Fenigidine - instructions for use, dose, side effects, contraindications

Each tablet contains the active substance: nifedipine 10 mg; auxiliary substances: sucrose (refined sugar), lactose (sugar milk), potato starch, calcium stearate, polysorbate (Tween-80).

Description:Tablets are yellow or greenish-yellow in a flat-cylindrical form.

Pharmacotherapeutic group:blocker of "slow" calcium channels.

ATX: & nbsp

C.08.C.A.05 Nifedipine

Pharmacodynamics:

Phenigidine is a vasodilator, a blocker of "slow" calcium channels dihydropyridine type, has an antianginal and antihypertensive effect. Suppresses the transmembrane current of calcium ions in myocardial cells and smooth muscle cells of arteries and reduces intracellular calcium release, thereby causing relaxation of the muscles of the peripheral and coronary arteries.

Expanding the arteries, Fenigidine reduces the peripheral resistance of the vessels, reducing the work of the heart, the need for myocardium in oxygen and afterload.Fenigidin expands intact and atherosclerotic coronary arteries, in connection with which it protects the heart from coronary spasm and improves the blood supply of the ischemic myocardium. In people with normal arterial pressure (BP), phenygidine does not or almost does not affect BP.

Expansion of the coronary arteries and suppression of their spasm improve the oxygenation of the myocardium.

Pharmacokinetics:

Fenigidine is almost completely absorbed in the gastrointestinal tract (more than 90%). Absolute bioavailability is 40 - 70%. Phenigidine undergoes intensive metabolism during "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 -2-4 hours. The connection with plasma proteins (albumins) is 94 -91%.

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.

Phenigidine is mainly 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 pectoris, including vasospastic angina pectoris (Prinzmetal angina).

- arterial hypertension of various genesis.

Contraindications:

- hypersensitivity to Phenigidin (and other dihydropyridine derivatives) or other components of the drug;

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

- acute myocardial infarction (first 4 weeks);

- lactose intolerance;

- pregnancy;

- age under 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 sinus node weakness, tachycardia, idiopathic subaortic stenosis.

Carefully:Chronic heart failure, severe renal and / or liver dysfunction, severe cerebral circulation disorders, diabetes mellitus, malignant form of arterial hypertension, patients on hemodialysis (due to the risk of arterial hypotension), expressed stenosis of the mitral valve, hypertrophic obstructive cardiomyopathy, pronounced bradycardia, elderly age.

Pregnancy and lactation:Fenigidine penetrates the placental barrier and is excreted into breast milk. Fenigidine should be withdrawn for the time of breastfeeding or to stop breastfeeding.

Dosing and Administration:

The dosage regimen is set individually, depending on the degree of severity of the disease and the patient's response to ongoing therapy.

Phenyhydidine tablets, coated with a shell, should be swallowed whole before meals, without chewing, with a small amount of water. Initial dose: 1 tablet (10 mg) 2-3 times a day. If necessary, the dose of the drug can be increased to 2 tablets (20 mg) - 1 -2 times a day. The maximum daily dose is 40 mg.

To accelerate the effect of the drug at the beginning of the development of an attack of angina or hypertensive crisis, the tablet should be chewed, held for a while in the mouth, and then swallowed with a small amount of water.

Phenigidine is mainly metabolized in the liver. Therefore, the dose should be selected in accordance with the state of the patient's liver function.

In case of impaired renal function, the dose of Fenigidine should not be adjusted.

In elderly patients, the pharmacokinetics of Fenigidine are altered, so that lower doses of phenygidine may be required to maintain a sufficient therapeutic effect.

Side effects:

The most common side effects (> 1%, <10%) often occur early in the course of treatment and may disappear throughout the course.

The cardiovascular system: rapidity palpitations, excessive

vasodilation (asymptomatic decrease in blood pressure, "hot flushes" of blood to the skin of the face, hyperemia of the facial skin, a feeling of heat), peripheral edema.

Gastrointestinal tract: constipation.

Central nervous system: dizziness, headache, lethargy.

Skin: redness of the face and a feeling of heat, itching, rash,

angioedema, pustular or vesicle-bullous rash, sweating, urticaria, hypersensitivity reactions, exfoliative dermatitis.

Frequent side effects (> 0.1%, <1%):

General: pain (in the abdomen, chest, legs), weakness.

Cardiovascular system: decreased blood pressure, orthostatic hypotension, syncope, tachycardia.

