2010/06/16

Obsidan

Composition, structure and packing

The tablets are white, round, beveled edges, with the risk on one side, on one side risks stamped "4", on the other - "0", the second side of the tablet is smooth.

1 tab. propranolol hydrochloride 40 mg

Excipients: lactose monohydrate, potato starch, talc, sodium karboksimetilkrahmal (type A), gelatin, magnesium stearate, silicon dioxide highly dispersed.

20 pcs. - Blisters (3) - packs cardboard.

Clinico-pharmacological group:

Beta 1 -, beta 2-blocker

Registration № №: pi. 40 mg: 60 pcs. - P № 011665/01, 08.09.06

Pharmacological action

Nonselective beta-blocker. Possesses antianginal, antihypertensive and antiarrhythmic action. Selectively blocking β-adrenergic receptors (75% β1-adrenergic receptors and 25% β2-adrenergic receptors), decreases catecholamines stimulated formation of cAMP from ATP, resulting in reduced intracellular calcium intake has a negative chrono-, Drome, BATM-and inotropic effects (slows heart rate, depresses conduction and excitability, reduces myocardial contractility).

In the first 24 hours of the drug increases TPVR (as a result of reciprocal increase in the activity of α-adrenoceptor stimulation and removal of β2-adrenoceptor vessels of skeletal muscle), but after 1-3 days, returned to baseline, and at long assignment decreases.

Antihypertensive effect of the drug is associated with a decrease in cardiac output, decrease in sympathetic stimulation of peripheral blood vessels, decreased activity of the renin-angiotensin system (counts in patients with initial hypersecretion of renin), decrease the sensitivity of baroreceptors of the aortic arch (not going to enhance their activity in response to BP decrease) and the impact on the CNS. Antihypertensive effect will stabilize by the end of 2 weeks localizer destination.

Antianginal is due to reduced myocardial oxygen demand (due to the negative chronotropic and inotropic effect). The decrease in heart rate leads to a lengthening of diastole and improve myocardial perfusion. Due to increasing end-diastolic pressure in the left ventricle and increase the tension of muscle fibers of the ventricles can increase oxygen demand, especially in patients with chronic heart failure.

Antiarrhythmic effect is due to the elimination of arrhythmogenic factors (tachycardia, increased activity of the sympathetic nervous system, increase of cAMP, arterial hypertension), decrease in the rate of spontaneous excitation of sinus and ectopic pacemakers and slowing AV-holding. Inhibition of the pulses observed mainly in the antegrade and to a lesser extent in the retrograde direction through the AV-node and on additional routes. By reducing myocardial oxygen demand decreases the severity of myocardial ischemia, postinfarction mortality may also decrease due to antiarrhythmic action.

The ability to prevent the development of headache of vascular origin due to a decrease in severity of cerebral arteries due to expansion of β-adrenoceptor blockade vessels, inhibition of catecholamines induced platelet aggregation and lipolysis, reduction of platelet adhesiveness, prevention of activation of blood clotting factors during the release of adrenaline, stimulation of oxygen to the tissues and a decrease in secretion renin.

Reduction of tremor during treatment with propranolol may be due to blockade of β2-adrenergic receptors.

Improves Atherogenic properties of blood. Promotes uterine contractions (spontaneous and drug-induced, stimulating the myometrium). Increases tone of the bronchi.

Pharmacokinetics

Absorption

After ingestion is absorbed quickly and adequately (90%). Cmax plasma levels achieved after 1-1.5 h. Bioavailability after a single oral administration of 30-40% (the effect of "first pass" through the liver microsomal oxidation), Propafenone - increases (formation of metabolites that inhibit liver enzymes), its magnitude depends on the nature of food and the intensity of hepatic blood flow.

Distribution

It has high lipophilicity, accumulate in the tissue of the lungs, brain, kidneys and heart. " Penetrates through the blood-brain and placental barriers in breast milk. Relationship to plasma proteins - 90-95%. Vd - 3-5 L / kg.

Metabolism

Biotransformiruetsya in the liver by glyukuronirovaniya. Falls into the bile into the intestine, deglyukuroniziruetsya and reabsorbed.

Withdrawal

Relatively rapidly excreted from the body. T1 / 2 - 3-5 hours on the background of the introduction of exchange rate may grow up to 12 hours with urine - 90%, unchanged - less than 1%. Not deleted at hemodialysis.

