Atenolol: release form, indications and contraindications, dosage and drug reviews

Atenolol is a drug with an active substance belonging to the group of beta1-adrenergic receptor blockers (often referred to as beta-blockers).

Beta blockers are used primarily in the treatment of cardiovascular disease.

Introduced in 1976, Atenolol was developed as a replacement for Propranolol in the treatment of hypertension.

The active substance of the drug blocks beta1-adrenergic receptors, tiny areas, stimulation of which causes the expansion of the coronary arteries and an increase in the strength and frequency of the heart contractions (heart rate). As a result of the blockade of beta1-adrenergic receptors, the heart beats more slowly and with less force. The pressure of the blood in the blood vessels decreases and it is easier for the heart to pump blood. The need for myocardial oxygen decreases, while the activity of the heart improves.

Pharmacokinetics:

• Atenolol is rapidly and incompletely absorbed from the gastrointestinal tract (50-60%).
• Has the lowest lipid solubility within the class.
• Bioavailability: 46-60%.
• The onset of the hypotensive response: 3 hours after administration.
• Duration of action: 12-24 hours (with normal kidney function).
• Peak Plasma Concentration Time: 2-4 h
• Metabolized: to a limited extent in the liver.
• Metabolites: No clinically active metabolites.
• Half-life: in children, 4-6 hours; in adults 6-7 hours; in neonates <35 hours; end-stage kidney disease 15-35 hours.
• Excretion: feces (50%), urine (40-50%).
• Atenolol is excreted from the body during hemodialysis.

The drug has three types of effects:

1. antianginal (it is anti-ischemic, prevents an attack of angina pectoris);
2. antihypertensive (lowers high blood pressure - blood pressure);
3. antiarrhythmic (normalizes the heart rate).

Unlike Propranolol, Atenolol hardly passes through the blood-brain (between blood and nervous tissue) barrier, thereby reducing the frequency of negative "responses" from the central nervous system.

During the first days after taking atenolol orally, there is a reactive increase in the total peripheral vascular resistance. This effect gradually decreases over a period of one to three days.

Atenolol: release form, indications for use

There is no injection ampoule, cream, or ointment called Atenolol. Release form - tablets of 50 and 100 mg, the drug is intended for oral administration.

Atenolol Tablets Auxiliary Fillers: corn starch, pregelatinized corn starch, lactose monohydrate, povidone, sodium lauryl sulfate, colloidal anhydrous silicon dioxide, magnesium stearate.

There is also Atenolol in the form of "substance-powder" release in polyethylene two-layer sachets of 5, 10 and 25 kg. The manufacturer is the Indian company Kopran Limited.

Atenolol blocks beta-1 receptors that are present in the heart. This causes the heart to beat at a slower speed and with less force, and thus pumps less blood into the blood vessels. Thanks to Atenolol, blood pressure is reduced in patients with hypertension. Since the heart beats slower and with less force after taking Atenolol, it requires less energy. Thus, pain in angina pectoris is reduced, as well as the risk of a heart attack is reduced.

The indications for use of the drug Atenolol are represented by a number of diseases, including hypertension, angina pectoris, acute myocardial infarction, supraventricular tachycardia, ventricular tachycardia and symptoms of the syndrome alcohol withdrawal.

Beta blockers are effective in treating the physical (physical) effects of anxiety. In these cases, the medication is used sporadically instead of the regular daily intake.

Atenolol tablets: dosage and combined use with diuretics

If you are prescribed Atenolol tablets, the dosage and frequency of use will depend on: age, treatment conditions, severity of the condition, response to the first dose.

You can take Atenolol with or without food, but you should try to take the dose at the same time of day every day. The tablets are best swallowed with water.

When using the agent in the form of a powder substance, the standard dosage for an adult at the beginning of treatment is 25 mg orally once a day, then it can be increased to 50 mg.

