Nadolol chemical structure
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Corgard

Nadolol (Corgard) is a non-selective beta-blocker used in the treatment of high blood pressure and chest pain. more...

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Chemistry and pharmacokinetics

Nadolol is nonpolar and hydrophobic, with low lipid solubility. Its half-life is 14-24 hours.

Mechanism of action

Nadolol non-selectively blocks beta-1 adrenergic receptors mainly in the heart, inhibiting the effects of the catecholamines epinephrine and norepinephrine and decreasing heart rate and blood pressure. It also blocks beta-2 adrenergic receptors located in bronchiole smooth muscle, causing vasoconstriction. By binding beta-2 receptors in the juxtaglomerular apparatus, nadolol inhibits the production of renin, thereby inhibiting angiotensin II and aldosterone production. Nadolol therefore inhibits the vasoconstriction and water retention due to angiotensin II and aldosterone, respectively.

The drug impairs AV node conduction and decreases sinus rate.

Nadolol may also increase plasma triglycerides and decrease HDL-cholesterol levels.

Indications

Nadolol is indicated for treatment of moderate hypertension and chest pain. In patients with severe hypertension, nadolol can also treat reflex tachycardia due to treatment with vasodilators.

Contraindications

Patients whose heart rate is largely mediated by the sympathetic nervous system (e.g. patients with congestive heart failure or myocardial infarct) should avoid nadolol as it inhibits sympathetic function. Nadolol is also contraindicated in patients with bradycardia (slow heart rate) because of its vasodilatory effects and tendency to cause bradycardia.

Because of its beta-2 activity, nadolol causes pulmonary vasoconstriction and should be avoided in asthma patients in preference of a beta-1 blocker.

As nadolol, like other beta-2 blockers, inhibits the release of insulin in response to hypoglycemia, it slows patients' recovery from acute hypoglycemic episodes and should be avoided in some patients with diabetes mellitus. In patients with insulin-dependent diabetes, a selective beta-1 blocker is preferred over non-selective blockers.

Side effects

  • Bradycardia
  • Fatigue
  • Bronchospasms

Read more at Wikipedia.org


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Beta blockers
From Gale Encyclopedia of Medicine, 4/6/01 by Nancy Ross-Flanigan

Definition

Beta blockers are medicines that affect the body's response to certain nerve impulses. This, in turn, decreases the force and rate of the heart's contractions, which lowers blood pressure and reduces the heart's demand for oxygen.

Purpose

The main use of beta blockers is to treat high blood pressure. Some also are used to relieve the type of chest pain called angina or to prevent heart attacks in people who already have had one heart attack. These drugs may also be prescribed for other conditions, such as migraine, tremors, and irregular heartbeat. In eye drop form, they are used to treat certain kinds of glaucoma.

Description

Beta blockers, also known as beta-adrenergic blockers, are available only with a physician's prescription. The come in capsule, tablet, liquid, and injectable forms. Some common beta blockers are atenolol (Tenormin), metoprolol (Lopressor), nadolol (Corgard), propranolol (Inderal), and timolol (Blocadren). Timolol and certain other beta blockers are also sold in eye drop form for treating glaucoma. Eye drops that contain beta blockers include betaxolol (Betoptic), cartelol (Ocupress), and timolol (Timoptic).

Recommended dosage

The recommended dosage depends on the type, strength, and form of beta blocker and the condition for which it is prescribed. Check with the physician who prescribed the drug or the pharmacist who filled the prescription for the correct dosage.

This medicine may take several weeks to noticeably lower blood pressure. Taking it exactly as directed is important.

Do not stop taking this medicine without checking with the physician who prescribed it. Some conditions may get worse when patients stop taking beta blockers abruptly. This may also increase the risk of heart attack in some people. Because of these possible effects, it is important to keep enough medicine on hand to get through weekends, holidays, and vacations.

Physicians may recommend that patients check their pulse before and after taking this medicine. If the pulse becomes too slow, circulation problems may result.

Precautions

Seeing a physician regularly while taking beta blockers is important. The physician will check to make sure the medicine is working as it should and will watch for unwanted side effects. People who have high blood pressure often feel perfectly fine. However, they should continue to see their physicians even when they feel well so that the physician can keep a close watch on their condition. Patients also need to keep taking their medicine even when they feel fine.

Beta blockers will not cure high blood pressure, but will help control the condition. To avoid the serious health problems that high blood pressure can cause, patients may have to take medicine for the rest of their lives. Furthermore, medicine alone may not be enough. Patients with high blood pressure may also need to avoid certain foods and keep their weight under control. The health care professional who is treating the condition can offer advice on what measures may be necessary. Patients being treated for high blood pressure should not change their diets without consulting their physicians.

Anyone taking beta blockers for high blood pressure should not take any other prescription or over-the-counter medicine without first checking with his or her physician. Some medicines may increase blood pressure.

Anyone who is taking beta blockers should be sure to tell the health care professional in charge before having any surgical or dental procedures or receiving emergency treatment.

Some beta blockers may change the results of certain medical tests. Before having medical tests, anyone taking this medicine should alert the health care professional in charge.

Some people feel drowsy, dizzy, or lightheaded when taking beta blockers. Anyone who takes these drugs should not drive, use machines or do anything else that might be dangerous until they have found out how the drugs affect them.

Beta blockers may increase sensitivity to cold, especially in older people or people who have poor circulation. Anyone who takes this medicine should dress warmly in cold weather and should be careful not to be exposed to the cold for too long.

