1 tabl contains 10 mg or 20 mg of nitrendipine; tablets contain lactose, in addition 10 mg tablets contain cochineal red.
Action:
Calcium channel antagonist, dihydropyridine derivative. It blocks the transmembrane inflow of Calcium ions to the vascular muscle cells, which leads to: protection against excessive calcium intake into the cell; inhibition of calcium-dependent contractions of vascular muscles; reduction of peripheral vascular resistance; reduction of pathologically increased blood pressure; gentle natriuretic effect, especially at the beginning of treatment. After oral administration, nitrendipine is absorbed quickly and practically completely (around 88%), reaching Cmaxafter about 1-3 h. Due to the significant first-pass metabolism, the systemic availability of nitrendipine is 20-30%. In 96-98% it binds to plasma proteins (albumin), therefore it does not undergo dialysis. It is practically completely metabolized in the process of oxidation in the liver. Metabolites are pharmacologically inactive. Less than 0.1% of the oral dose is excreted unchanged in the urine. Nitrendipine in the form of metabolites is mainly excreted by the kidneys - 77%, the remainder is excreted in faeces and bile. Final T0,5 in the elimination phase of nitrendipine administered in the form of tablets, it is about 8-12 h. In patients with chronic liver failure, one should expect an extended elimination time and 2-3 times longer T0,5.
Contraindications:
Hypersensitivity to nitrendipine, other drugs from the group of 1,4-dihydropyridine calcium antagonists or other ingredients of the preparation. Cardiogenic shock. Hypotension (systolic blood pressure <90 mmHg). Significant narrowing of the left arterial outlet. Condition after acute myocardial infarction (within the first 4 weeks). Unstable angina is painful. Concomitant use of rifampicin. Pregnancy and breastfeeding.
Precautions:
Exercise caution and carefully monitor patients with uncorrected (unstable) heart failure and patients with sick sinus syndrome (without pacemaker). As with other substances that act on blood vessels, nitrendipine with immediate release, especially at the beginning of treatment, may experience angina pectoris. Exercise caution and monitor blood pressure in patients with severe hepatic impairment (the effect of the preparation may be severe and / or prolonged); in patients with chronic renal failure; during combination therapy with drugs that inhibit or induce CYP3A4 (see interactions). Calcium antagonists in rare cases may cause gingival hyperplasia; it is necessary to maintain proper oral hygiene (regular teeth cleaning, plaque control). The use of nitrendipine in children and adolescents aged 18 years is not recommended due to lack of data on safety and efficacy. Due to the lactose content, the preparation should not be used in patients with rare hereditary galactose intolerance, Lapp lactase deficiency or malabsorption of glucose-galactose. Due to the content of cochineal red, 10 mg tablets can cause allergic reactions.
Pregnancy and lactation:
The drug is contraindicated during pregnancy and breastfeeding. In individual cases of fertilizationin vitro the use of calcium antagonists was associated with reversible biochemical changes in the sperm head that could cause sperm abnormalities; in men who repeatedly failed and determined the reason they tried to become fathers through fertilizationin vitro, calcium antagonists should be considered as a possible cause of failure; when planning a pregnancy, alternative treatments may be considered for fertility disorders.
Side effects:
Very common: headache (especially at the beginning of treatment, transient), peripheral edema (especially at the beginning of treatment, transient), sudden redness of the face (especially at the beginning of treatment, transient). Common: anxiety reactions, angina pectoris, and in patients with pre-existing angina pectoris - an increase in the frequency, duration or severity of seizures (especially at the beginning of treatment), palpitations, tachycardia, vasodilatation, bloating, malaise. Uncommon: allergic reaction (including skin reactions and angioneurotic edema), sleep disturbances, paresthesia, central dizziness, fatigue, syncope, migraine, drowsiness, hypoaesthesia, blurred vision, blurred labyrinthosis, tinnitus, pain in the chest, hypotension, shortness of breath, nosebleed, nausea, vomiting, stomach, intestinal and stomach pain, diarrhea, constipation, dry mouth, indigestion, gastroenteritis, gonorrhea, hepatic dysfunction (transient hepatic enzymes), hypersensitivity reactions (pruritus, urticaria, rash, hypersensitivity to light), muscle pain, arthralgia, more frequent urination, polyuria, unusual pain, weight gain, excessive sweating. Rare: leukocytoclastic vasculitis. Very rare: leukopenia, agranulocytosis, myocardial infarction, exfoliative dermatitis, erectile dysfunction, gynecomastia, menorrhagia, fever. When using calcium antagonists severe skin reactions (including erythema multiforme or Stevens-Johnson syndrome) may occur, which disappear after discontinuation of the drug.
Dosage:
Orally. Adults: treatment starts at a dose of 5-10 mg once a day. The dose adjustment period consists of increasing the dose by 5 to 10 mg at weekly intervals, under the control of blood pressure within 24 hours of taking the drug, to achieve diastolic blood pressure <90 mmHg or blood pressure <140/90 mmHg (in hypertensive patients and diabetes mellitus or renal insufficiency <130/80 mmHg). Beginning with a pre-dose of 20 mg increases the incidence of side effects twice. The maximum dose is 40 mg / day, given in 2 divided doses, every 12 hours. During long-term treatment, the dose can be reduced to 10 mg a day.Special groups of patients. In the elderly and people with hepatic impairment it is recommended to start treatment with a dose of 5 mg once a day and gradually increase the daily dose by 5 mg under the control of blood pressure; it is often possible to achieve the desired reduction in blood pressure using a dose of 5-10 mg 2 times a day. If a significant reduction in blood pressure occurs despite a low dose, treatment should be changed. Caution should be exercised when increasing the dose in the elderly. No dose adjustment is necessary for patients with impaired renal function.Way of giving. The tablets should be taken after a meal with a sufficient amount of liquid (eg a glass of water). Do not drink grapefruit juice. Since nitrendipine is sensitive to light, the tablets should be removed from the blister just before use. The 10 mg tablets have a dividing groove enabling division into 2 parts.
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