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GIT-PHARMA > Serotonin Agonists and Antagonists > Flashcards

Serotonin Agonists and Antagonists Flashcards

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1
Q

Carcinoid syndrome is an unusual manifestation of carcinoid tumor, a neoplasm of __________ cells.

A

enterochromaffin

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2
Q

___________, an orally active hydroxylase inhibitor, has been approved for the treatment of diarrhea due to carcinoid tumor

A

Telotristat ethyl

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3
Q

__________ serves as a precursor of melatonin

A

serotonin

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4
Q

5-HT is concentrated in vesicles by a vesicle-associated transporter (VAT) that is blocked by ____________

A

reserpine

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5
Q

The 24-hour excretion of 5-HIAA can be used as a diagnostic test for ___________

A

carcinoid tumor

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6
Q

__________ must be prohibited during such

diagnostic tests

A

Bananas or food having serotonin and precursors

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7
Q

__________, a 5-HT1A agonist currently in clinical trials, appears to have some antinociceptive action at higher doses while reversing opioid-induced respiratory depression

A

Repinotan

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8
Q

_________ receptors in the gastrointestinal tract and in the vomiting center of the medulla participate in the vomiting reflex

A

5-HT3

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9
Q

Serotonin is a potent _________ (stimulant/inhibitor) of pain and itch sensory nerve endings

A

stimulant

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10
Q

What is Chemoreceptor reflex (Bezold-Jarisch reflex)?

A

Activation of 5-HT3 receptors on these afferent

vagal nerve endings leading to marked bradycardia and hypotension

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11
Q

The bradycardia in chemoreceptor reflex is mediated by vagal outflow to the heart and can be blocked by __________

A

atropine

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12
Q

A cardiac glycoside, oubain can also _________ (activate/ inhibit) the chemoreceptor reflex

A

activate

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13
Q

Administration of _______ blockers appears to reduce skeletal muscle spasm following spinal cord injury

A

5-HT2

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14
Q

Serotonin can cause bronchoconstriction when acts on ________ receptors.

A

5-HT2A receptors

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15
Q

Serotonin may also cause ___________ (hypoventilation/hyperventilation) as a result of the chemoreceptor reflex or stimulation of bronchial sensory nerve endings

A

hyperventilation

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16
Q

Serotonin can also elicit reflex bradycardia by activation of __________ receptors on chemoreceptor nerve endings

A

5-HT3

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17
Q

What is responsible for the flush that is observed after serotonin administration or release from a carcinoid tumor?

A

Serotonin constricts veins, and venoconstriction with increased capillary filling leading to the flush

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18
Q

Prolonged elevation of the blood level of serotonin (which occurs in carcinoid syndrome) is associated with ______________, which may result in valvular or electrical malfunction

A

subendocardial fibroplasia

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19
Q

Why serotonin in high levels affecting heart?

A

Serotonin has small direct positive chronotropic

and inotropic effects on the heart

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20
Q

Serotonin causes blood platelets to aggregate by activating _________ receptors

A

5-HT2

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21
Q

Increasing tone and peristalsis are caused by the direct action of serotonin on ______ smooth muscle receptors on GI tract.

A

5-HT2

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22
Q

Activation of _______ receptors in the enteric nervous system causes increased acetylcholine release and thereby mediates a motilityenhancing or “prokinetic” effect.

A

5-HT4

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23
Q

How does cisapride work?

A

Activation of 5-HT4 receptors by cisapride in the enteric nervous system causes increased Ach release and thereby mediates a prokinetic effect

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24
Q

Overproduction of serotonin in carcinoid tumor is associated with severe ________ (constipation/diarrhea)

A

diarrhea

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25
Q

_______ receptors are present on skeletal muscle membranes

A

5-HT2

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26
Q

Serotonin syndrome is associated with skeletal muscle ___________ (contractions/relaxations)

A

contractions

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27
Q

Serotonin syndrome is associated with skeletal muscle contractions which are precipitated when _________ inhibitors are given with serotonin agonists

