Anaprilin

General characteristics. Structure:

Active ingredient: 40 mg of propranolol in 1 tablet.

Excipients: icing sugar, granulated sugar, potato starch, talc, calcium stearate.

Pharmacological properties:

Pharmacodynamics. Anaprilin blocks β1 and β2-адренорецепторы. Owing to reduction of sympathetic influences on β1-адренорецепторы hearts decrease in force and frequency of its reductions, oppression of excitability and conductivity is observed. Reduces secretion of a renin. Due to the blockade β2-адренорецепторов Anaprilin raises a tone of bronchial tubes, sokratitelny activity of a myometrium, narrows blood vessels (including coronary), reduces hyper glycemic effect of adrenaline.

Possesses anti-anginal, hypotensive and antiarrhytmic action.

Pharmacokinetics. After intake it is soaked up quickly and rather fully (90%). The maximum concentration of medicine (Cmax) in a blood plasma is reached in 1-1,5 h. Bioavailability after a single dose inside makes 30-40% (effect of "the first passing" through a liver), at long reception - increases (the metabolites inhibiting liver enzymes are formed).

Has high lipophilicity, collects in tissue of lungs, a brain, kidneys, heart. Gets through hematoencephalic and placental barriers, into breast milk. Communication with proteins of a blood plasma – 90-95%.

It Biotransformirutsya in a liver by a glyukuronirovaniye. Gets with bile into intestines, it deglyukuronizirutsya and reabsorbirutsya.

It is rather quickly brought out of an organism. The elimination half-life of medicine (T1/2) – 3-5 h, against the background of course introduction can be extended to 12 h. It is removed with urine – 90%, in not changed look – less than 1%. Is not removed at a hemodialysis.

Indications to use:

Arterial hypertension, stable stenocardia of rest and tension; essential tremor; in complex therapy of a thyrotoxicosis, alarming frustration; prevention of migraine.

Route of administration and doses:

Appoint inside after food. At arterial hypertension - on 40 mg 2 times a day. At insufficient expressiveness of effect the dose is increased to 40 mg by 3 times or on 80 mg 2 times a day. The maximum daily dose – 320 mg (in exceptional cases – 640 mg).

At stenocardia – in an initial dose of 20 mg 3 times a day, then gradually increase a dose to 80-120 mg in 2-3 receptions. The maximum daily dose – 240 mg.

For prevention of migraine, and also at an essential tremor – in an initial dose of 40 mg 2-3 times a day, if necessary gradually increasing to 160 mg/days.

At treatment of a thyrotoxicosis Anaprilin's reception there begin with 40 mg 3-4 times a day. Further the dose is raised by each 3-4 days to optimum, allowing to control heart rate in the range of 60-90 blows in min.

At an abnormal liver function decrease in doses is necessary. The renal failure of dose adjustment does not demand.

Features of use:

Control of patients has to include heart-rate monitoring and arterial pressure (in an initiation of treatment – daily, then 1 time in 3-4 months), the electrocardiogram, concentration of glucose in blood at patients with a diabetes mellitus (1 time in 4-5 months). At elderly patients it is recommended to monitor function of kidneys (1 times in 4-5 months). Medical consultation at heart rate is necessary less than 50/mines against the background of Anaprilin's reception.

Treatment of coronary heart disease and arterial hypertension has to be long. The termination of treatment by Anaprilin is carried out gradually (lowering a dose by 25% each 3-4 days): sharp cancellation can strengthen an anginous syndrome and ischemia of a myocardium, to worsen tolerance to an exercise stress, to change rheological properties of blood, etc. At patients with a diabetes mellitus use of medicine is carried out under control of content of glucose to blood in view of risk of development of a hypoglycemia without characteristic clinical picture. Patients should be instructed as regards the main symptom of a hypoglycemia during treatment by β-adrenoblockers is the increased sweating.

Patients with chronic heart failure (early stages) need to apply Anaprilin against the background of therapy by diuretics or inhibitors of an angiotensin-converting enzyme, cardiac glycosides.

When smoking efficiency of β-adrenoblockers is lower.

