Equator is a drug with antihypertensive effect.
Release form and composition of Equator
Equator is available in the form of white tablets, the main active ingredients of which are: lisinopril dihydrate and amlodipine besylate.
The excipients of Equator tablets are: sodium carboxymethyl starch, magnesium stearate, microcrystalline cellulose.
Equator is available in dosages of 10 mg/5 mg and 20 mg/10 mg.
Pharmacological action of Equator
Equator is a combination drug.
The effect of the drug consists of the actions of its main substances - lisinopril and amlodipine.
Lisinopril, which is one of the main active ingredients of the drug, is an ACE inhibitor. Reduces blood pressure, peripheral vascular resistance, preload, and in patients with chronic heart failure increases myocardial tolerance to stress.
Long-term use leads to a decrease in the walls of resistive arteries and myocardial hypertrophy. Helps improve blood supply to ischemic myocardium.
Increases the life expectancy of people with chronic heart failure, inhibits the development of left ventricular dysfunction in patients who have suffered myocardial infarction.
Lisinopril begins to act an hour after entering the body. The maximum effect appears after 6 hours. In the case of arterial hypertension, improvement occurs in the first days after the start of therapy, and a stable effect develops after 1-2 months.
The second active ingredient in Equator, amlodipine, is a slow calcium channel blocker. Has antihypertensive and antianginal effect. By blocking calcium channels, it reduces the transmembrane transition of calcium ions into the cell.
The antianginal effect of amlodipine is associated with the expansion of peripheral and coronary arterioles and arteries.
Reduces the severity of myocardial ischemia during angina pectoris, reduces peripheral vascular resistance, myocardial oxygen demand, afterload on the heart, helps to increase the supply of oxygen to the myocardium, and prevents spasm of the coronary arteries.
With stable angina, it reduces the frequency of angina attacks, increases exercise tolerance, and helps reduce the consumption of nitroglycerin and other nitrates.
The antihypertensive effect is based on a direct vasodilating effect on vascular smooth muscle.
Indications for use of Equator
According to the instructions, Equator is prescribed as part of combination therapy for essential arterial hypertension.
Contraindications
According to the instructions, Equator cannot be used if:
- severe arterial hypotension;
- hemodynamically significant stenosis of the mitral valve or aorta;
- idiopathic or hereditary angioedema;
- a history of Quincke's edema;
- cardiogenic shock;
- unstable angina;
- hypertrophic obstructive cardiomyopathy;
- stenosis of the artery of a single kidney;
- heart failure after acute myocardial infarction (first 28 days);
- high level of sensitivity to any components included in the drug, other ACE inhibitors, other dihydropyridine derivatives;
- bilateral renal artery stenosis;
- pregnancy and lactation;
and also under the age of 18 years.
Directions for use and dosage of Equator
Equator tablets are intended for oral administration, regardless of food intake.
Equator tablets are taken once a day with water.
Before starting treatment with Equator (2-3 days before), you must stop taking diuretics. If this is not possible, then the initial dose of Equator should be 0.5 tablets.
To determine the optimal initial and maintenance dose for individuals with renal impairment and elderly patients, dosages should be determined for each patient individually, taking amlodipine and lisinopril separately.
Side effects of Equator
According to reviews, Equator can cause various side effects.
Nervous system: headache, dizziness, increased drowsiness, asthenia, muscle fasciculation of the lips and limbs, confusion, mood lability, feeling of a rush of blood to the face, fainting, increased fatigue, paresthesia, hypoesthesia, insomnia, peripheral neuropathy, nervousness, anxiety, depression , apathy, convulsions, ataxia, agitation, amnesia.
Cardiovascular system: orthostatic hypotension, arrhythmia, tachycardia, palpitations, vasculitis, worsening or development of heart failure.
Musculoskeletal system: arthralgia, myalgia, muscle cramps, back pain, myasthenia gravis, arthrosis.
Respiratory system: dry cough, rhinitis, shortness of breath, nosebleeds.
Digestive system: diarrhea, nausea, vomiting, bowel dysfunction, abdominal pain, dry mouth, cholestatic or hepatocellular jaundice, pancreatitis, gingival hyperplasia, hepatitis, decreased appetite, flatulence, constipation, anorexia, dyspepsia, gastritis, thirst.
Sense organs: tinnitus, diplopia, visual impairment, xerophthalmia, accommodation disturbance, conjunctivitis, eye pain.
Dermatological reactions: skin rash and itching, alopecia, increased sweating, xeroderma, dermatitis, skin pigmentation disorders.
Hematopoietic system: leukopenia, agranulocytosis, neutropenia, thrombocytopenia, erythrocytopenia.
Reproductive system: gynecomastia, impotence.
Urinary system: renal dysfunction, painful and frequent urination, nocturia, polyuria, dysuria, oliguria, acute renal failure, anuria, proteinuria, uremia.
Immune system: lupus-like syndrome, myalgia, fever, erythema multiforme.
Allergic reactions: urticaria, angioedema.
Other: redness of the face, weakness, chest pain, swelling of the ankles, chills, change in body weight.
Overdose on Equator
According to reviews to Equator, symptoms of drug overdose are manifested: excessive peripheral vasodilation, collapse, renal failure, water and electrolyte imbalance, shortness of breath, tachycardia, dizziness, bradycardia, anxiety, cough.
For the treatment of overdose, the following are used: symptomatic therapy, control of blood pressure, cardiac activity, water and electrolyte balance, diuresis.
Use during pregnancy and lactation
Equator tablets are contraindicated during pregnancy, since lisinopril penetrates the placental barrier and has a negative effect on the fetus, and the safety of using amlodipine during pregnancy has not been studied.
If there is a need to take the drug during lactation, breastfeeding should be stopped.
Interaction with other drugs
The drug interactions with Equator are the same as with Lisinopril and Amlodipine.
Storage conditions for Equator
The equator is stored in a place out of reach of children at a temperature of no more than 25º.
In practice, combination medications are very often used to effectively control blood pressure. One of them is Equator tablets.
They contain lisinopril and amlodipine, which affect various mechanisms of blood pressure regulation. Therefore, their use in combination gives a more pronounced hypotensive effect than the use of single drugs. Instructions for use Equator contains all the key information, so it must be read before use.
The medication contains amlodipine and lisinopril. These active ingredients have a long history of use for the treatment of hypertension.
Amlodipine is selective. According to the instructions for use, its action is based on the ability to reduce the flow of individual ions into the muscle cells of the heart and blood vessels.
This leads to their expansion and a decrease in peripheral pressure - one of the key components of hypertension. At the same time, amlodipine has a pronounced cardioprotective effect, since it improves blood supply to the heart muscle and reduces the load on it.
Equator tablets contain lisinopril, one of the most common ACE inhibitors (angiotensin-converting enzyme). It has been used in practice since the early 90s of the 20th century. Its difference from other tablets in this group is its longer duration of action.
Manufacturer
The manufacturer of the drug Equator is the famous Hungarian pharmaceutical company Gedeon Richter, which specializes in the production of cardiac, hormonal, anti-inflammatory and antibacterial drugs. The blood pressure pills in question are successfully used by patients in our country.
Gedeon Richter produces Equator blood pressure tablets in different ratios of active ingredients. According to the instructions for use, there are the following dosages of Equator:
- 5 mg amlodipine and 10 mg lisinopril (Equator 5 / 10–10 or 30 tablets);
- 5 mg amlodipine and 20 mg lisinopril (Equator 5 / 20–10 or 30 tablets)
- 10 mg amlodipine and 20 mg lisinopril (Equator 10 / 20–10 or 30 tablets);
Currently, such release forms as Equator 5/5, Equator 10/10 and instructions for them, respectively, do not exist, but their appearance is possible in the future.
What are these pills for?
You can find information about what Equator tablets are prescribed for below. It is used for primary disease, when there is an increase in pressure that is not caused by a dysfunction of any organ. Without adequate treatment for this condition, numerous complications are possible:
- dissection of the aortic wall;
- stroke (ischemic or hemorrhagic);
- decreased vision;
- renal failure.
Typically, the drug Equator for blood pressure is prescribed to patients who have previously taken other antihypertensive tablets, but they did not achieve target pressure values. Various forms of the Equator medication allow you to use tablets for all stages of high blood pressure.
The presence of lisinopril, according to the instructions for use, makes the tablets preferable if the patient has heart failure, diabetes mellitus and decreased filtration capacity of the kidneys. The medicine Equator 10/20 in the form of 10 or 30 tablets is prescribed only when the patient has previously taken amlodipine and lisinopril in a similar dosage separately.
Acute coronary syndrome
Instructions for use
Before starting treatment, the patient is advised to carefully read the instructions for use of the medication. This allows you to increase the effectiveness of drug therapy, as well as avoid serious side effects from taking it.
How to use?
The patient must use blood pressure medication for a long time. You need to take the tablet every day in the morning at a fixed time. Wash down the Equator with a sufficient amount of plain water. The use of carbonated drinks and dairy products for this purpose is prohibited.
