Norvasс 5 mg tablets 30
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Active substance: amlodipine besylate 6.944 mg, which corresponds to the content of amlodipine 5 mg.
Excipients: microcrystalline cellulose - 124.056 mg, calcium hydrogen phosphate anhydrous - 63 mg, sodium carboxymethyl starch - 4 mg, magnesium stearate - 2 mg.
Slow calcium channel blocker (BMCC), a derivative of dihydropyridine. It has an antihypertensive and antianginal effect. Blocks slow calcium channels, reduces the transmembrane transition of calcium ions into cells (to a greater extent - into smooth muscle cells of blood vessels than into cardiomyocytes).
Antianginal action is due to the expansion of coronary and peripheral arteries and arterioles.
With angina pectoris, it reduces the severity of myocardial ischemia; expanding peripheral arterioles, reduces OPSS, reduces the afterload on the heart, reduces the need for myocardium in oxygen. Expanding the coronary arteries and arterioles in unchanged and ischemic zones of the myocardium, increases the supply of oxygen to the myocardium (especially with vasospastic angina); prevents spasm of the coronary arteries (including those caused by smoking).
In patients with stable angina pectoris, a single daily dose increases exercise tolerance, slows down the development of angina attacks and ischemic depression of the ST segment, reduces the frequency of angina attacks and consumption of nitroglycerin and other nitrates.
It has a long-term dose-dependent antihypertensive effect, the mechanism of which is due to a direct relaxing effect on the smooth muscles of the vessels. In arterial hypertension, a single dose provides a clinically significant decrease in blood pressure for 24 hours (in the position of the patient lying and standing).
Orthostatic hypotension with the use of amlodipine is quite rare.
Amlodipine does not cause a decrease in exercise tolerance, the left ventricular ejection fraction. Reduces the degree of hypertrophy of the left ventricular myocardium. It does not affect the contractility and conductivity of the myocardium, does not cause a reflex increase in heart rate, inhibits platelet aggregation, increases GFR, has a weak natriuretic effect. In diabetic nephropathy, the severity of microalbuminuria does not increase. It does not have any adverse effect on the metabolism and concentration of blood plasma lipids and can be used in the treatment of patients with bronchial asthma, diabetes mellitus and gout.
A significant decrease in blood pressure is observed after 6-10 hours, the duration of the effect is 24 hours.
In patients with diseases of the cardiovascular system (including coronary atherosclerosis with the defeat of one vessels and up to stenosis of 3 or more arteries and atherosclerosis of the carotid arteries), who have undergone myocardial infarction, percutaneous transluminal angioplasty of the coronary arteries (PTCA) or in patients with angina pectoris, the use of amlodipine prevents the development of thickening of the intima-media of the carotid arteries, reduces mortality from myocardial infarction, stroke, PTCA, coronary artery bypass grafting, leads to a decrease in the number of hospitalizations for unstable angina pectoris and the progression of chronic cardiac heart disease insufficiency (CHF), reduces the frequency of interventions aimed at restoring coronary blood flow.
Does not increase the rate of mortality or the development of complications and deaths in patients with chronic heart failure (III-IV functional class according to the NYHA classification) against the background of therapy with digoxin, diuretics and ACE inhibitors.
In patients with CHF (III-IV functional class according to the NYHA classification) of non-ischemic etiology with the use of amlodipine there is a possibility of pulmonary edema.
Indications for use
- arterial hypertension (both as monotherapy and in combination with other antihypertensive drugs);
- stable angina and vasospastic angina (Prinzmetal angina) (both as monotherapy and in combination with other antianginal agents).
- severe arterial hypotension (systolic blood pressure less than 90 mm Hg);
- obstruction of the outgoing tract of the left ventricle (including severe aortic stenosis);
- shock (including cardiogenic);
- hemodynamically unstable heart failure after myocardial infarction;
- age up to 18 years (efficacy and safety have not been established);
- hypersensitivity to amlodipine and other derivatives of dihydropyridine, as well as excipients that make up the drug.
With caution, the drug should be used in patients with hepatic insufficiency, CHF of non-ischemic etiology III-IV functional class according to the NYHA classification, unstable angina, aortic stenosis, mitral stenosis, hypertrophic obstructive cardiomyopathy, acute myocardial infarction (and within 1 month after it), SSSU (severe tachycardia, bradycardia), arterial hypotension, with simultaneous use with inhibitors or inducers of the CYP3A4 isoenzyme.
Use in pregnancy and lactation
Safety of the drug Norvask ® during pregnancy and breastfeeding has not been established, so the use during pregnancy and lactation is possible only when the benefit to the mother exceeds the risk to the fetus and newborn.
The experience of using the drug shows that amlodipine is excreted in breast milk. The average milk/plasma ratio for amlodipine concentration was 0.85 among 31 lactating women who suffered from pregnancy-related hypertension and received amlodipine at an initial dose of 5 mg/day. The dose of the drug, if necessary, was adjusted (depending on the average daily dose and body weight: 6 mg and 98.7 μg / kg, respectively). The estimated daily dose of amlodipine received by an infant through breast milk is 4.17 μg / kg.
