Equator - instructions for use, analogs, testimonials and release forms (5 mg and 10 mg tablets) of a medicament for the treatment of pressure (arterial hypertension) in adults, including during pregnancy

In this article, you can read the instructions for using the drug Equator. Presented are reviews of visitors to the site - consumers of this medication, as well as opinions of doctors of specialists on the use of the Equator in their practice. A big request is to actively add their feedback on the drug: the medicine helped or did not help get rid of the disease, which were observed complications and side effects, possibly not declared by the manufacturer in the annotation. Equator analogues in the presence of existing structural analogues. Use for the treatment of hypertension (hypertension) in adults, including during pregnancy and lactation.

Equator - A combined antihypertensive drug containing lisinopril and amlodipine.

Lizinopril - an ACE inhibitor (angiotensin-converting enzyme), reduces the formation of angiotensin 2 from angiotensin 1. Reducing angiotensin 2 leads to a direct reduction in the release of aldosterone. Reduces the degradation of bradykinin and increases the synthesis of prostaglandins. Reduces OPSS, reduces blood pressure, preload, pressure in the pulmonary capillaries, causes an increase in the minute volume of blood and increased tolerance of the myocardium to loads in patients with chronic heart failure. Expands arteries more than veins. Some effects are explained by the effect on tissue RAAS.

With prolonged use, myocardial hypertrophy and the walls of arteries of resistive type decrease. Improves the blood supply of the ischemic myocardium.

ACE inhibitors prolong life expectancy in patients with chronic heart failure, slow the progression of left ventricular dysfunction in patients who underwent myocardial infarction without clinical manifestations of heart failure.

With a sharp withdrawal of the drug, there was no pronounced increase in blood pressure.Despite the primary effect, which manifests itself in the effect on RAAS, it is also effective in hypertension with low renin activity.

In addition to reducing blood pressure, lisinopril reduces albuminuria. Lizinopril does not affect the concentration of glucose in the blood in patients with diabetes mellitus and does not increase the incidence of hypoglycemia.

The onset of action is 1 hour after ingestion. The maximum antihypertensive effect is determined after 6 hours and persists for 24 hours. With arterial hypertension, the effect is observed in the first days after the start of treatment, stable effect develops after 1-2 months.

Amlodipine is a blocker of slow calcium channels, a derivative of dihydropyridine. Has antianginal and antihypertensive effect. Blocking calcium channels, reduces the transmembrane passage of calcium ions into the cell (mainly in vascular smooth muscle cells than cardiac myocytes).

Antianginal effect is due to the expansion of coronary and peripheral arteries and arterioles: with angina decreases the severity of myocardial ischemia; expanding peripheral arterioles, reduces OPSS, reduces afterload on the heart, reduces the need for myocardium in oxygen.Expanding coronary arteries and arterioles in unchanged and ischemic zones of the myocardium, increases the flow of oxygen into the myocardium (especially with vasospastic angina); prevents spasm of the coronary arteries (including caused by smoking).

In patients with stable angina, a single daily dose increases exercise tolerance, slows the development of angina pectoris and ischemic depression of the ST segment, reduces the incidence of angina attacks and the consumption of Nitroglycerin and other nitrates.

Has a long-term dose-dependent antihypertensive effect. Antihypertensive action is due to direct vasodilating effect on smooth muscle vessels. With arterial hypertension, a single dose provides a clinically significant decrease in blood pressure over a period of 24 hours (in the position of the patient lying down and standing). Orthostatic hypotension in the appointment of Amlodipine is rare. Does not cause a decrease in exercise tolerance, a fraction of the ejection of the left ventricle.

Reduces the degree of myocardial hypertrophy of the left ventricle. Does not affect the contractility and conductance of the myocardium, does not cause a reflex increase in heart rate, inhibits platelet aggregation,increases the rate of glomerular filtration, has a weak natriuretic effect.

