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2nd U2 Pharm > Histamine, serotonin, and Antagonists > Flashcards

Histamine, serotonin, and Antagonists Flashcards

1
Q

What are the main uses for H1 receptor antagonists?

A

Allergic reactions
motion sickness
N/V in pregnancy
sleep aids

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2
Q

Name the 5 H1 receptor antagonists…

A 
Diphenhydramine
Tripelennamine
Meclizine/Hydroxyzine
Promethazine
Chlorpheniramine
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3
Q

What are the major side effects of the H1 receptor antagonists?

A 
Sedation
anti-muscarinic action
poisoning with convulsions
allergy
local anesthesia
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4
Q

H1 receptor antagonist used as an OTC sleep aid?

A

Tripelennamine

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5
Q

H1 receptor antagonist used for motion sickness?

A

Meclizine

Hydroxyzine

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6
Q

H1 receptor antagonist used as an antiemetic (N/V treatment)?

A

Promethazine

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7
Q

H1 receptor antagonist used as a component of cold medications?

A

Chlorpheniramine

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8
Q

Name the 4 2nd generation H1 receptor antagonists?

A

Loratadine
Fexofenadine
Azelastine
Cetirizine

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9
Q

What are the 2 2nd generation H1 receptor antagonist in the piperidine derivative class?

A

Loratadine

Fexofenadine

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10
Q

What is so special about the 2nd generation H1 receptor antagonists?

A

Poorly cross the BBB–fewer central side effects

No sedation effects

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11
Q

What is the primary use of all 4 2nd generation H1 receptor antagonists?

A

Allergic rhinitis

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12
Q

What 2 2nd generation H1 receptor antagonist can cause cardiovascular effects at high doses?

A

Loratadine

Fexofenadine

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13
Q

What is the mechanism of action of the H2 receptor antagonists?

A

Block gastric acid secretion–more so with nocturnal acid secretion than meal secretion

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14
Q

What are the 4 H2 receptor antagonists?

A

Cimetidine
Ranitidine
Famotidine
Nizatidine

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15
Q

What are the 3 uses for the H2 receptor antagonists?

A

Dyspepsia
duodenal and gastric ulcers
hypersecretory conditions

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16
Q

Which of the H2 receptor antagonist have the worst side effect, which include anti androgen (causing impotence and gynecomastia) and inhibition of the P450 enzymes?

A

Cimetidine

17
Q

What is the one major side effect of Ranitidine?

A

Liver toxicity

18
Q

Which of the H2 receptor antagonist have the least side effects?

A

Nizatidine

19
Q

What are the two mechanisms of cyproheptadine?

A

Antihistaminic

Antiserotinergic

20
Q

What are the uses of cyproheptadine?

A

Skin allergies–urticaria, anti-5HT1

Diarrhea of carcinoid syndrome-anti-5HT2

21
Q

What are the mechanisms of ketanserin?

A

Selective 5HT2A,2C receptor antagonist

a1 and H1 receptor antagonist

22
Q

What are the uses of ketanserin?

A

Antihypertensive

antiplatelet aggregation

23
Q

What is the mechanism of Odansetron and Granisetron?

A

5HT3 receptor antagonist

24
Q

What are the uses of odansetron and granisetron?

A

N/V in chemo and postop patients

25
Q

What are the mechanisms of action for the ergot alkaloids?

A

Agonist and antagonist actions at 5HT and a-adrenergic receptors

26
Q

What are the side effects seen with ergot alkaloids?

A

Powerful hallucinations

smooth muscle contraction–vascular and uterine

27
Q

What are the 4 ergot alkaloids?

A

Ergotamine
Methysergide
Ergonovine
Bromocriptine

28
Q

Ergot alkaloid that is a nonspecific partial agonist at all 5HT 1,2 receptors and partial agonist at a-adrenergic receptors…

A

Ergotamine

29
Q

Ergot alkaloid that is a partial agonist at all 5HT1 receptors and antagonist at 5HT2…

A

Methysergide

30
Q

Ergot alkaloid that is a dopamine agonist…

A

Bromocriptine

31
Q

What ergot alkaloid is used at the start of a migraine?

A

Ergotamine

32
Q

What ergot alkaloid is used as a prophylaxis for migraines?

A

Methysergide

33
Q

What ergot alkaloid is used for the treatment of postpartum hemorrhage?

A

Ergonovine

34
Q

Which ergot alkaloid is used for the treatment of hyperprolactinemia?

A

Bromocriptine

35
Q

A non-ergot serotonin analog that is a 5HT1B,D receptor agonist used for migraine treatment?

A

Triptans

2nd U2 Pharm (9 decks)

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