Nifedipine 10 mg tablets number 50

Nifedipine (Nifedipine) Instructions for use

Composition:

active ingredient: nifedipine; 1 tablet contains nifedipine 10 mg or 20 mg;
auxiliary substances: lactose monohydrate, potato starch, microcrystalline cellulose, povidone, sodium lauryl sulfate, magnesium stearate, gipromelose (hydroxypropyl methylcellulose), polysorbate 80, titanium dioxide (E 171), polyethylene glycol 6000, talc, quinoline yellow (E 104).

Dosage form

Tablets coated.

Pharmacotherapeutic group

Selective calcium antagonists with a predominant effect on the vessels. Derivatives of dihydropyridine. Code АТС С08С А05.

Clinical characteristics

Indications

Arterial hypertension; ischemic heart disease: chronic stable angina pectoris, vasospastic angina pectoris (angina pectoris).

Contraindications

• Hypersensitivity to the active substance or to any of the components of the preparation;
• increased sensitivity to other dihydropyridines;
• cardiogenic shock;
• aortic stenosis of severe degree;
• porphyria;
• a condition during myocardial infarction or for a month after it;
• secondary prevention of myocardial infarction;
• combination with rifampicin (due to the inability to reach the effective levels of nifedipine in plasma due to the induction of enzymes);
• unstable angina;
• inflammatory bowel disease or Crohn's disease.

Method of administration and dose

The dose of the drug and the length of the course of treatment is set by the doctor individually, taking into account the severity of the disease and the patient's response to treatment.

Depending on the clinical picture, in each individual case the main dose should be administered gradually. Patients with impaired liver function may require careful monitoring of their condition, and in severe cases, a dose reduction.

For the treatment of coronary heart disease, it is recommended to take 1 tablet (20 mg dose) or 2 (10 mg daily) tablets twice a day (40 mg / day).

If higher doses are required, they should be increased gradually to a maximum dose of 60 mg / day.

For the treatment of hypertension, it is recommended to take Nifedipine 1 (dose 20 mg) or 2 (10 mg daily) twice a day (40 mg / day).

If you are simultaneously using Nifedipine with CYP 3A4 inhibitors or CYP 3A4 inducers, you may need to correct the dose of nifedipine or discontinue nifedipine.

In view of the expressed anti-ischemic and antihypertensive effect of the drug, it should be phased out gradually, especially in the case of high doses.

Pills should be swallowed with a little liquid. The drug is used regardless of food intake.

It is recommended to avoid the use of grapefruit juice while taking the drug.

The recommended interval between tablets is 12 hours (at least 6 hours).

Adverse reactions

Adverse reactions are fed by organ systems.

From the cardiovascular system: increased heartbeat; tachycardia; At the beginning of therapy in patients with angina pectoris may increase the frequency, duration of seizures, or increase in the severity of symptoms; cases of asymptomatic myocardial ischemia, exacerbation of existing myocardial ischemia, cardiac conduction impairment, pain in the humbug (angina pectoris).

From the side of the blood and lymphatic system: changes in the blood's formula, thrombocytopenia, anemia, leukopenia, aplastic anemia; agranulocytosis.

From the nervous system: headache, dizziness, increased fatigue, weakness; paresthesia, increased excitability, sleep disturbance (insomnia, drowsiness, restless sleep), disturbance of balance, depression; tremor, disturbance in coordination of movements, feeling of danger, dysesthesia, migraine, loss of consciousness.

From the organs of vision: temporary blindness with a maximum concentration of nifedipine in the serum, temporary retinal ischemia, excessive tearing (lichen); reduction of visual acuity, pain in the eyes.

On the part of the hearing and inner ear: ringing in the ears.

From the respiratory tract, the chest and mediastinum: dyspnea; nasal hemorrhage; upper respiratory tract infections, cough and nasal congestion; angioedema edema

From the gastrointestinal tract: constipation; diarrhea, nausea, abdominal pain, dry mouth, flatulence; vomiting, hypertrophy of the gums, lacerations; black stool, heartburn, taste disturbance, dysphagia, intestinal obstruction, ulcer of the intestine, gastroesophageal sphincter deficiency.

