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Spring '20/ L. Pharm Exam 3 - sympatholytics/mimetics, LAs, antiarrhythmics, vaso > SYMPATHOMIMETIC DRUGS > Flashcards

SYMPATHOMIMETIC DRUGS Flashcards

1
Q

Natural Catecholamines what are they called? what are 3 examples?

A

endogenous

EPI
NE
Dopamine

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2
Q

Synthetic catecholamine

2

A

Isoproterenol

Dobutamine

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3
Q

Synthetic non-catecholamine (Indirect acting)

4

A

Ephedrine
Mephentermine
Amphetamine
Metaraminol

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4
Q

Synthetic non-catecholamine (Direct acting)

2

A

Phenylephrine

Methoxamine

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5
Q

what medication inhibits the transport of dopamine into the synaptic vesicle

A

reserpine

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6
Q

what does dopamine become when it enters the vesicle

A

norepinephrine

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7
Q

which 2 drugs blocks the release of NE from the presynaptic cell membrane

A

guanethidine and bretylium

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8
Q

how is NE released from the cell membrane

A

exocytosis from the Ca++ influx

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9
Q

once NE is released it binds to the receptors activating what

A

adenylate cyclase

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10
Q

once NE activates adenylate cyclase what does it do next

A

opening of ion channel/ formation of cAMP

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11
Q

once NE channels are open and camp is activated what is the last step

A

contraction of arterial smooth muscles, increase heart rate and contractility

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12
Q

removal of NE. what inhibits reuptake

A

cocaine and TCA

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13
Q

what metabolizes NE

A

COMT (PLASMA) and MAO (synaptic cleft)

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14
Q

what are Adrenergic Receptors

A

a1, a2, b1, b2, b3

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15
Q

what are cholinergic receptors

A

nicotinic and muscarinic receptors

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16
Q

a1 Receptors

located where?

A

vascular smooth muscle of skin

splanchnic regions

GIT

bladder sphincter

radial muscle of iris

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17
Q

a1 Receptors what is their effect?

A

Produce excitation (contraction of vascular smooth muscles)

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18
Q

a1 Receptors what are they equally sensitive to?

A

NE and EPi

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19
Q

a1 receptor arterial vasoconstriction leads to what CV effects ?

A

increase SVR, LV afterload, and BP

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20
Q

a1 receptor venous vasoconstriction causes what effect ?

A

increase venous return, increase SV, increase CO

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21
Q

a1 receptor stimulation inhibit what

A

insulin secretion and lipolysis

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22
Q

a1 receptor m/a

A

formation of IP3 and increased intracellular calcium

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23
Q

a1 receptor pre synaptic or post synaptic?

A

postsynaptic adrenergic

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24
Q

a2 receptors location?

A

presynaptic membrane & postsynaptic in brainstem, walls of GIT, platelets, and fat cells

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25
Q

a2 receptors are postsynaptic in?

A

brainstem, platelets, fat cells, and walls of GIT

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26
Q

a2 receptors produce

A

inhibition of NE release and synthesis (relaxation and dilatation) blocks Ca entry

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27
Q

a2 receptors produce what type of feed back loop

A

-ve

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28
Q

a2 receptors inhibit what

A

sympathetic outflow in brain stem

29
Q

a2 receptors produce

A

sedation and analgesia in substantia gelatinosa

30
Q

a2 receptors m/a

A

inhibition of adenylate cyclase, decrease camp and decreases ca entry

31
Q

b1 receptors are located where

A

sa node and av node ventricular muscle

32
Q

b1 receptors produce

A

excitation, increase hr, increase conduction, increase contractility, and increase cardiac output.

33
Q

b1 receptors are sensitive to

A

NE and EPI

34
Q

b1 receptors m/a

A

activation of adenylate cyclase and increase camp

35
Q

b2 receptors location

A

smooth muscle of skeletal muscle blood vessel

bronchial smooth muscle

walls of GIT and bladder

36
Q

b2 receptors produce what?

