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PHARMA > HISTAMINE AND CORTICOSTEROIDS > Flashcards

HISTAMINE AND CORTICOSTEROIDS Flashcards

1
Q

Histamine

A
  1. Chemical messenger mostly generated in mast cells
  2. Mediates a wide range of cellular responses
    ○ Allergic and inflammatory reactions
    ○ Gastric secretion
    ○ Neurotransmission in parts of the brain
  3. One of the earliest mediator released during allergies and
    anaphylaxis
  4. Involved in Type 1 Hypersensitivity
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2
Q

Present in practically all tissue

A

Histamine

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3
Q

Histamine is found in significant amount in

A

Lungs, skin, blood vessels and
GI tract

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4
Q

Massive histamine release

A

Anaphylaxis

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5
Q

Histamine is found at high concentration in

A

Mast cells and basophils

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6
Q

Function of histamine in brain

A

Neurotransmitter

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7
Q

Formed by the __________ of the amino acid _________
by the enzyme _________ _____________

A

decarboxylation, histidine, histidine decarboxylase

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8
Q

Histamine precursor

A

Histidine

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9
Q

Decarboxylation of histamine

A

Decarboxylation→ liberate the carbon dioxide→
amine group will remain

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10
Q

Histamine binds to what type of receptors

A

H1, H2, H3, H4

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11
Q

Widely expressed and clinically relevant

A

H1 and H2

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12
Q

Histamine promotes ___________ by causing vascular endothelium to release ______ _______

A

Vasodilation, nitric oxide

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13
Q

Vasodilation caused by NO results to

A
  1. Increase in blood vessel caliber →
    laminar flow→ decreased in pressure (blood
    pressure)
  2. Promotes severe vasodilation capable of
    producing shock
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14
Q

Histamine enhance the secretion of

A

Pro-inflammatory cytokines

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15
Q

Pro-inflammatory cytokines

A

IL1, IL5, IL6, IL8, TNF

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16
Q

Histamine is stored in

A

Mast cells and basophils

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17
Q

Immunologic Release:
If sensitized by ___ ________ attached to their surface membranes, ____ _____ and _________ __________ explosively when exposed to the appropriate antigen

A

IgE antibodies, mast cells and basophils degranulate

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18
Q

Amines that competitively inhibit histamine by displacing it from its bound form

A

Morphine and tubocurarines

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19
Q

Receptor in smooth muscle

A

H1

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20
Q

Receptor in gastric mucosa

A

H2

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21
Q

Receptors found both in the brain

A

H1 and H2

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22
Q

Receptors with CNS role and plexuses

A

H3 and H4

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23
Q

H1 post receptor mechanism

A

H1→ IP3, DAG

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24
Q

H1 distribution

A

Smooth muscle, endothelium, brain

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25
Q

H1 partially selective agonist

A

Histaprodifen

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26
Q

H1 partially selective antagonists or inverse agonists

A

Mepyramine, triprolidine, cetirizie

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27
Q

H2 distribution

A

Gastric mucosa, cardiac muscle, mast cells, brain

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28
Q

H2 partially selective agonist

A

Amthamine

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29
Q

H2 partially selective antagonists or inverse agonists

A

Cimetidine, ranitidine, tiotidine

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30
Q

H3 distribution

A

presynaptic autoreceptors and heteroreceptors; brain, myenteric plexus, other neurons

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31
Q

H3 partially selective agonist

A

R-a-methylhistamine, imetit, immepip

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32
Q

H3 partially selective antagonists or inverse agonists

A

Thioperamide, iodophenpropit, clobenpropit, tioptrolisant, proxyfan

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33
Q

H4 distribution

A

Eosinophils, neutrophils, CD4 T cells

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34
Q

H4 partially selective agonist

A

Clobenpropit, imetit, clozapine

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35
Q

H4 partially selective antagonists or inverse agonists

A

Thioperamide

36
Q

H1 actions

A

Exocrine secretion, Bronchial Smooth Muscle, Intestinal Smooth Muscle, Sensory Nerve
Endings

37
Q

Exocrine Secretion

A

Increased production of nasal and
bronchial mucus, resulting in
respiratory symptoms

38
Q

Bronchial Smooth
Muscle

A

Constriction of bronchioles results
in symptoms of asthma and
decreased lung capacity

39
Q

Intestinal Smooth
Muscle

A

Constriction results in intestinal
cramps and diarrhea

40
Q

Sensory Nerve
Endings

A

Causes itching and pain

41
Q

H1 and H2 actions in

A

CVS and skin

42
Q

CVS action of H1 and H2

A
  1. Reduced peripheral resistance = low systemic BP
  2. (+) chronotropism (heart rate; H2-mediated)
  3. (-) inotropism (myocardial contractility)
43
Q

Skin action of H1 and H2

A
  1. Dilation and increased
    permeability of the capillaries
    ○ Results in leakage of proteins
    and fluid into the tissues
    ○ Transcellular shift from intravascular to the interstitial→ edema
  2. Results in Triple Response
    ○ Wheal formation
    ○ Reddening due to local vasodilation
    ○ Flare (Halo)
44
Q

Stomach action of H2

A

Stimulation of gastric
hydrochloric acid secretion

45
Q

Have smooth muscle actions opposite to those of histamine
→ act at different receptors

A

Antihistamines (physiologic antagonist)

