Norvask

width = Norvasc - a blocker of slow calcium channels, a derivative of dihydropyridine. 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.

This tool is widely used in cardiological practice. In particular, it is prescribed to people suffering from angina pectoris, atherosclerosis. As a preventive measure used to prevent thickening of the arteries, reduces the number of deaths from cardiac pathologies.

Clinical and pharmacological group

The calcium channel blocker.

Conditions of leave from pharmacies

It is released on prescription.

Price list

How much does Norvask cost in pharmacies? The average price is at the level of500 rubles.

Form of issue and composition

The active component of Norvasca is amlodipine besylate. The substance is a dihydropyridine derivative and has a pronounced antianginal and hypotensive effect.

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The drug is available in the form of tablets with different concentrations of active substance - one tablet can contain 5 or 10 mg of amlodipine. Tablets are painted white or almost white, have the form of an octahedron with uneven sides, outwardly resemble an emerald. On one side of each tablet is the logo "Pfizer", on the other - depending on the concentration of amlodipine - "AML5" or "AML10".

Excipients: microcrystalline cellulose, anhydrous calcium hydrogenphosphate, sodium starch glycolate type A, magnesium stearate.

Pharmacological effect

Norvasc provides the blocking of so-called "slow" calcium channels, thereby contributing to a decrease in the tone of the smooth muscle wall of blood vessels.

This process provides prevention of myocardial ischemia. Ischemia is a narrowing of the lumen of the vessel to the extent that blood loses its ability to fully nourish the heart muscle, resulting in the necrosis of the heart site - heart attack. With the relaxation of coronary and nearby vessels, their lumen increases, thereby reducing ischemic risks. The drug provides a reduction in the need of the heart in nutrients and oxygen. This circumstance becomes possible due to the expansion of the vessels and the reduction of the load on the heart.

Norvasc helps to reduce the pressure in the patient in a sitting and lying position. Due to the slow onset of the drug, the possibility of a pressure jump is excluded.

Indications for use

According to the instructions to Norvascu, the drug is designed to treat patients who are diagnosed with such diseases:

Arterial hypertension (high blood pressure). Expanding large coronary and peripheral vessels, Norvask acts as a hypotensive, pressure-lowering agent.
Stenocardia, stable or vasospastic. The use of the drug Norvasc allows to reduce the severity of ischemia of the heart muscle. Provoking vasodilating effect, the medicine, as noted in the instructions for use, reduces resistance to the blood flow, relieves excess burden on the myocardium.
The active substances in Norvask, when applied, have an antispasmodic effect on the coronary arteries.

In this case, the agent can be used as a monotherapeutic agent, or as an adjunct to the main therapy.

Contraindications

Absolute:

Age under 18 years (studies confirming the safety and efficacy of Norvasca for this age group were not performed);
Hypersensitivity to the components of the preparation, as well as to other dihydropyridine derivatives;
Severe course of arterial hypotension (systolic pressure less than 90 mm Hg);
Hemodynamically unstable heart failure after myocardial infarction;
Obstruction of the outflow tract of the left ventricle, including severe aortic stenosis.

Relative (the appointment of Norvasca requires caution against the background of the following diseases / conditions):

Pregnancy and lactation;
Unstable angina;
Arterial hypotension;
Aortic and mitral stenosis;
Chronic heart failure of non-ischemic etiology (according to NYHA classification - III-IV functional class);
Acute myocardial infarction (in addition - for 30 days after it);
Liver failure;
Hypertrophic obstructive cardiomyopathy;
Syndrome of weakness of the sinus node, including pronounced tachycardia, bradycardia;
Simultaneous application with inductors or inhibitors of the isoenzyme CYP3A4.

Use in pregnancy and lactation

Do not recommend the appointment of Norvasc during pregnancy, due to lack of validated data in this period.

You should stop taking medication during breastfeeding or cancel the drug itself.

Dosage and route of administration

In the instructions for use indicated that Norvasc taken orally 1 time / day, washed down with the necessary 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.

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

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

Despite the fact that T1 / 2 amlodipine, like all calcium channel blockers, increases in patients with impaired liver function, dose adjustment in this category of patients is usually not it takes.

In patients with impaired renal function, it is recommended to use Norvasc in normal doses, but it is necessary to take into account the possible slight increase in T1 / 2.

Side effects

During the application of Norvascus, various abnormalities can develop (& g; 0% - very often; & g;% and & lt; 0% often; & g;, 1%, and & lt; % - infrequently; & g;, 01% and?, 1% - rarely; & l;, 01%, including individual messages - very rarely):

Respiratory system: infrequently - rhinitis, shortness of breath, nosebleed; very rarely - cough;
Sexual system: infrequently - gynecomastia, violation of erectile function;
Musculoskeletal system: infrequently - arthrosis, muscle cramps, arthralgia, back pain, myalgia; rarely - myasthenia gravis;
The system of hematopoiesis: very rarely - leukopenia, thrombocytopenic purpura, thrombocytopenia;
Digestive system: often - nausea, abdominal pain; sometimes - constipation, vomiting, diarrhea, anorexia, flatulence, dry mouth, indigestion, thirst; less often - increase activity of hepatic transaminases, increased appetite, increased appetite and gingival hyperplasia; rarely - jaundice, gastritis, hepatitis, pancreatitis and hyperbilirubinemia;
Urinary system: infrequently - nocturia, frequent and / or painful urination; very rarely - polyuria, dysuria;
Skin: rarely - dermatitis; very rarely - xeroderma, alopecia, a violation of skin pigmentation, cold sweat;
Allergic reactions: infrequently - skin itching, rash (including erythematous, maculopapular rash, hives); very rarely - erythema multiforme, angioedema;
Body of vision: infrequently - pain in the eyes, conjunctivitis, accommodation disorder, diplopia, xerophthalmia, other visual impairment;
Metabolism: infrequently - decrease / increase in body weight; very rarely - hyperglycemia;
Nervous system: often - dizziness, headaches, drowsiness and fatigue; sometimes - hypoesthesia, asthenia, paresthesia, general malaise, peripheral neuropathy, insomnia, tremor, mood lability, depression, unusual dreams, anxiety, increased excitability, perversion of taste, ringing in the ears; less often - apathy, migraine, ataxia, increased sweating, amnesia, agitation;
Cardiovascular system: often - tides of blood to the face, a feeling of palpitation, peripheral edema (stop and ankle); infrequently excessive lowering of blood pressure; very rarely - shortness of breath, fainting, vasculitis, orthostatic hypotension, chest pain, chronic cardiac insufficiency (development or aggravation of the course), heart rhythm disturbances (including ventricular tachycardia, atrial fibrillation and bradycardia), myocardial infarction;
Other: infrequently - chills; very rarely - parosmia.

