:L-17 Adrenergic Antagonists and Their Functions

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Questions and Answers

What is the primary function of adrenergic antagonist drugs?

  • To directly synthesize adrenaline and noradrenaline in neuron.
  • To prevent or reverse the effects of adrenergic agonists. (correct)
  • To stimulate the synthesis of norepinephrine.
  • To enhance the release of epinephrine.

With which specific types of receptors do adrenergic antagonist drugs primarily interact?

  • Only with muscarinic receptors.
  • With both α- and β-adrenoceptors. (correct)
  • Only with ligand-gated ion channels in neurons.
  • Only with cholinergic receptors.

What actions do adrenergic antagonists counteract?

  • Actions of endogenously released norepinephrine or epinephrine. (correct)
  • Actions of exogenously administered parasympathomimetic drugs.
  • Actions of endogenously released acetylcholine.
  • Synthesis of norepinephrine within the vesicles.

According to the content provided, how do adrenergic antagonists function at the receptor level?

<p>By preventing agonist binding or signaling. (D)</p> Signup and view all the answers

If a patient is administered with an adrenergic antagonist, what response would you expect to observe?

<p>A reduced adrenergic response and sympathetic symptoms. (B)</p> Signup and view all the answers

Which of the following best describes the effect of beta-blockers like propranolol on glucose metabolism?

<p>Decreased glycogenolysis and decreased glucagon secretion (A)</p> Signup and view all the answers

Why is caution advised when administering propranolol to a diabetic patient receiving insulin?

<p>Propranolol may cause pronounced hypoglycemia after insulin injection. (B)</p> Signup and view all the answers

Besides hypertension, which of the following is a therapeutic use of propranolol?

<p>Migraine prophylaxis due to CNS penetration. (D)</p> Signup and view all the answers

Which beta-blocker exhibits partial agonist activity and is beneficial for patients with bronchoconstrictive conditions like asthma or COPD?

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

What is the primary mechanism by which propranolol provides a protective effect on the myocardium following a myocardial infarction?

<p>Decreasing the oxygen demand (B)</p> Signup and view all the answers

Which beta-blocker is known for its ability to decrease aqueous humor production in the eye, making it suitable for treating glaucoma?

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

In the context of thyrotoxicosis, what specific symptom control is achieved with propranolol?

<p>Decreased heart rate, decreased palpitations, and decreased tremor (A)</p> Signup and view all the answers

Which of the following is a known adverse effect of propranolol?

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

Which beta-blocker is noted for its long duration of action, lasting up to 24 hours, and having less CNS effect compared to propranolol?

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

Which of the following is a key adverse effect associated with nonselective beta-adrenoceptor antagonists?

<p>Bronchoconstriction in patients with asthma (D)</p> Signup and view all the answers

What is the mechanism by which Propranolol reduces portal hypertension in variceal bleeding?

<p>Decreasing hepatic venous pressure gradient. (B)</p> Signup and view all the answers

Which of the following beta-blockers is described as more potent than propranolol?

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

A patient with diabetes and hypertension requires a beta-blocker. Which of these would be an appropriate option considering this patient's conditions?

<p>Pindolol or Penbutolol (C)</p> Signup and view all the answers

What is the primary mechanism of action of propranolol on the heart?

<p>Blocking both β1 and β2 receptors (D)</p> Signup and view all the answers

Which of the following adverse effects of propranolol is due to its effect on glucose metabolism?

<p>Inhibition of glycogenolysis (A)</p> Signup and view all the answers

Which beta-blocker, when administered as ophthalmic drops, has a high bioavailability that can lead to systemic side effects?

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

How do beta-blockers affect the cardiovascular system during exercise or stress?

<p>They attenuate the expected increase in heart rate (B)</p> Signup and view all the answers

Which of the following beta-blockers are considered to have intrinsic sympathomimetic activity?

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

What effect do beta-adrenoceptor blockers have on peripheral vasoconstriction?

<p>They block vasodilation mediated by β2-receptors leading to reflex vasoconstriction (D)</p> Signup and view all the answers

Which of these beta-blockers is most likely to be prescribed for a patient with hypertension and open-angle glaucoma?

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

Why is the use of non-selective beta-antagonists contraindicated in patients with COPD or asthma?

<p>They cause contraction of the bronchiolar smooth muscle (B)</p> Signup and view all the answers

How do β-adrenoceptor blockers influence the renin-angiotensin system?

<p>They reduce β1 stimulated release of renin (A)</p> Signup and view all the answers

What is a potential side effect of propranolol due to its ability to cross the central nervous system?

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

Which of the following is true regarding the receptor affinity of propranolol?