Statement
arterial hypertension
angina
unstable angina (excluding Prinzmetal angina)
sinus tachycardia (including in hyperthyroidism)
SVT
atrial tachyarrhythmia;
supraventricular and ventricular extrasystoles
prevention of myocardial infarction (systolic blood pressure above 100 mm Hg)
essential tremor
migraine (prevention of attacks)
as symptomatic treatment of thyrotoxicosis and hyperthyrosis crisis (when intolerance thyreostatic drugs)
sympatho-adrenal crises against the background of diencephalic syndrome

Dosage regimen

Tablets, taken orally, before a meal, without chewing, and squeezed a small amount of liquid.

When hypertension appoint 40 mg 2 times / day. In case of insufficient severity of the hypotensive effect of daily dose increased to 120 mg (40 mg 3 times / day) or up to 160 mg (80 mg 2 times / day). The maximum daily dose - 320 mg.

In angina, cardiac arrhythmia initial daily dose is 60 mg (20 mg 3 times / day), then the daily dose increased to 80-120 mg, divide it into 2-3 reception. The maximum daily dose - 240 mg.

To prevent migraines, as well as essential tremor drug is prescribed in an initial dose of 120 mg (40 mg 3 times / day).

To prevent recurrent myocardial infarction therapy Obzidanom should begin between 5 th and 21 th day after myocardial infarction. The drug is prescribed at a dose of 120 mg (40 mg 3 times) per day for 2-3 days, and then continue taking the drug at 80 mg 2 times / day. You can assign Obzidan a daily dose of 180-240 mg in 2-3 reception.

In hyperthyroidism (symptomatic treatment) Obzidan appoint 40 mg 3-4 times / day.

In case of violation of renal function is necessary to reduce the initial dose or increase the interval between doses of the drug.

If abnormal liver function should reduce the dose of the drug.

Side effect

Since the cardiovascular system: sinus bradycardia, AV-block, heart failure, palpitation, myocardial conduction disturbances, arrhythmias, lowering blood pressure, orthostatic hypotension, chest pain, spasm of peripheral arteries, cold extremities.

On the part of the digestive system: dry mouth, nausea, vomiting, diarrhea, constipation, pain in the epigastric region, abnormal liver function, changes in taste.

From the side of the central nervous system and peripheral nervous system: Rarely - headache, insomnia, nightmares, asthenia syndrome, reducing the capacity for rapid mental and motor reactions, agitation, depression, paresthesia, fatigue, weakness, dizziness, drowsiness, confusion, or momentary loss of memory, hallucinations, tremor.

On the part of the respiratory system: rhinitis, nasal congestion, dyspnea, bronchospasm, laryngism.

From the Metabolic: hypoglycemia (in patients with diabetes mellitus type 1), hyperglycemia (in patients with diabetes mellitus type 2).

From the sensory organs: eye dryness of the mucous membrane (a decrease of secretion of tear fluid), the violation of visual acuity, keratoconjunctivitis.

On the part of the reproductive system: reduction of libido, reduced potency.

Dermatological reactions: alopecia, exacerbation of psoriasis, sweating, flushing of skin, rash, psoriazopodobnye skin reactions.

On the part of the endocrine system: reduction of thyroid function.

Allergic reactions: skin rash, itching.

From the laboratory parameters: agranulocytosis, leukopenia, thrombocytopenia, increase in liver transaminases and bilirubin.

Other: muscle weakness, back pain or joint pain, chest pain, withdrawal syndrome.

Contraindications
AV-block II and III degree
sinoatrial block
sinus bradycardia
hypotension (systolic blood pressure below 90 mm Hg)
uncontrolled chronic heart failure stage IIB-III
acute heart failure
acute myocardial infarction (systolic blood pressure below 100 mm Hg)
cardiogenic shock
pulmonary edema
sick sinus syndrome
Prinzmetal angina
cardiomegaly (with no signs of heart failure)
vasomotor rhinitis
occlusive peripheral vascular disease (complicated with gangrene, a symptom of intermittent claudication or pain at rest)
diabetes mellitus
metabolic acidosis (including diabetic ketoacidosis)
bronchial asthma
propensity to bronhospasticheskim reactions
chronic obstructive pulmonary disease (including a history)
pheochromocytoma (without the simultaneous use of alpha-blockers)
spastic colitis
simultaneous reception of antipsychotic drugs and anxiolytic (chlorpromazine, trioxazine, etc.)
simultaneous reception with MAO inhibitors
Lactation (breastfeeding)
Hypersensitivity to the drug

