Nifedipine-Akrihin - instructions for use, dose, side effects, contraindications

Pharmacodynamics:Selective blocker of "slow" calcium channels, 1,4-dihydropyridine derivative. Has vasodilating, antianginal and hypotensive action. Reduces the current of calcium ions in cardiomyocytes and smooth muscle cells of the coronary and peripheral arteries; in high doses, suppresses the release of calcium ions from the intracellular depot.Reduces the number of functioning channels, without affecting the time of their activation, inactivation and recovery. Separates the processes of excitation and contraction in the myocardium mediated by tropomyosin and troponin, and in smooth muscles of vessels, mediated by calmodulin. In therapeutic doses normalizes the transmembrane current of calcium ions, disrupted in a number of pathological conditions, especially in hypertension. Does not affect the tone of the veins. Strengthens the coronary blood flow, improves the blood supply of the ischemic zones of the myocardium without the development of the phenomenon of "stealing", activates the functioning of collaterals. Expanding the peripheral arteries, reduces the overall peripheral vascular resistance, myocardial tone, postload, myocardial oxygen demand and prolongs the diastolic relaxation of the left ventricle (LV). Virtually does not affect the sinouauricular and atrioventricular nodes and does not have antiarrhythmic activity. It enhances kidney blood flow, causes a moderate natriuresis. Negative chrono-, dromo- and inotropic action is blocked by reflex activation of the sympathoadrenal system and an increase in the heart rate in response to peripheral vasodilation. The effect occurs after 20 minutes - when taking the drug inside, the duration of the effect is 4-6 hours.

Pharmacokinetics:

Nifedipine is almost completely absorbed in the gastrointestinal tract (more than 90%). Absolute bioavailability is 40 - 70%. Nifedipine is subjected to intensive metabolism at the "first passage" through the liver (40-60%).

After ingestion of 1 tablet 10 mg the maximum concentration of the drug in the blood plasma is reached after 30 - 60 minutes. Half-life is 2 to 4 hours. The association of nifedipine with plasma proteins (albumins) is 94 - 97%.

The active substance penetrates the placental barrier and is excreted into breast milk. Less than 5% of the administered dose penetrates the blood-brain barrier. Nifedipine in the main it is metabolized to 3 pharmacologically inactive metabolites, and in this form approximately 60-80% of the administered dose is excreted in the urine. The rest of the dose is excreted through the bile ducts and with feces.

Indications:

- Ischemic heart disease - for the prevention of seizures with various forms of angina, including vasospastic angina (Prinzmetal angina).

- arterial hypertension (monotherapy or in combination with other antihypertensive drugs).

Contraindications:

- Hypersensitivity to nifedipine (and other dihydropyridine derivatives) or other components of the drug.

- cardiogenic shock, collapse, severe aortic stenosis, unstable angina

- after a previous myocardial infarction (the first 4 weeks)

- lactose intolerance

- age to 18 years (effectiveness and safety not established)

- arterial hypotension (systolic blood pressure less than 90 mm Hg), chronic heart failure in the stage of decompensation, syndrome of weakness of the sinus node, pregnancy (up to 20 weeks), lactation.

Carefully:Severe stenosis of the aortic or mitral valve mouth, hypertrophic obstructive cardiomyopathy, severe bradycardia or tachycardia, sinus node weakness syndrome, malignant hypertension, myocardial infarction with left ventricular failure, unstable angina, simultaneous administration of beta-blockers or cardiac glycosides, simultaneous administration of rifampicin, severe disorders cerebral circulation,impaired liver and / or kidney function, hemodialysis (risk of arterial hypotension), and advanced age.

Pregnancy and lactation:The administration of nifedipine to pregnant women is only indicated if the intended benefit to the mother exceeds the potential risk to the fetus. Nifedipine it is not recommended to appoint in the 1st trimester of pregnancy (up to 20 weeks). The drug is excreted in breast milk, so it is recommended to stop breastfeeding while taking the drug.

