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Pharmacology > Anti-histamines Part 1 > Flashcards

Anti-histamines Part 1 Flashcards

1
Q

What is the histamine precursor?

A

Histidine

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2
Q

What enzyme converts histidine to histamine?

A

Histidine Decarboxylase

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3
Q

What are 4 functions of histamine?

A
  • immediate allergic and inflammatory reactions
  • gastric acid secretion
  • neurotransmission and neuromodulation
  • chemotactic factor for recruitment of neutrophils, eosinophils, basophils, monocytes, and lymphocytes
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4
Q

Where is histamine stored in the blood?

A

In basophils- preformed granules

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5
Q

Where is histamine stored in the tissue?

A

Mast cells

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6
Q

Where is histamine stored? (4 locations)

A
  • blood basophils
  • tissue mast cells
  • gastric mucosal cells
  • neurotransmitter vesicles
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7
Q

What does the Histamine 1 Receptor cause an increase in?

A

IP3/DAG

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8
Q

Which histamine receptors causes a decrease in cAMP?

A

H3 and H4

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9
Q

What receptor leads to an increased cAMP?

A

H2

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10
Q

What effects does histamine have in the cardiovascular system?

A
  • vasodilation of arterioles and precapillary sphincters via H1
  • increased vascular permeability via H1 (hives)
  • increased heart rate
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11
Q

What histamine receptor is involved in increased vascular permeability?

A

H1

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12
Q

What are the effects of histamine in the GI?

A

increased acid secretion via H2

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13
Q

What histamine receptor is involved in increasing gastric acid secretion?

A

H2

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14
Q

Which histamine receptor leads to bronchoconstriction?

A

H1

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15
Q

What are the nervous system effects of histamine?

A

stimulation of sensory nerve endings via H1

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16
Q

What cell types are involved in the wheal and flare reaction?

A

vasculature- dilation
endothelium- permeability –> edema
sensory nerve endings - red, irregular flare surrounds wheal (can have itching)

17
Q

What two mediators are increased with histamine to cause vasodilation?

A

Nitric oxide and prostaglandin

18
Q

What causes the edema with histamine?

A

Endothelial- H1 receptor

Contraction of endothelial cells which causes vascular permeability

19
Q

Chlorpheniramine

A

1st Gen H1 receptor competitive antagonist

20
Q

Diphenhydramine

A

1st Gen H1 receptor competitive antagonist

21
Q

What is the duration of 1st Gen H1 receptor competitive antagonists?

A

Short duration of 3-6 hours

22
Q

What effects are related to 1st Gen H1 receptor competitive antagonists?

A 
anticholinergic
anti a-adrenergic : 
anti-serotonergic : anti seretonin effects
sedation
antiemetic- against vomiting and nausea
anti-motion sickness
23
Q

What drug class has a long duration of 12-24 hours?

A

2nd/3rd Gen H1 receptor competitive antagonists

24
Q

loratadine

A

2nd/3rd Gen H1 receptor competitive antagonists

25
Q

fexofenadine

A

2nd/3rd Gen H1 receptor competitive antagonists

26
Q

cetirizine

A

2nd/3rd Gen H1 receptor competitive antagonists

27
Q

What is the difference in side effects between 1st Gen and 2nd/3rd Gen H1 receptor competitive antagonists?

A

2nd/3rd Gen H1 receptor competitive antagonists have LITTLE TO NO anticholinergic, anti a-adrenergic, anti-serotonergic effects. Less sedation. And are not useful for nausea or motion sickness.

28
Q

H2 Receptor Antagonists are thought to be useful for…

A

reducing NSAID induced dyspepsia

29
Q

Gastric ulcers are due to

A

NSAID use

30
Q

Most peptic ulcers are due to…

A

H. Pylori infection

31
Q

H2 receptor antagonists are associated with…

A

esophageal reflux

few side effects

infrequent GI irritation

32
Q

cimetidine

A

potent inhibitor of P450 metabolism

Pharmacology (6 decks)

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