Steroidal Hormones Overview
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Questions and Answers

The use of anabolic steroids by athletes began in the 1940s.

True (A)

Which of the following is a common route of administration for testosterone esters?

  • Oral
  • Intramuscular (correct)
  • Subcutaneous
  • Intravenous

What is the primary reason for the use of anabolic steroids by athletes?

To enhance athletic performance

The use of anabolic steroids by athletes became ______ after its initial introduction in the late 1940s.

<p>widespread</p> Signup and view all the answers

Testosterone is a naturally occurring hormone found in both males and females.

<p>True (A)</p> Signup and view all the answers

Which of these options is NOT a reason for the use of anabolic steroids by athletes?

<p>To improve cardiovascular health (A)</p> Signup and view all the answers

What does the abbreviation 'IM' stand for in the context of testosterone administration?

<p>Intramuscular</p> Signup and view all the answers

Match the following terms with their definitions:

<p>Anabolic steroids = Synthetic hormones that mimic the effects of testosterone Athletic performance = The ability to perform physical tasks efficiently and effectively Widespread = Occurring or affecting a large number of people or areas</p> Signup and view all the answers

Synthetic anabolic androgenic steroids are chemically similar to ______ and can have significant side effects.

<p>testosterone</p> Signup and view all the answers

Match the following terms with their corresponding descriptions:

<p>Testosterone = A naturally occurring hormone responsible for male sexual development Anabolic androgenic steroids = Synthetic compounds that mimic testosterone's effects 17b-Esters = Chemical modifications that enhance the duration of action of testosterone</p> Signup and view all the answers

Testosterone is the major natural and androgenic hormone.

<p>True (A)</p> Signup and view all the answers

What is the primary effect of the hormones mentioned in the content on protein synthesis?

<p>They increase protein synthesis (A), They decrease protein catabolism (C)</p> Signup and view all the answers

Explain how the hormones described in the content cause nitrogen retention.

<p>They stimulate protein synthesis, leading to an increased requirement for nitrogen to build new proteins. Additionally, they decrease protein breakdown, further reducing nitrogen loss from the body.</p> Signup and view all the answers

The hormones described in the content promote an ______ effect.

<p>anabolic</p> Signup and view all the answers

Match the following terms with their correct definitions:

<p>Androgenic = Relating to the development of male characteristics Anabolic = Promoting the synthesis of complex molecules from simpler ones Catabolism = The breakdown of complex molecules into simpler ones Nitrogen retention = The body holding onto nitrogen, essential for protein synthesis</p> Signup and view all the answers

Which of the following is NOT a symptom of an enlarged prostate in men?

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

Antiandrogenic agents are drugs that block or inhibit the effects of androgens.

<p>True (A)</p> Signup and view all the answers

What are two common symptoms of excess androgen levels in women?

<p>Beard growth and baldness</p> Signup and view all the answers

Antiandrogenic agents are ______ of androgens.

<p>antagonists</p> Signup and view all the answers

Match the following symptoms with their associated condition:

<p>Enlarged prostate = Impotency Excess androgen in women = Beard growth Excess androgen in men = Breast enlargement Antiandrogenic agents = Block androgen action</p> Signup and view all the answers

What is the major metabolite of Flutamide that has more powerful antiandrogenic effects?

<p>2-hydroxyflutamide (C)</p> Signup and view all the answers

Flutamide has a higher affinity for androgen receptors than its metabolite, 2-hydroxyflutamide.

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

What process does Flutamide undergo that affects its metabolism?

<p>extensive first-pass metabolism</p> Signup and view all the answers

Flutamide acts by competing with D for __________ receptors.

<p>androgen</p> Signup and view all the answers

Which of the following is an example of a non-steroidal competitive antagonist?

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

5α-Reductase inhibitors are used to enhance androgenic biosynthesis.

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

Name a class of drugs used as competitive antiandrogens.

<p>Steroidal competitive antagonists</p> Signup and view all the answers

Flutamide is classified as a __________ antiandrogen.

<p>non-steroidal</p> Signup and view all the answers

Match the following antiandrogens with their categories:

<p>Cyproterone = Steroidal competitive antagonist Flutamide = Non-steroidal competitive antagonist 5α-Reductase inhibitors = Inhibitors of androgenic biosynthesis</p> Signup and view all the answers

Flashcards

Nitrogen Retention

The process of retaining nitrogen in the body, enhancing protein synthesis.

Protein Synthesis

The formation of proteins from amino acids, stimulated by certain hormones.

Protein Catabolism

The breakdown of proteins into amino acids, which decreases with certain hormones.

Anabolic Effect

The physiological outcome that promotes the building of complex molecules, like proteins.

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Testosterone

The primary natural androgenic hormone responsible for male traits and anabolic effects.

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Anabolic Steroids

Synthetic substances that mimic testosterone to enhance muscle growth and performance.

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History of Use

Athletes began using anabolic steroids in the late 1940s.

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Widespread Usage

The practice of using anabolic steroids has become common among athletes.

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Performance Enhancement

Using substances like anabolic steroids to improve athletic ability.

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Legal and Ethical Issues

The use of anabolic steroids raises legal and moral questions in sports.

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Androgenic effects

Effects related to male characteristics, such as facial hair and deeper voice.

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17b-Esters

Chemical modifications for testosterone used for longer-lasting effects when injected.

