, nausea, vomiting, diarrhea, HR changes, hypotension |
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contraindication of cholinergic agonists
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asthma,
peptic ulcer, Parkinsonism, Pregnancy, Severe cardiac disease, hyperthyroidism (arrhythmias), mechanical obstruction or impairment of GI or urinary tract |
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Indirect acting drugs potentiate the effects of ACh by inhibiting ________
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hydrolysis
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Indirect acting drug effects are due to ACh stimulating __________
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muscarinic and nicotinic receptors
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Reversible Anticholinesterases
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Physostigmine, Pyridostigmine, Neostigmine,
Demecarium, Ambenoenium, Edrophonium |
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Irreversible Anticholinesterases
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Isoflurophate, Echothiophate,
Malathion, Parathion, Tabun, Paraoxon |
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Physostigmine can be used to treat _______, but pilocarpine is preferred
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glaucoma
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Physostigmine is used for treatment of ___________, but be careful to avoid seizures, bradycardia
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anticholinergic intoxication (ex. curare overdose)
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Neostigmine has ACh-esterase action and direct _____-like action
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ACh
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Neostigmine has muscarinic effects due to ___________ inhibition
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cholinesterase
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Neostigmine has nicotinic effects at neuromuscular sites due to _____________
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direct stimulation
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Neostigmine's muscarinic action are used to treat ________
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postoperative distension and urinary retention
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Neostigmine' nicotinic actions can be used to reverse ________
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paralysis induced by neuromuscular blocking agents
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Side effects of neostigmine
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Elevation of skin temperature,
Sweating, Salivation, Bradycardia with hypotension Skeletal muscle fasciculations |
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Neostigmine Substitutes
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Pyridostigmine
Ambenonium Demecarium |
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Pyridostigmine used for _____
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-used for chronic management of myasthenia gravis
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Ambenonium used for______
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- used also for management of myasthenia
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Demecarium used for _______
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-used for glaucoma
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Edrophonium has a _____ duration of action
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short
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Edrophonium is Used as a diagnostic tool for ______
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myasthenia
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Edrophonium produces ________ in untreated myasthenia patient
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rapid, transient increase in muscular strength
If strength improves, increase therapy If response is unfavorable, decrease therapy |
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Edrophonium Used as an antidote to
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curare
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Irreversible organophosphorus anticholinesterases Bind _____
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irreversibly with the enzyme - enzyme becomes permanently phosphorylated
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Irreversible organophosphorus anticholinesterases Effects remain until ________
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new enzyme is regenerated
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Irreversible organophosphorus anticholinesterases Effects may persist for ______
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weeks or months
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Measurement of RBC Achase can be used to assess _______
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severity of intoxication of Irreversible organophosphorus anticholinesterases
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Isoflurophate and echothiophate are used for ______ therapeutically
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glaucoma
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Malathion can be used to treat _________
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head lice
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Organophosphates Most commonly used as ____________
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insecticides
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Organophosphates Developed as _________
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chemical warfare agents
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Organophosphates Toxicology is significant due to___________
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High lipid solubility
Absorbed through skin, ingestion or inhalation Readily enter CNS |
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Most common symptoms of Organophosphate Toxicity include __________________
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nausea, dizziness, vomiting, abdominal pain, weakness, blurred vision and headache
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Plasma cholinesterase is regenerated in _______
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2 weeks
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Neural cholinesterase may require _____ months to completely restore the enzyme
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1-3
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Organophosphate Toxicity Vision disturbances and headache can persist for ________
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more than a month
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Muscarinic manifestations of Organophosphate Toxicity
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bronchoconstriction, increased bronchial secretions, sweating, salivation, lacrimation, bradycardia, miosis, blurred vision, urinary incontinence
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Nicotinic manifestations of Organophosphate Toxicity
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muscular fasciculations, tachycardia, hypertension
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CNS manifestations of Organophosphate Toxicity