Precautions should be prescribed drug in AV-blockade of I degree, hepatic and / or renal failure, hyperthyroidism, myasthenia gravis, chronic cardiac insufficiency stage I-IIA, pheochromocytoma, psoriasis, allergic reactions, a history of Raynaud's syndrome, pregnancy, elderly patients, children and adolescents under the age of 18 years (the efficacy and safety have not been established).

Application of pregnancy and breastfeeding

Application Obzidana during pregnancy is possible only when the intended benefits to the mother outweighs the potential risk to the fetus. If you want to use in this period should be careful monitoring of the fetus, because Reception Obzidana during pregnancy can cause intrauterine growth retardation, hypoglycemia and bradycardia in a fetus. For 48-74 hours before delivery Obzidan should be abolished.

Application Obzidana contraindicated during lactation. If necessary, its use in this period, breast-feeding should be discontinued.

Application for violations of liver function

If abnormal liver function should reduce the dose of the drug.

Application for violations of renal function

In case of violation of renal function is necessary to reduce the initial dose or increase the interval between doses of the drug.

Cautions

In appointing Obzidana should systematically monitor the heart rate and blood pressure (at the beginning of treatment - every day, then 1 every 3-4 months), ECG.

In elderly patients should be monitoring of kidney function (1 every 4-5 months).

In the case of elderly patients increasing bradycardia (less than 50 bpm), arterial hypotension (systolic blood pressure below 100 mm Hg), AV-blockade, bronchospasm, ventricular arrhythmias, severe disturbances of liver function and / or kidneys, necessary to reduce the dose or stop treatment.

It should teach the patient methods of calculating heart rate and instruct on the need of medical advice in the heart rate below 50 bpm.

It is recommended to discontinue therapy Obzidanom in the development of depression caused by his reception.

Patients who use contact lenses should be aware that during the treatment Obzidanom may decrease production lacrimal fluid.

Before the appointment Obzidana patients with heart failure (early stage) should be used with cardiac glycosides and / or diuretics.

Treatment of ischemic heart disease and resistant hypertension should be prolonged. Receiving Obzidana possible within a few years.

Termination of treatment carried out gradually, under medical supervision, abrupt withdrawal may intensify myocardial ischemia, pain in angina, worse exercise tolerance. Cancel Obzidana conducted within 2 weeks or more, gradually reducing the dose (by 25% every 3-4 days).

In patients with diabetes using the product under the control of blood glucose (1 every 4-5 months). In appointing Obzidana patients receiving hypoglycemic medications should be careful, because during long breaks in food intake can develop hypoglycemia. And its such symptoms as tachycardia or tremor will be blacked out due to the action Obzidana. Patients should be warned that the main symptom of hypoglycemia during treatment Obzidanom is increased sweating.

Precautions should be appointed Obzidan with hypoglycemic agents (the risk of hypoglycemia in insulin therapy and hyperglycemia - at the intake of oral hypoglycemic funds).

When thyrotoxicosis Obzidan may mask certain clinical signs of hyperthyroidism (eg tachycardia). Abrupt withdrawal of the drug is contraindicated in patients with thyrotoxicosis, as can intensify symptoms.

At the same time taking clonidine its reception can be terminated only after a few days after the cancellation Obzidana.

When pheochromocytoma Obzidan appoint only in combination with alpha-blockers.

Drugs that reduce the supply of catecholamines (eg reserpine) may enhance the action Obzidana, so patients taking a combination of these drugs should be under constant medical supervision in order to identify arterial hypotension and bradycardia.

The treatment should be avoided Obzidanom in / introduction of verapamil, diltiazem.

A few days before the general anesthesia with chloroform or ether must stop taking the drug (increased risk of depression of the myocardium and the development of arterial hypotension).

It should cancel the drug before the study of blood and urine catecholamines, normetanephrine and vinilamidalnoy acid, antinuclear antibody titers.

