Ekvamer (Equamer) caps 5mg + 10mg + 20mg #30
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User manual for Ekvamer
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Ekvamer is an antihypertensive and lipid-lowering drug.
Release form and composition
Ekvamer is available in capsule form: gelatinous, hard; the contents of the capsules are round biconvex white tablets (lisinopril + amlodipine) and yellow film-coated tablets (rosuvastatin); capsule in a dosage of 5 mg + 10 mg + 10 mg - size No. 1, light pink, contains 1 white and 1 yellow tablet; capsule in a dosage of 5 mg + 10 mg + 20 mg - size No. 1, pink, contains 1 white and 2 yellow tablets; a capsule in a dosage of 10 mg + 20 mg + 10 mg - size No. 1, purple, contains 2 white and 1 yellow tablets; capsule at a dosage of 10 mg + 20 mg + 20 mg - size No. 0, dark purple, contains 2 white and 2 yellow tablets (in blisters: 5 pcs., 6 blisters in a cardboard box; 7 pcs., in a cardboard box a pack of 4 blisters, 10 pcs., in a cardboard box 3 blisters. Each pack also contains instructions for the use of Ekvamer).
1 capsule contains the following active ingredients:
dosage 5 mg + 10 mg + 10 mg: amlodipine besylate - 6.94 mg (equivalent to 5 mg amlodipine), lisinopril dihydrate - 10.88 mg (10 mg lisinopril), rosuvastatin calcium - 10.4 mg (10 mg rosuvastatin);
dosage 5 mg + 10 mg + 20 mg: amlodipine besylate - 6.94 mg (5 mg amlodipine), lisinopril dihydrate - 10.88 mg (10 mg lisinopril), rosuvastatin calcium - 20.8 mg (20 mg rosuvastatin);
dosage 10 mg + 20 mg + 10 mg: amlodipine besylate - 13.88 mg (10 mg amlodipine), lisinopril dihydrate - 21.76 mg (20 mg lisinopril), rosuvastatin calcium - 10.4 mg (10 mg rosuvastatin);
dosage 10 mg + 20 mg + 20 mg: amlodipine besylate - 13.88 mg (10 mg amlodipine), lisinopril dihydrate - 21.76 mg (20 mg lisinopril), rosuvastatin calcium - 20.8 mg (20 mg rosuvastatin).
Auxiliary components: lactose monohydrate, microcrystalline cellulose (types 12 and 101), sodium carboxymethyl starch, magnesium stearate, magnesium hydroxide, Opadray II yellow (code 85F32410).
Composition of a hard gelatin capsule: gelatin, titanium dioxide and, depending on the dosage, the following colorants:
dosage 5 mg + 10 mg + 10 mg: azorubin, patented blue, sunset yellow;
dosage 5 mg + 10 mg + 20 mg: azorubin;
dosage 10 mg + 20 mg + 10 mg: azorubin, indigo carmine;
dosage 10 mg + 20 mg + 20 mg: azorubin, patented blue, sunset yellow.
Pharmacodynamics
Ekvamer is a combined antihypertensive and lipid-lowering drug.