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restlessness, insomnia, tremors, confusion, ataxia, convulsions, respiratory depression, CVS collapse
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Used to regenerate Achase after it has been phosphorylated by irreversible anticholinesterase
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Pralidoxime
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Pralidoxime is Not used in intoxication by reversible anticholinesterase due to __________
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its own anticholinesterase activity
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Treatment of Organophosphorus Toxicity
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Treat symptomatically - support respiration and CVS
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___________ reverses neuromuscular effects of Organophosphorus Toxicity
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Pralidoxime
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_________used for muscarinic and CNS effects but scopolamine may be more effective for CNS effects of Organophosphorus Toxicity
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Atropine
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Prototype Cholinergic Antagonists are _______
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atropine and scopolamine
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Sensitivity of tissues to atropine:
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Salivary glands>sweat glands>eye and heart>GI and urinary tract
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________ is more effective in the eye and has more prominent CNS actions
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Scopolamine
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Cholinergic Antagonists Effects on CVS:
High therapeutic dosages produce _______ |
tachycardia
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Cholinergic Antagonists Effects on CVS:
Small doses may decrease ____ due to central stimulation of vagus |
HR
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Cholinergic Antagonists effects on blood pressure
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Minimal
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Large doses of atropine may cause ________
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flushing (atropine flush)
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Cholinergic Antagonists Effects on GI and urinary tract
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Requires large doses
Reduces motility and tone more than secretion Favors urinary retention by promoting contraction of sphincter |
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Cholinergic Antagonists Effects on eye
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Produce prolonged (up to 2 weeks) mydriasis and cycloplegia
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Cholinergic Antagonists Contraindicated in
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narrow angle glaucoma patients
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Cholinergic Antagonists Effects on CNS
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High doses produce excitation, hallucinations, delirium
Scopolamine used for motion sickness, preanesthetic, sedation Can produce amnesia |
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Opthalmologic Uses of Cholinergic Antagonists
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Mydriatic
Break adhesions |
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Perioperative uses of Cholinergic Antagonists
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Dry secretions
Prevent vagal bradycardia Reduce dose of anesthetic Scopolamine used for sedative and amnesic effects Prevent muscarinic effects of neuromuscular blocking agent |
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Cardiac uses of Cholinergic Antagonists
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Prevent bradycardia after MI
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GI disease uses of Cholinergic Antagonists
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Once used to treat peptic ulcer by decreasing vagal mediated secretion, relieve spasm, and slowing gastric emptying
Side effects limited use |
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Uses of Cholinergic Antagonists
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Motion sickness
Antimuscarinic intoxication Asthma |
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Atropine Substitutes: Mydriatics (short acting)
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Homatropine Cyclopentolate
Tropicamide |
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Atropine Substitutes: Anticholinergic smooth muscle relaxants
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Methscopolamine Propantheline
Dicyclomine Use for GI problems has been replaced by antihistamines Used for urinary incontinence |
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Neuromuscular Blocking Agents Act on ________
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nicotinic receptors
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Nondepolarizing Agents compete with ____ for receptors
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Ach
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Depolarizing agents initially stimulate the neuromuscular junction and then _______
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block it.
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Nondepolarizing Agents
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Tubocurare Metocurine
Pancuronium Gallamine Atracurium Vercuronium |
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Botulinum Toxin Enters cholinergic nerve endings and inhibit ________
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exocytosis
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Botulinum Toxin Used for treatment of __________ of eye
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strabismus and blepharospasm
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Botulinum Toxin Used for smoothing _______
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wrinkles
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Side effects of Botulinum Toxin include excessive tearing and _________
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unilateral ptosis
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Ganglionic Blocking Drugs
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Hexamethonium
Trimethaphan |
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Ganglionic Blocking Drugs In past, used as antihypertensives. Now, Rarely used due to _______
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toxicity
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The majority of therapeutic actions of cholinergic drugs are focused on an interaction at the __________ receptor
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muscarinic
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Side effects of cholinergic drugs are predictable, dose related
Excessive action on the muscarinic receptor Interaction with ________ receptor |
nicotinic
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A
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B
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