Does not have any adverse effect on the metabolism and concentration of plasma lipids and can be used in the treatment of patients with bronchial asthma, diabetes and gout. A significant reduction in blood pressure is observed after 6-10 h, the duration of the effect is 24 h.

Amlodipine + lisinopril

The combination of lisinopril with amlodipine in a single medicine can prevent the development of possible undesirable effects caused by one of the active substances. So, the calcium channel blocker, directly expanding the arterioles, can lead to a delay in sodium and fluid in the body, and, therefore, can activate RAAS. The ACE inhibitor blocks this process.

Pharmacokinetics

Lisinopril

After ingestion in unchanged form enters the systemic circulation. It penetrates the GEB and the placental barrier. It is not metabolized. It is excreted unchanged in the urine. After excretion of most of the free lisinopril, the fraction associated with ACE is removed, providing a long-term therapeutic effect.

Amlodipine

After ingestion, amlodipine slowly and almost completely (90%) is absorbed from the digestive tract. It is subject to intensive metabolism in the liver (90%). Most of it turns into a liver in an inactive metabolite. 10% of amlodipine is excreted unchanged in urine, 60% in the form of metabolites; 20-25% - in the form of metabolites with bile through the intestine; penetrates into breast milk.

Indications

• essential arterial hypertension (high blood pressure) (patients who are shown combined therapy).

Forms of release

Tablets 5 mg + 10 mg, 10 mg + 20 mg.

Instructions for use and dosing regimen

It is recommended to use in cases when taking medications containing separately active substances of the Equator in the same doses does not provide the necessary control of blood pressure.

The drug is taken orally 1 time per day, regardless of food intake, with a sufficient amount of liquid.

Equator 5mg + 10mg

The recommended dose is 1 tablet 1 time per day. The maximum daily dose is 1 tablet.

At the beginning of therapy, Equator may develop symptomatic arterial hypotension, which is more likely to occur in patients with impaired water-electrolyte balance, due to previous therapy with diuretics.Admission diuretikov should be discontinued 2-3 days before the start of therapy with the drug Equator. In cases where the elimination of diuretics is not possible, the initial dose of the drug Equator is 1/2 tablet once a day, after which the patient should be monitored for several hours because of the possible development of symptomatic arterial hypotension.

To determine the optimal initial and maintenance dose for patients with renal insufficiency, the dose should be titrated and determined individually, using separately lisinopril and amlodipine. Equator 5 mg + 10 mg is indicated only for those patients in whom the optimal maintenance dose of lisinopril and amlodipine is titrated to 10 mg and 5 mg, respectively. During treatment with the Equator preparation, it is necessary to monitor the kidney function, the content of potassium and sodium in the blood serum. In case of impaired renal function, the preparation of Equator should be discontinued and replaced with lisinopril and amlodipine in adequate doses.

Excretion of amlodipine may be delayed in patients with impaired hepatic function. Clear recommendations on the dosage regimen in such cases are not established,therefore, the Equator preparation should be administered with caution to patients with hepatic insufficiency.

In clinical studies, age-related changes in efficacy or safety profile for amlodipine and lisinopril have not been observed. Equator 5 mg + 10 mg is indicated only for those patients in whom the optimal maintenance dose of lisinopril and amlodipine is titrated to 10 mg and 5 mg, respectively. To determine the optimal maintenance dose in elderly patients (over 65 years of age), it is necessary to determine the dosing regimen individually, using separately lisinopril and amlodipine.

Equator 10 mg + 20 mg

The recommended dose is 1 tablet daily. The maximum daily dose is 1 tablet.

To determine the optimal initial and maintenance dose in patients with renal insufficiency, the dose should be titrated and determined individually, using separately lisinopril and amlodipine. The 10 mg + 20 mg equator is indicated only for those patients in whom the optimal maintenance dose of lisinopril and amlodipine is titrated to 20 mg of lisinopril and 10 mg of amlodipine.During treatment with the Equator preparation, it is necessary to monitor the kidney function, the content of potassium and sodium in the blood serum. In case of worsening kidney function, the reception of the Equator should be canceled and replaced with mono preparations in adequate doses.

