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CPR PHARM > Adrenergics > Flashcards

Adrenergics Flashcards

1
Q

What drugs are direct acting adrenomimetics- alpha agonists?

A

Phenylephrine (Neo-synephrine) and Clonidine (Catapres)

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2
Q

What drugs are direct acting adrenomimetics- mixed alpha and beta agonists?

A

Norepinephrine (Levophed) and Epinephrine (Adrenalin)

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3
Q

What drugs are direct acting adrenomimetics- beta agonists?

A

Dobutamine (Dobutrex), Isoproterenol (Isuprel), and Albuterol (Ventolin)

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4
Q

What drugs are direct acting adrenomimetics- Dopamine agonists?

A

Dopamine (intropin)

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5
Q

What drugs are indirect acting adrenomimetics- inhibiting the re-uptake of DA and NE?

A

Cocaine

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6
Q

What drugs are indirect acting adrenomimetics- inhibitors of MAO?

A

Selegiline (Eldepryl) and Phenelzine (Nardil)

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7
Q

What drugs are indirect acting adrenomimetics- reverse NE and DA uptake mechanisms and increase their release?

A

Amphetamines, Methylphenidate (Ritalin), Tyramine (byproduct, not a drug)

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8
Q

What drugs are indirect acting adrenomimetics- releasing agent AND a direct adrenergic receptor agonist?

A

Ephedrine

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9
Q

What drugs are direct acting antiadrenergic- alpha adrenoreceptor antagonists (NONSELECTIVE)?

A

Phentolamine (OraVerse) and Phenoxybenzamine (Dibenzyline)

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10
Q

What drugs are direct acting antiadrenergic- alpha adrenoceptor antagonists (A1 RECEPTOR SELECTIVE)?

A

Prazosin (Minipress), Tamsulosin (Flomax), and Doxazosin (Cardura)

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11
Q

What drugs are direct acting antiadrenergic- mixed blockers?

A

Labetalol (Trandate) and Carvedilol (Coreg)

Both are Beta and a1 antagonists

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12
Q

What drugs are direct acting antiadrenergic- Beta adrenoceptor blockers (B1 AND B2)?

A

Propranolol (Inderal), Pindolol (Visken), and Nadolol (Corgard)

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13
Q

What drugs are direct acting antiadrenergic- Beta adrenoceptor blockers (B1 SELECTIVE)?

A

Metoprolol (Toprol), Betaxolol (kerlone), Acebutolol (Sectral), and Atenolol (Tenormin)

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14
Q

What drugs are indirect acting antiadrenergic - NE release inhibitor?

A

Guanethidine (Ismelin)

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15
Q

What drugs are indirect acting antiadrenergic- inhibitor of tyrosine hydroxylase?

A

Metyrosine (Demser)

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16
Q

What receptor types are Gq?

A

Alpha 1

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17
Q

What receptor types are Gi?

A

Alpha 2

Also D2, D3, D4

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18
Q

What receptor types are Gs?

A

B1, B2, and B3

Also, D1 and D5

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19
Q

Where are alpha 1 receptors most prevalent?

A

Most vascular smooth muscle, pupillary dilator m., prostate, heart

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20
Q

What actions do alpha 1 receptors induce?

A

Contraction in vascular smooth muscle, dilates the pupil, contracts the prostate, and increases FORCE of contraction in heart (inotropy)

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21
Q

Where are alpha 2 receptors most prevalent?

A

Postsynaptic CNS neurons, platelets, adrenergic and cholinergic nerve terminals, some vascular smooth muscle, and fat cells

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22
Q

What action do alpha 2 receptors induce?

A

Platelet aggregation, inhibits transmitter release in adrenergic and cholinergic nerve terminals, contracts vascular smooth muscle, and inhibits lipolysis

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23
Q

What tissues are beta 1 receptors most prevalent?

A

The heart and juxtaglomerular cells

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24
Q

What actions do beta 1 receptors induce?

A

Increases FORCE and RATE of contraction (inotropic and chronotropic) in the heart and increases renin release

25
Q

What tissues are Beta 2 receptors most prevalent?

A

Respiratory, uterine, and vascular smooth muscle; skeletal muscle; human liver

26
Q

What actions do beta 2 receptors induce?

A

Promotes smooth muscle relaxation in the lungs, uterus, and vascular smooth muscle; promotes potassium uptake in skeletal muscle; activates glycogenolysis and gluconeogenesis in the liver

27
Q

What tissues are beta 3 receptors most prevalent?

