Inderal
Inderal
Inderal (Propranolol)Pharmacological action
Not selective beta adrenoblocker. Possesses antianginal, antihypertensive and antiarrhytmic action.
The antihypertensive effect of a preparation is bound to reduction of minute volume of heart, reduction of sympathetic stimulation of peripheric vessels, depression of activity a system renin-angiotenzinovoj (matters at patients with an initial hypersecretion of a renin), depression of sensitivity of baroreceptors of an aortic arch (there is no intensifying of their activity in reply to BP depression). The antihypertensive effect is stabilised to the extremity of 2 weeks of course appointment.
Antianginal action is caused by depression of requirement of a myocardium in oxygen (at the expense of negative chronotropic and inotropic effect). CARDIAC CONTRACTIONS RATE reduction conducts to elongation of a diastole and improvement of perfusion of a myocardium. At the expense of rising of final diastolic pressure in a left ventricle and augmentations of a stretching of muscular fibers of ventricles can raise requirement for oxygen, especially at patients with a chronic heart failure.
At the expense of depression of requirement of a myocardium in oxygen there is a reduction of expression of an ischemia of a myocardium, the postinfarction lethality can decrease also thanks to antiarrhytmic action.
Ability to warn development of a headache of a vascular genesis is caused by reduction of expression of expansion of cerebral arteries owing to blockade of b-adrenoreceptors of vessels, inhibition caused by catecholamins of aggregation of thrombocytes and a lipolysis, platelet stickness depression, prevention of activation of factors of coagulation of blood during adrenaline liberation, stimulation of entering of oxygen in a tissue and reduction of secretion of a renin.
Reduction of a tremor against propranolol application can be caused blockade of b2-adrenoreceptors.
Raises atherogenous properties of blood. Strengthens uterus reductions (spontaneous and caused by the medical products stimulating a myometrium). Raises a tonus of bronchuses.
Inderal Indications
- An arterial hypertensia;
- An angina of exertion;
- An astable stenocardia;
- A tachycardia;
- A ciliary tachyarrhythmia;
- Myocardial infarction preventive maintenance (a systolic BP above 100 mm hg);
- An essential tremor;
- A migraine (preventive maintenance of attacks);
- As symptomatic therapy of a thyrotoxicosis and a thyrocardiac crisis (at intolerance of thyreostatic medical products);
Inderal Dosage regimen
Tablets should be accepted inside, to meal, not chewing and washing down with a liquid small amount.
At an arterial hypertensia prescribe on 40 mg 2 times/days At insufficient expression of hypotensive effect a daily dose enlarge to 120 mg (on 40 mg 3 times/sut) or to 160 mg (on 80 mg 2 times/sut). The maximum daily dose - 320 mg.
At a stenocardia, disturbances of a warm rhythm the initial daily dose makes 60 mg (on 20 mg 3 times/sut), then a daily dose enlarge to 80-120 mg, parting it by 2-3 receptions. The maximum daily dose - 240 mg.
For migraine preventive maintenance, and also at an essential tremor the preparation is prescribed in an initial dose by of 120 mg (on 40 mg 3 times/sut).
For preventive maintenance of a repeated myocardial infarction therapy by Obsidanum should be begun between 5th and 21st day after the transferred myocardial infarction. The preparation is prescribed in a dose by of 120 mg (on 40 mg 3 times)/sut within 2-3 days, and then continue preparation reception on 80 mg 2 times/days If necessary it is possible to prescribe Obsidanum in a daily dose of 180-240 mg in 2-3 receptions.
At a hyperthyroidism (symptomatic therapy) Obsidanum is prescribed on 40 mg by 3-4 times/days
At disturbance of function of kidneys it is necessary to lower an initial dose or to enlarge an interval between preparation receptions.
At disturbance of function of a liver the preparation dose decline is necessary.
Inderal Side effect
From cardiovascular system: a sinus bradycardia, AV-blockade, a heart failure, palpitation, disturbance of conductivity of a myocardium, an arrhythmia, BP depression, an orthostatic hypotension, a stethalgia, a spastic stricture of peripheric arteries, a cold snap of extremities.
From the alimentary system: dryness in a mouth, a nausea, vomiting, a diarrhoeia, a constipation, pains in epigastric area, disturbance of function of a liver, taste change.
From party TSNS and peripheric nervous system: seldom - a headache, a sleeplessness, dreadful dreamings, an asthenic syndrome, depression of ability to fast mental and impellent reactions, excitation, depression, paresthesias, undue fatigability, delicacy, giddiness, drowsiness, confusion of consciousness or short-term loss of memory, hallucination, a tremor.