1. Atenolol: dosage for hypertension for an adult (aged 18-64 years old): 50 mg once a day. If necessary, the dose is gradually adjusted.
   • Dosage for a child (aged 0-17 years old). The benefits of this medication have not been studied for children, and it should not be used to treat children under the age of 18.
   • Dosage for Seniors (Ages 65 and Over): There are no specific recommendations.
2. Atenolol: dosage for angina pectoris (chest pain) for an adult: 50 mg once a day. If necessary, the dose is gradually adjusted.
   • Child dosage: Not for use on persons under 18 years of age.
   • Dosage for the elderly: a lower dose may be required than for adults due to the longer half-life of the drug.
3. Atenolol: dosage for acute myocardial infarction and for the prevention of mortality after a heart attack for an adult: the dose is purely individual. Depends on the cause and effect of the heart attack. A cardiologist will monitor the patient's blood pressure. The drug is often prescribed during hospitalization. The most common dosage is 100 mg once daily or in 2 divided doses.
4. Atenolol: Dosage to prevent supraventricular premature beats for an adult: 50 mg per day, starting at 3 days before surgery and continue for up to 7 days after surgery. The dose can be increased up to 100 mg per day.
5. Atenolol: Dosage for the treatment of lithium-induced tremor in adults: Limited evidence suggests that a dose of 50 mg once daily may be effective. One of the reports described a case of a decrease in the amplitude and frequency of occurrence of lithium-induced tremor after treatment with Atenolol.
6. Atenolol: dosage for the treatment of atrial fibrillation or atrial flutter in adults: 25 to 100 mg daily.

Older people may need smaller doses of Atenolol tablets. First, because they may be more sensitive to the effects of the drug on the body. Secondly, because due to age, the drug is removed from the body more slowly. After a small first dose, you can then gradually increase the dose.

If a dose is missed, the next dose should be taken at the scheduled time. There is no need to double the dose. You can find out that Atenolol tablets work to lower blood pressure in hypertension or to reduce chest pain in angina pectoris.

Keeping Atenolol in the correct conditions is essential to its effectiveness. Store tablets at controlled room temperature: 20-25 ° C. The medicine should be kept in a tightly closed and lightfast container, away from moisture.

Because atenolol can lower blood pressure, the doctor may ask the patient to check their blood pressure periodically while taking the drug. It is necessary to notify the doctor if the pressure readings are either too high or too low when taking Atenolol.

High blood pressure - when the systolic (top number) is greater than 120 mmHg. Art. or diastolic (lower) is greater than 80 mm Hg. Art. Low blood pressure - when the systolic number is below 90 mmHg. Art or diastolic number below 60 mm Hg. Art.

Atenolol tablets during pregnancy and lactation are a category D drug:

1. Studies have shown that there is a risk of adverse effects on the fetus when the mother takes the drug.
2. The benefits of taking Atenolol during pregnancy may outweigh the potential risks in certain situations.

The use of Atenolol in the second trimester of pregnancy is associated with the birth of premature babies. In addition, newborns from mothers taking Atenolol at the time of birth may be at risk hypoglycemia (blood sugar levels below normal) and bradycardia (heartbeats slower than normal).

Atenolol passes into breast milk. Newborns who are breastfed by mothers taking Atenolol are at risk of developing hypoglycemia and bradycardia. However, children who are older than 3 months may not be at risk of the effects of Atenolol in breast milk.

The combination of atenolol with diuretics can lead to too much lowering of blood pressure. However, the combination of a β1-blocker and a diuretic may be prescribed by the attending physician to enhance the antihypertensive effect of both drugs.

In one of the studies SHEP (Systolic Hypertension in the Elderly Program) from 1993, almost 5 thousand subjects over 60 years old were divided into two groups. One took a combination of chlorthalidone and Atenolol tablets, the other a placebo. The observations were carried out for 4.5 years. Blood pressure decreased significantly more in the group receiving active antihypertensive therapy compared with the group receiving placebo. The combination of a β1-blocker and a diuretic has reduced the incidence of strokes, coronary artery bypass grafting and transluminal angioplasty. There was also a negative consequence of therapy: the risk of developing diabetes mellitus increased.

Medication Atenolol: interactions with other drugs, side effects and patient reviews

When taking beta-blockers (which include the drug Atenolol) and Verapamil together, or Diltiazem, bradycardia and heart block may occur, and an increase in diastolic pressure.

