Pharm of Adrenergic Agonists/Antagonists (L6)

stimulation of alpha-1 will cause vaso___________

contraction (in most vascular smooth muscles, pupils (dilates them), heart (increases force of pumping)

blocking of alpha-1 will cause vaso___________

dilation (in most vascular smooth muscles, pupils, heart (decreases force of pumping =lower BP)

stimulation of alpha-2 receptors will cause decreased release of _______

NE (lowers BP)

stimulation of alpha-2 receptors will cause __________ release of NE

decreased (lowers BP)

blocking of alpha-2 receptors will increase release of _______

NE (increases BP)

blocking of alpha-2 receptors will _________ release of NE

increase (increases BP)

stimulation of beta-1 receptors causes the heart muscles to _________

contract (increased force =increased BP)

blocking of beta-1 receptors causes the heart muscles to _________

relax (less force =lower BP)

stimulation of beta-2 receptors will cause broncho_________

dilation (easier to breath =lower RR)

blocking of beta-2 receptors will cause broncho_________

constriction (difficult to breathe =increased RR)

stimulation of beta-3 receptors causes the detrusor (bladder) muscle to _________

relax (bigger bladder =can hold more pee =peeing less)

blocking of beta-3 receptors causes the detrusor (bladder) muscle to _________

constrict (smaller bladder =cant hold much pee =peeing more)

adrenergic agonists are drugs capable of mimicking the effects of adrenergic nerve _______________

stimulation

adrenergic ____________ are drugs capable of mimicking the effects of adrenergic nerve stimulation

agonists

circulating catecholamines are metabolized mostly by hepatic _________________

Catecholamine-O-MethylTransferase (COMT)

why aren’t catecholamines given PO

they are not orally bioavailable

non-catecholamines can be administered ________ and they can cross the BBB

orally

non-catecholamines can have a substitution on the ________ carbon that will block oxidation by MonoAmine Oxidase (MAO) —> prolongs the action of the drug

alpha (closer to N)

non-catecholamines can have a substitution on the alpha carbon that will block oxidation by ___________ —> prolongs the action of the drug

MonoAmine Oxidase (MAO)

alpha-1 agonists constrict _______ and ________

arterioles and veins

______-___ agonists can be used as decongestants of mucous membranes and eyes

alpha-1 (smaller veins =less blood flow to the area =smaller, not so puffy and stuffy)

alpha-1 _________ can be used as decongestants

agonists (smaller veins =less blood flow to the area =smaller, not so puffy and stuffy)

beta-2 agonists can be used to manage acute _______ _______, or as ________ prophylaxis

asthma attacks (short-acting), asthma (long-acting)

(stimulation of beta-2 causes bronchodilation)

_____-___ agonists can be used to manage acute asthma attacks, or as asthma prophylaxis

beta-2 (stimulation of beta-2 causes bronchodilation)

beta-2 __________ can be used to manage acute asthma attacks, or as asthma prophylaxis

agonists (stimulation of beta-2 causes bronchodilation)

______-____ agonists can be used to treat urinary incontinence by increasing the pressure of muscles in the bladder neck

alpha-1 (constrict muscles below bladder =able to hold pee in)

alpha-1 agonists can be used to treat _________________ by increasing the pressure of muscles in the bladder neck

urinary incontinence

Epinephrine (non-selective) can be used in anaphylactic shock because it dilates ___________ and constricts _________

bronchioles (stimulate b2 =increase RR), blood vessels (stimulate a1 =increases BP)

adrenergic antagonists are compounds that inhibit catecholamine action at ___________ (direct) or by inhibiting _____ __________ (indirect)

adrenoreceptors, NE release

stimulation of alpha-2 receptors in the pre-synaptic neuron _________ the release of NE

inhibit (less NE =less of it to bind alpha-1 =less vasoconstriction =more vasodilation) (ex: Clonidine)

________ of the L-tyrosine hydroxylase enzyme, leading to less production of NE, which lowers BP

inhibits (can’t convert L-tyrosine into L-DOPA… and the next steps cant happen either then)

inhibition of ________ lowers the amount of NE uptake, which lowers BP

VMAT2 (or VAChT) (NE can’t get put into the vesicle =can’t get brought to membrane for release into cleft)

alpha ___________ lower peripheral vascular resistance (PVR) and lower BP

antagonists (less stimulation of a-1 =less vasoconstriction =more vasodilation)

we can administer Epinephrine along with a ____ receptor __________ in order to lower BP

alpha antagonist (since Epi stimulates alpha and beta =we give another drug to block alpha =cancelled out) (now only beta-2 gets stimulated =bronchodilation)

______-___ receptors are found at the base of the bladder (neck) and in the prostate

alpha-1

alpha ___________ can be used to treat Benign Prostatic Hyperplasia

antagonists (less a1 stimulation =less vasoconstriction in prostate =relaxes muscles in prostate)

patients with asthma or COPD should avoid beta-____ blockers

2 (blocking beta2 =blocking bronchodilation =causes bronchoconstriction)

______-___ antagonists can be used to reduce intraocular pressure

beta-1 (less b1 stimulation =less constriction of heart muscles =lower BP)

beta antagonists with partial alpha __________ activity are useful in HFrEF

antagonist (less stimulation of a1 =less vasoconstriction =lower BP) (less stimulation of b1 =less contraction of heart muscles =lower BP)