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Pharmacology Exam V > Anti-Histamines > Flashcards

Anti-Histamines Flashcards

1
Q

2 Broad mechanisms of histamine release from mast cells

A

cytolytic - membrane damage, high levels of drugs, mechanical damage

non-cytolytic - immune response, non-immunological response, substances can displace it from granules

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2
Q

H1 receptor

A

Smooth muscle cells (vascular, respiratory, GI)
Vascular endothelial cells
CNS neurons
Peripheral sensory nerves

Gq protein

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3
Q

H2 receptor

A

Gastric parietal cells
Cardiac muscle
CNS neurons

Gs protein

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4
Q

H3 receptor

A

CNS neurons
Peripheral sensory nerves

Gi/o protein

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5
Q

H4 receptor

A

Neutrophils
Eosinophils
Monocytes
Other immune cells

Gi/o protein

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6
Q

Both peripheral and CNS histamine receptors mediate _____

A

itch

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7
Q

Histamine in the CNS released in _____

A

circadian pattern

controls release of pituitary hormones, wakefullness, appetite, satiety

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8
Q

Histamine physiologic effects

A

vasodilation - decreased TPR

increased vascular permeability - edema

epidermis - itch
dermis - pain

lungs - increased fluid and electrolyte secretion, bronchoconstriction

Cardiac (H2) - increase calcium (increase contracitility), increase SA node

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9
Q

Diseases that increase histamine levels

A

myelogenous leukemia

gastric carcinoid tumors

systemic mast cell diseases - mast cell leukemia

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10
Q

Classes of Anti-histamines

A

Physiological antagonists
Release inhibitors
Receptor Antagonists

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11
Q

Important characteristic of 2nd generation H1-anti-histamines

A

Non-sedating - don’t penetrate BBB

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12
Q

H1-antihistamines MOA

A

reversibly bind receptor and stabilize INACTIVE FORM

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13
Q

Potential adverse effects of 1st generation H1-antihistamines

A

CNS H1 receptors - sedation, decreased alertness

Muscarinic receptors - dry mouth, urinary retention, sinus tachycardia

Serotonin receptors - increase appetite and wt gain

Alpha- receptors - dizziness and postural hypotension

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14
Q

1st generation H1-antihistamines

A 
Chlorpheniramine
Diphenhydramine
Pyrilamine
Hydroxyzine
Meclizine
Promethazine
Cyproheptadine
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15
Q

Chlorpheniramine primary uses

A

allergic rhinitis and other allergic conditions

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16
Q

Diphenhydramine characteristics

A

sedative
anti-muscarinic
anti-motion sickness

17
Q

Pyrilamine characteristics

A

low to moderate sedative actions

18
Q

Hydroxyzine important characteristics

A

marked sedation and anti-muscarinic

19
Q

Meclizine important characteristics

A

less sedating than hydroxyzine
minimal anti-muscarinic

primarily for motion sickness and vertigo

20
Q

Promethazine important characteristics

A

strong anti-motion sickness and anti-emetic activities

local anesthetic

alpha-1 and muscarinic inhibition

21
Q

Phenothiazines (promethazine and chlorpromazine) can also

A

BLOCK D2 RECEPTORS

anti-psychotic

22
Q

Cyproheptadine important characteristics

A

Low to moderate sedative and antimuscarinic actions

Anti-serotonin activity

23
Q

H1 Antihistamines with strongest anti-emetic effects (4)

A

Diphenhydramine
Promethazine
Hydroxyzine
Meclazine

24
Q

H1 Antihistamines with strongest sedative effects (3)

A

Diphenhydramine
Hydroxyzine
Promethazine

25
Q

Strongest cholinergic anti-histamines

A

diphenhydramine

promethazine

26
Q

Strongest alpha-1 antagonist anti-histamine

A

promethazine

27
Q

strongest serotonin antagonist anti-histamine

A

cyproheptadine

28
Q

Drug-interactions with 1st generation H1 antihistamines

A

MAOI’s
Opioids, alcohol, sedatives
Anti-cholinergics

29
Q

2nd Generation H1 Anti-histamines characteristics

A

bind non-competitively to H1

reduced lipophilicity

higher selectivity toward H1

30
Q

2nd Generation H1 Anti-histamines

A 
Fexofenadine
Loratadine
Desloratadine
Levocetirizine
Cetirizine
Azelastine
31
Q

Azelastine characteristics

A

ALSO INHIBITS MAST CELL HISTAMINE RELEASE

INTRANASAL AND OPTHALMIC

32
Q

Cromolyn and Nedocromil MOA

A

stabilize mast cells

inhibition of chloride channels in cell membranes

nasal spray, eye drops, aerosols

33
Q

Omalizumab MOA

clinical

A

recombinant humanized IgE ANTIBODY - binds and sequesters IgE

urticaria, asthma

34
Q

Other drugs with anti-histaminic activity

A

Doxepin - TCA

Ketotifen - H1 antihistamine with mast cell and basophil stabilizing properties

Pharmacology Exam V (11 decks)

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