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USMLE Pharmacology Autonomic

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eliot2014's version from 2016-01-14 23:15

Mnemonics

Question Answer Column 3
Cholinesterase inhibitor poisoningDiarrhea/Urination/Miosis/Bradycardia/Bronchospasm/Excitation of skeletal muscle-CNS/Lacrimation/Sweating/SalivationDUMBBELSS
Carbachol actionCholinergicCarbon Copy of ACh
Atropine/muscarinic antagonist SEHot temp/low sweating-dry mouth/flushed skin/cycloplegia/disorientationHot as hare/Dry as bone/Red as beet/Blind as Bat/Mad as Hatter
B1 blockersAcebut/Betax/Esm/Aten/Metopr/ololA BEAM of B1 blockers
Nonselective B blockerPropran/Tim/Nad/(Beta)/Pind/ololPlease Try Not Being Picky
Partial B agonistsPartial Agonists/Pindolol/AcebutololPAPA
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G protein

ReceptorG-Protein
Alpha 1Gq
Alpha 2Gi
Beta 1Gs
Beta 2Gs
M1Gq
M2Gi
M3Gq
D1Gs
D2Gi
H1Gq
H2Gs
V1Gq
V2Gs
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Enzymes

ReceptorEnzyme Activity
Alpha 1Phospholipase C up
Alpha 2Adenylyl cyclase down
Beta 1Adenylyl cyclase up
Beta 2Adenylyl cyclase up
M1Phospholipase C up
M2Adenylyl cyclase down
M3Phospholipase C up
D1Adenylyl cyclase up
D2Adenylyl cyclase down
H1Phospholipase C up
H2Adenylyl cyclase up
V1Phospholipase C up
V2Adenylyl cyclase up
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2nd Messengers

Receptor2nd messenger
Alpha 1DAG/IP3 up
Alpha 2cAMP down
Beta 1cAMP up
Beta 2cAMP up
M1DAG/IP3 up
M2cAMP down
M3DAG/IP3 up
D1cAMP up
D2cAMP down
H1DAG/IP3 up
H2cAMP up
V1DAG/IP3 up
V2cAMP up
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Receptor Major Functions

ReceptorMajor Fxns
Alpha 1Vascular SM contraction/pupillary dilator contraction-mydriasis/intestinal-bladd SM contraction
Alpha 2Decrease sypathetic outflow/decrease insulin release/decrease lipolysis/increase platelet aggregation
Beta 1Increase HR/contractility/renin release/lipolysis
Beta 2Increase HR/contractility/lipolysis/vasodilation/bronchodilation/decrease uterine tone/ciliary muscle relaxation/decrease aqueous production
M1CNS/enteric nervous system
M2Decrease HR/decrease atrial contractility
M3Increase exocrine secretion/peristalsis/bladder contraction/bronchoconstriction/pupillary sphinctor-miosis/ciliary muscle accomodation
D1Relaxes renal vascular SM
D2Modualtes transmitter release
H1Nasal-bronchial mucus production/bronchiole contraction/pruritus/pain
H2Gastric acid production
V1Vascular SM contraction
V2H2O permeability in CT of kidney
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Autonomic Drugs

DrugMoA
VesamicolInhibits ACh incorporation into vesicles
HemicholiniumInhibits choline uptake
BotulinumInhibits ACh degranulation
MetyrosineInhibits conversion of tyrosine to dopamine
ReserpineInhibits dopamine incorporation into vesicles
GuanethidineInhibits NE degranulation
BretyliumInhibits NE degranulation
AmphetamineIncreases NE degranulation, blocks NE reuptake
CocaineBlocks NE reuptake
TCAsBlocks NE reuptake
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Cholinomimetics

