Active substanceLacidipineLacidipine
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  • Lazipil®
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  • Dosage form: & nbspfilm-coated tablets
    Composition:

    Each tablet contains:

    Component name

    Amount,

    mg / tablet

    Active substance



    Lacidipine

    2,00

    4,00

    Excipients



    Lactose Monohydrate

    219,00

    197,00

    Lactose monohydrate (dry spray)

    58,25

    58,25

    Povidone K30

    20,00

    40,00

    Magnesium stearate

    0,75

    0,75

    Film membrane



    Fold the white YS-I-18043

    13 (12.5% ​​m / m)

    Uncoated tablet weight

    300,0

    300,0

    Composition of the film shell:

    Colour

    Name of components

    Amount,% m / m

    White

    Hypromellose

    67,74

    Titanium dioxide

    23,26

    Macrogol-400

    8,00

    Polysorbate 80

    1,00

    Description:

    Dosage 2 mg: white, round tablets covered with a film sheath, engraved "2" on one side.

    Dosage 4 mg: white, oval biconvex tablets, covered with a film sheath, with a risk applied to both sides. The transverse section is white.

    Pharmacotherapeutic group:The blocker of "slow" calcium channels
    ATX: & nbsp

    C.08.C.A   Dihydropyridine derivatives

    C.08.C.A.09   Lacidipine

    Pharmacodynamics:

    Latsidipin is a BCCC from the group of dihydropyridine derivatives and has a selective effect on calcium channels of smooth muscle vessels. Reduces the flow of calcium through the potential-dependent calcium channels (mainly Ltype) into cardiomyocytes and smooth muscle cells of the coronary and peripheral arteries; in high doses reduces the release of calcium from the intracellular depot. Disintegrates the processes of excitation and contraction in the myocardium, smooth muscles of the vessels, mediated by tropomyosin, troponin and calmodulin. In therapeutic doses normalizes the transmembrane flow of calcium, does not affect the venous tone, sinoatrial and atrioventricular nodes, does not have a negative inotropic effect, causes dilatation of peripheral arterioles and a decrease in OPSS (total peripheral vascular resistance).

    Latsidipin expands the peripheral arterioles, reduces the overall peripheral vascular resistance and lowers blood pressure (BP). The antiatherogenic effect of lacidipine was justified in the course of the study, the primary point of effectiveness evaluation was the evaluation of the thickness of the inner and middle shells of the carotid artery wall by the ultrasonography method.

    When lacidipine is used at a dose of 4 mg, the minimum elongation of the interval QT.

    In patients after kidney transplantation who took ciclosporin, lacidipine eliminates cyclosporine-induced decrease in renal blood flow and glomerular filtration rate.

    Lacidipine does not affect the automatism of the sinoatrial node and does not slow the excitation through the atrioventricular node.

    There is no evidence that lacidipine impairs glucose tolerance or reduces the effectiveness of hypoglycemic therapy.

    Pharmacokinetics:

    Suction

    After oral administration lacidipine quickly, but to a small extent absorbed from the gastrointestinal tract and subjected to intensive metabolism during the "first passage" through the liver. Its absolute bioavailability is approximately 10%.

    The maximum concentration of lacidipin in blood plasma is reached after 30-150 minutes. Lacidipine has a very high (more than 95%) ability to bind to plasma proteins (albumin and α1-acid glycoprotein).

    Metabolism

    Latsidipin undergoes metabolism mainly in the liver with the formation of four major metabolites, with little pharmacological activity. Metabolism in the liver occurs with the participation of isoenzyme CYP3A4.

    There is no evidence to confirm the ability of lacidipine to induce or inhibit cytochrome P450 isoenzymes.

    Excretion

    Approximately 70% of the internal dose of lacidipine is excreted as metabolites through the intestine, and the remainder of the dose is metabolized through the kidneys. When the equilibrium concentration is reached, the half-life of lacidipine varies from 13 to 19 hours.

    Indications:

    Arterial hypertension (in monotherapy or in combination with other antihypertensive drugs, for example, with β-adrenoblockers, diuretics and angiotensin-converting enzyme inhibitors).

    Contraindications:

    - Hypersensitivity to lacidipine, other derivatives dihydropyridine and other components of the preparation.

    - Clinically pronounced stenosis of the aorta.

    - Galactose intolerance, lactase deficiency or glucose-galactose malabsorption syndrome (the preparation contains lactose).

    - Age to 18 years (effectiveness and safety not established).

    Carefully:

    Violation of intracardiac conduction, low coronary reserve, unstable angina, impaired liver function, congenital and acquired (documented) lengthening of the interval QT, after a 1-month myocardial infarction, with simultaneous application with drugs that extend the interval QT.

    Given the possibility of BCCI to affect the function of the sinoatrial and atrioventricular node, lacidipine It should be used with caution in patients with concomitant conductivity disorders.

    Lacidipine should be used with caution in patients with severe hepatic dysfunction (10 points or more on the Child-Pugh scale).

    Pregnancy and lactation:

    Pregnancy

    There is no data on the safety of the use of the drug Lazipil® during pregnancy. In preclinical studies it was shown that lacidipine does not have a teratogenic effect or influence on fetal growth. The use of the drug Lazipil® during pregnancy is possible only if the potential benefit to the mother exceeds the potential risk to the fetus or newborn.

    Consideration should be given to the possible relaxation of the uterine muscles during labor during exposure to Lazipil®.

    Breastfeeding period

    Pre-clinical studies have shown that lacidipine or its metabolites can be excreted in breast milk.

