Finoptin - instructions for use, doses, side effects, contraindications

Tablets Finoptin® 40 mg: white, round, biconcave, film-coated tablets with engraving VL 40 on one side, on a fracture of white color without inclusions.

Tablets Phinoptin® 80 mg: white, round, biconcave, film-coated tablets with engraving VL80 on one side, on a fracture of white color without inclusions.

Pharmacotherapeutic group:blocker of "slow" calcium channels

ATX: & nbsp

C.08.D.A.01 Verapamil

C.08.D.A Phenylalkylamine derivatives

Pharmacodynamics:

Verapamil is one of the main drugs group of blockers of "slow" calcium channels (BCCC).It has antiarrhythmic, anti-anginal and antihypertensive activity.

BCCI (inhibits the transmembrane transport of calcium ions to the contractile fibers of smooth muscle cells) is a derivative of phenylalkylamines.

Antianginal effect is associated with both direct action on the myocardium and with influence on peripheral hemodynamics (reduces the tone of the peripheral arteries, the general peripheral vascular resistance). The blockade of calcium ions entering the cell leads to a decrease in the transformation of the energy encapsulated in the macroergic ATP bonds into mechanical work, a decrease in the contractility of the myocardium. Reduces the need for myocardium in oxygen, has a vasodilating, hypotensive, negative foreign and chronotropic action. Significantly reduces the conductivity of the atrioventicular (AV) compound, lengthens the period of its refractoriness, suppresses the automatism of the sinus node.

The action of verapamil appears 1-2 hours after ingestion. The maximum effect on ingestion is manifested in most cases 48 hours after the start of treatment, but in individual patients this interval may be prolonged.

Antiarrhythmic action is noted at a drug concentration in the blood plasma of at least 100 ng / ml. There was no statistical relationship between the concentration of verapamil and the degree of decrease in blood pressure (BP).

The drug reduces the need for myocardium in oxygen by decreasing myocardial contractility and reducing the heart rate. Causes the enlargement of the coronary vessels of the heart and increases coronary blood flow; reduces the tone of the smooth muscles of peripheral arteries and the general peripheral vascular resistance.

Verapamil significantly slows the atrioventricular conduction, depresses the automatism of the sinus node, which allows the use of the drug for the treatment of supraventricular arrhythmias.

Verapamil is the drug of choice for the treatment of angina of vasospastic genesis (Prinzmetal angina). Has an effect in angina pectoris, as well as in the treatment of angina with supraventricular rhythm disorders.

Pharmacokinetics:

After ingestion, more than 90% of the dose taken is absorbed. Bioavailability is 10-20% (intensive metabolism with the "first pass" through the liver).The maximum concentration of the drug in the blood plasma is achieved 1-2 hours after taking the drug inside. Intra- and interindividual concentrations in blood plasma vary considerably.

Eating does not reduce the absorption of the drug.

Liver failure can significantly increase the bioavailability of verapamil when ingested.

Verapamil penetrates the blood-brain and placental barrier.

It is actively metabolized at the "first passage" through the liver, mainly through N-dealkylation and O-demethylation. The main metabolites are norverapamil, which has a plasma concentration level exceeding the concentration of verapamil, N-dealkylverapamil and N-dealkylnorverapamil. Accumulation of the drug and its metabolites in the body explains the increased effect of course treatment. Connection with blood plasma proteins - 90%.

Half-life is from 2 to 8 hours with a single dose. When taking repeated doses, the elimination half-life is extended to 4.5-12 hours. It is excreted in a small amount in unchanged form (3-4%), the rest - in the form of metabolites (70%) by the kidneys and about 25% - with bile. The secretion of breast milk is low.

In patients with liver disease it was found that the bioavailability of verapamil increased, the association with plasma proteins decreased, the volume of distribution increased, the clearance decreased, and the half-life increased.

Patients with kidney disease the changes in kinetics are mostly absent. Hemodialysis, hemofiltration and peritoneal dialysis do not affect the excretion of verapamil.

In elderly patients the total clearance and volume of distribution may decrease, the maximum concentration in the blood plasma may increase, possibly as a consequence of a reduced metabolism during the "first passage" through the liver.