If the patient missed taking Equator, then according to the instructions for use, he takes this dose of the medication as quickly as possible. During treatment, it is often recommended to keep a blood pressure diary, in which the patient records his blood pressure readings daily. This provides valuable information about the effectiveness of the prescribed tablets. If any side effects develop, the patient consults a doctor, who decides on the advisability of further use of Equator.
Dosage
The regimen for taking Equator does not depend on the dosage - 1 time per day (mainly in the morning). Instructions Equator 10/20 allows you to use the highest daily dose - 1 tablet. Food does not affect the pharmacological parameters of the tablets, so Equator can be taken with it.
special instructions
In case of insufficiency of renal function, it is recommended to use lisinopril and amlodipine tablets separately until a therapeutic constant dose is achieved. Only if the patient takes them in a fixed amount for a long time without developing side effects, is he allowed to switch to Equator.
There are a number of groups of patients who, according to the instructions for use, are prohibited from using Equator 5/20 pressure:
- children (due to lack of data on the safety of tablets);
- pregnancy (according to the instructions for use, lisinopril has a toxic effect on the fetus);
- hypersensitivity to the components of the tablets;
- damage to the renal artery, which led to its stenosis;
- hemodynamic disturbance (shock) with a drop in blood pressure;
- with renal artery stenosis;
- with hemodynamic disturbances;
- development of edema after taking amlodipine.
If the patient develops renal failure, the dose of Equator 5/10 is adjusted. For diabetes mellitus, the concentration of glucose in the blood is carefully checked, since, according to the instructions for use, fluctuations in this indicator are possible.
In some patients, with prolonged use of Equator, a gradual increase in the concentration of potassium in the blood occurs. This is dangerous for the development of cardiac arrhythmias. Therefore, all patients who take the medicine Equator for blood pressure on a regular basis are advised to take an electrolyte test several times a year.
Compatibility of blood pressure medication with alcohol
Products that contain ethyl alcohol are not recommended to be taken with pharmacological agents. Using the example of several clinical cases, it was shown that drinking alcoholic beverages while taking Equator increases the hypotensive effect of the tablets.
Therefore, patients experienced aching headaches, dizziness and general fatigue. Changes in the pharmacodynamics of the drug, the incidence of side effects and the therapeutic outcome are also possible. And although there are no direct instructions in the instructions for the drug Equator, it has poor compatibility with alcohol.
Side effects
In general, the medicine is well tolerated by most patients. According to the instructions, the side effects of the medication are due to the characteristic features of the two active ingredients that are part of the Equator tablets. Instructions for use indicate the following possible side effects from the cardiovascular system:
- (decrease in blood pressure below 90/60 mmHg);
- rapid heartbeat (beat rate above 100 beats per minute);
- bradycardia;
- acute coronary syndrome (in patients at high risk of developing cardiovascular events);
- disturbance of the sinus rhythm of the heart, the occurrence of blockades of the cardiac impulse;
- ischemic stroke due to a rapid or excessive decrease in blood pressure;
- vasculitis (inflammation of the walls of blood vessels);
- the appearance of swelling in the lower extremities, especially in the evening;
- a burning sensation or pain in the chest.
If the patient has hypersensitivity to any of the components of the Equator, allergic reactions of varying severity develop. They manifest themselves according to the instructions for use as skin rash, a feeling of heaviness in the abdomen, indigestion, angioedema of the neck and head.
Also, Equator tablets for normalizing blood pressure affect the metabolic processes of blood glucose, which sometimes leads to an increase or decrease in its concentration in the blood. According to the instructions for use, cases of toxic effects of tablets on the liver are described with an increase in enzyme levels (AST, ALT), bilirubin, and in some patients - with the development of toxic hepatitis. There was inhibition of hematopoietic processes with a drop in the number of formed elements in the blood.
In some patients, while taking it, there was a violation of the filtration function of the kidneys and an increase in creatinine concentration. Episodes of frequent urination and pain during this process were also noted. From the nervous system, according to the instructions for use, cases of the following side effects have been recorded:
- drowsiness or sleep disturbances;
- severe dizziness, short-term loss of consciousness (syncope) due to decreased blood pressure;
- disturbance of sensory systems (tinnitus, changes in taste);
- paresthesia (feeling of crawling, numbness of body parts, areas of skin);
- increased muscle tone of the limbs;
- depression;
- emotional lability;
- increased fatigue, decreased performance when performing mental tasks;
- decreased vision;
- impaired coordination of precise movements.
Among the other side effects of the drug Equator, the instructions for use highlight the development of cough in patients due to lisinopril, broncho-obstructive syndrome, and the appearance of shortness of breath (due to heart failure). There is information about cases of sexual dysfunction in men with long-term use of the medication.
What can you do to avoid high blood pressure? This question worries many people susceptible to hypertension. In this article we will understand how Equator tablets affect the body, what are its indications for use, and in what cases they are not recommended.
Active ingredients and pharmacokinetics
Equator tablets are an antihypertensive drug, the main active ingredients of which are lisinopril and amlodipine.
Long-term use of lisinopril has a positive effect on blood supply, myocardial and artery hypertrophy. Lisinopril helps to effectively reduce blood pressure, peripheral vascular resistance, and pressure in the capillaries of the lungs. Begins to act one hour after administration. The maximum effect is achieved after six hours and lasts throughout the day.
After administration, lisinopril enters the bloodstream. It is not metabolized and is excreted in the urine. For a long time it provides a therapeutic effect, maintaining normal blood pressure.
Amlodipine has an antihypertensive effect, lowering blood pressure. Significant improvement is observed 6 hours after oral administration and persists for a day. Amlodipine has a beneficial effect on cardiac activity.
Equator tablets should be taken only as prescribed by a doctor.
Amlodipine is absorbed almost completely from the gastrointestinal tract. Metabolized in the liver. About 10% of the substance is excreted in the urine, 20-25% through the intestines.
The combination of these two active components, amlodipine and lisinopril, in Equator makes it possible to block the development of possible negative consequences caused by one of them.
In addition to lisinopril and amlodipine, the drug tablet contains:
- Sodium carboxymethyl starch;
- Microcrystalline cellulose;
- Magnesium stearate.
Instructions for dosage regimen, release form
There are 2 types of Equator tablets:
- tablets 5/10 mg;
- tablets 10/20 mg.
The tablets are white, with the letters A+L engraved on the sides. Packages may contain different numbers of tablets, it all depends on the expected duration of the course of treatment.
The optimal dosage is 1 tablet per day to normalize blood pressure. It is also the maximum dose. Depending on the patient’s condition and his body’s perception of the active ingredients of Equator, tablets with the required quantitative content of the main substances are prescribed.
You can take the drug at any time, no matter - before or after meals. The tablet is washed down with a sufficient amount of clean drinking water.
While taking Equator, it is important to monitor kidney function and the levels of potassium and sodium in the blood. If renal function is impaired, the drug should be immediately discontinued and replaced with another.
Contraindications and side effects
"Equator" is prescribed only if therapeutic treatment for high blood pressure has not brought a positive result. The drug may cause:
- arrhythmias, rapid heartbeat;
- heart failure;
- headaches and dizziness;
- excessive sleepiness;
- worsening mood;
- feeling of a rush of blood to the head;
- fainting, insomnia, constant feelings of anxiety;
- neuropathy;
- seizures;
- cough, shortness of breath;
- diarrhea, vomiting, constipation, nausea, flatulence;
- pain in the stomach and head;
- skin itching and rash;
- excessive sweating;
- back pain;
- swelling of the face, tongue, larynx;
- frequent urination;
- renal failure;
- visual impairment;
- impotence;
- fever;
- leukopenia, erythrocytopenia.
If adverse symptoms occur, you should immediately stop taking the drug
The negative effects that can be caused by the use of Equator appear no more often than when taking each of the active ingredients separately.
Contraindications to treatment with Equator are as follows:
- Quincke's edema;
- angioedema;
- arterial hypotension;
- angina pectoris;
- myocardial infarction suffered less than a month ago;
- stenosis of the renal arteries (for the drug in tablets 20/10 mg);
- pregnancy;
- lactation;
- age less than 18 years;
- individual intolerance to components.
Before you start taking the drug, you must carefully read the contraindications
When treated with Equator, it is not recommended to drive or operate other complex mechanisms, as this is unsafe. At the beginning of the course, you may feel dizzy, so you should not do any work that requires concentration.
If the patient used diuretics before starting treatment with Equator, arterial hypotension may occur, since the water-electrolyte balance was disturbed. To avoid this, you should stop taking diuretics 2-3 days before starting the course of Equator therapy.
Analogues
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.
"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.
Overdose
In case of an overdose of Equator, blood pressure drops sharply and the pulse quickens. To stabilize the patient's condition, gastric lavage is performed, colloids, vasoconstrictors, and calcium gluconate are administered.
Purpose of treatment
The decision to start therapy using Equator can only be made by a competent specialist who has written an appropriate prescription or prescription while the patient is in the hospital. Remember: self-medication is dangerous to your health!