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IM injection

Intramuscular injection method for delivering steroids into the body.

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Competitive Antiandrogens

Drugs that block androgen receptors to inhibit androgen effects.

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Steroidal Competitive Antagonists

A type of antiandrogen, like Cyproterone, that is steroid-based.

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Non-Steroidal Competitive Antagonists

Antiandrogens such as Flutamide that are not steroid-based.

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5α-Reductase Inhibitors

Drugs that inhibit the conversion of testosterone to DHT.

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DHT

Dihydrotestosterone, a potent androgen derived from testosterone.

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Enlarged prostate

An increase in the size of the prostate gland, often causing urinary issues.

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Breast enlargement in men

An increase in breast tissue in males, often linked to hormonal changes.

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Antiandrogenic agents

Medications that block the effects of androgens, like testosterone.

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Effects of excess androgens in women

Symptoms include beard growth, baldness, deepened voice, and breast reduction.

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Deepened voice in women

A lower pitch of voice in females, often due to hormonal imbalance.

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Flutamide

An antiandrogen medication that competes with D for androgen receptors.

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First-pass metabolism

The process where drug concentration is significantly reduced before reaching systemic circulation.

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CYP1A2

A cytochrome P450 enzyme involved in drug metabolism, specifically flutamide.

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2-hydroxyflutamide

The major metabolite of flutamide with higher receptor affinity and potency.

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Antiandrogen

A substance that inhibits the biological effects of androgens like testosterone.

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Study Notes

Steroidal Hormones

  • Steroidal hormones include male sex hormones, also known as androgens.
  • Androgens control the development of male characteristics, sperm production, growth of sex organs (prostate and seminal vesicles), and metabolic effects during adolescence.
  • Androgens promote nitrogen retention by stimulating protein synthesis (anabolic effect) and decreasing the rate of protein catabolism.
  • Testosterone is the major natural androgenic hormone.

Active Form of Testosterone

  • The active metabolite of testosterone is 5α-dihydrotestosterone (DHT).
  • DHT is formed by the action of the 5α-Reductase enzyme.
  • DHT is considered the most potent endogenous androgen.
  • Testosterone is considered a prohormone.

Testosterone Esters

  • Natural steroids, like testosterone, are inactive when taken orally.
  • Long-acting forms of testosterone are achieved through ester derivatives.
  • Esterification of testosterone with acids (like cyclopentylpropionate and undecanoate) at the 17β-position enhances duration of action when administered intramuscularly (IM).

Metabolism of Testosterone and 5α-Dihydrotestosterone (5α-DHT)

  • Metabolites, including conjugates, are formed during the metabolism of testosterone and 5α-DHT.
  • The process involves various enzymes and reactions that transform these hormones into different compounds.

Synthetic Androgens and Anabolic Agents

  • 17α-Methyltestosterone is an orally active derivative with androgenic and anabolic activity.
  • Increasing the length of the 17α-alkyl side chain decreases androgenic activity.
  • The 17α-ethynyl group creates compounds with pregestational activity.
  • Separating androgenic from anabolic activity is important in developing anabolic agents.

Specific Anabolic Steroids

  • Oxandrolone is a heterocyclic analogue of 17α-methyltestosterone with a lactone ring, susceptible to hydrolysis.
  • Oxandrolone has a higher anabolic activity and slightly androgenic activity. It is used as an anabolic agent.
  • Stanozolol is another heterocyclic compound primarily used for its anabolic activity.

17β-Testosterone Acetate Derivatives

  • Alkylation at the C1 position generally increases anabolic activity in androstane molecules.
  • Methenolone despite not containing 17α-CH3 has potent anabolic activity and is often administered orally.
  • Methenolone acetate, and other derivatives, are available as IM injections for long-acting anabolic effects.

19-Norandrogens

  • Removing the 19-methyl group from androgens produces 19-norandrogens with a more favorable anabolic-to-androgenic ratio.
  • Nandrolone exemplifies this class, with a potent 4:1 anabolic-to-androgenic ratio.
  • Nandrolone decanoate is a slower-acting ester suitable for deep intramuscular injections..

Abuse of Steroidal Anabolic Agents

  • Anabolic steroid use by athletes has increased since the late 1940s.
  • The FDA has issued alerts about the risks involved in abuse.
  • Side effects of misuse can include increased risk of cardiovascular issues, aggression, liver damage, and various problems in both men and women (e.g., testicular damage, prostate enlargement, and feminization in men).

Antiandrogenic Agents

  • Antiandrogens include both steroidal and nonsteroidal competitive antagonists.

  • Steroidal competitive antagonists block androgen receptors(e.g., Cyproterone).

  • Nonsteroidal competitive antagonists block androgen receptors(e.g., Flutamide).

  • 5α-reductase inhibitors directly block the conversion of testosterone to DHT. The resulting lowered DHT levels can have beneficial effects (e.g., for benign prostatic hyperplasia (BPH)). Finasteride and Dutasteride are examples of this class, impacting androgenic activity.

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Steroidal Hormones PDF

Description

Explore the essential concepts of steroidal hormones, focusing on androgens like testosterone and its active form, DHT. Understand the role of these hormones in male development, protein synthesis, and the use of testosterone esters. This quiz provides a comprehensive review of hormonal functions and metabolites.

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