What are examples of non-selective alpha blockers?
Click to see answer
Phenoxybenzamine and Phentolamine.
Click to see question
What are examples of non-selective alpha blockers?
Phenoxybenzamine and Phentolamine.
What type of alpha blocker is Phentolamine?
Phentolamine is a competitive, non-selective alpha blocker.
What are the clinical uses of Propranolol?
Propranolol is used to treat hypertension, angina pectoris, arrhythmias, prevent migraines, treat infantile hemangiomas, thyroid storm, prevent esophageal variceal bleeding, and aortic dissection.
What are the specific agents of beta-receptor antagonist drugs mentioned?
Metoprolol, atenolol, celiprolol, esmolol.
What are examples of selective alpha-2 blockers?
Yohimbine and Idazoxan.
What type of beta-receptor antagonist is Levobunolol?
Nonselective.
What type of drug is Propranolol?
Propranolol is a β-blocking drug that also blocks some serotonin receptors in the brain.
Which type of beta-blockers is preferred for patients with resting bradycardia?
Beta-blockers with intrinsic sympathetic activity.
What are examples of long-acting selective alpha-1 blockers?
Doxazosin, Terazosin, and Tamulosin.
Name two reversible alpha-receptor antagonists.
Phentolamine and prazosin.
What is the nature of the bond formed by Phenoxybenzamine with alpha receptors?
Phenoxybenzamine forms a covalent bond with alpha receptors.
Which type of beta-adrenoceptor antagonist is preferred for patients with asthma, COPD, diabetes mellitus, or peripheral vascular disease?
β1-selective antagonists.
What are examples of short-acting selective alpha-1 blockers?
Prazosin and Alfuzosin.
What is unique about celiprolol among beta-receptor antagonists?
Celiprolol is a β1-selective antagonist that modestly activates β2 receptors, resulting in less adverse bronchoconstrictor effect in asthma.
How can the block caused by reversible alpha-receptor antagonists be overcome?
By sufficiently high concentrations of agonists.
What is a common respiratory adverse effect of beta-receptor antagonist drugs?
Asthma.
What are the clinical uses of Yohimbine?
Yohimbine is used for the treatment of orthostatic hypotension and male erectile dysfunction, though it has been superseded by phosphodiesterase-5 inhibitors like sildenafil.
Give an example of a beta-blocker used in open-angle glaucoma.
Timolol.
Which β-adrenoceptor antagonist is β1 selective according to Table 10-1?
MABCEN.
Which type of beta-blockers is preferred for patients with heart failure or hypertension?
Vasodilating β blockers.
What effect do Tolazoline and Dibenamine have on the maximum response to norepinephrine?
They reduce the maximum response.
What is the half-life of esmolol and what conditions is it used to control?
Esmolol has a half-life of 10 minutes and is used to control supraventricular arrhythmias, arrhythmias associated with thyrotoxicosis, perioperative hypertension, and myocardial ischemia in acutely ill patients.
Name an irreversible alpha-receptor antagonist.
Phenoxybenzamine.
What type of receptors does Phentolamine antagonize?
Phentolamine is a potent competitive antagonist of both α1 and α2 receptors.
How do α-receptor antagonist drugs affect urine flow?
They decrease urine flow resistance.
What is recommended to avoid acute withdrawal symptoms from beta-receptor antagonist drugs?
Gradual dose tapering is recommended.
What does Table 10-1 in Basic & Clinical Pharmacology, 14e describe?
The related selectivity of antagonists for β-adrenoceptors.
Why are metoprolol and atenolol considered low β1-selective?
They are suitable for patients with COPD, myocardial infarction, diabetes, or peripheral vascular disease.
What type of beta-receptor antagonist is Betaxolol?
β1-selective.
How do beta-receptor antagonist drugs affect the respiratory tract?
Beta-receptor antagonist drugs can cause bronchoconstriction, which may be problematic for patients with asthma or chronic obstructive pulmonary disease (COPD).
What effect does propranolol have on infantile hemangiomas?
It decreases the volume, color, and elevation of infantile hemangiomas.
What are the main types of adrenoceptors?
Alpha and beta adrenoceptors.
What are the antiarrhythmic effects of Sotalol?
Sotalol has antiarrhythmic effects due to its ion channel blocking and beta-blocking actions.
What is the primary function of adrenoceptor antagonist drugs?
To block the action of adrenaline and noradrenaline on adrenoceptors.
Which beta-receptor antagonists are known for reducing mortality in chronic heart failure patients?
Metoprolol, bisoprolol, and carvedilol.
What type of drug is Nadolol?
Nadolol is a nonselective β blocker without local anesthetic activity.
What is the benefit of combining variceal band ligation with beta antagonists?
Combining variceal band ligation with beta antagonists is beneficial in managing esophageal varices.
Why should Tamsulosin be avoided in patients undergoing cataract surgery?
Tamsulosin should be avoided due to the increased risk of intraoperative floppy iris syndrome (IFIS).
What are the clinical applications of Propranolol, Nadolol, and Timolol?
Hypertension, arrhythmias, angina pectoris, migraine, hyperthyroidism, and glaucoma (topical timolol).
Why are beta blockers used in the treatment of hypertension?
They lower blood pressure by reducing cardiac output and inhibiting renin release from the kidneys.
How does Prazosin affect vascular and prostate smooth muscle?
Prazosin relaxes both arterial and venous vascular smooth muscle, as well as prostate smooth muscle cells.
What is the first choice of treatment for glaucoma?
Topical prostaglandins.
What type of blocker is Dibenamine?
Irreversible blocker.
What is shown by dose-response curves to norepinephrine in the presence of two different α-adrenoceptor-blocking drugs?
They show reduced maximum response.
How do beta-receptor antagonist drugs affect body weight and metabolism?
They can increase body weight and negatively affect metabolism and lipids (increase triglycerides and decrease HDL).
Which type of beta-blockers are associated with negative effects on metabolism and lipids?
Non-vasodilating beta-blockers.
What is the effect of beta-receptor antagonist drugs on intraocular pressure?
