Instruction for Amlotop
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Amlotop is a drug that has antianginal and antihypertensive effects.
Release form and composition
The drug is available in tablets with a dosage of 5 and 10 mg.
The active ingredient is amlodipine.
Amlodipine is a dihydropyridine derivative belonging to the second generation slow calcium channel blockers. They are blocked by binding to the S6III and IV domains of the alpha 1-subunit of the L-type calcium channel. This ensures a decrease in the transmembrane transition of calcium ions into cells (to a greater extent into vascular smooth muscle cells than into cardiomyocytes).
The antianginal effect is due to the expansion of the coronary and peripheral arteries and arterioles. With angina pectoris, amlodipine reduces the severity of symptoms of myocardial ischemia. At the same time, due to the expansion of the peripheral arterioles, the total peripheral vascular resistance decreases (the afterload on the heart weakens), which is not accompanied by a reflex increase in the frequency of cardiovascular contractions. These effects help reduce energy consumption by reducing myocardial oxygen demand. Due to the expansion of the coronary arteries and arterioles in the unchanged and ischemic areas of the myocardium, the supply of oxygen to the myocardium increases in vasospastic angina pectoris, which prevents the development of coronary spasm (including those provoked by smoking).
In patients with angina pectoris, taking amlodipine 1 time per day increases the time interval until the onset of the first ischemic episode caused by physical activity, prevents the occurrence of angina pectoris and "ischemic" depression of the ST segment (by about 1 mm) against the background of physical efforts, contributes to more rare development of angina attacks and reduces the consumption of nitroglycerin.
The antihypertensive effect is caused by a direct vasodilating effect on vascular smooth muscle. A prolonged dose-dependent hypotensive effect is characteristic of amlodipine.
With arterial hypertension, taking amlodipine 1 time per day guarantees a clinically significant decrease in blood pressure within 24 hours (while the patient can be both in the supine position and in the standing position). Taking the drug does not lead to a sharp drop in blood pressure and a decrease in the left ventricular ejection fraction and does not affect myocardial contractility and conductivity. Amlodipine also reduces the degree of left ventricular myocardial hypertrophy.
In patients with ischemic heart disease (including coronary atherosclerosis, accompanied by both a lesion of one vessel and atherosclerosis of the carotid arteries and stenosis of 3 or more arteries), suffering from angina pectoris or with a history of myocardial infarction or percutaneous transluminal angioplasty (PTA coronary arteries) ), taking Amlotop prevents the appearance of thickening of the intima-media of the carotid arteries, reduces the frequency of interventions designed to restore coronary blood flow, reduces the number of hospitalizations associated with the progression of chronic heart failure and unstable angina, reduces the risk of death in the case of PTCA, myocardial infarction, coronary artery bypass grafting , stroke.
Amlodipine does not increase the likelihood of death or the development of complications that can lead to death of patients with chronic heart failure (CHF) (belonging to the III-IV functional class according to the NYHA classification) during treatment with angiotensin-converting enzyme inhibitors, diuretics and digoxin.
In patients with CHF (III-IV functional class according to the NYHA classification) of non-ischemic etiology, when taking Amlotop, there is a risk of developing pulmonary edema.
No adverse effects of amlodipine on plasma lipids and metabolism have been identified. The substance inhibits platelet aggregation, increases the glomerular filtration rate and is characterized by a slight natriuretic effect. In patients with diabetic nephropathy, the severity of microalbuminuria does not increase.
The drug takes effect 2–4 hours after administration, and the therapeutic effect lasts for 24 hours.
When taken orally, amlodipine is well absorbed from the gastrointestinal tract. Food intake does not affect the degree of its absorption. The maximum level of the substance in the blood serum is observed 6-12 hours after ingestion. The bioavailability of amlodipine is approximately 60-65%, and the average volume of distribution is 21 l / kg. The active component of Amlotop binds to plasma proteins by 90–97% and penetrates the blood-brain barrier.
