Amlodipine-VERTEX
Latin name: Amlodipine-VERTEX
ATX code: C08CA01
Active ingredient: amlodipine (Amlodipine)
Manufacturer: JSC "VERTEX" (Russia)
Description and photo update: 2020-14-05
Prices in pharmacies: from 53 rubles.
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Amlodipine-VERTEX is a drug with antihypertensive and antianginal action.
Release form and composition
The drug is produced in the form of tablets: flat-cylindrical, round, almost white or white, with a chamfer (10, 15, 20 or 30 pcs. In a blister strip packaging, a cardboard box may contain: 1-3 or 6 packs of 10 pcs.; 2 or 4 packs of 15 pcs; 1 or 3 packs of 20 pcs; 1 or 2 packs of 30 pcs. Each pack also contains instructions for the use of Amlodipine-VERTEX).
Composition for 1 tablet:
- active substance: amlodipine besylate - 6.95 or 13.9 mg (in terms of amlodipine - 5 or 10 mg, respectively);
- additional components: microcrystalline cellulose, lactose monohydrate, calcium stearate, croscarmellose sodium.
Pharmacological properties
Pharmacodynamics
Amlodipine is a derivative of dihydropyridine, a third-generation slow calcium channel blocker (BMCC), with antianginal and antihypertensive effects. Interacting with dihydropyridine receptors, it leads to blocking of calcium channels and a decrease in the transmembrane transition of calcium ions into the cell (to a greater extent in vascular smooth muscle cells than in myocardial cells).
The antianginal effect of Amlodipine-VERTEX is associated with the expansion of the coronary and peripheral arteries and arterioles. Against the background of angina pectoris, the active substance weakens the severity of ischemia of the heart muscle, causing expansion of peripheral arterioles; provides a decrease in the level of total peripheral vascular resistance (OPSS), a decrease in afterload on the heart, a decrease in myocardial oxygen demand. By expanding the main coronary arteries and arterioles in the unchanged and ischemic zones of the myocardium, the drug increases the supply of oxygen to the heart muscle (especially in patients with vasospastic angina), and also prevents the occurrence of spasm of the coronary arteries (including those caused by smoking).
The use of a single daily dose of amlodipine in patients with angina pectoris leads to an increase in exercise tolerance, a slowdown in the development of angina pectoris and ischemic depression of the ST segment, a decrease in the incidence of angina attacks and a decrease in the need for nitroglycerin or other nitrates.
Due to the direct vasodilating effect on vascular smooth muscle, Amlodipine-VERTEX has a prolonged dose-dependent hypotensive effect. After taking the drug in a single dose, with arterial hypertension, a clinically significant decrease in blood pressure (BP) is recorded after 6-10 hours, and then it is noted for 24 hours in the patient's lying and standing position. The development of orthostatic hypotension during treatment with the drug is recorded quite rarely.
Amlodipine-VERTEX helps to reduce the degree of left ventricular (LV) myocardial hypertrophy, without causing a decrease in the LV ejection fraction. The drug does not shorten the time for performing physical activity; in patients with coronary heart disease (IHD) it demonstrates antiatherosclerotic and cardioprotective effects.
During the period of use of the drug, no reflex increase in heart rate (HR) and the effect on myocardial contractility and conductivity are recorded. Amlodipine-VERTEX helps to suppress platelet aggregation, increase glomerular filtration rate, and exhibits a weak natriuretic effect. Does not increase the severity of microalbuminuria in diabetic nephropathy. There is no negative effect of amlodipine on the plasma level of lipids in the blood and the metabolism of substances in the body, therefore it can be used in patients with gout, bronchial asthma and diabetes mellitus.
In patients with diseases of the cardiovascular system (including with atherosclerosis of the carotid arteries, coronary atherosclerosis with damage to 1 vessel and before stenosis of 3 or more arteries) who have undergone percutaneous transluminal coronary angioplasty (PTCA), myocardial infarction, or suffering from angina pectoris, the use of amlodipine prevents the development of thickening of the intima-media complex of the carotid arteries, reduces mortality from stroke, myocardial infarction, PTCA, coronary artery bypass grafting. Amlodipine-VERTEX provides a decrease in the number of hospitalizations for unstable angina pectoris and progression of chronic heart failure (CHF), reduces the frequency of surgical interventions aimed at restoring coronary blood flow.
