Amlovas
Amlovas: instructions for use and reviews
- 1. Release form and composition
- 2. Pharmacological properties
- 3. Indications for use
- 4. Contraindications
- 5. Method of application and dosage
- 6. Side effects
- 7. Overdose
- 8. Special instructions
- 9. Application during pregnancy and lactation
- 10. Use in childhood
- 11. In case of impaired renal function
- 12. For violations of liver function
- 13. Use in the elderly
- 14. Drug interactions
- 15. Analogs
- 16. Terms and conditions of storage
- 17. Terms of dispensing from pharmacies
- 18. Reviews
- 19. Price in pharmacies
Latin name: Amlovas
ATX code: C08CA01
Active ingredient: amlodipine (Amlodipine)
Manufacturer: Unique Pharmaceutical Laboratories (India)
Description and photo update: 2019-10-07
Prices in pharmacies: from 219 rubles.
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Amlovas is a drug with antianginal, antihypertensive, vasodilating and antispasmodic action.
Release form and composition
The drug is produced in the form of tablets: flat, round, almost white or white, with a risk on one of the sides and a chamfer on both sides (10 pieces in an aluminum strip, in a cardboard box 2 or 3 strips and instructions for using Amlovas).
1 tablet contains:
- active substance: amlodipine besylate - 6.944 or 13.889 mg (equivalent to amlodipine in the amount of 5 and 10 mg, respectively);
- additional components: colloidal silicon dioxide, sodium carboxymethyl starch, anhydrous calcium hydrogen phosphate, microcrystalline cellulose, magnesium stearate.
Pharmacological properties
Pharmacodynamics
Amlovas belongs to dihydropyridine derivatives - slow calcium channel blockers (BMCC) of the second generation, has hypotensive and antianginal effects. By communicating with dihydropyridine receptors, the active substance blocks calcium channels, weakens the transition of calcium ions through membranes into cells, mainly into vascular smooth muscle cells, to a lesser extent, into myocardial cells. The antianginal effect of amlodipine is due to the expansion of the coronary and peripheral arterioles and arteries produced by it, which reduces the severity of ischemia of the heart muscle against the background of angina pectoris. As a result of the expansion of peripheral arterioles, the total peripheral vascular resistance (OPSR) is weakened, the preload on the heart decreases, and oxygen consumption by the myocardium decreases.
Providing the expansion of the main coronary arteries and arterioles in both unaffected and ischemic areas of the heart muscle, the active substance increases the flow of oxygen to the myocardium (especially in vasospastic angina pectoris) and prevents the occurrence of constriction of the coronary arteries (including those caused by smoking).
In patients with angina pectoris, the daily dose of Amlovas, taken once a day, can increase the duration of physical activity, slow the development of angina pectoris and ischemic ST segment depression, reduce the frequency of angina attacks and reduce the use of nitrates, including nitroglycerin.
The active substance demonstrates a long-term dose-dependent antihypertensive effect caused by a direct vasodilating effect on the smooth muscles of the vascular walls. As a result of taking a single daily dose of the drug in the treatment of arterial hypertension, a clinically significant decrease in blood pressure (BP) occurs throughout the day in the patient's lying and standing position. Amlodipine does not lead to a sharp decrease in blood pressure and a decrease in exercise tolerance, and also does not affect the left ventricular ejection fraction. The time of the onset of the Amlovas effect is 2–4 hours, the duration of the action is 24 hours.
Helping to reduce the degree of left ventricular myocardial hypertrophy, the active substance exhibits anti-atherosclerotic and cardioprotective effects in ischemic heart disease (IHD). Amlovas does not cause changes in myocardial contractility and conductivity, does not lead to a reflex increase in heart rate (HR), activates glomerular filtration, slows down platelet aggregation, demonstrates a weak natriuretic effect.
In diabetic nephropathy, the agent does not enhance the severity of microalbuminuria. Against the background of therapy with Amlovas, no adverse effects on the metabolism of substances and plasma lipids are recorded.
