Allapinin

General characteristics. Structure:

Active вещество:аллапинин – 25 mg.

Auxiliary veshchestva:sakharoza (sugar), potato starch, calcium stearate (calcium stearate).

Pharmacological properties:

Аллапинин® represents hydrobromic alkaloid salt of a lappakonitin with the accompanying alkaloids, received from a grass of the fighter belousty – Aconitum leucostomum Worosch. and rhizomes with roots of the fighter northern (the fighter high) – Aconitum septentrionale Koelle (A. excelsum Reichenb.), this. A crowfoot family – Ranunculaceae.

Pharmacodynamics. Antiarrhytmic drug of 1 class, alkaloid of monk's-hood belousty. Blocks "bystry" natrium channels of membranes of cardiomyocytes. Causes delay of atrioventricular and intra ventricular conductivity, shortens the effective and functional refractory periods of auricles, an AV node, ventriculonector and Purkinye's fibers, does not influence QT interval duration, conductivity on an AV node in the anterograde direction, the heart rate and arterial pressure, contractility of a myocardium (at initial lack of the phenomena of heart failure). Automatism does not oppress (a sinus node. Has no negative inotropic and hypotensive effect. Renders moderate spasmolytic, coronarodilator, holinoblokiruyushchy, mestnoanesgeziruyushchy and sedative action. At intake the effect develops in 40-60 minutes reaches a maximum in 4-5 hours and 8 hours and more proceed.

Pharmacokinetics. Bioavailability makes 40%, has effect of "the first passing" through a liver. Gets through a blood-brain barrier. The elimination half-life makes of 1-1,2 o'clock. It is removed by kidneys. At prolonged use lengthening of an elimination half-life is possible, at a chronic renal failure by 2-3 times, cirrhosis – at 3-10 times. Distribution volume at intake – 690 l.

Indications to use:

Supraventricular and ventricular premature ventricular contraction, paroxysms of blinking and Atrial flutter, Bouveret's supraventricular disease, including at a WPW-syndrome (WPW, a paroxysmal ventricular takhikaoliya (in the absence of organic lesions of heart).

Route of administration and doses:

Inside. Before reception of a tablet it is desirable to crush. Drug is accepted in 30 minutes prior to food, washing down with warm water, on 1 tablet 3 times a day, in the absence of therapeutic effect – 2 tablets 3-4 times a day. The highest single dose – 0,15 g, daily – 0,3 g. The beginning of action after one-time reception – in 40-60 minutes, the general duration of action – over 8 hours. At a heavy chronic renal failure the drug dose decline is required. Duration of treatment is defined by the doctor.

Features of use:

At a headache, dizziness, a diplopia it is necessary to reduce a drug dose. At emergence of sinus tachycardia against the background of long administration of drug beta adrenoblockers (small doses) are shown.

Side effects:

At reception of Allapinina® dizziness, a headache, heavy feeling in the head are possible, the hyperemia of integuments, an ataxy, a diplopia, allergic reactions, are possible disturbances of intra ventricular and atrioventricular conductivity, emergence of sinus tachycardia (at prolonged use), aritmogenny action, changes on an ECG: lengthening of an interval of PQ, expansion of the QRS complex.

Interaction with other medicines:

Inductors of microsomal enzymes of a liver reduce efficiency, increase risk of development of toxic effects. Antiarrhytmic means of other classes increase risk of aritmogenny action. Strengthens effect of not depolarizing muscle relaxants.

Contraindications:

Hypersensitivity to drug, sinuatrial blockade, an atrioventricular block of II and III degrees (without pacemaker), cardiogenic shock, the blockade of the right leg of a ventriculonector which is combined with blockade of one of branches of the left leg, blockade of intra ventricular conductivity, the expressed arterial hypotension, chronic heart failure, the expressed hypertrophy of a myocardium of a left ventricle (≥1,4 cm), existence of a postinfarction cardiosclerosis, the expressed abnormal liver functions and/or kidneys, pregnancy, the lactation period, age up to 18 years (efficiency and safety are not established).
With care to apply at an atrioventricular block of 1 degree, disturbance of intra ventricular conductivity, a sick sinus syndrome, bradycardia, the expressed blood circulation disturbances, closed-angle glaucoma, a prostatauxe, disturbance of conductivity on Purkinye's fibers, blockade of one of ventriculonector legs, disturbance of electrolytic exchange (a hypopotassemia, a hyperpotassemia, a hypomagnesiemia).

Overdose:

There are no data.

Storage conditions:

List B. In the place protected from light, at a temperature not above 25 °C. To store in the place, unavailable to children.

Issue conditions:

According to the recipe

Packaging:

Tablets on 25 mg.
On 10 or 30 tablets in blister strip packagings. 3 planimetric packagings No. 10 or 1 place planimetric packaging No. 30 together with the application instruction in a pack from a cardboard for a retail container.