Universal reference book for medicines
Product name: SAKUR (SAKURE)

Active substance: lacidipine

Type: Calcium channel blocker

Manufacturer: ФП ОБОЛЕНСКОЕ (Russia)
Composition, form of production and packaging
The tablets covered with a cover
1 tab.

lacidipine 2 mg

7 pcs.
- blisters (1) - packs of cardboard.
7 pcs.
- blisters (2) - packs of cardboard.
7 pcs.
- blisters (3) - packs of cardboard.
7 pcs.
- blisters (4) - packs of cardboard.
14 pcs.
- blisters (4) - packs of cardboard.
14 pcs.
- blisters (1) - packs of cardboard.
14 pcs.
- blisters (2) - packs of cardboard.
14 pcs.
- blisters (3) - packs of cardboard.
10 pieces.
- blisters (3) - packs of cardboard.
10 pieces.
- blisters (1) - packs of cardboard.
10 pieces.
- blisters (2) - packs of cardboard.
10 pieces.
- blisters (4) - packs of cardboard.
The tablets covered with a cover 1 tab.

lacidipine 4 mg

7 pcs.
- blisters (1) - packs of cardboard.
7 pcs.
- blisters (2) - packs of cardboard.
7 pcs.
- blisters (3) - packs of cardboard.
7 pcs.
- blisters (4) - packs of cardboard.
10 pieces.
- blisters (4) - packs of cardboard.
10 pieces.
- blisters (3) - packs of cardboard.
10 pieces.
- blisters (2) - packs of cardboard.
10 pieces.
- blisters (1) - packs of cardboard.
14 pcs.
- blisters (1) - packs of cardboard.
14 pcs.
- blisters (2) - packs of cardboard.
14 pcs.
- blisters (3) - packs of cardboard.
14 pcs.
- blisters (4) - packs of cardboard.
INSTRUCTION FOR THE SPECIALIST.

Description of the drug approved by the manufacturer for the printed edition of 2014.

PHARMACHOLOGIC EFFECT

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 transplantation of the kidney that took cyclosporine, lacidipin 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 ingestion, lacidipine is quickly, but slightly absorbed from the digestive 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? 1-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 the 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 T 1/2 of lacidipine is reached, it varies from 13 to 19 hours.

INDICATIONS

- arterial hypertension.

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

DOSING MODE

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 up 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 EFFECT

Some patients may experience mild side effects associated with the widening of peripheral vessels.
The most frequent are side effects such as headache, dizziness, "hot flashes" 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 an exacerbation of angina 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 very rare cases, a reversible increase in the level of alkaline phosphatase in the blood plasma is observed.
From the side of the nervous system: headache, dizziness, tremor, depression, lability of mood.

Cardiovascular system: palpitation, 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), fainting, 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.

Influence on the results of laboratory and instrumental studies: a reversible increase in the activity of alkaline phosphatase.

Common reactions: asthenia, peripheral edema, weakness.

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

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 period;

- age under 18 years (efficiency and safety not established).

Carefully

Patients with impaired intracardiac conduction, with low cardiac
in cases of unstable angina, with congenital and acquired (documented) QT interval prolongation, with simultaneous use with drugs that can induce prolongation of the QT interval, such as antiarrhythmic drugs of classes I and III, tricyclic antidepressants, some antipsychotics (antipsychotics) , antibiotics (eg, erythromycin) and some H1-histamine receptor blockers (eg, terfenadine).
Caution should be exercised 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 of the drug may be more pronounced in them.

Given the possibility of blockers of "slow" calcium channels to affect the function of the sinoatrial and atrioventricular node, lacidipine should be used with caution in patients with concomitant conductivity disorders.

PREGNANCY AND LACTATION

The use of the drug during pregnancy and breastfeeding is not recommended.
If you need to use the drug during breastfeeding, breastfeeding should be discontinued.
APPLICATION FOR FUNCTIONS OF THE LIVER

In patients with impaired renal function, dose adjustments are not required.

APPLICATION FOR VIOLATIONS OF THE FUNCTION OF KIDNEYS

Caution should be exercised in patients with impaired liver function.

APPLICATION FOR CHILDREN

The drug is contraindicated in children under the age of 18 years (efficacy and safety not established).

APPLICATION IN ELDERLY PATIENTS

In elderly patients, dose adjustment is not required.

SPECIAL INSTRUCTIONS

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.
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 of therapy Sakur, and also at the expressed arterial hypotension the preparation needs to be canceled.
Impact on the ability to drive vehicles and manage mechanisms

It causes dizziness, and therefore care must be taken when driving vehicles or moving machinery.

OVERDOSE

Symptoms: marked decrease in blood pressure, tachycardia (associated with prolonged expansion of peripheral vessels), violation of 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).

DRUG INTERACTION

Perhaps the combined use of lacidipine and other antihypertensive drugs, such as diuretics,

β-adrenoblockers 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.
Since lacidipine is metabolized by the CYP3A4 isoenzyme, inducers, and inhibitors of this isoenzyme can influence the metabolism and excretion of lacidipine.
The hypotensive effect of lacidipine weaken NSAIDs (sodium retention and blockage of prostaglandin synthesis by the kidneys) and estrogens (sodium retention).
In patients taking ciclosporin, lacidipin 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.

TERMS OF RELEASE FROM PHARMACY

The drug is released by prescription.

TERMS AND CONDITIONS OF STORAGE

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.

Alphabetical index of medicines:
A  B  V  G  D  E  J
Z  I  Y  K  L  M  N
O  P  R  S  T  U  F
H  C  CH  SH  E  U  Y
Rambler's Top100
Privacy policy:
Copyright 2009 - 2017. Universal reference book of medicines. All rights reserved.
When using site materials, an active hyperlink is required!