Pharmacokinetics
After oral administration, the active substance is slowly absorbed from the gastrointestinal tract (GIT). The average absolute bioavailability is 64%, the maximum concentration (C max) of amlodipine in the blood serum is noted after 6-9 hours. After 7 days of the course, a stable equilibrium concentration is achieved, the absorption of the agent does not depend on food intake. The average volume of distribution (V d) is 21 l / kg of body weight, which indicates the penetration of a significant part of the drug taken into the tissues, and relatively less into the blood. Moreover, most of the agent detected in the blood (95%) communicates with blood plasma proteins.
Slow but extensive biotransformation (90%) of amlodipine is produced in the liver with the formation of inactive metabolites. Has the effect of the first passage through the liver. Metabolites do not exhibit significant pharmacological activity.
After oral use of the active substance, the half-life (T ½) can vary from 31 to 48 hours, and with repeated administration, it can be approximately 45 hours. On average, 60% of the dose of amlodipine taken is excreted in the urine (mainly in the form of metabolites, 10% - unchanged), approximately 20-25% - with feces, as well as with breast milk. The total clearance of the agent is 0.116 ml / s / kg (7 ml / min / kg; 0.42 l / h / kg). Amlodipine passes through the blood-brain barrier and is not eliminated by hemodialysis.
Indications for use
- arterial hypertension - in monotherapy mode or in combination with other antihypertensive drugs, such as beta-blockers, diuretics, verapamil, angiotensin-converting enzyme (ACE) inhibitors;
- vasospastic angina (Prinzmetal angina), exertional angina - in monotherapy mode or in combination with other antianginal drugs.
Contraindications
Absolute:
- severe arterial hypotension (systolic blood pressure below 90 mm Hg);
- unstable angina (except for Prinzmetal's angina);
- collapse, cardiogenic shock;
- clinically significant aortic stenosis, obstruction of the outflow tract of the left ventricle;
- pregnancy (except in exceptional cases of extreme necessity and only if the benefit to the mother exceeds the risk to the fetus);
- lactation period;
- age up to 18 years;
- hypersensitivity to amlodipine and other dihydropyridine derivatives.
Relative (use Amlovas tablets with extreme caution):
- chronic heart failure (CHF) in the stage of decompensation;
- sick sinus syndrome (severe tachycardia, bradycardia);
- mild / moderate arterial hypotension;
- hypertrophic obstructive cardiomyopathy;
- aortic / mitral stenosis;
- acute myocardial infarction and within 1 month after it (taking Amlovas is possible after stabilization of hemodynamic parameters);
- diabetes;
- functional disorders of the liver and / or kidneys;
- elderly age.
Amlovas, instructions for use: method and dosage
Amlovas tablets are taken orally with the required amount of water.
For the treatment of angina pectoris and arterial hypertension, the initial dose is 5 mg of amlodipine 1 time per day. With arterial hypertension, the maintenance daily dose can vary from 2.5 to 5 mg. If necessary, the dose can be increased to the maximum allowable - 10 mg 1 time per day. For vasospastic angina and exertional angina, Amlovas is recommended to be taken once a day at a dose of 5–10 mg, for the prevention of angina attacks - at a dose of 10 mg.
Patients with insufficient body weight, patients of short stature, the elderly and patients with functional disorders of the liver should use Amlovas at an initial dose of 2.5 mg as an antihypertensive agent, at a dose of 5 mg as an antianginal agent. When conducting combination therapy with ACE inhibitors, thiazide diuretics and beta-blockers, changes in amlodipine doses are not required.
