Anticholinergic Drugs Flashcards

1
Q

MAO inhibitor we must know

A

Pargyline

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2
Q

Pargyline is a _______

A

MAO inhibitor

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3
Q

Synthesis of norepinephrine

A

tyrosine –> dopa –> dopamine –> norepinephrine, epinephrine in adrenal medulla

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4
Q

norepinephrine inhibits its own release at ___ receptors

A

alpha 2

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5
Q

tyramine, amphetamine, ephedrine are ______

A

indirectly acting sympathomimetics

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6
Q

tyramine, amphetamine, ephedrine mechanism

A

induce release of norepi via reversing direction of axoplasmic catecholamine transporter

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7
Q

indirectly acting sympathomimetics

A

tyramine, amphetamine, ephedrine

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8
Q

Cocaine and imipramine mechanism

A

inhibit axoplasmic pump to potentiate sympathetic responses

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9
Q

Reserpine (serpasil) mechanism

A

inhibits the granular pump accumulating catecholamines in vesicles (results in depletion of catecholamines)

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10
Q

inhibits the granular pump accumulating catecholamines in vesicles (results in depletion of catecholamines)

A

reserpine

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11
Q

inhibit axoplasmic pump to potentiate sympathetic responses

A

cocaine and imipramine mechanism

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12
Q

induce release from vesicle, probably via displacement
depletes norepinephrine stores
reduces responses to sympathetic stimulation

A

Guanethidine and Guanadrel

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13
Q

Guanethidine and Guanadrel mechanism

A

induce release from vesicle, probably via displacement
depletes norepinephrine stores
reduces responses to sympathetic stimulation

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14
Q

adrenergic amines - termination of effects

A

uptake
dilution and diffusion
degradation (COMT, MAO)

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15
Q

MAO inhibitors ______ the action of catecholamines

A

potentiate

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16
Q

individuals receiving MAO inhibitors avoid foods high in

A

tyramine (cheese, wine, beer :( ) - tyramine releases catecholamines and is normally degraded by MAO in intestine.

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17
Q

urinary products of catecholamine breakdown

A

vanillylmandelic acid (VMA), normetanephrine

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18
Q

alpha 1 specificity

A

epinephrine >= norepinephrine&raquo_space; isoproterenol

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19
Q

alpha 1 role

A

mediates smooth muscle contraction (primary Cardiovascular location is blood vessels)

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20
Q

alpha 1 mechanism

A

activates phospholipase C (Gaq dependent process)

To increase intracellular calcium via inositol trisphosphate

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21
Q

alpha 2 specificity

A

epinephrine >= norepinephrine&raquo_space; isoproterenol

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22
Q

alpha 2 role

A

inhibition of neural norepinephrine release

23
Q

alpha 2 location

A

prejunctional nerve terminal, platelets, gut, medulla oblongata

24
Q

alpha 2 mechanism

A

acts to decrease cAMP or activate Na/H antiporter

Gai dependent process

25
beta 1 specificity
isoproterenol > epinephrine = norepinephrine
26
beta 1 role
adrenergic cardiac effects, renin release
27
beta 1 location
located in heart, JG apparatus & adipose tissue
28
beta 1 mechanism
acts to increase cAMP via Gas
29
beta 2 specificity
isoproterenol > epinephrine >> norepinephrine
30
beta 2 role
relaxation of smooth muscle & metabolic (glycogenolytic) effects
31
beta 2 location
primary site in cardiovascular system is blood vessels (smooth muscle in general)
32
beta 2 mechanism
acts to increase cAMP via Gas
33
dopaminergic role
dilation of renal and mesenteric vasculature | react with dopamine
34
Synthetic B1 agonist
dobutamine (dobutrex)
35
Dobutamine specificity
selective B1 agonist (net effect)
36
Dobutamine actions
positive inotrope (contractility)
37
dopamine effect
CV: positive inotrope (B1), vasodilator in renal/mesenteric at low doses (dopaminergic), vasoconstrictor (a1) at higher doses Neural: release NE from nerves
38
therapeutic uses of dopamine
shock (maintain renal perfusion), hypotension, chronic refractory heart failure
39
therapeutic use dobutamine
congestive heart failure, acute MI with heart failure
40
alpha 1 agonists
PHENYLEPHRINE (Donatussin, Duo-Medihaler, Albatussin, Neosynephrine, etc.) Midodrine (ProAmatine)
41
alpha 1 agonist uses
used to reverse hypotension or to treat paroxysmal atrial tachycardia also used as a decongestant (5 mg orally), topical vasoconstrictor and mydriatic
42
what do alpha 1 agonists do to BP
raise it
43
B2 selective agonists
METAPROTERENOL , Terbutaline (Brethine, Bricanyl), ALBUTEROL (Proventil, Ventolin), RITODINE (Yutopar), Pirbuterol (Maxair, SALMETEROL (Serevent), Isoetharine (Bronkosol, Bronkometer), Bitolterol (Tornalate)
44
B2 agonist uses
bronchodilation for all except ritodrine | delay labor - ritodrine, terbutaline
45
What do B2 selective agonists do to blood pressure
vasodilation --> lower BP
46
synthetic catecholamine stimulating ß receptors
Isoproterenol
47
effects of Isoproterenol
vasodilate (ß2), tachycardia (ß1) | Overall - lower BP (dilation predominant effect)
48
use of isoproterenol
cardiac stimulant (B1)
49
Norepi CV actions
vasoconstriction (a1); increased heart rate & force (ß1); reflex reduction in heart rate (mediated by vagus nerve)
50
therapeutic use for Norepi
to tx htx
51
what does Norepi do to BP
raise BP
52
epinephrine actions CV
therapeutically usually vasoconstricts (a1), can vasodilate (ß2); directly increases heart rate and force but reflexes to the elevation in blood pressure can suppress heart rate (vagal stimulation)
53
therapeutic uses epi
``` hypersensitivity reactions-low BP and bronchospasm (a 1 and ß2) with anesthetics (a 1)- vasoconstriction prevents diffusion of anesthetic; topical hemostatic (a1); restore heart beat (ß1) ```
54
what does epi do to BP
raise it (can lower it in some vessels)