NameInaprilin tabl. Composition One tablet contains: active ingredient – propranolol hydrochloride – 40 mg; excipients: sucrose, potato starch, talc, calcium stearate. Pharmacotherapeutic group Non-selective ?-blockers. ATX code: C07AA05. Pharmacological properties Pharmacodynamics Anaprilin blocks ?1- and ?2-adrenergic receptors. Due to the decrease in sympathetic influences on ?1-adrenergic receptors of the heart, a decrease in the strength and frequency of its contractions, inhibition of excitability and conduction is observed. Reduces the secretion of renin. In connection with the blockade of α2-adrenergic receptors, propranolol increases the tone of the bronchi, the contractile activity of the myometrium, constricts blood vessels (including coronary), reduces the hyperglycemic effect of adrenaline. It has antianginal, hypotensive and antiarrhythmic action. Pharmacokinetics After oral administration, it is absorbed quickly and fairly completely (90%). The maximum concentration of the drug (Cmax) in the blood plasma is reached after 1-1.5 hours. Bioavailability after a single oral intake is 30-40% (the effect of “first pass” through the liver), with prolonged use it increases (metabolites are formed, inhibitory liver enzymes). It has a high lipophilicity, accumulates in the tissue of the lungs, brain, kidneys, heart. Penetrates through the blood-brain and placental barriers, into breast milk. Communication with blood plasma proteins – 90-95%. Biotransformed in the liver by glucuronidation. It enters the intestine with bile, is deglucuronized and reabsorbed. Relatively quickly excreted from the body. The half-life of the drug (T1 / 2) is 3-5 hours, against the background of a course administration, it can be extended up to 12 hours. Excreted in the urine – 90%, unchanged – less than 1%. Not removed by hemodialysis. Indications for use Arterial hypertension; angina; essential tremor; in the complex therapy of thyrotoxicosis, anxiety disorders; migraine prevention. Dosage and administration Assign inside after meals. With arterial hypertension – 40 mg 2 times a day. With insufficient severity of the effect, the dose is increased to 40 mg 3 times or 80 mg 2 times a day. Dose adjustment is carried out after a week of taking the previous dose. The maximum daily dose is 320 mg. With angina – at an initial dose of 20 mg 3 times a day, then with a weekly interval, the dose is gradually increased to 80-120 mg in 2-3 doses. The maximum daily dose is 240 mg. For anxiety disorders: a dose of 40 mg per day can be used to relieve the state of situational anxiety. Long-term treatment of generalized anxiety disorder should be initiated at a dose of 40 mg twice daily, which may be increased to 40 mg three times daily if necessary. The duration of treatment will be determined by the response to the treatment. After six months, treatment should be reviewed. For the prevention of migraine, as well as for essential tremor – at an initial dose of 40 mg 2-3 times a day, if necessary, gradually increasing to 160 mg / day. In the treatment of thyrotoxicosis, the drug is started with 40 mg 3-4 times a day. In the future, the dose is increased every 3-4 days to the optimum, allowing you to control the heart rate in the range of 60-90 beats per minute. The maximum daily dose is 160 mg / day. In case of impaired liver function, dose reduction is necessary. Impaired renal function does not require dose adjustment. Children This drug is not used in pediatric practice. Contraindications Hypersensitivity, childhood, cardiogenic shock, acute myocardial infarction, sick sinus syndrome, Prinzmetal’s angina, decompensated circulatory failure, sinus bradycardia (heart rate less than 55 beats / min), incomplete or complete atrioventricular block, severe right and left ventricular heart failure, arterial hypotension (systolic blood pressure less than 90 mm Hg), bronchial asthma, hay fever, tendency to bronchospasm, history of bronchospasm attacks, diabetes mellitus with ketoacidosis, arterial peripheral blood flow disorders, spastic colitis. With caution Chronic obstructive pulmonary disease, bronchitis, diabetes mellitus (danger of hypoglycemia when taken simultaneously with hypoglycemic agents), renal and / or hepatic insufficiency, hyperthyroidism, depression, myasthenia gravis, pheochromocytoma, psoriasis, peripheral vascular occlusive diseases, pregnancy, lactation, elderly age, children’s age (efficacy and safety have not been determined). Undesirable reactions From the nervous system: fatigue, weakness, dizziness, headache, drowsiness or insomnia, nightmares, depression, memory loss, confusion, hallucinations, tremor, nervousness, anxiety. From the sensory organs: impaired visual acuity, decreased secretion of lacrimal fluid, dryness and soreness of the eyes, keratoconjunctivitis. From the side of the cardiovascular system: sinus bradycardia, atrioventricular blockade, arrhythmias, development (decompensation) of chronic heart failure, lowering blood pressure, orthostatic hypotension, angiospasm (increased peripheral circulatory disorders, coldness of the lower extremities, Raynaud’s syndrome) , chest pain. On the part of the digestive system: nausea, vomiting, discomfort in the epigastric region, constipation or diarrhea, abnormal