Amlotop - instructions for use, doses, side effects, contraindications

Excipients: lactose monohydrate - 77.67 mg or 111.70 mg (lactose 200 / flowulac 100 - 12.97 mg / 64.70 mg or 18.69 mg / 93.01 mg); cellulose microcrystalline 11.60 mg or 17.00 mg; calcium stearate - 1.00 mg or 1.40 mg; croscarmellose sodium (impellose) - 1.80 mg or 2.70 mg; silicon dioxide colloid (aerosil) - 1.00 mg or 3.34 mg.

Description:

Tablets of white or almost white color are flat-cylindrical with a facet and a risk.

Pharmacotherapeutic group:The blocker of "slow" calcium channels

ATX: & nbsp

C.08.C.A.01 Amlodipine

Pharmacodynamics:

Derivative of dihydropyridine - blocker of "slow" calcium channels (BCCI) of the second generation, has an antianginal and hypotensive effect. Linking to the segment S6III and IV domains of the alpha 1-subunit of the calcium channel Ltype, blocks calcium channels, reduces the transmembrane transition of calcium ions into the cell (mostly in the smooth muscle cells of the vessels, rather than in cardiomyocytes).

Antianginal action is due to the expansion of peripheral and coronary arteries and arterioles. When angina decreases the severity of myocardial ischemia; expanding peripheral arterioles, reduces the overall peripheral, vascular, resistance (reduces afterload on the heart) without causing a reflex increase in the heart rate, which helps to reduce energy consumption; reduces myocardial oxygen demand. Expanding coronary arteries and arterioles in unchanged and ischemic zones of the myocardium, increases the flow of oxygen into the myocardium with vasospastic angina; prevents the development of coronary spasm (including those caused by smoking).

In patients with angina, a single daily dose of amlodipine increases the time until the onset of the first ischemic episode during exercise, prevents the development of an attack of angina and the "ischemic" depression of the segment ST (1 mm) against the background of physical activity, reduces the frequency of angina attacks and the consumption of nitroglycerin.

Hypotensive effect is caused by a direct vasodilating effect on the smooth muscles of the vessels. Has a long-term dose-dependent hypotensive effect.

In arterial hypertension, a single daily dose of amlodipine provides a clinically significant decrease in blood pressure (BP) for 24 hours (in the patient's position "lying" and "standing"). Does not cause a sharp decrease in blood pressure, the fraction of the ejection of the left ventricle. Does not affect the contractility and conductivity myocardium. Reduces the degree of myocardial hypertrophy of the left ventricle.

Have patients with ischemic heart disease (CHD) (Including coronary atherosclerosis with a lesion of the vessel and to the stenosis 3 or more arteries and carotid atherosclerosis), myocardial infarction, percutaneous transluminal angioplasty of coronary arteries (PTCA) or angina pectoris, amlodipine prevents development thickening IMT of carotid arteries reduces mortality from myocardial infarction, stroke, PTCA, coronary artery bypass grafting,leads to a reduction in the number of hospitalizations for unstable angina and the progression of chronic heart failure, reduces the frequency of interventions aimed at restoring coronary blood flow.

Amlodipine does not increase the risk of death or development of complications leading to fatal outcomes in patients with chronic heart failure (CHF) (III-IV functional class by classification NYHA) on the background of therapy with digoxin, diuretics and angiotensin-converting enzyme (ACE) inhibitors.

In patients with XFROMH (III-IV functional class by classification NYHA) non-ischemic etiology in the use of amlodipine, there is a possibility of pulmonary edema.

Amlodipine does not have any adverse effect on the metabolism and concentration of plasma lipids. It inhibits platelet aggregation, increases the rate of glomerular filtration, and has a weak natriuretic effect. When diabetic nephropathy does not increase the severity of microalbuminuria.

The time of onset of the effect is 2-4 hours, the duration of the effect is 24 hours.

Pharmacokinetics:

Suction. After oral administration amlodipine well absorbed from the gastrointestinal tract. Food intake does not affect the absorption of amlodipine. The maximum concentration in the serum is achieved 6-12 hours after administration. Bioavailability is 60-65%. The average volume of distribution is 21 l / kg of body weight. The connection with plasma proteins is 90-97%. The drug penetrates the blood-brain barrier.

Metabolism and excretion. Amlodipine undergoes a slow but significant metabolism (90%) in the liver with the formation of inactive metabolites, has a low hepatic clearance (the "first pass" effect through the liver). Half-life is an average of 35 hours (varies from 35 to 50 hours), which corresponds to the appointment of the drug once a day. The total clearance is 500 ml / min. A stable equilibrium concentration in plasma is achieved after 7-8 days of therapy. It is excreted by the kidneys (10% unchanged, 60% in the form of metabolites), with bile and through the intestine - 20-25% in the form of metabolites, as well as with breast milk. When hemodialysis is not removed.

In elderly patients, patients with hepatic insufficiency and severe CHF, the elimination half-life increases to 60-65 hours; if the kidney function is not affected - does not change.

