Autonomic Pharmacology Flashcards
AA origin of NE, epi
tyrosine –> L-DOPA –> DA –> NE –> Epi
AA origin of 5-HT
tryptophan
AA origin of histamine
histidine
AA origin of NO
arginine
1st order neuron of ANS uses ____ on _____ receptor.
ACh, Nn
2nd order neurons of ANS in PSNS use _____ on _____ receptor.
ACh, M
2nd order neurons of ANS in SNS use _____ on ______ receptors.
- ACh, M (sweat glands)
- NE, a/B (most)
- DA, D1 (kidneys)
- epi from adrenal medulla acting diffusely
NMJ uses ____ on ____ receptors.
ACh, Nm
Removal of ACh from the synapse occurs by:
AChesterase, acetate (diffuses away) + choline (recycled)
NE degraded by ____ vs epi degraded by:
reuptake, MAO/COMT (epi is more processed so requires more enzyme for uptake)
GPCR receptor types
- a1 - Gq
- a2 - Gi
- B1 - Gs
- B2 - Gs
- M1 - Gq
- M2 - Gi
- M3 - Gq
- D1 - Gs
- D2 - Gi
- H1 - Gq
- H2 - Gs
- V1 - Gq
- V2 - Gs
“qiss and qiq til you’re siq of sqs”
a1 receptor roles:
- Gq
- vasoconstriction
- mydriasis
- intestinal/bladder sphincter contraction
a2 receptor roles:
- Gi
- decreased SNS
- decreased insulin release from B cells and lipolysis from adipocytes
- decreased production of aqueous humor
- increased platelet aggregation
B1 receptor roles:
- Gs
- increase in heart rate and contractility
- increase in renin release from in cells
- increased lipolysis
B2 receptor roles:
- Gs
- vasodilation
- bronchodilation
- increased lipolysis and insulin release from B cells
- decreased uterine/bladder tone
- ciliary muscle relaxation (opposite of accommodation)
- increased aqueous humor production
M2 receptor roles:
- Gi
- decreased heart rate and contractility
- relaxation of internal sphincter
M3 receptor roles:
- Gq
- increased exocrine gland secretions
- increased gut peristalsis
- bladder contraction
- bronchoconstriction
- miosis
- accommodation (contraction of ciliary muscle)
D1 receptor roles:
- Gs
- relaxes renal vascular smooth muscle
H1 receptor roles:
- Gq
- increased nasal/bronchial mucus production
- increased vascular permeability
- contraction of bronchioles
- pruritus
- pain
- constricts the venules causing edema
H2 receptor roles:
- Gs
- gastric acid secretion
V1 receptor roles:
- Gq
- vascular smooth muscle contraction
V2 receptor roles:
- Gs
- increased H2O permeability and reabsorption in collectube duct of nephron via AQ2 channels
bethanechol
- cholinergic agonist resistant to AChesterase
- postop ileus, neurogenic ileus, urinary retention, xerostomia
carbachol
- cholinergic agonist resistant to AChesterase
- causes miosis and decrease in IOP
methacholine
- cholinergic agonist with very short t 1/2
- dx of asthma
pilocarpine
- cholinergic agonist resistant to AChesterase
- stimulates sweat, tears, saliva and treats open and closed angle glaucoma
“cry, drool, and sweat on my pillow”
galantamine, rivastigmine, donepezil
AChesterase inh specific to CNS used to boost ACh for memory consolidation in Alzheimer dz
edrophonium
AChesterase inh used to test for myasthenia gravis
neostigmine
AChesterase inh used for ileus, urinary retention, reversal of NMJ blockade
“NeO CNS penetration”
physostigmine
AChesterase inh that can cross BBB and thus used to treat anticholinergic toxicity
“phyxes atropine OD”
pyridostigmine
AChesterase inh. used for myasthenia gravis
“get RID of myasthenia gravis”
organophosphate
- irreversible AChesterase inh
- DUMBBELSS - diarrhea, urination, miosis, bronchospasm, bradycardia, excitation of NMJ, lacrimation, sweating, salivation
- also nausea and vomiting
atropine
muscarinic antagonist, eye/heart
benztropine
muscarinic antagonist, CNS (Parkinson’s)
glycopyrrolate
muscarinic antagonist, GI/resp
-tropium
