Amlotop tab 10mg 30 pc

Description

Composition
Active substance:
Amlodipine besylate based on amlodipine 10 mg.
Description:
Tablets white or almost white ploskotsilindricheskoy form chamfered and Valium.
Product form:
Tablets of 10 mg – 30
Contraindications
Hypersensitivity to amlodipine and other dihydropyridine derivatives, as well as to other components within the preparation. Severe hypotension (blood pressure less cistolicheskoe 90 mm Hg). Shock (including cardiogenic shock). Obstruction of the left ventricular outflow tract (eg, severe aortic stenosis). Hemodynamically unstable heart failure after myocardial infarction. Age 18 years (effectiveness and safety have been studied). Lactose Intolerance, Lactase deficiency or glucose-galactose malabsorption (formulation contains lactose). During breastfeeding.
Dosage
10 mg
Indications
Arterial hypertension (monotherapy or in combination with other antihypertensive agents). Stable angina, and vasospastic angina (Prinzmetal’s angina) (monotherapy or in combination with other antianginal drugs).
Interaction with other drugs
Amlodipine can be safely used for the therapy of hypertension with thiazide diuretics, alpha blockers, beta-blockers or ACE inhibitors. In patients with stable angina pectoris, amlodipine can be combined with other antianginal agents, such as nitrates, prolonged or short-acting beta-blockers. Unlike other BCCI amlodipine clinically significant interaction was detected in the combined use with nonsteroidal anti-inflammatory drugs (NSAIDs), including indomethacin. May increase antianginal and hypotensive action BCCI when combined with thiazide and “loop” diuretics, APF inhibitors, beta-blockers and nitrates, as well as strengthening their hypotensive effect when combined with alpha 1-blockers, neuroleptics. Although the study of amlodipine negative inotropic action is usually not observed, nevertheless, some BCCI may increase the severity of the negative inotropic effects of antiarrhythmic agents causing the lengthening of the interval QT (e.g., amiodarone and quinidine). Amlodipine may also safely be used in conjunction with antibiotics and hypoglycemic agents for oral administration. A single dose of 100 mg sildenafil in patients with essential hypertension have not effect on the pharmacokinetic parameters of amlodipine. Repeated application of amlodipine 10 mg and atorvastatin 80 mg is not accompanied by a significant change in the pharmacokinetics of atorvastatin. Simvastatin: simultaneous multiple use of amlodipine 10 mg of simvastatin and 80 mg resulting in increased exposure of simvastatin by 77%. In such cases it is necessary to limit the dose to 20 mg of simvastatin. Ethanol (drinks containing alcohol): amlodipine with single and repeated administration in a dose of 10 mg did not affect the pharmacokinetics of ethanol. Antiviral agents (ritonavir) increase the plasma concentrations of BCCI, including amlodipine. Neuroleptics and isoflurane: increased hypotensive effect of dihydropyridine derivatives. Calcium can reduce the effect of BCCI. When the joint application BCCI with lithium drugs (for amlodipine no data) may increase their neurotoxicity symptoms (nausea, vomiting, diarrhea, ataxia, tremor, tinnitus). Research simultaneous use of amlodipine and ciclosporin in healthy volunteers and patients of all groups, except in patients after kidney transplantation, were not carried out. Various studies amlodipine interaction with cyclosporine in patients after kidney transplantation showed that the use of this combination may not lead to any effect or increase the minimum concentration of cyclosporine to varying degrees up to 40%. It should be appreciated that data and control the concentration of cyclosporin in this patient group, while the application of cyclosporine and amlodipine. It has no effect on serum digoxin concentration in the blood and its renal clearance. It does not significantly affect the action of warfarin (prothrombin time). Cimetidine does not affect the pharmacokinetics of amlodipine. In in vitro studies, amlodipine has no effect on protein binding of digoxin plasma blood, phenytoin, warfarin and indomethacin. Grapefruit juice: simultaneous single dose of 240 mg of grapefruit juice and 10 mg amlodipine inwardly not accompanied by a significant change in the pharmacokinetics of amlodipine. However, it is not recommended to use grapefruit juice and amlodipine at the same time, since the genetic polymorphism of CYP3A4 may increase the bioavailability of amlodipine and, consequently, increased hypotensive effect. Aluminum- or magnesium-containing antacids: their single dose has no significant effect on the pharmacokinetics of amlodipine. Inhibitors of the isoenzyme CYP3A4: while applying diltiazem dose of 180 