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Manufacturers: Isis Pharmaceuticals Inc.
Active ingredients
- Propranolol
Disease class
- Some infectious and parasitic diseases
- Thyrotoxicosis (hyperthyroidism)
- Migraine without aura [simple migraine]
- Autonomic nervous system disorders
- Essential [primary] hypertension
- Secondary hypertension
- Renovascular hypertension
- Angina [angina pectoris]
- Unstable angina
- Chronic ischemic heart disease
- Obstructive hypertrophic cardiomyopathy
- Heart rhythm disorder, unspecified
- Pain in the heart area
- Tremor, unspecified
- Cardiac glycosides and drugs with similar effects
Clinical and pharmacological group
- Not indicated. See instructions
Pharmacological action
- Antianginal
- Antiarrhythmic
- Hypotensive
Pharmacological group
- Beta blockers
Pharmacodynamics and pharmacokinetics
Pharmacodynamics
Non-selective beta-blocker with moderate antihypertensive, antianginal and antiarrhythmic effects. Indiscriminately blocks beta-adrenergic receptors , weakens catecholamine- biosynthesis of cAMP from ATP , after which it reduces the intracellular supply of calcium ions, has a negative dromotropic , bathmotropic , chronotropic and inotropic effect (reduces heartbeat, inhibits conductivity and excitability, reduces the ability of the myocardium to contract).
On the first day of using the drug, peripheral vascular resistance increases (as a result of an increase in the activity of alpha-adrenergic receptors and blocking of beta-2-adrenergic receptors in muscle vessels), but after two days its value returns to its original value, and with long-term administration it decreases.
The antihypertensive effect is associated with a decrease in cardiac output, a weakening of sympathetic stimulation of the vessels of peripheral organs, inhibition of the renin-angiotensin system , a decrease in the sensitivity of aortic arch pressure receptors and an effect on the nervous system. This antihypertensive effect is completely stabilized by the end of the second week of the course of administration of the drug.
The antianginal effect is caused by a decrease in the heart's oxygen demand (due to negative inotropic and chronotropic effects). A decrease in heart rate leads to prolongation of diastole and increased myocardial perfusion. As a result of increased diastolic pressure in the left side of the heart and increased stretching of the ventricular muscles, the need for oxygen and nutrients may increase, especially in patients suffering from heart failure .
The antiarrhythmic effect manifests itself as a result of blocking arrhythmogenic factors (excessive activity of the sympathetic system, tachycardia , increased levels of cAMP in tissues, arterial hypertension ), reducing the speed of spontaneous excitation of ectopic and sinus pacemakers and inhibition of AV conduction . Suppression of impulse conduction is recorded primarily in the forward direction and, to a lesser extent, in the reverse direction through the AV node and along additional pathways. Due to a decrease in the heart's oxygen demand, the severity of cardiac ischemia is weakened, and post-infarction mortality may decrease due to the antiarrhythmic effect .
The ability to prevent the occurrence of headaches of vascular etiology is caused by a decrease in the severity of enlargement of the cerebral arteries due to blocking of beta-adrenergic receptors of platelet adhesion and lipolysis caused by catecholamines adhesiveness , inhibition of activation of blood coagulation factors during the release of adrenaline , stimulation of oxygen transport into tissues and weakening of renin .
The decrease in the severity of tremor with the use of propranolol is due to the blocking of beta-2 adrenergic receptors.
The drug enhances the ability of the uterus to contract. Stimulates the tone of the bronchial walls.
Pharmacokinetics
After internal administration, up to 90% of the product is quickly absorbed. The maximum concentration in the blood occurs after an hour and a half. Bioavailability after a single dose reaches 40%, with long-term use it increases. The value of bioavailability depends on the nature of the meal and the intensity of liver perfusion.
The drug is highly lipophilic and accumulates in the kidneys, brain, lungs and heart. Penetrates through histohematic barriers and is excreted in breast milk. Reaction with blood proteins is 90-95%.
Transformed in the liver by glucuronidation. Then it enters the intestine with bile, where it is deglucuronidated and reabsorbed.
The half-life is four hours. Excreted in the urine in the form of metabolites (99%). Not evacuated during hemodialysis .
Obzidan
Monitoring of patients taking the drug should include monitoring heart rate and blood pressure (at the beginning of treatment - daily, then once every 3-4 months), ECG, blood glucose concentration in patients with diabetes (once every 4-5 months) . In elderly patients, it is recommended to monitor renal function (once every 4-5 months).
