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

Excipients: cellulose microcrystalline-116.550 mg, calcium hydrophosphate - 60,000 mg, sodium carboxymethyl starch - 4,000 mg, magnesium stearate - 2,000 mg.

one 10 mg tablet contains active substance: Amlodipine besylate 13.868 mg, equivalent to amlodipine - 10 mg;

Excipients: cellulose microcrystalline -109.092 mg, calcium hydrophosphate - 60,000 mg, sodium carboxymethyl starch - 4,000 mg, magnesium stearate - 2,000 mg.

Description:White or almost white round flat pills with chamfer and risk on one side.

Pharmacotherapeutic group:The blocker of "slow" calcium channels

ATX: & nbsp

C.08.C.A.01 Amlodipine

Pharmacodynamics:

Amlodipine is a blocker of "slow" calcium channels, a derivative of dihydropyridine, has an antianginal and antihypertensive effect. Blocks calcium channels, reduces the transmembrane transition of calcium ions into the cell (mostly in the smooth muscle cells of the vessels than in the cardiomyocytes).

Antianginal effect is due to the expansion of coronary and peripheral arteries and arterioles: with angina decreases the severity of myocardial ischemia; expanding peripheral arterioles, reduces the overall peripheral vascular resistance (OPSS), reduces afterload 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 spasm of the coronary arteries (incl. 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 antihypergene effect. Antihypertensive action is due to direct vasodilating effect on smooth muscle vessels.

With arterial hypertension, a single dose provides a clinically significant reduction in blood pressure (BP) for 24 hours (in the patient's "lying" and "standing" position). 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.

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.

In patients with cardiovascular diseases, including coronary atherosclerosis with single vessel damage and up to stenosis of 3 or more arteries, atherosclerosis of carotid arteries after myocardial infarction, percutaneous transluminal angioplasty (PTCA) of coronary arteries or patients with angina, the use of amlodipine prevents development of thickening of intima-media of carotid arteries, reduces mortality from myocardial infarction, stroke, PTCA, aorto-coronary shunting; leads to a decrease in the incidence of unstable angina and the progression of chronic heart failure (CHF); reduces the frequency of interventions, aimed at the restoration of coronary blood flow.

Does not increase the risk of death or development of complications and deaths in patients with 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 CHF (III-IV functional class by classification NYHA) non-ischemic etiology in the use of amlodipine, there is a possibility of pulmonary edema.

Pharmacokinetics:

After ingestion, amlodiene is slowly absorbed from the gastrointestinal tract (GIT). The mean absolute bioavailability is <64%, the maximum concentration (C_m_Oh) in the serum is observed after 6-9 hours. The equilibrium concentrations (C_ss) 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 is subject to a slow but active metabolism in the liver in the absence of a significant effect of "primary passage. "Metabolites do not have a significant pharmacological activity. After a single administration, the elimination half-life (T_1/2) varies from 35 to 50 hours, with reuse T_1/2 is approximately 45 hours. About 60% of the adopted inside the dose is excreted, by the kidneys mainly in the form of metabolites, 10% - in unchanged form, and 20-25% - through the intestines with bile. 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_1/2is 65 hours) compared with young patients, but this difference has no clinical significance. Elongation T_1/2 in patients with hepatic insufficiency suggests that with prolonged use, cumulation of the drug in the body will be higher (T_1/2 - up to 60 hours). Renal failure does not significantly affect the kinetics of amlodipine. 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. When hemodialysis is not removed.

Indications:

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

Stenocardia of tension, vasospastic angina (Prinzmetal angina)

Contraindications:

Hypersensitivity to amlodipine and other dihydropyridine derivatives or other components of the drug;
severe arterial hypotension (systolic blood pressure less than 90 mm Hg);
cardiogenic shock, collapse;
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;
age to 18 years (efficacy and safety not established).

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, impaired renal function.

Pregnancy and lactation:

In experimental studies fetotoxic and embryotoxic action the drug is not established, but use in pregnancy is possible only if the benefit to the mother exceeds the potential risk to the fetus.

There is no evidence of excretion of amlodipine in breast milk. However, it is known that other BCCC - dihydropyridine derivatives are excreted in breast milk. In this connection, if it is necessary to prescribe the drug Amlong during lactation, the question of stopping breastfeeding should be solved.

Dosing and Administration:

Inside, once a day, washing down with the necessary amount of water (100 ml).

With arterial hypertension and angina, the initial dose is 5 mg 1 time per day. If there is no therapeutic effect for 2-4 weeks, the dose may be increased up to 10 mg / day once.

Have elderly patients

Correction of the dose is not required.

Have patients with impaired liver function

Although T_1/2 Amlodipine, like all BCCCs, is increased in patients with impaired liver function, dose adjustment is usually not required (see section "Special instructions").

Have patients with renal insufficiency

It is recommended to use Amlong in usual doses (see section "Special instructions").

There is no need for dose changes with simultaneous administration with thiazide diuretics, beta-blockers and angiotensin-converting enzyme (ACE) inhibitors.

Side effects:

The frequency of adverse reactions listed below was determined according to the following (World Health Organization classification):

very often - not less than 10%; often - not less than 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 reports.

From the central nervous system: often - headache (especially at the beginning of treatment), dizziness, fatigue, drowsiness; infrequent - general malaise, hypoesthesia, asthenia, paresthesia, peripheral neuropathy, tremor, insomnia, emotional lability, unusual dreams, nervousness, increased excitability, depression, anxiety, increased sweating; rarely - cramps, apathy, agitation; very rarely - ataxia, amnesia.

