Equacard, tablets 5 mg+10 mg 30 pcs

Equacard is a combination drug containing the active ingredients: lisinopril and amlodipine.

Lisinopril

An angiotensin-converting enzyme (ACE) inhibitor, reduces angiotensin II formation from angiotensin I. Decreased angiotensin II leads to a direct decrease in aldosterone release. Reduces bradykinin degradation and increases prostaglandin synthesis. Reduces total peripheral vascular resistance (TPR), BP, preload, pulmonary capillary pressure, causes an increase in the minute blood volume and increases myocardial tolerance to load in patients with chronic heart failure. Dilates arteries more than veins. Some effects are attributed to effects on the renin-angiotensin-aldosterone system (RALS). Long-term use reduces myocardial hypertrophy and resistive arterial wall hypertrophy. It improves blood supply of ischemic myocardium.
ACE inhibitors prolong life expectancy in patients with chronic heart failure, delay progression of left ventricular dysfunction in patients who have had acute myocardial infarction without clinical manifestations of heart failure.

The onset of action of the drug in 1 hour, the maximum antihypertensive effect is achieved in 6-7 hours and lasts for 24 hours. The duration of the effect also depends on the amount of dose taken. In arterial hypertension, the effect is noted in the first days after treatment start, a stable effect develops after 1-2 months of therapy. When lisinopril is abruptly withdrawn, no marked increase in BP has been observed. Lisinopril reduces albuminuria. It does not affect blood glucose concentration in diabetic patients and does not lead to increased incidence of hypoglycemia.

Amlodipine

. Slow calcium channel blocker, a dihydropyridine derivative slow calcium channel blocker (BMCC), has antianginal and antihypertensive effects, blocks calcium channels, reduces the granemembrane transition of calcium ions into the cell (more in vascular smooth muscle cells than in cardiomyocytes).

The antianginal action is caused by the dilation of coronary and peripheral arteries and arterioles: in angina pectoris it reduces myocardial ischemia; by dilation of peripheral arterioles it reduces myocardial hypertension, decreases postload on heart, reduces myocardial oxygen demand. By dilating coronary arteries and arterioles in unchanged and in ischemic areas of the myocardium, increases the flow of oxygen to the myocardium (especially in vasospastic angina); prevents coronary artery spasm (including that caused by smoking). In patients with stable angina a single daily dose increases exercise tolerance, increases time to angina attack and “coronary” ST-segment depression, reduces the frequency of angina attacks and consumption of nitroglycerin and other nitrates.

It has a long-term dose-dependent antihypertensive effect. The antihypertensive effect is due to a direct vasodilatory effect on vascular smooth muscle. In arterial hypertension a single dose provides clinically significant BP reduction for 24 hours (in patient “lying” and “standing”). Orthostatic hypotension when prescribing amlodipine is rare. It does not cause reduction of left ventricular ejection fraction. It reduces the degree of left ventricular myocardial hypertrophy. It does not affect myocardial contractility and conduction, does not cause reflex increase in HR, inhibits platelet aggregation, increases glomerular filtration rate, 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 concentration of plasma lipids and can be used for therapy of patients with bronchial asthma, diabetes mellitus and gout. Significant decrease in BP is observed after 6-10 hours, the duration of effect is 24 hours.

Indications

Essential hypertension (patients for whom combination therapy is indicated).

Pharmacological effect

Equacard is a combination drug containing the active ingredients: lisinopril and amlodipine.

Lisinopril

An angiotensin-converting enzyme (ACE) inhibitor, reduces the formation of angiotensin II from angiotensin I. A decrease in the content of angiotensin II leads to a direct decrease in the release of aldosterone. Reduces the degradation of bradykinin and increases the synthesis of prostaglandins. Reduces total peripheral vascular resistance (TPVR), blood pressure, preload, pressure in the pulmonary capillaries, causes an increase in minute blood volume and an increase in myocardial tolerance to stress in patients with chronic heart failure. Dilates arteries more than veins. Some effects have been attributed to effects on the renin-angiotensin-aldosterone system (RALS). With long-term use, hypertrophy of the myocardium and the walls of resistive arteries decreases. Improves blood supply to ischemic myocardium.
ACE inhibitors extend life expectancy in patients with chronic heart failure and slow the progression of left ventricular dysfunction in patients who have suffered acute myocardial infarction without clinical manifestations of heart failure.

