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Block 5 > Pharm - Lecture 8 - Adrenergic agonists > Flashcards

Pharm - Lecture 8 - Adrenergic agonists Flashcards

1
Q

What drugs are Direct-acting Adrenergic agonists - Catecholamines? (6)

A

1) Norepinephrine
2) Epinephrine
3) Isoproterenol
4) Dopamine
5) Dobutamine
6) Methyldopa

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2
Q

What is the receptor selectivity for Norepinephrine?

A

a1, a2, B1

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3
Q

What are the cardiovascular effects of Norepinephrine? (3)

A

1) Peripheral vasoconstriction
- increased peripheral vascular resistence (a1)

2) Increased blood pressure (a1)
3) can cause reflex bradycardia (vagally mediated)

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4
Q

What are the therapeutc uses of Norepinephrine? (2)

A

1) used as a vasoconstrictor under certain intensive care situations (i.e. shock) (a1)
2) elevate blood pressure during reduced sympathetic tone (neurological injury or during use of spinal anesthesia) (a1)

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5
Q

What is the receptor selectivity of Epinephrine?

A

a1, a2, B1, B2

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6
Q

What are the cardiovascular effects of Epinephrine? (3)

A

1) Increased heart rate, contractile force, cardiac output (B1)
2) Increased systolic, decreased diastolic blood pressure (a1)
3) Constriction of most vascular beds but dilation of skeletal muscle blood vessels - net effect is to decrease peripheral vascular resistence (B2)

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7
Q

What are the respiratory effects of Epinephrine?

A

Bronchodilation (B2)

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8
Q

What are the metabolic effects of Epinephrine?

A

1) Hyperglycemia (stimulates gluconeogensis and glycogenolysis; inhibits insulin release) (B2)
2) Lipolysis - increase free fatty acids (B2)

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9
Q

What are the therapeutic uses of Epinephrine?

A

1) rapid relief of hypersensitivity reactions to drugs and other allergens
2) Co-administered with local anesthetics to increase duration of action (a1)
3) Bradyarrhythmias - restore rhythm in patients with cardiac arrest (B1)
4) opthalmic uses - mydriatic, decrease hemorrhage, conjunctival decongestion (a1)

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10
Q

What is the receptor selectivity for Isoproterenol?

A

B1, B2

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11
Q

What is the cardiovascular effects of Isoproterenol? (3)

A

1) Decrease peripheral resistance (B2)
2) Increase heart rate, contractile force, cardiac output (B1)
3) Decrease mean blood pressure (B2)

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12
Q

What are the respiratory effects of Isoproterenol?

A

Bronchodilation (B2)

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13
Q

What are the therapeutic uses of Isoproterenol?

A

In emergencies to stimulate heart rate during bradycardia or heart block (B1)

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14
Q

What is the receptor selectivity for Dopamine?

A

DA1, B1, a1

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15
Q

What are the cardiovascular effects of dopamine?

Low Dose?

Medium dose?

High dose?

A

Low dose: vasodilation of renal and mesenteric arteries - decreased peripheral resistance (DA1 receptor)

Medium dose: Increase heart rate, contractile force, cardiac output (B1 receptor)

High dose: vasoconstriction and increase peripheral resistance (a1)

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16
Q

What are the therapeutic uses of Dopamine?

A

severe decompensated heart failure, shock (cardiogenic; septic)

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17
Q

What is the receptor selectivity for Dobutamine?

A

racemic mixture: overall effect as B1 agonist

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18
Q

What are the cardiovascular effects of Dobutamine?

A

1) Increased cardiac rate, contractility and output (B1)
2) Minimal change in peripheral resistence and blood pressure

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19
Q

What are the therapeutic uses for Dobutamine?

A

1) short term treatment of cardiac decompensation (surgery, CHF, MI) (B1)
2) cardiac stress testing (B1)

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20
Q

How is Methyldopa metabolized in the body?

A

Methyldopa is an orally active pro-drug: it is meabolized in adrenergic nerve terminals in CNS to a-methyldopamine and a-methylnorepinephrine - these are stored in nerve terminals and released upon stimulation

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21
Q

What is the receptor specificty for a-methyldopamine and a-methylnorepinephrine?

A

1) potent a2 receptor agonist

Stimulation reduces sympathetic outflow

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22
Q

What is the therapeutic use of Methyldopa?

