p.17
Specific Agents of Alpha-Blockers
What are examples of non-selective alpha blockers?
Phenoxybenzamine and Phentolamine.
p.5
Specific Agents of Alpha-Blockers
What type of alpha blocker is Phentolamine?
Phentolamine is a competitive, non-selective alpha blocker.
p.35
Clinical Uses of Beta Blockers
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.
p.36
Specific Agents of Alpha-Blockers
What are the specific agents of beta-receptor antagonist drugs mentioned?
Metoprolol, atenolol, celiprolol, esmolol.
p.35
Beta-Receptor Antagonists: Mechanism of Action
What type of drug is Propranolol?
Propranolol is a β-blocking drug that also blocks some serotonin receptors in the brain.
p.47
Clinical Uses of Beta Blockers
Which type of beta-blockers is preferred for patients with resting bradycardia?
Beta-blockers with intrinsic sympathetic activity.
p.17
Specific Agents of Alpha-Blockers
What are examples of long-acting selective alpha-1 blockers?
Doxazosin, Terazosin, and Tamulosin.
p.4
Alpha-Receptor Antagonists: Mechanism of Action
Name two reversible alpha-receptor antagonists.
Phentolamine and prazosin.
p.5
Alpha-Receptor Antagonists: Mechanism of Action
What is the nature of the bond formed by Phenoxybenzamine with alpha receptors?
Phenoxybenzamine forms a covalent bond with alpha receptors.
p.47
Clinical Uses of Beta Blockers
Which type of beta-adrenoceptor antagonist is preferred for patients with asthma, COPD, diabetes mellitus, or peripheral vascular disease?
β1-selective antagonists.
p.36
Specific Agents of Alpha-Blockers
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.
p.4
Alpha-Receptor Antagonists: Mechanism of Action
How can the block caused by reversible alpha-receptor antagonists be overcome?
By sufficiently high concentrations of agonists.
p.16
Clinical Applications of Alpha-Receptor Antagonists
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Yohimbine is used for the treatment of orthostatic hypotension and male erectile dysfunction, though it has been superseded by phosphodiesterase-5 inhibitors like sildenafil.
p.6
Pharmacologic Effects of Alpha Blockers
What effect do Tolazoline and Dibenamine have on the maximum response to norepinephrine?
They reduce the maximum response.
p.36
Specific Agents of Alpha-Blockers
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.
p.11
Specific Agents of Alpha-Blockers
What type of receptors does Phentolamine antagonize?
Phentolamine is a potent competitive antagonist of both α1 and α2 receptors.
p.7
Pharmacologic Effects of Alpha Blockers
How do α-receptor antagonist drugs affect urine flow?
They decrease urine flow resistance.
p.50
Adverse Effects of Beta-Blockers
What is recommended to avoid acute withdrawal symptoms from beta-receptor antagonist drugs?
Gradual dose tapering is recommended.
p.32
Adrenoceptor Antagonist Drugs Overview
What does Table 10-1 in Basic & Clinical Pharmacology, 14e describe?
The related selectivity of antagonists for β-adrenoceptors.
p.36
Specific Agents of Alpha-Blockers
Why are metoprolol and atenolol considered low β1-selective?
They are suitable for patients with COPD, myocardial infarction, diabetes, or peripheral vascular disease.
p.29
Beta-Receptor Antagonists: Mechanism of Action
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).
p.46
Clinical Uses of Beta Blockers
What effect does propranolol have on infantile hemangiomas?
It decreases the volume, color, and elevation of infantile hemangiomas.
p.52
Adrenoceptor Antagonist Drugs Overview
What are the main types of adrenoceptors?
Alpha and beta adrenoceptors.
p.44
Clinical Uses of Beta Blockers
What are the antiarrhythmic effects of Sotalol?
Sotalol has antiarrhythmic effects due to its ion channel blocking and beta-blocking actions.
p.1
Adrenoceptor Antagonist Drugs Overview
What is the primary function of adrenoceptor antagonist drugs?
To block the action of adrenaline and noradrenaline on adrenoceptors.
p.44
Clinical Uses of Beta Blockers
Which beta-receptor antagonists are known for reducing mortality in chronic heart failure patients?
Metoprolol, bisoprolol, and carvedilol.
p.39
Specific Agents of Beta-Blockers
What type of drug is Nadolol?
Nadolol is a nonselective β blocker without local anesthetic activity.
p.46
Clinical Uses of Beta Blockers
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.
p.13
Adverse Effects of Beta-Blockers
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).
p.56
Clinical Uses of Beta Blockers
What are the clinical applications of Propranolol, Nadolol, and Timolol?
Hypertension, arrhythmias, angina pectoris, migraine, hyperthyroidism, and glaucoma (topical timolol).
p.26
Clinical Uses of Beta Blockers
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.
p.12
Pharmacologic Effects of Alpha Blockers
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.
p.6
Pharmacologic Effects of Alpha Blockers
What is shown by dose-response curves to norepinephrine in the presence of two different α-adrenoceptor-blocking drugs?
They show reduced maximum response.
p.50
Adverse Effects of Beta-Blockers
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).
p.50
Adverse Effects of Beta-Blockers
Which type of beta-blockers are associated with negative effects on metabolism and lipids?
Non-vasodilating beta-blockers.
p.29
Clinical Uses of 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.
p.44
Clinical Uses of Beta Blockers
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.
p.46
Clinical Uses of Beta Blockers
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.
p.29
Specific Agents of Beta-Blockers
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.
p.52
Adrenoceptor Antagonist Drugs Overview
What are the subtypes of beta adrenoceptors?
