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Instructions for use REXETIN®

Treatment with Rexetine® should be started with caution 2 weeks after stopping the use of irreversible MAO inhibitors, or 24 hours after stopping the reversible MAO inhibitor. The dose of paroxetine should be gradually increased until optimal effect is achieved.

Suicide/suicidal ideation or clinical worsening

Depression is associated with an increased risk of suicidal ideation, self-harm and suicide (suicidal acts and behavior). This risk persists until significant remission occurs. Since improvement may not occur for the first few weeks or more of use, patients should be under medical supervision until improvement occurs. Accumulated clinical experience suggests that the risk of suicide may increase in the early stages of recovery.

Other psychiatric disorders for which paroxetine is intended to treat may also be associated with an increased risk of suicidal behavior and behavior. In addition, these conditions may co-occur with major depressive disorder. The precautions that were observed in the treatment of patients with major depressive disorder should also be observed in the treatment of patients with other mental disorders.

Patients with a history of suicidal behavior or behavior or predominant suicidal ideation prior to treatment are known to be at significant risk for suicidal ideation or suicide attempts and should be closely monitored during treatment. A meta-analysis of placebo-controlled clinical trials of antidepressants in adult patients with mental disorders demonstrated an increased risk of suicidal behavior with antidepressants compared with placebo in patients <25 years of age.

Drug treatment, especially in the early stages and after dose changes, should be accompanied by careful monitoring of patients, especially high-risk patients. Patients (and their caregivers) should be prepared to monitor for any sudden clinical deterioration, suicidal behavior or thoughts, and unusual changes in behavior. If these symptoms appear, you should consult a doctor immediately.

Akathisia/psychomotor agitation

Paroxetine has been associated with the development of akathisia, which is characterized by an internal feeling of restlessness and psychomotor restlessness, such as the inability to sit or stand quietly, and which is usually associated with a subjective feeling of discomfort. The risk of developing akathisia is highest in the first few weeks of treatment. In patients with these symptoms, the condition may worsen as the dose is increased.

Serotonin syndrome/NMS

In rare cases, serotonin syndrome or NMS may occur when paroxetine is taken, especially in combination with serotonergic and/or antipsychotic drugs. Because these syndromes can be potentially life-threatening, treatment with paroxetine should be discontinued if these signs (characterized by a group of symptoms such as pyrexia, stupor, myoclonus, autonomic nervous system disturbance with possible sudden fluctuations in vital signs, mental status changes including confusion) are present , irritability, extreme agitation progressing to delirium and coma) and supportive symptomatic therapy was started. Paroxetine should not be used in combination with serotonin precursors (such as L-tryptophan, oxytriptan) due to the risk of serotonin syndrome.

Mania

As with other antidepressants, paroxetine should be used with caution in patients with a history of manic episodes. Paroxetine should be discontinued in all patients experiencing acute manic episodes.

Kidney/liver failure

Caution should be exercised when using paroxetine in patients with severe renal or hepatic impairment.

Diabetes

In patients with diabetes, treatment with selective serotonin reuptake inhibitors (SSRIs) should be accompanied by glycemic control. Doses of insulin and/or oral hypoglycemic agents may need to be revised.

Epilepsy

Like all antidepressants, paroxetine should be used with caution in patients with epilepsy.

Convulsions

The incidence of seizures is less than 0.1% in patients taking paroxetine. If seizures occur, the drug should be discontinued by all patients.

Electroconvulsive therapy

There is insufficient clinical experience with the use of paroxetine in electroconvulsive therapy.

Glaucoma

Like other SSRIs, paroxetine can cause mydriasis and should be used with caution in patients with acute-angle glaucoma or a history of glaucoma.

Cardiac disorders

Patients with cardiac disorders should take the usual precautions.

Hyponatremia

Hyponatremia is rare, mainly in elderly patients. The drug should be prescribed with caution to patients at risk of hyponatremia, for example, with concomitant drug therapy and cirrhosis. Hyponatremia usually resolves completely when paroxetine is stopped.

Bleeding

There is evidence of skin hemorrhages, such as ecchymosis and purpura, with SSRIs. Other hemorrhagic manifestations, such as gastrointestinal bleeding, have also been observed. Elderly patients are at increased risk.

SSRIs should be used with caution concomitantly with oral anticoagulants, drugs that affect platelet function, or with other drugs that may increase the risk of bleeding (for example, atypical antipsychotics such as clozapine, phenothiazines, most tricyclic antidepressants, acetylsalicylic acid, NSAIDs , COX-2 inhibitors), as well as in patients with bleeding episodes or conditions predisposing to bleeding.

Interaction with tamoxifen

Some studies have shown that the effectiveness of tamoxifen, as measured by the risk of recurrence/mortality from breast cancer, may be reduced when used concomitantly with paroxetine as a result of paroxetine's irreversible inhibition of the CYP2D6 isoenzyme. The concomitant use of paroxetine and tamoxifen used to treat or prevent breast cancer should be avoided if possible.

Withdrawal syndrome when stopping paroxetine

Withdrawal syndrome when stopping paroxetine is common, especially if patients stop taking the drug abruptly. Clinical studies found that 30% of patients experienced side effects when stopping paroxetine, compared with 20% of patients who experienced side effects when stopping placebo. The occurrence of withdrawal symptoms does not prove that the drug is addictive or addictive. The risk of withdrawal symptoms may depend on several factors, such as the duration of treatment, dose size, and rate of dose reduction.

