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Pharm > Histamine, Serotonin, and the Ergot Alkaloids > Flashcards

Histamine, Serotonin, and the Ergot Alkaloids Flashcards

1
Q

hormone or chemical produced by the body that acts locally to exert a biological effect

A

autoacoid

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2
Q

important mediator of immediate allergic and inflammatory reactions

A

histamine

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3
Q

modest role in anaphylaxis

A

histamine

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4
Q

formed by decarboxylation

A

histamine

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5
Q

either stored in granules or rapidly inactivated by 2 enzymes

  1. monoamine oxidase
  2. diamine oxidase
A

histamine

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6
Q

stored in mast cells (tissues), basophils (blood), enterochromaffin cells of the gut, and some neurons

A

histamine

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7
Q

which is an autoacoid?

A

histamine

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8
Q

precursor of histamine

A

histidine

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9
Q

2 enzymes that breaks histamine down?

A

monoamine oxidase and diamine oxidase

amine is in them- from histAMINE

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10
Q

histamine release is by :

A

Immune
Chemical
Mechanical

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11
Q

Most important pathohysiological mechanism of histamine release from __ and __ cells

A

mast cells and basophils

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12
Q

Sensitization of mast cells and basophils with __ causes rapid DEGRANULATION

A

IgE

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13
Q

degranulation of mast cells and basophils are dependent on what ___

A

Calcium and Energy Dependent

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14
Q

the immune release of histamine can exert a negative feedback through __ receptors

A

H2

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15
Q

what chemicals can cause histamine release?

A

morphine and tubocurarine

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16
Q

t/f chemical release of histamine is not dependent on energy or mast cell granulation

A

true

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17
Q

mast cell injury can cause degranulation and release is an example of what type of histamine release?

A

mechanical

cell wall is being destroyed so the cell’s goodies are being released

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18
Q

how many receptor subtypes of histamine are there? how many do we care about?

A

4, 2

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19
Q

Histamine subtypes receptor that mediates allergic rhinitis

A

H1

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20
Q

Histamine subtype receptor that mediates stomach acid production

A

H2

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21
Q

Gq coupled receptor that increases IP3 and DAG formation, histamine

A

H1

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22
Q

Gs coupled receptor that increased cAMP and PKA activity, histamine

A

H2

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23
Q

Gi coupled receptor, decrease in cAMP

A

H3 and H4

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24
Q

Histamine subtype that is in the SM, endothelium and brain

A

H1

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25
Q

Histamine subtype that is in the Gastric mucosa, cardiac muscle, mast cells and brain

A

H2

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26
Q

stimulation of sensory nerve endings, causes pain and itching via ___ stimulation - nervous system effects

A

H1

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27
Q

histamine will cause tachycardia with decrease of blood pressure, this is caused by __

A

vasodilation via H1 receptors

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28
Q

vasodilation of H1 receptors is caused by __ production of NO in the endothelium

A

increased

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29
Q

what causes separation of endothelial cells in the microcirculation? permits fluids and small proteins to escape to the perivascular space, this is responsible for hives and the hallmark of histamine release in the skin

A

edema

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30
Q

t/f asthmatics are more sensitive to histamine than nonasthmatics.

A

true - this is how you can test for asthma!

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31
Q

histamine has what kind of effect on the GI SM?

A

contraction - LARGE doses may cause DIARRHEAAAAAA

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32
Q

t/f histamine may induce contractions during anaphylaxis and cause abortion

A

t, so sad

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33
Q

histamine stimulates gastric acid secretion via __ receptors

A

H2

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34
Q

what is characteristics red spot, edema, and flare responses to intradermal histamine administration?

A

triple response

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35
Q

CNS effect of histamine?

