Norvask is a slow calcium channel blocker derived from dihydropyridine. Provides antihypertensive and antianginal effect.
Blocks slow calcium channels, inhibits the transmembrane transition of calcium ions into cells (to a greater extent - into vascular smooth muscle cells than into cardiomyocytes). Antianginal action due to the expansion of the coronary and peripheral arteries and arterioles.
This tool is widely used in cardiology practice. In particular, is assigned to people suffering from angina, atherosclerosis. As a prophylaxis, it is used to prevent arterial thickening, reduces the number of deaths from heart disease.
Calcium channel blocker.
Pharmacy sales terms
It is released on prescription.
How much does Norvask in pharmacies cost? The average price is at the level of 500 rubles.
Release form and composition
The active component of Norvaska is amlodipine besylate. The substance is a derivative of dihydropyridine and has a pronounced antianginal and hypotensive effect.
The drug is available in the form of tablets with different concentrations of the active substance - in one tablet may contain 5 or 10 mg of amlodipine. Tablets are painted in white or almost white color, have the shape of an octahedron with uneven sides, externally resemble emerald. On one side of each tablet there is a “Pfizer” logo, on the other - depending on the concentration of amlodipine - “AML5” or “AML10”.
Excipients: microcrystalline cellulose, anhydrous calcium phosphate, sodium starch glycolate type A, magnesium stearate.
Norvask blocks the so-called “slow” calcium channels, thereby helping to reduce the tone of the smooth muscle wall of blood vessels.
This process provides prevention of myocardial ischemia. Ischemia is a constriction of the lumen of the vessel to the extent that the blood loses the ability to fully nourish the heart muscle, resulting in the deceleration of a portion of the heart - a heart attack. When coronary and nearby vessels relax, their lumen increases, thereby reducing ischemic risks. The drug reduces the heart's need for nutrients and oxygen. This circumstance becomes possible due to the expansion of blood vessels and reducing the load on the heart.
Norvask helps to reduce the pressure in the patient in a sitting and lying position. Due to the slow onset of action of the drug, the possibility of a pressure jump is excluded.
Indications for use
According to the instructions to Norvasku, the drug is intended for the treatment of patients who have been diagnosed with the following diseases:
- Hypertension (high blood pressure). Expanding the large coronary and peripheral vessels, Norvask acts as an antihypertensive, pressure reducing, agent.
- Angina, stable or vasospastic. The use of Norvask helps to reduce the severity of ischemia of the heart muscle. Providing a vasodilating effect, the drug, as noted in the instructions for use, reduces the resistance to blood flow, relieves excessive stress on the myocardium.
- The active substances contained in Norvsk, when applied, have a spasmolytic effect on the coronary arteries.
In this case, the tool can be used as a monotherapeutic, and as an adjunct to the main therapy.
- Age up to 18 years (studies confirming the safety and efficacy of Norvaska for this age group of patients have not been conducted);
- Hypersensitivity to the components of the drug, as well as to other dihydropyridine derivatives;
- Severe 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;
- 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 the sinus node weakness, including severe tachycardia, bradycardia;
- Simultaneous use with inducers or inhibitors of an isoenzyme CYP3A4.
Use during pregnancy and lactation
Do not recommend the appointment Norvaska during pregnancy, due to lack of reliable data in this period.
You should stop taking the drug during breastfeeding or cancel the drug itself.
Dosage and method of use
The instructions for use indicate that Norvask is taken orally 1 time / day, with a necessary amount of water (100 ml).
- In hypertension and angina, the initial dose is 5 mg, depending on the patient's individual response, it can be increased to a maximum dose of 10 mg.
In elderly patients, the drug is recommended to be used in an average therapeutic dose, changing the dose of the drug is not required.
No dose adjustment of the drug Norvask with simultaneous use of thiazide diuretics, beta-blockers or ACE inhibitors is required.
Despite the fact that T1 / 2 of amlodipine, like all calcium channel blockers, increases in patients with impaired liver function, dose adjustment of the drug in these patients is usually not required.
In patients with impaired renal function, it is recommended to use Norvask in usual doses, however, it is necessary to take into account a possible slight increase in T1 / 2.
