Propranolol

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Nonselective beta-blockers . The drug has anti-arrhythmic, protivoanginalnoe, hypotensive effects. The principle of operation is based on the indiscriminate blocking beta-adrenergic receptors, to decrease the formation of cAMP from ATP stimulated catecholamines Which leads to a reduced supply of calcium ions into the cell, generated negative Drome, chrono, BATM, inotropic effects (reduced myocardial contractility, excitability and suppressed conductivity uryazhaetsya pulse).

In the early stages of treatment in the first day of PR can be increased as a result of removal of the stimulating effect of the beta-2 adrenoceptor vessels in skeletal muscle, and as a result of increased activity of reciprocal alpha-adrenoreceptor . After 1-3 days registers effect the return to the initial and long-term therapy is reduced. Hypotensive effect provided by sympathetic stimulation of peripheral receptacles, reducing IOC influence on the central nervous system, reducing the sensitivity of the baroreceptors in the aortic arch (no increased activity in response to a fall in blood pressure), a decrease in activity Renin-angiotensin system   (especially important for patients with initial hypersecretion renin). Stabilization of the antihypertensive effects achieved by the end of the second week course of therapy.

Antianginal effect is a decrease in the need of tissue infarction   oxygen (due to the negative inotropic and chronotropic effects). Reduced heart rate improves myocardial perfusion and causes elongation diastole . Due to the increase of the final diastolic pressure   in the left ventricle, enhance muscle ventricles stretching may increase in oxygen demand, especially such effect is registered in patients with chronic heart failure. Antiarrhythmic effects   achieved by the elimination of arrhythmogenic factors (hypertension, elevated levels of cAMP, increased activity of the sympathetic nervous system, tachycardia ), Deceleration atrioventricular conduction , Decrease in the rate of spontaneous excitation of the sinus and ectopic pacemakers. Oppression of the pulse is recorded mainly in the anterograde and to a lesser extent in the retrograde direction on additional ways and through the atrioventricular node.

In the classification of anti-arrhythmic medication Propranolol belongs to a drug group 2. Reducing the severity of myocardial ischemia provides a reduction in myocardial oxygen demand. Thanks antiarrhythmic effect is achieved by declines in post-infarction mortality. The drug is able to prevent the development of headaches of vascular origin by reducing the severity of the expansion of cerebral blood vessels as a result of beta-adrenoblockade receptors in blood vessels, decrease platelet adhesiveness, and inhibition of lipolysis Aggregation   platelets (under the influence of catecholamines) reducing renin secretion, enhanced stimulation of oxygen to the tissue, preventing the activation of coagulation factors during the release of adrenaline.

Use of the drug propranolol is to reduce the severity of the tremor due to blockade of circumferentially spaced beta-2 adrenoceptor agonist. The drug is able to increase the atherogenic properties of blood. The drug in high doses causes sedation , Increases the tone of the bronchi, strengthens the contraction of the walls of the uterus caused by the action of drugs that stimulate the myometrium. Propranolol is available in tablet dosage form, capsules, solution.

Indications:

Instructions for use of the drug propranolol is recommended to prescribe medication at angina , Hypertension, sinus tachycardia, unstable angina, Atrial tachyarrhythmias , Supraventricular tachycardia, myocardial infarction, alcohol withdrawal (tremor, agitation) ventricular arrhythmia , Atrial tachyarrhythmia, essential tremor , Ventricular arrhythmia, tireotoksicheskom Stroke   (auxiliary element of complex therapy) diffuse toxic goiter When sympathoadrenal crises (collateral diencephalic syndrome) with diffuse toxic goiter, pheochromocytoma , Anxiety.

Contraindications:

Propranolol is not prescribed for SA-blockade cardiogenic shock , Pregnancy, cardiomegaly, Prinzmetal angina , Sinus bradycardia, sick sinus syndrome, decompensated form of chronic heart failure, acute heart failure, intolerance of the main component in COPD, hypotension, asthma, psoriasis, myasthenia gravis, liver disease, breast feeding, diabetes with ketoacidosis, occlusive peripheral vascular disease (complicated by pain at rest, gangrene or intermittent claudication ), While receiving monoamine oxidase inhibitors, metabolic acidosis . In depression, Raynaud's syndrome , Renal disease, allergy, hyperthyroidism, children and the elderly Propranolol administered with caution.

Side effect:

Nervous system:   increased sleepiness, fatigue, "nightmarish" dreams, dizziness, weakness throughout the body, limb tremor, paresthesias in extremities   (in patients with Raynaud syndrome, " Intermittent "Claudication), depression, short-term memory impairment and going, confusion, anxiety , headache, myasthenia , Fatigue, hallucinations.