Beta-receptor antagonist drugs reduce intraocular pressure by decreasing the production of aqueous humor, which is beneficial in treating glaucoma.
What are beta-receptor antagonist drugs used for in the treatment of cardiac arrhythmias?
They are used for the treatment of both supraventricular and ventricular arrhythmias, suppression of arrhythmias, improving myocardial infarction survival rate, increasing atrioventricular nodal refractory period, slowing ventricular response rates in atrial flutter and fibrillation, and reducing ventricular ectopic beats.
What is the effect of beta blockers on portal vein pressure in patients with cirrhosis?
Beta blockers diminish portal vein pressure in patients with cirrhosis.
What is a unique effect of sotalol compared to other beta-receptor antagonists?
Sotalol lacks local anesthetic action but has marked class III antiarrhythmic effects, likely due to potassium channel blockade.
What are the subtypes of beta adrenoceptors?
Beta-1, beta-2, and beta-3 adrenoceptors.
Which beta-receptor antagonist drugs are used to treat open-angle glaucoma?
Timolol, Betaxolol, Carteolol, Levobunolol, and Metipranolol.
How can beta-receptor antagonist drugs affect body weight?
They can cause changes in body weight.
How is pheochromocytoma diagnosed?
By elevated plasma or urinary levels of norepinephrine, epinephrine, metanephrine, and normetanephrine.
What is the effect of alpha-receptor antagonists on blood vessels?
They cause vasodilation by blocking alpha-receptors, which reduces blood pressure.
What peripheral vascular effect can beta-receptor antagonist drugs cause?
Peripheral vasoconstriction.
Which beta-receptor antagonists are used for the prevention of migraine headaches?
Propranolol, Metoprolol, Timolol, Atenolol, and Nadolol.
Which alpha-adrenoceptor antagonist drug is mentioned for hypertensive emergencies?
Labetalol.
In what way can beta-blockers improve heart function?
They can improve heart function, especially in patients with diastolic dysfunction, thereby enhancing quality of life.
Which β-adrenoceptor antagonist is β2 selective according to Table 10-1?
PCNT.
只阻斷 β1 的藥物較適合用於哪些病患?
氣喘和COPD的病患。
What is the primary cardiovascular effect of α-receptor antagonist drugs?
They lower peripheral vascular resistance and blood pressure.
How do α-receptor antagonist drugs affect the eyes?
They elicit miosis, which means they cause small pupils.
What nasal effect can α-receptor antagonist drugs cause?
They can cause nasal stuffiness.
Why is Betaxolol less likely to induce bronchoconstriction?
Because it is β1-selective.
Which beta-receptor antagonist is used against acute perioperative arrhythmias?
Esmolol.
What are the subtypes of alpha adrenoceptors?
Alpha-1 and alpha-2 adrenoceptors.
What is a clinical application of Phentolamine?
Phentolamine is used in the treatment of pheochromocytoma.
What is Timolol commonly used to treat?
Timolol is commonly used topically for the treatment of glaucoma.
What severe interactions can occur between beta-receptor antagonists and calcium antagonists like verapamil?
Severe hypotension, bradycardia, heart failure, and cardiac conduction abnormalities.
Which alpha adrenoceptor subtype is primarily involved in vasoconstriction?
Alpha-1 adrenoceptors.
How do beta-receptor antagonists help in other cardiovascular disorders?
They increase stroke volume in patients with obstructive cardiomyopathy by slowing ventricular ejection and decreasing outflow resistance.
What causes closed-angle (narrow-angle) glaucoma?
A dilated iris that occludes the outflow drainage pathway at the angle between the cornea and the ciliary body.
What was the duration of the study on the effects of β-blocker therapy?
6 years.
What is the bioavailability of propranolol and why?
Propranolol has low bioavailability due to extensive hepatic (first-pass) metabolism.
Which beta-receptor antagonists are quite lipophilic and readily cross the blood-brain barrier?
Propranolol and penbutolol.
For which types of migraines is dihydroergotamine not recommended?
Hemiplegic migraine, basilar migraine, or for migraine prevention.
What type of blocker is Tolazoline?
Reversible blocker.
在治療高血壓時,較傾向使用哪種類型的β受體阻斷劑?
β1選擇性阻斷劑。
What are some common adverse effects of beta-receptor antagonist drugs?
Fatigue, depression, and sexual dysfunction.
What effects does Yohimbine have on the CNS and periphery?
Yohimbine blocks α2 receptors, promoting peripheral norepinephrine release and increasing central sympathetic activation.
What is Butoxamine used for?
Selective β2-blocking drug used in research.
What condition can α-receptor antagonist drugs treat related to the urinary system?
They can treat urinary retention due to prostatic hyperplasia.
What type of drug is Timolol?
Timolol is a nonselective β blocker without local anesthetic activity.
How do propranolol and nadolol affect bleeding from esophageal varices in patients with cirrhosis?
Propranolol and nadolol decrease the incidence of the first episode of bleeding from esophageal varices and reduce the mortality rate associated with bleeding in patients with cirrhosis.
What is a veterinary use of Yohimbine?
In veterinary medicine, Yohimbine is used to reverse anesthesia induced by xylazine, an α2 agonist used to calm animals.
How is open-angle glaucoma typically treated?
With drug treatment.
Which alpha adrenoceptor subtype is primarily involved in inhibiting norepinephrine release?
Alpha-2 adrenoceptors.
How do beta-receptor antagonists help in hyperthyroidism?
They reduce palpitations, tachycardia, tremulousness, and anxiety.
What imaging techniques are used to localize a pheochromocytoma?
Computed tomography, magnetic resonance imaging scans, and scanning with radio markers (131 I-meta-iodobenzylguanidine (MIBG)).
How do beta-receptor antagonists affect the heart?
They decrease heart rate and contractility by blocking beta-receptors.
Which alpha-receptor antagonist is useful in symptomatic patients with inoperable or metastatic pheochromocytoma?
Phenoxybenzamine.
What is a common clinical use of beta-blockers?
Treatment of hypertension and certain types of heart disease.
What is the bioavailability and half-life of Prazosin when taken orally?
Prazosin has an oral bioavailability of 50% and a half-life of 3 hours.