muscarinic antagonist, bronchi (bronchodilation)
oxybutynin
muscarinic antagonist, GI (overactive bladder)
scopolamine
muscarinic antagonist, motion sickness
succinylcholine
- depolarizing Nm antagonist –> paralysis
- very short half life
“-cur-“ drugs
- non-depolarizing Nm antagonist –> paralysis
- long half life –> need AChesterase inh + muscarinic antagonist to bring them off after surgery
malignant hyperthermia
- AD genetic disorder
- hyperthermia + hyperkalemia in response to inhaled anesthetics and succinylcholine releasing Ca 2+ from sarcoplasmic reticulum which activates ATPase to produce heat
- treat with dantrolene (prevents Ca 2+ release from sarcoplasmic reticulum)
-terol drugs
B2 > B1 agonists (works in smaller, more peripheral airways)
dobutamine
B1 > B2 agonist used for HF and cardiac stress testing as well as cardiogenic shock
dopamine
D > B > a agonist depending on dose used to preserve blood flow to kidneys and vital organs during shock
epinephrine
- B1,2 > a1,2 agonist used for anaphylaxis and asthma
- increase in SBP (a1) but decrease in DBP (B2) so MAP remains the same –> used with local anesthetics for vasoconstriction since it won’t raise BP
isoproterenol
- B1,2 agonist
- SBP only slightly increases, but DBP drops significantly so MAP decreases
norepinephrine
- a1 > a2 > B1 agonist used for hypotension
- SBP increased significantly, DBP unchanged so MAP increases
- can cause reflex bradycardia
phenylephrine
- a1 > a2 agonist
- used for hypotension, rhinitis (decongestant), priapism
amphetamine (Adderall)
- displaces NE/DA in vessicles
- partial adrenergic agonist
- blocks catecholamine re-uptake transporters
- used for narcolepsy and ADHD
cocaine
- inhibits DRTs causing vasoconstriction
- never give B blockers if cocaine use is suspected (unopposed a1)
ephedrine
- displaces NE in vessicles
- partial adrenergic agonist
- used for nasal congestion, urinary incontinence, hypotension
ritodrine
B2 agonist used to relax uterus and prevent premature delivery
methylphenidate (Ritalin)
- DRT, NERT in RAS
- first-line ADHD treatment
What should people on MAO inhibitors avoid?
consuming tyramine (in fermented foods/beverages)
NE will casue reflex ____.
bradycardia
isoproterenol will cause reflex ____.
tachycardia
clonidine, guanfacine
- a2 agonist that reduces SNS output
- used to treat hypertensive urgency, ADHD, Tourette
- rebound HTN if taken off too quickly
a-methyldopa
- a2 agonist that reduces SNS output
- treats HTN in pregnancy
phenoxybenzamine
- irreversible a1/a2 antagonist
- used before pheochromocytoma surgery
phentolamine
- reversible a1/a2 antagonist
- given to patients on MAO inhibitors who eat tyramine-containing foods
-azosin drugs, tamsulosin
- a1 antagonist
- urinary retention due to BPH, PTSD, HTN
mirtazapine
- a2 antagonist
- used for depression
-olol drugs
- B blockers
- angina pectoris, MI, SVT, HTN, CHF, glaucoma
acebutolol, atenolol, betaxolol, bisoprolol, emolol, metoprolol are ____ antagonists.
B1 selective (A –> M)
Avoid ____ in cocaine users.
B blockers –> unopposed a1 action and HTN
carvedilol, labetalol
a and B antagonists - great for HTN!!
homatropine
muscarinic antagonist - eye
tropicamide
muscarinic antagonist - eye
trihexyphenidyl
muscarinic antagonist - CNS (acute dystonia)
hyoscyamine
muscarinic antagonist - GI (prevents spasm in IBS)
dicyclomine
muscarinic antagonist - GI (prevents spasm in IBS)
solifenacin
muscarinic antagonist - bladder (reduces urge incontinence)
tolterodine
muscarinic antagonist - bladder (reduces urge incontinence)
BB used for SVT
metoprolol, esmolol
BB used for HF
metoprolol, bisoprolol, carvedilol
BB used for glaucoma
timolol
BB used for variceal ppx
propanolol