Amlocard-Sanovel - instructions for use, dose, side effects, contraindications

Excipients: cellulose microcrystalline 124,065 mg / 248,13 mg, calcium phosphate dihydrate 63 mg / 126 mg, sodium carboxymethyl starch 4 mg / 8 mg, magnesium stearate 2 mg / 4 mg.

Description:

Round biconvex tablets are white or almost white with a risk on one side.

Pharmacotherapeutic group:The blocker of "slow" calcium channels

ATX: & nbsp

C.08.C.A.01 Amlodipine

Pharmacodynamics:

The dihydropyridine derivative blocking the "slow" calcium channels of the second generation, has an antianginal and hypotensive effect. Linking with dihydropyridine receptors blocks calcium channels,reduce 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, reduces preload on the heart, reduces the need for myocardium in oxygen. Expanding the main 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 constriction of the coronary arteries (including caused by smoking). In patients with angina, a single daily dose increases the time of exercise, slows the development of angina and "ischemic" depression of the segment ST, reduces the incidence of angina attacks and consumption of nitroglycerin.

Has a long-term dose-dependent hypotensive effect. The hypotensive effect is due to a direct vasodilating effect on smooth muscle vessels. When arterial hypertension, a single dose provides a clinically significant reduction in blood pressure (BP) for 24 hours (in the patient's position "lying" and "standing"). Does not cause a sharp decrease in blood pressure, a decrease in exercise tolerance, a fraction of the ejection of the left ventricle. Reduces the degree of myocardial hypertrophy of the left ventricle, has antiatherosclerotic and cardioprotective action in ischemic heart disease (CHD). Does not affect the contractility and conductance of the myocardium, does not cause a reflex increase in the 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 adverse effects on the metabolism and lipids of blood plasma. The time of onset of the effect is 2-4 hours, the duration of the effect is 24 hours.

Pharmacokinetics:

After oral administration amlodipine slowly absorbed from the gastrointestinal tract. The average absolute bioavailability is 64%, the maximum concentration in the serum is observed concentration is achieved after 7 days of therapy.

Food 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 relatively less in the blood. Most of the drug in the blood (95%), binds to blood plasma proteins. Amlodipine is subjected to a slow but extensive metabolism (90%) in the liver with the formation of inactive metabolites, has the effect of a "first pass" through the liver. Metabolites do not have significant pharmacological activity.

After a single oral intake, the half-life (T_1/2) varies from 31 to 48 hours, with a reappointment of approximately 45 hours. About 60% of the ingested dose is excreted urine mainly in the form of metabolites, 10% unchanged, and 20-25% with feces, as well as breast milk. 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, but this difference is not of clinical significance. In patients with hepatic insufficiency, an extension T_1/2 and with a prolonged appointment, the cumulation of the drug in the body will be higher (T_1/2 up to 60 hours). Renal Insufficiency does not have a significant impact on kinetics of amlodipine. The drug penetrates the blood-brain barrier. When hemodialysis is not removed.

Indications:

Arterial hypertension (monotherapy or in combination with other antihypertensive agents).
Stenocardia of tension, vasospastic angina (Prinzmetal angina)

Contraindications:

Pincreased sensitivity to amlodipine and other dihydropyridine derivatives;
severe arterial hypotension;
collapse, cardiogenic shock;
unstable angina (with the exception of Prinzmetal angina)
pregnancy and lactation;
age to 18 years (efficacy and safety not established).

Carefully:

Dysfunction of the liver, syndrome of weakness of the sinus node (severe bradycardia, tachycardia), chronic heart failure in the stage of decompensation, mild or moderate degree of arterial hypotension, aortic stenosis, mitral stenosis, hypertrophic obstructive cardiomyopathy, acute myocardial infarction (and within 1 month after), diabetes mellitus, lipid profile disorder, elderly age.

Pregnancy and lactation:Contraindicated.

Dosing and Administration:

Inside, the initial dose for the treatment of hypertension is 5 mg of the drug once a day. The maximum dose can be increased to 10 mg once a day. With hypertension, the maintenance dose can be 5 mg per day.

With angina pectoris, vasospastic angina pectoris - 5-10 mg per day, once.

Not required dose changes with concomitant administration with thiazide diuretics, beta-adrenoblockers and angiotensin-converting enzyme (ACE) inhibitors.

Do not require dose changes in patients with renal insufficiency.

Side effects:

From the cardiovascular system: palpitations, dyspnea, marked decrease in blood pressure, fainting, vasculitis, peripheral edema (swelling of the ankles and feet), "tides" of blood to the face, rarely - rhythm disturbances (bradycardia, ventricular tachycardia, atrial flutter), myocardial infarction, chest pain, orthostatic hypotension, very rarely - development or aggravation of heart failure, extrasystole, migraine.

From the central nervous system: headache, dizziness, fatigue, drowsiness, change mood, cramps, rarely - loss of consciousness, hypoesthesia, nervousness, paresthesia, peripheral neuropathy, tremor, vertigo, asthenia, malaise, insomnia, depression, anxiety, unusual dreams, very rarely - ataxia, apathy, agitation, amnesia.