Name some cardioselective β-adrenergic blockers.
Metoprolol, Atenolol, Acebutalol, Bisoprolol, Esmolol, Betaxolol, Celiprolol, Nebivolol.
Which enzymes metabolize propranolol and metoprolol in the liver?
CYP2D6.
Which cardioselective β-adrenergic blocker has some intrinsic agonist activity?
Acebutalol.
What is the mechanism of action for Labetalol?
Labetalol is a reversible adrenoceptor antagonist with two centers: (S,R)-isomer is a potent α1-selective blocker, and (R,R)-isomer is a potent β blocker.
Name some nonselective β-adrenergic blockers without intrinsic sympathomimetic activity (ISA).
Propranolol, Sotalol, Nadolol, Timolol.
Which alpha-receptor antagonist drugs end with 'osin'?
Prazosin, Terazosin, Doxazosin, Tamsulosin.
Which drugs have both α1-selective and β-antagonistic effects?
Labetalol and carvedilol.
What does rigidity refer to in extrapyramidal effects?
Rigidity refers to muscle stiffness, leading to difficulty in movement and inflexibility.
What are some contraindications for the use of beta-blockers?
Bradycardia, hypotension, moderate or severe left ventricular failure, shock, heart block, and reactive airway disease.
What is a common adverse effect of neuroleptic drugs?
Hypotension.
What type of alpha blocker is Phenoxybenzamine?
Phenoxybenzamine is an irreversible, non-selective alpha blocker.
為什麼只阻斷 β1 的藥物較不會有收縮氣管的副作用?
因為它們不會阻斷 β2 受體。
What are the two types of alpha-receptor antagonists based on their mechanism of action?
Reversible and irreversible alpha-receptor antagonists.
What are common side effects of α-receptor antagonist drugs?
Orthostatic hypotension and tachycardia.
What is a clinical consideration when using beta1-selective antagonists in asthma patients?
Beta1-selective antagonists have fewer adverse effects on airways than nonselective beta antagonists.
How do beta blockers help in chemotherapy?
Beta blockers prevent chemotherapy-induced cardiomyopathy.
What happens when Yohimbine is combined with norepinephrine transport-blocking drugs?
Combining Yohimbine with norepinephrine transport-blocking drugs can greatly elevate blood pressure.
What additional receptors does Phentolamine affect?
Phentolamine has minor inhibitory effects on serotonin receptors and acts as an agonist on muscarinic, H1, and H2 receptors.
What is the primary mechanism of action for alpha-receptor antagonists?
Alpha-receptor antagonists block alpha-adrenergic receptors, preventing the binding of norepinephrine and epinephrine, which leads to vasodilation and decreased blood pressure.
What combination is more efficacious than sclerotherapy in preventing rebleeding in esophageal varices patients?
Nadolol in combination with isosorbide mononitrate is more efficacious than sclerotherapy in preventing rebleeding in esophageal varices patients.
How are beta-receptor antagonist drugs absorbed when taken orally?
They are well absorbed, with peak concentrations occurring 1-3 hours after ingestion.
What is a common adverse effect of beta blockers?
Bradycardia (slow heart rate).
為什麼β-拮抗劑會導致疲倦?
因為它們減少心臟的工作量,降低血壓和心率。
What effect do beta-receptor antagonist drugs have on metabolism and lipids?
They can affect metabolism and lipid levels.
Which type of beta antagonist is recommended for diabetic patients after myocardial infarction?
Beta1-selective antagonists.
Which β-blockers are more selective for β1 receptors over β2 receptors?
Metoprolol, Atenolol, Betaxolol, and Nebivolol.
What is unique about nebivolol among beta-receptor antagonists?
It has partial beta-agonist activity (ISA), leading to less bradycardia and fewer plasma lipid abnormalities.
Which beta antagonist is rapidly hydrolyzed with a half-life of 10 minutes?
Esmolol.
How does propranolol help with performance anxiety (stage fright)?
It reduces the somatic manifestations of anxiety.
What type of drug is Phenoxybenzamine?
Phenoxybenzamine is a non-selective, long-acting, irreversible α-antagonist.
What are some clinical applications of alpha-receptor antagonists?
Alpha-receptor antagonists are used to treat conditions such as hypertension, benign prostatic hyperplasia, and pheochromocytoma.
What is an inverse agonist?
A drug that stabilizes the inactive conformation of β receptors, reducing the number of active receptors.
Which beta antagonist is excreted unchanged in the urine and has the longest half-life?
Nadolol, with a half-life of 24 hours.
Why are alpha 1-selective antagonists like prazosin not usually recommended as monotherapy for hypertension?
Other classes of antihypertensives are more effective in preventing heart failure.
Name three beta-blockers mentioned in the text.
Metoprolol, Atenolol, and Timolol.
What is a common side effect of alpha 1-selective antagonists?
Orthostatic hypotension.
What are the two conformations in which β receptors can exist?
Active and inactive conformations.
What are the primary effects of beta-receptor antagonist drugs on the cardiovascular system?
Beta-receptor antagonist drugs primarily reduce heart rate, decrease myocardial contractility, and lower blood pressure.
What can happen if beta-receptor antagonist drugs are abruptly discontinued?
Abrupt cessation may lead to sudden onset of tachycardia, exacerbation of ischemic symptoms, and acute myocardial infarction.
What cardiovascular side effect can beta-receptor antagonist drugs cause?
Sinus bradycardia.
What is the effect of Phentolamine on presynaptic α2 receptors?
Phentolamine antagonizes presynaptic α2 receptors, leading to enhanced release of norepinephrine from sympathetic nerves and sympathetic activation from baroreflex mechanisms, resulting in cardiac stimulation.
What are the clinical uses of Doxazosin?
Treatment of hypertension and benign prostatic hyperplasia (BPH).
What are the pharmacologic effects of alpha blockers on blood vessels?
Alpha blockers cause vasodilation, which leads to a decrease in peripheral vascular resistance and blood pressure.
What are the common symptoms of pheochromocytoma?
Intermittent or sustained hypertension, headaches, palpitations, and sweating.
