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30 Cards in this Set
- Front
- Back
List the Direct acting cholinergic Agonists
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Acetylcholine
Bethanechol Carbachol Cevimeline Pilocarpine |
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List the Indirect acting Reversible cholinergic Agonists
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Ambenomium
Demecarium Donezepil Edrophonium Galantamine Neostigmine Physostigmine Pyridostigmine Rivastigmine Tacrine |
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List the Indirect acting Irreversible cholinergic Agonists
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Echotiophate
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What causes reactivation of acetylcholine esterase?
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Pralidoxime
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What are the effects of acetylcholine
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Decrease: HR, BP, CO
Increase: salivary, intestinal bronchiolar secretions; GI motility, detrusor muscle tone --> urine expulsion; ciliary m. contraction --> near vision; pupillary sphincter m. tone --> Miosis |
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What are the effects of Bethanechol
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Increase: GI motility & tone; destrusor m. tone --> urine expulsion
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What is Bethanechol used for in treatment
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stimulate atonic bladder
neurogenic atony megacolon |
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What are side effects of Bethanechol
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generalized cholinergic stimulation: sweating, salivation, flushing, dec. BP, nausea, abdominal pain, diarrhea, bronchiospasm
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What are the effects of Carbachol?
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- releases epinephrine from adrenal medullar by nicotinic action
- Miosis - spasm of accomodation --> const. state of contraction - cardiovascular and Gi system effects b/c ganglion stimulating activity |
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What is Carbachol used for in TX?
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RARELY for glaucoma
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What are the effects of pilocarpine?
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- Miosis
- ciliary m. contraction - spasm of accomodation * most potent stimulator of sweat, tears and saliva secretion |
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What is pilocarpine used to treat?
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It is the drug of choice for emergency narrow and wide-angle glaucoma - it leads of immediate opening of the canal of Schlemm
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How long does pilocarpine last?
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8 hours, can be repeated
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What are adverse effects of pilocarpine
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- It can enter the brain and cause CNS disturbances
- profuse sweating, salivation |
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What are the properties of Bethanechol?
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- not degraded bu acetylcholine esterase
- no nicotinic actions - strong muscarinic actions |
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What are the properties of Carbachol?
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- muscarinic and nicotinic actions
- Not acetylcholine esterase hydrolyzed |
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What are the properties of Pilocarpine?
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- tertiary amine --> penetrate CNS
- alkaloid - muscarinic actions |
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What are the properties of Physostigmine
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tertiary amine --> penetrate CNS
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What are the therapeutic uses of Physostigmine?
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1) increase intestinal and bladder motility
2) reduce intraocular pressure in glaucoma 3) reverse CNS and cardiac effects of tricyclic antidepressants 4) reverse CNS effects of atropine 5) Miosis |
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What are the adverse effects of Physostigmine?
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- convulsions in high doses
- bardycardia - dec. CO |
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What are the properties of Neostigmine
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acts for a long duration - 2-4 hrs
polar --> doesn't enter CNS |
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What are the therapeutic uses of Neostigmine?
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1) prevent postpartum, postoperative abdominal distention and urinary retention
2) stimulates GI, bladder 3) TX of myasthemia gravis 4) antidote for tubocurarine - Nm receptor blocker |
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What are adverse effects of Neostigmine?
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salivation, flushing, dec. BP, nausea, abdominal pain, diarrhea, bronchospasm
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What the some characteristics of edrophonium?
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quaternary amine
short duration of action; 10-20 min |
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What is edrophonium used in treatment for?
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For diagnosis of myasthenia gravis
as antidote for tubocurarine |
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What is used to alzheimer's treatment?
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donepezil, galantamine, rivastigmine, tacrine
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What is the duration of action of echotiophate?
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up to 1 week
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What is the mechanism of action of echothiophate?
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covalently binds vis its phosphate groups to the serine-OH group at the active site of acetylcholinesterase causing permanent inactivation
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What is echothiophate used for in treatment?
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TX: open angle glaucoma
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What are actions of echothipophate?
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cholinergic stimulation, paralysis of motor function, convulsions, intense miosis,
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