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30 Cards in this Set

  • Front
  • Back
List the Direct acting cholinergic Agonists
Acetylcholine
Bethanechol
Carbachol
Cevimeline
Pilocarpine
List the Indirect acting Reversible cholinergic Agonists
Ambenomium
Demecarium
Donezepil
Edrophonium
Galantamine
Neostigmine
Physostigmine
Pyridostigmine
Rivastigmine
Tacrine
List the Indirect acting Irreversible cholinergic Agonists
Echotiophate
What causes reactivation of acetylcholine esterase?
Pralidoxime
What are the effects of acetylcholine
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
What are the effects of Bethanechol
Increase: GI motility & tone; destrusor m. tone --> urine expulsion
What is Bethanechol used for in treatment
stimulate atonic bladder
neurogenic atony
megacolon
What are side effects of Bethanechol
generalized cholinergic stimulation: sweating, salivation, flushing, dec. BP, nausea, abdominal pain, diarrhea, bronchiospasm
What are the effects of Carbachol?
- 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
What is Carbachol used for in TX?
RARELY for glaucoma
What are the effects of pilocarpine?
- Miosis
- ciliary m. contraction
- spasm of accomodation
* most potent stimulator of sweat, tears and saliva secretion
What is pilocarpine used to treat?
It is the drug of choice for emergency narrow and wide-angle glaucoma - it leads of immediate opening of the canal of Schlemm
How long does pilocarpine last?
8 hours, can be repeated
What are adverse effects of pilocarpine
- It can enter the brain and cause CNS disturbances
- profuse sweating, salivation
What are the properties of Bethanechol?
- not degraded bu acetylcholine esterase
- no nicotinic actions
- strong muscarinic actions
What are the properties of Carbachol?
- muscarinic and nicotinic actions
- Not acetylcholine esterase hydrolyzed
What are the properties of Pilocarpine?
- tertiary amine --> penetrate CNS
- alkaloid
- muscarinic actions
What are the properties of Physostigmine
tertiary amine --> penetrate CNS
What are the therapeutic uses of Physostigmine?
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
What are the adverse effects of Physostigmine?
- convulsions in high doses
- bardycardia
- dec. CO
What are the properties of Neostigmine
acts for a long duration - 2-4 hrs

polar --> doesn't enter CNS
What are the therapeutic uses of Neostigmine?
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
What are adverse effects of Neostigmine?
salivation, flushing, dec. BP, nausea, abdominal pain, diarrhea, bronchospasm
What the some characteristics of edrophonium?
quaternary amine

short duration of action; 10-20 min
What is edrophonium used in treatment for?
For diagnosis of myasthenia gravis

as antidote for tubocurarine
What is used to alzheimer's treatment?
donepezil, galantamine, rivastigmine, tacrine
What is the duration of action of echotiophate?
up to 1 week
What is the mechanism of action of echothiophate?
covalently binds vis its phosphate groups to the serine-OH group at the active site of acetylcholinesterase causing permanent inactivation
What is echothiophate used for in treatment?
TX: open angle glaucoma
What are actions of echothipophate?
cholinergic stimulation, paralysis of motor function, convulsions, intense miosis,