How many patients were involved in the study on β-blocker therapy?
1884 patients.
How does the duration of action of Nadolol compare to Timolol?
Nadolol has a long duration of action similar to that of Timolol.
What is an indication for the use of beta-receptor antagonists in cardiovascular disorders?
Dissecting aortic aneurysms.
What is the half-life of Tamsulosin and how is it metabolized?
Tamsulosin has a half-life of 9-15 hours and is metabolized by the liver.
What was the condition of the patients involved in the β-blocker therapy study?
Patients who survived myocardial infarctions.
What is the relative potency of Tamsulosin in inhibiting contraction in prostate smooth muscle versus vascular smooth muscle?
Tamsulosin has relatively greater potency in inhibiting contraction in prostate smooth muscle compared to vascular smooth muscle.
How do selective α1 antagonists help in the treatment of urolithiasis?
They induce ureteral dilation and facilitate the expulsion of larger kidney stones (>5 mm).
What is a potential adverse effect of beta-blockers?
Bradycardia (abnormally slow heart rate).
What are some specific agents of beta-receptor antagonist drugs?
Labetalol, Carvedilol, Medroxalol, Bucindolol.
How do beta blockers help in the management of angina?
By reducing myocardial oxygen demand through decreased heart rate and contractility.
Which beta antagonists are less completely metabolized?
Atenolol, celiprolol, and pindolol.
How might pindolol affect traditional antidepressant medications?
Pindolol may potentiate the action of traditional antidepressant medications.
What is the mechanism of action for Pindolol, Acebutolol, Carteolol, Bopindolol, Oxprenolol, Celiprolol, and Penbutolol?
They block β1 and β2 receptors, with intrinsic sympathomimetic activity (ISA).
What are some common clinical uses of beta blockers?
Beta blockers are commonly used to treat hypertension, angina, heart failure, and arrhythmias.
List three other alpha-adrenoceptor antagonists.
Alfuzosin, Silodosin, Indoramin.
What is the primary function of α-adrenoceptor antagonists?
α-adrenoceptor antagonists primarily block the action of catecholamines on α-adrenoceptors, leading to vasodilation and decreased blood pressure.
Name a common clinical use of beta blockers.
Treatment of hypertension.
Name two alpha-adrenoceptor antagonists that are also used as antipsychotic medications.
Chlorpromazine, Haloperidol.
Which beta1-selective antagonists are mentioned, and what do they block?
Metoprolol and atenolol, which block beta1 receptors in the heart.
What is a potential risk associated with Alfuzosin?
Alfuzosin may increase the risk of QT prolongation.
What are the clinical applications of Labetalol?
Hypertension.
What type of antagonist is Yohimbine?
Yohimbine is an α2-selective antagonist.
What is the clinical application of Carteolol?
Topical ophthalmic application in glaucoma.
What is the clinical use of nonselective β-receptor antagonists?
Topical ophthalmic application in glaucoma.
What is glaucoma and what can it lead to if untreated?
Glaucoma is an increase in intraocular pressure that can damage the retina and optic nerve, leading to restriction of visual fields and potentially blindness.
What is the half-life of Doxazosin and how is it administered?
Doxazosin has a half-life of 22 hours and is administered orally.
What is the primary focus of the study on β-blocker therapy?
The effects of β-blocker therapy on life-table cumulated rates of mortality over 6 years among 1884 patients surviving myocardial infarctions.
What receptors does Tamsulosin have a higher affinity for?
Tamsulosin has a higher affinity for α1A and α1D receptors than for α1B receptors.
What is a potential interaction between topical timolol and oral verapamil?
It may increase the risk of heart block.
What are some specific agents of beta-receptor antagonist drugs?
Pindolol, acebutolol, penbutolol, carteolol, oxprenolol, celiprolol, nebivolol.
What are the treatment options for closed-angle glaucoma?
Drug control and prevention by iridectomy (surgical removal of part of the iris).
What is the role of subtype-selective α1A-receptor antagonists like tamsulosin?
They are used for smooth muscle contraction in the prostate, but caution is advised for patients susceptible to orthostatic hypotension and those undergoing eye surgery.
What are alpha-receptor antagonist drugs used for in clinical pharmacology?
They are used for hypertensive emergencies and chronic hypertension.
What is metyrosine and how does it work?
Metyrosine (α-methyltyrosine) is a competitive inhibitor of tyrosine hydroxylase, the rate-limiting step in the synthesis of dopamine, norepinephrine, and epinephrine.
What is the selectivity of acebutolol?
Acebutolol is a beta1-selective antagonist.
What are the primary clinical uses of Prazosin?
Prazosin is primarily used for the management of hypertension.
What additional receptor does pindolol antagonize?
Pindolol also antagonizes 5-HT1A serotonin receptors.
What is the role of beta-blockers in chronic stable angina?
They are considered first-line therapy.
What are extrapyramidal effects?
Extrapyramidal effects refer to a series of movement disorders caused by certain drugs, especially antipsychotics, involving the brain's lateral motor system and primarily related to motor control.
Which β-blockers are known as inverse agonists?
Betaxolol and metoprolol.
What effect does renal failure have on nadolol's half-life?
Renal failure prolongs nadolol's half-life.
Which receptors, besides α-receptors, does Phenoxybenzamine block?
Phenoxybenzamine blocks histamine (H1), acetylcholine, and serotonin receptors.
What are the effects of neuroleptic drugs on receptors?
They are potent dopamine receptor antagonists and α antagonists.
What are the benefits of nonselective β-adrenergic blockers with intrinsic sympathomimetic activity (ISA)?
They are less likely to cause bradycardia and have less interference with blood lipid levels.
What are some adverse effects of Phenoxybenzamine?
Adverse effects of Phenoxybenzamine include orthostatic hypotension, tachycardia, nasal stuffiness, inhibition of ejaculation, and CNS effects such as fatigue, sedation, and nausea.
What is the dual action of mixed α and β blockers like Labetalol and Carvedilol?
They cause vasodilation and inhibit the heart, leading to stronger blood pressure reduction.
Which class of drugs is commonly used as first-line treatment for open-angle glaucoma?
