Adrenergic Pharmacology Flashcards
Which part of the body has no sympathetic postganglionic neuron-effector cell synapses in most tissues?
- eccrine sweat glands
2. vasodilator sympathetic fibers in skeletal muscles
What drug inhibits the conversion of tyrosine to DOPA?
tyrosine hydroxylase
metyrosine
what drug inhibits the transfer of DOPA into vesicles?
Reserpine
what enzyme inactivates norepinephrine and dopamine in the cytoplasm?
monoamine oxidase
what drug class increases the stores of NE and dopamine by inhibiting its breakdown in the cytoplasm?
monoamine oxidase inhibitors
what dug inhibits the fusion of the the NE vesicles to the terminal membrane?
guanethedine
what drug promotes the fusion of the the NE vesicles to the terminal membrane?
amphetamine
tyramine
what drug inhibits the diffusion and reuptake of NE and Dopa via NET and DAT in synaptic cleft?
Cocaine
TCAs
What drug class inhibits the metabolism of metanephrines and VMA?
MAOi
COMi
[adrenoceptor]
causes smooth muscle contraction via increase in IP3, DAG
alpha 1, Gq
[adrenoceptor]
causes smooth muscle contraction via decrease in cAMP
alpha 2
[adrenoceptor]
increases heart rate by increasing cAMP
beta 1
[adrenoceptor]
relax smooth muscle, by increasing cAMP, lungs
beta 2
[adrenoceptor]
increase lipolysis, by increasing cAMP, seen in adipose cells
beta 3
[adrenoceptor]
relax renal vascular smooth muscle by increasing cAMP
dopamine 1
What adrenergic receptor causes contraction of the pupillary dilator muscle, and pilomotor smooth muscle
alpha 1
alpha 1 always contracts
what adrenergic receptor stimulates platelet aggregation?
alpha 2
What is the effect of alpha 2 receptors in the eyes?
it increases the outflow of aqueous humor
What is the effect if you stimulate beta 1 adrenergic receptors in the kidneys?
stimulation of renin release in the juxtaglomerular cells of the kidney
norepinephrine has no effect in beta 2 adrenoceptor in this part of the body
blood vessels
[sympathomimetics]
drug added to local anesthetic solution to decrease systemic absorption, and contributes to bloodless surgical field
epinephrine
beta 1 = beta 2 > alpha
[sympathomimetics]
epinephrine increases the HR by accelerating what phase of depolarization?
phase 4
[sympathomimetics]
can cross the placenta causing fetal anoxia
epipnephrine
[sympathomimetic]
first line treatment for refractory hypotension in severe sepsis
norepinephrine
has minimal metabolic effects
[sympathomimetics]
last resort drug in cardiogenic shock
norepinephrine
alpha 1 > beta 1
negligible beta 2
[sympathomimetics]
drug of choice in patients with cardiogenic shock
dopamine
[sympathomimetics]
drug of choice in acute heart failure accompanied with severe hypotension
dopamine
[sympathomimetic]
best used for patients with decreased contractility, low systemic blood pressure and low urine output
dopamine
[sympathomimetics]
unique among catecholamines since it can simultaneously increase myocardial contractility, GFR, excretion of Na and UO
dopamine
[sympathomimetics]
inactive per orem; does not enter CNS significantly; very effective in renal failure associated with shock
dopamine
[sympathomimetics]
What dopamine dose will lead to vasodilation D1 and D2 receptors?
0.5 to 3 mcg/kg/min - Low dose
[sympathomimetics]
What dopamine dose will lead to stimulation of beta 1 receptors leading to increased CO (increases chronotropy and contractility)
3-10 mcg/kg/min - medium dose
[sympathomimetics]
what dose of dopamine will lead to stimulation of alpha 1 receptors resulting to vasoconstriction, increased SVR, increased BP
> 10mcg/kg/min - high dose
[sympathomimetics]
used as an adjunct to beta 2 agonist in asthma treatment
isoproterenol
[sympathomimetics]
drug used during pacemaker insertion for bradyarrhythmia
isoproterenol
[sympathomimetics]
avoided in patient with CAD since it wont induce a compensatory decrease in HR.
isoproterenol
this drug is not readily taken up by the nerve endings also
[selective alpha 1 agonists]
drug that cause rebound nasal congestion
phenylephrine
[selective alpha 1 agonists]
ocular administration causes mydriasis WITHOUT cyclopegia
phenylephrine
What is the drug of choice for alpha 1 agonist overdose?
phentolamine
[selective alpha 1 agonists]
drug that is avoided in the first trimester because it is associated with gastroschisis
Pseudoephedrine
[selective alpha 1 agonists]
drug for orthostatic hypotension
midodrine
[selective alpha 1 agonists]
drug of choice for patients with CAD and aortic stenosis experiencing hypotension
phenylephrine
since it increases coronary perfusion pressure without chronotropic side effects (tachycardia)
[diagnose]
Ptosis
Anhidrosis
Miosis
Horner Syndrome
[diagnose: horners syndrome]
indirect acting sympathomimetics is unable to dilate the pupil but phenylephrine will
Postganglionic
[diagnose: horners syndrome]
indirect acting sympathomimetics and phenylephrine is able to dilate the constricted pupil
preganglionic
[selective alpha 2 agonist]
used in cancer pain and opioid withdrawal
clonidine
[selective alpha 2 agonist]
causes rebound hypertension due to abrupt discontinuation
clonidine
[selective alpha 2 agonist]
reduces CO due to decreased HR and relaxation of vascular resistance
clonidine
what is the drug of choice to reverse rebound hypertension due to clonidine?
phentolamine
Giving clonidine with pure autonomic failure cause ___ (increase/decrease)
increase
TCAs can reduce the antihypertensive effect of clonidine due to
alpha blocking effects of TCA
[selective alpha 2 agonist]
drug of choice for pre-eclampsia and gestational hypertension
methyldopa
[selective alpha 2 agonist]
this drug can cause hemolytic anemia, mental depression, vertigo, nightmares, impaired concentration
methyldopa
[selective alpha 2 agonist]
drug used for glaucoma since it activates alpha 2 adrenergic receptor; decreases secretion of aqueous humor
apraclonidine
[selective beta 1 agonist]
drug used to induce ischemia in the myocardium for cardiac stress testing
dobutamine
[selective beta 1 agonist]
may cause arrythmias, tachyplaxis, eosinophilic myocarditis
dobutamine
what is the enantiomer of dobutamine that cause alpha-1 agonist?
negative enantiomer
what is the enantiomer of dobutamine that is a competitive antagonist at alpha 1 and a strong agonist at beta 1
positive enantiomer
[Selective beta 2 agonist]
drug used for tocolysis for preterm labor
terbutaline
[Selective beta 2 agonist]
used as a vasodilator in Raynaud’s phenomenon
isoxuprine
[Selective beta 2 agonist]
this drug can cause maternal pulmonary edema
isoxuprine
___ is an alpha 1, direct sympathomimetic drug that is not a catechol derivative and not activated by COMT
phenylephrine