A

Bladder and fat cells

28
Q

What action do beta 3 receptors induce?

A

Relaxes the detrusor muscle and activates lipolysis

29
Q

Where are D1 receptors and what do they do?

A

Present in smooth muscle and lead to dilation of renal blood vessels

30
Q

Where are D2 receptors and what do they do?

A

Nerve endings and they modulate transmitter release

31
Q

What adrenergic receptor affinity does phenylephrine have?

A

A1> a2&raquo_space;» B

32
Q

What adrenergic receptor affinity does Clonidine have?

A

A2 > a1&raquo_space;» B

33
Q

What adrenergic receptor affinity does NE have?

A

A1 = A2; B1&raquo_space; B2

34
Q

What adrenergic receptor affinity does Epi have?

A

A1= A2; B1 = B2

35
Q

What adrenergic receptor affinity does Dobutamine have?

A

B1 > B2&raquo_space;» A

36
Q

What adrenergic receptor affinity does Isoproterenol have?

A

B1 = B2&raquo_space;» a

37
Q

What adrenergic receptor affinity does Albuterol have?

A

B2&raquo_space; B1&raquo_space;» a

38
Q

What adrenergic receptor affinity does Dopamine have?

A

D1 = D2&raquo_space; B&raquo_space; a

39
Q

What effect does epinephrine have on cardiac function? What receptor is it mainly affecting?

A

Increases the force of contraction, heart rate, and conduction velocity at AV node

B1 receptor

40
Q

What effect does Epi have on vascular tone? What receptors is it affecting?

A

Increases sBP, may decrease dBP and total peripheral vascular resistance, MAP unchanged

B2 and a1

41
Q

What effect does epi have on the respiratory system and what receptors does it affect?

A

Relaxes bronchial muscle and decreases secretion (B2)

congestion within bronchial mucosa (a1)

42
Q

What are the effects of NE?

A

Potent cardiac stimulant but reduces HR

Vasoconstriction

NO BRONCHODILATION AND VASODILATION

Increases peripheral vascular resistance and blood pressure

43
Q

What effect does phenylephrine have?

A

Effective mydriatic and decongestant

Vasconstriction

BP elevation

Severe bradycardia

44
Q

What effect does clonidine have?

A

Central effect on a2 receptors in lower brain stem

Decreasing sympathetic outflow

Reduction in BP

Bradycardia

45
Q

What effect does Isoproterenol have?

A

Positive inotropic and chronotropic action, so increases Cardiac output (B1)

Vasodilation and decreases arterial pressure (B2)

Bronchodilation (B2)

46
Q

What effect does Dobutamine have?

A

Potent inotropic action

Selective B1 agonist

Note: the negative isomer is an agonist for a1 but the positive isomer is an antagonist

47
Q

What effect does albuterol have?

A

Selective B2 agonist

Bronchodilation

Relaxation of uterus

48
Q

What effect does dopamine have?

A

Vasodilation

But activates B1 in heart at higher doses

At even HIGHER doses, stimulates vascular a1 to cause vasoconstriction

49
Q

What is the MOA and selectivity of Ephedrine?

A

Releases stored catecholamines

Nonselective

50
Q

What is the clinical use for ephedrine?

A

Nasal decongestant, increases BP, stress incontinence in women

51
Q

What is the MOA of Phenelzine, selegiline?

A

They inhibit MAO so they increase NE stores in the CNS

Antidepressants

52
Q

What does tyramine do?

A

Product of tyrosine metabolism and releases stored NE from presynaptic adrenergic terminals

53
Q

What are cardiovascular adverse side effects of adrenergic agonists?

A

Elevation in BP, increased cardiac work, sinus tach

54
Q

What are some adverse effects in the CNS of adrenergic agonists?

A

Insomnia, lack of appetite, anxiety/restlessness, psychoses, convulsions and hemorrhagic stroke (cocaine)

55
Q

What are adverse effects of ALPHA antagonists?

A

Postural hypotension, tachycardia, retention of fluid and salt, impaired ejaculation, nasal stuffiness

56
Q

Which beta blockers are antagonists?

A

Atenolol, nadolol, propranolol, betaxolol

57
Q

What beta blockers are partial agonists?

A

Acebutolol, labetalol, pindolol

58
Q

What beta blockers are inverse agonists?

A

Carvedilol and metoprolol

59
Q

What are some adverse effects of beta blockers?

A

Depression; sedation; increased airway resistance; decreased HR, contractility, excitability; hypoglycemic episodes

CPR PHARM (1 decks)

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