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Year 2 > Anti-Histamine Drugs > Flashcards

Anti-Histamine Drugs Flashcards

1
Q

What are 3 other terms for histamine?

A

Biogenic amine, vasoactive amine, autacoid

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2
Q

Is serotonin a vasoactive amine?

A

Yes

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3
Q

What does autacoid mean?

A

“Self-remedy” or local

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4
Q

What are some other examples of autacoids?

A

Endogenous peptides; prostaglandins; leukotrienes; and cytokines.

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5
Q

It what tissue areas is histamine most highly distributed?

A

Skin; GI and Nasal Mucosa; Lung; Stomach

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6
Q

What is histamine storage content directly related to in peripheral tissues?

A

The mast cell content. More mast cells = more stored histamine.

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7
Q

Is histamine stored in mast cells of the central nervous system?

A

No. The CNS is the notable exception to histamine storage in mast cells.

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8
Q

Aside from mast cells, where else is histamine stored?

A

In basophils, histaminergic neurons, and enterochromaffin-like cells.

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9
Q

What is the function of the subclass of G-proteins, Gs?

A

Gs proteins stimulate adenylyl cyclases.

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10
Q

What is the function of the subclass of G-proteins, Gq?

A

Gq proteins stimulate phospholipase C-beta.

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11
Q

What is the function of the subclass of G-proteins, Gi?

A

Gi proteins inhibit adenylyl cyclase.

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12
Q

What is the function of the subclass of G-proteins, G12/13?

A

G12/13 stimulate low molecular weight G protein Rho.

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13
Q

What is the post-receptor mechanism of the H1 receptor?

A

Increased levels of IP3 and DAG(Gq).

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14
Q

What is the post-receptor mechanism of the H2 receptor?

A

Increased levels of cAMP(Gs).

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15
Q

True or false: Drugs to block all 4 subtypes of histamine receptors are clinically available.

A

False. Only drugs for H1 and H2 are clinically available.

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16
Q

Intracellulary, how is histamine stored?

A

In granules.

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17
Q

What receptor subtype of histamine is involved in sensory nerve endings, stimulating pain and itching?

A

H1 receptor.

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18
Q

Which histamine receptors are involved in modulating release of acetylcholine, amine, and peptide transmitters?

A

H1, H2, H3.

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19
Q

True or false: In modulating the release of acetylcholine, amine, and peptide transmitters, the H3 receptor is post-synaptic.

A

False. The H3 receptor is presynaptic in modulating the release of acetylcholine, amine, and peptide transmitters.

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20
Q

True or false: H1 and H2 receptors are post synaptic in modulating the release of acetylcholine, amine, and peptide transmitters.

A

True.

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21
Q

Histamine binding to endothelial H1 receptors causes what effect?

A

Release of NO and subsequent smooth muscle relaxation (vasodilation).

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22
Q

True or false. Binding of histamine to endothelial H1 receptors results in decreased peripheral resistance and lowered systemic blood pressure.

A

True.

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23
Q

Define chronotropism and give an example of it.

A

Modification of the rate of a periodic movement, such as the heartbeat, through some external influence.

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24
Q

Define ionotropism and give an example.

A

A process leading to shortening and/or development of tension in muscle tissues, e.g. increased contractile force of the heart.

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25
Q

True or false: Binding of histamine to H1 receptors on the heart affects atrial-ventricular conductance.

A

True.

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26
Q

Histamine binding to H1/H2 receptors on smooth muscle results in rapid smooth muscle relaxation.

A

False. Slow smooth muscle relaxation.

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27
Q

What are examples of histamine’s actions on nonvascular smooth muscle?

A

Bronchioconstriction (H1) and intestine cramps and diarrhea (H1).

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28
Q

Which histamine receptor is involved in promoting gastric acid secretion?

A

H2.

29
Q

What is the effect of histamine binding to H1 receptors in the adrenal medulla and ganglia?

A

High concentration of histamine causes adrenal medullary discharge (epinephrine, catecholamines, etc)

30
Q

Which histamine receptor is involved with metabolic effects and what are these effects?

A

H3. Inhibits food intake; increases energy expenditure; reduces obesity.

31
Q

What is the “triple response” of an intradermal injection of histamine?

A

Erythema, wheal, and flare.

32
Q

Which histamine receptors are involved in the “triple response” of an intradermal injection of histamine?

A

Mostly H1; but also some H2 and H3.

