Amlodipine-Biocom - instructions for use, dose, side effects, contraindications

Excipients: lactose monohydrate (sugar milk) 0.07953 g or 0.11619 g, potato starch 0.00058 g or 0.00084 g, pregelatinized starch 0.00895 g or 0.01308 g, magnesium stearate 0,001 g or 0 , 0015 g, croscarmellose, sodium (impellose) - 0.003 g or 0.0045 g.

Description:

Tablets are white or white with a yellowish hue of color, flat-cylindrical with a bevel.

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 hypotensive effects. Linking to the segment S6 III and IV domains of alpha-1 subunit of the calcium channel Ltype, blocks calcium channels, reduces the transmembrane transition of Ca²⁺ in the cell (mostly in the smooth muscle cells of the vessels, than in the cardiomyocytes). Has hypotensive and antianginal effect.

The mechanism of hypotensive action of amlodipine is due to a direct relaxing effect on the smooth muscles of the vessels.

Reduction of myocardial ischemia occurs due to the expansion of coronary and peripheral arteries and arterioles in unchanged and in ischemic zones of the myocardium, reduction of total peripheral vascular resistance, decrease in postnagruzka, myocardial oxygen demand.

Increases oxygen supply to the myocardium in patients with vasospastic angina (Prinzmetal angina); prevents the development of coronarospasm caused by smoking. In patients with angina, a single daily dose increases the time of exercise, delays the development of another attack of angina and depression of the segment S-T (by 1 mm) with physical activity, reduces the frequency of angina attacks and consumption of nitroglycerin.

Has a long-term dose-dependent hypotensive effect.Hypotensive effect is caused by a direct vasodilating effect on the smooth muscles of the vessels. When hypertension single daily dose provides a clinically significant decrease in blood pressure (BP) for 24 hours (in the position of the patient "lying" and "standing").

Patients with diseases of the cardiovascular system (including coronary atherosclerosis lesion with one vessel to the stenosis and 3 or more arteries, carotid atherosclerosis), myocardial infarction (MI), percutaneous transluminal angioplasty of coronary arteries, or in patients with angina pectoris. Use of amlodipine prevents intima-media thickening of carotid arteries, reducing mortality from myocardial infarction, stroke, transluminal angioplasty, coronary artery bypass surgery; leads to a decrease in the number of hospitalizations for unstable angina and the 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 development of complications and deaths in patients with CHF (III-IV Functional class according to the classification of the New York Heart Association (NYHA)) on the background of therapy with digoxin, diuretics and angiotensin-converting enzyme (ACE) inhibitors. In patients with CHF (III)-IV functional class for tolassification NYHA) non-ischemic etiology in the use of amlodipine, there is a possibility of pulmonary edema.

Does not cause a sharp decrease in blood pressure, a decrease in exercise tolerance, a fraction of the release of the left ventricle (LV). Reduces the degree of myocardial hypertrophy of the LV.

Does not affect the contractility and conductance of the myocardium, does not cause a reflex increase in the heart rate, 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 adverse effects on the metabolism and plasma lipids.

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

Pharmacokinetics:

Absorption is slow, does not depend on food intake; is about 90%; bioavailability is 60-65%. The maximum concentration in the blood (TSmah) with oral intake is achieved, after 6-12 hours With constant "intake of stationary concentration in the blood" (Css) is created in 7-8 days. The volume of distribution is 21 l / kg. The connection with plasma proteins is 90-97%. Penetrates through the blood-brain barrier.

Intensively (90%) is metabolized in the liver with the formation of inactive metabolites, has the effect of "primary transmission" through the liver. Half-life (T_1/2) an average of 35 hours. The total ground clearance is 500 ml / min.

T_1/2 in patients with arterial hypertension - 48 hours, in elderly patients increases to 65 hours, with liver failure - up to 60 hours, similar magnification parameters T_1/2 are observed and with severe CHF, with a violation of kidney function - does not change. When hemodialysis is not removed.

It is excreted by the kidneys - 60% in the form of metabolites, 10% in unchanged form; with bile and through the intestine - 20-25% in the form of metabolites, as well as with breast milk.

Indications:

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

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

Contraindications:

- Hypersensitivity to amlodipine, other dihydropyridine derivatives and other components of the drug (the formulation includes lactose monohydrate);

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

- unstable angina (with the exception of Prinzmetal's stenocardia);

- clinically significant aortic stenosis;

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

- pregnancy and lactation.

Carefully:

Arterial hypotension, aortic stenosis; CHF of non-ischemic etiology (III-IV functional class by classification NYHA), mitral stenosis, hepatic insufficiency, acute myocardial infarction (and within 1 month after), hypertrophic obstructive cardiomyopathy, sinus node weakness syndrome, elderly age.

