Fevarin pills 50mg, 15pcs

Composition

1 coated tablet contains:

Active ingredient:

fluvoxamine maleate-50 mg

excipients:

mannitol-152.0 mg,

corn starch-40.0 mg,

pregelatinized starch-6.0 mg,

sodium stearyl fumarate-1.8 mg,

colloidal silicon dioxide-0.8 mg

shell:

hypromellose – 4.1 mg,

macrogol 6000-1.5 mg,

talc-0.3 mg,

titanium dioxide (E 171) – 1.5 mg

Pharmacological action

Pharmacodynamics

The mechanism of action of Fevarin is associated with selective inhibition of serotonin reuptake by brain neurons and is characterized by a minimal effect on the noradrenergic system. Fevarin has a weak ability to bind to a-adrenergic, b-adrenergic, histaminergic, m – holinoreceptors, dopaminergic or serotonergic receptors.

Pharmacokinetics

Suction: After oral use, fluvoxamine is completely absorbed from the gastrointestinal tract. Maximum concentrations of the drug in the blood plasma are observed 3-8 hours after use. Absolute bioavailability is 53% after primary liver metabolism. Concomitant use of fluvoxamine with food does not affect the pharmacokinetics.

Distribution: The binding of fluvoxamine to plasma proteins is 80% (in vitro). The volume of distribution is 25 l / kg.

Metabolism: Fluvoxamine is primarily metabolized in the liver. Although cytochrome P450 2D6 isoenzyme is the main one in fluvoxamine metabolism, the concentration of the drug in blood plasma in individuals with reduced function of this isoenzyme is not much higher than in individuals with normal metabolism. The average plasma half-life, which is 13-15 hours for a single dose, slightly increases with repeated use (17-22 hours), and the equilibrium concentration in blood plasma is usually reached within 10-14 days. Fluvoxamine undergoes biotransformation in the liver (mainly by oxidative demethylation) to at least nine metabolites that are excreted through the kidneys.

The two main metabolites have insignificant pharmacological activity. Other metabolites are probably pharmacologically inactive. Fluvoxamine significantly inhibits cytochrome P 450 1 A 2, moderately inhibits cytochromes P 450 2 C and P 450 ZA 4, and slightly-cytochrome P 450 2D6. The pharmacokinetics of a single dose of fluvoxamine are linear. The steady-state concentration of fluvoxamine is higher than that of a single dose and disproportionately higher at higher daily doses.

Special patient groups:

The pharmacokinetics of fluvoxamine are similar in healthy people, the elderly, and patients with renal insufficiency. Fluvoxamine metabolism is reduced in patients with liver disease. Steady-state plasma concentrations of fluvoxamine are twice as high in children (aged 6-11 years) as in adolescents (aged 12-17 years). Concentrations of the drug in the blood plasma in adolescents are similar to those in adults.

Indications

Depression of various origins; obsessive-compulsive disorders.

Use during pregnancy and lactation

Data from a small number of observations do not indicate any adverse effects of fluvoxamine during pregnancy. To date, no other epidemiological data are available.

The potential risk to humans is unknown. The drug should be administered to pregnant women with caution.

There have been isolated cases of withdrawal symptoms in newborns following fluvoxamine use at the end of pregnancy.

Some newborns after exposure to selective serotonin reuptake inhibitors in the third trimester of pregnancy experienced difficulty feeding and / or breathing, convulsive disorders, unstable body temperature, hypoglycemia, tremor, muscle tone disorders, increased neuro-reflex excitability syndrome and continuous crying, which may require longer hospitalization. Fluvoxamine passes into breast milk. In this regard, the drug should not be used during lactation.

Contraindications

• hypersensitivity to fluvoxamine maleate or to one of the excipients that make up the drug;
• simultaneous use of tizanidine and MAO inhibitors.
• Treatment with fluvoxamine can be initiated 2 weeks after discontinuation of an irreversible MAO inhibitor or the day after taking a reversible MAO inhibitor. The time interval between discontinuation of fluvoxamine and initiation of therapy with any MAO inhibitor should be at least one week.

