Norvasc 5mg tabs 30 pcs

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Norvasc 5mg tabs 30 pcs

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Description

Composition
Active substance:
1 tablet contains: Amlodipine – 5 mg (as amlodipine besylate – 6.944 mg) amlodipine or – 10 mg (as amlodipine besylate – 13.889 mg).
Excipients:
1 tablet contains 5 mg: microcrystalline cellulose – 124.056 mg calcium phosphate – 63 mg Sodium carboxymethyl – 4 mg of magnesium stearate – 2 mg.
1 tablet contains 10 mg: microcrystalline cellulose – 248.111 mg calcium hydrogen phosphate – 126 mg Sodium carboxymethyl – 8 mg Magnesium stearate 4 mg.
Description:
Tablets 5 mg – white or almost white pills emerald (irregular octagon with sides) Pfizer engraved on one side and AML-5 on the other.
Tablets 10 mg – white or almost white pills emerald (irregular octagon with sides) Pfizer engraved on one side and AML-10 on the other.
Product form:
The tablets of 5 and 10 mg.
10 or 14 tablets in a blister made of PVC / aluminum foil. 3, 4, 9 or 10 tablets blisters or blister 1 to 14 tablets with instructions for use in a carton box, which on the front side in order to control the first opening is applied to the perforated line.
Contraindications
Hypersensitivity to amlodipine and other dihydropyridine derivatives and the excipients included in the formulation.
Severe hypotension (systolic blood pressure less than 90 mmHg. Article).
Obstruction of the left ventricular outflow tract (including severe aortic stenosis).
Shock (including cardiogenic)
Hemodynamically unstable heart failure after myocardial infarction.
Age 18 years (effectiveness and safety have been established).
Used with caution in patients with liver failure, CHF nonischemic etiology III-IV functional class NYHA classification, unstable angina, aortic stenosis, mitral stenosis, hypertrophic obstructive cardiomyopathy, acute myocardial infarction (and for 1 month thereafter), sick sinus syndrome node (marked tachycardia, bradycardia), hypotension, while the use of inhibitors or inducers isoenzyme CYP3A4.
Dosage
5 mg
Indications
Arterial hypertension (in both monotherapy and in combination with other antihypertensive agents).
Stable angina pectoris and vasospastic angina (Prinzmetal angina or variant angina) both in monotherapy and in combination with other antianginal agents.
Interaction with other drugs
Amlodipine can be safely used for the therapy of hypertension with thiazide diuretics, alpha blockers, beta-blockers or ACE inhibitors. In patients with stable angina pectoris, amlodipine can be combined with other antianginal agents, such as nitrates, prolonged or short-acting beta-blockers.
Unlike other BCCI clinically significant interaction amlodipine (III BCCI generation) was not detected in the combined use with nonsteroidal anti-inflammatory drugs (NSAIDs), including indomethacin.
May increase antianginal and hypotensive action BCCI when combined with thiazide and “loop” diuretics, ACE inhibitors, beta-blockers and nitrates, as well as strengthening their hypotensive effect when combined with alpha 1-blockers, neuroleptics.
Although the study of amlodipine negative inotropic action is usually not observed, nevertheless, some BCCI may increase the severity of the negative inotropic effects of antiarrhythmic agents causing the lengthening of the interval QT (e.g., amiodarone and quinidine).
Amlodipine may also safely be used in conjunction with antibiotics and hypoglycemic agents for oral administration.
A single dose of 100 mg sildenafil in patients with essential hypertension have not effect on the pharmacokinetic parameters of amlodipine.
Repeated application of amlodipine 10 mg and atorvastatin 80 mg is not accompanied by a significant change in the pharmacokinetics of atorvastatin.
Simvastatin: simultaneous multiple use of amlodipine 10 mg of simvastatin and 80 mg resulting in increased exposure of simvastatin by 77%. In such cases it is necessary to limit the dose to 20 mg of simvastatin.
Ethanol (drinks containing alcohol): amlodipine with single and repeated administration in a dose of 10 mg did not affect the pharmacokinetics of ethanol.
Antiviral agents (ritonavir) increase the plasma concentrations of BCCI, including amlodipine.
Neuroleptics and isoflurane: increased hypotensive effect of dihydropyridine derivatives.
Calcium can reduce the effect of BCCI.
When the joint application BCCI with lithium drugs (for amlodipine no data) may gain its neurotoxicity symptoms (nausea, vomiting, diarrhea, ataxia, tremor, tinnitus).