From the digestive system: often - nausea, pain in the abdomen; infrequent - vomiting, changing the mode of defecation (including constipation, flatulence), dyspepsia, diarrhea, anorexia, dryness of the oral mucosa, thirst; rarely - gingival hyperplasia, increased appetite; very rarely - pancreatitis, gastritis, jaundice (usually cholestatic), hyperbilirubinemia, increased activity of "hepatic" transaminases, hepatitis.

From the cardiovascular system: often - peripheral edema (ankles and feet), a feeling of palpitations, "hot flashes" of blood to the skin of the face; infrequently - excessive reduction of blood pressure, orthostatic hypotension, vasculitis; rarely - development or aggravation of the course of CHF; very rarely - fainting, shortness of breath,heart rhythm disturbances (including bradycardia, ventricular tachycardia and atrial fibrillation), myocardial infarction, chest pain, pulmonary edema.

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

From the urinary system: infrequently - pollakiuria, painful urge to urinate, nocturia; very rarely - dysuria, polyuria.

On the part of the reproductive system and mammary glands: infrequently - gynecomastia, impotence.

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

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

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

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

From the sense organs: infrequent - ringing in the ears, impaired vision, diplopia, disruption of accommodation, xerophthalmia, conjunctivitis, pain in the eyes; very rarely - parosmia.

From the side of metabolism: very rarely - hyperglycemia.

Other: infrequently - weight loss, weight gain, taste distortion, epistaxis, chills.

Overdose:

Symptoms: 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 legal outcome).

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 heart and lung function, monitoring the volume of circulating blood (BCC) 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 be safely used for the therapy of arterial hypertension along with thiazide diuretics, alpha-adrenoblockers or ACE inhibitors. In patients with stable angina pectoris amlodipine can be combined with other antianginal agents, for example, with nitrates of prolonged or short-acting.

Unlike other BCCC, clinically significant interaction of amlodipine was not detected with simultaneous use with non-steroidal anti-inflammatory drugs (NSAIDs), including indomethacin. It is possible to intensify the anti-anginal and antihypertensive effects of BCCK with simultaneous use with thiazide and loop diuretics, inhibitors - ACE and nitrates, as well as enhance their antihypertensive action with simultaneous use with alpha 1-adrenoblockers.

Erythromycin in a joint application increases C_m_Oh Amlodipine 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 in the study of amlodipine, a negative inotropic effect was usually not observed, nevertheless, some BCCCs can enhance the severity of the negative inotropic effect of antiarrhythmics means elongating the interval Q-T (eg, amiodarone and quinidine).

A single dose of 100 mg of sildenafil in patients with arterial hypertension does not affect the pharmacokinetics 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 at a single and repeated application in a dose of 10 mg does not affect the pharmacokinetics of ethanol.

Antiviral drugs (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.

With the simultaneous use of amlodipine with lithium preparations, an increase in the manifestation of neurotoxicity (nausea, vomiting, diarrhea, ataxia, tremor, and tinnitus) is possible. Amlodipine does not change the pharmacokinetics of cyclosporine.

Does not affect the concentration of serum digoxin and its renal clearance.

He has a significant effect on the effect of warfarin (prothrombin time). Cimetidine does not affect the pharmacokinetics of amlodipine.

In studies in vitro Amlodipine does not affect the binding of blood proteins to digoxin, phenytoin, warfarin and indomethacin.

Grapefruit juice: simultaneous single intake of 240 mg of grapefruit juice and 10 mg of amlodipine by mouth is not accompanied by a significant change 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 therapy with Amlong, it is necessary to control body weight and consumption of table salt, the purpose of the appropriate diet is indicated.

It is necessary to maintain oral hygiene and supervision at the dentist (to prevent soreness, bleeding and gingival hyperplasia).

When using the drug, Amlong in patients with chronic heart failure III and IV functional class by classification NYIIA possibly the development of pulmonary edema.

In acute myocardial infarction, Amlong is appointed after stabilization of hemodynamic parameters (see section "Contraindications").

Patients with hepatic insufficiency, if necessary to take the drug Amlong should be under the supervision of a doctor.

In elderly patients may increase T_1/2 and decrease the clearance of the drug.

Dose changes are not required, but more careful monitoring of patients of this category is necessary.

Patients with low body weight, patients of low height and patients with severe - impaired liver function may need a smaller dose of the drug.

In patients with impaired renal function, monitoring of the condition is necessary. The efficacy and safety of Amlong hypertensive crisis is not established.

Despite the absence of the "cancellation" syndrome in BCC, it is advisable to stop the treatment with Amlong, gradually reducing the dose of the drug.

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

Although the intake of Amlong any negative effect on the ability to drive vehicles or other complex mechanisms were observed, however, due to the possible excessive reduction in blood pressure, development of dizziness, drowsiness and other side effects, caution should be exercised in these situations, especially at the beginning of treatment and with increasing dose.

Form release / dosage:

Tablets of 5 and 10 mg.

Packaging:For 10 tablets of 5 mg and 10 mg in an aluminum strip.

1 strip, 3 strips or 10 strips together with instructions for use in a cardboard box (for both dosages).

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:30 months. Do not use after the time specified on the package.

Terms of leave from pharmacies:On prescription

Registration number:LS-001987

Date of registration:30.11.2011

Expiration Date:Unlimited

The owner of the registration certificate:Micro Labs LimitedMicro Labs Limited India

Manufacturer: & nbsp

MICRO LABS, Limited India

Representation: & nbspMICRO LABS LIMITED MICRO LABS LIMITED India

Information update date: & nbsp25.07.2017

Illustrated instructions

Instructions

Amlong (Amlong)