A

MAO inhibitors

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28
Q

Hyperthermia of serotonin syndrome results from excessive muscle __________

A

contraction

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29
Q

_______, a 5-HT1A agonist is given as an anxiolytic

A

Buspirone

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30
Q

Appetite suppression appears to be associated with agonist action at _______ receptors in the central nervous system

A

5-HT2C

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31
Q

Dexfenfluramine, a selective 5-HT agonist, was widely used as an __________ but was withdrawn because of cardiac valvulopathy

A

appetite suppressant

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32
Q

____________, a 5-HT2C agonist, is approved by the FDA for use as a weight-loss medication

A

Lorcaserin

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33
Q

The 5-HT1D/1B agonists (triptans) are used almost exclusively for _______________

A

migraine headache

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34
Q

Migraine is in two forms, classic and common.

What is the difference between the two?

A

Classic Migraine: Aura followed by a severe throbbing unilateral headache that lasts for a few hours to 1–2 days.
Common migraine: Severe throbbing unilateral headache that lasts for a few hours to 1–2 days but NO AURA

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35
Q

What is aura?

A

Nausea, vomiting, visual scotomas or even hemianopsia, and speech abnormalities or any warning sensation

36
Q

Migraine involves the _________ nerve distribution to intracranial (and possibly extracranial) arteries

A

trigeminal

37
Q

Trigeminal nerve release three vasodilators that act on extra and intracranial arteries. What are the vasodilators?

A

Substance P
Neurokinin
Calcitonin gene related peptide

38
Q

What happens when arteries dilate in migraine patients?

A

Extravasation of plasma and plasma proteins into the perivascular space is found in biopsy specimens from migraine patients. This causes perivascular edema

39
Q

What causes headache in migraine patients?

A

The mechanical stretching caused by this perivascular

edema may be the immediate cause of activation of pain nerve endings in the dura

40
Q

What is the mechanism of action of triptans for treating migraine?

A
  1. Triptans activate 5-HT1D/1B receptors on presynaptic
    trigeminal nerve endings to inhibit the release of vasodilating peptides
  2. Vasoconstrictor actions of direct 5-HT agonists (the triptans and ergot) may prevent vasodilation and stretching of the pain endings
41
Q

How do antidepressants or antiseizure drugs work to stop migraine?

A

antiseizure agents may suppress excessive firing of

these trigeminal nerve endings

42
Q

Serotonin norepinephrine reuptake inhibitors (SNRIs) and selective serotonin reuptake inhibitors (SSRIs) are used to treat ____________

A

clinical depression

43
Q

What can trigger headache?

A

alcohol, chocolate, and stress

44
Q

Most commonly, aura is _______ (visual/audible)

A

visual (flashes, zigzag lines, and glare)

45
Q

Aura occur approximately 20 to 40 minutes _______ (before/after) headache pain begins

A

before

46
Q

________ (Men/Women) are threefold more likely to experience migraine.

A

Women

47
Q

The hypoperfusion persists throughout the ________ (aura and headache phase/aura phase only/headache phase only) in migraine.

A

aura and headache phase

48
Q

Patients who have migraine without aura ___ (do/do not) show hypoperfusion

A

do not

49
Q

Acute treatment for migraines can be classified as?

A

Nonspecific

Migraine specific

50
Q

What are the nonspecific treatment for migraine?

A

Analgesics (NSAIDs)
Antiemetics (prochlorperazine) to control vomiting
Opioids (when no other thing is working)

51
Q

Migraine-specific therapy includes _________ and ___________, which are 5-HT1B/1D receptor and 5-HT1D receptor agonists

A

triptans and ergot alkaloids

52
Q

Rate the severity of nausea that occurs with use of:

a. dihydroergotamine>triptans
b. dihydroergotamine

A

dihydroergotamine>triptans

More nausea w/ dihydroergotamine

53
Q

Rate the severity of vasoconstriction that occurs with use of:

a. ergotamine>triptans
b. ergotamine

A

a. ergotamine>triptans

More vasoconstriction w/ ergotamine

54
Q

sumatriptan is also available in a combination product with ____________

A

naproxen

55
Q

The onset of the parenteral drug sumatriptan is

about _____ minutes

A

20

56
Q

Headache commonly recurs within _______ hours after a single dose of sumatriptan, but in most patients, a second dose is effective in aborting the headache.