The patient should be taught how to calculate heart rate and instructed about the need for medical consultation if the heart rate is less than 50/min.
Before prescribing propranolol to patients with CHF (early stages), digitalis and/or diuretics should be used.
In smokers, the effectiveness of beta-blockers is lower.
Patients using contact lenses should take into account that during treatment the production of tear fluid may decrease.
Patients with pheochromocytoma are prescribed only after taking an alpha-blocker.
In thyrotoxicosis, propranolol may mask certain clinical signs of thyrotoxicosis (for example, tachycardia). Abrupt withdrawal in patients with thyrotoxicosis is contraindicated because it can increase symptoms.
When prescribing beta-blockers to patients receiving hypoglycemic drugs, caution should be exercised, since hypoglycemia may develop during long breaks in food intake. Moreover, its symptoms such as tachycardia or tremor will be masked due to the action of the drug. Patients should be instructed that the main symptom of hypoglycemia during treatment with beta-blockers is increased sweating.
When taking clonidine concomitantly, it can be discontinued only a few days after propranolol is discontinued.
It is possible that the severity of the hypersensitivity reaction may increase and the absence of effect from usual doses of epinephrine against the background of a burdened allergic history.
A few days before general anesthesia with chloroform or ether, you must stop taking the drug. If the patient took the drug before surgery, he should select a drug for general anesthesia with minimal negative inotropic effect.
Reciprocal activation of the n.vagus can be eliminated by intravenous administration of atropine (1-2 mg).
Drugs that reduce catecholamine reserves (for example, reserpine) can enhance the effect of beta-blockers, so patients taking such combinations of drugs should be under constant medical supervision to detect arterial hypotension or bradycardia.
Cannot be used simultaneously with antipsychotic drugs (neuroleptics) and anxiolytic drugs (tranquilizers).
Use with caution in combination with psychoactive drugs, such as MAO inhibitors, when taking them on a course for more than 2 weeks.
If elderly patients develop increasing bradycardia (less than 50/min), arterial hypotension (systolic blood pressure below 100 mm Hg), AV block, bronchospasm, ventricular arrhythmias, severe liver and kidney dysfunction, it is necessary to reduce the dose or stop treatment . It is recommended to discontinue therapy if depression caused by taking beta-blockers develops.
Treatment should not be abruptly interrupted due to the risk of developing severe arrhythmias and myocardial infarction. Cancellation is carried out gradually, reducing the dose over 2 weeks or more (by 25% in 3-4 days).
Use during pregnancy and lactation is possible if the benefit to the mother outweighs the risk of side effects in the fetus and child. If it is necessary to take it during pregnancy, carefully monitor the condition of the fetus; it should be discontinued 48-72 hours before birth.
Catecholamines, normetanephrine and vanillylmandelic acid should be discontinued before blood and urine tests; antinuclear antibody titers.
During the treatment period, care must be taken when driving vehicles and engaging in other potentially hazardous activities that require increased concentration and speed of psychomotor reactions.
Indications for use of Obzidan
The drug has the following indications for use:
- atrial fibrillation;
- angina pectoris of an unstable nature (excluding Prinzmetal angina );
- angina pectoris ;
- tachycardia of various etiologies;
- ventricular and supraventricular extrasystole ;
- arterial hypertension;
- prevention of myocardial infarction ;
- essential tremor;
- migraine (prevention of attacks);
- as a symptomatic treatment of thyrotoxicosis or thyrotoxic crisis (if intolerance to thyreostatic drugs is present);
- sympathoadrenal crises complicated by diencephalic syndrome.
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Contraindications
- sinoatrial block;
- AV block of the second and third degree;
- sinus bradycardia;
- uncontrolled heart failure of the chronic type, stage 2B-3;
- arterial hypotension;
- acute heart failure
- myocardial infarction (with systolic pressure up to 100 mm Hg);
- pulmonary edema;
- cardiogenic shock;
- sick sinus syndrome;
- cardiomegaly (without heart failure);
- Prinzmetal's angina;
- vasomotor rhinitis;
- occlusive diseases of peripheral vessels (including complicated);
- metabolic acidosis;
- diabetes;
- bronchial asthma;
- chronic obstructive pulmonary disease
- spastic colitis;
- pheochromocytoma (without combined use of alpha-blockers );
- simultaneous use with antipsychotics , MAO inhibitors and anxiolytics ;
- lactation period;
- sensitization to the drug.
