NORMODYPYN

Active material: Amlodipine
When ATH: C08CA01
CCF: Kalьcievыh channel blocker
ICD-10 codes (testimony): I10, i20, I20.1
When CSF: 01.03.02
Manufacturer: GEDEON RICHTER Ltd. (Hungary)

PHARMACEUTICAL FORM, COMPOSITION AND PACKAGING

Pills white or nearly white, lenticular, oblong-rounded shape, Engraved “5” on one side.

Excipients: microcrystalline cellulose, calcium hydrogen phosphate, anhydrous, sodium carboxymethyl starch type A, magnesium stearate.

10 PC. – blisters (3) – packs cardboard.

Pills white or nearly white, lenticular, oblong-rounded shape, Engraved “10” on one side and Valium – another.

Excipients: microcrystalline cellulose, calcium hydrogen phosphate, anhydrous, sodium carboxymethyl starch type A, magnesium stearate.

10 PC. – blisters (3) – packs cardboard.

Pharmacological action

Calcium channel blocker slow, dihydropyridine derivative. It has a high selectivity for receptors of the vascular wall. As a peripheral vasodilator has antianginal and hypotensive action. As a result of selective communication with the dihydropyridine receptor and blocking calcium channels reduces chrezmembranny transport of calcium ions into cardiac myocytes and vascular smooth muscle cells (effect, exerted on the vascular smooth muscle, more pronounced).

Antiischemic, antianginal effect is due to expansion of the coronary and peripheral arteries and arterioles. Reducing PR, reduces cardiac afterload, reducing myocardial oxygen demand, It prevents the development of coronary artery spasm (incl. caused by smoking) and restores blood flow in them, increases myocardial oxygen supply (especially in vasospastic angina). In patients with angina daily dose increases exercise tolerance: slows down the development of anginal attack and the formation of ischemic ST-segment depression, reduces the frequency of angina attacks and need for nitroglycerin. Angina, flowing with normal blood pressure, it does not cause a significant change in.

The antihypertensive effect is due to the direct vasodilating effect on vascular smooth muscle, and is dose-dependent. When hypertension 1 dose Normodipina^® It provides continuous blood pressure reduction (for 24 no) with the patient lying down and standing up. Lowering blood pressure in a clinically significant degree it is not accompanied by a reflex increase in heart rate and catecholamine levels in the blood. Due to the gradual development of the effect (2-4 no) It does not cause a sharp decline in blood pressure and orthostatic hypotension.

It does not cause a decrease in left ventricular ejection fraction and exercise tolerance. Reduces the degree of left ventricular hypertrophy, It has anti-atherosclerotic and cardioprotective effect in ischemic heart disease. No effect on the myocardial contractility and conductivity, inhibits platelet aggregation, increases glomerular filtration rate, It has a weak natriuretic effect.

In diabetic nephropathy does not increase microalbuminuria. No adverse effects on metabolism, blood lipid and blood glucose.

Pharmacokinetics

Absorption

When administered slowly and almost completely absorbed from the gastrointestinal tract. Eating does not affect the absorption. C_max plasma levels achieved after 6-12 no, in older, and young patients. Bioavailability is 63-80%.

Distribution

C_ss amlodipine plasma levels achieved after continuous use for 7-14 days.

V_d approximately 21 l / kg, indicating the prevailing tissue distribution. Penetrates the GEB and breast milk.

Plasma protein binding – 97%.

Metabolism

About 90% amlodipine biotransformed in the liver with the formation of active metabolites.

Deduction

Amlodipine is excreted in the urine (10% dose – unedited, and 60% – active metabolites) and faeces (20-25% as metabolites). Withdrawal is a two-phase, T_1/2 averages 35-50 no. The total clearance of amlodilina 7 ml / min / kg. With hemodialysis amlodipine is not removed.

Pharmacokinetics in special clinical situations

In elderly patients (senior 65 years) and chronic heart failure, moderate and severe degrees of severity clearance of amlodipine decreases followed 40-60% increase in AUC, it requires the appointment of a low initial dose of amlodipine. Such a change in AUC observed with abnormal liver function.

The presence of renal failure patient has no significant effect on the pharmacokinetics of amlodipine.

Testimony

- Arterial hypertension (as monotherapy or in combination with thiazide diuretics, beta-blockers or ACE inhibitors);

- Stable angina (as monotherapy or in combination with other antianginal drugs, incl. patients, refractory to treatment with nitrates and / or beta-blockers);

- Angiospastic angina (Prinzmetal angina) (as monotherapy or in combination with other antianginal drugs, incl. patients, refractory to treatment with nitrates).

Dosage regimen

The drug is taken orally, 1 time / day. Normodypyn^® It can be administered as a single agent or in combination with other antihypertensive agents (thiazide diuretics, beta-blockers and ACE inhibitors) and nitrates.

At hypertension and angina starting dose is 5 mg 1 time / day. The maximum daily dose -10 mg 1 time / day. Usually to assess the clinical effect is required 7-14 days of treatment.

The maintenance dose is 5-10 mg / day.

At renal failure dose modification is not required, tk. amplodipina concentration in blood plasma does not depend on the degree of reduction of the kidney.