Research simultaneous use of amlodipine and ciclosporin in healthy volunteers and patients of all groups, except in patients after kidney transplantation, were not carried out. Various studies amlodipine interaction with cyclosporine in patients after kidney transplantation showed that the use of this combination may not lead to any effect or increase the minimum concentration of cyclosporine to varying degrees up to 40%. It should be appreciated that data and control the concentration of cyclosporin in this patient group at odnovrmenno application of cyclosporine and amlodipine. It has no effect on serum digoxin concentration in the blood and its renal clearance.
It does not significantly affect the action of warfarin (prothrombin time).
Cimetidine does not affect the pharmacokinetics of amlodipine.
In in vitro studies, amlodipine has no effect on protein binding of digoxin plasma blood, phenytoin, warfarin and indomethacin.
Grapefruit juice: simultaneous single dose of 240 mg of grapefruit juice and 10 mg amlodipine inwardly 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 the genetic polymorphism of CYP3A4 may increase the bioavailability of amlodipine and, consequently, increased hypotensive effect.
Aluminum- or magnesium-containing antacids: their single dose has no significant effect on the pharmacokinetics of amlodipine.
Inhibitors of the isoenzyme CYP3A4: while applying diltiazem dose of 180 mg, and amlodipine 5 mg in patients 69 to 87 years with arterial hypertension, marked increase in systemic exposure to 57% amlodipine. The simultaneous use of amlodipine and erythromycin in healthy volunteers (18 to 43 years) does not lead to significant changes amlodipine exposure (increase in area under the curve “concentration-time» (AUC) 22%). Despite the fact that the clinical significance of these effects is not completely clear, they may be more pronounced in older patients.
Potent inhibitors isoenzyme CYP3A4 (e.g., ketoconazole, itraconazole) may lead to an increase amlodipine plasma concentration to a greater extent than diltiazem. Should be used with caution and amlodipine inhibitors isoenzyme CYP3A4.
Clarithromycin: an inhibitor of CYP3A4 isoenzyme. Patients taking both clarithromycin and amlodipine increased risk of lowering blood pressure. Patients receiving this combination is recommended to be kept under close medical supervision.
Inducers of CYP3A4: data on the effect of inducers of CYP3A4 on the pharmacokinetics of amlodipine is not. One should carefully monitor blood pressure while the use of amlodipine and inductors isoenzyme CYP3A4.
Tacrolimus: while the use of amlodipine is a risk of increasing the concentration of tacrolimus in the blood plasma. To avoid the toxicity of tacrolimus while the use of amlodipine, should control the concentration of tacrolimus in the blood plasma of patients and to adjust the dose of tacrolimus, if necessary.
Overdose
Symptoms: marked reduction of blood pressure with possible development of reflex tachycardia and excessive peripheral vasodilation (the risk of severe and persistent hypotension, including the development of shock and death).
Treatment: gastric lavage, appointment of activated carbon (especially in the first 2 hours after the overdose), maintaining the function of the cardiovascular system, raised position the lower extremities, monitoring parameters of the heart and lungs, control circulating blood volume (CBV) and diuresis. To restore vascular tone – the use of vasoconstrictors (in the absence of contraindications for their use); to eliminate the effects of calcium channel blockade – intravenous calcium gluconate. Hemodialysis is ineffective.
pharmachologic effect
Pharmacological group:
Blocker “slow” calcium channels.
Pharmacodynamics:
Dihydropyridine derivative – blocker “slow” calcium channel (BCCI) has hypotensive and anti-anginal action. Blocks “slow” calcium channels, reduces the transmembrane passage of calcium ions into the cell (mainly in the vascular smooth muscle cells than in cardiomyocytes).
Antianginal due to increased coronary and peripheral arteries and arterioles:
– angina reduces the severity of myocardial ischemia; expanding peripheral arterioles, reducing the total peripheral vascular resistance, reduces afterload on the heart, reducing myocardial oxygen demand;
– expanding the coronary arteries and arterioles in the unaltered and in ischemic areas of myocardium, increase oxygen supply to the myocardium (especially with vasospastic angina pectoris); prevents coronary artery spasm (including those caused by smoking).
In patients with stable angina single daily dose increases exercise tolerance, slows the development of angina and ‘ischemic »ST-segment depression, reduces the frequency of angina attacks and consumption of nitroglycerin and other nitrates.
It has a long dose-dependent hypotensive effect. Hypotensive effect caused by the direct vasodilating effect on vascular smooth muscle. When hypertension single dose provides a clinically significant decrease in blood pressure (BP) over 24 hours (at the position of the patient “lying” and “standing”).