A

nociception

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36
Q

smooth muscle actions opposite to histamine, used to counteract the effects of histamine during anaphylaxis

A

epinephrine

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37
Q

also known as mast cell stabilizers

A

release inhibitiors of histamine antagonism

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38
Q

prevent the degranulation of mast cells

A

release inhibitiors of histamine antagonism

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39
Q

used in the treatment of asthma

A

release inhibitiors of histamine antagonism

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40
Q

cromolyn and nedocromil are in what section?

A

release inhibitiors of histamine antagonism

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41
Q

antagonists for __ and __ are readily available (OTC) and are of the great therapeutic benefit

A

H1 and H2

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42
Q

Antagonists of __ and __ are not available for clinical use and are POINTLESSSSS

A

H3 and H4

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43
Q

What do you have to take for days before you see a response, dont work acutely?

A

Cromolyn and Nedodromil

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44
Q

what group of histamine antagonists are in generations?

A

H1 and First & Second generation

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45
Q

__ generation is generally less selective for H1 Receptors and is associated with the majority of the side effects

A

first generation

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46
Q

more selective for H1 receptors and dont cross the BBB

A

second generation

47
Q

prevent motion sickness but dont treat preexisting motion sickness is a side effect of what class of drugs?

A

first generation of h1 antagonists

48
Q

h1 antagonists - antiparkinsonism effect drug, suppress extrapyramidal symptoms of antipsychotics

A

diphenhydramine

49
Q

sedation, urinary retention, dry mouth and blurred vision are effects of what class of drugs

A

first generation of h1 antagonists

50
Q

may cause orthostatic hypotension - what side effect of first generation of h1 antagonists

A

antiadrenegic effects

51
Q

used to treat serotonin storm

A

cyproheptadine

52
Q

Name the side effects of h1 antagonists first generation

A 
Sedation
Antiemetic effects
Antiparkinsonism effects
Anticholinogic effects
Antiadrenergic effects
Antiserotonergic effects
Local anesthesia
53
Q

anticholingeric activity and marked sedation is a characteristics of what generation of h1 antagonists

A

first generation h1 antagonists

54
Q

clinical uses of antihistamines

A

allergic reactions
motion sickness
nausea and vomiting associated with pregnancy
gastric acid secretion

55
Q

some second generation drugs are metabolized by ___

56
Q

“jack of all trades” neurotransmitter, gut hormone, platelet activator and migraine mediator

57
Q

synthesized from L-tryptophan

58
Q

metabolized by monoamine oxidase then aldehyde dehrydogenase to 5-hydroxyindoleacetic acid

59
Q

24 hour urinary 5-HIAA levels can be used to assess ___ production

60
Q

brain __ neurons involved in: mood, sleep, appetite, thermoregulation, perception of pain, blood pressure, vomiting, depression, anxiety and migraine

61
Q

precursor of melatonin

62
Q

produced in pineal gland and promotes sleep

63
Q

5-ht3 receptors present in medullary center governing __

64
Q

__ receptors in afferent vagal nerve endings associated with chemoreceptors reflex

65
Q

powerful activator of sensory nerve endings involved in pain and itch of stings

66
Q

small bronchoconstrictive effect, may cause hyperventilation

A

respiratory effect of serotonin

67
Q

vasconstrictor in vascular smooth muscle with intact endothelium, vasodilator in skeletal muscle and heart, can elicit bradycardia due to chemoreceptor reflex

A

cardiovascular effect of serotonin

68
Q

triphasic blood pressure response upon ___ of serotonin

A

injection

he emphasized this route

69
Q

decreased HR, CO, BP dur to chemoreceptors
Increased in BP due to vasoconstriction
Decrease in BP due to vasodilation

A

triphasic blood pressure response after injection of serotonin

70
Q

serotonin promotes platelet aggregation via __

71
Q

powerful stimulant of GI smooth muscle that promotes peristalsis

A

GI tract effect of serotonin

72
Q

typically results from the combination of MAOI inhibitors and serotonin antagonists or SSRI’s, ranges mild to severe