Amlodipine-VERTEX does not exacerbate the risk of complications or mortality in patients with CHF III – IV functional class according to the classification of the New York Heart Association (NYHA) with concomitant treatment with diuretics, angiotensin-converting enzyme (ACE) inhibitors, and digoxin. However, it should be borne in mind that in the case of CHF III-IV class of non-ischemic etiology against the background of the use of amlodipine in the absence of signs of worsening heart failure, the risk of pulmonary edema increases.
Pharmacokinetics
Amlodipine after oral administration is quite well absorbed from the gastrointestinal tract (GIT). The maximum concentration of the substance (C max) in the blood plasma is recorded after 6–12 hours, the average absolute bioavailability can vary from 64 to 80%. The concentration of stable equilibrium (C ss) is reached 7–8 days after the start of the course of treatment. Simultaneous food intake does not affect the absorption of Amlodipine-VERTEX.
The average volume of distribution of amlodipine (V d) is 21 l / kg of body weight. This fact indicates that most of the substance is distributed in the tissue, and less in the blood. The drug passes through the blood-brain barrier. The predominant amount of amlodipine entering the blood (97.5%) interacts with plasma proteins.
Amlodipine is slowly but extensively (90%) metabolized in the liver, with a primary passage effect. The active substance metabolites do not show significant pharmacological activity.
After a single oral administration, the half-life (T 1/2) can be 35-50 hours, with repeated use - approximately 45 hours. The total clearance of amlodipine is 0.116 ml / s / kg (0.42 l / h / kg or 7 ml / min / kg). Eliminated by the kidneys on average 60% of the oral dose of the drug, mainly in the form of metabolites, and only 10% - unchanged, through the intestine with bile is excreted 20-25%.
Indications for use
Amlodipine-VERTEX is recommended for use both in monotherapy mode and as part of the combined treatment of the following diseases:
- arterial hypertension;
- vasospastic angina, including variant angina or Prinzmetal angina;
- exertional angina.
Contraindications
Absolute:
- obstruction of the outflow tract of the LV (including severe aortic stenosis);
- shock, including cardiogenic;
- collapse;
- severe arterial hypotension (systolic blood pressure below 90 mm Hg);
- hemodynamically unstable heart failure in the period after myocardial infarction;
- lack of lactase, lactose intolerance, glucose-galactose malabsorption;
- age under 18;
- hypersensitivity to any component of Amlodipine-VERTEX tablets.
Relative (therapy should be done with caution):
- mild / moderate arterial hypotension;
- unstable angina;
- sick sinus syndrome (tachycardia, severe bradycardia);
- CHF III and IV functional class according to NYHA classification, non-ischemic etiology;
- aortic / mitral stenosis;
- acute myocardial infarction (and the period within 1 month after it);
- hypertrophic obstructive cardiomyopathy;
- liver dysfunction;
- combined treatment with inhibitors / inducers of the CYP3A4 isoenzyme.
Amlodipine-VERTEX, instructions for use: method and dosage
Amlodipine-VERTEX tablets are taken orally 1 time / day with up to 100 ml of water.
The initial dose of the drug is 5 mg. Taking into account the therapeutic response, the dose may be increased to the maximum permissible daily dose of 10 mg. For arterial hypertension, the recommended maintenance dose is 5 mg / day.
For patients with vasospastic angina and exertional angina, the drug is prescribed in a dose of 5-10 mg / day once.
When taken simultaneously with β-blockers, thiazide diuretics, ACE inhibitors, dose adjustment is not required.
Side effects
In determining the incidence of adverse reactions, the recommendations of the World Health Organization (WHO) were used: ≥ 1/10 - very often; ≥ 1/100, but <1/10 - often; ≥ 1/1000, but <1/100 - infrequently; ≥ 1/10000, but <1/1000 - rarely; <1/10000, including individual messages - extremely rare; it is not possible to establish a frequency based on the available data - with an unknown frequency.