mg, and amlodipine 5 mg in patients 69 to 87 years with arterial hypertension marked increase in systemic exposure to 57% amlodipine. The simultaneous use of amlodipine and erythromycin in healthy volunteers (18 to 43 years) does not lead to significant changes amlodipine exposure (increase in area under the curve “concentration-time» (AUC) 22%). Despite the fact that the clinical significance of these effects is not completely clear, they may be more pronounced in older patients. Potent inhibitors isoenzyme CYP3A4 (e.g., ketoconazole, itraconazole) may lead to an increase amlodipine plasma concentration to a greater extent than diltiazem. Should be used with caution and amlodipine inhibitors isoenzyme CYP3A4. Clarithromycin: an inhibitor of CYP3A4 isoenzyme. Patients taking both clarithromycin and amlodipine increased risk of lowering blood pressure. Patients receiving this combination is recommended to be kept under close medical supervision. Inducers of CYP3A4: data on the effect of inducers of CYP3A4 on the pharmacokinetics of amlodipine is not. One should carefully monitor blood pressure while the use of amlodipine and inductors isoenzyme CYP3A4. Tacrolimus: while the use of amlodipine is a risk of increasing the concentration of tacrolimus in the blood plasma. To avoid the toxicity of tacrolimus while the use of amlodipine, should control the concentration of tacrolimus in the blood plasma of patients and to adjust the dose of tacrolimus, if necessary. mechanistic target of rapamycin inhibitors in mammals (tTOR) Inhibitors of mTOR, such as sirolimus, everolimus and temsirolimus are substrates isoenzyme CYP3A. Amlodipine is a weak inhibitor of isoenzyme CYP3A. While the use of inhibitors of mTOR amlodipine can increase their exposure.
Overdose
Symptoms: marked reduction of blood pressure with possible development of reflex tachycardia and excessive peripheral vasodilation (the risk of a pronounced and persistent reduction in blood pressure, including the development of shock and death).
Treatment: administration of activated carbon (especially in the first 2 hours after the overdose), gastric lavage (in some cases), the maintenance function of the cardiovascular system, control parameters of the heart and lung function, control of blood volume and diuresis. The patient should take a horizontal position to the elevated position of the lower extremities. In the absence of contraindications symptomatic therapy: vasoconstrictor drugs, intravenous administration of calcium gluconate. Hemodialysis is ineffective.
pharmachologic effect
Pharmacological group:
Blocker “slow” calcium channels.
Pharmacodynamics:
Dihydropyridine derivative – blocker “slow” calcium channel II generation, has antianginal and antihypertensive action. Communicating with the dihydropyridine receptor, blocks calcium channels, reduces the transmembrane passage of calcium ions into the cell (mainly in vascular smooth muscle cells than cardiac myocytes). Antianginal effect due to the expansion of the coronary and peripheral arteries and arterioles: angina reduces the severity of myocardial ischemia; expanding peripheral arterioles, reducing the total peripheral vascular resistance, reduces preload on the heart, reducing myocardial oxygen demand. Expanding the major coronary arteries and arterioles in the unaltered areas and ishemizirovanpyh myocardium, increases the oxygen supply to the myocardium (especially with vasospastic angina pectoris); It prevents the development of constriction of the coronary arteries (in t. h. caused by smoking). In patients with angina single daily dose increases the run-time physical activity slows the development of angina and ‘ischemic’ ST segment depression, reduces the frequency of angina attacks and nitroglycerin consumption. It has a long dose-dependent hypotensive effect. Hypotensive effect caused by the direct vasodilating effect on vascular smooth muscle. In arterial gimertenzii single dose provides a clinically significant decrease in blood pressure (BP) over 24 hours (at the position of the patient “lying” and “standing”). Does not cause a sharp decrease in blood pressure, reduction of exercise tolerance, left ventricular ejection fraction. Reduces the degree of left ventricular hypertrophy, antiatherosclerotic and cardioprotective effect in ischemic heart disease (CHD). No effect on the myocardial contractility and conductivity, does not cause reflex increase of heart rate (HR), inhibits platelet aggregation and increases glomerular filtration rate, has a weak natriuretic action. In diabetic nephropathy does not increase the severity of microalbuminuria. It does not have adverse effects on lipid metabolism and blood plasma. Time of onset of effect – 2-4 hours, duration of effect of 24 hours.