A

24 to 48 hrs

57
Q

Sumatriptan elimination half-life is of ________

A

2 hours

58
Q

__________ is the longest-acting triptan

A

Frovatriptan

59
Q

Triptans ________ (can/cannot) be administered to patients with risk factors for coronary artery disease

A

cannot

60
Q

What are the adverse effects of triptans?

A

Pain and pressure sensations in the chest, neck, throat, and jaw
Dizziness and malaise

61
Q

_________ and __________ (triptans) are contraindicated in patients with severe hepatic or renal impairment or peripheral vascular syndromes

A

Naratriptan and eletriptan

62
Q

___________ (triptan) in patients with peripheral vascular disease

A

Frovatriptan

63
Q

__________ (triptan) in patients with Wolff-Parkinson-White syndrome

A

Zolmitriptan

64
Q

Tegaserod, a 5-HT4 partial agonist, is used for ___________ with constipation

A

irritable bowel syndrome

65
Q

__________ is an example of SSRI used for depression

A

Fluoxetine

66
Q

Serotonin ________ (synthesis/metabolization) can be inhibited by p chlorophenylalanine and p-chloroamphetamine but too toxic

A

synthesis

67
Q

Why reserpine isn’t used in carcinoid tumor?

A
  1. Sympatholytic effects

2. High levels of circulating serotonin that result from release

68
Q

_____________ has a long-lasting blocking action at 5-HT2 receptors

A

Phenoxybenzamine

69
Q

_________ (histamine/ergot alkaloid) is partial agonists at serotonin receptors

A

ergot alkaloid

70
Q

_____________ is a potent H1-receptor antagonist, 5-HT1 and 5-HT2 receptors blockers but has no effect on gastric secretions like histamine has.

A

Cyproheptadine

71
Q

What is cyproheptadine used for?

A

Sedation (antimuscarinic effect)
Diarrhea and intestinal spasms (carcinoid syndrome; postgastrectomy dumping syndrome)
Smooth muscle manifestations of cold induces urticaria

72
Q

_____________also appears to reduce muscle spasms following spinal cord injury, in which constitutive activity of 5-HT2C receptors is associated with increases in Ca2+ currents leading to spasms

A

Cyproheptadine

73
Q

Ketanserin blocks _______ receptors on smooth muscle

A

5-HT2

74
Q

Ketanserin potently blocks vascular ____ adrenoceptors

A

α1

75
Q

___________ is used in the prevention of nausea and vomiting associated with surgery and cancer chemotherapy

A

Ondansetron (5-HT3 antagonist)

76
Q

Valvulopathy, which may lead to pulmonary hypertension, is linked to _________ receptors

A

5-HT2B

77
Q

_____________ is a serotonin agonist with selectivity for the 5-HT2C serotonin receptor

A

Locaserin

78
Q

What is locaserin used for?

A

Appetite suppressant

79
Q

Locaserin ______ (is/is not) recommended in severe renal impairment

A

is not

80
Q

What is the mechanism of action of Locaserin?

A

Activation of 5HT2C stimulates proopiomelanocortin (POMC) neurons, which activate melanocortin receptors, thereby causing a decrease in appetite

81
Q

If a patient does not lose at least ______ of his or her body weight after 12 weeks of use, locaserin should be discontinued

A

5%

82
Q

What are the adverse effects of locaserin?

A 
Nausea
headache
dry mouth
dizziness
constipation
lethargy
mood changes
suicidal ideation
serotonin syndrome
neuroleptic malignant syndrome
83
Q

Individuals with a history of _______ failure should use locaserin with caution

A

heart (due to valvulopathy)

84
Q

We should not use locaserin w/?

A

SSRIs
SNRIs
MAOIs

85
Q

Valvulopathy has been associated with the use of ___ receptor agonists

A

5-HT2B

86
Q

________ receptors are involved in thermoregulation, learning memory, and nociceptive processing

A

5-HT7

87
Q

_______ receptor mediates hallucinogenic effects

A

5-HT2

GIT-PHARMA (4 decks)

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