The mechanism of action of Ekvamer is due to the pharmacological properties of its three active ingredients:
amlodipine: a slow calcium channel blocker (BMCC), a dihydropyridine derivative. Reducing the transmembrane transition of calcium ions (mostly in vascular smooth muscle cells than in cardiomyocytes), amlodipine has an antihypertensive and antianginal effect. Long-term dose-dependent hypotensive effect is associated with a direct vasodilating effect on vascular smooth muscle. A single dose provides patients with a clinically significant decrease in blood pressure (blood pressure) in the supine and standing position within 24 hours after administration. As a result of the expansion of the coronary and peripheral arteries and arterioles, an antianginal effect is manifested - the total peripheral vascular resistance (OPSR) decreases, myocardial oxygen demand and afterload on the heart decreases, coronary artery spasm is prevented, and oxygen supply to the myocardium increases. In patients with angina pectoris, the severity of myocardial ischemia decreases, exercise tolerance increases, the development of angina attacks and ischemic ST-segment depression slows down, the frequency of angina attacks and the need to take nitroglycerin or other nitrates decrease;
lisinopril: an angiotensin-converting enzyme (ACE) inhibitor. Reducing the formation of angiotensin II from angiotensin I, it helps to reduce the secretion of aldosterone, degradation of bradykinin, OPSS, blood pressure, pressure in the pulmonary capillaries, preload. It causes an increase in the synthesis of prostaglandins, minute blood volume, an improvement in the blood supply to the ischemic myocardium, in patients with CHF (chronic heart failure) - an increase in myocardial tolerance to physical exertion. After oral administration, the hypotensive effect is observed after 1 hour, the maximum effect - after 6-7 hours and lasts for 24 hours. With arterial hypertension, a decrease in blood pressure is noted from the first days of therapy, a stable effect - after 30-60 days. In addition, lisinopril reduces albuminuria. In case of hyperglycemia, it normalizes the functions of the damaged glomerular endothelium. In diabetes mellitus, it does not affect the level of glucose in the blood, does not lead to an increase in cases of hypoglycemia;
rosuvastatin: a selective competitive inhibitor of hydroxymethylglutaryl coenzyme A (HMG-CoA) reductase, an enzyme that converts 3-hydroxy-3-methylglutaryl coenzyme A to mevalonate, a precursor of cholesterol. Promotes an increase in the number of LDL receptors (low density lipoproteins) on the surface of hepatocytes, increases the uptake and catabolism of LDL, inhibits the synthesis of VLDL (very low density lipoproteins). Reduces the increased concentration of total cholesterol (Chs), Chs-LDL, Chs-VLDL, triglycerides (TG), apolipoprotein B (ApoB), Chs-non-HDL, TG-VLDL. It causes an increase in the concentration of Xc high density lipoproteins (HDL-cholesterol), apolipoprotein A-I (ApoA-I). Reduces the ratio of Xs-LDL and Xs-HDL, total Xs and Xs-HDL, Xs-non-HDL and Xs-HDL, ApoB and ApoA-I. The maximum effect is achieved 21 days after the start of therapy and persists with regular use.
Pharmacokinetics
After oral administration, the maximum concentration (Cmax) of amlodipine in the blood is reached after 6-12 hours, lisinopril - after 6-8 hours, rosuvastatin - after 5 hours. The average absolute bioavailability of amlodipine is 64-80%, lisinopril - 29%, rosuvastatin - 20 %.
Amlodipine crosses the blood-brain and placental barriers.
The volume of distribution of amlodipine averages 21 l / kg of body weight, rosuvastatin - 134 l.
Plasma protein binding: amlodipine - 97.5% of the substance in the blood, rosuvastatin - 90%.
Amlodipine is biotransformed in the liver slowly, but actively, with the formation of metabolites with weak pharmacological activity.
Lisinopril is not metabolized in the body.
Rosuvastatin is metabolized mainly in the liver (about 10% of the dose taken), mainly with the participation of the isoenzyme CYP2C9, with the formation of N-desmethyl (activity 50% less than that of rosuvastatin) and inactive lactone metabolites.
Inhibition of circulating HMG-CoA reductase is provided mainly by the pharmacological activity of rosuvastatin (more than 90%).
Half-life (T1 / 2): amlodipine - about 45 hours, lisinopril - 12 hours, rosuvastatin - about 19 hours.
Amlodipine is excreted through the kidneys (70%) and intestines, not removed by hemodialysis.
Lisinopril is excreted in the urine unchanged.
Approximately 90% of the dose of rosuvastatin is excreted unchanged through the intestines.
The total clearance of amlodipine is 0.42 l / h / kg. The geometric mean plasma clearance of rosuvastatin is approximately 50 l / h.
In hepatic failure, T1 / 2 of amlodipine increases to 60 hours; in elderly patients - up to 65 hours.
Indicators Cmax and AUC (area under the curve "concentration - time") of lisinopril in elderly patients is 2 times higher than in young patients.
