Adrenergic drugs Flashcards

1
Q

Alpha 1 type AR G protein and effect

A

Gq, Increase IP3 and DAG

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2
Q

Alpha 2 type AR G protein and effect

A

Gi, decrease cAMP

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3
Q

Beta 1, 2, 3 type AR G protein and effect

A

Gs, increase cAMP

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4
Q

Dopamine 1-5 AR G protein and effect

A

1 and 5 Gs increase cAMP

2-4 Gi decrease cAMP

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5
Q
Alpha 1 physical effects:
Vascular smooth muscle
Pupillary dilator muscle
Prostate
Heart
A

Contraction
Contraction (mydriasis/dilation)
Contraction
Increases force of contraction

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6
Q
Alpha 2 physical effects:
Postsynaptic CNS neurons
Platelets
Adrenergic and cholinergic nerve terminals
Some vascular smooth muscle
Fat cells
A
Probably multiple
Aggregation
Inhibits NT release
Contraction
Inhibits lipolysis
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7
Q

Beta 1 physical effects:

Heart, juxtaglomerular cells

A

Increases force and rate of contraction; increases renin release

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8
Q

Beta 2 physical effects:
Respiratory, uterine and vascular smooth muscle
Skeletal muscle
Human liver

A

Promotes smooth muscle relaxation
Promotes potassium uptake, increase contractility
Activates glycogenolysis and gluconeogenesis

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9
Q

Beta 3 physical effects:
Bladder
Fat cells

A

Relaxes detrusor muscle

Activates lipolysis

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10
Q

Direct Alpha agonist drugs

A

Phenylephrine

Clonidine

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11
Q

Direct mixed alpha and beta agonists

A

NE and Epi

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12
Q

Direct beta agonist drugs

A

Dobutamine, isoproterenol, albuterol

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13
Q

Direct dopamine agonist drugs

A

Dopamine

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14
Q
Epinephrine
What receptors does it act on?
Effect on cardiac function
Effect on vasculature
Effect on respiratory system
Other effects
A

Acts on Alpha 1 and 2, Beta 1 and 2 agonist
Increases force of contraction, HR and conduction velocity
Increases systolic BP, but decreases diastolic and TPR, MAP often remains unchanged; cutaneous vessel contraction; skeletal muscle vasculature dilation
Relaxes bronchial muscle, decreases secretion and congestion
Causes muscle tremor, increases K uptake by skeletal muscle, elevates blood glucose levels, increases free fatty levels in blood, increases renin release

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15
Q
Norepinephrine
Receptors?
Effects on heart?
Effects on vasculature
Effects on lungs
A

Alpha 1 and 2, beta 1 agonist
Cardiac stimulant, but reduces heart rate
Vasoconstrictor
No bronchodilation
Increases peripheral vascular resistance and BP

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16
Q
Phenylephrine
Receptors?
Effect on eye
Effect on lung
Vasculature
Heart
A
Alpha 1 agonist
Mydriatic
Decongestant
Severe vasoconstriction, BP elevation
Severe bradycardia
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17
Q
Clonidine
Receptors
Effects?
Local application produces?
MOA
A

Selective alpha 2 agonist
Targets brainstem to decrease sympathetic outflow, reduces BP and bradycardia
Vasoconstriction
Regulates NE release by presynaptic alpha 2 adrenoceptors

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18
Q

Isoproterenol
Receptors
Effects

A

Beta 1 and 2 agonist

Increase HR, strength of contraction, CO, vasodilator, decrease arterial pressure, causes bronchodilation

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19
Q

Dobutamine
Receptors
Effects

A

Beta 1 agonist, alpha 1 receptor activity
Potent inotropic action
Less prominent chronotropic effect compared to isoproterenol

20
Q

Albuterol
Receptors
Effect

A

B2 agonist

causes bronchodilation and relaxation of uterus

21
Q

Dopamine
Receptors
Effect

A

D1 and 2 agonist
Causes vasodilation in renal, cerebral, mesenteric and coronary vessels
Suppresses NE release
Activates B1 in heart at higher doses
At even higher doses, stims alpha 1 receptors in vasculature to cause vasoconstriction

22
Q

Cocaine MOA and effect

A

Inhibits re uptake of DA and NE

Local anesthetic properties, peripheral and intense central action

23
Q

Phenelzine/selegiline MOA and effect

A

Inhibits MAO

Increases NE stores in CNS, antidepressant

24
Q

Amphetamines/methylphenidate MOA and effect

A

Inhibits reuptake of DA and NE, increases their release, may have weak direct effect
Stimulant on mood and alertness, decreases appetite

25
Q

Ephedrine MOA and effect

A

Releasing agent and direct adrenergic receptor agonist

Mild stimulant, enters CNS, used as nasal decongestant, increases BP, treats stress incontinence in women

26
Q

Tyramine MOA and effect

A

Releases stored NE from presynaptic adrenergic terminals, increase in BP

27
Q

Adrenergic agonists to use in hypotensive emergencies

A

NE, phenylephrine

28
Q

Adrenergic agonists to use in chronic hypotension

A

Ephedrine

29
Q

Adrenergic agonists to use in cardiogenic shock dt massive acute MI

A

Dopamine, dobutamine

30
Q

Ad agonists for heart failure

A

Dobutamine for acute, dopamine for congestive severe with reduced renal perfusion

31
Q

Ad agonists for HTN

A

Alpha 2 agonists

32
Q

Ad agonists for complete AV block and cardiac arrest

A

Epinephrine, isoproterenol

33
Q

Ad agonists for obesity

A

Ephedrine, amphetamines

34
Q

Bronchial asthma

A

Albuterol (b2 agonist)

35
Q

Decongestion of mucous membranes

A

Phenylephrine, ephedrine

36
Q

Anaphylaxis

A

Epinephrine

37
Q

Mydriasis

A

Phenylephrine

38
Q

Glaucoma

A

Alpha 2 agonists

39
Q

Alpha 1 and 2 antagonists

A

Phentolamine

Phenoxybenzamine

40
Q

Alpha 1 antagonists

A

Prazosin
Tamsulosin
Doxazosin

41
Q

Alpha antagonist effects
CV
GU
Eye

A

Decreased peripheral vascular resistance and BP, postural hypotension, reflex tachycardia
Relaxation of smooth muscle in prostate, decreased resistance to flow of urine
Relaxation of pupillary dilator muscle (miosis)

42
Q

Alpha antagonist uses

A

Pheochromocytoma (non selective)
Chronic hypertension (alpha 1 selective)
ED
BPH (tamsulosin)

43
Q

Mixed blockers

A

Labetalol (beta and alpha 1 antagonist)

Carvedilol (beta and alpha 1 antagonist)

44
Q

Beta blockers

A

Non selective: propranolol, pindolol, nadolol

B1 selective: metoprolol, betaxolol, acebutolol, atenolol

45
Q
Effect of beta blockers
Heart
BVs
RAS
Resp
Eye
Metabolism
A

Decrease HR and contractility, slow AV conduction
Initial rise in peripheral vascular resistance, chronic use leads to decrease in PVR (lowers BP in HTN individuals)
Inhibit renin release
Increase airway resistance
Reduce production of aqueous humor, reduced intraocular pressure
Inhibits lipolysis, increase VLDL and decrease HDL, inhibits glycogenolysis and gluconeogenesis

46
Q

Uses of beta blockers

A

HTN, angina pectoris, MI, arrhythmias, HF, glaucoma, hyperthyroidism