Universal reference book for medicines
Product name: OSMO-ADALAT ® (OSMO-ADALAT ® )

Active substance: nifedipine

Type: Calcium channel blocker

Manufacturer: BAYER PHARMA (Germany)
Composition, form of production and packaging
Controlled-release tablets coated with a
pink film cover , round, biconvex, marked "Adalat 30" on one side in black;
on the surface of tablets on either side with an arbitrary arrangement with respect to the center, there is a pore in the form of an irregularly shaped well with a diameter of up to 1 mm.
1 tab.

nifedipine 33 mg

Excipients: hypromellose - 8.2 mg, magnesium stearate - 0.4 mg, macrogol - 122.2 mg;
osmotic layer - hypromellose - 4.1 mg, magnesium stearate - 0.2 mg, sodium chloride - 23.9 mg, macrogol - 52.9 mg, iron oxide red oxide - 0.8 mg.
Sheath composition: film sheath - cellulose acetate - 32.3 mg, macrogol - 1.7 mg;
light barrier - giprolose - 7.1 mg, titanium dioxide - 5 mg, hypromellose - 2.3 mg, polyethylene glycol - 1.3 mg, iron dye oxide red 0.3 mg; polishing layer, inscription - hypromellose - 1.5 mg, black ink Opacode S-1-17823 (trace amounts).
14 pcs.
- blisters (2) - packs of cardboard.
Controlled-release tablets coated with a pink color, round, biconcave, labeled in black "Adalat 60" on the one hand;
on the surface of tablets on either side with an arbitrary arrangement with respect to the center, there is a pore in the form of an irregularly shaped well with a diameter of up to 1 mm.
1 tab.

nifedipine 66 mg

Excipients: hypromellose - 16.4 mg, magnesium stearate - 0.8 mg, macrogol - 244.4 mg;
osmotic layer - hypromellose - 8.2 mg, magnesium stearate - 0.4 mg, sodium chloride - 47.8 mg, macrogol - 105.8 mg, iron oxide red oxide - 1.6 mg.
Sheath composition: film sheath - cellulose acetate - 38 mg, macrogol - 2 mg;
light barrier - giprolose - 12.8 mg, titanium dioxide - 9.1 mg, hypromellose - 4.1 mg, polyethylene glycol - 2.4 mg, iron dye red oxide - 0.6 mg; polishing layer, inscription - hypromellose - 2.5 mg, black ink Opacode S-1-17823 (trace amounts).
14 pcs.
- blisters (2) - packs of cardboard.
INSTRUCTION FOR THE SPECIALIST.

Description of the drug approved by the manufacturer for the printed edition of 2011.

PHARMACHOLOGIC EFFECT

Selective blocker of slow calcium channels, derivative of 1,4-dihydropyridine.
Has antianginal and hypotensive effect.
Reduces the flow of calcium ions through slow calcium channels into cells, predominantly cardiomyocytes, smooth muscle cells of the coronary and peripheral arteries, while lowering the OPSS and dilating the coronary arteries, large vessels and intact segments of the walls of partially stenosed vessels.
Nifedipine reduces the tone of the smooth muscles of the coronary arteries, thereby preventing angiospasm, increases blood flow in the poststenotic parts of the vessels and increases the delivery of oxygen to the myocardium. Reduces the need for myocardium in oxygen by reducing the OPSS (afterload), and with prolonged admission, it can prevent the development of new atherosclerotic lesions in the coronary arteries. Nifedipine reduces the tone of the smooth muscles of the arterioles, thereby reducing the increased OPSS and, therefore, blood pressure.
At the beginning of nifedipine treatment, a temporary reflex increase in heart rate and, as a consequence, cardiac output may occur.
However, this increase is not so significant as to compensate for the dilatation of blood vessels. In addition, nifedipine in both short-term and long-term use increases the excretion of sodium and water ions from the body. The hypotensive effect of nifedipine is especially pronounced in patients with arterial hypertension. In patients with hypertension and the presence of at least one other risk factor, the incidence of cardiovascular and cerebrovascular episodes is reduced to the same extent as a combination of diuretics.
PHARMACOKINETICS

