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”