There was no effect of amlodipine on fertility in a study on rats.
Use in case of impaired liver functionWith caution, the drug should be used in patients with hepatic insufficiency.
Use in renal dysfunction
In patients with impaired renal function, it is recommended to use the drug in normal doses, but it is necessary to take into account possible slight increase in T 1/2 .
Use in childrenContraindicated in the appointment of the drug under the age of 18 years.
Use in elderly patientsIn elderly patients, the drug is recommended to be used in an average therapeutic dose, a change in the dose of the drug is not required.
During treatment with the drug, it is necessary to maintain oral hygiene and observation by a dentist (to prevent soreness, bleeding and hyperplasia of the gums).
In elderly patients, T may increase 1/2 and reduce the clearance of the drug. Dose changes are not required, but more careful monitoring of patients in this category is necessary.
Efficacy and safety of the drug Norvask ® with hypertensive crisis not established.
Despite the absence of the BMCC withdrawal syndrome, discontinuation of treatment with Norvask ® it is desirable to carry out, gradually reducing the dose of the drug.
Against the background of the use of amlodipine in patients with chronic heart failure (class III and IV according to the NYHA classification) of non-ischemic genesis, an increase in the incidence of pulmonary edema was noted, despite the absence of signs of worsening heart failure.
Influence on the ability to drive vehicles and mechanisms
Although against the background of the use of the drug Norvask ® No negative effect on the ability to drive a car or other complex mechanisms was observed, however, due to a possible excessive decrease in blood pressure, the development of dizziness, drowsiness and other adverse reactions, caution should be exercised in these situations, especially at the beginning of treatment and with an increase in dose.
Symptoms: a pronounced decrease in blood pressure with the possible development of reflex tachycardia and excessive peripheral vasodilation (the risk of developing severe and persistent arterial hypotension, incl. with the development of shock and death).
Treatment: gastric lavage, the appointment of activated charcoal (especially in the first 2 hours after an overdose), a horizontal position with a low headboard, maintaining the function of the cardiovascular system, monitoring the performance of the heart and lungs, monitoring BCC and diuresis. To restore vascular tone - the use of vasoconstrictors (in the absence of contraindications to their use); to eliminate the effects of calcium channel blockade - intravenous administration of calcium gluconate. Hemodialysis is ineffective.
Amlodipine can be safely used for the treatment of arterial hypertension along with thiazide diuretics, alpha-blockers, beta-blockers or ACE inhibitors. At of patients with stable angina, amlodipine can be combined with other antianginal agents, for example, with long-acting or short-acting nitrates, beta-blockers.
Unlike other BMCC, clinically significant interactions of amlodipine (iii generation BMCC) were not detected when combined with NSAIDs, including indomethacin.
It is possible to enhance the antianginal and antihypertensive effect of BMCC when combined with thiazide and "loop" diuretics, ACE inhibitors, beta-blockers and nitrates, as well as an increase in their antihypertensive effect when combined with alpha 1 -adrenergic blockers, neuroleptics.
Although in the study of amlodipine, a negative inotropic effect was usually not observed, nevertheless, some BMCC can increase the severity of the negative inotropic effect of antiarrhythmic agents that cause an elongation of the QT interval (for example, amiodarone and quinidine).
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 the pharmacokinetics of amlodipine.
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.
Simultaneous repeated use of amlodipine at a dose of 10 mg and simvastatin at a dose of 80 mg leads to an increase in simvastatin exposure by 77%. In such cases, the dose of simvastatin should be limited to 20 mg.
Amlodipine with a single and repeated use at a dose of 10 mg does not affect the pharmacokinetics of ethanol.
Antiviral drugs (eg, ritonavir) increase plasma concentrations of BMC, including amlodipine.
Neuroleptics and isoflurane enhances the antihypertensive effect of dihydropyridine derivatives.
Calcium supplements can reduce the effect of BMC.
With the combined use of BMC with lithium preparations (there are no data for amlodipine), it is possible to increase the manifestations of neurotoxicity of the latter (nausea, vomiting, diarrhea, ataxia, tremor, tinnitus).
Studies of 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 in varying degrees to 40%. These data should be taken into account and the concentration of cyclosporine in this group of patients should be monitored with the simultaneous use of cyclosporine and amlodipine.
Amlodipine does not affect the serum concentration of digoxin and its renal clearance.
Norvask ® does not have a significant effect on the action of warfarin (prothrombin time).
Cimetidine does not affect the pharmacokinetics of amlodipine.
In vitro studies, amlodipine does not affect the binding of digoxin, phenytoin, warfarin and indomethacin to blood plasma proteins.
Simultaneous single administration 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, because with genetic polymorphism of the isoenzyme CYP3A4, it is possible to increase the bioavailability of amlodipine and, as a result, increase the hypotensive effect.