Beta-1, beta-2, and beta-3 adrenoceptors.
p.45
Clinical Uses of Beta Blockers
Which beta-receptor antagonist drugs are used to treat open-angle glaucoma?
Timolol, Betaxolol, Carteolol, Levobunolol, and Metipranolol.
p.48
Adverse Effects of Beta-Blockers
How can beta-receptor antagonist drugs affect body weight?
They can cause changes in body weight.
p.18
Clinical Applications of Alpha-Receptor Antagonists
How is pheochromocytoma diagnosed?
By elevated plasma or urinary levels of norepinephrine, epinephrine, metanephrine, and normetanephrine.
p.1
Alpha-Receptor Antagonists: Mechanism of Action
What is the effect of alpha-receptor antagonists on blood vessels?
They cause vasodilation by blocking alpha-receptors, which reduces blood pressure.
p.48
Adverse Effects of Beta-Blockers
What peripheral vascular effect can beta-receptor antagonist drugs cause?
Peripheral vasoconstriction.
p.45
Clinical Uses of Beta Blockers
Which beta-receptor antagonists are used for the prevention of migraine headaches?
Propranolol, Metoprolol, Timolol, Atenolol, and Nadolol.
p.42
Clinical Uses of Beta Blockers
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.
p.7
Pharmacologic Effects of Alpha Blockers
What is the primary cardiovascular effect of α-receptor antagonist drugs?
They lower peripheral vascular resistance and blood pressure.
p.7
Pharmacologic Effects of Alpha Blockers
How do α-receptor antagonist drugs affect the eyes?
They elicit miosis, which means they cause small pupils.
p.7
Pharmacologic Effects of Alpha Blockers
What nasal effect can α-receptor antagonist drugs cause?
They can cause nasal stuffiness.
p.40
Adverse Effects of Beta-Blockers
Why is Betaxolol less likely to induce bronchoconstriction?
Because it is β1-selective.
p.52
Adrenoceptor Antagonist Drugs Overview
What are the subtypes of alpha adrenoceptors?
Alpha-1 and alpha-2 adrenoceptors.
p.11
Clinical Applications of Alpha-Receptor Antagonists
What is a clinical application of Phentolamine?
Phentolamine is used in the treatment of pheochromocytoma.
p.39
Clinical Uses of Beta Blockers
What is Timolol commonly used to treat?
Timolol is commonly used topically for the treatment of glaucoma.
p.49
Adverse Effects of Beta-Blockers
What severe interactions can occur between beta-receptor antagonists and calcium antagonists like verapamil?
Severe hypotension, bradycardia, heart failure, and cardiac conduction abnormalities.
p.44
Clinical Uses of Beta Blockers
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.
p.30
Clinical Applications of Alpha-Receptor Antagonists
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.
p.25
Pharmacokinetics of Beta-Receptor Antagonists
What is the bioavailability of propranolol and why?
Propranolol has low bioavailability due to extensive hepatic (first-pass) metabolism.
p.27
Pharmacokinetics of Beta-Receptor Antagonists
Which beta-receptor antagonists are quite lipophilic and readily cross the blood-brain barrier?
Propranolol and penbutolol.
p.15
Clinical Applications of Alpha-Receptor Antagonists
For which types of migraines is dihydroergotamine not recommended?
Hemiplegic migraine, basilar migraine, or for migraine prevention.
p.50
Adverse Effects of Beta-Blockers
What are some common adverse effects of beta-receptor antagonist drugs?
Fatigue, depression, and sexual dysfunction.
p.16
Alpha-Receptor Antagonists: Mechanism of Action
What effects does Yohimbine have on the CNS and periphery?
Yohimbine blocks α2 receptors, promoting peripheral norepinephrine release and increasing central sympathetic activation.
p.40
Specific Agents of Beta-Blockers
What is Butoxamine used for?
Selective β2-blocking drug used in research.
p.7
Clinical Applications of Alpha-Receptor Antagonists
What condition can α-receptor antagonist drugs treat related to the urinary system?
They can treat urinary retention due to prostatic hyperplasia.
p.39
Specific Agents of Beta-Blockers
What type of drug is Timolol?
Timolol is a nonselective β blocker without local anesthetic activity.
p.46
Clinical Uses of Beta Blockers
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.
p.16
Clinical Applications of Alpha-Receptor Antagonists
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.
p.45
Clinical Uses of Beta Blockers
How do beta-receptor antagonists help in hyperthyroidism?
They reduce palpitations, tachycardia, tremulousness, and anxiety.
p.18
Clinical Applications of Alpha-Receptor Antagonists
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)).
p.1
Beta-Receptor Antagonists: Mechanism of Action
How do beta-receptor antagonists affect the heart?
They decrease heart rate and contractility by blocking beta-receptors.
p.1
Clinical Uses of Beta Blockers
What is a common clinical use of beta-blockers?
Treatment of hypertension and certain types of heart disease.
p.12
Pharmacokinetics of Beta-Receptor Antagonists
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.
p.34
Beta-Receptor Antagonists: Mechanism of Action
Name some cardioselective β-adrenergic blockers.
Metoprolol, Atenolol, Acebutalol, Bisoprolol, Esmolol, Betaxolol, Celiprolol, Nebivolol.
p.38
Beta-Receptor Antagonists: Mechanism of Action
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.
p.34
Beta-Receptor Antagonists: Mechanism of Action
Name some nonselective β-adrenergic blockers without intrinsic sympathomimetic activity (ISA).
Propranolol, Sotalol, Nadolol, Timolol.
p.9
Specific Agents of Alpha-Blockers
Which alpha-receptor antagonist drugs end with 'osin'?