The onset of action of the drug is after 1 hour, the maximum antihypertensive effect is achieved after 6-7 hours and lasts for 24 hours. The duration of the effect also depends on the size of the dose taken. In arterial hypertension, the effect is observed in the first days after the start of treatment, a stable effect develops after 1-2 months of therapy. When lisinopril was abruptly discontinued, no significant increase in blood pressure was observed. Lisinopril reduces albuminuria. Does not affect the concentration of glucose in the blood in patients with diabetes and does not lead to an increase in cases of hypoglycemia.

Amlodipine

A blocker of “slow” calcium channels, a dihydropyridine derivative, a blocker of “slow” calcium channels (BMCC), has an antianginal and antihypertensive effect, blocks calcium channels, reduces the granomembrane transition of calcium ions into the cell (more into vascular smooth muscle cells than into cardiomyocytes).

The antianginal effect is due to the expansion of the coronary and peripheral arteries and arterioles: in case of angina pectoris, it reduces the severity of myocardial ischemia; by expanding peripheral arterioles, it reduces peripheral vascular resistance, reduces afterload on the heart, and reduces myocardial oxygen demand. By expanding the coronary arteries and arterioles in unchanged and ischemic areas of the myocardium, it increases the supply of oxygen to the myocardium (especially with vasospastic angina); prevents spasm of the coronary arteries (including those caused by smoking). In patients with stable angina, a single daily dose increases exercise tolerance, increases the time before the onset of an angina attack and “ischemic” depression of the ST segment, reduces the frequency of angina attacks and the consumption of nitroglycerin and other nitrates.

It has a long-term dose-dependent antihypertensive 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 when prescribing amlodipine is quite rare. Does not cause a decrease in the left ventricular ejection fraction. Reduces the degree of left ventricular myocardial hypertrophy. Does not affect myocardial contractility and conductivity, does not cause a reflex increase in heart rate, inhibits platelet aggregation, increases glomerular filtration rate, and has a weak natriuretic effect.

In diabetic nephropathy, it does not increase the severity of microalbumiuria. It does not have any adverse effect on metabolism and plasma 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.

Special instructions

Treatment with Equacard can be started only after correction of hyponatremia and restoration of circulating blood volume.

After taking the first dose of the drug, careful monitoring of blood pressure is recommended; a significant decrease in blood pressure is possible with the development of symptomatic arterial hypotension. Most often, a pronounced decrease in blood pressure occurs when there is a decrease in blood volume caused by diuretic therapy, a decrease in the content of sodium chloride in food, dialysis, diarrhea or vomiting.
In case of arterial hypotension, the patient is placed in a horizontal position and, if necessary, a solution is administered intravenously to replenish the volume of circulating fluid (infusion of 0.9% sodium chloride solution).

Similar rules should be followed when using the drug Equacard in patients with coronary artery disease, cerebrovascular insufficiency, in whom a sharp decrease in blood pressure can lead to myocardial infarction or stroke.

In case of aortic stenosis and hypertrophic obstructive cardiomyopathy, the prescription of a vasodilator requires caution.
During therapy with Equacard®, it is necessary to monitor body weight and salt intake, and prescribing an appropriate diet is indicated.

It is necessary to maintain oral hygiene and follow-up with a dentist (to prevent pain, bleeding and gum hyperplasia).

During the period of therapy, periodic monitoring of peripheral blood is necessary, because The potential risk of agranulocytosis cannot be excluded; periodic monitoring of peripheral blood is required.

In case of impaired renal function, for example, with renal artery stenosis (especially bilateral or with stenosis of the arteries of a single kidney), hyponatremia, dehydration, circulatory failure, taking the drug can provoke a deterioration in renal function and acute renal failure, reversible after cessation of treatment. Monitoring of patients with impaired renal function is necessary.

In elderly patients, T1/2 of amlodipine may increase and drug clearance may decrease. More careful monitoring of patients in this category is necessary.

If liver function is impaired, the half-life of amlodipine increases; in such patients the drug is prescribed with caution, after assessing the benefits and risks. When using ACE inhibitors, angioedema of the face, extremities, lips, tongue, epiglottis or larynx may develop, requiring immediate cessation of drug treatment and medical supervision until complete regression of symptoms. Angioedema with laryngeal edema can be fatal. Swelling of the tongue, epiglottis or larynx can cause airway obstruction, so it is necessary to immediately carry out appropriate therapy (0.3-0.5 ml of 1:1000 solution of epinephrine (adrenaline) subcutaneously) and/or measures to ensure airway patency. In cases where the swelling is localized only on the face and lips, the condition most often goes away without treatment, but the use of antihistamines is possible.

The risk of developing angioedema is increased in patients who have a history of angioedema from the use of ACE inhibitors.

