Ekvapress (Equapress) caps 10mg + 1.5mg + 20mg #28

User manual for Ekvapress

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Ekvapress is a combined antihypertensive drug.

Release form and composition

Ekvapress dosage form - capsules with modified release: hard gelatinous. Dosage 5 + 1.5 + 10 mg - size No. 1, yellow, contains 1 round, biconvex tablet of white color with the engraving "CF4" (amlodipine + lisinopril) and 1 film-coated oval, biconvex tablet of white color, on one side engraving "CP3", on the other - risk (indapamide). Dosage 10 + 1.5 + 20 mg - size No. 1, light orange, contains 2 round tablets (amlodipine + lisinopril) and 1 oval tablet (indapamide). Dosage 5 + 1.5 + 20 mg - size No. 0, dark orange, contain 2 round tablets (amlodipine + lisinopril) and 1 oval tablet (indapamide) (14 capsules in blisters, in a cardboard box 1, 2, 4 or 8 blisters and instructions for the use of Ekvapress).
Composition for 1 capsule of Ekvapress (5 + 1.5 + 10 mg / 10 + 1.5 + 20 mg / 5 + 1.5 + 20 mg):
    active ingredients: amlodipine besylate - 6.934 / 13.868 / 6.934 mg (amlodipine - 5/10/5 mg); indapamide - 1.5 mg; lisinopril dihydrate - 10.888 / 21.776 / 21.776 mg (lisinopril - 10/20/20 mg);
    excipients: hypromellose, lactose monohydrate, calcium hydrogen phosphate dihydrate, corn starch, mannitol, croscarmellose sodium, microcrystalline cellulose, magnesium stearate, talc, colloidal silicon dioxide;
    tablet shell: Opadry II white (polyvinyl alcohol, titanium dioxide, macrogol-3350, talc);
    capsule shell: gelatin, water, dye iron oxide yellow; additionally for dosages 5 + 1.5 + 10 mg and 10 + 1.5 + 20 mg - titanium dioxide; additionally for dosages of 10 + 1.5 + 20 mg and 5 + 1.5 + 20 mg - dye iron oxide red.

Pharmacodynamics

Ekvapress is an established combination of antihypertensive drugs (amlodipine + indapamide + lisinopril) with complementary mechanisms of action that allow you to control blood pressure (BP) and have a synergistic cardioprotective effect.
The main pharmacological properties of the active components of Ekvapress:
    amlodipine: a dihydropyridine derivative, a slow calcium channel blocker (BMCC), which reduces the transmembrane transport of Ca2 + ions into cells (to a greater extent in vascular smooth muscle cells than in cardiomyocytes); exhibits antihypertensive and antianginal activity;
    indapamide: a sulfonamide derivative containing an indole ring; in pharmacological action it is close to thiazide diuretics, which inhibit the absorption of Na + ions in the cortical segment of the nephron loop. While increasing the renal elimination of Na +, Cl− and, to a lesser extent, K + and Mg2 + ions, it provides increased diuresis and antihypertensive effect;
    lisinopril: an angiotensin-converting enzyme (ACE) inhibitor; inhibits the conversion of angiotensin I into angiotensin II (a drop in the level of the latter leads to a direct decrease in the secretion of aldosterone); inhibits the degradation of bradykinin, potentiates the synthesis of prostaglandins; reduces blood pressure, OPSS (total peripheral vascular resistance), preload and pulmonary capillary pressure.
This combination helps to prevent adverse reactions, the development of which is possible with the use of individual components of Ekvapress. For example, by expanding arterioles, BMCC are able to retain Na + and fluids in the body, thereby activating the RAAS (renin-angiotensin-aldosterone system). At the same time, an ACE inhibitor blocks activation, normalizing the body's response to salt load. ACE inhibitors clinically relieve diuretic-induced hypokalemia.

Pharmacokinetics

Amlodipine

    absorption: after oral administration, amlodipine is well absorbed from the gastrointestinal tract (gastrointestinal tract). The average F (absolute bioavailability) is 64–80%. TCmax (time to reach Cmax - maximum concentration in blood serum) varies from 6 to 12 hours; Css (steady-state concentration) is reached on the 7-8th day of therapy. Food intake does not affect absorption;
    distribution: average Vd (volume of distribution) - 21 l / kg, which indicates the intake of most of the substance in the tissues. Amlodipine penetrates into the blood to a lesser extent, where it binds to plasma proteins by 97.5%. Overcomes the BBB (blood-brain barrier);
    metabolism: amlodipine is slowly but actively metabolized in the liver in the absence of significant first-pass hepatic metabolism. The resulting metabolites have no significant pharmacological activity;
    excretion: T1 / 2 (half-life) from blood plasma - 35-50 hours, which allows you to take the drug 1 time / day. T1 / 2 with repeated use is ~ 45 hours. Up to 60% of the ingested substance is eliminated by the kidneys, mainly in the form of metabolites; through the intestines with bile, 20 to 25% of amlodipine is excreted; 10% is displayed unchanged. The total clearance is 0.116 ml / s / kg (7 ml / min / kg or 0.42 l / h / kg). During hemodialysis, the substance is not excreted from the blood plasma.