Active ingredients
Lisinopril
- amlodipine
Release form, composition and packaging
Pills white or almost white, round, flat, chamfered, scored on one side and engraved “A+L” on the other.
Excipients: magnesium stearate, sodium carboxymethyl starch (type A), microcrystalline cellulose (type 101), microcrystalline cellulose (type 12).
10 pieces. - blisters (2) - cardboard packs.
Pills white or off-white, round, biconvex, with "CF2" engraved on one side.
Excipients: magnesium stearate, sodium carboxymethyl starch (type A), microcrystalline cellulose (type 101), microcrystalline cellulose (type 12).
10 pieces. - blisters (3) - cardboard packs.
Pills white or almost white, oblong, biconvex, with a score on both sides and an engraving “CF” to the left of the score and the number “5” to the right of the score on one side.
Excipients: magnesium stearate, sodium carboxymethyl starch, microcrystalline cellulose (type 12), microcrystalline cellulose (type 101).
10 pieces. - blisters (3) - cardboard packs.
Pills white or off-white, round, biconvex, with "CF3" engraved on one side.
Excipients: microcrystalline cellulose 101, microcrystalline cellulose 12, sodium carboxymethyl starch, magnesium stearate.
10 pieces. - blisters (1) - cardboard packs.
10 pieces. - blisters (3) - cardboard packs.
pharmachologic effect
Equator is a combination drug containing the active ingredients amlodipine and lisinopril.
Amlodipine
The dihydropyridine derivative is a blocker of slow calcium channels (SCBC), reduces the transmembrane transition of calcium ions into the cell (more into vascular smooth muscle cells than into cardiomyocytes).
It has a long-term dose-dependent hypotensive effect. The antihypertensive effect is due to a direct vasodilating effect on vascular smooth muscle. For arterial hypertension, a single dose provides a clinically significant reduction in blood pressure over 24 hours (in the patient’s “lying” and “standing” position).
Orthostatic hypotension with amlodipine is quite rare.
Amlodipine does not cause a decrease in exercise tolerance or left ventricular ejection fraction. Reduces the degree of left ventricular myocardial hypertrophy. It has no effect on myocardial contractility and conductivity, does not cause a reflex increase in heart rate, inhibits platelet aggregation, increases the glomerular filtration rate, and has a weak natriuretic effect. In diabetic nephropathy, it does not increase the severity of microalbuminuria. It does not have any adverse effect on metabolism and blood lipid concentrations and can be used in the treatment of patients with bronchial asthma, diabetes mellitus and gout. A significant decrease in blood pressure is observed after 6-10 hours, the duration of the effect is 24 hours.
Does not increase the risk of death or the development of complications and deaths in patients with CHF (III-IV class according to the NYHA classification) during therapy with diuretics and ACE inhibitors.
In patients with CHF (III-IV FC according to the NYHA classification) of non-ischemic etiology, when using amlodipine, there is a possibility of pulmonary edema.
Lisinopril
Lisinopril is an ACE inhibitor that prevents the conversion of angiotensin I to angiotensin II. A decrease in angiotensin II levels leads to a direct decrease in aldosterone secretion. Lisinopril reduces the degradation of bradykinin and increases the synthesis of prostaglandins. Reduces peripheral vascular resistance, blood pressure, preload and pressure in the pulmonary capillaries. Lisinopril provides a more pronounced expansion of arteries than veins. Some of the effects of lisinopril are mediated by its effect on the tissue renin-angiotensin system. Its long-term use leads to a decrease in hypertrophy of the myocardium and the walls of resistive arteries.
Lisinopril improves blood supply to the myocardium during ischemia.
The effect occurs within 1 hour after taking lisinopril orally. The maximum effect develops within 6-7 hours; the duration of the effect lasts 24 hours. In patients with arterial hypertension, the effect is observed during the first days after the start of treatment; a stable effect is achieved within 1-2 months of treatment. With abrupt discontinuation of lisinopril, cases of significant increases in blood pressure were not observed. Lisinopril provides both a decrease in blood pressure and a decrease in albuminuria. In patients with hyperglycemia, lisinopril helps restore the function of damaged glomerular endothelium. In patients with diabetes mellitus, lisinopril has no effect on blood glucose concentrations; the use of lisinopril does not lead to an increase in the incidence of hypoglycemia.
Equator
A combination drug containing amlodipine and lisinopril helps prevent the development of possible side effects caused by one of the active ingredients. For example, a slow calcium channel blocker, by causing dilation of arterioles, can lead to sodium and fluid retention in the body, which, in turn, can lead to activation of the renin-angiotensin-aldosterone system. An ACE inhibitor blocks this process and normalizes the response to salt load.
Pharmacokinetics
Amlodipine
Suction
After oral administration, amlodipine is well absorbed from the gastrointestinal tract. The average absolute bioavailability of amlodipine is 64-80%. Cmax in the blood serum is observed after 6-12 hours. Food intake does not affect the absorption of amlodipine.
Distribution
Most of the amlodipine found in the blood (97.5%) is bound to plasma proteins. C ss are achieved after 7-8 days of therapy. The average V d is 21 l/kg body weight, which indicates that most of the amlodipine is in the tissues, and a smaller part is in the blood. Amlodipine penetrates the BBB.
Metabolism and excretion
Amlodipine undergoes slow but active metabolism in the liver with no significant first-pass effect. Metabolites do not have significant pharmacological activity.
T1/2 from plasma varies from 35 to 50 hours, which allows taking the drug 1 time per day. T1/2 with repeated use is approximately 45 hours. About 60% of the dose taken orally is excreted by the kidneys mainly in the form of metabolites, 10% unchanged, and 20-25% through the intestines with bile. The total clearance of amlodipine is 0.116 ml/s/kg (7 ml/min/kg, 0.42 l/h/kg).
Amlodipine is not removed from blood plasma during hemodialysis.
Elderly patients: in elderly patients (over 65 years of age), the elimination of amlodipine is slower (T 1/2 - 65 hours) compared to young patients, but this difference is not clinically significant.
Patients with liver failure: prolongation of T1/2 in patients with liver failure suggests that with long-term use the accumulation of the drug in the body will be higher (T1/2 - up to 60 hours).
Patients with renal failure: renal failure does not significantly affect the kinetics of amlodipine.
Lisinopril
Suction
When lisinopril is taken orally, 25% of the active substance is absorbed into the gastrointestinal tract. Absorption of lisinopril does not depend on food intake. The average level of absorption is 30%, bioavailability is 29%.
Distribution
Cmax in blood plasma is achieved within 6-8 hours after oral administration. Lisinopril binds poorly to plasma proteins and poorly penetrates the BBB.
Metabolism
Lisinopril does not undergo biotransformation in the body.
Removal
T 1/2 is 12 hours.
Pharmacokinetics in selected patient groups
U patients with CHF absorption and clearance of lisinopril are reduced. In this category of patients, the absolute bioavailability of lisinopril is reduced by approximately 16%, but AUC increases by an average of 125% compared to healthy volunteers.
Impaired renal function leads to an increase in AUC and T1/2 of lisinopril, but these changes become clinically significant only when GFR decreases below 30 ml/min/1.73 m2.
In mild to moderate renal failure (creatinine clearance from 30 to 80 ml/min), the average AUC value increases by 13%, while in severe renal failure (creatinine clearance from 5 to 30 ml/min) there is a 4.5-fold increase in the mean AUC value .
In patients with liver cirrhosis, lisinopril absorption is reduced (by approximately 30%), but drug exposure is increased (by approximately 50%) compared to healthy volunteers due to decreased clearance.
In elderly patients, the plasma concentration of lisinopril and AUC are 2 times higher than in young patients.
Equator
Interaction between the active ingredients of the drug Equator is unlikely. The values of AUC, Cmax, time to reach Cmax, as well as T1/2 do not change compared to the values of each individual active substance. Eating does not affect the absorption of active substances. Long-term circulation of both active substances in the body allows you to take the drug once a day.
Indications
- arterial hypertension (in patients for whom combination therapy is indicated).
Contraindications
- hypersensitivity to lisinopril or any other ACE inhibitor;
- hypersensitivity to amlodipine or any other dihydropyridine derivative;
- hypersensitivity to any of the excipients;
- history of angioedema, incl. in connection with the use of ACE inhibitors;
- hereditary or idiopathic angioedema;
— shock (including cardiogenic);
- unstable angina (with the exception of Prinzmetal's angina);
- severe arterial hypotension (systolic blood pressure less than 90 mm Hg);
- hemodynamically significant obstruction of the left ventricular outflow tract (for example, with severe aortic stenosis, hypertrophic obstructive cardiomyopathy), hemodynamically significant mitral stenosis;
- unstable hemodynamic parameters during acute myocardial infarction (and within 1 month after it);
- simultaneous use with aliskiren and drugs containing aliskiren in patients with diabetes mellitus and/or moderate or severe renal impairment (GFR less than 60 ml/min/1.73 m2 body surface area);
- simultaneous use with angiotensin II receptor antagonists (ARA II) in patients with diabetic nephropathy;
- simultaneous use with neutral endopeptidase inhibitors (such as sacubitril);
- pregnancy;
- period of breastfeeding;
- age under 18 years (efficacy and safety have not been established).
