Nifecard chl Table with modif.vysv. n / 30mg film about 60 pc

Description

Composition
Active substance:
1 tablet contains: nifedipine 30.00 mg or 60.00 mg.
Excipients:
Povidone, sodium lauryl sulfate, hypromellose (hydroxypropylmethylcellulose), hypromellose (hydroxypropylmethylcellulose 2906), hypromellose (hydroxypropylmethylcellulose 2208), * Ludipress®, magnesium hydrosilicate (Talc), magnesium stearate; sheath: hypromellose phthalate (hydroxypropylmethylcellulose phthalate), triethyl citrate, hypromellose (hydroxypropylmethylcellulose 2910), giproloza (hydroxypropyl cellulose), Macrogol (polyethylene glycol), magnesium hydrosilicate (Talc), titanium dioxide, iron oxide yellow dye. * Ludipress®- is a mixture of lactose monohydrate, povidone, crospovidone in a ratio of 93: 3.5: 3.5.
Description:
From light tan to light brownish-orange color, round biconvex tablets, film-coated, with «NDP 30″ embossed or labeled «NDP 60 ‘on one side. In cross section are yellow.
Product form:
The modified-release tablet, film-coated 30mg, 60 mg of 10 tablets in Al / Al blister. 2, 3 or 6 blister packs in a cardboard box, together with instructions for use.
Contraindications
Hypersensitivity to nifedipine or components of the drug and other derivatives of 1,4-dihydropyridine; severe hypotension (systolic blood pressure blood pressure below 90 mm Hg..); severe aortic valve stenosis with clinically significant hemodynamic disturbances; unstable angina; chronic heart failure decompensation, cardiogenic shock (risk of myocardial infarction), acute phase of myocardial infarction (within the first 4 weeks); simultaneous application of rifampicin; Rare hereditary forms of lactose intolerance, lactase deficiency or malabsorption of glucose / galactose (as in the composition contains lactose); pregnancy up to 20 weeks, the period of breast-feeding; age 18 years (effectiveness and safety have been established).
Precautions: aortic stenosis and mitral valve; hypertrophic obstructive cardiomyopathy; marked tachycardia; sick sinus syndrome; malignant hypertension; myocardial infarction with left ventricular failure; cerebrovascular diseases; human liver and / or kidney; hemodialysis (risk of arterial hypotension); diabetes; bowel obstruction; pregnancy after 20 weeks; Simultaneous use of beta-blockers or cardiac glycosides, inducers or inhibitors of CYP3A4 isozyme.
Dosage
30 mg
Indications
Arterial hypertension; ischemic heart disease (IHD): stable angina, vasospastic angina (Prinzmetal’s angina).
Interaction with other drugs
Nifedipine is metabolized mainly through the isoenzyme CYP3A4, therefore, drugs that induce or inhibit this enzyme may alter the presystemic metabolism or clearance of nifedipine.
Inducers of CYP3A4
rifampicin
Rifampicin is a potent inducer of CYP3A4 system. When applied simultaneously with rifampicin bioavailability of nifedipine significantly reduced and the effective concentration in plasma can not be achieved.
Phenytoin, carbamazepine, phenobarbital
Phenytoin induces the CYP3A4 isoenzyme. Capable of reducing the bioavailability of nifedipine and reduce its effectiveness. With simultaneous application of nifedipine and phenytoin should evaluate the clinical effect of the latter and increase the dose if necessary. If the dose of nifedipine in combination therapy has been raised, it is necessary to take into account the cases of phenytoin.
No significant interaction studies nifedipine and carbamazepine or phenobarbital, while the application was conducted. In other studies, carbamazepine, phenobarbital and reduce the plasma concentration of the other blocker “slow” calcium channels – nimodipine, so we can not exclude the possibility of reducing plasma concentrations of nifedipine and when the simultaneous use of phenobarbital and carbamazepine.
Inhibitors of CYP3A4
The simultaneous use of nifedipine, and drugs that have an inhibitory effect on CYP3A4 isozyme, causes an increase in the concentration of nifedipine in the blood plasma.
Blood pressure should be monitored and nifedipine decrease the dose if necessary.
Macrolide antibiotics (e.g. erythromycin)
Certain macrolide antibiotics are known to inhibit CYP3A4-mediated metabolism of other drugs. Therefore, we can not exclude the potential increase in plasma concentrations of nifedipine during their joint application.