Prostaglandin analogs.
What conditions is dihydroergotamine used to treat?
Migraine headaches and cluster headaches.
How does phenoxybenzamine achieve irreversible blockade of alpha receptors?
It forms a reactive ethyleneimonium intermediate that covalently binds to alpha receptors.
How does Phentolamine affect vascular smooth muscle?
Phentolamine reduces peripheral resistance by blocking α1 and α2 receptors on vascular smooth muscle.
What are some peripheral vascular effects of beta-receptor antagonist drugs?
Peripheral vasoconstriction, cold extremities, and worsening of peripheral vascular disease and Raynaud phenomenon.
How do beta-receptor antagonist drugs affect myocardial contractility?
They depress myocardial contractility.
How does Yohimbine interact with α2-adrenoceptor agonists like clonidine?
Yohimbine reverses the antihypertensive effects of α2-adrenoceptor agonists such as clonidine.
How can beta-receptor antagonist drugs affect myocardial contractility?
They can depress myocardial contractility.
What are some common clinical uses of beta blockers?
Treatment of hypertension, angina, heart failure, and arrhythmias.
What are the two main types of adrenoceptors that antagonist drugs target?
Alpha-receptors and beta-receptors.
What are alpha-receptor antagonist drugs used for in the context of urinary obstruction?
They improve urine flow by partially reversing smooth muscle contraction in the enlarged prostate and bladder base.
What are the clinical applications of alpha-receptor antagonists?
Alpha-receptor antagonists are used to treat conditions such as hypertension, benign prostatic hyperplasia (BPH), and pheochromocytoma.
β-拮抗劑如何影響四肢的溫度?
它們可能導致血管收縮,從而引起冷手冷腳。
Which beta adrenoceptor subtype is primarily found in the heart?
Beta-1 adrenoceptors.
Which beta-receptor antagonist drugs are not available in the USA?
Oxprenolol and celiprolol.
What is the primary mechanism of action for β-blocking drugs?
Antagonizing the effects of catecholamines at β adrenoceptors.
Which beta adrenoceptor subtype is primarily involved in lipolysis?
Beta-3 adrenoceptors.
β-拮抗劑如何影響睡眠?
它們可能導致失眠或夢魘。
What conditions can cause increased blood pressure that reflects excess circulating concentrations of alpha agonists?
Pheochromocytoma, overdosage of sympathomimetic drugs, or clonidine withdrawal.
Which beta-receptor antagonist is used for the symptomatic treatment of alcohol withdrawal?
Propranolol.
Which alpha 1-selective antagonist is mentioned for mild to moderate systemic hypertension?
Prazosin.
How do beta-blockers benefit patients during an acute myocardial infarction?
Early administration can reduce infarct size and acute mortality.
What is a notable effect of the most highly selective beta1-adrenergic receptor blockers?
They promote endothelial nitric oxide production, leading to vasodilation.
What are the clinical applications of Terazosin?
Terazosin is used for the management of hypertension and urinary retention symptoms in men due to benign prostatic hyperplasia (BPH).
How do highly selective beta1-adrenergic receptor blockers affect insulin sensitivity and lipid profiles?
They increase insulin sensitivity and do not adversely affect the lipid profile.
What is the primary clinical use of Phenoxybenzamine?
Phenoxybenzamine is primarily used for the treatment of pheochromocytoma.
What are the additional effects of Carvedilol besides β-blocking?
Carvedilol attenuates oxygen-free radical-initiated lipid peroxidation and inhibits vascular smooth muscle mitogenesis, which is beneficial in chronic heart failure.
How do α1-adrenoceptor antagonists affect the body?
α1-adrenoceptor antagonists cause vasodilation by blocking α1 receptors on blood vessels, which reduces blood pressure.
What is the physiological impact of inverse agonists?
They reduce the physiological response by decreasing the number of active receptors.
How does propranolol affect lipid metabolism?
Propranolol inhibits sympathetic nervous system stimulation of lipolysis, leading to increased plasma concentrations of VLDL and decreased concentrations of HDL cholesterol, which can increase the risk of coronary artery disease.
What cardiac effects can beta-receptor antagonist drugs induce?
Sinus bradycardia, slow atrioventricular (AV) node conduction, and potentially serious bradyarrhythmias.
What metabolic side effect can beta-receptor antagonist drugs induce?
Hypoglycemia.
How do beta-receptor antagonist drugs help in the treatment of glaucoma?
They reduce intraocular pressure by reducing the ciliary body's production of aqueous humor.
What are some common psychological and physical side effects of beta-receptor antagonist drugs?
Fatigue, depression, and sexual dysfunction.
β-拮抗劑的常見副作用有哪些?
疲倦、冷手冷腳、心跳過慢、胃腸不適、失眠、抑鬱。
Name a specific agent that is an alpha-blocker.
Prazosin is a specific agent that acts as an alpha-blocker.
Why should beta antagonists be avoided in frequent hypoglycemic insulin-dependent diabetic patients?
Because they can mask hypoglycemia symptoms, making it difficult to manage blood sugar levels.
What is the mechanism of action for Propranolol, Nadolol, and Timolol?
They block β1 and β2 receptors.
How do beta blockers affect the heart?
They decrease heart rate and contractility, reducing cardiac output.
What type of drug is Prazosin?
Prazosin is a piperazinyl quinazoline, highly selective for α1 receptors and acts as a competitive antagonist.
What can happen if beta-receptor antagonist drugs are withdrawn acutely?
Acute withdrawal can occur.
Which beta-receptor antagonist is used in the treatment of thyroid storm?
Propranolol.
Which beta adrenoceptor subtype is primarily involved in smooth muscle relaxation?
Beta-2 adrenoceptors.
β-拮抗劑可能引起哪些胃腸不適?
噁心、嘔吐、腹瀉或便秘。
How do alpha agonists, beta blockers, and carbonic anhydrase inhibitors help in treating glaucoma?
They decrease aqueous humor secretion.
What are the side effects of metyrosine?
Extrapyramidal effects.
What distinguishes alpha-blockers from beta-blockers in terms of their primary action?
