Amlodipin-Teva
Amlodipine can be safely used for the treatment of arterial hypertension together with thiazide diuretics, alpha-blockers, beta-blockers
or
ACE inhibitors.
In patients with stable angina, amlodipine can be combined with other antianginal agents, for example, long- or short-acting nitrates, beta-blockers.
Unlike other BMCCs, no clinically significant interaction with amlodipine (III generation BMCCs) was found when used simultaneously with nonsteroidal anti-inflammatory drugs (NSAIDs)
, including with
indomethacin
.
It is possible to enhance the antianginal and hypotensive effect of BMCC when used simultaneously with thiazide and loop diuretics, ACE inhibitors, beta-blockers and nitrates, as well as enhance their hypotensive effect when used simultaneously with alpha1-blockers and antipsychotics. Although negative inotropic effects have generally not been observed in amlodipine studies, some CBMCs may enhance the negative inotropic effects of antiarrhythmic drugs that cause QT prolongation (eg, amiodarone and quinidine).
Amlodipine can also be safely used concomitantly with antibiotics
and
hypoglycemic agents for oral administration.
Sildenafil:
A single dose of 100 mg of sildenafil in patients with essential hypertension does not affect the pharmacokinetic parameters of amlodipine.
Atorvastatin:
simultaneous repeated use of amlodipine at a dose of 10 mg and atorvastatin at a dose of 80 mg is not accompanied by significant changes in the pharmacokinetics of atorvastatin.
Simvastatin:
simultaneous repeated use of amlodipine at a dose of 10 mg and simvastatin at a dose of 80 mg leads to an increase in simvastatin exposure by 77%. In such cases, the dose of simvastatin should be limited to 20 mg.
Ethanol (beverages containing alcohol):
amlodipine with single and repeated use at a dose of 10 mg does not affect the pharmacokinetics of ethanol.
Antivirals (ritonavir):
increases plasma concentrations of BMCC, including amlodipine.
Neuroleptics and isoflurane:
enhancing the hypotensive effect of dihydropyridine derivatives.
Calcium preparations
may reduce the effect of BMCC.
With simultaneous use of BMCC with lithium preparations
(no data available for amlodipine) may increase the manifestation of neurotoxicity (nausea, vomiting, diarrhea, ataxia, tremor, tinnitus).
Studies of concomitant use of amlodipine and cyclosporine
in healthy volunteers and all groups of patients, with the exception of patients after kidney transplantation, were not carried out. Various studies of the interaction of amlodipine with cyclosporine in patients after kidney transplantation show 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%. These data should be taken into account and cyclosporine concentrations should be monitored in this group of patients when cyclosporine and amlodipine are co-administered.
Does not affect serum digoxin
and its renal clearance.
Does not significantly affect the action of warfarin
(prothrombin time).
Cimetidine
does not affect the pharmacokinetics of amlodipine.
In in
vitro
, amlodipine does not affect the plasma protein binding of
digoxin, phenytoin, warfarin and indomethacin.
Grapefruit juice:
A simultaneous single dose of 240 mg of grapefruit juice and 10 mg of amlodipine orally is 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 genetic polymorphism of the CYP3A4 isoenzyme may increase the bioavailability of amlodipine and. as a result, an increase in the hypotensive effect.
Aluminum-
or magnesium-containing antacids:
their single dose does not have a significant effect on the pharmacokinetics of amlodipine.
Inhibitors of the CYP3A4 isoenzyme
: with simultaneous
of age with arterial hypertension, an increase in systemic exposure of amlodipine by 57% was observed. Concomitant use of amlodipine and erythromycin in healthy volunteers (18 to 43 years of age) does not lead to significant changes in amlodipine exposure (increase in area under the concentration-time curve (AUC) by 22%). Although the clinical significance of these effects is unclear, they may be more pronounced in older patients.
Potent inhibitors of the CYP3A4 isoenzyme (for example, ketoconazole, itraconazole) may increase the plasma concentration of amlodipine to a greater extent than diltiazem. Amlodipine and inhibitors of the CYP3A4 isoenzyme should be used with caution.
Clarithromycin:
CYP3A4 isoenzyme inhibitor. Patients taking clarithromycin and amlodipine at the same time have an increased risk of low blood pressure. Patients taking this combination are advised to be under close medical supervision.