From the digestive system: nausea, vomiting, epigastric pain, rarely - increased levels of "liver" transaminases and jaundice (caused by cholestasis), pancreatitis, dry mouth, hepatitis, flatulence, gingival hyperplasia, constipation or diarrhea, anorexia, very rarely gastritis, increased appetite.

From the genitourinary system: rarely - pollakiuria, painful urge to urinate, nocturia, violation of sexual function (including a decrease in potency); very rarely - dysuria, polyuria.

From the skin: very rarely - xeroderma, alopecia, dermatitis, purpura, discoloration.

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

From the musculoskeletal system: rarely - arthralgia, muscle cramps, arthrosis, myalgia (with prolonged use); very rarely - myasthenia gravis.

Other: rarely - alopecia, gynecomastia, hyperuricemia, increase / decrease in weight body, thrombocytopenia, leukopenia, thrombocytopenic purpura, hyperglycemia, impaired vision, diplopia, conjunctivitis, eye pain, tinnitus, back pain, dyspnoea, epistaxis, increased sweating, thirst; very rarely - cold sticky sweat, cough, rhinitis, parosmia, taste disorders, accommodation disorder, xerophthalmia.

Overdose:

Symptoms: a marked decrease in blood pressure, tachycardia, excessive peripheral vasodilation.

Treatment: gastric lavage, the appointment of activated carbon to maintain the function of the cardiovascular system, the control performance of the heart and lungs, an elevated position of the limbs, control of blood volume and diuresis. To restore the vascular tone - the use of vasoconstrictive drugs (in the absence of contraindications to their use); to eliminate the effects of calcium channel blockade - intravenous calcium gluconate. Hemodialysis is not effective.

Interaction:

Inhibitors of microsomal oxidation increase the concentration of amlodipine in the blood plasma, increasing the risk of side effects, and inductors of microsomal liver enzymes reduce.

Hypotensive effect weakens non-steroidal anti-inflammatory drugs, especially indomethacin (sodium retention and synthesis blockade prostaglandins with kidneys), alpha-adrenostimulants, estrogens (sodium retention), sympathomimetics.

Thiazide and "loop" diuretics, beta-blockers, verapamil, ACE inhibitors and nitrates increase antianginal and antihypertensive effects.

Amiodarone, quinidine, alpha 1-adrenoblockers, antipsychotic medicines (antipsychotics) and blockers of "slow" calcium channels can intensify the hypotensive effect.

Does not affect the pharmacokinetic parameters of digoxin and warfarin. Cimetidine does not affect the pharmacokinetics of amlodipine.

When combined with preparations of lithium may be increased manifestations of neurotoxicity (nausea, vomiting, diarrhea, ataxia, tremor, tinnitus).

Calcium preparations can reduce the effect of blockers of "slow" calcium channels.

Procainamide, quinidine and other drugs that cause lengthening of the interval QT, reinforce the negative inotropic effect and may increase risk of significant lengthening of the interval QT.

Grapefruit juice can reduce the concentration of amlodipine in the blood plasma, but this decrease is so small that it does not significantly alter the effect of amlodipine.

Special instructions:

During the period of treatment, it is necessary to control the body weight and sodium intake, the appropriate diet.

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

Dosage regimen for the elderly is the same as for patients of other age groups. When increasing the dose, careful monitoring of elderly patients is necessary.

Despite the lack of "slow" calcium channels of the syndrome of "cancellation" in blockers, before the cessation of treatment it is recommended to gradually reduce the dose.

Amlodipine does not affect the plasma concentrations of potassium ions, glucose, triglycerides, total cholesterol, LDL, uric acid, creatinine and urea nitrogen.

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

There were no reports of the effects of amlodipine on driving or working with machinery. However, some patients may experience drowsiness and dizziness at the beginning of treatment. When they occur, the patient should refrain from driving and working with machinery.

Form release / dosage:

Tablets 5 mg, 10 mg.

Packaging:For 10 tablets in a blister of PVC-aluminum foil. For 3 blisters in a cardboard pack together with instructions for use.

Storage conditions:

In a dry 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 date shown on the package.

Terms of leave from pharmacies:On prescription

Registration number:LSR-000271/09

Date of registration:19.01.2009 / 02.11.2016

Expiration Date:Unlimited

The owner of the registration certificate:Sanovel Pharmaco-industrial trading companySanovel Pharmaco-industrial trading company Turkey

Manufacturer: & nbsp

SANOVEL PHARMACEUTICAL PRODUCTS IND., Inc. Turkey

Representation: & nbspSANOVEL branch of the company pharmaco-industrial trading companySANOVEL branch of the company pharmaco-industrial trading companyRussia

Information update date: & nbsp25.07.2017

Illustrated instructions

Instructions

Amlocard-Sanovel (Amlokard-Sanovel)