Alpha-blockers primarily cause vasodilation, while beta-blockers primarily reduce heart rate and contractility.
What is the role of tyrosine hydroxylase in catecholamine synthesis?
It is the rate-limiting step in the synthesis of dopamine, norepinephrine, and epinephrine.
Name three specific alpha-receptor antagonist drugs.
Phenoxybenzamine, Phentolamine, Prazosin.
What is the half-life and metabolism route of Terazosin?
Terazosin has a half-life of 9-12 hours and is metabolized by the liver.
Which nonselective β-adrenergic blocker has membrane stabilizing action?
Propranolol.
How does the β-blocking potency of Labetalol compare to Propranolol?
Labetalol has less β-blocking potency than Propranolol.
What conditions can prolong propranolol's half-life?
Liver disease, diminished hepatic blood flow, or hepatic enzyme inhibition.
What is bradykinesia?
Bradykinesia is the slowing down of movement and extended reaction time.
What happens to the number of active receptors when inverse agonists bind to them?
The number of active receptors decreases, reducing intracellular signaling.
How do beta-blockers reduce the heart's oxygen demand?
By decreasing heart rate and myocardial contractility.
What is akathisia?
Akathisia is a feeling of restlessness, where the patient may feel the need to keep moving.
What is tardive dyskinesia?
Tardive dyskinesia is a persistent involuntary movement disorder, usually affecting the face and mouth, that occurs after long-term use of antipsychotic drugs.
Why should caution be exercised when prescribing beta-receptor antagonists to insulin-dependent diabetic patients?
Beta-receptor antagonists inhibit glycogenolysis in the liver, which can interfere with glucose regulation and pose a risk for hypoglycemia in insulin-dependent diabetic patients.
What is the primary function of beta-receptor-blocking drugs?
To block the effects of adrenaline on beta receptors, reducing heart rate and blood pressure.
What hormones does pheochromocytoma secrete?
Catecholamines, especially norepinephrine and epinephrine.
What are the two major types of glaucoma?
Open-angle glaucoma and closed-angle (narrow-angle) glaucoma.
Which beta-receptor antagonist drugs have sustained-release preparations?
Propranolol and metoprolol.
Which alpha-receptor antagonists are used for treating Benign Prostatic Hyperplasia (BPH)?
Prazosin, doxazosin, and terazosin.
What is a common adverse effect of alpha-blockers?
A common adverse effect of alpha-blockers is orthostatic hypotension, which can cause dizziness or fainting upon standing.
β-拮抗劑為什麼會引起心跳過慢?
因為它們減少了心臟的興奮性和收縮力。
What is the typical half-life range for most beta antagonists?
3 to 10 hours.
What was measured in the study on β-blocker therapy?
Life-table cumulated rates of mortality from all causes.
What is a potential adverse effect of beta blockers in patients with asthma?
Bronchoconstriction, which can worsen asthma symptoms.
What are beta-receptor antagonist drugs commonly used for?
Hypertension, ischemic heart disease, and cardioprotection in patients with heart failure with reduced ejection fraction or coronary artery disease.
What is the effect of beta-receptor antagonist drugs on blood pressure in patients with hypertension?
They chronically lower blood pressure.
What are the applications of alpha2 antagonists?
They are used in the treatment of peripheral vascular disease.
What are the mechanisms by which beta-receptor antagonists lower blood pressure?
Suppression of renin release and effects in the CNS.
How does the α receptor affinity of Labetalol compare to Phentolamine?
Labetalol has less α receptor affinity than Phentolamine, resulting in less hypotension and tachycardia.
What is the primary effect of blocking Beta-1 receptors?
Reduction in heart rate and blood pressure.
How do inverse agonists differ from traditional agonists?
Inverse agonists stabilize the inactive state of receptors, reducing active receptors, while traditional agonists promote receptor activation.
What are some pharmacologic effects of alpha blockers?
Alpha blockers cause vasodilation, decreased peripheral resistance, and lower blood pressure.
Which alpha-adrenoceptor antagonists are also known as ergot derivatives?
Ergot derivatives.
What is dystonia?
Dystonia is uncontrollable muscle contractions that may lead to abnormal postures or movements.
Why should Carvedilol not be combined with CYP2D6 inhibitors?
Combining Carvedilol with CYP2D6 inhibitors like quinidine or fluoxetine can interfere with its metabolism.
Which alpha-adrenoceptor antagonist is also used as an antidepressant?
Trazodone.
Name a specific α1-adrenoceptor antagonist.
Prazosin is a specific α1-adrenoceptor antagonist.
What clinical conditions are α-adrenoceptor antagonists commonly used to treat?
α-adrenoceptor antagonists are commonly used to treat hypertension and benign prostatic hyperplasia (BPH).
What is the primary use of α1-selective antagonists?
α1-selective antagonists are primarily used as antihypertensive agents.
How do beta blockers benefit patients with congestive heart failure?
Beta blockers help manage symptoms and improve heart function in congestive heart failure.
What is the mechanism of action of Phenoxybenzamine?
Irreversibly blocks α1 and α2 receptors.
Which beta-receptor antagonists have limited bioavailability due to first-pass metabolism?
Most beta antagonists, except betaxolol, penbutolol, pindolol, and sotalol.
What is the pharmacokinetic property of beta blockers that affects their duration of action?
Their half-life, which determines how long the drug stays active in the body.
What are pure antagonists in the context of β-blocking drugs?
Drugs that occupy the β receptor without activating it.
What is the primary function of alpha-receptor antagonist drugs?
Alpha-receptor antagonist drugs primarily block alpha-adrenergic receptors, leading to vasodilation and decreased blood pressure.
What are partial agonists in the context of β-blocking drugs?
Drugs that partially activate β receptors while blocking them.
What is the primary mechanism of action for beta-receptor antagonists?
They block the effects of adrenaline on beta receptors.
What is the clinical application of Butoxamine?
None.
What are the two main types of beta receptors that beta blockers target?
Beta-1 and Beta-2 receptors.
What neurotransmitter's reuptake is inhibited by Phenoxybenzamine?
Phenoxybenzamine inhibits the reuptake of norepinephrine by presynaptic adrenergic nerve terminals.