Inducers of the CYP3A4 isoenzyme
: when used
CYP3A4 inducers, the plasma concentration of amlodipine may vary. Therefore, it is necessary to monitor blood pressure and adjust the dose both during and after therapy, especially with strong CYP3A4 inducers (eg, rifampicin, St. John's wort).
Tacrolimus:
When used simultaneously with amlodipine, there is a risk of increasing the concentration of tacrolimus in the blood plasma. To avoid toxicity of tacrolimus when used concomitantly with amlodipine, the concentration of tacrolimus in the blood plasma of patients should be monitored and the dose of tacrolimus should be adjusted if necessary.
Mammalian target of rapamycin
( mTOR ) inhibitors:
mTOR inhibitors such as sirolimus, temsirolimus, and everolimus are substrates of the CYP3A isoenzyme. Amlodipine is a weak inhibitor of the CYP3A isoenzyme. When used concomitantly with mTOR inhibitors, amlodipine may increase its exposure.
Dantrolene (with intravenous administration):
In animal experiments, cases of fatal ventricular fibrillation and cardiovascular failure associated with hyperkalemia were observed after the administration of verapamil and dantrolene (intravenously). Given the risk of developing hyperkalemia, the simultaneous use of BMCC (including amlodipine) and dantrolene should be avoided in patients with malignant hyperthermia.
Amlodipine-Teva 10 mg tbl N30
Amlodipine - Teva - instructions for use
Trade name of the drug: Amlodipine -Teva
International nonproprietary name:
amlodipine
Dosage form:
tablets
Composition
1 tablet contains: Active substance: Amlodipine besilate (amlodipine) - 6.944 mg (5.00 mg).
Amlodipine besylate (amlodipine) - 13.888 mg (10.00 mg). Excipients: Microcrystalline cellulose, calcium hydrogen phosphate (anhydrous), sodium carboxymethyl starch (type A), magnesium stearate. Description
Tablets 5 mg.
Round, biconvex, white tablets. On one side there is an engraving AB 5. The other side is smooth. Tablets 10 mg. Round, biconvex, white tablets. On one side there is a dividing line and engraving AB 10. The other side is smooth. Pharmacotherapeutic group:
slow calcium channel blocker (SCBC).
CodeATH: C08CA01
Pharmacological properties
Pharmacodynamics
A slow calcium channel blocker, a dihydropyridine derivative, is a second generation slow calcium channel blocker (SCBC), which has an antianginal and hypotensive effect.
Blocks calcium channels, reduces the transmembrane transition of calcium ions into the cell (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: in case of angina pectoris, it reduces the severity of myocardial ischemia; by expanding peripheral arterioles, it reduces total peripheral vascular resistance (TPVR), reduces afterload on the heart, and reduces myocardial oxygen demand. By expanding the coronary arteries and arterioles in unchanged and ischemic areas of the myocardium, it increases the supply of oxygen to the myocardium (especially with vasospastic angina); prevents spasm of the coronary arteries (including those caused by smoking). In patients with stable angina, a single daily dose increases exercise tolerance, increases the time before the onset of angina and ischemic depression of the ST segment, reduces the frequency of angina attacks and the consumption of nitroglycerin and other nitrates. It has a long-term dose-dependent hypotensive effect. The hypotensive effect is due to a direct vasodilating effect on vascular smooth muscle. For arterial hypertension, a single dose provides a clinically significant reduction in blood pressure (BP) over 24 hours (in the patient’s “lying” and “standing” position). Orthostatic hypotension when prescribing amlodipine is quite rare. Does not cause a decrease in left ventricular ejection fraction. Reduces the degree of left ventricular myocardial hypertrophy. It has no effect on myocardial contractility and conductivity, does not cause a reflex increase in heart rate (HR), inhibits platelet aggregation, increases the glomerular filtration rate, and has a weak natriuretic effect. In diabetic nephropathy, it does not increase the severity of microalbuminuria. It does not have any adverse effect on metabolism and plasma lipid concentrations and can be used in the treatment of patients with bronchial asthma, diabetes mellitus and gout. A significant decrease in blood pressure is observed after 6-10 hours, the duration of the effect is 24 hours. In patients with diseases of the cardiovascular system, including coronary atherosclerosis with damage to one vessel and up to stenosis of 3 or more arteries, atherosclerosis of the carotid arteries who have had myocardial infarction, percutaneous transluminal angioplasty (PTPA) of the coronary arteries or patients with angina pectoris, the use of amlodipine is prevented development of thickening of the intima-media of the carotid arteries, reduces mortality from myocardial infarction, stroke, PTAP, coronary artery bypass grafting; leads to a decrease in the incidence of unstable angina and progression of chronic heart failure (CHF); reduces the frequency of interventions aimed at restoring coronary blood flow. Does not increase the risk of death or the development of complications and deaths in patients with CHF (III-IV functional class according to the NYHA classification) during therapy with digoxin, diuretics and angiotensin-converting enzyme (ACE) inhibitors. In patients with CHF (III-IV functional class according to the NYHA classification) of non-ischemic etiology, when using amlodipine, there is a risk of pulmonary edema. Pharmacokinetics:
After oral administration, amlodipine is slowly absorbed from the gastrointestinal tract (GIT).
