2010/06/24

(Adalat Sl

Composition, structure and packing

dragee

drops for oral administration

capsules

solution for infusion,

tablets

coated tablets,

tablets with prolonged action,

Long-acting tablets coated

Clinico-pharmacological group: Calcium channel blockers

Pharmacological action

Selective BCCI, a derivative of 1,4-dihydropyridine.

Has vasodilatation, antianginal and hypotensive action.

Reduces Ca2 + current in cardiac myocytes and smooth muscle cells of coronary and peripheral arteries in high doses inhibits Ca2 + release from intracellular stores.

Reduces the number of active channels, without affecting the time of their activation, inactivation and recovery.

Separates the processes of excitation and reduction in the myocardium mediated by tropomyosin and troponin, and in smooth muscles of blood vessels mediated by calmodulin.

In therapeutic doses, normalizes the transmembrane current of Ca2 +, broken in several pathological states, particularly in arterial hypertension. It has no effect on the tone of veins.

Increases coronary blood flow, improves blood flow to ischemic areas of myocardium without the development of the phenomenon of "steal", activates the functioning of the collaterals. Expanding the peripheral arteries, reduces TPVR, tone of myocardial afterload, myocardial oxygen demand and increases the duration of LV diastolic relaxation. Virtually no effect on SA and AV nodes and has no antiarrhythmic activity.

Increases renal blood flow, causing moderate natriuresis.

The negative chrono-, Drome and inotropic effects offset reflex activation of the sympathoadrenal system and increases heart rate in response to peripheral vasodilation.

Time of onset of effect: 20 minutes - when taken orally, 5 minutes - at the sublingual capsules; duration of effect: 4-6 hours - for tablets and capsules, 12-24 h - for prolonged forms.

Statement
angina (voltage, stable without Angiospasm, vasospastic stable, unstable with vasospastic ineffectiveness of beta-blockers and nitrates);
hypertension (including renovascular), cupping hypertensive crisis;
disease and Raynaud syndrome;
spasm of the coronary arteries (in the course of diagnostic or therapeutic intervention - percutaneous transluminal coronary angioplasty, recanalization of vessels or coronary artery bypass grafting);
Differential diagnosis between functional and organic stenosis of the coronary arteries in hypertension "small" circle of blood circulation.

Dosage regimen

The maximum daily dose of short-nifedipine - 40 mg.

For continuous use is recommended to use prolonged forms of nifedipine, the maximum single dose - 30 mg daily dose - 180 mg of.

Sublingvalno: PNDS crises - 10 mg every 30 min (total dose to 40 mg), under the close supervision of blood pressure and heart rate.

After receiving the patient should be in position "lying" for 30-60 minutes.

The drug, taken orally, during or after a meal, washed down with sips of water, 10 mg 2-4 times a day.

In case of insufficient severity of the effect may increase the dose (if the transition to prolonged form) to 80-120 mg / day (depending on the drug) for 7-14 days.

When angina is recommended to begin therapy with 10 mg 3 times daily, with gradual increase in dose to 10 mg every 4-5 days.

In vasospastic angina appoint prolonged form in a dose of 80 mg / day.

In the genesis of unstable angina, etc. - only in combination with beta-blockers, in doses of 80 mg / day. For tablets with prolonged action - 30-60 mg 1 time a day.

Older patients or patients receiving combination (or antianginal antihypertensive) therapy, are usually assigned lower doses.

If any functions of the liver in patients with severe stroke dose should be reduced.

Acceptance of the drug in / drip for cupping gipertonichekogo crisis or an attack of angina pectoris: the rate of infusion should be 0.6-1.2 mg / h, the maximum daily dose - 30 mg, duration of treatment - 2-3 days.

To continue the therapy is appropriate translation prolonged oral form.

Intracoronary drug taking: when spasm of the coronary vessels - of 0.1-0.2 mg.

Patients with severe stenosis of the main trunk coronary artery therapy should begin with a dose of 0.05-0.1 mg, observing extreme caution. You should not to exceed a total dose of 1.2 mg for 3 hours duration of action is 5-15 min.

Intracoronary administration carried out during invasive interventions through the coronary catheter, located directly in the coronary artery. Introduction must be done evenly, slowly, over a 90-120. In the presence of two vascular obstruction can not do the injection in the third, open vessel, as usually a small negative inotropic effect in this case can cause serious complications.

Side effect

From the CCC:

tachycardia, arrhythmias, peripheral edema (ankles, feet, legs), the manifestations of excessive vasodilation (an asymptomatic decrease in blood pressure, "tides" of blood to the skin of the face, facial flushing, hot flashes), excessive blood pressure reduction (rare), syncope, development or exacerbation CH (most aggravating already existing).

Some patients (especially those with severe obstructive coronary artery) in the beginning of treatment or increasing the dose may cause angina attacks, until the development of myocardial infarction (requires discontinuation of the drug).

Of the nervous system:

headache, dizziness, fatigue, asthenia, somnolence.

With long-term ingestion of high doses - paresthesias of extremities, tremor, extrapyramidal (Parkinson) of violation (ataxia, masklike face, shuffling gait, stiff arms or legs, tremor hands and fingers, difficulty in swallowing), and depression.

The part of the digestive system:

dry mouth, increased appetite, dyspepsia (nausea, diarrhea or constipation);

rarely - gum hyperplasia (bleeding, pain, swelling), Propafenone - dysfunction of the liver (intrahepatic cholestasis, increased activity of "liver" of transaminases).

From the musculoskeletal system:

rarely - arthralgia, joint swelling, myalgia.

