Finoptin

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

The introduction of verapamil reduces the need for the heart muscle to receive oxygen, having a direct effect on the metabolic processes inside the myocardial cells, and at the same time weakening the afterload.

[1], [2], [3]

Indications Finoptina

It is used for the treatment of coronary artery disease, and in addition with these types of angina pectoris:

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

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

Use Finoptin and to reduce the increased blood pressure.

[4], [5]

Release form

The release of drugs is implemented in the form of tablets - 30 or 100 pieces inside the bottle; The box contains 1 such bottle.

[6]

Pharmacodynamics

Verapamil potentiates the blood flow to the myocardial region (directly affecting the vascular smooth muscle, reducing their tone and eliminating the spasm that affects the coronary vessels), and in addition to the post-stenotic 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 anti-arrhythmic effect (also in the case of supraventricular type arrhythmias). Verapamil inhibits the movement of the impulse inside the AV node, as well as, taking into account the type of arrhythmia, it helps to restore the sinus rhythm and stabilize the number of ventricular contractions.

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

Pharmacokinetics

When taken orally, about 90% of the drug is absorbed inside the small intestine. The level of bioavailability is 22% (due to pronounced metabolic processes during the 1st intrahepatic passage). In the case of repeated use, the bioavailability indicator almost doubles.

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

The metabolism of verapamil is realized inside the liver with the formation of a number of derivatives; however, only norverapamil has a medicinal effect.

Excretion of verapamil with its derivatives occurs through the kidneys. The amount of excreted unchanged substance is a maximum of 3-4%. Approximately 16% of the dosage is excreted through the intestine.

In the period of 24 hours, approximately 50% of the applied drug is excreted; about 5% is displayed in 5 days.

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

[7], [8], [9]

Dosing and administration

It is necessary to use medicine inside, washing down a tablet with usual water. Do not drink the drug grapefruit juice. It is recommended to take verapamil with food or immediately after the completion of a meal. Do not use the medicine in a horizontal position.

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

For people who have used verapamil for a long period of time, you need to perform a gradual abolition of the drug.

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

The size of the dosage of the drug for an adult.

In cases of arrhythmias and ischemic heart disease, people with a weight of more than 50 kg are often administered 0.12-0.48 g of verapamil per day. The daily portion is divided into 3-4 use at regular time intervals. At the beginning of treatment should be applied to the minimum dosage, and the increase in portions should occur under medical supervision. During the day, you can apply a maximum of 0.48 g of the drug.

People with a weight of less than 50 kg in the case of increased blood pressure indicators are mainly used at 0.12-0.36 g of the drug per day. The specified portion is divided into 3 uses. Therapy begins with small dosages; increase is allowed only with good tolerability of drugs and insufficient control of blood pressure levels.

Dosage regimens in pediatrics.

It is possible to prescribe medication to children only for disorders of the rhythm of the heartbeat, for other violations it is better not to use it.

For the age of 4-6 years, use of 0.08-0.12 g of verapamil per day (the dosage is divided into 2-3 use). Children from the older preschool group treatment is carried out only under the supervision of a doctor.

Age 6-14 years - in the case of any type of arrhythmia per day, 0.08-0.36 g of the drug should be applied. The division of the dosage is 2-4 use. At first, minimal portions are used, and the change in dosage is allowed only with a low intensity of the effects of drugs and good tolerance.

In persons older than 14 years of age with a weight of over 50 kg, Finotypin is used in portions that are prescribed to adults.

Other categories of patients.

Older people should begin treatment with minimal doses of drugs (patients in this group may experience increased sensitivity to the drug). Changing the dosage is performed only under the careful supervision of a physician and while monitoring the blood pressure and ECG values.

Persons with problems in the hepatobiliary structure need to change the dosage of the drug, taking into account the intensity of hepatic dysfunction (in such patients, the metabolic processes of verapamil slow down and the plasma index of the unchanged component increases). The size of the initial portion of the day - a maximum of 0.08 g. The change in dosage should be made very carefully.

[12], [13]

Use Finoptina during pregnancy

It is forbidden to appoint Finoptin on the 1st and 2nd trimesters. In the 3rd trimester, it is used only with strict indications and under close medical supervision. The active drug element can overcome the BBB.

Verapamil can be secreted in small quantities with breast milk. With limited clinical tests, no adverse effects on newborns were noted, but given the small number of tests performed, it is recommended to stop breastfeeding for the duration of therapy when using drugs.

Contraindications

The main contraindications:

• severe insufficiency of left ventricular function (pressure indicator with lung artery seizure -> 20 mm Hg or left ventricular ejection fraction <20-30%);
• intensive decrease in blood pressure values (systolic pressure level <90 mmHg) or the presence of cardiogenic shock;
• having a grade 2–3 blockade (there is no functioning pacemaker);
• SSS (in the absence of a functioning pacemaker in a patient);
• atrial fibrillation, accompanied by a disorder of conduction processes (for example, WPW syndrome or LGL syndrome);
• severe intolerance to verapamil hydrochloride;
• widespread ventricular tachycardia;
• introduction in combination with β-adrenergic blockers for intravenous injection;
• myocardial infarction in the active phase;
• SA blockade;
• bradycardia (with heart rate values <50 beats per minute);
• CH in uncompensated form.

