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|InnoPran XL 80 mg|
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|InnoPran XL 60 mg|
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Pharmacology of the drug InnoPran XL
Pharmacological action - antianginal, hypotensive, antiarrhythmic, uterotonic.
Blocks beta1 and beta2-adrenergic receptors, has a membrane stabilizing effect. Oppresses the automatism of the sinoatrial node, suppresses the occurrence of ectopic foci in the atria, AV junction, ventricles (to a lesser extent). Reduces the rate of conduction of excitation in the AV connection along the Kent's beam, mainly in the anterograde direction. Decreases heart rate, reduces the force of heart contractions and myocardial oxygen demand. Reduces cardiac output, renin secretion, blood pressure, renal blood flow and glomerular filtration rate. Suppresses the reaction of the aortic arch baroreceptors to lowering blood pressure.
After taking a single dose, the hypotensive effect lasts 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 prolonged use, it reduces venous return, has a cardioprotective effect (reliably reduces the risk of repeated myocardial infarction and sudden death by 20-50%). In patients with a moderate form of arterial hypertension, it reduces the likelihood of developing coronary artery disease and cerebral strokes. With ischemic heart 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 an increased content of renin. 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. It 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 coefficient of atherogenicity increase. Suppresses glycogenolysis, secretion of glucagon and insulin, conversion of thyroxine into triiodothyronine. Reduces intraocular pressure, reduces the secretion of aqueous humor
(Prolonged 18. mes) to rats and mice of doses up to 150 mg / kg / day revealed no carcinogenic properties and adverse effects on fertility. at a dose of 150 mg / kg / day, 10 times the MRDC, provided embryotoxic effects (increase in the incidence of fetal resorption).
When ingestion is rapidly and almost completely absorbed from the gastrointestinal tract (90%) Bioavailability is 30-40% ("first pass" effect), depends on the nature of the food and the intensity of hepatic blood flow and increases with prolonged use (formed metabolites that inhibit liver enzymes). Cmax in plasma is observed after 1-1.5 hours or 6 hours (for prolonged-release form). plasma lacquers by 90–95%; T1/2 is 2-5 hours (10 hours for a prolonged form). The volume of distribution is 3-5 l / kg. It accumulates in lung tissue, brain, kidneys, heart, passes through the placental barrier, and enters breast milk. Undergoes glucuronidation in the liver (99%). It is excreted with bile into the intestines, deglucuronized and reabsorbed (T1/2 against the background of a course of administration can lengthen up to 12 hours). Excreted by the kidneys as metabolites.
Application of the substance InnoPran XL
Arterial hypertension, angina pectoris, sinus tachycardia (including with hyperthyroidism), supraventricular tachycardia, tachysystolic form of atrial fibrillation, supraventricular and ventricular extrasystole, mytrophic cardiomyopathy, mitochondrial crisis, angina pectoris, angina pectoris diencephalic syndrome, neurocirculatory dystonia, portal hypertension, essential tremor, panic attacks, aggressive behavior, migraine (prevention), adjuvant treatment for pheochromocytoma (only in combination with alpha-blockers), thyrotoxicosis (including preoperative preparation), thyrotoxicosis , primary weakness of labor, menopausal vasomotor symptoms, withdrawal symptoms; treatment of akathisia caused by neuroleptics.
Arterial hypertension, angina pectoris, sinus tachycardia (including with hyperthyroidism), supraventricular tachycardia, tachysystolic form of atrial fibrillation, supraventricular and ventricular extrasystole, hypertrophic cardiomyopathy, myocardial infarction, myocardial infarction, patients with myocardial infarction syndrome, neurocirculatory dystonia, portal hypertension, essential tremor, panic attacks, aggressive behavior, migraine (prevention), adjuvant treatment for pheochromocytoma (only in combination with alpha-blockers), thyrotoxicosis (including preoperative preparation), thyrotoxic crisis, primary weakness of labor, menopausal vasomotor symptoms, withdrawal symptoms; treatment of akathisia caused by neuroleptics.
