Reduces current extracellular calcium into cardiomyocytes and smooth muscle cells of the coronary and peripheral arteries; at high doses inhibits the release of calcium ions from intracellular stores. It reduces the number of operating channels, without affecting the time of activation, inactivation and recovery. Dissociative trenbolone enanthate processes of excitation and contraction in the myocardium mediated by tropomyosin and troponin, and vascular smooth muscle mediated by calmodulin. At therapeutic doses, it normalizes the transmembrane current of calcium ions, disrupted in a number of pathological conditions, especially in arterial hypertension. No effect on venous tone. It increases coronary blood flow, and improves blood flow to ischemic areas of the myocardium without the development of the phenomenon of “steal”, activates the functioning of collaterals.
It improves myocardial function, reduces the force of heart rate and myocardial oxygen demand. Expanding the peripheral arteries, lowers blood pressure (BP) and reduce total peripheral resistance and afterload on the heart. Almost no effect on sinuauricular and atrioventricular nodes, has a weak anti-arrhythmic activity. It increases renal blood flow, causing a mild natriuresis. The negative chrono-, Drome and inotropic effect overlaps reflex activation simpatoadrenalovoj system in response to peripheral vasodilation.
Inhibits Platelet aggregation has antiatherogenic properties (especially with prolonged use). Lowers blood pressure in the pulmonary artery, it has a positive impact on the blood supply to the brain vessels.Time of onset of therapeutic effect when administered 20 minutes, the effect of the duration of 24 hours.
drug has a high absorption ratio – greater than 90%. Bioavailability ranges from 43% to 77%. It has the effect of “first pass” through the liver. Food intake increases the bioavailability of the drug. The drug provides a gradual release of active ingredient into the systemic circulation, where the maximum concentration achieved within 1.2 – 4.0 hours. Contact with blood plasma proteins – is high (92-98%). It is metabolized in the liver. Active metabolites have been identified.
The half-life ranged from 3.8 to 16.9 hours. Report from the body mainly by the kidneys in the form of inactive metabolites (70-80% of the dose). Nifedipine is not cumulated in the body. In small amounts it penetrates the blood-brain barrier, excreted in breast milk. Chronic renal failure, hemodialysis and peritoneal dialysis have no effect on the pharmacokinetics of the drug.
Long-term use of the drug (2-3 months) accompanied by the development of tolerance.
- Angina (voltage, trenbolone enanthate stable without vasospasm, stable vasospastic, the ineffectiveness of beta-blockers and nitrates);
- hypertension (including renovascular);
- Reynaud’s syndrome;
- pulmonary hypertension.
- Hypersensitivity to nifedipine or other components of the drug;
- acute myocardial infarction;
- cardiogenic shock;
- severe hypotension (systolic blood pressure below 90 mm Hg);
- heart failure in the stage of decompensation;
- pronounced aortic stenosis;
- idiopathic hypertrophic subaortic stenosis;
- pregnancy and lactation;
- age of 18 years (effectiveness and safety have been established).
Be wary appoint patients with chronic heart failure with stable, severe violations of cerebral circulation, diabetes, malignant hypertension, patients who are na hemodialysis (because of the risk of hypotension), in patients with renal and / or hepatic insufficiency, severe stenosis of the mitral valve, bradycardia and / or tachycardia, sick sinus syndrome, myocardial infarction with left ventricular failure, obstruction of the gastrointestinal tract, old age.
Dosing and Administration
Inside during or after a meal, washed down with a little water. The batch is individually, depending on the severity of the disease and the patient’s response to therapy.
Initial dose: 1 tablet (20 mg), 2 times a day. If necessary, the dose may be increased to two tablets (40 mg). The maximum daily dose – 120 mg. In elderly patients or patients receiving the combination (antianginal or antihypertensive) treatment usually prescribed lower doses of nifedipine.
Side effect On the part of the cardiovascular system: tachycardia, arrhythmias, peripheral edema (ankles, feet, legs), symptoms of excessive vasodilatation (asymptomatic decrease in blood pressure, “tides” of blood to the skin of the face, facial flushing, hot flashes), excessive reduction of blood pressure (rarely), fainting, development or exacerbation of congestive heart failure (often aggravating already existing). Some patients (especially those trenbolone enanthate with severe obstructive coronary artery disease) at the beginning of treatment or when increasing the dose may cause strokes, until the development of myocardial infarction (requires discontinuation of the drug).
On the part of the central nervous system: headache, dizziness, fatigue, asthenia, somnolence. Prolonged ingestion of high doses – paresthesias of extremities, tremor, extrapyramidal (parkinsonian) disorders (ataxia, masklike face, shuffling gait, stiffness of the joints of the hands or feet, tremor of the hands and fingers, difficulty in swallowing), depression. From the digestive system: dry mouth, increased appetite, dyspepsia (nausea, diarrhea or constipation); rarely – gingival hyperplasia (bleeding, pain, swelling), with a long reception – human liver (intrahepatic cholestasis, increased activity of “liver” transaminases).
From the side of blood: anemia, leukopenia, thrombocytopenia, thrombocytopenic purpura, agranulocytosis asymptomatic.
From the mochevydelitelnoy system: an increase in daily urine, worsening of renal function (in patients with renal insufficiency).
Allergic reactions: rarely – itching, hives, rash, autoimmune hepatitis.
From the musculoskeletal system: rarely – arthralgia, swelling of the joints, myalgia.
Other: rarely – visual disturbances (including transient loss of vision), gynaecomastia (in older patients, disappearing completely after the cancellation), galactorrhea, hyperglycemia, pulmonary edema (shortness of breath, cough, stridor), weight gain.
Interaction with other drugs
reduces the concentration of quinidine in blood plasma.
Increasing the concentration of digoxin and theophylline in blood plasma, and therefore should be controlled and the clinical effect of theophylline and digoxin concentration in the blood plasma.
Inductors of microsomal liver enzymes (rifampicin, etc.) Reduce the concentration of nifedipine.
Marked reduction of blood pressure increase other antihypertensive drugs, nitrates, cimetidine (metabolic suppression, ranitidine and famotidine are not significantly affect the metabolism iifedipina), inhaled anesthetics, tricyclic antidepressants and diuretics.
In combination with nitrates amplified tachycardia.
The hypotensive effect of reducing sympathomimetic, nonsteroidal anti-inflammatory drugs (prostaglandin synthesis inhibition in the kidney and sodium retention and body fluids), estrogens (fluid retention).Calcium can reduce the effect of blockers “slow” calcium channels.
May displace from its association with proteins, drugs, characterized by a high degree of binding (including indirect anticoagulants – coumarin derivatives and indandiona, anticonvulsant drugs nesteroidiye anti-inflammatory trenbolone enanthate quinine, salicylates, sulfinpyrazone), so that they may rise in plasma concentration.