Azithromycin, although structurally similar to the class of macrolide antibiotics, does not inhibit isoenzyme CYP3A4.
HIV-protease inhibitors (e.g., amprenavir, indinavir, nelfinavir, ritonavir or saquinavir)
No reliable clinical studies of drug interaction between nifedipine and inhibitors of HIV-protease. Drugs of this class are known to inhibit isoenzyme CYP3A4. Furthermore, it was shown in in vitro study that this class of drugs inhibit the metabolism of nifedipine. With simultaneous application of nifedipine with HIV-protease inhibitors, can not avoid an increase of its plasma concentrations.
The imidazole derivatives (e.g., ketoconazole, itraconazole or fluconazole)
Reliable studies on the interaction of nifedipine with azole antifungal drugs has been conducted, but it is known that the latter inhibit isoenzyme CYP3A4. When applied simultaneously with nifedipine inside can not avoid an increase of its plasma concentrations.
fluoxetine
Reliable studies on the interaction of nifedipine with fluoxetine was conducted. The in vitro study demonstrated that fluoxetine inhibited CYP3A4-mediated metabolism of nifedipine. Therefore, the increased plasma concentrations of nifedipine at their joint application can not be excluded.
nefazodone
Reliable studies on the interaction of nifedipine and nefadozona was conducted. In the in vitro study, it was shown that nefadozon inhibit CYP3A4-mediated metabolism of nifedipine. Therefore, the increased plasma concentrations of nifedipine at their joint application can not be excluded.
Quinupristin / dalfopristin
The simultaneous use of quinupristin / dalfopristin and nifedipine may lead to an increase in the plasma concentration of the latter.
valproic acid
No significant interaction studies nifedipine and valproic acid, while the application was conducted. In other studies, valproate decreased the plasma concentration of the other blocker “slow” calcium channels – nimodipine, so we can not exclude the possibility of reducing plasma concentrations of nifedipine and when the simultaneous use of valproic acid.
cimetidine
Because inhibition of isozyme CYP3A4, cimetidine increases the plasma concentrations of nifedipine and may enhance the antihypertensive effect.
Thus, while the use of nifedipine with cimetidine, quinupristin, dalfopristin, erythromycin, fluoxetine, nefazodone, valproic acid, protease inhibitors, HIV (e.g., amprenavir, indinavir, nelfinavir, ritonavir or saquinavir) and derivatives azole (ketoconazole, itraconazole or fluconazole) blood pressure should be monitored, and if necessary, the dose should be reduced.
Other drugs that affect the metabolism of nifedipine
cisapride
The simultaneous use of cisapride and nifedipine may lead to increased plasma concentrations of nifedipine.
diltiazem
Diltiazem and nifedipine decrease clearance, therefore, increases the plasma concentrations of nifedipine. Thus, caution should be exercised when using drugs in combination, and if necessary to reduce the dose of nifedipine.
cyclosporine
Simultaneous application can lead to increased plasma concentrations of nifedipine.
Effects of nifedipine on other drugs
Gipotezivnye drugs
Nifedipine may enhance the antihypertensive effect of diuretics, beta-blockers, angiotensin converting enzyme inhibitors, angiotensin II receptor antagonists, other blockers “slow” calcium channel blockers, alpha blockers, inhibitors of phosphodiesterase-5 (PDE-5), alpha-methyldopa.
In the application of nifedipine along with beta-blockers requires careful monitoring of the patient as possible flow worsening symptoms of heart failure (described sporadic cases).
Digoxin
The simultaneous use of nifedipine and digoxin may cause increased plasma digoxin concentrations, however should be controlled in the serum digoxin concentration, and if necessary, the dose of digoxin needs to be adjusted.
quinidine
With simultaneous application of nifedipine and quinidine a reduction in plasma concentration of quinidine and in some cases, the cancellation of nifedipine, an increase in its concentration in plasma. Therefore, the recommended dose of quinidine correction if necessary. Some authors have reported increased plasma concentrations of nifedipine while the use of both drugs. Thus, the blood pressure should be carefully monitored and the dose of nifedipine should be reduced if necessary.
tacrolimus
It has been shown that cyclosporin metabolized via isoenzyme CYP3A4. Published data indicate that it may be necessary to reduce the dose of tacrolimus with simultaneous application of nifedipine.
vincristine
While the use of nifedipine reduced excretion of vincristine, it may need to reduce the dose.