From the kidneys and urinary tract: polyuria, nicoturia; hematuria, dysuria.

From the skin and subcutaneous tissues: rash, itching, redness, erythema of the cheeks (face redness); urticaria, excessive sweating, chills, purpura; In case of prolonged use of nifedipine, gum hyperplasia is possible, which completely passes after the withdrawal of the drug; toxicodermal necrolysis, Stevens-Johnson syndrome, exfoliative dermatitis, polymorphic erythema, photosensitization, alopecia.

From the immune system: allergic reactions, angioneurotic edema; itching, urticaria, rash; anaphylactic / anaphylactoid reactions.

On the part of the musculoskeletal system and the connective tissue: back pain, myalgia, edema of the joints; gout, arthralgia, arthritis with the presence of positive antinuclear antibodies; muscle cramps.

From the side of metabolism and digestion: hyperglycemia (especially in patients with diabetes mellitus), increase in body weight, neoprene.

From the vascular system: swelling of the feet, ankles or shins, vasodilation; arterial hypotension, symptomatic hypotension, orthostatic hypotension.

From the liver and bile ducts: cholestasis; toxic allergic hepatitis, jaundice, transient increase in the activity of liver enzymes.

From the reproductive system and the mammary glands: gynecomastia, the process is reversible, the symptoms disappear after the termination of nifedipine administration; erectile dysfunction.

General disorders: feeling unwell, fever, nonspecific pain.

Mental disorders: depression, paranoid syndrome, anxiety, decreased libido.

Overdose

Symptoms: headache, facial hyperemia, prolonged system hypotension, lack of pulse in the peripheral arteries. In severe cases, there is a tachycardia or bradycardia, a violation of the function of the sinus node, retardation of atrioventricular conduction, hyperglycemia, metabolic acidosis and hypoxia, collapse with loss of consciousness and cardiogenic shock, which is accompanied by pulmonary edema, disturbance of consciousness up to the coma.

Treatment First aid measures should be aimed at eliminating the drug from the body and restoring stable hemodynamics. Patients should continuously monitor the functions of the cardiovascular and respiratory systems, levels of sugar and electrolytes (potassium, calcium) in plasma, diuretic diuresis and volume of circulating blood. Possible administration of calcium supplements. If calcium is not effective enough, it will be advisable to use such sympathomimetics as dopamine or norepinephrine to stabilize arterial pressure. Doses of these drugs are selected taking into account the achieved therapeutic effect. Bradycardia can be eliminated by the use of beta-sympathomimetics. When the cardiac rhythm is slowed down, which threatens life, it is recommended to use an artificial rhythm driver. In addition, the fluid should be treated with extreme caution, as it increases the risk of overloading the heart.

Since nifedipine is characterized by a high degree of binding to blood plasma proteins and a relatively small volume of distribution, hemodialysis is not effective, however, plasmapheresis is recommended.

Use during pregnancy and breastfeeding

Nifedipine is contraindicated for use during pregnancy up to the 20th week.

The use of nifedipine during pregnancy after the 20th week requires a thorough individual risk benefit analysis and should be considered only if all other treatment options are not possible or ineffective.

Careful monitoring of blood pressure should be performed when administering nifedipine with magnesium sulfate intravenously, as there is a potential for a sharp decrease in blood pressure that can be a threat to the woman and the fetus.

Nifedipine penetrates into breast milk. Since there are no data on the effects of nifedipine on infants, breastfeeding should be discontinued before using nifedipine.

Where are you

The drug does not apply to children (under 18 years of age).

Special safety measures

With caution, prescribe the drug at very low blood pressure (severe arterial hypotension with systolic blood pressure lower
90 mm Hg Art.), as well as with pronounced weakness of cardiac activity (decompensated cardiac insufficiency).

When severe arterial hypotension (systolic pressure below 90 mm Hg), severe cerebrovascular accidents, severe heart failure, severe aortic stenosis, diabetes mellitus, liver and kidney impairment, Nifedipine can be used only under continuous clinical observation, avoiding the appointment of high doses of the drug.