A

anti-hypertensive (a2)

23
Q

What are the side effects of Methyldopa? (4)

A

Sedation

dry mouth

edema

rebound hypertension with sudden discontinuation

(all a2 - CNS)

24
Q

What drugs are direct acting Adrenergic agonists that are non-catecholamines? (4)

A

1) Phenylephrine
2) Clonidine
3) Albuterol
4) Salmeterol

25
Q

What is the receptor specificty of Phenylephrine?

A

acts only on a1 adrenergic receptors

26
Q

What are the effects of Phenylephrine?

A

Increased systolic and diastolic blood pressure (a1)

Decrease Heart rate (reflex)

Decrease blood flow to most vascular beds (a1 - cause of higher resistence)

27
Q

What are the therapeutic uses of Phenylephrine? (4)

A

1) opthalmic: mydriatic, decrease hemorrhage, conjuctival decongestion (a1)
2) nasal decongestant: oral or nasal spray (a1)
3) used with local anesthetics to increase duration of action (a1)
4) treatment of hypotension (orthostatic hypotension, shock) i.v. administration (a1)

28
Q

What is the receptor specificty of Clonidine?

A

orally active a2 selectve agonist

29
Q

What is the major therapeutic use of Clonidine?

A

Anti-hypertensive (a2 - CNS)

30
Q

What does Clonidine cause?

A

1) Prolonged blood pressure lowering (a2 - CNS)
2) Decreased peripheral resistance, heart rate and cardiac output (a2 - CNS)

31
Q

What are the adverse effects of Clonidine? (3)

A

1) dry mouth and sedation (50% of patients)
2) edema
3) rebound hypertension with sudden discontinuation

(all a2 CNS issues)

32
Q

What is the receptor specificty for Salmeterol?

A

B2 adrenergic receptor agonist

33
Q

How is Salmeterol administered?

A

available only for inhalation

34
Q

What is the duration of action for Salmeterol?

A

over 12 hours

35
Q

What is the mechanism of action for indirect acting adrenergic agonists?

A

They release endogenous norepinephrine from nerve terminals

36
Q

What are the Indirect acting adrenergic agonist only drugs?

A

1) Tyramine

37
Q

What is the mechanism of Tyramine?

A

Releases norepinephrine from sympathetic nerves causing sympathomimetic actions

38
Q

Where is Tyramine found?

A

Found at high levels in certain foods (fermented foods such as wines, beer, certain cheeses and sausages)

39
Q

How is Tyramine metabolized and why is this significant?

A

Tyramine is metabolized by MAO to an inactive product. Patients taking MAO inhibitors can experience hypertensive crisis if they ingest foods with high Tyramine

40
Q

What is the mechanism for mixed acting adrenergic agonist drugs?

A

Increases norepinephrine release AND stimulates adrenergic receptors

41
Q

What are the Mixed acting adrenergic agonist drugs? (3)

A

1) Amphetamine
2) Ephedrine
3) Pseudoephedrine

42
Q

What is the effect of Amphetamine?

A

Powerful CNS stimulant

Releases NE from adrenergic neurons

Is a weak direct alpha and beta agonist itself

Depresses appetitie

43
Q

What is the therapeutic use of Amphetamine? (2)

A

1) Narcolepsy
2) attention deficit disorder

44
Q

What are the actions of Ephedrine?

A

1) Direct agonist of alpha and beta receptors
2) Releases NE that activates adrenergic receptors

45
Q

How is Ephedrine administerd?

A

orally

46
Q

What is the effect of Ephedrine?

A

CNS stimulation

47
Q

Where can ephedrine be found?

A

Some herbal suppliments contain ephedrine, leading to an inadvertant consumption of high doses. The FDA bannd the sale of supplements containing ephedra

48
Q

What is the specific receptor action of Pseudoephedrine?

A

Direct a1 agonist (little B2 activity)

49
Q

How is Pseudoephedrine administered?

A

Orally

50
Q

What is the effect of Pseudoephedrine?

A

CNS stimulation, but less than Ephedrine

51
Q

What is the therapeutic use of Ephedrine?

A

nasal decongestant (a1)

Illigally: used as a precurser to synthesize methamphetamine

52
Q

What are the side effects of adrenergic alpha receptor agonists? (3)

A

1) Throbbing headache due to potent vasoconstriction
2) Cerebral hemmorrhage - due to increase in system blood pressure
3) restlessness, anxiety

53
Q

What are the side effects of adrenergic Beta receptor agonists? (4)

A

1) Increased heart rate (palpitations)
2) Pericardial pain (angina) usually due to increased heart rate
3) Cardiac rrhythmias
4) Restlessness, anxiety

Block 5 (23 decks)

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