33
Q

What effect does histamine have on the exocrine glands of the nasal and respiratory areas?

A

Binds to H1 and increases production of nasal and bronchial mucus.

34
Q

What are 4 clinical uses of histamine?

A

Bronchial hyperreactivity testing; integrity test of sensory nerves; assess ability of stomach to secrete acid; test for pheochromocytoma.

35
Q

What has replaced histamine in testing stomach acid secretion?

A

Pentagastrin is now used.

36
Q

How does epinephrine act as an histamine antagonist?

A

It quickly reverses histamine’s effects on smooth muscle (treat acute anaphylaxis).

37
Q

What is cromolyn?

A

A histamine release inhibitor and mast cell stabilizer.

38
Q

What is the mechanism of action of cromolyn?

A

Acts on pulmonary mast cells to 1) Inhibit release of histamine and other autacoids during allergic runs; 2) inhibit the function of cells.

39
Q

How does suppression via cromolyn work?

A

Cromolyn blocks membrane chloride channels.

40
Q

True or false: Cromolyn is not useful for skin allergies.

A

True, it does not inhibit mast cell degranulation in skin.

41
Q

True or false: Cromolyn is easily absorbed orally.

A

False. Cromolyn is poorly absorbed orally.

42
Q

How is cromolyn administered?

A

Either as a powder (inhalation), a liquid nasal spray (Nasalcrom). or an ophthalmic solution (Opticrom).

43
Q

What are the clinical uses of cromolyn?

A

Prophylactic treatment for bronchial asthma. Also for allergic rhinoconjuctivitis.

44
Q

How is Cromolyn excreted?

A

Unchanged in bile and urine.

45
Q

True or false: Cromolyn is ineffective in reversing asthmatic bronchospasm.

A

True.

46
Q

What is nedocromil?

A

A histamine release inhibitor and mast cell stabilizer.

47
Q

What is the mechanism of action of nedocromil?

A

Acts on pulmonary mast cells to inhibit release of histamine and other autacoids during allergic rxns; inhibits the function of cells.

48
Q

How does suppression via nedocromil work?

A

Blocks membrane chloride channels.

49
Q

What are some toxic effects of cromolyn?

A

Wheezing, bronchospasm. Rarely: laryngeal edema. Nasal solution may cause nasal stinging, burning, and irritation.

50
Q

How is nedocromil administered?

A

In aerosol form.

51
Q

What is the toxicity of nedocromil?

A

Minor: Throat irritation, cough, mouth dryness, chest tightness, and wheezing.

52
Q

What is the clinical use of nedocromil?

A

Prophylactic treatment for bronchial asthma.

53
Q

True or false: Nedocromil is ineffective in reversing asthmatic bronchospasm.

A

True.

54
Q

Adding Nedocromil to a standard dose of inhaled corticosteroid appears to improve what?

A

It improves the control of asthma.

55
Q

True or false: Cromolyn is more effective than Nedocromil in reducing bronchospasm caused by exercise or cold air.

A

False. Nedocromil is more effective at reducing bronchospasm caused by exercise of cold air.

56
Q

What is the mechanism of action of histamine antagonists?

A

They occupy receptors on the effector cells completely and reversibly, which stops histamine from initiating a response.

57
Q

What is the name of the H3 blocker currently still under research?

A

Clobenpropit.

58
Q

What are the first generation of H1 blockers derivatives of?

A

They are derivatives of ethyl amine.

59
Q

What are the characteristics of H1 receptor blockers?

A

Strong sedative effects; actions at autonomic receptors.

60
Q

What class of compounds does diphenhydramine belong to?

A

Ethanol amines

61
Q

What class of compounds does Chlorpheniramine belong to?

A

Alkylamines

62
Q

What class of compounds does Promethazine belong to?

A

Ethylene diamines.

63
Q

True or false: Alkylamines has slight sedation.

A

True.

64
Q

True or false; Ethanolamines have marked sedation.

A

True.

65
Q

What is a common component of OTC cold medication?

A

Chlorpheniramine (an alkylamine)

66
Q

True or false: Promethazine is used as a pre-operative drug.

A

True.

67
Q

Pyrilamine

A

An ethylaminediamine. Moderate sedation. Present in OTC sleep aids.

68
Q

Hydroxyzine

A

A piperzine derivative. Moderate sedation.

69
Q

Cyproheptadine.

A

Moderate sedation; anti-serotonin activity.

Year 2 (9 decks)

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