Norvasc - instructions for use, reviews, analogs and forms of release (5 mg and 10 mg tablets) drug for the treatment of hypertension and pressure reduction, angina in adults, children and pregnancy. Composition

In this article, you can read the instructions for using the drug Norvask. Comments of visitors of the site - consumers of this medication, as well as opinions of doctors of specialists on the use of Norvasc in their practice are presented. A big request is to actively add their feedback on the drug: the medicine helped or did not help get rid of the disease, which were observed complications and side effects, possibly not declared by the manufacturer in the annotation. Analogues of Norvasc with available structural analogues. Use to treat hypertension and reduce blood pressure, angina in adults, children, as well as during pregnancy and lactation. Composition of the drug based on amlodipine.

Norvask - blocker of slow calcium channels, dihydropyridine derivative. Has antihypertensive and antianginal effect. It blocks slow calcium channels, inhibits the transmembrane transition of calcium ions into cells (mostly in smooth muscle cells of blood vessels, rather than in cardiomyocytes).

Antianginal action is due to the expansion of the coronary and peripheral arteries and arterioles.

When angina decreases the severity of myocardial ischemia; expanding peripheral arterioles, reduces OPSS, reduces afterload on the heart, reduces 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 vasospastic angina); prevents spasm of the coronary arteries (including caused by smoking).

In patients with stable angina, a single daily dose increases exercise tolerance, slows the development of angina attacks and ischemic depression of the ST segment, reduces the incidence of angina attacks and the consumption of Nitroglycerin and other nitrates.

Has a long-term dose-dependent antihypertensive effect, the mechanism of which is due to a direct relaxing effect on smooth muscle vessels. In patients with arterial hypertension, a single dose of Norvasca provides a clinically significant reduction in blood pressure for 24 hours in both the supine and standing positions.

Orthostatic hypotension with the use of Amlodipine (the active substance of the drug Norvasc) is rare.

Amlodipine does not cause a decrease in exercise tolerance, a fraction of the release of the left ventricle. Reduces the degree of myocardial hypertrophy of the left ventricle. Does not affect the contractility and conductance of the myocardium, does not cause a reflex increase in heart rate, inhibits platelet aggregation, increases GFR, has a weak natriuretic effect. When diabetic nephropathy does not increase the severity of microalbuminuria. Does not have any adverse effect on the metabolism and concentration of plasma lipids and can be used in the treatment of patients with bronchial asthma, diabetes and gout.

A significant reduction in blood pressure is observed after 6-10 h, the duration of the effect is 24 h.

In patients with cardiovascular diseases (including coronary atherosclerosis with one vessel and up to stenosis of 3 or more arteries and carotid artery atherosclerosis) who underwent myocardial infarction, percutaneous transluminal angioplasty of coronary arteries (TPL) or suffering from angina pectoris, Norvasca prevents the development of intimal thickening - carotid artery medicine, reduces the mortality from myocardial infarction, stroke, TPL, coronary artery bypass grafting, leads to a decrease in the number of hospitalizations for an unstable wall ardii and progression of chronic heart failure, reduces the frequency of interventions aimed at restoring coronary blood flow.

Norvasc does not increase the risk of death or development of complications leading to fatal outcomes in patients with chronic heart failure (3-4 functional class according to the NYHA classification) against the background of therapy with digoxin, diuretics and ACE inhibitors.

In patients with chronic cardiac insufficiency (3-4 functional class according to the NYHA classification) of non-ischemic etiology with the use of amlodipine, there is a possibility of pulmonary edema.

Composition

Amlodipine besylate + auxiliary substances.

Pharmacokinetics

After oral administration, Norvasc is well absorbed. Absolute bioavailability is 64-80%. Food intake does not affect the absorption of amlodipine. Binding to plasma proteins is approximately 97.5%. Amlodipine penetrates the blood-brain barrier (BBB). Amlodipine undergoes a slow but active metabolism in the liver in the absence of a significant "first pass" effect through the liver. Metabolites do not have significant pharmacological activity. About 60% of the dose taken internally is excreted in the urine mainly in the form of metabolites, 10% - unchanged, and 20-25% - through the intestines with bile. Amlodipine is not removed during hemodialysis.

In elderly patients (over 65 years of age) amlodipine withdrawal is slowed (T1 / 2 - 65 h) compared with young patients, but this difference is not clinically significant.

Indications

• arterial hypertension (both as a monotherapy, and in combination with other antihypertensive drugs);
• stable angina and angiospastic angina (Prinzmetal angina) (both as monotherapy and in combination with other antianginal agents).

Forms of release

Tablets 5 mg and 10 mg.

