Autacoids (Histamine, Serotonin, Ergot) Flashcards

1
Q

histamine is synthesized form what AA?

A

Histidine

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2
Q

what enzyme converts Histidine to Histamine

A

Histidine Decarboxylase

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3
Q

Histamine in mast cell is inactive in a complex with?

A

proteases
heparan sulfate
chondroitin sulfate

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4
Q

most histamine are contained in what type of cells? (2)

A

Mast cell

Basophil

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5
Q

histamine not in cell is found in what tissues and functions as what

A

Brain, Stimach
Neurotransmitter, neuromodulator, neuroendocrine control, cardiovascular regulation.thermal & body weight regulator, sleep & arousal

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6
Q

2nd most important site of histamine storage

A

Enterochromaffin like-cells(ECL cells)

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7
Q

functions of histamine released by Enterochromaffin like-cells(ECL cells)

A

activate parietal cells to produce HCl

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8
Q

immunologic release of histamine is mediated by

A

IgE

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9
Q

what mode of release: displaces histamine from the heparin-protien complex within cells

A

Chemical & Mechanical release (drugs and alcohol)

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10
Q

the type of histamine receptor subtypes

A

G-protein coupled receptors

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11
Q

distribution of H1 receptors

A

Endothelium Brain Smooth muscle

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12
Q

what is the triple response?

A

mediated through H1 receptor:
Red spot (vessel dilation)
Edematous
Wheal and flare

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13
Q

distribution of H2 receptors

A

Gastric mucosa
Cardiac muscle
Mast cell

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14
Q

effects of H2 stimulation

A

Gastric acid sceretion
Increase SA nodal rate
(+) Inotropism

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15
Q

Presynaptic AUTORECEPTORS & heteroceptors in the brain, myenteric plexus

A

H3 receptors

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16
Q

functions of H3 receptor stimulation

A

Feedback inhibitions

Neurotransmitters

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17
Q

distribution of H4 receptors

A

Eosinophils, neutrophils, CD4 and T cells

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18
Q

function of H4 stimulation

A

Chemotactic response

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19
Q

General Histamine Antagonists (and action)

A

Epi: physiologic antagonist
Cromolyn & Nedocromil: release inhibitors
Buramide: receptor antagonist (H2)

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20
Q

types of H1 antagonists

A
1st generation (sedating)
2nd generation (less sedating)
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21
Q

converts the 2nd generation H1 antagonists to active form

A

CYP3a4 isozyme

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22
Q

H1 antagonists: Allergic reaction

A

Diphenhydramine (atopic dermatitis)

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23
Q

H1 antagonists: Motion sickness & Vestibular DO

A

Scopalamine

Dimenhydrinate

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24
Q

H1 antagonists: Nausea and Vomiting in Pregnancy

A

Bedectin

Doxylamine

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25
Q

H1 antagonists: Anti parkinsonism

A

Diphenhydramine

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26
Q

H1 antagonists: Anti cholinoceptor

A

Ethanolamine

Ethylenediamine

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27
Q

H1 antagonists: Adrenoceptor-Blocking

A

Promethazine (orthostatic Hypotension)

Cyproheptadine (anti serotonin agent)

28
Q

H1 antagonists: Local Anesthesia

A

Procaine
Lidocaine
Diphenhydramine
Promethazine

29
Q

Toxicity: Fatal Arrhythmia in 2nd gen drugs is produced when?

