Amlodipharm - instructions for use, dose, side effects, contraindications

Excipientslactose monohydrate (sugar milk) 85.63 mg, povidone 3.22 mg, crospovidone 3.22 mg, magnesium stearate 1.0 mg or granulate Lodipress (lactose monohydrate, povidone, crospovidone) 92.07 mg, magnesium stearate 1, 0 mg.

Description:

Tablets of white or almost white color are flat-cylindrical with a facet and a risk. A slight unevenness of the surface is permissible.

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 (BCCC) II generation, has antianginal and antihypertensive effect.Linking with dihydropyridine receptors, blocks calcium channels, reduces the transmembrane transition of calcium ions into the cell (mostly in smooth muscle cells of blood vessels, rather than in cardiomyocytes).

Antianginal action is due to the expansion of the coronary and peripheral arteries and arterioles. When angina decreases the severity of myocardial ischemia; expanding peripheral arterioles, reduces the overall peripheral vascular resistance, reduces preload on the heart, reduces the need for myocardium in oxygen. Expanding coronary arteries and arterioles in unchanged and ischemic zones of the myocardium, increases the flow of oxygen into the myocardium (especially with vasospastic angina); prevents the development of 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 until the onset of an attack of angina and "ischemic" depression of the segment ST, reduces the incidence of angina attacks and consumption of nitroglycerin and other nitrates.

Has a long-term dose-dependent antihypertensive effect.The antihyperensive effect is due to a direct vasodilating effect on smooth muscle vessels. With arterial hypertension, a single dose provides a clinically significant decrease in blood pressure (BP) for 24 hours (in the patient's position "lying" and "standing"). Orthostatic hypotension in the appointment of amlodipine is rare. Does not cause a decrease in the fraction of the ejection of the left ventricle. Reduces the degree of myocardial hypertrophy of the left ventricle. Does not affect the contractility and conductance of the myocardium, does not cause a reflex increase in heart rate (HR), inhibits platelet aggregation, increases the rate of glomerular filtration, has a weak natriuretic effect.

In patients with ischemic heart disease (CHD) (including coronary atherosclerosis with single vessel damage and up to stenosis of 3 or more arteries and carotid artery atherosclerosis) who underwent myocardial infarction, percutaneous transluminal angioplasty of the coronary arteries (PTCA) or with angina, the use of amlodipine prevents the development of thickening of the intima-media of carotid arteries, reduces the mortality from myocardial infarction, stroke, PTCA, coronary artery bypass graft, leads to reducing 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-IY functional class by classification NYHA) on the background of therapy with digoxin, diuretics and angiotensin-converting enzyme (ACE) inhibitors. In patients with CHF (III-IV functional class by classification NYHA) non-ischemic etiology in the use of amlodipine, there is a possibility of pulmonary edema.

When diabetic nephropathy does not increase the severity of microalbuminuria. Does not have any adverse effect on the metabolism and concentration of plasma lipids and can be used in the treatment of patients with bronchial asthma, diabetes and gout. A significant reduction in blood pressure is observed after 6-10 hours, the duration of the effect is 24 hours.

Pharmacokinetics:

After oral administration amlodipine slowly absorbed from the gastrointestinal tract (GIT).The average absolute bioavailability is 64%, the maximum concentration (Cmah) in the serum is observed after 6-9 hours. Equilibrium concentrations are achieved after 7-8 days of therapy. Food intake does not affect the absorption of amlodipine.

The average volume of distribution is 21 l / kg body weight, indicating that most of the drug is in the tissues, and the smaller - in the blood. Most of the drug in the blood (95%), binds to blood plasma proteins.

Amlodipine undergoes a slow but active metabolism (90 %) in the liver in the absence of a significant effect of "first passage." Metabolites do not have significant pharmacological activity.

After a single administration, the elimination half-life (T_1/2) varies from 31 to 48 hours, with repeated application T_1/2 is approximately 45 hours. About 60 % taken internally dose 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 excretion of amlodipine is slowed (T_1/2 65 h) compared with young patients, however, this difference is not of clinical significance. Elongation T_1/2 In patients with hepatic insufficiency, it is

long-term cumulation of the drug in the body will be higher (T_1/2 up to 60 hours). In patients with impaired renal function, changes in amlodipine concentration in the blood plasma do not correlate with the degree of renal failure. Possible slight increase T_1/2.

