(1) Autonomic Drugs: Parasympathetic (1.1-1.3) Flashcards
where are M1 receptors found?
nerves and CNS
where are M2 receptors found?
(1) Atria
(2) SA
(3) AV
where are M3 receptors found?
(1) Smooth muscle
(2) Glands
how does M3 activation lead to vasodilation?
NO release
(Binding M3 on endothelium ⇒ NO release ⇒ Dilate smooth muscle)
Indications (2) : Bethanechol
(1) Non-obstructive GI dysmotility
(2) Urinary retention
how does pilocarpine treat glaucoma?
(1) Contract ciliary muscle
(2) Constricts pupillae muscle
* (Ciliary muscle contraction ⇒ ↑ Aqueous humor outflow)*
MOA: varenicline
nicotinic receptor PARTIAL agonist
what cholinomimetic drug is used for asthma testing?
methacholine
(methacholine challenge instigates asthma for pulmonary testing)
what cholinomimetic drug is used for smoking cessation?
varenicline
what effect do muscarinic agonists have on the lens of the eye?
induce accommodation
how does pilocarpine increase the outflow of aqueous humor?
contracts the ciliary muscle
why is pilocarpine helpful in acute angle-closure glaucoma?
contracts the sphincter pupillae m.
MOA: Carbachol
(1) Muscarinic agonist
(2) Nicotinic agonist
name 2 cholinergic drugs used to treat acute angle-closure glaucoma
(1) Pilocarpine
(2) Carbachol
what is the only cholinergic agonist used to treat xerostomia?
pilocarpine
Suffix: AChE inhibitors
“-stigmine”
What drug is used for long-term treatment of myasthenia gravis?
Pyridostigmine
What drug is administered to test for myasthenia gravis?
Edrophonium
What does a negative tensilon test suggest?
Cholinergic crisis
Is Curare a depolarizing or non-depolarizing NMJ blocker?
Non-depolarizing
Is Succinylcholine a depolarizing or non-depolarizing NMJ blocker?
Depolarizing
What AChE inhibitor has CNS effects?
Physostigmine
What drug is used to reverse Atropine poisoning?
Physostigmine
Name two naturally occurring forms of Atropine
(1) Belladona
(2) Jimson weed
Treatment: Organophosphate poisoning
(1) Pralidoxime
(2) Atropine
Name three AChE inhibitors used to treat Alzheimer’s
(1) Galantamine
(2) Rivastigmine
(3) Donepezil
MOA: Pralidoxime
Regenerates AChE
Do AChE inhibitors reverse nondepolarizing or depolarizing neuromuscular blockades?
Non-depolarizing
Would an AChE inhibitor reverse the action of succinylcholine during phase 1 or phase 2 of the blockade?
Phase 2
MOA: Organophosphates
AChE inhibitor
What determines whether Pralidoxime will be effective at treating organophosphate poisoning?
Whether the organophosphate-cholinesterase complex has aged
What are two naturally occurring forms of Atropine?
(1) Belladonna
(2) Jimson weed
MOA: Scopolamine
M1 antagonist
MOA: Ipratropium
M3 antagonist
What are two inhaled antimuscarinic bronchodilators?
(1) Ipratropium
(2) Tiotropium
What is the difference in action of Tiotropium and Ipratropium?
Tiotropium dissociates more slowly from M3 receptor
(Hence lingering Tio-ooooo rings)
Name 2 antimuscarinics used to treat incontinence
(1) Oxybutynin
(2) Tolteridine
Name 2 antimuscarinics used to treat Parkinson’s
(1) Benztropine
(2) Trihexyphenidyl
Which symptoms of Parkinson’s do antimuscarinics treat?
Tremor and rigidity
(Not bradycardia)
Inhibition of what muscarinic receptor is responsible for “hot as a hare, dry as a cracker, blind as a bat”?
M3
Indications (3) : Atropine
(1) Bradycardia
(2) Heart block
(3) Organophosphate poisoning
