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PHARMACOLOGY 1.0 > Autacoids (Histamine, Serotonin, Ergot) > Flashcards

Autacoids (Histamine, Serotonin, Ergot) Flashcards

(66 cards)

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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
H1 antagonists: Anti parkinsonism
Diphenhydramine
26
H1 antagonists: Anti cholinoceptor
Ethanolamine | Ethylenediamine
27
H1 antagonists: Adrenoceptor-Blocking
Promethazine (orthostatic Hypotension) | Cyproheptadine (anti serotonin agent)
28
H1 antagonists: Local Anesthesia
Procaine Lidocaine Diphenhydramine Promethazine
29
Toxicity: Fatal Arrhythmia in 2nd gen drugs is produced when?
Terfenadine/Astemizole + Ketoconazole/Itroconazole/Erytromycin
30
other toxicity of H1 antagonist drugs
``` Sedation, CNS depression Anti muscarinic Excitation Tolerance Seizure Fatal Arrhythmia ```
31
H2 receptor blocker
Ranitidine ( - acid secretion)
32
H3 receptor antagonists
Tiprolisant
33
Action of Tiprolisant
for sleep DO, Obesity, Narcolepsy, Cognitive and psychiatric DO
34
other name of serotonin
5'-Hydroxytryptamine
35
a mediator of the S/Sx of Carcinoid Syndrome
Serotonin
36
AA precursor of Serotonin
Tryptophan
37
what is the Rate Limiting step in the synthesis of Serotonin
Hydroxylation at C5
38
Blocker of Rate Limiting Step in Serotonin Synthesis
p-chlorophenylalanine | p-chloramphetamine
39
Stored serotonin can be depleted by
Reserpine
40
distribution of serotonin
ECL cells Platelets Brainstem (raphi cells)
41
Describe the serotonin receptors
7 receptors 6-G Protein mediated 1-Ligand gated ion channel
42
a simple methoxylated and N-acetylated product of Serotonin in the Pineal Gland
Melatonin
43
agonist at 5HT1a receptors ( a non Benzodiazepine anxiolytic)
Buspirone
44
Agonists at 5HT1d receptors in cerebral vessels that decreases migraine pain
Sumatriptan (all -"triptans")
45
Action of 5HT1 and 5HT2 on CNS
5HT1: Inhibitory 5HT2: Excitatory
46
Antagonist at 5HT2a receptors in the CNS that deceases Sx of Psychosis
Olanzapine
47
MOA of Ketanserine
Blocks vascular alpha1 receptor | antagonizes platelet aggregation by serotonin
48
5HT2 antagonist used in carcinoid and other GIT tumors
Cyproheptadine
49
5HT2 antagonist that alter bleeding time and thromboxane formation
Ritanserine
50
Distribution of 5HT3 receptors
``` CNS Chemoreceptive area Vomiting center Peripheral sensory Enteric nerves ```
51
5HT3 antagonist that decreases emesis in chemotherapy and Post-Op's
Ondansetron ("-setrons")
52
distribution of 5HT4 receptors
GI smooth muscles | Enteric nerves
53
MOA of Cisapride
Activator of 5HT4 receptor prokinetic in GERD cardiac K channel blocker
54
partial 5HT4 agonist that is used for irritable bowel syndrome and constipation
Tegaserod
55
Serotonin reuptake inhibitor | Its is combine with what other drug to produce "Fen-Phen"
Dexfenfluramine added with Phentermine
56
derived from fungus that grow on grain
Ergot Alkaloids
57
common actions of ergot alkaloids
agonists, partial agonists, antagaonists (Alpha Adrenoceptors and Serotonin receptors and dopamine receptors)
58
What are the effects of Ergot alkaloids in the following organs: Vessels Uterus Brain
Vessels: VC Uterus: Contraction Brain: Hallucination
59
drug used for hyperprolactinemia
Bromocriptine Carbegoline Pergolide
60
for the Dx of Angina
Ergonovine
61
for senile cerebral efficiency
Dihydroergonotoxine
62
used for Obstetric bleeding; however, What is the preferred agent?
Ergonovine and Ergotamine the preferred agent is still Oxytocin
63
(ergot alkaloid) used for Migraines
Ergotamine
64
Sever prolonged vasospasm in the GIT as a toxicity of Ergot alkaloids can be antagonized by
Nitroprusside
65
Chronic usage of Methysergide has what side effects?
hyperplasia of connective tissue
66
``` To what receptors do the following drugs have high affinities: Bromocriptine Ergonovine Ergotamine Lysergic Acid Diethylamine Methysergide ```
``` Bromocriptine: Dopamine receptors Ergonovine: Alpha adreno & 5HT2 Ergotamine: Uterine Muscle Lysergic Acid Diethylamine: Dopamine receptors Methysergide: none ```

PHARMACOLOGY 1.0 (3 decks)

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