Indications:

1. Treatment and prevention of cardiac arrhythmias:

- paroxysmal supraventricular tachycardia;

- flutter and atrial fibrillation (tachyarrhythmic variant);

- supraventricular extrasystole.

2. Treatment and prevention:

- angina pectoris tension;

- unstable angina;

- vasospastic angina (Prinzmetal angina, variant angina).

3. Treatment of arterial hypertension.

Contraindications:

- Hypersensitivity to the components of the drug;

- severe left ventricular dysfunction;

- severe bradycardia;

- flutter and atrial fibrillation;

- heart failure with a reduced ejection fraction of less than 35% and / or a pulmonary artery wedge pressure of more than 20 mm Hg, except for supraventricular tachycardia to be treated with verapamil;

- arterial hypotension (systolic blood pressure less than 90 mm Hg);

- cardiogenic shock;

- sinoauric blockade;

- atrioventricular blockade of II or III degree (except for patients with an artificial pacemaker);

- acute myocardial infarction complicated by bradycardia, severe arterial hypotension and left ventricular failure;

- syndrome of weakness of the sinus node (syndrome of "bradycardia-tachycardia") except for patients with an artificial pacemaker;

- stenosis of the aortic aorta;

- Wolff-Parkinson-White syndrome;

- Morgagni-Adams-Stokes syndrome;

- Laun-Ganong-Levin syndrome (except for patients with a pacemaker);

- digitalis intoxication;

- acute heart failure;

- simultaneous intravenous application of beta-blockers and during the previous 2 hours;

- simultaneous reception with colchicine;

- pregnancy and the period of breastfeeding;

- age under 18 years (effectiveness and safety not established);

- lactose intolerance, lactase deficiency and glucose-galactose malabsorption syndrome;

- fructose intolerance and glucose / galactose absorption impairment syndrome or deficiency.

Carefully:

Required prescribe the drug to patients with atrioventricular blockade of the first degree, idiopathic hypertrophic subaortal stenosis, chronic heart failure, severe impaired liver function, diseases related to neuromuscular transmission (myasthenia gravis gravis, Lambert-Eaton syndrome, Duchenne muscular dystrophy), hypertrophic obstructive cardiomyopathy, in old age.

Pregnancy and lactation:

A drug contraindicated for use during pregnancy and lactation. Determined that verapamil penetrates the placental barrier and is found in the blood of the umbilical vein, excreted in breast milk. If you need to use the drug during lactation breast-feeding is necessary to cease.

Dosing and Administration:

Finoptin® is taken orally during or after a meal, with a small amount of water.Tablets to take, not rassasyvaya and not chewing!

Dosage regimen and duration of treatment are set individually depending on the patient's condition, severity, the features of the course of the disease and the effectiveness of therapy. The daily intake dose should not exceed 480 mg.

Angina pectoris: the initial dose in adults is 40-80 mg 3-4 times a day. The dose may increase weekly (with unstable angina daily) to achieve the desired clinical effect. Usually a daily maintenance dose in adults varies between 240 mg and 480 mg, divided into 3 or 4 doses.

Arterial hypertension: the initial dose in adults is 40-80 mg 3 times a day. The dose may increase weekly until the desired clinical effect is achieved. Usually a daily maintenance dose in adults varies between 240 mg and 480 mg, divided into 2 or 3 doses.

Arrhythmias: in the preventive treatment of recurrent paroxysmal supraventricular tachycardia, usually the initial dose in adults is 240-480 mg per day for 3 or 4 doses.

To control the frequency of contractions of the ventricles with chronic flutter or atrial fibrillation, the daily dose in adults is usually 240-320 mg for 3 or 4 doses.

The maximum antiarrhythmic effect is usually observed within 48 hours from the start of therapy in the given dosages.

Elderly people may be more sensitive to the action of verapamil when taking an ordinary adult dose. Consequently, dosage reduction may be necessary.

With hepatic insufficiency dosage should be reduced; at the expressed insufficiency - to 1/3 from usual adult dose (a daily dose of 120 mg).

