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Histamine and Seretonin Antagonists Flashcards

1
Q

H1 distribution?

A

Smooth muscle, endothelium, brain

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2
Q

H1 mxn?

A

Gq

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3
Q

H2 distribution?

A

Gastric mucosa, cardiac muscle, mast cells, brain

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4
Q

H2 mxn?

A

Gs

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5
Q

H3 distribution?

A

Presynaptic brain

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6
Q

H3 mxn?

A

Gi

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7
Q

H4 distribution?

A

Eosinophils, neutrophils, CD4

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8
Q

H4 mxn?

A

Gi

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9
Q

Histamine on cardiovascular?

A

Immediate hypotension due to peripheral vasodilation (H1,2) – Anyphlactic shock; Increase vascular permeability (H1); Direct cardiac increase in contractility, rate (H2) – minor

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10
Q

Histamine on bronchiolar smooth muscle?

A

Bronchoconstrict (H1) – Hyperreaction in asthmatics

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11
Q

Histamine on GI?

A

Diarrhea via contraction (H1), Stimulates gastric acid, pepsin, intrinsic factor (H2)

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12
Q

Histamine on nervous system?

A

Stimulant of nerve endings: Pain (dermis) + Itching (epidermis) (H1); H3 feedback inhibition

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13
Q

5 general properties of H1 antagonists?

A

Rapidly absorbed with oral (1-2 hr peak), Widely distributed (older ones enter CNS), Rapidly metabolized via liver microsomes, Many non-Rx, Many actions not ascribable to H1 (promiscuous)

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14
Q

Diphenhydramine class and mxn?

A

Ether/Ethanolamine derivative, H1 antagonist

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15
Q

AKA Diphenhydramine?

A

Benadryl

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16
Q

AKA Benadryl?

A

Diphenydramine

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17
Q

Diphenhydramine for?

A

Anti-muscarinic, sedating (Tylenol PM, etc)

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18
Q

H1 receptor antagonists for?

A

Allergic reactions (allergic rhinitis urticaria, conjunctivitis – NOT colds, bronchocontriction), motion sickness, N/V in pregnancy, sleep aids

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19
Q

H1 receptor antagonist side effects?

A

Sedation, anti-muscarinic action, poisoning (esp children) with convulsions, allergy, local anasthesia

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20
Q

Tripelennamine class and mxn?

A

Ethylenediamine derivative, H1 receptor antagonist

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21
Q

Tripelennamine for?

A

OTC sleep aid

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22
Q

Cyclizine/Meclizine class and mxn?

A

Piperazine derivative, H1 receptor antagonist

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23
Q

Cyclizine/Meclizine for?

A

Motion sickness

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24
Q

Promethazine class and mxn?

A

Phenothiazine derivative,H1 receptor antagonist

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25
Q

Promethazine for?

A

Antiemetic (suppress chemoreceptor trigger zone)

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26
Q

Promethazine side effects?

A

Anti-muscarinic, Marked sedation

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27
Q

Chlorpheniramine class and mxn?

A

Alkylamine derivative, H1 receptor antagonist

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28
Q

Chlorpheniramine for?

A

Component of “cold” medication

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29
Q

Chlorpheniramine side effects?

A

Less sedating, often in “daytime” meds

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30
Q

Loratadine class and mxn?

A

Piperidine derivative, 2nd gen H1 receptor antagonist

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31
Q

Loratadine for?

A

Allergic rhinitis

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32
Q

Loratadine side effects?

A

No sedation, Cardiovascular effects rarely at high doses

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33
Q

Fexofenadine class and mxn?

A

Piperidine derivative, 2nd gen H1 receptor antagonist

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34
Q

Fexofenadine for?

A

Allergic rhinitis

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35
Q

Fexofenadine side effects?

A

No sedation, Cardiovascular effects rarely at high doses

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36
Q

Piperidine derivatives?

A

Loratadine, Fexofenadine

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37
Q

AKA Claritin?

A

Loratadine

38
Q

AKA Fexofenadine?

39
Q

AKA Allegra?

A

Fexofenadine

40
Q

AKA Loratadine?

41
Q

Piperidine derivatives cross BBB? Consequences?

A

No, so fewer central and overall side effects

42
Q

Piperidine timing versus 1st gen H1 receptor antagonists?

A

Longer acting, so can be used 1 daily

43
Q

Azelastine mxn?

A

2nd gen H1 receptor antagonist

44
Q

Cetirizine mxn?

A

2nd gen H1 receptor antagonist

45
Q

AKA Cetirizine?

46
Q

AKA Zyrtec?

A

Cetirizine

47
Q

Azelastine for?

A

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

48
Q

Azelastine side effects?

A

No sedation, crosses BBB poorly so less side effects in general

49
Q

Cetirizine for?

