L-16 Adrenergic Antagonists
37 Questions
1 Views

Choose a study mode

Play Quiz
Study Flashcards
Spaced Repetition
Chat to Lesson

Podcast

Play an AI-generated podcast conversation about this lesson

Questions and Answers

What is the primary function of adrenergic antagonist drugs?

  • To prevent or reverse the effects of norepinephrine or epinephrine. (correct)
  • To promote the synthesis of norepinephrine within the neuron.
  • To stimulate the actions of endogenously released epinephrine.
  • To enhance the release of norepinephrine from adrenergic neurons.
  • Which of the following is a primary target for adrenergic antagonist drugs?

  • Serotonergic receptors.
  • Cholinergic receptors.
  • Dopaminergic receptors.
  • Adrenoceptors. (correct)
  • How do adrenergic antagonists typically interact with adrenoceptors?

  • They prevent the agonist from binding to the receptor. (correct)
  • They promote the synthesis of the agonists within the neuron.
  • They increase the affinity of the receptors to agonists.
  • They act as full agonists, eliciting maximal response.
  • What is the main source of the agonists that adrenergic antagonists act upon?

    <p>Endogenously released norepinephrine or epinephrine. (C)</p> Signup and view all the answers

    Besides the primary endogenous agonists, what other type of substances can adrenergic antagonists counteract?

    <p>Exogenously, administered sympathomimetic agents. (B)</p> Signup and view all the answers

    Which of the following is a therapeutic use of an $\alpha_1$-selective antagonist?

    <p>Managing benign prostatic hyperplasia (B)</p> Signup and view all the answers

    A patient taking a monoamine oxidase inhibitor ingests tyramine-containing foods and experiences a hypertensive crisis. Which medication is most likely to treat this condition among the medications detailed in the text?

    <p>An α-blocker (D)</p> Signup and view all the answers

    What is the primary mechanism by which prazosin lowers blood pressure?

    <p>Relaxation of arterial and venous smooth muscle (D)</p> Signup and view all the answers

    Which of the following is a common adverse effect associated with taking prazosin?

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

    Which adrenoceptor subtype is primarily responsible for smooth muscle contraction in the prostate?

    <p>$\alpha_{1A}$ (A)</p> Signup and view all the answers

    Which of the following is a contraindication for the use of $\alpha_1$-selective antagonists mentioned in the text?

    <p>Coronary artery disease (D)</p> Signup and view all the answers

    What is the recommended approach to minimize the first-dose effect of orthostatic hypotension with prazosin?

    <p>Administering one-third or one-fourth of the normal dose at bedtime (C)</p> Signup and view all the answers

    Which of the following is an off-label therapeutic use of prazosin?

    <p>Treatment of nightmares and insomnia associated with PTSD (C)</p> Signup and view all the answers

    What is the primary distinction in categorizing α-blockers?

    <p>Their selectivity for α1 versus α2 receptors. (D)</p> Signup and view all the answers

    Which of the following is the longest-acting alpha-1 adrenergic antagonist?

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

    What is a characteristic of irreversible α-blockers?

    <p>They form a stable bond with the receptor. (A)</p> Signup and view all the answers

    What is the main effect of blocking α1-adrenoceptors on the cardiovascular system?

    <p>Reduced peripheral vascular resistance and decreased blood pressure. (A)</p> Signup and view all the answers

    A patient is starting on terazosin therapy. Which of the following instructions is most important to provide to the patient regarding medication administration?

    <p>Avoid sudden changes in position. (A)</p> Signup and view all the answers

    Which of the following alpha-adrenergic antagonists is primarily used for benign prostatic hyperplasia and is known to have the worst incidence of intraoperative floppy iris syndrome?

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

    Why does the lowering of blood pressure via α1-blockade often induce reflex tachycardia?

    <p>As a compensatory response to the fall in blood pressure. (B)</p> Signup and view all the answers

    Which of the following describes a key difference in mechanism of action between tamsulosin and terazosin?

    <p>Tamsulosin primarily blocks α1A receptors, while terazosin blocks both α1A and α1B receptors. (B)</p> Signup and view all the answers

    What is the primary mechanism by which α1-adrenergic receptor blockade reduces blood pressure?

    <p>By decreasing sympathetic tone in blood vessels. (C)</p> Signup and view all the answers

    What is a significant difference between reversible and irreversible α-blockers?

    <p>Reversible blockers bind temporarily to the receptors. (D)</p> Signup and view all the answers

    Which of the following is an adverse effect specifically associated with doxazosin, but not the other listed alpha-1 blockers?

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

    A patient is experiencing retrograde ejaculation while taking an alpha-adrenergic antagonist, which medication is most likely causing this side effect?

