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SBL > Adrenergic Drugs > Flashcards

Adrenergic Drugs Flashcards

1
Q

a1 type

G protein
Effect

A

Gq

Inc. IP3, DAG

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2
Q

a2 type

G protein
Effect

A

Gi

Dec. cAMP

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3
Q

b type

G protein
Effect

A

Gs

Inc. cAMP

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4
Q

Which D receptors are Gs?

A

D1 and D5

Inc. cAMP

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5
Q

Which D receptors are Gi?

A

D2, D3, D4

Dec. cAMP

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6
Q

a1 actions at:

Vascular SM
Pupillary dilator m.
Prostate
Heart

A

Vascular SM - contraction
Pupillary dilator m. - contraction (pupillary dilation)
Prostate - contraction
Heart - inc. force of contraction

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7
Q

a1 receptors are at which tissues? (4)

A

Vascular SM
Pupillary dilator m.
Prostate
Heart

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8
Q

a2 actions at:

Platelets
Adrenergic/cholinergic nerve terminals
Some vascular SM
Adipocytes

A

Platelets - aggregation
Adrenergic/cholinergic nerve terminals - inhibit transmitter release
Some vascular SM - contraction
Adipocytes - inhibit lipolysis

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9
Q

a2 receptors are at which tissues? (4)

A

Platelets
Adrenergic/cholinergic nerve terminals
Some vascular SM
Adipocytes

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10
Q

b1 actions at:

Heart
JG cells

A

Heart - inc. rate AND force of contraction

JG cells - inc. renin release

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11
Q

b1 receptors are at which tissues? (2)

A

Heart

JG cells

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12
Q

b2 actions at:

Respiratory, uterine and vascular SM
Skeletal m.
Liver

A

Respiratory, uterine and vascular SM: SM relaxation
Skeletal m.: inc. K+ uptake
Liver: activate glycogenolysis and gluconeogenesis

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13
Q

b2 receptors are at which tissues? (3)

A

Respiratory, uterine and vascular SM
Skeletal m.
Liver

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14
Q

D1 actions at:

SM

A

SM - dilates renal BVs

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15
Q

D2 actions at:

Nerve endings

A

Modulate NT release

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16
Q

How do indirect-acting adrenergic drugs produce an effect?

A

By increased/decreasing conc. of NE at target receptors.

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17
Q

Indirect-acting drugs and their manner of action (3)

A
  1. Cocaine: reuptake blockers of DA and NE.
  2. Phenelzine, selegiline: MAO inhibitors.
  3. Amphetamines and Ephedrine: releasing agents and direct receptor agonist.
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18
Q

Receptors for phenylephrine

A

a1>a2

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19
Q

Receptors for clonidine

A

a2>a1

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20
Q

Receptors for NE

A

a1=a2; b1>b2

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21
Q

Receptors for Epi

A

a1=a2; b1=b2

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22
Q

Receptors for Dobutamine

A

b1>b2 and a1

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23
Q

Receptors for Isoproterenol

A

b1=b2

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24
Q

Receptors for Albuterol

A

b2>b1

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25
Q

Receptors for DA

A

D1=D2

26
Q

Effects of Epi on cardiac function w/ b1 (3)

A

Ionotropic effect
Inc. HR
Inc. conduction velocity at AV node

27
Q

Effects of Epi on cardiac vascular tone w/ b2 and a1 (3)

A

Inc. systolic BP
May dec. diastolic BP and TPR
MAP does not change

28
Q

What receptors at which vascular sites are effected by Epi? (3)

A

Skin vessels and mucous membranes: a1

Skeletal m.: a1 and b2

Renal and cerebral: D1 and a1

*many different types of vascular beds have different receptors, so effects are varied

29
Q

Epi’s effects on the respiratory system and its receptors (2)

A

b2 - relaxes bronchial m.

a1 - decrease bronchial secretion and congestion in mucosa

30
Q

Epi’s effect on skeletal m. and its receptor (1)

A

b2 - muscle tremor, inc. K+ uptake

-promotes hypokalemia and dec. K+ secretion by kidneys.

31
Q

Epi’s effect on blood Glc levels and receptor (1)

A

b2 - enhance liver glycogenolysis and GNG

32
Q

What effect does Epi have on free fatty levels in blood?