Take the drug with caution in case of renal or hepatic failure , first degree AV blockade myasthenia gravis, hyperthyroidism, chronic heart failure stage 1-2A, psoriasis , pheochromocytoma, allergic reactions in the past, pregnancy, Raynaud's syndrome , in old age, persons in under 18 years of age.
Obsidan
Monitoring of patients taking Obzidan should include monitoring heart rate and blood pressure (at the beginning of treatment - daily, then once every 3-4 months), ECG.
In elderly patients, it is recommended to monitor kidney function (once every 4-5 months).
In case of increasing bradycardia (less than 50 beats per minute), arterial hypotension (systolic blood pressure less than 100 mm Hg), atrioventricular block, bronchospasm, ventricular arrhythmias, severe liver and/or kidney dysfunction in elderly patients, it is necessary reduce the dose of the drug or stop treatment.
The patient should be taught how to calculate heart rate and instructed to seek medical advice if the heart rate is less than 50 beats per minute.
It is recommended to discontinue therapy if depression caused by taking beta-blockers develops.
Patients using contact lenses should take into account that during treatment the production of tear fluid may decrease.
Before prescribing Obzidan, patients with heart failure (early stages) must use digitalis and/or diuretics.
Treatment of coronary heart disease and persistent arterial hypertension should be long-term - taking Obzidan is possible for several years.
Discontinuation of treatment is carried out gradually, under the supervision of a physician: abrupt withdrawal can dramatically increase myocardial ischemia, anginal syndrome, and worsen exercise tolerance.
Cancellation is carried out gradually, reducing the dose over 2 weeks or more (reduce the dose by 25% every 3-4 days).
In patients with diabetes mellitus, the drug is used under the control of blood glucose levels (once every 4-5 months).
In thyrotoxicosis, Obzidan may mask certain clinical signs of hyperthyroidism (for example, tachycardia). Abrupt withdrawal in patients with thyrotoxicosis is contraindicated, as it can intensify symptoms.
When prescribing beta-blockers to patients receiving hypoglycemic drugs, caution should be exercised, since hypoglycemia may develop during prolonged breaks in food intake. Moreover, its symptoms such as tachycardia or tremor will be masked due to the action of the drug. Patients should be instructed that the main symptom of hypoglycemia during treatment with beta-blockers is increased sweating.
Prescribe with caution in combination with hypoglycemic agents (the risk of hypoglycemia during insulin therapy and hyperglycemia during oral hypoglycemic agents).
When taking clonidine concomitantly, it can be discontinued only a few days after Obzidan is discontinued.
For pheochromocytoma, it is prescribed only in combination with alpha-blockers.
Do not use simultaneously with antipsychotic drugs (neuroleptics) and tranquilizers.
Drugs that reduce catecholamine reserves (for example, reserpine) can enhance the effect of beta-blockers, so patients taking combinations of drugs should be under constant medical supervision to detect arterial hypotension and bradycardia.
During treatment with Obzidan, intravenous administration of verapamil and diltiazem should be avoided.
Use with caution in combination with psychotropic drugs, for example, MAO inhibitors, when used for a course of more than 2 weeks.
A few days before general anesthesia with chloroform or ether, it is necessary to stop taking the drug (increased risk of depression of myocardial function and the development of arterial hypotension).
In smokers, the effectiveness of beta-blockers is lower.
During treatment, it is not recommended to take ethanol (a sharp decrease in blood pressure is possible).
The drug should be discontinued before testing the levels of catecholamines, normetanephrine and vinyl amidic acid in the blood and urine; antinuclear antibody titers.
Avoid using natural licorice during treatment; Protein-rich foods can increase bioavailability.
Side effects
- Reactions from the circulatory system: AV block, sinus bradycardia, heart failure , myocardial conduction disorders, decreased pressure, arrhythmias, hypotension, thoracalgia , spasm of the arteries of peripheral organs.
- Reactions from the digestive system: constipation, nausea, diarrhea , vomiting, epigastric pain, liver dysfunction.
