Finlepsin

Finlepsin is a drug from the anticonvulsant group. It is a derivative of dibenzazepine, which has antipsychotic, antidepressant, analgesic and antidiuretic effects.

The therapeutic effectiveness of the drug develops in the case of combined, as well as simple epileptic seizures, against the background of which generalization of a secondary nature may be observed, etc. When using the drug, a weakening of the signs of depression, aggression, anxiety and irritability is observed.

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Indications Finlepsin

It is used for the following disorders:

• neuralgia;
• different types of epilepsy;
• pain associated with nervous disorders in diabetics;
• alcohol withdrawal;
• various forms of convulsive disorders – attacks, spasms, etc.;
• psychotic disorders.

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Release form

The drug is released in the form of tablets - 10 pieces inside a cell plate. In a box - 3, 4 or 5 such plates.

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Pharmacodynamics

Under the influence of the drug, the activity of potential-dependent Na-channels is blocked, which helps to stabilize the walls of overexcited neurons, reduces the conduction of impulses through synapses and slows down serial neuronal discharges.

There is also a reduction in the volume of glutamate (a neurotransmitter amino acid) released by the body, which exhibits an excitatory effect, thereby helping to lower the seizure threshold of the nervous system, which ultimately reduces the risk of developing an epileptic seizure.

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Pharmacokinetics

The drug has a low absorption rate, but it is complete; the degree of absorption is not tied to food intake. The required level of the drug in the body is observed for 12 hours, and its therapeutic effect is maintained for 4-5 hours.

The drug reaches equilibrium values in plasma after 7-14 days of therapy. But these indicators may vary due to the characteristics of the patient's metabolic processes: autoinduction of intrahepatic enzyme systems, heteroinduction of other drugs used in combination, portion size, patient's condition and course duration. It has been determined that carbamazepine crosses the placenta and is excreted in breast milk.

The processes of drug metabolism are realized inside the liver with the formation of the main metabolic components: carbamazepine-10,11-epoxide, which has a pronounced activity, as well as a conjugate and glucuronic acid, which has no activity. During the metabolic processes, an active metabolic element is formed - 9-hydroxy-methyl-10-carbamoyl acridan, which can induce its own metabolism.

Excretion occurs mainly in urine; some is excreted in feces.

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Dosing and administration

The medication is prescribed for oral use, regardless of food intake.

During epilepsy, Finlepsin is used as monotherapy. In cases where it is added to antiepileptic treatment, this is done gradually, with strict monitoring of dosages. If a tablet is missed, it must be taken immediately after remembering (but taking a 2nd dosage is prohibited).

At first, the medicine is taken in a dose of 0.2-0.4 g per day. After that, the dose can be gradually increased to achieve the optimal result. The size of the maintenance dose per day is 0.8-1.2 g (this dose is divided into 1-3 uses). No more than 1600-2000 mg of the drug can be administered per day.

The dosage for a child is determined by his age. However, if he cannot swallow the tablet whole, it is allowed to crush, chew or dissolve it in a small amount of water.

For children aged 1-5 years, use a dose of 0.1-0.2 g, gradually increasing it to achieve the optimal effect.

Persons aged 6-10 years require a daily dosage of 0.2 g, and then it is gradually increased.

A child aged 11-15 years should initially take 0.1-0.3 g of the medicine. Then the dose is gradually increased by 0.1 g until the required therapeutic effect is achieved.

Average maintenance doses per day:

• 1-5 years of age – 0.2-0.4 g;
• 6-10 years of age – in the range of 0.4-0.6 g;
• 11-15 years of age – 0.6-1 g (split into several doses).

The duration of the treatment cycle is directly determined by the patient's personal characteristics and medical indications. In any situation, the attending physician should make a decision regarding the treatment regimen. Often, the option of reducing the dose or canceling the medication is considered when the patient has not had any attacks for a period of 2-3 years.

When discontinuing therapy, a gradual reduction in dosage should be performed over 1-2 years; EEG parameters should be continuously monitored. In a child, increasing age and weight should also be taken into account.

When treating other disorders, the dose size and duration of drug administration are selected by the doctor, taking into account the personal characteristics of the patient and the severity of the disease.

Use Finlepsin during pregnancy

Carbamazepine should be used with extreme caution in pregnant women with epilepsy. When tested on animals, oral administration of the drug resulted in defects.

In cases where a woman taking carbamazepine becomes pregnant (or plans to conceive, or if there is a need to use the drug during an existing pregnancy), it is necessary to carefully evaluate the probable benefit from the introduction of the substance and compare it with the possible consequences (this applies most of all to the 1st trimester).

Women of potential fertility are advised to use carbamazepine alone whenever possible.

It is necessary to administer minimal doses of the drug that give results and monitor plasma levels of carbamazepine.

Women should be advised of the increased risk of congenital anomalies and offered prenatal screening.

Effective anticonvulsant treatment should not be interrupted during pregnancy, since an exacerbation of the pathology may pose a threat to both the patient and the fetus.

During pregnancy, a woman may experience a deficiency of vitamin B9. Anticonvulsants can potentiate this deficiency, which is why it is necessary to additionally prescribe this element for intake during the specified period.

To prevent bleeding disorders in newborns, women (during the last weeks of pregnancy) and newborn babies need to take vitamin K1.

There are reports of seizures or respiratory depression in newborn infants, as well as diarrhea, vomiting, or poor appetite, which may be caused by carbamazepine.

