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Foundations 2 > Adrenergic Agents > Flashcards

Adrenergic Agents Flashcards

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1
Q

general principles for characterizing receptors and subtypes

A

block agonist effects by specific competitive agonists

potency (selectivity) sequences of agonists

molecular biology, cloning receptors and demonstrating different structural subtypes

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2
Q

EPI reversal

A

high doses of EPI with ergotoxin (alpha1 blocker) decreases blood pressure instead of increasing it

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3
Q

effects of alpha1 receptors

A

contraction of iris, bronchioles, vascular smooth muscle, splenic capsule, uterine smooth muscle, male sexual organs, pilomotor muscle, urinary bladder, gastrointestinal sphincters

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4
Q

effects of beta2 receptors

A

relaxation of bronchioles, vascular smooth muscle, splenic capsule, uterine smooth muscle, urinary bladder, and intestinal smooth muscle

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5
Q

effects of beta1 receptors

A

increase cardiac sinus rate, contractile force, and conduction

renin release in kidney

increases aqueous humor secretion

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6
Q

effects of alpha2 receptors

A

relaxation of intestinal smooth muscle

decrease in cardiac sinus rate

accumulation of fat

decrease in insulin secretion

decrease in aqueous humor secretion

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7
Q

contractile and secretory signal transduction motif

A

for alpha1 agonists

phospholipase C activation, fast enzymes

G protein stimulation, rapid increase in cytoplasmic Ca concentration

mediates CRAC channels aka store-operated calcium channels (SOCs) to open

amplifies contractile response

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8
Q

protein kinase A/cyclic AMP signal transduction motif

A

for beta agonists

slower, metabolic processes used by beta receptors

involves G protein-linked synthesis of cAMP and PKA phosphorylation

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9
Q

alpha2 receptor mechanism

A

G-protein mechanism that opens potassium channels and reduces excitability of cells

blocks calcium channels

inhibits adenylyl cyclase

direct effect on neurotransmitter release through the secretary apparatus

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10
Q

three prototype chatecholamines and their structure-activity releationships

A

norepinephrine - good stimulant of alpha and beta1, but no beta2

epinephrine - good stimulant of alpha, beta1, and beta2

isoproterenol - good stimulant of beta1 and beta2, but no alphas

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11
Q

non-cardiovascular effects of the prototypes

A

mydrasis - alpha potency

bronchiolar relaxation - beta2 potency

intestinal relaxation and glycogenolysis - produced by all types, EPI is the best

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12
Q

direct cardiovascular effects of the prototypes

A

heart rate increased by beta1 receptors, increased rate of diastolic depolarization by stimiulating pacemaker current If and Ca currents

force is augmented by increasing calcium entry from outside the cell and SR

most vascular beds have both alpha and beta2 receptors

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13
Q

three things to consider when looking at vascular bed effect of a catecholamine

A

selectivity of the drug

ratio of alpha to beta2 receptors

concentration of the drug

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14
Q

describe a cardiac action potential

A

sodium current

potassium opens at peak

L-type calcium channel maintains depolarization

delayed rectifiers restore the polarization

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15
Q

effect of norepinephrine on heartrate, blood pressure, and TPR

A

decrease TPR

increase in blood pressure

decreased heart rate

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16
Q

effect of epinephrine on heartrate, blood pressure, and TPR

A

decreas in TPR

small increase in blood pressure

increased pulse

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17
Q

effect of isoproterenol on heartrate, blood pressure, and TPR

A

decreased TPR

small decrease in pressure

increased heartrate

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18
Q

What happens when a high dose of EPI is administered to the heart?

A

increase and rate and force, leading to a great increase in systolic blood pressure

subsequent to this there is an increased diastolic pressure due to alpha vasoconstriction by the high EPI concentration

result is a rapid rise in mean blood pressure

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19
Q

therapeutic uses of prototypes

A

bronchodilator = beta 2

mydriatic = alpha

increased cardiac contractile force = beta1

vaso constrictor = alpha

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20
Q

contraindications of catecholamines

A

pressor effects - high bp, hyperthyroid problems

arrhytmias - hyperthyroid patients have more beta receptors

diabetes

narrow angle glaucoma

prostate enlargement

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21
Q

absorption, fate, and excretion of clinical prototypes

A

EPI - oral absorption satisfactory, but metabolized by MAO in gut and liver, little effect

NE - orally ineffective, poor absoprtion from subcutaneous injection site, usually given by IV infusion, quickly inactivated in the body

iSO - poor substrate for MAO due to N-isopropyl group so longer acting

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22
Q

selective alpha1 receptor agonists

A

phenylephrine

imidazoline derivatives

midodrine

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23
Q

physiologcially relevant alpha2 sites involved in the control of blood pressure

A

tonic firing of sympathetic nerves contribute to cardiac output via beta1 receptors and to the tonic constirction of blood vessels via alpha1 receptors

the activation of alpha2 receptors in the hypothalamus or the medulla inhibits this tonic sympathetic firing and relieves the tonic constriction of blood vessels, thus reducing blood pressure