With caution:

• hepatic and renal insufficiency;
• convulsions in the anamnesis, epilepsy;
• elderly age;
• patients with a tendency to bleeding (thrombocytopenia);
• pregnancy.
• It is not recommended for the treatment of depression in children (there is no clinical experience).

Side effects

The most frequently observed symptom associated with the use of Fevarin is nausea, sometimes accompanied by vomiting. This side effect usually disappears in the first 2 weeks of treatment.

Some of the side effects observed in clinical trials were often associated with symptoms of depression, rather than with treatment with Fevarin.

Common: often (1-10%) – asthenia, headache, malaise.

From the cardiovascular system: often (1-10%) – palpitations, tachycardia; sometimes (less than 1%) — postural hypotension.

Gastrointestinal disorders: common (1-10%) — abdominal pain, anorexia, constipation, diarrhea, dry mouth, dyspepsia; rarely (less than 0.1%) — impaired liver function (increased liver transaminases).

From the central nervous system: often (1-10%) – nervousness, anxiety, agitation, dizziness, insomnia or drowsiness, tremor; sometimes (less than 1%) — ataxia, confusion, extrapyramidal disorders, hallucinations; rarely (less than 0.1%) — convulsions, manic syndrome.

Skin disorders: common (1-10%) – sweating; sometimes (less than 1%) — hypersensitivity skin reactions (rash, pruritus, angioedema); rarely (less than 0.1%) — photosensitization.

Musculoskeletal disorders: sometimes (less than 1%) – arthralgia, myalgia.

From the genital system: sometimes (less than 1%) – delayed ejaculation; rarely (less than 0.1%) — galactorrhea.

Others: rarely (less than 0.1%) — changes in body weight; serotonergic syndrome, a condition similar to neuroleptic malignant syndrome, hyponatremia and syndrome of insufficient secretion of antidiuretic hormone; very rarely-paresthesia, anorgasmia and taste distortion.

If you stop taking fluvoxamine, withdrawal symptoms may develop — dizziness, paresthesia, headache, nausea, anxiety (most of the symptoms are mild and stop on their own). When the drug is discontinued, a gradual dose reduction is recommended.

Hemorrhagic manifestations — ecchymosis, purpura, gastrointestinal bleeding.

Interaction

Fevarin should not be used in combination with MAO inhibitors.

Fluvoxamine is a potent cytochrome P450 1A2 inhibitor, and to a lesser extent, P450 2C and P450 3A4. Drugs that are largely metabolized by these isoenzymes are more slowly eliminated and may have higher plasma concentrations if co-administered with fluvoxamine. This is especially important for drugs that are characterized by a small breadth of therapeutic action. Patients need to be closely monitored, and dose adjustments are recommended if necessary.

Fluvoxamine has minimal inhibitory effect on cytochrome P450 2D6 and probably does not affect non-oxidative metabolism and renal excretion.

Cytochrome P450 1A2. When Fevarin was co-administered, there was an increase in previously stable levels of tricyclic antidepressants (clomipramine, imipramine, amitriptyline) and neuroleptics (clozapine, olanzapine), which are largely metabolized by cytochromes P450 1A2. In this regard, it may be recommended to reduce the dose of these drugs.

Patients taking fluvoxamine concomitantly with drugs that are characterized by a low therapeutic range and are metabolized by cytochrome P450 1A2 (such as tacrine, theophylline, methadone, mexiletine) should be closely monitored. If necessary, adjust the dosage of these drugs.

When used in combination with warfarin, there was a significant increase in the concentration of warfarin in blood plasma and prolongation of PV.

Isolated cases of cardiotoxicity have been reported when fluvoxamine is co-administered with thioridazine.

In studies of Fevarin interactions, an increase in propranolol concentrations after Fevarin use was noted. In this regard, we can recommend reducing the dose of propranolol in the case of additional use of Fevarin.

While taking fluvoxamine, the level of caffeine in the plasma may increase. Therefore, when consuming large amounts of caffeinated beverages and experiencing adverse effects of caffeine such as tremors, palpitations, nausea, anxiety, and insomnia, it is necessary to reduce your caffeine intake while taking fluvoxamine.