Patients in the elderly (over 60 years old) the drug is dosed with great care.

Application features

Caution should be exercised when prescribing Nifedipine to patients undergoing hemodialysis, as well as patients with malignant hypotension or hypovolaemia (decreasing circulating blood volume), as the enlargement of the blood vessels can cause a significant reduction in blood pressure.

In the treatment of coronary angiospazma in the postinfarction period, treatment with Nifedipine should be started approximately 3-4 weeks after myocardial infarction and only if the coronary circulation is stabilized.

Grapefruit juice depresses the metabolism of nifedipine, which leads to an increase in the concentration of the latter in the blood plasma and an increase in the antihypertensive effect of the drug. The use of nifedipine may result in false-positive results in spectrophotometrically determining the concentration of vanillin-mandelic acid in urine (however, this effect is not observed when using the method of high-performance liquid chromatography).

Care should be taken when administering the drug to patients with severe narrowing of the gastrointestinal tract due to the possible occurrence of obstructive symptoms. Very rarely, nobody may appear, which may require surgical intervention.

In isolated cases obstructive symptoms were described in the absence of anamnesis of the gastrointestinal tract disorders.

Do not apply to patients with an iris-intestinal reservoir (ileostomy after proctocollectomy).

The use of the drug may result in false positive results in an X-ray study using a barium contrast agent (eg, filling defects are interpreted as polyps).

Patients with impaired liver function require careful monitoring, and in severe cases, in lowering the dose.

Nifedipine is metabolized via the cytochrome P450 3A4 system, so drugs that inhibit or induce this enzyme system can change the "first passage" or the clearance of nifedipine.

For drugs that are weak or moderate inhibitors of the cytochrome P450 3A4 system and may lead to an increase in the plasma concentration of nifedipine, for example:

• macrolide antibiotics (eg erythromycin);
• anti-HIV protease inhibitors (for example, ritonavir);
• Azole antimycotics (eg ketoconazole);
• antidepressants nefazodone and fluoxetine;
• quinupristine / dalfopristine;
• valproic acid;
• cimetidine

When simultaneous use of nifedipine with these drugs should be monitored for arterial pressure and, if necessary, consider reducing the dose of nifedipine.

Separate in vitro experiments have found the relationship between the use of calcium antagonists, in particular nifedipine, and reversible biochemical changes in sperm, which aggravate the ability of the latter to fertilize. In the event that in vitro fertilization attempts are unsuccessful, in the absence of other explanations, calcium antagonists such as nifedipine may be considered as a possible cause of this phenomenon.

The drug should not be used if there is a likelihood of association between the previous use of nifedipine and ischemic pain. In patients with angina pectoris, seizures may occur more often, and their duration and intensity may increase, especially at the onset of treatment.

Nifedipine-based drugs do not apply to patients with acute angina pectoris.

The use of nifedipine in patients with diabetes may require corrective treatment.

Ability to influence the reaction speed when driving or operating with other mechanisms

When using the drug, it is not recommended to drive vehicles and work with other potentially dangerous mechanisms.

Interaction with other drugs and other types of interactions

When simultaneous use of antihypertensive agents, beta-blockers, diuretics, nitroglycerin and isosorbide prolonged action must take into account the possibility of synergistic action of nifedipine.

Digoxin

Nifedipine may increase the concentration of digoxin in the blood plasma. The concentration of digoxin in the blood plasma should be monitored and the dose adjusted at the start of treatment with nifedipine when increasing the dose and discontinuing treatment with nifedipine.

Magnesium sulfate

Nifedipine may exacerbate the toxic effects of magnesium sulfate, which results in a neuromuscular blockade.Simultaneous administration of nifedipine and magnesium sulfate is dangerous and may endanger the patient's life, therefore the use of these drugs together is not recommended.

Cimetidine

Simultaneous administration of nifedipine and cimetidine may increase the concentration of nifedipine in plasma and increase the hypotensive effect of nifedipine. Cimetidine suppresses the activity of the cytochrome isoenzyme CYP3A4.For patients who already take cimetidine, nifedipine should be used with caution and gradually increasing the dose.

