Adrenergic Drugs and Alpha Blockers
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Questions and Answers

What is the primary cardiovascular effect of selective α₁ blockers?

  • Increased renal blood flow
  • Relaxation of arterial and venous smooth muscle (correct)
  • Enhanced glomerular filtration rate
  • Increased cardiac output

Which selective α₁ blocker is particularly noted for having the least effect on blood pressure?

  • Prazosin
  • Terazosin
  • Doxazosin
  • Tamsulosin (correct)

What therapeutic use is common for selective α₁ blockers in patients with benign prostatic hypertrophy (BPH)?

  • Increasing bladder neck tone
  • Inducing diuresis
  • Enhancing urinary retention
  • Reducing smooth muscle tone in the prostate (correct)

Which of the following is a potential adverse effect of selective α₁ blockers?

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

What is a contraindication for using Yohimbine?

<p>Central Nervous System diseases (B)</p> Signup and view all the answers

Which of the following is a non-selective α-receptor antagonist?

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

What is a common effect of α₁-selective blockers like doxazosin?

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

What is the mechanism of action for phenoxybenzamine?

<p>Irreversible non-competitive blockade of α-receptors (B)</p> Signup and view all the answers

Which drug is primarily to be used in the treatment of hypertension and benign prostatic hypertrophy (BPH)?

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

What outcome is NOT a result of blocking α-adrenergic receptors?

<p>Increased blood pressure (A)</p> Signup and view all the answers

Which of the following β-blockers are classified as β₁-selective in the second generation?

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

What can lead to decreased blood pressure in patients using nonselective α-blockers?

<p>Vasodilation through α₁ blockade (D)</p> Signup and view all the answers

Which statement correctly describes the effect of α₂ receptor antagonism?

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

What effect do alpha blockers have on the vasoconstriction caused by epinephrine?

<p>They block the vasoconstrictive effect. (D)</p> Signup and view all the answers

Which of the following conditions is a contraindication for the use of alpha blockers?

<p>Decreased coronary perfusion (A)</p> Signup and view all the answers

Which drug is indicated for the short-term treatment of pheochromocytoma?

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

What is a common side effect associated with α blocking?

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

Which selective α₁ blocker is specifically indicated for benign prostatic hypertrophy?

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

What is a likely consequence of taking phentolamine?

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

Which of the following is NOT an indication for phenoxybenzamine?

<p>Treatment of hypotension (A)</p> Signup and view all the answers

Which α blocker is known to be the longest-acting?

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

Flashcards

What are alpha blockers generally used for?

Alpha blockers are mainly used to treat hypertension and benign prostatic hypertrophy (BPH) by relaxing blood vessels and relieving prostate enlargement, respectively.

How do alpha blockers lower blood pressure?

They block alpha-adrenergic receptors, reducing the sympathetic tone in blood vessels, causing vasodilation and lowering peripheral resistance, ultimately decreasing blood pressure.

What is epinephrine reversal?

Epinephrine, a hormone with vasoconstrictive effects, is used to test the effectiveness of alpha blockers. Normally, epinephrine causes vasoconstriction. However, in the presence of alpha blockers, the expected vasoconstriction is reversed into vasodilation due to the blocked alpha receptors.

What is pheochromocytoma, and how are alpha blockers involved?

Pheochromocytoma is a tumor that releases excessive catecholamines (like epinephrine) causing high blood pressure. Alpha blockers, particularly nonselective ones like phenoxybenzamine and phentolamine, are used to control the high blood pressure caused by this tumor.

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How do nonselective alpha blockers work?

They block both α₁ and α₂ receptors, affecting both vasoconstriction and catecholamine release.

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Why are nonselective alpha blockers less commonly used?

They have a wider range of effects and can cause more side effects compared to selective ones.

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What are selective α₁ blockers, and how do they work?

They specifically block α₁ receptors, primarily affecting vasoconstriction and leading to blood pressure lowering.

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How do selective α₁ blockers help with BPH?

They relax muscles in the prostate gland, easing urinary flow and relieving symptoms of BPH.

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What is the 'first-dose' effect of selective α₁ blockers?

Selective α₁ blockers can cause a significant drop in blood pressure after the first dose, even if the patient is already taking other medications.

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How do selective α₁ blockers work for BPH?

They relax the smooth muscle in the prostate gland, reducing pressure on the urethra and improving urine flow.

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Why is tamsulosin preferred for BPH?

Tamsulosin is a more potent inhibitor of α₁ receptors in the prostate, effectively improving urine flow.

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What are the major adverse effects of selective α₁ blockers?