DrugMoAUse
BethanecholDirect agonist/AChE resistantPost-op ileus/neurogenic ileus/urinary retention
CarbacholDirect agonistGlaucoma/pupillary contraction/relief of IOP
PilocarpineDirect agonist/AChE resistantPotential stimulator of sweat-tears-saliva/OA and CA glaucoma
MethacholineDirect agonistChallenge test for asthma
NeostigmineIndirect agonist-AChEiPost-op ileus/neurogenic ileus/urinary retention/MG/reverseal of post-op NM jxn blockade
PyridostigmineIndirect agonist-AChEiMG/long acting/no CNS penetration
EdrophoniumIndirect agonist-AChEiMG/short acting (diagnosis)
PhysostigmineIndirect agonist-AChEiAnticholinergic toxicity/crosses into CNS
DonepezilIndirect agonist-AChEiAlzheimer's
AtropineMuscarinic antagonistMydriasis/cycloplegia
HomatropineMuscarinic antagonistMydriasis/cycloplegia
TropicamideMuscarinic antagonistMydriasis/cycloplegia
BenztropineMuscarinic antagonistParkinson's
ScopolamineMuscarinic antagonistMotion sickness
IpratropiumMuscarinic antagonistCOPD/asthma
TiotropiumMuscarinic antagonistCOPD/asthma
OxybutyninMuscarinic antagonistReduces bladder spasms/urgency in cystitis
GlycopyrrolateMuscarinic antagonistPre-op to reduce airway secretions/drooling/peptic ulcer
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Sympathomimetics

DrugReceptorUse
EpinephrineB>A agonistAnaphylaxis/OA glaucoma/asthma/hypotension
NorepinephrineA1>A2>B1 agonistHypotension/Septic Shock
BrimonidineAlpha 2 agonistGlaucoma
IsoproterenolB agonistEvaluation of tachyarrhythmias
DopamineD1=D1>B>A agonistUnstable bradycardia/ HF/ Shock
DobutamineB1>A/B2 agonistHeart failure/cardiac stress testing/inotropic>chronotropic
PhenylephrineA1>A2 agonistHypotension/mydriasis for ocular procedures/rhinitis
AlbuterolB2>B1 agonistAcute asthma
SalmeterolB2>B1 agonistLong term asthma/COPD
TerbutalineB2 agonistReduce premature contractions
RitodrineB2 agonistReduce premature contractions
AmphetamineReleases stored catecholaminesNarcolepsy/obesity/ADHD
EphedrineReleases stored catecholaminesNasal decongestion/urinary incontinence/hypotension
CocaineReuptake inhibitorsVasoconstriction/local anesthesia
ClonidineA2 agonistHypertension (especially w/renal disease), ADHD, Tourette syndrome
GuanfacineA2 agonistHypertension (especially w/renal disease), ADHD, Tourette syndrome
Alpha methyldopaA2 agonistHypertension in pregnancy (especially w/renal disease)
FenoldopamD1 agonistPostoperative hypertension/ hypertensive crisis / vasodilator (coronary, peripheral, renal, and splanchinc)/ promotes natriuresis/ can cause hypotension and tachycardia
MidodrineA1 agonistAutonomic insufficiency and postural hypotension / may exacerbate supine hypertension
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Sympatholytics

DrugReceptorUse
PhenoxybenzamineIrreversible A blockerPheochromocytoma (used preoperatively to prevent catecholamine crisis)
PhentolamineReversible A blockerPatients taking MAOi who eat tyramine
PrazosinA1 blockerHTN/urinary retention in BPH/PTSD
TerazosinA1 blockerHTN/urinary retention in BPH
DoxazosinA1 blockerHTN/urinary retention in BPH
TamsulosinA1 blockerurinary retention in BPH
MirtazapineA2 blockerDepression (may cause sedation, increased serum cholesterol, and increased appetite)/ also works on serotonin receptors
AcebutololB1>B2 blocker/partial agonistContraindicated in angina
MetoprololB1>B2 blockerSVT (class II antiarrhythmic--> decreases AV conducting velocity)/ HF/ may cause dyslipidemia
EsmololB1>B2 blockerSVT (class II antiarrhythmic--> decreases AV conducting velocity)/ very short acting
BisoprololB1>B2 blockerHF
NadololB blockerdecreases hepatic venous pressure gradient and portal hypertension (so it treats variceal bleeding)
PropranololB blockerMigraine prophylaxis/ antiarrhythmic/ thyroid storm / decreases hepatic venous pressure gradient and portal hypertension (so it treats variceal bleeding)/ can exacerbate Prinzmental angina
TimololB blockerGlaucoma
PindololB blocker/partial agonistContraindicated in angina
CarvedilolA/B blockerHF
LabetalolA/B blockerN/A
NebivololB1 blocker and B3 stimulatorB3 stimulation activates NO synthase in the vasculature
BetaxololB1>B2 blockerGlaucoma
CarteololB1>B2 blockerGlaucoma
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