Carefully: aortic stenosis, mitral stenosis, hypertrophic obstructive cardiomyopathy, arterial hypotension, cerebrovascular diseases (including cerebrovascular insufficiency), ischemic heart disease, non-ischemic heart failure FC III-IV, Prinzmetal's angina, SSSS (severe tachycardia or bradycardia), severe autoimmune systemic connective tissue diseases (including systemic lupus erythematosus, scleroderma), taking potassium-sparing diuretics, potassium preparations and potassium-based salt substitutes, hyperkalemia, hyponatremia, myelosuppression, diabetes mellitus, bilateral renal artery stenosis, renal artery stenosis in patients with a single kidney, renovascular hypertension, condition after kidney transplantation, renal failure, azotemia, hemodialysis using high-permeability membranes, primary aldosteronism, salt-restricted diet, conditions associated with a decrease in blood volume (including vomiting and diarrhea), old age , liver failure, simultaneous use with inhibitors or inducers of the CYP3A4 isoenzyme, simultaneous use with drugs containing aliskiren or angiotensin II receptor antagonists (increased risk of arterial hypotension, hyperkalemia and renal failure with double blockade of the RAAS), immunosuppressive therapy, simultaneous use of allopurinol or procainamide, or a combination of these complicating factors (risk of developing neutropenia and agranulocytosis), simultaneous use with lithium preparations, aggravated allergic history, simultaneous desensitization with an allergen from Hymenoptera venom, simultaneous LDL-apheresis procedure using dextran sulfate, gout, hyperuricemia, use during during major surgical interventions or during general anesthesia, in patients of the Negroid race.
Dosage
The drug is taken orally, regardless of food intake, with a sufficient amount of liquid.
Equator, tablets, 5 mg + 10 mg are indicated only for those patients whose optimal maintenance dose of amlodipine and lisinopril is 5 mg and 10 mg, respectively.
Equator, tablets, 5 mg + 20 mg are indicated only for those patients in whom the optimal maintenance dose of amlodipine and lisinopril is 5 mg and 20 mg, respectively.
Equator, tablets, 10 mg + 10 mg are indicated only for those patients whose optimal maintenance dose of amlodipine and lisinopril is 10 mg and 10 mg, respectively.
Equator, tablets, 10 mg + 20 mg are indicated only for those patients in whom the optimal maintenance dose of amlodipine and lisinopril is 10 mg and 20 mg, respectively.
The maximum daily dose of the drug Equator is 1 tablet.
Maximum daily doses of active substances in monotherapy: amlodipine - 10 mg, lisinopril - 40 mg.
If arterial hypotension develops at the beginning of therapy with Equator: if arterial hypotension develops, the patient should lie on his back, stop taking the drug and consult a doctor. Transient arterial hypotension usually does not require discontinuation of the drug, but the need to reduce the dose should be assessed. If it is necessary to select a dose, the drugs amlodipine and lisinopril should be used separately.
If the patient forgot to take a tablet of the drug Equator, then you should wait until the time of the next dose and take the drug at the usual dose. Do not take a double dose to make up for a missed dose.
Special patient groups
Patients with renal failure. To determine the optimal initial and maintenance dose for patients with renal failure, it is necessary to titrate doses and determine the dosage regimen on an individual basis, using lisinopril and amlodipine separately. During therapy with Equator, renal function should be monitored, as well as the content of potassium and sodium in the blood serum. If renal function deteriorates, Equator should be discontinued and therapy should be prescribed with correctly selected doses of the individual components.
Patients with liver failure. There may be a delay in the elimination of amlodipine in patients with impaired liver function. Clear recommendations regarding the dose of the drug Equator in such cases have not been established, so patients with impaired liver function should prescribe the drug with caution. To determine the optimal initial and maintenance dose for patients with liver failure, it is necessary to titrate doses and determine the dosage regimen on an individual basis, using lisinopril and amlodipine separately. Treatment should be started with lower doses, using caution.
Children and teenagers (up to 18 years old). The safety and effectiveness of Equator in children and adolescents have not been established.
Elderly patients (over 65 years old). Elderly patients should be treated with caution. Clinical studies have not identified age-related changes in the efficacy or safety profile of amlodipine and lisinopril. To determine the optimal maintenance dose, it is necessary to determine the dosage regimen on an individual basis, using lisinopril and amlodipine separately.
Side effects
The incidence of adverse reactions in patients taking the combination drug did not exceed that in patients receiving one of the active ingredients. Adverse reactions were consistent with data previously obtained for amlodipine and/or lisinopril. Adverse reactions were mild, transient and rarely required discontinuation of therapy. The most common adverse reactions with the combination drug were headache (8%), cough (5%), and dizziness (3%).
The frequency of adverse reactions is given separately for lisinopril and amlodipine. Below are the adverse drug reactions (ADRs) reported during separate use of amlodipine and lisinopril.
Determination of the frequency of adverse reactions: very often - 1/10 cases (≥10%), often - 1/100 cases (≥1% and<10%), нечасто - 1/1000 случаев (≥0.1% и <1%), редко - 1/10 000 случаев (≥0.01% и <0.1%), очень редко - менее 1/10 000 случаев (<0.01%), частота неизвестна - частота не могла быть установлена на основе имеющихся данных.
In each group, adverse reactions are presented in descending order of severity.
| Junkreaction | Amlodipine | Lisinopril |
| From the blood and lymphatic system | ||
| Decreased hemoglobin | - | Rarely |
| Decreased hematocrit | - | Rarely |
| Inhibition of bone marrow hematopoiesis | - | Very rarely |
| Leukopenia | Very rarely | Very rarely |
| Thrombocytopenia | Very rarely | Very rarely |
| Agranulocytosis | - | Very rarely |
| Hemolytic anemia | - | Very rarely |
| Neutropenia | - | Very rarely |
| Anemia | - | Very rarely |
| Lymphadenopathy | - | Very rarely |
| From the immune system | ||
| Allergic reactions | Very rarely | - |
| Autoimmune disorders | - | Very rarely |
| From the endocrine system | ||
| Syndrome of inappropriate antidiuretic hormone secretion | - | Rarely |
| Metabolism | ||
| Hyperglycemia | Very rarely | - |
| Hypoglycemia | - | Very rarely |
| Mental disorders | ||
| Mood lability | Infrequently | Infrequently |
| Sleep disorders | - | Infrequently |
| Hallucinations | - | Infrequently |
| Insomnia | Infrequently | - |
| Anxiety | Infrequently | - |
| Depression | Infrequently | Frequency unknown |
| Confusion | Rarely | Rarely |
| From the nervous system | ||
| Dizziness | Often | Often |
| Headache | Often | Often |
| Drowsiness | Often | - |
| Vertigo | - | Infrequently |
| Paresthesia | Infrequently | Infrequently |
| Dysgeusia | Infrequently | Infrequently |
| Fainting | Infrequently | Frequency unknown |
| Tremor | Infrequently | - |
| Hypesthesia | Infrequently | - |
| Parosmia (impaired sense of smell) | - | Rarely |
| Muscle hypertonicity | Very rarely | - |
| Peripheral neuropathy | Very rarely | - |
| Extrapyramidal disorders | Frequency unknown | - |
| From the side of the organ of vision | ||
| Visual impairment (including diplopia) | Often | - |
| Hearing and labyrinth disorders | ||
| Noise in ears | Infrequently | - |
| From the side of the heart | ||
| Feeling of heartbeat | Often | Infrequently |
| Myocardial infarction | Very rarely | Infrequently |
| Tachycardia | - | Infrequently |
| Ventricular tachycardia | Infrequently | - |
| Arrhythmia | Infrequently | - |
| Bradycardia | Infrequently | - |
| Atrial fibrillation | Infrequently | - |
| From the side of blood vessels | ||
| Orthostatic hypotension and associated symptoms | - | Often |
| “Rushes” of blood to the skin of the face | Often | - |
| Acute cerebrovascular accident (due to a pronounced decrease in blood pressure in high-risk patient groups) | - | Infrequently |
| Raynaud's syndrome | - | Infrequently |
| Vasculitis | Very rarely | - |
| Arterial hypotension | Infrequently | Often |
| From the respiratory system, chest organs and mediastinum | ||
| Dyspnea | Often | - |
| Cough | Infrequently | Often |
| Rhinitis | Infrequently | Infrequently |
| Bronchospasm | - | Very rarely |
| Allergic alveolitis | - | Very rarely |
| Eosinophilic pneumonia | - | Very rarely |
| Sinusitis | - | Very rarely |
| From the digestive system | ||
| Abdominal pain | Often | Infrequently |
| Nausea | Often | Infrequently |
| Dyspepsia | Often | Infrequently |
| Changing the rhythm of bowel movements | Often | - |
| Diarrhea | Often | Often |
| Constipation | Often | - |
| Vomit | Infrequently | Often |
| Dry mouth | Infrequently | Rarely |
| Pancreatitis | Very rarely | Very rarely |
