Pharmacological properties of the drug Equator
Equator is a combined antihypertensive drug containing two active components. Lisinopril belongs to the group of ACE inhibitors; it reduces the level of angiotensin II and aldosterone in the blood plasma and simultaneously increases the level of bradykinin, which has a vasodilatory effect. Under the influence of lisinopril, peripheral vascular resistance and blood pressure decrease, and IOC and renal blood flow may increase. Heart rate remains virtually unchanged. In patients with hyperglycemia, lisinopril helps restore impaired endothelial function. The antihypertensive effect develops 1 hour after administration, the maximum effect is achieved after 6 hours. The duration of action depends on the dose and is about 24 hours. The effectiveness of lisinopril is maintained with long-term use. When discontinuing therapy, no sharp and intense increase in blood pressure is observed due to drug withdrawal. Although the primary action of lisinopril is through the renin-angiotensin-aldosterone system, its use is also effective when renin levels are low. The use of lisinopril in patients with diabetes mellitus does not cause changes in blood glucose levels. Amlodipine is a calcium ion antagonist, a dihydropyridine derivative. By blocking slow calcium channels of the membrane, it prevents the transmembrane entry of calcium ions into cardiomyocytes and vascular smooth muscle cells. Under its action, vascular tone (arterioles) and peripheral vascular resistance decrease. By dilating arterioles and reducing afterload, amlodipine has an antianginal effect. Due to the fact that it does not cause the development of reflex tachycardia, its use reduces the myocardial oxygen demand. Amlodipine appears to dilate both intact and diseased coronary vessels, improving myocardial perfusion. Amlodipine is well absorbed after oral administration. It is widely distributed in the tissues of the body and is slowly eliminated, which ensures its long-lasting effect and makes it possible to take it once a day for 1 day. In patients with hypertension (arterial hypertension), taking amlodipine once a day significantly reduces blood pressure for at least 24 hours in both the supine and standing positions. The action of amlodipine develops slowly, so the likelihood of developing symptomatic hypotension is small. Amlodipine does not have adverse metabolic effects, including no effect on plasma lipid levels. The drug can be prescribed to patients with asthma, diabetes mellitus and gout. A calcium antagonist can cause an increase in the activity of the renin-angiotensin-aldosterone system, and lisinopril introduced into the drug ensures normalization of the body's response by counter-regulating the renin-angiotensin-aldosterone system. Lisinopril enters the systemic circulation unchanged. The maximum concentration in blood plasma is reached approximately 6 hours after administration. Bioavailability - 29%. Apart from ACE, it does not bind to other plasma proteins. It is not metabolized in the body and is excreted unchanged in the urine. The half-life is 12.6 hours. Free lisinopril is released quickly, and ACE-bound lisinopril is released more slowly, which contributes to the prolonged effect of the drug. In case of kidney disease, excretion slows down, so in this case, a reduction in the dose of the drug may be necessary. Lisinopril is eliminated by hemodialysis. Amlodipine after oral administration is slowly but almost completely absorbed from the digestive tract. Concomitant food intake does not affect its absorption. The maximum concentration in blood plasma is observed 6–10 hours after administration. The bioavailability of amlodipine is 64–80%, the volume of distribution is about 20 l/kg body weight. 95–98% of amlodipine is bound to plasma proteins. Metabolized mainly in the liver to inactive metabolites. About 10% of unchanged substance and 60% of metabolites are excreted in the urine. Elimination is biphasic, the half-life averages 35–50 hours. A stable equilibrium concentration is established after 7–8 days of administration. Amlodipine is not excreted during hemodialysis. The time to reach maximum plasma concentrations is similar in young and elderly patients. In elderly patients, the excretion of amlodipine is slightly reduced, the AUC value and half-life increase. No dose adjustment is required in elderly people. In case of liver pathology, the half-life of amlodipine is prolonged. In case of kidney diseases, the concentration of amlodipine in the blood plasma does not depend on the degree of kidney damage. When taking the drug Equator, there is no interaction between the active components, which is confirmed by pharmacokinetic studies. Important pharmacokinetic parameters (AUC, maximum plasma concentration, time to reach maximum concentration, half-life) did not differ when using active components in combination or separately. The absorption of the active ingredients of Equator does not depend on food intake. Due to the fact that the active components of Equator remain in the body for a long time, the drug can be used once a day.
