Adrenergic Pharmacology Flashcards

1
Q

NE receptors

A

Alpha 1
alpha 2
beta 1

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2
Q

Epinephrine receptors

A

Alpha 1
Alpha 2
Beta 1
Beta 2

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3
Q

Alpha 1 receptor mediated effects

A

Mydriasis
Construction of arteries and veins
Construction of GI GU sphincters
Ejaculation

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4
Q

Beta 1 receptor mediated effectsa

A

Heart
Increase renin secretion
Increase lipolysis- increase FFA

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5
Q

Beta 2 receptor mediated effects

A
Bronchodilation
Dilation of arteries in skeletal muscle
Increase glycogenolysis and gluconeigenesis
Increase insulin secretion
Relaxation of uterus
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6
Q

Alpha 2 receptor mediated effects

A

Decrease sympathetic outflow from CNS
Decrease NE release
Decrease insulin secretion

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7
Q

Most abundant urinary metabolite of NE and Epi

A

3-Methoxy-4-hydroxy-mandelic acid (VMA)

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8
Q

Inhibition of tyrosine hydroxylase

A

Metyrosine- used to reduce NE Epi in pheochromocytoma

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9
Q

Tyramine

A

Induced release of NE/Epi
Dietary constituent
Effects enhanced by MAOIs-hypertensive crisis

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10
Q

Amphetamine

A

Release of NE/Epi

Pronounced CNS stimulation

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11
Q

Cocaine

A

Inhibition of NE reuptake

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12
Q

Tranylcypromine and Phenelzine

A

Inhibit MAO

Predispose patients toward hypertensive crisis

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13
Q

Entacapone

A

Inhibition of COMT metabolism of levodopa

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14
Q

Catecholamines

A
Dopamine
Isoproterenol
NE
EPI
Dobutamine

Rapidly metabolized
Not effective orally

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15
Q

Non-catecholamine

A

Phenylephrine
Ephedrine
Amphetamine

Longer duration of action than catecholamine

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16
Q

Phenylephrine

A

Selective alpha 1 receptor agonist

Vasoconstriction- increase TPR- increase BP
Reflex decrease HR

Mydriatic
Decongestant
Prolong action of local Anesthetics

17
Q

Clonidine

A

Selective alpha 2 receptor agonists

Vasodilation- decrease TPR- decrease BP
Little reflex increase HR

Hypertension
Drug addiction
ADHD

18
Q

Albuterol

A

Selective Beta 2 receptor agonists

Bronchodilation
Vasodilation- reflex increase HR

Adverse effects- cardiac stimulation at high doses

19
Q

Isoproterenol

A

Agonist at beta 1 and beta 2 receptors

Net effect: decrease TPR, decrease BP, increase HR

Bronchospasm
Cardiac arrest: +chronotrope +inotrope
Heart block

20
Q

Epinephrine

A

CV effects of low dose:
Vasodilation (beta 2 effects-decrease TPR in skeletal muscle)
Net effect: decrease TPR decrease BP increase HR

CV effects of high dose:
Vasoconstriction (alpha predominates)
Net effect: increase TPR increase BP increase HR

Anaphylaxis
Bronchospasm
Cardiac arrest
Glaucoma

Marked hyperglycemia adverse effect
Decrease insulin secretion- increase blood glucose
Increase glycogenolysis- increase blood glucose

21
Q

Norepinephrine

A

Net effect: increase TPR increase BP

Septic and cardiogenic shock

22
Q

Dobutamine

A

Used in acute CHF:
+inotrope- increase CO

Adverse effects:
Arrhythmias, increase myocardial O2 consumption, increase AV nodal conduction

23
Q

Dopamine

A

Dilation of renal, splanchnic, cerebral and coronary vessels

Causes release of NE/Epi

Treat shock and acute CHF

24
Q

Low dose DA

A

D1 receptor mediated selective vasodilation of renal and splanchnic vessels

25
Q

Moderate doses DA

A

D1 receptor mediated vasodilation- decrease TPR

Direct and reflex Beta 1 receptor cardiac effects- increase HR, increase CO

26
Q

High dose DA

A

Alpha receptor vasoconstriction- increase TPR
Beta 1 receptor cardiac effects- increase HR
Increase BP

27
Q

Pseudoephedrine

A

Effects due to direct action at Adrenergic receptors + release of NE

Decongestant

Insomnia
Hypertension

28
Q

Phenoxybenzamine

A

Non competitive block of alpha 1 and alpha 2 receptors

Vasodilation- decrease TPR
Reflex increase HR

Long lasting

Preoperative or chronic Tx pheochromocytoma with Beta blockers

29
Q

Phentolamine

A

Competitively inhibits alpha 1 and alpha 2 receptors

Short duration of action
Must be administered IV

Hypertensive crisis
Surgical removal of pheochromocytoma
Reversible vasospastic disease

30
Q

Doxazosin

A

Specific alpha 1 receptor antagonists

Arteriolar dilation- decrease TPR- decrease BP
Relaxation of bladder sphincter

Benign prostatic hypertrophy
Hypertension

“First dose syncope” precipitous decrease BP

31
Q

Tamsulosin

A

Selective alpha receptor antagonists

Relaxation of bladder sphincter

Can cause orthostatic hypotension

32
Q

Propranolol

A

Competitively inhibits Beta 1 and Beta 2

CV effects:
Decrease automaticity- decrease HR- decrease CO
Decrease contractility- decrease CO
Decrease myocardial O2 consumption
Decrease AV nodal conduction velocity
Decrease coronary blood flow

Non-CV effects:
Inhibition of glycogenolysis
Decrease intraocular pressure in glaucoma
Decrease lipolysis- decrease FFA, increase triglycerides
Decrease HDL

33
Q

Propranolol uses

A
Hypertension
Chronic stable angina
Arrhythmias
Post MI
Hyperthyroidism
Pheochromocytoma
Migraine
Idiopathic hypertrophic subaortic stenosis
Stage fright
Essential tremors
34
Q

Metoprolol

A

Beta 1 receptor antagonist

Preferred for diabetes, Raynauds syndrome, COPD

35
Q

Esmolol

A

Short acting cardioselective Beta blocker

Metabolized by red cell esterase

Used as anti-arrhythmic

36
Q

Carvedilol

A

Alpha 1, beta 1, beta 2 receptor antagonists

Decrease TPR
Increase HDL

Hypertension and CHF

37
Q

Nebivolol

A

Cardioselective Beta 1 block + NO mediated vasodilation

Decrease TPR

Hypertension