Senses: keratoconjunctivitis , Sore eyes, reducing the production of lacrimal fluid, dryness in the eyes of the visual perception.

Cardiovascular system:   arrhythmia, atrioventricular block, conduction disturbances infarction, palpitations, sinus bradycardia , Exacerbation of chronic heart failure, weakening of myocardial contractility, chest pain, symptoms Angiospasm   (Raynaud's syndrome, cold lower limbs, increased peripheral circulation disorders), drop in blood pressure, orthostatic hypotension .

The digestive tract:   change in taste perception, irregularities in the hepatic system (cholestasis, jaundice of the skin and sclera, dark urine), violations of the chair, flatulence, epigastric pain, vomiting, nausea, dry mucous membranes of the oral cavity.

Respiratory system:   bronchospasm, laryngospasm, shortness of breath, rhinitis, nasal congestion.

Endocrine system:   hypoglycemia (in patients who receive insulin), decreased thyroid function, hyperglycemia (in patients with non-insulin dependent diabetes).

Allergic reactions: hives , Rashes on the skin, itching.

Skin:   exacerbation of psoriasis, psoriasis-like skin rash, alopecia, rash, flushing of the skin, sweating.

Laboratory findings : Increased liver enzymes, thrombocytopenia (uncharacteristic bleeding, bleeding) leukopenia , Agranulocytosis, hyperbilirubinemia.

Effect of propranolol on the fetus : Bradycardia, hypoglycemia, intrauterine growth retardation.

Other possible side effects : Weakening of libido, arthralgia , Back pain, the formation of the syndrome of "cancellation" in the form of high blood pressure, increased severity and frequency of angina attacks.

Overdose:

Manifested bronchospasm fainting , Cyanosis of nail plates on the fingers, ventricular premature beats, severe bradycardia, heart failure, seizures, arrhythmias, severe drop in blood pressure, atrioventricular block, dizziness. Treatment includes the administration of enterosorbents, if necessary - gastric lavage. If ventricular arrhythmia prescribe lidocaine (impermissible use of drugs class Ia).

In case of violation atrioventricular conduction   intravenous 1-2 mg of atropine, the ineffectiveness establish temporary elektrokardiostimultor. In case of a fall in blood pressure of a patient give Tredelenburga posture. When bronchospasm parenteral or inhaled beta adrenostimulyatorov apply. In convulsions shown intravenous diazepam. With the development of heart failure prescribed diuretic medications cardiac glycosides , Glucagon. Plazmozameschayuschie solutions can be administered in the absence of signs of pulmonary edema. In case of failure administered dopamine, epinephrine, dobutamine .

Mode of application:

Cardiac arrhythmias, angina pectoris:   three times a day to 20 mg; gradually increase the dose to 120 mg of (2-3 hours). The maximum daily dose is 240 mg. Hypertension:   twice daily at 40 mg. When failure, weak effect amount of propranolol was increased to 80 mg (2 times per day) or 40 mg (three times daily). The maximum daily dosage of medication is 320 mg (heavy, exceptional cases - 640 mg).   Essential tremor, prevention migraine :   initial amount - 40 mg 2-3 times a day, after the dosage was increased to 160 mg per day. Long-acting forms of medication (depot capsules 80 mg) taken 1 time a day.

Thyrotoxic crisis, paroxysmal cardiac arrhythmias : Intravenous, slow in the initial bolus dose of 1 mg (1 ml of 0, 1%), after 2 minutes the procedure was repeated. When failure amount of medicament administered intravenously, increased to 10 mg binding under the control of ECG and blood pressure levels. Induction of labor, childbirth: propranolol 20 mg 4-6 times at intervals of 30 minutes (80-120mg daily amount). With fetal hypoxia   reduce the dosage. In the pathology of renal dose adjustment is required. In diseases of the liver is necessary to reduce the amount of the drug. In order to prevent obstetric complications medicament administered 20 mg three times a day. The course of 3-5 days.

Special instructions:

Patients taking propranolol requires regular monitoring blood sugar ECG, blood pressure, pulse. The elderly need to control the state of the renal system. The attending doctor is necessary to teach the patient to self-rate control technology. Before treatment, patients with chronic heart failure at an early stage appointed diuretic medications , Digitalis. Decreased effectiveness of the drug at the "smokers". Patients who use contact lenses should be aware of reduced production lacrimal fluid while taking the drug propranolol.