Equator, tablets 5+10 mg, 30 pcs.
Manufacturer
Gedeon Richter, Hungary
Compound
1 tablet contains:
lisinopril dihydrate 10.88 mg, which corresponds to the content of lisinopril 10 mg,
amlodipine besilate 6.94 mg, which corresponds to the content of amlodipine 5 mg.
Excipients:
magnesium stearate 1 mg,
sodium carboxymethyl starch (type A) 4 mg,
microcrystalline cellulose 177.18 mg.
pharmachologic effect
Equator is a combination antihypertensive drug containing lisinopril and amlodipine.
Lisinopril is an ACE inhibitor that reduces the levels of angiotensin II and aldosterone in the blood, while simultaneously increasing the level of bradykinin, a vasodilator mediator. Affects tissue renin-angiotensin systems. Reduces OPSS and blood pressure, pre- and afterload, pressure in the pulmonary capillaries, does not affect heart rate, while it is possible to increase cardiac output and increase blood flow in the kidneys. Dilates arteries more than veins. Improves blood supply to ischemic myocardium.
With long-term use, it helps reduce hypertrophy of the myocardium and the walls of resistive arteries. Increases myocardial tolerance to physical activity in patients with chronic heart failure. Plays a role in restoring endothelial function damaged as a result of hyperglycemia.
Increases life expectancy in chronic heart failure. Slows the progression of left ventricular dysfunction after myocardial infarction not complicated by heart failure.
The hypotensive effect is observed 1 hour after taking the drug orally, reaching a maximum after 6 hours. The duration of action depends on the dose and is 24 hours. With long-term treatment, the effectiveness does not decrease. With abrupt cessation of treatment, withdrawal syndrome with a sharp increase in blood pressure does not occur.
Despite the primary effect, which manifests itself in the effect on the RAAS, it is also effective in arterial hypertension with low renin levels. Lisinopril reduces albuminuria not only due to a decrease in blood pressure, but also as a result of changes in the hemodynamics of the glomerular apparatus and its tissue structure. Does not affect blood sugar levels in patients with diabetes and does not increase the incidence of hypoglycemia. Amlodipine is a third-generation slow calcium channel blocker that has antianginal and hypotensive effects. Prevents the entry of calcium into myocardial cells and, to a greater extent, into smooth muscle cells of the vascular wall. Reduces the tone of smooth muscles of arterioles, peripheral vascular resistance and, consequently, blood pressure.
It has an antianginal effect by dilating arterioles and arteries and reducing afterload. Reduces the need for oxygen and energy consumption of the myocardium, because does not cause reflex tachycardia. Probably, due to the expansion of the coronary arteries and arterioles, it increases the oxygen supply to intact (especially with vasospastic angina) and ischemic areas of the myocardium. For angina pectoris, it improves exercise tolerance, prevents the development of an angina attack and the formation of an ischemic ST interval, reducing the frequency of angina attacks and the need for the use of nitroglycerin.
Does not affect the conductivity and contractility of the myocardium. It has a long-term, dose-dependent hypotensive effect. Does not reduce left ventricular ejection fraction. Reduces left ventricular hypertrophy. It has an antiatherosclerotic and cardioprotective effect in ischemic heart disease. Use during therapy with digoxin, diuretics and ACE inhibitors does not increase the risk of death in patients with chronic heart failure (III-IV functional class according to the NYHA classification).
Slow absorption, wide distribution in the body and slow excretion ensure a long-lasting effect, allowing you to take the drug 1 time. For more than 24 hours, it provides a significant reduction in blood pressure in the sitting and lying position from a clinical point of view. The effect develops gradually, 2-4 hours after administration and is not accompanied by arterial hypotension.
Inhibits platelet aggregation, enhances glomerular filtration, has a weak natriuretic effect, and does not increase microalbuminuria in diabetic nephropathy.
Does not have a negative effect on metabolic processes, does not change the level of plasma lipids. Can be prescribed to patients with concomitant bronchial asthma, diabetes mellitus and gout.
The combination of lisinopril with amlodipine in one drug helps prevent the development of possible undesirable effects caused by counterregulation of any of the active substances. Thus, a blocker of slow calcium channels, directly dilating arterioles, can lead to sodium and fluid retention in the body and, therefore, can activate the RAAS. An ACE inhibitor blocks this process and normalizes reactions to salt load.