Suction and distribution

After oral administration, nifedipine is almost completely absorbed from the digestive tract.
Bioavailability of nifedipine from tablets is 45-56% due to the effect of "first passage" through the liver. The bioavailability of nifedipine from tablets with controlled release relative to tablets is 68-86%. The intake of food slightly reduces the initial absorption rate, but does not affect the bioavailability. Nifedipine is released from the controlled-release tablets through a special osmotic-gradient membrane with a rate constant of zero order, with a controlled increase in plasma nifedipine concentration, which reaches a plateau approximately 6-12 hours after ingestion. For 24 hours, a constant concentration of the drug in the blood plasma is maintained. The release rate of nifedipine is independent of the pH of the environment and the motility of the gastrointestinal tract. When taking Osmo-Adalat in a dose of 30 mg and 60 mg of C max in blood plasma is respectively 20-21 ng / ml and 43-55 ng / ml and reached after 12-15 h and 7-9 h respectively. Binding to blood plasma proteins (albumin) is about 95%. It rises through the BBB and placental barrier, excreted in breast milk.
Metabolism

After ingestion, nifedipine is metabolized in the intestinal wall and in the liver with the formation of inactive metabolites.

Excretion

T 1/2 nifedipine is 1.7-3.4 hours when taken with tablets. The concentration of nifedipine in the administration of controlled release tablets in blood plasma is maintained as a plateau throughout the entire release and absorption period, and only after the last dose of nifedipine is released from the controlled-release tablet the concentration in the plasma begins to decrease, and T 1/2 corresponds to that of nifedipine in the form of tablets.
Nifedipine is excreted from the body in the form of inactive metabolites through the kidneys, only 5-15% - with bile through the intestine. Unchanged, nifedipine is present in the urine in small amounts (less than 0.1%).
During passage through the digestive tract, the biologically inactive components of the tablet remain unchanged and are excreted from the body in the form of an insoluble coat.

Pharmacokinetics in special clinical cases

When the renal function is impaired, the pharmacokinetics do not change.

If the liver function is impaired, the clearance of nifedipine is reduced.

Hemodialysis and peritoneal dialysis do not affect the pharmacokinetics of nifedipine, plasmapheresis enhances its excretion.

INDICATIONS

- IHD: stable angina (stress angina);

- arterial hypertension.

DOSING MODE

The drug is taken orally.

The initial dose is 30 mg 1 time / day.
In the future, if necessary, the dose can be gradually increased to 60 mg 1 time / day and even up to 120 mg 1 time / day, depending on the severity of the disease and the individual reaction of the patient. The duration of treatment is determined by the doctor.
The tablet should be swallowed whole, without chewing and not breaking, squeezed with a small amount of liquid, take irrespective of food intake, protect from moisture and remove it from the foil immediately before the reception.

With severe violations of liver function , the dosage regimen is corrected.

SIDE EFFECT

From the cardiovascular system :? 1- <10% - palpitation, sensation of blood flushes to the face (vasodilation), peripheral edema;
0.1- <1% - arterial hypotension (including orthostatic), syncope, tachycardia; ? 0.01- <0.1% - angina pectoris.
From the digestive system :? 1- <10% - constipation;
0.1- <1% - abdominal pain, diarrhea, dry mouth, indigestion, flatulence, nausea; 0.01 - <0.1% - anorexia, belching, gingivitis, gingival hyperplasia, increased activity of hepatic transaminases (ALT, AST, GGT), vomiting; <0.01% - bezoar (lumps from undigested remnants of food in the stomach), dysphagia, esophagitis, intestinal obstruction, intestinal ulcers, jaundice.
From the central nervous system and peripheral nervous system :? 1- <10% - dizziness, headache;
0.1- <1% - nervousness, paresthesia, insomnia, drowsiness; 0.01 - <0.1% - hypoesthesia, tremor.
On the part of the endocrine system: <0.01% - hyperglycemia, weight loss, gynecomastia.

On the part of the respiratory system :? 0.1- <1% - dyspnea;
0.01 - <0.1% - nasal bleeding.
From the urinary system :? 0.1- <1% - nocturia, polyuria;
0.01 - <0.1% - dysuria, frequent urination, impaired renal function (in patients with renal insufficiency).
From the musculoskeletal system :? 0.1- <1% - cramps in the calf muscles;
0.01 - <0.1% - arthralgia, myalgia.
Dermatological reactions :? 0.1- <1% - skin itching, rash (exanthema, erythema, urticaria);
? 0.01- <0.1% - angioedema, maculopapular, pustular, vesicle-bullous rash, urticaria; <0.01% - photodermatitis, exfoliative dermatitis, purpura.
Allergic reactions :? 0.01- <0.1% - edema of the tongue, decreased blood pressure, tachycardia, fever;
<0.01% - anaphylactic reactions.
On the part of the hematopoiesis system: <0.01% - leukopenia.