- Reactions from the nervous system: nightmares, headache , asthenic syndrome, insomnia, lethargy, agitation, paresthesia, depression, fatigue, dizziness , weakness, drowsiness, confusion, hallucinations, tremor.
- Reactions from the respiratory system: nasal congestion, rhinitis, bronchospasm , shortness of breath, laryngospasm.
- Metabolic reactions: hypoglycemia or hyperglycemia.
- Reactions from the senses: decreased visual acuity, dry mucous eyes, keratoconjunctivitis.
- Reactions from the genitourinary system: decreased libido and potency.
- Dermatological reactions: exacerbation of psoriasis, exanthema, alopecia, hyperemia, psoriasis-like reactions.
- Reactions from the hormonal system: decreased functioning of the thyroid gland.
- Allergic reactions: rash , itching .
- From the laboratory test indicators: leukopenia, agranulocytosis, thrombocytopenia , activation of liver transaminases and increased bilirubin .
- Other: weakness, arthralgia, lumbodynia, withdrawal syndrome.
Obzidan, instructions for use (Method and dosage)
Instructions for use Obzidan recommends taking the tablets without chewing them before meals and washing them down with a small volume of liquid when swallowed.
For angina pectoris and rhythm disturbances, the initial daily dose is 60 mg per day in three divided doses, then increase the dose to 80-120 mg per day in 2-3 divided doses. The highest daily dose is 240 mg.
For arterial hypertension , take 40 mg twice a day. If the indicated dose is not enough, it is increased to 120 mg per day in three divided doses or up to 160 mg per day in four divided doses. The highest daily dose is 320 mg.
To prevent migraine and essential tremor, the drug is prescribed at an initial dose of 120 mg per day in three divided doses.
To prevent recurrence of myocardial infarction, treatment begins between the first and fourth weeks after a heart attack . Obzidan is prescribed at 120 mg per day in three divided doses for three days, and then continues at 80 mg per day in two divided doses. The highest daily dose is 180-240 mg in three doses.
For symptomatic treatment of hyperthyroidism, take 40 mg three to four times a day.
Solution for injection Obzidan (Obsidan)
Instructions for medical use of the drug
Description of pharmacological action
Blocks beta-adrenergic receptors, weakens the effect of sympathetic impulses on the heart and reduces the frequency and strength of heart contractions, cardiac output and myocardial oxygen demand.
Indications for use
Angina pectoris, progressive angina pectoris, silent myocardial ischemia, arterial hypertension, arrhythmias, hypertrophic cardiomyopathy, neurocirculatory dystonia, digitalis intoxication, thyrotoxicosis, migraine, essential familial tremor.
Release form
injection solution 0.1%; ampoule 5 ml box (box) 10.
Pharmacodynamics
Blocks beta1 and beta2 adrenergic receptors and has a membrane-stabilizing effect. Inhibits the automatism of the sinoatrial node, suppresses the occurrence of ectopic foci in the atria, AV junction, and ventricles (to a lesser extent). Reduces the speed of excitation in the AV junction along the Kent bundle, mainly in the anterograde direction. Reduces heart rate, reduces the strength of heart contractions and myocardial oxygen demand. Reduces cardiac output, renin secretion, blood pressure, renal blood flow and glomerular filtration rate. Suppresses the response of the aortic arch baroreceptors to a decrease in blood pressure. After taking a single dose, the hypotensive effect continues for 20–24 hours. A single dose of prolonged forms is equivalent to taking several doses of propranolol hydrochloride. Hypotension stabilizes by the end of the 2nd week of treatment. With long-term use, it reduces venous return and has a cardioprotective effect (reliably reduces the risk of recurrent myocardial infarction and sudden death by 20–50%). In patients with moderate arterial hypertension, it reduces the likelihood of developing coronary artery disease and cerebral strokes. In case of coronary artery disease, it reduces the frequency of attacks, increases exercise tolerance, and reduces the need for nitroglycerin. It is most effective in young patients (up to 40 years old) with a hyperdynamic type of blood circulation and with increased renin levels. Increases bronchial tone and uterine contractility (reduces bleeding during childbirth and in the postoperative period), enhances the secretory and motor activity of the gastrointestinal tract. Inhibits platelet aggregation and activates fibrinolysis. Inhibits lipolysis in adipose tissue, preventing an increase in the level of free fatty acids (while the concentration of triglycerides in plasma and the atherogenicity coefficient increase). Suppresses glycogenolysis, the secretion of glucagon and insulin, and the conversion of thyroxine to triiodothyronine. Lowers intraocular pressure, reduces the secretion of aqueous humor.
