Composition
Active ingredients:
nifedipine – 10 mg;
Auxiliary substances:
magnesium stearate,
microcrystalline cellulose,
lactose monohydrate,
potato starch,
colloidal silicon dioxide (aerosil),
povidone (low molecular weight medical polyvinylpyrrolidone).
Pharmacological action
Nifedipine is a selective blocker of “slow calcium ropes”, a derivative of 1,4-dihydropyridine. It has antianginal and antihypertensive effects. Reduces the flow of extracellular calcium ions into cardiomyocytes and smooth muscle cells of coronary and peripheral arteries.
Reduces spasm and dilates coronary and peripheral (mainly arterial) vessels, reduces blood pressure, total peripheral vascular resistance, reduces afterload and myocardial oxygen demand. Increases coronary blood flow. The negative chrono -, dromo -, and inotropic effects are overlaid by reflex activation of the sympathoadrenal system in response to peripheral vasodilation. Increases renal blood flow, causes moderate natriuresis. The time of onset of the clinical effect is 20 minutes, the duration of the clinical effect is 4-6 hours
. Pharmacokinetics
Nifedipine is rapidly and almost completely (more than 90%) absorbed from the gastrointestinal tract. After oral use, its bioavailability is 40-60%. Food intake increases bioavailability. It has a “first pass” effect through the liver.
The maximum concentration in blood plasma is observed after 1-3 hours and is 65 ng / ml. Penetrates through the blood-brain and placental barrier, is excreted in breast milk. Binding to plasma proteins is 90%. It is completely metabolized in the liver.
It is excreted by the kidneys in the form of inactive metabolites (70-80% of the dose taken). The elimination half-life is 2-4 hours. There is no cumulative effect. Chronic renal failure, hemodialysis and peritoneal dialysis do not affect the pharmacokinetics. With prolonged use (for 2-3 months), tolerance to the action of the drug develops.
Indications
Ischemic heart disease – angina pectoris of tension and rest (including variant); arterial hypertension (in the form of monotherapy or in combination with other antihypertensive drugs).
Contraindications
- hypersensitivity to nifedipine and other derivatives of dihydropyridine;
- acute phase of myocardial infarction (first 4 weeks);
- cardiogenic shock, collapse;
- hypotension (systolic blood pressure below 90 mm Hg. St. )
- the syndrome of weakness of the sinus node;
- heart failure (decompensation);
- pronounced aortic stenosis;
- pronounced mitral stenosis;
- tachycardia;
- idiopathic hypertrophic subaortic stenosis;
- pregnancy, lactation;
- age to 18 years (efficacy and safety not established).
Use with caution in patients with: Â patients with chronic heart failure, severe liver and/ or kidney function disorders, severe cerebrovascular disorders, diabetes mellitus, malignant arterial hypertension, patients undergoing hemodialysis (due to the risk of arterial hypotension).
Side effects
From the cardiovascular system: Â hyperemia of the face, feeling hot, tachycardia, peripheral edema (ankles, feet, shins), excessive decrease in blood pressure (BP), syncope, heart failure, in some patients, especially at the beginning of treatment, angina attacks may occur, which requires discontinuation of the drug.
Nervous system disorders: Â headache, dizziness, fatigue, drowsiness. With prolonged oral use in high doses – paresthesia of the extremities, tremor.
From the gastrointestinal tract, liver: Â dyspeptic disorders (nausea, diarrhea or constipation), with prolonged use – impaired liver function (intrahepatic cholestasis, increased activity of “hepatic” transaminases).
From the musculoskeletal system: Â arthritis, myalgia.
Allergic reactions: Â pruritus, urticaria, exanthema, autoimmune hepatitis.
From the side of hematopoietic organs: Â anemia, leukopenia, thrombocytopenia, thrombocytopenic purpura.
From the urinary system: Â increased daily diuresis, deterioration of renal function (in patients with renal insufficiency).
Other services: Â “hot flashes” of blood to the skin of the face, changes in visual perception, gynecomastia (in elderly patients, completely disappearing after withdrawal), hyperglycemia, gum hyperplasia.
Interaction
The severity of lowering blood pressure increases when nifedigshna is co-administered with other antihypertensive drugs, cimetidine, ranitidine, diuretics and tricyclic antidepressants.
In combination with nitrates, tachycardia and the hypotensive effect of nifedish increase.
Concomitant use of beta-blockers should be carried out under close medical supervision, since this can lead to too pronounced a decrease in blood pressure, and in some cases – an aggravation of the symptoms of heart failure.
Nifedipine reduces the concentration of quinidine in the blood plasma. Increases the concentration of digoxin and theophylpine in the blood plasma, and therefore the clinical effect and/or the content of digoxin and theophylline in the blood plasma should be monitored.
Rifampicin weakens the effect of nifedipine (accelerates the metabolism of the latter by inducing the activity of liver enzymes).
How to take, course of use and dosage
The dosage and course of treatment is determined by the attending physician in each case individually. The initial dose of Nifedipine is 1 pc. (10 mg) 2 times a day. If necessary, the dose can be increased to 2 pcs. (20 mg) 4 times a day. The maximum daily dose is 80 mg.
Overdose
Symptoms: Â headache, hyperemia of the facial skin, decreased blood pressure, sinus node depression, bradycardia, arrhythmia.
Treatment: Â gastric lavage with the use of activated charcoal, symptomatic therapy aimed at stabilizing the activity of the cardiovascular system. The antidote is calcium, slow intravenous use of 10% calcium chloride or calcium gluconate is indicated, followed by switching to a long-term infusion.
With a marked decrease in blood pressure – intravenous use of dopamine or dobutamine. In case of conduction disorders, use of atropine, isoprenaline or the installation of an artificial pacemaker is indicated.
With the development of heart failure-intravenous use of strophanthin. Catecholamines should only be used in cases of life-threatening circulatory failure (due to their reduced effectiveness, a high dosage is required, which increases the risk of increasing the tendency to arrhythmia due to intoxication). Monitoring of blood glucose and electrolytes (potassium and calcium ions) is recommended, as the release of insulin is disrupted.
Hemodialysis is ineffective.
Special instructions
During treatment, it is necessary to refrain from engaging in potentially dangerous activities that require increased concentration of attention and speed of psychomotor reactions, and from using ethanol.
Discontinuation of the drug is carried out gradually (the risk of developing a “withdrawal” syndrome).
Form of production
Tablets
Storage conditions
In a place protected from light, at a temperature not exceeding 20 °C.
Shelf life
3 years
Active ingredient
Nifedipine
Conditions of release from pharmacies
By prescription
Dosage form
Tablets
Description
For adults as directed by your doctor
Indications
Hypertension, Angina
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