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|Inderal 80 mg|
270 pills - 80 mg
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Pharmacological action of the drug Inderal
Non-selective beta-blocker. It has antianginal, hypotensive and antiarrhythmic effects. Non-selectively blocking beta-adrenergic receptors (75% of beta1- and 25% of beta2-adrenergic receptors), reduces the formation of cAMP from ATP stimulated by catecholamines, as a result of which it reduces the intracellular intake of Ca2 +, has a negative chrono-, dromo-, batmo- and inotropic effect (decreases heart rate , inhibits conductivity and excitability, reduces myocardial contractility).
At the beginning of the use of beta-blockers, OPSS increases in the first 24 hours (as a result of a reciprocal increase in the activity of alpha-adrenergic receptors and the elimination of stimulation of beta2-adrenergic receptors of the vessels of skeletal muscles), but after 1-3 days it returns to the initial one, and decreases with prolonged administration.
The antihypertensive effect is associated with a decrease in IOC, sympathetic stimulation of peripheral vessels, a decrease in the activity of the renin-angiotensin system (important in patients with initial hypersecretion of renin), the sensitivity of the aortic arch baroreceptors (there is no increase in their activity in response to a decrease in blood pressure) and the effect on the central nervous system. The hypotensive effect stabilizes by the end of 2 weeks of the course appointment.
The antianginal effect is due to a decrease in myocardial oxygen demand (due to a negative chronotropic and inotropic effect). A decrease in heart rate leads to a lengthening of diastole and an improvement in myocardial perfusion. Due to an increase in the end-diastolic pressure in the LV and an increase in the stretching of the muscle fibers of the ventricles, it can increase the demand for oxygen, especially in patients with CHF.
The antiarrhythmic effect is due to the elimination of arrhythmogenic factors (tachycardia, increased activity of the sympathetic nervous system, increased cAMP content, arterial hypertension), a decrease in the rate of spontaneous excitation of sinus and ectopic pacemakers, and a slowdown in AV conduction. The suppression of impulse conduction is observed mainly in the antegrade and to a lesser extent in the retrograde directions through the AV node and along additional pathways. According to the classification of antiarrhythmic drugs, it belongs to group II drugs.
Decrease in the severity of myocardial ischemia - due to a decrease in myocardial oxygen demand, postinfarction mortality can also decrease due to antiarrhythmic action.
The ability to prevent the development of vascular headache is due to a decrease in the severity of dilation of cerebral arteries due to beta-blockade of vascular receptors, inhibition of platelet aggregation and lipolysis caused by catecholamines, a decrease in platelet adhesion, prevention of activation of blood coagulation factors during the release ofblood adrenalinein tissue, stimulation of the flow ofrenin.
A decrease in tremor against the background of the use of propranolol is mainly due to the blockade of peripheral beta2-adrenergic receptors. Increases atherogenic properties of blood. Strengthens uterine contractions (spontaneous and caused by drugs that stimulate the myometrium). Increases the tone of the bronchi, in large doses causes a sedative effect.
Indications for Inderal
Essential and renal hypertension, angina pectoris, arrhythmias, migraine, anxiety, essential tremors, thyrotoxicosis, hypertrophic obstructive cardiomyopathy, pheochromocytoma (with alpha-blockers).
How to use Inderal: dosage and course of treatment
With arterial hypertension - by mouth, 40 mg 2 times a day. If the hypotensive effect is insufficient, the dose is increased to 40 mg 3 times or 80 mg 2 times a day. The maximum daily dose is 320 mg (in exceptional cases - 640 mg).
With angina pectoris, cardiac arrhythmias - at an initial dose of 20 mg 3 times a day, then the dose is gradually increased to 80-120 mg in 2-3 doses. The maximum daily dose is 240 mg.
For the prevention of migraine, as well as with essential tremor - at an initial dose of 40 mg 2-3 times a day, if necessary, the dose is gradually increased to 160 mg / day.
When using the prolonged form (depot capsules 80 mg), the frequency of administration is 1 time per day.
In case of paroxysmal cardiac arrhythmias and thyrotoxic crisis - intravenous stream, slowly, in an initial dose of 1 mg (1 ml of 0.1% solution), then after 2 minutes the same dose of the drug is administered again. In the absence of an effect, intravenous administration is repeated until a maximum dose of 10 mg is reached, under the control of blood pressure and ECG.
For obstetrics and stimulation of labor - 20 mg 4-6 times at intervals of 30 minutes (80-120 mg / day) In case of fetal hypoxia, the dose is reduced. For the prevention of postpartum complications - 20 mg 3 times a day for 3-5 days.
If liver function is impaired, dose reduction is necessary Renal dysfunction does not require dose adjustment.
Hypersensitivity, acute heart failure or decompensated heart failure, cardiogenic shock, grade II-III AV block, SA block, SSS, sinus bradycardia (heart rate less than 55 / min), Prinzmetal's angina, cardiomegaly (without signs of heart failure), arterial hypotension (systolic blood pressure less than 90 mm Hg, especially with myocardial infarction); COPD, bronchial asthma (severe course); peripheral vascular occlusive disease (complicated by gangrene, "intermittent" claudication or pain at rest), diabetes mellitus with ketoacidosis, metabolic acidosis, concomitant use of MAO inhibitors, lactation period. With caution. History of allergic reactions, CHF, pheochromocytoma, liver failure, chronic renal failure, Raynaud's syndrome, myasthenia gravis, thyrotoxicosis, depression (including a history), psoriasis, pregnancy, old age, childhood (efficacy and safety have not been determined).