On the part of the respiratory system: dyspnoea.

Gastrointestinal tract: diarrhea, dry mouth, dyspepsia, increased formation of gases in the intestine, nausea.

Musculoskeletal system: spastic contraction of the calf muscles.

Central nervous system: insomnia, increased nervous excitability, paresthesia, drowsiness, systemic dizziness.

Genitourinary system: nocturnal urination, polyuria.

Rare side effects (> 0.01%, <0.1%):

General: allergic reactions, chest pain, fever, chills, face swelling, fever.

Respiratory: nosebleeds.

Gastrointestinal tract: vomiting, anorexia, regurgitation, inflammation of the gingival mucosa, gingival hyperplasia, increased GGT, impaired liver function. Musculoskeletal system: pain in the joints and muscles.

Central nervous system: hyperesthesia, sleep disturbance, tremor, mood lability.

The organ of the senses: visual disturbances, pain in the eyes.

Genitourinary system: dysuria, impotence.

Very rare side effects (<0.01%):

Cardiovascular system: in isolated cases, a heart attack was noted. myocardium, which may have been a consequence of the underlying disease.

On the part of the respiratory organs: allergic reactions with edema of the larynx, bronchospasm, dyspnea.

Gastrointestinal tract: esophagitis, intestinal obstruction, hepatitis.

Endocrine system: transitional hyperglycemia.Gynecomastia can be observed mainly in elderly patients and after prolonged use of the drug. In all cases, it passes after the drug is discontinued.

The system of hematopoiesis: anemia, leukopenia, thrombocytopenia, thrombocytopenic purpura.

Genitourinary system: when Fenigidine is administered to patients with renal insufficiency, temporary impairment of renal function may occur.

Overdose:

Symptoms. In addition to the side effects listed above, depending on the severity of the intoxication, a significant reduction in blood pressure, tachycardia, chest pain (angina pectoris), collapse, loss of consciousness, nodular or ventricular extrasystoles due to sinus node suppression and delayed atrioventricular conduction , bradycardia or fainting; inhibition of insulin secretion. In severe cases, there may be a violation of consciousness with a transition to coma, hyperkalemia, metabolic alkalosis, hypoxia, cardiogenic shock with pulmonary edema.

Treatment. There is no specific antidote, so emergency therapy should be aimed at removing the drug from the body and restoring the stability of the cardiovascular system.

In the early detection of intoxication, the first therapeutic intervention should be gastric lavage with activated charcoal, if necessary with washing of the small intestine. You can give laxatives; However, after taking blockers of "slow" calcium channels, the suppression of intestinal motility to full atony should be considered. Phenigidine is not excreted in dialysis, so hemodialysis is ineffective. It is recommended that plasmapheresis be carried out (due to the fact that phenygidine is largely associated with proteins and its relatively small volume of distribution). Atropine and / or beta-sympathomimetics can be used for the symptomatic treatment of bradycardia. In life-threatening bradycardia, artificial heart rate drivers should be used.

Arterial hypotension as a result of cardiogenic shock and arterial dilatation can be eliminated by the administration of calcium (1-2 g calcium gluconate intravenously struino, then slow infusion), dopamine (maximum dose 25 μg / kg body weight per minute), dobutamine (maximum dose 15 μg / kg body weight per minute), epinephrine or norepinephrine.Doses of these funds are selected depending on the patient's reaction. The level of calcium in the serum can be normal or slightly elevated. Additional quantities of fluid should be administered with caution under the control of hemodynamic parameters in order to avoid cardiac overload.

Interaction:

Care should be taken when combining the drug Fenigidine with the following drugs:

- antihypertensives (ACE inhibitors, diuretics, etc.), nitrates, psychotropic drugs and magnesium preparations, because they are antioxidant. possible summation of their antihypertensive effects;

- combination with beta-blockers increases antihypertensive and antianginal effects, which is usually desirable; However, this combination of drugs should be used with caution because of the danger of excessive reduction in blood pressure, development of arterial hypotension and heart failure;

- combined use with prazosin can cause severe orthostatic hypotension;

- joint use with digoxin can lead to an increase in the level of digoxin in the blood plasma;

- Joint use with quinidine requires extreme caution, becausethe level of quinidine in the blood plasma can decrease with the administration of nifedipine after its elimination to increase; the combined administration of these two agents can cause malignant ventricular arrhythmia (pathological lengthening of the interval QT on the ECG);