<p>It blocks both β1 and β2-receptors with equal affinity (D)</p> Signup and view all the answers

Which of the following best describes the primary mechanism of action for both atenolol and metoprolol?

<p>Selective β1-adrenoceptor antagonist. (B)</p> Signup and view all the answers

A patient with hypertension and a history of diabetes mellitus is prescribed a beta-blocker. Which medication would be preferred according to the text?

<p>Atenolol or Metoprolol (D)</p> Signup and view all the answers

In heart failure, which of the following is NOT a therapeutic benefit of metoprolol?

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

A patient with a specific condition was previously on propranolol but experienced cold extremities. Which of the following medications is a direct recommendation to replace such treatment, based on the content provided?

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

Which property differentiates atenolol from propranolol regarding their entry into the central nervous system?

<p>Propranolol enters the CNS readily, while atenolol does not. (A)</p> Signup and view all the answers

Which of the following is a therapeutic use for both atenolol and metoprolol?

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

A patient is being treated for cardiac dysrhythmias. Which of the following beta-blockers is indicated for this treatment, based on the text?

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

A patient who suffered a myocardial infarction (MI) is being treated with a beta-blocker. What effect of this intervention is mentioned in the content?

<p>Decreased risk of further cardiac events. (D)</p> Signup and view all the answers

Which beta-1 selective antagonist is characterized by its ultra-short duration of action due to plasma esterase hydrolysis?

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

Which beta-1 selective antagonist is associated with the ancillary effect of promoting vasodilation through nitric oxide release?

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

A patient with severe liver impairment is prescribed a beta-1 selective antagonist. Which of the following should be avoided due to contraindications?

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

Which beta-1 selective antagonist is associated with intrinsic sympathomimetic activity?

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

Which beta-1 antagonist is commonly used to reduce intraocular pressure in open-angle glaucoma?

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

A patient requires beta-blockade during surgery. Which of the following beta-1 antagonists would be the most suitable due to its rapid onset and short half-life?

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

Which beta-1 selective antagonist, when used in higher doses, could potentially inhibit beta-2 receptors, affecting bronchial and vascular musculature?

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

Which drug's therapeutic effect is directly linked to its ability to increase nitric oxide levels?

<p>Nebivolol (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.

α-Adrenergic Antagonists

Drugs that bind to and block α-adrenergic receptors, reducing the effects of norepinephrine and epinephrine.

β-Adrenergic Antagonists

Drugs that bind to and block β-adrenergic receptors, reducing the effects of norepinephrine and epinephrine.

How do Adrenergic Antagonists work?

These drugs prevent or reverse the actions of norepinephrine and epinephrine, either naturally released or given as medication.

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What are some uses of adrenergic antagonists?

Adrenergic antagonists can be used to treat conditions like high blood pressure, heart disease, anxiety, and migraines.

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What is Propranolol?

Propranolol is a nonselective beta-blocker that blocks both β1 and β2 receptors with equal affinity. It is a commonly used example of this type of drug.

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How does Propranolol affect the heart?

By blocking β1 receptors in the heart, propranolol reduces heart rate and force of contraction, leading to a decrease in cardiac output and blood pressure.

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How does Propranolol help with angina?

Propranolol acts on β1 receptors in the heart, lowering cardiac output, workload, and oxygen consumption. This makes it useful in managing angina.

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How does Propranolol impact heart rhythm?

Propranolol slows down the transmission of electrical impulses in the AV node, affecting the rhythm of the heart.

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Why does Propranolol cause vasoconstriction?

Propranolol blocks β2 receptors involved in vasodilation, leading to vasoconstriction. This contributes to its effect on blood pressure.

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What is a potential risk of Propranolol?

Propranolol can cause bronchoconstriction by blocking β2 receptors in the bronchioles. This can be dangerous for patients with asthma or COPD.

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How can Propranolol affect diabetic patients?

Propranolol can mask the symptoms of hypoglycemia by preventing the normal increase in heart rate and sweating associated with low blood sugar.

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Why are selective β1 blockers preferred?

Because of its potential side effects, selective β1 blockers have been developed to target heart issues without affecting other tissues.

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How does Propranolol affect blood sugar in type 2 diabetes?

Propranolol can decrease insulin secretion, leading to higher blood sugar levels in people with type 2 diabetes.

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How does Propranolol affect glycogenolysis?

Propranolol can cause a decrease in glycogen breakdown, leading to reduced glucose release into the bloodstream.

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How does Propranolol affect the heart in angina?

Propranolol can lower heart rate and decrease the force of heart contractions, reducing the heart's oxygen demand.