Pharmacokinetics
When taken orally, it is quickly and almost completely absorbed from the gastrointestinal tract (90%). Bioavailability is 30–40% (the “first pass” effect), depends on the nature of the food and the intensity of hepatic blood flow and increases with prolonged use (metabolites are formed that inhibit liver enzymes). Cmax in plasma is observed after 1–1.5 hours or 6 hours (for the prolonged form). Binds to plasma proteins by 90–95%; T1/2 is 2–5 hours (10 hours for the prolonged form). Volume of distribution: 3–5 l/kg. It accumulates in the lung tissue, brain, kidneys, heart, passes through the placental barrier, and penetrates into breast milk. Subject to glucuronidation in the liver (99%). It is excreted with bile into the intestine, deglucuronidated and reabsorbed (T1/2 during a course of administration can be extended to 12 hours). Excreted by the kidneys in the form of metabolites.
Use during pregnancy
Possibly if the expected effect of therapy exceeds the potential risk to the fetus. Breastfeeding should be stopped during treatment.
Contraindications for use
Hypersensitivity, AV block II-III degree, sinoatrial block, bradycardia (less than 55 beats/min), sick sinus syndrome, arterial hypotension, acute and severe chronic heart failure, Prinzmetal's angina, cardiogenic shock, obliterating vascular diseases, bronchial asthma.
Side effects
Weakness, dizziness, headache, paresthesia, cold extremities, dyspeptic disorders, conjunctivitis, skin rashes, itching.
Directions for use and doses
For hypertension - 40 mg 2 times a day. If necessary, the dose can be increased over 2–4 weeks to 80–160 mg 2 times a day. For angina, migraine, essential tremor - 20 mg 2-3 times a day. The dose can be increased over 1 week to 40 mg 4 times a day or up to 80 mg 2-3 times a day. The maximum daily dose is 240 mg for migraine and 480 mg for angina. For arrhythmia, hypertrophic cardiomyopathy, thyrotoxicosis - 10-40 mg 3-4 times a day (up to 240 mg/day).
Overdose
Symptoms: dizziness, bradycardia, arrhythmia, heart failure, hypotension, collapse, difficulty breathing, acrocyanosis, convulsions. Treatment: gastric lavage and administration of adsorbents, symptomatic therapy: atropine, beta-adrenergic agonists (isoprenaline, isadrin), sedatives (diazepam, lorazepam), cardiotonic (dobutamine, dopamine, epinephrine) drugs, vasopressors, glucagon, etc.; transvenous stimulation is possible. Hemodialysis is ineffective.
Interactions with other drugs
Barbiturates and nicotine increase the effect, cimetidine weakens it; enhances the negative inotropic effect of calcium antagonists, the negative dromotropic effect of cardiac glycosides, the hypotensive effect of antihypertensive drugs, and the antiarrhythmic effect of lidocaine. Increases the likelihood of developing hypoglycemia due to insulin.
Precautions for use
Treatment should be carried out with regular medical supervision. With long-term use, the possibility of additional administration of cardiac glycosides should be considered. Reduces compensatory cardiovascular reactions in response to the use of general anesthetics. A few days before anesthesia, it is necessary to stop taking it or choose an anesthetic with the least negative inotropic effect. IV administration is not recommended for children. Elderly patients have an increased risk of CNS side effects. If liver function is impaired, dose reduction and observation during the first 4 days of therapy are recommended. May mask the symptoms of hypoglycemia (tachycardia) in patients with diabetes mellitus taking insulin and other hypoglycemic drugs. It is possible that the severity of the hypersensitivity reaction may increase and the absence of effect from usual doses of epinephrine against the background of a burdened allergic history. During treatment, it is recommended to avoid drinking alcoholic beverages. Use with caution while working for vehicle drivers and people whose profession involves increased concentration. Stop treatment gradually over about 2 weeks.
Special instructions for use
During treatment, test results may change during laboratory tests (increased levels of urea, transaminases, phosphatases, LDH).
Storage conditions
List B.: In a dry place, protected from light, at room temperature.