Prazosin, Terazosin, Doxazosin, Tamsulosin.
p.15
Alpha-Receptor Antagonists: Mechanism of Action
Which drugs have both α1-selective and β-antagonistic effects?
Labetalol and carvedilol.
p.19
Adverse Effects of Beta-Blockers
What does rigidity refer to in extrapyramidal effects?
Rigidity refers to muscle stiffness, leading to difficulty in movement and inflexibility.
p.42
Adverse Effects of Beta-Blockers
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.
p.5
Specific Agents of Alpha-Blockers
What type of alpha blocker is Phenoxybenzamine?
Phenoxybenzamine is an irreversible, non-selective alpha blocker.
p.4
Alpha-Receptor Antagonists: Mechanism of Action
What are the two types of alpha-receptor antagonists based on their mechanism of action?
Reversible and irreversible alpha-receptor antagonists.
p.7
Pharmacologic Effects of Alpha Blockers
What are common side effects of α-receptor antagonist drugs?
Orthostatic hypotension and tachycardia.
p.49
Adverse Effects of Beta-Blockers
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.
p.46
Clinical Uses of Beta Blockers
How do beta blockers help in chemotherapy?
Beta blockers prevent chemotherapy-induced cardiomyopathy.
p.16
Adverse Effects of Beta-Blockers
What happens when Yohimbine is combined with norepinephrine transport-blocking drugs?
Combining Yohimbine with norepinephrine transport-blocking drugs can greatly elevate blood pressure.
p.11
Specific Agents of Alpha-Blockers
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.
p.3
Alpha-Receptor Antagonists: Mechanism of Action
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.
p.46
Clinical Uses of Beta Blockers
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.
p.25
Pharmacokinetics of Beta-Receptor Antagonists
How are beta-receptor antagonist drugs absorbed when taken orally?
They are well absorbed, with peak concentrations occurring 1-3 hours after ingestion.
p.26
Adverse Effects of Beta-Blockers
What is a common adverse effect of beta blockers?
Bradycardia (slow heart rate).
p.48
Adverse Effects of Beta-Blockers
What effect do beta-receptor antagonist drugs have on metabolism and lipids?
They can affect metabolism and lipid levels.
p.49
Adverse Effects of Beta-Blockers
Which type of beta antagonist is recommended for diabetic patients after myocardial infarction?
Beta1-selective antagonists.
p.56
Beta-Receptor Antagonists: Mechanism of Action
Which β-blockers are more selective for β1 receptors over β2 receptors?
Metoprolol, Atenolol, Betaxolol, and Nebivolol.
p.37
Specific Agents of Beta-Blockers
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.
p.45
Clinical Uses of Beta Blockers
How does propranolol help with performance anxiety (stage fright)?
It reduces the somatic manifestations of anxiety.
p.10
Specific Agents of Alpha-Blockers
What type of drug is Phenoxybenzamine?
Phenoxybenzamine is a non-selective, long-acting, irreversible α-antagonist.
p.2
Clinical Applications of Alpha-Receptor Antagonists
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.
p.24
Beta-Receptor Antagonists: Mechanism of Action
What is an inverse agonist?
A drug that stabilizes the inactive conformation of β receptors, reducing the number of active receptors.
p.27
Pharmacokinetics of Beta-Receptor Antagonists
Which beta antagonist is excreted unchanged in the urine and has the longest half-life?
Nadolol, with a half-life of 24 hours.
p.20
Clinical Applications of Alpha-Receptor Antagonists
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.
p.42
Specific Agents of Beta-Blockers
Name three beta-blockers mentioned in the text.
Metoprolol, Atenolol, and Timolol.
p.24
Beta-Receptor Antagonists: Mechanism of Action
What are the two conformations in which β receptors can exist?
Active and inactive conformations.
p.29
Beta-Receptor Antagonists: Mechanism of Action
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.
p.50
Adverse Effects of Beta-Blockers
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.
p.11
Alpha-Receptor Antagonists: Mechanism of Action
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.
p.13
Clinical Applications of Alpha-Receptor Antagonists
What are the clinical uses of Doxazosin?
Treatment of hypertension and benign prostatic hyperplasia (BPH).
p.3
Pharmacologic Effects of Alpha Blockers
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.
p.18
Clinical Applications of Alpha-Receptor Antagonists
What are the common symptoms of pheochromocytoma?
Intermittent or sustained hypertension, headaches, palpitations, and sweating.
p.39
Pharmacokinetics of Beta-Receptor Antagonists
How does the duration of action of Nadolol compare to Timolol?
Nadolol has a long duration of action similar to that of Timolol.
p.44
Clinical Uses of Beta Blockers
What is an indication for the use of beta-receptor antagonists in cardiovascular disorders?
Dissecting aortic aneurysms.
p.13
Pharmacokinetics of Beta-Receptor Antagonists
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.
p.43
Clinical Uses of Beta Blockers
What was the condition of the patients involved in the β-blocker therapy study?
Patients who survived myocardial infarctions.
p.13
Pharmacologic Effects of Alpha Blockers
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.
p.21
Clinical Applications of Alpha-Receptor Antagonists
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).
p.1
Adverse Effects of Beta-Blockers
What is a potential adverse effect of beta-blockers?
Bradycardia (abnormally slow heart rate).
p.38
Specific Agents of Alpha-Blockers
What are some specific agents of beta-receptor antagonist drugs?
Labetalol, Carvedilol, Medroxalol, Bucindolol.
p.26
Clinical Uses of Beta Blockers
How do beta blockers help in the management of angina?
