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Pharm Exam 2 > Sympathomimetics Drugs/and adrenergic receptors > Flashcards

Sympathomimetics Drugs/and adrenergic receptors Flashcards

1
Q

Direct Sympathomimetics name

A

Epinephrine
Norepinephrine
Isoproterenol
Dopamine
Dobutamine
Phenylephrine
Midodrine
Clonidine
Dexmedetomidine
Ephedrine

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2
Q

Epinephrine

A

Direct agonist of Sympathomimetics
Alpha
Beta 1 and 2
Treats hypotension
Cardiac
Respiratory

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3
Q

Norepinephrine

A

Alpha and beta 1
Cardiac

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4
Q

Isoproterenol

A

Selective beta agonist
Beta 1 and 2
Cardiac

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5
Q

Dopamine

A

Dopamine receptors and beta 1
Dose dependent
Vasodilation
Vasoconstriction

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6
Q

Dobutamine

A

Beta 1
Cardiogenic shock

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7
Q

Phenylephrine

A

Pure Alpha agonist
noncatecholamine bc lack OH groups
Decongestant

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8
Q

Midodrine

A

Alpha 1
Orthostatic hypotension

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9
Q

Clonidine

A

Also called catapres
Alpha 2
Hypertension
Hemodynamic instability

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10
Q

Dexamedotomidine

A

Alpha 2
Anesthesia

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11
Q

Ephedrine

A

BOTH DIRECT AND INDIRECT
decongestant

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12
Q

How do indirect Sympathomimetics agonist work and name them

A

Release catecholamines from presynaptic terminal so we have more norepi(NE) in the synapse for longer periods of time by either 1) blocking the reuptake of NE or 2) reversing the NET(norepi transporter) where the pump actually pumps more NE into synapse
Ampethamine
Cocaine
ephedrine

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13
Q

Amphetamine

A

Indirect agonist of Sympathomimetics
Displacement of Norepi
reverse NET(norepi transporter)
block DAT
diet, ADHD, and recreational

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14
Q

Cocaine

A

Block NET(norepi tranporter) AND DAT
recreational

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15
Q

Alpha agonist BP effect

A

INCREASED

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16
Q

Beta agonist BP Effect

A

DECREASED
EXCEPT
pulse pressure increased

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17
Q

Alpha agonist HEART effect

A

Contractility = no effect or little increase
HR= decreased; vagal reflex
SV= mixed
Cardiac output= decreased

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18
Q

Beta agonist HEART Effect

A

Contractility= increased !
HR= increased
SV= increased
Cardiac output = increased

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19
Q

Mixed agonist effect on HEART

A

Increased Contractility, SV, and CO

HR mixed

20
Q

Alpha agonist VASCULAR RESISTANCE (tone) effect

A

Increased everywhere

21
Q

Beta agonist VASCULAR RESISTANCE AKA TONE EFFECT

A

decreased everywhere

22
Q

Alpha 1 tissue and action

A

Vascular smooth muscle = contraction
Pupillary dilator muscle = contraction so pupillary dilates
Prostate = contraction
Heart= increases force of contraction

23
Q

Alpha 2 tissues

A

Adrenergic and Cholinergic nerve terminals

24
Q

Beta 1 tissues and actions

A

Heart= increases force and rate of contraction; increases renin release

25
Q

Beta 2 tissues and action

A

Respiratory, uterine, vascular smooth muscle = relaxes

26
Q

Beta 3 tissue

A

Fat cells

27
Q

Dopamine tissue and action

A

Smooth muscle = dilates renal blood vessels

28
Q

Alpha 1 receptor G protein and effects

A

Gq which activates phospholipase C so then increases IP3 and DAG

29
Q

Alpha 2 G Protein and effect

A

Gi= inhibitory
And decreases cAMP

30
Q

Beta G protein and effect

A

Gs= stimulatory
Increases cAMP

31
Q

adrenergic receptors

A

respond to the endogenous ligands–> norepi and epi

signal transduction happens when drug binds to them

alpha(1 and 2), beta(1,2,3), and dopamine(1-5)

32
Q

Adrenergic Gq is found in

A

alpha 1 receptors

the smooth muscle cell that surrounds the blood vasculature

33
Q

adrenergic beta 1 is found in

A

the heart and is stimulatory and gives contraction

34
Q

adrenergic beta 2

A

some is found in the heart but mainly in the peripheral smooth muscle and is inhibitory/relaxation

35
Q

describe beta 2 in the skeletal muscle

A

associated with blood vessels that feed into the skeletal muscle so important during the sympathetic responses to shunt blood to the skeletal muscles

75% of blood shunted to skeletal muscles during SNS away from the GI

36
Q

generic–>in the SNS the heart

A

increases contractility and HR by epi and norepi binding to beta 1 or beta 2 receptors

37
Q

generic–> SNS in the skeletal muscle blood vessels

A

vasodilate if epi and norepi bind to beta 2 receptors to increase the BP

and increase the blood flow to skeletal muscles

38
Q

generic–> SNS in the smooth muscle blood vessels

A

vasoconstrict if epi and norepi bind to alpha 1 receptors to increase BP

39
Q

generic–> SNS in the bronchiole smooth muscle

A

bronchodilates if epi and norepi bind to beta 2 receptors in lungs to increase O2 to lungs

40
Q

can catecholamines cross the BBB

A

not usually so not a lot of effect on CNS unless given in high doses which then would cause nervousness/feeling of doom

41
Q

can noncatecholamines cross the BBB

A

yes so amphetamines and cocaine can have effect on CNS

42
Q

why cant catecholamines be taken orally

A

bc they are inactivated by COMT(catechol-O-methyltransferase) in the gut

43
Q

why can noncatecholamines be taken orally

A

because they are not broken down by COMT in the gut(catechol-O-methyltransferase)

44
Q

what breaks down catecholamines in the gut

A

COMT

catechol-O-methytransferase

45
Q

bc noncatecholamines are not inactivated in the gut this means

A

1) can be taken orally 2) longer half lives 3) increased lipid solubility 4) increased oral bioavailability

46
Q

describe the anatomy of catecholamines

A

have a catechol group and amine group on the side chain

benzene ring with 2 adjacent OH groups(hydroxyl groups)

47
Q

what does substituting the benzene ring on catecholamines do

A

greatly reduces potency of drug

Pharm Exam 2 (9 decks)

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