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
Q

neuroinflammation migraine theory

A

activation of trigeminal nerve terminals in meninges and extracranial vessels

26
Q

what happens to 5HT concentrations in the blood during a migrane attack

A

falls

- increase in 5-HIAA metabolite in urine

27
Q

sumatriptan mechanism

A

5HT receptor agonist = causes vasoconstriction and inhibits trigeminal nerve transmission

28
Q

side effects of sumatriptan

A

coronary vasoconstriction

dysrhythmia

29
Q

what are some prophylactic antimigraine drugs

A

pizotifen and cyproheptidine

30
Q

pizotifen and cyproheptidine are

A

5HT receptor antagonists that prevent vasoconstriction

31
Q

side effects of pizotifen and cyproheptidine

A

weight gain, sedation, antimuscarinic effects

32
Q

carcinoid syndrome

A

rare tumor or cancer of enterochromaffin cells = excess amounts of 5HT

33
Q

what is used as treatment of carcinoid syndrome, mechanism

A

cyproheptadine

- 5HT2 receptor antagonist

34
Q

symptoms of carcinoid syndrome

A
flushing
diarrhea
bronchoconstriction
hypotension
fibrotic stenosis of heart valves
35
Q

5HT1 is responsible for

A

cerebral vasoconstriction

36
Q

5HT2 is responsible for

A

smooth muscle contraction
platelet aggregation
vasoconstriction