Side effect

Cardio-vascular system: heartbeat, breathlessness, marked reduction in blood pressure, fainting, vasculitis, swelling (swelling of the ankles and feet), flushing; rarely - cardiac arrhythmia (bradycardia, ventricular tachycardia, auricular flutter), chest pain, orthostatic hypotension; rarely – development or exacerbation of congestive heart failure, arrythmia, migraine.

From the digestive system: nausea, epigastric pain; very rarely - increased liver transaminases, jaundice, dyspepsia, giperplaziya right.

From the central and peripheral nervous system: headache, dizziness, fatigue, drowsiness, mood changes, blurred vision, diplopia; rare - loss of consciousness, giperesteziya, nervousness, paresthesia, tremor, vertigo, asthenia, malaise, insomnia, depression, unusual dreams; in rare cases - ataxia, apathy, ažitaciâ, amnesia.

From the urinary system: rarely - thamuria, dizurija, nocturia; in rare cases - polyuria.

On the part of the reproductive system: rarely – sexual dysfunction (incl. reduced potency), gynecomastia.

Allergic reactions: rarely – erythema multiforme, angioedema;

Dermatological reactions: very rarely - dry skin, alopecia, purpura, dermatitis, livor.

On the part of the musculoskeletal system: a rare - arthralgia, arthrosis, myalgia (prolonged use); very rarely - myasthenia gravis.

Other: gipoglikemiâ.

Contraindications

- Severe hypotension;

- Collapse;

- Cardiogenic shock;

- Symptomatic aortic stenosis;

- Unstable angina (except Prinzmetal angina);

- Pregnancy (due to lack of clinical experience on the use of);

- Lactation (safety have not been established);

- Up to 18 years (because of the lack of adequate clinical experience);

- Hypersensitivity to amlodipine and other dihydropyridine derivatives.

FROM caution It should appoint a drug in the human liver, SSS (vыrazhennaya bradycardia, tachycardia), chronic heart failure, decompensated, mild or moderate hypotension, mitral stenosis, hypertrophic obstructive cardiomyopathy, acute myocardial infarction (and for 1 months thereafter), elderly patients.

Pregnancy and lactation

The drug is contraindicated during pregnancy and lactation (breast-feeding).

Cautions

During treatment normodipin^® you must respect the basic principles of treatment of hypertension, restrictions on sodium intake and the need for weight control.

The patient should be informed of the need to comply with oral hygiene and periodic visit to the dentist to prevent soreness, krovotochivosti and giperplazii right.

Amlodipine has no effect on plasma concentrations of potassium, Glucose, triglycerides, total cholesterol, LDL, Uric acid, creatinine and uric acid nitrogen.

Effects on ability to drive vehicles and management mechanisms

As clinical experience, unlikely, that amlodipine may affect the ability of, necessary for driving and working mechanisms. However, patients should pay attention to the possibility of side effects such as drowsiness and dizziness, especially in the initial period of treatment. The development of such symptoms by a contraindication to driving and mechanisms.

Overdose

Symptoms: chrezmernaya perifericheskaya vasodilation, marked and prolonged decrease in blood pressure, reflex tachycardia.

Treatment: gastric lavage, appointment of activated carbon, elevated position limbs, control performance of the heart, light, OCK and diuresis, To maintain the function of the cardiovascular system with volume replacement if necessary. At insufficiency of the above measures and in the absence of contraindications – vazopressivnyh use drugs, in / with the introduction of calcium gluconate to remove calcium channel blockade. Because amlodipine largely bound to plasma proteins, Hemodialysis is not effective.

Drug Interactions

Inhibitors of microsomal oxidation increase the concentration of amlodipine in plasma (increasing the risk of side effects), and inducers of microsomal enzymes - reduce.

The hypotensive effect normodipin^® NSAIDs weaken, especially indomethacin (due to sodium retention and blockade of prostaglandin synthesis by the kidneys), alpha-adrenergic agonists, Estrogens (due to sodium retention), sympathomimetic.

And thiazide “loop” Diuretic, beta-blockers, verapamil, ACE inhibitors and nitrates increase antianginal and hypotensive effects normodipin^®.

Amiodarone, quinidine, alpha₁-adrenoblokatorы, neuroleptics, blockers of slow calcium channels may increase the hypotensive effects normodipin^®.

In an application with lithium may increase manifestations of neurotoxicity (nausea, vomiting, diarrhea, ataxia, tremor, noise in ears).

Calcium can decrease the effects of normodipin^®.

Prokaynamyd, quinidine and other drugs, causing prolongation of the QT interval, reinforce the negative inotropic effect and may increase risk of significant lengthening of the QT interval.

The pharmacokinetics of amlodipine is not changed while the appointment with cimetidine.

Amlodipine has no effect on the connection of digoxin and warfarin, and indomethacin phenytoin plasma proteins. It does not alter the effect of warfarin on prothrombin time.

Amlodipine has no effect on the action of antibiotics, nitrates and hypoglycemic agents.

Grapefruit juice has no significant effect on the pharmacokinetics of amlodipine.

Conditions of supply of pharmacies

The drug is released under the prescription.

Conditions and terms

The drug should be stored out of reach of children at temperature from 15 ° to 30 ° C. Storage life – 3 year.