| Gastritis | Very rarely | - |
| Intestinal angioedema | - | Very rarely |
| Gingival hyperplasia | Very rarely | - |
| From the liver and biliary tract | ||
| Hepatitis | Very rarely | - |
| Hepatitis (including hepatocellular or cholestatic) | - | Very rarely |
| Jaundice | Very rarely | Very rarely |
| Liver failure | - | Very rarely |
| Increased liver enzyme activity | Very rarely | Infrequently |
| From the skin and subcutaneous tissues | ||
| Alopecia | Infrequently | Rarely |
| Exanthema | Infrequently | - |
| Purpura | Infrequently | - |
| Skin depigmentation | Infrequently | - |
| Hyperhidrosis | Infrequently | Very rarely |
| Itchy skin | Infrequently | Infrequently |
| Skin rash | Infrequently | Infrequently |
| Hives | Infrequently | Rarely |
| Psoriasis | - | Rarely |
| Erythema multiforme | Very rarely | Very rarely |
| Angioedema | Very rarely | Rarely |
| Exfoliative dermatitis | Very rarely | - |
| Toxic epidermal necrolysis | Frequency unknown | Very rarely |
| Stevens-Johnson syndrome | Very rarely | Very rarely |
| Quincke's edema | Very rarely | - |
| Photosensitivity | Very rarely | - |
| Pemphigus vulgaris | - | Very rarely |
| Benign cutaneous lymphadenosis* | - | Very rarely |
| Increased sensitivity/angioedema of the face, arms and legs, lips, tongue, glottis and/or larynx | - | Rarely |
| From the musculoskeletal system | ||
| Muscle cramps | Often | - |
| Swelling in the ankle area | Often | - |
| Arthralgia | Infrequently | - |
| Myalgia | Infrequently | - |
| Backache | Infrequently | - |
| From the kidneys and urinary tract | ||
| Renal dysfunction | - | Often |
| Urination disorder | Infrequently | - |
| Nocturia | Infrequently | - |
| Frequent urination | Infrequently | - |
| Acute renal failure | - | Rarely |
| Uremia | - | Rarely |
| Oliguria | - | Very rarely |
| Anuria | - | Very rarely |
| From the genital organs and breast | ||
| Gynecomastia | Infrequently | Rarely |
| Impotence | Infrequently | Infrequently |
| General disorders | ||
| Edema | Often | - |
| Increased fatigue | Often | Infrequently |
| Asthenia | Often | Infrequently |
| Chest pain | Infrequently | - |
| Pain | Infrequently | - |
| Malaise | Infrequently | - |
| Laboratory and instrumental data | ||
| Increased creatinine and urea concentrations | - | Infrequently |
| Hyperkalemia | - | Infrequently |
| Hyperbilirubinemia | - | Rarely |
| Hyponatremia | - | Rarely |
| Decrease or increase in weight | Infrequently | - |
* A symptom complex has been reported that may include one or more of the following: fever, vasculitis, myalgia, arthralgia/arthritis, antinuclear antibody (ANA) positivity, increased ESR, eosinophilia and leukocytosis, skin rash, photosensitivity or other changes in the skin.
Overdose
Amlodipine
Symptoms: a pronounced decrease in blood pressure with the possible development of reflex tachycardia and excessive peripheral vasodilation (risk of developing severe and persistent arterial hypotension, including the development of shock and death).
Treatment: gastric lavage, administration of activated charcoal (especially in the first 2 hours after an overdose), maintaining the function of the cardiovascular system, elevated position of the lower extremities, monitoring heart and lung performance, monitoring blood volume and diuresis. To restore vascular tone - use vasoconstrictors (in the absence of contraindications to their use); to eliminate the consequences of blockade of calcium channels - intravenous administration. Hemodialysis is ineffective.
Lisinopril
Symptoms: marked decrease in blood pressure, dry mouth, drowsiness, urinary retention, anxiety, irritability.
Treatment: symptomatic therapy, infusion of 0.9% solution and vasopressors (if possible), blood pressure control, maintaining water and electrolyte balance. Hemodialysis is possible.
Drug interactions
Amlodipine
Contraindicated combinations of drugs
Dantrolene (IV administration)
In laboratory animals, cases of ventricular fibrillation with death and collapse have been reported during the use of verapamil and intravenous administration of dantrolene, accompanied by hyperkalemia. Due to the risk of developing hyperkalemia, simultaneous use of slow calcium channel blockers, incl. amlodipine, in patients susceptible to malignant hyperthermia, as well as in the treatment of malignant hyperthermia.
Grapefruit juice
Taking amlodipine with grapefruit or grapefruit juice is not recommended as the bioavailability of amlodipine may be increased in some patients, resulting in increased blood pressure lowering effects.
Inducers of the CYP3A4 isoenzyme
With simultaneous use of known CYP3A4 inducers, the concentration of amlodipine in the blood plasma may fluctuate. For this reason, it is necessary to both monitor blood pressure and adjust the dose of the drug during and after simultaneous use, especially with strong CYP3A4 inducers (for example, rifampicin, St. John's wort preparations).
CYP3A4 isoenzyme inhibitors
Concomitant use of amlodipine and strong or moderate CYP3A4 inhibitors (protease inhibitors, for example, ritonavir, azole antifungals, macrolides, for example, erythromycin or clarithromycin, verapamil or diltiazem) can lead to a significant increase in amlodipine concentrations. Clinical manifestations of these pharmacokinetic abnormalities may be more pronounced in elderly patients. In this regard, monitoring of the clinical condition and dose adjustment of the drug Equator may be required.
Simvastatin
Repeated administration of amlodipine at a dose of 10 mg in combination with simvastatin at a dose of 80 mg resulted in an increase in simvastatin exposure by 77% compared with simvastatin monotherapy. Therefore, patients receiving amlodipine should take simvastatin at a daily dose of no more than 20 mg.
Calcium preparations
May reduce the effect of BMCC.
Lithium preparations
When BMCC is used together with lithium preparations (no data are available for amlodipine), their neurotoxicity (nausea, vomiting, diarrhea, ataxia, tremor or tinnitus) may increase.
Baclofen
Strengthening the antihypertensive effect. Blood pressure and renal function should be monitored and the dose of amlodipine adjusted if necessary.
Amifostin
The antihypertensive effect of amlodipine may be enhanced.
Glucocorticoids
Decreased antihypertensive effect (retention of fluid and sodium ions as a result of the action of corticosteroids).
Tricyclic antidepressants, antipsychotics
There is an increased risk of orthostatic hypotension and increased antihypertensive effect (additive effect).
Tacrolimus
When used simultaneously with amlodipine, there is a risk of increasing the concentration of tacrolimus in the blood plasma. To avoid toxicity of tacrolimus when used concomitantly with amlodipine, the concentration of tacrolimus in the blood plasma of patients should be monitored and the dose of tacrolimus should be adjusted if necessary.
Tasonermin: when used concomitantly, amlodipine may increase systemic exposure tasonermina in blood plasma. In such cases, regular monitoring of tasonermin in the blood and dose adjustment if necessary is necessary.
Interaction of amlodipine with other drugs
For the treatment of arterial hypertension, amlodipine can be safely used with thiazide diuretics, alpha-blockers, beta-blockers and ACE inhibitors. In patients with stable angina, concomitant use of amlodipine with other antianginal drugs, such as nitrates long and short acting, beta blockers.
It is likely that the antianginal and antihypertensive effects of BMCC are enhanced when used simultaneously with thiazide and loop diuretics, ACE inhibitors, beta-blockers and nitrates, as well as their antihypertensive effect is enhanced when prescribed with alpha 1-blockers and antipsychotics.
Amlodipine does not cause a negative inotropic effect. However, some CBMCs may increase the negative inotropic effect of antiarrhythmic drugs that cause QT prolongation (eg, amiodarone and quinidine).
Unlike other BMCCs, no significant interaction was detected between amlodipine (3rd generation BMCCs) and NSAIDs, including indomethacin.
It is safe to administer amlodipine with oral hypoglycemic drugs.
Single dose sildenafil at a dose of 100 mg in patients with essential arterial hypertension had no effect on the pharmacokinetics of amlodipine.
Combined multiple doses of amlodipine at a dose of 10 mg and atorvastatin at a dose of 80 mg led to an insignificant change in the pharmacokinetic parameters of atorvastatin at steady state concentration.
Ethanol (beverages containing alcohol): amlodipine does not have a significant effect on the pharmacokinetics of ethanol with single or repeated use at a dose of 10 mg.
Interaction Research cyclosporine and amlodipine in healthy volunteers and in special groups of patients have not been conducted, with the exception of patients after kidney transplantation. Various studies of the interaction of amlodipine with cyclosporine in patients after kidney transplantation show that the use of this combination may not lead to any effect, or increase the minimum concentration of cyclosporine to varying degrees, up to 40%. Cyclosporine concentrations should be monitored in patients after kidney transplantation.
