Equator, pills 5+20mg, 30pcs

Composition

1 tablet contains

amlodipine 5 mg,

lisinopril 20 mg

Pharmacological action

Equator has a hypotensive, vasodilating, antianginal effect.

Indications

Essential hypertension (patients who are indicated for combination therapy).

Use during pregnancy and lactation

The drug is contraindicated for use during pregnancy.

If pregnancy is detected, treatment should be discontinued as early as possible.

Taking lisinopril in the second and third trimesters of pregnancy can cause damage and death of 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 deformity of the skull and face, impaired limb development, hypoplasia of the lungs 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 release of amlodipine in breast milk. There are no data indicating the penetration of lisinopril into breast milk.

Contraindications

• hypersensitivity to any component of the Equator, or to other dihydropyridine derivatives;
• a history of angioedema, including caused by the use of other ACE inhibitors, hereditary or idiopathic;
• hemodynamically significant stenosis of the aortic or mitral valve disease or hypertrophic cardiomyopathy;
• severe hypotension, cardiogenic shock;
• pregnancy;
• breastfeeding;
• age to 18 years (due to the lack of data on efficacy and safety of the Equator in this age group).

Side effects

The side effects that occur are usually mild and transient, and discontinuation of treatment is required in rare cases.

Side effects caused by the combined drug do not occur more often than in cases of taking each component separately. The most common symptoms are headache (8%), dry cough (5%) and dizziness (3%). Possible: weakness, diarrhea, nausea, vomiting, orthostatic hypotension, pruritus, skin rash, swelling of the ankles, redness of the face, chest pain, arthralgia (1-3%). The frequency of other side effects is less than 1%.

With hypersensitivity, 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 should be monitored until all symptoms disappear completely.

From the laboratory parameters: hyperkalemia, increased 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 (ACE inhibitor effect), 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 with a high risk of myocardial infarction, cerebrovascular stroke.

From the digestive tract: impaired intestinal function, dry mouth, abdominal pain, pancreatitis, hepatocellular or cholestatic jaundice, hepatitis, gum hyperplasia, decreased appetite.

From the skin: urticaria, increased sweating, pruritus, 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, lability of mood, confusion.

Interaction

Lisinopril potassium-sparing diuretics (such as spironolactone, amiloride, and triamterene), potassium supplements, potassium-containing salt substitutes, and other medications that can increase serum potassium levels (such as heparin) can lead to hyperkalemia when combined with ACE inhibitors, especially in patients with renal insufficiency and a history of other kidney diseases. When prescribing a drug that affects the concentration of potassium, simultaneously with lisinopril, the concentration of potassium in the blood serum should be monitored.

Therefore, concomitant use should be carefully justified and performed with extreme caution and regular monitoring of both serum potassium levels and renal function. Potassium-sparing diuretics can be taken together with 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® in combination with diuretics with extreme caution. Lisinopril softens the kaliyuretic effect of diuretics. With the simultaneous use of other antihypertensive drugs, it is possible to increase the hypotensive effect of Equator.

When taken concomitantly with nitroglycerin, other nitrates or vasodilators, a more pronounced decrease in blood pressure is possible. Concomitant use with ACE inhibitors of tricyclic antidepressants/ antipsychotics, general anesthesia, opioid analgesics: a more pronounced decrease in blood pressure is possible.

Ethanol enhances the antihypertensive effect of the drug. Allopurinol, procainamide, cytostatics or immunosuppressants (systemic corticosteroids) may increase the risk of leukopenia when co-administered with ACE inhibitors.

Aitacids and colestyramine when co-administered with ACE inhibitors reduce the bioavailability of the latter.

Sympathomimetics can reduce the antihypertensive effect of ACE inhibitors; careful monitoring should be carried out to achieve the desired effect. Concomitant use of ACE inhibitors and hypoglycemic medications (insulins and oral hypoglycemic agents) may increase the likelihood of a decrease in blood glucose concentration and the risk of hypoglycemia. Most often, this phenomenon is observed during the first week of combined treatment and in patients with renal insufficiency. Long-term use of NSAIDs, including high-dose acetylsalicylic acid, may reduce the effectiveness of ACE inhibitors. The additive effect of NSAIDs and ACE inhibitors is manifested by an increase in serum potassium levels and may lead to deterioration of renal function. These effects are usually reversible. Acute renal failure is very rare, especially in elderly and dehydrated patients.

The elimination of lithium may be slowed down during concomitant use with ACE inhibitors and therefore the concentration of lithium in the blood serum should be monitored during this period. When combined with lithium preparations, 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 hyperemia, nausea, vomiting, and arterial hypotension.

