Pharm--Antihistamines Flashcards

1
Q

Smooth muscles have which histamine receptors?

A

H1

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2
Q

Gastric parietal cells have which receptors?

A

H2

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3
Q

What are some functions of H1 receptors?

A

Smooth muscle contraction (bronchoconstriction), endothelial cell contraction (microvascular leakage), increased vascular permeability, airway blood vessel dilation (H1)

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4
Q

What role does histamine play in the stomach?

A

Stimulates parietal cell to secrete H+; ACh can also stimulate ECL cells to release histamine which will then act on the parietal cell

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5
Q

H1 effects on smooth muscle?

A

Constriction

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6
Q

H1 effects on endothelium?

A

Dilation

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7
Q

H2 effects on smooth muscle?

A

Dilation

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8
Q

What is a major type of side effect in H1 antagonists?

A

Anticholinergic effects

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9
Q

Which 1st gen H1 antags are the most sedative?

A

Ethanolamines (diphenhydramine and dimenhydrinate)

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10
Q

Which 1st gen H1 antags have the most anticholinergic activity?

A

Ethanolamines (diphenhydramine and dimenhydrinate)

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11
Q

What are some side effects caused by alpha adrenergic receptor blockage?

A

Hypotension, dizziness, reflex tachycardia

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12
Q

Which drugs are ethanolamines?

A

Diphenhydramine and dimenhydrinate

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13
Q

Which drugs are alkylamines?

A

Chlorpheniramine

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14
Q

Which drugs are piperazine derivatives?

A

Hydroxyzine (1st generation) and Cetirizine (2nd generation / Zyrtec)

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15
Q

Compare desloratadine and loratadine

A

Desloratadine has a much higher specificity for H1 receptor

Much lower affinity for muscarinic receptors

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16
Q

What is the deal with desloratadine half life?

A

Long - about 27 hrs

17
Q

What’s cool about azelastine?

A

It’s both an H1 and leukotriene inhibitor

Also block calcim mobilization, 5-Lipoxygenase, and PAF

18
Q

Which class is best for allergic rhinitis?

A

2nd (compliance)

19
Q

Which class is better for motion sickness?

A

1st

20
Q

Which class is the better antiemetic?

A

1st

21
Q

Which class is better for appetite stimulation?

A

1st

22
Q

Which class is best for insomnia?

A

1st

23
Q

Which class is better for urticaria?

A

2nd (compliance)

24
Q

What are some side effects associated with muscarinic stimulation by the first gen drugs?

A

Xerostomia, urinary retention, sinusoidal tachycardia

25
Q

What mechanism causes appetite stimulation with 1st gen drugs?

A

Serotonergic receptor stimulation