Amlodipine penetrates the blood-brain barrier into the breast milk. When hemodialysis is not removed.

Indications:

Arterial hypertension (monotherapy or in combination with other antihypertensive drugs);

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

Contraindications:

Hypersensitivity to amlodipine, other derivatives of dihydropyridine and other components of the drug; severe arterial hypotension (systolic blood pressure less than 90 mm Hg); collapse, cardiogenic shock; acute myocardial infarction (within the first 28 days); unstable angina (with the exception of Prinzmetal's stenocardia); obstruction of the outflow tract of the left ventricle; clinically significant aortic stenosis; pregnancy and lactation;age to 18 years (efficacy and safety not established).

Due to the fact that the composition of the drug includes lactose, Amlodipine is not recommended for patients with lactose intolerance, lactase deficiency, glucose-galactose malabsorption.

Carefully:

Dysfunction of the liver, syndrome of weakness of the sinus node (pronounced bradycardia, tachycardia), CHF of non-ischemic etiology III-IV functional class by classification NYHA, arterial hypotension, aortic stenosis, mitral stenosis, hypertrophic obstructive cardiomyopathy, acute myocardial infarction (after the first 28 days), elderly age.

Pregnancy and lactation:

The safety of the drug during pregnancy and during lactation is not established, so the drug Amlodipine should not be given to pregnant women and during lactation.

Women of childbearing age in the period of treatment should use reliable methods of contraception. At the onset of pregnancy, the drug should be stopped immediately.

Dosing and Administration:

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

Initial dose for treatment arterial hypertension and angina pectoris is 5 mg of the drug once a day. The maximum dose can be increased to 10 mg once a 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).

In patients with impaired liver function, the half-life of amlodipine increases. Recommendations on the dosage of the drug in this case is not developed, so this patient should be used with caution and under the supervision of the attending physician.

In elderly patients may increase T_1/2 Amlodipine and decrease the clearance of creatinine (CC). Dose changes are not required, but more careful monitoring of patients is necessary.

Do not require dose changes when used simultaneously with thiazide diuretics, beta-blockers and angiotensin-converting enzyme (ACE) inhibitors.

Do not require dose changes in patients with renal insufficiency.

Side effects:

Classification of the frequency of development of side effects of the World Organization Health (WHO):

very often: more than 1/10;

often: more than 1/100 and less than 1/10;

infrequently: more than 1/1000 and less than 1/100;

rarely: more than 1/10000 and less than 1/1000;

very rarely: more than 1/10000, including individual messages.

From the side of the cardiovascular system: often - peripheral edema (ankles and feet), a feeling of palpitations, a feeling of heat and "tides" of blood to the skin of the face; infrequent - marked decrease in blood pressure, orthostatic hypotension, vasculitis; rarely - development or aggravation of the course of heart failure; very rarely - rhythm disturbances (bradycardia, ventricular tachycardia, atrial fibrillation), myocardial infarction, chest pain.

From the central and peripheral nervous system: often - headache, dizziness, fatigue, drowsiness; infrequently - asthenia, general malaise, hypoesthesia, paresthesia, peripheral neuropathy, tremor, vertigo, fainting, insomnia, mood lability, unusual dreams, increased excitability, depression, anxiety; rarely - cramps, apathy, agitation; very rarely - ataxia, amnesia.

From the digestive system: often - nausea, abdominal pain; infrequent - vomiting, constipation or diarrhea, flatulence, dyspepsia, anorexia, dryness of the oral mucosa, thirst; rarely - gingival hyperplasia,increased appetite; very rarely - pancreatitis, gastritis, jaundice (caused by cholestasis), hyperbilirubinemia, increased activity of "liver" transaminases, hepatitis.

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

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

From the skin: rarely - dermatitis; very rarely - xeroderma, a violation of skin pigmentation.

From 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.

Allergic reactions: infrequently - skin itching, rash (including erythematous, maculopapular rash); very rarely - hives, angioedema, erythema multiforme.

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; very rarely - parosmia, "cold" sweat.

Overdose:

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

Treatment: gastric lavage, the use of activated charcoal (especially in the first 2 hours after an overdose), maintaining the function of the cardiovascular system, elevating the position of the lower limbs, monitoring the performance of the heart and lungs, monitoring the volume of circulating blood and diuresis. To restore the vascular tone - the use of vasoconstrictor (in the absence of contraindications to their use); to eliminate the effects of calcium channel blockade - intravenous calcium gluconate. Hemodialysis is ineffective.