In renal failure with creatinine clearance (CC) from 5 to 30 ml / min, the average AUC of lisinopril increases 4.5 times, the level of rosuvastatin in blood plasma - 3 times, its metabolite N-desmethyl - 9 times. In patients on hemodialysis, the concentration of rosuvastatin is 50% higher than in healthy volunteers.
The increase in systemic exposure of rosuvastatin occurs in proportion to the dose. AUC and Cmax of rosuvastatin in patients of the Mongoloid race increases 2 times, of Indian nationality - 1.3 times.
There was a 1.6-fold increase in the AUC of rosuvastatin in carriers of the SLCO1B1 (OATP1B1) c.521CC genotypes and 2.4 times in carriers of the ABCG2 (BCRP) c.421AA genotypes compared to carriers of the SLC01B1 c.521TT and ABCG2 c.421CC genotypes, respectively ...
Indications for use
The use of Ekvamer is indicated as a replacement therapy for patients with arterial hypertension and concomitant dyslipidemia, in whom previous treatment with the same doses of amlodipine, lisinopril and rosuvastatin, as in the drug, adequately controlled the condition:
primary hypercholesterolemia (type IIa according to Fredrickson's classification), except for familial heterozygous hypercholesterolemia, or mixed hypercholesterolemia (type IIb according to Fredrickson's classification) - if non-drug methods (including diet, exercise, weight loss) are ineffective;
hypertriglyceridemia (type IV according to the Fredrickson classification);
familial homozygous hypercholesterolemia - with insufficient effect of diet, LDL-apheresis or other lipid-lowering therapy.
Contraindications
Absolute:
a history of angioedema;
hereditary or idiopathic angioedema;
shock;
unstable angina, except for Prinzmetal's angina;
severe arterial hypotension - systolic blood pressure less than 90 mm Hg;
hemodynamically unstable heart failure after acute myocardial infarction;
hemodynamically significant obstruction of the left ventricular outflow tract, hemodynamically significant mitral stenosis;
active phase of liver disease, including any increase in the activity of transaminases (more than 3 times compared to the upper limit of the norm), a persistent increase in the activity of transaminases in the blood serum;
severe hepatic impairment (above 9 points according to Child-Pugh);
severe renal dysfunction (CC less than 30 ml / min);
myopathy;
tendency to the occurrence of myotoxic complications;
combination with aliskiren in the presence of diabetes mellitus and / or moderate to severe renal failure;
simultaneous use of angiotensin II receptor antagonists (ARA II) in diabetic nephropathy;
concomitant therapy with cyclosporine, neutral endopeptidase inhibitors;
lactase deficiency, lactose intolerance, glucose-galactose malabsorption;
period of pregnancy;
breast-feeding;
use in women who do not use adequate methods of contraception;
age under 18;
hypersensitivity to dihydropyridine derivatives, ACE inhibitors or Ekvamer's components.
Care should be taken to use Ekvamer capsules for arterial hypotension, aortic or mitral stenosis, hypertrophic obstructive cardiomyopathy, cerebrovascular diseases, cerebrovascular insufficiency, coronary heart disease, chronic heart failure of non-ischemic etiology of functional class III – IV according to NYHA classification (New York Heart Association) , coronary insufficiency, acute myocardial infarction (and within 30 days after it), Prinzmetal angina pectoris, severe tachycardia or bradycardia, severe autoimmune systemic diseases of connective tissue, myelosuppression, diabetes mellitus, a history of liver disease, sepsis, hyponatremia, bilateral stenosis , stenosis of the artery of a single kidney, mild to moderate renal failure (CC 30-80 ml / min), azotemia, primary aldosteronism, hyperkalemia, decreased blood volume (including vomiting and diarrhea f), mild and moderate liver failure (5-9 points according to Child-Pugh), hypothyroidism, uncontrolled seizures, alcohol abuse, trauma, major surgical interventions, severe metabolic, endocrine or water-electrolyte disorders, treatment with potassium-sparing diuretics and drugs potassium, taking potassium-based salt substitutes, a diet restricted to table salt, a personal or family history of hereditary muscle diseases, a history of muscle toxicity due to the use of other HMG-CoA reductase inhibitors or fibrates; in conditions accompanied by an increase in the concentration of rosuvastatin in plasma, a condition after kidney transplantation; in patients of the Negroid and Mongoloid race; with hemodialysis using highly permeable membranes; in combination with fibrates, inhibitors or inducers of the isoenzyme CYP3A4, aliskiren or ARA II; in old age.
