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Questions and Answers
Which of the following is NOT a selective alpha-1 adrenergic receptor blocker?
Which of the following is NOT a selective alpha-1 adrenergic receptor blocker?
- Yohimbine (correct)
- Prazosin
- Tamsulosin
- Terazosin
A patient is prescribed a non-selective alpha-adrenergic blocker. What are the most likely pharmacological effects you would anticipate?
A patient is prescribed a non-selective alpha-adrenergic blocker. What are the most likely pharmacological effects you would anticipate?
- Increased peripheral vascular resistance and bradycardia.
- Mydriasis and decreased nasal stuffiness.
- Lowered peripheral vascular resistance, postural hypotension, and reflex tachycardia. (correct)
- Increased blood pressure and decreased heart rate.
Why is surgical removal of a pheochromocytoma considered a significant intervention?
Why is surgical removal of a pheochromocytoma considered a significant intervention?
- It only provides temporary relief from hypertension.
- It has minimal effect on blood pressure.
- It is effective in less than 10% of patients.
- It is curative in the majority of patients and significantly impacts hypertension-related mortality and morbidity. (correct)
A patient presents with a rare tumor causing hypertension. Which drug would be appropriately administered along with a beta-blocker in preparation for surgery?
A patient presents with a rare tumor causing hypertension. Which drug would be appropriately administered along with a beta-blocker in preparation for surgery?
Which of the following drugs is an irreversible non-selective alpha-1 and alpha-2 antagonist?
Which of the following drugs is an irreversible non-selective alpha-1 and alpha-2 antagonist?
A patient taking an alpha-adrenergic blocker reports experiencing nasal congestion. What is the most likely cause of this side effect?
A patient taking an alpha-adrenergic blocker reports experiencing nasal congestion. What is the most likely cause of this side effect?
A patient is prescribed Prazosin. What primary effect does this medication have on blood pressure and peripheral vascular resistance?
A patient is prescribed Prazosin. What primary effect does this medication have on blood pressure and peripheral vascular resistance?
A doctor wants to prescribe a drug that will lower a patient's blood pressure but is concerned about reflex tachycardia. Which class of drugs should they consider and why?
A doctor wants to prescribe a drug that will lower a patient's blood pressure but is concerned about reflex tachycardia. Which class of drugs should they consider and why?
Which mechanism primarily contributes to the reduction of arterial blood pressure by alpha-1 receptor blockers?
Which mechanism primarily contributes to the reduction of arterial blood pressure by alpha-1 receptor blockers?
A patient taking an alpha-1 blocker experiences postural hypotension. Which physiological effect of the drug is most directly responsible for this?
A patient taking an alpha-1 blocker experiences postural hypotension. Which physiological effect of the drug is most directly responsible for this?
Which of the following is an advantage of using alpha-1 blockers, besides their antihypertensive effect?
Which of the following is an advantage of using alpha-1 blockers, besides their antihypertensive effect?
Why is tamsulosin preferred over other alpha-1 blockers for treating benign prostatic hyperplasia (BPH)?
Why is tamsulosin preferred over other alpha-1 blockers for treating benign prostatic hyperplasia (BPH)?
What is the recommended strategy to mitigate the 'first-dose hypotension' associated with alpha-1 blockers?
What is the recommended strategy to mitigate the 'first-dose hypotension' associated with alpha-1 blockers?
How do alpha-1 blockers contribute to ejaculatory dysfunction in some patients?
How do alpha-1 blockers contribute to ejaculatory dysfunction in some patients?
What is the mechanism of action of alpha-methyl dopa in reducing blood pressure?
What is the mechanism of action of alpha-methyl dopa in reducing blood pressure?
Terazosin and doxazosin alleviate BPH symptoms by acting on both α1A and α1B receptors. Which of the following effects contributes MOST to this alleviation?
Terazosin and doxazosin alleviate BPH symptoms by acting on both α1A and α1B receptors. Which of the following effects contributes MOST to this alleviation?
What is the primary mechanism by which alpha-methyl dopa reduces blood pressure?
What is the primary mechanism by which alpha-methyl dopa reduces blood pressure?
Which of the following is a key pharmacological effect directly attributed to the blockade of alpha-1 receptors in the ejaculatory ducts?
Which of the following is a key pharmacological effect directly attributed to the blockade of alpha-1 receptors in the ejaculatory ducts?
Why are small initial doses of alpha-adrenergic blockers, administered at bedtime, recommended to mitigate 'first-dose hypotension'?
Why are small initial doses of alpha-adrenergic blockers, administered at bedtime, recommended to mitigate 'first-dose hypotension'?
A patient with benign prostatic hyperplasia (BPH) also has concerns about potential blood pressure changes. Which alpha-1 blocker would be most suitable to minimize hypotensive effects?
A patient with benign prostatic hyperplasia (BPH) also has concerns about potential blood pressure changes. Which alpha-1 blocker would be most suitable to minimize hypotensive effects?
What is the most likely reason for fluid retention observed as a side effect in patients treated with alpha-adrenergic antagonists?
What is the most likely reason for fluid retention observed as a side effect in patients treated with alpha-adrenergic antagonists?