The patients using contact lenses have to consider that against the background of treatment reduction of products of the lacrimal liquid is possible.

The patient with a pheochromocytoma appoint only after α-adrenoblocker reception..........

At a thyrotoxicosis Anaprilin can mask clinical signs of a thyrotoxicosis (for example, tachycardia). Sharp cancellation at patients with a thyrotoxicosis is contraindicated as it is capable to strengthen symptomatology.

At a concomitant use of a clonidine its reception can be stopped only in several days after Anaprilin's cancellation.

Sympatholytics (for example, Reserpinum), can strengthen effect of β-adrenoblockers, such patients have to be under constant observation of the doctor for detection of arterial hypotension or bradycardia.

In case of emergence in patients of advanced age of the accruing bradycardia (less than 50/mines), arterial hypotension (systolic arterial pressure is lower than 100 mm hg), atrioventricular blocks, a bronchospasm, ventricular arrhythmias, heavy abnormal liver functions and kidneys it is necessary to reduce a dose or to stop treatment. It is recommended to stop therapy at development of the depression caused by reception of β-adrenoblockers..........

It is necessary to cancel before a research of level of catecholamines in blood and urine; credits of antinuclear antibodies.

At drivers of motor transport, operators at Anaprilin's reception easing of attention and reduction of speed of response are possible.

Anaprilin's use at pregnancy is possible in that case when the estimated advantage for mother exceeds potential risk for a fruit. In need of use during this period it is necessary to make careful observation of a condition of a fruit. For 48-74 h before childbirth Anaprilin it is necessary to cancel.

Anaprilin's use is contraindicated in the period of a lactation. In need of its use breastfeeding should be stopped.

Side effects:

From a nervous system: increased fatigue, weakness, dizziness, headache, drowsiness or sleeplessness, nightmares, depression, decrease in memory, confusion of consciousness, hallucination, tremor, nervousness, concern.

From sense bodys: reduction of secretion of the lacrimal liquid (dryness and morbidity of eyes).

From cardiovascular system: sinus bradycardia, atrioventricular blocks, arrhythmias, development (decompensation) of chronic heart failure, lowering of arterial pressure, orthostatic hypotension, vasomotor spasm (strengthening of disturbance of peripheric circulation, cold snap of the lower extremities, Reynaud's syndrome), stethalgia.

From the alimentary system: nausea, vomiting, discomfort in epigastric area, a lock or diarrhea, abnormal liver functions (cholestasia), taste changes.

From respiratory system: nose congestion, bronchospasm.

From endocrine system: hypo - or a hyperglycemia.

Allergic reactions: itch, skin rash, small tortoiseshell.

From skin and its derivatives: sweating strengthening, psoriazopodobny skin reactions, aggravation of symptoms of psoriasis, alopecia.

Laboratory indicators: thrombocytopenia (bleedings and hemorrhages), leukopenia, increase in activity of transaminases, lactate dehydrogenase.

Influence on a fruit: pre-natal growth inhibition, hypoglycemia, bradycardia.

Others: dorsodynia, arthralgia, decrease in a potentiality, syndrome of "cancellation" (strengthening of attacks of stenocardia, myocardial infarction, increase in arterial pressure).

Treatment of complications. At development of side effects, especially persistent bradycardia intravenously slowly enter Atropini sulfas (1-2 mg) or β-adrenostimulyator.

The moderate bradycardia arising in the course of treatment is not the indication to cancellation, at severe bradycardia it is necessary to reduce a dose.

Interaction with other medicines:

At Anaprilin's use with inhibitors of a monoaminooxidase considerable strengthening of hypotensive action is observed, this combination is contraindicated; having rummaged in treatment between reception of inhibitors of a monoaminooxidase and Anaprilin has to make not less than 14 days.

At simultaneous use with diuretics, Reserpinum, gidralaziny, nifedipine and other anti-hypertensive medicines, and also ethanol the hypotensive effect of Anaprilin amplifies.

Simultaneous use with rizatriptany leads to increase in its concentration in blood and demands dose adjustment of a rizatriptan towards decrease.

