Nadolol

2024 Author: Rachel Wainwright | [email protected]. Last modified: 2023-12-15 07:39

Nadolol: instructions for use and reviews

1. Release form and composition
2. Pharmacological properties
3. Indications for use
4. Contraindications
5. Method of application and dosage
6. Side effects
7. Overdose
8. Special instructions
9. Application during pregnancy and lactation
10. Use in childhood
11. In case of impaired renal function
12. For violations of liver function
13. Use in the elderly
14. Drug interactions
15. Analogs
16. Terms and conditions of storage
17. Terms of dispensing from pharmacies
18. Reviews
19. Chain of pharmacies

Latin name: Nadolol

ATX code: C07AA12

Active ingredient: nadolol (Nadololum)

Manufacturer: Sanofi (France)

Description and photo update: 2019-10-07

Nadolol is a beta-blocker.

Release form and composition

Dosage form - tablets (10 pcs. In blisters and 100 pcs. In vials, in a cardboard box 3 blisters or 1 bottle and instructions for use of Nadolol).

The active substance of the drug is nadolol: in 1 tablet - 20, 40, 80, 120 or 160 mg.

Pharmacological properties

Pharmacodynamics

Nadolol is a non-selective beta-blocker that has antianginal, antiarrhythmic and antihypertensive effects, does not have sympathomimetic activity.

By blocking β-adrenergic receptors of the heart (of which 75% are β ₁ -adrenergic receptors, 25% are β ₂ -adrenergic receptors), the drug reduces the formation of cyclic adenosine monophosphate (cAMP) from adenosine triphosphate (ATP) stimulated by catecholamines, as a result of which the intracellular current of calcium ions decreases.

It has a negative batmo-, dromo-, chrono- and inotropic effect: it slows down the heart rate (HR), reduces myocardial contractility, inhibits excitability and conductivity. In the first 24 hours after taking the drug, due to a reciprocal increase in the activity of α-adrenergic receptors and elimination of stimulation of β ₂ -adrenergic receptors, an increase in the volume of peripheral vascular resistance (OPSR) is noted, however, after 1-3 days this indicator returns to the initial one, and with prolonged use of nadolol decreases.

The antianginal effect develops due to a decrease in myocardial oxygen demand against the background of a decrease in heart rate and a decrease in contractility. Also, a decrease in heart rate causes an improvement in myocardial perfusion and an increase in diastole. An increase in left ventricular end-diastolic pressure and an increase in ventricular muscle fiber stretching may increase oxygen demand, especially in patients with chronic heart failure.

The antiarrhythmic effect is explained by the ability of nadolol to inhibit some arrhythmogenic factors, such as high blood pressure (BP), tachycardia, cAMP (which plays an important role in the occurrence of ventricular fibrillation in myocardial ischemia), increased activity of the sympathetic nervous system (in ventricular tachyarrhythmia and myocardial infarction). Nadolol reduces the rate of spontaneous excitation of sinus and ectopic pacemakers. Suppresses the conduction of the impulse in the antegrade direction (to a lesser extent - in the retrograde) through the atrioventricular node (AV node), practically without affecting the conduction along the additional pathways.

The hypotensive effect is due to a decrease in the minute blood volume and sympathetic stimulation of peripheral vessels, a decrease in the activity of the renin-angiotensin-aldosterone system (RAAS) (important in patients with initial renin hypersecretion), restoration of the sensitivity of the aortic arch baroreceptors (their activity does not increase in response to a decrease in AD), as well as the effect on the central nervous system.

The drug also restores the sensitivity of the baroreceptor depressor reflex.

Blockade of presynaptic β ₂ -adrenoreceptors causes a decrease in the release of norepinephrine from the endings of sympathetic fibers and a decrease in adrenergic innervation of blood vessels.

Nadolol increases the concentration of thyroglobulin (TG) and low-density lipoprotein (LDL), lowers the concentration of high-density lipoprotein (HDL) in blood plasma.