Side effects Finoptina

Adverse effects associated with treatment were investigated during post-marketing and clinical tests. Among the violations found:

• disorders in the work of the cardiovascular system: AV block (grade 1–3), blockage of the sinus node, heartbeat, sinus bradycardia, increased heart rate, peripheral puffiness, a decrease in blood pressure and tides. There is information about the appearance of HF and potentiation of the intensity of manifestations of an already existing HF;
• problems with the gastrointestinal tract function: intestinal obstruction, nausea, pain and discomfort in the epigastric and abdominal zone, stool disorders, gingival hyperplasia, and vomiting;
• lesions associated with the central nervous system: headaches, increased fatigue, extrapyramidal signs, dizziness, tremor and paresthesias;
• disorders of the senses: ear ringing;
• symptoms associated with reproductive function: galactorrhea, gynecomastia or erectile dysfunction;
• lesions of the musculoskeletal structure: myalgia or arthralgia, as well as myasthenia;
• laboratory test readings: hyperprolactinemia and elevated intrahepatic enzyme values;
• manifestations of allergy: urticaria, erythema polyforme, SSD, alopecia, maculopapular rash, angioedema, purpura, erythromelalgia and epidermal itching.

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

[10], [11]

Overdose

Verapamil poisoning can lead to a significant decrease in blood pressure, renal disorders, problems with the rhythm of the heartbeat, as well as disturbances in EBV and pH.

Taking into account the size of a portion of Finotypin and the patient's age, such manifestations may be noted: a decrease in blood pressure and arrhythmia (also rhythms having a borderline character, with AV dissociation, and in addition a significant AV blockade), reaching a shock with subsequent cardiac arrest and death. Along with this, there may be metabolic acidosis, hypoxia, hyperglycemia or hypokalemia, convulsions and problems with the filtration ability of the kidneys. Severe intoxication causes dizziness and loss of consciousness, reaching coma, and in addition to this cardiogenic shock, accompanied by pulmonary edema.

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

Therapy includes the elimination of signs of poisoning and maintaining a stable activity of the cardiovascular system and the respiratory system.

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

Performing hemodialysis in case of verapamil intoxication will have no effect. This can help the procedure plasmapheresis and hemofiltration.

Verapamil has an antidote - Ca element. In case of overdose, it is used in / in the introduction of 10% Ca gluconate (10-20 ml). If required, the intravenous injection can be repeated (an additional intravenous procedure can also be performed via an IV drip - a portion of approximately 5 mmol per hour).

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

Reduced blood pressure (associated with enhanced vasodilation and the development of cardiogenic shock) requires the use of dopamine (per serving not more than 25 µg / kg per minute), norepinephrine or dobutamine (per serving maximum 15 µg / kg per minute).

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

Plasma Ca values should be monitored (with verapamil intoxication, the optimal value is within or slightly above the upper norm).

[14]

Interactions with other drugs

The use together with antiarrhythmic drugs and β-blockers causes mutual potentiation of cardiovascular activity and an increase in the likelihood of AV blockade, arrhythmias, HF and lower blood pressure values. It is necessary to carefully combine these drugs and change the dosage according to need.

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

Finoptin leads to a 10% reduction in fleckinidine clearance, but this does not have any significant clinical effect.

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

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

Verapamil increases Prazozin's Cmax by 40%, and in addition to this AUC and Cmax of Terazosin (by 24% and 25% respectively). Co-administration of these drugs enhances the antihypertensive effect.

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

The drug increases the level of AUC of carbamazepine, and at the same time increases its neurotoxic effect, increasing the likelihood of developing diplopia, dizziness, headaches, and ataxia.

The 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 indices of the drug inside the serum.

The drug increases the rate of exposure to colchicine.

Substances that block neuromuscular impulses are able to potentiate the therapeutic activity of verapamil.

The introduction of sulfinpirazon causes a weakening of the antihypertensive effects of the drug.

Combining drugs with aspirin increases the likelihood of bleeding.

LS increases the plasma values of ethanol.

The drug increases the statins (among them, simvastatin with lovastatin and atorvastatin) inside the serum, which may require a change in their portions. At the same time, the combination of such drugs increases the level of AUC of verapamil (when administered with atorvastatin - by 42.8%, and also 2.6 times in the case of combination with simvastatin). Verapamil metabolism does 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 allympriptan inside the blood serum.

The combination with cimetidine causes an increase in the level of AUC medication.

The introduction of the drug together with doxorubicin causes an increase in its serum values in individuals with small-cell pulmonary carcinoma. In people with advanced neoplasms, there are no significant changes in the pharmacokinetics of doxorubicin when administered with Finoptin.

The drug increases by 45% intracellular indicators Cmax and the level of AUC of cyclosporine.

Introduction simultaneously with tacrolimus or sirolimus may increase their intraplasma values.

When taking drugs with grapefruit juice, the indicators of verapamil inside the serum increase.

Hypericum substances reduce the value of the drug inside the serum.

[15], [16], [17]

Storage conditions

Finoptin should be kept in a closed place for small children at standard temperature marks.

Shelf life

Finoptin can be used for 5 years from the date of sale of the drug product.

Analogs

Analogues of drugs are Enap, Vazar, Ketanserin, Lipril with Kapilar, Sulfur and Anaprilin, and in addition Atacand and Tivortin with Hepar Compositum, Lodoz, Aprovel and Ionic with Glyoxal Compositum. In addition, the list of cordipin, Adalat, Bidop with Amlotop, Teveten and Amprilan.

[18], [19], [20]