Pharmacodynamics in Endocrine Disorders Quiz

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Questions and Answers

Which of the following is NOT a focus of the pharmacodynamic evaluations discussed in the provided text?

  • Hormone receptor interaction similarities
  • New classes of oral antidiabetics
  • Neuroendocrinology pharmacodynamic evaluation (correct)
  • The classical hypothalamus-pituitary-adrenal-gonadal axis

What concept related to hormone-receptor interaction is prominently featured in the discussion?

  • Intracellular signaling pathways
  • Hormone metabolism and degradation
  • The presence of hormone agonists and antagonists (correct)
  • Hormone synthesis mechanisms

Which endocrine disorders are reviewed separately from the classical hypothalamus-pituitary-adrenal-gonadal axis?

  • Pituitary disorders
  • Gonadal disorders
  • Adrenal disorders
  • Thyroid disorders (correct)

Among the listed drug classes, which one is NOT specifically mentioned as being evaluated as part of the pharmacodynamic evaluations?

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

What is the general focus of the pharmacological review in relation to endocrine disorders?

<p>The classical hypothalamus-pituitary-adrenal-gonadal axis (B)</p> Signup and view all the answers

According to the provided text, which of the following is given particular focus?

<p>The mechanism of action of new sophisticated insulin analogues (B)</p> Signup and view all the answers

What aspect of hormone action receives specific attention within the context of pharmacodynamics?

<p>The hormonal interaction with the receptor (B)</p> Signup and view all the answers

Which hormone is mentioned in the text as being evaluated, but that is not primarily secreted by the pituitary gland?

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

Which of the following accurately describes the primary function of glucagon?

<p>Elevating blood glucose levels by stimulating gluconeogenesis and glycogenolysis. (C)</p> Signup and view all the answers

Which of the following hormones does not directly stimulate glucagon secretion?

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

Glucagon belongs to the secretin family of hormones; what mechanism does it use to elicit its response?

<p>A membrane G-protein-coupled receptor that uses the adenylate cyclase system. (D)</p> Signup and view all the answers

Under what condition does glucagon induce lipolysis?

<p>In conditions of insulin suppression, like type 1 DM. (C)</p> Signup and view all the answers

Which of the following is a scenario in which glucagon would likely be considered a critical treatment option?

<p>A diabetic patient experiencing severe hypoglycemia who has lost consciousness. (B)</p> Signup and view all the answers

What is the name of short-acting insulin?

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

What is the approximate duration of action of insulin glargine?

<p>24 hours (C)</p> Signup and view all the answers

Which of the following best describes premixed insulin Humulin I?

<p>A premixed insulin that combines a short-acting and an intermediate-acting insulin. (C)</p> Signup and view all the answers

What is the primary role of progesterone during the luteal phase of the menstrual cycle?

<p>To prepare the endometrium for implantation. (A)</p> Signup and view all the answers

What effect does progesterone have on the immune response during pregnancy?

<p>It decreases the immune response. (A)</p> Signup and view all the answers

Which of the following is NOT a known effect of progesterone?

<p>Increasing the immune response. (A)</p> Signup and view all the answers

What is the primary hormonal component found in morning-after pills and abortion pills?

<p>Progestogens only. (A)</p> Signup and view all the answers

A drop in progesterone levels most likely facilitates the onset of which process?

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

Which uterine tissue is altered by progesterone?

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

Which of the following best describes the role of progestogens in combined oral contraceptive pills?

<p>They work in conjunction with estrogens to prevent pregnancy. (A)</p> Signup and view all the answers

What is the effect of progesterone specifically on the uterus during pregnancy?

<p>It decreases the contractility of the smooth muscle. (B)</p> Signup and view all the answers

What is the primary mechanism by which dihydrotestosterone (DHT) exerts its androgenic effects?

<p>By having a higher affinity for the testosterone receptor than testosterone. (A)</p> Signup and view all the answers

Besides an increase in muscle mass, which of the following is an additional anabolic effect of AASs?

<p>Upregulation of IGF-1 receptors (C)</p> Signup and view all the answers

What is the role of 5-alpha reductase in the context of androgenic effects?