Indications
Essential arterial hypertension (if combination therapy is necessary).
Use during pregnancy and breastfeeding
The drug is contraindicated for use during pregnancy. If pregnancy is detected, treatment should be stopped as soon as possible.
Taking lisinopril in the second and third trimesters of pregnancy can cause damage and death to the fetus as a result of the effect on its kidneys
(hypotension, renal failure, hyperkalemia). A decrease in the amount of amniotic fluid can lead to deformation of the skull and face, impaired development of the limbs, pulmonary hypoplasia and fetal death. There are no data on similar or other effects in earlier pregnancy.
Taking the drug during lactation is contraindicated due to the excretion of amlodipine in breast milk. There are no data indicating that lisinopril passes into breast milk.
Contraindications
- history of angioedema, incl. caused by the use of other ACE inhibitors; - hereditary or idiopathic angioedema; - hemodynamically significant stenosis of the aorta or mitral valve; — hypertrophic obstructive cardiomyopathy; - severe arterial hypotension; - cardiogenic shock; - pregnancy; - lactation period; - children and adolescents under 18 years of age (due to the 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 dihydropyridine derivatives.
Equator should be used with caution in cerebrovascular diseases (including cerebrovascular insufficiency), ischemic heart disease, severe bradycardia, tachycardia, chronic heart failure in the stage of decompensation, mild or moderate arterial hypotension, cardiovascular disease, severe autoimmune diseases (including including scleroderma, SLE), with suppression of bone marrow hematopoiesis, diabetes mellitus, hyperkalemia, condition after kidney transplantation, renal failure, sodium-restricted diet, in elderly patients, with liver failure.
In case of acute myocardial infarction and for one month after it.
Side effects
The adverse reactions encountered are usually mild and transient; discontinuation of treatment is required in rare cases.
Side effects caused by the combination drug do not occur more often than when each component is taken separately. The most common: headache (8%), dry cough (5%) and dizziness (3%). Possible: weakness, diarrhea, nausea, vomiting, orthostatic hypotension, skin itching, skin rash, swelling of the ankles, redness of the facial skin, chest pain, arthralgia (1-3%). The incidence of other side effects is less than 1%.
With increased sensitivity, angioedema of the face, limbs, lips, tongue, epiglottis and larynx may develop (0.1%). In such cases, treatment should be stopped immediately and the patient observed until all symptoms disappear completely.
From laboratory parameters: hyperkalemia, increased levels of creatinine, urea nitrogen, liver enzyme activity and blood bilirubin, especially in kidney disease, diabetes mellitus and renovascular hypertension.
From the hematopoietic organs: leukopenia, neutropenia, agranulocytosis (exposure to an ACE inhibitor), thrombocytopenia, erythrocytopenia; with long-term treatment, a slight decrease in the concentration of hemoglobin and hematocrit is possible.
Other rare adverse reactions:
From the cardiovascular system: arrhythmias, increased heart rate, tachycardia, probably as a result of an excessive decrease in blood pressure in patients at high risk of myocardial infarction, cerebrovascular stroke.
From the digestive tract: impaired intestinal function, dry mouth, abdominal pain, pancreatitis, hepatocellular or cholestatic jaundice, hepatitis, gingival hyperplasia, loss of appetite.
From the skin: urticaria, increased sweating, itching, alopecia.
From the genitourinary system: impaired renal function, frequent urination, oliguria, anuria, acute renal failure, uremia, proteinuria, impotence.
From the immune system: syndrome with the appearance of antinuclear antibodies, accelerated ESR and arthralgia; myalgia; erythema multiforme; fever.
From the central nervous system: increased drowsiness, muscle fasciculation of the limbs and lips, asthenia, mood lability, confusion.
Interaction
Lisinopril
Potassium-sparing diuretics (eg, spironolactone, amiloride, and triamterene), potassium supplements, potassium-containing salt substitutes, and other medications that can increase serum potassium levels (eg, heparin) may cause hyperkalemia when combined with ACE inhibitors, especially in patients with a history of renal failure and other kidney diseases.
When prescribing a drug that affects potassium concentrations concomitantly with lisinopril, serum potassium concentrations should be monitored. Therefore, simultaneous administration should be carefully justified and carried out with extreme caution and regular monitoring of both serum potassium levels and renal function.