Pregnancy and lactation:

The safety of the use of amlodipine in pregnancy is not established, so 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 with breast milk. In connection with this, if it is necessary to prescribe Amlodipine during the period lactation should resolve the issue of stopping breastfeeding.

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 once a day. If necessary, the daily dose can be increased to 10 mg, at one time.

Have elderly patients

Amlodipine is recommended for use in an average therapeutic dose, dose adjustment is not required.

Have patients with impaired liver function

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

In patients with renal insufficiency

It is recommended that Amlodipine in normal doses, but it is necessary to take into account the possible slight increase T_1/2.

No dosage adjustment is required for simultaneous administration with thiazide diuretics, beta-blockers and ACE inhibitors.

Side effects:

The frequency of adverse reactions listed below was determined according to the following (World Health Organization classification): very often more than 1/10, often from more than 1/100 to less than 1/10, infrequently from more than 1/1000 to less than 1/100 , rarely from more than 1/10000 to less than 1/1000, very rarely from less than 1/10000, including individual messages.

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

From the digestive system: often - nausea, pain in the abdomen; 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.

From the cardiovascular system: often - palpitations, peripheral edema (ankles and feet), "hot flashes" of blood to the skin of the face; infrequent reduction of blood pressure; very rarely - fainting, shortness of breath, vasculitis, orthostatic hypotension, development or exacerbation of current CHF, cardiac arrhythmias (including bradycardia, ventricular tachycardia and atrial fibrillation), heart attack, chest pain.

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

From the genitourinary system: infrequently - frequent urination, painful urination, nocturia, impotence; very rarely - dysuria, polyuria.

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 gravis.

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

Allergic reactions: skin itching, rash (including erythematous, maculopapular rash, urticaria), angioedema, erythema multiforme.

Other: infrequent - ringing in the ears, diplopia, accommodation disorder, xerophthalmia, conjunctivitis, eye pain, chills, nosebleeds, gynecomastia; very rarely - parosmia, hyperglycemia.

Overdose:

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

Treatment: gastric lavage, appointment of activated carbon (especially in the first 2 hours after the overdose), maintaining the function of the cardiovascular system, raised position the lower extremities, monitoring parameters of the heart and lungs, control blood volume 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 thiazidediuretics, alpha-adrenoblockers, beta-blockers or 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, beta-blockers.

In contrast to other BCCC, the clinically significant interaction of amlodipine (III generation BCCI) was not detected when combined with non-steroidal anti-inflammatory drugs, including indomethacin.

It is possible to strengthen the anti-anginal and hypotensive action of BCCC when combined with thiazide and loop diuretics, ACE inhibitors, beta-blockers and nitrates, as well as enhance their hypotensive effect when combined with alpha1-adrenoblockers, neuroleptics.

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

A single dose of 100 mg of sildenafil in patients with essential 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 hypotensive effect 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 concentration of serum 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 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 inwards is not accompanied by a significant change in the pharmacokinetics of amlodipine.

Aluminum- or magnesium-containing - antacids: they do not have a single dose, a significant effect on the pharmacokinetics of amlodipine.

Special instructions:During the period of therapy with the drug Amlodipine-Biocom it is necessary to control body weight and sodium intake, the purpose of the appropriate diet is indicated.

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

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, low growth patients and patients with severe liver function impairment may need a smaller dose of the drug.

The efficacy and safety of the use of Amlodipine-Biocoma in hypertensive crisis is not established.

Despite the absence of the "cancellation" syndrome in BCC, it is desirable to stop the treatment with Amlodipine-Biocome, gradually reducing the dose of the drug.

Effect on the ability to drive transp. cf. and fur:Amlodipine was not adversely affected by the ability to control motor vehicles or other complex mechanisms, however, due to possible excessive blood pressure lowering, development of dizziness, drowsiness and other adverse reactions, caution should be exercised in these situations, especially at the beginning of treatment and increasing the dose.

Form release / dosage:

Tablets of 5 mg and 10 mg.

Packaging:For 10 or 12 tablets in a contour mesh package. By 1, 2, 3, 4, 5, 6 or 9 contour cell packs together with instructions for medical 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:

Shelf life 3 years.

Do not use the product after the expiry date printed on the package.

Terms of leave from pharmacies:On prescription

Registration number:LS-001969

Date of registration:21.09.2011 / 31.01.2013

Expiration Date:Unlimited

The owner of the registration certificate:BIOKOM, CJSC BIOKOM, CJSC Russia

Manufacturer: & nbsp

BIOKOM, CJSC Russia

Information update date: & nbsp09.08.2017

Illustrated instructions

Instructions

Amlodipine-Biocom (Amlodipine-Biocom)