Side effects
Side effects are classified as follows: often -> 1% and 0.1% and 0.01% and <0.1%; extremely rare - <0.01%, including isolated cases:
- central nervous system: often - drowsiness, headache, fatigue, mood changes, dizziness, convulsions; infrequently - insomnia, malaise, asthenia, nervousness, unusual dreams, tremor, hypesthesia, paresthesia, vertigo, depression, loss of consciousness; extremely rare - agitation, apathy, ataxia, amnesia;
- genitourinary system: infrequently - painful urge to urinate, nocturia, pollakiuria, sexual dysfunction (including decreased potency); extremely rare - polyuria, dysuria;
- digestive system: often - epigastric pain, nausea, vomiting; infrequently - dry mouth, constipation / diarrhea, flatulence, pancreatitis, elevated liver transaminases, and jaundice (associated with cholestasis); rarely - increased appetite, gingival hyperplasia; extremely rare - gastritis;
- cardiovascular system: often - flushing of the face, palpitations, shortness of breath, edema (including swelling of the feet and ankles), vasculitis, fainting; infrequently - a significant decrease in blood pressure; rarely - orthostatic hypotension, chest pain, rhythm disturbances (ventricular tachycardia, bradycardia, atrial flutter); extremely rare - development / worsening of heart failure, migraine, extrasystole;
- musculoskeletal system: infrequently - myalgia, arthralgia, arthrosis (with prolonged use); rarely - myasthenia gravis;
- allergic reactions: infrequently - rash (including urticaria, maculopapular and erythematous rash), itching; extremely rarely - erythema multiforme, angioedema;
- skin: rarely - dermatitis; extremely rare - discoloration of the skin, alopecia, xeroderma, purpura;
- others: infrequently - weight gain / loss, back pain, thirst, chills, increased sweating, visual impairment, ringing in the ears, eye pain, epistaxis, dyspnea, conjunctivitis, diplopia, polyuricemia, gynecomastia, hyperglycemia, leukopenia, thrombocytopenia; extremely rarely - a violation of taste, cold sticky sweat, parosmia, rhinitis, cough, xerophthalmia, violation of accommodation.
Overdose
Symptoms of an Amlovas overdose include: tachycardia, marked decrease in blood pressure, excessive peripheral vasodilation. In this condition, it is necessary to prescribe gastric lavage, the intake of activated carbon, to ensure the elevated position of the patient's limbs, to support the functions of the cardiovascular system, to monitor the performance of the heart and lungs, the volume of circulating blood and urine output. To restore vascular tone, vasoconstrictor drugs are used (if there are no contraindications to their appointment), in order to remove the effects of calcium channel blockade - calcium gluconate by intravenous infusion. Hemodialysis is ineffective.
special instructions
Against the background of CHF III and IV functional class according to the classification of the New York Heart Association (NYHA) during treatment with Amlovas, the risk of developing pulmonary edema is aggravated.
During therapy, it is necessary to control body weight and sodium intake, as well as adhere to an appropriate diet.
In order to prevent bleeding, soreness and gingival hyperplasia, it is required to be observed by a dentist.
Before the end of therapy, it is recommended to gradually reduce the dose of Amlovas (due to the possible worsening of the course of angina pectoris).
Amlovas has no effect on plasma levels of low density lipoproteins (LDL), total cholesterol, triglycerides, potassium, glucose, creatinine, uric acid and urea nitrogen.
With a hypertensive crisis, taking Amlovas is not recommended.
Influence on the ability to drive vehicles and complex mechanisms
It should be borne in mind that in some patients, dizziness and drowsiness may be noted mostly at the beginning of therapy. In the event of the development of such side effects, special care must be taken when driving a vehicle or working with complex and moving mechanisms.
Application during pregnancy and lactation
According to experimental studies, the embryotoxic and fetotoxic effects of amlodipine were not identified, but, despite this, drug treatment is allowed only if the expected benefit from its implementation for the mother significantly exceeds the possible threat to the fetus.
Women of childbearing age should use reliable methods of preventing pregnancy during all therapy.
It is known that dihydropyridine derivatives penetrate into breast milk, therefore, if the appointment of Amlovas is necessary during lactation, it is necessary to resolve the issue of stopping breastfeeding.
