Name Amlodipine ft. Forms of release tablets MNNA amlodipine FTGBmkk Composition Each tablet contains 5 mg or 10 mg of amlodipine as an active substance (in the form of amlodipine besylate, respectively, 6.934 mg and 13.868 mg). Excipients: anhydrous calcium hydrogen phosphate, sodium starch glycolate (type A), magnesium stearate, anhydrous colloidal silicon dioxide, microcrystalline cellulose. Pharmacotherapeutic group Selective calcium channel blockers with a predominant effect on blood vessels. Pharmacological properties Amlodipine is a slow calcium channel blocker or calcium ion antagonist that blocks the flow of calcium ions through membranes into smooth muscle cells of the vascular myocardium. The mechanism of the hypotensive action of amlodipine is due to a direct relaxing effect on vascular smooth muscle cells. The exact mechanism of action of amlodipine in angina pectoris has not been fully established, but amlodipine reduces ischemia in the following two ways: Amlodipine dilates the peripheral arterioles and thus reduces the total peripheral resistance (afterload) that the heart needs to work to overcome. Since the heart rate does not change, reducing the load on the heart leads to a decrease in energy consumption and oxygen demand. The mechanism of action of amlodipine probably also involves the expansion of the main coronary arteries and coronary arterioles in both unchanged and ischemic areas of the myocardium. This dilatation increases the supply of oxygen to the myocardium in patients with vasospastic angina (Prinzmetal’s angina or variant angina) and prevents the development of coronary vasoconstriction caused by smoking. In patients with arterial hypertension, a single daily dose of amlodipine provides a clinically significant reduction in blood pressure over 24 hours, both in the supine and standing positions. Due to the slow onset of action, amlodipine does not cause acute hypotension. In patients with angina pectoris, a single daily dose of amlodipine increases the time of exercise, delays the development of an angina attack and ST segment depression (by 1 mm) during exercise, reduces the frequency of angina attacks and the consumption of nitroglycerin tablets. Absorption: After oral administration in therapeutic doses, amlodipine is well absorbed, reaching the maximum concentration in the blood 6-12 hours after administration. Absolute bioavailability is calculated to be 64-80%. The volume of distribution is approximately 21 l/kg. Eating does not affect the absorption of amlodipine. In vitro studies have shown that approximately 97.5% of circulating amlodipine is bound to plasma proteins. Biotransformation/elimination: The plasma half-life is about 35-50 hours, which corresponds to the administration of the drug once a day. Stable equilibrium plasma concentration is achieved after 7-8 days of continuous administration of the drug. Amlodipine is biotransformed in the liver to form inactive metabolites; 10% of the unchanged drug and 60% of the metabolites are excreted in the urine. Use in the elderly: in the elderly and younger people, it is necessary to achieve the maximum concentration of amlodipine in the blood plasma, almost the same. In the elderly, there is a trend towards a decrease in the clearance of amlodipine, which leads to an increase in UAC (area under the concentration-time curve) and half-life. As expected, in patients of various age groups suffering from congestive heart failure, there was an increase in AUC and half-life of the drug. Indications for use arterial hypertension; chronic stable angina pectoris; vasospastic angina (Prinzmetal’s angina). Contraindications for use known hypersensitivity to amlodipine, dihydropyridines and / or other components of the drug; unstable angina; clinically significant aortic stenosis; arterial hypotension (BP less than 90 mm Hg); acute myocardial infarction; shock (including cardiogenic shock); children under 18 years of age (no clinical experience); pregnancy and lactation (see section Use during pregnancy and lactation). Prescribed with caution to patients: with impaired liver function, sick sinus syndrome (severe bradycardia, tachycardia), chronic heart failure III-IV class in the stage of decompensation, mild or moderate arterial hypotension, aortic and / or mitral stenosis, hypertrophic obstructive cardiomyopathy, acute myocardial infarction (and within 1 month after), diabetes mellitus, lipid profile disorders, old age. Due to the fact that the efficacy and safety of amlodipine in children under 18 years of age have not been precisely established, it should be refrained from prescribing it to patients of