Drugs Acting on Androgen Receptors
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Questions and Answers

What primary action does Drospirenone perform as a mineralocorticoid receptor antagonist?

  • Stimulates testosterone production
  • Reduces the action of aldosterone (correct)
  • Increases aldosterone levels
  • Enhances fluid retention

Which of the following conditions is NOT typically treated with Spironolactone?

  • Myocardial Infarction (correct)
  • Acne
  • Androgenetic alopecia
  • Hirsutism

How does Nilutamide achieve its anti-androgenic effects?

  • By promoting fluid retention
  • By inhibiting testosterone's actions (correct)
  • By enhancing aldosterone activity
  • By stimulating progesterone receptors

What is a common use for drugs like Drospirenone and Spironolactone?

<p>Treating conditions related to androgen excess (A)</p> Signup and view all the answers

Which of the following best describes the relationship between Spironolactone and androgen receptors?

<p>It blocks androgen receptors and inhibits androgen synthesis (A)</p> Signup and view all the answers

Which of the following is NOT an anabolic effect of testosterone?

<p>Decreased bone density (A)</p> Signup and view all the answers

What significant adverse effect can result from supraphysiologic doses of anabolic steroids in males?

<p>Testicular atrophy (D)</p> Signup and view all the answers

How does the anabolic:androgenic ratio of nandrolone compare to that of testosterone?

<p>Higher than testosterone (A)</p> Signup and view all the answers

Which of the following conditions is a result of high estrogen levels due to anabolic steroid use in males?

<p>Gynecomastia (C)</p> Signup and view all the answers

What effect can anabolic steroids have when interacting with glucocorticoid receptors?

<p>Influenced metabolism and immune function (B)</p> Signup and view all the answers

In females, virilization may lead to which of the following symptoms?

<p>Amenorrhea (C)</p> Signup and view all the answers

Which type of administration method for testosterone bypasses first-pass metabolism?

<p>Transdermal patches (A), Intramuscular injection (B)</p> Signup and view all the answers

Which of the following is a possible adverse effect associated with anabolic steroids affecting the liver?

<p>Peliosis hepatis (C)</p> Signup and view all the answers

What is a potential irreversible effect of anabolic steroid use in females?

<p>Deepening of the voice (D)</p> Signup and view all the answers

Which of the following conditions can be treated with cyproterone acetate?

<p>Severe acne and hirsutism (B)</p> Signup and view all the answers

What is the primary cause of acne associated with anabolic steroid use?

<p>Increased sebum production (A)</p> Signup and view all the answers

Which of the following is NOT a characteristic commonly associated with virilization in females due to anabolic steroid use?

<p>Elevated cortisol levels (B)</p> Signup and view all the answers

How does cyproterone acetate work to counteract the effects of androgens?

<p>By blocking androgen receptors (D)</p> Signup and view all the answers

What dermatological condition is caused by rapid increases in muscle size due to steroid use?

<p>Striae (D)</p> Signup and view all the answers

What characterizes male pattern baldness associated with steroid use?

<p>Acceleration of hair loss in predisposed individuals (B)</p> Signup and view all the answers

What condition is characterized by the presence of hemorrhagic liver cysts in individuals using anabolic steroids?

<p>Peliosis hepatis (B)</p> Signup and view all the answers

What is the primary mechanism of action of muscarinic receptor antagonists in treating overactive bladder?

<p>Blockade of cholinergic receptors (C)</p> Signup and view all the answers

Which drug class is primarily indicated for the treatment of benign prostatic hyperplasia (BPH)?

<p>5-alpha reductase inhibitors (C)</p> Signup and view all the answers

Which of the following is a selective α1A adrenoceptor antagonist used for urinary symptoms?

<p>Tamsulosin (C)</p> Signup and view all the answers

What is the main effect of phosphodiesterase-5 inhibitors in the context of prostate conditions?

<p>Smooth muscle relaxation (C)</p> Signup and view all the answers

What is the consequence of dihydrotestosterone (DHT) binding to hair follicle androgen receptors in genetically predisposed individuals?

<p>Shrinkage of hair follicles leading to thinning (D)</p> Signup and view all the answers

Which enzyme is primarily responsible for converting testosterone to dihydrotestosterone (DHT) in the prostate?

<p>5-alpha reductase type 2 (B)</p> Signup and view all the answers

What potential side effect is associated with the use of prazosin, a non-selective α1 adrenoceptor antagonist?

<p>Intraoperative floppy iris syndrome (C)</p> Signup and view all the answers

Which drug primarily inhibits both type 1 and type 2 5-alpha reductase enzymes?

<p>Dutasteride (B)</p> Signup and view all the answers

What is the primary role of dihydrotestosterone (DHT) in benign prostatic hyperplasia (BPH)?

<p>Encourages prostate tissue growth (A)</p> Signup and view all the answers

Which of the following statements about 5α-reductase inhibitors is true?