Potassium-sparing diuretics can be taken together with the drug Equator only under medical supervision. If a diuretic is prescribed to a patient receiving Equator, the hypotensive effect is usually enhanced. Therefore, it is necessary to take Equator® with extreme caution in combination with diuretics. Lisinopril softens the kaliuretic effect of diuretics. With the simultaneous use of other antihypertensive drugs, the hypotensive effect of the drug Equator may be enhanced.
When taken simultaneously with nitroglycerin, other nitrates or vasodilators, a more pronounced decrease in blood pressure is possible. When used simultaneously with ACE inhibitors, tricyclic antidepressants/antipsychotics, general anesthesia, opioid analgesics: a more pronounced decrease in blood pressure is possible.
Ethanol enhances the hypotensive effect of the drug. Allopurinol, procainamide, cytostatics or immunosuppressants (systemic corticosteroids) may increase the risk of developing leukopenia when used simultaneously with ACE inhibitors.
Aitacids and cholestyramine, when taken simultaneously with ACE inhibitors, reduce the bioavailability of the latter.
Sympathomimetics may reduce the hypotensive effect of ACE inhibitors; it is necessary to carefully monitor the achievement of the desired effect. When taking ACE inhibitors and hypoglycemic drugs (insulins and oral hypoglycemic agents) simultaneously, the likelihood of a decrease in blood glucose concentrations and the risk of hypoglycemia may increase. This phenomenon is most often observed during the first week of combination treatment and in patients with renal failure. With long-term use of NSAIDs, including acetylsalicylic acid in high doses, the effectiveness of ACE inhibitors may decrease.
The additive effect when taking NSAIDs and ACE inhibitors is manifested by an increase in serum potassium levels and can lead to a deterioration in renal function. These effects are usually reversible. Very rarely, acute renal failure may develop, especially in elderly patients and patients in a state of dehydration.
Lithium excretion may be slowed during concomitant use with ACE inhibitors and therefore serum lithium concentrations should be monitored during this period. When used together with lithium drugs, it is possible to increase the manifestation of their neurotoxicity (nausea, vomiting, diarrhea, ataxia, tremor, tinnitus).
With the simultaneous use of ACE inhibitors and gold preparations (sodium aurothiomalate) intravenously, a symptom complex has been described, including facial flushing, nausea, vomiting and arterial hypotension.
Amlodipine
Studies in elderly patients have shown that diltiazem suppresses the metabolism of amlodipine, probably due to inhibition of the CYP3A4 isoenzyme (plasma concentration increases by almost 50% and the effect of amlodipine is increased).
We cannot exclude the possibility that stronger inhibitors of the CYP3A4 isoenzyme (i.e. ketoconazole, itraconazole, ritonavir) are capable of increasing the plasma concentration of amlodipine to a greater extent than diltiazem. Concomitant use should be done with caution.
When used simultaneously with inducers of the CYP3A4 isoenzyme - with antiepileptic drugs (for example, carbamazepshyum, phenobarbital, phenytoin, fosphenytoin, primidone), rifampicin, herbal preparations containing St. John's wort - a decrease in the concentration of amlodipine in the blood plasma is possible. Clinical monitoring with possible dose adjustment of amlodipine is indicated during treatment with inducers of the CYP3A4 isoenzyme and after their discontinuation. Concomitant use should be done with caution.
As monotherapy, amlodipine was well combined with thiazide and loop diuretics, general anesthesia, beta-blockers, ACE inhibitors, long-acting nitrates, sublingual nitroglycerin, digoxin, warfarin, atorvastatin, sildenafil, antacids (aluminum hydroxide, magnesium hydroxide) , simethicone, cimetidine, NSAIDs, antibiotics and oral hypoglycemic drugs.
Amlodipine does not have a significant effect on the pharmacokinetics of ethanol. Calcium supplements may reduce the effect of slow calcium channel blockers. Amlodipine does not cause significant changes in the pharmacokinetics of cyclosporine. It is possible to reduce the hypotensive effect of Equator when taken simultaneously with estrogens and adrenergic stimulants. When used simultaneously with Equator®, procainamide, quinidine and other drugs that prolong the QT interval can contribute to its significant prolongation.