Indications:

Arterial hypertension (monotherapy or in combination with other antihypertensive agents).

Stable exertional angina and vasospastic angina (Prinzmetal angina) (monotherapy or in combination with other antianginal agents).

Contraindications:

- Hypersensitivity to amlodipine and other dihydropyridine derivatives, as well as to other components included in the preparation;

- severe arterial hypotension (systolic blood pressure less than 90 mm Hg);

- collapse, cardiogenic shock;

- clinically significant aortic stenosis;

- pregnancy and lactation;

- age under 18 years (effectiveness and safety not studied);

- lactose intolerance, lactase deficiency or glucose-galactose malabsorption.

Carefully:

Dysfunction of the liver, syndrome of weakness of the sinus node (pronounced bradycardia, tachycardia), chronic heart failure of non-ischemic etiology III-IV functional class by classification NYHA, hypotension (systolic blood pressure greater than 90 and less than 100 mm Hg), aortic stenosis, mitral stenosis, hypertrophic obstructive cardiomyopathy (GOKMP), acute myocardial infarction (and within 1 month after myocardial infarction), advanced age.

Pregnancy and lactation:

Women of childbearing age during the treatment with amlodipine should use reliable methods of contraception.

Dosing and Administration:

Inside, once a day, regardless of food intake, with a sufficient amount of water (100 ml).

The initial dose for arterial hypertension and angina is usually 5 mg. Depending on the individual reaction of the patient, the dose can be increased to a maximum of 10 mg per day. It is recommended to increase the dose 7-14 days after the start of therapy (a faster increase in the dose requires careful monitoring of the patient).

Patients with a small body weight, low growth, elderly patients, patients with impaired liver function as an antihypertensive drug amlodipine appoint an initial dose of 2.5 mg (1/2 tablet 5 mg), as an antianginal agent - 5 mg. An initial dose of 2.5 mg can also be used when adding amlodipine to therapy with other antihypertensive drugs.

In patients with renal insufficiency, dose adjustment is not required.

Side effects:

Frequency of adverse reactions: often - more than 1%, infrequently - more than 0.1% and less than 1%, rarely - more than 0.01% and less than 0.1%, very rarely - less than 0.01%.

From the side of the cardiovascular system: often - peripheral edema (ankles and feet), a feeling of palpitation, a feeling of heat and "tides" of blood to the skin of the face; infrequently - excessive reduction of blood pressure, orthostatic hypotension, vasculitis; rarely - development or exacerbation of heart failure; very rarely - cardiac arrhythmias (including bradycardia, ventricular tachycardia and atrial fibrillation), heart attack, chest pain.

From the central and peripheral nervous system: often - increased fatigue, dizziness, headache, drowsiness; infrequently - malaise, fainting, sweating, asthenia, hypesthesia, paresthesia, peripheral neuropathy, tremor, insomnia, emotional lability, abnormal dreams, nervousness, depression, anxiety; rarely - cramps, apathy, agitation; very rarely - ataxia, amnesia, migraine.

From the digestive system: often - pain in the abdominal cavity, nausea; infrequent - vomiting, constipation, flatulence, indigestion, diarrhea, anorexia, dry mouth, thirst; rarely - gingival hyperplasia, increased appetite; very rarely - gastritis, pancreatitis, hyperbilirubinemia, jaundice (usually cholestatic), increased activity of "hepatic" transaminases, hepatitis.

On the part of the hematopoiesis system: very rarely - thrombocytopenic purpura, leukopenia, thrombocytopenia.

From the side of the musculoskeletal system: infrequently - arthralgia, muscle cramps, myalgia, back pain, arthrosis; rarely - myasthenia gravis.

From the side of metabolism: very rarely - hyperglycemia.

From the respiratory system: infrequently - shortness of breath, rhinitis; very rarely - cough.

From the genitourinary system: infrequent - frequent urination (pollakiuria), painful urge to urinate, nocturia, impotence; very rarely - dysuria, polyuria.

Allergic reactions: infrequently - itchy skin, rash; very rarely - angioedema, erythema multiforme, urticaria.

Other: infrequently - alopecia, ringing in the ears, gynecomastia, increase / decrease in body weight, visual impairment, diplopia, accommodation disorder, xerophthalmia, conjunctivitis, eye pain, taste perversion, chills, nosebleeds; rarely - dermatitis; very rarely - parosmia, xeroderma, "cold" sweat, pigmentation disorder skin.

Overdose:

Symptoms: a marked decrease in blood pressure with the possible development of reflex tachycardia and excessive peripheral vasodilation (the risk of a pronounced and persistent reduction in blood pressure, including with the development of shock and death).

Treatment: reception of activated carbon (especially in the first 2 hours after an overdose), gastric lavage (in some cases), maintenance of cardiovascular function, control of heart and lung function, control of circulating blood volume and diuresis. The patient should take a horizontal position with an elevated position of the lower extremities.

In the absence of contraindications, symptomatic therapy: vasoconstrictive drugs, intravenous calcium gluconate. Hemodialysis is ineffective.

