Autonomic Drugs - Unit 3 Flashcards
post-ganglionic parasympathetic fibers release _____
Acetylcholine
post-ganglionic sympathetic fibers release ____
Norepinephrine
Chromaffin cells release ________
catecholamines: Epi+Norepi
(~80% Epinephrine ~20% Norepinephrine)
Chromaffin cells are stimulated by the (sympathetic/parasympathetic) nervous system
sympathetic
Classically, Preganglionic sympathetics release ________, and post ganglionic sympathetics release _______
Preganglionic symps: Acetylcholine
Postganglionic symps: Norepinephrine
Classically, Preganglionic parasympathetics release ________, and postganglionic parasympathetics release _______
Preganglionic parasympathetics: Acetylcholine
postganglionic parasympathetics: Acetylcholine
Sympathetic output is generally (discrete/diffuse) while parasympathetic output is (discrete/diffuse)
sympathetic: diffuse
parasympathetic: discrete
Exceptions: for renal vessels, Pregang symps release ________, and postgang symps release _______
Preganglionic symps: Acetylcholine
Postganglionic symps: Dopamine!
Which is degraded rapidly once released from a nerve terminal? (NE/ACh)
ACh
Name 2 drugs that inhibit NE re-uptake:
- Cocaine
2. Tricyclic antidepressants, TCAs
How does botulinum toxin work?
Blocks ACh release
Why is an Nn receptor a bad target for ANS drugs?
It is in both the Symp and Parasymp systems!
M1, M3, M5 are all (Gq/Gi/Gs) coupled
Gq, (increase IP3, Ca2+, DAG)
M2, M4 are (Gq/Gi/Gs) coupled
Gi (decrease cAMP)
Gs, stimulatory proteins (increase/decrease) cAMP
increase cAMP
Gi, inhibitory proteins (increase/decrease) cAMP
decrease cAMP
Which Muscarinic receptor is predominant in slowing heart rate?
M2
Which Muscarinic receptor is common in the exocrine glands, blood vessels and smooth muscle?
M3
Which Muscarinic receptor is predominant in creating myosis of the eye?
M3
muscarinic receptors respond to release of (Epi/Norepi/ACh)
ACh
Which Muscarinic receptor is predominant in bronchoconstriction?
M3
What enzyme is inhibited by INDIRECT acting cholinomimetics?
acetylcholine esterase
Drug: Direct-acting muscarinic cholinomimetic for Post-operative and neurogenic ileus and urinary retention
Bethanechol
What makes Inocybe genus and Clitocybe genus of mushrooms toxic?
too much muscarine
Drug: Direct-acting muscarinic cholinomimetic for Glaucoma (ACh activates sphincter and ciliary muscles of eye
Pilocarpine
Drug: Direct-acting muscarinic cholinomimetic for Dry mouth Esp. Sjogren’s (and post- radiation therapy) increased salivation
Cevimeline
Drug: ACh esterase inhibitor, a volatile nerve gas
Sarin
Drug: ACh esterase inhibitor, an insecticide
Parathion
Drug: ACh Esterase inhibitor, covalently carbamylates AChE, for myasthenia gravis and Post-op and neurogenic ileus; urinary retention
Neostigmine
If you are exposed to Sarin gas what you like be be given quickly before irreversible aging?
Pralidoxime
In myasthenia gravis, muscle weakness is caused by ________ that block acetylcholine receptors
auto-immune antibodies
What are the SLUDGE side effects that result from too much cholinergic stimulation?
Salivation Lacrimation Urination Defication GI distress Emesis
Which 2 drug classes have the SLUDGE effects?
- Muscarinic cholinomimetics
2. AChE inhibitors
Drug: AChE inhibitor for Alzheimer’s (amplifies endogenous ACh in brain)
Donepezil
2 drugs: indirect acting AChE inhibitor for Glaucoma (ACh activates papillary sphincter and ciliary muscles of eye)
- Physostigmine (short acting)
2. Echothiophate (long acting)
Too much neostigmine can lead to flooding the ACh and paralysis. What do you use to check the effect of the neostigmine?
Edrophonium
List the tertiary amine, anti-muscarinics (9) which generally block muscarinic function (2 each for eye, CNS, Bronchi, G; 1 for GU )
Eye: 1. Atropine 2. Tropicamide CNS: 3. Benztropine 4. Scopolamine Bronchi: 5. Ipratropium 6. Tiotropium GI: 7. Glycopyrrolate 8. Dicyclomine GU: 9. Tolterodine
Paralysis of the eye’s ciliary muscles (and thus lens) is called _______
cycloplegia
Parasympathetic innervation drives pupillary (constriction/dilation)
constriction
hint: Mio*sis
Sympathetic innervation drives pupillary (constriction/dilation)
dilation
hint: Mydria*sis
A muscarinic antagonist (promotes/ inhibits) sweating
inhibits! (receptors are muscarinic cholinergic)
hint: dry as a bone
Drug: Tertiary amine, anti-muscarinics
Targets CNS For parkinson’s, penetrates BBB
Benztropine
2 Drug: Tertiary amine, anti-muscarinics
For Mydriasis and cycloplegia
- Atropine
2. Tropicamide
Drug: Tertiary amine, anti-muscarinics
Targets CNS for Prevention or reduction of motion sickness, penetrates BBB
Scopolamine
2 Drugs: Tertiary amine, anti-muscarinics
Target G.I. tract to reduce transient hypermobility
- Glycopyrrolate
2. Dicyclomine
Drug: Tertiary amine, anti-muscarinics
For postoperative bladder spams, incontinence
Tolterodine
2 Drug: Tertiary amine, anti-muscarinics
For bronchidilation in asthma, COPD
- Ipratropium
2. Tiotropium
Two ganglion blockers that block Nn receptors and sympathetic tone are
- Hexamethonium
2. Mecamylamine