Pharmacokinetics:
Suction.
After oral administration of amlodipine is well absorbed from the gastrointestinal tract. Eating does not affect the absorption of amlodipine. The maximum serum concentration achieved after 6-12 hours after administration. Bioavailability was 60-65%. The average distribution volume – 21 liters / kg of body weight. Relationship to plasma proteins – 90-97%. The drug penetrates the blood-brain barrier.
Metabolism and excretion.
Amlodipine undergoes slow but significant metabolism (90%) in the liver into inactive metabolites has low hepatic clearance (effect of “first pass” through the liver). The half-life averages 35 hours (ranging from 35 to 50 hours), which corresponds to the destination of the drug once a day. Total clearance – 500 ml / min. A stable equilibrium plasma concentration achieved after 7-8 days of therapy. Excreted by the kidneys (10% in unaltered, 60% as a metabolite) through the bile and gut – 20-25% in the form of metabolites, and in breast milk. When hemodialysis is not removed.
In elderly patients, patients with liver failure and severe heart failure half-life is increased to 60-65 hours; with impaired renal function – no change.
Pregnancy and breast-feeding
Safety of application of amlodipine during pregnancy has not been established. Use of the drug during pregnancy is possible with caution, only when benefit to the mother outweighs the risk to the fetus. Amlodipine is released in a woman’s breast milk. The average ratio of “milk / plasma” for amlodipine concentration was 0.85 in 31 lactating women who suffer arterial hypertension caused by pregnancy, and was prepared in primary amlodipine 5 mg per day. Dosage was adjusted, if necessary, the average daily dose of amlodipine was 6 mg (98.7 mg / kg body weight). The estimated daily dose of amlodipine obtained infant breast milk is 4.17 mg / kg / day. Use of the drug during breast feeding is contraindicated. If necessary, use during lactation should stop breastfeeding. In studies on rats observed undesirable effect of amlodipine on fertility in males. Reversible biochemical changes in the sperm heads were seen in some patients treated with BCCI. Clinical data on the potential impact of amlodipine on fertility are not enough.
Conditions of supply of pharmacies
On prescription.
side effects
The frequency listed below possible side effects listed in accordance with the World Health Organization classification (WHO): very often – more than 1/10; often – from more than 1/100 to 1/10 less; infrequently – from more to less than 1/100 to 1/1000; rarely – from more to less than 1/1000 1/10000; very rare – from less than 1/10000, including isolated reports; frequency not known – can not be determined on the basis of available data.
Blood disorders and lymphatic system: very rarely – leukopenia, thrombocytopenia purpura, thrombocytopenia.
Disorders of immune system: very rarely – allergic reactions.
Violations by the Metabolism and nutrition: very rarely – hyperglycemia.
Mental disorders: rarely – insomnia, mood changes (including anxiety), depression; rarely – confusion.
Disorders of the nervous system: often – drowsiness, dizziness, headache (especially at the beginning of treatment); infrequent – tremor, dysgeusia, syncope, hypoesthesia, paresthesia; very rarely – hypertonicity, peripheral neuropathy; the frequency is unknown – extrapyramidal disorders.