A

Increases it

33
Q

What effect doe Epi have on renin release?

A

Increases it

34
Q

NE effects on the heart

A

Cardiac stimulant, but reduces HR

35
Q

What role does NE have on vasculature?

A

Potent vasoconstrictor -> increased PVR and BP

36
Q

What role does NE have on respiration?

A

None, because there is no b2 effect of NE.

37
Q

Phenylephrine actions (3)

A

Decongestant/mydriatic
Severe vasoconstriction, BP elevation
Severe bradycardia

a1

38
Q

Clonidine actions (4)

A

Dec sympathetic outflow
Reduce BP
Bradycardia
If applied locally, vasoconstriction*

a2

39
Q

Isoproterenol actions (3)

A

Ionotropy and chronotropy -> inc. CO (b1)

Vasodilator (b2)

Bronchodilator (b2)

40
Q

Dobutamine action (1)

A

Ionotropy

41
Q

What is unique about the a1 activity of Dobutamine?

A

(-) isomer is an agonist

(+) isomer is an antagonist

42
Q

Albuterol actions (2)

A

Bronchodilation

Uterine relaxation

43
Q

DA actions (4)

A

Vasodilation at renal tissue
Suppress NE release
At higher doses, b1 in heart is activated.
Even higher doses activates a1 in vasculature.

44
Q

What are indirect adrenergic agonists?

Example (7)

A

Usually more lipophilic and can easilty penetrate BBB to have CNS effects (stimulant).

Amphetamine
Methamphetamine
Methylphenidate
Cocaine
Ephedrine
Phenelzine, selegiline
Tyramine
45
Q

Ephedrine indirect action:

It is a mild…

What is it used for clinically? (3)

A

Release stored cetacholamines w/ some direct action.

Enters CNS.

Nasal decongestant, increased BP, stress incontinence in women.

46
Q

What is the use of Phenelzine, selegiline?

A

Antidepressive

47
Q

Anti-adrenergic synthesis inhibitor (1) and MOA

A

Metyrosine inhibits tyrosine hydroxylase.

Indirect acting.

48
Q

Guanethidine is ________.

MOA?

A

Anti-adrenergic.

Prevents storage of NE.
Indirect acting.

49
Q

Non-selective a1 and a2 receptor antagonists (2)

A

Phentolamine

Phenoxybenzamine

50
Q

a1 receptor selective antagonists (3)

A

Prazosin
Tamsulosin
Doxazosin

51
Q

What kind of inhibitor is phentolamine?

A

Reversible competitive alpha antagonist

Shorter-acting

52
Q

What kind of inhibitor is phenoxybenzamine?

A

Non-competitive irreversible alpha antagonist

Longer-acting

53
Q

Effects of alpha-antagonists on CVS (3)

A

Dec. PVR and BP
Posttural hypotension
Reflex tachy

54
Q

Effects of alpha-antagonists on GU system (2)

A

Prostate SM relaxation

Dec. resistance to urine flow

55
Q

Effect of alpha-antagonists on the eye (1)

A

Miosis (pupillary constriction)

56
Q

Adverse effects of alpha-antagonists examples

A 
Postural hypoTN
Tachy
Salt/fluid retention
Impaired ejaculation
Nasal stiffness
57
Q

Beta-blockers w/ ISA (intrinsic sympathomimetic activity) are known as:

What is the effect?

How are they useful?

A

Partial agonists at beta adrenergic receptors.

A blunted SNS response.

Less risk for bradycardia and increase in LDL

58
Q

Beta-blockers’ effects on the heart (3)

A

Negative ionotropic effect
Negative chronotropic effect
Slow AV conduction

59
Q

Beta-blockers’ effect on BVs chronically vs. initially

A

Initially - rise in PVR

Chronically - decrease PVR due to lower BP

60
Q

Beta-blockers’ effect on the respiratory system (1)

A

Inc airway resistance

61
Q

Beta-blockers’ effect on the eyes (1)

A

Reduce production of aqueous humor and intraocular pressure

62
Q

Beta-blockers’ effect on metabolism (3)

A

Inhibit lipolysis
Inc LDL and dec. HDL (inc. the ratio)
Inhibit sugar breakdown in the liver

SBL (44 decks)

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