The average absolute bioavailability is 64%, the maximum concentration (Cmax) in the blood serum is observed after 6-9 hours. Steady-state concentrations (Css) are achieved after 7-8 days of therapy. Food intake does not affect the absorption of amlodipine. The mean volume of distribution is 21 L/kg body weight, indicating that most of the drug is in the tissues and a smaller part is in the blood. Most of the drug in the blood (95%) binds to blood plasma proteins. Amlodipine undergoes slow but active metabolism in the liver with no significant first-pass effect. Metabolites do not have significant pharmacological activity. After a single dose, the half-life (T1/2) varies from 35 to 50 hours; with repeated use, T1/2 is approximately 45 hours. About 60% of the dose taken orally is excreted by the kidneys mainly in the form of metabolites, 10% unchanged, and 20-25% through the intestines with bile. The total clearance of amlodipine is 0.116 ml/s/kg (7 ml/min./kg, 0.42 l/h/kg). In elderly patients (over 65 years of age), the elimination of amlodipine is slower (T1/2 is 65 hours) compared to young patients, but this difference is not clinically significant. Prolongation of T1/2 in patients with liver failure suggests that with long-term use the accumulation of the drug in the body will be higher (T1/2 - up to 60 hours). Renal failure does not significantly affect the kinetics of amlodipine. In patients with impaired renal function, changes in plasma concentrations of amlodipine do not correlate with the degree of renal failure. A slight increase in T1/2 is possible. Amlodipine penetrates the blood-brain barrier. It is not removed by hemodialysis. Indications for use
: arterial hypertension;
stable angina pectoris and vasospastic angina. Contraindications:
hypersensitivity to amlodipine, other dihydropyridine derivatives or other components of the drug;
severe arterial hypotension (systolic blood pressure less than 90 mm Hg); cardiogenic shock; acute myocardial infarction (within the first 28 days); unstable angina (with the exception of Prinzmetal angina); obstruction of the outflow tract of the left ventricle; clinically significant aortic stenosis; age under 18 years (efficacy and safety have not been established). With caution: liver dysfunction, sick sinus syndrome (severe bradycardia, tachycardia), CHF of non-ischemic etiology of functional class III-IV according to the NYHA classification, arterial hypotension, aortic stenosis, mitral stenosis, acute myocardial infarction (after the first 28 days), elderly age, renal dysfunction. Use during pregnancy and lactation
In experimental studies, the fetotoxic and embryotoxic effects of the drug have not been established, but use during pregnancy is possible only when the benefit to the mother outweighs the potential risk to the fetus.
There is no data indicating the excretion of amlodipine in breast milk. However, it is known that other BMCCs, dihydropyridine derivatives, are excreted in breast milk. In this connection, if it is necessary to prescribe the drug Amlodipine-Teva during lactation, the issue of stopping breastfeeding should be resolved. Method of administration and dosage
: Orally, once a day, with the required amount of water (100 ml).
