OSMO-Adalat 30 mg tablets # 28

OSMO-Adalat (OSMO-Adalat) instructions for use

pharmachologic effect

OSMO-ADALAT is a selective calcium antagonist with a predominant effect on blood vessels, a derivative of 1,4-dihydropyridine. The drug has a pronounced antianginal and hypotensive effect, reduces the transmembrane flow of calcium ions through slow calcium channels into myocardiocytes and smooth muscle cells of the coronary and peripheral arteries. When the drug is used, the tonus of smooth muscle arteiol decreases, resulting in an expansion of the spas coronary arteries and an increase in coronary blood flow. Lowering the tone of the smooth muscles of the coronary arteries, the drug prevents the appearance of coronary spasm, and with prolonged use - the formation of new atherosclerotic plaques in the coronary vessels. There is a reduction in myocardial oxygen demand, afterloading the heart by lowering the OPSS, which results in a lowering of blood pressure. With the use of nifedipine, the excretion of sodium and water from the body increases. The hypotensive effect of nifedipine is particularly pronounced in patients with AH. At the beginning of treatment with nifedipine, transient reflex tachycardia may occur and cardiac output may increase.

Indications

Treatment of AH, treatment of IHD - stable angina pectoris, including vasospastic (angina of Prinzmetal); prevention of angina pectoris attacks, as well as crises in AH patients.

Contraindications

Acute period of myocardial infarction (first 8 days), cardiogenic shock, severe aortic and mitral stenosis, heart failure in the stage of decompensation, severe arterial hypotension. Hypersensitivity to nifedipine, as well as the period of pregnancy and lactation. Age is up to 15 years.

special instructions

Impact on the ability to drive vehicles and manage mechanisms

Individual reaction of the body to Osmo-Adalat reception can cause a decrease in the speed of psychomotor reactions, a decrease in the ability to concentrate, which negatively affects the ability to drive and work with complex mechanisms.This is especially important to consider at the beginning of treatment, with the change of the drug and the simultaneous use of alcohol.

Composition

1 controlled release tablet coated with a coating contains:

Active substances:

Nifedipine 30 mg.

Excipients:

Gipromellose, magnesium stearate, polyethylene oxide, sodium chloride, cellulose acetate, polyethylene glycol 4000, Opadry OY-S-24914 (iron oxide red + titanium dioxide).

Dosing and Administration

For 30 mg - 1 tablet 1 time per day, 60 mg tablets - 1 tablet once a day. It is recommended to start treatment with 30 mg of nifedipine per day. Depending on the severity of the disease and individual patient response, the dose of nifedipine can be gradually increased to 120 mg / day. The maximum daily dose is 120 mg / day for 1 reception. If within 14 days of treatment of a patient with angina pectoris, it is impossible to achieve an adequate therapeutic effect, fast-acting forms of the drug should be prescribed.

Side effects

From the side of the cardiovascular system

≥1- <10% - a sensation of flushing of the blood to the face, palpitation, peripheral edema; ≥0.1- <1% - arterial hypotension (including Orthostatic hypotension),

Fainting, tachycardia, pain in the chest.

From the digestive system

≥1- <10% - constipation; ≥0.1- <1% - diarrhea, indigestion, bloating, nausea;

≥0.01- <0.1% - a violation of appetite, belching, gingivitis, gingival hyperplasia, increased activity of hepatic transaminases, intrahepatic cholestasis;

<0.01% - Dysphagia, esophagitis, intestinal obstruction, ulceration of the intestinal wall, jaundice.

From the side of the central nervous system and peripheral nervous system

≥1- <10% - Dizziness, headaches; ≥0.1- <1% - sleep disorders, nervousness, paresthesia, vertigo, drowsiness; ≥0.01- <0.1% - hyposthenia, tremor (at high doses), visual impairment; <0.01% is diplopia.

From the endocrine system

<0.01% - hyperglycemia, weight loss, gynecomastia.

From the respiratory system

≥0.1- <1% - dyspnea; ≥0.01 - <0.1% - nasal bleeding.