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

    What is the clinical utility of selective α2-adrenergic blockers?

    <p>They have limited clinical usefulness. (C)</p> Signup and view all the answers

    Where does the normal sympathetic control of vasculature largely occur?

    <p>Through agonist actions on α1-adrenergic receptors. (D)</p> Signup and view all the answers

    Which of the following statements best explains the pharmacological effect of alpha-1 adrenergic antagonists on blood pressure?

    <p>They decrease peripheral vascular resistance by causing relaxation of smooth muscle, resulting in decreased BP. (D)</p> Signup and view all the answers

    Which of the following medications increases central sympathetic activity through its mechanism of action?

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

    Which of the following best describes the mechanism of action of phenoxybenzamine?

    <p>A noncompetitive antagonist that forms a covalent bond with α-receptors causing irreversible blockade. (A)</p> Signup and view all the answers

    What is the primary reason phenoxybenzamine is no longer a first-line treatment for chronic hypertension?

    <p>It leads to significant reflex tachycardia, counteracting the desired effect of lowering blood pressure. (C)</p> Signup and view all the answers

    A patient is experiencing reflex tachycardia after being administered phenoxybenzamine. Which of the following medications could be used to manage this side effect?

    <p>A β-blocker, such as metoprolol. (C)</p> Signup and view all the answers

    Which of the following best describes the mechanism of action of phentolamine?

    <p>A competitive, reversible antagonist of both α1- and α2-receptors. (B)</p> Signup and view all the answers

    Which of the following is a therapeutic use for phentolamine that is NOT listed for phenoxybenzamine?

    <p>Prevention of rebound hypertension due to abrupt clonidine withdrawal. (C)</p> Signup and view all the answers

    A patient with pheochromocytoma is prescribed phenoxybenzamine. Why is this drug considered a suitable initial choice?

    <p>Its long-lasting, irreversible blockade of α-receptors makes it effective in controlling the hypertension associated with this condition. (C)</p> Signup and view all the answers

    A patient taking phenoxybenzamine reports difficulty with ejaculation. What is the best explanation for this effect?

    <p>Blockade of α-receptors in the reproductive system. (C)</p> Signup and view all the answers

    Which of the following adverse effects is MOST likely to occur with both phenoxybenzamine and phentolamine treatment?

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

    Flashcards

    Adrenergic Antagonists

    Drugs that block the effects of norepinephrine and epinephrine by binding to adrenergic receptors.

    How do adrenergic antagonists work?

    These drugs interact with either alpha (α) or beta (β) adrenoceptors to prevent or reverse the effects of adrenaline or noradrenaline.

    What do adrenergic antagonists do?

    These drugs prevent or reverse the actions of naturally released norepinephrine or epinephrine or even synthetically made adrenaline-like drugs.

    What are some clinical uses of Adrenergic Antagonists?

    They can be used to treat conditions like high blood pressure, anxiety, or even some types of heart problems.

    Signup and view all the flashcards

    Why do we use adrenergic antagonists?

    These drugs are used to manage symptoms related to the excess production or actions of adrenaline or noradrenaline.

    Signup and view all the flashcards

    α-blockers

    Drugs that block α-adrenergic receptors, classified based on their selective affinity for α1 or α2 receptors.

    Signup and view all the flashcards

    Nonselective α-blockers

    α-blockers that bind to both α1 and α2 receptors indiscriminately.

    Signup and view all the flashcards

    Selective α-blockers

    α-blockers that target either α1 or α2 receptors specifically.

    Signup and view all the flashcards

    Reversible α-blockers

    α-blockers that can be reversed, allowing the receptor to regain function.

    Signup and view all the flashcards

    Irreversible α-blockers

    α-blockers that permanently bind to the receptor, rendering it inactive.

    Signup and view all the flashcards

    α1-adrenoceptor blockade

    Blocking α1-adrenergic receptors primarily affects blood pressure, leading to decreased peripheral vascular resistance.

    Signup and view all the flashcards

    Reflex tachycardia

    Blocking α1 receptors results in lower blood pressure, causing the heart to beat faster to compensate.

    Signup and view all the flashcards

    Selective α2-adrenergic blockers

    Selective targeting of α2 receptors has limited use in clinical practice.

    Signup and view all the flashcards

    Hypertensive Crisis

    A condition of dangerously high blood pressure, often caused by tyramine-rich foods in patients taking monoamine oxidase inhibitors (MAOIs).

    Signup and view all the flashcards

    Alpha-Blocker Antagonist

    A drug used to reverse the effects of alpha-agonists, such as dopamine, epinephrine, norepinephrine, and phenylephrine.

    Signup and view all the flashcards

    Preventing Dermal Necrosis

    The use of an alpha-blocker to prevent tissue damage after accidental injection of norepinephrine outside a vein.

