PHARM Chapter 10 - Adrenergic Pharmacology Flashcards

1
Q

ME of Alpha-Methyltyrosine

A

Inhibit tyrosine hydroxylase, the rate-limiting enzyme in the catecholamine biosynthesis pathway

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2
Q

Uses of Alpha Methyltyrosine

A

Pheochromocytoma-associated hypertension

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3
Q

Structural analogue of tyrosine

A

Alpha-Methyltyrosine

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4
Q

Pheochromocytoma

A

Tumor of the enterochromaffin cells of the adrenal medulla that produces norepinephrine and epinephrine

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5
Q

Inhibitors of Catecholamine Storage

A

Reserpine, Guanethidine, Guanadrel, Amphetamine, Methylphenidate, Pseudoephedrine

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6
Q

ME of Reserpine, Guanethidine, Guanadrel, Amphetamine, Methylphenidate, Pseudoephedrine

A

Inhibitors of catecholamine storage in vesicles - results in short-term increase in release of catecholamines from the synaptic terminal but long term depletion of available pool of catecholamines

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7
Q

Uses of Reserpine

A

Hypertension

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8
Q

Uses of Guanethidine and Guanadrel

A

Hypertension

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9
Q

Uses of Amphetamine and Methylphenidate

A

ADHD

Narcolepsy (Amphetamine)

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10
Q

Uses of Pseudoephedrine

A

Allergic rhinitis

Nasal Congestion

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11
Q

Irreversibly inhibits VMAT - results in vesicles that lose the ability to concentrate and store norepinephrine and dopamine

A

Reserpine

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12
Q

Used experimentally to assess whether effect of drug requires its concentration in presynaptic terminals

A

Reserpine

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13
Q

Low vs. High Dose of Reserpine

A

Low: causes neurotransmitter leak into cytoplasm where catecholamine is destroyed by MAO

High: rate of transmitter leak can be sufficiently high to overwhelm MAP in presynaptic neuron - has transient sympathetic effect

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14
Q

Why is Reserpine not used therapeutically?

A

Associated w/ severe depression

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15
Q

Concentrates in transmitter vesicles and displaces norepinephrine, leading to gradual depletion of norepinephrine

A

Guanethidine and guanadrel

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16
Q

Effect of Guanethidine and Guanadrel on Cardiac sympathetic nerves

A

Reduced cardiac output

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17
Q

Effect of Guanethidine and Guanadrel on sympathetic nerves

A

Leads to symptomatic hypotension following exercise

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18
Q

How does Guanethidine enter neurons

A

Actively transported by NET, concentrates in vesicles and displaces norepinephrine

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19
Q

1) Displace endogenous catecholamines from storage vesicle
2) weakly inhibit MAO
3) block catecholamine reuptake mediated by NET and DAT

A

Amphetamine and Methylpenidate

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20
Q

Carries risk of dependence and tolerance

A

Amphetamine and Methylpenidate

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21
Q

Binds to postsynaptic adrenergic receptors, but has little agonist action at alpha or beta adrenoceptors

A

Amphetamine

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22
Q

Used as OTC decongestant

A

Pseudoephedrine

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23
Q

Ephedrine used for the treatment of

A

persistent hypotension

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24
Q

Herbal source of ephedrine

A

ma huang

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25
Q

Dietary amine that is ordinarily metabolized by MAO in GI tract and liver

A

Tyramine

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26
Q

Fermented foods such as red wine and aged cheese possess high concentrations of

A

Tyramine

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27
Q

In patients taking MAOIs tyramine is absorbed in gut, transported in blood, and taking up sympathetic neurons where it is transported into synaptic vesicles by ____ to cause _____

A

VMAT

acute displacement of vesicular norepinephrine and massive non-veiscular release of norepinephrine from the nerve terminal via reversal of NET

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28
Q

Tyramine is hydroxylated into a metabolite, ____ which is better able to _____

A

octopamine

Be stored at high concentrations in the vesicles

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29
Q

ME of Cocaine

A

Inhibits voltage-gated sodium channels in excitable cell membranes

Inhibits norepinephrine transport (NET)-mediated reuptake of catecholamines - potentiates catecholamine action