Magnesium sulfate
Blood pressure must be carefully controlled with intravenous magnesium sulphate in patients receiving nifedipine, since perhaps marked reduction in blood pressure.
cephalosporins
While the use of nifedipine increased plasma concentration of cephalosporins.
phenytoin
Nifedipine phenytoin may slow metabolism and increase its toxic effects. Patients taking phenytoin, early treatment with nifedipine is recommended to monitor the plasma concentration of phenytoin.
nitrates
It is necessary to take into account the synergistic effect, while the use of nifedipine and nitrates.
theophylline
Nifedipine increases the concentration of theophylline in the plasma, while the application.
fentanyl
Concomitant use of nifedipine and fentanyl can lead to severe hypotension, so it is advisable to abolish the use of nifedipine (if possible) at least 36 hours prior to anesthesia with the use of fentanyl.
Anticoagulants of indirect action
Registered rare reports increase in prothrombin time, while the application of nifedipine with indirect anticoagulants (eg, warfarin). The relationship to therapy with nifedipine has not been established, the clinical significance of this effect is unknown.
Other forms of interaction
In the spectrophotometric determination of vanillylmandelic acid in urine can be a cause of nifedipine obtaining a false positive result. It is recommended to perform other measurements.
Grapefruit juice
Grapefruit juice inhibits the isoenzyme CYP3A4. At the same time taking grapefruit juice increases the concentration of nifedipine in blood plasma due to decreased first-pass metabolism. In view of the increase in bioavailability of nifedipine in patients with severe hypertension or stable angina pectoris may develop ischemic complications (heart attack, unstable angina). Drinking grapefruit juice during treatment with nifedipine is not recommended.
With simultaneous application of nifedipine and acetylsalicylic acid, benazepril, candesartan debrisokvina, doxazosin, irbesartan, omeprazole, orlistat, pantoprazole, ranitidine, rosiglitazone and triamterene / hydrochlorothiazide any influence on the pharmacokinetics of nifedipine offline.
Overdose
Symptoms: peripheral vasodilation with marked and probably prolonged pronounced decrease in blood pressure (headache, facial flushing, suppression of sinus node activity, bradycardia and / or tachycardia, bradyarrhythmias), hyperglycemia, metabolic acidosis, hypoxia, cardiogenic shock with the development of pulmonary edema. In severe poisoning – loss of consciousness, coma.
Treatment of overdoses is standard procedures of excretion of the drug (assignment activated charcoal, gastric lavage) restoring the stable hemodynamic, careful control of the heart, lung, and urinary system.
In cases of drug overdose prolonged action necessary to provide the most complete excretion of the drug, possible washing of the small intestine to prevent further absorption of the active substance. In the application of laxatives be appreciated that blockers “slow” calcium channel may cause a reduction of intestinal muscle tone up to intestinal atony. Hemodialysis not effective, plasmapheresis recommended due to high degree of protein binding and distribution of a relatively small volume.
Treatment of symptomatic bradyarrhythmias with atropine, and / or beta-sympathomimetics; in the event of life-threatening bradyarrhythmias necessary staging temporary pacemaker.
When persistent marked decrease in blood pressure as a result of cardiogenic shock and arterial vasodilation calcium should be used (2.1 g of calcium gluconate, i.v.), dopamine (up to 25 ug / kg / min), dobutamine (up to 15 ug / kg / min), epinephrine ( adrenaline) and norepinephrine (noradrenaline). The doses of these drugs should be determined solely on the basis of the obtained effect.
In view of the possible volume overload of the heart, fluid therapy is recommended with caution under the control of hemodynamic parameters.
Safener are calcium preparations. The clearance of nifedipine is increased in patients with impaired hepatic function.
pharmachologic effect
Pharmacological group:
Blocker “slow” calcium channels.
Pharmacodynamics:
Nifedipine – selective blocker “slow” calcium channels, a derivative of 1,4-dihydropyridine. It has antianginal and antihypertensive effect. Decreases current of extracellular calcium into cardiomyocytes and smooth muscle cells of coronary and peripheral arteries; at high doses inhibits the release of calcium ions from intracellular stores. Reduces the number of operating channels, without affecting the time of activation, inactivation and recovery.