For arterial hypertension and angina pectoris, the initial dose is 5 mg 1 time per day. If there is no therapeutic effect within 2-4 weeks, the dose of the drug can be increased to 10 mg/day. once. In elderly patients, no dose adjustment is required. In patients with impaired liver function Despite the fact that T1/2 of amlodipine, like all BMCCs, increases in patients with impaired liver function, dose adjustment is usually not required (see section Special instructions). In patients with renal failure, it is recommended to use Amlodipine-Teva in normal doses (see section Special instructions). Side effects
The frequency of adverse reactions listed below was determined according to the following (World Health Organization classification): very often - at least 10%;
often - at least 1%, but less than 10%; infrequently - not less than 0.1%, but less than 1%; rarely - not less than 0.01%, but less than 0.1%; very rarely - less than 0.01%, including individual messages. From the central nervous system: often - headache (especially at the beginning of treatment), dizziness, increased fatigue, drowsiness; uncommon - general malaise, hypoesthesia, asthenia, paresthesia, peripheral neuropathy, tremor, insomnia, emotional lability, unusual dreams, nervousness. increased excitability, depression, anxiety, increased sweating; rarely - convulsions, apathy, agitation; very rarely - ataxia, amnesia, migraine. From the digestive system: often - nausea, abdominal pain; uncommon - vomiting, change in bowel habits (including constipation, flatulence), dyspepsia, diarrhea, anorexia, dry oral mucosa, thirst; rarely - gum hyperplasia, increased appetite; very rarely - pancreatitis, gastritis, jaundice (usually cholestatic), hyperbilirubinemia, increased activity of liver transaminases, hepatitis. From the cardiovascular system: often - peripheral edema (ankles and feet), palpitations, flushing of the facial skin; uncommon - excessive decrease in blood pressure, orthostatic hypotension, vasculitis; rarely - development or worsening of CHF; very rarely - fainting, shortness of breath, cardiac arrhythmias (including bradycardia, ventricular tachycardia and atrial fibrillation), myocardial infarction, chest pain, pulmonary edema. From the hematopoietic and lymphatic systems: very rarely - thrombocytopenic purpura, leukopenia, thrombocytopenia. From the urinary system: infrequently - pollakiuria, painful urge to urinate, nocturia; very rarely - dysuria, polyuria. From the reproductive system and mammary glands: infrequently - gynecomastia, impotence. From the respiratory system: infrequently - shortness of breath, rhinitis; very rarely - cough. From the musculoskeletal system: infrequently - muscle cramps, myalgia, arthralgia, back pain, arthrosis; rarely - myasthenia. From the skin: infrequently - alopecia; rarely - dermatitis; very rarely - alopecia, xeroderma, cold sticky sweat, skin pigmentation disorder. Allergic reactions: rarely - skin itching, rash (including erythematous, maculopapular rash); very rarely - urticaria, angioedema, erythema multiforme. From the senses: infrequently - ringing in the ears, blurred vision, diplopia, impaired accommodation, xerophthalmia, conjunctivitis, eye pain; very rarely - parosmia. Metabolism: very rarely - hyperglycemia. Other: uncommon - weight loss, weight gain, taste disturbance, nosebleeds, chills. Overdose
Symptoms: pronounced decrease in blood pressure with the possible development of reflex tachycardia and excessive peripheral vasodilation (risk of developing severe and persistent arterial hypotension, including the development of shock and death).
Treatment: gastric lavage, use of activated charcoal (especially in the first 2 hours after an overdose), maintaining the function of the cardiovascular system, elevated position of the lower extremities, monitoring heart and lung performance, monitoring circulating blood volume (CBV) and diuresis. To restore vascular tone, use vasoconstrictors (in the absence of contraindications to their use); to eliminate the effects of blockade of calcium channels - intravenous administration of calcium gluconate. Hemodialysis is ineffective. Interaction with other drugs
Amlodipine can be safely used for the treatment of arterial hypertension together with thiazide diuretics, alpha-blockers or ACE inhibitors.