With the simultaneous use of amlodipine and digoxin renal clearance and serum digoxin concentrations do not change.
When used simultaneously warfarin with amlodipine, prothrombin time does not change.
When used simultaneously with cimetidine the pharmacokinetics of amlodipine does not change.
Amlodipine does not affect the degree of binding digoxin, phenytoin, warfarin and indomethacin with blood plasma proteins in vitro.
Aluminum and magnesium-containing antacids: a single dose of such antacids together with amlodipine does not have a significant effect on the pharmacokinetics of amlodipine.
mTOR inhibitors (eg, temsirolimus, sirolimus, everolimus) are substrates of CYP3A4. Because amlodipine is a weak CYP3A4 inhibitor, concomitant use may increase exposure to mTOR inhibitors.
Lisinopril
Contraindicated drug combinations
Aliskiren
Concomitant use of ACE inhibitors with aliskiren and aliskiren-containing drugs in patients with diabetes mellitus and/or moderate or severe renal impairment (GFR less than 60 ml/min/1.73 m 2 body surface area) is contraindicated.
The administration of ACE inhibitors with angiotensin II receptor antagonists is contraindicated in patients with diabetic nephropathy.
Angiotensin II receptor antagonists (ARA II)
The literature has reported that in patients with established atherosclerotic disease, chronic heart failure, or diabetes mellitus with end-organ damage, concomitant therapy with an ACE inhibitor and an ARB II is associated with a higher incidence of hypotension, syncope, hyperkalemia, and deterioration of renal function (including acute renal failure) compared with the use of only one drug that affects the RAAS. Dual blockade (for example, when combining an ACE inhibitor with an ARB II) should be limited to selected cases with careful monitoring of renal function, potassium levels and blood pressure.
Potassium supplements, potassium-sparing diuretics (spironolactone, triamterene, amiloride, eplerenone) or potassium-containing salt substitutes
Hyperkalemia may develop (with possible death), especially if renal function is impaired (additional effects associated with hyperkalemia). ACE inhibitors should not be used concomitantly with substances that increase plasma potassium levels, except in cases of hypokalemia. The combination of lisinopril and the above agents is not recommended. If, however, concomitant use is indicated, they should be used with caution and regular monitoring of serum potassium levels.
Lithium preparations
With the simultaneous use of lithium preparations and ACE inhibitors, a reversible increase in the concentration of lithium in the blood serum and associated toxic effects may be observed. The simultaneous use of lisinopril and lithium preparations is not recommended. If such therapy is necessary, the concentration of lithium in the blood serum should be regularly monitored.
Combinations of drugs that require special caution when used
Insulin and oral hypoglycemic agents
Epidemiological studies have shown that the combined use of ACE inhibitors and hypoglycemic agents (insulins, oral hypoglycemic agents) can enhance their hypoglycemic effect up to the development of hypoglycemia. This effect is most likely to be observed during the first weeks of concomitant therapy, as well as in patients with impaired renal function.
Baclofen
Enhances the antihypertensive effect of ACE inhibitors. Blood pressure levels should be carefully monitored and, if necessary, the dose of antihypertensive drugs should be adjusted.
Diuretics
In patients taking diuretics, especially those that remove fluid and/or salts, a significant decrease in blood pressure may be observed when initiating therapy with an ACE inhibitor. The risk of developing antihypertensive effects can be reduced by discontinuing the diuretic and replacing fluid or salt losses before starting ACE inhibitor therapy. For arterial hypertension in patients with previous diuretic therapy, which could lead to excessive excretion of fluid and/or salts, diuretics should be discontinued before starting use of the drug Equator.
Kidney function (creatinine concentration) should be monitored in the first weeks of using Equator.
NSAIDs, including at a dose of ≥3 g/day
The simultaneous use of ACE inhibitors with NSAIDs (acetylsalicylic acid in a dose that has an anti-inflammatory effect, COX-2 inhibitors and non-selective NSAIDs) may lead to a decrease in the antihypertensive effect of ACE inhibitors. The simultaneous use of ACE inhibitor drugs and NSAIDs may lead to deterioration of renal function, including the development of acute renal failure and an increase in serum potassium, especially in patients with reduced renal function. Caution should be exercised when prescribing this combination, especially in elderly patients. Patients need to compensate for fluid loss and carefully monitor renal function, both at the beginning of treatment and during treatment.
Estramustine, mTOR inhibitors (sirolimus, everolimus, temsirolimus), neutral endopeptidase inhibitors (omapatrilat, ilepatril, daglutril, sacubitril)
Concomitant use with ACE inhibitors is accompanied by an increased risk of developing angioedema.
DPP-4 inhibitors (gliptins)
Linagliptin, saxagliptin, sitagliptin, vildagliptin: when used together with ACE inhibitors, the risk of angioedema increases due to the inhibition of dipeptidyl peptidase-4 (DPP-IV) activity by gliptin.
Neutral endopeptidase inhibitors (NEP)
An increased risk of angioedema has been reported with concomitant use of ACE inhibitors and racecadotril (an enkephalipase inhibitor).
When ACE inhibitors are used simultaneously with drugs containing sacubitril (neprilysin inhibitor), the risk of developing angioedema increases, and therefore the simultaneous use of these drugs is contraindicated. ACE inhibitors should be prescribed no earlier than 36 hours after discontinuation of drugs containing sacubitril. Prescription of drugs containing sacubitril is contraindicated in patients receiving ACE inhibitors, as well as within 36 hours after discontinuation of ACE inhibitors.
Combinations of drugs that require caution when used
Other antihypertensive agents (eg, beta blockers, calcium channel blockers, diuretics) and vasodilators
The antihypertensive effect of the drug may be enhanced. Caution should be exercised when administered concomitantly with nitroglycerin, other nitrates or other vasodilators, as this may further reduce blood pressure.
Antacids and cholestyramine
Concomitant use with antacids and cholestyramine leads to suppression of gastrointestinal absorption.
Tricyclic antidepressants, neuroleptics, general anesthesia, barbiturates, phenothiazine, ethanol
When taken together, the effect of lisinopril may be enhanced.
Sympathomimetics
Sympathomimetics may reduce the antihypertensive effect of ACE inhibitors.
Muscle relaxants
The simultaneous use of muscle relaxants with ACE inhibitors can lead to a pronounced decrease in blood pressure.
Gold preparations
When using ACE inhibitors, incl. lisinopril, rare cases of nitritoid reactions (a symptom complex including facial flushing, nausea, dizziness and hypotension) have been described in patients receiving IV gold (sodium aurothiomalate), which can be very severe.
Co-trimoxazole (sulfomethoxazole and trimethoprim)
Increased risk of developing hyperkalemia.
Selective serotonin reuptake inhibitors (escitalopram, paroxetine, fluoxetine, sertraline)
When used simultaneously with SSRIs, severe hyponatremia may develop.
Allopurinol, procainamide, cytostatics (5-fluorouracil, vincristine, docetaxel)
Leukopenia may develop.
Tissue plasminogen activators (alteplase, reteplase, tenecteplase)
Increased risk of angioedema when used simultaneously with ACE inhibitors. Observational studies have shown an increased incidence of angioedema in patients taking ACE inhibitors following the use of alteplase for thrombolytic therapy of ischemic stroke.
special instructions
The equator should not be used to relieve a hypertensive crisis.
Upon admission to the hospital, the patient must inform the doctor about taking the drug Equator.
When using the drug Equator, you should take into account the warnings regarding its individual components, listed below.
Amlodipine related
It is necessary to maintain dental hygiene and follow-up with a dentist (to prevent pain, bleeding and gum hyperplasia.
In elderly patients, T1/2 may increase and drug clearance may decrease. No dose changes are required, but more careful monitoring of patients in this category is necessary.
The effectiveness and safety of amlodipine in hypertensive crisis have not been established.
Withdrawal syndrome
Despite the absence of withdrawal syndrome in BMCC, it is advisable to discontinue treatment with amlodipine by gradually reducing the dose of the drug. Amlodipine does not prevent the development of withdrawal syndrome upon abrupt cessation of beta-blockers.
Cardiovascular diseases
In rare cases, in patients with coronary artery disease (especially with severe obstructive lesions of the coronary arteries), an increase in the frequency, duration and/or severity of angina attacks was observed after starting the use of BMCC or after increasing their dose.
During the use of amlodipine in patients with NYHA class III and IV chronic heart failure of non-ischemic origin, an increase in the incidence of pulmonary edema was observed, despite the absence of signs of worsening heart failure.
Peripheral edema
Mild to moderate peripheral edema was the most common adverse event of amlodipine in clinical studies. The incidence of peripheral edema increases with increasing dose of amlodipine. Peripheral edema associated with the use of amlodipine should be carefully differentiated from symptoms of progression of left ventricular heart failure.
