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Anti Androgen

Antiandrogens are antagonists to androgens (the hormone). They were first discovered in 1960s. Androgen hormones are steroid hormones known to stimulate and control the male characteristics in vertebrates; this includes male secondary sexual characters and sex organs. Antiandrogens alter the androgen pathway by blocking the appropriate receptors, competing for binding sites on the cell's surface, or affecting androgen production. Many industrial chemicals, pesticides and insecticides are known to show antiandrogenic effects. Certain plant species are also well known to show antiandrogenic effects.  Read more

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OVERVIEW:

Antiandrogens are antagonists to androgens (the hormone). They were first discovered in 1960s. Androgen hormones are steroid hormones known to stimulate and control the male characteristics in vertebrates; this includes male secondary sexual characters and sex organs.  Antiandrogens alter the androgen pathway by blocking the appropriate receptors, competing for binding sites on the cell's surface, or affecting androgen production. Many industrial chemicals, pesticides and insecticides are known to show antiandrogenic effects. Certain plant species are also well known to show antiandrogenic effects.

TYPES ANTIANDROGEN DRUGS:

Antiandrogens are generally classified into two types:

  • Cyproterone acetate: reduces androgen, estrogen and LH levels. Cyproterone acetate acts both directly as an antiandrogen in prostate cancer cells and also functions indirectly to decrease serum testosterone levels.
  • Flutamide: the largest clinical experience has been with Flutamide which has shown to produce clinical lessening in patients with prostate cancer, and is also used in hyper androgenic state such as acne and hirsutism.
  • Nilutamide:  it has been extensively studied and is recommended for use in combination with surgical castration for the treatment of prostate cancer and is suggested to be started at the time of orchiectomy.
  • Bicalutamide: it is the most recent antiandrogen to be approved for use in the United States. It is also preferred in therapy of prostate cancer, but has not been approved for use in nonmalignant hyperandrogenic situations.

Another group of anti-androgens is also found including the drugs such as:

  • Leuprolide: It resembles LH-RH (luteinizing hormone-releasing hormone) produced by the hypothalamus that lowers the level of testosterone in the bloodstream. It is presently under research as a possible cure for the Paraphilias.
  • Goserelin works in the same way as Leuprolide.
  • Triptorelin: Triptorelin is an LHRH agonist, and it works in the same way as Leuprolide, however it is not usually given to females.
  • Abarelix: It is recommended for the treatment of prostate cancer in men with severe disease who refuse surgery, or cannot take hormonal treatments, or are poor candidates for surgery.

WHY ARE THEY USED?

  • An antiandrogen is frequently added to luteinizing hormone-releasing hormone (LH-RH) agonist therapy to prevent a rise in testosterone at the beginning of LH-RH agonist therapy because the rise in testosterone can cause a tumor flare with bone pain, urinary blockage, or other symptoms of rapid cancer growth.
  • Prostate cancer therapy: Antiandrogens are used before or after radiation for men in prostate cancer therapy. Prostate cancer is the most commonly diagnosed form of cancer found in men. Prostate cancer cells require androgens for their growth. Antiandrogenic drugs are used for hormone therapy called androgen deprivation therapy (ADT). The antiandrogenic drugs suppress androgen production while some of them inhibit androgens from binding to the cancer cell’s androgen receptors. Androgen-deprivation therapy (ADT) has been shown to cause initial reduction of prostate tumors.
  • Anti androgen therapy: Anti-androgen therapy refers to medication taken by women to offset the effect of male hormones such as testosterone on the skin. Male hormones in female become prominent as a result of hyperandrogenism. Anti-androgens are not suitable for skin problems in men.

Skin/hair conditions in women that may be caused or initiated by local or circulating androgenic hormones include:

  • Seborrhoea
  • Ameorrhea (absence of menstrual cycle)
  • Acne
  • Hirsutism (excessive facial and bodily hair in women)
  • Alopecia ( pattern hair loss)
  • Gender reassignment: It is used in transsexuals, as a component of hormone replacement therapy involving male-to-female (MTF) conversion. It commonly prevents any erections occurring, stops production of sperm and reduces stimulation of hair follicles. The effect of estrogen may be enhanced as there is no competition from the ‘male hormone’ because these drugs will reduce and in many cases stop all of the effects normally brought about by the body’s natural androgen, i.e. testosterone.
  • Paraphilias: Paraphilias is an assemblage of mental disorders characterized by intense and recurring sexual urges or behaviors involving non-human objects, children or non-consenting adults, or pain and humiliation. Antiandrogen drugs have been prescribed for men diagnosed with such condition in order to lower levels of testosterone in blood and help them control their sexual urges.
  • It also used for male contraception

WHAT ARE THE SIDE EFFECTS OF ANTI ANDROGENIC DRUGS?

 There are various side effects of each drug individually but those which are   commonly seen during the treatment process are:

  • Mood/Cognitive Changes: Serious mood swings, impatience and feeling of depression are commonly found in the patients of prostate cancer ongoing with antiandrogenic treatment.
  • Sexual changes: (Leuprolide and Goserelin) here the most common change is the loss of libido. Loss of potency or inability to get erection has proper meditational cure yet the loss of libido doesn’t have any special cure.
  • Gynecomystia: (Flutamide especially) It is the condition where male breasts increase in size and become tender and or painful, is a common side effect of anti-androgen medications.
  • Muscular changes: muscle strength and mass are surely affected due to this anti androgenic therapy along with it pains in the chest, groin, or legs is also seen.
  • Liver disorder: the drugs Flutamide, Nilutamide and Bicalutamide are known to show signs of liver damage, such as pain in abdomen, discoloration of eyes and skin. Such patients should consult their doctor and stop taking the medicines after doctor’s consent only.
  • Allergy: (Abarelix especially) one can develop life threatening allergic symptoms and can face severe respiratory problems; in such case one should consult their physician.
  • Pregnancy complications: Flutamide and Cyproterone are not prescribed for pregnant women.
  • Nausea and vomiting  specially during the intake of Goserelin
  • Stomach problems like indigestion, diarrhea, constipation and gas etc.

DRUG INTERACTIONS:

DRUG

COUNTER DRUG INTERACTION

Flutamide

  • With warfarin (Coumadin) and blood-thinning drugs
  •  It has also been reported to intensify the effects of phenytoin (Dilantin), a drug given to control seizures.

Nilutamide

  • With theophylline, a drug given to treat asthma

Bicalutamide

Same as Flutamide

Cyproterone

  • With oral medications  used for diabetes control

Leuprolide

No interaction

Triptorelin

No interaction

Goserelin

No interaction

Abarelix

  • With heart medicines like Procainamide, Amiodarone, Sotalol, and Dofetilde
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