In extremely rare cases, patients taking ACE inhibitors during desensitization to hymenoptera venom may develop life-threatening anaphylactoid reactions. This can be avoided by temporarily stopping ACE inhibitor treatment before each hymenoptera desensitization procedure.

Surgery/general anesthesia: When using general anesthesia agents with antihypertensive effects and during major surgical procedures, lisinopril inhibits the formation of angiotensin-II in response to compensatory release of renin. With such arterial hypotension, blood pressure is normalized by increasing the volume of circulating blood.

Before surgery (including dental surgery), the surgeon/anesthetist should be informed about the use of an ACE inhibitor.

Anaphylactoid reactions have also been observed in patients on hemodialysis using high-flow dialysis membranes (AN69) who are also taking ACE inhibitors. In such cases, the use of a different type of dialysis membrane or another antihypertensive agent should be considered. When selecting a dose, it should be taken into account that in elderly patients both active substances are determined in the blood in higher concentrations, but the effectiveness does not change.

Cough has been reported when using ACE inhibitors. The cough is dry and prolonged, which disappears after stopping treatment with an ACE inhibitor. In the differential diagnosis of cough, cough caused by the use of an ACE inhibitor must also be taken into account.

Active ingredient

Amlodipine, Lisinopril

Composition

1 tablet contains amlodipine 5 mg,

lisinopril 10 mg.

Pregnancy

The use of Equacard is not recommended during pregnancy.

If pregnancy is diagnosed, taking Equacard should be stopped as soon as possible.

Taking ACE inhibitors in the second and third trimester of pregnancy has an adverse effect on the fetus (a marked decrease in blood pressure, renal failure, hyperkalemia, hypoplasia of the skull bones, and intrauterine death are possible). There is no data on the negative effects of the drug on the fetus when used during the first trimester. For newborns and infants who have been exposed in utero to ACE inhibitors, it is recommended to conduct careful monitoring for timely detection of a pronounced decrease in blood pressure, oliguria, and hyperkalemia.

The safety of amlodipine during pregnancy has not been established; therefore, use during pregnancy is possible only when the benefit to the mother outweighs the potential risk to the fetus.

Lisinopril crosses the placenta. There is no data on the penetration of lisinopril into breast milk.

There is no data indicating the excretion of amlodipine into breast milk.

However, it is known that other BMCCs, dihydropyridine derivatives, are excreted in breast milk.

The use of Equacard® during breastfeeding is not recommended.

If the use of the drug is necessary during lactation, then breastfeeding must be stopped.

Contraindications

hypersensitivity to any of the components of the drug or to other dihydropyridine derivatives, other ACE inhibitors;
history of angioedema, including those caused by the use of other ACE inhibitors;
hereditary and/or idiopathic angioedema;
hemodynamically significant aortic or mitral valve stenosis or hypertrophic obstructive cardiomyopathy;
severe arterial hypotension (systolic blood pressure less than 90 mm Hg);
cardiogenic shock;
pregnancy, lactation period;
age under 18 years;
acute myocardial infarction (within the first 28 days), unstable angina (with the exception of Prinzmetal’s angina);
lactose intolerance, lactose deficiency and glucose-galactose malabsorption.

Side Effects

The frequency of adverse reactions listed below was determined according to the following (World Health Organization classification): very often – at least 10%; often – at least 1%, but less than 10%; infrequently – not less than 0.1%, but less than 1%; rarely – not less than 0.01%, but less than 0.1%; very rarely – less than 0.01%, including individual messages.

Lisinopril

From the cardiovascular system: often – marked decrease in blood pressure, orthostatic hypotension; uncommon – acute myocardial infarction, tachycardia, palpitations; Raynaud’s syndrome; rarely – bradycardia, tachycardia, worsening symptoms of chronic heart failure, atrioventricular conduction disturbance, chest pain.

From the side of the central nervous system: often – dizziness, headache; uncommon – mood lability, paresthesia, sleep disturbances, stroke; rarely – confusion, asthenic syndrome, convulsive twitching of the muscles of the limbs and lips, drowsiness.

From the hematopoietic and lymphatic systems: rarely – decrease in hemoglobin, hematocrit; very rarely – leukopenia, neutropenia, agranulocytosis, thrombocytopenia, eosinophilia, erythropenia, hemolytic anemia, lymphadenopathy, autoimmune diseases.

From the respiratory system: often – cough; infrequently – rhinitis; very rarely – sinusitis, bronchospasm, allergic alveolitis/eosinophilic pneumonia, shortness of breath.