Best before date
60 months
ATX classification:
C Cardiovascular system
C07 Beta blockers
C07A Beta blockers
C07AA Non-selective beta-blockers
C07AA05 Propranolol
Overdose
Signs: fainting, convulsions, bradycardia , decreased blood pressure , arrhythmia , shortness of breath , cyanosis of the fingers or palms, cardiac arrest (with intravenous injection).
Treatment: perform gastric lavage, take activated charcoal ; for AV conduction - administer intravenously up to 2 mg of Epinephrine , Atropine ; for ventricular extrasystole, administer L idocaine ; for arterial hypotension plasma-substituting solutions are administered intravenously ; for convulsions , diazepam is administered intravenously; for bronchospasm - beta-agonists .
Interaction
When the drug is used together with MAO inhibitors an excessive hypotensive effect , so this combination is prohibited; The interval between taking these medications should be more than 14 days.
When used together with R eserpine, Nifedipine, diuretics, ethanol, hydralazine and other antihypertensive drugs, the hypotensive effect of the drug is enhanced.
The hypotensive effect of Obzidan is weakened by glucocorticosteroids, non-steroidal anti-inflammatory drugs, and estrogens .
When used together, Obzidan enhances the effect of uterotonic and thyreostatic drugs and weakens the effect of antihistamines .
Cardiac glycosides, Guanfacine, Reserpine, Methyldopa, and antiarrhythmic drugs increase the risk of or intensify the manifestations of AV block, bradycardia, and heart failure.
Oral tablets Obsidan
Instructions for medical use of the drug
Description of pharmacological action
Blocks beta-adrenergic receptors, weakens the effect of sympathetic impulses on the heart and reduces the frequency and strength of heart contractions, cardiac output and myocardial oxygen demand.
Indications for use
Angina pectoris, progressive angina pectoris, silent myocardial ischemia, arterial hypertension, arrhythmias, hypertrophic cardiomyopathy, neurocirculatory dystonia, digitalis intoxication, thyrotoxicosis, migraine, essential familial tremor.
Release form
tablets 40 mg; blister 20 cardboard pack 3;
Pharmacodynamics
Blocks beta1 and beta2 adrenergic receptors and has a membrane-stabilizing effect. Inhibits the automatism of the sinoatrial node, suppresses the occurrence of ectopic foci in the atria, AV junction, and ventricles (to a lesser extent). Reduces the speed of excitation in the AV junction along the Kent bundle, mainly in the anterograde direction. Reduces heart rate, reduces the strength of heart contractions and myocardial oxygen demand. Reduces cardiac output, renin secretion, blood pressure, renal blood flow and glomerular filtration rate. Suppresses the response of the aortic arch baroreceptors to a decrease in blood pressure. After taking a single dose, the hypotensive effect continues for 20–24 hours. A single dose of prolonged forms is equivalent to taking several doses of propranolol hydrochloride. Hypotension stabilizes by the end of the 2nd week of treatment. With long-term use, it reduces venous return and has a cardioprotective effect (reliably reduces the risk of recurrent myocardial infarction and sudden death by 20–50%). In patients with moderate arterial hypertension, it reduces the likelihood of developing coronary artery disease and cerebral strokes. In case of coronary artery disease, it reduces the frequency of attacks, increases exercise tolerance, and reduces the need for nitroglycerin. It is most effective in young patients (up to 40 years old) with a hyperdynamic type of blood circulation and with increased renin levels. Increases bronchial tone and uterine contractility (reduces bleeding during childbirth and in the postoperative period), enhances the secretory and motor activity of the gastrointestinal tract. Inhibits platelet aggregation and activates fibrinolysis. Inhibits lipolysis in adipose tissue, preventing an increase in the level of free fatty acids (while the concentration of triglycerides in plasma and the atherogenicity coefficient increase. Suppresses glycogenolysis, the secretion of glucagon and insulin, the conversion of thyroxine to triiodothyronine. Lowers intraocular pressure, reduces the secretion of aqueous humor. Long-term administration (18 months) in rats and mice doses up to 150 mg/kg/day did not reveal carcinogenic properties and adverse effects on fertility.At a dose of 150 mg/kg/day, 10 times higher than the MRDC, it had an embryotoxic effect (increased incidence of fetal resorption).
