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

Active ingredient: amlodipine (in the form of amlodipine besylate 6,944 mg) 5 mg; Excipients: magnesium stearate - 2,000 mg, sodium carboxymethyl starch - 4,000 mg, calcium hydrophosphate - 63,000 mg, microcrystalline cellulose - 124, 056 mg.

1 tablet of 10 mg contains:

Active ingredient: amlodipine (in the form of amlodipine besylate 13.889 mg) 10 mg; Excipients: magnesium stearate - 4,000 mg, sodium carboxymethyl starch - 8,000 mg, calcium hydrophosphate - 126,000 mg, microcrystalline cellulose - 284.111 mg.

Description:

Tablets 5 mg: white or almost white biconvex tablets oblong-rounded with an engraving "5" on one side

Tablets 10 mg: white or almost white biconvex tablets oblong-rounded with an engraving "10" on one side andrisk to another.

Pharmacotherapeutic group:blocker of "slow" calcium channels

ATX: & nbsp

C.08.C.A.01 Amlodipine

Pharmacodynamics:Amlodipine - a derivative of dihydropyridine, a blocker of "slow" calcium channels of the second generation, has a high selectivity for receptors of the vascular wall. As a peripheral vasodilator has antianginal and hypotensive effect. As a result of selective binding with dihydropyridine receptors and blocking of calcium channels, it reduces the over-membrane transport of calcium ions to cardiomyocytes and smooth muscle cells of vessels (the effect on the smooth muscles of the vessels is more pronounced). Anti-ischemic, antianginal action is due to the expansion of peripheral and coronary arteries and arterioles. Reducing the overall peripheral vascular resistance, reduces afterload on the heart, reduces the need for myocardium in oxygen, prevents the constriction of the coronary arteries (including caused by smoking) and restores blood circulation in them, increases oxygen supply to the myocardium (especially with the vasospastic form of angina).With angina, the daily dose increases exercise tolerance: it slows the development of an anginal attack and the formation of an ischemic depression of the segment ST, reduces the incidence of angina attacks and the need for nitroglycerin. With angina that flows normal arterial pressure, does not cause a significant change in blood pressure (BP). Hypotensive the effect is due to a direct vasodilatory effect on the smooth muscle of the vessels, and is dose-dependent. With arterial hypertension, a single dose of amlodipine provides a continuous decrease in blood pressure (for 24 hours) in the patient's position while lying and standing. Reduction of blood pressure in a clinically significant degree is not accompanied by a reflex increase in heart rate (heart rate) and the level of catecholamines in the blood. In connection with the gradual development of the effect (2-4 hours) does not cause a sharp decrease in blood pressure and orthostatic hypotension. Does not cause a decrease in the fraction of the ejection of the left ventricle and exercise tolerance. Reduces the degree of myocardial hypertrophy of the left ventricle, has antiatherosclerotic and cardioprotective effects in coronary heart disease.Does not affect the contractility and conductance of the myocardium, prevents platelet aggregation, increases the rate of glomerular filtration, has a weak natriuretic effect. With diabetic nephropathy does not increase microalbuminuria. It has no adverse effect on metabolism, lipid and blood glucose levels.

Pharmacokinetics:

Absorbability: When ingested slowly and almost completely absorbed from the gastrointestinal tract. Eating does not affect absorption. The maximum concentration in blood plasma is achieved in 6-12 hours, both in the elderly and in young patients. The stage of saturation in the plasma occurs after 7-14 days of treatment. Bioavailability of 63-80%.

Distribution: The volume distribution of 21 l / kg, indicating a prevalent distribution in the tissues. Relationship with plasma proteins 97%. Penetrates through the blood-brain barrier and into breast milk.

Metabolism: ~ 90% biotransformed in the liver with the formation of inactive metabolites.

Excretion: with urine output 10% unchanged and 60% - in the form of metabolites, 20-25% - with feces in the form of metabolites. Excretion of a two-phase, average half-life of 35-50 h.The total clearance of amlodipine is 7 ml / min / kg. When hemodialysis is not removed.

In elderly patients (over 65 years) and with chronic heart failure of moderate to severe severity, the clearance of amlodipine decreases, followed by a 40-60% increase in the area under the concentration / time curve (AUC), which requires the appointment of lower initial doses of amlodipine. A similar change AUC there is also a violation of liver function.

Renal failure does not significantly affect the kinetics of amlodipine.

Indications:

Treatment of arterial hypertension - as a monotherapy or in combination with other antihypertensive agents: thiazide diuretics, beta-adrenoblockers or ACE inhibitors.

Treatment of angina pectoris, vasospastic angina pectoris (Prinzmetal angina) - as a monotherapy or in combination with other antianginal agents, including in the case of refractory to nitrates and (or) beta-blockers.