Effect on fertility
In some patients receiving slow calcium channel blockers, reversible biochemical changes in the sperm head were found, which may be clinically significant during IVF. However, there is currently insufficient clinical data regarding the potential effects of amlodipine on fertility. A preclinical study identified undesirable effects on fertility in males.
Related to lisinopril
Symptomatic hypotension
Most often, a significant decrease in blood pressure occurs with a decrease in blood volume caused by the use of diuretics, reducing the amount of salt in food, dialysis, diarrhea or vomiting. In patients with chronic heart failure, with or without renal failure, symptomatic arterial hypotension may develop. It develops more often in patients with severe heart failure, which is associated with the use of high doses of diuretics, hyponatremia or impaired renal function. Such patients require careful medical monitoring (with careful selection of doses of lisinopril and diuretics). The same recommendations apply to patients with coronary artery disease and cerebrovascular insufficiency, when a rapid decrease in blood pressure can lead to the development of myocardial infarction or stroke.
Patients with a pronounced decrease in blood pressure should be placed in a horizontal position; if necessary, an infusion of 0.9% sodium chloride solution is performed. Transient arterial hypotension is not a contraindication to taking the next dose of lisinopril.
In patients with chronic heart failure with normal or low blood pressure, the use of lisinopril may lead to a decrease in blood pressure; as a rule, this does not require discontinuation of treatment. If hypotension becomes symptomatic, indications for lisinopril dose reduction or discontinuation should be evaluated.
In patients at risk of developing symptomatic arterial hypotension (patients on a salt-free or low-salt diet) with or without hyponatremia, as well as in patients receiving high doses of diuretics, it is necessary to compensate for these deviations (loss of water and salts) before starting treatment.
It is necessary to monitor the effect of the starting dose of lisinopril on blood pressure.
Acute myocardial infarction
The use of the drug Equator in patients with acute myocardial infarction is not recommended due to insufficient experience in clinical use.
Kidney failure
In patients with chronic heart failure, a significant decrease in blood pressure that occurs after initiation of ACE inhibitor therapy may lead to worsening renal dysfunction. Cases of acute renal failure have been reported.
In patients with bilateral renal artery stenosis or renal artery stenosis of a solitary kidney, cases of increased serum urea and creatinine concentrations associated with the use of ACE inhibitors have been reported; As a rule, these disorders were transient and ceased after discontinuation of lisinopril. They occurred more often in patients with renal failure.
Kidney transplant
There is no experience with the use of lisinopril in patients who have recently undergone kidney transplantation.
Hypersensitivity, angioedema
In patients receiving ACE inhibitors, incl. lisinopril, rare cases of angioedema of the face, extremities, lips, tongue, epiglottis and/or larynx have been reported, which could occur during any period of treatment. In such cases, it is necessary to immediately discontinue lisinopril; Patients should be monitored until symptoms disappear completely. Typically, cases of angioedema of the face and lips are temporary and do not require any treatment; it is possible to prescribe antihistamines.
Angioedema of the larynx can lead to death. Angioedema of the tongue, epiglottis or larynx can lead to secondary airway obstruction, so it is necessary to immediately begin appropriate therapy (0.3-0.5 ml of epinephrine solution (adrenaline) at a concentration of 1:1000 subcutaneously) and/or take measures to ensure airway patency .
In rare cases, angioedema of the intestine has developed during therapy with ACE inhibitors. In this case, patients experienced abdominal pain as an isolated symptom or in combination with nausea or vomiting, in some cases, without previous angioedema of the face and with normal C1-esterase levels. Diagnosis was made using abdominal CT, ultrasound, or at the time of surgery. Symptoms disappeared after stopping the ACE inhibitors. Therefore, in patients with abdominal pain receiving ACE inhibitors, when carrying out differential diagnosis, it is necessary to take into account the possibility of developing angioedema of the intestine.
In patients with a history of angioedema not associated with ACE inhibitor use, use of ACE inhibitors may be associated with a higher risk of developing angioedema.
Anaphylactic reactions associated with desensitization by hymenoptera venom
There are reports of very rare cases of life-threatening anaphylactic reactions that developed in patients taking ACE inhibitors during desensitization with hymenoptera venom. To prevent such cases, ACE inhibitors should be temporarily discontinued before desensitization.
Hemodialysis
Anaphylactic reactions have also been reported in patients undergoing hemodialysis using high-permeability membranes (eg, AN69) who were concomitantly prescribed ACE inhibitors. In this group of patients, the use of other dialysis membranes or other antihypertensive drugs should be considered.
Cough
The use of ACE inhibitors may be associated with cough. A dry cough that continues for a long time usually disappears after discontinuation of the ACE inhibitor. When carrying out differential diagnosis, the possibility of cough associated with the use of ACE inhibitors should be taken into account.
Surgery/general anesthesia
The use of blood pressure-lowering drugs during major surgery or general anesthesia may suppress the formation of angiotensin II in response to compensatory renin secretion. A significant decrease in blood pressure, which is considered as a result of this effect, can be controlled by reducing the volume of blood volume.
Patients taking ACE inhibitors should inform their surgeon/anesthetist before undergoing surgery (including dental procedures).
Cases of hyperkalemia have been reported. Risk factors for the development of hyperkalemia include renal failure, diabetes mellitus and concomitant use of potassium-sparing diuretics (spironolactone, triamterene, and amiloride), as well as potassium supplements and potassium-based salt substitutes, especially in patients with impaired renal function. If simultaneous use of lisinopril and the above drugs is necessary, caution should be exercised and serum potassium levels should be regularly monitored.
Double blockade of the RAAS
It has been proven that the simultaneous administration of ACE inhibitors, angiotensin II receptor blockers or aliskiren increases the risk of arterial hypotension, hyperkalemia and renal dysfunction (including acute renal failure). Therefore, it is not recommended to prescribe ACE inhibitors, angiotensin II receptor blockers, or aliskiren for dual blockade of the RAAS.
If there are absolute indications for double blockade of the RAAS, then it should be carried out under the careful supervision of a specialist with frequent monitoring of blood pressure, renal function and electrolyte levels.
The simultaneous use of ACE inhibitors with drugs containing aliskiren is contraindicated in patients with diabetes mellitus and/or with moderate or severe renal failure (GFR less than 60 ml/min/1.73 m 2 body surface area) and is not recommended in other patients.
Concomitant use of ACE inhibitors with angiotensin II receptor antagonists is contraindicated in patients with diabetic nephropathy and is not recommended in other patients.
Neutropenia/agranulocytosis/thrombocytopenia/anemia
While taking ACE inhibitors, neutropenia/agranulocytosis, thrombocytopenia and anemia may occur. In patients with normal renal function and in the absence of other aggravating factors, neutropenia rarely develops. Neutropenia and agranulocytosis are reversible and disappear after discontinuation of the ACE inhibitor.
Equator should be prescribed with extreme caution to patients with systemic connective tissue diseases, while taking immunosuppressants, allopurinol or procainamide, or a combination of these risk factors, especially patients with impaired renal function. Some patients developed severe infections, in some cases resistant to intensive antibiotic therapy. When prescribing Equator to such patients, it is recommended to periodically monitor the number of leukocytes in the blood plasma. Patients should report any signs of infectious diseases (eg, sore throat, fever) to their doctor.
Mitral stenosis/aortic stenosis/hypertrophic cardiomyopathy
ACE inhibitors should be prescribed with caution to patients with mitral stenosis, as well as to patients with left ventricular outflow tract obstruction (aortic stenosis, hypertrophic cardiomyopathy).
Liver failure
Very rarely, cholestatic jaundice occurs while taking ACE inhibitors. As this syndrome progresses, fulminant liver necrosis develops, sometimes with death. The mechanism of development of this syndrome is unclear. If jaundice or a significant increase in the activity of liver enzymes occurs while taking ACE inhibitors, the drug Equator should be discontinued and the patient should be carefully monitored.
Diabetes
When using lisinopril in patients with diabetes mellitus receiving oral hypoglycemic agents or insulin, blood glucose concentrations should be regularly monitored during the first month of therapy.
Elderly age
In elderly patients, the use of standard doses leads to higher concentrations of lisinopril in the blood, so special care is required when determining the dose, despite the fact that differences in the antihypertensive effect of lisinopril in elderly and young patients were not identified.
Ethnic differences
In patients of the Negroid race, angioedema develops more often than in representatives of other races while taking ACE inhibitors. ACE inhibitors may have a less pronounced antihypertensive effect in patients of the Black race compared to representatives of other races. This difference may be due to the fact that black patients with arterial hypertension are more likely to have low renin activity.
Impact on the ability to drive vehicles and machinery
There are no data on the effect on the ability to drive vehicles and machinery. Due to the possibility of an excessive decrease in blood pressure, dizziness, drowsiness and other side effects at the beginning of treatment, patients should refrain from driving a car or other vehicles, operating machinery or performing other work that requires concentration.
Pregnancy and lactation
Pregnancy
The use of Equator is contraindicated during pregnancy.
