Nitremed tablets 20mg, No. 30

• Arterial hypertension.

Nitremed is used orally, after a meal, by swallowing the tablet whole and drinking plenty of water. To facilitate swallowing, the tablet can be divided into parts according to the risk, which is not intended for dividing the tablet into doses!

It is not recommended to drink the tablets with grapefruit juice (see the section 'Special instructions')!

Nitrendipine is light sensitive, so the tablets should be removed from the blister just before use!

Treatment is prescribed strictly individually in accordance with the severity of the disease and for a long time.

Nitremed at a dosage of 10 mg is prescribed 1 tab. 2 times / day, morning and evening (20 mg nitrendipine / day). In case of insufficient decrease in blood pressure, the daily dose can be increased to 2 tab. 10 mg 2 times / day (40 mg nitrendipine / day).

Nitremed in a dosage of 20 mg is prescribed 1 tab. 1 time / day in the morning (20 mg nitrendipine / day). In case of insufficient decrease in blood pressure, the daily dose can be increased to 1 tab. 20 mg 2 times / day (40 mg nitrendipine / day).

The maximum daily dose is 40 mg of nitrendipine.

The usual starting dose of nitrendipine in patients with grade I-II arterial hypertension is 10 mg 1 time / day in the morning. Depending on the therapeutic effect, the dose can be increased to 20 mg 1 or 2 times / day. The drug is used in monotherapy or in combination therapy in combination with a diuretic, ACE inhibitor, angiotensin II receptor antagonist or beta-blocker.

Elderly patients and patients with renal insufficiency do not need a special dose adjustment. Elderly patients and patients with I degree of arterial hypertension are recommended to start using with an initial dose of 10 mg. In elderly patients and patients with impaired liver function, the metabolism of nitrendipine may be slowed down, which can lead to an undesirable decrease in blood pressure. Since the therapeutic effect of the drug in such patients can be enhanced and / or prolonged, treatment begins with low doses (10 mg / day) with careful monitoring of the patient's condition. With a pronounced decrease in blood pressure, even at low doses, treatment should be discontinued.

Active substance:

Nitrendipine - 20 mg

Excipients:

Lactose monohydrate - 68.2 mg, corn starch - 36 mg, microcrystalline cellulose - 15 mg, povidone-25 thousand - 9 mg, magnesium stearate - 0.75 mg, sodium docusate - 1.05 mg.

• hypersensitivity to nitrendipine and / or to any of the excipients of the drug, to other derivatives of 1,4-dihydropyridine;

• severe arterial hypotension (systolic blood pressure below 90 mm Hg);

• cardiogenic shock;

• severe aortic valve stenosis;

• acute period of myocardial infarction (within the first 4 weeks);

• unstable angina;

• simultaneous reception with rifampicin;

• rare hereditary diseases such as lactose intolerance, lactase deficiency or glucose-galactose malabsorption;

• pregnancy;

• breastfeeding period;

• age up to 18 years.

Carefully

• hypertrophic obstructive cardiomyopathy;

• SSSU;

• severe stenosis of the aortic orifice or mitral stenosis;

• chronic heart failure;

• myocardial infarction with left ventricular failure;

• arterial hypotension;

• renal failure;

• liver failure;

• elderly age.

Description:

The tablets are yellow, round, flat, chamfered, scored on one side and engraved '20' on the other.

Ingredients: 1 tab.

Active substance:

Nitrendipine - 20 mg

Excipients:

Lactose monohydrate - 68.2 mg, corn starch - 36 mg, microcrystalline cellulose - 15 mg, povidone-25 thousand - 9 mg, magnesium stearate - 0.75 mg, sodium docusate - 1.05 mg.

Clinical and pharmacological group: Calcium channel blocker

Pharmaco-therapeutic group: BMCC

pharmachologic effect

Nitrendipine is a slow calcium channel blocker, a dihydropyridine derivative. Has antianginal, antihypertensive effect. Reduces the flow of extracellular calcium (Ca2 +) into cardiomyocytes and smooth muscle cells of the coronary and peripheral arteries. Reduces the number of functioning channels without affecting the time of their activation, inactivation and restoration. It separates the processes of excitation and contraction in the myocardium, mediated by tropomyosin and troponin, and in vascular smooth muscles, mediated by calmodulin. In therapeutic doses, it normalizes the transmembrane calcium flow, impaired in a number of pathological conditions, primarily in arterial hypertension.

