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

active substance: Amlodipine besylate in terms of amlodipine - 5 mg and 10 mg; Excipients: calcium phosphate dihydrate, potato starch, sodium carboxymethyl starch (primogel), microcrystalline cellulose, silicon dioxide colloid (aerosil), magnesium stearate.

Description:

Tablets are white or white with a cream shade of color, a flat-cylindrical shape. Light marble is allowed.

Pharmacotherapeutic group:The blocker of "slow" calcium channels

ATX: & nbsp

C.08.C.A.01 Amlodipine

Pharmacodynamics:

The "slow" calcium channel blocker (BCCC), a dihydropyridine derivative, blocks "slow" calcium channels, reduces the transmembrane transition of calcium ions into the cell (mostly in the smooth muscle cells of the vessels, rather than in cardiomyocytes).

Has antianginal and hypotensive effect.

Reduces the severity of myocardial ischemia. Antianginal action is due to the expansion of coronary and peripheral arteries and arterioles: expanding peripheral arterioles, reduces the overall peripheral vascular resistance (OPSS), reduces afterload on the heart, thereby reducing 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 prismmetal vasospastic angina), prevents the development of spasm of the coronary arteries (including those caused by smoking). In patients with angina, a single daily dose of amlodipine increases the time of exercise, delays the development of an attack of angina and the "ischemic" depression of the segment ST with physical activity, reduces the incidence of angina attacks and the 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.With arterial hypertension, a single dose of amlodipine 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 fraction of the ejection of the left ventricle and a decrease in exercise tolerance. Reduces the degree of myocardial hypertrophy of the left ventricle, has a cardioprotective effect 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, inhibits platelet aggregation, increases the rate of glomerular filtration, has a weak natriuretic effect. When diabetic nephropathy does not increase the severity of microalbuminuria.

Patients with cardiovascular diseases (including coronary atherosclerosis with one vessel and up to stenosis of 3 or more arteries, carotid atherosclerosis) who underwent myocardial infarction, percutaneous transluminal angioplasty (TLC) of coronary arteries or patients with angina, use of amlodipine prevents the development of thickening of the intima-media of the carotid arteries,reduces mortality from myocardial infarction, stroke, pulmonary tuberculosis, aorto-coronary shunting; 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 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.

It does not adversely affect the metabolism and concentration of plasma lipids.

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

Pharmacokinetics:

After oral administration amlodipine is well absorbed (about 90%), food intake does not affect the absorption of amlodipine, absolute bioavailability is 64-80%. The time to reach the maximum concentration in the blood plasma is 6-9 hours.The average volume of distribution is 21 l / kg body weight. The connection with plasma proteins is about 97%. Penetrates through the blood-brain barrier. Equilibrium concentrations are achieved after 7-8 days of drug therapy. Amlodipine metabolized in the liver with the formation of inactive metabolites. Half-life (T_1/2) of the drug on average - 35-50 hours, which allows you to take the drug once a day. The total clearance is 500 ml / min. In patients with hypertension T_1/2 - 48 hours, in elderly patients (over 65 years) - increases to 65 hours, with liver failure - up to 60 hours, similar magnification parameters T_1/2 are observed in severe CHF. Disturbance of renal function does not significantly affect the kinetics of amlodipine.

About 60% of the dose is excreted by the kidneys in the form of inactive metabolites, 10% - unchanged; with bile and through the intestine - 20-25% in the form of metabolites.

When hemodialysis is not removed.

Indications:

- arterial hypertension (monotherapy or in combination with other antihypertensive drugs);

- stable exertional angina, vasospastic angina (Prinzmetal angina) (monotherapy or in combination with other antianginal agents).

Contraindications:

- hypersensitivity to amlodipine and / or other components of the drug, as well as to other dihydropyridine derivatives;

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

- unstable angina (Except for Prinzmetal angina pectoris

- age under 18 years (data on efficiency and safety are limited).

Carefully:

Arterial hypotension, impaired liver function, sinus node weakness syndrome (pronounced bradycardia, tachycardia), aortic stenosis, mitral stenosis, hypertrophic obstructive cardiomyopathy, acute myocardial infarction (and within 1 month after), CHF of non-ischemic etiology (III-IV functional class by classification NYHA), 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 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 Vero-amlodipine during the lactation period, the question of stopping breastfeeding should be solved.

Dosing and Administration:

Inside.

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.

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

Have elderly patients amlodipine recommend to use in an average therapeutic dose, dose adjustment is not required.

Have patients with impaired liver function dose adjustment is usually not required.

Have patients with renal insufficiency correction of the dose is not required.

Side effects:

Classification of adverse reactions according to the frequency of development: often (more than 1%), infrequently (0.1% - 1%), rarely (0.01% - 0.1%) and very rarely (less than 0.01%).