Most of amlodipine is slowly metabolized in the liver (approximately 90%), forming inactive metabolites. Differs in low hepatic clearance (weak effect of "first pass" through the liver). The half-life on average reaches 35 hours (the range is possible from 35 to 50 hours), which corresponds to taking Amlotop 1 time per day. The total clearance is 500 ml / min. A stable equilibrium concentration of amlodipine in blood plasma is recorded after 7-8 days of treatment.
Excretion of amlodipine is carried out through the kidneys (unchanged - 10%, in the form of metabolites - 60%), through the intestine (in the form of metabolites - 20-25%), as well as with bile and breast milk. The drug is not excreted from the body through hemodialysis.
In patients with severe CHF, liver failure and elderly patients, the elimination half-life usually increases to 60-65 hours. With renal dysfunction, this indicator does not change.
Indications for use
In accordance with the instructions, the drug is prescribed for arterial hypertension, vasospastic angina pectoris and stable exertional angina pectoris. The drug can be used in combination with other drugs of similar action or as monotherapy.
The use of Amlotop allows to reduce the frequency of angina attacks and the amount of nitroglycerin taken. There is also a dose-dependent long-term hypotensive effect of the drug due to relaxation of vascular smooth muscles. With high blood pressure, the effect of a single dose of the drug is maintained throughout the day.
The use of Amlotop has the following contraindications:
Severe arterial hypotension;
Aortic stenosis (clinically significant);
Pregnancy in any trimester;
Age under 18;
Hypersensitivity to drug components and other dihydropyridine derivatives.
Amlotop should be taken with caution in the elderly, as well as in: chronic heart failure, severe bradycardia, tachycardia, liver dysfunctions, mitral and aortic stenosis, hypertrophic obstructive cardiomyopathy, acute myocardial infarction.
Instructions for use: method and dosage
Amlotop is taken regardless of food intake, 1 time per day with water.
In the treatment of angina pectoris and arterial hypertension, an initial daily dose of 5 mg is prescribed. The dose is adjusted depending on the individual response of the patient and can be increased up to 10 mg. Increasing the dose is allowed after 7-14 days from the moment you start taking the drug.
For patients with low body weight, short stature, the elderly and patients with impaired liver function, Amlotop, as an antihypertensive agent, is prescribed in a reduced initial dose of 2.5 mg of the active substance.
When Amlotop is combined with other drugs, an initial dose of 2.5 mg of the active ingredient is prescribed.
The use of Amlotop can cause the following side effects:
From the side of the cardiovascular system: swelling of the feet and ankles, excessive decrease in blood pressure, increased heart rate, vasculitis, heart failure, bradycardia, atrial fibrillation, ventricular tachycardia, heart attack;
From the hematopoietic system: leukopenia, thrombocytopenia;
From the side of the central and peripheral nervous system: migraine, chest pain, dizziness, drowsiness, malaise, asthenia, fainting, fatigue, paresthesia, tremor, lability, peripheral neuropathy, anxiety, depression;
From the digestive system: nausea, stool disorders, abdominal pain, diarrhea, anorexia, dry mucous membranes, thirst, gastritis, jaundice, pancreatitis;
From the respiratory system: rhinitis, shortness of breath;
From the senses: diplopia, eye pain, conjunctivitis.
Allergic reactions: itching, angioedema, urticaria, dermatitis;
From the musculoskeletal system: myalgia, muscle cramps;
A symptom of an overdose of Amlotop is a pronounced decrease in blood pressure, sometimes accompanied by excessive peripheral vasodilation and reflex tachycardia. At the same time, the risk of developing a persistent and pronounced decrease in blood pressure increases, which does not exclude the likelihood of shock and death.
As a therapeutic measure, it is recommended to take activated charcoal (especially effective in the first 2 hours after an overdose), gastric lavage (in some cases), control of BCC and urine output, monitoring of parameters responsible for lung and heart function, normalization of the function of the cardiovascular system. The patient needs to remain in a horizontal position, giving the lower limbs an elevated position.
In the absence of contraindications, intravenous administration of calcium gluconate, vasoconstrictor drugs and other means of symptomatic therapy are also prescribed. Hemodialysis is considered ineffective.
