Clinical and pharmacological group: & nbsp

Beta-blockers

Included in the formulation
АТХ:

C.07.A.A.12   Nadolol

Pharmacodynamics:

Competitive reversible blockade of β1- and β2-adrenergic receptors.Blockade of β1-adrenergic receptors of the heart leads to a decrease in heart rate and heart rate, a decrease in cardiac output and a decrease in systolic pressure; blockade of β1-adrenergic receptors of the juxtaglomerular renal apparatus causes a decrease in renin release and a decrease in the activity of the renin-angiotensin-aldosterone system; a decrease in vasoconstrictor action of angiotensin II causes the dilatation of blood vessels, a decrease in the overall peripheral vascular resistance and diastolic pressure; the use of β-adrenoblockers restores the sensitivity of the baroreceptor depressor reflex.

In addition, the blockade of presynaptic β2-adrenoreceptors leads to a decrease in the release of norepinephrine from the endings of sympathetic fibers and a decrease in the adrenergic innervation of blood vessels. In addition to this, propranolol has a depressing effect on the central nervous system.

Pharmacokinetics:

Bioavailability is 30%. Relationship with plasma proteins 4-30%. Low solubility in fats is characteristic. Poorly passes through the blood-brain and placental barrier.Biotransformation in the liver (minimal). Half-life 20-24 hours Elimination by the kidneys (90-70% unchanged). Removed during hemodialysis.

Indications:

Ischemic heart disease, angina pectoris, myocardial infarction (secondary prevention), arterial hypertensionHyperkinetic cardiac syndrome, arrhythmias (sinus tachycardia, paroxysmal atrial tachycardia, supraventricular arrhythmias, supraventricular tachycardia), tremor, migraine (prevention), the control heart rate during blink or atrial flutter), arrhythmias with pheochromocytoma (in combination with alpha-blockers ), mitral valve prolapse, congenital syndrome of prolonged QT interval, myocardial infarction without signs of heart failure, thyrotoxicosis.

VI.G40-G47.G43.1   Migraine with aura [classic migraine]

VI.G40-G47.G43.0   Migraine without aura [simple migraine]

VI.G40-G47.G43.9   Migraine, unspecified

VI.G40-G47.G43.8   Another migraine

VI.G40-G47.G43.3   Complicated migraine

VI.G40-G47.G43   Migraine

IX.I20-I25.I20.90   Angina pectoris unspecified with hypertension

IX.I20-I25.I20.9   Angina pectoris, unspecified

IX.I20-I25.I20.80   Other forms of angina with hypertension

IX.I20-I25.I20.8   Other forms of angina pectoris

IX.I20-I25.I20.10   Angina with documented spasm with hypertension

IX.I20-I25.I20.1   Angina with documented spasm

IX.I20-I25.I20.00   Unstable angina with hypertension

IX.I20-I25.I20   Angina pectoris [angina pectoris]

IX.I10-I15.I10   Essential [primary] hypertension

IX.I30-I52.I48   Atrial fibrillation and flutter

IX.I20-I25.I21   Acute myocardial infarction

Contraindications:

Hypersensitivity, acute heart failure or decompensated chronic heart failure, cardiogenic shock, atrioventricular blockade of II-III degrees, sinoatrial block, sinus node weakness syndrome, bradycardia (heart rate less than 40 per minute), prinzmetal angina, cardiomegaly (no signs of heart failure), arterial hypotension (systolic pressure less than 90 mm Hg, especially with myocardial infarction); severe course of bronchial asthma; Occlusal diseases of peripheral vessels complicated by gangrene, intermittent claudication or restless pain; diabetes, simultaneous administration of MAO inhibitors, breast-feeding.

Carefully:

Low fraction of the left ventricle by echocardiogram, allergic reactions in the history, chronic heart failure, pheochromocytoma,liver failure, chronic renal failure, myasthenia gravis, thyrotoxicosis, depression (including history), psoriasis, pregnancy, advanced age, children's age (efficacy and safety not established).

Pregnancy and lactation:

Category FDA FROM.

