Ethinylestradiol
An Introduction to Ethinylestradiol
Ethinylestradiol or [EE] is a derivative compound formed from estradiol and is a bioactive estrogen used in nearly all modern combined contraceptive pills or better known as simply [The Pill]. It is likely among the most common drugs in use today and is normally marketed as NuvaRing. It was the first of many generic brands of synthetic estrogen.
Ethinylestradiol was the first orally activated synthetic steroidal estrogen known as 17α-ethynylestradiol and was first synthesized in 1938 by Hans Herloff Inhoffen and Walter Hohlweg out of Berlin at Scherling AG. EE gained FDA approval in the United States in 1943 and was being sold by Scherling under the name Estinyl. Scherling itself called for it to be withdrawn beginning on 24 June 2004, since they had stopped selling Estinyl.
Estradiol is quickly metabolized by the liver becoming inactive and though it is absorbed readily when taken orally. So certain substitutions of an ethinyl group were made that provided an estrogen that was far more hardy and disparate to rapid breakdown; this was the beginning and expansion of oral contraceptives.
EE absorption occurs in the small bowel and reaches peak effectiveness in the body within two hours. Ethinylestradiol goes through a broad metabolic process in the liver that involves the super family of hemoproteins and enzyme reactions causing the metabolized EE to be excreted in the bile. This reaction causes a secondary crest of the EE effect a few hours later. This process of absorption is far from fixed, as it will fluctuate in individuals with many variations occurring. These disparities in absorption will undergo further modifications caused by other drug use in combination with the EE. After this chemical process takes place, EE is then passed from the body in urine and feces as glucuronoside and sulfate chemical substances.
Ethinylestradiol is an effective hormonal drug because of its activation of the estrogen receptor, which makes it an estrogen. It is most commonly used as a combination estrogen and progestin, a synthetic progestagen, for the formulation of oral contraceptives. Formulations of contraceptives have decreased in strength with the amounts of EE required for effective doses due to advancements in research.
Anyone taking any estrogen-based medication for a prescribed condition should be advised to apply the same cautions with ethinylestradiol use as they would with any other estrogen medications when considering contraindications. It should be noted that Estinyl in its original form derived from EE was used as a medication to control medically control menopausal symptoms and hypogonadism [in females, a defect of the reproductive system that results in lack of function of the ovaries].
Ethinylestradiol has caused some concerns amongst those in the medical community because of the adverse nature of the synthesized hormone within the human anatomy and the effect on the environment from its release as a xenoestrogen through urine and feces from those who take and metabolize the drugs in their systems. These xenoestrogens have been drawn into controversy because of the potential to cause medical problems but unfortunately, there has been minimal evidence to back up these assumptions of how humans have reacted to their presence.
By far the biggest concern is that since the introduction of these xenoestrogens into the mainstream of pharmaceuticals they are causing a disturbance in the normal behavior of the reproduction systems in women AND men. Synthetic estrogen has the same effect as naturally produced estrogen, which can increase the development of the endimetrium, or the lining of the uterus, increasing the need for endometriosis treatment. In effect, the first line of defense is the immediate cessation of estrogen-based products from the system. The thickening of the lining of the uterus can extend into the muscular tissue causing the start of adenomyosis, which can result in painful menstruation or worse.
There have been some studies, which have shown a disturbing pattern in wildlife due to the introduction of estrogen into the flora and fauna due to societal waste expulsion. Because of the introduction of estrogen in women there is cause for concern that constant fetal contact with estrogen presence in the female that male birth defects such as hypospadias, or the misplacement of the male urethra and its abnormal opening.
There is also the concern of male reproduction capabilities because of low sperm counts being investigated due to estrogen toxicity. In 1993, the famed science journal The Lancet featured an article by researchers who apparently showed the relationship between dropping sperm levels in males because of the direct presence of estrogen while in the uterus.
Also on subject is the matter of what effect the presence of estrogen has on the oncogenes. These are the genes that for whatever reason when they are mutated or occur in higher levels can turn a normal cell into a cancerous cell. This is of major concern when dealing with breast cancer specifically and is causing quite a stir amongst those active in this community. Of course, there are those scientists who deem the threat by xenoestrogen to be benign in the levels currently found in the environment.