By reducing myocardial oxygen demand through decreased heart rate and contractility.
p.27
Pharmacokinetics of Beta-Receptor Antagonists
Which beta antagonists are less completely metabolized?
Atenolol, celiprolol, and pindolol.
p.37
Specific Agents of Beta-Blockers
How might pindolol affect traditional antidepressant medications?
Pindolol may potentiate the action of traditional antidepressant medications.
p.56
Beta-Receptor Antagonists: Mechanism of Action
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).
p.2
Clinical Uses of Beta Blockers
What are some common clinical uses of beta blockers?
Beta blockers are commonly used to treat hypertension, angina, heart failure, and arrhythmias.
p.9
Specific Agents of Alpha-Blockers
List three other alpha-adrenoceptor antagonists.
Alfuzosin, Silodosin, Indoramin.
p.8
Alpha-Receptor Antagonists: Mechanism of Action
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.
p.23
Clinical Uses of Beta Blockers
Name a common clinical use of beta blockers.
Treatment of hypertension.
p.9
Specific Agents of Alpha-Blockers
Name two alpha-adrenoceptor antagonists that are also used as antipsychotic medications.
Chlorpromazine, Haloperidol.
p.28
Specific Agents of Beta-Blockers
Which beta1-selective antagonists are mentioned, and what do they block?
Metoprolol and atenolol, which block beta1 receptors in the heart.
p.14
Adverse Effects of Beta-Blockers
What is a potential risk associated with Alfuzosin?
Alfuzosin may increase the risk of QT prolongation.
p.16
Alpha-Receptor Antagonists: Mechanism of Action
What type of antagonist is Yohimbine?
Yohimbine is an α2-selective antagonist.
p.40
Clinical Uses of Beta Blockers
What is the clinical application of Carteolol?
Topical ophthalmic application in glaucoma.
p.40
Clinical Uses of Beta Blockers
What is the clinical use of nonselective β-receptor antagonists?
Topical ophthalmic application in glaucoma.
p.30
Clinical Applications of Alpha-Receptor Antagonists
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.
p.13
Pharmacokinetics of Beta-Receptor Antagonists
What is the half-life of Doxazosin and how is it administered?
Doxazosin has a half-life of 22 hours and is administered orally.
p.43
Clinical Uses of Beta Blockers
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.
p.13
Alpha-Receptor Antagonists: Mechanism of Action
What receptors does Tamsulosin have a higher affinity for?
Tamsulosin has a higher affinity for α1A and α1D receptors than for α1B receptors.
p.45
Clinical Uses of Beta Blockers
What is a potential interaction between topical timolol and oral verapamil?
It may increase the risk of heart block.
p.37
Specific Agents of Beta-Blockers
What are some specific agents of beta-receptor antagonist drugs?
Pindolol, acebutolol, penbutolol, carteolol, oxprenolol, celiprolol, nebivolol.
p.30
Clinical Applications of Alpha-Receptor Antagonists
What are the treatment options for closed-angle glaucoma?
Drug control and prevention by iridectomy (surgical removal of part of the iris).
p.21
Clinical Applications of Alpha-Receptor Antagonists
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.
p.20
Clinical Applications of Alpha-Receptor Antagonists
What are alpha-receptor antagonist drugs used for in clinical pharmacology?
They are used for hypertensive emergencies and chronic hypertension.
p.18
Specific Agents of Alpha-Blockers
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.
p.37
Specific Agents of Beta-Blockers
What is the selectivity of acebutolol?
Acebutolol is a beta1-selective antagonist.
p.12
Clinical Applications of Alpha-Receptor Antagonists
What are the primary clinical uses of Prazosin?
Prazosin is primarily used for the management of hypertension.
p.37
Specific Agents of Beta-Blockers
What additional receptor does pindolol antagonize?
Pindolol also antagonizes 5-HT1A serotonin receptors.
p.42
Clinical Uses of Beta Blockers
What is the role of beta-blockers in chronic stable angina?
They are considered first-line therapy.
p.19
Adverse Effects of Beta-Blockers
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.
p.24
Beta-Receptor Antagonists: Mechanism of Action
Which β-blockers are known as inverse agonists?
Betaxolol and metoprolol.
p.27
Pharmacokinetics of Beta-Receptor Antagonists
What effect does renal failure have on nadolol's half-life?
Renal failure prolongs nadolol's half-life.
p.10
Alpha-Receptor Antagonists: Mechanism of Action
Which receptors, besides α-receptors, does Phenoxybenzamine block?
Phenoxybenzamine blocks histamine (H1), acetylcholine, and serotonin receptors.
p.15
Alpha-Receptor Antagonists: Mechanism of Action
What are the effects of neuroleptic drugs on receptors?
They are potent dopamine receptor antagonists and α antagonists.
p.34
Beta-Receptor Antagonists: Mechanism of Action
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.
p.10
Adverse Effects of Beta-Blockers
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.
p.34
Beta-Receptor Antagonists: Mechanism of Action
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.
p.15
Clinical Applications of Alpha-Receptor Antagonists
What conditions is dihydroergotamine used to treat?
Migraine headaches and cluster headaches.
p.4
Alpha-Receptor Antagonists: Mechanism of Action
How does phenoxybenzamine achieve irreversible blockade of alpha receptors?
It forms a reactive ethyleneimonium intermediate that covalently binds to alpha receptors.
p.11
Pharmacologic Effects of Alpha Blockers
How does Phentolamine affect vascular smooth muscle?
Phentolamine reduces peripheral resistance by blocking α1 and α2 receptors on vascular smooth muscle.
p.49
Adverse Effects of Beta-Blockers
What are some peripheral vascular effects of beta-receptor antagonist drugs?