From the digestive system: often – diarrhea, vomiting; uncommon – dyspepsia, taste changes, abdominal pain; rarely – dryness of the oral mucosa; very rarely – pancreatitis, jaundice (hepatocellular or cholestatic), hepatitis, liver failure, interstitial edema, anorexia.

From the skin: infrequently – itching, rash; rarely – angioedema of the face, limbs, lips, tongue, larynx, urticaria, alopecia, psoriasis; very rarely – increased sweating, vasculitis, pemphigus, photosensitivity, toxic epidermal necrolysis (Lyell’s syndrome), erythema multiforme, Stevens-Johnson syndrome.

From the urinary system: often – impaired renal function; uncommon – uremia, acute renal failure; very rarely – anuria, oliguria, proteinuria.

From the reproductive system: infrequently – impotence, rarely – gynecomastia.

Metabolism: very rarely – hypoglycemia.

From laboratory parameters: infrequently – increased concentration of urea in the blood, hypercreatininemia, hyperkalemia, increased activity of “liver” transaminases, rarely – hyperbilirubinemia, hyponatremia, increased erythrocyte sedimentation rate, false positive test results for antinuclear antibodies.

From the musculoskeletal system: rarely – arthralgia/arthritis, myalgia.

Amlodipine

From the side of the central nervous system: often – headache (especially at the beginning of treatment), dizziness, increased fatigue, drowsiness; uncommon – general malaise, hypoesthesia, asthenia, paresthesia, peripheral neuropathy, tremor, insomnia, emotional lability, unusual dreams, nervousness, increased excitability, depression, anxiety, increased sweating; rarely – convulsions, apathy, agitation; very rarely – ataxia, amnesia.

From the digestive system: often – nausea, abdominal pain; uncommon – vomiting, change in bowel habits (including constipation, flatulence), dyspepsia, diarrhea, anorexia, dry oral mucosa, thirst; rarely – gum hyperplasia, increased appetite; very rarely – pancreatitis, gastritis, jaundice (usually cholestatic), hyperbilirubinemia, increased activity of liver transaminases, hepatitis.

From the cardiovascular system: often – peripheral edema (ankles and feet), palpitations, “flushes” of blood to the skin of the face; uncommon – excessive decrease in blood pressure, orthostatic hypotension, vasculitis; rarely – development or worsening of chronic heart failure; very rarely – fainting, shortness of breath, cardiac arrhythmias (including bradycardia, ventricular tachycardia and atrial fibrillation), myocardial infarction, chest pain, pulmonary edema, migraine.

From the hematopoietic and lymphatic systems: very rarely – thrombocytopenic purpura, leukopenia, thrombocytopenia.

From the urinary system: infrequently – pollakiuria, painful urge to urinate, nocturia; very rarely – dysuria, polyuria.

From the reproductive system and mammary glands: infrequently – gynecomastia, impotence.

From the respiratory system: infrequently – shortness of breath, rhinitis; very rarely – cough.

From the musculoskeletal system: infrequently – muscle cramps, myalgia. arthralgia, back pain, arthrosis; rarely – myasthenia.

From the skin: infrequently – alopecia; rarely – dermatitis; very rarely – alopecia, xeroderma, cold sticky sweat, skin pigmentation disorder.

Allergic reactions: rarely – skin itching, rash (including erythematous, maculopapular rash); very rarely – urticaria, angioedema, erythema multiforme.

From the senses: infrequently – ringing in the ears, blurred vision, diplopia, impaired accommodation, xerophthalmia, conjunctivitis, pain in the eyes; very rarely – parosmia.

From the side of metabolism: very rarely – hyperglycemia.

Other: uncommon – weight loss, weight gain, taste disturbance, nosebleeds, chills.

Interaction

Lisinopril
Lisinopril should be used with caution simultaneously with potassium-sparing diuretics (spironolactone, triamterene, amiloride, eplerenone), potassium supplements, salt substitutes containing potassium, cyclosporine – the risk of hyperkalemia increases, especially with impaired renal function. Therefore, these combinations should be used only on the basis of an individual physician’s decision with regular monitoring of serum potassium levels and renal function.
When used simultaneously with diuretics and other antihypertensive drugs, the antihypertensive effect of lisinopril is enhanced.

When used simultaneously with nonsteroidal anti-inflammatory drugs (NSAIDs) (including selective cyclooxygenase-2 (COX-2) inhibitors), estrogens, and sympathomimetics, the antihypertensive effect of lisinopril is reduced. NSAIDs, including COX-2, and ACE inhibitors increase serum potassium and may impair renal function. This effect is usually reversible.

Lisinopril slows down the elimination of lithium preparations, therefore, with simultaneous use, there is a reversible increase in its concentration in the blood plasma, which may increase the likelihood of adverse events, so the concentration of lithium in the blood serum should be regularly monitored.

