Expiration date: 11/2025

Form and composition:

The tablets are round, flat, white or almost white, with chamfer, with risk on one side and engraving A+L on the other side.

1 tablet contains:

lisinopril dihydrate 10.88 mg,

EMCO corresponds to the content of lisinopril 10 mg

amlodipine besylate 6.94 mg,

EMCO corresponds to the content of amlodipine 5 mg

Excipients: magnesium stearate, sodium carboxymethyl starch type A, microcrystalline cellulose.

10 PCs. - blisters (1) - cardboard packs.

10 PCs. - blisters (2) - cardboard packs.

10 PCs. - blisters (3) - cardboard packs.

Pharmacological action:

Combined antihypertensive drug containing lisinopril and amlodipine.

Lisinopril - ACE inhibitor, reduces blood levels of angiotensin II and aldosterone, while increasing the level of bradykinin is a vasodilator mediator. It affects the tissue renin-angiotensin system. It reduces blood pressure and blood pressure, pre-and postnagruzku, pressure in the pulmonary capillaries, does not affect the heart rate, while it is possible to increase the cardiac output and increase blood flow in the kidneys. It expands the artery to a greater extent than veins. Improves blood supply to ischemic myocardium. With long-term use, it helps to reduce myocardial hypertrophy and the walls of resistive arteries. Increases myocardial tolerance to physical activity in patients with chronic heart failure. Plays a role in restoring the function of endothelium damaged as a result of hyperglycemia.

Increases life expectancy in chronic heart failure. Slows down the progression of left ventricular dysfunction after myocardial infarction, not complicated by heart failure.

The hypotensive effect observed after 1 h after administration of the drug inside, reaching a maximum after 6 h. Duration of action depends on the dose at 24 h. prolonged treatment efficiency is not reduced. With a sharp cessation of treatment of withdrawal syndrome with a sharp increase in blood PRESSURE does not occur.

Despite the primary effect, manifested in the impact on the renin-angiotensin-aldosterone system, it is also effective in hypertension with low renin level.

Lisinopril reduces albuminuria not only due to lower blood PRESSURE, but also as a result of changes in hemodynamics of the glomerular apparatus and its tissue structure. It does not affect blood sugar levels in diabetic patients and does not increase the incidence of hypoglycemia.

Amlodipine - blocker of slow calcium channels of the III generation, has antianginal and hypotensive effect. It prevents calcium from entering the myocardial cells and, to a greater extent, in the smooth muscle cells of the vascular wall. Reduces the tone of smooth muscles of the arterioles, systemic vascular resistance and therefore BP.

It has an antianginal effect due to the expansion of arterioles and arteries and reduce postnagruzki. Reduces oxygen demand and myocardial energy consumption, as it does not cause reflex tachycardia. Probably due to the expansion of the coronary arteries and arterioles increases the supply of oxygen intact (especially in vasospastic angina) and ischemic areas of the myocardium. In angina pectoris improves exercise tolerance, prevents the development of angina attack and the formation of an ischemic interval ST, reducing the frequency of angina attacks and the need for nitroglycerin. It does not affect the conductivity and contractility of the myocardium.

Has a long, dose-dependent hypotensive effect. Does not reduce the left ventricular ejection fraction. Reduces left ventricular hypertrophy. It has anti-atherosclerotic and cardioprotective effect in ischemic heart disease. The use of dioxin, diuretics and ACE inhibitors on the background of therapy does not increase the risk of death in patients with chronic heart failure (III-IV functional class classification NYHA).

Slow absorption, wide distribution in the body and slow excretion provides long-lasting action, allowing to take the drug 1 time/day. More than 24 hours provides a significant clinical reduction in blood PRESSURE in the sitting and lying down position. The action develops gradually, after 2-4 hours after administration and is not accompanied by hypotension.

Inhibits platelet aggregation, enhances glomerular filtration, has a weak natriuretic effect, in diabetic nephropathy does not increase microalbuminuria.

It does not have a negative impact on metabolic processes, does not change the level of plasma lipids. It can be prescribed to patients with concomitant asthma, diabetes and gout.

The combination of lisinopril with amlodipine in one drug can prevent the development of possible adverse effects caused by the anti-regulation of any of the active substances. Thus, the blocker of slow calcium channels, directly expanding arterioles, can lead to sodium and fluid retention in the body and, therefore, can activate the renin-angiotensin-aldosterone system. ACE inhibitor blocks this process, normalizes the reaction to the load salts.