At diagnosis " pheochromocytoma "Drug may be prescribed only after receiving alpha-blockers. Unacceptable abrupt withdrawal of the drug in patients with hyperthyroidism due to the risk of increasing the severity of symptoms. It is important to bear in mind that propranolol on the background of hyperthyroidism may mask clinical signs of disease. Care must be taken in the treatment of beta-blocker patients who take hypoglycemic medications (possible hypoglycemia during long breaks).

Signs hypoglycemia   (tremor, tachycardia) may be masked by the action of propranolol. Patients should be aware that the main feature of hypoglycemia while taking beta-blockers is hyperhidrosis , Sweating. Taking medication is stopped for a few days before the general anesthesia with ether, chloroform. In that case, if the patient received propranolol before surgery, then he picked up a medicament for general anesthesia, which are the least pronounced negative inotropic effect . Reciprocal vagal activation persists intravenous atropine in an amount of 1-2 mg. Medicines that reduce stocks of catecholamines ( reserpine   and others) increase the impact of yueta-blockers, which requires constant monitoring of the patient by the physician for the early detection of bradycardia and hypotension. It is unacceptable the simultaneous use of tranquilizers (anxiolytics) neuroleptics   (antipsychotics). With care prescribe MAO inhibitors, psychoactive medications (for course therapy for more than 2 weeks).

In identifying the elderly ventricular arrhythmias, bronchospasm, atrioventricular block, hypotension , Increasing bradycardia, severe kidney or liver disease, or reduce the dosage of propranolol drug overturned. With the development of depression during treatment with a beta-blocker drug is replaced. Unacceptable abrupt withdrawal of the drug because of the risk of myocardial infarction, severe arrhythmias. The medicament shall be progressively reduced within two weeks, once every three days to reduce the dosage of 25%.

Propranolol during pregnancy and breastfeeding is prescribed in exceptional cases, if the benefit justifies the potential risk. In the treatment during gestation pregnancy requires careful monitoring of the fetus and the mother. The drug is cancel 48-72 hours before delivery. Before determining the level normetanephrine, catecholamines, antinuclear antibodies, vanillylmandelic acid   drug overturned. Propranolol affects the concentration and the ability to drive vehicles.

Drug Interactions:

The extracts of allergens for skin testing, and allergens themselves, used for Immunotherapy It may increase the likelihood of developing severe allergic reactions or systemic nature of anaphylaxis in patients who are taking propranolol. Radiopaque medications based on intravenous administration of iodine increases the risk of anaphylaxis . The probability of falling blood pressure, severity cardiodepressive action   increased by intravenous administration of phenytoin and inhaled medicines for general anesthesia (derivatives of hydrocarbons).

Proparnolol affect the effectiveness of oral hypoglycemic agents, insulin And is able to mask the symptoms of hypoglycemia emerging as hypertension and tachycardia. The drug increases the concentration xanthine   (the exception is dyphylline) lidocaine in the blood plasma, reducing their clearance. This effect was more pronounced in patients with initially high theophylline clearance in the background smoking. NSAIDs weaken hypotensive effect of the drug (the blockade of prostaglandin synthesis of renal system, the delay of sodium ions in the body).

Antiarrhythmics, amiodarone, BCCI (diltiazem, verapamil), guanfacine, reserpine, methyldopa, cardiac glycosides aggravate heart failure, atrioventricular block, bradycardia, can cause cardiac arrest. Simultaneous treatment with nifedipine causes a significant drop in blood pressure. Antihypertensives, sympatholytic, dirueticheskie agents, hydralazine, clonidine cherzemernomu lead to lower blood pressure. Propranolol is capable of extending anticoagulant effect   coumarin and non-depolarizing muscle relaxants. Hypnotics, sedatives, natipsihoticheskie (neuroleptics) Funds tetracyclic antidepressants , Tricyclic antidepressants increase the depressant effect on the central nervous system. It is recommended to make a break between taking propranolol and MAO inhibitors for at least 2 weeks; concomitant use of these medications is not valid because of a significant increase in the hypotensive effect.

Propranolol and enhances the action of uterotoniziruyuschih thyreostatic drug inhibits the action antihistamine medication . Non-hydrogenated ergot alkaloids increase the severity of pathology of the peripheral circulation. When concurrent therapy phenothiazine derivatives marked increase in the concentration of both drugs in blood plasma. Rifampicin shortens the half-life, as cimetidine and sulfasalazine slows metabolic processes by increasing the concentration of propranolol in the plasma.