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pharmacoloy/pain control > Histamines and antihistamines > Flashcards

Histamines and antihistamines Flashcards

1
Q

Which granulocyte cell type is involved in IgE-mediated allergic responses like anaphylaxis?

A

Mast cells

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2
Q

What non-IgE-dependent triggers can activate mast cells?

A

Tissue trauma, cold air, viruses, opioids, vancomycin

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3
Q

Where are enterochromaffin-like (ECL) cells located?

A

In the stomach

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3
Q

Which granulocyte contributes to inflammatory responses?

A

Basophils

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4
Q

What stimulates ECL cells to release histamine?

A

Parasympathetic signals

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5
Q

What is the role of ECL cell histamine release?

A

Stimulates acid release from parietal cells

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6
Q

Where are histaminergic neurons located?

A

Central nervous system (CNS)

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7
Q

What is the function of histaminergic neurons?

A

Promote wakefulness and arousal

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8
Q

Which cells store histamine in granules?

A

Mast cells and basophils

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9
Q

What substances are stored with histamine in granules?

A

Heparin, chondroitin sulfate, eosinophilic chemotactic factors, neutrophilic chemotactic factors, proteases (e.g., tryptase)

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10
Q

Which cell types synthesize histamine on demand rather than store it?

A

ECL cells and histaminergic neurons

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11
Q

Where are H1 receptors found in the vasculature?

A

Endothelial cells of blood vessels

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12
Q

Where in the nervous system are H1 receptors found?

A

Central Nervous System (CNS)

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13
Q

Where are H1 receptors located in the respiratory and digestive systems?

A

Smooth muscle in the airway and gut

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14
Q

Where are H2 receptors found in the gastrointestinal system?

A

Parietal cells of the stomach

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15
Q

What is the function of H2 receptors on parietal cells?

A

Stimulate acid secretion

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16
Q

Where are H2 receptors located in the vasculature?

A

Smooth muscle of blood vessels

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17
Q

What effect do H2 receptors have on blood vessels?

A

Cause vasorelaxation via increased cAMP

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18
Q

What do H1 receptors on endothelial cells cause?

A

Vasodilation and increased vascular permeability

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19
Q

What do H1 receptors on smooth muscle cause?

A

Bronchoconstriction

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20
Q

What happens when H1 receptors on sensory nerves are activated?

A

Pain and itch

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21
Q

What is the effect of H1 activation in the CNS?

A

Promotes wakefulness

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22
Q

How do H1 blockers help treat skin allergies?

A

Reduce vasodilation and capillary permeability

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23
Q

What allergy symptoms are relieved by H1 blockers?

A

Sneezing, itchy/watery eyes, runny nose

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24
What are first-generation H1 blockers used for besides allergies?
Sleep aid and anti-nausea
25
How do H1 blockers affect the vestibular system?
Prevent motion sickness and nausea
26
What happens during the first exposure to an allergen in IgE-mediated reactions?
Allergen-specific IgE is produced
27
Where does IgE bind after the first exposure?
Mast cell receptors
28
What triggers mast cell degranulation upon re-exposure?
Crosslinking of IgE
29
What are the effects of histamine release in IgE-mediated responses?
Vasodilation, mucus production, nerve stimulation, bronchoconstriction
30
What are common symptoms of an IgE-mediated allergic reaction?
Rhinorrhea, itch, shortness of breath, anaphylaxis
31
How long does it take to reaccumulate histamine in mast cells?
Days to weeks
32
What kind of drugs can directly trigger mast cell histamine release without IgE?
Opioids (morphine, codeine, meperidine), vancomycin, d-tubocurarine, protamine sulfate, radiocontrast media
33
What physical stimuli can cause non-IgE histamine release?
Cold, heat, sunburn, exercise, mechanical trauma
34
What causes the Triple Response of Lewis?
Histamine release at the site of injury (e.g., bee sting)
35
What is the first phase (reddening) caused by?
Localized vasodilation; mediated by H1 and H2
36
What causes the wheal in the Triple Response of Lewis?
Edema from increased capillary permeability; mediated by H1
37
What causes the flare reaction?
Itching and pain from sensory nerve stimulation and widespread vasodilation; mediated by H1
38
What are the H1 Antihistamine-Responsive Symptoms?
Sneezing – responsive Nasal itching – responsive Runny nose (discharge) – responsive Watery, bloodshot eyes – responsive
39
What are not H1 Antihistamine-Responsive?
Nasal congestion – not responsive (may involve H3 or other mechanisms)
40
Do first-generation H1 antihistamines cross the blood-brain barrier?
Yes
41
What is a common CNS effect of first-generation H1 blockers?
Sedation
42
What type of receptor activity causes dry mouth and blurred vision with first-gen H1 blockers?
Antimuscarinic activity
43
Are first-generation H1 antihistamines used for motion sickness?
Yes
44
How often are first-generation H1 blockers typically dosed?
Multiple times daily
45
Are first-generation H1 blockers selective for peripheral receptors?
No
46
Name three first-generation H1 antihistamines.
Diphenhydramine, Promethazine, Hydroxyzine
47
Do second-generation H1 antihistamines cross the blood-brain barrier?
No
48
Are second-generation H1 antihistamines sedating?
Generally no
49
Do second-generation H1 blockers have strong antimuscarinic activity?
No
50
Are second-generation H1 blockers used for sleep or motion sickness?
No
51
What is the dosing frequency of second-generation H1 antihistamines?
Once daily
52
Are second-generation H1 antihistamines peripherally selective?
Yes
53
Name three second-generation H1 antihistamines.
Loratadine, Fexofenadine, Cetirizine
54
What are common uses of first-generation H1 antihistamines?
Allergies, sleep aids, motion sickness, nausea in pregnancy, insect bites
55
What is Diclegis used for and what is it made of?
Nausea during pregnancy; doxylamine + vitamin B6
56
What are CNS-related side effects of first-generation H1 blockers?
Sedation, drowsiness, CNS excitation at high doses (especially in children)
56
What antimuscarinic side effects are common with first-generation H1 antihistamines?
Dry mouth, blurred vision, urinary retention
57
What are the contraindications for first-generation H1 blockers?
Narrow-angle glaucoma, urinary retention
58
What symptoms are associated with overdose of first-generation H1 blockers?
Fever, delirium, flushed/dry skin, dilated pupils, drowsiness
59
What drug interactions should be avoided with first-generation H1 blockers?
CNS depressants, anticholinergics
60
What are second-generation H1 antihistamines primarily used for?
Seasonal allergies
60
Which second-generation drugs also stabilize mast cells?
Azelastine, olopatadine
60
What dosage form options are available for some second-generation antihistamines?
Nasal sprays and eye drops
61
Which second-generation H1 blocker is truly non-sedating?
Fexofenadine
62
Which second-generation drugs may cause slight sedation?
Cetirizine, levocetirizine
63
What is a unique benefit of fexofenadine regarding heart safety?
No QT prolongation
64
What is loratadine’s half-life like?
Long half-life
65
What is cetirizine the active metabolite of?
Hydroxyzine
66
What is levocetirizine the L-isomer of?
Cetirizine
67
Name two nasal sprays with H1-blocking and mast cell stabilizing activity.
Azelastine, olopatadine

pharmacoloy/pain control (36 decks)

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