The beta-adrenergic blocking agents are used to treat CV problems (hypertension, angina, migraine headaches) and to prevent reinfarction after MI. These drugs are widely used and include carteolol (generic), metipranolol (OptiPranolol), nadolol (Corgard), nebivolol (Bystolic), propranolol (Inderal), sotalol (Betapace, Betapace AF), and timolol (Timoptic). The prototype drug, propranolol, was in fact the most prescribed drug in the United States in the 1980s.
The therapeutic effects of these drugs are related to their competitive blocking of the beta-adrenergic receptors in the SNS. The blockade of the beta-receptors in the heart and in the juxtaglomerular apparatus of the nephron accounts for the majority of the therapeutic benefit. Decreased heart rate, contractility, and excitability, as well as a membrane-stabilizing effect, lead to a decrease in arrhythmias, decreased cardiac workload, and decreased oxygen consumption. The juxtaglomerular cells are not stimulated to release renin, which further decreases the blood pressure. These effects are useful in treating hypertension and chronic angina and can help to prevent reinfarction after an MI by decreasing cardiac workload and oxygen consumption. Sotalol is used exclusively for treating life-threatening ventricular arrhythmias and to maintain sinus rhythm in patients with atrial flutter or atrial fibrillation.
These drugs are absorbed from the GI tract after oral administration and undergo hepatic metabolism. Food has been found to increase the bioavailability of propranolol, although this effect was not found with other beta-adrenergic blocking agents. Absorption of sotalol is decreased by the presence of food. Propranolol also crosses the blood–brain barrier, but nadolol, and sotalol do not, making them a better choice if CNS effects occur with propranolol. These drugs are all excreted in the urine. Carteolol and metipranolol are only available in an ophthalmic form and are not usually absorbed systemically.
Propranolol is very effective in blocking all of the beta-receptors in the SNS and was one of the first drugs of the class. Since the introduction of propranolol, newer and more selective drugs have become available that are not associated with some of the adverse effects seen with total blockade of the SNS beta-receptors. In 2014 propranolol was approved in an oral solution form for the treatment of proliferating infantile hemoangioma in children 5 weeks to 5 months of age (Hemangeol). Nebivolol is the newest adrenergic blocker available and is not associated with the variety of adverse effects seen with propranolol use. Timolol has several recommended uses; timolol, carteolol, and metipranolol are available in an ophthalmic form of the drug for reduction of intraocular pressure in patients with open-angle glaucoma. When these drugs are used topically, eye muscle relaxation occurs. In addition, because they are applied topically, they are usually not absorbed systemically from this route.
Drug–Drug Interaction is a major concern in use of beta blockers.
药药相互作用是β阻滞剂使用的一个重大问题
A paradoxical hypertension occurs when beta-blockers are given with clonidine, and an increased rebound hypertension with clonidine withdrawal may also occur. It is best to avoid this combination.
Β阻滞药与可乐定联用时出现反常高血压；可乐定停用时可能出现反跳性高血压。最好避免此种联用。
A decreased antihypertensive effect occurs when beta-blockers are given with nonsteroidal anti-inflammatory drugs (NSAIDs); if this combination is used the patient should be monitored closely and dose adjustment should be made to achieve the desired control of blood pressure.
β阻滞药与非甾类消炎药（NSAIDs）一起使用时降压效应下降；联用时，应密切监测患者，及时调整剂量，以获得预期的血压控制效应。
An initial hypertensive episode followed by bradycardia may occur if these drugs are given with epinephrine. Peripheral ischemia may occur if the beta-blockers are taken in combination with ergot alkaloids.
上述药物若与肾上腺素一起使用，可能出现最初高血压性发作及随后的心动过缓。如果β阻滞药与与麦角生物碱类联用，可能出现周围神经缺血。
When these drugs are given with insulin or other antidiabetic agents, there is a potential for change in blood glucose levels. The patient also will not display the usual signs and symptoms of hypoglycemia or hyperglycemia, which are caused by activation of the SNS. Because these effects are blocked the patient will need new indications to alert him or her to potential problems. If this combination is used the patient should monitor blood glucose levels frequently throughout the day and should be alert to new manifestations indicating glucose imbalance.
reinfarction – n. 再梗塞
carteolol – n. 卡替洛尔
metipranolol – n. 美替洛尔
OptiPranolol – n. 0.3%盐酸美替洛尔眼液
nadolol – n. 纳多洛尔
Corgard – n. 【奥】可佳得
nebivolol – n. 奈必洛尔
Bystolic – n. 【奥】必思托里克
propranolol – n. 普萘洛尔
Inderal – n. 心得安
sotalol – n. 索他洛尔
Betapace – n. 【奥】倍他佩斯
Betapace AF – n. 倍他佩斯AF
timolol – n. 噻吗洛尔
Timoptic – n. 青眼露
juxtaglomerular – a. 肾小球旁的
juxtaglomerular apparatus -- 肾小球旁器
hemoangioma – n. 血管瘤
Hemangeol – n. 盐酸普萘洛尔 注：带【奥】标记者为奥医临时用名，只为方便学员记忆，不得作为临床使用依据。
1. A client with asthma is given albuterol sulfate (Proventil), a selective adrenergic drug that stimulates the beta2-receptor site. Which response should the nurse expect to see in the client?
A. Bronchoconstriction
B. Bronchodilation
C. Decreased heart rate
D. Increased blood pressure 2. Albuterol sulfate (Proventil) has a short half-life and duration of action. Based on this information, what should the nurse select as an appropriate dosing schedule for this drug?
A. Once a day
B. Once every other day
C. 3 or 4 times a day
D. 2 times a day
奥医教育“在线自测”正式上线，复习练习、效果检验，奥医NCLEX-RN/ISPN题库一站完成。
答案 Answers
1. B. Bronchodilation Rationale: Albuterol sulfate is a bronchodilator. 2. C: 3 or 4 times a day Rationale: A short half-life indicates that a medication must be given more frequently.
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