- diltiazem raises the level of nifedipine in blood plasma;

- nifedipine may enhance anticoagulant effects of coumarin derivatives;

Because the nifedipine metabolized by enzyme CYP3A4, any inhibitor or inducer of this enzyme can affect the metabolism of nifedipine:

- juice of grapefruit, erythromycin and azole antimycotics (fluconazole, intraconazole, ketoconazole) can suppress the metabolism of nifedipine and therefore enhance its effects: Similarly, the simultaneous use of nifedipine and cimetidine increases the level of nifedipine in the blood plasma and enhances its effects; However, simultaneous administration with ranitidine does not lead to a significant increase in the level of nifedipine in blood plasma;

- rifampicin and phenytoin (inducers of metabolism) - significantly reduce the level of nifedipine in blood plasma; it is impossible to exclude the same interaction with barbiturates and carbamazepine;

- Ciclosporin is also an enzyme substrate CYP3A4; so when combined administration of cyclosporine and nifedipine, each can increase the duration of the effect of another.

Dand the potentiating effect reduces sympathomimetics, non-steroidal anti-inflammatory drugs (suppression of prostaglandin synthesis in the kidneys and sodium and liquid retention in the body), estrogens (fluid retention in the body).

- calcium preparations can reduce the effect of BCCI

- medicines with a high degree of binding (including indirect anticoagulants - indanedione derivatives, anticonvulsant drugs, NSAIDs, quinines, salicylates, sulfinpyrazon) can be displaced from the bond with proteins, so that their concentration in the blood plasma can increase.

- the severity of blood pressure lowering is enhanced by inhalational anesthetics.

- in combination with nitrates, tachycardia increases.

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

Prokainamide and other drugs that cause lengthening of the interval QT, reinforce the negative inotropic effect and may increase risk of significant lengthening of the interval QT.

Special instructions:

Special caution is necessary when prescribing the drug to patients with severe arterial hypotension (systolic blood pressure below 90 mmHg). The antihypertensive effect of this drug is enhanced with hypovolemia.

With renal diseases, a dose of Fenigidine is not necessary to correct. Reduction of pressure in the pulmonary artery and hypovolemia after dialysis can enhance the effects of the drug, and therefore, it is recommended to reduce its dose.

Care should be taken when administering this drug to patients with liver disease. With portal hypertension and cirrhosis of the liver, the dose should be reduced.

In rare cases, at the beginning of a course of treatment with Phenigidine or with an increase in its dose, chest pain (paradoxical angina due to decreased blood circulation in the ischemic zone) may occur soon after taking the drug. If there is a causal relationship between taking the drug and stenocardia, treatment should be discontinued. Patients with diabetes need to be closely monitored during therapy with phenygidine.

At the beginning of treatment, angina attacks may occur, and in patients with angina in history, the frequency, duration and severity of her attacks may increase.In the presence of arterial hypertension or coronary artery disease, abrupt withdrawal of phenygidine can cause hypertensive crisis or myocardial ischemia (the phenomenon of "bounce").Despite the absence of the "cancellation" syndrome in BCC, before the cessation of treatment a gradual reduction of doses is recommended.

During treatment, positive results are possible with a direct Coombs reaction and laboratory tests for antinuclear antibodies.

During the course of treatment the drug should avoid drinking alcohol.

In the case of lactose intolerance, the presence of lactose should be considered.

(15 mg) in the tablet shell.

During the treatment it is necessary to refrain from taking ethanol.

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

Patients should be advised to refrain from driving vehicles and working with mechanisms at the beginning of the course of treatment until their individual sensitivity to the drug becomes known. After this period, the degree of restrictions depends on the individual sensitivity of the patient.

Form release / dosage:

Tablets 10 mg. 10 tablets per contour cell package; 50 tablets per bottle of polymer.5 contour mesh packages or one vial of polymer together with instructions for use are placed in a cardboard pack.

Storage conditions:

In a dry, the dark place at a temperature of no higher than 25 ° C.

Keep out of the reach of children.

Shelf life:

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

Terms of leave from pharmacies:On prescription

Registration number:P N001714 / 01

Date of registration:23.07.2008

The owner of the registration certificate:FARMPROJECT, CJSC FARMPROJECT, CJSC Russia

Manufacturer: & nbsp

FARMPROJECT, CJSC Russia

Information update date: & nbsp15.03.2011

Illustrated instructions

Instructions

Phenyhydidine (Phenihidinum)