People who usually have chest pain when they exercise or exert themselves may not have the pain when they are taking beta blockers. This could lead them to be more active than they should be. Anyone taking this medicine should ask his or her physician how much exercise and activity is safe.

Older people may be unusually sensitive to the effects of beta blockers. This may increase the chance of side effects.

Physicians may advise people taking beta blockers to wear or carry medical identification indicating that they are taking this medicine.

Special conditions

People who have certain medical conditions or who are taking certain other medicines may have problems if they take beta blockers. Before taking these drugs, be sure to let the physician know about any of these conditions:

Allergies

Anyone who has had unusual reactions to beta blockers in the past should let his or her physician know before taking the drugs again. The physician should also be told about any allergies to insect stings, medicines, foods, dyes, preservatives, or other substances. In people with allergies to medicines, foods, or insect stings, beta blockers may make the allergic reactions more severe and harder to treat. Anyone who has an allergic reaction while taking beta blockers should get medical attention right away and should make sure the physician in charge knows that he or she is taking this medicine.

Beta blockers may also cause serious reactions in people who take allergy shots. Anyone taking this medicine should be sure to alert the physician before having any allergy shots.

Diabetes

Beta blockers may make blood sugar levels rise and may hide some symptoms of low blood sugar. Diabetic patients should discuss these possible problems with their physicians.

Pregnancy

Some studies of beta blockers show that these drugs cause problems in newborns whose mothers use them during pregnancy. Other studies do not show such effects. Women who are pregnant or who may become pregnant should check with their physicians about the use of beta blockers.

Breastfeeding

Some beta blockers pass into breast milk and may cause breathing problems, slow heartbeat, and low blood pressure in nursing babies whose mothers take the drugs. Women who need to take beta blockers and who want to breastfeed their babies should check with their physicians.

Other medical conditions

Beta blockers may increase breathing problems or make allergic reactions more severe in people who have allergies, bronchitis, or emphysema.

In people with an overactive thyroid, stopping beta blockers suddenly may cause an increase in symptoms. Also, taking this medicine may hide a fast heartbeat, which is one of the symptoms of overactive thyroid.

Effects of these drugs may be greater in people with kidney or liver disease because the medicine is cleared from the body more slowly.

Beta blockers may also make the following medical conditions worse:

  • Heart or blood vessel disease
  • Unusually slow heartbeat (bradycardia)
  • Myasthenia gravis (chronic disease causing muscle weakness and possibly paralysis)
  • Psoriasis (itchy, scaly, red patches of skin)
  • Depression (now, or in the past).

Before using beta blockers, people with any of the medical problems listed in this section should make sure their physicians are aware of their conditions.

Use of certain medicines

Taking beta blockers with certain other drugs may affect the way the drugs work or may increase the chance of side effects.

Side effects

The most common side effects are dizziness, drowsiness, lightheadedness, sleep problems, unusual tiredness or weakness, and decreased sexual ability. In men, this can occur as impotence or delayed ejaculation. These problems usually go away as the body adjusts to the drug and do not require medical treatment unless they persist or they interfere with normal activities.

More serious side effects are possible. If any of the following side effects occur, check with the physician who prescribed the medicine as soon as possible:

  • Breathing problems
  • Slow heartbeat
  • Cold hands and feet
  • Swollen ankles, feet, or lower legs.
  • Mental depression.

Other side effects may occur. Anyone who has unusual symptoms after taking beta blockers should get in touch with his or her physician.

Interactions

Beta blockers may interact with a number of other medicines. When this happens, the effects of one or both of the drugs may change or the risk of side effects may be greater. Anyone who takes beta blockers should let the physician know all other medicines he or she is taking. Among the drugs that may interact with beta blockers are:

  • Calcium channel blockers and other blood pressure drugs. Using these drugs with beta blockers may cause unwanted effects on the heart.
  • Insulin and diabetes medicines taken by mouth. Beta blockers cause high blood sugar or hide the symptoms of low blood sugar.
  • Monoamine oxidase inhibitors (MAO) such as phenelzine (Nardil) or tranylcypromine (Parnate), used to treat conditions including depression and Parkinson's disease. Taking beta blockers at the same time or within two weeks of taking MAO inhibitors may cause severe high blood pressure.
  • Airway-opening drugs (bronchodilators) such as aminophylline (Somophyllin), dyphylline (Lufyllin) oxtriphylline (Choledyl), or theophylline (Somophyllin-T). When combined with beta blockers, the effects of both the beta blockers and the airway-opening drugs may be lessened.
  • Cocaine. High blood pressure, fast heartbeat, and heart problems are possible when cocaine and beta blockers are combined. Also, cocaine may interfere with the effects of beta blockers.
  • Allergy shots or allergy skin tests. Beta blockers may increase the chance of serious reactions to these medicines.

The list above may not include every drug that interacts with beta blockers. Be sure to check with a physician or pharmacist before combining beta blockers with any other prescription or nonprescription (over-the-counter) medicine.

Key Terms

Angina pectoris
A feeling of tightness, heaviness, or pain in the chest, caused by a lack of oxygen in the muscular wall of the heart.
Glaucoma
A condition in which pressure in the eye is abnormally high. If not treated, glaucoma may lead to blindness.
Migraine
A throbbing headache that usually affects only one side of the head. Nausea, vomiting, increased sensitivity to light, and other symptoms often accompany migraine.

Further Reading

Gale Encyclopedia of Medicine. Gale Research, 1999.

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