How to take, course of administration and dosage
It is recommended for use in cases where taking drugs containing separately the active substances of Equator in the same doses does not provide the necessary blood pressure control. The drug is taken orally, regardless of food intake.
For patients not receiving antihypertensive drugs, the daily dose is 1 tablet.
In case of previous therapy with diuretics, the diuretic should be discontinued 2-3 days before starting to take Equator. If discontinuation of the diuretic is not possible, the initial dose of Equator is 1/2 tablet. After taking the drug, the patient must be provided with medical supervision for several hours due to the possible development of symptomatic hypotension.
For heart failure and severe arterial hypertension, the maintenance dose is 1 tablet.
In case of renal failure and CC 30-70 ml/min, half the usual initial dose is prescribed (since lisinopril is excreted by the kidneys). The maintenance dose depends on the individual response of the patient; during therapy, regular monitoring of renal function, potassium and sodium levels in the blood is required.
In case of liver diseases, the excretion of amlodipine may slow down, so the initial dose of Equator is 1/2 tablet. The use of the drug in this category of patients requires special caution.
Overdose
Symptoms: excessive peripheral vasodilation with a pronounced decrease in blood pressure, acute vascular insufficiency, water and electrolyte imbalance, renal failure, hyperventilation, tachycardia, bradycardia, dizziness, anxiety, cough.
Treatment: symptomatic therapy, monitoring of cardiac activity, blood pressure, diuresis and water-electrolyte balance, and, if necessary, its correction. With a pronounced decrease in blood pressure, the patient is placed in a lying position and the lower limbs are raised; If the therapeutic response to intravenous fluid replacement is unsatisfactory, dopamine may be required.
To stop the action of amlodipine, calcium gluconate can be administered intravenously. If necessary, intravenous administration of angiotensin II. Due to the slow absorption of amlodipine, in some cases the stomach is washed out and activated charcoal is used. Lisinopril is eliminated by hemodialysis; the strong degree of binding to blood proteins makes amlodipine dialysis ineffective.
Special instructions
Arterial hypotension: a pronounced decrease in blood pressure with the development of clinical symptoms can be observed in patients with reduced blood volume and/or sodium content due to diuretics, fluid loss, or for other reasons, for example, profuse sweating, prolonged vomiting and/or diarrhea. In case of arterial hypotension, the patient should be laid down and fluid loss should be replaced (iv infusion of 0.9% sodium chloride solution) if necessary. It is preferable that restoration of fluid and/or sodium loss be carried out before starting Equator therapy. It is necessary to monitor blood pressure after taking the initial dose.
Aortic and mitral stenosis: like all vasodilators, Equator® should be administered with caution to patients with left ventricular outflow tract obstruction and mitral valve stenosis.
Impaired renal function: in some patients with arterial hypertension without significant manifestations of renovascular diseases, an increase in creatinine and urea in the blood serum was observed, in most cases minimal or transient, more pronounced when taking ACE inhibitors and a diuretic simultaneously. This is most common in patients with a history of kidney disease.
Angioedema of the face, extremities, lips, tongue, vocal folds and/or larynx has been reported in patients taking an ACE inhibitor, including lisinopril. In these cases, taking Equator should be stopped immediately and the patient should be closely monitored until symptoms disappear completely. Swelling of the face, lips and limbs usually goes away on its own, however, antihistamines should be used to reduce the severity of symptoms. Angioedema, accompanied by swelling of the larynx, can be fatal. If swelling of the tongue, pharynx or larynx is detected, which is the cause of airway obstruction, emergency measures must be immediately initiated. Appropriate measures include: subcutaneous administration of 0.3-0.5 mg or slow intravenous administration of 0.1 mg of a 0.1% solution of epinephrine (adrenaline), followed by intravenous administration of corticosteroids and antihistamines and simultaneous monitoring of vital functions.
Swelling of the gastrointestinal tract wall has rarely occurred in patients taking ACE inhibitors. These patients complained of abdominal pain (with or without nausea and vomiting); in some cases, no previous facial edema was observed and C-1 esterase activity was within normal limits. Angioedema was diagnosed by computed tomography of the gastrointestinal tract, or after ultrasound examination, or during surgery, the symptoms disappeared after stopping the ACE inhibitor. Swelling of the gastrointestinal tract wall should be included in the differential diagnostic range of abdominal pain in patients taking ACE inhibitors.