In patients with impaired liver function, excretion of amlodipine can be slowed down. Clear recommendations on the dosage regimen in such cases are not established, therefore the preparation of Equator should be administered with caution.

In elderly patients (over 65 years) in clinical studies on the efficacy and safety of amlodipine or lisinopril, no changes were detected. To determine the optimal maintenance dose, it is necessary to determine the dosage regimen individually, using separately lisinopril and amlodipine. The 10 mg + 20 mg equator is indicated only for those patients in whom the optimal maintenance dose of lisinopril and amlodipine is titrated to 20 mg of lisinopril and 10 mg of amlodipine.

Side effect

• orthostatic hypotension;
• arrhythmias, increased heart rate, tachycardia (probably as a result of excessive blood pressure lowering in patients with a high risk of myocardial infarction, stroke);
• vasculitis;
• development or exacerbation of heart failure;
• headache;
• dizziness;
• increased drowsiness;
• asthenia;
• mood lability;
• confusion of consciousness;
• sensation of heat and tides of blood to the skin of the face;
• increased fatigue;
• fainting;
• paresthesia;
• peripheral neuropathy;
• insomnia;
• nervousness;
• depression, anxiety;
• convulsions;
• apathy;
• dry cough;
• dyspnea;
• rhinitis;
• nose bleed;
• diarrhea, nausea, vomiting;
• dry mouth;
• abdominal pain;
• pancreatitis;
• decreased appetite;
• constipation;
• flatulence, indigestion;
• anorexia;
• arthralgia;
• skin itching, skin rash;
• increased sweating;
• hives;
• angioedema, swelling of the face, extremities, lips, tongue, epiglottis and larynx (in such cases, immediately stop treatment and observe the patient until all symptoms disappear);
• leukopenia, neutropenia, agranulocytosis (ACE inhibitor effect), thrombocytopenia, erythrocytopenia;
• impaired renal function;
• frequent urination;
• painful urination;
• acute renal insufficiency;
• impotence;
• gynecomastia;
• fever;
• muscle cramps, myalgia;
• backache;
• tinnitus;
• visual impairment;
• conjunctivitis;
• Pain in the eyes;
• weakness;
• swelling of the ankles;
• redness of facial skin;
• chest pain;
• increase / decrease in body weight.

Side effects caused by the combined drug do not occur more often than in cases of taking each component separately.

Contraindications

• Quincke's swelling in the anamnesis, incl. on the background of the use of ACE inhibitors;
• hereditary or idiopathic angioedema;
• hemodynamically significant stenosis of the aorta or mitral valve;
• hypertrophic obstructive cardiomyopathy;
• severe arterial hypotension (systolic blood pressure less than 90 mm Hg);
• cardiogenic shock;
• unstable angina (with the exception of Prinzmetal's stenocardia);
• heart failure after acute myocardial infarction (within the first 28 days);
• bilateral stenosis of the renal arteries (for the drug Equator 20 mg / 10 mg);
• stenosis of the artery of a single kidney (for the preparation Equator 20 mg / 10 mg);
• pregnancy;
• lactation period;
• children and adolescents under 18 years of age (efficacy and safety not established in this age group);
• hypersensitivity to the components of the drug;
• increased sensitivity to other ACE inhibitors;
• hypersensitivity to other dihydropyridine derivatives.

Application in pregnancy and lactation

The drug is contraindicated for use in pregnancy.

When diagnosing a pregnancy, taking Equator should be stopped immediately.

Lizinopril penetrates the placental barrier. Admission of ACE inhibitors in the 2nd and 3rd trimester of pregnancy has an adverse effect on the fetus (there may be a marked decrease in blood pressure, renal failure, hyperkalemia, hypoplasia of the skull bones, fetal death). Data on the negative effect of the drug on the fetus in the case of application in the first trimester of pregnancy there. For newborns and infants who have undergone intrauterine exposure to ACE inhibitors, careful monitoring is recommended to timely detect a marked decrease in blood pressure, oliguria, and hyperkalemia.