A

serotonin syndrome

73
Q

Presents as hyperthermia, hyperreflexia, tremor, clonus, hyperactive bowels, diarrhea, mydriasis, agitation and possible coma

A

serotonin syndrome

74
Q

Treatment of serotonin syndrome

A

cyproheptadine

75
Q

5HT1 antagonists first generation but also blocks 5HT2 Receptors

A

cyproheptadine

76
Q

5HT1A agonist, nonbenzodiazepine anxiolytic

77
Q

d-enantiomer of fenfluramine, a component of Fen-Phen

A

DEXFENFLURAMINE

78
Q

Appetite suppressant that was withdrawn from market

A

DEXFENFLURAMINE

79
Q

prototype of triptans

A

sumatriptin

80
Q

5HT1D/1B agonists

81
Q

used from acute migraine treatment and cluster headaches

82
Q

5HT2C agonist, appetite suppressant

A

LORCASERIN (BELVIQ)

83
Q

5HT4 agonist, treatment of GERD, restricted use due to toxicity

84
Q

5HT4 partial agonist, irritable bowel syndrome

85
Q

SM manifestations of carcinoid tumor and cold induced urticaria

A

CYPROHEPTADINE

86
Q

significant alpha 1 adrenoceptor blockage = hypotension

A

KETANSERIN

87
Q

no alpha adrenoceptor activity, antiplatelet activation

A

RITANSERIN

88
Q

5HT2 antagonists

89
Q

5HT3 antagonists

90
Q

prototype of setrons - 5-HT 3 antagonists

A

ondansetron

91
Q

prevents nausea and vomiting associated with chemotherapy

A

ondansetron

92
Q

compounds found commonly in nature, fungi

A

ergot alkaloids

93
Q

have been ingested for thousands of years, epidemics of ergotism or ergot poisoning

A

ergot alkaloids

94
Q

St. Anthony’s fire

95
Q

Symptoms include dementia with vivid hallucinations, prolonged vasospasm that could cause gangrene, uterine contraction that can result in abortion, nausea, vomiting, diarrhea

96
Q

classic example of ergot poisoning

97
Q

behavioral effects via pre and post synaptic 5-ht2 agonism

A

cns effect of ergots

98
Q

extrapyramidal motor control, agonism at ___ receptor for ergot effects

99
Q

regulation of pituitary prolactin release via pituitary dopamine receptor agonism, effective treatment for ___

A

prolactinemia

100
Q

agonist and partial agonist effects at ___ receptors, can cause epinephrine reversal

A

alpha adrenoceptors

101
Q

severe and prolonged vasospasm upon OD

A

vascular smooth muscle effects of ergots

102
Q

used to induce labor by working on uterine smooth muscle

103
Q

causes nausea, vomiting, diarrhea at even low doses

A

ergot effect on GI tract

104
Q

systemic effects of ergots

A

CNS
Vascular SM
Uterine SM
GI tract

105
Q

clinical uses of ergots

A

Migraine
Hyperprolactinemia
Postpartum hemorrhage

106
Q

contraction is unlike natural labor, never give before delivery

A

postpartum hemorrhage use of ergots

107
Q

second line to oxytocin to control postpartum bleeding

A

ERGONOVINE

108
Q

usually effective in 1-5 minutes, usually given during placental delivery or immediately afterward if bleeding is significant

A

ergonovine

109
Q

reduces high serum prolactin levels associated with pituitary tumor

A

BROMOCRIPTINE

110
Q

similar to bromocriptine but more potent

A

CABERGOLINE

111
Q

favored by some clinicans over ergotamine

A

DIHYDROERGOTAMINE

112
Q

most clinicans prefer the triptans but ergotamine can be effective when given during the ___ of the attack of a mirgraine

113
Q

often combined with caffeine to speed its absorption

A

ergotamine

114
Q

vasoconstriction can be prolonged and cumulative, no more than 6mg/attack and 10 mg/week

A

ergotamine

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