Hinupristine, dalfoprish can increase the plasma level of nifedipine.

Phenytoin, carbamazepine

The use of nifedipine may increase the concentration of carbamazepine and phenytoin in plasma. Patients who are already taking nifedipine and phenytoin or carbamazepine at the same time should be under constant supervision by the doctor. In the event of signs of toxicity or an increase in the concentration of carbamazepine and phenytoin in the plasma, the dose of these drugs should be reduced.

Quinidine

Nifedipine may cause a decrease in the quinidine concentration in the serum, while quinidine may increase the patient's sensitivity to nifedipine. If a patient who is already taking quinidine has begun treatment with nifedipine, attention should be paid to the side effects of nifedipine. It is necessary to monitor the level of quinidine in the serum before the start of treatment and in case of discontinuation of treatment with nifedipine; You should also adjust the dose of quinidine.

Theophylline

When concurrently using nifedipine and theophylline, the concentration of the latter in the blood plasma may increase, decrease or remain unchanged. It is recommended to control the concentration of theophylline in the blood plasma and, if necessary, adjust its dose.

Rifampicin

The simultaneous use of rifampicin and nifedipine may be accompanied by a decrease in the concentration of nifedipine in the blood plasma and, as a consequence, a decrease in its therapeutic effect. In the event of attacks of angina or elevated blood pressure, with nifedipine and rifampicin simultaneously, the dose of nifedipine should be increased.

Diltiazem weakens the dissolution of nifedipine, which may lead to a lowering of the dose.

Vincristine

At concurrent vincristine administration, the withdrawal of vincristine is observed.

Cephalosporin

With the simultaneous administration of nifedipine and cephalosporin, cefalosporin levels increase in plasma.

Itraconazole, erythromycin, clarithromycin

Simultaneous administration of nifedipine and itraconazole (as well as with other azole antifungal agents, erythromycin and clarithromycin, which slow down the action of cytochrome isoenzyme CYP3A4) may increase the concentration of nifedipine in plasma and increase its effect. When side effects of nifedipine appear, it is necessary to reduce its dose (if possible) or to stop the use of antifungal agents.

Ciclosporin, ritonavir or saquinavir

Concentration of nifedipine in blood whey and ego action mogut also usylyvatsya simultaneously with Application nifedipine, cyclosporine, or rytonavyra sakvynavyra (Preparations zamedlyayut These actions isoenzyme cytochrome CYP3A4). In appearance pobochnыh эffektov neobhodimo umenshyt ego nifedipine dose.

tacrolimus

In patsyentov with liver transplant, simultaneously poluchavshyh tacrolimus and nifedipine, tacrolimus concentrations was observed Increase in blood whey (tacrolimus is metabolized posredstvom cytochrome CYP3A4). Clinical significance and implications эtoho not yssledovalys interaction.

fentanyl

In patsyentov, kotoryya prymenyayut nifedipine, fentanyl Can vыzvat arteryalnuyu hypotension. At least 36 hours before conducting operations with primeneniem Targets fentanylovoho anesthesia neobhodimo prekratyt Application nifedipine.

Antykoahulyantы sort of coumarin

In patsyentov, prynymayuschyh antykoahulyantы sort of coumarin, was observed Increase of administering a prothrombin of time after nifedipine. Эtoho importance of interaction is not completely bыla research.

methacholine

Nifedipine Can Change otvetnuyu bronchial reaction to methacholine. Treatment of nifedipine sleduet prekratyt to conducting nonspecific bronhoprovokatsyonnoho test with methacholine (by Opportunity).

Application Experience kaltsyevoho nimodipin svydetelstvuet antagonist, nifedipine is not something to ysklyuchenы sleduyuschye interaction, carbamazepine, phenobarbital - Reduction plasma level of nifedipine; Simultaneously with standard receiving macrolides (erythromycin in particular), fluoxetine, nefazodone, valproevoy acid - grows plasma level of nifedipine.

