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

7) Histamine, Serotonin, and Antagonists Flashcards

(83 cards)

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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
What are the important side effects for Loratadine (Claritin)
No sedation
26
What are the other side effects for Loratadine (Claritin)
Cardiovascular effects (rare, with high doses)
27
What are the miscellaneous for Loratadine (Claritin)
Poorly crosses BBB, so fewer central and side effects
28
What is the class for Fexofenadine (Allegra)
Piperidine derivitive
29
What is the mechanism for Fexofenadine (Allegra)
2nd generation H1 receptor antagonist
30
What are the therapeutics for Fexofenadine (Allegra)
Allergic rhinitis
31
What are the important side effects for Fexofenadine (Allegra)
No sedation
32
What are the other side effects for Fexofenadine (Allegra)
Cardiovascular effects (rare, with high doses)
33
What are the miscellaneous for Fexofenadine (Allegra)
Poorly crosses BBB, so fewer central and side effects
34
What is the mechanism for Azelastine (Astelin)
2nd generation H1 receptor antagonist
35
What are the therapeutics for Azelastine (Astelin)
Allergic rhinitis (intranasal spray), allergic conjunctivitis (ophthalmic solution)
36
What are the important side effects for Azelastine (Astelin)
No sedation
37
What are the miscellaneous for Azelastine (Astelin)
Poorly crosses BBB, so fewer central and side effects
38
What is the mechanism for Cetirizine (Zyrtec)
2nd generation H1 receptor antagonist
39
What are the therapeutics for Cetirizine (Zyrtec)
Allergic rhinitis
40
What are the important side effects for Cetirizine (Zyrtec)
No sedation
41
What are the miscellaneous for Cetirizine (Zyrtec)
Poorly crosses BBB, so fewer central and side effects
42
What is the mechanism for Cimetidine (Tagamet)
H2 receptor antagonist; blocks gastric acid secretion (more so with nocturnal acid secretion than meal secretion)
43
What are the therapeutics for Cimetidine (Tagamet)
Dyspepsia, duodenal and gastric ulcers, hypersecretory conditions
44
What are the important side effects for Cimetidine (Tagamet)
Antiandrogen (causing impotence and gynecomastia), inhibition of P450 enzymes
45
What are the other side effects for Cimetidine (Tagamet)
CNS dysfunction possible
46
What are the miscellaneous for Cimetidine (Tagamet)
Most side effects of H2-blocker class
47
What is the mechanism for Ranitidine (Zantac)
H2 receptor antagonist; blocks gastric acid secretion (more so with nocturnal acid secretion than meal secretion)
48
What are the therapeutics for Ranitidine (Zantac)
Dyspepsia, duodenal and gastric ulcers, hypersecretory conditions
49
What are the important side effects for Ranitidine (Zantac)
Liver toxicity
50
What are the other side effects for Ranitidine (Zantac)
CNS dysfunction possible
51
What is the mechanism for Famotidine (Pepcid)
H2 receptor antagonist; blocks gastric acid secretion (more so with nocturnal acid secretion than meal secretion)
52
What are the therapeutics for Famotidine (Pepcid)
Dyspepsia, duodenal and gastric ulcers, hypersecretory conditions
53
What are the other side effects for Famotidine (Pepcid)
CNS dysfunction possible
54
What is the mechanism for Nizatidine (Axid)
H2 receptor antagonist; blocks gastric acid secretion (more so with nocturnal acid secretion than meal secretion)
55
What are the therapeutics for Nizatidine (Axid)
Dyspepsia, duodenal and gastric ulcers, hypersecretory conditions
56
What are the other side effects for Nizatidine (Axid)
CNS dysfunction possible
57
What are the miscellaneous for Nizatidine (Axid)
Least side effects of H2-blocker class
58
What is the mechanism for Cyproheptadine (Periactin)
Antihistaminic and antiserotinergic
59
What are the therapeutics for Cyproheptadine (Periactin)
Skin allergies (urticaria, anti-5HT1), diarrhea of carcinoid syndrome (anti-5HT2)
60
What are the other side effects for Cyproheptadine (Periactin)
Sedation, antimuscarinic
61
What is the mechanism for Ketanserin
Selective 5HT2A,2C receptor antagonist, as well as ?1 and H1 receptor antagonist
62
What are the therapeutics for Ketanserin
Antihypertensive (relaxes vascular and tracheal smooth muscle), antiplatelet aggregation
63
What is the mechanism for Odansetron (Zofran)
5HT3 receptor antagonist
64
What are the therapeutics for Odansetron (Zofran)
Nausea and vomiting in chemotherapy
65
What is the mechanism for Ergot alkaloids
Agonist and antagonist actions at 5HT and ?-adrenergic receptors
66
What are the important side effects for Ergot alkaloids
Powerful hallucinations, smooth muscle contraction (vascular and uterine)
67
What is the class for Ergotamine (Ergomar)
Ergot alkaloid
68
What is the mechanism for Ergotamine (Ergomar)
Nonspecific partial agonist at all 5HT1,2 receptors; partial agonist at ?-adrenergic receptors
69
What are the therapeutics for Ergotamine (Ergomar)
Prodrome of migraines
70
What are the other side effects for Ergotamine (Ergomar)
N/V, cumulative and prolonged vasoconstriction
71
What is the class for Methysergide (Cycloset)
Ergot alkaloid
72
What is the mechanism for Methysergide (Cycloset)
Partial agonist at all 5HT1 receptors, antagonist at 5HT2
73
What are the therapeutics for Methysergide (Cycloset)
Prophylaxis of migraines
74
What are the other side effects for Methysergide (Cycloset)
GI disturbances, inflammatory fibrosis (chronic use), hallucinations
75
What are the miscellaneous for Methysergide (Cycloset)
Withdrawn from U.S. market
76
What is the class for Ergonovine
Ergot alkaloid
77
What are the therapeutics for Ergonovine
Postpartum hemorrhage (Oxytocic)
78
What is the class for Bromocriptine (Sansert)
Ergot alkaloid
79
What is the mechanism for Bromocriptine (Sansert)
Dopamine agonist
80
What are the therapeutics for Bromocriptine (Sansert)
Hyperprolactinemia
81
What is the class for Triptans
Non-ergot serotonin analogs
82
What is the mechanism for Triptans
5HT1B,D receptor agonist
83
What are the therapeutics for Triptans
Effective (70%) migraine treatment

Pharm U2 (11 decks)

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