Amino acid based mediators- Histamine and 5HT Flashcards

1
Q

histamine is a ____ amine derived frm _____

A

basic

histidine

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2
Q

tissue histamine is proportional to

A

tissue mast cell content

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3
Q

there is a high conc of mast cells in

A

skin and mucous membranes

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4
Q

nonmast cel histamine comes frm

A

brain (NT) and stomach (signals acid secretion)

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5
Q

Mast cell histamine release id mediated by

A

IgE
complement stimulated
initiated by rise in intracellular calcium levels

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6
Q

how many types of histamine receptors are there

A

4

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7
Q

histamine receptors are coupled to

A

GPCR

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8
Q

which H receptor is for allergy and inflammation

A

H1

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9
Q

which H receptor stimulates gastric acid secretion

A

H2

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10
Q

wheal and flare entails

A

local vasodulation, vascular permeability, stimulation of nerve endings in skin

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11
Q

antihistamines exert effects primarily by acting on

A

H1 receptor

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12
Q

peptic ulcer drugs act on

A

H2 as antagonists

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13
Q

antihistamines are ____ agonists

A

inverse

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14
Q

5HT is synthesized from

A

tryotophan

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15
Q

5HT is degraded by

A

MAO

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16
Q

functions of 5HT in vascular system and in CNS

A

local hormone in vascular system

neurotransmitter in CNS

17
Q

where is 5HT found

A

enterochromaffin cells of intestinal wall
blood platelets
CNS

18
Q

_____ and _____ have high affinity reuptake transporters such as ____

A

platelets and neurons

SERT

19
Q

effects of 5HT(6)

A
  • vascular constriction in larger vessels and dilation of arterioles
  • smooth muscle contraction in bronchi and uterous
  • increases GI motility
  • stimulate platelet aggregation
  • stimulate peripheral nociceptive nerve endings
  • excitation/ inhibition in CNS
20
Q

pathophysiological effects of 5HT

A
migraine 
pulmonary hypertension
carcinoid syndrome
nausea, vomiting
mood disorders and anxiety
21
Q

4 migraine phases

A
  1. premonitory phase
  2. aura
  3. headache
  4. postdromal phase
22
Q

migraine theories

A
  1. vascular
  2. brain
  3. neuroinflammation
23
Q

vascular migraine theory

A

intracerebral vasoconstriction, followed by vasodilation

24
Q

brain migraine theory

A

wave of cortical spreading depression

25
neuroinflammation migraine theory
activation of trigeminal nerve terminals in meninges and extracranial vessels
26
what happens to 5HT concentrations in the blood during a migrane attack
falls | - increase in 5-HIAA metabolite in urine
27
sumatriptan mechanism
5HT receptor agonist = causes vasoconstriction and inhibits trigeminal nerve transmission
28
side effects of sumatriptan
coronary vasoconstriction | dysrhythmia
29
what are some prophylactic antimigraine drugs
pizotifen and cyproheptidine
30
pizotifen and cyproheptidine are
5HT receptor antagonists that prevent vasoconstriction
31
side effects of pizotifen and cyproheptidine
weight gain, sedation, antimuscarinic effects
32
carcinoid syndrome
rare tumor or cancer of enterochromaffin cells = excess amounts of 5HT
33
what is used as treatment of carcinoid syndrome, mechanism
cyproheptadine | - 5HT2 receptor antagonist
34
symptoms of carcinoid syndrome
``` flushing diarrhea bronchoconstriction hypotension fibrotic stenosis of heart valves ```
35
5HT1 is responsible for
cerebral vasoconstriction
36
5HT2 is responsible for
smooth muscle contraction platelet aggregation vasoconstriction