Overdose

An overdose of the drug Norvasc can be expressed in the form of a number of such symptoms:

Development of reflex tachycardia;
The development of excessive peripheral vasodilation (there is a risk of development of a pronounced and sufficiently stable hypotension followed by the development of shock and death).

Therapy for overdose: it is necessary to appoint gastric lavage, reception of activated charcoal (preferably in the first 2 hours after taking a high dose). The patient is recommended to put it horizontally, the headboard should be low. It is necessary to prescribe drugs and procedures to actively maintain the functionality of the cardiovascular system, it is recommended to monitor lung and heart function, control diuresis and BCC. To bring the tone of the vessels in the norm, it is necessary to prescribe vasoconstrictors (provided there are no contraindications to them). To eliminate the effects of calcium channel blockade, intravenous calcium gluconate is prescribed.

When an overdose of the drug Norvasc hemodialysis is ineffective.

special instructions

Before you start using the drug, read the 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.
In elderly patients, T1 / 2 may increase and the clearance of the drug may decrease. Dose changes are not required, but more careful monitoring of patients of this category is necessary.
Against the background of the use of amlodipine in patients with chronic heart failure (class III and IV according to the NYHA classification) non-ischemic origin, there was an increase in the incidence of pulmonary edema, despite the absence of signs of worsening of the cardiac insufficiency.
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.

Although against the background of taking Norvasc drug any negative effect on the ability to drive a car or other technical no funds were observed, but due to the possible excessive decrease in blood pressure, development of dizziness, drowsiness and other side effects should carefully consider the individual effects of the drug in these situations, especially at the beginning of treatment and when changing the regimen dosing.

Drug Interactions

When using the drug, it is necessary to take into account the interaction with other drugs:

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 in vitro, amlodipine does not affect the binding of blood proteins to digoxin, phenytoin, warfarin, and indomethacin.
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 pharmacokinetics parameters of amlodipine.
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.
Antiviral drugs (eg, ritonavir) increase plasma concentrations of slow calcium channel blockers, incl. amlodipine.
Neuroleptics and isoflurane increase the antihypertensive effect of dihydropyridine derivatives.
Calcium preparations can reduce the effect of blockers of slow calcium channels.
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, the clinically significant interaction of amlodipine (III generation of blockers of slow calcium channels) was not detected when combined with 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-adrenergic blockers and nitrates, as well as strengthening their antihypertensive action when combined with alpha1-blockers, Neuroleptics.
Although in the study of amlodipine, a negative inotropic effect was usually not observed, nevertheless, some slow calcium channel blockers can increase the severity of the negative inotropic effect of antiarrhythmic agents that cause prolongation of the QT interval (for example, amiodarone and quinidine).
When combined with slow calcium channel blockers with lithium preparations (for amlodipine, data are absent), it is possible to intensify manifestations of neurotoxicity of the latter (nausea, vomiting, diarrhea, ataxia, tremor, noise in the ears).
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 cyclosporine to varying degrees before 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.
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. in genetic polymorphism of the isoenzyme CYP3A4, it is possible to increase the bioavailability of amlodipine and, as a result, antihypertensive effect.
A single intake of aluminum / magnesium-containing antacids does not significantly affect the pharmacokinetics of amlodipine.
Data on the effect of inducers of the isoenzyme CYP3A4 on the pharmacokinetics of amlodipine are not available. It is necessary to carefully monitor blood pressure while using amlodipine and inducers of the isoenzyme CYP3A4.
With the simultaneous use of diltiazem (inhibitor of the isoenzyme CYP3A4) at a dose of 180 mg and amlodipine at a dose of 5 mg in patients elderly (from 69 to 87 years) with arterial hypertension, an increase in the systemic exposure of amlodipine to 57%. 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.

Reviews

We picked up some reviews of people who used the drug Norvasc:

Christina. At me a hypertensia pressure 150 \ 90, after reception norvaksa has felt strong rush of a blood to the face, and otdyshka, has decided to measure pressure, to my horror it was 185 \ 100 and pulse 95. After reading the side effects found there myocardial infarction, it became even worse, thank God everything turned out, I do not take any more fears, I'll go to see a doctor. Be careful!
Irina, the doctor. The best, original amlodipine. Well compensates for BP with a single admission for a whole day, keeps the night BP, does not give hypotension. Well studied. Helps to be more effectively and more easily tolerated than any generics of amlodipine, tested on their own experience. I have patients who take more than 5 years only with amlodipine for the treatment of arterial hypertension, compensate for blood pressure and have no side effects, so I can be sure that even such a safe and effective long-term therapy. The price still bites for many, although sometimes an inefficient cheaper replacement comes out more.