<p>It converts testosterone into dihydrotestosterone (DHT). (B)</p> Signup and view all the answers

Which of the following conditions in men is NOT typically treated with antiandrogens?

<p>Anemia of chronic renal disease (B)</p> Signup and view all the answers

What is a known side effect of AASs related to hair and skin?

<p>Exacerbation of acne and male baldness (C)</p> Signup and view all the answers

In women, which of the following is a condition antiandrogens are used to treat?

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

What is the mechanism of action of antiandrogens?

<p>They block the androgen receptor and/or inhibit or suppress androgen production. (A)</p> Signup and view all the answers

Which of the following is NOT a clinical application of AASs?

<p>Treatment of hypersexuality (D)</p> Signup and view all the answers

Elevated glucagon levels may be associated with which condition?

<p>Necrolytic erythema migrans (D)</p> Signup and view all the answers

Which hormone is NOT synthesized in the anterior pituitary?

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

Pegylation of a GH analogue is primarily used for what purpose?

<p>Creating sustained release formulations (C)</p> Signup and view all the answers

Which factor does NOT directly modify GH receptor expression?

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

Which of the following is primarily used to measure a pharmacodynamic response to GH analog injection in GH-deficient children?

<p>Plasma GH levels, IGF-1 levels, glucose, and FFA levels (D)</p> Signup and view all the answers

Synthetic human growth hormone is NOT typically used for which condition?

<p>Addison's disease (B)</p> Signup and view all the answers

ACTH (Synachten) is primarily used for:

<p>Assessing suspected adrenocortical hypofunction (C)</p> Signup and view all the answers

Which of the following is a product released by the hypothalamus?

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

Which medication is associated with reduced rates of prostate surgery for benign prostate hyperplasia?

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

What type of drug is Elagolix, used in the treatment of endometriosis-associated pain?

<p>Oral GnRH antagonist (A)</p> Signup and view all the answers

Which medication has been historically linked to the treatment of diabetes and is also being researched for potential effects on longevity?

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

What is one of the studied side effects of peptide receptor radionuclide therapy for neuroendocrine tumors?

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

Which of the following is described as a less expensive option for treating type 2 diabetes?

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

In treating hypoparathyroidism, which is associated with less severe hypocalcemia?

<p>Vitamin D2 (D)</p> Signup and view all the answers

Which medication class is associated with functional outcomes, death, and rehospitalization in elderly nursing home residents after myocardial infarction?

<p>Beta-blockers (D)</p> Signup and view all the answers

Which of these medications is discussed in the context of opioid addiction?

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

Flashcards

Thiazolidinediones

These medications work by increasing the sensitivity of body tissues to insulin, leading to improved glucose control. Examples include pioglitazone and rosiglitazone.

DPP-4 Inhibitors

These drugs slow down the breakdown of incretin hormones, leading to increased insulin secretion and reduced glucagon release, improving glucose control.

GLP-1 Agonists

These medications mimic the action of the naturally occurring hormone GLP-1, leading to increased insulin secretion, reduced glucagon release, and slower gastric emptying.

SGLT-2 Inhibitors

These drugs block the reabsorption of glucose in the kidneys, leading to increased glucose excretion in the urine, improving glucose control.

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Prandial Glucose Regulators

These medications are specifically designed to control blood sugar levels after meals, improving postprandial glycemic control.

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Amylin Analogues

These medications mimic the action of the hormone amylin, leading to a reduction in glucagon secretion and slowing of gastric emptying.

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What are Androgen Anabolic Steroids (AASs)?

A group of synthetic compounds that mimic the effects of testosterone, either by binding to the same receptor or by increasing testosterone production. They are often used for their anabolic (muscle-building) effects.

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What is testosterone?

A type of steroid hormone that plays a crucial role in male sexual development, including the development of secondary sex characteristics, production of sperm, and maintenance of muscle mass.

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What is the testosterone receptor?

A specific type of receptor found inside cells that binds to testosterone and its synthetic counterparts, initiating a chain of events that leads to the expression of androgenic effects.