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How does Propranolol benefit heart attack patients?

Propranolol can reduce the size of a heart attack and the risk of sudden death after a heart attack.

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How does Propranolol help with hyperthyroidism?

Propranolol helps control symptoms of hyperthyroidism by slowing down the heart rate and reducing tremor.

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How does Propranolol help with tremors?

Propranolol's ability to enter the brain allows it to treat tremors by acting on the central nervous system.

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How does Propranolol help with migraine prophylaxis?

Propranolol can be used to prevent migraines by reducing the frequency and intensity of headaches.

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How does Propranolol help with variceal bleeding?

Propranolol reduces the pressure in the veins leading to the liver, helping to prevent bleeding from varices.

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Esmolol

A short-acting β1-selective blocker rapidly hydrolyzed by plasma esterases. It is particularly useful in unstable patients needing β-blockade.

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Betaxolol

A long-acting β1-selective blocker used for open-angle glaucoma and hypertension.

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Nebivolol

A once-daily β1-selective blocker with added vasodilatory effects due to nitric oxide release.

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Acebutolol

A β1-selective blocker with partial agonist activity, meaning it also has some stimulating effect.

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Bisoprolol

A β1-selective blocker useful in angina, hypertension, heart failure, and preventing tachycardias during surgery.

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β1-selective blockers and heart failure

β1-selective blockers may reduce mortality in patients with severe heart failure.

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β1-selective blockers and β2-receptor antagonism

β1-selective blockers, especially at higher doses, can block β2-receptors, which can lead to bronchospasm and problems with breathing.

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β-blockers and anti-arrhythmic action

β-blockers are classified as Class II antiarrhythmic agents. They help regulate heart rhythm and slow down heart rate.

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Pindolol: What is it?

A type of β-blocker with partial agonist activity, meaning it can also activate the receptor to a limited extent. It's helpful for patients with asthma or COPD who need β-blocker therapy, as it can minimize bronchoconstriction.

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Penbutolol: What is it?

Another β-blocker with partial agonist activity. Comparable to Pindolol in therapeutic uses but considered stronger.

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Timolol: What is it?

A nonselective β-blocker without intrinsic sympathomimetic activity. It lowers eye pressure by inhibiting aqueous humor production, making it effective for treating glaucoma.

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Timolol: What's a key characteristic?

It's a nonselective β-blocker with the unique property of being absorbed into the bloodstream after eye drops application. This can lead to systemic side effects, such as affecting heart function.

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Nadolol: What is it?

A nonselective β-blocker, known for its potency and long-lasting effect. It's similar to Propranolol, but with a longer duration and fewer side effects on the nervous system.

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What does 'combination therapy' in hypertension refer to?

A combination of drugs that are used together to treat high blood pressure.

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How are β-blockers used in managing high blood pressure?

A combination of β-blockers and other drugs like diuretics is a common approach to manage high blood pressure. This is where β-blockers come in, effectively managing the heart's workload and reducing blood pressure.

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Atenolol

A type of beta blocker that selectively blocks beta-1 receptors in the heart, slowing heart rate and decreasing blood pressure. It's often used to treat high blood pressure, chest pain, and irregular heartbeats. This drug is also preferred in individuals with diabetes or vascular issues due to its selective action.

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Metoprolol

Another selective beta-1 blocker used to control heart rate and blood pressure. Often prescribed for conditions like high blood pressure, heart failure, and certain arrhythmias.

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Mechanism of Action of Beta Blockers

Beta-blockers, including propranolol, work by blocking the action of adrenaline and noradrenaline (epinephrine and norepinephrine). This reduces the signaling through beta receptors, which are found in the heart, lungs, and other organs. The result is a slower heart rate, decreased blood pressure, and reduced stress on the heart.

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Atenolol and Metoprolol - Ideal for Diabetes and Vascular Issues

Atenolol and metoprolol are often preferred for individuals with diabetes or peripheral vascular disease because they have a higher selectivity for beta-1 receptors found in the heart. This means they are less likely to affect other organs that also have beta receptors, like the lungs.

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Metoprolol vs. Propranolol - Cold Hands and Feet

While similar in function, metoprolol is more commonly prescribed for patients experiencing cold hands and feet. This is because its limited entry into the central nervous system (CNS) reduces the risk of side effects associated with CNS activity.

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Beta Blockers - Treatment for Congestive Heart Failure

Beta blockers, like propranolol, help manage congestive heart failure by reducing stress on the heart and decreasing its remodeling process, leading to better function.