During the application of Norvasc, various disorders can develop (> 10% - very often;> 1% and 0.1% and 0.01% and <0.1% - rarely; <0.01%, including individual messages - very rarely ):
- Respiratory system: rarely - rhinitis, shortness of breath, nosebleeds; very rarely - cough;
- The reproductive system: infrequently - gynecomastia, impaired erectile function;
- Musculoskeletal system: infrequently - arthrosis, muscle cramps, arthralgia, back pain, myalgia; rarely - myasthenia gravis;
- Blood system: very rarely - leukopenia, thrombocytopenic purpura, thrombocytopenia;
- The digestive system: often - nausea, abdominal pain; sometimes - constipation, vomiting, diarrhea, anorexia, flatulence, dry mouth, dyspepsia, thirst; less commonly, increased liver transaminase activity, 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 - xerodermia, alopecia, disturbed skin pigmentation, cold sweat;
- Allergic reactions: infrequently - pruritus, rash (including erythematous, maculopapular rash, urticaria); very rarely - erythema multiforme, angioedema;
- Organ of vision: infrequently - eye pain, conjunctivitis, accommodation disturbance, diplopia, xerophthalmia, other visual disturbances;
- Metabolism: infrequently - decrease / increase in body weight; very rarely - hyperglycemia;
- Nervous system: often - dizziness, headaches, drowsiness and fatigue; sometimes - hypesthesia, asthenia, paresthesia, general malaise, peripheral neuropathy, insomnia, tremor, mood lability, depression, unusual dreams, anxiety, irritability, taste distortion, ringing in the ears; less often - apathy, migraine, ataxia, increased sweating, amnesia, agitation;
- Cardiovascular system: often - flushing, palpitations, peripheral edema (feet and ankles); infrequently, excessive lowering of blood pressure; very rarely - shortness of breath, fainting, vasculitis, orthostatic hypotension, chest pain, chronic heart failure (development or worsening of the course), heart rhythm disturbances (including ventricular tachycardia, atrial fibrillation and bradycardia), myocardial infarction;
- Other: Infrequent - chills; very rarely parosmia.
An overdose of the drug Norvask can be expressed as a series of such symptoms:
- Development of reflex tachycardia;
- Development of excessive peripheral vasodilation (there is a risk of severe and sufficient persistent hypotension with subsequent development of shock and death).
Therapy in case of overdose: it is necessary to appoint gastric lavage, taking activated carbon (preferably in the first 2 hours after taking a high dose). It is recommended to put the patient horizontally, the head 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 the work of the lungs and the heart, control diuresis and BCC. To bring the vascular tone to normal, it is necessary to prescribe vasoconstrictor drugs (provided there are no contraindications to them). To eliminate the effects of calcium channel blockages, intravenous calcium gluconate is administered.
With an overdose of the drug Norvask hemodialysis is ineffective.
Before you start using the drug, read the specific instructions:
- During drug treatment, it is necessary to maintain oral hygiene and observation at the dentist (to prevent pain, bleeding and gingival hyperplasia).
- The efficacy and safety of the use of the drug Norvask in hypertensive crisis has not been established.
- Elderly patients may increase T1 / 2 and decrease the clearance of the drug. Changes in dose is not required, but more careful monitoring of patients in this category is needed.
- Amlodipine was used in patients with chronic heart failure (class III and IV according to the NYHA classification) of non-ischemic genesis, and there was an increase in the incidence of pulmonary edema, despite no signs of worsening heart failure.
- Despite the fact that blockers of slow calcium channels have no withdrawal syndrome, it is advisable to stop treatment with Norvasc by gradually reducing the dose of the drug.
While taking the drug Norvask, there was no adverse effect on the ability to drive a car or other technical means, but due to the possible excessive decrease in blood pressure, the development of dizziness, drowsiness and other side effects, one should carefully consider the individual action of the drug in these situations, especially the beginning of treatment and when changing the dosing regimen.
When using the drug, you must consider the interaction with other drugs:
- Amlodipine does not affect the serum concentration of digoxin and its renal clearance.
- Norvask has no significant effect on the effect of warfarin (prothrombin time).
- Cimetidine does not affect the pharmacokinetics of amlodipine.
- In in vitro studies, amlodipine does not affect the binding to plasma proteins of digoxin, phenytoin, warfarin, and indomethacin.
- Amlodipine can also be safely used simultaneously with antibiotics and hypoglycemic agents for oral administration.
- A single dose of sildenafil at a dose of 100 mg in patients with essential hypertension does not affect the parameters of amlodipine pharmacokinetics.
- Repeated use of amlodipine at a dose of 10 mg and atorvastatin at a dose of 80 mg is not accompanied by significant changes in the pharmacokinetics of atorvastatin.