Common side effects include dizziness, nasal congestion, headache, drowsiness, and orthostatic hypotension (a sudden drop in blood pressure when standing up).

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What is yohimbine, and how does it work?

Yohimbine is a selective α₂ blocker of plant origin that works at the CNS level. It is used to relieve vasoconstriction and may be used as an aphrodisiac.

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α-Adrenergic Blockers and Isoproterenol

α-Adrenergic blockers have no effect on the actions of isoproterenol, a pure β agonist.

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α-Adrenergic Blockers and Vasoconstriction

α-Adrenergic blockers reverse the vasoconstrictive action of epinephrine.

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Phenoxybenzamine for Pheochromocytoma

Phenoxybenzamine is used to treat and prevent hypertensive crises in patients with pheochromocytoma.

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Phenoxybenzamine for Raynaud's Disease

Phenoxybenzamine can relieve vasoconstriction in Raynaud's disease.

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Phenoxybenzamine and Autonomic Hyperreflexia

Phenoxybenzamine treats autonomic hyperreflexia, which increases the risk of strokes in paraplegics.

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Phenoxybenzamine Side Effects: α-Blocking

Phenoxybenzamine can cause postural hypotension, tachycardia, ejaculation problems, nasal congestion, and nausea.

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Phentolamine: Competitive Blocker of α Receptors

Phentolamine is a competitive blocker of both α₁ and α₂ receptors.

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Tamsulosin: Selective α₁ Blocker for BPH

Tamsulosin is a selective α₁ blocker used to treat benign prostatic hypertrophy (BPH).

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Study Notes

Adrenergic Drugs

  • Adrenergic drugs are categorized as agonists or antagonists, affecting alpha and beta receptors.
  • Alpha receptor antagonists block the effects of norepinephrine and epinephrine, leading to various physiological responses.
  • Nonselective alpha antagonists, such as phenoxybenzamine and phentolamine, block both alpha-1 and alpha-2 receptors.
  • Selective alpha-1 antagonists are used in treating hypertension and benign prostatic hyperplasia.
  • Selective alpha-2 antagonists, like yohimbine, are used in treating Raynaud's disease and for improving erectile dysfunction.
  • Beta receptor antagonists block the effects of norepinephrine and epinephrine on beta receptors (beta blockers).
  • Nonselective beta blockers affect both beta-1 and beta-2 receptors.
  • Beta-1-selective blockers primarily target beta-1 receptors.
  • Beta blockers are used in treating hypertension, angina, and cardiac arrhythmias.

Alpha Blockers

  • Alpha blockers prevent sympathetic nerve impulses in the sympathetic nervous system.
  • Nonselective alpha blockers include phenoxybenzamine and phentolamine, and they are used in treating pheochromocytoma.
  • Selective alpha blockers, such as Prazosin, Terazosin, and Doxazosin, are used in treating hypertension and benign prostatic hyperplasia (BPH).
  • Tamsulosin is a selective alpha-1 blocker used to treat BPH.

Phenoxybenzamine

  • Phenoxybenzamine is a non-selective alpha-adrenergic antagonist.
  • Its mechanism of action is irreversible non-competitive blocking.
  • It causes a sustained reduction in peripheral vascular tone.
  • Effects include decreased blood pressure, preventing vasoconstriction, and reflex tachycardia.
  • Indications include pheochromocytoma.
  • Side effects include postural hypotension, tachycardia, and nasal congestion.

Phentolamine

  • Phentolamine is a competitive alpha-adrenergic antagonist.
  • Its duration of action is shorter than that of phenoxybenzamine.
  • It's primarily used for short-term treatment of pheochromocytoma.
  • Used to induce penile erection when injected intravenously along with papaverine.

Selective α1 Blockers

  • Selective alpha-1 blockers, like prazosin, terazosin, doxazosin, and tamsulosin, block only the alpha-1 adrenergic receptors.
  • They are used in treating hypertension and benign prostatic hyperplasia.
  • Tamsulosin is effective in treating BPH due to its selective alpha-1A receptor blockage in the prostate.
  • Adverse effects include dizziness, nasal congestion, headache, drowsiness, postural hypotension, and a possible tendency toward salt and water retention.

Selective α2 Blockers

  • Yohimbine is a selective alpha-2 blocker with no established clinical role.
  • May be used to improve or treat erectile dysfunction.

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Description

Explore the categories and effects of adrenergic drugs, focusing on agonists and antagonists that target alpha and beta receptors. Learn about the different types of alpha blockers, their applications in treating various medical conditions, and the role of beta blockers in managing cardiovascular issues.

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