Separates the excitation and contraction in the myocardium, tropomyosin and troponin mediated, in vascular smooth muscle mediated by calmodulin. At therapeutic doses, current normalizes transmembrane calcium ions disturbed in several pathological states, especially in hypertension. It does not affect the tone of veins. It strengthens coronary blood flow, improves blood flow to the ischemic myocardium zones without the development of the phenomenon of “steal”, activates the functioning of collaterals.
Improves myocardial function, reduces the force of heart contractions and myocardial oxygen demand. Expanding peripheral arteries, reducing blood pressure (BP) and reduces the total peripheral resistance and afterload on the heart. Almost no effect on the sinoatrial and atrioventricular nodes. Enhances the renal blood flow, natriuresis is moderate.
Inhibits Platelet aggregation has antiatherogenic properties (especially with prolonged use). Lowers blood pressure in the pulmonary artery, has a positive effect on blood flow of cerebral vessels.
Pharmacokinetics:
Nifekard® chemiluminescence due to delayed release of the active substance, providing a gradual controlled growth of plasma nifedipine concentrations. Nifedipine plasma concentration reaches a plateau after approximately 6 hours and is supported with slight fluctuations during the 24 hours. Nifedipine is rapidly and almost completely absorbed after oral administration (92-98%). Characterized by a high percentage of binding to plasma proteins (90%). The half-life of approximately 2 hours. It is metabolized in the liver. Active metabolites have been identified. It is displayed as inactive metabolites in the kidneys (80%) and in bile (20%).
Nifedipine penetrates the blood-brain and placental barrier, excreted in breast milk.
The cumulative effect is not.
Chronic renal failure, hemodialysis and peritoneal dialysis have no effect on the pharmacokinetics.
When violations of the liver reduced clearance of nifedipine. In severe hepatic dysfunction may require a dosage adjustment.
Elderly patients with intravenous administration of nifedipine clearance was reduced by 33% as compared to young healthy volunteers.
With prolonged use can be observed the development of tolerance to nifedipine.
Pregnancy and breast-feeding
fertility
In some studies, blockers “slow” calcium channel blockers such as nifedipine, resulted in reversible biochemical changes in the head of spermatozoa which can impair their function. У мужчин, неоднократно испытывающих проблемы с зачатием ребенка при экстракорпоральном оплодотворении, в качестве одной из возможных причин следует рассматривать применение нифедипина, если никакого другого объяснения не может быть найдено.
Pregnancy
Контролируемых исследований по применению нифедипина у беременных женщин не проводилось. Исследования на животных показали тератогенность и эмбрио-/фетотокичность нифедипина. Применение препарата Нифекард® ХЛ до 20 недели противопоказано. Применение препарата Нифекард® ХЛ после 20-ой недели беременности возможно только в том случае, если предполагаемая польза для матери превышает потенциальный риск для плода и препарат следует применять только в условиях стационара с соответствующим контролем состояния матери и плода (контроль артериального давления матери; регулярный ультразвуковой контроль развития и жизнеспособности плода). При возникновении аномалий следует прекратить применение препарата.
Breastfeeding
Нифедипин проникает в грудное молоко, поэтому при применении в период лактации, необходимо решить вопрос о прекращении грудного вскармливания.
Conditions of supply of pharmacies
Prescription.
side effects
According to the World Health Organization (WHO) adverse reactions are classified according to their rate of development as follows: very common (> 1/10), common (> 1/100,
special instructions
Прекращать лечение препаратом Нифекард® ХЛ рекомендуется постепенно. Следует иметь ввиду, что в начале лечения может возникнуть приступ стенокардии, особенно после недавней резкой отмены бета-адреноблокаторов (последние следует отменять постепенно).
Одновременное применение бета-адреноблокаторов необходимо проводить в условиях тщательного врачебного контроля, поскольку это может обусловить чрезмерное снижение АД, а в некоторых случаях – усугубление симптомов течения сердечной недостаточности.
При выраженной сердечной недостаточности препарат дозируют с большой осторожностью. Редко у пациентов с выраженным стенозом коронарных артерий в начале терапии или при увеличении дозы нифедипина может увеличиваться частота и выраженность ангинозных болей, вплоть до развития инфаркта миокарда.