Contraindications:

Hypersensitivity to amlodipine or other dihydropyridine derivatives; severe arterial hypotension; collapse,cardiogenic shock; clinically pronounced aortic stenosis; unstable angina (with the exception of Prinzmetal's stenocardia); pregnancy (due to lack of clinical experience in the application); lactation period (safety of use not established); age to 18 years (due to lack of relevant clinical experience).

Carefully:

abnormal liver function; syndrome of weakness of the sinus node (pronounced bradycardia, tachycardia), decompensated chronic heart failure; slight or moderate degree of arterial hypotension; mitral stenosis; hypertrophic obstructive cardiomyopathy; acute myocardial infarction (and within a month after it); elderly age.

Pregnancy and lactation:Contraindicated.

Dosing and Administration:

Take in, once a day. Normodipine can be prescribed as a monotherapy or in combination with other antihypertensive agents (thiazide diuretics, β-blockers and ACE inhibitors) nitrates.

With arterial hypertension and angina the usual initial dose of 5 mg once a day. The maximum daily dose of 10 mg, once a day.Usually, to assess the clinical effect requires 7-14 days of treatment.

With arterial hypertension, the maintenance dose may be 5 to 10 mg per day.

For angina pectoris and vasospastic angina, 5-10 mg per day.

When renal failure a dose change is not required; Amlodipine concentration in the blood plasma does not depend on the degree of decrease in kidney function.

Side effects:

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

From the digestive system: nausea; pain in epigastrium; very rarely - jaundice, increased level of hepatic transaminases; dyspepsia; gingival hyperplasia;

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

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

From the skin and skin: rarely erythema multiforme; angiodema; very rarely - dry skin, alopecia, dermatitis, purpura, discoloration of the skin;

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

Other: impaired vision; diplopia; gynecomastia; hypoglycemia.

Overdose:

Symptoms: excessive peripheral vasodilation; marked and prolonged decrease in arterial pressure, reflex tachycardia.

Treatment: gastric lavage, the appointment of activated charcoal, sublime the position of the limbs, the maintenance of cardiovascular function with the replenishment of the fluid volume, if necessary, monitoring the parameters of heart and lung function, the volume of circulating blood and diuresis.If the above measures are inadequate and if there are no contraindications - the use of vasopressive drugs; intravenous administration of calcium gluconate to eliminate blockade of calcium channels. Because the Amlodipine is largely associated with blood plasma proteins - 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.

Anti-inflammatory drugs, non-steroidal anti-inflammatory drugs, especially indomethacin (causing sodium retention and blocking the synthesis of renal prostaglandins), a-adrenostimulants, estrogens (sodium retention), sympathomimetics reduce the hypotensive effect.

Thiazide and loop diuretics, β-adrenoblockers, verapamil, ACE inhibitors and nitrates increase antianginal and hypotensive effects.

Amiodarone, quinidine, a1-adrenoblockers, neuroleptics and blockers of "slow" calcium channels can increase the hypotensive effect.

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 has no significant effect on the pharmacokinetics of amlodipine.

Cimetidine does not affect the pharmacokinetics of amlodipine.

Amlodipine has no effect on the association of digoxin and warfarin, phenytoin and indomethacin with plasma proteins.

Does not change the effect of warfarin on prothrombin time.

Does not affect the action of antibiotics, nitrates and hypoglycemic agents.

Special instructions:

It is important to comply with the basic principles of treatment of hypertension, concerning the limitation of sodium intake and the need for control over body weight.

During treatment, oral hygiene and periodic examination at the dentist are necessary because of the possible development of soreness, bleeding and gingival hyperplasia.

Amlodipine does not affect plasma concentrations of K⁺, glucose, triglycerides, total cholesterol, LDL, uric acid, creatinine and uric acid nitrogen.

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

As follows from clinical experience, it is unlikely that amlodipine can influence the the abilities necessary for driving and working mechanisms. However, patients should be alerted to the possibility of developing side effects such as drowsiness and dizziness, especially in the initial treatment period. The development of such side effects is a contraindication to driving and working machines.

Form release / dosage:

Tablets, 5 mg and 10 mg.

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

Storage conditions:

At a temperature of no higher than 30 ° C. Keep out of the reach of children!

Shelf life:

3 years.

Do not use after the expiration date printed on the package.

Terms of leave from pharmacies:On prescription

Registration number:П N012274 / 01

Date of registration:15.03.2010

The owner of the registration certificate:GEDEON RICHTER, OJSC GEDEON RICHTER, OJSC Hungary

Manufacturer: & nbsp

GEDEON RICHTER-RUS, CJSC Russia

Representation: & nbspGEDEON RICHTER OJSC GEDEON RICHTER OJSC Hungary

Information update date: & nbsp11.02.2014

Illustrated instructions

Instructions

Normodipine® (Normodipine®)