From respiratory system: a rhinitis, a dyspnea, a bronchospasm, a laryngospasm.
From a metabolism: a hypoglycaemia (at 1 type sick of a diabetes), a hyperglycaemia (at 2 types sick of a diabetes).
From sense organs: dryness mucous an eye (reduction of secretion of a plaintive liquid), visual acuity disturbance, a keratoconjunctivitis.
From sexual system: potency depression.
Dermatological reactions: an alopecia, an exacerbation of a current of a psoriasis, diaphoresis intensifying, a dermahemia, an exanthema, psoriasiform dermal reactions.
From endocrine system: a thyroid gland depression of function.
Allergic reactions: a dermal eruption, an itch.
From laboratory indicators: an agranulocytosis, a leukopenia, a thrombocytopenia; rising of activity of hepatic transaminases and bilirubin level.
The other: muscular delicacy, a dorsodynia or joints, a pain in a thorax, a withdrawal.
Inderal Contraindications
- AV-blockade II and III degrees;
- Sinuatrial blockade;
- A sinus bradycardia;
- An arterial hypotension (a systolic BP below 90 mm hg);
- Uncontrollable chronic heart failure IIB-III of a stage;
- An acute heart failure;
- An acute myocardial infarction (a systolic BP below 100 mm hg);
- A cardiogenic shock;
- A fluid lungs;
- A sick sinus syndrome;
- A cardiomegaly (without heart failure signs);
- A vasculomotor rhinitis;
- Occlusal diseases of peripheric vessels (complicated by a gangrene, a symptom of an alternating lameness or a pain in rest);
- A diabetes;
- A metabolic acidosis;
- A bronchial asthma;
- Chronic obstructive illness of lungs (including in the anamnesis);
- A pheochromocytoma (without simultaneous use of alpha adrenoblockers);
- A spastic colitis;
- Simultaneous reception with antipsychotic agents;
- Simultaneous reception with inhibitors MAO;
- The lactemia period;
- A hypersensibility to a preparation.
With care it is necessary to prescribe a preparation at AV-blockade of I degree, hepatic and-or renal insufficiency, a hyperthyroidism, myasthenias, chronic heart failure I-IIA of a stage, a pheochromocytoma, a psoriasis, allergic reactions in the anamnesis, at pregnancy, to patients of advanced age, to children and teenagers about 18 years (efficiency and safety are not established) are elderly.
Pregnancy and lactemia
Obsidanum application at pregnancy is possible only in that case when the prospective advantage for mother exceeds potential risk for a foetus. In need of application it is necessary to spend careful observation over a foetus condition since Obsidanum reception at pregnancy can cause a pre-natal growth inhibition, to this period a hypoglycaemia and a bradycardia at a foetus. For 48-74 h to sorts Obsidanum should be cancelled.
Obsidanum application is contraindicative in a lactemia. In need of its application during this period thoracal feeding should be stopped.
Inderal Special indicatings
At Obsidanum appointment it is necessary to supervise regularly the CARDIAC CONTRACTIONS RATE and a BP (in the treatment beginning - daily, then 1 time in 3-4 months), an electrocardiogram.
At elderly patients it is necessary to carry out the control of function of kidneys (1 times in 4-5 months).
In case of occurrence in patients of advanced age of an accruing bradycardia (less than 50 ud./mines), an arterial hypotension (a systolic BP below 100 mm hg), AV-blockade, a bronchospasm, ventricular arrhythmias, serious disturbances of function of a liver and-or kidneys, it is necessary to reduce a dose of a preparation or to stop treatment.
It is necessary to train the patient in a technique of calculation of the CARDIAC CONTRACTIONS RATE and to instruct about necessity of medical consultation at the CARDIAC CONTRACTIONS RATE less than 50 ud./minutes
It is recommended to stop therapy by Obsidanum at development of the depression caused by its reception.
The patients using contact lenses, should consider, that against treatment by Obsidanum probably reduction of production of a plaintive liquid.
Before appointment of Obsidanum with a heart failure (early stages) it is necessary for patients to apply warm glycosides and-or diuretics.
Treatment of an ischemic heart disease and proof arterial hypertensia should be long - Obsidanum reception is possible within several years.
The treatment termination carry out gradually, under observation of the doctor, sharp cancellation can strengthen an ischemia of a myocardium, a painful syndrome at a stenocardia, worsen tolerance to an exercise stress. Obsidanum cancellation spend within 2 weeks and more, gradually reducing a dose (on 25 % each 3-4 days).