Indapamide

    absorption: indapamide in a film-coated tablet is enclosed in a special matrix carrier, which ensures its slow controlled release in the gastrointestinal tract; after release, it is rapidly and completely absorbed from the digestive tract. Food intake increases the period of absorption of the substance slightly, but does not affect its completeness. TCmax is 12 hours after a single oral dose. During repeated use, fluctuations in the level of indapamide in the blood plasma are leveled. There is individual variability in the degree of absorption;
    distribution: about 79% of indapamide binds to blood plasma proteins. Css is reached after 7 days from the start of therapy. With repeated administration, the substance does not cumulate;
    excretion: T1 / 2 - 14-24 hours (on average - 18 hours); excreted mainly in the form of inactive metabolites; from the dose received by the kidneys - 70%, through the intestines - 22%.

Lisinopril

    absorption: after oral administration, about 25% of lisinopril is absorbed from the gastrointestinal tract. Food does not affect absorption. F - 29%, TCmax - 6–8 h;
    distribution: lisinopril weakly binds to blood plasma proteins, poorly penetrates through the BBB;
    metabolism: lisinopril is not metabolized in the human body;
    excretion: T1 / 2 - 12 hours

Indications for use

Ekvapress is used for the treatment of arterial hypertension in patients requiring combined treatment.

Contraindications

Absolute:
    severe hypotension (systolic blood pressure below 90 mm Hg);
    angioedema (genetically determined or idiopathic), a history of angioedema, including caused by the use of ACE inhibitors;
    severe renal failure with creatinine clearance (CC) less than 30 ml / min;
    hepatic encephalopathy, severe hepatic dysfunction;
    hypokalemia;
    hemodynamically significant obstruction of LVOT (left ventricular outflow tract), caused, for example, by severe aortic stenosis or hypertrophic obstructive cardiomyopathy; hemodynamically significant mitral stenosis;
    heart failure (hemodynamically unstable) after myocardial infarction;
    shock (including cardiogenic);
    unstable angina (excluding Prinzmetal's angina);
    simultaneous administration with drugs containing aliskiren in patients with diabetes mellitus and / or moderate / severe renal impairment [GFR (glomerular filtration rate) less than 60 ml / min / 1.73 m2];
    simultaneous administration with ARA (angiotensin receptor antagonists) II in patients with diabetic nephropathy;
    simultaneous administration with NEP (neutral endopeptidase) inhibitors, for example, containing sacubitrile, due to an increased risk of Quincke's edema;
    the period of pregnancy and breastfeeding;
    age under 18;
    galactosemia, hereditary lactose intolerance, glucose-galactose malabsorption syndrome;
    established hypersensitivity to amlodipine and other dihydropyridine derivatives, to lisinopril and other ACE inhibitors, to indapamide and other sulfonamide derivatives, as well as to auxiliary components in Ekvapress.
With caution, Ekvapress is prescribed to patients with aortic / mitral stenosis, hypertrophic obstructive cardiomyopathy, arterial hypotension, Prinzmetal angina, cerebrovascular diseases (including cerebrovascular insufficiency), ischemic heart disease, coronary insufficiency, acute a months after myocardial infarction), chronic heart failure of non-ischemic etiology of III-IV class, SSS (sick sinus syndrome), severe autoimmune systemic diseases of the connective tissue [including SLE (systemic lupus erythematosus), scleroderma], myelosuppression, sugar diabetes, hyperkalemia, hepatic failure, renal failure, bilateral renal artery stenosis, stenosis of an artery of a single kidney, with primary aldosteronism, azotemia, diet with salt restriction, condition after kidney transplantation, conditions associated with a decrease in CV K (circulating blood volume), including with vomiting and diarrhea, and elderly patients (over 65 years old).
In addition, caution should be exercised when prescribing Ekvapress to weakened patients, persons receiving combination therapy with drugs that lengthen the QT interval on an ECG (electrocardiogram); simultaneously with aliskiren-containing drugs or ARA II receptor antagonists (double blockade of the RAAS increases the risk of hyperkalemia, arterial hypotension, renal failure); with violations of water and electrolyte balance, prolongation of the QT interval on the ECG, hyperuricemia (especially accompanied by gout and urate nephrolithiasis), hyperparathyroidism and black patients.

