Sakur (Sakure)

Composition Pharmacodynamics Indications Carefully Contraindications Dosing and Administration Side effects Form release / dosage
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Active substanceLacidipineLacidipine
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  • Lazipil®
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    GlaxoSmithKline Trading, ZAO     Russia
  • Sakur
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    OBOLENSKOE PHARMACEUTICAL ENTERPRISE, CJSC     Russia
    • Dosage form: & nbspcoated tablets
    Composition:

    1 tablet contains:

    Active substance:

    Lacidipine 2.0 mg 4.0 mg

    Excipients:

    lactose monohydrate 86.0 mg 129.0 mg

    calcium hydrophosphate dihydrate 10.0 mg 15.0 mg

    potato starch 14.6 mg 20.9 mg

    Copovidone 3.8 mg 5.7 mg

    talc 2.4 mg 3.6 mg

    magnesium stearate 1.2 mg 1.0 mg

    Excipients for the shell

    Hypromellose (hydroxypropylmethylcellulose) 4.2 mg 6.3 mg

    macrogol 6000 (polyethylene glycol 6000) 0.72 mg 1.08 mg

    titanium dioxide 0.84 mg 1.26 mg

    talc 0.24 mg 0.36 mg

    Description:The tablets covered with a film membrane of white or almost white color, round, biconcave form. On the cross section, the inner layer is white or almost 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 blocker of "slow" calcium channels from the group of dihydropyridine derivatives. Reduces the flow of calcium through the potential-dependent calcium channels (mainly L-type) in 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 tone of the veins, sinoatrial and atrioventricular nodes, does not have a negative inotropic effect, causes dilatation of peripheral arterioles and a decrease in the total peripheral resistance of the vessels.

    Latsidipin expands the peripheral arterioles, reduces the overall peripheral vascular resistance and lowers blood pressure. Has an anti-atherogenic effect.

    When latsidipina is used in a dose of 4 mg, the minimum elongation of the QT interval is observed. 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 "primary passage" through the liver. The absolute bioavailability of lacidipine 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

    Lacidipine is metabolized 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. Lacidipine is used as a monotherapy or in combination with other antihypertensive drugs, for example c β-adrenoblockers, diuretics or ACE inhibitors (angiotensin-converting enzyme).

    Contraindications:Hypersensitivity to lacidipin, other derivatives of dihydropyridine and other components of the drug; severe aortic stenosis; acute myocardial infarction (within 1 month after an acute myocardial infarction); congenital lactase deficiency, lactose intolerance, glucose-galactose malabsorption syndrome (the preparation contains lactose); pregnancy, lactation, age under 18 years (efficacy and safety not established).
    Carefully:

    Patients with impaired intracardiac conduction, with low cardiac output, with unstable angina; with congenital and acquired (documented) lengthening of the interval QT, with simultaneous use 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).

    Caution should be observed when using lacidipine in patients with impaired liver function, including in patients with hepatic insufficiency (10 points or more on the Child-Pugh scale), since the antihypertensive effect the drug may be more pronounced in them.

    Given the possibility of blockers of "slow" calcium channels to influence the function of the sinoatrial and atrioventricular node, lacidipine It should be used with caution in patients with concomitant conductivity disorders.
    Pregnancy and lactation:Application drug during pregnancy and breastfeeding is not recommended. If you need to use the drug in the period of breast breastfeeding should be discontinued.
    Dosing and Administration:

    Inside, preferably in the morning, regardless of meal time. The initial dose is 2 mg once a day. 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 per day and even to 6 mg per 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.

    In elderly patients, patients with impaired renal and hepatic function, dose adjustment is not required.

    Side effects:

    Some patients may experience mild side effects associated with peripheral vasodilation. The most frequent are side effects such as headache, dizziness, "tides" of blood to the skin of the face, a feeling of palpitations. They are usually transitory in nature and, as a rule, disappear during further therapy with the continued use of lacidipine at the recommended dose.

    Rare side effects include asthenia, skin rashes (including erythema and pruritus), functional disorders of the stomach, nausea, polyuria and gingival hyperplasia.

    Like other dihydropyridine drugs, in a small number of patients the drug causes exacerbation of angina pectoris, usually at the beginning of treatment. To this side effect, patients with clinically expressed ischemic heart disease are most likely.

    The drug does not cause significant changes in blood and biochemical parameters. In a very In rare cases, a reversible increase in the level of alkaline phosphatase in the blood plasma is observed.

    From the nervous system: headache, dizziness, tremor, depression, mood lability.

    From the cardiovascular system: heart palpitations, tachycardia, blood flushes to the skin of the face, 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), Syncope, marked decrease in blood pressure.

    From the gastrointestinal tract: discomfort in the stomach, nausea, constipation, hypertrophic gingivitis.

    From the skin and subcutaneous tissues: allergic reactions, skin rash (including erythema and pruritus), angioedema, hives.

    From the side of the kidneys and urinary tract: polyuria.

    Impact on laboratory and instrumental research results: reversible increase in alkaline phosphatase activity.

    Common reactions: asthenia, peripheral edema, weakness.

    If any of the above, the side effects are aggravated or you notice any other side effects not listed in the instructions, tell your doctor.
    Overdose:

    Symptoms: marked decrease in arterial pressure, tachycardia (associated with prolonged peripheral vasodilation), impaired sinoatrial conductance and atrioventricular conduction, bradycardia, confusion, stupor, nausea, vomiting, metabolic acidosis, hyperglycemia.

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

    Treatment: symptomatic (there is no specific antidote).

    Interaction:

    Perhaps the combined use of lacidipine and other antihypertensive drugs, for example, diuretics, β-blockers or 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. Lacidipine 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. The hypotensive effect of lacidipine impairs non-steroidal anti-inflammatory drugs (sodium retention and blockage of prostaglandin synthesis by the kidneys) and estrogens (sodium retention).

    In patients receiving ciclosporin, lacidipine eliminates cyclosporine-induced decrease in renal blood flow and glomerular filtration rate. The simultaneous use of lacidipine with corticosteroids and tetracosactide can reduce the antihypertensive effect of the drug.
    Special instructions:During the period of treatment, it is necessary to take standard measures for monitoring the functional activity of the myocardium and blood pressure. At occurrence of attacks of a stenocardia or at aggravation of a stenocardia after the beginning Sakura, as well as severe arterial hypotension drug should be discarded.
    Effect on the ability to drive transp. cf. and fur:During the period of treatment, care must be taken when practicing potentially dangerous activities that require an increased concentration of attention and speed of psychomotor reactions.

    It causes dizziness, and therefore care must be taken when driving vehicles or moving machinery.
    Form release / dosage:Tablets, film-coated, 2 mg and 4 mg.
    Packaging:

    According to 7, 10, 14, 15, 20 or 30 tablets in a contour cell package of polyvinylchloride film and aluminum foil printed lacquered.

    For 1, 2, 3 or 4 contour squares, together with the instructions for use, are placed in a pack of cardboard.
    Storage conditions:

    In a dry, protected from light place at a temperature of no higher than 25 ° C.

    Keep out of the reach of children.

    Shelf life:2 years. Do not use after the expiry date printed on the package.
    Terms of leave from pharmacies:On prescription
    Registration number:LS-001870
    Date of registration:01.11.2011
    The owner of the registration certificate:OBOLENSKOE PHARMACEUTICAL ENTERPRISE, CJSC OBOLENSKOE PHARMACEUTICAL ENTERPRISE, CJSC Russia
    Manufacturer: & nbsp
    Information update date: & nbsp17.11.2015
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