Overview
A drug
Propranolol - antiarrhythmic, antianginal, hypotensive, uterotonizing drug that blocks beta1 and beta2-adrenergic receptors, has a membrane-stabilizing effect.
Inhibits the automatism of the sinoatrial node, suppresses the occurrence of ectopic foci in the atria, AV connection, ventricles (to a lesser extent).
Reduces the speed of the excitation in the AV connection along the Kent beam, mainly in the anterograde direction. Reduces heart rate, reduces heart rate and myocardial oxygen demand.
Reduces cardiac output, renin secretion, blood pressure, renal blood flow and glomerular filtration rate. Suppresses the reaction of baroreceptors of the aortic arch to lower 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 at the end of the 2nd week of treatment.
With prolonged use, it reduces venous return, has a cardioprotective effect (significantly reduces the risk of repeated myocardial infarction and sudden death by 20-50%).
In patients with moderate form of arterial hypertension - reduces the likelihood of developing coronary artery disease and cerebral strokes. With coronary heart disease, it reduces the frequency of seizures, increases the tolerance of physical activity, and lowers the need for nitroglycerin. It is most effective in patients of a young age (up to 40 years) with hyperdynamic type of blood circulation and with an increased content of renin.
It increases the tone of the bronchi and contractility of the uterus (reduces bleeding during childbirth and in the postoperative period), increases the secretory and motor activity of the gastrointestinal tract.
Inhibits platelet aggregation and activates fibrinolysis.
It inhibits lipolysis in adipose tissue, preventing an increase in the level of free fatty acids (while the concentration Blockonol triglycerides in the plasma and the atherogenic coefficient increase.
Suppresses glycogenolysis, secretion of glucagon and insulin, the conversion of thyroxine to triiodothyronine.
Reduces intraocular pressure, reduces the secretion of aqueous humor.
Pharmacokinetics
Cmax in plasma is observed after 1-1.5 hours or 6 hours (for prolonged form).
It binds to plasma proteins by 90–95%; T1 / 2 is 2–5 hours (10 hours for a prolonged form). Distribution volume - 3-5 l / kg. It accumulates in the lung tissue, brain, for example, heart, passes through the placental barrier, penetrates into breast milk. Subjected to glucuronidation in the liver (99%).
It is excreted in the intestines with bile, deglucuronized and reabsorbed (T1 / 2 against the background of course administration can be extended up to 12 hours). Excreted by the kidneys in the form of metabolites.
Indications for use
Indications for use of the drug Propranolol are: arrhythmia, arterial hypertension, coronary heart disease, hypertrophic cardiomyopathy, myocardial dystrophy, neurocirculatory dystonia, thyrotoxicosis, cirrhosis of the liver, withdrawal syndrome, migraine (prevention), weakness of labor.
Mode of application
Pills Propranolol taken orally, with hypertension - 40 mg 2 times a day, gradually increasing the dose to 160-480 mg in 2 divided doses; with angina pectoris and migraine - 20 mg 4 times a day, then - up to 40 mg per reception; with arrhythmias, cardiomyopathy, thyrotoxicosis - 10–40 mg 3-4 times a day.
Side effects
From the cardiovascular system and blood (hematopoiesis, hemostasis): bradycardia, heart failure, AV block, hypotension, impaired peripheral circulation, thrombocytopenic purpura, leukopenia, agranulocytosis.
From the nervous system and sensory organs: asthenia, dizziness, headache, insomnia, drowsiness, nightmares, decreased 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.
From the respiratory system: pharyngitis, chest pain, cough, shortness of breath, bronchus and laryngospasm, respiratory distress syndrome.
From the skin: alopecia, Blockonol, itching, exacerbation of psoriasis.
Other: withdrawal syndrome, weakening of libido, impotence, Peyronie's disease, arthralgia, allergic reactions, lupus syndrome, hypoglycemia, fever.
Contraindications
Contraindications to the use of the drug Propranolol are: uncompensated heart failure, bronchial asthma, bradycardia, hypotension, peripheral circulatory disorders, Raynaud's disease, insulin therapy, treatment with MAO inhibitors.
Pregnancy
Drug use Propranolol possibly if the expected effect of therapy exceeds the potential risk to the fetus. Breastfeeding should be discontinued during treatment.
Interactions with other drugs:
Propranolol enhances the (mutually) negative effect of verapamil and diltiazem on the myocardium, prolongs the action of non-depolarizing muscle relaxants, and inhibits the excretion of lidocaine.
Weaken the hypotensive effect of NSAIDs, glucocorticoids, estrogens, cocaine; strengthen - nitrates and other antihypertensive agents. Heparin, antacids lower plasma levels; cimetidine and phenothiazines - increase.
Concomitant use with MAO inhibitors is not recommended.
Slows down theophylline metabolism and increases its concentration in blood plasma.
Overdose
Symptoms of a drug overdose Propranolol: dizziness, bradycardia, arrhythmia, heart failure, hypotension, collapse, shortness of breath, acrocyanosis, convulsions.
Treatment: gastric lavage and the use of adsorbing agents, symptomatic therapy: atropine, beta-adrenergic agonists (isoprenaline, isadrin), sedatives (diazepam, lorazepam), cardiotonic (dobutamine, dopamine, epinephrine) vasopressor drugs, glucagon, etc .; transvenous stimulation is possible. Hemodialysis is ineffective.
Storage conditions
A drug Propranolol should be stored in a dry place inaccessible to children at room temperature.
Release form
Propranolol - tablets of 0.01 and 0.04 g and 0.08 g (10, 40 and 80 mg).
0.1% solution in ampoules of 5 ml;
0.25% solution in ampoules of 1 ml.
Latin name: Propranolol
ATX Code: C07AA05
Active substance: propranolol
Producer: Weimer Pharma GmbH (Germany), Vector (Russia)
Description overdue on: 12.10.17
Propranolol is a non-selective beta-blocker with antihypertensive, antiarrhythmic and antianginal effects.