Pharmacokinetics:

Lisinopril

Suction

After oral administration in unchanged form enters the systemic circulation and after 6 h reaches Cmax in blood plasma (90 ng/ml). Absorption is 30% (6-60%), bioavailability 29%.

Distribution

Associated exclusively with the ACE.

It penetrates the BBB and placental barrier.

Metabolism

Not metabolized.

Breeding

Return with urine in an unmodified form, T1/2 12.6 h After the removal of the greater part of the free lisinopril is excreted fraction associated with ACE, providing long-lasting therapeutic effect.

Pharmacokinetics in special clinical cases

In renal failure, the excretion of lisinopril slows down. Displayed in dialysis.

Amlodipine

Suction

After intake of amlodipine is slowly and almost completely (90%) absorbed from the gastrointestinal tract. Cmax in blood plasma is achieved after 6-10 h. Undergoes the effect of the first passage through the liver. Bioavailability is 64-80%.

Distribution

The equilibrium state is achieved on 7-8 day of regular intake. Vd is approximately 20 l/kg.

Binding to plasma proteins-95-98%. Penetrates the GAB.

Metabolism

Undergoes intensive metabolism in the liver (90%). Most of it turns into an inactive metabolite in the liver.

Breeding

10% amlodipine excreted in the urine unchanged, 60% - in the form of metabolites 20-25% - in the form of metabolites of bile through the intestine enters the breast milk. Total clearance of 500 ml/min.

Excretion has a two-phase character. T1/2 of the final phase of 35-50 hours.

Pharmacokinetics in special clinical cases

T1/2 in hypertension - 48 h, in elderly patients - up to 65 h, with liver failure - up to 60 h, T1 / 2 increases and with severe heart failure, does not reflect the degree of renal dysfunction. Approximately at the same time achieved Cmax in blood plasma in young and elderly patients. In elderly patients, amlodipine clearance is slightly lower, T1 / 2 and AUC more. Not subjected to dialysis. Tolerance is the same, so dose adjustment for elderly patients is not required.

Ekvator®

The interaction between the active substances that are part of the drug is unlikely. AUC, the time of achievement and the value of Cmax in blood plasma, T1 / 2 do not change compared to the performance of each individual active substance. Eating does not affect the absorption of active substances. Long-term circulation in the body of both active substances makes it possible to take the drug 1 time/day.

Indications:

• essential hypertension (if necessary, combination therapy).
  

Dosage regimen:

It is recommended to use in cases where the reception of drugs containing separately active substances of the Ekvator in the same doses, does not provide the necessary control of blood PRESSURE.

For patients who do not receive antihypertensive agents, the daily dose - 1 tab. regardless of the meal.

In the case of previous diuretic therapy for 2-3 days before the start of the Ekvator diuretic should be canceled. If you can not cancel the diuretic, the initial dose of the Ekvator is 1/2 tab./ day. After taking the drug, the patient is required to provide medical monitoring for several hours due to the possible development of symptomatic hypotension.

With heart failure and severe hypertension, the maintenance dose is 1 tab.

When kidney failure and QC 30-70 ml/min appoint half the usual initial dose (because the excretion of lisinopril kidney). The maintenance dose depends on the individual reaction of the patient, during therapy requires regular monitoring of kidney function, potassium and sodium levels in the blood.

In diseases of the liver excretion of amlodipine may slow, so the initial dose of the Ekvator is 1/2 tab. per day. The use of the drug in this category of patients requires special caution.

Side effect:

From the cardiovascular system: 1-3% - orthostatic hypotension rarely-arrhythmia, palpitations, tachycardia (probably as a result of excessive blood PRESSURE reduction in patients with high risk of myocardial infarction, cerebrovascular stroke).

From the Central and peripheral nervous system: 8% - headache, 3% - dizziness 1-3% - weakness rarely - increased drowsiness, muscular fasciculation of the limbs and lips, asthenia, mood lability, confusion.

From the respiratory system: 5% - dry cough.

From the digestive system: possible 1-3% of diarrhea, nausea, vomiting 1% - increase in liver enzymes and bilirubin in the blood (especially kidney disease, diabetes and renovascular hypertension), rarely - violation of bowel function, dry mouth, abdominal pain, pancreatitis, hepatocellular or cholestatic jaundice, hepatitis, gingival hyperplasia, loss of appetite.

