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
Q

beta 1 specificity

A

isoproterenol > epinephrine = norepinephrine

26
Q

beta 1 role

A

adrenergic cardiac effects, renin release

27
Q

beta 1 location

A

located in heart, JG apparatus & adipose tissue

28
Q

beta 1 mechanism

A

acts to increase cAMP via Gas

29
Q

beta 2 specificity

A

isoproterenol > epinephrine&raquo_space; norepinephrine

30
Q

beta 2 role

A

relaxation of smooth muscle & metabolic (glycogenolytic) effects

31
Q

beta 2 location

A

primary site in cardiovascular system is blood vessels (smooth muscle in general)

32
Q

beta 2 mechanism

A

acts to increase cAMP via Gas

33
Q

dopaminergic role

A

dilation of renal and mesenteric vasculature

react with dopamine

34
Q

Synthetic B1 agonist

A

dobutamine (dobutrex)

35
Q

Dobutamine specificity

A

selective B1 agonist (net effect)

36
Q

Dobutamine actions

A

positive inotrope (contractility)

37
Q

dopamine effect

A

CV: positive inotrope (B1), vasodilator in renal/mesenteric at low doses (dopaminergic), vasoconstrictor (a1) at higher doses
Neural: release NE from nerves

38
Q

therapeutic uses of dopamine

A

shock (maintain renal perfusion), hypotension, chronic refractory heart failure

39
Q

therapeutic use dobutamine

A

congestive heart failure, acute MI with heart failure

40
Q

alpha 1 agonists

A

PHENYLEPHRINE (Donatussin, Duo-Medihaler, Albatussin, Neosynephrine, etc.)
Midodrine (ProAmatine)

41
Q

alpha 1 agonist uses

A

used to reverse hypotension or to treat paroxysmal atrial tachycardia

also used as a decongestant (5 mg orally), topical vasoconstrictor and mydriatic

42
Q

what do alpha 1 agonists do to BP

A

raise it

43
Q

B2 selective agonists

A

METAPROTERENOL , Terbutaline (Brethine, Bricanyl), ALBUTEROL (Proventil, Ventolin), RITODINE (Yutopar), Pirbuterol (Maxair, SALMETEROL (Serevent), Isoetharine (Bronkosol, Bronkometer), Bitolterol (Tornalate)

44
Q

B2 agonist uses

A

bronchodilation for all except ritodrine

delay labor - ritodrine, terbutaline

45
Q

What do B2 selective agonists do to blood pressure

A

vasodilation –> lower BP

46
Q

synthetic catecholamine stimulating ß receptors

A

Isoproterenol

47
Q

effects of Isoproterenol

A

vasodilate (ß2), tachycardia (ß1)

Overall - lower BP (dilation predominant effect)

48
Q

use of isoproterenol

A

cardiac stimulant (B1)

49
Q

Norepi CV actions

A

vasoconstriction (a1);
increased heart rate & force (ß1);
reflex reduction in heart rate (mediated by vagus nerve)

50
Q

therapeutic use for Norepi

A

to tx htx

51
Q

what does Norepi do to BP

A

raise BP

52
Q

epinephrine actions CV

A

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
Q

therapeutic uses epi

A
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
Q

what does epi do to BP

A

raise it (can lower it in some vessels)