Pharmacokinetics
When taken orally, it is quickly and almost completely absorbed from the gastrointestinal tract (90%). Bioavailability is 30–40% (the “first pass” effect), depends on the nature of the food and the intensity of hepatic blood flow and increases with prolonged use (metabolites are formed that inhibit liver enzymes). Cmax in plasma is observed after 1–1.5 hours or 6 hours (for the prolonged form). Binds to plasma proteins by 90–95%; T1/2 is 2–5 hours (10 hours for the prolonged form). Volume of distribution: 3–5 l/kg. It accumulates in the lung tissue, brain, kidneys, heart, passes through the placental barrier, and penetrates into breast milk. Subject to glucuronidation in the liver (99%). It is excreted with bile into the intestine, deglucuronidated and reabsorbed (T1/2 during a course of administration can be extended to 12 hours). Excreted by the kidneys in the form of metabolites.
Use during pregnancy
Possibly if the expected effect of therapy exceeds the potential risk to the fetus. Breastfeeding should be stopped during treatment.
Contraindications for use
Hypersensitivity, AV block II-III degree, severe bradycardia, hypotension, obstructive airway diseases; relative contraindications - diabetes mellitus in the sub- and decompensation stage, psoriasis in the acute stage.
Side effects
Weakness, dizziness, headache, paresthesia, cold extremities, dyspeptic disorders, conjunctivitis, skin rashes, itching.
Directions for use and doses
For hypertension - 40 mg 2 times a day. If necessary, the dose can be increased over 2–4 weeks to 80–160 mg 2 times a day. For angina, migraine, essential tremor - 20 mg 2-3 times a day. The dose can be increased over 1 week to 40 mg 4 times a day or up to 80 mg 2-3 times a day. The maximum daily dose is 240 mg for migraine and 480 mg for angina. For arrhythmia, hypertrophic cardiomyopathy, thyrotoxicosis - 10-40 mg 3-4 times a day (up to 240 mg/day).
Overdose
Symptoms: dizziness, bradycardia, arrhythmia, heart failure, hypotension, collapse, difficulty breathing, acrocyanosis, convulsions. Treatment: gastric lavage and administration of adsorbents, symptomatic therapy: atropine, beta-adrenergic agonists (isoprenaline, isadrin), sedatives (diazepam, lorazepam), cardiotonic (dobutamine, dopamine, epinephrine) drugs, vasopressors, glucagon, etc.; transvenous stimulation is possible. Hemodialysis is ineffective.
Interactions with other drugs
Barbiturates and nicotine increase the effect, cimetidine weakens it; enhances the negative inotropic effect of calcium antagonists, the negative dromotropic effect of cardiac glycosides, the hypotensive effect of antihypertensive drugs, and the antiarrhythmic effect of lidocaine. Increases the likelihood of developing hypoglycemia due to insulin.
Precautions for use
Treatment should be carried out with regular medical supervision. With long-term use, the possibility of additional administration of cardiac glycosides should be considered. Reduces compensatory cardiovascular reactions in response to the use of general anesthetics. A few days before anesthesia, it is necessary to stop taking it or choose an anesthetic with the least negative inotropic effect. IV administration is not recommended for children. Elderly patients have an increased risk of CNS side effects. If liver function is impaired, dose reduction and observation during the first 4 days of therapy are recommended. May mask the symptoms of hypoglycemia (tachycardia) in patients with diabetes mellitus taking insulin and other hypoglycemic drugs. It is possible that the severity of the hypersensitivity reaction may increase and the absence of effect from usual doses of epinephrine against the background of a burdened allergic history. During treatment, it is recommended to avoid drinking alcoholic beverages. Use with caution while working for vehicle drivers and people whose profession involves increased concentration. Stop treatment gradually over about 2 weeks.
Special instructions for use
During treatment, test results may change during laboratory tests (increased levels of urea, transaminases, phosphatases, LDH).
Storage conditions
List B.: In a place protected from light, at a temperature of 15–25 °C.
Best before date
60 months
ATX classification:
C Cardiovascular system
C07 Beta blockers
C07A Beta blockers
C07AA Non-selective beta-blockers
C07AA05 Propranolol
Obzidan's analogs
Level 4 ATC code matches:
Sotalol Canon
SotaHEXAL
Propranolol
Sotalex
Anaprilin
The most common analogues of Obzidan: Adrenoblock, Anaprilin, Vero-Anaprilin, Inderal, Inderal LA, Propranobene, Propranolol, Propranolol Nycomed.