Possible side reactions when taking Amlodipine-VERTEX from systems and organs:
- nervous system: often - drowsiness, increased fatigue, dizziness, headache; infrequently - general malaise, asthenia, insomnia, hypesthesia, mood lability, tremors, increased excitability, ringing in the ears, anxiety, taste perversion, depression, unusual dreams, paresthesia, peripheral neuropathy; extremely rare - increased sweating, ataxia, apathy, amnesia, agitation, migraine; with an unknown frequency - extrapyramidal disorders;
- respiratory system, chest and mediastinal organs: infrequently - rhinitis, epistaxis, shortness of breath; extremely rare - chest pain, cough;
- blood and lymphatic system: extremely rare - leukopenia, thrombocytopenic purpura, thrombocytopenia;
- organ of vision: infrequently - accommodation disturbances, diplopia, conjunctivitis, xerophthalmia, visual impairment, eye pain;
- muscle, skeletal and connective tissue: infrequently - myalgia, muscle cramps, back pain, arthralgia, arthrosis; rarely - myasthenia gravis;
- heart: often - palpitations; extremely rare - the appearance or deterioration of the course of CHF, myocardial infarction, cardiac arrhythmias c. h. bradycardia, ventricular tachycardia and atrial fibrillation;
- vessels: often - rush of blood to the skin of the face, peripheral edema, including the feet and ankles; infrequently - a significant decrease in blood pressure; extremely rare - fainting, orthostatic hypotension, vasculitis;
- metabolism and nutrition: infrequently - increase / decrease in body weight, thirst, anorexia; rarely - increased appetite; extremely rare - hyperglycemia;
- digestive system: often - nausea, epigastric pain; infrequently - dryness of the oral mucosa, flatulence, dyspepsia, constipation / diarrhea, vomiting; rarely - gingival hyperplasia; extremely rarely - increased activity of hepatic transaminases, hyperbilirubinemia, jaundice (caused by cholestasis), gastritis, pancreatitis, hepatitis;
- reproductive system and mammary gland: infrequently - erectile dysfunction; extremely rare - polyuria, dysuria;
- kidneys and urinary tract: infrequently - nocturia, frequent and / or painful urination;
- immune system: infrequently - rash (including maculopapular, erythematous), pruritus, urticaria; extremely rarely - erythema multiforme, angioedema, Stevens-Johnson syndrome;
- skin and subcutaneous tissues: rarely - dermatitis; extremely rare - cold sweat, xeroderma, alopecia, skin pigmentation disorders;
- general disorders and reactions together introduction: infrequently - pain of unspecified localization, chills, gynecomastia; extremely rare - parosmia.
Overdose
Symptoms of an overdose of Amlodipine-VERTEX may include tachycardia, a significant decrease in blood pressure, excessive peripheral vasodilation with the possible occurrence of severe and persistent arterial hypotension, including the development of shock and death.
In this condition, gastric lavage and the intake of activated carbon are prescribed, especially during the first 2 hours after an overdose. The patient should be kept in a horizontal position with raised legs. It is recommended to carry out measures to maintain the work of the cardiovascular system and monitor indicators of lung and heart function, as well as urine output and circulating blood volume (BCC). In order to restore vascular tone in the absence of contraindications, vasoconstrictor agents are used, the consequences of blockade of calcium channels are eliminated by intravenous administration of calcium gluconate. Hemodialysis for the elimination of amlodipine is ineffective.
special instructions
During therapy, it is necessary to control body weight and sodium intake, as well as adhere to an appropriate diet.
To prevent soreness, bleeding and gingival hyperplasia, it is necessary to observe oral hygiene and regularly see a dentist.
Patients of short stature or low body weight may need to reduce the dose of Amlodipine-VERTEX.
Although BMCCs do not cause withdrawal symptoms, it is recommended to complete the course of treatment by gradually reducing the dose of amlodipine.