46
Q

Epinephrine

A

■ Promotes vasoconstriction
■ Stimulation of α1 → α1 is for vasoconstriction
■ Inhibition of α2 → α2 is for vasodilation
■ Stimulates β1 → ↑ heart rate
■ Stimulates β2 → promoting bronchodilation
■ Stimulates β3 → promoting glycolysis
■ For anaphylaxis

47
Q

Release inhibitors

A

Reduce the degranulation of mast cells

48
Q

Examples of release inhibitors

A

Cromolyn and Nedocromil

49
Q

Cromolyn and Nedocromil

A

■ For cough and asthma
■ Mast cells stabilizers→ control release of histamine

50
Q

Receptor antagonist

A

Reduction of histamine-mediated responses

51
Q

H1-Receptor Antagonists

A

● Competitively block the histamine or act as inverse agonists at H1 receptors
○ Prevention of vasodilation and other inflammatory reactions

52
Q

H1-Receptor Antagonists actions

A

● Sedation
● Antinausea and antiemetic actions
● Antiparkinsonism effects
● Antimuscarinic actions
● Adrenoreceptor-blocking actions
● Serotonin-blocking actions
● Local anesthesia
○ First-generation H1 antagonists are potent local anesthetics

53
Q

Sedation

A

○ Common effect of first-generation H1-antagonists
○ Benadryl
■ Antihistamine with sedating effect

54
Q

Antinausea and antiemetic drug

A

Doxylamine

55
Q

Antiparkinsonism drug

A

Diphenhydramine

56
Q

Antimuscarinic

A

Ethanolamine and Ethylenediamine subgroup

57
Q

Adrenoreceptor-blocker

A

Promethazine

58
Q

Serotonin-blocker

A

Cyproheptadine

59
Q

Anticholinergic activity

A

● Controls secretion
● Anti GI and GU

60
Q

Diphenhydramine

A

● Promote dry mouth and constipation
● Anti-motion sickness activity
● Marked sedation
○ Groggy

61
Q

Alkylamines

A

● Brompheniramine
○ Dimetapp (dropper for kids)
● Chlorpheniramine
○ Slight sedating effect
○ Over-the-counter cold medication
○ Generic name of Bioflu
■ Phenylephrine + chlorphenamine maleate

62
Q

Phenothiazine derivative

A

Promethazine

63
Q

Hydroxyzine

A

● Atarax
● Not available in the market
● Anti-allergy that is stronger than Cetirizine but not as strong as Diphenhydramine
● Levocetirizine → Cetirizine → Hydroxyzine → Diphenhydramine
● The older the generation of antihistamine the greater the sedative effect

64
Q

Second generation antihistamines have some ____ sedating

A

mild

65
Q

2nd gen antihistamine that is the safest, minimal sedating, longer action

A

Loratadine

66
Q

Often the first drug used to
prevent or treat the symptoms of allergic reactions

A

H1 antihistaminic agents

67
Q

Used mainly for the treatment of allergic rhinitis and chronic urticaria

A

Second-generation H1 antagonists

68
Q

Motion Sickness and Vestibular Disturbances:
Most effective agents available for the prevention of motion sickness

A

Scopolamine and certain first-generation H1 antagonists

69
Q

Drugs for Nausea and Vomiting of Pregnancy

A

Doxylamine, an ethanolamine H1 antagonist

70
Q

1st gen drugs with marked potential for producing sedation

A

Brompheniramine
Chlorpheniramine
Clemastine
Cyproheptadine
Diphenhydramine
Doxylamine
Hydroxyzine
Promethazine

71
Q

1st gen drugs used to treat motion sickness

A

Cyclizine
Diphenhydramine
Dimenhydrinate
Hydroxyzine
Meclizine
Promethazine

72
Q

2nd gen drugs with weak potential for producing sedation

A

Cetirizine
Lovecetirizine

73
Q

Non-sedating 2nd gen drugs

A

Desloratadine
Loratadine
Fexofenadine

74
Q

Promethazine prevents ____-_______ receptors thereby producing _______, ________, and ______
________

A

alpha-adrenergic
hypotension, dizziness, and reflex
tachycardia

75
Q

If anticholinergic receptors are prevented, it will produce

A

Dry mouth, urinary retention, and sinus tachycardia

76
Q

Anti-serotonin that increases
appetite

A

Cyproheptadine

77
Q

Their chief clinical use is as inhibitors of gastric acid secretion in the treatment of ulcers and heartburn

A

H2-Receptor Antagonists

78
Q

The four H2 receptor blockers

A

Cimetidine
Ranitidine
Famotidine
Nizatidine

79
Q

Cimetidine

A

■ No longer widely used
■ Promotes gynecomastia and hirsutism
■ Promotes drug-to-drug interactions in CYP liver enzymes

80
Q

Ranitidine

A

Most commercially available

81
Q

Famotidine

A

Longest acting and most potent

82
Q

H3-selective ligands may be of value

A

Sleep disorders, narcolepsy, obesity, and cognitive and psychiatric disorders

83
Q

An inverse H3-receptor agonist shown to reduce sleep cycles in mutant mice and in humans with narcolepsy

A

Tiprolisant

84
Q

Side effect of H1 and H3 receptor in
mice

A

Increased obesity

85
Q

H1 receptor affects serotonergic pathway →

A

↑ appetite → obesity

85
Q

Have potential in chronic inflammatory conditions, such as asthma in which eosinophils and mast cells play a prominent role

A

H4-receptor Blockers

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