How do terazosin and doxazosin's actions on both α1A and α1B receptors contribute to the symptomatic relief of BPH?
How do terazosin and doxazosin's actions on both α1A and α1B receptors contribute to the symptomatic relief of BPH?
What is the clinical significance of alpha-adrenergic blockers causing a false-positive test for antinuclear antibodies (ANA) and rheumatoid factor (RF)?
What is the clinical significance of alpha-adrenergic blockers causing a false-positive test for antinuclear antibodies (ANA) and rheumatoid factor (RF)?
A researcher is investigating the effects of a novel alpha-adrenergic drug on blood pressure and observes a significant decrease in peripheral vascular resistance without a corresponding increase in heart rate. Which of the following mechanisms is LEAST likely to explain this observation?
A researcher is investigating the effects of a novel alpha-adrenergic drug on blood pressure and observes a significant decrease in peripheral vascular resistance without a corresponding increase in heart rate. Which of the following mechanisms is LEAST likely to explain this observation?
A patient with benign prostatic hyperplasia (BPH) and concomitant hypertension is being considered for alpha-1 adrenergic blocker therapy. Considering the receptor subtypes involved, which of the following strategies would be MOST effective in managing both conditions while minimizing potential side effects?
A patient with benign prostatic hyperplasia (BPH) and concomitant hypertension is being considered for alpha-1 adrenergic blocker therapy. Considering the receptor subtypes involved, which of the following strategies would be MOST effective in managing both conditions while minimizing potential side effects?
What underlies the improvement of lipid profiles, specifically a reduction in LDL and triglycerides, observed with some alpha-adrenergic blockers?
What underlies the improvement of lipid profiles, specifically a reduction in LDL and triglycerides, observed with some alpha-adrenergic blockers?
A patient undergoing treatment with phenoxybenzamine for pheochromocytoma is scheduled for elective surgery. What is the MOST critical consideration regarding the continued use of phenoxybenzamine in the perioperative period?
A patient undergoing treatment with phenoxybenzamine for pheochromocytoma is scheduled for elective surgery. What is the MOST critical consideration regarding the continued use of phenoxybenzamine in the perioperative period?
A researcher aims to develop a novel drug that selectively blocks alpha-2 adrenergic receptors to enhance norepinephrine release. Which of the following potential adverse effects would be of GREATEST concern during the drug's preclinical development?
A researcher aims to develop a novel drug that selectively blocks alpha-2 adrenergic receptors to enhance norepinephrine release. Which of the following potential adverse effects would be of GREATEST concern during the drug's preclinical development?
A patient with a history of orthostatic hypotension is prescribed terazosin for BPH. Which of the following instructions would be MOST appropriate to minimize the risk of syncope?
A patient with a history of orthostatic hypotension is prescribed terazosin for BPH. Which of the following instructions would be MOST appropriate to minimize the risk of syncope?
A patient with Raynaud's phenomenon, a condition characterized by vasospasm in the extremities, is being considered for alpha-adrenergic blocker therapy. Which agent would be LEAST appropriate?
A patient with Raynaud's phenomenon, a condition characterized by vasospasm in the extremities, is being considered for alpha-adrenergic blocker therapy. Which agent would be LEAST appropriate?
Following the administration of an alpha-adrenergic blocker, a patient exhibits exaggerated nasal congestion and difficulty breathing through their nose. Which of the following physiological mechanisms BEST explains these symptoms?
Following the administration of an alpha-adrenergic blocker, a patient exhibits exaggerated nasal congestion and difficulty breathing through their nose. Which of the following physiological mechanisms BEST explains these symptoms?
A researcher is evaluating the effects of a novel alpha-adrenergic antagonist in an experimental model. They observe that the drug effectively reduces blood pressure but also causes a significant increase in plasma renin activity. Which of the following mechanisms BEST explains the observed increase in renin activity?
A researcher is evaluating the effects of a novel alpha-adrenergic antagonist in an experimental model. They observe that the drug effectively reduces blood pressure but also causes a significant increase in plasma renin activity. Which of the following mechanisms BEST explains the observed increase in renin activity?
Flashcards
Adrenergic receptor blockers
Adrenergic receptor blockers
Drugs that block adrenergic receptors, thus inhibiting sympathetic nervous system effects.
Centrally acting sympatholytics
Centrally acting sympatholytics
Drugs acting on the central nervous system to reduce sympathetic outflow.
Phenoxybenzamine
Phenoxybenzamine
A non-selective alpha-adrenergic blocker.
Pheochromocytoma
Pheochromocytoma
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Mechanism of Phenoxybenzamine
Mechanism of Phenoxybenzamine
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Postural Hypotension
Postural Hypotension
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Reflex Tachycardia
Reflex Tachycardia
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Prazosin, Terazosin, Doxazosin
Prazosin, Terazosin, Doxazosin
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How do α1-blockers lower BP?
How do α1-blockers lower BP?
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Effects of α1-blockers on CO and kidneys?
Effects of α1-blockers on CO and kidneys?
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Longest-acting α1-blocker?
Longest-acting α1-blocker?
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Uses of α1-blockers?
Uses of α1-blockers?
