Fluoxetine is a selective 5-HT reuptake inhibitor widely used in clinic, which can selectively inhibit 5-HT transporter, block the reuptake of 5-HT by presynaptic membrane, prolong and enhance the effect of 5-HT, thus producing antidepressant effect. It has low affinity for adrenergic, histamine and cholinergic receptors, weak action and few adverse reactions. It is well absorbed after oral administration and its bioavailability is 70%. It can easily pass through the blood-brain barrier, and a small amount can be secreted into milk. Mefluoxetine is metabolized by CYP2D6 in the liver and also has antidepressant effect.
Although there are many newer drugs, fluoxetine is still a very commonly used drug in clinic. In 2007, American medical institutions prescribed more than 222 million prescriptions of fluoxetine, which made fluoxetine the third most commonly used antidepressant in the American market (after sertraline and escitalopram). In China, Baiyoujie used to be the most prescribed antidepressant.
According to David Wong, the main inventor of Baiyoujie, the related work of fluoxetine discovery began with the cooperative research of Bryan Molloy and Robert Rathburn 1970 of Lilly Company. At that time, the medical community knew that the antihistamine diphenhydramine had a certain antidepressant effect, so they started with 3- phenoxy -3- phenylpropanolamine with similar molecular structure, synthesized dozens of derivative variants and tested their physiological effects in mice, and finally got a selective norepinephrine reuptake inhibitor-nisoxetine, which was widely used in biochemical experiments.
Later, Wong proposed to re-test the in vitro reabsorption of serotonin, norepinephrine and dopamine in order to obtain a derivative variant that only inhibits serotonin reabsorption. 1972 In May, Sirhorn Zhong got fluoxetine according to this suggestion. Baiyoujie 1986 is an antidepressant produced by Lilly Company, which was first approved for the treatment of depression in Belgium. /kloc-0 was approved to enter the American market by the US Food and Drug Administration (FDA) at the end of 1987, and/kloc-0 entered the China market in April 1995.
Lilly's patent on Baiyoujie expired in August, 20001,and since then, a large number of fluoxetine drugs have appeared on the market.