Histaminergic System + Antihistamines Flashcards

1
Q

What are autacoids?

A

LOCAL HORMONES
Short acting endogenous mediators usually acting as part of an inflammatory response

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2
Q

What is histamine?

A

Endogenous substance synthesised, stored + released by professional histamine cells

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3
Q

What are the histamine cells?

A

Mast cells
Basophils
Some neurons in CNS + PNS

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4
Q

What histamine synthesised by?

A

Decarboxylation from histidine

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5
Q

Where is histamine stored?

A

In granules in mast cells, basophils + enterocytes

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6
Q

When is histamine released?

A

Response to certain stimuli

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7
Q

What is histamine eliminated by?

A

Oxidative deamination +/ transmethylation

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8
Q

How does the histamine process work?

A

L-amino acid transporter
Histidine converted to histamine
By histidine decarboxylase
Vesicular monoamine transporter
Histamine methyltransferase released
To form tele-methylhistamine

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9
Q

What are the histamine receptors?

A

H1 = allergy
H2 = acid reflux
H3 = CNS
H4 = inflammation + itch

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10
Q

Where are H1?

A

Smooth muscle
Endothelium
CNS

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11
Q

Where are H2?

A

Gastric parietal cell
Vascular smooth muscle cells
Basophils

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12
Q

Where are H3?

A

CNS cells
Peripheral NS

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13
Q

Where are H4?

A

Bone marrow
White blood cells

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14
Q

What do H1 do?

A

Bronchoconstriction
Vasodilation
Allergic rhinitis
Pain + itching

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15
Q

What do H2 do?

A

Gastric acid secretion
Vasodilation
Inhibition of IgE-dependent degranulation

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16
Q

What do H3 do?

A

Presynaptic
Feedback inhibition of histamine synthesis

17
Q

What do H4 do?

A

Mediate mast cell chemotaxis

18
Q

What is H1 G-protein coupled receptor?

A

Gq coupled to phospholipase C (PLC)

19
Q

What is H2 G-protein coupled receptor?

A

Gs coupled to adenyl cyclase (AC)

20
Q

What is H3 G-protein coupled receptor?

A

Gi/o coupled to AC

21
Q

What is H4 G-protein coupled receptor?

A

Gi/o in mast cells

22
Q

What is the response to histamine in the skin?

A

Initial red line
Flare
Wheal

23
Q

What is the response to injected intradermally histamine?

A

Red spot
Flare
Wheal

24
Q

What effect does histamine have on the heart?

A

Cardiac contractility + electrical events
Increases force of contraction by promoting Ca2+ influx

25
Q

What effect does H1 have on the lungs?

A

Bronchoconstriction, increased mucus viscosity
Stimulation of vagal sensory nerve endings = cough

26
Q

What effect does H2 have on the lungs?

A

Slight bronchodilation, increased mucus sceretion

27
Q

What is the effect of histamine on peripheral vascular resistance?

A

Decreases

28
Q

What is the effect of histamine on vascular permeability?

A

Increases

29
Q

What does histamine (H3) stimulate?

A

Nerve endings (pain)

30
Q

Describe type I allergic response?

A

IgE Abs
IgE binds to mast cells/basophils
Ab binds antigen = release of histamine

31
Q

Describe what happens in anaphylaxis

A

Decreased BP
Decreases cardiac output
Bronchoconstriction + increased pulmonary secretions
Pruritis

32
Q

What is the treatment for anaphylaxis?

A

Epinephrine = physiological antagonist of histamine

33
Q

What are the 3 mechanistically different approaches to minimise histamine reactions?

A

Physiological antagonism
Inhibit release of histamine
Pharmacological antagonism