The safety of the use of amlodipine in pregnancy is not established, therefore its use in this category of patients is contraindicated.

Lizinopril can be excreted in breast milk. There is no evidence that amlodipine is excreted in breast milk. However, it is known that other calcium channel blockers of dihydropyridine derivatives are excreted in breast milk.If you need to use the drug Equator during lactation, breastfeeding should be discontinued.

special instructions

Arterial hypotension

A marked decrease in blood pressure with the development of clinical symptoms can be observed in patients with reduced BCC and / or sodium content due to diuretics, fluid loss or other reasons, for example, with excessive perspiration with prolonged vomiting and / or diarrhea. In case of arterial hypotension, the patient should be laid and compensated for fluid loss (intravenous infusion of 0.9% sodium chloride solution) if necessary.

Preferably, the recovery of loss of fluid and / or sodium is carried out before the start of therapy with the Equator. It is necessary to monitor BP after taking the initial dose. This is especially true for patients with IHD or cerebrovascular disease, when a pronounced decrease in blood pressure can lead to myocardial infarction or stroke.

Aortic and mitral stenosis

Like all vasodilating drugs, the Equator should be administered with caution to patients with obstruction of the outflow tract of the left ventricle and stenosis of the mitral valve.

Impaired renal function

In some patients with arterial hypertension without pronounced manifestations of renovascular diseases, an increase in creatinine and urea in the blood serum was observed, in most cases minimal or transitory, more pronounced with concurrent administration of ACE inhibitors and a diuretic. This is most typical for patients with a history of kidney disease.

Angioedema

Angioedema, facial edema, extremities, lips, tongue, vocal folds and / or larynx have been reported in patients taking an ACE inhibitor, including lisinopril. In these cases the reception of the Equator should be immediately stopped and the patient should be carefully monitored until the symptoms disappear completely.

Edema of the face, lips and extremities usually pass independently, however, to reduce the severity of symptoms should use antihistamines.

Angioedema, accompanied by swelling of the larynx, can lead to death. If you detect edema of the tongue, pharynx or larynx, which are the cause of airway obstruction, emergency measures should be urgently started.The proper measures include: s / c administration of 0.3-0.5 mg or slow iv injection of 0.1 mg 0.1% solution of epinephrine (adrenaline), followed by intravenous administration of GCS and antihistamines and simultaneous monitoring of vital functions.

Patients taking ACE inhibitors rarely had angioneurotic edema of the intestine. These patients complained of abdominal pain (with or without nausea and vomiting); in some cases, the previous edema was not observed, and the activity of C-1 esterase was within normal limits. Angioedema of the intestine was diagnosed by computed tomography of the gastrointestinal tract, or after an ultrasound examination, or during surgery, the symptoms disappeared after discontinuation of the ACE inhibitor. When performing differential diagnosis of abdominal pain in patients taking ACE inhibitors, you should also consider angioedema of the intestine.

Anaphylactic reactions in patients on hemodialysis

In patients who underwent hemodialysis through a polyacrylonitrile membrane (for example, AN69) and who simultaneously received ACE inhibitors, cases of anaphylactic shock have been recorded, so avoid this combination.Patients are recommended to use either another type of dialysis membrane, or another type of antihypertensive drug.

Anaphylactic reactions in patients during apheresis of LDL

Rarely in patients who received ACE inhibitors during the apheresis of LDL with dextran sulfate, life-threatening anaphylactic reactions developed. Such reactions were prevented by abolishing the administration of ACE inhibitors prior to each apheresis procedure.