Side effects:

With the use of verapamil possible:

- From the side of the cardiovascular system: tachycardia; rarely angina pectoris, up to the development of myocardial infarction (especially in patients with severe obstructive lesion of the coronary arteries), arrhythmia (including fibrillation and flutter of the ventricles), severe bradycardia, atrioventricular blockade, marked decrease in blood pressure, the appearance of symptoms of chronic heart failure with application of the drug in high doses, especially in predisposed patients, asystole, "hot flushes" of blood to the skin of the face, stopping the activity of the sinus node "sinus arrest".

- From the gastrointestinal side tract: nausea, constipation (rare diarrhea), vomiting, increased appetite, intestinal obstruction, dryness of the oral mucosa; in some cases - a transient increase in the activity of "liver" transaminases and alkaline phosphatase in the blood plasma.

- From the central nervous systems: dizziness, headache, fainting, anxiety, retardation, fatigue, asthenia, drowsiness, depression, paresthesia, extrapyramidal disorders (ataxia, "masky" face, "shuffling" gait, stiffness of hands and feet, trembling of hands and fingers, difficulty swallowing ).

- From the side of musculoskeletal systems: muscle weakness, myalgia, arthralgia.

- Allergic reactions: skin itch, rash, hyperemia of the facial skin, multiforme exudative erythema (including Stevens-Johnson syndrome).

- Other: increase in body weight; very rarely - agranulocytosis, gynecomastia, hyperprolactinaemia, impaired potency, irregular menstrual cycle, sleep disturbance, nightmares, blurred vision, ringing in the ears, frequent urination, angioedema, galactorrhea, arthritis, pulmonary edema, thrombocytopenia, asymptomatic, peripheral edema, bronchospasm, laryngospasm, gingival hyperplasia, photosensitivity, chest pain.

BCCI can reduce fertility in men, which should be taken into account if a man taking BCCI is diagnosed with an unexplained other causes of infertility. This action is completely reversible after withdrawal of drugs.

Overdose:

Clinical symptoms overdoses are mainly observed 30-60 minutes after ingestion, 5-10 times higher than the therapeutic dose.

From the central nervous system: confusion, convulsions; collapse can lead to coma.

There may be nausea, vomiting, metabolic acidosis and secondary hyperglycemia.

From the side of the cardiovascular system the most typical decrease in blood pressure, bradycardia, atrioventricular block, nodal elusive rhythm and asystole.

Treatment overdose individually and is based on the clinical condition. With early detection - gastric lavage, Activated carbon. With rhythm and conduction disturbances - intravenous injection of isoprenaline, norepinephrine, atropine, 10 - 20 ml of 10% calcium gluconate solution, artificial pacemaker; IV infusion of plasma-substituting solutions.To increase blood pressure in patients with IHSS prescribed alpha-adrenostimulants (phenylephrine); do not use isoprenaline and norepinephrine. Hemodialysis is ineffective. It is recommended to monitor the cardiovascular system.

Interaction:

Raises the AUC (area under the concentration-time curve) of carbamazepine in patients with stable partial epilepsy (risk of side effects such as diplopia, headache, ataxia and dizziness).

- enhances AUC, Css (ground clearance) and FROM_max (the maximum concentration of the drug) cyclosporine;

- enhances AUC and FROM_max glibenclamide;

- increases the concentration of sirolimus and tacrolimus;

- significantly increases AUC and FROM_max buspirone and midazolam;

- increases the concentration of theophylline (due to lower clearance), ethanol (and lengthens its effect), the concentration of quinidine (the risk of a pronounced decrease in blood pressure);

- can increase the concentration of atorvastatin and lovastatin;

- increases significantly AUC and FROM_max simvastatin;

- enhances AUC and FROM_max almotriptan;

- increases the concentration of cardiac glycosides (requires careful monitoring and dose reduction of glycosides) 4

- enhances AUC and FROM_max metoprolol and propranolol in patients with angina pectoris;

- increases the plasma concentration of colchicine (a substrate for CYP3A and p-glycoprotein);

- when taken orally significantly increases AUC and FROM_maxdoxorubicin;

- slightly increases AUC imipramine; does not affect the concentration of the active metabolite, desipramine;

- enhances FROM_max prazosin and terazosin and AUC terazosin;

- inhibitors CYP3A (including erythromycin, ritonavir and other antiviral HIV drugs), telithromycin increase plasma concentrations of verapamil;

- grapefruit juice increases AUC and FROM_max R- and S-isomer of verapamil;

