Histamine, serotonin, and Antagonists Flashcards
What are the main uses for H1 receptor antagonists?
Allergic reactions
motion sickness
N/V in pregnancy
sleep aids
Name the 5 H1 receptor antagonists…
Diphenhydramine Tripelennamine Meclizine/Hydroxyzine Promethazine Chlorpheniramine
What are the major side effects of the H1 receptor antagonists?
Sedation anti-muscarinic action poisoning with convulsions allergy local anesthesia
H1 receptor antagonist used as an OTC sleep aid?
Tripelennamine
H1 receptor antagonist used for motion sickness?
Meclizine
Hydroxyzine
H1 receptor antagonist used as an antiemetic (N/V treatment)?
Promethazine
H1 receptor antagonist used as a component of cold medications?
Chlorpheniramine
Name the 4 2nd generation H1 receptor antagonists?
Loratadine
Fexofenadine
Azelastine
Cetirizine
What are the 2 2nd generation H1 receptor antagonist in the piperidine derivative class?
Loratadine
Fexofenadine
What is so special about the 2nd generation H1 receptor antagonists?
Poorly cross the BBB–fewer central side effects
No sedation effects
What is the primary use of all 4 2nd generation H1 receptor antagonists?
Allergic rhinitis
What 2 2nd generation H1 receptor antagonist can cause cardiovascular effects at high doses?
Loratadine
Fexofenadine
What is the mechanism of action of the H2 receptor antagonists?
Block gastric acid secretion–more so with nocturnal acid secretion than meal secretion
What are the 4 H2 receptor antagonists?
Cimetidine
Ranitidine
Famotidine
Nizatidine
What are the 3 uses for the H2 receptor antagonists?
Dyspepsia
duodenal and gastric ulcers
hypersecretory conditions
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?
Cimetidine
What is the one major side effect of Ranitidine?
Liver toxicity
Which of the H2 receptor antagonist have the least side effects?
Nizatidine
What are the two mechanisms of cyproheptadine?
Antihistaminic
Antiserotinergic
What are the uses of cyproheptadine?
Skin allergies–urticaria, anti-5HT1
Diarrhea of carcinoid syndrome-anti-5HT2
What are the mechanisms of ketanserin?
Selective 5HT2A,2C receptor antagonist
a1 and H1 receptor antagonist
What are the uses of ketanserin?
Antihypertensive
antiplatelet aggregation
What is the mechanism of Odansetron and Granisetron?
5HT3 receptor antagonist
What are the uses of odansetron and granisetron?
N/V in chemo and postop patients
What are the mechanisms of action for the ergot alkaloids?
Agonist and antagonist actions at 5HT and a-adrenergic receptors
What are the side effects seen with ergot alkaloids?
Powerful hallucinations
smooth muscle contraction–vascular and uterine
What are the 4 ergot alkaloids?
Ergotamine
Methysergide
Ergonovine
Bromocriptine
Ergot alkaloid that is a nonspecific partial agonist at all 5HT 1,2 receptors and partial agonist at a-adrenergic receptors…
Ergotamine
Ergot alkaloid that is a partial agonist at all 5HT1 receptors and antagonist at 5HT2…
Methysergide
Ergot alkaloid that is a dopamine agonist…
Bromocriptine
What ergot alkaloid is used at the start of a migraine?
Ergotamine
What ergot alkaloid is used as a prophylaxis for migraines?
Methysergide
What ergot alkaloid is used for the treatment of postpartum hemorrhage?
Ergonovine
Which ergot alkaloid is used for the treatment of hyperprolactinemia?
Bromocriptine
A non-ergot serotonin analog that is a 5HT1B,D receptor agonist used for migraine treatment?
Triptans