Amlodipine

Studies in elderly patients have shown that diltiazem inhibits the metabolism of amlodipine, probably due to inhibition of the CYP3A4 isoenzyme (plasma concentration increases by almost 50% and the effect of amlodipine increases). The possibility that stronger inhibitors of the CYP3A4 isoenzyme (i. e. ketoconazole, itraconazole, ritonavir)can not be excluded they can increase the concentration of amlodipine in blood plasma to a greater extent than diltiazem. Concomitant use should be carried out with caution. When used concomitantly with inducers of the CYP3A4 isoenzyme-with antiepileptic drugs (for example, carbamazepam, phenobarbital, phenytoin, phosphenytoin, primidone), rifampicin, herbal preparations containing St. John’s wort, it is possible to reduce the concentration of amlodipine in blood plasma.

Clinical control with possible dose adjustment of amlodipine is indicated during treatment with inducers of the CYP3A4 isoenzyme and after their withdrawal. Concomitant use should be carried out with caution.

As monotherapy, amlodipine was well combined with thiazide and loop diuretics, general anesthetics, 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 medications.

Amlodipine has no 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 the Equator when taken simultaneously with estrogens, adrenostimulants. When used concomitantly with Equator® procainamide, quinidine and other drugs that prolong the QT interval may contribute to its significant prolongation.

How to take it, course of use and dosage

Inside, regardless of food intake. It is recommended in cases when taking drugs that contain the active components of Equator separately in the same doses does not provide proper blood pressure control.

The daily dose for patients not taking antihypertensive drugs is 1 table.

The diuretic should be discontinued 2-3 days before the start of therapy, if such treatment is carried out. If the withdrawal of the diuretic is not possible, the initial dose of Equator is 1/2 table. per day, after which the patient should be monitored for several hours due to the possible development of symptomatic hypotension.

In case of heart failure and severe arterial hypertension, the maintenance dose is 1 table.

In case of renal insufficiency, with a creatinine clearance of 30-70 ml/min,1/2 of the usual initial dose is prescribed, since lisinopril is excreted by the kidneys. The maintenance dose of Equator depends on the individual response of the patient, treatment requires regular monitoring of kidney function, potassium and sodium levels in the blood.

Overdose

Symptoms: excessive peripheral vasodilation with a marked decrease in blood pressure, acute vascular insufficiency, impaired water-electrolyte balance, renal failure, hyperventilation, tachycardia, bradycardia, dizziness, anxiety, cough.

Treatment: symptomatic therapy, monitoring of heart activity, blood pressure, diuresis and water-electrolyte balance, if necessary, its correction. With a marked decrease in blood pressure, the patient is given a supine position, raise the lower extremities; if the therapeutic response to IV use of fluid substitutes is unsatisfactory, dopamine use may be required.

To stop the action of amlodipine, intravenous calcium gluconate can be administered. If necessary, intravenous use of angiotensin II. Due to the slow absorption of amlodipine, in some cases, the stomach is washed, activated charcoal is used.

Lisinopril is eliminated by hemodialysis; a strong degree of binding to blood proteins makes amlodipine dialysis ineffective.

Special instructions

Arterial hypotension: a marked decrease in blood pressure with the development of clinical symptoms may occur in patients with reduced BCC and/or sodium content due to diuretics, fluid loss, or other causes, such as heavy sweating, prolonged vomiting, and / or diarrhea. In case of arterial hypotension, the patient should be laid down and replaced with fluid loss (intravenous infusion of 0.9% sodium chloride solution), if necessary. Preferably, recovery of fluid and/or sodium loss should be performed prior to initiation of Equator therapy. Blood pressure should be monitored after the initial dose.

Aortic and mitral stenosis: like all vasodilators, Equator® should be used with caution in patients with left ventricular outlet obstruction and mitral valve stenosis.

Impaired renal function: in some patients with arterial hypertension without pronounced manifestations of renovascular diseases, an increase in serum creatinine and urea was observed, in most cases minimal or transient, more pronounced with simultaneous use of ACE inhibitors and a diuretic. 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 treated with an ACE inhibitor, including lisinopril. In these cases, Equator should be discontinued immediately and the patient should be closely monitored until symptoms disappear completely. Swelling of the face, lips, and extremities usually goes away on their own, but antihistamines should be used to reduce the severity of symptoms. Angioedema accompanied by laryngeal edema can be fatal. If edema of the tongue, pharynx or larynx is detected, which is the cause of airway obstruction, it is necessary to urgently start emergency measures. Appropriate measures include: subcutaneous use of 0.3-0.5 mg or slow intravenous use of 0.1 mg of 0.1% epinephrine (epinephrine), followed by intravenous use of corticosteroids and antihistamines and simultaneous monitoring of vital functions.