A

Terfenadine/Astemizole + Ketoconazole/Itroconazole/Erytromycin

30
Q

other toxicity of H1 antagonist drugs

A
Sedation, CNS depression
Anti muscarinic
Excitation
Tolerance
Seizure
Fatal Arrhythmia
31
Q

H2 receptor blocker

A

Ranitidine ( - acid secretion)

32
Q

H3 receptor antagonists

A

Tiprolisant

33
Q

Action of Tiprolisant

A

for sleep DO, Obesity, Narcolepsy, Cognitive and psychiatric DO

34
Q

other name of serotonin

A

5’-Hydroxytryptamine

35
Q

a mediator of the S/Sx of Carcinoid Syndrome

A

Serotonin

36
Q

AA precursor of Serotonin

A

Tryptophan

37
Q

what is the Rate Limiting step in the synthesis of Serotonin

A

Hydroxylation at C5

38
Q

Blocker of Rate Limiting Step in Serotonin Synthesis

A

p-chlorophenylalanine

p-chloramphetamine

39
Q

Stored serotonin can be depleted by

A

Reserpine

40
Q

distribution of serotonin

A

ECL cells
Platelets
Brainstem (raphi cells)

41
Q

Describe the serotonin receptors

A

7 receptors
6-G Protein mediated
1-Ligand gated ion channel

42
Q

a simple methoxylated and N-acetylated product of Serotonin in the Pineal Gland

A

Melatonin

43
Q

agonist at 5HT1a receptors ( a non Benzodiazepine anxiolytic)

A

Buspirone

44
Q

Agonists at 5HT1d receptors in cerebral vessels that decreases migraine pain

A

Sumatriptan (all -“triptans”)

45
Q

Action of 5HT1 and 5HT2 on CNS

A

5HT1: Inhibitory
5HT2: Excitatory

46
Q

Antagonist at 5HT2a receptors in the CNS that deceases Sx of Psychosis

A

Olanzapine

47
Q

MOA of Ketanserine

A

Blocks vascular alpha1 receptor

antagonizes platelet aggregation by serotonin

48
Q

5HT2 antagonist used in carcinoid and other GIT tumors

A

Cyproheptadine

49
Q

5HT2 antagonist that alter bleeding time and thromboxane formation

A

Ritanserine

50
Q

Distribution of 5HT3 receptors

A
CNS
Chemoreceptive area
Vomiting center
Peripheral sensory
Enteric nerves
51
Q

5HT3 antagonist that decreases emesis in chemotherapy and Post-Op’s

A

Ondansetron (“-setrons”)

52
Q

distribution of 5HT4 receptors

A

GI smooth muscles

Enteric nerves

53
Q

MOA of Cisapride

A

Activator of 5HT4 receptor
prokinetic in GERD
cardiac K channel blocker

54
Q

partial 5HT4 agonist that is used for irritable bowel syndrome and constipation

A

Tegaserod

55
Q

Serotonin reuptake inhibitor

Its is combine with what other drug to produce “Fen-Phen”

A

Dexfenfluramine added with Phentermine

56
Q

derived from fungus that grow on grain

A

Ergot Alkaloids

57
Q

common actions of ergot alkaloids

A

agonists, partial agonists, antagaonists (Alpha Adrenoceptors and Serotonin receptors and dopamine receptors)

58
Q

What are the effects of Ergot alkaloids in the following organs:
Vessels
Uterus
Brain

A

Vessels: VC
Uterus: Contraction
Brain: Hallucination

59
Q

drug used for hyperprolactinemia

A

Bromocriptine
Carbegoline
Pergolide

60
Q

for the Dx of Angina

A

Ergonovine

61
Q

for senile cerebral efficiency

A

Dihydroergonotoxine

62
Q

used for Obstetric bleeding; however, What is the preferred agent?

A

Ergonovine and Ergotamine

the preferred agent is still Oxytocin

63
Q

(ergot alkaloid) used for Migraines

A

Ergotamine

64
Q

Sever prolonged vasospasm in the GIT as a toxicity of Ergot alkaloids can be antagonized by

A

Nitroprusside

65
Q

Chronic usage of Methysergide has what side effects?

A

hyperplasia of connective tissue

66
Q
To what receptors do the following drugs have high affinities:
Bromocriptine
Ergonovine
Ergotamine
Lysergic Acid Diethylamine
Methysergide
A
Bromocriptine: Dopamine receptors
Ergonovine: Alpha adreno & 5HT2
Ergotamine: Uterine Muscle
Lysergic Acid Diethylamine: Dopamine receptors
Methysergide: none