In patients with stable angina, amlodipine can be combined with other antianginal agents, such as long- or short-acting nitrates. Unlike other BMCCs, no clinically significant interaction with amlodipine (II generation BMCCs) was detected when used together with non-steroidal anti-inflammatory drugs (NSAIDs), including indomethacin. It is possible to enhance the antianginal and hypotensive effect of BMCC when used together with thiazide and loop diuretics, ACE inhibitors and nitrates, as well as enhance their hypotensive effect when used together with alpha1-blockers. Erythromycin, when used together, increases the Cmax of amlodipine in young patients by 22%, and in elderly patients by 50%. Beta-blockers, when used simultaneously with amlodipine, can cause an exacerbation of heart failure. Although negative inotropic effects have generally not been observed in amlodipine studies, some CBMCs may enhance the negative inotropic effects of antiarrhythmic drugs that prolong the QT interval (eg, amiodarone and quinidine). A single dose of 100 mg of sildenafil in patients with arterial hypertension does not affect the pharmacokinetic parameters of amlodipine. Repeated use of amlodipine at a dose of 10 mg and atorvastatin at a dose of 80 mg is not accompanied by significant changes in the pharmacokinetics of atorvastatin. Ethanol (drinks containing alcohol): amlodipine with single and repeated use in a dose of 10 mg does not affect the pharmacokinetics of ethanol. Antiretroviral drugs (ritonavir) increase plasma concentrations of BMCC, including amlodipine. Neuroleptics and isoflurane - enhance the hypotensive effect of dihydropyridine derivatives. Calcium supplements can reduce the effect of BMCC. When amlodipine is used together with lithium preparations, it is possible to increase the manifestation of neurotoxicity (nausea, vomiting, diarrhea, ataxia, tremor, tinnitus). Amlodipine does not change the pharmacokinetics of cyclosporine. Does not affect the serum concentration of digoxin and its renal clearance. Does not significantly affect the effect of warfarin (prothrombin time). Cimetidine does not affect the pharmacokinetics of amlodipine. In in vitro studies, amlodipine does not affect the plasma protein binding of digoxin, phenytoin, warfarin and indomethacin. Grapefruit juice: simultaneous single administration of 240 mg of grapefruit juice and 10 mg of amlodipine orally is not accompanied by a significant change in the pharmacokinetics of amlodipine. Aluminum- or magnesium-containing antacids: their single dose does not have a significant effect on the pharmacokinetics of amlodipine. Special instructions
During therapy with Amlodipine-Teva, it is necessary to monitor body weight and sodium intake, and the appointment of an appropriate diet is indicated.
It is necessary to maintain oral hygiene and follow-up with a dentist (to prevent pain, bleeding and gum hyperplasia). When using Amlodipine-Teva in patients with chronic heart failure of functional class III and IV according to the NYHA classification, pulmonary edema may develop. In acute myocardial infarction, Amlodipine-Teva is prescribed after stabilization of hemodynamic parameters (see section Contraindications). Patients with liver failure who need to take Amlodipine-Teva should be under medical supervision. In elderly patients, T1/2 may increase and drug clearance may decrease. No dose changes are required, but more careful monitoring of patients in this category is necessary. In patients with impaired renal function, monitoring of the condition is necessary. The effectiveness and safety of Amlodipine-Teva in hypertensive crisis has not been established. Despite the absence of withdrawal syndrome in BMCC, it is advisable to discontinue treatment with Amlodipine-Teva by gradually reducing the dose of the drug. Effect on the ability to drive vehicles and other complex mechanisms
Although no negative effects on the ability to drive vehicles or other complex mechanisms were observed while taking Amlodipine-Teva, however, due to a possible excessive decrease in blood pressure, the development of dizziness, drowsiness and other adverse reactions, Caution should be exercised in these situations, especially at the beginning of treatment and when increasing the dose.
Release form
Tablets 5 mg and 10 mg.
10 tablets per blister made of Al/PVC/PVDC. For a dosage of 5 mg: 1 or 3 blisters in a cardboard pack along with instructions for use. For a dosage of 10 mg: 1, 2 or 3 blisters in a cardboard pack along with instructions for use. Storage conditions
Store at a temperature not exceeding 25 C. Keep out of the reach of children!
Shelf life:
5 years.
Do not use after expiration date. Conditions for dispensing from pharmacies
By prescription.
Manufacturer:
Pharmaceutical Plant TEVA Private Co. Ltd., Hungary st. Pallagi 13, N-4042 Debrecen, Hungary Owner of the plant in Russia: TEVA Pharmaceutical Enterprises Ltd., Israel 5 Basel St., P/B 3190, Petah Tikva 49131 Address for receiving claims: 119049, Moscow, st. Shabolovka, 10, building 2, Business - December 1, 2011
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You can find detailed and up-to-date instructions for the drug on the website of the State Register of Medicines www.grls.rosminzdrav.ru.