At sick of a diabetes preparation application spend under the control of the maintenance of a glucose of blood (1 times in 4-5 months). At appointment of Obsidanum to the patients receiving hypoglycemic preparations, it is necessary to be careful, as during long breaks in food intake the hypoglycaemia can develop. And its such symptoms as the tachycardia or a tremor will mask at the expense of Obsidanum action. Patients should be warned, that the basic symptom of a hypoglycaemia during treatment by Obsidanum is the raised diaphoresis.
With care it is necessary to prescribe Obsidanum together with hypoglycemic agents (danger of occurrence of a hypoglycaemia against therapy by insulin and hyperglycemias - against reception of peroral hypoglycemic agents).
At a thyrotoxicosis Obsidanum can mask certain clinical signs of a hyperthyroidism (for example, a tachycardia). Sharp cancellation of a preparation at sick of a thyrotoxicosis is contraindicative, as is capable to strengthen semiology.
At simultaneous reception of Clonidinum its reception can be stopped only in some days after Obsidanum cancellation.
At a pheochromocytoma Obsidanum prescribe only in a combination to alpha adrenoblockers.
The preparations reducing stocks of catecholamins (for example, Reserpinum) can strengthen Obsidanum action, therefore the patients accepting combinations of given preparations, should be under constant observation of the doctor about revealing of an arterial hypotension and a bradycardia.
For some days before carrying out of the general narcosis by Chloroformium or an Aether it is necessary to stop preparation reception (rising of risk of oppression of function of a myocardium and development of an arterial hypotension).
It is necessary to cancel a preparation before maintenance research in blood and urine of catecholamins ; a caption of antinuclear antibodies.
At the patients abusing smoking, efficiency of Obsidanum decreases.
During treatment by Obsidanum it is not recommended to accept alcohol (probably sharp depression of a BP).
Use in pediatrics
Efficiency and safety of application of Obsidanum at children and teenagers is elderly till 18 years are not established.
Influence on ability to driving of motor transport and to management of mechanisms
In treatment by Obsidanum it is necessary to abstain from driving of motor transport and employment by potentially dangerous kinds of the activity demanding raised concentration of attention and speed of psychomotor reactions.
Inderal Overdosage
Symptoms: a bradycardia, giddiness or a syncope, depression of a BP, an arrhythmia, the complicated breath, a cyanosis of fingernails of fingers or palms, cramps, a cardiac standstill (at i.v. introduction).
Treatment: a gastric lavage, appointment of the activated coal (at intake); at AV-conductivity disturbance - i.v. enter 1-2 mg of atropine, Epinephrinum, at low efficiency carry out statement of a time cardiostimulator; at an arterial hypotension (the patient should be in a prone position with the lowered head extremity of a bed) if there are no fluid lungs signs, i.v. enter plasma substituting solutions, at an inefficiency - Epinephrinum, Dopaminum, Dobutaminum; at cramps - i.v.
Inderal Medicinal interaction
At simultaneous application of Obsidanum with inhibitors MAO is observed appreciable intensifyings of the hypotensive action, therefore the given combination is contraindicative; having rummaged in treatment between reception of inhibitors MAO and Obsidanum should make not less than 14 days.
At simultaneous application with diuretics, Reserpinum, and also ethanol the hypotensive effect of Obsidanum amplifies.
Obsidanum at simultaneous application strengthens action thyreostatic preparations; reduces action of antihistamine preparations.
Obsidanum at simultaneous application changes efficiency of insulin and peroral hypoglycemic preparations, masks symptoms of a developing hypoglycaemia (a tachycardia, BP rising).
Warm glycosides, Methyldopum, Reserpinum and antiarrhytmic preparations at simultaneous reception with Obsidanum raise risk of development or aggravation of a bradycardia, AV-blockade, a cardiac standstill and a heart failure.
Nifedipine at simultaneous application with Obsidanum can lead to appreciable depression of a BP.
Not hydrogenated alkaloids of an ergot at simultaneous application with Obsidanum raise risk of development of disturbances of a peripheric circulation.
Obsidanum application raises probability of development of serious system reactions (anaphylaxis) against introduction of the allergens used for an immunotherapy or for dermal assays.
Pharmacokinetic interaction
Cimetidinum enlarges bioavailability of propranolol.
Propranolol raises concentration of lidocaine in a blood plasma, reduces Theophyllinum clearance.
Propranolol reduces a clearance of xanthines (except Diphyllinum).
Sulfasalazinum enlarges concentration of propranolol in a blood plasma (the metabolism brakes), rifampicin shortens the period of semideducing of propranolol.
Inderal Conditions and periods of storage
B.Preparat's list should be stored in protected from light, a place inaccessible to children at temperature from 15 to 25 C. The Period of validity - 5 years.
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