What are α-adrenoceptors?
α-adrenoceptors are a class of G-protein-coupled receptors that are targets for catecholamines like norepinephrine and epinephrine.
What is the effect of blocking beta receptors in the atrioventricular node?
It slows atrioventricular conduction and increases the PR interval.
What is the half-life and metabolism route of Labetalol?
Labetalol has a half-life of 6-8 hours and is metabolized by the liver.
What are the two main types of α-adrenoceptors?
The two main types of α-adrenoceptors are α1 and α2 receptors.
Name some mixed α and β blockers.
Labetalol and Carvedilol.
What is the significance of pharmacokinetics in beta-receptor antagonists?
Pharmacokinetics of beta-receptor antagonists determine their absorption, distribution, metabolism, and excretion, which influence their efficacy and safety.
What are the names of two alpha-adrenoceptor antagonists that also have beta-blocking properties?
Labetalol, Carvedilol.
Which alpha-adrenoceptor antagonist is known for its use in treating erectile dysfunction?
Yohimbine.
Why are beta blockers not used for vasospastic angina pectoris?
Beta blockers are not effective for vasospastic angina pectoris.
Which class of agents do beta blockers belong to for treating cardiac arrhythmias?
Beta blockers are Class II type of agents for treating cardiac arrhythmias.
Name a cholinergic agent used in open-angle glaucoma.
Pilocarpine.
What is the clinical application of Phentolamine?
Pheochromocytoma.
What is the mechanism of action of Prazosin, Doxazosin, Terazosin, Alfuzosin, Indoramin, and Urapidil?
They block α1 receptors but not α2 receptors.
What are the clinical applications of Yohimbine?
Male erectile dysfunction and hypotension.
What are the clinical applications of Metoprolol, Atenolol, Betaxolol, and Nebivolol?
Hypertension, arrhythmias, angina pectoris, and glaucoma (topical betaxolol).
What are beta-receptor antagonist drugs commonly known as?
Beta blockers.
Which β-blocker specifically blocks β2 receptors more than β1 receptors?
Butoxamine.
What is the effect of phenoxybenzamine (Dibenzyline) on blood pressure in a patient with pheochromocytoma?
Phenoxybenzamine lowers blood pressure in patients with pheochromocytoma.
What type of antagonist is Terazosin?
Terazosin is a reversible α1-selective antagonist.
How do beta-receptor antagonist drugs work?
Beta-receptor antagonist drugs block beta-adrenergic receptors, reducing heart rate, cardiac output, and blood pressure.
How do beta-receptor antagonists affect the heart?
They are used in the treatment of angina, chronic heart failure, and following myocardial infarction due to their negative inotropic and chronotropic effects.
What are some non-prescription sources of alpha-receptor antagonists?
Extracts from the bark of the yohimbine tree, which are available as dietary and health supplements.
Name some nonselective β-adrenergic blockers with intrinsic sympathomimetic activity (ISA).
Acebutolol, Carteolol, Penbutolol, Pindolol, Oxprenolol.
What type of drug is Alfuzosin?
Alfuzosin is a quinazoline derivative and an α1-selective antagonist.
What are some adverse effects associated with beta blockers?
Adverse effects of beta blockers can include bradycardia, fatigue, depression, and worsening of asthma symptoms.
What is a potential adverse effect of beta blockers on respiratory function?
Bronchoconstriction, which can worsen asthma.
What is the primary goal of topical drugs used in open-angle glaucoma?
To reduce intraocular pressure (IOP).
Why should beta blockers be used cautiously in diabetic patients?
They can mask the symptoms of hypoglycemia.
Which receptor does Silodosin primarily block?
Silodosin primarily blocks the α1A receptor.
What condition is Silodosin used to treat?
Silodosin is used to treat benign prostatic hyperplasia (BPH).
What is the mechanism of action of alpha agonists in treating open-angle glaucoma?
They decrease aqueous humor production and increase uveoscleral outflow.
What is the role of cholinergic agents in the treatment of open-angle glaucoma?
They increase the outflow of aqueous humor through the trabecular meshwork.
What is the mechanism of action of Yohimbine?
Blocks α2 receptors.
Which conditions involving excessive reversible vasospasm in the peripheral circulation can be treated with prazosin or phenoxybenzamine?
Raynaud phenomenon and other similar conditions.
Which drugs increase aqueous outflow in the treatment of glaucoma?
Prostaglandin F2 alpha analogs, cholinomimetics, and rho kinase inhibitors.
β-拮抗劑為什麼會引起抑鬱?
可能與它們對中樞神經系統的影響有關。
How long does the effect of Phenoxybenzamine last?
The effect of Phenoxybenzamine lasts between 14 to 48 hours.
Why might calcium channel blockers be preferable in some cases of peripheral vascular disease?
Calcium channel blockers may be more effective in certain cases of peripheral vascular disease.
What is tremor in the context of extrapyramidal effects?
Tremor is an involuntary shaking, usually affecting the hands or limbs.
What are the clinical applications of β-blockers with intrinsic sympathomimetic activity (ISA)?
Hypertension, arrhythmias, migraine, and may avoid worsening of bradycardia.
What is the primary effect of blocking Beta-2 receptors?
Constriction of bronchial muscles and blood vessels.
How do beta-receptor antagonists affect the vascular system?
They oppose beta2-mediated vasodilation, which may acutely increase peripheral resistance but ultimately lower blood pressure due to a fall in cardiac output.
What is the bioavailability and half-life of Alfuzosin when taken orally?
The bioavailability is 60% and the half-life is 5 hours.
What is a key difference between alpha and beta blockers?
Alpha blockers primarily affect blood vessels by causing vasodilation, while beta blockers primarily affect the heart by reducing heart rate and contractility.
How do beta-blockers help in reducing the frequency and severity of angina attacks?
By lowering the heart's workload.
Why should beta antagonists generally be avoided in patients with asthma?
Because they increase airway resistance by blocking beta2 receptors in bronchial smooth muscle.
In which patients might beta antagonists still be used despite the risk of increased airway resistance?