- Cimetidine increases bioavailability of verapamil by almost 40-50% (due to a decrease in hepatic metabolism), in connection with which it may be necessary to reduce the dose of the latter;

- rifampicin can significantly reduce bioavailability (up to 92%), and AUC and FROM_max verapamil;

- phenobarbital increases the clearance of verapamil 5 times;

- sulfinpyrazone increases the clearance of verapamil by about 3 times and reduces bioavailability (60%);

- preparations of St. John's wort penetrate lower AUC R- and S-isomer of verapamil and accordingly FROM_max;

- when used simultaneously with inhalation anesthetics, the risk of bradycardia, atrioventricular blockade, heart failure increases;

- a combination with beta-blockers can lead to an increase in the negative inotropic effect, an increased risk of developing atrioventricular conduction disorders, bradycardia (the administration of verapamil and beta-blockers should be performed at intervals of several hours);

- prazosin and other alpha-blockers, as well as other antihypertensives (angiotensin-converting enzyme (ACE) inhibitors, vasodilators, diuretics, beta-blockers) intensify the hypotensive effect;

- disopyramide and flecainide should not be administered within 48 hours or 24 hours after using verapamil (summation of a negative inotropic effect, up to a lethal outcome);

- increases the risk of neurotoxic effect of lithium preparations;

- strengthens the action of peripheral muscle relaxants (a change in the dosage regimen may be required);

- with simultaneous use with acetylsalicylic acid (ASA), there was a slightly greater increase in bleeding time,than when applying only ASA;

- carbamazepine and lithium, the risk of neurotoxic effects increases.

Special instructions:

Patients with hypertrophic obstructive cardiomyopathy are at high risk of adverse cardiac effects. The incidence of adverse cardiac effects is also increased in patients who simultaneously take beta-blockers.

Doses of the drug Finoptin® should be reduced in patients with liver disease. During treatment with Finoptin®, liver function should be monitored periodically.

Patients with renal insufficiency should be carefully observed, despite the fact that, basically, the change in dosage is not necessary for them. Therapy with Finoptin® continues during dialysis.

Phinoptin ® should be used with caution in patients with chronic heart failure of moderate or moderate severity. Before therapy with Finoptin®, chronic heart failure should be treated with cardiac glycosides and / or diuretics.In the treatment it is necessary to monitor the function of the cardiovascular system, the respiratory system, the concentration of glucose and electrolytes in the blood, the volume of circulating blood and the amount of urine released.

It may be necessary to reduce the dosage of Finoptin® in patients with reduced neuromuscular conductivity (eg, with Duchenne muscular dystrophy, with the use of muscle relaxants during general anesthesia).

It is not recommended to stop the drug suddenly.

In the case of heart failure or conduction disorders during treatment, the dosage of the drug should be reduced or its use should be discontinued and / or appropriate therapy initiated.

The preparation contains lactose and sucrose. Patients with such rare hereditary diseases, such as galactose or fructose intolerance, lactase deficiency, glucose-galactose malabsorption or insulinase sucrose deficiency, should not take this medication.

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

Verapamil may affect the ability to driving and managing mechanisms, especially at the beginning of treatment,therefore it is necessary to refrain from engaging in potentially dangerous activities that require an increased concentration of attention and speed of psychomotor reactions.

Form release / dosage:

Tablets, film-coated, 40 mg and 80 mg.

Packaging:

For 30 or 100 tablets in a bottle of high-density polyethylene (HDPE) with a lid of the same material and with a ring of the first opening.

1 bottle per cardboard pack together with instructions for use.

Storage conditions:

Store at a temperature of 15 to 25 ° C.

Keep out of the reach of children.

Shelf life:

5 years.

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

Terms of leave from pharmacies:On prescription

Registration number:П N014974 / 01

Date of registration:22.07.2008

Date of cancellation:2016-10-18

The owner of the registration certificate:Orion CorporationOrion Corporation Finland

Manufacturer: & nbsp

ORION CORPORATION ORION PHARMA Finland

Representation: & nbspORION CORPORATION ORION PHARMA ORION CORPORATION ORION PHARMA Finland

Information update date: & nbsp18.10.2016

Illustrated instructions

Instructions

Finoptin® (Finoptin®)