Peripheral vasoconstriction, cold extremities, and worsening of peripheral vascular disease and Raynaud phenomenon.
p.48
Adverse Effects of Beta-Blockers
How do beta-receptor antagonist drugs affect myocardial contractility?
They depress myocardial contractility.
p.16
Alpha-Receptor Antagonists: Mechanism of Action
How does Yohimbine interact with α2-adrenoceptor agonists like clonidine?
Yohimbine reverses the antihypertensive effects of α2-adrenoceptor agonists such as clonidine.
p.49
Adverse Effects of Beta-Blockers
How can beta-receptor antagonist drugs affect myocardial contractility?
They can depress myocardial contractility.
p.26
Clinical Uses of Beta Blockers
What are some common clinical uses of beta blockers?
Treatment of hypertension, angina, heart failure, and arrhythmias.
p.1
Adrenoceptor Antagonist Drugs Overview
What are the two main types of adrenoceptors that antagonist drugs target?
Alpha-receptors and beta-receptors.
p.21
Clinical Applications of Alpha-Receptor Antagonists
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.
p.3
Clinical Applications of Alpha-Receptor Antagonists
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.
p.37
Specific Agents of Beta-Blockers
Which beta-receptor antagonist drugs are not available in the USA?
Oxprenolol and celiprolol.
p.24
Beta-Receptor Antagonists: Mechanism of Action
What is the primary mechanism of action for β-blocking drugs?
Antagonizing the effects of catecholamines at β adrenoceptors.
p.20
Clinical Applications of Alpha-Receptor Antagonists
What conditions can cause increased blood pressure that reflects excess circulating concentrations of alpha agonists?
Pheochromocytoma, overdosage of sympathomimetic drugs, or clonidine withdrawal.
p.42
Clinical Uses of Beta Blockers
How do beta-blockers benefit patients during an acute myocardial infarction?
Early administration can reduce infarct size and acute mortality.
p.37
Specific Agents of Beta-Blockers
What is a notable effect of the most highly selective beta1-adrenergic receptor blockers?
They promote endothelial nitric oxide production, leading to vasodilation.
p.12
Clinical Applications of Alpha-Receptor Antagonists
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).
p.37
Specific Agents of Beta-Blockers
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.
p.10
Clinical Applications of Alpha-Receptor Antagonists
What is the primary clinical use of Phenoxybenzamine?
Phenoxybenzamine is primarily used for the treatment of pheochromocytoma.
p.38
Clinical Uses of Beta Blockers
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.
p.8
Pharmacologic Effects of Alpha Blockers
How do α1-adrenoceptor antagonists affect the body?
α1-adrenoceptor antagonists cause vasodilation by blocking α1 receptors on blood vessels, which reduces blood pressure.
p.24
Beta-Receptor Antagonists: Mechanism of Action
What is the physiological impact of inverse agonists?
They reduce the physiological response by decreasing the number of active receptors.
p.29
Adverse Effects of Beta-Blockers
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.
p.49
Adverse Effects of Beta-Blockers
What cardiac effects can beta-receptor antagonist drugs induce?
Sinus bradycardia, slow atrioventricular (AV) node conduction, and potentially serious bradyarrhythmias.
p.45
Clinical Uses of Beta Blockers
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.
p.48
Adverse Effects of Beta-Blockers
What are some common psychological and physical side effects of beta-receptor antagonist drugs?
Fatigue, depression, and sexual dysfunction.
p.3
Specific Agents of Alpha-Blockers
Name a specific agent that is an alpha-blocker.
Prazosin is a specific agent that acts as an alpha-blocker.
p.49
Adverse Effects of Beta-Blockers
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.
p.56
Beta-Receptor Antagonists: Mechanism of Action
What is the mechanism of action for Propranolol, Nadolol, and Timolol?
They block β1 and β2 receptors.
p.26
Beta-Receptor Antagonists: Mechanism of Action
How do beta blockers affect the heart?
They decrease heart rate and contractility, reducing cardiac output.
p.12
Specific Agents of Alpha-Blockers
What type of drug is Prazosin?
Prazosin is a piperazinyl quinazoline, highly selective for α1 receptors and acts as a competitive antagonist.
p.48
Adverse Effects of Beta-Blockers
What can happen if beta-receptor antagonist drugs are withdrawn acutely?
Acute withdrawal can occur.
p.30
Clinical Applications of Alpha-Receptor Antagonists
How do alpha agonists, beta blockers, and carbonic anhydrase inhibitors help in treating glaucoma?
They decrease aqueous humor secretion.
p.1
Comparison of Alpha and Beta Blockers
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.
p.18
Alpha-Receptor Antagonists: Mechanism of Action
What is the role of tyrosine hydroxylase in catecholamine synthesis?
It is the rate-limiting step in the synthesis of dopamine, norepinephrine, and epinephrine.
p.9
Specific Agents of Alpha-Blockers
Name three specific alpha-receptor antagonist drugs.
Phenoxybenzamine, Phentolamine, Prazosin.
p.12
Pharmacokinetics of Beta-Receptor Antagonists
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.
p.38
Pharmacologic Effects of Alpha Blockers
How does the β-blocking potency of Labetalol compare to Propranolol?
Labetalol has less β-blocking potency than Propranolol.
p.27
Pharmacokinetics of Beta-Receptor Antagonists
What conditions can prolong propranolol's half-life?
Liver disease, diminished hepatic blood flow, or hepatic enzyme inhibition.
p.19
Adverse Effects of Beta-Blockers
What is bradykinesia?
