Pharm 11: Adrenergic Flashcards
Dopamine is hydroxilated to yield _________
NorEpi
Dopamine is transported into synaptic vessels by
VMAT
Cocaine MOA
inhibits norepi transporter
This transporter brins norepi back into the neuron
Reserpine MOA
Blocks VMAT so norepi cannot be transported into vesicles
alpha adrenergic receptors signaling mediators
Gq/Gi/Go
beta adrenergic signaling mediator (receptor type)
Gs
α1 receptor tissues and effects
Vascular smooth muscle = contraction
Intestinal smooth muscle = relaxation
Heart = increased inotropy and excitability
Liver: glycogenolysis and gluconeogenesis
α2receptor tissues and effects
Pancreatic B cells = decreased insulin secretion
Platelet = aggregation
Nerves = decreased norepi release (feedback)
Vascular smooth muscle = contraction
β1 receptor tissues and effects
Heart = dromotropy, inotropy, chronotropy
Kidneys = renin secretion
β2 receptor tissues and effects
Smooth muscle = relaxation (albuterol)
Liver= glycogenolysis and gluconeogenesis
Muscle = K+ uptake (albuterol for hyperk)
β3 receptor tissue and effect
Adipose tissue lipolysis
Epinephrine MOA
agonist of both α and β. Mostly β at low concentrations
Norepi MOA
β1 and α1 but not β2
Dopamine MOA
Low doses acts on D receptors
High doses acts on β1 receptors
Higher even doses it starts hitting α1
α-methyltyrosine MOA
inhibits catecholamine synthesis
used to treat pheochromocytoma associated HTN
Tyramine MOA
Gets taken up into synaptic vesicles, displacing norepi. Norepi. in short term causes hypertension. Long term hypotension
Octopamine MOA
Metabolite of tyramine. Doesnt cause hypertension initially but retains the chronic hypotension
Guanethidine MOA
actively transported by NET into neurons, displacing norepi
Amphetamine MOA
ADDERALL BB
Phenylephrine MOA
α1 agonist used IN to vasoconstrict and reduce nasal congestion
Clonidine MOA and use
α2 agonist.
used to lower sympathetic activity in brain stem
decreases norepi release
Dexmedetomine MOA
α2 receptor agonist
decreases sympathetic activity causes sedation
α-Methyldopa MOA and use
Prodrug that metabolizes to α2 agonist. Lowers blood pressure
used only in pregnancy
Isoproterenol MOA
non selective β agonist
Increases CO with little increased BP
Dobutamine MOA and use
Isomer properties cancel each other. Effectively a β1 agonist.
Inotrope and chronotrope
Used for heart failure IV
β2 agonists
Terbutaline and albuterol
also salmeterol as long acting
Terazosin, prazosin, doxazosin MOA and use
α1 antagonist. Used for treatment of hypertension
Yohimibine MOA and use
α2 selective blocker. Increased norepi release. Gives you a boner. Kinda useless tho
Non selective β blockers
PNT
Propranolol
Nadolol
Timolol
Propranolol MOA and use
non selective beta blocker
used for hypertension and coronary artery disease
Drugs that are nonselective beta blockers and also α1 antagonists
Labetalol
Carvedilol
β1 selective antagonists
EMAC
Esmolol
Metoprolol
Atenolol
Celiprolol
Treatment for benign prostatic hyperplasia
Tamsulosin
α1a blocker
Acebutolol MOA
partial β1agonist
Used for ischemic heart disease with heart failure
Buzzword: intrinsic sympathomemetic activity
Think partial agonist