this age category. Dosing and Administration The usual initial dose for arterial hypertension and angina pectoris is 5 mg / day. preferably at the same time of day. Depending on the clinical response, it is possible to increase the dose to 10 mg / day. With the simultaneous use of thiazide diuretics, β-blockers and angiotensin-converting enzyme inhibitors, dose adjustment is not required. Elderly people, people with low body weight, and patients with impaired liver function can be given a dose of 2.5 mg. The same dose can be given when amlodipine is combined with other antihypertensive agents. The dose of the drug should be chosen taking into account the individual needs of the patient. Typically, dose selection (titration) is carried out from 7 to 14 days, which allows the doctor to evaluate the patient’s response to each dose. If clinically necessary, titration can be accelerated if the patient can be assessed frequently. In stable and vasospastic angina, the recommended dose is 5-10 mg, a low dose is recommended for the elderly and patients with impaired liver function. To obtain an adequate effect, most patients need a dose of 10 mg. The recommended dose interval for patients with coronary artery disease is 5-10 mg per day. Use in children The safety and efficacy of amlodipine in children has not been established. Use in patients with impaired liver function See Precautions section. If you forget to take AMLODIPINE FT, take your tablet as soon as possible before your next dose is due. If it is time for your next dose of medication, do not take the missed dose. You can not double the dosage of the drug to compensate for the missed! Further, the drug is used according to the recommended dosing regimen. Adverse reactions reported with the use of amlodipine are given below by the systems and classes of organs and the frequency of occurrence: very often (≥1 / 10), often (≥1 / 100 – <1/10), infrequently (≥1 / 1000 - ≤1/100), rare (≥1/10000 - ≤1/1000), very rare (<1/10000). From the blood and lymphatic system. Very rare: leukopenia, thrombocytopenia. From the immune system. Very rare: allergic reactions. Metabolic disorders and alimentary disorders. Very rare: hyperglycemia. Mental disorders. Uncommon: insomnia, mood changes (including anxiety), depression. Rare: confusion. From the side of the nervous system. Often: drowsiness, dizziness, headache (mainly at the beginning of treatment). Infrequently: tremor, dysgeusia, hypesthesia, paresthesia. Very rare: hypertension, peripheral neuropathy. From the organs of vision. Infrequently: visual impairment (including diplopia). From the organs of hearing and balance. Uncommon: ringing in the ears. From the side of the heart. Uncommon: palpitations. Very rare: myocardial infarction, arrhythmia (including bradycardia, ventricular tachycardia and atrial fibrillation). From the side of the vessels. Often: hot flashes. Infrequently: arterial hypotension. Very rare: vasculitis. Respiratory, thoracic and mediastinal disorders. Uncommon: dyspnea, rhinitis. Very rare: cough. From the gastrointestinal tract. Often: abdominal pain, nausea. Uncommon: Vomiting, dyspepsia, intestinal motility disorders (including constipation and diarrhea), dry mouth. Very rare: pancreatitis, gastritis, gingival hyperplasia. From the hepatobiliary system. Very rare: hepatitis, jaundice, elevated liver enzymes (more commonly associated with cholestasis). From the skin and subcutaneous tissue. Infrequently: alopecia, purpura, discoloration of the skin, sweating, itching, rash, exanthema. Very rare: angioedema, erythema multiforme, urticaria, exfoliative dermatitis, Stevens Johnson syndrome, angioedema, photosensitivity. From the musculoskeletal and connective tissues. Often: swelling of the legs. Uncommon: arthralgia, myalgia, convulsions, back pain. From the side of the kidneys and urinary tract. Infrequently: urinary incontinence, nocturia, increased frequency of urination. From the reproductive system and mammary glands. Uncommon: impotence, gynecomastia. General disorders and conditions at the injection site. Often: edema, fatigue. Uncommon: chest pain, asthenia, pain, malaise. Research. Infrequently: increase or decrease in body weight. If you experience other side effects not mentioned above or if you feel unwell, you should consult your doctor. OverdoseSymptoms: a pronounced decrease in blood pressure with the possible development of reflex tachycardia, excessive peripheral vasodilation (there is a possibility of severe and persistent arterial hypotension, including the development of shock and death). Treatment: prescribing activated charcoal (especially in the first 