Nitrendipine (Nitrendipine) - instructions for use, description, pharmacological action, indications for use, dosage and method of administration, contraindications, side effects. Medicinal reference book geotar Application for violations of liver function

Pharmacological action - antianginal, vasodilating, hypotensive, nephroprotective.
Specifically binds to membrane receptors that regulate the function of voltage-gated L-type calcium channels, reduces the flow of calcium ions into the cell during membrane depolarization. Predominantly affects vascular smooth muscle cells (less coronary than td;). It has a highly selective long-term vasodilating effect. It causes systemic vasodilation, a decrease in peripheral vascular resistance, and, as a result, hypotension. Lowers blood pressure in proportion to the dose, does not cause orthostatic hypotension and the development of tolerance, does not violate the circadian rhythm of blood pressure changes. Expands the vessels of the kidneys, increases the content of atrial natriuretic peptide in the blood, increases the excretion of sodium and water, does not activate the sympathoadrenal (heart rate usually does not change) and renin-aldosterone (the content of angiotensin and renin in plasma does not increase significantly) systems. However, at the beginning of therapy, short-term reflex tachycardia may occur. Does not affect the sinus and AV nodes. After taking 20 mg of nitrendipine in patients with mild to moderate hypertension, there is a decrease in SBP and diastolic blood pressure by 15-20%.
It is effective both in monotherapy and in combination with hypothiazide and propranolol. Long-term therapy contributes to the reverse development of left ventricular hypertrophy and the manifestation of a nephroprotective effect. The greatest hypotensive effect is observed in elderly patients with low level plasma renin. In elderly patients (60 years and older) with isolated systolic hypertension (systolic blood pressure of at least 160 mm BP with diastolic blood pressure below 95 mm) when used for 2 years (initial dose - 10 mg / day, then up to 20-40 mg / day in 2 doses) prevents the development of cardiovascular complications: reduces the overall frequency of cerebral strokes by 42%, the frequency of cardiac complications (heart failure, myocardial infarction, sudden death) - by 26%, the frequency of all cardiovascular complications - by 31%. With sublingual application, the possibility of cupping is shown hypertensive crisis. At a dose of 10–20 mg / day, it is effective (especially with continuous therapy for many years) to prevent attacks of vasospastic angina and improve long-term prognosis.
When taken orally, it is rapidly and almost completely absorbed. Bioavailability - 60-70%. Cmax in plasma is reached after 1-2 hours, the plasma level is 9-42 ng / ml, it binds to blood proteins by 98%. Almost completely metabolized in the liver by oxidation. Excreted in the urine (30%) in the form of four polar metabolites, T1 / 2 ranges from 8-24 Total Cl - 1.3 l / min. In the elderly and patients with cirrhosis of the liver, T1 / 2 and blood concentrations increase (a decrease in the daily dose is required). It has a teratogenic effect.

- a drug of the calcium channel blockers group, is a derivative of dihydropyridine.

Description of the pharmacological properties of the drug Nitrendipine

The drug has a hypotensive, vasodilating, nephroprotective and antianginal effect.

It has a predominant effect on the cells of the ugly muscles of the vessels (to a lesser extent - coronary).

Nitrendipine lowers blood pressure without causing orthostatic hypotension, without disturbing the circadian rhythm of changes in blood pressure. Also, the drug dilates the renal vessels, promotes an increase in the blood of atrial natriuretic peptide substance. Besides active ingredient increases the excretion of water and sodium without activating the sympathoadrenal system. But at the beginning, during treatment, reflex short-term tachycardia can be observed. Has a teratogenic effect. By oxidation, it is almost completely metabolized in the liver cells.

Indications for use

The drug Nitrendipine is indicated in cases of heart failure, angina pectoris (stable without angiospasm), vasospastic angina, unstable vasospastic, as well as in the ineffectiveness of nitrates and beta-blockers, with (shown as a symptomatic treatment).