Instructions for use: method and dosage

Ekvapress capsules are intended for oral administration, the dosage regimen does not depend on food intake. It is preferable to take the capsules in the morning, at the same time every day.
Fixed-dose combination drugs are not recommended for initial therapy.
The combined drug is intended for the treatment of adult patients who have achieved adequate blood pressure control by taking lisinopril, amlodipine and indapamide in doses similar to those in Ekvapress:
    amlodipine 5 mg, indapamide 1.5 mg, lisinopril 10 mg: Ekvapress 5 + 1.5 + 10 mg;
    amlodipine 10 mg, indapamide 1.5 mg, lisinopril 20 mg: Ekvapress 10 + 1.5 + 20 mg;
    amlodipine 5 mg, indapamide 1.5 mg, lisinopril 20 mg: Ekvapress 5 + 1.5 + 20 mg.
The recommended daily (it is also the maximum) dose is 1 capsule.
If symptomatic arterial hypotension develops at the beginning of the course of therapy, the patient should take the supine position, suspend treatment and consult a specialist. As a rule, transient arterial hypotension does not require discontinuation of the drug, however, when it appears, the need to reduce the dose is assessed.
If dose selection is required Ekvapress, amlodipine, indapamide and lisinopril are taken separately during dose titration.
If you skip taking a capsule, take the next one at the usual time. Do not take two capsules at the same time to make up for a missed dose.

Side effects

    blood and lymph: rarely - a decrease in hemoglobin, a decrease in hematocrit; extremely rare - anemia, leukopenia, inhibition of bone marrow hematopoiesis, agranulocytosis, thrombocytopenia, aplastic / hemolytic anemia, neutropenia, lymphadenopathy;
    immune system: extremely rare - hypersensitivity reactions, autoimmune disorders;
    endocrine system: rarely - SNADH (syndrome of inadequate secretion of antidiuretic hormone); extremely rare - hypoglycemia, hyperglycemia, hypercalcemia; the frequency has not been established - a decrease in the content of K + and the development of hypokalemia (especially significant for people at risk), hyponatremia;
    psyche: infrequently - sleep disturbances, mood lability, insomnia, anxiety, hallucinations, depression; rarely - confusion of consciousness;
    nervous system: often - headache, dizziness, drowsiness; infrequently - dysgeusia, vertigo, paresthesia, fainting, hypesthesia, tremor; rarely - increased fatigue, parosmia (impaired sense of smell); extremely rare - hypertonicity, peripheral neuropathy; frequency not established - extrapyramidal disorders;
    organ of vision: often - visual impairment (including diplopia); frequency not established - blurred vision, myopia;
    organ of hearing and vestibular apparatus: infrequently - tinnitus;
    heart: often - palpitations; infrequently - arrhythmia, bradycardia, tachycardia, ventricular tachycardia, atrial fibrillation, myocardial infarction; frequency not established - polymorphic ventricular tachycardia of the "pirouette" type (potentially fatal);
    vessels: often - orthostatic hypotension, including associated symptoms, flushing of the skin of the face; infrequently - Raynaud's syndrome, stroke (acute cerebrovascular accident) as a result of a pronounced fall in blood pressure in patients at increased risk, arterial hypotension; extremely rare - a pronounced decrease in blood pressure, vasculitis;
    respiratory system: often - cough, shortness of breath; infrequently - rhinitis; extremely rare - bronchospasm, eosinophilic pneumonia, allergic alveolitis, sinusitis;
    Gastrointestinal tract: often - nausea, abdominal pain, dyspepsia, diarrhea, constipation, changes in the rhythm of bowel movements, vomiting; infrequently - dry mouth; extremely rare - gastritis, pancreatitis, gingival hyperplasia, angioedema of the intestine;
    hepatobiliary system: extremely rarely - jaundice, hepatitis (including hepatocellular or cholestatic), impaired liver function, increased activity of liver enzymes (primarily due to cholestasis); the frequency has not been established - in patients with hepatic insufficiency, hepatic encephalopathy may develop;
    skin and subcutaneous tissues: often - hypersensitivity reactions, maculopapular rash; infrequently - exanthema, alopecia, purpura, hyperhidrosis, skin depigmentation, rash, pruritus, urticaria; rarely - psoriasis, Quincke's edema, hypersensitivity, angioedema of the face, hands and feet, lips, tongue, glottis and / or larynx; extremely rare - erythema multiforme, exfoliative dermatitis, toxic epidermal necrolysis, Stevens-Johnson syndrome, photosensitivity, pemphigus vulgaris, benign skin lymphadenosis [symptom complex, including one or more of the following symptoms: myalgia, arthralgia / arthritis, fever, vasculitis reaction, positive (antinuclear antibodies), increased ESR (erythrocyte sedimentation rate), eosinophilia, leukocytosis, skin rash, photosensitivity or other skin changes]; frequency not established - exacerbation of SLE;
    musculoskeletal system: often - cramps, swelling of the ankles; infrequently - myalgia, arthralgia, back pain;
    urinary system: often - impaired renal function; infrequently - nocturia, urinary disorder, frequent urination; rarely - uremia, acute renal failure; extremely rare - oliguria, anuria;
    genitals and mammary gland: infrequently - impotence, gynecomastia;
    general disorders: very often - edema; often - asthenia, increased fatigue; infrequently - pain, malaise, chest pain;
    results of laboratory and instrumental testing: infrequently - hyperkalemia, an increase in the level of creatinine and urea in plasma, an increase in the activity of liver enzymes, a decrease / increase in body weight; rarely - hyponatremia, hyperbilirubinemia; frequency not established - prolongation of the QT interval on the ECG, increased blood glucose.

