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Doxepin is a mixture of and stereoisomers with an approximate ratio of 85:15. [5] When doxepin was developed, no effort was made to separate or balance the mixture following its synthesis, resulting in the asymmetric ratio. [5] (Z)-Doxepin is more active as an inhibitor of serotonin and norepinephrine reuptake than (E)-doxepin. [5]
The antidepressant drug doxepin has been associated with a number of different adverse effects, including the following. [1] [2] [3] The incidence of these adverse effects is not totally known as the scarcity of well-designed clinical trials involving doxepin prohibits it.
Total exposures to both doxepin and nordoxepin differ by almost 10-fold in CYP2D6 ultra-rapid versus poor metabolizers. [3] Both doxepin and nordoxepin are also transformed into glucuronide conjugates. [3] The elimination half-life of nordoxepin is approximately 31 hours, which is almost twice that of doxepin (mean 17 hours). [1]
The first-generation sedating antihistamines diphenhydramine, doxepin, doxylamine, and pyrilamine are the most widely used medications in the world for preventing and treating insomnia. [6] As of 2004, doxylamine and diphenhydramine, which are both over-the-counter medications, were the agents most commonly used to treat short-term insomnia. [11]
This multi-page article lists pharmaceutical drugs alphabetically by name. Many drugs have more than one name and, therefore, the same drug may be listed more than once. ...
Section 5.5 of the article Doxefazepam in volume 66 of the World Health Organization's (WHO) and International Agency for Research on Cancer's (IARC) IARC Monographs On The Evaluation Of Carcinogenic Risks To Humans, an article describing the carcinogenic/toxic effects of doxefazepam on humans and experimental animals, states that there is "inadequate evidence in humans for the carcinogenicity ...
It is the parent structure of certain drugs such as the tricyclic antidepressant doxepin and the analgesic fluradoline. [ 1 ] [ 2 ] [ 3 ] The former is the only tricyclic antidepressant that is a dibenzoxepin.
The second-generation antidepressants are a class of antidepressants characterized primarily by the era of their introduction, approximately coinciding with the 1970s and 1980s, rather than by their chemical structure or by their pharmacological effect.