Dosing and Administration:

Pills Nifedipine-Akrihin are intended for oral administration. Accepted regardless of food intake. Tablets should be swallowed whole, washed down with a small amount of liquid.

The initial dose is 10 mg (1 tablet) 3 times a day. If necessary, the dose can be increased to 20 mg 2 times a day under the control of blood pressure. The maximum daily dose is 40 mg.

In elderly patients or patients receiving combined (antianginal or antihypertensive) therapy, as well as in violation of liver function, in patients with severe impairment of cerebral circulation, the dose should be reduced.

In patients requiring higher doses of nifedipine, the drug should be used in long-acting dosage forms.

Side effects:

From the cardiovascular system: manifestations of excessive vasodilation (asymptomatic decrease in blood pressure, development or exacerbation of heart failure, "flushing" of blood to the skin of the face, hyperemia of the facial skin, a feeling of heat), tachycardia, palpitation, arrhythmia, peripheral edema, chest pains; rarely - excessive decrease in blood pressure, fainting, in some patients, especially at the beginning of treatment, there may be angina attacks, which requires withdrawal of the drug. Single cases of myocardial infarction are described.

From the central nervous system: head pain, dizziness, increased fatigue, weakness, drowsiness. With prolonged ingestion in high doses - paresthesia of the extremities, depression, anxiety, extrapyramidal (parkinsonian) disorders (ataxia, "masky" face, shuffling gait, stiffness of the arms and legs movements, tremor of hands and fingers, difficulty swallowing).

From the digestive system: dry mouth, increased appetite, dyspepsia (nausea, diarrhea, or constipation); rarely - gingival hyperplasia (bleeding, soreness, swelling), with prolonged admission - violations of the liver (intrahepatic cholestasis, increased activity of "liver" enzymes).

From the hematopoiesis: anemia, asymptomatic agranulocytosis, thrombocytopenia, thrombocytopenic purpura, and leukopenia.

Allergic reactions: rarely - skin itching, hives, exanthema, exfoliative dermatitis, photodermatitis; rarely - autoimmune hepatitis.

From the musculoskeletal system: arthritis, rarely - arthralgia, swelling of the joints, myalgia, convulsions of the upper and lower extremities.

From the urinary system: an increase in daily diuresis, impaired renal function (in patients with renal insufficiency).

Other: rarely - difficulty breathing, coughing; rarely - visual impairment (including transient blindness at the maximum concentration of nifedipine in plasma blood), gynecomastia (in elderly patients, completely disappearing after drug discontinuation), hyperglycemia, galactorrhea, pulmonary edema, bronchospasm, weight gain.

Overdose:

Symptoms: headache, hyperemia of the facial skin, prolonged pronounced decrease in blood pressure, inhibition of sinus node function, bradycardia, bradyarrhythmia.

Treatment: in case of severe poisoning (collapse, suppression of the sinus node), gastric lavage is performed, Activated carbon. Antidote are preparations of calcium ions: a slow intravenous injection of a 10% solution of calcium chloride or calcium gluconate is shown, followed by a switch to a long infusion. With a pronounced decrease in blood pressure - iv injection of dopamine or dobutamine. In the case of conduction disturbances - atropine, isoprenaline or an artificial pacemaker. With the development of heart failure - in / in the introduction of strophanthin. Catecholamines should be used only with a life threat (due to their reduced efficacy, a high dosage is required, which increases the risk of arrhythmia). It is recommended to monitor the concentration of glucose in the blood (insulin release may decrease) and electrolytes (potassium and calcium ions). Hemodialysis is ineffective.

Interaction:

The severity of lowering blood pressure is enhanced by the simultaneous use of other antihypertensive drugs, nitrates, cimetidine (to a lesser extent ranitidine), inhalational anesthetics and tricyclic antidepressants. Medicines from the group of blockers of the "slow" calcium channels can further increase the negative inotropic effect (reducing the force of cardiac contraction) of such antiarrhythmic agents as amiodarone and quinidine. Nifedipine causes a decrease in the concentration of quinidine in the blood plasma, after the withdrawal of nifedipine, a sharp increase in the concentration of quinidine can occur. Increases the plasma concentration of digoxin and theophylline, and therefore it is necessary to monitor the clinical effect and the content of digoxin and theophylline in the blood plasma.