Bradykinesia is the slowing down of movement and extended reaction time.
p.24
Beta-Receptor Antagonists: Mechanism of Action
What happens to the number of active receptors when inverse agonists bind to them?
The number of active receptors decreases, reducing intracellular signaling.
p.42
Beta-Receptor Antagonists: Mechanism of Action
How do beta-blockers reduce the heart's oxygen demand?
By decreasing heart rate and myocardial contractility.
p.19
Adverse Effects of Beta-Blockers
What is akathisia?
Akathisia is a feeling of restlessness, where the patient may feel the need to keep moving.
p.19
Adverse Effects of Beta-Blockers
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.
p.29
Adverse Effects of Beta-Blockers
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.
p.26
Beta-Receptor Antagonists: Mechanism of Action
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.
p.18
Clinical Applications of Alpha-Receptor Antagonists
What hormones does pheochromocytoma secrete?
Catecholamines, especially norepinephrine and epinephrine.
p.30
Clinical Applications of Alpha-Receptor Antagonists
What are the two major types of glaucoma?
Open-angle glaucoma and closed-angle (narrow-angle) glaucoma.
p.25
Pharmacokinetics of Beta-Receptor Antagonists
Which beta-receptor antagonist drugs have sustained-release preparations?
Propranolol and metoprolol.
p.21
Clinical Applications of Alpha-Receptor Antagonists
Which alpha-receptor antagonists are used for treating Benign Prostatic Hyperplasia (BPH)?
Prazosin, doxazosin, and terazosin.
p.3
Adverse Effects of Beta-Blockers
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.
p.43
Clinical Uses of Beta Blockers
What was measured in the study on β-blocker therapy?
Life-table cumulated rates of mortality from all causes.
p.26
Adverse Effects of Beta-Blockers
What is a potential adverse effect of beta blockers in patients with asthma?
Bronchoconstriction, which can worsen asthma symptoms.
p.42
Clinical Uses of Beta Blockers
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.
p.28
Beta-Receptor Antagonists: Mechanism of Action
What is the effect of beta-receptor antagonist drugs on blood pressure in patients with hypertension?
They chronically lower blood pressure.
p.21
Clinical Applications of Alpha-Receptor Antagonists
What are the applications of alpha2 antagonists?
They are used in the treatment of peripheral vascular disease.
p.28
Beta-Receptor Antagonists: Mechanism of Action
What are the mechanisms by which beta-receptor antagonists lower blood pressure?
Suppression of renin release and effects in the CNS.
p.38
Pharmacologic Effects of Alpha Blockers
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.
p.23
Pharmacokinetics of Beta-Receptor Antagonists
What is the primary effect of blocking Beta-1 receptors?
Reduction in heart rate and blood pressure.
p.24
Beta-Receptor Antagonists: Mechanism of Action
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.
p.2
Pharmacologic Effects of Alpha Blockers
What are some pharmacologic effects of alpha blockers?
Alpha blockers cause vasodilation, decreased peripheral resistance, and lower blood pressure.
p.19
Adverse Effects of Beta-Blockers
What is dystonia?
Dystonia is uncontrollable muscle contractions that may lead to abnormal postures or movements.
p.38
Pharmacokinetics of Beta-Receptor Antagonists
Why should Carvedilol not be combined with CYP2D6 inhibitors?
Combining Carvedilol with CYP2D6 inhibitors like quinidine or fluoxetine can interfere with its metabolism.
p.8
Specific Agents of Alpha-Blockers
Name a specific α1-adrenoceptor antagonist.
Prazosin is a specific α1-adrenoceptor antagonist.
p.8
Clinical Applications of Alpha-Receptor Antagonists
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).
p.14
Clinical Applications of Alpha-Receptor Antagonists
What is the primary use of α1-selective antagonists?
α1-selective antagonists are primarily used as antihypertensive agents.
p.41
Clinical Uses of Beta Blockers
How do beta blockers benefit patients with congestive heart failure?
Beta blockers help manage symptoms and improve heart function in congestive heart failure.
p.55
Alpha-Receptor Antagonists: Mechanism of Action
What is the mechanism of action of Phenoxybenzamine?
Irreversibly blocks α1 and α2 receptors.
p.25
Pharmacokinetics of Beta-Receptor Antagonists
Which beta-receptor antagonists have limited bioavailability due to first-pass metabolism?
Most beta antagonists, except betaxolol, penbutolol, pindolol, and sotalol.
p.26
Pharmacokinetics of Beta-Receptor Antagonists
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.
p.24
Beta-Receptor Antagonists: Mechanism of Action
What are pure antagonists in the context of β-blocking drugs?
Drugs that occupy the β receptor without activating it.
p.2
Alpha-Receptor Antagonists: Mechanism of Action
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.
p.24
Beta-Receptor Antagonists: Mechanism of Action
What are partial agonists in the context of β-blocking drugs?
Drugs that partially activate β receptors while blocking them.
p.23
Beta-Receptor Antagonists: Mechanism of Action
What is the primary mechanism of action for beta-receptor antagonists?
They block the effects of adrenaline on beta receptors.
p.23
Beta-Receptor Antagonists: Mechanism of Action
What are the two main types of beta receptors that beta blockers target?
Beta-1 and Beta-2 receptors.
p.10
Alpha-Receptor Antagonists: Mechanism of Action
What neurotransmitter's reuptake is inhibited by Phenoxybenzamine?
Phenoxybenzamine inhibits the reuptake of norepinephrine by presynaptic adrenergic nerve terminals.
p.8
Adrenoceptor Antagonist Drugs Overview
What are α-adrenoceptors?