Anaphylactic reactions in patients undergoing hemodialysis: Cases of anaphylactic shock have been reported in patients undergoing hemodialysis through a polyacrylonitrile membrane (eg AN 69) and who were concomitantly receiving ACE inhibitors, so this combination should be avoided. Patients are advised to use either a different type of dialysis membrane or a different class of antihypertensive drug.
Anaphylactic reactions in patients during LDL apheresis: Rarely, life-threatening anaphylactic reactions have developed in patients receiving ACE inhibitors during LDL apheresis with dextran sulfate. Such reactions were prevented by discontinuation of ACE inhibitors before each apheresis procedure.
Desensitization by wasp or bee venom: Sometimes patients taking ACE inhibitors have developed anaphylactic reactions when desensitized by hymenoptera venom (for example, wasps or bees). Such life-threatening situations can be avoided with timely discontinuation of ACE inhibitors.
Hepatotoxicity: In rare cases, the use 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 led to death. The mechanism of this syndrome is unclear. Patients receiving Equator® who develop jaundice or have elevated liver enzymes should discontinue Equator and monitor their condition.
Liver failure: in patients with impaired liver function, T1/2 of amlodipine is prolonged. At the moment, recommendations on the dosage regimen have not been developed, so Equator should be prescribed with caution, having previously assessed the expected benefits and potential risks 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 discontinuation of the ACE inhibitor.
Equator should be used with extreme caution in patients with collagen vascular disease, those receiving immunosuppressive therapy, during treatment with allopurinol or procainamide, or a combination of these aggravating factors, especially in the presence of pre-existing renal impairment. Some of these patients developed serious infectious diseases, which in several cases did not respond to antibiotic therapy. When prescribing Equator, it is recommended to periodically monitor the level of leukocytes in such patients, as well as warn them of the need to report the appearance of the first signs of an infectious disease.
Cough: Cough has been reported frequently during use of ACE inhibitors. As a rule, the cough is non-productive, constant and stopped after discontinuation of the drug. When making a differential diagnosis of cough, cough caused by the use of ACE inhibitors must also be taken into account.
Surgery/general anesthesia: In patients undergoing major surgery or during general anesthesia with drugs that cause hypotension, lisinopril may block the formation of angiotensin II following compensatory renin release. If arterial hypotension develops, probably as a result of the above mechanism, correction can be made by increasing the volume of blood volume.
Elderly patients with impaired renal function should undergo a dose adjustment of the drug Equator.
Hyperkalemia: Increases in serum potassium levels have been observed in some patients receiving ACE inhibitors. Patients at risk for the development of hyperkalemia include patients with renal failure, diabetes mellitus, acute heart failure, dehydration, metabolic acidosis, or while taking potassium-sparing diuretics, potassium supplements, potassium-containing salt substitutes, or any other medications that increase serum potassium levels blood (for example, heparin). If necessary, simultaneous use with the above drugs should monitor the concentration of potassium in the blood serum.
Patients with low body weight, patients of short stature and patients with severe liver dysfunction may require a dose reduction.
Equator does not have any adverse effect on metabolism and blood plasma lipids and can be used in the treatment of patients with bronchial asthma, diabetes and gout.
During treatment, body weight control and dental supervision are necessary (to prevent pain, bleeding and gum hyperplasia).
Impact on the ability to drive vehicles and operate machinery:
The equator can affect the ability to drive vehicles and complex machinery. Transient hypotension and dizziness may occur mainly at the beginning of treatment. Therefore, at the beginning of treatment, patients are advised to avoid driving vehicles, operating machinery, and performing other work that requires concentration.
Release form
The tablets are round, flat, white or almost white, chamfered, scored on one side and engraved “A+L” on the other side.