Carbamazepine is secreted with milk during breastfeeding (equals 25-60% of the plasma marks of the drug). It is necessary to carefully evaluate the benefits and possible consequences of using the drug during breastfeeding. Breastfeeding in parallel with taking carbamazepine is allowed only under the condition that the infant is monitored for possible occurrence of side effects (for example, allergic epidermal manifestations or increased drowsiness).

Contraindications

Main contraindications:

• severe sensitivity to the components of the drug or tricyclics;
• disorders of hematopoietic processes within the bone marrow;
• intermittent porphyria in the active phase;
• AV block;
• combination with MAOIs or lithium agents.

It is used with great caution in individuals with decompensated CHF, renal/hepatic dysfunction, dilutional hyponatremia, suppression of hematopoiesis in the bone marrow, prostatic hyperplasia, alcoholism in the active phase and increased IOP values, as well as in combination with other drugs and in the elderly.

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Side effects Finlepsin

Often, side effects when administering a medication appear due to exceeding the dose or significant variations in the active ingredient levels within the body.

Mainly, disorders associated with the function of the nervous system are observed: ataxia, headaches, systemic weakness, dizziness, drowsiness, etc.

Signs of allergy may occur, including erythroderma, urticaria, epidermal rash, etc.

Among the hematopoietic disorders: eosinophilia, lymphadenopathy, thrombocytopenia or leukopenia, and leukocytosis.

There is a risk of developing problems in the gastrointestinal tract: xerostomia, vomiting, constipation, nausea, diarrhea, as well as an increase in the action of intrahepatic transaminases and GGT.

Lesions affecting metabolic processes and endocrine function may occur: water retention, vomiting, edema, weight gain, hyponatremia, etc.

There is a possibility of disturbances in the functioning of the urogenital system, cardiovascular system, musculoskeletal system, and also sensory organs.

Overdose

Poisoning with Finlepsin leads to the development of various symptoms associated with disorders of the cardiovascular system, nervous system, and also the sense organs, respiratory system and systemic deviations. This includes disorientation, hallucinations, suppression of the central nervous system, visual blurring, agitation, coma and drowsiness. In addition, fainting, tachycardia, pulmonary edema, abnormal blood pressure, nausea, breathing problems, urinary retention, vomiting, etc.

It is found that the drug has no antidote, so supportive actions are performed depending on the manifestations that have developed. In case of complex disorders, the patient is sent to the hospital.

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Interactions with other drugs

The combination of the drug and substances that slow down the action of CYP3A4 leads to an increase in the plasma level of carbamazepine and the appearance of negative signs. Use together with inducers of CYP3A4 activity usually increases the rate of metabolic processes of carbamazepine, reducing its indicators and medicinal effect.

Administration together with diltiazem, viloxazine, fluvoxamine, and also verapamil, acetazolamide, felodipine, cimetidine and dextropropoxyphene, as well as desipramine, danazol, nicotinamide, macrolides (troleandromycin, erythromycin with clarithromycin and josamycin) and individual azoles (ketoconazole together with itraconazole and fluconazole) can significantly increase carbamazepine levels.

A similar effect is observed with isoniazid, grapefruit juice, loratadine with terfenadine, drugs that inhibit the action of viral protease, and propoxyphene. In such cases, it is necessary to change the portion size and monitor the plasma values of the drug.

A mutual increase or decrease in therapeutic parameters is observed when combined with felbamate.

Theophylline, valpromide and phenobarbital with clonazepam, as well as primidone, cisplatin, oxcarbazepine with valproic acid, methsuximide, doxorubicin with phenytoin, as well as rifampicin with phensuximid and some herbal medicines containing St. John's wort can lead to a decrease in carbamazepine levels.

The drug reduces plasma levels of alprazolam, haloperidol, cyclosporine with clobazam, tetracycline, primidone with clonazepam, valproic acid with ethosuximide, and orally administered drugs that contain progesterone with estrogen.

It has been determined that tetracyclines reduce the therapeutic activity of carbamazepine.

Administration in combination with paracetamol increases the likelihood of developing toxic effects on the liver, while at the same time weakening the drug's effect.

Combination with pimozide, haloperidol, maprotiline, phenothiazines and tricyclics, as well as with clozapine, thioxanthenes and molindone potentiates the suppressive effect on the nervous system, reducing the anticonvulsant effect of Finlepsin.

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Storage conditions

Finlepsin should be stored in a place inaccessible to small children, out of moisture and sunlight.

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Shelf life

Finlepsin is permitted to be used within a 36-month period from the date of release of the therapeutic substance for sale.

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Application for children

Children may require higher doses of the drug (because carbamazepine is eliminated faster in them). Finlepsin can be prescribed in pediatrics from the age of 5.

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Analogues

Analogues of the drug are Carbamazepine, Zagretol, Aktinerval, Stazepine with Carbalepsin retard, and in addition to this, Apo-Carbamazepine, Storilat, Mazepine with Zeptol, Tegretol, etc.

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Reviews

Finlepsin receives quite contradictory reviews from people who take it or have taken it. There are comments from people with epilepsy who say that the drug has a negative effect on mental abilities, causes communication disorders in society and apathy; but at the same time they confirm that its therapeutic effectiveness is very high - the drug helps to eliminate epileptic seizures.

There are also reviews of the use of the drug for panic attacks due to being in closed or open spaces. Therapy often helps eliminate panic, but there are also comments about not being able to get rid of unsteadiness in gait.

In general, Finlepsin is still considered one of the most popular anticonvulsants, which is effective in treating the disorders indicated in the indications. Doctors say that this drug is the most effective - you just need to strictly follow all the doctor's instructions regarding the dose of the drug and other conditions.

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