Pharmacokinetics

After oral administration, nadolol is poorly and unevenly absorbed from the gastrointestinal tract (about 30%). The maximum plasma concentration (C _max) is reached within 3-4 hours, the equilibrium concentration in the blood is established after 6-9 days of regular use of the drug.

Binds to plasma proteins 4–30% of the dose. The drug is characterized by low fat solubility. It penetrates poorly through the blood-brain and placental barriers. Excreted in breast milk.

Undergoes minimal biotransformation in the liver. It is excreted unchanged mainly by the kidneys (70–90%), to a lesser extent - with bile. The half-life (T _½) is 20-24 hours and may increase in patients with renal insufficiency. After a single dose, it is completely excreted after 4 days.

Nadolol is removed from the body by hemodialysis.

Indications for use

arterial hypertension;
angina pectoris;
hyperkinetic cardiac syndrome;
cardiac ischemia;
rhythm disturbances (supraventricular tachycardia, paroxysmal atrial tachycardia, sinus tachycardia, supraventricular extrasystole);
secondary prevention of myocardial infarction (with a clinically stable patient's condition);
heart rate control with atrial fibrillation or flutter;
control of arrhythmia in pheochromocytoma (in combination with alpha-blockers), congenital syndrome of prolonged QT interval, mitral valve prolapse, myocardial infarction without signs of heart failure and thyrotoxicosis;
tremor;
prevention of migraine.

Contraindications

Absolute:

decompensated chronic heart failure or acute heart failure;
Prinzmetal's angina;
arterial hypotension (systolic blood pressure <90 mm Hg, especially with myocardial infarction);
sick sinus syndrome;
atrioventricular block II – III degree;
sinoatrial blockade;
cardiogenic shock;
cardiomegaly (no signs of heart failure);
bradycardia (heart rate <40 beats per minute);
Raynaud's disease and peripheral vascular occlusive disease, complicated by intermittent claudication, pain at rest or gangrene;
severe bronchial asthma;
diabetes;
severe renal and / or liver dysfunction;
simultaneous administration of monoamine oxidase inhibitors (MAO);
period of pregnancy and lactation;
hypersensitivity to the drug.

Relative (Nadolol should be used with extreme caution):

compensated chronic heart failure;
low fraction of the left ventricle on echocardiogram;
renal / hepatic impairment;
thyrotoxicosis;
myasthenia gravis;
pheochromocytoma;
depression (current or history);
psoriasis;
a history of allergic reactions;
children and old age.

Nadolol, instructions for use: method and dosage

Nadolol tablets should be taken orally, regardless of meals.

Recommended dosage regimens:

arrhythmia: 40 mg once a day, if necessary, at intervals of 7 days, the dose is gradually increased to the optimal therapeutic, the maximum daily dose is 160 mg;
angina pectoris: 40 mg 1 time per day, then at intervals of 7 days the dose is gradually increased to the optimal therapeutic 120–160 mg, the maximum daily dose is 240 mg;
arterial hypertension: initial dose - 80 mg once a day, then, if necessary, observing 7-day intervals, the dose is gradually increased to the optimal therapeutic 160 mg, the maximum daily dose is 240 mg;
migraine: the initial dose is 40 mg once a day, then, if necessary, observing 7-day intervals, the dose is gradually increased to 80–160 mg;
hyperthyroidism: depending on the clinical response, the daily dose may be 80–160 mg.

In case of impaired renal function, depending on creatinine clearance (CC), the intervals between doses of the drug should be:

CC 50 ml / min - 20 h;
CC 31–49 ml / min - 24–36 h;
CC 11-30 ml / min - 24-48 h;
CC 10 ml / min - 40-60 h.