- The simultaneous repeated use of amlodipine at 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 dose of simvastatin should be limited to 20 mg.
- Amlodipine with single and repeated use at a dose of 10 mg does not affect the pharmacokinetics of ethanol.
- Antiviral drugs (for example, ritonavir) increase plasma concentrations of slow calcium channel blockers, including amlodipine.
- Neuroleptics and isoflurane enhance the antihypertensive effect of dihydropyridine derivatives.
- Calcium preparations can reduce the effect of slow calcium channel blockers.
- Amlodipine can be safely used for the treatment of arterial hypertension along with thiazide diuretics, alpha-blockers, 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 slow calcium channel blockers, the clinically significant interaction of amlodipine (III generation slow calcium channel blockers) was not found when used together with NSAIDs, including and with indomethacin.
- It is possible to enhance the antianginal and antihypertensive action of blockers of slow calcium channels when used in combination with thiazide and “loop” diuretics, ACE inhibitors, beta-blockers and nitrates, as well as their anti-hypertensive effect when combined with alpha1-blockers, neuroleptics.
- Although in the study of amlodipine negative inotropic effects are usually not observed, however, some blockers of slow calcium channels may enhance the severity of the negative inotropic effects of antiarrhythmic drugs that cause lengthening of the QT interval (eg, amiodarone and quinidine).
- The combined use of slow calcium channel blockers with lithium preparations (for amlodipine data are not available), may increase the manifestations of neurotoxicity of the latter (nausea, vomiting, diarrhea, ataxia, tremor, tinnitus).
- Studies on the simultaneous use of amlodipine and cyclosporine in healthy volunteers and all groups of patients, with the exception of 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 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 should be used simultaneously.
- The simultaneous single dose of 240 ml of grapefruit juice and 10 mg of amlodipine orally is not accompanied by a significant change in the pharmacokinetics of amlodipine. However, it is not recommended to use grapefruit juice and amlodipine at the same time, since with genetic polymorphism of the CYP3A4 isoenzyme, the bioavailability of amlodipine can be increased and, consequently, an increase in the hypotensive effect.
- A single dose of aluminum / magnesium-containing antacids has no significant effect on the pharmacokinetics of amlodipine.
- There is no data on the effect of CYP3A4 isoenzyme inducers on amlodipine pharmacokinetics.Blood pressure should be carefully monitored with simultaneous use of amlodipine and CYP3A4 isoenzyme inducers.
- With simultaneous use of diltiazem (CYP3A4 isoenzyme inhibitor) 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 systemic exposure to amlodipine is noted by 57%. The simultaneous use of amlodipine and erythromycin in healthy volunteers (from 18 to 43 years old) does not lead to significant changes in the exposure to amlodipine (an increase in AUC by 22%). Although the clinical significance of these effects is not completely clear, they may be more pronounced in older patients. Potent inhibitors of the isoenzyme CYP3A4 (for example, ketoconazole, itraconazole) can lead to an increase in the concentration of amlodipine in the blood plasma to a greater extent than diltiazem. Amlodipine and CYP3A4 isoenzyme inhibitors should be used with caution.
We picked up some reviews of people who used the drug Norvask:
- Kristina. I have hypertension pressure of 150/90, after taking norvax I felt a strong rush of blood to my face, and shortness of breath, decided to measure the pressure, to my horror it was 185 100 and pulse 95. After reading side effects I discovered myocardial infarction, this made it even worse Thank God everything turned out, I no longer accept, I'm afraid I will go to the doctor’s appointment. Be careful!
- Irina, a doctor. The best, the original amlodipine. Well compensates for blood pressure in a single dose for the whole day, keeps nocturnal blood pressure, does not give hypotension. Well studied. Helps more efficiently and more easily transferred than any amlodipine generic, tested on their own experience. I have patients who, for more than 5 years, take only amlodipine for the treatment of arterial hypertension, perfectly compensate for blood pressure and have no side effects, so I can be sure that even such long-term therapy is safe and effective. The price still bites for many, although sometimes an inefficient, cheaper replacement is more expensive.
Structural analogues of the active substance:
- Amlodipine Cardio;
- Amlodipine besylate;
- Amlodipine maleate;
- Amlokard Sanovel;
- Cordy Kor;
- Omelar Cardio;
Before using analogues consult your doctor.
Storage conditions and shelf life
Keep out of reach of children at temperature up to 25 ° C.
Shelf life - 4 years.