选择性β1受体阻断药，有内在拟交感活性和膜稳定作用。其β1受体选择性不如阿替洛尔，β受体阻断强度约为普萘洛尔的1/2，内在拟交感活性介于氧烯洛尔和烯丙洛尔之间。对静息时心率的减慢作用较小，增加外周阻力的作用也比普萘洛尔为弱。对血浆肾素活性的降低作用不如非选择性β受体阻断药。
药动学
口服吸收率为70%，首过效应为30%，生物利用度为20%-60%，代谢率为65%-85%，血浆蛋白结合率为15%-75%，口服后血浆药物浓度达峰时间为1-4h，t1/2为2-7h，分布容积为1-3L/kg，可广泛地分布到身体各部，能透过胎盘屏障，也可分泌在乳汁中，较少进入脑内。血药浓度的个体差异为6-24倍。主要代谢产物为双醋洛尔。该代谢产物与醋丁洛尔有相等的β受体阻断作用，其t1/2为8-12h。1次口服本品后36h，血中双醋洛尔的浓度为母体的13倍。两种物质均可分泌于胆汁中，都有肠肝循环。
适应症
偶见过敏反应，表现为皮疹、结膜炎和过敏性肺炎等。免疫反应有狼疮样综合征、抗核抗体升高等。一例服本品6g者过量中毒，救活。另一例服本品16g，4h后昏迷，心率减慢至每分钟25次，血压下降。20h后死亡。
规格
Acebutolol capsules
What are acebutolol capsules?
ACEBUTOLOL (Sectral®) belongs to a group of medicines called beta-blockers. Beta-blockers reduce the workload on the heart and help it to beat more regularly. Acebutolol is used to control high blood pressure (hypertension), and to treat or prevent certain heart rhythm problems (ventricular arrhythmias). Acebutolol does not cure high blood pressure. Generic acebutolol capsules are available.
What should I tell my health care provider before I take this medicine?
They need to know if you have any of these conditions:
• asthma or bronchitis
• blood vessel disease (such as Raynaud's disease)
• depression
• diabetes
• emphysema
• history of heart attack, or heart disease
• kidney disease
• liver disease
• muscle weakness or disease
• psoriasis
• thyroid disease
• an unusual or allergic reaction to acebutolol, other beta-blockers, medicines, foods, dyes, or preservatives
• pregnant or trying to get pregnant
• breast-feeding
How should I take this medicine?
Take acebutolol capsules by mouth. Follow the directions on the prescription label. Swallow the capsules whole with a drink of water. Take your doses at regular intervals. Do not take your medicine more often than directed. Do not stop taking except on your prescriber's advice.
Contact your pediatrician or health care professional regarding the use of this medicine in children. Special care may be needed.
What if I miss a dose?
If you miss a dose, take it as soon as you can. If it is almost time for your next dose, take only that dose. Do not take double or extra doses. There should be at least 4 hours between doses.
What drug(s) may interact with acebutolol?
• cimetidine
• cocaine
• hawthorn
• medicines for colds and breathing difficulties
• medicines for diabetes
• medicines for high blood pressure
• medicines to control heart rhythm
• monoamine oxidase inhibitors (Azilect®, Eldepryl®, Emsam®, Marplan®, Nardil®, Parnate®, Zelapar™)
• water pills
Tell your prescriber or health care professional about all other medicines you are taking, including nonprescription medicines, nutritional supplements, or herbal products. Also tell your prescriber or health care professional if you are a frequent user of drinks with caffeine or alcohol, if you smoke, or if you use illegal drugs. These may affect the way your medicine works. Check with your health care professional before stopping or starting any of your medicines.
What should I watch for while taking acebutolol?
Check your heart rate and blood pressure regularly while you are taking acebutolol. Ask your prescriber or health care professional what your heart rate and blood pressure should be, and when you should contact him or her.
Do not stop taking this medicine suddenly. This could lead to serious heart-related effects.
You may get drowsy or dizzy. Do not drive, use machinery, or do anything that requires mental alertness until you know how acebutolol affects you. To reduce the risk of dizzy or fainting spells, do not sit or stand up quickly. Alcohol can make you more drowsy, increase flushing, and cause rapid heartbeats. Therefore, it is best to avoid alcoholic drinks.
Acebutolol can affect blood sugar levels. If you are diabetic, check with your prescriber or health care professional before you change your diet or the dose of your diabetic medicine.
If you are going to have surgery, tell your prescriber or health care professional that you are taking acebutolol.
What side effects may I notice from taking acebutolol?
Side effects that you should report to your prescriber or health care professional as soon as possible:
• changes in vision
• chest pain
• cold, tingling, or numb hands or feet
• confusion
• difficulty breathing, wheezing
• dizziness or fainting spells
• irregular heartbeat
• muscle aches and pains
• skin rash
• slow heart rate (less than recommended by your prescriber or health care professional)
• sweating
• swollen legs or ankles
• tremor, shakes
• vomiting
Side effects that usually do not require medical attention (report to your prescriber or health care professional if they continue or are bothersome):
• anxiety
• depression, nightmares
• diarrhea
• difficulty sleeping
• dry itching skin
• dry or burning eyes
• headache
• nausea
• unusual tiredness
Where can I keep my medicine?
Keep out of the reach of children in a container that small children cannot open.
Store at room temperature between 15 and 30 degrees C (59 and 86 degrees F). Throw away any unused medicine after the expiration date.