From the sense organs :? 0.01- <0.1% - diplopia, amblyopia, pain in the eyeballs;
<0.01% - blurred vision.
From the autonomic nervous system :? 0.01- <0.1% - increased sweating.

Other :? 1- <10% - asthenia, swelling of the face (including around the eyes);
? 0.1- <1% - pain in the chest, pain in the lower extremities, malaise, pain of uncertain localization; 0.01 - <0.1% - chills, chest pain.
When taking nifedipine, there are also side effects such as asymptomatic agranulocytosis, thrombocytopenia, development or exacerbation of heart failure, rarely - pulmonary edema (difficulty breathing, coughing or stridor breathing), transient loss of vision, swelling of the joints.

CONTRAINDICATIONS

- cardiogenic shock;

- severe arterial hypotension (systolic pressure <90 mmHg);

- Ileostomy, established after proctocolectomy;

- simultaneous application of rifampicin;

- Pregnancy;

- lactation (breastfeeding);

- children and adolescents under 18 years of age (efficacy and safety not established);

- Hypersensitivity to nifedipine.

Caution should be given to the drug with heart failure, severe aortic stenosis, subaortal stenosis, acute myocardial infarction with left ventricular failure, severe bradycardia, liver failure, stenosis of any part of the gastrointestinal tract, severe disorders of cerebral circulation, mild or moderate arterial hypotension, elderly patients, patients with malignant arterial hypertension and hypovolemia, who are on hemodialysis.

PREGNANCY AND LACTATION

Osmo-Adalat ® is contraindicated in pregnancy;
possibly embryotoxic, fetotoxic and teratogenic effects of the drug.
Nifedipine excreted in breast milk, so if you need to use Osmo-Adalat ® during lactation, breastfeeding should be discontinued.

APPLICATION FOR VIOLATIONS OF THE FUNCTION OF KIDNEYS

When violations of liver function of a serious degree , the dosage regimen is corrected.

When liver failure is recommended to monitor patients, if necessary - reduce the dose or use of the drug in other dosage forms.

APPLICATION FOR CHILDREN

The effectiveness and safety of the use of the drug to 18 years are not established.

APPLICATION IN ELDERLY PATIENTS

Caution should be given to elderly patients.

SPECIAL INSTRUCTIONS

With extreme caution, nifedipine should be administered to patients with severe stenosis of any part of the digestive tract, since intestinal obstruction may develop.
In some cases, the symptoms of intestinal obstruction can be observed in patients without pathology on the part of the gastrointestinal tract.
It should be borne in mind that when carrying out an X-ray of the intestine with barium, false-positive symptoms of the polyp (filling defect) can be detected.

In patients with hepatic impairment, follow-up is recommended;
If necessary, reduce the dose of the drug or apply nifedipine in other dosage forms.
With the simultaneous use of Osmo-Adalat ® and β-adrenoceptor blockers, the patient needs careful observation, since it is possible to develop a marked decrease in blood pressure and worsen the symptoms of heart failure.

With simultaneous administration with grapefruit juice, it is possible to intensify the hypotensive effect, which persists for 3 days after the last reception of the juice.

Nifedipine causes a false positive increase in the concentration of vanillylmandelic acid in the urine as determined by the spectrophotometric method and does not affect the result of this reaction when using the high performance liquid chromatography (HPLC) method.

Impact on the ability to drive vehicles and manage mechanisms

During the period of treatment, care must be taken when engaging in potentially dangerous activities that require a high concentration of attention and speed of psychomotor reactions, and refrain from using ethanol.

OVERDOSE

Symptoms: loss of consciousness right up to coma, pronounced decrease in blood pressure.
tachycardia / bradycardia, hyperglycemia, metabolic acidosis, hypoxia, cardiogenic shock accompanied by pulmonary edema.
Treatment: emergency interventions for overdose should first of all be aimed at removing nifedipine from the body and restoring stable hemodynamics.
It is recommended to wash the stomach and, if necessary, irrigation of the small intestine to prevent further absorption of the drug. Carrying out of a hemodialysis is inexpedient, as nifedipine is not deduced or removed at a dialysis; recommended the appointment of plasmapheresis (because for nifedipine is characterized by a high degree of binding to plasma proteins and a relatively small V d ).
With bradycardia prescribe? -adrenomimetics, with life-threatening bradycardia - the implantation of a temporary artificial pacemaker.

With a marked decrease in blood pressure, a slow intravenous administration of 10-20 ml of 10% calcium gluconate solution is recommended (repeated administration is permissible), with ineffectiveness - the appointment of vasoconstrictive sympathomimetics of dopamine or norepinephrine (doses are selected depending on the therapeutic effect obtained).