From the urinary system: increased levels of creatinine, urea nitrogen (especially in kidney disease, diabetes and renovascular hypertension) rarely - impaired renal function, urination, oliguria, anuria, acute renal failure, uremia, proteinuria.

Metabolism: hyperkalemia.

Dermatological reactions: 1-3% - itching, skin rash, redness of the skin rarely-increased sweating, alopecia.

Allergic reactions: rarely-urticaria 0.1% - angioedema of the face, limbs, lips, tongue, epiglottis, larynx. In such cases, you should immediately stop treatment and observe the patient until all symptoms disappear.

From the hematopoietic system: leukopenia, neutropenia, agranulocytosis (effect of ACE inhibitor), thrombocytopenia, erythrocytopenia, with prolonged treatment may slightly reduce the concentration of hemoglobin and hematocrit.

Other: 1-3% - swelling of the ankles, chest pain, arthralgia rarely-a syndrome accompanied by the appearance of antinuclear antibodies, accelerated ESR and arthralgia, impotence.

Adverse reactions are usually mild and transient, treatment withdrawal is required in rare cases. Side effects caused by the combination drug, there are no more often than in the case of each component separately.

Contraindications:

• hereditary or idiopathic hemodynamically significant stenosis of the aorta or mitral valve
  
• hypertrophic cardiomyopathy
  
• severe arterial hypotension
  
• cardiogenic shock
  
• angioedema in history, including caused by the use of other ACE inhibitors
  
• pregnancy
  
• lactation
  
• children and adolescents up to 18 years (due to lack of data on the effectiveness and safety of the drug in this age group)
  
• hypersensitivity to the components of the drug or to other derivatives of dihydropyridine.
  

With caution the drug should be used in cerebrovascular diseases (including in case of insufficiency of cerebral circulation), ischemic heart disease, coronary insufficiency, severe bradycardia, tachycardia, chronic heart failure being decompensation, if mild or moderate arterial hypotension, acute myocardial infarction and for one month afterwards, severe autoimmune diseases (including scleroderma, SLE), with oppression of bone marrow hematopoiesis, diabetes, hyperkalemia, state after kidney transplantation, renal failure, diet with sodium restriction, in elderly patients, with liver failure.

Pregnancy and lactation:

The drug is contraindicated in pregnancy.

If pregnancy is detected, treatment should be stopped as soon as possible.

The administration of lisinopril in the II and III trimesters of pregnancy can cause damage and death of the fetus as a result of the effect on its kidneys (hypotension, renal failure, hyperkalemia). Reducing the amount of amniotic fluid can lead to deformation of the skull and face, disruption of limb development, hypoplasia of the lungs and fetal death. Data on these and other exposures in the earlier stages of pregnancy do not exist.

Taking the drug during lactation is contraindicated due to the release of amlodipine with breast milk. The data indicate that the penetration of lisinopril in breast milk are not available.

Special instruction:

Treatment can be started only after correction of hyponatremia and restoration of BCC in case of dehydration.

After taking the first dose of the drug should be carefully monitored for changes in blood PRESSURE. There may be a significant decrease in blood PRESSURE with the development of symptomatic hypotension in patients taking diuretics and in a state of dehydration and/or hyponatremia as a result of increased sweating, prolonged vomiting or diarrhea. With hypotension, the patient is given a horizontal position and, if necessary, a solution is introduced to fill the BCC (infusion of saline solution).

In heart failure in the stage of decompensation, IHD, cerebrovascular diseases Ekvator® can cause hypotension, myocardial infarction or stroke.

In case of aortic stenosis, hypertrophic cardiomyopathy, the appointment of a vasodilator requires caution.

During treatment, body weight control and supervision by the dentist are necessary.

It is necessary to regularly monitor the picture of peripheral blood for timely detection of possible agranulocytosis.

In violation of renal function, for example, with renal artery stenosis (especially bilateral or with stenosis of the arteries of the single kidney), hyponatremia, dehydration, circulatory failure, drug administration can provoke deterioration of renal function and acute renal failure, reversible after treatment.

When the liver T1 / 2 amlodipine increases, such patients are prescribed with caution, after assessing the ratio of benefit and risk.

It is possible to develop a reaction to the ACE inhibitor in the form of angioedema of the face, limbs, lips, tongue, epiglottis or larynx, requiring immediate cessation of treatment with the drug and the establishment of medical supervision of the patient until the complete disappearance of all symptoms.