Orthostatic hypotension when using amlodipine is quite rare. Amlodipine does not cause reduction of exercise tolerance, left ventricular ejection fraction. Reduces the degree of left ventricular hypertrophy. No effect on the myocardial contractility and conductivity, does not cause reflex increase of heart rate (HR), inhibits platelet aggregation and increases glomerular filtration rate, has a weak natriuretic action. In diabetic nephropathy does not increase the severity of microalbuminuria. It does not have any adverse effect on metabolism and lipid concentration in blood plasma and can be used in therapy of patients with asthma, diabetes and gout. A significant decrease in blood pressure was observed after 6-10 hours, duration of effect – 24 hours.
Patients with diseases of the cardiovascular system (including coronary atherosclerosis with a lesion of the vessel and to the stenosis 3 or more arteries, carotid atherosclerosis), myocardial infarction, percutaneous transluminal coronary angioplasty (PTCA) or in patients with angina pectoris, amlodipine It prevents the development of thickening intima-media carotid arteries, reduces mortality from myocardial infarction, stroke, PTCA, coronary artery bypass surgery; leads to a decrease in the number of hospitalizations for unstable angina and progression of chronic heart failure (CHF); It reduces the frequency of interventions aimed at restoring coronary blood flow.
It does not increase mortality or development of complications and mortality in patients with CHF (III-IV functional class NYHA classification) during therapy with digoxin, diuretics and angiotensin-converting enzyme (ACE) inhibitors. In patients with CHF (III-IV NYHA functional class classification) with nonischemic etiology amlodipine exists the likelihood of pulmonary edema.
Pharmacokinetics:
After oral administration, amlodipine is well absorbed from the gastrointestinal tract. The mean absolute bioavailability of 64-80%, maximal serum concentration is determined 6-12 hours. The equilibrium concentrations are achieved after 7-8 days of therapy.
Simultaneous food intake does not affect the absorption of amlodipine. The mean volume of distribution of 21 l / kg of body weight, indicating that most of the drug is in the tissues, and smaller – in the blood. Most of the drug present in the blood (97.5%) bound to plasma proteins. Amlodipine undergoes slow but actively metabolized in the liver in the absence of a significant effect of “first pass” through the liver. Metabolites not possess significant pharmacological activity.
After receiving a single half-life (T1 / 2) ranges from 35 to 50 hours on repeated administration of T1 / 2 of approximately 45 hours Approximately 60% of an oral dose is excreted by the kidneys mainly as metabolites, 10% -. In unmodified form, and 20 -25% – through the intestine with bile. Total Amlodipine clearance is 0.116 ml / sec / kg (7 ml / min. / Kg, 0.42 L / h / kg).
Use in elderly patients
In elderly patients (over 65 years) the excretion of amlodipine slowed down (T1 / 2 – 65 hours) compared to younger patients, but this difference has no clinical significance.
Use in patients with hepatic insufficiency
Elongation T1 / 2 in patients with hepatic failure suggests that prolonged application of drug accumulation in the body is higher (T1 / 2 – 60 h).
Use in patients with renal insufficiency
Renal failure does not significantly affect the kinetics of amlodipine.
Amlodipine penetrates the blood-brain barrier. When hemodialysis is not removed.
Pregnancy and breast-feeding
Norvask® safety of the drug during pregnancy has not been established, therefore use during pregnancy is possible only when the benefits to the mother outweigh the risks to the fetus and newborn.
Evidence of amlodipine allocation in breast milk are not available. However, we know that other BCCI – dihydropyridine derivatives are allocated to breast milk. In this connection, when the need for Norvask® during lactation should decide the issue of termination of breastfeeding.
There was no evidence of amlodipine effects on fertility in studies on rats.
Conditions of supply of pharmacies
On prescription.
side effects
The frequency of adverse reactions listed below, was determined according to the following (World Health Organization):
very often – 1/10
often – from more than 1/100 to less than 1/10
infrequently – by more than 1/1000 and less than 1/100,
rarely – from more than 1/10000 and less than 1/1000,
very rare – from less than 1/10000, including isolated reports,
unknown – it is impossible to estimate the frequency on the basis of the available data.