Yhybytorы anti-HIV proteazy

Clinical Studies Study Between BUILDING interaction of nifedipine and nekotorыmy inhibitor of HIV-proteazy (for example rytonavyrom) were conducted. Preparations эtoho class, How known ynhybyruyut cytochrome P450 3A4 system. In addition, Data Preparations ynhybyruyut oposredovannыy in vitro cytochrome P450 3A4 metabolism of nifedipine. In the Application simultaneously with nifedipine impossible ysklyuchyt Increase significantly the ego plasma concentrations due to the metabolism pervogo prohozhdenyya Reduction Reduction and withdrawal IZ body.

Azolnыe antimycotics

Study interaction Between nifedipine and antifungal agents nekotorыmy azolnoy group (for example ketoconazole) else not conducted. Preparations эtoho class ynhybyruyut cytochrome P450 3A4 system. Application simultaneously with oral nifedipine s impossible ysklyuchyt Increase significantly the ego systemnoy bioavailability due to the Reduction pervogo prohozhdenyya metabolism.

antihypertensive Preparations

Application simultaneous nifedipine and others antyhypertenzyvnыh drugs, pryvedennыh below, can cause for the effect of antihypertensive Increase:

• diuretics;
• β-blockers (Perhaps also in the emergence of heart Pristoupa otdelnыh cases);
• ynhybytorы ACE;
• angiotensin receptor antagonists;
• Other calcium antagonists;
• α-blockers;
• ynhybytorы FDЭ-5;
• α-metildofa.

Hreypfrutovыy juice

Can uvelychyvat Hreypfrutovыy juice concentrations of nifedipine in blood whey and usylyvat ego hypotensive effect and frequency vazodylatatornыh pobochnыh effects.

Other types of interaction

Application nifedipine Can cause lozhnopovыshennыh for obtaining results with spectrophotometric Determination of Concentration vanylyl-myndalnoy acid in the urine (but Application chromatography method vыsokoэffektyvnoy zhydkostnoy this effect is not observed).

Pharmacological properties

Pharmacodynamics. Selektyvnыy blocker kaltsyevыh channels, proyzvodnoe dyhydropyrydyna. Slowing postuplenye kardyomyotsytы calcium in cells and smooth muskulaturы vessels. Okazыvaet antyanhynalnыy and antihypertensive эffektы. Snyzhaet smooth tone muskulaturы vessels. Rasshyryaet koronarnыe and peryferycheskye artery, vascular peryferycheskoe snyzhaet Global Resistance, arteryalnoe pressure of a neznachytelno - myocardial contractility, reduces afterload and myocardial the needs in oxygen. Koronarnыy improves blood flow. Not uhnetaet myocardial conduction. In dlytelnom Application nifedipine Can preduprezhdat Education novyh blyashek in atherosclerotic vessels koronarnыh. In the early of treatment nifedipine mogut otmechatsya prehodyaschaya reflektornaya tachycardia and cardiac Increase vыbrosa not kompensyruyuschye vasodilation, vыzvannuyu drug.Usylyvaet withdrawal of nifedipine IZ organism sodium and water. In Raynaud's syndrome or drug Can preduprezhdat umenshat vessels spasm of limbs.

Pharmacokinetics. In standard receiving nifedipine inside quickly and Almost completely (more than 90%) absorbyruetsya IZ gastrointestinal tract. Bioavailability - about 50%. Maximum Concentration in plasma dostyhaetsya in 1-3 hours after reception. Period poluvыvedenyya -
2-5 hours. Vыvodytsya mainly with urine in a video neaktyvnыh metabolites. The effect Clinical offensive Time: 20 minutes - the oral standard receiving, 5 minutes - with sublingual. The effect Clinical Duration - 4-6 hours.

Pharmaceutical characteristics

Basic Physical and Chemical Properties: kruhloy tablet forms, pokrыtыe obolochkoy, yellow Color, Upper and Lower kotorыh vыpuklыe surface. At a break, when viewed under a magnifying glass, a kernel, surrounded by one solid layer, is visible.

Shelf life

3 years.

Storage conditions

Store in original packaging at a temperature not exceeding 25 oC. Keep out of the reach of children.

Packaging

10 tablets in a blister; 5 blister packs in cardboard.

Vacation category

By recipe