Beta blockers such as Atenolol may increase the risk, severity and / or duration of hypoglycemia in patients taking Glibenclamide and some other antidiabetic drugs.

In addition, beta blockers can mask some of the symptoms of hypoglycemia, such as tremors and heart palpitations, making it difficult to recognize an impending attack.

Other symptoms of hypoglycemia, such as headache, dizziness, drowsiness, nervousness, confusion, nausea, weakness, and sweating, do not occur.

Along with alpha agonists such as Ephedrine, the drug Atenolol can cause an excessive increase in blood pressure, while co-administration with alpha-blockers such as Prazosin can cause an excessive decrease in blood pressure.

Atenolol should be avoided when taking asthma medications because of the opposite effects on the bronchi.

NSAIDs such as Ibuprofen and Naproxen can block the effect of Atenolol on blood pressure.

It is not allowed to take the drug Atenolol together with anticholinesterase drugs used for Alzheimer's diseases such as Rivastigmine due to an additive effect on the heart and blood pressure.

Atenolol is absolutely contraindicated in patients with the following conditions:

• clinical depression;
• an allergic reaction to the drug;
• low heart rate (bradycardia);
• poor circulation due to heart failure;
• a tumor of the adrenal gland called pheochromocytoma;
• pregnancy;
• lactation.

The medicine Atenolol carries a high risk of developing type 2 diabetes.

Antihypertensive therapy with Atenolol provides a weaker protective effect against cardiovascular complications (eg, myocardial infarction and stroke) compared to others antihypertensive drugs. In some cases, diuretics are preferable.

You should immediately contact your attending cardiologist if any of these side effects appear while taking Atenolol:

Often:

• blurred vision;
• cold hands or feet;
• labored breathing;
• dizziness, faintness, or lightheadedness when lying or sitting;
• shortness of breath;
• sweating;
• tightness in the chest;
• unusual tiredness or weakness;
• wheezing in the chest.

Sometimes:

• anxiety;
• chest pain or discomfort;
• chills;
• cold sweat;
• cough;
• dizziness or lightheadedness;
• fainting;
• fast heartbeat;
• leg pain;
• noisy breathing;
• slow or irregular heartbeat;
• sudden shortness of breath.

Rarely:

• bloody urine;
• decreased frequency or amount of urine;
• high blood pressure;
• increased thirst;
• loss of appetite;
• pain in the side;
• nausea;
• swelling of the face, fingers, or lower extremities;
• vomit;
• weight gain;
• black, tarry stools;
• bleeding gums;
• blurred or lost vision;
• pain in the bones of the joints;
• impaired color perception;
• fever;
• halo around light sources;
• night blindness;
• pallor or cold feeling in the tips of the fingers and toes;
• red or purple spots on the skin;
• depressed mood or mental change;
• skin irritation or rash, including a rash that looks like psoriasis;
• tunnel vision;
• unusual bleeding or bruising.

Overdose symptoms are due to the excessive pharmacodynamic action of Atenolol on beta-receptors. These include bradycardia (slow heart rate), severe hypotension with shock, acute heart failure, hypoglycemia, and bronchospastic reactions.

Treatment is mostly symptomatic. Activated charcoal is beneficial for drug absorption in overdose. Atropine will counteract bradycardia, Glucagon helps with hypoglycemia, Dobutamine can help against hypotension, and inhalation of Hexoprenaline or Salbutamol helps with bronchospasm.

Analogs of the drug Atenolol with a similar active ingredient are the following tablets: Atenobene, Atenova, Atenol, Atenolan, Betacard, Velorin 100, Prinorm, Tenormin.

The price of Atenolol (100 mg) produced by the German company Nycomed is 55 rubles and more, depending on the pharmacy's markup. Atenolol (100 mg), produced by the Russian company "Sintez" is much cheaper - from 20 rubles and more.

In reviews of the drug Atenolol, its fast and long-term action is noted. It effectively normalizes heart rate and lowers blood pressure. Users praise the convenient plastic packaging that is convenient to take with them and the ease with which you can split the pill in half. The main disadvantage is the impossibility of using it in diabetes mellitus.