In the treatment of angina pectoris, Amlodipine-VERTEX can be used as a monotherapy drug or in combination with other antianginal agents, including in patients who are refractory to treatment with β-blockers and / or nitrates in adequate doses.
In hypertensive crisis, the safety and efficacy of drug therapy have not been established.
The drug has no effect on the plasma level of potassium ions, triglycerides, glucose, high density lipoproteins, total cholesterol, uric acid, creatinine and urea nitrogen.
Amlodipine can be used in patients who are prone to vasospasm / vasoconstriction.
Influence on the ability to drive vehicles and complex mechanisms
There are no reports of any adverse effects of Amlodipine-VERTEX on the ability to drive complex mechanisms, including vehicles. However, given the possible excessive decrease in blood pressure, the development of drowsiness, dizziness and other undesirable effects, caution should be exercised when performing complex and potentially hazardous work, especially at the beginning of the course of therapy and during the period of increasing the dose.
Application during pregnancy and lactation
During pregnancy, the safety of using Amlodipine-VERTEX has not been established, therefore, its use during this period is allowed only if the benefit to the woman significantly exceeds the possible threat to the fetus.
The experience of using the drug has shown that amlodipine is excreted in breast milk. For its concentration, the ratio in milk / in plasma averaged 0.85 in 31 lactating women who suffered from pregnancy-related hypertension and received the drug at an initial dose of 5 mg / day. If necessary, the dose was adjusted taking into account the weight and the average daily dose - 0.0987 mg / kg and 6 mg, respectively. The dose of Amlodipine-VERTEX received by an infant with mother's milk is estimated to be 0.00417 mg / kg / day.
In animal studies, the effect of the active substance on fertility was not found.
Pediatric use
Amlodipine-VERTEX is contraindicated for use in children and adolescents under 18 years of age, since its effectiveness and safety in patients of this age group have not been established.
With impaired renal function
Renal failure does not significantly alter the kinetics of amlodipine. In patients with impaired renal function, dose changes are not required, however, it is important to take into account the likelihood of a slight lengthening of T 1/2 of the drug.
For violations of liver function
In the presence of liver failure, T 1/2 of amlodipine, like the rest of the BMCC, increases, and in the case of a prolonged course of treatment, its cumulation will increase (T 1/2 to 60 hours). Patients with severe hepatic impairment may need a lower dose of Amlodipine-VERTEX.
Use in the elderly
In patients over 65, compared with patients in other age groups, the elimination of amlodipine is slower, T 1/2 can reach 65 hours, but this fact has no clinical significance.
Elderly people do not need to adjust the dosage regimen and are recommended to take Amlodipine-VERTEX in an average therapeutic dose, however, when prescribing an increase in dose, the condition of these patients should be carefully monitored.
Drug interactions
- nonsteroidal anti-inflammatory drugs, including indomethacin: no clinically significant interaction is recorded;
- ACE inhibitors, thiazide and loop diuretics, nitrates (prolonged or short-acting), β-blockers: potentiate the antianginal and antihypertensive effect of BMCC;
- α1-adrenergic blockers, neuroleptics: enhance the antihypertensive effect of BMCC;
- amiodarone, quinidine and other antiarrhythmic drugs that cause prolongation of the QT interval: an increase in the severity of negative inotropic action is possible when combined with some BMCC (in the study of amlodipine, this effect usually did not develop)
- antibiotics and hypoglycemic oral agents: no adverse reactions are observed;
- simvastatin (at a dose of 80 mg): with the simultaneous repeated use of amlodipine at a dose of 10 mg, an increase in the exposure of simvastatin is noted by 77%, in these cases the dose of the latter must be reduced to 20 mg;
- isoflurane, antipsychotics: the antihypertensive efficacy of dihydropyridine derivatives is potentiated;
- ritonavir (antiviral agents): increased plasma levels of BMCC, including amlodipine;
- atorvastatin (80 mg): when used repeatedly with amlodipine at a dose of 10 mg, no significant changes in the pharmacokinetic parameters of atorvastatin are recorded;
