Biogenic Amines - Histamine and Serotonin Flashcards

1
Q

Histamine is an essential ______

A

Essential amino acid

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2
Q

When is histamine derived from?

A

Histidine

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3
Q

Where is histamine found?

A

In almost all tissues

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4
Q

What enzyme converts histidine to histamine?

A

Histidine Decarboxylase

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5
Q

What are the 4 functions of Histamine for NORMAL physiology?

A
  1. Tissue growth and regeneration
  2. Neuromodulation (affects neurotransmission)
  3. Regulator or microcirculation (smaller vessels)
  4. Body Defense Mechanisms
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6
Q

Where is histamine STORED?

A

Mast cells of skin and lungs

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7
Q

Histamine release is part of both a _____ mechanism and a _____ system.

A

Protective mechanism and a Warning system

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8
Q

What causes histamine to be released following tissue injury?

A

As part of the inflammatory response to tissue injury, stored histamine is released as part of an ANTIGEN-ANTIBODY interaction

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9
Q

What are the 4 kinds of tissue injuries that would induce histamine release?

A
  1. Mechanical (ie scrape)
  2. Thermal (i.e. burn)
  3. Radiant (ie sunburn/frost bite)
  4. Chemical (i.e. acid, drugs, insect venom)
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10
Q

In what 2 ways does histamine serve as a “warning system”?

A
  1. Serves to prevent further tissue damage

2. Serves as enhancer of immunological response

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11
Q

What is Histamines MECHANISM OF ACTION

A

ACTIVATES A RECEPTOR – binds to specific histamine receptors H1 and H2

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12
Q

What are the 4 physiological effects of histamine?

A
  1. Vascular
  2. Neuronal
  3. Smooth Muscle
  4. Exocrine secretion
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13
Q

What are the 5 ways in which histamine induces vascular physiological effects?

A
  1. Constricts LARGER vessels
  2. Dilates SMALLER vessels (esp. in head and neck)
  3. Can cause pooling of blood at injury site
  4. Causes endothelial cell leakage (edema –> wheal)
  5. Induces “triple response”
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14
Q

What is the significance of histamine inducing local edema?

A

Endothelial cell leakage (local edema) serves to increase access of immune cells to site of injury

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15
Q

What is the ‘triple response’ induced by histamine?

A
  • Central red spot = due to vasodilation
  • Flare = surrounding the area
  • Wheal = swelling due to edema
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16
Q

In what 2 ways does histamine induces neuronal physiological effects?

A
  1. Stimulates sensory neurons leading to ITCHING and PAIN

2. In CNS, Increases Alertness

17
Q

In what 2 ways does histamine induce smooth muscle physiological effects?

A
  1. Constricts bronchioles (bronchoconstriction)

2. Constricts intestinal muscles (diarrhea)

18
Q

In what 2 ways does histamine induce exocrine secretion?

A

Stimulates bronchiole, salivary, and digestive secretions – helps to dilute and thus wash out bugs

19
Q

T/f: Histamine plays no role in asthma

20
Q

What is the MECHANISM of action for ANTI-histamines?

A

INHIBIT A RECEPTOR – blocks H1 and H2 receptors

21
Q

What are the 4 physiological targets/effects of H1 blocking antihistamines?

A
  1. CNS effects
  2. Drying of mucous membranes
  3. PNS effects
  4. Smooth muscle dilation
22
Q

How do H1 specific anti-histamines effect the CNS?

A
  1. Sedative effect (exception: kids and elderly)
  2. Anti-nausea
  3. Anti-emetic
23
Q

How do H1 specific antihistamines dry out mucous membranes

A

Blockade of H1 receptors leads to Anti-muscarinic effects

24
Q

How do H1 specific antihistamines effect the PNS?

A

Act as a local anesthetic (neuromodulator activity blocks pain)

25
How do H1 specific antihistamines dilate smooth muscles?
1. Dilates BRONCHIOLE smooth muscle (bronchodialation) | 2. Can inhibit secretory interleukins and other inflammatory mediators
26
What is the physiological target of H2 specific antihistamines?
Gastric secretions
27
How do H2 antihistamines decrease gastric secretions
Histamine is required to stimulated acid secretion from parietal cells, thus blockade of H2 receptors leads to a decrease in acid secretions in the gut
28
What are the 2 therapeutic indications for "Classic" (first generation) H1 Antihistamines?
Treatment of allergic responses: 1. Dermatoses - uticaria/itching and insect bites 2. Allergic rhinitis/conjunctivitis (decrease congestion and sneezing)
29
First generation H1 antihistamines are NOT of value in the treatment of _____ or _____
NOT for asthma or common cold
30
What are 3 names for H1 antihistamine SEDATIVES
Nytol, Somminex, Dormin
31
What do all 3 H1 antihistamine Sedatives contain?
Diphenyhdramine (Benedryl)