Obsidanum

Obsidanum – _beta1-and _{beta2-adrenoblocker}, the medicine having anti-hypertensive, anti-anginal and antiarrhytmic effect.

Form of release and structure

Dosage form – tablets: white color, a round form, with slanted edges, on one of the parties – risk, dividing the squeezed-out figures "4" and "0", on the other hand – a smooth surface (on 20 pieces in blisters, on 3 blisters in a pack cardboard).

Active agent: propranolol the hydrochloride, its contents in 1 tablet makes 40 mg.

Auxiliary components: potato starch, magnesium stearate, gelatin, silicon dioxide colloid, sodium carboxymethylstarch (type A), talc, lactoses monohydrate.

Indications to use

• Ciliary tachyarrhythmia;
• Supraventricular tachycardia;
• Angina of exertion;
• Essential tremor;
• Arterial hypertension;
• Supraventricular and ventricular premature ventricular contraction;
• Sinus tachycardia (including at a hyperthyroidism);
• Unstable stenocardia (except for Printsmetal's stenocardia);
• Sympathoadrenal crises against the background of a diencephalic syndrome;
• Thyrotoxicosis and thyrocardiac crisis (Obsidanum is applied as symptomatic drug in case of intolerance of thyreostatic medicines);
• Prevention of attacks of migraine;
• Prevention of a myocardial infarction (systolic arterial pressure is higher than 100 mm hg).

Contraindications

Absolute:

• Chronic obstructive pulmonary disease (in the anamnesis including);
• Tendency to bronkhospastichesky reactions;
• Bronchial asthma;
• Vasculomotor rhinitis;
• Diabetes mellitus;
• Spastic colitis;
• Pheochromocytoma (without co-administration of alpha adrenoblockers);
• Metabolic acidosis (including diabetic ketoacidosis);
• The occlusal diseases of peripheral vessels (complicated by pain at rest or the alternating lameness, gangrene);
• Cardiomegaly if it is not followed by symptoms of heart failure;
• Fluid lungs;
• Sick sinus syndrome;
• Acute heart failure;
• Uncontrollable chronic heart failure of IIB-III of a stage;
• Sinus bradycardia;
• Printsmetal's stenocardia;
• Acute myocardial infarction (systolic arterial pressure is less than 100 mm hg);
• Sinuatrial blockade;
• Atrioventricular block of II and III degrees;
• Arterial hypotension (systolic arterial pressure is lower than 90 mm hg);
• Cardiogenic shock;
• Simultaneous use of antipsychotic means, anxiolytics or monoamine oxidase inhibitors;
• Lactation;
• Hypersensitivity to drug components.

Relative:

• Age up to 18 years;
• Advanced age;
• Pregnancy period;
• Allergic reactions in the anamnesis;
• Reynaud's syndrome;
• Atrioventricular block of the I degree;
• Chronic heart failure of I-IIA of a stage;
• Psoriasis;
• Myasthenia;
• Renal and/or liver failure;
• Pheochromocytoma;
• Hyperthyroidism.

Route of administration and dosage

It is necessary to accept Obsidanum inside, to food: to swallow of tablets entirely and to wash down with enough liquid.

The recommended dosing modes:

• Hyperthyroidism (symptomatic treatment): on 40 mg 3-4 times a day;
• Arterial hypertension: on 40 mg 2 times a day. In case of insufficiency of hypotensive effect the daily dose is raised to 120 mg (on 40 mg 3 times a day) or to 160 mg (on 80 mg 2 times a day). The highest admissible daily dose – 320 mg;
• Disturbances of a cordial rhythm, stenocardia: in an initiation of treatment – on 20 mg 3 times a day (a daily dose – 60 mg), further gradually increase a daily dose to 80-120 mg in 2-3 receptions. The highest daily dose should not exceed 240 mg;
• Treatment of an essential tremor and prevention of migraine: on 40 mg 3 times a day, if necessary further adjust a dose;
• Prevention of a repeated myocardial infarction: treatment is begun between 5 and 21 day after an attack, the first 2-3 days appoint 40 mg 3 times a day (a daily dose – 120 mg), then – on 80 mg 2 times a day (a daily dose – 160 mg). If there is a need, the daily dose is raised to 180-240 mg in 2-3 receptions.

