ÏÑÓ¬á¼Ñ¡® 10/20

General characteristics. Structure:

Kernel:

Active ingredient: a lerkanidipina a hydrochloride - 10,0 / 20,0 mg

Excipients: lactoses monohydrate, cellulose microcrystallic, sodium carboxymethylstarch (type A), povidone - K 30, magnesium stearate.

Cover:

Опадрай OY-SR-6497 consisting from: gipromelloza, talc, titanium of dioxide, macrogoal 6000, dye ferrous oxide yellow.

Pharmacological properties:

Pharmacodynamics. The blocker of "slow" calcium channels, derivative a dihydropyridinic row, inhibits transmembrane current of calcium ions in cells of smooth muscles of vessels. The mechanism of hypotensive action is caused by the direct running-down action on smooth muscle cells of vessels therefore the general peripheric resistance of vessels decreases. Possesses the prolonged anti-hypertensive action. Thanks to high selectivity to smooth muscle cells of vessels negative inotropic effect is absent.

Pharmacokinetics. Lerkanidipin is completely soaked up after intake. The maximum concentration in a blood plasma is found in 1,5-3 hours and makes 3,3 ng/ml and 7,66 ng/ml after reception of 10 and 20 mg respectively. Distribution in fabrics and bodies comes from a blood plasma quickly. Communication with proteins of a blood plasma exceeds 98%.

At patients with a renal and liver failure the content of proteins of plasma is reduced therefore the free fraction of a lerkanidipin can be increased.

Elimination happens by biotransformation (it is metabolized by CYP 3A4 enzyme), about 50% of the accepted dose are excreted with urine. Average value of an elimination half-life makes 8-10 hours. Duration of therapeutic action makes 24 hours.

Cumulation at repeated reception is not observed.

Indications to use:

Essential hypertensia of soft and moderate severity.

Route of administration and doses:

Inside.

ÏÑÓ¬á¼Ñ¡® 10

On 1 tablet (10 mg) of 1 times a day not less than in 15 minutes prior to food, it is preferable in the morning, without chewing, washing down with enough water. Depending on the reached therapeutic effect the dose can be increased to 2 tablets (20 mg). The therapeutic dose is selected gradually, increase in a dose up to 20 mg is carried out in 2 weeks after the beginning of administration of drug.

ÏÑÓ¬á¼Ñ¡® 20

On 1/2 tablets (10 mg) once a day not less than in 15 minutes prior to food, it is preferable in the morning, without chewing, washing down with enough water. Depending on individual effect the dose can be increased to 1 tablet (20 mg). The therapeutic dose is selected gradually, if necessary increase in a dose up to 20 mg is carried out in 2 weeks after the beginning of administration of drug.

Features of use:

Use for elderly patients:

Correction of a dose is not required.

Use for patients with renal failures or a liver:

In the presence of a renal or liver failure of dose adjustment easy or moderately severe, as a rule, it is not required, an initial dose - 10 mg, then it is necessary to increase with care a dose to 20 mg days.

Influence on ability to driving of motor transport and to control of mechanisms:

As against the background of therapy by the drug Lerkamen® emergence of dizziness, an adynamy, fatigue and in rare instances of drowsiness is possible, during drug use patients should drive with extra care the car and to be engaged in other potentially dangerous types of activity demanding the high speed of psychomotor reactions.

Side effects:

Drug is well transferred. Seldom: the effects connected with vasodilating properties of drug - peripheral hypostases, feeling of rushes of blood to the person, heartbeat, tachycardia, a stethalgia, a lowering of arterial pressure, stenocardia, a myocardial infarction, an adynamy, fatigue, a headache, dizziness; very seldom: gastrointestinal disturbances (dyspepsia, nausea, vomiting, pain in epigastriums, diarrhea), increase in activity of "hepatic" enzymes (reversible), a polyuria, skin rash, drowsiness, a mialgiya, a hyperplasia of gums.

Interaction with other medicines:

When performing complex therapy of Lerkamen® it is well compatible to beta adrenoblockers, diuretics, inhibitors of an angiotensin-converting enzyme (IAPF).

With care it is necessary to appoint with CYP 3A4 inhibitors: кетоконазол, итраконазол, erythromycin, etc.

At purpose of drug together with the inductors CYP 3A4: antidepressants, rifampicin, decrease in hypotensive effect of drug is possible. At use of Lerkamena® along with cardiac glycosides, it is necessary to carry out monitoring on symptoms of intoxication by digoxin.

Simultaneous use with Cimetidinum does not cause considerable changes of concentration of a lerkanidipin in plasma, at high doses of Cimetidinum bioavailability and hypotensive effect of a lerkanidipin can increase. Strengthening of hypotensive action at the grapefruit juice use is possible. The use of ethanol can exponentiate effect of drug.

Contraindications:

• Hypersensitivity to a lerkanidipin, other derivatives of a dihydropyridinic row or any component of drug.
• Chronic heart failure (in a decompensation stage).
• Unstable stenocardia; obstruction of the vessels proceeding from a left ventricle of heart; within 1 month after the postponed myocardial infarction; the expressed abnormal liver functions; renal failure (clearance of creatinine less than 12 ml/min.).
• A lactose intolerance, a galactosemia, a syndrome of the broken absorption of a glucose/galactose.
• Pregnancy and period of feeding by a breast; the women of childbearing age who are not using reliable contraception.
• Age up to 18 years (efficiency and safety are not studied).

With care: a renal and/or liver failure, advanced age, a sick sinus syndrome (without pacemaker), coronary heart disease, dysfunction of a left ventricle.

Overdose:

There are no data on overdose. It is possible to assume that symptoms are similar to those at other derivatives of dihydropyridine (a peripheral vazodilatation with arterial hypotension and reflex tachycardia, increase in frequency and duration of attacks of stenocardia, a myocardial infarction). In case of overdose symptomatic therapy is carried out.

 

Storage conditions:

At a temperature not above 30 °C. To store in the place, unavailable to children! Period of validity 3 years. Not to apply after the expiration specified on packaging.

Issue conditions:

According to the recipe

Packaging:

ÏÑÓ¬á¼Ñ¡® 10

Tablets, film coated, 10 mg.

On 7 or 14 tablets in the blister (an aluminum opaque PVC film / foil).

On 1 (on 7 or 14 tablets) or 2 (on 14 tablets) the blister together with the application instruction place in a cardboard pack.

ÏÑÓ¬á¼Ñ¡® 20

Tablets, film coated, 20 mg.

On 7, 10 or 14 tablets in the blister (an aluminum opaque PVC film / foil).

On 1 (on 7 or 14 tablets), 2 (on 14 tablets), 3 (on 14 tablets), 4 (on 14 tablets), 5 (on 7 or 10 tablets), 7 (on 14 tablets) or 10 (on 10 tablets) blisters together with the application instruction place in a cardboard pack.