α-adrenoceptors are a class of G-protein-coupled receptors that are targets for catecholamines like norepinephrine and epinephrine.
p.28
Beta-Receptor Antagonists: Mechanism of Action
What is the effect of blocking beta receptors in the atrioventricular node?
It slows atrioventricular conduction and increases the PR interval.
p.38
Pharmacokinetics of Beta-Receptor Antagonists
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.
p.8
Adrenoceptor Antagonist Drugs Overview
What are the two main types of α-adrenoceptors?
The two main types of α-adrenoceptors are α1 and α2 receptors.
p.34
Beta-Receptor Antagonists: Mechanism of Action
Name some mixed α and β blockers.
Labetalol and Carvedilol.
p.2
Pharmacokinetics of Beta-Receptor Antagonists
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.
p.41
Clinical Uses of Beta Blockers
Why are beta blockers not used for vasospastic angina pectoris?
Beta blockers are not effective for vasospastic angina pectoris.
p.41
Clinical Uses of Beta Blockers
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.
p.55
Alpha-Receptor Antagonists: Mechanism of Action
What is the mechanism of action of Prazosin, Doxazosin, Terazosin, Alfuzosin, Indoramin, and Urapidil?
They block α1 receptors but not α2 receptors.
p.55
Clinical Applications of Alpha-Receptor Antagonists
What are the clinical applications of Yohimbine?
Male erectile dysfunction and hypotension.
p.56
Clinical Uses of Beta Blockers
What are the clinical applications of Metoprolol, Atenolol, Betaxolol, and Nebivolol?
Hypertension, arrhythmias, angina pectoris, and glaucoma (topical betaxolol).
p.19
Clinical Applications of Alpha-Receptor Antagonists
What is the effect of phenoxybenzamine (Dibenzyline) on blood pressure in a patient with pheochromocytoma?
Phenoxybenzamine lowers blood pressure in patients with pheochromocytoma.
p.12
Specific Agents of Alpha-Blockers
What type of antagonist is Terazosin?
Terazosin is a reversible α1-selective antagonist.
p.2
Beta-Receptor Antagonists: Mechanism of Action
How do beta-receptor antagonist drugs work?
Beta-receptor antagonist drugs block beta-adrenergic receptors, reducing heart rate, cardiac output, and blood pressure.
p.28
Clinical Uses of Beta Blockers
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.
p.21
Clinical Applications of Alpha-Receptor Antagonists
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.
p.34
Beta-Receptor Antagonists: Mechanism of Action
Name some nonselective β-adrenergic blockers with intrinsic sympathomimetic activity (ISA).
Acebutolol, Carteolol, Penbutolol, Pindolol, Oxprenolol.
p.14
Specific Agents of Alpha-Blockers
What type of drug is Alfuzosin?
Alfuzosin is a quinazoline derivative and an α1-selective antagonist.
p.2
Adverse Effects of Beta-Blockers
What are some adverse effects associated with beta blockers?
Adverse effects of beta blockers can include bradycardia, fatigue, depression, and worsening of asthma symptoms.
p.23
Adverse Effects of Beta-Blockers
What is a potential adverse effect of beta blockers on respiratory function?
Bronchoconstriction, which can worsen asthma.
p.31
Clinical Applications of Alpha-Receptor Antagonists
What is the primary goal of topical drugs used in open-angle glaucoma?
To reduce intraocular pressure (IOP).
p.23
Adverse Effects of Beta-Blockers
Why should beta blockers be used cautiously in diabetic patients?
They can mask the symptoms of hypoglycemia.
p.14
Alpha-Receptor Antagonists: Mechanism of Action
Which receptor does Silodosin primarily block?
Silodosin primarily blocks the α1A receptor.
p.14
Clinical Applications of Alpha-Receptor Antagonists
What condition is Silodosin used to treat?
Silodosin is used to treat benign prostatic hyperplasia (BPH).
p.31
Clinical Applications of Alpha-Receptor Antagonists
What is the mechanism of action of alpha agonists in treating open-angle glaucoma?
They decrease aqueous humor production and increase uveoscleral outflow.
p.31
Clinical Applications of Alpha-Receptor Antagonists
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.
p.21
Clinical Applications of Alpha-Receptor Antagonists
Which conditions involving excessive reversible vasospasm in the peripheral circulation can be treated with prazosin or phenoxybenzamine?
Raynaud phenomenon and other similar conditions.
p.30
Clinical Applications of Alpha-Receptor Antagonists
Which drugs increase aqueous outflow in the treatment of glaucoma?
Prostaglandin F2 alpha analogs, cholinomimetics, and rho kinase inhibitors.
p.10
Specific Agents of Alpha-Blockers
How long does the effect of Phenoxybenzamine last?
The effect of Phenoxybenzamine lasts between 14 to 48 hours.
p.21
Clinical Applications of Alpha-Receptor Antagonists
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.
p.19
Adverse Effects of Beta-Blockers
What is tremor in the context of extrapyramidal effects?
Tremor is an involuntary shaking, usually affecting the hands or limbs.
p.56
Clinical Uses of Beta Blockers
What are the clinical applications of β-blockers with intrinsic sympathomimetic activity (ISA)?
Hypertension, arrhythmias, migraine, and may avoid worsening of bradycardia.
p.23
Pharmacokinetics of Beta-Receptor Antagonists
What is the primary effect of blocking Beta-2 receptors?
Constriction of bronchial muscles and blood vessels.
p.28
Beta-Receptor Antagonists: Mechanism of Action
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.
p.14
Pharmacokinetics of Beta-Receptor Antagonists
What is the bioavailability and half-life of Alfuzosin when taken orally?