When used simultaneously with antacids and tyrants, the absorption of lisinopril from the gastrointestinal tract is reduced.
Ethanol enhances the effect of lisinopril.

When used simultaneously with insulin and oral hypoglycemic agents, the risk of developing hypoglycemia increases.

With simultaneous use of lisinopril with vasodilators, barbiturates, antipsychotics (neuroleptics), tricyclic antidepressants.

BMCC, beta-blockers may enhance the antihypertensive effect. With the simultaneous use of ACE inhibitors and intravenous gold preparations (sodium aurothiamalate), a symptom complex has been described, including facial flushing, nausea, vomiting and decreased blood pressure.

Combined use with allopurinol, procainamide, and cytostatics can lead to leukopenia.

Amlodipine
Amlodipine can be safely used for the treatment of arterial hypertension together with thiazide diuretics, alpha-blockers or ACE inhibitors.

Unlike other BMCCs, no clinically significant interaction of amlodipine was found when used together with NSAIDs, including indomethacin.

It is possible to enhance the antianginal and hypotensive effect of BMCC when used together with thiazide and loop diuretics, ACE inhibitors and nitrates, as well as enhance their antihypertensive effect when used simultaneously with alpha1-blockers.

Erythromycin, when used together, increases the Cmax of amlodipine in young patients by 22%, and in elderly patients by 50%.

Beta-blockers, when used simultaneously with amlodipine, can cause an exacerbation of chronic heart failure.

Although negative inotropic effects have not generally been observed in amlodipine studies, some CBMCs may enhance the negative inotropic effects of antiarrhythmic drugs that cause QT prolongation (eg, amiodarone and quinidine).

A single dose of 100 mg of sildenafil in patients with arterial hypertension does not affect the pharmacokinetic parameters of amlodipine.
Repeated use of amlodipine at a dose of 10 mg and atorvastatin at a dose of 80 mg is not accompanied by significant changes in the pharmacokinetics of atorvastatin.

Ethanol (drinks containing alcohol): amlodipine with single and repeated use in a dose of 10 mg does not affect the pharmacokinetics of ethanol.

Antiretroviral drugs (ritonavir) increase plasma concentrations of BMCC, including amlodipine.
Neuroleptics and isoflurane enhance the hypotensive effect of dihydropyridine derivatives.
Calcium supplements can reduce the effect of BMCC.

When amlodipine is used together with lithium preparations, it is possible to increase the manifestation of neurotoxicity (nausea, vomiting, diarrhea, ataxia, tremor, noise and tinnitus).

Amlodipine does not change the pharmacokinetics of cyclosporine.

Does not affect the serum concentration of digoxin and its renal clearance.

Does not significantly affect the effect of warfarin (prothrombin time).

Cimetidine does not affect the pharmacokinetics of amlodipine.

In in vitro studies, amlodipine does not affect the plasma protein binding of digoxin, phenytoin, warfarin and indomethacin.

Grapefruit juice: simultaneous single administration of 240 mg of grapefruit juice and 10 mg of amlodipine orally is not accompanied by a significant change in the pharmacokinetics of amlodipine.

Aluminum- or magnesium-containing antacids: their single dose does not have a significant effect on the pharmacokinetics of amlodipine.

Overdose

Lisinopril

Symptoms: marked decrease in blood pressure, dryness of the oral mucosa, water-electrolyte imbalance, renal failure, increased breathing, tachycardia, palpitations, bradycardia, dizziness, anxiety, increased irritability, cough, drowsiness, urinary retention, constipation.

Treatment: there is no specific antidote. Gastric lavage, use of enterosorbents and laxatives. Intravenous administration of 0.9% sodium chloride solution is indicated. In case of treatment-resistant bradycardia, the use of an artificial pacemaker is necessary. Monitoring of blood pressure and water and electrolyte balance is necessary. Hemodialysis is effective.

Amlodipine
Symptoms: marked decrease in blood pressure with the possible development of reflex tachycardia and excessive peripheral vasodilation (risk of severe and persistent arterial hypotension, including the development of shock and death).

Treatment: gastric lavage, use 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 circulating blood volume (CBV) and diuresis.

To restore vascular tone, use vasoconstrictors (in the absence of contraindications to their use); to eliminate the effects of calcium channel blockade, intravenous administration of calcium gluconate. Hemodialysis is not effective.

Storage conditions

In a place protected from light, at a temperature not exceeding 30 °C

Shelf life

3 years

Manufacturer

Micro Labs Ltd, India