From the urinary system

≥0.1- <1% - an increase in daily diuresis; ≥0.01- <0.1% - dysuria, increased frequency of urination, impaired renal function (in patients with renal insufficiency).

From the musculoskeletal system

≥0.1- <1% - cramps in the calf muscles, Myalgia; ≥0.01 - <0.1% - arthralgia.

On the part of the hematopoiesis system

<0.01% - leukopenia, thrombocytopenic purpura.

Dermatological reactions

≥0.1- <1% - itching, rash (exanthema, erythema, urticaria); <0.01% - photodermatitis, exfoliative dermatitis.

Other

≥1- <10% - asthenia, weakness; ≥0.1- <1% - pain in the limbs; ≥0.01 - <0.1% - allergic reactions, chills, fever; <0.01% - anaphylactic reactions.

Drug Interactions

The antihypertensive effect of Osmo-Adalat can increase with the simultaneous use of other antihypertensive drugs, diuretics and ranitidine.

With the simultaneous application of Osmo-Adalat with beta-blockers, it is possible to develop severe arterial hypotension; in some cases - aggravation of heart failure (thorough medical control is necessary).

With simultaneous application of Osmo-Adalat with nitrates, tachycardia and arterial hypotension increase.

Nifedipine increases the concentration of theophylline in the blood plasma, and therefore it is necessary to monitor the clinical effect and the content of theophylline in the blood plasma.

The simultaneous use of Osmo-Adalat and digoxin can lead to a delay in the excretion of digoxin from the body and, consequently, to an increase in its concentration in the blood plasma (careful monitoring of the possible appearance of symptoms of an overdose of digoxin, and if necessary, a reduction in the dose of glycoside, taking into account its concentration in the blood plasma) .

When combined in some cases, nifedipine causes a decrease in the concentration of quinidine in the blood plasma, and when nifedipine is abolished, a significant increase in the concentration of quinidine in the blood plasma is possible (it is recommended to control the concentration of quinidine in the blood plasma and, if necessary, to correct its dose). When prescribing quinidine, patients receiving Osmo-Adalat should carefully monitor blood pressure. If necessary, the dose of nifedipine should be reduced.

Simultaneous application of Osmo-Adalat with cisapride may lead to an increase in the concentration of nifedipine in the blood plasma (careful monitoring of blood pressure is required, if necessary, the dose of nifedipine may be reduced).

Since diltiazem slows the withdrawal of nifedipine from the body, simultaneous therapy with these drugs should be conducted with caution, if necessary, reducing the dose of nifedipine.

Phenytoin is the inducer of the isoenzyme CYP3A4, so when Osmo-Adalat is used with phenytoin, the bioavailability, and consequently the effectiveness of nifedipine, is reduced. If necessary, the dose of Osmo-Adalat can be increased.After the cessation of treatment with phenytoin, an increased dose of Osmo-Adalat should be reduced.

Rifampicin is a strong inducer of the isoenzyme CYP3A4; therefore, when Osmo-Adalat is used together with rifampicin, the bioavailability and clinical efficacy of nifedipine decrease (combined treatment is contraindicated).

Studies of the interaction of nifedipine with carbamazepine, phenobarbital and valproic acid have not been conducted.Since it has been shown that by activating liver enzymes, carbamazepine, phenobarbital and valproic acid reduce the concentration in the plasma of another blocker of slow calcium channels of nimodipine, one can not exclude a similar decrease in the concentration of nifedipine in the blood plasma.

Since cimetidine suppresses the activity of the isoenzyme CYP3A4, it can increase the concentration of nifedipine in the blood plasma and, thus, enhance its hypotensive effect.

Clinical studies of the interaction of nifedipine and erythromycin were not conducted. Due to the fact that erythromycin suppresses the metabolism of drugs, performed with the participation of the isoenzyme CYP3A4, it can not be ruled out that with the joint use of erythromycin and nifedipine, the latter concentrations in plasma can increase.