The drug should be withdrawn gradually.
During therapy, the patient should control his weight, as well as undergo regular examinations at the dentist to prevent gum hyperplasia, soreness and bleeding.
Amlotop affects the speed of reactions, which should be taken into account by patients who work with complex mechanisms and control vehicles.
Application during pregnancy and lactation
Amlotop is contraindicated during pregnancy and breastfeeding, so women of reproductive age should use reliable contraceptives during the course of treatment.
With impaired renal function
In patients with renal insufficiency, no changes in the kinetics of amlodipine are observed.
For violations of liver function
The drug is prescribed with caution for liver dysfunctions. In patients with hepatic insufficiency, the elimination half-life is presumably prolonged (up to 60 hours) and, with prolonged therapy, the accumulation of the drug in the body increases.
Use in the elderly
The drug is used with caution in elderly patients. In this category of patients, the dosage regimen remains the same as in patients from other age groups. When the dose is increased, careful monitoring of the patient's condition is recommended.
Inhibitors of microsomal oxidation increase the level of the active component of Amlotop in blood plasma (increasing the risk of side reactions), and inducers of microsomal liver enzymes reduce its concentration.
Amlodipine, unlike other slow calcium channel blockers, is not characterized by clinically significant interactions with NSAIDs, especially with indomethacin. Sometimes there is an increase in the hypotensive and antianginal action of the drug when taken together with nitrates, "loop" and thiazide diuretics, ACE inhibitors, beta-blockers, verapamil, alpha1-blockers.
When Amlotop is combined with isoflurane and neuroleptics, the hypotensive effect may be enhanced.
When taking some blockers of slow calcium channels, there is sometimes a pronounced negative inotropic effect of antiarrhythmic drugs that cause an extension of the QT interval (quinidine, amiodarone), but in the case of amlodipine, this effect is rare. Calcium supplements can reduce the effectiveness of Amlotop.
When blockers of slow calcium channels are combined with lithium preparations, it is possible to increase the manifestations of neurotoxicity of the latter, expressed in tinnitus, nausea, vomiting, diarrhea, tremor, ataxia, but in the case of Amlotop this fact has not been experimentally confirmed.
Cimetidine and a single dose of antacids, which include magnesium or aluminum, do not alter the pharmacokinetics of amlodipine. The active component of Amlotop does not significantly affect the pharmacokinetics of cyclosporine.
A single dose of sildenafil at a dose of 100 mg in patients with essential arterial hypertension, as well as the simultaneous administration of 10 mg of amlodipine and 240 mg of grapefruit juice, do not have a clinically significant effect on the pharmacokinetic parameters of amlodipine. Repeated simultaneous administration of atorvastatin at a dose of 80 mg and amlodipine at a dose of 10 mg does not affect the pharmacokinetics of atorvastatin.
The combination of amlodipine and digoxin does not alter serum digoxin levels and clearance. The use of amlodipine does not affect the prothrombin time parameter associated with warfarin. Single and repeated administration of Amlotop at a dose of 10 mg does not affect the pharmacokinetics of ethanol. Antiviral drugs (ritonavir) increase plasma concentrations of amlodipine.
Storage conditions and periods
Amlotop should be stored at an air temperature not exceeding 25 ° C, in a dry place protected from sunlight. Keep out of the reach of children.
The shelf life of the drug is 3 years from the date of manufacture.
Usually doctors prescribe the drug for angina pectoris and hypertension. According to reviews, Amlotop is considered a very effective remedy. Consumers note its low cost and high availability in pharmacy chains. Many patients claim that with only a daily dose of 5 mg Amlotop stabilizes blood pressure and eliminates angina attacks. There are also negative opinions associated with the side effects of the drug: drowsiness, pain when urinating, skin rashes, itching, headache, swelling. Cardiologists say that puffiness is quite acceptable side effect for Amlotop, if it is not too pronounced and is not accompanied by a significant deterioration in well-being.
Terms of sell
You can buy Amlotop without a prescription.