Диагностическими критериями применения препарата при вазоспастической стенокардии являются: классическая клиническая картина, сопровождающаяся повышением сегмента ST на ЭКГ, возникновение эргоновин-индуцированной стенокардии или спазма коронарных артерий, выявление коронароспазма при ангиографии или выявление ангиоспастического компонента без подтверждения (например, при разном пороге напряжения или при нестабильной стенокардии, когда данные электрокардиограммы свидетельствуют о преходящем ангиоспазме).
Для пациентов с тяжелой гипертрофической обструктивной кардиомиопатией существует риск увеличения частоты, тяжести проявления и продолжительности приступов стенокардии после применения нифедипина; в данном случае необходима отмена препарата.
У пациентов с сахарным диабетом при применении препарата Нифекард® XЛ может потребоваться контроль концентрации глюкозы в плазме крови.
У пациентов, находящихся на гемодиализе, с высоким АД и необратимым нарушением функции почек, со сниженным объемом циркулирующей крови препарат следует применять с осторожностью, может произойти резкое падение АД.
За пациентами с нарушенной функцией печени устанавливается тщательное наблюдение и при необходимости снижают дозу препарата и/или применяют другие лекарственные формы нифедипина.
У пациентов с выраженным стенозом любого отдела желудочно-кишечного тракта возможно развитие непроходимости кишечника. В очень редких случаях могут развиться безоары, для удаления которых может потребоваться хирургическое вмешательство. В единичных случаях симптомы кишечной непроходимости могут наблюдаться у пациентов, не имеющих патологии со стороны желудочно-кишечного тракта. Риск развития безоаров повышен у пациентов с пониженной перистальтикой кишечника (запор, гастроэзофагеальный рефлюкс, ожирение, гипотиреоз, сахарный диабет), опухолями кишечника, дивертикулитом, воспалительными изменениями кишечника, вертикальной гастропластикой, шунтированием желудка, после резекции тонкого кишечника, наложения колостомы, а также при одновременном применении с блокаторами Н2-гистаминовых рецепторов, опиатами, нестероидными противовоспалительными препаратами, антихолинергическими препаратами, нейромышечными блокаторами (миорелаксанты), лаксативами (слабительные средства).
Имеются единичные сообщения «прилипания» таблеток к стенке кишечника с формированием язв, потребовавших госпитализации и хирургического вмешательства.
Следует иметь в виду, что при проведении рентгенологического исследования кишечника с барием можно выявить ложноположительные симптомы полипа (дефект «наполнения»).
Если во время терапии пациенту требуется провести хирургическое вмешательство под общей анестезией, необходимо информировать врача-анестезиолога о характере проводимой терапии.
Нифедипин, как и другие блокаторы «медленных» кальциевых каналов, угнетают агрегацию тромбоцитов in vitro. Малое количество сообщений подтверждают данные о статистически значимом снижении агрегации тромбоцитов и увеличении времени кровотечения. Клиническая значимость этого не известна.
Во время лечения возможен положительный результат при проведении прямой реакции Кумбса и повышение титра антинуклеарных антител.
В период лечения препаратом Нифекард® ХЛ необходимо соблюдать осторожность при занятиях потенциально опасными видами деятельности, требующими повышенной концентрации внимания и быстроты психомоторных реакций, и воздержаться от применения алкоголя.
Storage conditions
At a temperature of not higher than 25 C.
Keep out of the reach of children.
Dosing and Administration
Таблетки следует принимать в одно и то же время суток, не разжевывая, нельзя их дробить или делить. The batch is individually. Нельзя запивать таблетки грейпфрутовым соком.
Доза препарата Нифекард® ХЛ составляет 1 таблетка препарата 30 мг или 60 мг в сутки однократно. Подбор дозы начинается с 30 мг/сутки, коррекция осуществляется с интервалами в 7-14 дней.
Максимальная суточная доза Нифекард® ХЛ – 90 мг.
Возможно замедление выведения нифедипина у пожилых пациентов, поэтому могут потребоваться меньшие поддерживающие дозы препарата по сравнению с молодыми пациентами.
У пациентов с нарушением функции печени применение нифедипина должно проводиться под тщательным наблюдением и при необходимости может потребоваться снижение дозы препарата.
In patients with impaired renal function dose adjustment is required.
Пациентам с тяжелыми цереброваскулярными заболеваниями необходимо проводить лечение низкой дозой.
При необходимости отмены препарата Нифекард® ХЛ, дозу следует снижать постепенно.
Information
Appearance may differ from that depicted in the picture. There are contraindications. You need to read the manual or consult with a specialist