Concomitant use of fluvoxamine and ropinirole may increase the concentration of the latter in plasma, thus increasing the risk of overdose. In such cases, it is recommended to monitor the dosage of ropinirole or reduce it during treatment with fluvoxamine.

Cytochrome P450 2C. Patients taking fluvoxamine concomitantly with drugs that are characterized by a small therapeutic range and are metabolized by cytochrome P450 2C (phenytoin) should be carefully monitored, and dosage adjustments are recommended for these drugs.

Patients taking fluvoxamine concomitantly with drugs that are characterized by a small therapeutic range and are metabolized by cytochrome P450 3A4 (such as carbamazepine, cyclosporine) should be carefully monitored, and dosage adjustments of these drugs are recommended.

Couse with fluvoxamine of oxidative-metabolizing benzodiazepines such as triazolam, midazolam, alprazolam and diazepam may increase their plasma concentrations. The dosage of these benzodiazepines should be reduced while taking fluvoxamine.

Glucuronidation. Fluvoxamine does not affect the concentration of digoxin in plasma.

Renal excretion. Fluvoxamine does not affect the concentration of atenolol in plasma.

Pharmacodynamic reactions. In the case of combined use of fluvoxamine with serotonergic drugs (triptans, serotonin reuptake inhibitors), tramadol, the serotonergic effects of fluvoxamine may increase.

Fluvoxamine is used with lithium preparations for the treatment of severe patients who do not respond well to pharmacotherapy. Lithium and possibly tryptophan enhance the serotonergic effects of Fevarin and therefore treatment with this combination should be carried out with caution.

Concomitant use of oral anticoagulants and fluvoxamine may increase the risk of hemorrhage. Such patients should be under the supervision of a doctor.

How to take, course of use and dosage

Inside, without chewing and with a small amount of water.

Depression. The recommended starting dose is 50 or 100 mg (once, in the evening). It is recommended to gradually increase the starting dose to the effective level. The effective daily dose, usually 100 mg, is selected individually, depending on the patient’s response to treatment. The daily dose can reach 300 mg. Daily doses of more than 150 mg should be divided into several doses. According to official WHO guidelines, antidepressant treatment should be continued for at least 6 months of remission after a depressive episode. To prevent relapses of depression, it is recommended to take 100 mg of Fevarin 1 time a day.

Obsessive-compulsive disorders. It is recommended to start with a dose of 50 mg of Fevarin per day for 3-4 days. The effective daily dose is usually between 100 and 300 mg. Doses should be increased gradually until the effective daily dose is reached, which should not exceed 300 mg in adults. Doses up to 150 mg can be taken as a single dose, preferably in the evening. Daily doses of more than 150 mg are recommended to be divided into 2 or 3 doses.

Doses for children over 8 years of age and adolescents: initial-25 mg / day for 1 dose, maintenance-50-200 mg/day. The daily dose should not exceed 200 mg. Daily doses of more than 100 mg are recommended to be divided into 2 or 3 doses.

With a good response to the drug, treatment can be continued in an individually selected daily dose. If no improvement is achieved after 10 weeks of treatment, fluvoxamine should be discontinued. So far, no systematic studies have been conducted that could answer the question of how long fluvoxamine treatment can last, but obsessive-compulsive disorders are chronic, and therefore it is advisable to extend treatment with Fevarin for up to 10 weeks in patients who responded well to this drug. The selection of the minimum effective maintenance dose should be carried out with caution on an individual basis. Some clinicians recommend concomitant psychotherapy in patients who have responded well to pharmacotherapy.

Treatment of patients suffering from hepatic or renal insufficiency should begin with the lowest doses under strict medical supervision.

Due to the lack of clinical experience, Fevarin is not recommended for the treatment of depression in children.