Overdose

Amlodipine

Symptoms: a strong decrease in blood pressure, in some cases with the development of excessive peripheral vasodilation and reflex tachycardia (increased risk of developing significant and persistent arterial hypotension, up to shock and death).
Therapy: gastric lavage, intake of activated charcoal (especially the first 2 hours after an overdose), after which the patient should take a horizontal position and raise his legs. He is provided with active support of the cardiovascular system with control of indicators of heart and lung function, control of urine output and BCC. If there are no contraindications for restoring vascular tone and blood pressure, it is advisable to prescribe vasoconstrictors. Intravenous infusion of calcium gluconate can relieve the effects of calcium channel blockade. Hemodialysis is ineffective.

Indapamide

The toxic effect of indapamide was not observed even when very high doses were taken (up to 40 mg, that is, 27 times higher than the therapeutic dose).
Symptoms: acute intoxication with indapamide is primarily associated with a violation of water-electrolyte metabolism (hypokalemia, hyponatremia), the clinical signs of which may be nausea, vomiting, convulsions, decreased blood pressure, dizziness, confusion, drowsiness, polyuria or oliguria leading to anuria ( due to hypovolemia).
Therapy: emergency care - elimination of indapamide from the body, gastric lavage and / or intake of adsorbents (activated carbon) with restoration of water-electrolyte balance.

Lisinopril

Symptoms: clinically significant decrease in blood pressure, anxiety, increased irritability, drowsiness, dry mouth, urinary retention, constipation.
Therapy: intravenous administration of 0.9% sodium chloride solution; if there are no contraindications, vasopressors are administered. The patient is provided with monitoring of blood pressure and water-electrolyte balance, if necessary, symptomatic treatment is carried out. Hemodialysis is effective.

Special instructions

When hospitalized, the patient is obliged to inform the staff about the use of Ekvapress.
During therapy with Ekvapress, all special instructions regarding the individual active components of the drug are taken into account.

Influence on the ability to drive vehicles and complex mechanisms

The presence of the risk of dizziness, drowsiness, lowering blood pressure, etc., in the profile of side effects of Ekvapress, requires caution when performing potentially hazardous types of work, such as driving vehicles, controlling moving mechanisms, etc.

Application during pregnancy and lactation

It is contraindicated to use Ekvapress capsules for the treatment of pregnant and breastfeeding women.

Childhood use

Ekvapress is not used in pediatrics.

With impaired renal function

    severe renal failure (CC <30 ml / min) - the use of Ekvapress is contraindicated;
    renal failure, stenosis of the artery of a single kidney, bilateral stenosis of the renal arteries, condition after kidney transplant - use with caution.
For violations of liver function
    hepatic encephalopathy or severe liver dysfunction - the use of Ekvapress is contraindicated;
    liver failure - use with caution.

Use in the elderly

Patients over 65 years of age should be prescribed Ekvapress with caution.

Drug interactions

Taking into account the high pharmacological activity of all active substances of Ekvapress and the clinical significance of their drug interactions with substances / drugs used simultaneously, the appointment of any means during the combination therapy of arterial hypertension must be agreed with the attending physician. The specialist will be able to take into account the potential mutual influence concerning all active components of the drug.

Terms and conditions of storage

Store at a temperature not exceeding +25 ° C. Keep out of the reach of children.
Shelf life is 2 years.

Reviews

According to reviews, Ekvapress relieves blood pressure well and quickly. Patients find the form of release and dosage regimen of the drug convenient. They note that each capsule cell is labeled by day of the week, which helps to keep track of whether the medicine is taken on that day or not. At the same time, a large number of side effects are noted that negatively affect the quality of life.

Terms of sell

You can buy Ekvapress without a prescription.