Antihistamines Flashcards

1
Q

Doxylamine

A

Insomnia, Allergies
Highly Sedating
Large doses can cause arrhythmias (QT Prolongation)
Avoid in elders

First Generation H1 Antihistamine

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2
Q

Diphenhydramine

A

Insomnia, Allergies
Highly Sedating
Large doses can cause arrhythmias (QT Prolongation)
Avoid in elders

First Generation H1 Antihistamine

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3
Q

Cyclizine

A

Motion Sickness
Vertigo
Mildly Sedating

First Generation H1 Antihistamine

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4
Q

Meclizine

A

Motion Sickness
Vertigo
Mildly Sedating

First Generation H1 Antihistamine

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5
Q

Chlorpheniramine

A
Allergies
Moderately sedating
Possible paradoxical CNS stimulation 
Often found in combo w/ cold products
avoid in elders 

First Generation H1 Antihistamine

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6
Q

Brompheniramine

A
Allergies
Moderately sedating
Possible paradoxical CNS stimulation 
Often found in combo w/ cold products
avoid in elders 

First Generation H1 Antihistamine

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7
Q

Hydroxyzine HCL

A

Allergies Urticaria
Mild - moderate sedation

First generation H1 antihistamine

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8
Q

Hydrozyzine PAMoate

A

Insomnia
Anxiety
Mild - moderate sedation

First generation H1 antihistamine

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9
Q

Histamine H1 Receptor

Location , Action

A

Location - Bronchial smooth muscle, CNS, Endothelium, cardiac muscle

Action - sleep wake cycle, learning, memory, stimulate nerve endings, bronchoconstriction, vasodilation of blood vessels, contraction smooth muscle

Mainly thinking histamine on H1 causes:

  • Bronchoconstriction
  • Increases bowel peristalsis
  • Increased vasodilation permeability
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10
Q

Histamine H2 Receptor

Location , Action

A

Location - parietal cells of stomach, cardiac muscle, CNS

Action - Gastric acid production

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11
Q

H3 Receptor

Location, Action

A

Location - CNS, peripheral tissue

Action - modulation of neurotransmitter release

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12
Q

H4 receptor

Location, Action

A

Location - basophils, bone marrow, SI, colon, spleen, thymus

Action - facilitates made cell chemotaxis

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13
Q

Cardiovascular Effects of Histamine

A

Mast cells are present in normal cardiac tissue (higher presence in diseased hearts)

Histamine enhances influx of Ca into cardiac myocytes =

  • increase contractility
  • tachycardia
  • hypotension secondary to vasodilation
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14
Q

Antihistamine actions on H1

A

Bronchodilaiton
Constipation
Anti-itch, reduce pain
Reduced the inflammatory / allergic response

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15
Q

Antihistamine actions on H2

A

Suppression of gastric acid production

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16
Q

First Generation H1 Antihistamines

  • Treats
  • Features
A

Used to treat allergic symptoms, motion sickness & insomnia

Poor receptor selectivity

Highly lipophilic = crosses BBB = interfere w/ histaminergic transmission

Leads to many ADRs limiting its use

17
Q

Second Generation H1 antihistamines

A

Used to treat allergic symptoms

Highly selective for H1 Receptor with no anticholinergic effects

Minimall or non-seriating
- limited penetration to BB

Preferred in elders

Rapid onset of action about a hour

Longer duration of action

18
Q

Azelastin

A

Nasal Spray - RX

Second Generation H1 antihistamines

Local application to nose - less associated systemic side effects

Location irratation can occur (nasal irritation, nose bleeds, Bitter taste)

Avoid use if any preexisting damage to the nasal passage

19
Q

Olopatidine

A

Nasal Spray - Rx

Second Generation H1 antihistamines

Local application to nose - less associated systemic side effects

Location irratation can occur (nasal irritation, nose bleeds, Bitter taste)

Avoid use if any preexisting damage to the nasal passage

20
Q

Fexofenadine

A

Second Generation H1 antihistamines

Oral, OTC

Highest safety profile = b/c not metabolized by CYP450
Not metabolize
Excreted in feces

useful in pt on a lot of medication b/c not a lot DDI

Avoid in grapefruit juice, orange & apple juice
- must separate by at least 4 hours

21
Q

Cetirizine

A

Second Generation H1 antihistamines

Oral, OTC

Most SOMNOLENCE!

active metabolite of hydroxyzine

Not metabolized via CYP450 but both are PgP substrates
Watch DDI grapefruit juice
Avoid other sedative drugs — additive effects

22
Q

Loratitdine

A

Second Generation H1 antihistamines

Oral , OTC

Metabolized by 3A4
check for 3A4 inhibitors

23
Q

Levocetirizine

A

Second Generation H1 antihistamines

Oral , OTC

active metabolite of cetirizine

Not metabolized via CYP450 but both are PgP substrates
Watch DDI grapefruit juice
Avoid other sedative drugs — additive effects

24
Q

Desloratidine

A

Second Generation H1 antihistamines

Oral, RX

Least likely to cause somnolence

active metabolite of loratadine

Most likely for DDI because hepatic ally metabolized

25
Q

H2 receptor antagonists

A

Reversibly decrease fasting and food stimulated acid secretion by inhibiting histamine on the histamine 2 receptor of the parietal cell

Indicated for treatment of :
- Mild - moderate, infrequent, episodic heartburn

Good for on demand, meal provoked symptoms

Onset 30 - 45 min
Duration 4 - 10 hours

All drugs equally efficacious - considered interchangeable

All available both OTC & prescription doses

Well absorbed; absorption may be delayed by administration of antacid but not by food

26
Q

Ranitidine

A

H2 Receptor antagonist

Reversibly decrease fasting and food stimulated acid secretion by inhibiting histamine on the histamine 2 receptor of the parietal cell

Indicated for treatment of :
- Mild - moderate, infrequent, episodic heartburn

Good for on demand, meal provoked symptoms

27
Q

Cimetidine

A

H2 Receptor antagonist

Reversibly decrease fasting and food stimulated acid secretion by inhibiting histamine on the histamine 2 receptor of the parietal cell

Indicated for treatment of :
- Mild - moderate, infrequent, episodic heartburn

Good for on demand, meal provoked symptoms

Dose related gynecomastia occurs with cimetidine

Cimetidine inhibits CYP450 enzymes

28
Q

Nizatidine

A

H2 Receptor antagonist

Reversibly decrease fasting and food stimulated acid secretion by inhibiting histamine on the histamine 2 receptor of the parietal cell

Indicated for treatment of :
- Mild - moderate, infrequent, episodic heartburn

Good for on demand, meal provoked symptoms

29
Q

Famotidine

A

H2 Receptor antagonist

Reversibly decrease fasting and food stimulated acid secretion by inhibiting histamine on the histamine 2 receptor of the parietal cell

Indicated for treatment of :
- Mild - moderate, infrequent, episodic heartburn

Good for on demand, meal provoked symptoms

30
Q

ADRs of 2nd generation antihistamines

A

Somnolence - usually at higher doses
- highest with cetirizine & levocetirizine

Constipation
Headache

31
Q

H2 Antagonists ADRs

A

Well tolerated

Common ADRs are CNS effects

  • Headache, dizziness, fatigue, confusion
  • Incidence increased in elderly / renal impairment

Dose related gynecomastia occurs with cimetidine

Tolerance has been reported with prolonged daily use
- take PRN “on demand”

Self treatment should be limited to no more than 2 times a day for no more than 2 weeks

32
Q

H2 antagonists DDI

A

Drugs depend on acid for proper absorption

Cimetidine inhibits CYP450 enzymes