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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
Receptors for DA
D1=D2
26
Effects of Epi on cardiac function w/ b1 (3)
Ionotropic effect Inc. HR Inc. conduction velocity at AV node
27
Effects of Epi on cardiac vascular tone w/ b2 and a1 (3)
Inc. systolic BP May dec. diastolic BP and TPR MAP does not change
28
What receptors at which vascular sites are effected by Epi? (3)
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
Epi's effects on the respiratory system and its receptors (2)
b2 - relaxes bronchial m. a1 - decrease bronchial secretion and congestion in mucosa
30
Epi's effect on skeletal m. and its receptor (1)
b2 - muscle tremor, inc. K+ uptake | -promotes hypokalemia and dec. K+ secretion by kidneys.
31
Epi's effect on blood Glc levels and receptor (1)
b2 - enhance liver glycogenolysis and GNG
32
What effect does Epi have on free fatty levels in blood?
Increases it
33
What effect doe Epi have on renin release?
Increases it
34
NE effects on the heart
Cardiac stimulant, but reduces HR
35
What role does NE have on vasculature?
Potent vasoconstrictor -> increased PVR and BP
36
What role does NE have on respiration?
None, because there is no b2 effect of NE.
37
Phenylephrine actions (3)
Decongestant/mydriatic Severe vasoconstriction, BP elevation Severe bradycardia a1
38
Clonidine actions (4)
Dec sympathetic outflow Reduce BP Bradycardia If applied locally, vasoconstriction* a2
39
Isoproterenol actions (3)
Ionotropy and chronotropy -> inc. CO (b1) Vasodilator (b2) Bronchodilator (b2)
40
Dobutamine action (1)
Ionotropy
41
What is unique about the a1 activity of Dobutamine?
(-) isomer is an agonist | (+) isomer is an antagonist
42
Albuterol actions (2)
Bronchodilation | Uterine relaxation
43
DA actions (4)
Vasodilation at renal tissue Suppress NE release At higher doses, b1 in heart is activated. Even higher doses activates a1 in vasculature.
44
What are indirect adrenergic agonists? Example (7)
Usually more lipophilic and can easilty penetrate BBB to have CNS effects (stimulant). ``` Amphetamine Methamphetamine Methylphenidate Cocaine Ephedrine Phenelzine, selegiline Tyramine ```
45
Ephedrine indirect action: It is a mild... What is it used for clinically? (3)
Release stored cetacholamines w/ some direct action. Enters CNS. Nasal decongestant, increased BP, stress incontinence in women.
46
What is the use of Phenelzine, selegiline?
Antidepressive
47
Anti-adrenergic synthesis inhibitor (1) and MOA
Metyrosine inhibits tyrosine hydroxylase. Indirect acting.
48
Guanethidine is ________. MOA?
Anti-adrenergic. Prevents storage of NE. Indirect acting.
49
Non-selective a1 and a2 receptor antagonists (2)
Phentolamine | Phenoxybenzamine
50
a1 receptor selective antagonists (3)
Prazosin Tamsulosin Doxazosin
51
What kind of inhibitor is phentolamine?
Reversible competitive alpha antagonist | Shorter-acting
52
What kind of inhibitor is phenoxybenzamine?
Non-competitive irreversible alpha antagonist | Longer-acting
53
Effects of alpha-antagonists on CVS (3)
Dec. PVR and BP Posttural hypotension Reflex tachy
54
Effects of alpha-antagonists on GU system (2)
Prostate SM relaxation | Dec. resistance to urine flow
55
Effect of alpha-antagonists on the eye (1)
Miosis (pupillary constriction)
56
Adverse effects of alpha-antagonists examples
``` Postural hypoTN Tachy Salt/fluid retention Impaired ejaculation Nasal stiffness ```
57
Beta-blockers w/ ISA (intrinsic sympathomimetic activity) are known as: What is the effect? How are they useful?
Partial agonists at beta adrenergic receptors. A blunted SNS response. Less risk for bradycardia and increase in LDL
58
Beta-blockers' effects on the heart (3)
Negative ionotropic effect Negative chronotropic effect Slow AV conduction
59
Beta-blockers' effect on BVs chronically vs. initially
Initially - rise in PVR Chronically - decrease PVR due to lower BP
60
Beta-blockers' effect on the respiratory system (1)
Inc airway resistance
61
Beta-blockers' effect on the eyes (1)
Reduce production of aqueous humor and intraocular pressure
62
Beta-blockers' effect on metabolism (3)
Inhibit lipolysis Inc LDL and dec. HDL (inc. the ratio) Inhibit sugar breakdown in the liver

SBL (44 decks)

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