Pediatric use
For patients under 18 years of age, Amlovas is contraindicated due to the lack of data confirming the safety and effectiveness of its use in children and adolescents.
With impaired renal function
The presence of renal failure does not significantly affect the kinetics of amlodipine. Individual selection of doses for patients with impaired renal function is not required, however, a possible slight increase in T ½ should be taken into account and Amlovas should be used with caution.
For violations of liver function
In the presence of liver failure, it is assumed that the T ½ of the drug will be lengthened, and in the case of prolonged use, its increased accumulation in the body is noted (T ½ increases to 60 hours). Patients with impaired liver function are required to use Amlovas with caution.
Use in the elderly
In patients over 65 years of age, when compared with younger patients, a slowdown in the elimination of amlodipine was revealed (T ½ was 65 hours). This difference has no clinical significance, nevertheless, Amlovas should be used with caution in patients of this category. Elderly people do not need to change the dose of the drug. However, patients of this age group during the period of therapy need careful monitoring, especially when the dose is increased.
Drug interactions
- loop and thiazide diuretics, ACE inhibitors, beta-blockers, nitrates, verapamil: antianginal and hypotensive action is potentiated;
- inhibitors of microsomal oxidation: the plasma content of amlodipine increases, the risk of adverse reactions is aggravated;
- inducers of liver microsomal enzymes: the likelihood of developing undesirable effects decreases;
- non-steroidal anti-inflammatory drugs (especially indomethacin), estrogens, alpha-adrenostimulants, sympathomimetics: the hypotensive effect is weakened;
- digoxin, warfarin: no effect on the pharmacokinetic parameters of these substances is recorded;
- alpha 1 -adrenergic blockers, quinidine, amiodarone, antipsychotics (antipsychotics) and BMCC: possibly increased hypotensive action
- lithium preparations: manifestations of neurotoxicity of these drugs, such as diarrhea, nausea, vomiting, ataxia, tinnitus, tremors, may be aggravated;
- cimetidine: no effect on the pharmacokinetics of amlodipine is observed;
- drugs leading to prolongation of the QT interval (including procainamide and quinidine): the negative inotropic effect increases, and the threat of a significant prolongation of the QT interval may increase;
- calcium preparations: it is possible to reduce the effect of BMCC;
- grapefruit juice: a slight decrease in the plasma level of amlodipine in the blood is possible, which does not cause a significant change in the effect of the drug.
Analogs
Amlovas analogs are: Amlodipine, Amlodipine Sandoz, Amlodipine Zentiva, Amlong, Norvask, Amlorus, Amlodipine-Ajio, Amlodipine Cardio, Amlonorm, Amlodak, Cordi Cor, Vero-Amlodipine, Stamlo M, Kardilopin, Karmagipchek, and Korvadil.
Terms and conditions of storage
Store in a place protected from light and moisture, out of the reach of children, at a temperature not exceeding 30 ° C.
The shelf life is 3 years.
Terms of dispensing from pharmacies
Dispensed by prescription.
Reviews about Amlovas
According to the few reviews about Amlovas found on medical sites, the drug effectively reduces high blood pressure and is successfully used to prevent cardiovascular diseases. The drug, according to reviews, normalizes blood pressure indicators and supports the work of the heart.
However, some patients indicate a selective action of Amlovas, since during the period of therapy they could not achieve stabilization of blood pressure. Also, the disadvantages of the remedy include manifestations of side effects.
Price for Amlovas in pharmacies
The price of Amlovas, 5 mg tablets, can be 225-280 rubles. per package containing 30 pcs.
Amlovas: prices in online pharmacies
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Drug name Price Pharmacy |
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Amlovas 5 mg tablets 30 pcs. 219 r Buy |
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Amlovas tablets 5mg 30 pcs. 274 r Buy |
Anna Kozlova Medical journalist About the author
Education: Rostov State Medical University, 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!