Instructions for use: method and dosage
Ekvamer capsules are taken orally, regardless of food intake, 1 pc. 1 time a day at a fixed time.
The doctor prescribes the drug as replacement therapy only for those patients who are already taking amlodipine, lisinopril and rosuvastatin in titrated optimal maintenance doses.
During treatment, the patient should continue to follow the standard cholesterol diet.
It is recommended to use the following capsule dosage, taking into account the titrated optimal maintenance daily doses of preliminary therapy:
amlodipine - 5 mg, lisinopril - 10 mg, rosuvastatin - 10 mg: Ekvamer 5 mg + 10 mg + 10 mg;
amlodipine - 5 mg, lisinopril - 10 mg, rosuvastatin - 20 mg: Ekvamer 5 mg + 10 mg + 20 mg;
amlodipine - 10 mg, lisinopril - 20 mg, rosuvastatin - 10 mg: Ekvamer 10 mg + 20 mg + 10 mg;
amlodipine - 10 mg, lisinopril - 20 mg, rosuvastatin - 20 mg: Ekvamer 10 mg + 20 mg + 20 mg.
To adjust the dose, the patient should be transferred to individual dosage forms of the active components of the drug.
Side effects
lymphatic system and blood system: very rarely - anemia, leukopenia, thrombocytopenia, lymphadenopathy, agranulocytosis, neutropenia, inhibition of bone marrow hematopoiesis, hemolytic anemia;
immune system: very rarely - allergic reactions, autoimmune disorders; rarely - hypersensitivity reactions, angioedema;
endocrine system: often - type 2 diabetes mellitus; rarely - syndrome of inappropriate secretion of antidiuretic hormone; very rarely - hyperglycemia, hypoglycemia;
mental disorders: rarely - confusion; infrequently - mood lability, sleep disturbances, insomnia, anxiety, depression, hallucinations; rarely - mental disorders;
nervous system: often - headache, dizziness, drowsiness; infrequently - tremor, dysgeusia, vertigo, fainting, paresthesia, hypesthesia; rarely - impaired sense of smell; very rarely - muscle hypertonicity, peripheral neuropathy, polyneuropathy, decreased or loss of memory; frequency not established - extrapyramidal disorders, nightmares, insomnia and other sleep disorders;
cardiovascular system: often - a feeling of palpitations, rushes of blood to the skin of the face, symptoms of orthostatic hypotension; infrequently - heart rhythm disturbances, myocardial infarction, tachycardia, excessive lowering of blood pressure, Raynaud's syndrome, acute cerebrovascular accident; very rarely - vasculitis;
digestive system: often - abdominal pain, nausea, dyspepsia, diarrhea, constipation, changes in the rhythm of bowel movements, vomiting; infrequently - dry mouth, indigestion; rarely - increased activity of liver enzymes; very rarely - gingival hyperplasia, pancreatitis, gastritis, intestinal angioedema, hepatitis, hepatocellular or cholestatic hepatitis, jaundice, liver failure, increased activity of liver enzymes associated with cholestasis;
respiratory system, chest and mediastinal organs: often - shortness of breath, cough; infrequently - rhinitis; very rarely - bronchospasm, sinusitis, allergic alveolitis or eosinophilic pneumonia; frequency not established - interstitial lung disease;
skin and subcutaneous tissue: often - myalgia; infrequently - itching, rash, urticaria, alopecia, purpura, skin depigmentation, hyperhidrosis, exanthema; rarely - angioedema of the face, lips, tongue, glottis, larynx, hands and / or feet, psoriasis; very rarely - angioedema, erythema multiforme, exfoliative dermatitis, Stevens-Johnson syndrome, Quincke's edema, photosensitivity, toxic epidermal necrolysis, pemphigus vulgaris, benign skin lymphadenosis;
musculoskeletal system and connective tissue: often - swelling of the ankles and feet, muscle cramps; infrequently - arthralgia, back pain; rarely - myopathy (including myositis), rhabdomyolysis (including with the development of acute renal failure), lupus-like syndrome, muscle rupture; frequency not established - immune-mediated necrotizing myopathy, tendon diseases (including those complicated by rupture), temporary increase in creatine phosphokinase activity;