Monitoring of patients taking propranolol should include monitoring of 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 mellitus (1 time in 4-5 months). In elderly patients, it is recommended to monitor renal function (1 time in 4-5 months).
The patient should be trained in the method of calculating the heart rate and instructed on the need for medical advice if the heart rate is less than 50 / min.
Before prescribing propranolol to patients with CHF (early stages),should be used digitalis and / or diuretics.
In "smokers" the effectiveness of beta-blockers is lower.
Patients using contact lenses should take into account that during treatment, it is possible to reduce the production of tear fluid.
Patients with pheochromocytoma are prescribed only after taking an alpha-blocker.
With thyrotoxicosis, propranolol can mask certain clinical signs of thyrotoxicosis (for example, tachycardia). Abrupt withdrawal in patients with thyrotoxicosis is contraindicated, since it can aggravate the 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, her symptoms such as tachycardia or tremor will be masked by the action of the drug. Patients should be instructed that the main symptom of hypoglycemia during treatment with beta-blockers is increased sweating.
With the simultaneous administration of clonidine, its reception can be stopped only a few days after the discontinuation of propranolol.
It is possible that the severity of the hypersensitivity reaction and the lack of effect from the usual doses of epinephrine against the background of a burdened allergic history are possible.
A few days before the general anesthesia with chloroform or ether, you must stop taking the drug. If the patient has taken the drug before the operation, he should choose drugs for general anesthesia with minimal negative inotropic effect.
Reciprocal activation of n.vagus can be eliminated by intravenous administration of atropine (1-2 mg).
Drugs that reduce the supply of catecholamines (for example, reserpine) can enhance the action of beta-blockers, therefore, patients taking such drug combinations should be under constant medical supervision for the detection of arterial hypotension or bradycardia.
Cannot be used simultaneously with antipsychotic drugs (neuroleptics) and anxiolytic drugs (tranquilizers).
Caution should be used in conjunction with psychoactive drugs, such as MAO inhibitors, with their course use for more than 2 weeks.
If elderly patients develop bradycardia (less than 50 / min), arterial hypotension (systolic blood pressure below 100 mm Hg), AV blockade, bronchospasm, ventricular arrhythmias, severe liver and kidney dysfunctions, it is necessary to reduce the dose or stop treatment ... It is recommended to discontinue therapy with the development of depression caused by the intake of beta-blockers.
It is impossible to abruptly interrupt treatment due to the risk of developing severe arrhythmias and myocardial infarction. Cancellation is carried out gradually, reducing the dose for 2 weeks or more (by 25% in 3-4 days).
Use during pregnancy and lactation is possible if the benefits to the mother outweigh the risk of side effects in the fetus and child. If necessary, admission during pregnancy - close monitoring of the condition of the fetus, 48-72 hours before delivery should be canceled.
Should be canceled before testing in the blood and urine of catecholamines, normetanephrine and vanilla-mandelic acid; 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 of attention and speed of psychomotor reactions.
Allergens used for immunotherapy or allergen extracts for skin tests increase the risk of severe systemic allergic reactions or anaphylaxis in patients receiving propranolol. Iodine-containing X-ray contrast drugs for intravenous administration increase the risk of developing anaphylactic reactions.
Phenytoin when administered intravenously, drugs for inhalation general anesthesia (hydrocarbon derivatives) increase the severity of the cardiodepressant effect and the likelihood of lowering blood pressure.
Changes the effectiveness of insulin and oral hypoglycemic drugs, masks the symptoms of developing hypoglycemia (tachycardia, increased blood pressure).
Reduces the clearance of lidocaine and xanthines (except diphylline) and increases their plasma concentration, especially in patients with an initially increased clearance of theophylline under the influence of smoking.
The antihypertensive effect is weakened by NSAIDs (Na + delay and blockade of Pg synthesis by the kidneys), GCS and estrogens (Na + delay).
Cardiac glycosides, methyldopa, reserpine and guanfacine, BMCC (verapamil, diltiazem), amiodarone, and other antiarrhythmic drugs increase the risk of developing or worsening bradycardia, AV blockade, cardiac arrest and heart failure. Nifedipine can lead to a significant decrease in blood pressure.
Diuretics, clonidine, sympatholytics, hydralazine, and other antihypertensive drugs can lead to an excessive decrease in blood pressure.
Prolongs the action of non-depolarizing muscle relaxants and the anticoagulant effect of coumarins.
Tri- and tetracyclic antidepressants, antipsychotic drugs (antipsychotics), ethanol, sedative and hypnotic drugs increase CNS depression.
Simultaneous use with MAO inhibitors is not recommended due to a significant increase in the hypotensive effect, the break in treatment between taking MAO inhibitors and propranolol should be at least 14 days.
Non-hydrogenated ergot alkaloids increase the risk of developing peripheral circulatory disorders.
Strengthens the effect of thyrostatic and uterotonizing drugs; reduces the effect of antihistamine drugs.
Concomitant administration with phenothiazine derivatives increases plasma concentrations of both drugs.
Sulfasalazine and cimetidine increase the concentration of propranolol in plasma (inhibit metabolism), rifampicin shortens T1 / 2.
Hallucinations, psychosis, bradycardia, thrombocytopenia, visual disturbances, withdrawal syndrome, heart failure, impaired conduction, orthostatic hypotension, cold extremities, intermittent claudication, Raynaud's syndrome, dizziness, sleep disturbance, hypoglycemia, dyspeptic disorders, psoriasis, paresthesia, alopecia.