Storage conditions
At a temperature not exceeding 25 °C
Best before date
3 years
Active substance
Amlodipine, Lisinopril
Conditions for dispensing from pharmacies
On prescription
Dosage form
pills
Purpose
For adults as prescribed by a doctor
Indications
Hypertension
Barcode and weight
Barcode: 5997001326848, 5997001360828 Weight: 0.016 kg
Use of the drug Equator
The drug is prescribed if it is not possible to achieve the desired reduction in blood pressure with monotherapy with one of the components included in the drug. The dose of the drug for adults who do not take other antihypertensive drugs is 1 tablet per day, regardless of meals. Patients taking diuretics should stop taking them 2-3 days before starting therapy with Equator. If this is not possible, the initial dose of the drug should be 1/2 t of tablet per day. In this case, after the first dose of the drug, the patient’s condition should be monitored due to the possibility of developing symptomatic hypotension. In case of renal failure, it is recommended to reduce the initial dose of the drug. The maintenance dose is determined individually depending on the response to the drug and subject to sufficiently frequent monitoring of kidney function indicators, potassium and sodium levels in the blood serum. In case of liver failure, the elimination of amlodipine from the body may slow down, so the drug should be used with extreme caution in these patients.
"Equator" during pregnancy
An impressive list of contraindications to taking the drug includes pregnancy. The fact is that the main active ingredient, lisinopril, penetrates the placenta, which can cause developmental disorders of the fetus in the womb:
- decreased blood pressure;
- hypoplasia of the skull;
- renal failure;
- hyperkalemia.
Equator should not be taken during pregnancy.
The baby may die before being born. Therefore, taking Equator during pregnancy is prohibited. The same can be said about breastfeeding - the substances of the drug penetrate into the milk, as a result, during lactation, treatment with Equator or any other drugs that contain lisinopril as a component is prescribed only as a last resort.
Side effects of the drug Equator
Usually transient, mild and rarely require discontinuation of the drug. The most common symptoms are headache, cough and dizziness. Possible weakness, diarrhea, nausea, vomiting, orthostatic hypotension, skin itching and rash, swelling, flushing of the facial skin, chest pain, arthralgia. With increased sensitivity, angioedema of the face, extremities, lips, epiglottis and larynx may develop; in this case, the drug is immediately discontinued, the patient should be under medical supervision until the symptoms completely disappear. When using other drugs of the ACE inhibitor group, the development of agranulocytosis was noted, so the possibility of its occurrence cannot be excluded when using Equator. With long-term use of the drug, hemoglobin and hematocrit levels may decrease slightly. Hyperkalemia, increased levels of creatinine, residual nitrogen, as well as increased activity of liver enzymes and serum bilirubin levels are possible, especially in patients with kidney disease, diabetes mellitus or renovascular hypertension. The following rarely reported side effects are also possible: palpitation, tachycardia, dyspeptic symptoms, dry mouth, abdominal pain, pancreatitis, hepatocellular or cholestatic jaundice, hepatitis, gingival hyperplasia, edema, urticaria, increased sweating, alopecia, impaired renal function, frequent urges to urination, oliguria, anuria, acute renal failure, uremia, proteinuria, impotence. Pathological conditions with the appearance of antibodies to nucleic acids, increased ESR and arthralgia, as well as the appearance of polymorphic (exudative) erythema are described.
Special instructions for the use of the drug Equator
The drug may cause significant symptomatic hypotension in patients with hyponatremia and/or hypovolemia caused by taking diuretics or dehydration due to another reason (intense sweating, prolonged vomiting, diarrhea). If hypotension occurs, the patient should be placed in a horizontal position and, if necessary, replenish the fluid deficiency (infusion of isotonic sodium chloride solution). Before prescribing the drug, it is necessary to eliminate hyponatremia or hypovolemia, and when taking the first doses of the drug, monitor blood pressure levels. In patients with aortic stenosis or hypertrophic cardiomyopathy, Equator, like other vasodilators, should be used with caution due to the narrowing of the outflow tract. In case of renal artery stenosis (especially bilateral or solitary kidney), in the presence of hyponatremia and/or hypovolemia, as well as in case of circulatory failure, the use of lisinopril can lead to impaired renal function up to acute renal failure (usually reversible and goes away after discontinuation of the drug). When taking any ACE inhibitor, including lisinopril, angioedema of the face, extremities, lips, epiglottis and larynx may develop. In this case, you must immediately discontinue the drug. For swelling localized to the face, lips and limbs, the use of antihistamines is indicated. Angioedema