To patients with renal failures increase an interval between receptions or reduce a dose.

At abnormal liver functions reduce a drug dose.

Side effects

• From respiratory system: asthma, laryngospasm, bronchospasm, nose congestion, rhinitis;
• From cardiovascular system: arrhythmias, stethalgia, cold snap of extremities, heartbeat, lowering of arterial pressure, atrioventricular block, sinus bradycardia, orthostatic hypotension, spasm of peripheral arteries, disturbance of conductivity of a myocardium, heart failure;
• From the central and peripheral nervous system: seldom – an asthenic syndrome, excitement, a headache, decline in the ability to bystry mental and motor reactions, drowsiness, dreadful dreams, increased fatigue, hallucinations, dizziness, paresthesias, sleeplessness, short-term loss of memory or confusion of consciousness, weakness, a tremor, a depression;
• From a reproductive system: decrease in a potentiality;
• From the alimentary system: pains in epigastric area, taste change, dryness in a mouth, nausea, lock/diarrhea, vomiting, an abnormal liver function;
• From endocrine system: depression of function of a thyroid gland;
• From sense bodys: visual acuity disturbance, dryness of a mucous membrane of eyes (owing to reduction of secretion of the lacrimal liquid), a keratoconjunctivitis;
• Allergic and dermatological reactions: skin rash, itch, sweating strengthening, aggravation of a course of psoriasis, dieback, alopecia, psoriazopodobny skin reactions, dermahemia;
• From a metabolism: at patients with a diabetes mellitus of type 1 – a hypoglycemia, at patients with a diabetes mellitus of type 2 – a hyperglycemia;
• Others: withdrawal, thorax, spin or joints pain, muscular weakness;
• From laboratory indicators: increase in activity of hepatic transaminases and level of bilirubin, decrease in quantity of leukocytes, granulocytes or thrombocytes in blood.

Special instructions

During treatment it is regularly necessary to control the heart rate and arterial pressure (at the beginning of administration of drug – daily, further – 1 time in 3-4 months), and also the electrocardiogram. Elderly people, besides, need monitoring of a condition of function of kidneys (each 4-5 months).

If at the patient of advanced age renal failures and/or a liver are noted, the amplifying bradycardia (it is less than 50 beats per minute), arterial hypotension (systolic arterial pressure less than 100 mm hg), an atrioventricular block, ventricular arrhythmias, a bronchospasm, it is necessary to lower a dose of Obsidanum or to cancel it at all.

The doctor has to train each patient in a technique of calculation of heart rate and inform on need to address for consultation if this indicator makes less than 50 beats per minute.

It is recommended to stop treatment in case of development of the depression caused by the carried-out therapy.

Propranolol can reduce products of the lacrimal liquid that should be considered to people who carry contact lenses.

To patients with heart failure (at early stages) Obsidanum can be appointed only after a therapy course diuretics and/or cardiac glycosides.

Treatment of persistent arterial hypertension and coronary heart disease has to be long, up to several years.

Drug withdrawal should be made gradually, reducing a dose under control of the doctor as in case of the sharp termination of treatment deterioration in tolerance to an exercise stress, strengthening of ischemia of a myocardium and a pain syndrome is possible at stenocardia. The optimum period of cancellation of Obsidanum – not less than 2 weeks with a dose decline for 25% each 3-4 days.

Under control of content of glucose in blood (each 4-5 months) treatment there have to undergo patients with a diabetes mellitus. Extra care should be observed to people who receive hypoglycemic means as during long breaks in meal there is a risk of development of a hypoglycemia. At the same time its expressed signs, such as tremor and tachycardia, will mask effect of propranolol. The doctor has to inform patients that the main symptom of a hypoglycemia during use of this drug is the increased sweating.