With the cardiovascular system: often – palpitations, peripheral edema (ankles and feet), “tides” of blood to the facial skin; rare – an excessive fall in blood pressure; very rarely – fainting, shortness of breath, vasculitis, orthostatic hypotension, development or exacerbation of current CHF, cardiac arrhythmias (including bradycardia, ventricular tachycardia and atrial fibrillation), heart attack, chest pain.
On the part of the musculoskeletal system: rarely – arthralgia, muscle cramps, myalgia, back pain, arthritis, rarely – myasthenia gravis.
From the nervous system: often – headache, dizziness, fatigue, drowsiness; rarely – fatigue, malaise, hypoesthesia, paresthesia, peripheral neuropathy, tremor, insomnia, mood lability, abnormal dreams, anxiety, depression, anxiety, tinnitus, taste perversion; very rarely – headache, increased sweating, lethargy, agitation, ataxia, amnesia; unknown – extrapyramidal disorders.
From the digestive system: often – nausea, stomach pain; infrequently – vomiting, constipation or diarrhea, flatulence, dyspepsia, anorexia, dryness of the oral mucosa, thirst; rarely – gingival hyperplasia, increased appetite; very rarely – pancreatitis, gastritis, jaundice (caused by cholestasis), hyperbilirubinemia, increased activity of “liver” transaminases, hepatitis.
From the side of hematopoiesis: rarely – thrombocytopenia purpura, leukopenia, and thrombocytopenia.
The respiratory system: rarely – dyspnea, rhinitis, epistaxis; very rarely – cough.
From the sensory organs: rarely – diplopia, disturbance of accommodation, xerophthalmia, conjunctivitis, eye pain, blurred vision;
With the genitourinary system: Infrequent – frequent urination, painful urination, nocturia, erectile dysfunction; very rarely – dysuria, polyuria.
For the skin: rarely – dermatitis; very rare – alopecia, dermatoxerasia, cold sweat, violation of skin pigmentation.
Metabolic disorders: very rarely – hyperglycemia; infrequently -increase / decrease in body weight
Allergic reactions: infrequently – pruritus, rash (including erythematous, maculopapular rash, urticaria), very rarely – angioneurotic edema, erythema multiforme.
Laboratory findings: very rarely – hyperglycemia
Other: rarely – fever, gynecomastia, pain, unspecified; very rarely – parosmiya.
special instructions
It is necessary to maintain dental hygiene and observation at the dentist (to prevent pain, bleeding and gingival hyperplasia).
Elderly patients may increase the T1 / 2 and to decrease the clearance of the drug. Changes in dose are not required, but patients should be more carefully monitored in this category.
Efficacy and safety of the drug has not been established Norvask® for hypertensive crisis.
Despite the lack of BCCI syndrome “cancel” the cessation of drug treatment Norvask® it is desirable to gradually reducing the dose of the drug.
Against the background of Norvaska® in patients with chronic heart failure class III and IV NYHA functional class classification
non-ischemic origin, marked increase in the incidence of pulmonary edema, although no evidence of deterioration of heart failure.
Impact on the ability to drive vehicles and other complex mechanisms: while on the background of the drug Norvask® any negative effect on the ability to drive vehicles or other complex mechanisms were observed, however, due to the possible excessive reduction in blood pressure, development of dizziness, drowsiness and other side effects caution should be exercised in these situations, especially at the beginning of treatment and when the dose is increased.
Storage conditions
At temperatures above 25 ° C.
Keep out of the reach of children!.
Dosing and Administration
Inside, once a day, washing down the necessary amount of water (100 mL).
In hypertension, angina usually starting dose is 5 mg, it can be increased to a maximum daily dose, depending on the therapeutic response – 10 mg.
Use in elderly patients
Norvask® recommended in high therapeutic dose, dose adjustment is required.
Use in patients with impaired liver function
Despite the fact that T1 / 2 Norvaska® as all BCCI increases in patsietov with impaired liver function, the dose correction is not usually required (see. The section “Special instructions”).
Use in patients with impaired renal function
Norvask® recommended to use conventional doses but must take into account the possible slight increase in T1 / 2
No dose adjustment is required while the use of thiazide diuretics, beta-blockers and ACE inhibitors.
Information
Appearance may differ from that depicted in the picture. There are contraindications. You need to read the manual or consult with a specialist

Additional information

Weight0.100 kg
Manufacturer

Pfizer

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