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Antiandrogen

Overview

Antiandrogens are the drugs that obstruct the effect of androgens or male sex hormones. It disables the binding of testosterone and reduces the overall production of testosterone in body. There are wide array of drugs present in the market that are used to treat disorders occurring due to excess production of testosterone. They are most widely employed in hyperandrogenism in women, Prostate cancer in men. Anti androgens is the well known therapy option in the treatment of Prostate Cancer

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Applications of Anti androgens

Antiandrogens are employed in various disease and disorders. The most common conditions are explained as below:

  • Prostate Cancer - It is a cancer of Prostate gland present in men. Prostate is a tiny gland of the male reproductive gland and is present in front of the rectum and is under the bladder. In this gland, milky fluid is produced that protects and nourishes the sperm. During ejaculation, there is secretion of the milky fluid that delivers the sperm into the urethra and leaves the body through the penis. Cancer of prostate takes place when there is slight changes takes place in the size and shape of prostate glands. It keeps on accelerating but at slow scale and can be treated at early stages. In advanced stages, it can’t be cured. Anti androgen drugs controls the production of androgen hormone in some cases and it also doesn’t allow the binding of androgen to the cancer cell’s androgen receptor. This way, in initial stages it decreases the growth of prostate tumor 
  • Hyper sexuality - is a condition in which there is abrupt or recurrent sexual urge or desire. It can also be termed as Excessive sexual drive or Masturbation. In this, an individual is obsessed with sexual thoughts and feelings and it can really effect on your health, psychology and other parts of life also. Anti androgens directly act the Androgen hormone and keeps control on the effects of that is responsible for sexual urge or desire 
  • Gender reassignment – this is a procedure in which alteration of genital organs are done. The physical and biological characteristics are changed according to the individual’s choice. Intersex abnormalities in new born babies can be treated by this procedure. It helps to allocate a particular gender. Some people suffer from gender identity disorder and they want to change their gender. This is most commonly seen in men than women. Reshaping of genital tissues like Penis removal and vaginal construction by skin grafting technique is done. Anti androgen therapy is recommended for male to female transsexuals before the Gender reassignment surgery
  • Paraphilias: it is a condition in which there is an atypical and extreme sexual behavior and involves unusual objects, children, tricks or behavior. This could be a result of childhood trauma or sexual abuse. Anti androgen decreases the production of Androgen and controls the unusual sexual activity
  • Hyperandrogenism – in this, there is abnormal and extreme levels of male sex hormones such as Androgen that can occur in male and females. There is excessive growth of body hair (hirsutism), increased libido, infertility, obesity and increased androgen levels. Decreasing androgen levels in the body can really help in restraining the sexual desire or activity 

Anti androgen drugs at a glance

These are the drugs that control the androgen secretion in body. They can be classified into two types one is steroidal and non steroidal anti androgens.

Non steroidal anti androgens

Flutamide is a non steroidal anti androgen drug that fights with testosterone and doesn’t allow them to bind with androgen receptors present in Prostate gland. This way, it avoids the growth of prostate cancerous cells. Over the counter, it is also a part of hormonal replacement therapy used in treatment of transsexual women. Flutamide is also recommended in the Hyperandrogenism conditions like Acne or hirsutism. It shows drug interaction with Warfarin and Phenytoin so simultaneous administration of these drugs should be avoided

Nilutamide is another anti androgen drug that blocks the androgen actions by getting attached at the site where this hormone is released. This all stops the growth of malignant tumors in prostate glands. It is given in surgical castration for the treatment of prostate cancer. It has counter drug interaction with a Theophylline drug used in the treatment of Asthma

Bicalutamide is another drug falling in the same above category of drugs. It acts via the same mechanism and is given in advanced stage of Prostate Cancer. Specifically indicated in combination with luteinizing hormone releasing hormone (LHRH) analog in the treatment of Prostate gland

Leuprolide and Goserelin are the drugs that looks like a LH-RH (luteinizing hormone-releasing hormone) that has a role in decreasing the levels of testosterone in bloodstream. They are indicated in the treatment of Prostate Cancer. They are also given to adjourn puberty in transgender youth until they reach at certain age suitable for the hormone replacement therapy

Abarelix and Triptorelin are other drugs which act in the same way as Leuprolide. They are given in the patients of Prostate cancer who cannot take surgery or other treatment. Abarelix interacts with heart medicines like Procainamide, Amiodarone, Sotalol, and Dofetilde.

Steroidal Anti androgen

Cyproterone Acetate is a steroidal drug that inhibits the production of Testosterone which is needed by the cancerous cells for their growth and proliferation. It is indicated in men who have increased sexual desire and sexual deviation (Hypersexuality). It interacts with various drugs such as Ketoconazole, Itraconazole, Clotrimazole, Phenytoin and Rifampicin

Side effects of Antiandrogens

The common side effects experienced with these drugs are as follows:

  • Mood swings and depression in patients suffering from Prostate Cancer
  • Muscular pain in chest, groin and legs
  • Abdominal pain, discoloration of eyes are the few signs of Hepatotoxicity shown by Cyproterone acetate ,Flutamide, Nilutamide and Bicalutamide
  • Pregnancy related complications can occur due to Cyproterone acetate and Flutamide
  • Indigestion, diarrhea and constipation
  • Gynecomystia is generally shown by the drug Flutamide
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