Interaction:

Amlodipine can safely be used to treat arterial hypertension along with thiazide diuretics, alpha-blockers or angiotensin-converting enzyme (ACE) inhibitors. In patients with stable angina pectoris amlodipine can be combined with other antianginal agents, for example, with long-acting or short-acting nitrates.

Unlike other BCCI, clinically significant interaction of amlodipine (II generation of BCCI) was not observed when combined with nonsteroidal anti-inflammatory drugs (NSAIDs), including indomethacin.

It is possible to strengthen the anti-anginal and antihypertensive action of BCCC when combined with thiazide and "loop" diuretics, ACE inhibitors and nitrates, as well as enhancing their antihypertensive effect when combined with alpha 1-blockers.

Erythromycin in a joint application increases Cmamlodipine in young patients by 22%, and in the elderly by 50%.

Beta-adrenoblockers with simultaneous application with amlodipine may cause an exacerbation of chronic heart failure.

Although no negative inotropic effects were usually observed in the study of amlodipine, nevertheless, some BCCCs can increase the negative inotropic effect of antiarrhythmic agents that cause prolongation of the QT interval (for example, amiodarone and quinidine).

A single dose of 100 mg of sildenafil in patients with arterial hypertension does not affect the pharmacokinetics parameters of amlodipine.

The repeated use of amlodipine in 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 a single and repeated application in a dose of 10 mg does not affect the pharmacokinetics of ethanol.

Antiretroviral agents (ritonavir) increases plasma concentrations of BCCC, including amlodipine.

Neuroleptics and isoflurane - increased antihypertensive action of dihydropyridine derivatives.

Calcium preparations can reduce the effect of BCCC.

When amlodipine is used together with lithium preparations, it is possible to intensify manifestations 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.

Has no significant effect on the effect of warfarin (prothrombin time).

Cimetidine does not affect the pharmacokinetics of amlodipine.

In vitro studies amlodipine does not affect the binding of blood plasma proteins digoxin, phenytoin, warfarin and indomethacin.

Grapefruit juice: simultaneous single intake of 240 mg of grapefruit juice and 10 mg of amlodipine inwards is not accompanied by a significant change in the pharmacokinetics of amlodipine.

Aluminum- or magnesium-containing antacids: their single administration does not have a significant effect on the pharmacokinetics of amlodipine.

Special instructions:

During the period of drug treatment Amlodipine it is necessary to control body weight and sodium intake, the purpose of the appropriate diet is indicated. It is necessary to maintain oral hygiene and monitor the dentist (prevention of soreness, bleeding and gingival hyperplasia).

When using the drug Amlodipine in patients with chronic cardiac insufficiency III and IV of the functional class according to the NYHA classification, the development of pulmonary edema is possible.

Patients with hepatic insufficiency, if necessary, taking the drug Amlodipine should be under medical supervision.

In elderly patients, the half-life may be prolonged and the clearance of the drug may decrease. Dose changes are not required, but careful monitoring of patients of this category is necessary.

The effectiveness and safety of the drug during hypertensive crisis is not established.

Despite the absence of the "cancellation" syndrome in BCCC, gradual reduction of doses is recommended before discontinuation of treatment with the drug.

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 the vehicle and work with mechanisms that require an increased concentration of attention and speed of psychomotor reactions.

Form release / dosage:

Tablets of 5 mg.

Packaging:

For 10 tablets in a contour mesh box made of polyvinylchloride film and aluminum foil printed lacquered.

1, 2 or 3 contour squares with instructions for use in a pack of cardboard.

Storage conditions:

In the dark place at a temperature of no higher than 30 ° C.

Keep out of the reach of children.

Shelf life:

3 years.

Do not use after expiry date.

Terms of leave from pharmacies:On prescription

Registration number:LS-000540

Date of registration:04.04.2011 / 27.11.2013

Expiration Date:Unlimited

The owner of the registration certificate:FARMAKOR PRODUCTION, LTD. FARMAKOR PRODUCTION, LTD. Russia

Manufacturer: & nbsp

FARMAKOR PRODUCTION, LTD. Russia

Information update date: & nbsp25.07.2017

Illustrated instructions

Instructions

Amlodipharm® (Amlodipharm®)