Sympathomimetics Flashcards
Transportvof Dopamine into vesicles is blocked by?
Reserpine
Release of vesicles from cell membrane is blocked by?
Guanethidine and bretylium
Reputake of NorEpi is inhibited by?
Cocaine and TCA
Where is NorEpi metabolized?
By COMT in plasma and MAO in synaptic cleft
What is the MOA of M2 receptors in the heart?
Inhibition of adenylate cyclase > opening of K channels, slowing rate of Phase 4 depolarization and decrease HR
MOA of M3 receptors in smooth muscles and glands
Formation of IP3 and increase intracellular Ca+
Epinephrine (chart)
Mechanism: direct general agonist (a1, a2, b1, b2)
App: anaphylaxis, glaucoma (open angle), asthma, hypotension with LA
NorEpinephrine (chart)
Mechanism: a1, a2, b1
App: Hypotension (decreases renal perfusion) (organ ischemia)
Isoproterenol (chart)
Mechanism: B1=B2
App: AV block (rare)
Dopamine (chart)
Mechanism: D1=D2 > B > a
App: Shock (increases renal perfusion & GFR), heart failure
Dobutamine (chart)
Mechanism: B1>B2
App: Shock, CHF
Amphetamine (chart)
Mechanism: indirect general agonist, releases stored catecholamines
App: narcolepsy, obesity, ADHD
Ephedrine (chart)
Mechanism: indirect general agonist, releases stored catecholamines
App: nasal decongestant, urinary incontinence, hypotension, hypotension w/ epidural/spinal A.
Phenylephrine (chart)
Mechanism: a1>a2 “pure agonist”
App: pupil dilator, vasoconstrictor, increases SVR & MAP, nasal decongestant
Albuterol, terbutaline (chart)
Mechanism: B1> B2
App: asthma, premature labor
Cocaine (chart)
Mechanism: indirect general agonist, uptake inhibitor
App: causes vasoconstriction and local anesthesia
Clonidine, a-methyl dopa (chart)
Mechanism: centrally acting a2 agonist, decreases central sympathetic outflow
App: HTN, decreases MAC, increases anesthesia/analgesia
Prototype of sympathomimetics
Epinephrine
Where is Epinephrine?
Synthesized, stored, and released from adrenal medulla
_____ is 2-10 x more potent than ______ as a renal vasoconstrictor
Epinephrine; NorEpinephrine
___ receptors are more sensitive to lower epi doses while effects on ___ receptors predominate at higher doses
B2; a1
Where is NorEpi located?
Synthesized and stored in postganglionic sympathetic nerve endings
Vascular capacitance is = to?
Change in volume/ change in pressure
Vascular capacitance
The measure of a blood vessel’s ability to increase the volume of blood it holds w/o a large increase in BP