- sildenafil (100 mg): with a single dose of this substance against the background of essential hypertension, there is no effect on the pharmacokinetics of amlodipine;
- calcium preparations: the effectiveness of BMCC decreases;
- ethanol-containing agents: the pharmacokinetics of ethanol with single and repeated use with amlodipine (10 mg) does not change;
- cyclosporine: in some cases, an increase in the minimum concentration (C min) of this substance up to 40% is recorded; in patients after kidney transplantation, it is required to monitor the concentration of cyclosporine;
- warfarin: there is no significant effect on the effect of this substance (prothrombin time);
- indomethacin, phenytoin, digoxin, warfarin: the effect of amlodipine on the binding of these drugs to plasma blood proteins is not observed in in vitro studies;
- digoxin: plasma levels of this substance and its renal clearance are not affected by amlodipine;
- lithium preparations: possible aggravation of the manifestation of neurotoxicity of these drugs (tinnitus, tremor, ataxia, vomiting, nausea, diarrhea) when combined with BMCC (there are no research results for amlodipine);
- aluminum or magnesium-containing antacids (with a single dose), cimetidine: the pharmacokinetic parameters of amlodipine do not change significantly;
- diltiazem at a dose of 180 mg (inhibitors of the isoenzyme CYP3A4): there is a 57% increase in systemic exposure to amlodipine in elderly patients (69–87 years old) with arterial hypertension;
- itraconazole, ketoconazole and other potent inhibitors of the CYP3A4 isoenzyme: an increase in the plasma level of amlodipine in the blood is possible;
- clarithromycin (inhibitors of the isoenzyme CYP3A4): the threat of lowering blood pressure is aggravated, which requires medical monitoring of the patient's condition;
- inducers of the isoenzyme CYP3A4: there is no data on the effect on the pharmacokinetics of amlodipine; careful monitoring of blood pressure is recommended;
- tacrolimus: the risk of an increase in the concentration of this substance in the blood increases, its plasma level should be monitored and the dose adjusted if necessary;
- temsirolimus, everolimus, sirolimus - inhibitors of the mechanistic target for rapamycin in mammals (mTOR) (substrates of the CYP3A isoenzyme): there may be an increase in the exposure of these agents;
- grapefruit juice (240 mg): there are no significant changes in the pharmacokinetics of amlodipine when taken at a dose of 10 mg, however, it is not recommended to use these drugs simultaneously due to a possible increase in the bioavailability of amlodipine and, as a result, an increase in the antihypertensive effect.
Analogs
Amlodipine-VERTEX analogs are: Amlodivel, Amlodipine, Karmagip, Amlovas, Normodipin, Amlong, Corvadil, Cardilopin, Amlotop, Kalchek, etc.
Terms and conditions of storage
Store at a temperature not exceeding 25 ° C in a place protected from light and out of reach of children.
The shelf life is 3 years.
Terms of dispensing from pharmacies
Dispensed by prescription.
Reviews about Amlodipine-VERTEX
Reviews of Amlodipine-VERTEX are mostly positive. The drug gently reduces elevated blood pressure, has a long-term hypotensive effect, slows down the development of angina pectoris and reduces the frequency of its attacks, leading to a decrease in the intake of nitroglycerin or other antianginal drugs. Patients also note a convenient dosing regimen and a low cost of the drug.
The disadvantages of Amlodipine-VERTEX are that it is not intended to relieve a hypertensive crisis, has a large number of contraindications and side reactions.
Price for Amlodipine-VERTEX in pharmacies
The price of Amlodipine-VERTEX depends on the dosage of the drug and can be per pack containing 20 or 60 pieces, respectively: 5 mg tablets - 60 or 110 rubles, 10 mg tablets - 80 or 160 rubles.
Amlodipine-VERTEX: prices in online pharmacies
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Amlodipine-vertex tablets 5mg 60pcs 106 RUB Buy |
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Amlodipine-Vertex tablets 10mg 60 pcs. 156 r Buy |
Maria Kulkes Medical journalist About the author
Education: First Moscow State Medical University named after I. M. Sechenov, specialty "General Medicine".
Information about the drug is generalized, provided for informational purposes only and does not replace the official instructions. Self-medication is hazardous to health!