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Beta Blockers - Treatment for Angina Pectoris

Beta blockers like propranolol are effective in managing angina pectoris by reducing the heart's oxygen demand, preventing chest pain during exertion.

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Beta Blockers - Treatment for Myocardial Infarction (MI)

Beta-blockers are used to reduce the risk of heart complications after a heart attack. They also play a role in preventing additional heart attacks by stabilizing the heartbeat and reducing blood pressure.

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Study Notes

Adrenergic Antagonists II - Lecture 17

  • Lecturer: Mayur S. Parmar, Ph.D.
  • Affiliation: Assistant Professor of Pharmacology, Department of Foundational Sciences, Dr. Kiran C. Patel College of Osteopathic Medicine, Nova Southeastern University, Tampa Bay/Clearwater Campus
  • Email: [email protected]
  • Phone: 813-574-5357

Learning Objectives

  • Identify specific beta-adrenergic antagonists and the receptor subtypes they act on.
  • Discuss the mechanism of action of beta-adrenergic antagonists.
  • Discuss the pharmacological effects and clinical efficacy based on receptor interactions.
  • Discuss therapeutic uses and adverse effects.
  • Discuss potential contraindications and drug interactions.

Adrenergic Antagonists

  • Adrenergic antagonists interact with α or β adrenoceptors to prevent or reverse the actions of norepinephrine or epinephrine, or exogenously administered sympathomimetic agents.
  • α blockers:
    • Nonselective (α₁ and α₂): Block both α₁ and α₂ receptors
    • Selective (α₁ or α₂): Block specific α₁ or α₂ receptors
  • β blockers:
    • Nonselective (β₁ and β₂): Block both β₁ and β₂ receptors
    • Selective (β₁): Block specifically β₁ receptors
    • Mixed blockers (α & β): Block both α and β receptors

β-adrenergic Antagonists (Key Points)

  • Nonselective β-blockers act on both β₁ and β₂ receptors.
  • Cardioselective β-antagonists primarily block β₁ receptors.
  • Clinically useful β₂-selective antagonists are not available.
  • β-blockers with intrinsic sympathomimetic activity (ISA) partially stimulate β-receptors while blocking catecholamine effects; they do not decrease heart rate to the same degree as β-blockers without ISA.
  • Most β-blockers end in "-olol," except labetalol and carvedilol.

β-adrenoceptor Antagonists: Nonselective (Key Points)

  • Propranolol (prototypical):
    • Blocks β₁ and β₂ receptors, causing bronchoconstriction (life-threatening in asthma)
    • Masks hypoglycemia in diabetics
  • Pindolol
  • Penbutolol
  • Timolol
  • Nadolol
  • Labetalol
  • Carvedilol

Propranolol (Pharmacological Effects)

  • Renin-angiotensin: Reduces renin release.
  • Respiratory: Blocks β₂-receptors causing bronchoconstriction (avoid in COPD/asthma).
  • Glucose Metabolism: Decreases glycogenolysis and glucagon secretion. Caution in diabetics taking insulin. May lead to hypoglycemia.
  • Other Effects: Decreases cardiac output (reducing rate and force of contraction), workload, and oxygen consumption; useful in angina.

Propranolol (Therapeutic Uses)

  • Hypertension
  • Angina Pectoris
  • Myocardial Infarction
  • Migraine prophylaxis
  • Thyrotoxicosis
  • Glaucoma
  • Arrhythmias

Propranolol (Adverse Effects)

  • Bronchoconstriction
  • Bradycardia
  • Arrhythmias
  • Glucose metabolism disturbances
  • Fatigue
  • Insomnia
  • Sexual dysfunction
  • Hypotension

Other Nonselective β-blockers (Salient Features)

  • Additional information on specific non-selective beta-blockers (e.g., Pindolol, Penbutolol, Timolol, Nadolol).

Other Beta-Blockers (Salient Features)

  • Additional information on specific beta-blockers (e.g., Atenolol, Metoprolol, Acebutolol, Carvedilol, Labetalol, Nebivolol) including mechanisms of action, therapeutic uses, and contraindications.

β₁-selective Blockers: Contraindications

  • Specific contraindications and cautions for the use of β₁-selective blockers (e.g., cardiogenic shock, severe bradycardia,2nd or 3rd degree AV block, decompensated heart failure).

ẞ-adrenergic Antagonists: Summary

  • Detailed table summarizing drugs, receptor specificity, and therapeutic uses.

Resources

  • Books:
    • Katzung Basic & Clinical Pharmacology
    • Lippincott Illustrated Reviews: Pharmacology
    • Principles of Pharmacology: The Pathophysiologic Basis of Drug Therapy, Fourth Edition

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