Estrogen Agonist + Antagonists Drug Class

Estrogen Agonists + antagonists are compounds that have tissue selective actions. In other words, how they act or function will differ according to the actual tissue in which they find themselves. If you think of the word antagonist it, sounds a bit adversarial. Indeed it is, and in this case, something, that is antagonistic toward Estrogen, will work to block its release and effects. Essentially, these compounds have the goal of producing beneficial Estrogen actions and activities in specific tissues, whether that be in bones or the brain. The other goal is to produce antagonistic activity (i.e. blocking the effects) in tissues like the breast or the endometrium, where long term Estrogen activity could become a problem. Having said this, it should also be readily apparent there are a number of specific uses and treatments that might be able to take advantage of these drugs.

Estrogen Agonist + Antagonists Drugs

There are a number of drugs within the category of Estrogen agonists and antagonists, including:

Estrogen Agonist + Antagonists Uses

Estrogen agonist and antagonists are useful in a number of different types of treatments and situations. For example, the antagonist side of these drugs is very helpful in breast cancer, which is indeed currently the most commonly prescribed use of these compounds. However, it can also be helpful in conditions such as Osteoporosis, PCOS, and menopause. There are even doctors and medical professionals who like using these drugs for help with fertility treatments.

Taking the above example of breast cancer a bit further, there are multiple uses. In addition to actually being a potential treatment, or part of a treatment mix, these types of drugs may also be helpful in decreasing the chance of breast cancer coming back in women have already received treatment, even if they used different drugs and medications to do so. There is also the chance it may help prevent breast cancer in some women who have a high risk of developing this disease.

Perhaps the most interesting aspect of these compounds is that some are true Estrogen agonists and antagonists at the same time. In other words, there are some medications that work as an agonist at bone, but an antagonist at the breast and the uterus.

Estrogen Agonist + Antagonists Side Effects

Since there are so many different types of these Estrogen agonist and antagonist drugs, you should expect to see a wide range of side effects, which is certainly the case. The side effects will depend on which actual drug was used, which conditions were being treated, and the person who was being treated. These include:

  • Hot flashes
  • Cataracts
  • Nausea
  • Deep vein thrombosis
  • Pulmonary embolism
  • Endometrial cancer
  • Leg cramps

Estrogen Agonist + Antagonists Interactions

Although most drug interactions with Estrogen Agonists and antagonists are not dangerous, there are several other substances to avoid. This includes some selective serotonin reuptake inhibitors and antidepressants like Paxil, Prozac, and Zoloft. In most cases, these compounds are all competing for the same enzyme that is needed to metabolize the Estrogen into its active form.