Dosage and administrationof the drug Propranolol
Inside before meals, drinking liquid or semi-liquid food (water, juice, applesauce, pudding), adults: with arterial hypertension - an initial dose of 80 mg 2 times a day, a maintenance dose of 160-320 mg. Prolonged-release forms: 80 mg once a day, if necessary up to 120-160 mg once, under the control of blood pressure. With arrhythmias - 10-30 mg 3-4 times a day, with subaortic stenosis - 20-40 mg 3-4 times a day. For portal hypertension, angina pectoris, migraine, agitation, tremor, the initial dose is 40 mg 2-3 times a day, the maintenance dose is 160, 120-240, 80-160, 80-120, 80-160 mg / day, respectively. With pheochromocytoma - 30-60 mg / day for 3 days (before surgery). With myocardial infarction - in the period from 5 to 21 days after a heart attack, 40 mg 4 times a day for 2-3 days, then - 80 mg 2 times a day. To stimulate labor - 20 mg every 30 minutes 4-6 times (80-120 mg / day), for the prevention of postpartum bleeding - 20 mg 3 times a day for 3-5 days. With glaucoma - intraconjunctivally into the affected eye.
Children: by mouth, initial dose: 0.5-1 mg / kg / day, maintenance dose - 2-4 mg / kg / day in 2 divided doses.
Hypersensitivity, II – III degree AV block, sinoatrial block, bradycardia (less than 55 beats / min), sick sinus syndrome, arterial hypotension, acute and severe chronic heart failure, Prinzmetal angina, cardiogenic shock, obliterating vascular diseases, bronchial asthma.
Restrictions on use
Chronic bronchitis, emphysema, diabetes mellitus, hypoglycemia, acidosis, impaired liver and kidney function, psoriasis, spastic colitis, myasthenia gravis, pregnancy, breastfeeding, old age.
Application during pregnancy and lactation
Possibly if the expected effect of therapy outweighs the potential risk to the fetus. During treatment, breastfeeding should be discontinued.
Symptoms: dizziness, bradycardia, arrhythmia, heart failure, hypotension, collapse, difficulty breathing, acrocyanosis, convulsions.
Treatment: gastric lavage and the appointment of adsorbing agents, symptomatic therapy: atropine, beta-adrenomimetics (isoprenaline, izadrin), sedatives (diazepam, lorazepam), cardiotonic (dobutamine, dopamine, epinephrine) drugs, vasopressor agents, glucagon, etc.; it is possible to carry out transvenous stimulation. Hemodialysis is ineffective.
Precautions for the substance Propranolol
Treatment should be carried out with regular medical supervision. With prolonged 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 the anesthesia, you must stop taking or choose an anesthetic with the least negative inotropic effect. Intravenous administration is not recommended for children. Elderly patients are at increased risk of CNS side effects. In case of impaired liver function, dose reduction and observation in the first 4 days of therapy are recommended. It can 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 and the lack of effect from the usual doses of epinephrine against the background of a burdened allergic history are possible. During treatment, it is recommended to exclude the use of alcoholic beverages. Use with caution during work for drivers of vehicles and people whose profession is associated with increased concentration of attention. Stop treatment gradually, over a period of about 2 weeks.
During treatment, it is possible to change the test results during laboratory tests (increased levels of urea, transaminases, phosphatases, LDH).
Side effects of the substance Propranolol
From the side of the cardiovascular system and blood (hematopoiesis, hemostasis): bradycardia, heart failure, AV blockade, hypotension, impaired peripheral circulation, thrombocytopenic purpura, leukopenia, agranulocytosis.
From the nervous system and sensory organs: asthenia, dizziness, headache, insomnia, drowsiness, nightmares, a decrease in the speed of mental and motor reactions, emotional lability, depression, agitation, hallucinations, disorientation in time and space, short-term amnesia, impaired sensitivity, paresthesia; dry eyes, visual disturbances, keratoconjunctivitis.
From the digestive tract: nausea, vomiting, abdominal pain, diarrhea or constipation, mesenteric artery thrombosis, ischemic colitis.
Respiratory system: pharyngitis, chest pain, cough, shortness of breath, broncho- and laryngospasm, respiratory distress syndrome.
On the part of the skin: alopecia, rash, itching, exacerbation of psoriasis.
Others: withdrawal syndrome, weakening of libido, impotence, Peyronie's disease, arthralgia, allergic reactions, lupus syndrome, hypoglycemia, fever.