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Androgens and Anabolic Steroids and Anti-androgens.pptx

Androgens, Anabolic Steroids and Anti-androgens summarizes various androgenic and anti-androgenic drugs. It describes how testosterone and its synthetic derivatives like methyltestosterone promote muscle and bone growth but can also cause masculinization in women. It then discusses several classes of anti-androgens like flutamide, bicalutamide and finasteride that block androgen receptors or inhibit testosterone synthesis. These are used to treat prostate cancer, excess hair growth, acne and other androgen-dependent conditions by preventing the biological effects of androgens.

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Androgens, Anabolic Steroids and Anti-androgens By Dr. Faraza Javaid
Introduction Androgen anabolic steroids are synthetic types of male sex hormone – Testosterone. Anabolic – Building of muscle tissue Androgenic – Masculine characteristics Steroid – Any fat-soluble organic compounds (such as sterols, bile acids and hormones) that have specific physiological effects.
History 1935 – Testosterone was first synthesized, and German soldiers were reportedly using it to perform better and to become more aggressive. 1950 – During 1952 Olympics, the Russian weightlifting team won he gold medal due to synthetic steroid use. Australian pharmaceutical company develops the first anabolic steroid.
Classification Natural Androgens From testis: Testosterone (5-12 mg daily) Dihydrotestosterone From adrenal cortex: Dehydroepiandrosterone (Female testosterone – 0.25 – 5 mg/day [ovary + adrenals])
Synthetic Androgens Methyltestosterone Fluoxymesterone Orally effective: Testosterone undecanoate, Masterolone Lipid soluble ester: Propionate, Enanthate salts Oxandrolone and Stanozolol – Anabolic action only.
Testosterone AR receptors exist in multiple tissue type. Binds ligand in the cytoplasm and translocate into the nucleus. Upon binding, facilitate appropriate gene activation.
Pharmacological Actions Androgenic Effects: In the fetus, testosterone promotes development of male reproductive tract. During puberty, testosterone promotes the development of: Primary sexual characteristics Secondary sexual characteristics During adulthood, it may cause baldness, benign prostatic hyperplasia and prostate cancer.
Anabolic Effects: Bone growth – Thickness and length Fuse of bone and mineralization - Estrogen from testosterone Muscle building – If aided by exercise
Pharmacokinetics Absorption: Undergoes high first pass metabolism. Therefore, IM injections or synthetic oral preparations are used. Metabolism and Excretion: Metabolized by liver enzymes to androsterone and excreted in urine.
Side Effects In females, Virilization (Masculinization) Hirsutism Acne, Menstrual disorders In males, gynecomastia, salt and water retention Gall bladder stone Prostate enlargement Prostate cancer
Clinical Uses Replacement therapy in testicular failure Hypopituitarism AIDS related muscle wasting
Antiandrogens Antiandrogens, also known as androgen antagonists or testosterone blockers, are a class of drugs that prevent androgens like testosterone and dihydrotestosterone (DHT) from mediating their biological effects in the body. They act by blocking the androgen receptor (AR) and/or inhibiting or suppressing androgen production.
Flutamide Bicalutamide Nilutamide Topilutamide Enzalutamide Apalutamide Spironolactone
Finasteride Dutasteride Epristeride Alfatradiol
Flutamide Flutamide acts as a selective antagonist of the androgen receptor, competing/with androgens like testosterone and dihydrotestosterone (DHT) for binding to ARs in tissues like the prostate gland. Uses: Used primarily to treat prostate cancer. It is also used in the treatment of androgen-dependent conditions like acne, excessive hair growth, and high androgen levels in women.
Side Effects: Diarrhea and elevated liver enzymes can occur in both genders. Flutamide can cause liver damage, lung disease, sensitivity to light, elevated methemoglobin, elevated sulfhemoglobin, and deficient neutrophils. Numerous cases of liver failure and death have been reported, which has limited the use of flutamide.
Bicalutamide It is used for early prostate cancer at a higher dosage as a monotherapy. It is the most widely used antiandrogen in the treatment of prostate cancer, and has been prescribed to millions of men with the disease. Bicalutamide is well-absorbed, and its absorption is not affected by food. The elimination half-life of the medication is around one week. It is believed to cross the blood–brain barrier and affect both the body and brain
Uses: Bicalutamide is also used to treat excessive hair growth in women, as a component of feminizing hormone therapy for transgender women, To treat early puberty in boys
Side Effects: Common side effects in men include breast enlargement, breast tenderness, and hot flashes. Other side effects in men include feminization and sexual dysfunction. Rarely, it has been associated with cases of liver damage, lung toxicity, and sensitivity to light. Although the risk of adverse liver changes is small, monitoring of liver function is recommended during treatment.
Spironolactone Spironolactone also possess an antiandrogenic effect which could be due to the antagonism of androgens. Spironolactone inhibits 5- alpha reductase weakly. For this reason, it is frequently used to treat a variety of dermatological conditions in which androgens play a role. Some of these uses include acne, seborrhea, hirsutism, and pattern hair loss in women.
The specific actions of spironolactone as an antiandrogen are not well understood. It appears to act at two sites: It blocks androgens at the hair follicle/sebaceous gland and It reduces the secretion of androgens from the adrenal gland. To check the effectiveness of this therapy, the hair growth and/or acne are assessed at 2 to 4 month intervals.
Finasteride Finasteride is a 5α-reductase inhibitor and therefore an antiandrogen. It works by decreasing the production of dihydrotestosterone (DHT) by about 70%, including in the prostate gland and the scalp. Uses: Used to treat hair loss and benign prostatic hyperplasia in men. It can also be used to treat excessive hair growth in women and as a part of hormone therapy for transgender women.
Adverse Effects: Adverse effects from finasteride are rare, however, some men experience sexual dysfunction, depression, and breast enlargement. In some men, sexual dysfunction may persist after stopping the medication. It may also hide the early symptoms of certain forms of prostate cancer.
Dutasteride Dutasteride is used for treating benign prostatic hyperplasia (BPH); also known as an "enlarged prostate". It is approved by the Food and Drug Administration (FDA) in the U.S. for this indication. It is also used for scalp hair loss in men and as a part of hormone therapy in transgender women.
Side Effects: Dutasteride has overall been found to be well tolerated in studies of both men and women, producing minimal side effects. Adverse effects include headache and gastrointestinal discomfort. Isolated reports of menstrual changes, acne, and dizziness also exist.
Abiraterone Acetate Abiraterone acetate, is a medication used to treat prostate cancer. Common side effects include tiredness, vomiting, headache, joint pain, high blood pressure, swelling, low blood potassium, high blood sugar, hot flashes, diarrhea, and cough. Other severe side effects include liver failure and adrenocortical insufficiency.
Question? A 76 year old man complains of progressive difficulty starting his urine stream and having to get up several times during each night to urinate. Rectal examination reveals a generally enlarged, smooth surfaced prostate. Prostate specific antigen (PSA) titers are elevated. Finasteride treatment is started and eventually urine flow increases and prostate size decreases. Which of the following phrases best summarizes the mechanism by which finasteride caused symptoms relief? a) Blocks α-adrenergic receptors b) Blocks testosterone receptors c) Inhibits dihydrotestosterone synthesis d) Lower plasma testosterone by increasing renal clearance
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