Patients taking ACE inhibitors rarely experienced edema of the gastrointestinal tract wall. 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 the normal range. Angioedema was diagnosed by computed tomography of the gastrointestinal tract, or after ultrasound examination, or during surgery, the symptoms disappeared after stopping taking an ACE inhibitor. Edema of the gastrointestinal tract wall should be included in the differential diagnostic series of abdominal pain in patients taking ACE inhibitors.

Anaphylactic reactions in patients undergoing hemodialysis: Cases of anaphylactic shock have been reported in patients undergoing polyacrylonitrile membrane hemodialysis (e. g., AN 69) and receiving concomitant ACE inhibitors, so this combination should be avoided. Patients are recommended to use either a different type of dialysis membrane or a different class of antihypertensive drug.

Anaphylactic reactions in patients with LDL apheresis: rarely, patients treated with ACE inhibitors during LDL apheresis with dextran sulfate developed life-threatening anaphylactic reactions. Such reactions were prevented by discontinuing ACE inhibitors before each apheresis procedure.

Desensitization by wasp or bee venom: sometimes patients treated with ACE inhibitors developed anaphylactic reactions when desensitized by hymenopteran venom (for example, wasps or bees). Such life-threatening situations can be avoided with timely withdrawal 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 experience increased liver enzyme activity should discontinue Equator ® and be monitored for their condition.

Liver failure: in patients with impaired liver function, the T1/2 of amlodipine is prolonged. Currently, no recommendations on the dosage regimen have been developed, so Equator should be prescribed with caution, having previously evaluated the expected benefit and potential risk of treatment.

Hematological toxicity: neutropenia, agranulocytosis, thrombocytopenia, and anemia have been reported in rare cases in patients treated with ACE inhibitors. Neutropenia is rare in patients with normal renal function and in the absence of other aggravating factors. Neutropenia and agranulocytosis are reversible and disappear after discontinuation of the ACE inhibitor. Equator should be used with extreme caution in patients with vascular collagenosis, during immunosuppressive therapy, during treatment with allopurinol or procainamide, or with a combination of these aggravating factors, especially in the presence of previous renal dysfunction. Some of these patients developed serious infectious diseases, which in several cases were not corrected by antibiotic therapy. When prescribing Equator, it is recommended to periodically monitor the level of white blood cells in such patients, as well as warn them about the need to report the first signs of an infectious disease.

Cough: Cough was frequently reported during the use of ACE inhibitors. As a rule, the cough is unproductive, permanent and stopped after discontinuation of the drug. In the differential diagnosis of cough, it is necessary to take into account the cough caused by the use of ACE inhibitors. Surgical intervention/General anesthesia: in patients undergoing extensive surgery or during general anesthesia with drugs that lead to hypotension, lisinopril may block the formation of angiotensin II after a compensatory release of renin. If arterial hypotension develops, probably as a result of the above mechanism, correction can be made by increasing the BCC.

Elderly patients with impaired renal function should adjust the dose of Equator.

Hyperkalemia: Elevated serum potassium levels were observed in some patients treated with ACE inhibitors. Patients with renal insufficiency, diabetes mellitus, acute heart failure, dehydration, metabolic acidosis, or concomitant use of potassium-sparing diuretics, potassium supplements, potassium-containing salt substitutes, or any other medications that increase serum potassium levels (for example, heparin) are at risk for hyperkalemia. If necessary, simultaneous use with the above drugs should monitor the concentration of potassium in the blood serum.

Patients with low body weight, short stature and patients with severe hepatic impairment may need to reduce the dose.

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

During treatment, it is necessary to monitor body weight and follow up with a dentist (to prevent soreness, bleeding and gum hyperplasia).

Influence on the ability to drive motor vehicles and manage mechanisms:

The equator can affect the ability to drive vehicles and complex mechanisms. Mainly at the beginning of treatment, transient hypotension and dizziness may occur. Therefore, at the beginning of treatment, patients are advised to avoid driving vehicles, working with mechanisms and performing other work that requires concentration of attention.

Form of production

Pills.

Storage conditions

In a dark place, at a temperature not exceeding 30 °C

Shelf life

2 years

Active ingredient

Amlodipine, Lisinopril

Conditions of release from pharmacies

By prescription

Dosage form

Tablets

Purpose

For adults as directed by your doctor

Indications

Hypertension