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30
Q

Uses of Cocaine

A

Mucosal and opthalmic local anesthetic, diagnosis of Horner’s syndrome pupil

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31
Q

Major side effect of Cocaine

A

Cariotoxicity and euphoria

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32
Q

ME of Amitriptyline and Imipramine

A

Inhibit reuptake of 5-Ht and NE from the synaptic cleft by blocking reuptake transporters, causes enhancement of postsynaptic responses

Inhibit norepinephrine transporter (NET)-mediated reuptake of catecholamines, potentiating catecholamine action

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33
Q

Uses of Amitriptyline and Imipramine

A

Depression, Pain syndromes, nocturnal enuresis (imipramine)

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34
Q

Tricyclic antidepressants that affect cardiac sodium channels in a quinidine-like manner, leading to potentially lethal conduction delays

A

Amitriptyline and Imipramine

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35
Q

Can precipitate mania in patients w/ bipolar disorder

A

Amitriptyline and imipramine

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36
Q

Monoamine Oxidase (MAO) Inhibitors

A
Phenelzine
Iproniazid
Tranylcypromine
Clorgyline
Brofaromine
Befloxatone
Moclobemide
Selegiline
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37
Q
ME of Phenelzine
Iproniazid
Tranylcypromine
Clorgyline
Brofaromine
Befloxatone
Moclobemide
Selegiline
A

Inhibit MAO - increases catecholamine levels by blocking catecholamine degradation

Block deamination of monoamines by inhibiting the functional flavin moiety of MAO; increase the 5-HT and NE available in the cytoplasm of presynaptic neurons, which leads to increased uptake and storage of 5-HT and NE in synaptic vesicles and to some constitutive leakage of monoamines into the synaptic cleft

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38
Q
Uses of Phenelzine
Iproniazid
Tranylcypromine
Clorgyline
Brofaromine
Befloxatone
Moclobemide
Selegiline
A

Depression

39
Q

A1 adrenergic agonists

A

Methoxamine
Phenylephrine
oxymetazoline
tetrahydrozoline

40
Q

ME of A1 adrenergic agonists

A

selectively activate A1 adrenergic recpetors to increase peripheral vascular resistance

41
Q

Uses of methoxamine

A

hypotension and shock

42
Q

Uses of Phenylephrine, oxymetazoline, tetrahydrozoline

A

Opthalmic hyperemia
nasal congestion
hypotension (phenylephrine only)

43
Q

Which A1 adrenergic agonist has very limited clinical use in treatment of shock

A

methoxamine

44
Q

Contraindication of A1 adrenergic agonists

A

severe hypertension and narrow angle glaucoma (not methoxamine)

45
Q

SE of phenylephrine, oxymetazoline, tetrahydrozoline

A

cardiac arrythmia, hypertension

46
Q

Afrin and Visine are what type of drugs and what do they treat

A

A1 adrenergic agonists - nasal congestion and opthalmic hyperemia

47
Q

What is used intravenously in treatment of shock

A

phenylephrine

48
Q

alpha-adrenergic antagonists

A
penoxybenzamine
phentolamine
prazosin
terazosin
doxazosin
tamsulosin
yohimbine
49
Q

ME of alpha adrenergic antagnoists

A

block endogenous catecholamines from binding to A1 and A1 adrenoceptors - causing vasodilation, decreased blood pressure and decreased peripheral resistance

50
Q

Uses of penoxybenzamine and phentolamine

A

pheochromocytoma associated hypertension and sweating

51
Q

Blocks A1 and A2 receptors irreversibly

A

phenoxybenzamine

52
Q

reversible, nonselective alpha-adrenoceptor antagnoist

A

phentolamine

53
Q

SE of phentolamine

A

coronary artery disease

54
Q

Uses of prazosin, terazosin, doxazosin

A

hypertension, benign prostatic hyperplasia

55
Q

nonsubtype-selective antagonists of A1 receptors in arterioles and veins

A

prazosin, terazosin, doxazosin

56
Q

why do patients have to remain supine w/ first dose of prazosin, terazosin, doxazosin

A

severe postural hpotension

57
Q

SE of prazosin, terazosin, doxazosin

A

pancreatitis, hepatotoxicit, systemic lupus eruthematosus

58
Q

uses of tamsulosin

A

benign prostatic hyperplasia

59
Q

why is tamsulosin different?

