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Pharm U2 > 7) Histamine, Serotonin, and Antagonists > Flashcards

7) Histamine, Serotonin, and Antagonists Flashcards

1
Q

What is the mechanism for H1 receptor antagonist

A

H1 receptor antagonist; rapidly absorbed orally, widely distributed, rapidly metabolized via liver microsomes

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2
Q

What are the therapeutics for H1 receptor antagonist

A

Allergic reactions, motion sickness, nausea and vomiting in pregnancy, sleep aids

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3
Q

What are the important side effects for H1 receptor antagonist

A

Sedation, anti-muscarinic action, poisoning (especially children) with convulsions, allergy, local anesthesia

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4
Q

What are the miscellaneous for H1 receptor antagonist

A

Older agents cross CNS to cause central effects

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5
Q

What is the class for Diphenhydramine (Benadryl)

A

Ether/ethanolamine derivitive

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6
Q

What is the mechanism for Diphenhydramine (Benadryl)

A

H1 receptor antagonist

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7
Q

What are the important side effects for Diphenhydramine (Benadryl)

A

Anti-muscarinic, sedating

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8
Q

What is the class for Tripelennamine (Pyribenzamine)

A

Ethylenediamine derivitive

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9
Q

What is the mechanism for Tripelennamine (Pyribenzamine)

A

H1 receptor antagonist

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10
Q

What are the therapeutics for Tripelennamine (Pyribenzamine)

A

OTC sleep aid

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11
Q

What is the class for Cyclizine (Marezine)

A

Piperazine derivative

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12
Q

What is the mechanism for Cyclizine (Marezine)

A

H1 receptor antagonist

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13
Q

What are the therapeutics for Cyclizine (Marezine)

A

Motion sickness

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14
Q

What is the class for Promethazine (Phenergan)

A

Phenothiazine derivative

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15
Q

What is the mechanism for Promethazine (Phenergan)

A

H1 receptor antagonist

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16
Q

What are the therapeutics for Promethazine (Phenergan)

A

Antiemetic

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17
Q

What are the important side effects for Promethazine (Phenergan)

A

Anti-muscarinic, sedating

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18
Q

What is the class for Chlorpheniramine (Chlor-Trimeton)

A

Alkylamine derivitive

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19
Q

What is the mechanism for Chlorpheniramine (Chlor-Trimeton)

A

H1 receptor antagonist

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20
Q

What are the therapeutics for Chlorpheniramine (Chlor-Trimeton)

A

Component of “cold” medications

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21
Q

What are the important side effects for Chlorpheniramine (Chlor-Trimeton)

A

Less sedating

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22
Q

What is the class for Loratadine (Claritin)

A

Piperidine derivitive

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23
Q

What is the mechanism for Loratadine (Claritin)

A

2nd generation H1 receptor antagonist

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24
Q

What are the therapeutics for Loratadine (Claritin)

A

Allergic rhinitis

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25
Q

What are the important side effects for Loratadine (Claritin)

A

No sedation

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26
Q

What are the other side effects for Loratadine (Claritin)

A

Cardiovascular effects (rare, with high doses)

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27
Q

What are the miscellaneous for Loratadine (Claritin)

A

Poorly crosses BBB, so fewer central and side effects

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28
Q

What is the class for Fexofenadine (Allegra)

A

Piperidine derivitive

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29
Q

What is the mechanism for Fexofenadine (Allegra)

A

2nd generation H1 receptor antagonist

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30
Q

What are the therapeutics for Fexofenadine (Allegra)

A

Allergic rhinitis

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31
Q

What are the important side effects for Fexofenadine (Allegra)

A

No sedation

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32
Q

What are the other side effects for Fexofenadine (Allegra)

A

Cardiovascular effects (rare, with high doses)

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33
Q

What are the miscellaneous for Fexofenadine (Allegra)

A

Poorly crosses BBB, so fewer central and side effects

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34
Q

What is the mechanism for Azelastine (Astelin)

A

2nd generation H1 receptor antagonist

35
Q

What are the therapeutics for Azelastine (Astelin)

A

Allergic rhinitis (intranasal spray), allergic conjunctivitis (ophthalmic solution)

36
Q

What are the important side effects for Azelastine (Astelin)

A

No sedation

37
Q

What are the miscellaneous for Azelastine (Astelin)

A

Poorly crosses BBB, so fewer central and side effects

38
Q

What is the mechanism for Cetirizine (Zyrtec)

A

2nd generation H1 receptor antagonist

39
Q

What are the therapeutics for Cetirizine (Zyrtec)

A

Allergic rhinitis

40
Q

What are the important side effects for Cetirizine (Zyrtec)

A

No sedation

41
Q

What are the miscellaneous for Cetirizine (Zyrtec)

A

Poorly crosses BBB, so fewer central and side effects

42
Q

What is the mechanism for Cimetidine (Tagamet)

A

H2 receptor antagonist; blocks gastric acid secretion (more so with nocturnal acid secretion than meal secretion)