Clinical studies of the potential interaction of nifedipine and fluoxetine have not been conducted. It is shown that in vitro fluoxetine inhibits the metabolism of nifedipine, which is carried out with the participation of the CYP3A4 isoenzyme.Therefore, it can not be ruled out that the concentration of nifedipine in the blood plasma is increased with the simultaneous use of these two drugs. When co-prescribing nifedipine and fluoxetine, careful monitoring of blood pressure is necessary; if necessary, the dose of nifedipine should be reduced.

Clinical studies on the potential interaction of nifedipine with indinavir, ritonavir and saquinavir have not been conducted.It is known that preparations of this class suppress the activity of CYP3A4; In addition, in vitro studies it has been shown that indinavir and ritonavir inhibit the metabolism of nifedipine, which occurs with the participation of CYP3A4. With the combined use of nifedipine with these drugs can not exclude an increase in the concentration of nifedipine in blood plasma due to a decrease in the initial metabolism and excretion of nifedipine from the body. When combined treatment requires close monitoring of blood pressure; if necessary, the dose of nifedipine should be reduced.

Studies of the interaction of nifedipine with ketoconazole, itraconazole and fluconazole were not conducted. It is known that preparations of this class suppress the activity of the isoenzyme CYP3A4. With the combined use of nifedipine with these drugs, a significant reduction in the systemic bioavailability of nifedipine is possible because of a decrease in its initial metabolism. When combined treatment requires close monitoring of blood pressure; if necessary, the dose of nifedipine should be reduced.

There was no drug interaction of nifedipine with aymalin, benazepril, doxazosin, omeprazole, orlistat, pantoprazole, ranitidine and triamterene; the pharmacokinetics of nifedipine does not change.

Simultaneous reception of acetylsalicylic acid in a dose of 100 mg does not affect the pharmacokinetics of nifedipine.Simultaneous use of nifedipine does not affect the effects of acetylsalicylic acid on platelet aggregation and clotting time.

The combined use of nifedipine with candesartan, cilexetil does not affect the pharmacokinetics of any of the drugs.

The combined use of nifedipine and irbesartan does not affect the pharmacokinetics of irbesartan.

Grapefruit juice reduces the activity of the isoenzyme CYP3A4, so its use during treatment with nifedipine may lead to increased bioavailability, and consequently, the concentration of the drug in the blood plasma. In this regard, the hypotensive effect of nifedipine may be enhanced.

Overdose

Symptoms : with severe intoxication, there may be impairment of consciousness up to coma, collapse, cardiac rhythm disturbances like tachy- or bradycardia, hyperglycemia, metabolic acidosis, hypoxia, cardiogenic shock with pulmonary edema.

Treatment:

It is recommended to wash the stomach, if necessary - in conjunction with washing the small intestine.

Conduct symptomatic therapy:

With bradycardia - the introduction of beta-sympathomimetics (with a life threatening bradycardia can recommend the establishment of an artificial pacemaker.

In case of arterial hypotension due to cardiogenic shock and vasodilation, the use of calcium preparations is indicated (IV infusion of 10-20 ml of 10% calcium gluconate solution, if necessary repeat the infusion). If a sufficient increase in blood pressure does not occur, an additional introduction of sympathomimetics, dopamine or norepinephrine, is recommended; doses of these drugs are selected individually depending on the clinical effect. Catecholamines should be used only in life-threatening circulatory disorders (due to their low efficacy, a high dose is required, thereby increasing the risk of arrhythmia due to intoxication).

With the development of heart failure - in / in the introduction of strophanthin.

Because of the danger of increasing the burden on the heart, additional fluid administration should be done with caution.

It is recommended to monitor the glucose and electrolytes (K +, Ca 2+) in the blood.

Conduction of hemodialysis is not effective, because nifedipine is not dialyzed; at the same time, plasmapheresis can be effective (high binding to plasma proteins and, as a consequence, low V d).

Storage conditions

At a temperature of no higher than 25 ° C in a dry, dark place.

Shelf life

4 years.

Conditions of leave from pharmacies

Available on prescription