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Pharmacology > Histamine and Seretonin Antagonists > Flashcards

Histamine and Seretonin Antagonists Flashcards

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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
Promethazine for?
Antiemetic (suppress chemoreceptor trigger zone)
26
Promethazine side effects?
Anti-muscarinic, Marked sedation
27
Chlorpheniramine class and mxn?
Alkylamine derivative, H1 receptor antagonist
28
Chlorpheniramine for?
Component of "cold" medication
29
Chlorpheniramine side effects?
Less sedating, often in "daytime" meds
30
Loratadine class and mxn?
Piperidine derivative, 2nd gen H1 receptor antagonist
31
Loratadine for?
Allergic rhinitis
32
Loratadine side effects?
No sedation, Cardiovascular effects rarely at high doses
33
Fexofenadine class and mxn?
Piperidine derivative, 2nd gen H1 receptor antagonist
34
Fexofenadine for?
Allergic rhinitis
35
Fexofenadine side effects?
No sedation, Cardiovascular effects rarely at high doses
36
Piperidine derivatives?
Loratadine, Fexofenadine
37
AKA Claritin?
Loratadine
38
AKA Fexofenadine?
Allegra
39
AKA Allegra?
Fexofenadine
40
AKA Loratadine?
Claritin
41
Piperidine derivatives cross BBB? Consequences?
No, so fewer central and overall side effects
42
Piperidine timing versus 1st gen H1 receptor antagonists?
Longer acting, so can be used 1 daily
43
Azelastine mxn?
2nd gen H1 receptor antagonist
44
Cetirizine mxn?
2nd gen H1 receptor antagonist
45
AKA Cetirizine?
Zyrtec
46
AKA Zyrtec?
Cetirizine
47
Azelastine for?
Allergic rhinitis (intranasal spray), allergic conjunctivitis (ophthalmic solution)
48
Azelastine side effects?
No sedation, crosses BBB poorly so less side effects in general
49
Cetirizine for?
Allergic rhinitis
50
Cetirizine often in combo with?
Pseudoephedrine
51
Cetirizine side effects?
No sedation, crosses BBB poorly so less side effects in general
52
H2 receptor antagonists?
Cimetidine, Ranitidine, Famotidine, Nizatidine
53
1st gen H1 receptor antagonists?
Diphenyhydramine, Tripelennamine, Cyclizine/Meclizine, Promethazine, Chlorpheniramine
54
2nd gen H1 rec antagonists?
Loratadine, Fexofenadine, Azelastine, Cetirizine
55
Cimetidine mxn?
H2 receptor antagonist; block gastric acid secretion, more so with nocturnal than meal
56
Ranitidine mxn?
H2 receptor antagonist; block gastric acid secretion, more so with nocturnal than meal
57
Famotidine mxn?
H2 receptor antagonist; block gastric acid secretion, more so with nocturnal than meal
58
Nizatidine mxn?
H2 receptor antagonist; block gastric acid secretion, more so with nocturnal than meal
59
Cimetidine for?
Dyspepsia, duodenal and gastric ulcers, hypersecretory conditions (Zollinger Ellison gastrin-secreting tumor)
60
Ranitidine for?
Dyspepsia, duodenal and gastric ulcers, hypersecretory conditions (Zollinger Ellison gastrin-secreting tumor)
61
Famotidine for?
Dyspepsia, duodenal and gastric ulcers, hypersecretory conditions (Zollinger Ellison gastrin-secreting tumor)
62
Nizatidine for?
Dyspepsia, duodenal and gastric ulcers, hypersecretory conditions (Zollinger Ellison gastrin-secreting tumor)
63
Cimetidine side effects?
Most side effects of H2 blockers: Antiandrogen (impotence and gynecomastia), inhibition of P450
64
Ranitide side effect?
Liver toxicity
65
Least side effects of H2 blockers?
Nizatadine
66
H2 blockers that will not inhibit P450?
Famotidine, Nizatidine
67
All H2 blockers can cause?
CNS dysfunction (confusion, slurred speech)
68
Cyproheptadine class?
Antihistaminic & Antiserotinergic
69
Cyproheptadine for?
Skin allergies (urticaria, anti H1), Diarrhea of carcinoid (anti-5HT2)
70
Cyproheptadine side effects?
Sedation, antimuscarinic
71
Ketanserin mxn?
Selective 5HT2a,2C receptor antagonist, as well as Alpha 1 and H1 antagonist
72
Ketanserin for?
Antihypertensive (relaxes vascular and tracheal muscle), Antiplatelet aggregation
73
Is Ketanserin available in the U.S.?
No
74
Odansetron mxn?
5HT3 receptor antagonist
75
Odansetron for?
N/V with chemo
76
Ergot alkaloid mxn?
Agonist and antagonist actions at 5HT and alpha adrenergic receptors
77
Ergot alkaloids side effects?
Powerful hallucinations, smooth muscle contraction (vascular and uterine)
78
Ergotamine class and mxn?
Nonspecific partial agonist at all 5HT1,2 receptors; partial agonist at alpha adrenergic receptors
79
Ergotamine for?
Prodrome of migranes
80
Ergotamine side effects?
N/V, cumulative and prolonged vasoconstriction
81
Methysergide class and mxn?
Ergot alkaloid; Partial agonist at all 5HT1 receptors, antagonist at 5HT2
82
Methysergide for?
Prophylaxis of migranes
83
Methysergide side effects?
GI disturbances, inflammatory fibrosis (chronic use), hallucinations, withdrawn from market
84
Ergonovine class and mxn?
Ergot alkaloid, sustains uterine contraction
85
Ergonovine for?
postpartum hemorrhage
86
Bromocriptine class and mxn?
Ergot alkaloid, dopamine agonist
87
Bromocriptine for?
Hyperprolactinemia
88
Triptans class and mxn?
Non-ergot serotonin analogs; 5HT1B,D receptor agonist
89
Triptans for?
Effective (70%) migraine treatment in 1-2 hours
90
Name 4 triptans.
Sumatriptan, naratriptan, rizatriptan, zolmitriptan
91
Triptan mxn?
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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