2 hours after an overdose), gastric lavage (in some cases), giving an elevated position to the limbs, actively maintaining the function of the cardiovascular system, monitoring indicators of heart and lung function, monitoring circulating blood volume and diuresis . To restore vascular tone and blood pressure, if there are no contraindications, it may be useful to use vasoconstrictor drugs; to eliminate the effects of blockade of calcium channels - intravenous administration of calcium gluconate. Due to the fact that amlodipine is largely bound to plasma proteins, hemodialysis is not effective. Interaction with other drugs If you are currently or have recently taken other drugs, tell your doctor. Amlodipine has been safely used with thiazide diuretics, alpha-blockers, beta-blockers, angiotensin-converting enzyme inhibitors, long-acting nitrates, sublingual nitroglycerin, non-steroidal anti-inflammatory drugs, antibiotics, and oral hypoglycemic agents. The results of in vitro studies using human plasma indicate that amlodipine does not affect protein binding of the drugs tested (digoxin, phenytoin, warfarin and indomethacin). SIMVACTATIN: Co-administration of multiple doses of amlodipine 10 mg with simvastatin 80 mg resulted in a 77% increase in simvastatin exposure compared to simvastatin alone. It is recommended to limit the dose of simvastatin in patients taking amlodipine to 20 mg per day. GRAPEFRUIT JUICE: Simultaneous single oral administration of 240 ml of grapefruit juice and 10 mg of amlodipine in 20 healthy volunteers did not significantly affect the pharmacokinetics of amlodipine. In this study, it was not possible to study the effect of the genetic polymorphism of CYP3A4 (the main enzyme responsible for the metabolism of amlodipine). Taking amlodipine with grapefruit or grapefruit juice is not recommended, since the bioavailability and, accordingly, the hypotensive effect of amlodipine may increase. CYP3A4 INHIBITORS: Co-administration of diltiazem 180 mg and amlodipine 5 mg in elderly patients (69-87 years) resulted in a 57% increase in systemic exposure to amlodipine. Simultaneous administration with erythromycin in healthy volunteers (aged 18 to 43 years) did not lead to a significant change in the systemic exposure of amlodipine (22% increase in AUC). Although the clinical significance of these data is unclear, pharmacokinetic changes can be clearly expressed in the elderly. Strong inhibitors of CYP3A4 (eg, ketoconazole, itraconazole, ritonavir) may increase amlodipine concentrations to a greater extent than diltiazem. Amlodipine should be used with caution in combination with CYP3A4 inhibitors. CYP3A4 STIMULANTS: There are no data on the effect of CYP3A4 stimulants on amlodipine. Simultaneous administration of CYP3A4 stimulants (for example, rifampicin, St. John's wort) can lead to a decrease in plasma concentrations of amlodipine. Amlodipine should be used with caution in combination with CYP3A4 stimulants. In the studies below, there were no significant changes in the pharmacokinetics of both amlodipine and other drugs while taking it. Special studies: the effect of other drugs on amlodipine CIMETIDINE: the simultaneous use of amlodipine and cimetidine was not accompanied by a change in the pharmacokinetics of amlodipine. ALUMINUM / MAGNESIUM (antacid): A single dose of aluminum / magnesium containing antacids with amlodipine did not significantly affect the pharmacokinetics of amlodipine. SILDENAFIL: A single dose of sildenafil at a dose of 100 mg in patients with essential hypertension had no effect on the pharmacokinetic parameters of amlodipine. With the combined use of amlodipine and sildenafil, both drugs had an independent hypotensive effect. DANTROLENE (infusion): when administered intravenously with verapamil and dantrolene, animals developed ventricular fibrillation and fatal cardiovascular failure, accompanied by hyperkalemia. Due to the risk of hyperkalemia, it is recommended that concomitant administration of calcium channel blockers such as amlodipine be avoided in patients at risk of developing malignant hyperthermia or for the treatment of malignant hyperthermia. Special studies: effect of amlodipine on other drugs ATORVACTATIN: Repeated use of amlodipine at a dose of 10 mg and atorvastatin at a dose of 80 mg was not accompanied by significant changes in the equilibrium parameters of the pharmacokinetics of atorvastatin. DIGOXIN: Serum levels and renal clearance of digoxin did not change when amlodipine was co-administered with digoxin in healthy volunteers. ETHANOL (alcohol): with a single and repeated use at a dose of 10 mg, amlodipine did not