Nitrendipine is not only a slow calcium channel blocker, but also a calcium channel agonist with some positive inotropic effect. The negative inotropic effect is masked by a reflex increase in heart rate. In case of heart failure, due to the peripheral vasodilating effect, it increases the ejection fraction of the left ventricle, contributes to a decrease in the size of the heart. The antihypertensive effect is also associated with inhibition of aldosterone secretion. Does not affect the tone of the veins. Relaxes vascular smooth muscle, causes expansion of peripheral and coronary arteries, reduces total peripheral vascular resistance and insignificantly - myocardial contractility. Reduces pre- and afterload and myocardial oxygen demand. Strengthening coronary blood flow,improves blood supply to the ischemic zones of the myocardium without the development of the phenomenon of 'steal', activates the functioning of collaterals. Does not inhibit conduction in the myocardium. Strengthens renal blood flow, has moderate natriuresis.

Pharmacokinetics

Absorption and distribution

Absorption - more than 90%, bioavailability - 60-70%, binding to blood plasma proteins - 98%. Tmax in blood plasma - 1-2 hours, Cmax in blood plasma - 9-40 ng / ml.

Metabolism and excretion

Metabolized in the liver by oxidation. The isoenzymes CYP3A4, CYP3A5 and CYP3A7 are involved in metabolism. Has a 'first pass' effect through the liver. T1 / 2 - 8-12 hours

It is excreted by the kidneys and with bile through the intestines in the form of four polar metabolites (30%). The total plasma clearance is 1.3 l / min. In elderly patients, T1 / 2 increases, with cirrhosis of the liver - AUC and plasma concentration.

Indications of the drug Nitremed

• arterial hypertension.

Dosage regimen

Nitremed is used orally, after a meal, by swallowing the tablet whole and drinking plenty of water. To facilitate swallowing, the tablet can be divided into parts according to the risk, which is not intended for dividing the tablet into doses!

It is not recommended to drink the tablets with grapefruit juice (see the section 'Special instructions')!

Nitrendipine is light sensitive, so the tablets should be removed from the blister just before use!

Treatment is prescribed strictly individually in accordance with the severity of the disease and for a long time.

Nitremed at a dosage of 10 mg is prescribed 1 tab. 2 times / day, morning and evening (20 mg nitrendipine / day). In case of insufficient decrease in blood pressure, the daily dose can be increased to 2 tab. 10 mg 2 times / day (40 mg nitrendipine / day).

Nitremed in a dosage of 20 mg is prescribed 1 tab. 1 time / day in the morning (20 mg nitrendipine / day). In case of insufficient decrease in blood pressure, the daily dose can be increased to 1 tab. 20 mg 2 times / day (40 mg nitrendipine / day).

The maximum daily dose is 40 mg of nitrendipine.

The usual starting dose of nitrendipine in patients with grade I-II arterial hypertension is 10 mg 1 time / day in the morning. Depending on the therapeutic effect, the dose can be increased to 20 mg 1 or 2 times / day. The drug is used in monotherapy or in combination therapy in combination with a diuretic, ACE inhibitor, angiotensin II receptor antagonist or beta-blocker.

Elderly patients and patients with renal insufficiency do not need a special dose adjustment. Elderly patients and patients with I degree of arterial hypertension are recommended to start using with an initial dose of 10 mg. In elderly patients and patients with impaired liver function, the metabolism of nitrendipine may be slowed down, which can lead to an undesirable decrease in blood pressure. Since the therapeutic effect of the drug in such patients can be enhanced and / or prolonged, treatment begins with low doses (10 mg / day) with careful monitoring of the patient's condition. With a pronounced decrease in blood pressure, even at low doses, treatment should be discontinued.

Side effect

The frequency of side effects is classified according to the WHO recommendations: very often (? 1/10); often (? 1/100 to <1/10); infrequently (? 1/1000 to <1/100); rarely (? 1/10 000 to <1/1000); very rare (<1/10 000), frequency not known (cannot be estimated from available data).

From the hematopoietic system: very rarely - leukopenia, agranulocytosis.

From the nervous system: very often - headache (especially at the beginning of treatment, passing); infrequently - paresthesia, dizziness, fatigue, fainting, nervousness.

From the side of the organ of vision: infrequently - abnormal vision, blurred vision.

Hearing disorders and labyrinthine disorders: infrequently - dizziness.

From the side of the heart: often - angina pectoris and further aggravation of angina attacks, palpitations, tachycardia is possible; very rarely - myocardial infarction.