The bioavailability is 60% and the half-life is 5 hours.
p.2
Comparison of Alpha and Beta Blockers
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.
p.42
Clinical Uses of Beta Blockers
How do beta-blockers help in reducing the frequency and severity of angina attacks?
By lowering the heart's workload.
p.28
Adverse Effects of Beta-Blockers
Why should beta antagonists generally be avoided in patients with asthma?
Because they increase airway resistance by blocking beta2 receptors in bronchial smooth muscle.
p.28
Clinical Uses of Beta Blockers
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.
p.15
Clinical Applications of Alpha-Receptor Antagonists
What is Cafergot® used for?
Treating migraine attacks and vascular headaches.
p.41
Clinical Uses of Beta Blockers
What neurological condition characterized by severe headaches can be treated with beta blockers?
Beta blockers can be used to treat migraines.
p.22
Adverse Effects of Beta-Blockers
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。
p.42
Clinical Uses of Beta Blockers
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.
p.14
Clinical Applications of Alpha-Receptor Antagonists
What condition is Alfuzosin used to treat?
Alfuzosin is used to treat benign prostatic hyperplasia (BPH).
p.15
Alpha-Receptor Antagonists: Mechanism of Action
What is the action of ergot derivatives like ergotamine and dihydroergotamine?
They cause reversible α-receptor blockade with partial agonist action.
p.23
Clinical Uses of Beta Blockers
How do beta blockers help in the management of angina pectoris?
By reducing myocardial oxygen demand.
p.23
Comparison of Alpha and Beta Blockers
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.
p.42
Clinical Uses of Beta Blockers
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.
p.14
Clinical Applications of Alpha-Receptor Antagonists
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.
p.41
Clinical Uses of Beta Blockers
How do beta blockers help with anxiety, specifically social phobia?
Beta blockers reduce physical symptoms of anxiety, such as heart palpitations, in social phobia.
p.55
Clinical Applications of Alpha-Receptor Antagonists
What is the clinical application of Tamsulosin and Silodosin?
Benign prostatic hyperplasia.
p.28
Adverse Effects of Beta-Blockers
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.
p.24
Beta-Receptor Antagonists: Mechanism of Action
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.
p.31
Clinical Applications of Alpha-Receptor Antagonists
How do beta-blockers help in the treatment of open-angle glaucoma?
By decreasing the production of aqueous humor.
p.41
Clinical Uses of Beta Blockers
How do beta blockers help in the prophylaxis of myocardial infarction?
Beta blockers prevent reinfarction and ventricular fibrillation.
p.41
Clinical Uses of Beta Blockers
What condition involving a tumor can be treated with beta blockers?
Beta blockers can be used to treat pheochromocytoma.
p.55
Alpha-Receptor Antagonists: Mechanism of Action
Which α-blockers are slightly selective for α1A receptors?
Tamsulosin and Silodosin.
p.22
Adverse Effects of Beta-Blockers
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。
p.8
Pharmacologic Effects of Alpha Blockers
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.
p.2
Specific Agents of Alpha-Blockers
Name a specific agent of alpha-blockers and its use.
Prazosin is an alpha-blocker used to treat hypertension and benign prostatic hyperplasia.
p.41
Clinical Uses of Beta Blockers
What are beta blockers used for in the treatment of hypertension?
Beta blockers are used to lower blood pressure in patients with hypertension.
p.8
Adverse Effects of Beta-Blockers
What is a common adverse effect of α-adrenoceptor antagonists?
A common adverse effect of α-adrenoceptor antagonists is orthostatic hypotension.
p.41
Clinical Uses of Beta Blockers
Which beta blocker is commonly used for cardiac arrhythmias?
Propranolol is commonly used for cardiac arrhythmias.
p.55
Clinical Applications of Alpha-Receptor Antagonists
Which α-blockers are used for hypertension and benign prostatic hyperplasia?
Prazosin, Doxazosin, Terazosin, Alfuzosin, Indoramin, Urapidil.
p.22
Adverse Effects of Beta-Blockers
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。
p.55
Beta-Receptor Antagonists: Mechanism of Action
What is the mechanism of action of Labetalol, Carvedilol, Medroxalol, and Bucindolol?
They block β receptors more than α1 receptors.
p.19
Adverse Effects of Beta-Blockers
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.
p.19
Adverse Effects of Beta-Blockers
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.
p.14
Alpha-Receptor Antagonists: Mechanism of Action
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.
p.41
Clinical Uses of Beta Blockers
How do beta blockers help in hyperthyroidism?
Beta blockers reduce T4 to T3 conversion and alleviate sympathetic symptoms in hyperthyroidism.
p.55
Alpha-Receptor Antagonists: Mechanism of Action
What is the mechanism of action of Phentolamine?
Reversibly blocks α1 and α2 receptors.
p.22
Adverse Effects of Beta-Blockers
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。
p.42
Clinical Uses of Beta Blockers
How do beta-blockers contribute to reducing the risk of arrhythmias in ischemic heart disease patients?
By helping to stabilize the heart's rhythm.
p.19
Adverse Effects of Beta-Blockers
What should be done if extrapyramidal effects occur?
Consult a healthcare professional to discuss potential adjustments to medication or alternative treatments to alleviate symptoms.
p.41
Clinical Uses of Beta Blockers
Which eye condition can be treated with beta blockers?
Beta blockers can be used to treat glaucoma.
p.31
Clinical Applications of Alpha-Receptor Antagonists
How do carbonic anhydrase inhibitors work in open-angle glaucoma?
They reduce aqueous humor production.
p.41
Clinical Uses of Beta Blockers
What type of tremor can be managed with beta blockers?
Beta blockers can be used to manage essential tremor.