Instructions for use and dosing regimen

The drug is taken orally 1 time per day, with a sufficient amount of water (100 ml).

With arterial hypertension and angina, the initial dose is 5 mg, depending on the individual reaction of the patient, it can be increased to a maximum dose of 10 mg.

It is not necessary to correct the dose of Norvasc with simultaneous use of thiazide diuretics, beta-blockers or ACE inhibitors.

In elderly patients, the drug is recommended for use in an average therapeutic dose, a dose change is not required.

Side effect

• a feeling of palpitations;
• peripheral edema (ankle and foot);
• flushes of blood to the face;
• excessive decrease in blood pressure;
• fainting;
• dyspnea;
• vasculitis;
• orthostatic hypotension;
• development or aggravation of the course of chronic heart failure;
• heart rhythm disturbances (including bradycardia, ventricular tachycardia and atrial fibrillation);
• myocardial infarction;
• pain in the chest;
• arthralgia;
• muscle cramps;
• myalgia;
• backache;
• arthrosis;
• myasthenia gravis;
• headache;
• dizziness;
• increased fatigue;
• drowsiness;
• asthenia;
• general malaise;
• paresthesia;
• peripheral neuropathy;
• tremor;
• insomnia;
• unusual dreams;
• increased excitability;
• depression;
• anxiety;
• tinnitus;
• perversion of taste;
• migraine;
• increased sweating;
• apathy;
• amnesia;
• abdominal pain;
• nausea, vomiting;
• constipation or diarrhea;
• flatulence;
• dyspepsia;
• anorexia;
• dry mouth;
• thirst;
• gingival hyperplasia;
• increased appetite;
• jaundice (usually cholestatic);
• hepatitis;
• thrombocytopenic purpura, leukopenia, thrombocytopenia;
• dyspnea;
• rhinitis;
• nose bleed;
• cough;
• conjunctivitis;
• Pain in the eyes;
• visual impairment;
• frequent urination;
• painful urination;
• violation of erectile function;
• gynecomastia;
• dermatitis;
• alopecia;
• violation of skin pigmentation;
• increase / decrease in body weight;
• itching;
• rash (including erythematous, maculopapular rash, urticaria);
• angioedema;
• erythema multiforme;
• chills.

Contraindications

• severe arterial hypotension (systolic blood pressure less than 90 mm Hg);
• obstruction of the outflow tract of the left ventricle (including severe aortic stenosis);
• hemodynamically unstable heart failure after myocardial infarction;
• children and adolescents under 18 years of age (efficacy and safety not established);
• increased sensitivity to amlodipine and other dihydropyridine derivatives, as well as the auxiliary substances that make up the drug.

Application in pregnancy and lactation

The safety of the drug Norvasc during pregnancy is not established, therefore, use during pregnancy is possible only if the intended benefit for the mother exceeds the potential risk to the fetus.

There is no evidence that amlodipine is excreted in breast milk. However, it is known that other blockers of slow calcium channels (dihydropyridine derivatives) are excreted in breast milk. In this regard, if you need to use the drug Norvasc during lactation should resolve the issue of termination of breastfeeding.

Use in children

Contraindicated the appointment of the drug to children and adolescents under the age of 18, tk. The efficacy and safety of its use in this group of patients have not been accurately established.

Application in elderly patients

In elderly patients, the drug is recommended for use in an average therapeutic dose, a dose change is not required.

special instructions

During the treatment, the preparation needs oral hygiene maintenance and supervision at the dentist (to prevent soreness, bleeding and gingival hyperplasia).

The effectiveness and safety of the Norvasc drug for hypertensive crisis is not established.

Despite the lack of slow calcium channel blockers for withdrawal syndrome, discontinuation of treatment with Norvasc is desirable, gradually reducing the dose of the drug.

The use of amlodipine in patients with chronic heart failure (class 3 and 4 in the NYHA classification) of non-ischemic genesis was associated with an increased incidence of pulmonary edema, despite the absence of signs of worsening heart failure.

Impact on the ability to drive vehicles and manage mechanisms

Although no adverse effect on the ability to drive a car or other technical means was observed with the use of the Norvasc drug, however, due to the possible excessive decrease in blood pressure, the development of dizziness, drowsiness and other side effects, one should carefully consider the individual effect of the drug in these situations,especially at the beginning of treatment and when the dosage regimen is changed.

Drug Interactions

Amlodipine can safely be used to treat arterial hypertension along with thiazide diuretics, alpha-adrenoblockers, beta-blockers, or ACE inhibitors. In patients with stable angina, amlodipine can be combined with other antianginal agents, for example, with prolonged or short-acting nitrates, beta-blockers.

