Finoptin

Finoptin helps block the activity of Ca channels. Its active ingredient is verapamil, which blocks the flow of calcium ions penetrating the walls of cardiomyocytes, as well as cells inside the smooth vascular muscles.

Verapamil administration reduces the heart muscle's need for oxygen by directly influencing metabolic processes within myocardial cells and thereby reducing afterload.

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Indications Finoptina

It is used to treat coronary heart disease, and in addition to this, for the following types of angina:

• unstable angina - progressive phase or resting phase;
• angina pectoris (stable);
• vasospastic angina (this includes spontaneous angina);
• angina pectoris developing after a heart attack (without symptoms of heart failure), which requires the administration of substances that block β-adrenergic receptors.

It can also be prescribed for arrhythmias of various forms (for example, atrial fibrillation accompanied by acceleration of AV conduction (except for WPW syndrome)) or paroxysmal supraventricular tachycardia.

Finoptin is also used to reduce elevated blood pressure.

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Release form

The drug is released in the form of tablets - 30 or 100 pieces in a bottle; the box contains 1 such bottle.

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Pharmacodynamics

Verapamil potentiates blood flow to the myocardial region (directly affecting the smooth muscles of the vessels, reducing their tone and eliminating spasm affecting the coronary vessels), and in addition to this, to the poststenotic zones.

The hypotensive effect of the drug develops with a weakening of the systemic resistance of peripheral vessels; however, the heart rate does not increase.

The drug has an intense antiarrhythmic effect (also in the case of supraventricular arrhythmia). Verapamil inhibits the movement of the impulse inside the AV node, and also, taking into account the type of arrhythmia, helps to restore the rhythm of the sinuses and stabilize the number of ventricular contractions.

Verapamil has almost no effect on normal blood pressure and pulse rates (if the pulse rate is normal, then the heart rate may change only slightly).

Pharmacokinetics

When taken orally, about 90% of the drug is absorbed in the small intestine. The bioavailability level is 22% (due to pronounced metabolic processes during the first intrahepatic passage). In case of repeated use, the bioavailability index increases almost twofold.

Serum Cmax values of verapamil are recorded after 1-2 hours from the moment of oral administration. The half-life is 3-7 hours. Approximately 90% of the consumed portion is synthesized with whey protein.

Verapamil metabolism processes are realized inside the liver with the formation of a number of derivatives; however, only norverapamil has a medicinal effect.

Verapamil and its derivatives are excreted via the kidneys. The amount of excreted unchanged substance is a maximum of 3-4%. Approximately 16% of the dosage is excreted via the intestines.

Approximately 50% of the administered drug is excreted within 24 hours; approximately 70% is excreted within 5 days.

In individuals with liver failure, the half-life of the active substance of the drug is prolonged.

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Dosing and administration

The medicine must be taken orally, with a tablet washed down with plain water. The medicine must not be washed down with grapefruit juice. It is recommended to take verapamil with food or immediately after finishing a meal. The medicine must not be used while in a horizontal position.

People who have had a myocardial infarction can take the medicine at least 7 days after the end of the acute phase.

In people who have been using verapamil for a long period of time, the drug should be gradually discontinued.

The dose sizes of verapamil are selected individually, taking into account the existing clinical situation, the personal characteristics of the patient and additional treatment.

Dosage sizes of medication for an adult.

For people over 50 kg in case of arrhythmia and coronary heart disease, 0.12-0.48 g of verapamil per day is often administered. The daily dose is divided into 3-4 doses at equal time intervals. At the beginning of treatment, minimal dosages should be used, and the dose should be increased under medical supervision. A maximum of 0.48 g of the drug can be used per day.

People weighing less than 50 kg in case of increased blood pressure are usually given 0.12-0.36 g of the drug per day. The specified portion is divided into 3 doses. Therapy begins with small doses; an increase is allowed only with good tolerance of the drug and insufficient control of blood pressure.

Drug dosing regimens in pediatrics.

The medication can be prescribed to children only in case of heart rhythm disorders; it is better not to use it for other disorders.

For children aged 4-6 years, 0.08-0.12 g of verapamil is used per day (the dosage is divided into 2-3 doses). For children from the senior preschool group, treatment is carried out only under the supervision of a doctor.

Age 6-14 years – in case of any type of arrhythmia, 0.08-0.36 g of the drug should be used per day. The dosage is divided into 2-4 uses. At first, minimal portions are used, and a change in dosage is allowed only with a weak intensity of the drug's effect and good tolerability.

For individuals over 14 years of age weighing over 50 kg, Finotipine is used in the doses prescribed for adults.