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24
Q

alpha2 receptor agonists

Study These Flashcards
A

clonidine

guanfacine

guanabenz

alpha-methyl dopa

apraclonidine

brimonidine

25
clonidine suppression test
used to distinguish essential hypertension from pheochromocytoma has no effect in pheo because there is such a high amount of NE present
26
beta1 receptor agonist
dobutamine
27
"selective" beta2 receptor agonists
all are resistant to COMT action and are metabolized by sulfate conjucation albuterol terbutaline ritodrine salmeterol formoterol
28
indirect sympathomimetic agents
tyramine and amphetamines
29
tachyphylaxis
depletion of NE with indirect sympathomimetic amines such as tyramine
30
effect of Uptake 1 inhibitor on tyramine
drastic increase in bp
31
effect of a MAO inhibitor tyramine
hypertensive crisis
32
mixed acting sympathomimetic amines
epedrine derivatives such as speudoephedrine
33
clinical uses of sympathomimetic amines in the periphery
treatment of spasm of bronchiolar smooth muscle associated with asthma nasal decongestants cardiac effects premature labor and other OB uses
34
treatment of asthma
EPI inhaler for quick action isoproterenol also available over-the-counter prophylaxis - primatene tablets with ephedrine non-selective agents that produce tachycardia such as albuterol, salmeterol, and formoterol
35
mechanism of nasal congestion
unusual vessles with erectile properties that fill the sinusoids vessels ahve venous fluid reservoir, so that when they dilate, then more fluid is in the mucosa, and more mucus is secreted and mroe nasal congestion occurs
36
nasal decongestants
phenylephrine for short term relief imidazoline derivatives problem with long-term use is the release of metabolites locally so that the rebound congestion is worse blood vessels also constrict because of extrajunctional alpha2B effects - reactive hyperemia
37
cardiac arrest treatments
EPI has been found to be useful here for a great number of years the beta1 stimulatory effect is obvious but the main benefit may be secondary to vasoconstriction
38
cardiogenic shock treatments
tremendous fall in cardiac output fall in areterial systolic pressure reflex tachcardia reflex venous constriction oliguria treatment with dobutamine to increase CO with minimal increas in heart rate treatment with dopamine to increase cardiac output with an additional vasodilator effect
39
treatment for severe hypotension in the ICU
levophed because it is norepinephrine, only clinical use
40
premature labor and other OB treatments
terbutaline - beta2 agonist, so relaxes uterus
41
adrenergic blocking agetns
drugs that block adrenergic activity traditionally termed sympatholytics prevent the action of NE released from nerve endings by competing with NE at receptor site
42
alpha2 inhibition effect on heart rate
increases
43
alpha2 inhibition on GI tract
increases motility
44
alpha2 inhibition on corpus cavernosum
increases erectile function
45
alpha2 inhibitors on CNS
stimulant
46
alpha receptor blockers
phenoxybenzamine phentolamine
47
side effects of phenoxybenzamine
orthostatic hypotension nasal congestion inhibition of emission inhibition of mydriasis increases motility (blocks alpha2 on cholinergic nerve endings) persistent tachycardia (blocks alpha2 on adrenergic nerve endings)
48
alpha1 receptor blockers
prazosin - alpha1 selective tamsulosin - alpha1A selective alfluzosin - alpha1A selective silodosin - the most selective alpha 1A antagonist
49
alpha2 receptor blocker
disinhibition of neurotransmitter release effects may be similar to nerve stimulation produces persistent tachycardia by disinhibition of NE release yohimbine - most selective alpha2 antagonist
50
innervation of the corpus caverosum
non-ad-renergic, non-cholinergic (NANC) innervation has alpha receptors on it and is responsible for the stimulation of arousal - alpha2 leads to inhibition of relaxation through NO and PDE5 sympathetic nerves are responsible for detumescence
51
sexual dysfunction treatments
drugs of choice are \_\_\_denafils or \_\_\_afils prototype is sildenafil (viagra) selective inhibiotrs of phosphodiesterase type 5 (PDE 5 this causes the breakdown of cGMP
52
beta receptor blockers
sometimes called "first generation" effects are predictable based on the functions of beta receptors propranolol is the prototype timolol
53
therapeutic uses of proranolol
anti-arrythmic anti-anginal antihypertensive-block of renin pheochromocytoma stage fright
54
contraindications of propranolol
asthmatics need beta2 drive diabetics, propranolol masks signs of hypoglycemia and decreases glycogenolysis
55
metabolism for beta blockers
phase I oxidation by CYP2D6 phase II by glucuronidation and sulfation
56
latanoprost
current therapy for glaucoma PGF2alpha derivative that increases AH outflow by the uveal-scleral route major side effect - may produce irreversible darkening of the iris and eyelashes
57
beta1 receptor blockers
spare bronchioles because it is selective for beta1 receptors at low concentrations metoprolol atenolol betaxolol esmolol
58
mixed alpha1 and beta blocker
beta blockers with additional actions that are sometiems called "third generation" labetalol - current drug of choice to treat hypertension in pregnancy carvedilol - durg of choice to treat patients with mild heart failure

Foundations 2 (33 decks)

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