liver function (cholestasis), taste changes, mesenteric thrombosis, ischemic colitis. From the respiratory system: nasal congestion, pharyngitis, cough, shortness of breath, respiratory distress syndrome, bronchospasm and laryngospasm. From the endocrine system: hypo- or hyperglycemia. Allergic reactions: itching, skin rash, urticaria. On the part of the skin and its derivatives: increased sweating, psoriasis-like skin reactions, exacerbation of symptoms of psoriasis, alopecia. From the blood system: thrombocytopenia, thrombocytopenic purpura, leukopenia, agranulocytosis. Laboratory indicators: thrombocytopenia (bleeding and hemorrhage), leukopenia, increased activity of transaminases, lactate dehydrogenase. Effect on the fetus: intrauterine growth retardation, hypoglycemia, bradycardia. Others: back pain, arthralgia, decreased potency, “withdrawal” syndrome (increased angina attacks, myocardial infarction, increased blood pressure), fever, Peyronie’s disease, myasthenia gravis. Treatment of complications With the development of side effects, especially persistent bradycardia, atropine sulfate (1–2 mg) or ?-agonists are slowly injected intravenously. Moderate bradycardia that occurs during treatment is not an indication for withdrawal; with severe bradycardia, the dose should be reduced. Interaction with other drugs When using the drug with monoamine oxidase inhibitors, a significant increase in the hypotensive effect is observed, this combination is contraindicated; the break in treatment between taking monoamine oxidase inhibitors and Anaprilin should be at least 14 days. With simultaneous use with diuretics, reserpine, hydralazine, nifedipine and other antihypertensive drugs, as well as ethanol, the hypotensive effect of Anaprilin is enhanced. Simultaneous use with rizatriptan leads to an increase in its concentration in the blood and requires dose adjustment of rizatriptan downward. The hypotensive effect of the drug is weakened by glucocorticoids, non-steroidal anti-inflammatory drugs (sodium retention and a decrease in prostaglandin synthesis in the kidneys), estrogens (sodium retention). Anaprilin enhances the effect of thyreostatic and uterotonic drugs; reduces the effect of antihistamines. When used simultaneously with amiodarone, verapamil and diltiazem, it enhances the severity of negative chrono-, ino- and dromotropic effects. With intravenous administration of iodine-containing radiopaque drugs, the risk of developing anaphylactic reactions increases. Phenytoin when administered intravenously, agents for inhalation anesthesia (derivatives of hydrocarbons), when used simultaneously with Anaprilin, increase the severity of the cardiodepressive effect and the likelihood of lowering blood pressure. Anaprilin, with simultaneous use, changes the effectiveness of insulin and oral hypoglycemic drugs, masks the symptoms of developing hypoglycemia (tachycardia, increased blood pressure). Cardiac glycosides, methyldopa, reserpine and guanfacine, antiarrhythmic drugs, when taken simultaneously with Anaprilin, increase the risk of developing or exacerbating bradycardia, atrioventricular block, cardiac arrest and heart failure. Anaprilin prolongs the action of non-depolarizing muscle relaxants and the anticoagulant effect of coumarins. Tri- and tetracyclic antidepressants, antipsychotic drugs (neuroleptics), ethanol, sedative and hypnotic drugs increase the inhibitory effect of propranolol on the central nervous system. Ergot alkaloids, when used simultaneously with Anaprilin, increase the risk of developing peripheral circulatory disorders. Anaprilin increases the likelihood of developing severe systemic reactions (anaphylaxis) against the background of the introduction of allergens used for immunotherapy or for skin tests. Cimetidine, sulfasalazine increase the bioavailability of Anaprilin. Anaprilin increases the concentration of lidocaine, phenothiazine antipsychotics in blood plasma, reduces the clearance of theophylline. Precautions Control over patients should include monitoring of heart rate and blood pressure (at the beginning of treatment – daily, then 1 time in 3-4 months), electrocardiogram, blood glucose concentration in patients with diabetes mellitus (1 time in 4-5 months) . In elderly patients, it is recommended to monitor kidney function (1 time in 4-5 months). A medical consultation is necessary if the heart rate is less than 50 beats / min while taking Anaprilin. Treatment of coronary heart disease and arterial hypertension should be long-term. Termination of drug treatment is carried out gradually (reducing the dose by 25% every 3-4 days): abrupt cancellation can increase anginal syndrome and myocardial ischemia, worsen exercise tolerance, change the rheological properties of blood, etc. In patients with diabetes mellitus, the use of the drug is carried out under the control of blood glucose levels due to the risk of developing hypoglycemia without a characteristic clinical picture. Patients should be instructed that the main symptom of hypoglycemia during treatment with ?-blockers is increased sweating. Patients with chronic heart failure (early stages) should use Anaprilin during therapy with diuretics or angiotensin-converting enzyme inhibitors, cardiac glycosides under close medical supervision. When smoking, the effectiveness of ?