Pharm 43 Histamine Flashcards
MOA:
Inverse agonists binding preferntially to inactive conformation of H1 receptors
First-Generation H1-Antihistamine
More CNS affect (more lipid soluble)
First-Generation H1-Antihistamine
Ethanolamines (1st generation) (4)
Diphenhydramine, Carbinoxamine, Clemastine, Dimenhydrinate
Tx:
Allergic rhinitis, insomnia, motion sickness, urticaria, anaphylaxis, parkinsonism
First-Generation H1-Antihistamines
Ethylenediamines (1st generation) (2)
Pyrilamine, Tripelennamine
Alkylamines (1st generation) (2)
Chlorpheniramine, Brompheniramine
Piperidines (1st generation) (2)
cyproheptadine, phenidndamine
Phenothiazine (1st generation) (1)
Promethazine
Tx:
preoperative anxiety and reduce postoperative nausea and vomiting
Promethazine (1st generation)
Piperazines (1st generation) (3)
Hydroxyzine, Cyclizine, Meclizine
Tx:
Pruritis, alcohol withdrawal, motion sickness, vertigo
Hydroxyzine, cyclizine, meclizine (1st generation)
Tricyclic dibenzoxepins (1st generation) (1)
Doxepin
Tx:
Anxiety, Depression, Pruritis
Doxepin
Piperizines (2nd generation) (2)
Cetirizine, Levocetirizine
Considerations:
less sedating, less anticholinrgic effects
2nd generation H1-Antihistamine
Alkylamines (2nd generation) (1)
Acrivastine
Piperidines (2nd generation) (6)
Loratidine, Desloratadine, Levocabastine, Ebastine, Mizolastine, Fexofenadine
Phthalazinones (2nd generation) (1)
Azelastine
Tricyclic dibenzoxepins (2nd generation) (1)
Olopatadine
H2 Receptor Antagonists (4)
Cimetidine, Famotidine, Nizatidine, Ranititdine
Tx:
GERD, Peptic Ulcers, Acid Reflux
H2 Receptor Antagonist (Cimetidine, Famotidine, Nizatidine, Ranititdine)
Consideration:
H2 receptor antagonist with most interactions with other drugs
Cimetidine