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pharm III exam 2 > Antihistamines > Flashcards

Antihistamines Flashcards

1
Q

Diphenhydramine

A
  • (Benadryl®)
  • Sedating Antihistamines
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2
Q

Dimenhydrinate

A
  • (Dramamine®)
  • Sedating Antihistamines
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3
Q

Promethazine

A
  • (Phenergan®)
  • Sedating Antihistamines
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4
Q

Loratadine

A
  • (Claritin®)
  • Second-generation (Non-Sedating) H1 Antagonists
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5
Q

Cetirizine

A
  • (Zyrtec®)
  • Second-generation (Non-Sedating) H1 Antagonists
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6
Q

Azelastine (Astelin NS®; Astepro®)

A

Nasal H1 Antagonists

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7
Q

The allergic response is mediated by what antibody

A

IgE

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8
Q

In allergic response, IgE binds to Fc receptors on surface of what cells

A
  • mast cells
  • basophils
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9
Q

What happens when antigen binds to IgE

A
  • activates protein kinases to increase IP3 and Ca2+ -> activates Phospholipase A2 -> increases
    • platelet activating factor
    • leukotrienes
    • kinins
    • mast cell degranulation -> histamine
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10
Q

H1 histamine receptor acts through what messenger system

A

Gq

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11
Q

H1 histamine receptor is found in what tissues

A
  • smooth muscle
  • endothelium
    • activates NO
    • vasodilation
  • brain
    • wakefullness
    • appetite control
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12
Q

H2 histamine receptor activation is coupled with what messenger system

A

Gs -> increases cAMP

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13
Q

H2 histamine receptor activation causes what

A
  • gastric acid secretion
  • vasodilation (at higher concentrations)
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14
Q

List the 4 main effects of histamine and which receptors are responsible

A
  1. vasodilation (H1 and H2)
  2. Bronchospasm (H1)
  3. Gastric acid secretion (H2)
  4. Itching
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15
Q

vasodilation effect of H1 and H2 stimulation leads to what effects

A
  • decreased BP, reflex tachycardia
  • increased capillary permeability
  • edema and swelling
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16
Q

what is the triple response that occurs after intradermal injection of histamine.

A
  1. Dilation of capillaries in immediate area (flush), which appears in seconds. This is a direct histamine effect.
  2. Dilation of arterioles causing redness over a wider area (flare) develops more slowly, due to stimulation of axon reflexes
  3. Swelling (wheal) in the area of capillary dilation; appears after 1-2 minutes and is the result of edema due to increased capillary permeability.
17
Q

MOA of antihistamines

A
  • inverse agonist
  • decrease normal histamine activity
  • block effects of released histamine
  • Since they compete with histamine, the ability to block histamine depends on the amount of histamine present
18
Q

what is unique about the first generation H1 antagonists

A
  • enter the brain
  • block muscarinic receptors -> sedation
19
Q

List the sedating first generation H1 antagonists

A
  • Diphenhydramine
  • Promethazine
  • Dimenhydrinate
20
Q

which first generation H1 antagonists are useful against motion sickness

A
  • Dimenhydrinate
  • Diphenhydramine

**due to muscarinic blockade

21
Q

which first generation H1 antagonists is used as an antiemetic

A

Promethazine

22
Q

How are second generation H1 antagonists different from first generation

A
  • second generation
    • do not enter brain
      • far less sedation
    • no anticholinergic effects
      • not useful for motion sickness
23
Q

Most antihistamines are excreted by the liver, what are the three that are excreted by the kidney and thus are better for patients with liver disease

A
  • Cetirizine
  • Levocetrizine
  • Acrivastine
24
Q

antihistamines for allergic rhinitis are best when used

A

prophylactically

25
Q

antihistamines taken for motion sickness should be taken when

A
  • prophylactic, BEFORE you get sick
26
Q

side effects of first generation antihistamines

A
  • Sedation
  • Dry mouth -> anticholinergic
27
Q

side effects of all antihistamines

A
  • GI: nausea, inc appetite
  • decrease seizure threshold
28
Q

first generation antihistamines have what effect on CNS

A

CNS depressants

29
Q

overdose of first generation antihistamines have what effect

A
  • similar to atropine poisoning
  • sedation, dry of salivary and bronchial secretions
30
Q

overdose of second generation antihistamines have what effect

A

sinus tachycardia

31
Q

MOA and route of administration of Azelastine

A
  • nasal spary
  • a non-competitive H1 blocker that also decreases the release of histamine from mast cells
  • used for allergic rhinitis.
32
Q

List the drugs that act to inhibit the release of histamine

A
  • Azelastine
  • Cetirizine

pharm III exam 2 (10 decks)

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