Analogues of Nitrendipine

Analogues of the drug Nitrendipine in this case are drugs that have the same active substance nitrendipine.

These are drugs such as:

• Bypress;
• Lusopress;
• Nitrepin;
• Unipress;
• Octidipine.

All these medicines have the same indications for use as the drug in question.

pharmachologic effect

Indications for use

Mode of application

Side effects

Contraindications

Release form

Storage conditions

Synonyms

Active substance:

The authors

Links

• The official instructions for the drug Nitrendipine.
• Modern medications: a complete practical guide. Moscow, 2000. S. A. Kryzhanovsky, M. B. Vititnova.

Name:

Nitrendipine (Nitrendipine)

Pharmachologic effect:

Like nifedipine and other drugs in this group, it is an antagonist of calcium ions, but it has a predominant effect on peripheral blood vessels. Reduces vascular resistance. It has little effect on the excitability of the heart and conduction of excitation. It has a long-term effect (for long-term therapy, a single dose per day is sufficient).

Indications for use:

Taken with various forms of arterial hypertension (raising blood pressure).

Application method:

Usually appoint 0.02 g (20 mg) 1 time per day (in the morning). Depending on the effect and tolerability, gradually increase the daily dose to 40 mg in 2 doses or reduce the dose to 10 mg 1 time per day. The daily dose should not exceed 0.04 g (40 mg).

Undesirable phenomena:

Nitredipine is generally well tolerated. However, reddening of the face and skin of the upper body, headache are relatively common, probably associated with a decrease in the tone of the cerebral (cerebral) vessels (mainly capacitive) and their stretching due to an increase in blood flow through arteriovenous anastomoses (connections of the artery and vein). In these cases, the dose is reduced or the drug is taken after meals. Palpitations, nausea, dizziness, swelling of the lower extremities, hypotension (lowering blood pressure), and drowsiness are also possible.

Contraindications:

Severe forms of heart failure, unstable angina, acute myocardial infarction, sick sinus syndrome (heart disease accompanied by rhythm disturbance), severe arterial hypotension (low blood pressure). Nitredipine is contraindicated in pregnancy and lactation. Caution is needed when prescribing the drug to drivers of transport and other professions that require a quick mental and physical reaction.

Release form of the drug:

Tablets of 0.02 g (20 mg) and 0.01 g (10 mg).

Storage conditions:

Drug from list B. In a dark place.

Synonyms:

Baypress, Nitrepin, Lusopress, Unipress.

Similar drugs:

Nisoldipine (Nisoldipine) Foridon (Foridonum) Isradipine (Isradipine) Lacidipine (Lacidipine) Nicardipine (Nicardipine)

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"Nitrendipine (Nitrendipine)" used in the treatment and/or prevention the following diseases(nosological classification - ICD-10):

Molecular formula: C18-H20-N2-O6

CAS Code: 39562-70-4

Description

Characteristic: A derivative of 1,4-dihydropyridine is a calcium antagonist of the second generation.

pharmachologic effect

Pharmacology: Pharmacological action - hypotensive, vasodilating, antianginal, nephroprotective. Specifically binds to membrane receptors that regulate the function of voltage-gated L-type calcium channels, reduces the flow of calcium ions into the cell during membrane depolarization. It mainly affects the smooth muscle cells of the vessels (less coronary than others). It has a highly selective long-term vasodilating effect. It causes systemic vasodilation, a decrease in peripheral vascular resistance, and, as a result, hypotension. Lowers blood pressure in proportion to the dose, does not cause orthostatic hypotension and the development of tolerance, does not violate the circadian rhythm of blood pressure changes. Expands the vessels of the kidneys, increases the content of atrial natriuretic peptide in the blood, increases the excretion of sodium and water, does not activate the sympathoadrenal (heart rate usually does not change) and renin-aldosterone (the content of angiotensin and renin in plasma does not increase significantly) systems. However, at the beginning of therapy, short-term reflex tachycardia may occur. Does not affect the sinus and AV nodes. After taking 20 mg of nitrendipine in patients with mild to moderate hypertension, there is a decrease in SBP and diastolic blood pressure by 15-20%.