43
Q

What are the therapeutics for Cimetidine (Tagamet)

A

Dyspepsia, duodenal and gastric ulcers, hypersecretory conditions

44
Q

What are the important side effects for Cimetidine (Tagamet)

A

Antiandrogen (causing impotence and gynecomastia), inhibition of P450 enzymes

45
Q

What are the other side effects for Cimetidine (Tagamet)

A

CNS dysfunction possible

46
Q

What are the miscellaneous for Cimetidine (Tagamet)

A

Most side effects of H2-blocker class

47
Q

What is the mechanism for Ranitidine (Zantac)

A

H2 receptor antagonist; blocks gastric acid secretion (more so with nocturnal acid secretion than meal secretion)

48
Q

What are the therapeutics for Ranitidine (Zantac)

A

Dyspepsia, duodenal and gastric ulcers, hypersecretory conditions

49
Q

What are the important side effects for Ranitidine (Zantac)

A

Liver toxicity

50
Q

What are the other side effects for Ranitidine (Zantac)

A

CNS dysfunction possible

51
Q

What is the mechanism for Famotidine (Pepcid)

A

H2 receptor antagonist; blocks gastric acid secretion (more so with nocturnal acid secretion than meal secretion)

52
Q

What are the therapeutics for Famotidine (Pepcid)

A

Dyspepsia, duodenal and gastric ulcers, hypersecretory conditions

53
Q

What are the other side effects for Famotidine (Pepcid)

A

CNS dysfunction possible

54
Q

What is the mechanism for Nizatidine (Axid)

A

H2 receptor antagonist; blocks gastric acid secretion (more so with nocturnal acid secretion than meal secretion)

55
Q

What are the therapeutics for Nizatidine (Axid)

A

Dyspepsia, duodenal and gastric ulcers, hypersecretory conditions

56
Q

What are the other side effects for Nizatidine (Axid)

A

CNS dysfunction possible

57
Q

What are the miscellaneous for Nizatidine (Axid)

A

Least side effects of H2-blocker class

58
Q

What is the mechanism for Cyproheptadine (Periactin)

A

Antihistaminic and antiserotinergic

59
Q

What are the therapeutics for Cyproheptadine (Periactin)

A

Skin allergies (urticaria, anti-5HT1), diarrhea of carcinoid syndrome (anti-5HT2)

60
Q

What are the other side effects for Cyproheptadine (Periactin)

A

Sedation, antimuscarinic

61
Q

What is the mechanism for Ketanserin

A

Selective 5HT2A,2C receptor antagonist, as well as ?1 and H1 receptor antagonist

62
Q

What are the therapeutics for Ketanserin

A

Antihypertensive (relaxes vascular and tracheal smooth muscle), antiplatelet aggregation

63
Q

What is the mechanism for Odansetron (Zofran)

A

5HT3 receptor antagonist

64
Q

What are the therapeutics for Odansetron (Zofran)

A

Nausea and vomiting in chemotherapy

65
Q

What is the mechanism for Ergot alkaloids

A

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

66
Q

What are the important side effects for Ergot alkaloids

A

Powerful hallucinations, smooth muscle contraction (vascular and uterine)

67
Q

What is the class for Ergotamine (Ergomar)

A

Ergot alkaloid

68
Q

What is the mechanism for Ergotamine (Ergomar)

A

Nonspecific partial agonist at all 5HT1,2 receptors; partial agonist at ?-adrenergic receptors

69
Q

What are the therapeutics for Ergotamine (Ergomar)

A

Prodrome of migraines

70
Q

What are the other side effects for Ergotamine (Ergomar)

A

N/V, cumulative and prolonged vasoconstriction

71
Q

What is the class for Methysergide (Cycloset)

A

Ergot alkaloid

72
Q

What is the mechanism for Methysergide (Cycloset)

A

Partial agonist at all 5HT1 receptors, antagonist at 5HT2

73
Q

What are the therapeutics for Methysergide (Cycloset)

A

Prophylaxis of migraines

74
Q

What are the other side effects for Methysergide (Cycloset)

A

GI disturbances, inflammatory fibrosis (chronic use), hallucinations

75
Q

What are the miscellaneous for Methysergide (Cycloset)

A

Withdrawn from U.S. market

76
Q

What is the class for Ergonovine

A

Ergot alkaloid

77
Q

What are the therapeutics for Ergonovine

A

Postpartum hemorrhage (Oxytocic)

78
Q

What is the class for Bromocriptine (Sansert)

A

Ergot alkaloid

79
Q

What is the mechanism for Bromocriptine (Sansert)

A

Dopamine agonist

80
Q

What are the therapeutics for Bromocriptine (Sansert)

A

Hyperprolactinemia

81
Q

What is the class for Triptans

A

Non-ergot serotonin analogs

82
Q

What is the mechanism for Triptans

A

5HT1B,D receptor agonist

83
Q

What are the therapeutics for Triptans

A

Effective (70%) migraine treatment

Pharm U2 (11 decks)

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