-blockers is lower. Patients using contact lenses should take into account that during treatment, a decrease in the production of lacrimal fluid is possible. Patients with pheochromocytoma are prescribed only after taking a β-blocker. With thyrotoxicosis, Anaprilin can mask the clinical signs of thyrotoxicosis (for example, tachycardia). Abrupt withdrawal in patients with thyrotoxicosis is contraindicated, as it can exacerbate symptoms. With the simultaneous administration of clonidine, its administration can be stopped only a few days after the withdrawal of Anaprilin. Sympatholytics (for example, reserpine) may enhance the effect of ?-blockers, such patients should be under constant medical supervision to detect arterial hypotension or bradycardia. In case of increasing bradycardia (less than 50 beats / min), arterial hypotension (systolic blood pressure below 100 mm Hg), atrioventricular blockades, bronchospasm, ventricular arrhythmias, severe violations of the liver and kidneys, it is necessary to may reduce the dose or stop treatment. It is recommended to stop therapy with the development of depression caused by taking ?-blockers. It should be canceled before the study of the level of catecholamines in the blood and urine; titers of antinuclear antibodies. Propranolol is contraindicated in severe peripheral circulatory disorders; use for less severe peripheral circulatory disorders may lead to a worsening of the condition. Propranolol should be used with caution in patients with first degree AV block as a result of the drug’s negative effect on conduction time. Propranolol should be used with caution in patients with decompensated liver cirrhosis. In patients with severe impairment of liver or kidney function, propranolol is used with caution and the selection of the initial dose. In patients with renal insufficiency, the interval between doses of the drug should be increased or the dose of propranolol should be reduced to avoid accumulation of the drug. Patients with portal hypertension may have impaired liver function and develop hepatic encephalopathy. The use of propranolol in such cases may increase the risk of developing hepatic encephalopathy. When conducting anesthesia against the background of the use of propranolol, caution is needed. It is necessary to inform the anesthesiologist and select an anesthetic agent with as little negative inotropic effect as possible. Just like other ?-adrenolytic drugs, propranolol can increase both sensitivity to allergens and exacerbate anaphylactic reactions. Adrenaline does not always give the desired therapeutic result in patients treated with β-adrenergic drugs. This medicinal product is contraindicated in patients with rare hereditary fructose intolerance or glucose-galactose malabsorption. Use during pregnancy or lactation Use during pregnancy is not possible, unless the expected therapeutic effect for the pregnant woman outweighs the potential risk to the fetus. There is no evidence of teratogenicity of propranolol. However, ? ? blockers reduce placental perfusion, which can lead to intrauterine fetal death, early and premature births. In addition, adverse reactions may occur, especially hypoglycemia and bradycardia in neonates and fetal bradycardia. There is an increased risk of cardiac and pulmonary complications in newborns in the postpartum period. Most ?-blockers, especially lipophilic compounds, can pass into breast milk. As a result, it is recommended to stop breastfeeding during the period of use of the drug. The ability to influence the reaction rate when driving vehicles or other mechanisms Drivers of vehicles, operators, while taking the drug, may have a weakening of attention and a decrease in the reaction rate. Overdose Symptoms: fainting, ventricular extrasystole, arrhythmias, heart failure, bradycardia, dizziness, lowering blood pressure, shortness of breath, cyanosis of fingernails or palms, convulsions. Treatment: gastric lavage, administration of activated charcoal (when taken orally); in violation of atrioventricular conduction – in / in 1-2 mg of atropine, epinephrine, with low efficiency, a temporary pacemaker is placed; with ventricular extrasystole – lidocaine (class IA drugs are not used); in case of arterial hypotension, the patient should be in the supine position with the head end of the bed lowered, if ineffective – epinephrine, dopamine, dobutamine; with convulsions – in / in diazepam; with bronchospasm – inhalation or parenteral?-Adrenergic stimulants. Upakovka10 tablets in a blister pack of PVC film and aluminum foil. 1, 3 or 5 blisters together with a leaflet in a pack of cardboard (No. 10×1, No. 10×3, No. 10×5). Storage conditions In a place protected from light and moisture, at a temperature not exceeding 25? Keep out of the reach of children. Shelf life 4 years. Do not use after the expiration date. Conditions for dispensing from pharmacies By prescription. Buy Anaprilin tablets 40 mg No. 10×5 Price for Anaprilin tablets 40 mg No. 10×5
INN | PROPRANOLOL |
---|---|
The code | 19 303 |
Barcode | 4 810 201 002 538 |
Dosage | 40mg |
Active substance | propranolol |
Manufacturer | Borisov plant of medical preparations, Belarus |
Reviews
There are no reviews yet.