Side effects

on the part of the cardiovascular system: weakening of myocardial contractility, arrhythmias, impaired myocardial conduction, palpitations, sinus bradycardia, decreased blood pressure, chest pain, orthostatic hypotension, manifestation of angiospasm (cooling of the lower extremities, increased disturbance of peripheral circulation, Raynaud's syndrome), development / worsening of chronic heart failure (shortness of breath, swelling of the ankles and feet), AV block until the development of complete transverse blockade and cardiac arrest;
from the respiratory system: nasal congestion, laryngospasm, difficulty breathing, bronchospasm;
from the central and peripheral nervous system: asthenic syndrome, dizziness, increased fatigue, nightmares, drowsiness, headache, insomnia, anxiety, weakness, short-term memory loss, hallucinations, confusion, depression, paresthesia in the extremities, muscle weakness, tremor;
from the digestive system: changes in taste, dryness of the oral mucosa, diarrhea, constipation, abdominal pain, nausea, vomiting, changes in the activity of liver enzymes and bilirubin levels, liver dysfunction (cholestasis, dark urine, yellowness of the skin or sclera);
from the hematopoietic system: leukopenia, agranulocytosis, thrombocytopenia (unusual bleeding and hemorrhage);
from the endocrine system: hypothyroidism, hypoglycemia (in patients receiving insulin) or hyperglycemia (in patients with non-insulin dependent diabetes mellitus);
on the part of the organ of vision: decreased secretion of lacrimal fluid, soreness and dryness of the eyes, blurred vision, conjunctivitis;
dermatological and allergic reactions: rash, urticaria, itching, flushing of the skin, exacerbation of psoriasis symptoms, psoriasis-like skin reactions, exanthema, increased sweating;
others: withdrawal syndrome (increased blood pressure, increased angina attacks), arthralgia, back pain, decreased potency, weakened libido.

Overdose

When taking an excessive dose of nadolol, the following symptoms may occur: arterial hypotension, dizziness, arrhythmia, bradycardia, acrocyanosis, difficulty breathing, heart failure. In severe cases, collapse is possible.

To remove the drug from the body, hemodialysis is performed. Depending on the clinical picture, the following drugs may be prescribed: atropine (0.25-1 mg intravenously), beta-adrenomimetics (isoprenaline), diuretics, cardiotonics (cardiac glycosides, dopamine, dobutamine, epinephrine, norepinephrine), tranquilizers (lorazepam, diazepam) and other symptomatic agents.

special instructions

In order to avoid the development of a withdrawal syndrome with prolonged treatment, you should stop taking Nadolol gradually - for at least 2 weeks, under close medical supervision.

For patients with pheochromocytoma, the drug can be prescribed only after preliminary treatment with alpha-blockers.

If necessary, surgical intervention (including dental) with the use of general anesthesia, Nadolol should be canceled a few days before its implementation. If this is not possible, the anesthesiologist should be warned about taking the drug so that he selects the anesthetic with the least negative inotropic effect.

In case of preparation of the patient for partial thyroidectomy during the previous 10 days, potassium iodide is prescribed simultaneously with the drug Nadolol.

The drug may interfere with the results of some laboratory tests.

Nadolol has the ability to mask some signs of hypoglycemia (changes in blood pressure and the development of tachycardia) and hyperthyroidism (the appearance of tachycardia).

In patients with a burdened allergic history and in patients receiving immunotherapy or allergen extracts for skin tests, Nadolol may increase the severity and duration of anaphylactic reactions to allergens, as well as neutralize the effect of conventional doses of epinephrine. In this regard, it is recommended to replace Nadolol with another drug of this pharmacological group.

Influence on the ability to drive vehicles and complex mechanisms

Nadolol in some cases causes disturbances from the central nervous system (including muscle weakness, dizziness, drowsiness, hallucinations), therefore, during the treatment period, it is recommended to refrain from potentially dangerous work and driving.