<p>They can reduce prostate size over several months (C)</p> Signup and view all the answers

What is NOT a common adverse effect of 5α-reductase inhibitors?

<p>Increased hair loss (A)</p> Signup and view all the answers

Intraoperative floppy iris syndrome is associated with the use of which type of medication?

<p>α1 adrenoceptor antagonists (A)</p> Signup and view all the answers

What is a key consequence of elevated DHT in the prostate?

<p>Obstructive urinary symptoms (A)</p> Signup and view all the answers

What is the consequence of discontinuing medication for intraoperative floppy iris syndrome?

<p>Has no effect on the syndrome's occurrence (B)</p> Signup and view all the answers

Which enzyme is primarily targeted by 5α-reductase inhibitors?

<p>5-alpha-reductase (C)</p> Signup and view all the answers

What is the effect of reducing DHT levels on hair follicles?

<p>Prevents miniaturization and promotes regrowth (B)</p> Signup and view all the answers

Flashcards

Anabolic Steroid Effect

Anabolic steroids stimulate protein synthesis, leading to increased muscle size and strength.

Testosterone Replacement Therapy

Using testosterone to treat men with low testosterone levels.

Anabolic-Androgenic Ratio

A measure of the anabolic (muscle-building) and androgenic (male characteristics) effects of a steroid.

Adverse Effects of Anabolic Steroids

High doses can cause issues like testicular shrinkage, breast growth in men, and virilization in women.

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Doping in Sports

Using anabolic steroids to enhance athletic performance, which is prohibited.

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Testicular Atrophy (from steroids)

Shrinking of the testicles caused by suppression of the body's natural testosterone production.

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Gynecomastia (from steroids)

Development of breast tissue in males due to steroid-induced estrogen increase.

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Virilisation in Females (from steroids)

Development of male characteristics in females due to increased androgens (male hormones).

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Virilization in Females

Development of male characteristics in women due to exposure to androgens.

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Hirsutism

Excessive hair growth in female pattern areas.

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Amenorrhea

Absence of menstruation (periods).

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Clitoral Hypertrophy

Enlargement of the clitoris.

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Cyproterone Acetate

Synthetic steroid with anti-androgenic and progestogenic effects.

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Androgen Antagonist

Medications that block the effects of androgens.

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Acne (steroid use)

Increased skin oil production leading to clogged pores and pimples.

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Male Pattern Baldness (steroid use)

Accelerated hair loss in individuals predisposed.

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Drospirenone's function

Drospirenone is a synthetic progestin that blocks mineralocorticoid receptors and reduces aldosterone's effect, leading to anti-androgenic effects and lowering fluid retention.

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Spironolactone's action

Spironolactone is a mineralocorticoid receptor blocker, reducing excessive androgen effects by interfering with androgen receptor function and lowering the production of androgens.

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Drospirenone's use in hormone therapy

Drospirenone, due to its anti-androgenic properties, is used in hormonal treatments for conditions linked to excess androgens, like acne and hirsutism.

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Spironolactone's use for women's health

Spironolactone helps treat women's conditions like acne, hirsutism, and hair loss (androgenetic alopecia), all related to excess androgen action.

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Mineralocorticoid receptor antagonist

A substance that blocks mineralocorticoid receptors, preventing the actions of aldosterone.

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Overactive Bladder

A condition marked by frequent urination, urgency, and leakage, often due to involuntary bladder muscle contractions.

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Muscarinic Receptor Antagonists

Drugs that block the action of acetylcholine at muscarinic receptors in the bladder, reducing muscle spasms and improving bladder control.

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Selective (M3) Muscarinic Antagonists

These drugs target primarily the M3 receptor, which is predominantly found in the bladder, minimizing side effects on other organs.

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Non-Selective Muscarinic Antagonists

These drugs block both M2 and M3 receptors, impacting other organs like salivary glands, heart, and gut, potentially causing dry mouth or heart rate changes.

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BPH (Benign Prostatic Hyperplasia)

Enlargement of the prostate gland, causing pressure on the urethra and urinary symptoms like frequent urination and difficulty starting.

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α1 Adrenoceptor Antagonists (BPH Treatment)

Drugs that block α1 receptors in the prostate and bladder, relaxing muscles and improving urine flow.

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Phosphodiesterase-5 (PDE-5) Inhibitors

Drugs that relax smooth muscles in the prostate and bladder, improving urine flow and potentially having anti-proliferative effects.

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First-Dose Hypotension (α1 Antagonists)

A sudden drop in blood pressure after the first dose of α1 adrenoceptor antagonists, especially with prazosin.

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Hair Follicle Miniaturization

A process where hair follicles shrink, leading to thinner hair and eventually hair loss. This is often caused by hormonal changes like an increase in DHT.

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DHT's Role in Hair Loss

Dihydrotestosterone (DHT) is a hormone that can shrink hair follicles, causing hair loss. It's a potent androgen, meaning it has a strong effect on male characteristics.