A single dose of aluminum / magnesium-containing antacids does not have a significant effect on the pharmacokinetics of amlodipine.
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 elderly patients (from 69 to 87 years old) with arterial hypertension, there is an increase in systemic exposure to amlodipine 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 amlodipine exposure (a 22% increase in AUC). Although the clinical significance of these effects is not fully understood, 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 inhibitors of the isoenzyme CYP3A4 should be used with caution.
In patients taking simultaneously clarithromycin (inhibitor of the isoenzyme CYP3A4) and amlodipine, the risk of reducing blood pressure is increased. Patients taking such combination, it is recommended to be under close medical supervision.
There are no data on the effect of inducers of the isoenzyme CYP3A4 on the pharmacokinetics of amlodipine. Blood pressure should be carefully monitored with the simultaneous use of amlodipine and inducers of the isoenzyme CYP3A4.
With simultaneous use with amlodipine, there is a risk of increasing the concentration of tacrolimus in the blood plasma. In order to avoid the toxicity of tacrolimus when used concomitantly with amlodipine, the concentration of tacrolimus in the blood plasma of patients should be monitored and the dose of tacrolimus should be adjusted if necessary.
mTOR inhibitors, such as sirolimus, temsirolimus, and everolimus, are substrates of the CYP3A isoenzyme. Amlodipine is a weak inhibitor of the isoenzyme CYP3A. When used simultaneously with mTOR inhibitors, amlodipine can increase their exposure.
Dosage and Administration
The drug is taken inside 1 time / day, washed down with the necessary amount of water (100 ml).
With arterial hypertension and angina pectoris, the initial dose is 5 mg, depending on the therapeutic response, it can be increased to a maximum daily dose of 10 mg.
Dose adjustment of the drug is not required with the simultaneous use of thiazide diuretics, beta-blockers or ACE inhibitors.
In elderly patients, the drug is recommended to be used in an average therapeutic dose, a change in the dose of the drug is not required.
Despite the fact that T 1/2 amlodipine, like all BMCC, increases in patients with impaired liver function, dose adjustment of the drug in this category of patients is usually not required.
In patients with impaired renal function, it is recommended to use the drug in normal doses, but it is necessary to take into account a possible slight increase in T 1/2 .
The frequency of adverse reactions given below has been determined according to the WHO classification: very often (>1/10), often (from >1/100 to <1/10), infrequently (from >1/1000 to <1/100), rarely (from >1/10000 to <1/1000), very rarely (from <1/10000), including individual reports, unknown (it is impossible to estimate the frequency based on available data).
From the cardiovascular system: often - a feeling of palpitations, peripheral edema (ankles and feet), "flushes" of blood to the skin of the face; infrequently - excessive decrease in blood pressure; very rarely - fainting, shortness of breath, 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, chest pain.
From the musculoskeletal system: infrequently - arthralgia, muscle cramps, myalgia, back pain, arthrosis; rarely - myasthenia gravis.
From the nervous system: often - headaches, dizziness, increased fatigue, drowsiness; infrequently - asthenia, general malaise, hypoesthesia, paresthesia, peripheral neuropathy, tremor, insomnia, mood lability, unusual dreams, increased excitability, depression, anxiety, ringing in the ears, perversion of taste; very rarely - migraine, increased sweating, apathy, agitation, ataxia, amnesia; unknown - extrapyramidal disorders.
From the digestive system: often - abdominal pain, nausea; infrequently - vomiting, constipation or diarrhea, flatulence, dyspepsia, anorexia, dryness of the oral mucosa, thirst; rarely - hyperplasia of the gums, increased appetite; very rarely - pancreatitis, gastritis, jaundice (caused by cholestasis), hyperbilirubinemia, increased activity of hepatic transaminases, hepatitis.
From the hematopoietic system: very rarely - thrombocytopenic purpura, leukopenia, thrombocytopenia.
From the respiratory system: infrequently - shortness of breath, rhinitis, nosebleeds; very rarely - cough.
From the side of the organ of vision: infrequently - diplopia, impaired accommodation, xerophthalmia, conjunctivitis, eye pain, visual impairment.
From the urinary system: infrequently - frequent urination, painful urination, nocturia; very rarely - dysuria, polyuria.
From the reproductive system: infrequently - a violation of erectile function, gynecomastia.
From the skin: rarely - dermatitis; very rarely - alopecia, xeroderma, cold sweat, impaired skin pigmentation.
From the side of metabolism: infrequently - an increase / decrease in body weight; very rarely - hyperglycemia.
Allergic reactions: infrequently - skin itching, rash (including erythematous, maculo-papular rash, urticaria); very rarely - angioedema, erythema multiforme.
Other: infrequently - chills, pain of unspecified localization; very rarely - parosmia.
The drug should be stored out of the reach of children at a temperature not exceeding 25 ° C.
Shelf life - 4 years. Do not use after the expiration date.
- Dosage form
- 10 mg
- Number of tablets
- INN Russian
- Russian title