Violations by the organ of vision: often – visual disturbances (including diplopia).
Violations by the organ of hearing and labyrinth disorders: rarely – ringing in the ears.
Violations of the heart: Often – palpitations; infrequently – arrhythmia (including bradycardia, ventricular tachycardia and atrial fibrillation); very rare – myocardial infarction.
Violations by vessels: often – flushing; rarely – hypotension; very rarely – vasculitis.
Violations of the respiratory system, thorax and mediastinum: often – shortness of breath; infrequently – cough, rhinitis.
Violations of the digestive system: often – abdominal pain, nausea, indigestion, change in bowel movement mode (including diarrhea and constipation); infrequently – vomiting, dryness of the oral mucosa; very rarely – pancreatitis, gastritis, hypertrophic gingivitis.
Disorders of the liver and biliary tract: very rarely – hepatitis, jaundice, elevated liver enzymes (mainly caused by cholestasis).
Violations of the skin and subcutaneous tissue disorders: rare – alopecia, purpura, skin discoloration, excessive sweating, itching, skin rash, rash, urticaria; very rarely – angioneurotic edema, erythema multiforme, exfoliative dermatitis, Stevens-Johnson syndrome, photosensitivity.
Violations by musculoskeletal and connective tissue disorders: often – swelling of the ankles, muscle cramps; Infrequent – arthralgia, myalgia, back pain.
Violations of the kidneys and urinary tract: infrequently – impaired urination, nocturia, increased frequency of urination.
Violations by the genitals and breast: rarely – impotence, gynecomastia.
General disorders and at the injection site: very often – peripheral edema; often – fatigue, asthenia; infrequently – chest pain, pain, malaise.
Laboratory and instrumental data: rarely – weight gain, weight loss.
special instructions
The efficacy and safety of amlodipine during hypertensive crisis has not been established. Patients with heart failure should be used with caution amlodipine. In the long, placebo-controlled study in patients with severe heart failure (III or IV functional class NYHA classification) incidence of pulmonary edema was higher in the amlodipine group than in the placebo group. Calcium channel blockers, including amlodipine, should be used with caution in patients with congestive heart failure, as they may increase the risk of cardiovascular events and deaths. In patients with impaired liver function T1 / 2 and AUC parameters of amlodipine may be increased, according to the drug dosage recommendations have not been established. Therefore amlodipine application should begin with the lower end of the range of therapeutic doses and caution at the beginning of treatment and at higher doses. Patients with severe hepatic impairment may have to be gradual dose selection and careful monitoring of the patient. Elderly patients may increase the T1 / 2 and to decrease the clearance of the drug. No dose adjustment is required, but requires careful monitoring of patients. The period of treatment is necessary to control body weight and sodium intake. It is necessary to oral hygiene and regular visits to the dentist (to prevent pain, bleeding and gingival hyperplasia).
In some patients, especially at the beginning of the treatment or when changing the dosing regimen, due to the potential expressed by BP reduction might occur drowsiness, dizziness and other side effects. If this happens, the patient should be careful when driving and working with complex mechanisms.
Storage conditions
In the dark place at a temperature not higher than 25 ° C. Keep out of the reach of children.
Dosing and Administration
Inside, once a day, regardless of food intake, drinking plenty of water (100 mL). The initial dose of hypertension and angina is usually 5 mg. Depending on the individual patient response, dosage may be increased to a maximum of 10 mg per day. Increasing the dose is recommended 7-14 days after initiation of therapy (more rapid dose escalation requires close monitoring of the patient). Patients with a small body weight, short, elderly patients, patients with impaired liver function as an antihypertensive amlodipine is administered in an initial dose of 2.5 mg (1.2 mg tablet 5), as anti-anginal agents – 5 mg. The initial dose of 2.5 mg can also be used when adding amlodipine to other antihypertensive therapy drugs. In patients with renal impairment dose adjustment is required.
Information
Appearance may differ from that depicted in the picture. There are contraindications. You need to read the manual or consult with a specialist