Hepatotoxicity

In rare cases, the administration of ACE inhibitors was accompanied by a syndrome that began with cholestatic jaundice or hepatitis and developed into fulminant liver necrosis and in several cases resulted in death. The mechanism of this syndrome is unclear. In patients receiving the Equator, with the development of jaundice or increased activity of liver enzymes, it is necessary to cancel the Equator with subsequent monitoring of their condition.

Liver failure

In patients with impaired liver function, T1 / 2 amlodipine is elongated. At the moment, recommendations on the dosage regimen have not been developed, so the Equator should be administered with caution, having previously estimated the expected benefit and the potential risk of treatment.

Hematological toxicity

In rare cases, neutropenia, agranulocytosis, thrombocytopenia and anemia have been reported in patients receiving ACE inhibitors. In patients with normal renal function and in the absence of other aggravating factors, neutropenia is rare. Neutropenia and agranulocytosis are reversible and disappear after the withdrawal of the ACE inhibitor. The equator should be used with extreme caution in patients with vascular collagen, during immunosuppressive therapy, during treatment with Allopurinol or procainamide, or in a combination of these aggravating factors, especially in the presence of a previous impairment of kidney function. Some of these patients developed serious infectious diseases, which in a few cases did not undergo correction with antibiotic therapy. During treatment with the drug Equator it is recommended to periodically monitor the level of leukocytes in such patients, and also to warn them about the need to report the appearance of the first signs of an infectious disease.

Cough

Cough was often recorded during the use of ACE inhibitors. As a rule, cough is unproductive, persistent and stopped after the drug was discontinued.With a differential diagnosis of cough, one should also consider a cough caused by the use of ACE inhibitors.

Surgery / general anesthesia

In patients undergoing major surgery or during general anesthesia drugs, resulting in hypotension, lisinopril may block angiotensin 2 after compensatory renin release. If arterial hypotension develops, probably as a result of the above mechanism, it is possible to correct the increase in BCC.

Elderly patients

Older patients with impaired renal function should be corrected for the dose of the drug Equator.

Hyperkalemia

In some patients who received ACE inhibitors, an increase in the serum potassium level was observed. Risk group for the development of hyperkalemia consists of patients with renal failure, diabetes, congestive heart failure, dehydration, metabolic acidosis or while receiving potassium-sparing diuretics, supplementation with potassium, potassium-based salt substitutes or any other medications, leading to an increase in potassium level in serum blood (for example, heparin).If you need a simultaneous intake with the above drugs should monitor the concentration of potassium in the blood serum.

Patients with low body weight, low growth patients and patients with severe liver dysfunction may need a dose reduction.

Equator does not have any adverse effect on the metabolism and lipids of blood plasma and can be used in the treatment of patients with bronchial asthma, diabetes and gout.

During treatment, it is necessary to control body weight and monitor the dentist (to prevent soreness, bleeding and gingival hyperplasia).

Impact on the ability to drive vehicles and manage mechanisms

Equator can affect the ability to drive vehicles and complex mechanisms. Predominantly at the beginning of treatment, transient arterial hypotension and dizziness may occur. Therefore, at the beginning of the treatment, patients are advised to avoid driving controls, work with mechanisms and perform other work that requires concentration.

Drug Interactions

Lisinopril

Potassium-sparing diuretics (e.g., spironolactone, amiloride and triamterene), dietary supplementation with potassium kalisodergaszczye salt substitutes and other medicines capable of increasing potassium levels in the serum (e.g., heparin) can cause hyperkalemia when combined with ACE inhibitors, particularly in patients with renal insufficiency and other kidney diseases in the anamnesis. When assigning a drug that affects the concentration of potassium, together with lisinopril should monitor the concentration of potassium in blood serum. Therefore, co-administration should be carefully justified and carried out with extreme caution and regular monitoring as the level of potassium in the blood serum and renal function. Potassium-sparing diuretics can be taken together with the preparation of Equator only under the condition of medical control.

In case of diuretics to the patient receiving the Equator, hypotensive effect usually increases. Therefore, it is necessary to take with special care the Equator in combination with diuretics.