Embryotoxic and fetotoxic when administered to rabbits at a dose of ten maximum recommended doses for humans. These effects are absent in hamsters and rats. Penetrates into breast milk in a concentration exceeding the plasma one. In the application of nadolol in a dose of 80 mg per day for 5 days in 12 lactating women, the average concentration of the drug in milk after 24 hours after the last dose was 357 ng / ml, in plasma - only 77 ng / ml. It was estimated that a child with a body weight of 5 kg receives milk with a 2-7% equivalent dose for an adult. Complications in children are not registered. Contraindicated in pregnancy and lactation.

Dosing and Administration:

Inside, regardless of food intake. With angina, arrhythmia, migraine - 40 mg once a day, if necessary, increase the dose (1 time per week) with angina pectoris to 120-160 mg per day, arrhythmia to 160 mg per day and migraine to 80-160 mg per day. When arterial hypertension - 80-240 mg, once. When hyperthyroidism - 80-160 mg per day. If the renal function is impaired, the interval between doses during creatinine clearance 50 ml / min should be 20 h, 31-50 ml / min 24-36 h, 10-30 ml / min 24-48 h, 10 ml / min 40- 60 hours

Side effects:

From the central nervous system and peripheral nervous system: increased fatigue, weakness, dizziness, headache, drowsiness, insomnia, nightmares, depression, anxiety, confusion, short-term memory loss, hallucinations, asthenic syndrome, muscle weakness, paresthesia in the extremities, tremor.

From the side of the organ of vision: blurred vision, a decrease in the secretion of tear fluid, dryness and soreness of the eyes, conjunctivitis.

From the cardiovascular system: sinus bradycardia, palpitations, myocardial conduction disturbance, atrioventricular block (up to the development of complete transverse blockade and cardiac arrest), arrhythmias, weakening of myocardial contractility, development of chronic heart failure (swelling of the ankles, stop, dyspnea ), decreased blood pressure, orthostatic hypotension, manifestation of angiospasm (increased peripheral circulatory disturbance, lower extremities cooling, Raynaud's syndrome), chest pain.

On the part of the digestive system: dryness of the oral mucosa, nausea, vomiting, abdominal pain, diarrhea, constipation, impaired liver function (dark urine, icteric sclera or skin, cholestasis), changes in taste; change in the activity of enzymes, the level of bilirubin.

On the part of the respiratory system: nasal congestion, difficulty breathing, laryngo- and bronchospasm.

From the endocrine system: hyperglycemia (in patients with insulin-dependent diabetes mellitus), hypoglycemia (in patients receiving insulin), hypothyroid status.

From the hemopoietic system: thrombocytopenia (unusual bleeding and hemorrhage), agranulocytosis, leukopenia.

Allergic reactions: itching, rash, hives.

Dermatological reactions: increased sweating, skin hyperemia, exanthema, psoriasis-like skin reactions, exacerbation of psoriasis symptoms.

Others: back pain, arthralgia, weakening of libido, decreased potency, withdrawal syndrome (increased angina attacks, increased blood pressure).

Overdose:

Symptoms: dizziness, bradycardia, arrhythmia, hypotension, difficulty breathing, acrocyanosis, heart failure, in severe cases - collapse.

Treatment: hemodialysis, the introduction of atropine (intravenously 0.25-1 mg), beta-adrenomimetics (isoprenaline), tranquilizers (diazepam, lorazepam), cardiotonic (dobutamine, dopamine, epinephrine, norepinephrine, cardiac glycosides), diuretics and other symptomatic agents.

Interaction:

It should not be used simultaneously with MAO inhibitors. Dihydropyridine calcium antagonists, sympatholytics, peripheral vasodilators, diuretics potentiate hypotension; epinephrine and isoprenaline - weaken. The probability of violations of automatism, conduction and contractility of the heart increases against amiodarone, diltiazem, verapamil, quinidine drugs and general anesthetics.

Allergens used for immunotherapy, or allergen extracts for skin tests increase the risk of severe systemic allergic reactions or anaphylaxis.

Special instructions:

During the treatment, it is possible to change the test results when carrying out laboratory tests.

During the treatment period it is necessary to refrain from driving motor vehicles and practicing potentially dangerous activities,requiring increased concentration of attention and speed of psychomotor reactions.

Instructions
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