A

relaxation (dilation of vascular smooth muscle, dilation of bronchioles, relaxation of the pregnant uterus- tocolysis)

37
Q

b2 receptors also produce increase

A

bg calorigenesis

glycogenolysis and gluconeogenesis

38
Q

b2 receptors m/a

A

activation of adenylate cyclase and increase cAMP (same as b1)

39
Q

b3 receptors located where

A

gallbladder and adipose tissue

40
Q

b3 receptor function

A

unknown function

41
Q

nicotinic receptors located where

A

autonomic ganglia (Nn) of the sympathetic and parasympathetic neuromuscular junction(n1) and adrenal medulla (n2) the receptors at these locations are similar but no identical

42
Q

nicotinic receptors are activated by

A

ach or nicotine

43
Q

nicotinic receptors produce

A

excitation

44
Q

cholinergic receptors nicotinic receptors ganglion blockers examples and what do they do

A

hexamthonium trimethaphan block the nicotinic receptors for Ach in autonomic ganglia but not at the NMH

45
Q

cholinergic receptors nicotinic receptors m/a

A

opening of Na+ and K+ channels

46
Q

cholinergic muscarinic receptors - location

A

in heart (m2) smooth muscle (m3) (except vascular smooth muscle) and glands(m3)

47
Q

cholinergic receptors muscarinic receptors -activated by

A

Ach and muscarine

48
Q

cholinergic receptors muscarinic receptors are inhibitory

A

in heart (decrease heart rate decrease conduction velocity in AV node)

49
Q

cholinergic receptors muscarinic receptors are excitatory

A

in smooth muscle and glands increase motility and increase secretion

50
Q

cholinergic receptors muscarinic receptors are blocked by

A

atropine

51
Q

cholinergic receptors muscarinic receptors mediate

A

sux induced bradycardia

52
Q

cholinergic receptors muscarinic receptors m/a

in heart?

in smooth muscles?

A

in heart sa node: inhibition of adenylate cyclase leads to opening k channels, slowing rate of phase 4 depolarization and decrease heart rate.

in smooth muscles and glands: formation of IP3 and increase intracellular Ca++

53
Q

cAMP Mechanism receptors

A

B1 &B2 & A2

54
Q

receptors couples with ion channels

A

cholinergic nicotinic

55
Q

IP3 mechanism receptor

A

A1 receptor

cholinergic muscarinic

56
Q

Nitric Oxide utilizes this second messanger

A

cGMP

57
Q

Epinephrine

mechanism
application

A

Direct general agonist (a1, a2, b1, b2)

Anaphylaxis, glaucoma (open angle) asthma, hypotension with LA

58
Q

Norepinephrine

mechanism
application

A

a1, a2, b1

hypotension decrease renal perfusion organ ischemia

59
Q

isoproterenol

mechanism
application

A

B1=B2

av block (rare)

60
Q

dopamine

mechanism
application

A

D1=D2 >b>a

shock increase renal perfusion and GFR heart failure

61
Q

dobutamine

mechanism
application

A

b1>b2

shock and CHF

62
Q

amphetamine

mechanism
application

A

indirect general agonist
releases stored catecholamines

narcolepsy, obesity, adhd

63
Q

ephedrine

mechanism
application

A

indirect general agonist, releases stored catecholamines

nasal decongestants urinary incontinence hypotension hypotension with epidural/spinal anesthesia

64
Q

phenylephrine

mechanism
application

A

a1>a2

pure a agonist

pupil dilation vasoconstrictor increase SVR increase MAP nasal decongestant

65
Q

albuterol, terbutaline

A

B2>b1

asthma & premature labor

66
Q

cocaine

mechanism
application

A

indirect general agonist uptake inhibitor

causes vasoconstriction and local anesthesia

67
Q

clonidine & a-methyl dopa

A

centrally acting a2 agonist, decrease central sympathetic outflow

hypertension, decrease MAC, increase Anesthesia/analgesia

224
Q

Nonselective Beta 1 Beta 2 antagonist (propranolol) what effect ok K+ level?

A

Hypokalemia prevention .

( explanation) By blocking beta 2 .Prevents the Beta 2 activation of Na/K pump which causes K+ to move inside inside cell. Prevent the K movement inside cell, prevents hypokalemia.

225
Q

Cardioselfrive Beta 1 antagonist ( atenolol ) effect of K+level

A

Cause hypokalemia

Spring '20/ L. Pharm Exam 3 - sympatholytics/mimetics, LAs, antiarrhythmics, vaso (17 decks)

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