From the side of the vessels: very often - peripheral edema (especially at the beginning of treatment. Passing); infrequently - a pronounced decrease in blood pressure; rare - leukocytoclastic vasculitis.

From the respiratory system, chest and mediastinal organs: infrequently - shortness of breath.

From the digestive system: infrequently - nausea, vomiting, abdominal pain, diarrhea, constipation; very rarely - gingival hyperplasia.

From the liver and biliary tract: rarely - an increase in the activity of liver enzymes, especially transaminases.

On the part of the skin and subcutaneous tissues: very often - rush of blood to the skin of the face (especially at the beginning of treatment, passing); infrequently - itching, urticaria, rash, photosensitivity; very rarely - exfoliative dermatitis, angioedema.

From the musculoskeletal system: infrequently - myalgia, arthralgia.

On the part of the kidneys and urinary tract: infrequently - increased urge to urinate, polyuria.

On the part of the genitals and mammary gland: very rarely - erectile dysfunction, gynecomastia, menorrhagia.

General reactions: infrequently - weight gain, increased sweating; very rarely - fever.

In the event of side effects not listed in the instructions, the patient should consult a doctor.

Contraindications for use

• hypersensitivity to nitrendipine and / or to any of the excipients of the drug, to other derivatives of 1,4-dihydropyridine;

• severe arterial hypotension (systolic blood pressure below 90 mm Hg);

• cardiogenic shock;

• severe aortic valve stenosis;

• acute period of myocardial infarction (within the first 4 weeks);

• unstable angina;

• simultaneous reception with rifampicin;

• rare hereditary diseases such as lactose intolerance, lactase deficiency or glucose-galactose malabsorption;

• pregnancy;

• breastfeeding period;

• age up to 18 years.

Carefully

• hypertrophic obstructive cardiomyopathy;

• SSSU;

• severe stenosis of the aortic orifice or mitral stenosis;

• chronic heart failure;

• myocardial infarction with left ventricular failure;

• arterial hypotension;

• renal failure;

• liver failure;

• elderly age.

Application during pregnancy and lactation

Nitremed is contraindicated for use during pregnancy and during breastfeeding.

Pregnancy

In studies carried out in laboratory animals, it was shown that the tested doses of nitrendipine were toxic to both the mother and the offspring, which manifested itself in a number of mild malformations in the young. There have been no adequate and well-controlled studies in pregnant women.

Breast-feeding

In experiments on laboratory rats, it was shown that nitrendipine is secreted into the milk of lactating rats. The concentration of nitrendipine in milk corresponded to its concentration in blood plasma. There have been no specific clinical studies involving humans. Due to insufficient data on the manifestation of the effect of nitrendipine when breastfeeding, it is recommended to interrupt feeding.

Application for violations of liver function

Use with caution in patients with hepatic impairment.

Patients with impaired liver function are prescribed the lowest possible dose.

Application for impaired renal function

Use with caution in patients with renal insufficiency.

No dose adjustment is required in patients with renal insufficiency.

Application in children

The use of the drug is contraindicated in children and adolescents under the age of 18 years.

Use in elderly patients

Use with caution in elderly patients.

special instructions

To facilitate swallowing, the tablet can be divided into parts according to the risk, which is not intended for dividing the tablet into doses!

The intake of dihydropyridines requires strict food and beverage standardization. Grapefruit juice reduces the metabolism of nitrendipine, enhances its absorption in the gastrointestinal tract, leading to an increase in the concentration of nitrendipine in the blood plasma. During treatment, you should refrain from the simultaneous use of the drug with alcohol intake.

Although slow calcium channel blockers do not have a 'withdrawal' syndrome, a gradual dose reduction is recommended before discontinuing treatment.

Ќе следует принимать двойную дозу препарата, чтобы компенсировать пропущенную дозу: при последующем приеме необходимо следовать предписанному режиму приема препарата.

¬ случа¤х некомпенсированной сердечной недостаточности, а также при ———” (sick-sinus синдром), при отсутствии искусственного водител¤ ритма требуетс¤ особое внимание к состо¤нию пациента и регул¤рный контроль сердечной де¤тельности.

ѕациенты с нарушением функции печени, а также пожилые пациенты нуждаютс¤ в наблюдении и возможной коррекции дозы препарата: им назначают минимально возможную дозу.

ѕациенты с нарушением функции почек не нуждаютс¤ в специальной коррекции дозы.

?ет¤м и подросткам (менее 18 лет) препарат не назначают в св¤зи с отсутствием достаточного опыта относительно последствий приема препарата в этой возрастной группе.

