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Pharmacology 3 > Adrenergics I > Flashcards

Adrenergics I Flashcards

1
Q

Dopamine is important in the regulation of:

A

Sodium excretion and renal function

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2
Q

Chemical structure of the catechol nucleus:

A

3,4 dihydroxyl benzene ring

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3
Q

Mechanisms of Indirect agonism:

A

1) Displacement and release of stored catecholamines
2) Inhibition of catecholamine reuptake
3) Blockade of metabolic enzymes

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4
Q

Differences in between non-catecholamines and catecholamines:

A

Less efficacious
Lipid soluble, penetrate the BBB (no OH)
Well absorbed orally
Longer duration of action (resistant to COMT)

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5
Q

MAO degradation of neurotransmitters occurs in the:

A

nerve terminal cytoplasm

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6
Q

MAO resistant neurotransmitter enter the nerve via this transporter:

A

Vesicular monoamine transporter (VMAT)

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7
Q

NE in the extra-synaptic space and circulating epinephrine are metabolized by:

A

COMT (Extraneuronal uptake)

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8
Q

The principal metabolite of norepinephrine in the brain:

A

3-hydroxy-4-methoxyphenyl glycol

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9
Q

The end-stage catecholamine metabolite ___ is excreted via the ____:

A

Vanilyllmandelic acid (VMA); urine

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10
Q

Stimulation of these alpha receptors leads to vasoconstriction:

A

Post-junctional Alpha-1 and Alpha-2

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11
Q

Stimulation of these alpha receptors leads to vasodilation:

A

Pre-junctional Alpha receptors

Endothelial Alpha-2

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12
Q

Beta-2 stimulation leads to ___ of muscle due to phosphorylation of ____:

A

relaxation; myosin light chain kinase (MLCK)

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13
Q

The dopamine receptors that stimulate adenylyl cyclase:

A

D1 and D5

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14
Q

Dopamine receptors inhibition adenylyl cyclase:

A

D2 (hyperpolarization)

D3 and D4

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15
Q

The most powerful stimulant of liver glycolysis:

A

Epinephrine

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16
Q

The most powerful stimulant of muscle glycolysis:

A

Isoproterenol

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17
Q

α1 > α2&raquo_space;> β

A

Phenylephrine

Methoxamine

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18
Q

α2 > α1 &raquo_space;> β

A

clonidine and methyldopa:

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19
Q

α1 = α2; β1&raquo_space;> β2

A

Norepinephrine

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20
Q

α1 = α2; β1 = β2

A

epinephrine

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21
Q

β1 > β2&raquo_space;> α

A

Dobutamine

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22
Q

β1 = β2&raquo_space;> α

A

Isoproterenol

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23
Q

β2&raquo_space; β1&raquo_space;> α

A

terbutaline and albuterol

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24
Q

D1 = D2&raquo_space; β&raquo_space; α

A

Dopamine

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25
Q

D1&raquo_space; D2

A

Fenoldopam

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26
Q

Best choice for cardiogenic shock:

A

Dopamine

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27
Q

Tachyphylaxis desensitization is exemplified by:

A

indirectly acting sympathomimetic drugs

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28
Q

Two categories of GPCR mediated desensitization:

A

Homologous (arrestin)

Heterologous (phosphorylation)

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29
Q

The parent compound of catecholamines, ___, is composed of:

A

phenylethylamine; benzene ring + ethylamine with terminal amino group

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30
Q

Dopamine structure is a catechol nucleus + ___:

A

ethylamine

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31
Q

Norepinephrine structure is dopamine + ___:

A

OH at β-carbon

32
Q

Epinephrine structure is norepinephrine + ___:

A

methyl group at amino terminal

33
Q

Isoproterenol structure is epinephrine + ___:

A

2 methyl groups at methyl substitution

34
Q

in catecholamines, the larger the ___ substitution, the greater the affinity to __ receptors:

A

alkyl; β receptors

35
Q

Phenylephrine is epinephrine structure without the ____:

A

1 OH group on benzene ring

36
Q

Ephedrine has these differences from epinephrine structure:

A

less 2 OH groups

Methyl-substitution on the α-carbon

37
Q

Absence of this group makes non-catecholamines resistant to COMT:

A

OH groups

38
Q

Presence of this group makes non-catecholamines resistant to MAO:

A

α-carbon methyl group

39
Q

As size of amino group substituents increases:

A

Increased β receptor activity

Decreased α receptor activity

40
Q

Groups with substitution to the α-carbon block ___ metabolism and act ___:

A

MAO; indirectly

41
Q

Groups with substitution to the β-carbon act ___ and may be important in the ___:

A

Directly; storage of transmitters in neural vesicles

42
Q

Tissues with α1 receptors:

A

Most vascular smooth muscle
Pupillary dilator muscle
Pilomotor smooth muscle
Heart

43
Q

Tissues with α2 receptors:

A 
Postsynaptic CNS adrenoreceptors
Platelets
Adrenergic and cholinergic nerve terminals
Vascular smooth muscle
Fat cells
JG cells
44
Q

Tissues with β2 receptors:

A

Respiratory, uterine and vascular smooth muscle
Skeletal muscle
Human liver

45
Q

Use of pure α agonists lead to this cardiovascular reflex:

A

Reflex bradycardia

46
Q

Receptors for decreased insulin secretion:

A

α2

47
Q

Receptors for increased insulin secretion:

A

β

48
Q

These receptors stimulate renin secretion:

A

β1

49
Q

These receptors inhibit renin secretion:

A

α2

50
Q

Adrenoreceptors modulate the secretion of:

A

PTH
Calcitonin
Thyroxine
Gastrin

51
Q

In high concentrations, Epi and others cause:

A

Leukocytosis

52
Q

At high doses of epinephrine __ receptors are more sensitive, but __ receptor effects predominate, leading to a ____ response:

A

β2 (decreased DP); α (increased DP); biphasic

53
Q

Chief vascular action of epinephrine is on the components:

A

Smaller arterioles

Precapillary sphincters

54
Q

Metabolic effects of epinephrine:

A

Hyperglycemia
Hyperlipediemia
Increased calorigenic action
Hypokalemia

55
Q

___ is CI in pregnant women due to it’s lack of ___ receptor sensitivity:

A

Norepinephrine; β2

56
Q

Adverse effects associated with epinephrine:

A 
Cerebral hemorrhage (α1 BP effects)
Cardiac arrythymias (β1)
Skeletal muscle tremors (β2)
57
Q

Therapeutic uses of epinephrine:

A 
Anaphylactic shock
Prolong local anesthetics
Control of hemorrhage
Cardiac arrest
Chronic angle glaucoma
Acute bronchial asthma
58
Q

CI for epinephrine:

A

Patients on non-selective beta blockers

Patients with CAD

59
Q

Unlike epinephrine, norepinephrine is associated with reflex _____:

A

bradycardia (no β2 effects leads to tremendous BP increase)

60
Q

Locked-lung syndrome:

A

Congestion of the bronchial mucosa caused by repeated administration is isoproterenol

61
Q

Major use of dopamine:

A

Chronic refractory congestive heart failure

62
Q

Dobutamine substitutes an ___ group in place of the amino group and is a ____ receptor agonist:

A

aromatic; dopamine and β1

63
Q

The effect of dobutamine is more on ____ than on ____:

A

myocardial contraction (inotropic); heart rate (chronotropic)

64
Q

CI of dobutamine:

A

Idiopathic hypertrophic subaortic stenosis

65
Q

Therapeutic uses of phenylephrine:

A

Topical nasal decongestant
Mydriatic (increase pupillary size)
Vasopressor drug
Paroxysmal supraventricular tachycardia

66
Q

Rebound congestion is minimal if:

A

The drug is taken orally

67
Q

Ephedrine has a receptor sensitivity profile identical to ___:

A

Epinephrine

68
Q

Ephedrine has this mode of action:

A

Direct and Indirect

69
Q

Amphetamine is an ____ acting agent increasing ____ release and duration:

A

indirectly; norepinephrine

70
Q

Therapeutic uses of amphetamine:

A

ADHD
Narcolepsy
Obesity

71
Q

Terbutaline is a ___ agonist and not easily metabolized by___:

A

β2; COMT

72
Q

Clonidine is a ____ agonist associated with ____ when discontinued suddenly:

A

α2; rebound hypertension (sympathetic compensation)

73
Q

General CI when using adrenergic drugs:

A 
Hypertension
Cerebral arteriosclerosis
Hyperthyroidism
Acute coronary disease
Diabetes
BPH
Narrow angle glaucoma
74
Q

α2 selective drugs have _____ effects:

A

Sympathetic depressant

75
Q

α2 selective drugs used in wide angle glaucoma:

A

Apraclonidine

Brimonidine

Pharmacology 3 (5 decks)

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