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What is Dihydrotestosterone (DHT)?

A powerful androgen that is produced within the body by the conversion of testosterone. It is even more potent than testosterone itself.

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What are antiandrogens?

A class of drugs that block the action of testosterone, either by preventing it from binding to its receptor or by inhibiting its production. They are often used to treat conditions like prostate cancer and hirsutism.

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Glucagon

A hormone produced by the pancreas, responsible for elevating blood glucose levels. When abnormally elevated, it can lead to conditions like glucagonoma, characterized by necrolytic erythema migrans.

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What is gynecomastia?

A condition that can occur as a result of testosterone or anabolic steroid use, characterized by the development of enlarged breasts in males.

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What is aromatization of testosterone?

The process of turning testosterone into a weaker form, known as estrogen. This can contribute to the development of gynecomastia in males.

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Glucagonoma

A type of tumor that occurs in the pancreas and produces excessive amounts of glucagon, resulting in abnormal blood glucose levels and symptoms like skin lesions.

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Necrolytic Erythema Migrans

A rare skin condition characterized by painful, red, and scaly patches that migrate over the body, often associated with glucagonoma.

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What is benign prostate hyperplasia (BPH)?

A medical condition characterized by an enlarged prostate gland, often found in older men. Anabolic steroids can worsen this condition.

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Multiple Endocrine Neoplasia (MEN) Type 1

A condition involving multiple tumors affecting different endocrine glands, including the pancreas. It can cause glucagonoma and other hormonal imbalances.

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Growth Hormone (GH)

A pituitary hormone that plays a crucial role in regulating growth and development. It's produced by the anterior pituitary gland and has a short half-life.

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Pegylation

The process of attaching polyethylene glycol (PEG) to a molecule, used to increase its size and extend its lifespan. Applied to GH, it creates a long-acting form.

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Pegvisomant (Somavert)

A type of GH analogue that has been pegylated, making it a long-acting treatment for acromegaly. It works by blocking GH receptor activity.

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Acromegaly

A disease characterized by excessive growth hormone production by the pituitary gland, resulting in abnormal growth and other symptoms.

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Rapid-acting Insulin

Insulin lispro (Humalog) and insulin aspart (Novorapid) are examples of rapid-acting insulins. They start working quickly within 15-20 minutes after injection and their effects last for 2-5 hours.

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Short-acting Insulin

Actrapid, Humulin S, and Velosulin are short-acting insulins. They begin working after 20 minutes and their effects last for 6-8 hours.

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Intermediate-acting Insulin

Humulin I is a premixed insulin combining 30% short-acting insulin and 70% intermediate-acting insulin. This combination provides a longer-lasting effect, peaking between 1 and 8 hours and lasting up to 22 hours.

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Long-acting Insulin

Long-acting insulins, such as insulin glargine (Lantus), insulin detemir (Levemir), or insulin degludec (Tresiba), have no peak activity. They provide a continuous, basal delivery of insulin over a period of time, ensuring a consistent blood sugar control.

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Premixed Insulin

Premixed insulin analogues, like Humalog Mix 25, Humalog Mix 50, and Novomix 30, combine both rapid and long-acting insulins in a single injection for a combined effect on blood sugar.

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Glucagon-Insulin Feedback System

Glucagon and insulin work together in a feedback system to maintain stable blood glucose levels. When blood sugar is low, glucagon is released to increase it. When blood sugar is high, insulin is released to lower it.

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Glucagon as Emergency Treatment

Glucagon is an emergency medicine used to treat severe hypoglycemia (low blood sugar) in patients with diabetes who are treated with insulin. It is administered when a patient has passed out or is unable to take sugar by mouth. It helps rapidly raise blood sugar levels.

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What is progesterone's nickname?

Progesterone is known as the "pregnancy hormone" because it plays a crucial role in preparing the uterus for implantation.

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How does progesterone prepare the uterus for implantation?

Progesterone converts the endometrium into a suitable environment for implantation by thickening the uterine lining and preparing it for a potential pregnancy.

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What happens to progesterone levels if pregnancy does not occur?

