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

A

TRUE!

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
Q

How do H1 specific antihistamines dilate smooth muscles?

A
  1. Dilates BRONCHIOLE smooth muscle (bronchodialation)

2. Can inhibit secretory interleukins and other inflammatory mediators

26
Q

What is the physiological target of H2 specific antihistamines?

A

Gastric secretions

27
Q

How do H2 antihistamines decrease gastric secretions

A

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
Q

What are the 2 therapeutic indications for “Classic” (first generation) H1 Antihistamines?

A

Treatment of allergic responses:

  1. Dermatoses - uticaria/itching and insect bites
  2. Allergic rhinitis/conjunctivitis (decrease congestion and sneezing)
29
Q

First generation H1 antihistamines are NOT of value in the treatment of _____ or _____

A

NOT for asthma or common cold

30
Q

What are 3 names for H1 antihistamine SEDATIVES

A

Nytol, Somminex, Dormin

31
Q

What do all 3 H1 antihistamine Sedatives contain?

A

Diphenyhdramine (Benedryl)