Hypotensive effect of Anaprilin glucocorticoids, non-steroidal anti-inflammatory drugs (a delay of sodium and reduction of synthesis of prostaglandins in kidneys) weaken, estrogen (a sodium delay).

Anaprilin strengthens effect of thyreostatic and uterotoniziruyushchy medicines; reduces effect of antihistamines.

At simultaneous use with Amiodaronum, verapamil and diltiazem increases expressiveness negative hrono-, other and dromotropic action.

At an intravenous vvvedeniye of yodosoderzhashchy X-ray contrast medicines the risk of development of anaphylactic reactions increases.

Phenytoinum at intravenous administration, means for an inhalation anesthesia (derivatives of hydrocarbons) at simultaneous use with Anaprilin increase expressiveness of cardiodepressive action and probability of a lowering of arterial pressure.

Anaprilin at simultaneous use changes efficiency of insulin and peroral hypoglycemic medicines, masks symptoms of the developing hypoglycemia (tachycardia, increase in arterial pressure).

Cardiac glycosides, Methyldopum, Reserpinum and гуанфацин, antiarrhytmic medicines at a concomitant use with Anaprilin increase risk of development or aggravation of bradycardia, atrioventricular blocks, cardiac standstills and heart failure.

Anaprilin extends action of not depolarizing muscle relaxants and anticoagulating effect of coumarins.

Rub - and tetracyclic antidepressants, antipsychotic medicines (neuroleptics), ethanol, sedative and somnolent medicines strengthen the oppressing Anaprilin's action on the central nervous system.

Ergot alkaloids at simultaneous use with Anaprilin increase risk of development of disturbances of peripheric circulation.

Anaprilin increases probability of development of heavy system reactions (anaphylaxis) against the background of administration of the allergens used for an immunotherapy or for skin tests.

Cimetidinum, Sulfasalazinum increase Anaprilin's bioavailability.

Anaprilin increases concentration of lidocaine, fenotiazinovy neuroleptics in a blood plasma, reduces clearance of theophylline.

Contraindications:

Hypersensitivity, children's age, cardiogenic shock, acute myocardial infarction, sick sinus syndrome, Printsmetal's stenocardia, dekompensirovanny circulatory unefficiency, sinus bradycardia (heart rate less than 55/mines), an incomplete or total atrioventricular block, the expressed right-and left ventricular heart failure, arterial hypotension (systolic arterial pressure less than 90 mm hg), bronchial asthma, hay fever, tendency to bronchospasms, bronchospasm attacks in the anamnesis, a diabetes mellitus with ketoacidosis, disturbances of an arterial peripheral blood-groove, a spastic colitis.

With care. A chronic obstructive pulmonary disease, bronchitis, a diabetes mellitus (danger of emergence of a hypoglycemia at a concomitant use with hypoglycemic means), a renal and/or liver failure, a hyperthyroidism, a depression, a myasthenia, a pheochromocytoma, psoriasis, occlusal diseases of peripheral vessels, pregnancy, the lactation period, advanced age, children's age (efficiency and safety are not defined).

Overdose:

Symptoms: unconscious conditions, ventricular premature ventricular contraction, arrhythmias, heart failure, bradycardia, dizziness, a lowering of arterial pressure, the complicated breath, cyanosis of nails of fingers or palms, spasms.

Treatment: a gastric lavage, purpose of absorbent carbon (at intake); at disturbance of atrioventricular conductivity – in/in 1-2 mg of atropine, Epinephrinum, at a low performance carry out statement of a temporary pacemaker; at ventricular premature ventricular contraction – lidocaine (the drugs IA of a class are not used); at arterial hypotension of the patient has to be in a prone position with the lowered head end of a bed, at inefficiency – Epinephrinum, a dopamine, Dobutaminum; at spasms – in/in diazepam; at a bronchospasm - it is inhalation or parenterally β - adrenostimulyator.

Storage conditions:

In the place protected from light and moisture, at a temperature not over 25 ºС. To store in the place, unavailable to children. A period of validity - 4 years. Not to use medicine after the term specified on the label.

Issue conditions:

According to the recipe

Packaging:

On 10 tablets in a blister strip packaging, in packaging No. 10x1, 10x3, 10x5.