From the side of hematopoiesis:

anemia, leukopenia, thrombocytopenia, thrombocytopenic purpura, asymptomatic agranulocytosis.

From the urinary system:

increase in daily diuresis, worsening renal function (in patients with renal insufficiency).

Allergic reactions:

rarely - itching, hives, rash, autoimmune hepatitis.

Local reactions:

burning in place of / in the introduction.

Other:

rarely - visual impairment (including transient loss of vision on the background plasma Cmax), gynecomastia (in elderly patients, completely disappeared after the withdrawal), galactorrhea, hyperglycemia, edema of the lung (shortness of breath, cough, crowing breathing), weight gain body.

Antidote is drugs Ca2 +: shows a slow i / v injection of 10% CaCl2 or calcium gluconate, and switched to long-term infusion.

In marked decrease in blood pressure - in / to the introduction of dopamine or dobutamine.

When violations conductivity - atropine, isoprenaline or artificial pacemaker.

With the development of CH - in / introduction of strophanthin. Catecholamines should be used only when life is threatened (due to their low efficiency requires a high dosage, resulting in an increased risk of arrhythmias).

We recommend monitoring of blood glucose concentrations (may be reduced release of insulin) and electrolytes (K +, Ca2 +). Hemodialysis is ineffective.

Contraindications
hypersensitivity
severe hypotension (systolic blood pressure below 90 mm Hg),
pregnancy
lactation.

C Precautions:

marked stenosis of aortic or mitral valve GOKMP, pronounced bradycardia or tachycardia, SSS, CHF, mild or moderate hypotension, severe ischemic attacks, myocardial infarction with left ventricular failure, obstruction of the gastrointestinal tract (for slow-release forms), hepatic failure, renal failure (particularly patients undergoing hemodialysis - a high risk of excessive BP reduction and serendipity), advanced age, children's age to 18 years (efficacy and safety have not been studied).

Pregnancy and lactation

Acceptance of the drug during pregnancy and lactation is prohibited.

Cautions

During the period of treatment must refrain from receiving ethanol. Despite the lack of BCCI syndrome "cancel" before the cessation of treatment is recommended a gradual reduction in dose.

The simultaneous appointment of beta-blockers should be conducted under careful medical supervision, because it may lead to excessive lowering of blood pressure, and in some cases - the aggravation of the phenomena CH.

Do not spend time in / therapy beta-adrenoceptor blockers and intracoronary administration of nifedipine. During treatment, the possible positive results during the direct reaction of Coombs and laboratory tests Antinuclear antibodies. It is important to the regularity of treatment, regardless of the illness, since the patient can not feel the symptoms of hypertension.

Diagnostic criteria of appointment of the drug with vasospastic angina are: classical clinical picture is accompanied by-segment elevation ST; emergence of ergonovine-induced angina, or spasm of the coronary arteries in coronary angiography to identify or detect angiospastic component without confirmation (eg with different threshold voltage or unstable angina when ECG evidence of transient Angiospasm).

It should be borne in mind that in the beginning of treatment may be angina, especially after recent abrupt cancellation of beta-blockers (the latter recommended to cancel gradually).

Precautions should be administered simultaneously with dizopiramid and flekainamidom because of the possible increase in inotropic effect. If during therapy the patient requires a surgical intervention under general anesthesia, must inform the physician-anesthesiologist about the nature of the treatment.

Caution must be exercised in elderly patients because the most likely age renal dysfunction.

During the treatment you should be careful when driving and other lesson potentially hazardous activities that require high concentration and speed of psychomotor reactions.

Overdose

Symptoms: headache, flushing skin, long marked reduction of blood pressure, suppressing the function of sinus node bradycardia, bradyarrhythmia.

Treatment: with severe poisoning (collapse, inhibition of the sinus node) conduct gastric lavage, activated charcoal designate

Drug Interactions

Reduces the concentration of quinidine in plasma. Increasing the concentration of digoxin in plasma, and therefore should be monitored clinical effect and the concentration of digoxin in plasma. Inductors microsomal liver enzymes (rifampicin, etc.) reduce the concentration of nifedipine. BP decrease reinforce other antihypertensive drugs, nitrates, cimetidine (suppression of metabolism ranitidine and famotidine did not significantly affect the metabolism of BCCI), inhaled anesthetics, diuretics, and tricyclic antidepressants. In combination with nitrates increases tachycardia.

Antihypertensive effect of reducing sympathomimetic, NSAIDs (inhibition of synthesis of Pg in the kidneys and delay Na + and fluid in the body), estrogens (fluid retention in the body). Preparations of Ca2 + can reduce the effect of BCCI. Maybe being squeezed out of context with protein drugs characterized by a high degree of binding (including the indirect anticoagulants - coumarin derivatives and indandiona, anticonvulsant drugs, NSAIDs, quinine, salicylates, sulfinpirazon), so that could increase their concentration in plasma. Inhibits metabolism prazozina and other alpha-blockers, resulting in possible increased hypotensive effect. Preparations of Li + may enhance the toxic effects (nausea, vomiting, diarrhea, ataxia, tremor, tinnitus). Procainamide, quinidine and other drugs causing prolongation of the interval QT, reinforce the negative inotropic effect and may increase the risk of significant lengthening of the interval QT. In infusions of nifedipine as a solvent use ethanol, that must be considered in combination with drugs, with inconsistent. It is unacceptable intracoronary administration of nifedipine together with other drugs.

Terms and Conditions of storage

In a dry, dark place at temperatures not above 30 ° C.

Shelf life - 5 years.