In a combination with insulin Obsidanum can lead to a hypoglycemia, with peroral hypoglycemic drugs – to a hyperglycemia.

At a thyrotoxicosis propranolol can mask the main symptoms of a disease (for example, tachycardia). In case of sharp drug withdrawal strengthening of symptomatology is possible.

At a pheochromocytoma Obsidanum can be appointed only in a combination with alpha adrenoblockers.

Patients who along with propranolol receive a clonidine can carry out its cancellation only in several days after cancellation of Obsidanum.

The patients receiving Obsidanum in combination with the drugs reducing stocks of catecholamines (for example, Reserpinum), during treatment have to be under constant medical control as strengthening of effect of propranolol is possible that is shown by bradycardia and arterial hypotension.

In need of performing surgery under the general anesthesia using ether or chloroform for several days it is necessary to stop reception of Obsidanum since the risk of development of arterial hypotension and oppression of function of a myocardium increases.

It is also necessary to cancel drug before carrying out researches on the content in urine and blood of vinilamidalny acid, catecholamines and a normetanefrin, and also credits of antinuclear antibodies.

Efficiency of propranolol decreases at patients who abuse smoking.

During therapy it is necessary to refrain from the use of a natural liquorice and alcohol, and also from driving of the car and performance of any kinds of the works requiring special attention and high speed of psychophysical reactions.

It is necessary to consider that food rich with protein can increase bioavailability of propranolol.

Medicinal interaction

• Monoamine oxidase inhibitors: considerably anti-hypertensive effect of propranolol amplifies (use of such combination is contraindicated; the interval between administrations of drugs should not be less than 14 days);
• Amiodaronum, verapamil, diltiazem: expressiveness negative dromo-, other and chronotropic action amplifies (such combinations are not recommended);
• Derivatives of a fenotiazin: mutual increase in concentration of both drugs is observed;
• Ethanol, hypnotic drugs and sedative drugs, neuroleptics, three - and tetracyclic antidepressants: expressiveness of the oppressing effect of propranolol on the central nervous system amplifies;
• Cimetidinum: bioavailability of propranolol increases;
• Ethanol, diuretics, гидралазин, Reserpinum and other hypotensive drugs: anti-hypertensive effect of propranolol amplifies;
• Glucocorticosteroids, non-steroidal anti-inflammatory drugs, estrogen: the hypotensive effect of Obsidanum is weakened;
• Uterotoniziruyushchy drugs, tireostatik: their action amplifies;
• Antihistaminic drugs: their action decreases;
• Rifampicin: the propranolol elimination half-life decreases;
• Antiarrhytmic drugs, cardiac glycosides, гуанфацин, Reserpinum, Methyldopum: the risk of development or aggravation of bradycardia, development of an atrioventricular block and heart failure, a cardiac standstill increases;
• Theophylline, xanthines (except for Diphyllinum): their clearance decreases;
• Coumarins: their anticoagulating effect is prolonged;
• Insulin and peroral hypoglycemic means: their effect changes, symptoms of the developing hypoglycemia are not shown;
• Lidocaine: concentration of propranolol in a blood plasma increases;
• Phenytoinum entered intravenously, the means of an inhalation anesthesia which are derivatives of hydrocarbons: expressiveness of cardiodepressive effect of propranolol and probability of a lowering of arterial pressure increases;
• Sulfasalazinum: propranolol metabolism is slowed down owing to what its concentration in a blood plasma increases;
• Nifedipine: arterial pressure can decrease considerably;
• Not depolarizing muscle relaxants: their action is extended;
• The allergens applied to an immunotherapy or skin tests: the risk of development of heavy system reactions (anaphylaxis) increases;
• Not hydrogenated ergot alkaloids: the probability of development of disturbances of peripheric circulation increases;
• Iodinated X-ray contrast agents intravenously: the risk of development of anaphylactic reactions increases.

Terms and storage conditions

To store in the unavailable to children, protected from light place at a temperature of 15-25 ºС.

Period of validity – 5 years.