Inductors of microsomal liver enzymes (rifampicin and others) reduce the concentration of nifedipine.

In combination with nitrates, tachycardia increases. Hypotensive effect reduces sympathomimetics, non-steroidal anti-inflammatory drugs (suppression of synthesis Pg in kidney and delay Na⁺ and fluid in the body), estrogens (fluid retention in the body). Calcium preparations can reduce the effect of blockers of "slow" calcium channels.

Nifedipine can displace from the bond with proteins preparations characterized by a high degree of binding (incl.indirect anticoagulants - coumarin and indanedione derivatives, anticonvulsants, non-steroidal anti-inflammatory drugs, quinine, salicylates, sulfinpyrazone), so that their concentration in the blood plasma can increase.

Suppresses the metabolism of prazosin and other alpha-adrenoblockers, as a result of which the hypotensive effect may increase.

Nifedipine inhibits the excretion of vincristine from the body and can cause an increaseside effects of vincristine, if necessary, reduce the dose of vincristine.

Lithium preparations can enhance toxic effects (nausea, vomiting, diarrhea, ataxia, tremor, tinnitus).

Procainamide, quinidine and other drugs that cause lengthening of the interval Q - T may increase the risk of significant lengthening of the interval Q - T.

Grapefruit juice inhibits the metabolism of nifedipine in the body, in connection with which, their simultaneous reception is contraindicated.

Special instructions:

The drug may increase the symptoms of coronary heart disease, cause manifestations of acute myocardial infarction, especially in patients, at the beginning of treatment or with an increase in the dose of the drug.

Patients who took beta-blockers should not abruptly discontinue treatment with these drugs (prior to initiation of nifedipine therapy), in view of the possibility of increasing the symptoms of myocardial ischemia.

It should be used with caution in patients with heart failure, aortic stenosis, especially with concomitant treatment with beta-blockers. nifedipine can accelerate the manifestation or worsen the already existing symptoms of heart failure.

Pay attention to peripheral edema.

Nifedipine, reducing the overall vascular peripheral resistance, can cause severe arterial hypotension, so you should carefully monitor blood pressure, especially in the initial period of treatment and after increasing the dose of the drug.

Nifedipine, used for a long time, can enhance the symptoms of coronary heart disease, cause myocardial infarction, and increase the death rate of patients with arterial hypertension or chronic coronary heart disease.

Nifedipine can be used in patients with intolerance or resistance to organic nitrates.

If during the therapy the patient is required to undergo surgery under general anesthesia, it is necessary to inform the anesthetist about the nature of the therapy.

Effect on the ability to drive transp. cf. and fur:

When you receive Nifedipine-Akrihin, especially at the beginning of treatment, possibly slowing down the speed reaction associated with a decrease in blood pressure.

This should be taken into account by persons engaged in potentially hazardous activities requiring increased attention and speed of psychomotor reactions.

Form release / dosage:

Tablets, film-coated, 10 mg.

Packaging:

25 tablets per foil blister Al / PVC.

2 blisters together with instructions for use are placed in a cardboard box.

Storage conditions:

In a dry, protected from light place at a temperature of no higher than 25 ° C.

Keep out of the reach of children.

Shelf life:

3 years. Do not use after the expiration date printed on the package.

Terms of leave from pharmacies:On prescription

Registration number:П N013683 / 01

Date of registration:10.09.2008 / 11.06.2015

Expiration Date:Unlimited

The owner of the registration certificate:Pharmaceutical factory "POLFARMA" JSCPharmaceutical factory "POLFARMA" JSC Poland

Manufacturer: & nbsp

POLPHARMA, S.A. Poland

Representation: & nbspAKRIKHIN OJSC AKRIKHIN OJSC Russia

Information update date: & nbsp23.06.2018

Illustrated instructions

Instructions

Nifedipine-Akrihin (Nifedipine-Akrikhin)