Interaction:

Inhibitors of microsomal liver enzymes can increase the concentration of amlodipine in the blood plasma, increasing the risk of side effects, and inducers of microsomal liver enzymes - reduce. Unlike other BCCI, there is no clinically significant interaction of amlodipine with non-steroidal anti-inflammatory drugs (NSAIDs), especially indomethacin.

It is possible to strengthen the anti-anginal and hypotensive action of BCCC when combined with thiazide and loop diuretics, beta-blockers, alpha-adrenoblockers, verapamil, ACE inhibitors and nitrates.

Simultaneous reception of BCC with neuroleptics and isoflurane may increase the hypotensive effect.

Some BCCI can enhance the expressed negative inotropic effect of antiarrhythmic drugs that cause lengthening of the interval QT (amiodarone, quinidine), however, when the drug is used amlodipine negative inotropic action is usually not observed.

Calcium preparations can reduce the effect of BCCC.

With the joint application of BCCA to lithium preparations, it is possible to intensify manifestations of their neurotoxicity (nausea, vomiting, diarrhea, ataxia, tremor, tinnitus), but the drug data amlodipine are absent. Cimetidine does not affect the pharmacokinetics of amlodipine.

Amlodipine does not cause significant changes in the pharmacokinetics of cyclosporine.

A single administration of antacids containing aluminum / magnesium does not significantly affect the pharmacokinetics of amlodipine.

A single dose of sildenafil in a dose of 100 mg in patients with essential hypertension does not affect the pharmacokinetics parameters of amlodipine. The repeated simultaneous use of amlodipine in a dose of 10 mg and atorvastatin 80 mg does not significantly affect the pharmacokinetics of atorvastatin.

With the simultaneous use of digoxin and amlodipine, the serum digoxin concentration and its clearance do not change.

Amlodipine does not affect the change in prothrombin time caused by warfarin. At a single and repeated application in a dose of 10 mg amlodipine has no significant effect on the pharmacokinetics of ethanol.

Antiviral drugs (ritonavir) increase plasma concentrations of BCCC, including amlodipine.

Simultaneous single intake of 240 mg of grapefruit juice and 10 mg of amlodipine by mouth is not accompanied by a significant change in the pharmacokinetics of amlodipine.

Special instructions:

In the treatment of hypertension amlodipine can be used in combination with thiazide diuretics, alpha and beta-adrenoblockers, ACE inhibitors, short and prolonged-action nitrates, NSAIDs, antibiotics and oral hypoglycemic agents.

In the treatment of angina pectoris amlodipine can be administered in the form of monotherapy or in combination with other antianginal drugs, including in patients refractory to treatment with nitrates and / or beta-adrenoblockers, in adequate doses.

During the treatment period it is necessary to control body weight and sodium intake. It is necessary to maintain oral hygiene and regular visits to the dentist (to prevent soreness, bleeding and gingival hyperplasia).

Amlodipine does not affect the plasma concentrations of potassium, glucose, triglycerides, total cholesterol, LDL, uric acid, creatinine and uric acid and can be used in patients with bronchial asthma, diabetes and gout. Amlodipine can be used in patients prone to vasospasm / vasoconstriction.

Patients with low body weight or low growth, elderly patients, as well as patients with severe hepatic insufficiency, may require less dose. When increasing the dose, careful monitoring of the elderly is necessary patients.

Despite the lack of "slow" calcium channels of the syndrome of "cancellation" in blockers, a gradual decrease in doses is recommended before cessation of treatment.

Women of childbearing age during the treatment with amlodipine should use reliable methods of contraception.

Amlodipine tablets are not recommended for hypertensive crisis.

Effect on the ability to drive transp. cf. and fur:

In some patients, mainly at the beginning of treatment or when changing the dosage regimen, due to a possible pronounced decrease in blood pressure, drowsiness, dizziness and other side effects may occur. When they occur, it is not recommended to drive and operate machinery.

Form release / dosage:

Tablets 5 mg and 10 mg.

Packaging:

For 10 or 30 tablets in a planar cell packaging from a polyvinylchloride film and aluminum foil.

2, 3, 5, 9 or 10 contour cell packs of 10 tablets, or 1 or 3 contour packs of 30 tablets together with instructions for use in a pack of cardboard.

Storage conditions:In a dry, the dark place at a temperature of no higher than 25 ° C. Keep out of the reach of children.

Shelf life:

3 years. Do not use after the expiration date.

Terms of leave from pharmacies:On prescription

Registration number:P N003030 / 01

Date of registration:22.07.2009 / 20.11.2013

Expiration Date:Unlimited

The owner of the registration certificate:MAKIZ-PHARMA, LLC MAKIZ-PHARMA, LLC Russia

Manufacturer: & nbsp

MAKIZ-PHARMA, LLC Russia

HEMOFARM, LLC Russia

Representation: & nbspNizhpharm, JSCNizhpharm, JSCRussia

Information update date: & nbsp14.08.2017

Illustrated instructions

Instructions

Amlotop (Amlotop)