of the tongue, larynx or epiglottis can be fatal due to mechanical asphyxia, therefore, if it develops, urgent therapeutic measures should be taken: administer 0.3–0.5 ml of 0.1% epinephrine (adrenaline) solution (0.3 –0.5 mg subcutaneously or 0.1 ml (0.1 mg) intravenously slowly, prescribe corticosteroids and antihistamines, monitor the vital functions of the body. When using anesthetics that cause hypotension, lisinopril inhibits the compensatory release of angiotensin II. The hypotension that occurs in this case can be eliminated by administering an isotonic solution of sodium chloride. Carrying out hemodialysis using a polyacrylonitrile membrane (for example AN 69) in a patient taking an ACE inhibitor can lead to the development of anaphylactic shock, so their simultaneous use should be avoided. A different type of filter should be used or an antihypertensive drug of a different group should be prescribed. In some patients taking an ACE inhibitor, during desensitization to the venom of Hymenoptera insects, anaphylactic reactions occurred that were life-threatening. Their development can be avoided by temporarily interrupting the course of treatment with an ACE inhibitor. Due to the fact that the possibility of developing agranulocytosis cannot be unequivocally excluded, it is necessary to monitor the cellular composition of the blood during the treatment period. When using both active ingredients of the drug in usual doses in elderly patients, no decrease in effectiveness was detected, although their higher concentration in the blood plasma was noted, and therefore the dose of the drug in these patients should be selected with caution. With liver damage, the half-life of amlodipine increases, so the drug should be used with caution, individually assessing the expected effect and risk of therapy. During pregnancy and breastfeeding, the use of lisinopril, as well as other ACE inhibitors, is contraindicated; If pregnancy occurs, Equator should be discontinued immediately. The use of Equator during breastfeeding is not indicated, since lisinopril is excreted in breast milk. The drug may affect the ability to drive vehicles or operate potentially dangerous machinery (especially during the initial period of treatment), so this effect of the drug should be assessed individually.
Analogs
The closest analogue of "Equator" is the drug "Equacard", containing the same active ingredients - amlodipine (5 mg) and lisinopril (10 mg) in one tablet. Also a related drug is Eclamise.
All drugs are based on the interaction of two main components. They can be found separately, Amlodipine and Lisinopril tablets in different release forms and from different manufacturers.
The following drugs are also similar in action:
- "Perestance"
- "Enanorm"
- "Egipres"
- "Triapin"
- "Dalneva"
- "Coriprene"
- "Enal L CombI".
If side effects occur when taking Equator, it is usually changed to one of the above drugs.
Drug interactions Equator
The drug is used with extreme caution in combination:
- with potassium-sparing diuretics (for example, spironolactone, amiloride, triamterene), with potassium and table salt containing potassium. In this case, hyperkalemia may develop, especially with impaired renal function, so the drug can be prescribed only after a careful assessment of the benefit-risk ratio of therapy, subject to regular monitoring of serum potassium levels and renal function indicators;
- with allopurinol, cytostatics, immunosuppressants, corticosteroids, procainamide, since their combination with lisinopril can lead to the development of leukopenia.
Use with caution at the same time:
- with diuretics: a sharp decrease in blood pressure may be noted;
- with other antihypertensive drugs (additive effect);
- with NSAIDs (reduced antihypertensive effectiveness);
- with lithium salts (lithium accumulation may occur, so its level in the blood plasma should be regularly monitored);
- narcotic drugs, anesthetics (strengthen the hypotensive effect of lisinopril).
Lisinopril reduces potassium excretion when combined with diuretics. Lisinopril increases the manifestations of alcohol intoxication. No interactions between lisinopril and amlodipine have been identified.
Overdose of the drug Equator, symptoms and treatment
It may manifest itself as a pronounced dilatation of peripheral vessels, accompanied by an excessive decrease in blood pressure and reflex tachycardia. The patient is placed in a horizontal position with the lower limbs raised, heart function, blood pressure, and water-electrolyte balance are monitored; if necessary, these indicators are corrected and symptomatic treatment is carried out. In case of severe hypotension, intravenous infusion solutions are prescribed; in case of insufficient effectiveness, peripherally acting vasopressors are prescribed. To eliminate the effects of blockade of calcium channels, intravenous administration of calcium gluconate is indicated. Due to the slow absorption of amlodipine in the gastrointestinal tract, gastric lavage can be effective. Lisinopril is excreted from the body during hemodialysis, but amlodipine is not excreted during hemodialysis due to its high degree of binding to plasma proteins.