A

Allergic rhinitis

50
Q

Cetirizine often in combo with?

A

Pseudoephedrine

51
Q

Cetirizine side effects?

A

No sedation, crosses BBB poorly so less side effects in general

52
Q

H2 receptor antagonists?

A

Cimetidine, Ranitidine, Famotidine, Nizatidine

53
Q

1st gen H1 receptor antagonists?

A

Diphenyhydramine, Tripelennamine, Cyclizine/Meclizine, Promethazine, Chlorpheniramine

54
Q

2nd gen H1 rec antagonists?

A

Loratadine, Fexofenadine, Azelastine, Cetirizine

55
Q

Cimetidine mxn?

A

H2 receptor antagonist; block gastric acid secretion, more so with nocturnal than meal

56
Q

Ranitidine mxn?

A

H2 receptor antagonist; block gastric acid secretion, more so with nocturnal than meal

57
Q

Famotidine mxn?

A

H2 receptor antagonist; block gastric acid secretion, more so with nocturnal than meal

58
Q

Nizatidine mxn?

A

H2 receptor antagonist; block gastric acid secretion, more so with nocturnal than meal

59
Q

Cimetidine for?

A

Dyspepsia, duodenal and gastric ulcers, hypersecretory conditions (Zollinger Ellison gastrin-secreting tumor)

60
Q

Ranitidine for?

A

Dyspepsia, duodenal and gastric ulcers, hypersecretory conditions (Zollinger Ellison gastrin-secreting tumor)

61
Q

Famotidine for?

A

Dyspepsia, duodenal and gastric ulcers, hypersecretory conditions (Zollinger Ellison gastrin-secreting tumor)

62
Q

Nizatidine for?

A

Dyspepsia, duodenal and gastric ulcers, hypersecretory conditions (Zollinger Ellison gastrin-secreting tumor)

63
Q

Cimetidine side effects?

A

Most side effects of H2 blockers: Antiandrogen (impotence and gynecomastia), inhibition of P450

64
Q

Ranitide side effect?

A

Liver toxicity

65
Q

Least side effects of H2 blockers?

A

Nizatadine

66
Q

H2 blockers that will not inhibit P450?

A

Famotidine, Nizatidine

67
Q

All H2 blockers can cause?

A

CNS dysfunction (confusion, slurred speech)

68
Q

Cyproheptadine class?

A

Antihistaminic & Antiserotinergic

69
Q

Cyproheptadine for?

A

Skin allergies (urticaria, anti H1), Diarrhea of carcinoid (anti-5HT2)

70
Q

Cyproheptadine side effects?

A

Sedation, antimuscarinic

71
Q

Ketanserin mxn?

A

Selective 5HT2a,2C receptor antagonist, as well as Alpha 1 and H1 antagonist

72
Q

Ketanserin for?

A

Antihypertensive (relaxes vascular and tracheal muscle), Antiplatelet aggregation

73
Q

Is Ketanserin available in the U.S.?

74
Q

Odansetron mxn?

A

5HT3 receptor antagonist

75
Q

Odansetron for?

A

N/V with chemo

76
Q

Ergot alkaloid mxn?

A

Agonist and antagonist actions at 5HT and alpha adrenergic receptors

77
Q

Ergot alkaloids side effects?

A

Powerful hallucinations, smooth muscle contraction (vascular and uterine)

78
Q

Ergotamine class and mxn?

A

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

79
Q

Ergotamine for?

A

Prodrome of migranes

80
Q

Ergotamine side effects?

A

N/V, cumulative and prolonged vasoconstriction

81
Q

Methysergide class and mxn?

A

Ergot alkaloid; Partial agonist at all 5HT1 receptors, antagonist at 5HT2

82
Q

Methysergide for?

A

Prophylaxis of migranes

83
Q

Methysergide side effects?

A

GI disturbances, inflammatory fibrosis (chronic use), hallucinations, withdrawn from market

84
Q

Ergonovine class and mxn?

A

Ergot alkaloid, sustains uterine contraction

85
Q

Ergonovine for?

A

postpartum hemorrhage

86
Q

Bromocriptine class and mxn?

A

Ergot alkaloid, dopamine agonist

87
Q

Bromocriptine for?

A

Hyperprolactinemia

88
Q

Triptans class and mxn?

A

Non-ergot serotonin analogs; 5HT1B,D receptor agonist

89
Q

Triptans for?

A

Effective (70%) migraine treatment in 1-2 hours

90
Q

Name 4 triptans.

A

Sumatriptan, naratriptan, rizatriptan, zolmitriptan

91
Q

Triptan mxn?

A

activation of 5HT1B,D in cerebral blood vessels producing vasoconstriction; “ “ on trigeminal nerve endings to inhibit the release of pro-inflammatory neuropeptides

Pharmacology (46 decks)

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