    Signup and view all the flashcards

    Orthostatic Hypotension

    A potential side effect of alpha-blockers, especially during the first dose, causing a sudden drop in blood pressure when standing.

    Signup and view all the flashcards

    Alpha1A Receptor

    A type of alpha-receptor found in the prostate gland.

    Signup and view all the flashcards

    Alpha1B Receptor

    A type of alpha-receptor located in both the prostate and blood vessels.

    Signup and view all the flashcards

    Alpha1D Receptor

    A type of alpha-receptor primarily found in blood vessels.

    Signup and view all the flashcards

    How do alpha-blockers help with BPH?

    Alpha-blockers like Prazosin, Doxazosin, Terazosin, Alfuzosin, Tamsulosin, and Silodosin can relax the prostate muscle, improving urine flow.

    Signup and view all the flashcards

    What is the main action of Phenoxybenzamine?

    A medication that blocks alpha-receptors, causing a decrease in peripheral vasoconstriction and leading to reduced blood pressure. It primarily affects alpha-1 receptors.

    Signup and view all the flashcards

    What kind of duration effect does Phenoxybenzamine have?

    A persistent effect, lasting for a longer period, due to the formation of a strong bond with the receptor.

    Signup and view all the flashcards

    Is the blocking effect of Phenoxybenzamine reversible or not?

    Since Phenoxybenzamine binds permanently to alpha-receptors, it can't be reversed easily, unlike other medications.

    Signup and view all the flashcards

    Which type of alpha receptor does Phenoxybenzamine predominantly target?

    The ability of a drug to affect the body can vary based on how strongly it binds to a specific type of receptor. Phenoxybenzamine acts more strongly on alpha-1 receptors.

    Signup and view all the flashcards

    What is the main action of Phentolamine?

    Phentolamine is a medication that temporarily blocks alpha-1 and alpha-2 receptors, reversing the effects of adrenaline-like chemicals.

    Signup and view all the flashcards

    Is the blocking effect of Phentolamine reversible or not?

    Unlike Phenoxybenzamine's permanent binding, Phentolamine's interaction with receptors is temporary and can be reversed.

    Signup and view all the flashcards

    How are Phenoxybenzamine and Phentolamine used in treating pheochromocytoma?

    Both Phenoxybenzamine and Phentolamine are used to control high blood pressure caused by tumors in the adrenal glands (pheochromocytoma), but Phenolamine's action is shorter.

    Signup and view all the flashcards

    In what other situation might Phentolamine be used?

    Phentolamine can be used to treat high blood pressure caused by withdrawal from medications like clonidine. This helps prevent sudden pressure increases.

    Signup and view all the flashcards

    What does the term α1A selectivity refer to?

    α1-blockers that relax smooth muscle in the prostate and bladder, improving urine flow. They are primarily prescribed for benign prostatic hyperplasia.

    Signup and view all the flashcards

    What is Intraoperative Floppy Iris Syndrome (IFIS)?

    A condition characterized by a floppy iris during cataract surgery, often caused by α1A-blockers such as tamsulosin.

    Signup and view all the flashcards

    How can α1-blockers affect cataract surgery?

    A side effect of α1-blockers, especially tamsulosin, that can occur during cataract surgery, leading to difficulty in accessing the lens.

    Signup and view all the flashcards

    What are non-selective α-blockers?

    Non-selective α-blockers that act on both α1 and α2 receptors, causing vasodilation and lowering blood pressure.

    Signup and view all the flashcards

    What is yohimbine and what are its actions?

    A selective α2-blocker that increases central sympathetic activity and norepinephrine release, primarily found in the bark of the Yohimbe tree.

    Signup and view all the flashcards

    What is orthostatic hypotension?

    α1-blockers can cause a sudden drop in blood pressure upon standing, leading to dizziness or fainting, especially with the first dose.

    Signup and view all the flashcards

    What are the main effects of α1-blockers on blood pressure?

    α1-blockers such as terazosin and doxazosin, used for hypertension and benign prostatic hyperplasia, are potent vasodilators that lower blood pressure by decreasing peripheral vascular resistance.

    Signup and view all the flashcards

    What is angioedema?

    A rare adverse effect of α1-blockers, specifically doxazosin, involving swelling under the skin, potentially caused by an immune reaction.

