Histamine Flashcards
Histamine acted on by diamine oxidase forms
Imidazole acetic acid
Histamine acted on by histamine n-methyltransferase forms
N-methylhistamine
Receptor found on smooth muscle, endothelium, and brain
H1
Receptor found on gastric mucosa, cardiac muscle, mast cells, brain
H2
Gq receptor. Increase IP3 and DAG
H1
Gs receptor. Increases cAMP
H2
Partially selective agonist 2-methyl-histamine
H1
Partially selective antagonist chlorpheniramine
H1
Partially selective agonist dimaprit
H2
Partially selective antagonist ranitidine
H2
Chlorpheniramine, Diphenhydramine, Hydroxyzine, Promethazine
Histamine antagonist 1st gen
Cetirizine, Loratadine, Fexofenadine
Histamine antagonist 2nd gen
Diphenhydramine, Promethazine have
CNS sedation and antimuscarinic properties
Cetirizine has
CNS sedation
Metabolized by cyp3A4.
Important in drugs that inhibit CYP3A4, such as ketoconazole
2nd gen (Loratadine)