In patients with chronic obstructive pulmonary disease (COPD) who also have ischemic heart disease.
What is Cafergot® used for?
Treating migraine attacks and vascular headaches.
Name an alpha agonist used in the treatment of open-angle glaucoma.
Brimonidine.
What neurological condition characterized by severe headaches can be treated with beta blockers?
Beta blockers can be used to treat migraines.
α-阻滯劑如何引起性功能障礙?
α-阻滯劑可能影響陰莖的血流和勃起功能,因為它們改變了血管的擴張和收縮機制。此外,交感神經系統的調節也可能受到影響,導致性功能問題。
Why are beta-blockers used in ischemic heart disease?
To reduce cardiac workload, decrease the frequency and severity of angina attacks, improve heart function, reduce the risk of arrhythmias, and provide long-term cardiac protection.
Which receptors do antidepressants block?
α1 receptors.
What condition is Alfuzosin used to treat?
Alfuzosin is used to treat benign prostatic hyperplasia (BPH).
What is the action of ergot derivatives like ergotamine and dihydroergotamine?
They cause reversible α-receptor blockade with partial agonist action.
How do beta blockers help in the management of angina pectoris?
By reducing myocardial oxygen demand.
What is the difference between selective and non-selective beta blockers?
Selective beta blockers primarily target Beta-1 receptors, while non-selective beta blockers target both Beta-1 and Beta-2 receptors.
What long-term benefit do beta-blockers provide to the heart?
They reduce the incidence of cardiac events such as myocardial infarction and improve patient prognosis.
In which region is Urapidil used as an antihypertensive agent and for treating BPH?
Urapidil is used in Europe as an antihypertensive agent and for treating BPH.
How do beta blockers help with anxiety, specifically social phobia?
Beta blockers reduce physical symptoms of anxiety, such as heart palpitations, in social phobia.
What is the clinical application of Tamsulosin and Silodosin?
Benign prostatic hyperplasia.
What is the effect of beta-receptor antagonists on the respiratory tract?
They block bronchial smooth muscle beta2 receptors, increasing airway resistance, which can be problematic in asthma patients.
In what therapeutic applications might inverse agonists be useful?
They may be useful in treating conditions like anxiety and cardiovascular diseases by reducing β receptor activity.
Name a commonly prescribed prostaglandin analog for open-angle glaucoma.
Latanoprost.
How do beta-blockers help in the treatment of open-angle glaucoma?
By decreasing the production of aqueous humor.
How do beta blockers help in the prophylaxis of myocardial infarction?
Beta blockers prevent reinfarction and ventricular fibrillation.
What condition involving a tumor can be treated with beta blockers?
Beta blockers can be used to treat pheochromocytoma.
What is the clinical application of Phenoxybenzamine?
Pheochromocytoma.
Which α-blockers are slightly selective for α1A receptors?
Tamsulosin and Silodosin.
為什麼α-阻滯劑會導致心跳過速?
由於血壓下降,身體會啟動交感神經系統以補償,釋放腎上腺素等激素,導致心跳加快。
What is the effect of α2-adrenoceptor antagonists?
α2-adrenoceptor antagonists increase the release of norepinephrine by blocking α2 receptors, which can lead to increased sympathetic activity.
Name a specific agent of alpha-blockers and its use.
Prazosin is an alpha-blocker used to treat hypertension and benign prostatic hyperplasia.
What are beta blockers used for in the treatment of hypertension?
Beta blockers are used to lower blood pressure in patients with hypertension.
What is a common adverse effect of α-adrenoceptor antagonists?
A common adverse effect of α-adrenoceptor antagonists is orthostatic hypotension.
Which beta blocker is commonly used for cardiac arrhythmias?
Propranolol is commonly used for cardiac arrhythmias.
Which α-blockers are used for hypertension and benign prostatic hyperplasia?
Prazosin, Doxazosin, Terazosin, Alfuzosin, Indoramin, Urapidil.
什麼是直立性低血壓的機制?
α-阻滯劑通過拮抗α-1腎上腺素受體來擴張血管,降低外周血管阻力。在站立或改變姿勢時,血液可能無法有效地從下肢回流到心臟,導致血壓下降,從而引起頭暈或昏厥。
What is the mechanism of action of Labetalol, Carvedilol, Medroxalol, and Bucindolol?
They block β receptors more than α1 receptors.
Which drugs are most commonly associated with extrapyramidal effects?
Antipsychotic drugs, especially first-generation ones like chlorpromazine, but some antidepressants and anticonvulsants can also cause these effects.
How does drug dosage affect the risk of extrapyramidal effects?
The higher the dosage of the drug, the greater the risk of experiencing extrapyramidal effects.
What additional actions does Urapidil have besides being an α1 antagonist?
Urapidil also has weak α2-agonist, 5-HT1A-agonist, and weak β1-antagonist actions.
How do beta blockers help in hyperthyroidism?
Beta blockers reduce T4 to T3 conversion and alleviate sympathetic symptoms in hyperthyroidism.
What is the mechanism of action of Phentolamine?
Reversibly blocks α1 and α2 receptors.
頭暈的機制是什麼?
由於直立性低血壓或血流變化,可能影響大腦的血液供應,導致暈眩或頭暈的感覺。
How do beta-blockers contribute to reducing the risk of arrhythmias in ischemic heart disease patients?
By helping to stabilize the heart's rhythm.
What should be done if extrapyramidal effects occur?
Consult a healthcare professional to discuss potential adjustments to medication or alternative treatments to alleviate symptoms.
Provide an example of a topical carbonic anhydrase inhibitor used for open-angle glaucoma.
Dorzolamide.
Which eye condition can be treated with beta blockers?
Beta blockers can be used to treat glaucoma.
What are the clinical applications of Carvedilol, Medroxalol, and Bucindolol?
Heart failure.
How do carbonic anhydrase inhibitors work in open-angle glaucoma?
They reduce aqueous humor production.
What type of tremor can be managed with beta blockers?
Beta blockers can be used to manage essential tremor.
α-阻滯劑的常見副作用有哪些?
直立性低血壓、心跳過速、頭暈和性功能障礙。