urinary system: often - impaired renal function; infrequently - urination disorder, frequent urination, nocturia; rarely - acute renal failure, uremia; very rarely - oliguria or anuria, hematuria; frequency not established - proteinuria;
genitals and mammary gland: infrequently - gynecomastia, impotence; frequency not established - sexual dysfunction;
organs of vision, hearing and labyrinthine disorders: often - diplopia and other visual impairments; infrequently - tinnitus;
general disorders: very often - edema; often - increased fatigue, asthenia; infrequently - malaise, peripheral edema, chest pain, pain;
laboratory parameters: infrequently - an increase or decrease in body weight, serum urea and creatinine levels, hyperkalemia; rarely - hyponatremia, decreased hemoglobin and hematocrit, hyperbilirubinemia.
Overdose
Symptoms: dizziness, anxiety, cough, hypotension (up to the development of shock and death), reflex tachycardia, excessive peripheral vasodilation, hyperventilation, electrolyte imbalance, circulatory shock, renal failure, heart palpitations, bradycardia.
Treatment: immediate gastric lavage, intake of activated charcoal. The patient should take a horizontal position with the legs raised up. The control and maintenance of the functions of vital organs and systems, the volume of circulating blood and diuresis, indicators of electrolytes, urea and creatinine in the blood serum, checking the activity of the enzyme creatine phosphokinase are shown. To eliminate the consequences of calcium channel blockade, intravenous (i / v) administration of calcium gluconate is recommended, to replenish the BCC - i / v administration of plasma-substituting solutions, to restore vascular tone (in the absence of contraindications) - the use of vasoconstrictors. If necessary (in case of development of bradycardia resistant to drug therapy), an artificial pacemaker is used.
The use of hemodialysis is effective only for removing lisinopril.
Special instructions
You cannot use Ekvamer for initial therapy.
It is necessary to inform the doctor about taking the combined drug upon admission to the hospital for treatment.
In addition to these side reactions, which were established when taking certain dosage forms of active substances, it is possible to develop allergic reactions caused by the content of food dyes in the capsule shell.
Influence on the ability to drive vehicles and complex mechanisms
During the period of taking Ekvamer, it is recommended to be careful when driving vehicles, moving mechanisms and engaging in other potentially hazardous activities, the implementation of which requires concentration of attention and high speed of psychomotor reactions.
Application during pregnancy and lactation
The use of Ekvamer is contraindicated during pregnancy and lactation.
Women of childbearing age need to use reliable methods of contraception, in case of conception while taking the drug, therapy should be stopped immediately.
Childhood use
Pediatric patients (children and adolescents under the age of 18) are not prescribed Ekvamer.
With impaired renal function
The use of Ekvamer in severe renal failure (CC less than 30 ml / min) is contraindicated.
Precautions should be taken in patients with mild to moderate renal failure (CC 30–80 ml / min).
For violations of liver function
The use of Ekvamer in severe liver dysfunction and active phase of liver disease is contraindicated.
Precautions should be taken in patients with mild to moderate hepatic impairment.
Use in the elderly
Elderly patients are prescribed with caution.
Drug interactions
During the period of treatment with Ekvamer, taking into account the combined composition of the capsules, taking other medicines is indicated only as directed by the attending physician.
Terms and conditions of storage
Keep out of the reach of children.
Store at temperatures up to 25 ° C.
Shelf life is 3 years.
Reviews
Reviews about Ekvamer are positive. The advantages of the drug include efficiency, ease of use, and price.
Terms of sell
You don't need to have a prescription from a doctor to buy Ekvamer.