    Signup and view all the flashcards

    Study Notes

    Adrenergic Antagonists Lecture - 16

    • Mayur S. Parmar, Ph.D., Assistant Professor of Pharmacology, Department of Foundational Sciences, Dr. Kiran C. Patel College of Osteopathic Medicine, Nova Southeastern University
    • Lecture focused on Adrenergic Antagonists

    Learning Objectives

    • Identify specific alpha-adrenergic antagonists and the receptor subtype they act upon.
    • Discuss the mechanism of action of alpha-adrenergic antagonists.
    • Discuss the pharmacological effects and clinical efficacy of alpha-adrenergic antagonists based on receptor interactions.
    • Discuss the therapeutic uses and adverse effects of alpha-adrenergic antagonists.
    • Discuss potential contraindications and drug interactions for selected alpha-adrenergic antagonists and the reasons.

    Adrenergic Antagonists

    • Drugs interacting with alpha or beta adrenoceptors, preventing or reversing norepinephrine/epinephrine or sympathomimetic agent actions.
    • Alpha blockers: Nonselective (alpha-1 and alpha-2) or Selective (alpha-1 or alpha-2).
    • Beta blockers: Nonselective (beta-1 and beta-2) or Selective (beta-1).
    • Mixed Blockers: Alpha and Beta

    Alpha-Adrenergic Antagonists

    • Key Points:
      • Based on selective affinity for alpha-1 vs. alpha-2 receptors.
      • Some are reversible (e.g., phentolamine, prazosin) and some are irreversible (e.g., phenoxybenzamine).
      • Drugs that block alpha-1 receptors affect blood pressure significantly.

    Alpha-Adrenergic Antagonists: Nonselective

    • Phenoxybenzamine
    • Phentolamine

    Phenoxybenzamine

    • Key Points:
      • Long duration of action, irreversible.
      • Blocks alpha-1 receptors more than alpha-2.
      • Mechanism involves covalent bond formation with the receptor.
      • Use in pheochromocytoma (presurgical).
      • Adverse effects: orthostatic hypotension, reflex tachycardia, myocardial ischemia.

    Phentolamine

    • Key Points:
      • Short duration of action, reversible.
      • Blocks alpha-1 and alpha-2 receptors.
      • Pharmacological effects similar to phenoxybenzamine.
      • Used in short-term management of pheochromocytoma, controlling rebound hypertension from clonidine, and treating hypertensive crisis.

    a1-Selective Adrenoceptor Antagonists

    • Prazosin
    • Doxazosin
    • Terazosin
    • Alfuzosin
    • Tamsulosin
    • Silodosin

    Alpha 1A-Receptor subtypes

    • Important for prostatic smooth muscle relaxation, improving urine flow in BPH

    Prazosin

    • Short duration of action; selective alpha-1 blocker.
    • Beneficial in hypertension and benign prostatic hyperplasia.
    • Risk of first-dose hypotension.
    • Other related issues: Intraoperative floppy iris syndrome, dizziness, and night terrors and insomnia

    Terazosin and Doxazosin

    • Longer duration of action than prazosin; selective alpha-1 blockers.
    • Used for hypertension and benign prostatic hyperplasia.
    • Note: Doxazosin has a longer half-life (22 hrs) than Terazosin(9–12 hrs).

    Tamsulosin, Alfuzosin, Silodosin

    • More selective for alpha-1A receptors in the prostate.
    • Useful for benign prostatic hyperplasia.
    • Note: Tamsulosin should be taken with food, while terazosin does not need to be taken with food

    a2-Selective Adrenoceptor Antagonist

    • Yohimbine

    Yohimbine

    • Found in Yohimbe bark, selective alpha-2 antagonist.
    • Causes increased central sympathetic activity.
    • Increases norepinephrine release.
    • Obsolete therapeutic use in erectile dysfunction and used in research.

    Adrenergic Antagonists: Contraindications and Drug Interactions

    • Contraindications:

      • Hypersensitivity to the drug.
      • Hepatic impairment.
      • Severe renal impairment (Silodosin only).
      • DO NOT USE Alfuzosin in patients at risk for QT prolongation (prolong QT intervals).
    • Drug interactions:

      • Tricyclic antidepressants may increase the risk of postural hypotension.
      • Concurrent use with strong CYP3A4 inhibitors (Silodosin or alfuzosin only).

    Resources

    • Basic & Clinical Pharmacology, 15e
    • Lippincott Illustrated Reviews: Pharmacology, 7e
    • Principles of Pharmacology: The Pathophysiologic Basis of Drug Therapy Fourth Edition, 4e

    Studying That Suits You

    Use AI to generate personalized quizzes and flashcards to suit your learning preferences.

    Quiz Team

    Related Documents

    Description

    This quiz covers the key concepts of adrenergic antagonists, focusing on alpha-adrenergic antagonists including their mechanisms of action, pharmacological effects, and therapeutic uses. It also addresses their adverse effects, contraindications, and potential drug interactions. Ideal for pharmacology students seeking to deepen their understanding of these important medications.

    More Like This

    Use Quizgecko on...
    Browser
    Browser