Lizinopril softens the potassium-diuretic effect of diuretics.

With the simultaneous use of other antihypertensive drugs may increase the hypotensive effect of the drug Equator.

With simultaneous administration with nitroglycerin, other nitrates or vasodilators, a more pronounced decrease in blood pressure is possible.

When used simultaneously with ACE inhibitors, tricyclic antidepressants / antipsychotics, agents for general anesthesia, opioid analgesics: a more pronounced decrease in blood pressure is possible.

Ethanol (alcohol) enhances the hypotensive effect of the drug.

Allopurinol, procainamide, cytostatics or immunosuppressants (systemic SCS) may increase the risk of developing leukopenia while being used with ACE inhibitors.

Aitacids and colestyramine, when taken concomitantly with ACE inhibitors, reduce the bioavailability of the latter.

Sympathomimetics can reduce the hypotensive effect of ACE inhibitors; it is necessary to carefully monitor the achievement of the desired effect.

With the simultaneous administration of ACE inhibitors and hypoglycemic drugs (insulin and hypoglycemic agents for oral administration), it is possible to increase the likelihood of lowering blood glucose and the risk of hypoglycemia.This phenomenon is most often observed during the first week of combined treatment and in patients with renal insufficiency.

With prolonged use of NSAIDs, including Acetylsalicylic acid in high doses, a decrease in the effectiveness of ACE inhibitors is possible. The additive effect of taking NSAIDs and ACE inhibitors is manifested by increased potassium levels in the blood serum and can lead to impaired renal function. These effects are usually reversible. It is very rare to develop acute renal failure, especially in elderly patients and patients in a state of dehydration.

The excretion of lithium can be delayed during simultaneous administration with ACE inhibitors and therefore, the concentration of lithium in serum should be monitored during this period. When combined with lithium preparations, it is possible to intensify the manifestation of their neurotoxicity (nausea, vomiting, diarrhea, ataxia, tremor, tinnitus).

Amlodipine

Studies among elderly patients have shown that diltiazem inhibits the metabolism of amlodipine, probably due to inhibition of the isoenzyme CYP3A4 (plasma concentration increases by almost 50% and the effect of amlodipine increases). It is impossible to exclude the possibility that stronger inhibitors of the isoenzyme CYP3A4 (i.e.ketoconazole, itraconazole, ritonavir) are able to increase the concentration of amlodipine in the blood plasma to a greater extent than diltiazem. Simultaneous use should be carried out with caution.

When used simultaneously with inducers of the isoenzyme CYP3A4 - with antiepileptic drugs (for example, carbamazepine, phenobarbital, phenytoin, fosphenytoin, primidon), rifampicin, herbal preparations containing St. John's wort - it is possible to reduce the concentration of amlodipine in the blood plasma. Clinical control is shown with the possible correction of amlodipine dose during treatment with CYP3A4 isoenzyme inducers and after their cancellation. Simultaneous use should be carried out with caution.

As monotherapy, amlodipine was well combined with thiazide and loop diuretics, agents for general anesthesia, beta-blockers, ACE inhibitors, long-acting nitrates, sublingual nitroglycerin, digoxin, warfarin, atorvastatin, sildenafil, antacid drugs (aluminum hydroxide, magnesium hydroxide) , simethicone, cimetidine, NSAIDs, antibiotics and oral hypoglycemic drugs.

Amlodipine does not significantly affect the pharmacokinetics of ethanol (alcohol).

Calcium preparations can reduce the effect of blockers of slow calcium channels.

Amlodipine does not cause significant changes in the pharmacokinetics of cyclosporine.

It is possible to reduce the hypotensive effect of the Equator with simultaneous admission with estrogens, adrenostimulators.

When used simultaneously with the preparation Equator procainamide, quinidine and other drugs that extend the QT interval may contribute to its significant elongation.

Analogues of the drug Equator

Structural analogs for the active substance (aggregate of active substances):

• Ecquard.

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