When pregnancy does not occur, progesterone levels decrease, triggering menstruation.

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How does progesterone affect the immune system during pregnancy?

Progesterone acts as an immune suppressant, temporarily reducing the body's natural immune response during pregnancy to protect the fetus from rejection.

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How does progesterone affect uterine contractions?

Progesterone inhibits uterine contractions, ensuring a smooth and peaceful environment for the developing fetus.

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How does progesterone influence lactation?

Progesterone suppresses lactation during pregnancy, preventing the release of breast milk until after birth.

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What possible role does progesterone play in labor onset?

A decrease in progesterone levels is thought to be one of the triggers that initiates labor.

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What is the difference in the hormonal composition of combined oral contraceptives, morning-after pills, and abortion pills?

Combined oral contraceptive pills contain both estrogens and progestogens, while morning-after pills and abortion pills primarily contain progestogens.

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Study Notes

Pharmacodynamic Evaluation: Endocrinology

  • This chapter discusses pharmacodynamic evaluations for common clinical endocrine disorders
  • Special focus on new oral antidiabetics and sophisticated insulin analogues
  • Clinical pharmacology reviews the hypothalamus-pituitary-adrenal-gonadal axis, and thyroid disorders separately
  • Emphasis on hormone receptor interactions and drug-ligand-receptor binding
  • Concepts of hormone agonists and antagonists are featured
  • Neuroendocrinology pharmacodynamic evaluation is excluded

Thiazolidinediones

  • DPP-4 Inhibitors
  • GLP-1 Agonists
  • SGLT-2 Inhibitors
  • Prandial Glucose Regulators
  • Amylin Analogues
  • Insulin Types and Forms
  • Glucagon
  • ACTH
  • Growth Hormone
  • Prolactin
  • Somatostatin
  • Melanocyte-Stimulating Hormones
  • Oxytocin
  • Antidiuretic Hormone

Contents

  • Introduction
  • Diabetes Mellitus
  • Metformin-Biguanides
  • Sulfonylureas
  • Alpha-Glucosidase Inhibitors
  • Thiazolidinediones
  • The Thyroid Gland: Hyper- and Hypothyroidism
  • Methimazole
  • Propylthiouracil
  • The Parathyroids
  • The Adrenals
  • Epinephrine
  • The Renin-Angiotensin-Aldosterone System

Diabetes Mellitus

  • Pharmacodynamics in DM are studied at a population level, mechanistic mode, metric model, or drug-targeted-mediated approach
  • Metformin improves glucose tolerance by decreasing hepatic glucose production, intestinal glucose absorption, and increasing peripheral glucose uptake
  • Metformin does not cause hypoglycemia under normal conditions
  • Metformin bioavailability is around 50-60%, and increasing doses result in absorption decrease
  • Food delays Metformin absorption; peak plasma levels are observed around 7 hours
  • Metformin is not metabolized in the liver and is excreted unchanged by the kidneys with a half-life of approximately 17 hours (plasma 6 hours)
  • Metformin contraindicated in severe renal impairment, known hypersensitivity, and acute/chronic metabolic acidosis
  • Lactic acidosis is an infrequent complication

Sulfonylureas

  • Acts as insulin secretagogues by binding to ATP potassium channels in the pancreas
  • Examples include Glimepiride, Glibenclamide, Gliclazide, Glipizide, and Tolbutamide
  • Sulfonylureas have extended effect despite short half-life due to active metabolites
  • Renal dysfunction prolongs half-life
  • Genetic mutations affect response to sulfonylureas

Alpha-Glucosidase Inhibitors

  • Slows carbohydrate digestion, reducing post-meal blood glucose
  • Examples include Acarbose and Miglitol
  • Primarily used as single treatment or combined with sulfonylureas
  • Gastrointestinal side effects (meteorism, flatulence, diarrhea) are common

Thiazolidinediones (TZDs) or Glitazones

  • Acts by targeting PPAR-gamma receptors affecting glucose and fat metabolism
  • Examples include Pioglitazone
  • Potential for boosting insulin sensitivity

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