Histamine Antagonists Flashcards

1
Q

What are the types of histamine antagonists

A

Physiologic antagonists
Release inhibitors (mast cell stabilizers)
Receptor blockers

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2
Q

What is the physiologic antagonist

A

Adrenaline - opposite action, different receptor

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3
Q

What is the mast cell stabilizer

A
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4
Q

Which receptors can be blocked by receptor blockers

A

H1
H2

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5
Q

Explain H1 antagonists

A

Antihistamines
Inverse agonists

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6
Q

What are the two types of H1 receptor antagonists

A

First and second generation

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7
Q

List the first generation H1 receptor antagonists

A
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8
Q

List the second generation H1 receptor antagonists

A
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9
Q

What is the difference between first and second generation of H1 receptor antagonists

A

First generation is more lipophilic so will go to CNS
more side effects

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10
Q

Explain the absorption of H1 receptor antagonists

A
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11
Q

Explain the distribution of H1 receptor antagonists

A
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12
Q

Explain metabolism of H1 receptor antagonists

A
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13
Q

What are the pharmacological effects of H1 receptor antagonists

A
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14
Q

Explain the anticholinergic effects of H1 receptor antagonists

A
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15
Q

What is the effect of cyproheptadine

A

Significant anti serotonin activity

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16
Q

Explain effect of promethazine

A

Alpha block activity
Postural hypotension

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17
Q

What is more potent than procaine as local anesthetics

A

Diphenhydramine and promethazine

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18
Q

What are the therapeutic uses of H1 receptor antagonists

A

Allergic diseases
Common cold
Motion sickness, vertigo and sedation
Sedative, anxiolytic

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19
Q

Explain the allergic diseases as the therapeutic use of histamine antagonists

A
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20
Q

Explain the common cold as the therapeutic use of histamine antagonists

A
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21
Q

What is scopolamine

A

The most effective for prevention of motion sickness, vertigo, and sedation

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22
Q

Which H1 antagonists are useful for milder cases of motion sickness, vertigo, and sedation

A
23
Q

Explain promethazine

A
24
Q

Why are some H1 receptor antagonists used as hypnotics

A
25
Q

What is used as anxiolytic

A
26
Q

What is used for insomnia

A
27
Q

What are the adverse effects related to CNS of H1 receptor antagonists ?

A

Sedation
Dizziness
Tinnitus
In coordination
Fatigue
Blurred vision
Euphoria
Nervousness
Insomnia
Tremors

28
Q

Which are the side effects if H1 receptor antagonists that can be reduced by taking drug with meals

A

Nausea
Vomiting
Epigastric distress
Constipation or diarrhea

29
Q

What can cause weight gain

A
30
Q

What are the side effects of some first generation H1 antagonists

A

Dryness of the mouth and respiratory passages (inducing cough)
Urinary retention of frequency
Dysuria

31
Q

What is preferred for elderly patients

A
32
Q

What are not recommended for use in children

A
33
Q

What have been approved by FDA for use in children

A
34
Q

H1 histamines are advised with caution to who

A
35
Q

What is the effect of lactating women taking antihistamines

A
36
Q

What are the members of H2 receptor antagonists

A

Cimetidine
Ranitidine
Famotidine
Nizatidine

37
Q

What are H2 receptors antagonists known as

A

Antisecretory agents

38
Q

What is the action of H2 receptor antagonists

A
39
Q

What are the uses of H2 receptor antagonists

A
40
Q

What do the proton pump inhibitors do

A
41
Q

What is the mechanism involved in antacid healing of peptic ulcer

A
42
Q

Explain the absorption of H2RAs

A
43
Q

Explain the elimination of H2RAs

A
44
Q

Explain the bioavailability of H2RAs

A
45
Q

Explain the renal clearance in H2RAs

A
46
Q

What are the types of adverse effects of H2RAs

A

Gynecomastia and impotence
Hematopoietic and immune effects
CNS effects
Hepatic effects
Cardiac effects
Renal effects
Other

47
Q

Explain gynecomastia and impotence as adverse effects of H2RAs

A
48
Q

Explain hematopoietic and immune effects as adverse effects of H2RAs

A
49
Q

Explain the CNS effects as adverse effects of H2RAs

A
50
Q

Explain hepatic effects as adverse effects of H2RAs

A
51
Q

Explain the cardiac effects as adverse effects of H2RAs

A
52
Q

Explain the renal effects as adverse effects of H2RAs

A
53
Q

Explain the other adverse effects of H2RAs

A