Unlike other blockers of slow calcium channels, clinically significant interaction of amlodipine (3 generation of slow calcium channel blockers) was not detected when combined with non-steroidal anti-inflammatory drugs (NSAIDs), including. and with indomethacin.

It is possible to intensify the antianginal and antihypertensive action of slow calcium channel blockers when combined with thiazide and loop diuretics, ACE inhibitors, beta-blockers and nitrates, as well as enhance their antihypertensive effect when combined with alpha1-adrenergic blockers, antipsychotics.

Although no negative inotropic effects were usually observed in the study of amlodipine, nevertheless some slow calcium channel blockers may increase the negative inotropic effect of antiarrhythmic agents that cause prolongation of the QT interval (for example, Amiodarone and quinidine).

Amlodipine can also be safely administered concomitantly with antibiotics and hypoglycemic agents for oral administration.

A single dose of Sildenafil in a dose of 100 mg in patients with essential hypertension does not affect the parameters of the pharmacokinetics of Norvasc.

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.

Simultaneous repeated use of amlodipine in a dose of 10 mg and Simvastatin at a dose of 80 mg leads to an increase in the exposure of simvastatin by 77%. In such cases, the dosage of simvastatin should be limited to 20 mg.

Amlodipine with a single and repeated application in a dose of 10 mg does not affect the pharmacokinetics of ethanol (alcohol).

Antiviral drugs (eg, ritonavir) increase plasma concentrations of slow calcium channel blockers,in t.ch. amlodipine.

Neuroleptics and isoflurane increase the antihypertensive effect of dihydropyridine derivatives.

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

With the combined use of slow calcium channel blockers with lithium preparations (there are no data for amlodipine), it is possible to intensify manifestations of neurotoxicity of the latter (nausea, vomiting, diarrhea, ataxia, tremor, and tinnitus).

Studies of simultaneous use of amlodipine and cyclosporine in healthy volunteers and all patient groups, except for patients after kidney transplantation, have not been conducted. Various studies of the interaction of amlodipine with cyclosporine in patients after kidney transplantation show that the use of this combination may not lead to any effect, or increase the minimum concentration of cyclosporin to varying degrees to 40%. These data should be taken into account and the concentration of cyclosporine in this group of patients should be monitored while cyclosporine and amlodipine are used simultaneously.

Amlodipine has no effect on serum concentration of Digoxin and its renal clearance.

Norvasc does not have a significant effect on the effects of Warfarin (prothrombin time).

Cimetidine does not affect the pharmacokinetics of amlodipine.

In studies, amlodipine does not affect the binding of plasma proteins to digoxin, phenytoin, warfarin, and indomethacin.

Simultaneous single intake of 240 ml of grapefruit juice and 10 mg of amlodipine inside is not accompanied by a significant change in the pharmacokinetics of amlodipine. Nevertheless, it is not recommended to use grapefruit juice and amlodipine at the same time. the genetic polymorphism of the isoenzyme CYP3A4 may increase the bioavailability of amlodipine and, as a result, enhance the hypotensive effect.

A single intake of aluminum / magnesium-containing antacids does not significantly affect the pharmacokinetics of amlodipine.

With the simultaneous use of diltiazem (inhibitor of isoenzyme CYP3A4) at a dose of 180 mg and amlodipine at a dose of 5 mg in elderly patients (from 69 to 87 years) with arterial hypertension, an increase in system exposure of amlodipine by 57% is noted. The simultaneous use of amlodipine and Erythromycin in healthy volunteers (18 to 43 years old) does not lead to significant changes in the exposure of amlodipine (an AUC increase of 22%).Despite the fact that the clinical significance of these effects is not completely clear, they can be more pronounced in elderly patients. Powerful inhibitors of the isoenzyme CYP3A4 (eg, ketoconazole, itraconazole) can lead to an increase in the concentration of amlodipine in the blood plasma to a greater extent than diltiazem. Caution is advisable to use amlodipine and inhibitors of the isoenzyme CYP3A4.

Analogues of Norvasc drug

Structural analogs for the active substance:

• Agen;
• Acridipine;
• Amlovas;
• Amlodak;
• Amlodigamma;
• Amlodipine;
• Amlodipine Cardio;
• Amlodipine besylate;
• Amlodipine maleate;
• Amlodipharm;
• Amocardium of Sanovel;
• Amlong;
• Ammonorm;
• Amrorus;
• Amlotop;
• Kalchek;
• Cardilopin;
• Karmagip;
• Corvadil;
• Cordy Cor;
• Normodipine;
• Omerar Cardio;
• Stamlo;
• Tenox.

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