The introduction of fluid should be limited in connection with the risk of cardiac overload.

DRUG INTERACTION

The hypotensive effect of nifedipine may increase with simultaneous use with drugs that lower blood pressure, as well as with inhalation anesthetics, prazosin and other alpha-blockers.

The hypotensive effect of nifedipine reduces sympathomimetics, NSAIDs due to suppression of prostaglandin synthesis in the kidneys and sodium and liquid retention in the body, estrogens (due to fluid retention in the body) and calcium preparations.

Nifedipine is metabolized by the CYP3A4 isoenzyme, so drugs that inhibit or induce these enzymes can interact with nifedipine when ingested, disrupting the clearance or the effect of a "first pass" through the liver.

Nifedipine decreases the clearance of digoxin, which leads to an increase in its concentration in the blood plasma, so patients need careful monitoring to detect symptoms of an overdose of cardiac glycoside, and its dose should be reduced if necessary.

Nifedipine reduces the concentration of quinidine in blood plasma, however, when it is withdrawn, the content of quinidine can significantly increase, which requires an adjustment of its dose.
In some cases, the concentration of nifedipine in the blood plasma may increase, so if there is evidence, you should reduce its dose. In the period of combined therapy, it is necessary to monitor the concentration of quinidine in the blood plasma and the level of blood pressure. When taken concomitantly with nifedipine, it increases the risk of prolonging the QT interval.
When combined with procainamide, there is a risk of prolonging the QT interval and enhancing the negative inotropic effect of both drugs.

Nifedipine induces the isoenzyme CYP3A4 and reduces the bioavailability of nifedipine and, as a consequence, reduces its effectiveness, which may require an increase in its dose.

Nifedipine inhibits the isoenzyme CYP3A4 and causes an increase in the concentration of nifedipine in the blood plasma, thereby increasing its antihypertensive effect.

Nifedipine is a powerful inducer of liver enzymes, speeding up the metabolism of nifedipine, which leads to a weakening of its effectiveness.

Diltiazem slows the withdrawal of nifedipine from the body, so combination therapy should be carried out very carefully, if necessary, reducing the dose of nifedipine.

Cisapride increases the concentration of nifedipine in the blood plasma, so you should monitor blood pressure and, if necessary, reduce the dose of nifedipine.

Grapefruit juice inhibits the isoenzyme CYP3A4 and increases the concentration of nifedipine in plasma, due to a decrease in the effect of "first passage" through the liver.

Since valproic acid causes a rise in plasma concentrations of nimodipine, in a structure close to nifedpine blocker of slow calcium channels, it is not ruled out that the plasma concentration of nifedipine increases and its effectiveness is increased.

Nifedipine does not change the antiaggregant effect of acetylsalicylic acid in a dose of 100 mg (platelet aggregation and bleeding time).
Acetylsalicylic acid, in turn, does not affect the pharmacokinetic parameters of nifedipine.
Since carbamazepine and fenaparbital cause a decrease in plasma concentrations of nimodipine, a structure similar to nifedipine blocker of slow calcium channels, it is possible to reduce plasma concentrations of nifedipine and reduce its effectiveness.

Nifedipine can displace drugs with a high degree of binding (indirect anticoagulants - coumarin and indanedione derivatives, quinine, sulfinpyrazone, anticonvulsant drugs, salicylates, NSAIDs), with the subsequent possible increase in their concentration in plasma.

Since erythromycin, fluoxetine, ritonavir, indinavir, amprenavir, nelfinavir, saquinavir, ketoconazole, itraconazole, fluconazole inhibit the isoenzyme CYP3A4, it is not excluded that the concentration of nifedipine in the blood plasma is increased as a result of their interaction.
It is recommended to monitor blood pressure and, if necessary, reduce the dose of nifedipine.
In the case of simultaneous application with disopyramide, an increase in the negative inotropic effect is possible.
Preparations containing lithium, when combined with nifedipine, can cause neurotoxic symptoms (nausea, vomiting, diarrhea, ataxia, tremor and / or tinnitus).
Aymalin, omeprazole, benazepril, irbesartan, orlistat, ranitidine, rosiglitazone, doxazosin, pantoprazole, talinolol, triamterene hydrochlorothiazide did not affect the pharmacokinetics of nifedipine.
TERMS OF RELEASE FROM PHARMACY

The drug is released by prescription.

TERMS AND CONDITIONS OF STORAGE

List B. The drug should be kept out of the reach of children, dry place at a temperature not higher than 25 ° C. Shelf life - 4 years.
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