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How do α1-blockers help with BPH?
How do α1-blockers help with BPH?
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How to prevent first-dose hypotension?
How to prevent first-dose hypotension?
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α1-blockers MOA in BPH
α1-blockers MOA in BPH
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α-methyl dopa's Mechanism?
α-methyl dopa's Mechanism?
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Selective α1-receptor blockers
Selective α1-receptor blockers
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Selective α2-receptor blockers
Selective α2-receptor blockers
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Example of selective α2-blocker
Example of selective α2-blocker
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Pharmacologic effects of α-blockers
Pharmacologic effects of α-blockers
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Postural hypotension with α-blockers
Postural hypotension with α-blockers
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Reflex tachycardia with α-blockers
Reflex tachycardia with α-blockers
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Miosis
Miosis
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Phenoxybenzamine's Mechanism
Phenoxybenzamine's Mechanism
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How do alpha-1 blockers decrease BP?
How do alpha-1 blockers decrease BP?
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Effect of alpha-1 blockers on lipids?
Effect of alpha-1 blockers on lipids?
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Why is tamsulosin used for BPH?
Why is tamsulosin used for BPH?
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Prevention of First-dose hypotension
Prevention of First-dose hypotension
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Alpha-blockers and ejaculation
Alpha-blockers and ejaculation
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Alpha-blockers in BPH: Result?
Alpha-blockers in BPH: Result?
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Tamsulosin's selectivity
Tamsulosin's selectivity
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Alpha-methyl dopa MOA
Alpha-methyl dopa MOA
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Study Notes
Sympatholytics
- Drugs inhibit effects of the sympathetic nervous system.
Classification of Sympatholytics
- Adrenergic Receptor Blockers consist of alpha (α)-adrenergic blockers and beta (β)-adrenergic blockers
- Centrally Acting Drugs (Alpha 2 Agonist) include Alpha-methyl dopa, a false transmitter, and Clonidine, an agonist but also sympatholytic.
Alpha (α)-Adrenergic Blockers
- Non-Selective α-Receptor Blockers include Phenoxybenzamine and Phentolamine
- Selective α1-Receptor Blockers are Prazosin, Terazosin, Doxazosin and Tamsulosin
- Selective α2-Receptor Blockers include Yohimbine
Pharmacologic Effects
- These drugs lower peripheral vascular resistance and blood pressure
- Postural hypotension and reflex tachycardia are common side effects
- Other minor effects include miosis and nasal stuffiness
Non-Selective α-Blocker: Phenoxybenzamine
- Functions as an Irreversible non-selective α1 and α2 antagonist
- Used for Pheochromocytoma (with β-blocker), a rare tumor causing hypertension, an uncommon cause of hypertension (0.1 to 1% of hypertensive patients)
- Clinical awareness of this tumor is important because surgical removal is curative in >90% of patients and tumor excision has a significant effect on hypertension, the most important cause of pheochromocytoma-related mortality/morbidity.
- Side effects of Phenoxybenzamine include hypotension, reflex tachycardia, and miosis
Selective α1-Receptor Blockers
- Examples: Prazosin, Terazosin and Doxazosin
- Mechanism: Lowers peripheral resistance arterial BP by α1-receptor blockade and direct vasodilation of arterial and venous smooth muscles, may cause minimal changes in COP, RBF, and GFR, but can lead to postural hypotension, may affect ejaculation, improves lipid profile (↓LDL & TGs)
- Doxazosin has the longest duration of action at 22 hours
- Uses: Mild to moderate Hypertension, Raynaud’s syndrome, Benign prostatic hyperplasia (BPH): reduces the tone of internal sphincter of urinary bladder
- Tamsulosin: commonly used in BPH due to high selectivity on α1A & α1D in prostatic tissue with little effect on standing BP
- Side Effects: First-dose hypotension (orthostatic): start with a small dose at bedtime and increase the dose gradually, Fluid retention: due to salt and water retention, False-positive test for ANA & RF, Worsens incontinence in females with pelvic floor pathology, Ejaculatory dysfunction: block α1 receptors in ejaculatory ducts to cause inhibition of ejaculation
Alpha 1 Blockers in BPH
- The mechanism of action in treatment of Benign Prostatic Hyperplasia is competitive blockers of α1 receptors to cause prostatic smooth muscle relaxation and improved urine flow
- Terazosin & doxazosin: block α1A & α1B receptors to cause relaxation of vascular smooth muscles, decrease peripheral vascular resistance, and hypotension
- Tamsulosin (uroselective α1A blockers): selectively block α1A receptors, with minimal effect on BP
Centrally Acting Drugs
- α-methyl dopa is an example of a centrally acting drug
- Mechanism:. In the CNS, α-methyl dopa competes with dopa for dopa decarboxylase enzyme to cause formation of α-methyl NE, which is a false chemical transmitter stimulating the central α2-receptor resulting in a decreased central sympathetic outflow and BP.
- α-methyl dopa is used for treatment of hypertension with pregnancy (DOC).
- Side Effects: Sedation, Nightmares and mental depression due to central deficiency of norepinephrine, Positive Coombs test and autoimmune hemolytic anemia
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