Other categories of patients.

Elderly people should start treatment with minimal doses of the drug (patients in this group may have increased sensitivity to the drug). Dosage changes are performed only under close medical supervision and with monitoring of blood pressure and ECG.

People with problems in the functioning of the hepatobiliary structure need to change the dosage of the drug, taking into account the intensity of liver dysfunction (in such patients, the metabolic processes of verapamil slow down and the intraplasmic index of the unchanged component increases). The size of the initial portion per day is a maximum of 0.08 g. Dosage changes should be made with extreme caution.

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Use Finoptina during pregnancy

It is prohibited to prescribe Finoptin in the 1st and 2nd trimesters. In the 3rd trimester, it is used only under strict indications and under careful medical supervision. The active element of the drug can overcome the BBB.

Verapamil may be secreted in small amounts into breast milk. No negative effects on newborns were observed in limited clinical trials, but given the small number of tests conducted, if there is a need to use the drug, it is recommended to stop breastfeeding for the period of therapy.

Contraindications

Main contraindications:

• severe left ventricular dysfunction (pulmonary artery occlusion pressure >20 mmHg or left ventricular ejection fraction <20-30%);
• an intense decrease in blood pressure values (systolic pressure level is <90 mm Hg) or the presence of cardiogenic shock;
• having a 2-3 degree block (there is no functioning pacemaker);
• SSSU (if the patient does not have a functioning pacemaker);
• atrial fibrillation accompanied by a disorder of conduction processes (for example, WPW syndrome or LGL syndrome);
• severe intolerance to verapamil hydrochloride;
• wide complex ventricular tachycardia;
• administration in combination with β-blockers for intravenous injection;
• myocardial infarction in the active phase;
• SA block;
• bradycardia (with heart rate values <50 beats per minute);
• Heart failure in uncompensated form.

Side effects Finoptina

Treatment-related adverse events have been investigated during post-marketing and clinical testing. Among the disorders identified are:

• disorders in the functioning of the cardiovascular system: AV block (1-3 degrees), block affecting the sinus node, palpitations, sinus bradycardia, increased heart rate, peripheral edema, decreased blood pressure and hot flashes. There is information about the appearance of heart failure and potentiation of the intensity of manifestations of existing heart failure;
• problems with the gastrointestinal tract: intestinal obstruction, nausea, pain and discomfort in the epigastric and abdominal area, bowel disorders, hyperplasia affecting the gums, and vomiting;
• CNS-related lesions: headaches, increased fatigue, extrapyramidal symptoms, dizziness, tremor and paresthesia;
• disturbances of the sensory organs: tinnitus;
• symptoms related to reproductive function: galactorrhea, gynecomastia or erectile dysfunction;
• lesions of the musculoskeletal structure: myalgia or arthralgia, as well as myasthenia;
• laboratory test results: hyperprolactinemia and increased intrahepatic enzyme levels;
• Allergy manifestations: urticaria, erythema multiforme, SJS, alopecia, maculopapular rashes, Quincke's edema, purpura, erythromelalgia and epidermal pruritus.

In post-marketing testing, the development of tetraparesis associated with the combined use of Finoptin and colchicine was noted in isolated cases. Such an effect could be caused by the passage of colchicine through the BBB due to the suppression of P-gp and CYP3 A4 activity under the influence of verapamil.

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Overdose

Verapamil poisoning can lead to significant decreases in blood pressure, renal dysfunction, problems with heart rhythm, and disturbances in EBV and pH levels.

Depending on the dose of Finotipin and the patient's age, the following symptoms may occur: decreased blood pressure and arrhythmia (also rhythms of a borderline nature, with AV dissociation, and in addition, significant AV block), leading to shock followed by cardiac arrest and death. Metabolic acidosis, hypoxia, hyperglycemia or hypokalemia, seizures and problems with the filtration capacity of the kidneys may also occur. Severe intoxication causes dizziness and loss of consciousness, leading to coma, and in addition, cardiogenic shock, accompanied by pulmonary edema.

Overdose should be treated in hospital. Immediately after the administration of a large dose of the drug, gastric lavage and the use of sorbents are performed to reduce the absorption of verapamil.

Therapy includes eliminating signs of poisoning and maintaining stable activity of the cardiovascular and respiratory systems.

In case of severe poisoning, resuscitation measures are performed, including artificial respiration, defibrillation, cardiac stimulation and indirect massage of the heart area.

Performing hemodialysis in case of verapamil intoxication will not have an effect. However, plasmapheresis and hemofiltration procedures can help.