There are no data on the use of Equator in pregnant women in adequately controlled clinical studies. If pregnancy is detected, treatment with Equator should be stopped immediately. Patients planning pregnancy should consult a doctor to prescribe antihypertensive therapy with an established safety profile during pregnancy.
Amlodipine
The safety of amlodipine during pregnancy has not been established. In preclinical studies, the fetotoxic and embryotoxic effects of amlodipine were not detected. In rats, amlodipine increased the duration of the gestational period and labor. Some other BMCCs are teratogenic.
Lisinopril
The use of ACE inhibitors in the II-III trimesters of pregnancy can lead to the death of the fetus and newborn. It is recommended to carefully monitor newborns and infants exposed in utero to ACE inhibitors in order to promptly detect a significant decrease in blood pressure, oliguria and hyperkalemia. Possible occurrence of oligohydramnios, hypoplasia of the facial bones, deformation of the bones of the face and skull, hypoplasia of the lungs and abnormal development of the kidneys in the child.
Women of childbearing age should use effective methods of contraception when treated with lisinopril.
Lisinopril can penetrate the blood-placental barrier. Treatment with lisinopril should not be started during pregnancy. Patients planning pregnancy should consult a doctor to prescribe antihypertensive therapy with an established safety profile during pregnancy.
Breastfeeding period
The use of Equator during breastfeeding is contraindicated.
Amlodipine
Experience with the drug shows that amlodipine is excreted in breast milk. The mean milk/plasma ratio for amlodipine concentration was 0.85 among 31 lactating women who had pregnancy-related hypertension and received amlodipine at an initial dosage of 5 mg/day. The dose of the drug was adjusted if necessary (depending on the average daily dose and weight: 6 mg and 98.7 mcg/kg, respectively). The estimated daily dose of amlodipine received by an infant through breast milk is 4.17 mcg/kg.
The use of amlodipine during breastfeeding is contraindicated. If it is necessary to use the drug during lactation, breastfeeding should be stopped.
The drug should be prescribed with caution in case of liver failure.
Equator, tablets, 5 mg + 20 mg: the shelf life of the drug is 3 years.
Equator, tablets, 10 mg + 20 mg: - 3 years.
Do not use after the expiration date stated on the package.
High blood pressure is one of the main problems of the civilized world.
Doctors never tire of warning about the risk factors for the development of this disease and its consequences, which are fraught with life-threatening conditions, in particular, myocardial infarction, stroke, and aneurysm rupture.
Currently, the development and production of effective medications that eliminate the symptoms of hypertension is a priority in the activities of many pharmaceutical companies.
Thanks to modern technologies and innovative developments, scientists have managed to create a line of combined drugs with a unidirectional effect that quickly eliminate the main manifestations of the disease and prevent the occurrence of its complications.
Among such medicines, Equator blood pressure tablets deserve special attention. Instructions for use, at what pressure it is recommended to take the medicine, contraindications and side effects - points that we will discuss in detail in this article.
Equator is a combination drug with an antihypertensive effect, which has a pronounced effect aimed at persistently lowering blood pressure.
The composition of the drug includes the following components:
- lisinopril;
- amlodipine;
- magnesium stearate;
- microcrystalline cellulose;
- carboxymethyl starch.
The active substance lisinopril is a modern inhibitor of angiotensin converting factor. This component blocks the process of conversion of angiotensin I to angiotensin II in the kidney parenchyma, which increases the synthesis of prostaglandins and reduces the negative effect of aldosterone on water-salt balance.
Lisinopril has several important effects that ensure the normal functioning of the cardiovascular system:
- reduces blood pressure by dilating blood vessels and reducing their peripheral resistance;
- reduces pressure in the pulmonary capillaries;
- promotes a minute increase in blood flow;
- increases myocardial resistance to stress;
- prevents the development of swelling;
- reduces the amount of albumin in the blood;
- does not affect the concentration of glucose in the body;
- normalizes water-salt balance.
Amlodipine - which inhibits the process of transition of Ca ions into the structures of the smooth muscles of the heart. This substance is similar in action to lisinopril, and therefore enhances its effects. In addition, amlodipine has pronounced antianginal properties, which allows it to be used in patients suffering from arterial hypertension in combination with coronary heart disease.
Among the main effects of amlodipine are:
- antihypertensive effect;
- analgesic effect;
- expansion of coronary vessels and normalization of coronary blood flow;
- prevention of myocardial ischemia;
- increased oxygen supply to the heart muscle;
- reducing blood viscosity by reducing platelet aggregation;
- decrease in general vascular resistance;
- prevention of heart failure.
Indications and contraindications
Equator is prescribed to patients with hypertension and symptomatic high blood pressure, especially if these conditions are combined with chronic heart failure. The accompanying Equator tablets for normalizing blood pressure, reviews emphasize its mild effect and the rare development of side effects. It perfectly reduces blood pressure in case of no effect from monocomponent drugs.
The combined drug Equator should not be taken by patients who have:
- significant narrowing of the lumen (stenosis) of the mitral and aortic valves;
- angioedema of idiopathic origin, Quincke's edema;
- arterial hypotension;
- severe cardiomyopathy;
- post-infarction heart failure;
- cardiogenic shock;
- unstable angina;
- age under 18 years;
- pregnancy and breastfeeding;
- intolerance to the main components of the drug or other drugs from the group of calcium channel blockers.
The product should be used only after a doctor's prescription. It should be used with extreme caution in patients diagnosed with renal artery stenosis, insufficiency of renal and liver function, hyperaldosteronism, and hyperkalemia. It is not recommended to take Equator after a kidney transplant.
Side effects
Undesirable effects from the use of Equator occur, according to statistical studies, extremely rarely.
In some cases, patients note the occurrence of such adverse reactions as:
- headache;
- episodic dizziness and weakness in the body;
- disruption of hematopoietic processes (anemia, leukopenia);
- not severe nausea;
- disorders of the gastrointestinal tract;
- rare dry cough;
- changes in urine analysis, where proteinuria and decreased density are determined, and oligo- and even anuria may be observed.
An overdose of the drug is also possible when the patient experiences a rapid heartbeat and a sharp decrease in blood pressure. If such a condition develops, it is necessary to lay the person in a horizontal position and raise his lower limbs. Correction of normal activity of the cardiovascular system is carried out through medication.
Such side effects go away on their own after some time and do not cause much suffering to the sick person, so they do not require discontinuation of the drug.
Features of application
Equator is an original Hungarian-made combination drug, the rights to which are owned by the world-famous pharmaceutical brand Gedeon Richter. The medicine is available in the form of tablets of 5 and 10 mg.
Equator tablets for blood pressure
The drug is prescribed 1 tablet (5 mg) 1 time per day. It is better to take the medication in the morning and drink it with enough water. Taking Equator is not tied to food consumption.
If the initial regimen is ineffective, the dosage of the drug must be increased, but only after the doctor’s permission. The maximum daily dose of the drug is 20 mg. While using Equator, experts recommend that patients monitor the state of their kidney function, as well as the levels of potassium and sodium in the blood.
Compatibility with other drugs
The medicine for hypertension Equator should be taken with caution by patients who use diuretics, as they can provoke a significant decrease in blood pressure.
It is better to stop diuretics 3-4 days before starting treatment with a combination medication.
You cannot combine the antihypertensive combination drug Equator with non-steroidal anti-inflammatory drugs. Hormonal medications, and especially estrogens, can reduce the hypotensive effect of Equator, so it should not be taken by menopausal women who are on replacement therapy.
It has been proven that the simultaneous use of the combined drug Equator and narcotic analgesics increases the hypotensive effect and can provoke a sharp decrease in blood pressure to critical levels.
Price and analogues
The price in Russia for Hungarian tablets Equator for normalizing blood pressure is as follows:- 5+10 mg, 10 pcs. – from 225 rubles;
- 5+10 mg, 30 pcs. – from 550 rubles;
- 10+20 mg, 30 pcs. – from 770 rubles.
Equacard is the only structural analogue of Equator blood pressure tablets. Such drugs as Amlipin, Gipril-A, Combipril-Q, Neocard have similar effects.
– a medicine that helps reduce blood pressure and relieve pain due to angina pectoris. The effect occurs 20 minutes after taking the tablets and lasts from 4 to 7 hours.
In what cases do doctors prescribe the drug Panangin and how to take it correctly, read the material.
For high blood pressure, as well as for heart rhythm disturbances and panic attacks, it is often prescribed. Patients note the quick and effective results of this remedy.
Video on the topic
Visual instructions for use with Equator blood pressure tablets:
Equator is an effective means of correcting blood pressure, which works in cases where taking single medications has not had a positive therapeutic effect. The reviews from both doctors and patients about Equator high blood pressure tablets are quite high. This modern medicine is widely used in medical practice and can quickly normalize the condition of patients suffering from various types of arterial hypertension. Despite the effectiveness of the medicine and the relative absence of side effects from its use, Equator has a number of contraindications for use, and that is why its use should be agreed with the attending physician.