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Therapeutics > Histamines > Flashcards

Histamines Flashcards

1
Q

where is histamine synthesized

A

Mast cells and basophils

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2
Q

Where is histamine stored

A

granules

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3
Q

How is histamine metabolized

A

Methylated, oxidized or conjugated and excreted

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4
Q

2 types of histamine releases from mast cells

A

Antigen mediated release and non-antigen mediated release

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5
Q

Describe antigen mediated release

A

Mast cells bind to IgEs. When they encounter an antigen, they undergo degranulation of mast cell and release histamine

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6
Q

Describe mechanism of mast cell degranulation

A

binding of IgE to FcER
binding of antigen to IgE antibodies
clustering of FcER receptors
Influx of Ca2+ via CRAC

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7
Q

How does binding of antigen to antibodies affect Ca2+

A

Causes an increase in cytoplasmic Ca2+

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8
Q

What are the two drugs that prevent histamine release

A

Cromolyn sodium
Nedocromil

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9
Q

H1 receptor location

A

Vascular endothelium

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10
Q

H1 receptor physiologic effects

A

Vasodilation (due to increase in NO)
Contraction of endothelial cells

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11
Q

Effect of NO in H1

A

Causes vasodilation, even though H1 causes constriction in endothelial cells

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12
Q

Where are H2 receptors found

A

Vascular muscle

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13
Q

H2 effect on vasculature

A

Vasodilation

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14
Q

Pathway of H1

A

Gq

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15
Q

pathway of H2

A

Gs

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16
Q

effects of histamine on CVS

A

Heart- moderate increase in force and rate of contraction (mediated by h2 causes increase in SA conduction)
vasodilation- H1 in endothelium
H2 in smooth muscle

17
Q

Effects of histamine on respiratory

A

H1 mediated constriction of bronchial smooth muscle

18
Q

What class does chloromphenamine belong to? structure?

A

Alkylamines, Two carbons attatched to nitrogen

19
Q

What class does diphenhydramine belong to? structure?

A

Instead of just two carbons and an amine, Oxygen is added before carbons

20
Q

What class does pyrilamine belong to? structure

A

Ethylene diamines. Instead of an O, we have two nitrogens on either side of the carbons

21
Q

What class does promethazine belong to? structure?

A

Phenothiazine, has sulfur

22
Q

What class does cyproheptadine belong to?

A

piperadines. Six member ring with an N

23
Q

What class does hydroxyzine belong to? structure?

A

Two N in six member ring

24
Q

Name the 4 2nd gen antihistamines

A

Loratidine (claratin)
allegra (fexofenadine)
deslovatidine(clarinex)
etrizine (zyrtec)

25
Q

role of fluticasone and budesonide in treating allergic rhinitis

A

Slow onset, slow absorption, treats allergic rhinitis

Therapeutics (46 decks)

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