Verapamil has an antidote – the element Ca. In case of overdose, intravenous administration of 10% Ca gluconate (10-20 ml) is used. If necessary, the intravenous injection can be repeated (an additional intravenous procedure can also be performed through a drip – a dose of approximately 5 mmol per hour).

In case of AV block, sinus bradycardia or cardiac arrest, isoprenaline, atropine and orciprenaline are used or cardiac pacing is performed.

A decrease in blood pressure (associated with increased vasodilation and the development of cardiogenic shock) requires the use of dopamine (in a dose of no more than 25 mcg/kg per minute), norepinephrine or dobutamine (in a dose of maximum 15 mcg/kg per minute).

Enhanced vasodilation (early phases) requires intravenous injections of Ringer's solution or physiological fluid.

It is necessary to monitor plasma Ca values (in case of verapamil intoxication, the optimal value is within or slightly above the upper limit).

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Interactions with other drugs

Use together with antiarrhythmic drugs and β-blockers causes mutual potentiation of cardiovascular activity and an increased likelihood of AV block, arrhythmia, heart failure and a decrease in blood pressure. It is necessary to combine these medications very carefully and change the dosages as needed.

When verapamil is administered with quinidine, the clearance of the latter decreases. The combined use of these drugs can lead to a decrease in blood pressure and pulmonary edema (mainly in people with hypertrophic cardiomyopathy, which is obstructive in nature).

Finoptin causes a 10% decrease in flecainidine clearance, but this does not have any significant clinical effect.

In people with angina pectoris, the drug increases the Cmax and AUC values of metoprolol (by 41% and 32.5%, respectively), as well as propranolol (by 94% and 65%, respectively).

Use in combination with diuretics, vasodilators and antihypertensive drugs causes an increase in antihypertensive activity.

Verapamil increases the Cmax of prazosin by 40%, and in addition, the AUC and Cmax of terazosin (by 24% and 25%, respectively). The combined administration of these drugs enhances the antihypertensive effect.

Antiretroviral agents when combined with the drug increase the verapamil index in the serum. It is necessary to use such combinations very carefully, adjusting the dosage of Finoptin.

The drug increases the AUC level of carbamazepine, and along with this increases its neurotoxic effect, increasing the likelihood of developing diplopia, dizziness, headaches and ataxia.

Combination with lithium leads to potentiation of its neurotoxic properties.

Rifampicin reduces serum Cmax values of verapamil and, at the same time, weakens its antihypertensive activity.

Clarithromycin with erythromycin, as well as telithromycin, increase the serum levels of the drug.

The drug increases the exposure rate of colchicine.

Substances that block neuromuscular impulses are capable of potentiating the therapeutic activity of verapamil.

The introduction of sulfinpyrazone causes a weakening of the antihypertensive effect of the drug.

Combining the drug with aspirin increases the risk of bleeding.

LS increases plasma ethanol levels.

The drug increases the levels of statins (including simvastatin with lovastatin and atorvastatin) in serum, which may require a change in their dose. At the same time, when combining such drugs, the level of AUC of verapamil increases (when administered with atorvastatin - by 42.8%, and by 2.6 times in the case of combination with simvastatin). Metabolic processes of verapamil do not change when used with fluvastatin, lovastatin, pravastatin and rosuvastatin.

The drug increases the values of digitoxin with digoxin, and in addition to this, individual hypoglycemic substances (glyburide), imipramine with midazolam, theophylline and buspirone with almotriptan in the blood serum.

Combination with cimetidine causes an increase in the AUC level of the drug.

Administration of the drug together with doxorubicin causes an increase in its serum values in individuals with small cell lung carcinoma. In individuals with advanced tumors, no significant changes in the pharmacokinetics of doxorubicin are observed when administered with Finoptin.

The drug increases intra-serum Cmax and AUC levels of cyclosporine by 45%.

Concomitant administration with tacrolimus or sirolimus may increase their intraplasmic levels.

When taking the drug with grapefruit juice, verapamil levels in the serum increase.

St. John's wort substances reduce the values of the drug inside the serum.

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Storage conditions

Finoptin should be stored in a place out of the reach of small children at standard temperatures.

Shelf life

Finoptin can be used for a period of 5 years from the date of sale of the medicinal product.

Analogues

Analogues of the drug are Enap, Vazar, Ketanserin, Lipril with Kapilar, Sulfur and Anaprilin, and in addition Atacand and Tivortin with Gepar Compositum, Lodoz, Aprovel and Ionic with Glyoxal compositum. In addition, the list includes Cordipin, Adalat, Bidop with Amlotop, Teveten and Amprilan.

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