significantly affect the pharmacokinetics of ethanol. WARFARIN: Amlodipine did not affect changes in prothrombin time induced by warfarin. Cyclosporine: Pharmacokinetic studies have shown that amlodipine does not cause significant changes in the pharmacokinetics of cyclosporine. LITHIUM: when used together with lithium preparations, it is possible to increase the manifestations of their neurotoxicity. Precautions The safety and efficacy of amlodipine in hypertensive crisis has not been evaluated. Patients with heart failure. In this category of patients, amlodipine should be used with caution. In a long-term, placebo-controlled study in patients with severe heart failure (NYHA class III and IV), amlodipine had a higher incidence of pulmonary edema compared with placebo, but this effect was not associated with an exacerbation of heart failure. Patients with impaired liver function. The elimination half-life of amlodipine is increased in patients with hepatic impairment, but dosing recommendations have not yet been developed. Therefore, this category of patients should be used with caution. Elderly patients. Increasing the dose of the drug in this category of patients should be done with caution. Patients with renal insufficiency. In this category of patients, the usual doses of the drug should be used. Changes in the concentration of amlodipine in plasma do not correlate with the degree of impaired renal function. Amlodipine is not removed by dialysis. Amlodipine does not affect the results of laboratory tests. It is not recommended to use amlodipine together with grapefruit or grapefruit juice, since in some patients the bioavailability may be increased, which will lead to an increase in the hypotensive effect of the drug. Patients with low body weight, short stature and patients with severe liver dysfunction may require a lower dosage of amlodipine. It is necessary to maintain dental hygiene and frequent visits to the dentist (to prevent soreness, bleeding and gum hyperplasia). The dosage regimen for elderly patients is the same as for patients of other age groups. When increasing the dose, careful monitoring of elderly patients is necessary. Despite the absence of “withdrawal” syndrome in blockers of “slow” calcium channels, a gradual reduction in doses is recommended before stopping treatment. Amlodipine does not affect plasma concentrations of K +, glucose, triglycerides, total cholesterol, LDL, uric acid, creatinine and uric acid nitrogen, so Amlodipine FT can be used with caution in patients with bronchial asthma, diabetes mellitus and gout. Use during pregnancy and lactation If you are pregnant or breastfeeding, if you suspect that you are pregnant or do not exclude the possibility of pregnancy, tell your doctor about it. The safety of amlodipine during pregnancy and lactation has not been established. When studying the effect of the drug on reproductive function in animals, no signs of toxicity were detected, with the exception of delayed labor and an increase in the duration of contractions in rats when taking amlodipine in doses exceeding the maximum recommended for humans by 50 times. Thus, the use of amlodipine during pregnancy is recommended only in cases where there is no safer alternative, and the risk associated with the disease itself outweighs the possible harm to the mother and fetus. A decision should be made to discontinue nursing mothers taking the drug or stop breastfeeding, based on the importance of taking the drug to the mother or the benefits of breastfeeding. Influence on the ability to drive a car and mechanisms Amlodipine affects the ability to drive a car and use machinery in cases where the patient develops dizziness, headache, weakness or nausea. These effects may affect the patient's response rate. In such situations, caution is necessary, especially at the beginning of treatment. Storage conditions Store in a place protected from moisture at a temperature not exceeding 25°C. Keep out of the reach of children. Shelf life 3 years. The expiration date is indicated on the packaging. This drug should not be used after the date indicated on the package. Conditions of leave By doctor's prescription. Release form Tablets in blisters No. 10x1, No. 10x2, No. 10x3 and in jars No. 50. Together with the leaflet, 1, 2 or 3 blister packs or a jar are placed in a cardboard box. Buy Amlodipine FT tablets 5 mg No. 10x3 Price for Amlodipine FT tablets 5 mg No. 10x3
INN | AMLODIPINE |
---|---|
The code | 137 204 |
Barcode | 4 810 183 007 743 |
Dosage | 5mg |
Active substance | Amlodipine |
Manufacturer | Pharmtekhnologiya LLC, Belarus |
Reviews
There are no reviews yet.