    Latsipil® should be used during the period of breastfeeding only if the potential benefit to the mother exceeds the potential risk for the child.

    Dosing and Administration:

    Inside.

    The initial dose is 2 mg once a day, taken internally, preferably in the morning, regardless of the time of ingestion.

    When treating arterial hypertension, it is necessary to focus on the severity of the disease and the individual response of the patient to treatment.

    If necessary, it is possible to increase the dose to 4 mg / day and even up to 6 mg / day after the time necessary to achieve a therapeutic effect.

    Usually in clinical practice, this period is at least 3-4 weeks, unless the patient's condition requires a faster dose increase.

    Patients with impaired hepatic function

    In patients with mild or moderate impairment of liver function, dosage adjustment of the drug Lazipil® is not required.

    Patients with impaired renal function

    Correction of the dose of the drug Lazipil® in patients with impaired renal function is not required.

    Children

    Data on the use of the drug Latsipil ® in children under 18 years of age do not.

    Elderly patients

    Correction of the dose of the drug Latsipil® in elderly patients is not required.

    Side effects:

    The following criteria for assessing adverse events were used: Often (≥ 1/10), often (≥ 1/100 and <1/10), infrequently (≥ 1/1 000 and <1/100), rarely (≥ 1/10 000 and <1/1 000), rarely (<1/10 000, including individual messages). Frequency categories were formed on the basis of clinical studies of the drug and post-registration surveillance.

    The drug Latsipil® is well tolerated. Some patients may experience mild side effects associated with peripheral vasodilation. The most frequent were side effects such as headache, dizziness, "tides" of blood to the skin of the face, a feeling of palpitations. They were transient in nature and, as a rule, disappeared during further therapy with the continued use of the drug Lazipil® at the recommended dose.

    From the nervous system

    Often: headache, dizziness

    Rarely: tremor, depression, mood lability

    From the side of the cardiovascular system

    Often: heart palpitations, tachycardia, blood tides to face skin

    Infrequently: worsening of the course of concomitant angina (identified in a small number of patients usually at the beginning of treatment, more likely in patients with clinically severe coronary heart disease), fainting, marked lowering of blood pressure

    From the gastrointestinal tract

    Often: discomfort in the stomach, nausea, constipation

    Infrequently: hypertrophic gingivitis

    Laboratory indicators

    Often: reversible increase in alkaline phosphatase activity

    From the skin and subcutaneous fat

    Often: skin rash (including erythema and itching)

    Rarely: angioedema, urticaria

    From the side of the kidneys and urinary tract

    Often: polyuria

    General reactions

    Often: asthenia, peripheral edema, weakness

    Overdose:

    Symptoms

    Pronounced decrease in blood pressure, bradycardia, tachycardia, violation of sinoatrial conductance and atrioventricular conduction, confusion, stupor, nausea, vomiting, metabolic acidosis.

    Most likely, an overdose of lacidipin may be manifested by symptoms of prolonged vasodilation: arterial hypotension and tachycardia.

    Treatment

    There is no specific antidote.Common measures should be taken to monitor hemodynamic parameters and conduct symptomatic therapy.

    Interaction:

    Perhaps the combined use of lacidipine and other antihypertensive drugs, such as diuretics, βadrenoblockers or angiotensin-converting enzyme (ACE) inhibitors.

    There were no interactions of lacidipine with digoxin, tolbutamide and warfarin.

    The concentration of lacidipin in the blood plasma may increase with simultaneous admission with cimetidine.

    Grapefruit juice reduces the metabolism and bioavailability of lacidipine, as well as other drugs - dihydropyridine derivatives. The drug Lazipil® can not be washed down with grapefruit juice.

    Because the lacidipine is metabolized by isoenzyme CYP3A4, inducers and inhibitors of this isoenzyme may affect the metabolism and excretion of lacidipine.

    Special instructions:

    The drug Latsipil® should be used with caution in patients with congenital or acquired (documented) lengthening of the interval QT, with simultaneous administration with drugs that can cause lengthening of the interval QT, such as antiarrhythmic drugs I and III classes, tricyclic antidepressants, some antipsychotics (antipsychotics), antibiotics (for example, erythromycin) and some H1-histamine receptor blockers (eg, terfenadine).

    The drug Latsipil ® should be used with caution in patients with low cardiac output, with unstable angina and transferred for 1 month myocardial infarction. Care should be taken when using the drug Lazipil® in patients with hepatic insufficiency, since the hypotensive effect of the drug in them can be more pronounced.

    Effect on the ability to drive transp. cf. and fur:

    Causes dizziness, in connection with which you must be careful when driving vehicles or moving mechanisms.

    Form release / dosage:

    Tablets, film-coated, 2 mg and 4 mg.

    Packaging:

    For 7 tablets in blisters from A1 / PVC / A1. For 2 or 4 blisters together with instructions for use in a cardboard box.

    Storage conditions:

    Store at a temperature not exceeding 30 ° C.

    Keep out of the reach of children.

    Shelf life:

    2 years.

    Do not use after the expiration date stated on the package.

    Terms of leave from pharmacies:On prescription
    Registration number:П N011555 / 01
    Date of registration:25.03.2009 / 19.05.2017
    Expiration Date:Unlimited
    The owner of the registration certificate:GlaxoSmithKline Trading, ZAO GlaxoSmithKline Trading, ZAO Russia
    Manufacturer: & nbsp
    Representation: & nbspGlaxoSmithKline Trading, ZAOGlaxoSmithKline Trading, ZAO
    Information update date: & nbsp11.03.2018
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