ѕрепарат содержит в качестве вспомогательного вещества лактозы моногидрат. ѕациентам с редким наследственным заболеванием непереносимости лактозы, дефицитом лактазы или нарушением всасывани¤ глюкозы и галактозы препарат принимать не рекомендуетс¤.

¬ли¤ние на способность к управлению транспортными средствами и механизмами

¬ период лечени¤ (особенно вначале, при коррекции доз в св¤зи с переходом на другую терапию) необходимо соблюдать осторожность при вождении автотранспорта и зан¤тии другими потенциально опасными видами де¤тельности, требующими повышенной концентрации внимани¤ и быстроты психомоторных реакций.

ѕередозировка

—имптомы: головна¤ боль, гипереми¤ кожи лица, длительное выраженное снижение ј? (вплоть до развити¤ коллапса), подавление функции синусового узла, брадикарди¤, тахикарди¤.

Ћечение: промывание желудка, активированный уголь. јнтидотом ¤вл¤ютс¤ препараты кальци¤: показано медленное в/в введение 10% растворов кальци¤ хлорида или кальци¤ глюконата с последующим переключением на длительную инфузию.

ѕри выраженном снижении ј? - в/в введение допамина или добутамина. ѕри нарушени¤х проводимости - атропин, изопреналин или искусственный водитель ритма. vемодиализ не эффективен.

Ћекарственное взаимодействие

ѕри одновременном применении нитрендипин повышает концентрацию в плазме крови: хинидина, теофиллина и дигоксина (почти в 2 раза). ѕри одновременном приеме нитрендипина и дигоксина провод¤т контроль концентрации дигоксина в плазме крови и при необходимости снижают дозу дигоксина.

Ќитрендипин метаболизируетс¤ с помощью изофермента CYP3A4, который находитс¤ в печени и в слизистой оболочке кишечника. Ћекарственные препараты, ингибирующие или индуцирующие этотизофермент, могут вли¤ть на эффект 'первого прохождени¤' через печень или плазменный клиренс нитрендипина.

јнтигипертензивный эффект нитрендипина ослабл¤ют:

• Ќѕ¬ѕ - задерживают натрий и блокируют синтез простагландина почками;

• препараты кальци¤;

• эстрогены - задерживают натрий;

• симпатомиметики, индукторы микросомальных ферментов печени, в т.ч. рифампицин, рифампин, фенитоин, карбамазепин и фенобарбитал - значительно снижают биодоступность нитрендипина.

ќдновременное применение нитрендипина с рифампицином противопоказано.

јнтигипертензивный эффект нитрендипина усиливают:

• альфа- и бета-адреноблокаторы и/или другие гипотензивные средства: уменьша¤ печеночный кровоток, повышают концентрацию нитрендипина в плазме крови;

• ингал¤ционные анестетики;

• диуретики: могут привести к увеличению экскреции натри¤ почками;

• миорелаксанты (панкуроний, векуроний): продолжительность и интенсивность их воздействи¤ повышена у пациентов, принимающих нитрендипин;

• циметидин и ранитидин: хот¤ и в меньшей степени, вызывают увеличение плазменных концентраций нитрендипина;

• трициклические антидепрессанты, противовирусные препараты (ампренавир, атазанавир, ритонавир, индинавир, нелфинавир, саквинавир), противогрибковые препараты (кетоконазол, итраконазол, флуконазол), противоэпилептические средства (вальпроева¤ кислота), противомикробные препараты (хинупристин, дальфопристин), антибиотики (эритромицин, тролеандомицин, кларитромицин, рокситромицин): ¤в뤤сь сильными ингибиторами изоферментов цитохрома –450, в частности изофермента CYP3A4, увеличивают биодоступность нитрендипина в результате снижени¤ его метаболизма в печени, привод¤ к увеличению его концентрации в плазме крови;

Ќитраты, препараты лити¤ усиливают токсические эффекты нитрендипина (тошноту, рвоту, диарею, атаксию, тремор, шум в ушах).

Procainamide, quinidine and other drugs that cause prolongation of the QT interval increase the negative inotropic effect and may increase the risk of a significant prolongation of the QT interval.

Storage conditions of the drug Nitremed

The drug should be stored out of the reach of children, in a dry, dark place at a temperature of 15 ? to 25 ? C.

Shelf life of the drug Nitremed

Shelf life is 4 years. Do not use after the expiration date.

Terms of sale

The drug is available with a prescription.