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5α-Reductase Inhibitors

Medications that block the production of DHT by inhibiting the 5α-reductase enzyme. This can slow down hair loss and even promote hair regrowth.

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Finasteride

A 5α-reductase inhibitor that primarily blocks type-I 5α-reductase, reducing DHT levels.

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Dutasteride

A 5α-reductase inhibitor that blocks both type-I and type-II 5α-reductase, leading to even lower DHT levels.

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DHT's Role in BPH

Dihydrotestosterone (DHT) promotes prostate growth. Higher levels of DHT can lead to an enlarged prostate, causing BPH symptoms.

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5α-Reductase Inhibitors for BPH

These drugs reduce DHT levels, shrinking the prostate and relieving urinary symptoms associated with BPH.

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Study Notes

Drugs Acting on Androgen Receptors

  • Testosterone undergoes extensive first-pass metabolism
  • Available as intramuscular injections and transdermal patches
  • Replacement therapy is used in male hypogonadism
  • Testosterone is abused for its anabolic effects

Anabolic Effects

  • Skeletal muscle hypertrophy (protein synthesis)
  • Increased muscle size and strength
  • Disproportionately large upper-body mass
  • Increased collagen synthesis in connective tissue
  • Increased bone density (suppression of osteoclast activity)
  • Increased erythropoietin production leading to increased red blood cell count

Structural Modification of Testosterone

  • Introduction of a double bond
  • Removal of the angular methyl group
  • Attachment of a methyl group
  • Attachment of various groups at carbon-2
  • Attachment of a pyrazole ring to the A-ring
  • Attachment of chlorine or hydroxyl group
  • Attachment of a 17-alpha alkyl group improves oral activity
  • Attachment of a 7-alpha methyl group improves intravenous activity

Anabolic:Androgenic Ratio

  • Testosterone (1)
  • Nandrolone (10)
  • Stanozolol (30)

Anabolic Steroids & Doping in Sports

  • Used as a performance-enhancing agent by athletes
  • Significant adverse effects
  • Banned by the World Anti-Doping Agency (WADA)

Anabolic Steroids: Adverse Effects

  • Supraphysiologic doses can affect other steroid receptors
  • Testicular atrophy and gynecomastia in males
  • Virilisation in females (hirsutism, amenorrhoea, hoarse voice, clitoral hypertrophy)
  • Acne, male pattern baldness, striae
  • Peliosis hepatis (hemorrhagic liver cysts)

Androgen Antagonists

Steroidal

  • Cyproterone acetate (progesterone agonist)
  • Drospirenone (progesterone agonist & mineralocorticoid antagonist)
  • Spironolactone (mineralocorticoid antagonist)
  • Used in androgen-dependent conditions (acne, hirsutism, androgenetic alopecia)

Non-Steroidal

  • Flutamide
  • Bicalutamide
  • Nilutamide
  • Enzalutamide
  • Used in prostate cancer

Drugs Acting on the Urinary System

Muscarinic Receptor Antagonists

  • Treatment of overactive bladder
  • Selective (M3) - darifenacin, solifenacin
  • Non-selective (M2) - trospium, oxybutynin, tolterodine, fesoterodine
  • present in salivary glands, cardiovascular system, brain, and GIT
  • More adverse effects in non-selective drugs

Phosphodiesterase-5 Inhibitors

  • Smooth muscle relaxation
  • Antiproliferative effects in prostatic & bladder smooth muscle
  • Tadalafil
  • Sildenafil (erectile dysfunction)

Drugs for Benign Prostatic Hyperplasia (BPH)

  • Bladder outlet obstruction (Lower urinary tract symptoms, LUTS)
  • Obstruction has static and dynamic components. Static->Muscle hyperplasia Dynamic-> Muscle spasm
  • α1-adrenergic receptor antagonists (Dynamic)
  • 5α-reductase inhibitors (Static)

α1-Adrenoceptor Antagonists

  • Non-selective - Prazosin, Terazosin, Doxazosin
  • Selective (α1A) - Tamsulosin, Silodosin

α1-Adrenoceptor Antagonists: Intraoperative Floppy Iris Syndrome

  • Intraoperative miosis, flaccid iris, prolapse (during cataract surgery in patients taking α1-adrenoceptor antagonists especially tamsulosin)
  • Discontinuation of medication does not reduce incidence, avoid starting treatment before surgery

5α-Reductase Inhibitors

  • 5α-reductase present in prostate & hair follicles (static obstruction)
  • Finasteride (inhibits type-1)
  • Dutasteride (inhibits type-1 & type-2)
  • Reduce the size of the prostate
  • Treatment for several months needed
  • Adverse effects: reduced libido, breast tenderness

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Description

Explore the mechanisms and effects of drugs acting on androgen receptors, with a focus on testosterone. This quiz covers testosterone metabolism, its anabolic effects, and structural modifications that enhance its activity. Test your knowledge on the implications of testosterone treatment and abuse.

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