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| Trade names | Optimine |
| AHFS/Drugs.com | Micromedex Detailed Consumer Information |
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| Formula | C20H22N2 |
| Molar mass | 290.410 g·mol−1 |
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Azatadine (Optimine) is afirst-generation antihistamine andanticholinergic drug that was synthesized in 1963 bySchering-Plough, a former American pharmaceutical company.[1][2] It is a nitrogen analog ofcyproheptadine.[3]
It was patented in 1967.[4] It has been succeeded by bothloratadine anddesloratadine.[5]: 53 and marketing approvals have been widely withdrawn.[6][7][8][9]: 290 [10]
Azatadine exhibits potentantihistamine[11],anticholinergic, antiserotonin, and antianaphylactic properties. Its anticholinergic potency is one-third that ofatropine and equivalent to that ofpromethazine andcyproheptadine. Azatadine is among the more potent antianaphylactic agents.[3]
Azatadine is a first-generation antihistamine.[12]
The medicinal form of azatadine is the salt ofmaleic acid,azatadine maleate. It is described as an effective treatment for acute and chronic allergicrhinitis[11], vasomotor rhinitis,urticaria, and certain forms of atopic and contact dermatitis. At the maximum recommended therapeutic dose of 4 mg per day, the drug markedly reduced the severity of perennial allergic rhinitis in most patients (80%) over a 7-day period and significantly decreased swelling in histamine provocation and allergen tests. It was generally well tolerated. Drowsiness was reported by 40% of patients.[13]
Antihistamines such as azatadine compete withhistamine for thehistamine H1 receptor onplasma cell. This antagonism counteracts the pharmacological effects of histamine mediated through H1 receptor activation, thereby reducing the intensity of allergic reactions and the tissue damage associated with histamine release.[14] In addition, azatadine has been shown to downregulateleukotrienes as part of the immediate allergic response.[12]
The multi-step synthesis has been described in the literature.[15]
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