It is effective both in monotherapy and in combination with hypothiazide and propranolol. Long-term therapy contributes to the reverse development of left ventricular hypertrophy and the manifestation of a nephroprotective effect. The greatest hypotensive effect is observed in elderly patients with low plasma renin levels. In elderly patients (60 years and older) with isolated systolic hypertension (systolic blood pressure of at least 160 mm Hg with diastolic blood pressure below 95 mm Hg) when used for 2 years (initial dose - 10 mg / day, then - up to 20-40 mg / day in 2 doses) prevents the development of cardiovascular complications: reduces the overall frequency of cerebral strokes by 42%, the frequency of cardiac complications (heart failure, myocardial infarction, sudden death) - by 26%, the frequency of all cardiovascular vascular complications — by 31%. With sublingual application, the possibility of stopping a hypertensive crisis has been shown. At a dose of 10-20 mg / day, it is effective (especially with continuous therapy for many years) to prevent attacks of vasospastic angina and improve long-term prognosis.

When taken orally, it is rapidly and almost completely absorbed. Bioavailability - 60-70%. C_max in plasma achieved through 1-2 hours, plasma levels - 9-42 ng/ml, binds to blood proteins by 98%. Almost completely metabolized in the liver by oxidation. Excreted in the urine (30%) in the form of four polar metabolites, T_1/2 ranges from 8-24 hours Total Cl - 1.3 l/min. In the elderly and patients with cirrhosis of the liver T_1/2 and the concentration in the blood increases (requires a decrease in the daily dose). It has a teratogenic effect.

Indications for use

Application: Arterial hypertension (monotherapy or in combination with beta-blockers and diuretics), diabetic nephropathy (if there are contraindications to the appointment or intolerance to ACE inhibitors).

Contraindications

Contraindications: Severe forms of heart failure, sick sinus syndrome, aortic stenosis, severe arterial hypotension, the first week after myocardial infarction, pregnancy, breastfeeding.

Use during pregnancy and lactation: Contraindicated in pregnancy. At the time of treatment should stop breastfeeding.

Side effects

Side effects: From the side of cardio-vascular system and blood (hematopoiesis, hemostasis): flushing of the skin of the face and upper body, hypotension, tachycardia, anemia, thrombocytopenia.

From the side nervous system and sensory organs: headache, drowsiness, paresthesia; rarely - visual impairment, myalgia, tremor (at higher doses).

From the genitourinary system: peripheral edema (swelling of the ankles, lower extremities); rarely - an increase in the frequency of urination; deterioration of kidney function (with renal failure).

On the part of the digestive tract: nausea, feeling of fullness in the stomach, vomiting, constipation; rarely - diarrhea; in some cases, intrahepatic cholestasis.

From the side skin: erythema, pruritis, urticaria, maculopapular exanthema.

Others: withdrawal syndrome (5-10%); rarely - gingival hyperplasia, increased levels of transaminases, gynecomastia (in elderly patients).

Interaction: Antihypertensive drugs, blockers H_2-histamine receptors increase the effect, estrogens, NSAIDs - weaken. May increase the plasma concentration of cardiac glycosides with the development of toxic effects. Metoprolol, acebutolol, atenolol and ranitidine may decrease plasma clearance.

Dosage and method of application

Dosage and administration: Inside, usually 20 mg in the morning. Depending on the effect and tolerability, the daily dose can be gradually increased to a maximum of 40 mg (20 mg 2 times a day) or reduced to 10 mg.

Precautions: Use with caution while driving Vehicle and people whose profession is associated with increased concentration of attention. During treatment, you must refrain from drinking alcohol.