Angioedema, localized on the face, lips, limbs, usually spontaneously disappears, taking antihistamines, helps to reduce symptoms.

Angioedema of the larynx can be fatal. Edema of the tongue, epiglottis and larynx can cause obstruction of the respiratory tract and requires immediate drug intervention: the introduction of 0.1% epinephrine (adrenaline) p/K (0.3-0.5 ml, i.e. 0.3-0.5 mg) or slowly in/(0.1 ml, i.e. 0.1 mg), the use of GCS, antihistamines and control of vital functions of the body.

Surgery / General anesthesia: in the application of General anesthesia with hypotensive effect and during extensive surgical procedures, lisinopril inhibits the formation of angiotensin II in response to the compensatory renin. If such hypotension HELL normalize by increasing the BCC.

The use of polyacrylnitrile membranes for dialysis during treatment with an ACE inhibitor can provoke anaphylactic shock, their simultaneous use should be avoided, or a dializing membrane of another type or another antihypertensive agent should be used.

Desensitization against arthropods during treatment with an ACE inhibitor can cause an anaphylactic reaction. The reaction can be avoided by temporarily interrupting treatment with an ACE inhibitor.

When choosing a dose should be taken into account that in elderly patients, both active substances are determined in the blood at a higher concentration, while the effectiveness does not change.

Impact on the ability to drive and operate machinery

The drug may affect the ability to drive and work with mechanisms, especially at the beginning of treatment, when the risk of hypotension is more likely. The dose and dosing regimen at which it is possible to operate the car and to carry out the works connected with the increased risk of traumatism, are established individually.

Overdose:

Symptoms: vasodilation with a marked decrease in blood PRESSURE and the appearance of reflex tachycardia.

Treatment: symptomatic therapy, control of cardiac activity, blood pressure, diuresis and water-electrolyte balance, if necessary, its correction. With a marked decrease in blood PRESSURE, the patient is given a lying position, the lower limbs are lifted with an unsatisfactory therapeutic response to the I/V administration of fluid substitutes may require the introduction of dopamine. To stop the action of amlodipine, calcium gluconate can be injected into/into. Due to the slow absorption of amlodipine in some cases, the stomach is washed, activated carbon is used. Lisinopril is excreted by hemodialysis a strong degree of binding to blood proteins makes amlodipine dialysis ineffective.

Drug interaction:

Inhibitors of microsomal oxidation can increase the concentration of amlodipine in the blood plasma, increasing the risk of side effects, and inducers of microsomal liver enzymes reduce.

While the use of potassium-spiking diuretics (spironolactone, triamterene, amiloride), potassium preparations, salt substitutes and dietary SUPPLEMENTS containing potassium, may develop hyperkalemia, especially in patients with impaired renal function. When using such combinations requires special care. The appointment is possible after a thorough assessment of the benefits and risks of therapy, subject to regular monitoring of potassium in the blood and kidney function.

With the simultaneous use of the drug with diuretics, a sharp decrease in blood PRESSURE is possible, with other hypotensive agents (beta-blockers, calcium channel blockers (including verapamil), ACE inhibitors, nitrates), there is an additive effect (with combination therapy requires caution).

May decrease the effectiveness of the drug while the use of NSAIDs (especially indomethacin, as NSAIDs cause sodium retention and inhibit prostaglandin synthesis in the kidneys), estrogens, agonists, sympathomimetics (with combination therapy requires careful).

At simultaneous application with preparations of lithium may be reduced excretion of lithium, requires monitoring of lithium level in blood plasma (with combination therapy requires careful).

Antacids and colestyramine reduce the absorption of active substances from the gastrointestinal tract (with combination therapy requires caution).

Amiodarone, quinidine, beta-blockers, antipsychotics (neuroleptics) can enhance the hypotensive effect.

Calcium preparations can reduce the effect of calcium channel blockers.

Procainamide, quinidine and other drugs that extend THE Qt interval can contribute to its significant increase.

It has no effect on the pharmacokinetics of digoxin and warfarin. Cimetidine does not affect the pharmacokinetics of amlodipine.

Lisinopril reduces potassium loss in the treatment of thiazide diuretics.

Storage conditions and terms:

The drug should be stored out of reach of children at a temperature of 15° to 25°C. shelf life - 3 years.