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Questions and Answers
What primary action does Drospirenone perform as a mineralocorticoid receptor antagonist?
What primary action does Drospirenone perform as a mineralocorticoid receptor antagonist?
Which of the following conditions is NOT typically treated with Spironolactone?
Which of the following conditions is NOT typically treated with Spironolactone?
How does Nilutamide achieve its anti-androgenic effects?
How does Nilutamide achieve its anti-androgenic effects?
What is a common use for drugs like Drospirenone and Spironolactone?
What is a common use for drugs like Drospirenone and Spironolactone?
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Which of the following best describes the relationship between Spironolactone and androgen receptors?
Which of the following best describes the relationship between Spironolactone and androgen receptors?
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Which of the following is NOT an anabolic effect of testosterone?
Which of the following is NOT an anabolic effect of testosterone?
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What significant adverse effect can result from supraphysiologic doses of anabolic steroids in males?
What significant adverse effect can result from supraphysiologic doses of anabolic steroids in males?
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How does the anabolic:androgenic ratio of nandrolone compare to that of testosterone?
How does the anabolic:androgenic ratio of nandrolone compare to that of testosterone?
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Which of the following conditions is a result of high estrogen levels due to anabolic steroid use in males?
Which of the following conditions is a result of high estrogen levels due to anabolic steroid use in males?
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What effect can anabolic steroids have when interacting with glucocorticoid receptors?
What effect can anabolic steroids have when interacting with glucocorticoid receptors?
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In females, virilization may lead to which of the following symptoms?
In females, virilization may lead to which of the following symptoms?
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Which type of administration method for testosterone bypasses first-pass metabolism?
Which type of administration method for testosterone bypasses first-pass metabolism?
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Which of the following is a possible adverse effect associated with anabolic steroids affecting the liver?
Which of the following is a possible adverse effect associated with anabolic steroids affecting the liver?
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What is a potential irreversible effect of anabolic steroid use in females?
What is a potential irreversible effect of anabolic steroid use in females?
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Which of the following conditions can be treated with cyproterone acetate?
Which of the following conditions can be treated with cyproterone acetate?
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What is the primary cause of acne associated with anabolic steroid use?
What is the primary cause of acne associated with anabolic steroid use?
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Which of the following is NOT a characteristic commonly associated with virilization in females due to anabolic steroid use?
Which of the following is NOT a characteristic commonly associated with virilization in females due to anabolic steroid use?
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How does cyproterone acetate work to counteract the effects of androgens?
How does cyproterone acetate work to counteract the effects of androgens?
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What dermatological condition is caused by rapid increases in muscle size due to steroid use?
What dermatological condition is caused by rapid increases in muscle size due to steroid use?
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What characterizes male pattern baldness associated with steroid use?
What characterizes male pattern baldness associated with steroid use?
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What condition is characterized by the presence of hemorrhagic liver cysts in individuals using anabolic steroids?
What condition is characterized by the presence of hemorrhagic liver cysts in individuals using anabolic steroids?
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What is the primary mechanism of action of muscarinic receptor antagonists in treating overactive bladder?
What is the primary mechanism of action of muscarinic receptor antagonists in treating overactive bladder?
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Which drug class is primarily indicated for the treatment of benign prostatic hyperplasia (BPH)?
Which drug class is primarily indicated for the treatment of benign prostatic hyperplasia (BPH)?
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Which of the following is a selective α1A adrenoceptor antagonist used for urinary symptoms?
Which of the following is a selective α1A adrenoceptor antagonist used for urinary symptoms?
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What is the main effect of phosphodiesterase-5 inhibitors in the context of prostate conditions?
What is the main effect of phosphodiesterase-5 inhibitors in the context of prostate conditions?
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What is the consequence of dihydrotestosterone (DHT) binding to hair follicle androgen receptors in genetically predisposed individuals?
What is the consequence of dihydrotestosterone (DHT) binding to hair follicle androgen receptors in genetically predisposed individuals?
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Which enzyme is primarily responsible for converting testosterone to dihydrotestosterone (DHT) in the prostate?
Which enzyme is primarily responsible for converting testosterone to dihydrotestosterone (DHT) in the prostate?
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What potential side effect is associated with the use of prazosin, a non-selective α1 adrenoceptor antagonist?
What potential side effect is associated with the use of prazosin, a non-selective α1 adrenoceptor antagonist?
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Which drug primarily inhibits both type 1 and type 2 5-alpha reductase enzymes?
Which drug primarily inhibits both type 1 and type 2 5-alpha reductase enzymes?
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What is the primary role of dihydrotestosterone (DHT) in benign prostatic hyperplasia (BPH)?
What is the primary role of dihydrotestosterone (DHT) in benign prostatic hyperplasia (BPH)?
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Which of the following statements about 5α-reductase inhibitors is true?
Which of the following statements about 5α-reductase inhibitors is true?
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What is NOT a common adverse effect of 5α-reductase inhibitors?
What is NOT a common adverse effect of 5α-reductase inhibitors?
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Intraoperative floppy iris syndrome is associated with the use of which type of medication?
Intraoperative floppy iris syndrome is associated with the use of which type of medication?
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What is a key consequence of elevated DHT in the prostate?
What is a key consequence of elevated DHT in the prostate?
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What is the consequence of discontinuing medication for intraoperative floppy iris syndrome?
What is the consequence of discontinuing medication for intraoperative floppy iris syndrome?
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Which enzyme is primarily targeted by 5α-reductase inhibitors?
Which enzyme is primarily targeted by 5α-reductase inhibitors?
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What is the effect of reducing DHT levels on hair follicles?
What is the effect of reducing DHT levels on hair follicles?
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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.