In patients who abuse tobacco, efficiency Obzidana reduced.

During treatment Obzidanom not recommended to take alcohol (probably a sharp decline in BP).

During the reception Obzidana should avoid the use of natural licorice, food, rich in protein, can increase the bioavailability of propranolol.

Use in Pediatrics

Efficacy and safety of Obzidana in children and adolescents under the age of 18 is not installed.

Effects on ability to drive vehicles and management mechanisms

During treatment Obzidanom must refrain from driving motor vehicles and classes of potentially hazardous activities that require high concentration and speed of psychomotor reactions.

Overdose

Symptoms: bradycardia, dizziness or fainting, decrease blood pressure, arrhythmia, shortness of breath, cyanosis of nails of fingers or palms, convulsions, cardiac arrest (in into / in the introduction).

Treatment: gastric lavage, the appointment of activated carbon (ingestion), with violations of AV-conduction - in / injected 1-2 mg of atropine, epinephrine, at low efficiency exercise staging temporary pacemaker with ventricular arrhythmia - lidocaine (Class IA drugs are not applicable), with arterial hypotension (the patient must be in a supine position with a lowered head end of bed), if there are no signs of pulmonary edema in / injected plazmozameschayuschie solutions for inefficiency - epinephrine, dopamine, dobutamine, with convulsions - in / diazepam; with bronchospasm - inhalation or parenteral beta-adrenostimulyatorov.

Drug Interactions

With simultaneous application of Obzidana with MAO inhibitors there is a considerable strengthening of the hypotensive action, so this combination is contraindicated, interruption in the treatment between the intake of MAO inhibitors and Obzidana must be at least 14 days.

With the simultaneous use of diuretics, reserpine, hydralazine and other antihypertensives, as well as the hypotensive effect of ethanol Obzidana increases.

The hypotensive effect Obzidana weaken GCS, NSAIDs (sodium retention and blocking prostaglandin synthesis by the kidneys), estrogens (sodium retention) and MAO inhibitors.

Obzidan while the application increases the effects thyreostatic and uterotoniziruyuschih drugs, reduces effect of antihistamines.

At simultaneous application with Obzidanom amiodarone, verapamil and diltiazem increased the severity of negative chrono-, foreign-and dromotropic actions.

When in / introduction of iodine radiopaque drugs on a background of reception Obzidana increases the risk of anaphylactic reactions.

Phenytoin at a / in the introduction, means for inhalation anesthesia (derivatives of hydrocarbons), while applying to increase the severity Obzidanom cardiodepressive action and the probability of reducing blood pressure.

Obzidan while the application modifies the effectiveness of insulin and oral hypoglycemic drugs, masking the symptoms of developing hypoglycemia (tachycardia, increased BP).

Cardiac glycosides, methyldopa, reserpine, and guanfatsin, antiarrhythmics, while admission to Obzidanom increase the risk of development or worsening of bradycardia, AV-blockade, cardiac arrest and heart failure.

Nifedipine while applying to Obzidanom can lead to a significant reduction in blood pressure.

Obzidan prolongs the action nondepolarizing muscle relaxants and anticoagulant effect of coumarins.

Three-and tetracyclic antidepressants, antipsychotic drugs (neuroleptics), ethanol, sedatives and sleeping pills, while applying to Obzidanom enhance the inhibitory effect on the CNS.

Negidrirovannye ergot alkaloids when used with a Obzidanom increase the risk of disorders of peripheral circulation.

Application Obzidana increases the likelihood of severe systemic reactions (anaphylaxis) against the introduction of allergens used for immunotherapy or skin tests.

Pharmacokinetic interaction

Cimetidine increases bioavailability of propranolol.

Propranolol increases the concentration of lidocaine in blood plasma, reduces the clearance of theophylline.

In case of simultaneous appointment of propranolol with the derivatives of phenothiazine concentrations of both drugs in blood plasma increased.

Propranolol reduces the clearance of xanthine (except difillina).

Sulfasalazine increases the concentration of propranolol in the blood plasma (inhibits metabolism), rifampicin shortens the half-life of propranolol.

Terms and Conditions of storage

List B. preparation should be kept in the dark, away from children at a temperature of 15 ° to 25 ° C. Shelf life - 5 years.

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