Overdose

Symptoms: The most common symptoms include gastrointestinal disorders (nausea, vomiting, and diarrhea), drowsiness, and dizziness. In addition, there are reports of cardiac disorders (tachycardia, bradycardia, hypotension), liver function disorders, convulsions and coma. Treatment: There is no specific antidote for fluvoxamine. In case of overdose, gastric lavage is recommended, which should be carried out as early as possible after taking the drug, as well as symptomatic treatment. In addition, it is recommended to repeatedly take activated carbon, if necessary, the appointment of osmotic laxatives. Forced diuresis or dialysis is not effective.

Description

White coated tablets, round, biconvex, with a risk on one side, with the inscription “291” on both sides of the risk on one side of the tablet, and the letter “S” above the ∇ icon on the other side of the tablet.

Special instructions

Alcohol consumption is not recommended during treatment with the drug.

In patients with depression, there is usually a high probability of suicide attempt, which may persist until sufficient remission is achieved. Such patients should be monitored.

Treatment of patients suffering from hepatic or renal insufficiency should begin with the minimum effective doses of Fevarin under strict medical supervision. In rare cases, treatment with Fevarin may lead to an increase in the level of hepatic transaminases, most often accompanied by appropriate clinical symptoms. In these cases, Fevarin should be discontinued.

Blood glucose control may be compromised, especially in the early stages of treatment. You may need to adjust the dosage of antidiabetic medications.

Caution should be exercised when prescribing the drug to patients with a history of seizures. Fevarin should be avoided in patients with unstable epilepsy, and patients with stable epilepsy should be under strict medical supervision. Treatment with Fevarin should be discontinued if epileptic seizures develop or increase in frequency.

Rare cases of serotonergic syndrome or a condition similar to neuroleptic malignant syndrome, which may be associated with taking fluvoxamine, in combination with other serotonergic antidepressants and neuroleptics, have been described. Since these syndromes can lead to potentially life — threatening conditions such as hyperthermia, muscle rigidity, myoclonus, lability of the autonomic nervous system with possible rapid changes in vital parameters, changes in mental status, including increased irritability, agitation, confusion, delirious disorders and coma, treatment with fluvoxamine should be discontinued. If necessary, appropriate treatment should be initiated.

As with the use of other selective serotonin reuptake inhibitors, in rare cases, hyponatremia may occur while taking fluvoxamine, which is reversed after discontinuation of the drug. Some cases were caused by the syndrome of insufficient secretion of antidiuretic hormone. Most of these cases were observed in elderly patients.

Intradermal hemorrhages such as ecchymosis and purpura, as well as hemorrhagic events (such as gastrointestinal bleeding), have been reported with the use of selective serotonin reuptake inhibitors. Caution should be exercised when prescribing these drugs in elderly patients and patients receiving concomitant medications that affect platelet function (atypical antipsychotics and phenothiazines, many tricyclic antidepressants, aspirin, NSAIDs) or drugs that increase the risk of bleeding, as well as in patients with a history of bleeding and prone to bleeding (for example, patients with thrombocytopenia).

When combined with fluvoxamine, the concentration of terfenadine, astemizole or cisapride in the blood plasma may increase, increasing the risk of prolongation of the QT interval. Therefore, fluvoxamine should not be administered with these medications.

Data obtained in the treatment of elderly patients and younger patients indicate that there are no clinically significant differences between the daily doses usually used in them. However, increasing the dose of the drug in elderly patients should always be carried out more slowly and with more caution. Fevarin may lead to a slight decrease in heart rate (by 2-6 beats per minute).

Due to the lack of clinical experience, Fevarin is not recommended for the treatment of depression in children.

Fevarin, given to healthy volunteers in doses up to 150 mg, did not affect or had a slight effect on the ability to drive a car or drive cars. At the same time, there are reports of drowsiness observed during treatment with the drug. In this regard, caution is recommended until the final determination of the individual response to the drug.

Form of production

Film-coated tablets

Storage conditions

Store in a dry place, protected from direct sunlight, at a temperature not exceeding 20 °C.

Shelf life

1 year

Active ingredient

Fluvoxamine

Conditions of release from pharmacies

By prescription

Dosage form

Tablets

Purpose

For adults as prescribed by a doctor, For Pregnant women as prescribed by a doctor, For adults

Indications

Manic-depressive Psychosis, Obsessive-compulsive disorder, Depression