From the cardiovascular system: often - peripheral edema (swelling of the ankles and feet), a feeling of palpitations; infrequently - excessive reduction of blood pressure, orthostatic hypotension, vasculitis; rarely - development or exacerbation of heart failure; very rarely - heart rhythm disturbances (bradycardia, ventricular tachycardia, atrial flutter), myocardial infarction,pain in the chest, migraine.

From the central and peripheral nervous system: often - headache, dizziness, fatigue, a feeling of heat and "tides" of blood to the face, drowsiness; infrequent - malaise, fainting, asthenia, hypoesthesia, paresthesia, peripheral neuropathy, tremor, insomnia, emotional lability, unusual dreams, nervousness, depression, anxiety; rarely - cramps, apathy, agitation; very rarely - ataxia, amnesia.

From the digestive system: often - nausea, abdominal pain; infrequently - vomiting, constipation, diarrhea, flatulence, dyspepsia, anorexia, dry mouth, thirst; rarely - gingival hyperplasia, increased appetite; very rarely - gastritis, pancreatitis, hyperbilirubinemia, jaundice (usually cholestatic), increased activity of "hepatic" transaminases, hepatitis.

From the hematopoiesis: very rarely - thrombocytopenic purpura, leukopenia, thrombocytopenia.

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

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

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

Allergic reactions: infrequently - itchy skin, rash; very rarely - angioedema, erythema multiforme, urticaria.

Other: infrequently - alopecia, ringing in the ears, gynecomastia, increase / decrease in body weight, impaired vision, diplopia, accommodation disorder, xerophthalmia, conjunctivitis, eye pain, taste distortion, chills, epistaxis, increased sweating; rarely - parosmia, xeroderma, a violation of skin pigmentation, cold sweat, hyperglycemia.

Overdose:

Symptoms: marked decrease in blood pressure with the possible development of reflex tachycardia and excessive peripheral vasodilation (the risk of a pronounced and persistent decline in blood pressure, including with the development of shock and death).

Treatment: Rinsing the stomach, taking activated charcoal (especially in the first 2 hours after an overdose), the patient should take a horizontal position with an elevated position of the lower extremities.

Maintaining the function of the cardiovascular system, monitoring the performance of the heart and lungs, 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:

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

Unlike other BCCI, there is no clinically significant interaction with non-steroidal anti-inflammatory drugs (NSAIDs), especially with indomethacin.

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

Does not affect the pharmacokinetic parameters of digoxin and warfarin.

Cimetidine does not affect the pharmacokinetics of amlodipine.

Calcium preparations can reduce the effect of BCCC.

Antiviral drugs (ritonavir) increase the plasma concentrations of BCCI, incl. amlodipine.

Neuroleptics enhance the hypotensive effect of dihydropyridine derivatives.

With the joint use of BCCC with lithium preparations, neurotoxicity may be enhanced.

Means for inhalation anesthesia (derivatives of hydrocarbons, incl. isoflurane), amiodarone, quinidine, BCCI can enhance the hypotensive effect.

The repeated use of amlodipine at a dose of 10 mg and atorvastatin at a dose of 80 mg is not accompanied by a significant change in the pharmacokinetics of atorvastatin. Simultaneous intake of 240 ml of grapefruit juice and 10 mg of amlodipine is not accompanied by a significant change in the pharmacokinetics of amlodipine.

Simultaneous reception of 100 mg of sildenafil in patients with hypertension does not affect the pharmacokinetics parameters of amlodipine.

Special instructions:

Amlodipine has no effect on plasma concentrations of potassium, glucose, hormones thyroid gland, lipids, uric acid, creatinine, urea nitrogen.

It should be avoided the abrupt withdrawal of amlodipine due to the risk of worsening angina.

During the period of treatment, it is necessary to control the body weight and be observed at the dentist (prevention of soreness, bleeding and gingival hyperplasia).

The efficacy and safety of the use of amlodipine in hypertensive crisis is not established.

In elderly patients may increase T_1/2 and decrease the clearance of the drug. Correction of the dose is not required, but more careful monitoring of patients of this category is necessary.

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

During the treatment period, care should be taken when driving vehicles and engaging in other activities that require concentration of attention and speed of psychomotor reactions.

Form release / dosage:

Tablets 5 mg and 10 mg.

Packaging:For 10 tablets in a planar cell package. For 10 or 30 tablets in a jar of polymer materials. Each bank, 1 or 3 contour mesh packages together with instructions for use in a pack of cardboard. By 2.0 or 2.5 kg tablets in a container of polymer materials (for export delivery).

Storage conditions:

At a temperature not exceeding 30 ° C.

Keep out of the reach of children.

Shelf life:

4 years.

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

Terms of leave from pharmacies:On prescription

Registration number:P N002653 / 01

Date of registration:02.06.2008

The owner of the registration certificate:VEROPHARM SA VEROPHARM SA Russia

Manufacturer: & nbsp

VEROPHARM SA Russia

Information update date: & nbsp29.01.2017

Illustrated instructions

Instructions

Vero-Amlodipine (Vero-Amlodipine)