Application during pregnancy and lactation

During trials of nadolol in rabbits at a dose that was 10 times higher than the maximum recommended for humans, the drug demonstrated embryotoxic and fetotoxic properties. These effects were absent in rats and hamsters. It has been suggested that nadolol used during pregnancy can cause intrauterine growth retardation, hypoglycemia and bradycardia in the fetus. In this regard, the administration of the drug is contraindicated for pregnant women.

It has been established that nadolol penetrates into the mother's milk at a concentration exceeding the plasma concentration. In studies in 12 lactating women who received the drug for 5 days at a daily dose of 80 mg, the average concentration of nadolol in milk 24 hours after taking the last dose was 357 ng / ml, while the plasma concentration was 77 ng / ml. It has been calculated that a child weighing 5 kg receives from 2 to 7% of the equivalent adult dose through milk. Although the development of side effects and complications has not been recorded, the administration of the drug is contraindicated during lactation.

Pediatric use

The safety and efficacy of Nadolol in children and adolescents under 18 years of age have not been established, therefore the drug is not recommended for this age group of patients.

With impaired renal function

severe functional disorders of the kidneys: the drug is contraindicated;
mild to moderate disturbances: Caution required.

For violations of liver function

severe functional disorders of the liver: the drug is contraindicated;
mild to moderate disturbances: Caution required.

Use in the elderly

In elderly patients, the drug Nadolol should be used with caution, dosage adjustment may be required.

Drug interactions

Nadolol is contraindicated for use in conjunction with MAO inhibitors.

Particular care should be taken with the simultaneous administration of psychotropic drugs.

Arterial hypotension can be potentiated by peripheral vasodilators, sympatholytics, diuretics, dihydropyridine calcium antagonists; weaken - isoprenaline and epinephrine.

With the simultaneous use of quinidine drugs, general anesthetics, diltiazem and amiodarone increase the likelihood of violations of automatism, contractility and conduction of the heart.

In case of cancellation of clonidine against the background of ongoing therapy with nadolol, there is a risk of sudden development of severe arterial hypertension. Presumably, this is associated with an increase in the circulating blood content of catecholamines and with an increase in their vasoconstrictor action.

Cases of severe arterial hypotension with the simultaneous use of sodium amidotrizoate have been described.

Nadolol can block the positive inotropic effect of theophylline, as well as enhance the effects (including toxic) of lidocaine, which is apparently due to a slowdown in its metabolism in the liver.

Erythromycin is able to increase the concentration of nadolol in the blood plasma.

Fenelzine increases the risk of bradycardia, neostigmine - arterial hypotension and bradycardia, theophylline - bronchospasm in patients with obstructive chronic pulmonary disease and bronchial asthma.

Nadolol, when used in conjunction with allergen extracts for skin tests or allergens used for immunotherapy, increases the risk of anaphylaxis or severe systemic allergic reactions.

Analogs

Nadolol's analogues are: Korgard, Atenolol, Betacard, Tenormin, Betak, Lokren, Biprol, Concor, Betalok, Bisoprolol, Egilok, Nebivolol, Xonef, Visken, Obzidan, Prinorm, Atenova, Metoprolol, Sotalex, Timolol, Celivipre dr.

Terms and conditions of storage

Store at room temperature in a dark place out of reach of children.

Expiration date - see the package.

Terms of dispensing from pharmacies

Dispensed by prescription.

Reviews about Nadolol

There are practically no reviews about Nadolol on medical forums and specialized sites. There are rare reports in which patients confirm the effectiveness of this drug in diseases of the cardiovascular system, but complain about its unavailability in pharmacy chains.

Price at Nadolol pharmacies

The price of Nadolol is currently unknown due to the lack of the drug in pharmacies. The cost of an analogue of Korgard for a pack of 28 tablets of 80 mg is approximately 1950 rubles.

Maria Kulkes Medical journalist About the author

Education: First Moscow State Medical University named after I. M. Sechenov, specialty "General Medicine".

Information about the drug is generalized, provided for informational purposes only and does not replace the official instructions. Self-medication is hazardous to health!