A

subtpe-selective A1a receptor antagonist that has more specificity towards smooth muscle in GU tract - lower incidence of orthostatic hypotension

60
Q

uses of yohimbine

A

organic and psychogenic impotence

61
Q

SE of yohimbine

A

bronchospasm, nervousness, tremor, anxiety, agitationq

62
Q

A2-selective antagonist that leads to increased release of norepinephrine, stimulates cardiac B1-receptors and peripheral vascular A1 receptors

A

yohimbine

63
Q

What does yohimbine inadvertently release

A

increased insulin due to blockade of A2 receptors in pancreatic islets

64
Q

Suffix for B-adrenergic antagonists

A

olol

65
Q

ME of B-adrenergic antagonists

A

block B-adrenergic receptors

66
Q

block B1 and B2 receptors equally

A

propranolol, nadolol, timolol

67
Q

Ocular formation used in the treatment of glucagoma

A

timolol, levobunolol, carteolol

68
Q

Uses of propranolol, nadolol, timolol, prenbutolol, levobunolol, careolol

A

hypertension, angina, heart failure, phenocrhromocytoma

69
Q

SE of propranolol, nadolol, timolol, prenbutolol, levobunolol, careolol

A

bronchospasm AV block, bradyarrythmia

70
Q

Uses of labetalol, carvedilol, pindolol, acebutolol

A

hypertension, angina

71
Q

what additional sideeffect does labetalol have

A

hepatotoxicity

72
Q

block A1, B1, and B2 receptors

A

labetalol and carvedilol

73
Q

partial agonist at B1 and B2 receptors, preferred in hypertensive patients who have bradycardia or decreased cardiac reeserve

A

pindolol

74
Q

partial agonist at B1 adrenoceptors, no effect on B2 receptors

A

acebutolol

75
Q

Uses for esmolol, metoprolol, atenolol, betaxolol, nebivolol

A

hypertension, angina, heart failure, thyroid storm (esmolol)

76
Q

B1 selective adrenergic antagonists

A

esmolol, metoprolol, atenolol

77
Q

extremely short half life (3-4) used for emergency B-blockade

A

esmolol

78
Q

has ancillary property of promoting vasodilation via NO release from endothelial cells

A

nebivolol

79
Q

MAOI approved for treatment of Parkinsons

A

selegiline

80
Q

concomitant use of MAOIs and SSRIs contraindicated because

A

it can cause serotonin syndrome

81
Q

A2 receptor agonist that lowers blood pressure by acting in brainstem vasomotor centers to suppress sympathetic flow

A

clonidine

82
Q

A2 receptor that can cause sedation and respiratory depression

A

dexmedetomidine

83
Q

endogenous enzymes catalyze its metabolism which is then released by adrenergic nerve terinal which it acts presynaptically as A2 antagonist

A

a-Methyldopa

84
Q

antihypertensive drug in pregnancy

A

a-methyldopa

85
Q

diastolic bp is a __ effect, whereas systolic bp is a __ effect

A

B2, B1

86
Q

used intravenously for heart failure and as diagnostic agent in ischemic heart disease

A

dobutamine

87
Q

ME of dobutamine and isoproterenol

A

increase cAMP by activating G protein coupled adrenergic recpetors, acting at cardiac B1 adrenergic receptors to have positive inotropic, chronotropic, and lusitropic effects

88
Q

uses of dobutamine

A

short term treatment of cardiac decompensation secondary to depressed contractility (cardiogenic shock)

89
Q

overall effect of dobutamine is predominantly on __ and modestly on ___

A

B1 and B2

90
Q

uses for isoproterenol

A

emergency treatment of arrythmias, atropine-resistant hemodynamically significant bradycardia, heart block and shock, bronhospasm

91
Q

ME of metaproterenol, terbutaline, albuterol/salbutamol

A

agonists at B-adrenergic receptors on airway smooth muscle, act through stimulatory G protein to cause relaxation and bronchodilation

92
Q

Uses of metaproterenol, terbutaline, albuterol/salbutamol

A

asthma/copd

93
Q

Selective agonists at B2 receptors

A

metaproterneol, terbutaline, albuterol/salbutamol