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Pharmacology > 2. Adrenergic Agonists (Sympathomimetics) > Flashcards

2. Adrenergic Agonists (Sympathomimetics) Flashcards

1
Q

What is the Rate Limiting Step in the mechanism of adrenergic agonists (synthesis of NE)?

A

Hydroxylation of tyrosine

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2
Q

How is NE stored?

A
  • Dopamine enters a vesicle and is converted to NE
  • NE is protected from degradation in the vesicle
  • Transport in the vsicle is inhibited by reserpine
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3
Q

What is the release of NE blocked by?

A
  • guanethidine
  • bretylium
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4
Q

What inhibits the reuptake of NE into the neuron?

A
  • Cocaine
  • Imipramine
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5
Q

How is NE metabolised?

A
  • NE is methylated by COMT
  • Oxidized by MAO
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6
Q

Alpha adrenoceptors response to isoproterenol?

A

Weak

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7
Q

Beta adrenoceptors response to isoproterenol?

A

Strong

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8
Q

Alpha adrenoceptors response to Epi + NE?

A

Strong

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9
Q

Beta adrenoceptors response to Epi + NE?

A

Less responsive

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10
Q

Rank order of catecholamine potency for alpha adrenoceptors?

A

Epi > NE >> isoproterenol

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11
Q

Rank order of catecholamine potency for beta adrenoceptors?

A

Isoproterenol > Epi > NE

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12
Q

What is the location of α1 adrenoceptors?

A

Mainly POST-synaptic

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13
Q

What is the location of α2 adrenoceptors?

A

Mainly PRE-synaptic

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14
Q

What is the location of β1 adrenoceptors?

A

Heart

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15
Q

What is the location of β2​ adrenoceptors?

A

Smooth Muscle

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16
Q

What is the location of β3​ adrenoceptors?

A

Adipocytes

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17
Q

What drug has a selective afinity for α1 adrenoceptors?

A

Phenylephrine

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18
Q

What drug has a selective afinity for α2 adrenoceptors?

A

Clonidine

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19
Q

What is the potency of endogenous ligands for β1​ adrenoceptors?

A

Epi = NE

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20
Q

What is the potency of endogenous ligands for β2 adrenoceptors?

A

Epi > NE

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21
Q

What is the mode of action of α1 adrenoceptors?

A

Activate phospholipase C

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22
Q

What is the mode of action of α2 adrenoceptors?

A

Inhibit adenylyl cyclase

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23
Q

What is the mode of action of all β adrenoceptors?

A

Activate adenylyl cyclase to inc cAMP

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24
Q

What is the distribution of α1 adrenoceptors?

A
  • Heart
  • Vasc. smooth muscle
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25
Q

What is the distribution of α2 adrenoceptors?

A
  • Kidneys
  • CNS
26
Q

What is the distribution of β1 adrenoceptors?

27
Q

What is the distribution of β2 adrenoceptors?

A

Smooth muscle

28
Q

What is the distribution of β3 adrenoceptors?

A

Adipocytes

29
Q

What are the effects of α1 adrenoceptors?

A
  • Vasoconstriction
  • Inc peripheral resistance
  • Inc BP
  • Mydriasis
  • Inc closure of bladder’s internal sphincter
30
Q

What are the effects of α2 adrenoceptors?

A
  • Inhib NE release
    • Tx HTN
  • Inhib ACh release
  • Inhib insulin release
31
Q

What are the effects of β1 adrenoceptors?

A
  • Tachycardia
  • Inc lipolysis
  • Inc myocardial contractility
  • Inc release of renin
32
Q

What are the effects of β2 adrenoceptors?

A
  • Vasodilation
  • Dec peripheral resistance
  • Bronchodilation
  • Inc muscle + liver glycogenolysis
  • Inc release of glucagon
  • Relaxed uterine smooth muscle
33
Q

What are the pharmacological effects of low doses of Epi?

A

Predom β-effects = vasodilation

34
Q

What are the pharmacological effects of high doses of Epi?

A

Predom α-effects = vasoconstriction

35
Q

What are the overall cardiovascular effects of Epi?

A
  • Net increase in systolic BP
  • Slight decrease in diastolic BP
36
Q

What are the cardiac effects of Epi?

A

Increased CO

37
Q

What is Epi’s effect on vascular smooth muscle?

A

Decreased renal BF

38
Q

What are the respiratory effects of Epi?

A

Bronchodilation = β2

39
Q

How does Epi cause Hyperglycemia?

A
  • Inc glycogenolysis = β2
  • Inc glucagon release = β2
  • Dec insulin release = α2
40
Q

What are the therapeutic uses of Epi?

A
  • Bronchospasms
  • Anaphylactic shock
  • Cardiac arrest
  • Local anesthetics
41
Q

What are the pharmacokinetics of Epi?

A
  • Not effective orally
  • Absorp more rapid with IM injection
  • In emergencies = IV
42
Q

What are pt contraindications for Epi?

A
  • Hyperthyroidism (inc adrenoreceptors)
  • Pts taking digoxin
  • DB pts
43
Q

What can have drug interactions with Epi?

A
  • Inhalation anesthetics
  • Cocaine
  • β - blockers
44
Q

What are the cardiovascular effects of NE?

A
  • Inc SBP and DBP
  • Inc TPR
  • CO unchanged or dec
45
Q

What are the therapeutic uses for NE?

A
  • Raises or support BP in ICU
  • Tx shock
46
Q

What is an adverse affect from NE?

A

Causes necrosis at site of injection (due to vasoconstriction)

47
Q

What does the stimulation of dopaminergic receptors cause?

A

vasodilation

48
Q

What are the cardiovascular effects of Dopamine?

A
  • Stimulate β1 - adrenoceptors
  • At very high doses stimulates α1 - adrenoceptors
49
Q

What are the Renal effects of Dopamine?

A
  • Dilates renal and splanchnic arterioles
  • Inc renal BF (opposite of Epi)
50
Q

What are the therapeutic uses for Dopamine?

A
  • Tx cardiogenic and septic shock
    • ​Raises BP via β1 stimulation
    • Vasoconstriction via α1
    • And inc renal perfusion via D1 and D2
  • Tx hypotension
  • Tx severe CHF
51
Q

Non-selective α adrenergic agonist

A

oxymetazoline

52
Q

α1 selective agonists

A

phenylephrine

53
Q

α2 selective agonists

A

Clonidine, guanabenze, guanafanecine

54
Q

Non-selective β agonists

A

isoproterenol, dobutamine

55
Q

β1 - selective agonists

A

dobutamine

56
Q

β2 - selective agonists

A

terbutaline

57
Q

What is clonidine used to tx?

58
Q

What is the therapeutic use of Dobutamine?

A

Acute cardiac insufficiency

59
Q

What are the adverse effects of Dobutamine?

A
  • Contraindicated in A-fib
    • May inc AV conductance
60
Q

What are the therapeutic uses for short acting β2 - selective agonists (albuterol)?

A
  • Bronchodilation
  • Pre-mature labor (terbutaline)
61
Q

What are the therapeutic uses for long acting β2 - selective agonists?

A

Chronic managment of asthma

(salmeterol, formoterol, carmoterol, ritodrine, indacaterol)

Pharmacology (18 decks)

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