Dizziness, sensory disturbances (including paresthesia, electric shock sensation, ringing in the ears), sleep disturbances (including intense dreams), agitation or restlessness, nausea, tremors, confusion, sweating, headache, diarrhea, rapid heartbeat, emotional instability, irritability and visual impairment. In general, these symptoms are mild to moderate, but may be severe in some patients. Symptoms usually occur within the first few days after stopping the drug, and very rarely in patients who accidentally missed taking the drug. Most symptoms go away on their own within 2 weeks, although in some patients they may last longer (2-3 months or more). Therefore, when stopping the drug, it is recommended to gradually reduce the dose over several weeks or months, according to the individual characteristics of the patient.

Alcohol

Although paroxetine does not exacerbate alcohol-induced psychomotor depression, as with other psychotropic drugs, concomitant use of Rexetine and alcohol should be avoided.

Use in pediatrics

Paroxetine should not be prescribed to children and adolescents under 18 years of age.

Suicidal behavior (suicide attempt and suicidal ideation) and hostility (primarily aggression, resistance, anger) were most frequently observed in clinical studies in children and adolescents treated with paroxetine compared with placebo. If a decision to prescribe a drug based on clinical need is made, the patient should be carefully monitored for the presence of suicidal symptoms. In addition, there is insufficient data from long-term studies on the safety of the drug in children and adolescents with regard to their growth, puberty, behavior, and cognitive development.

Impact on the ability to drive vehicles and operate machinery

Clinical studies have not revealed a negative effect of the drug Rexetine® on cognitive and psychomotor function. Despite this, as with other psychoactive drugs, patients should exercise caution in assessing their ability to drive or work in environments where there is an increased risk of injury.

Experimental results

Toxicological studies

were carried out on rhesus monkeys and albino rats. The metabolism of the drug in both groups of animals was similar to that in humans. Lipophilic amines, including tricyclic antidepressants, were hypothesized to induce phospholipidosis in rats. A one-year study of phospholipidosis found that the dose used was 6 times the recommended clinical dose range.

Carcinogenicity:

A two-year study of paroxetine did not show a carcinogenic effect of paroxetine.

Genetic toxicity:

no genetic toxicity was detected in in vivo and in vitro tests.

Reproductive toxicity:
Results from experiments in rats indicate that paroxetine affects the fertility of males and females. In rats, neonatal mortality was increased and ossification was delayed. Late effects were mostly related to maternal toxicity and did not have a direct effect on the fetus/newborn.

Overdose of the drug Rexetine, symptoms and treatment

Paroxetine therapy is safe over a wide range of doses. Overdose symptoms have occurred with a single dose of 2000 mg or with high doses of paroxetine in combination with other drugs or alcohol. Signs of overdose - nausea, vomiting, tremor, mydriasis, feeling of dryness in the mouth, agitation, sweating, drowsiness, dizziness, flushing of the facial skin; convulsions or coma did not develop. Death occurred only with a simultaneous overdose of paroxetine and another drug as a result of an adverse interaction. There is no specific antidote. In case of overdose, it is necessary to ensure airway patency, if necessary, oxygen therapy, perform gastric lavage or induce vomiting, and prescribe 20–30 g of activated carbon orally every 4–6 hours in the first 2 days. Continuous monitoring of vital signs is recommended. Forced diuresis, hemodialysis or hemoperfusion are ineffective if most of the paroxetine has already been transferred from the blood to the tissues.

Drug interactions Rexetine

After completing a course of treatment with a MAO inhibitor, paroxetine therapy should be started cautiously, with low initial doses, gradually increasing the dose until the optimal effect is achieved. After completing the course of treatment with Rexetine, MAO inhibitors should not be prescribed for 2 weeks. Simultaneous administration of drugs or the absence of the required period of time between their use threatens the development of serotonergic reactions (nausea, vomiting, diarrhea, convulsions, tremor, hyperreflexia, impaired coordination of movements, profuse sweating, skin flushing, increased blood pressure, lethargy, drowsiness), which can sometimes be significantly expressed and lead to death. Neuroleptic malignant syndrome-like events have been reported rarely. When tryptophan and paroxetine are used simultaneously, headache, nausea, increased sweating, and dizziness are possible, so this combination should be avoided. There may be a pharmacodynamic interaction between paroxetine and warfarin (increased bleeding with unchanged prothrombin time), so paroxetine should be prescribed with caution to patients taking oral anticoagulants. In some cases of simultaneous use with sumatriptan, weakness, hyperreflexia, and coordination problems were noted. When using this combination, medical supervision is required. Undesirable interactions with tricyclic antidepressants are typical for all serotonin reuptake inhibitors. Since paroxetine can also inhibit the metabolism of tricyclic antidepressants via cytochrome P450 IID6, the dose of the latter should be reduced . Use with caution in combination with antipsychotics (extrapyramidal disorders are possible). When used simultaneously with lithium salts, regularly monitor the level of lithium in the blood serum. Inducers or inhibitors of liver microsomal enzymes may affect the pharmacokinetics of paroxetine. Like other antidepressants that are metabolized by cytochrome P450 IID6, paroxetine inhibits the activity of this enzyme. Therefore, it should be used with caution with drugs metabolized by this isoenzyme: some antidepressants (for example, nortriptyline, amitriptyline, imipramine, desipramine and fluoxetine), phenothiazines (for example, thioridazine), class Ic antiarrhythmic drugs (for example, propafenone, flecainide and encainide ), as well as quinidine, cimetidine, codeine. Cimetidine inhibits some cytochrome P450 isoenzymes. As a result, with simultaneous use, the concentration of paroxetine in the blood plasma increases. Phenobarbital increases the activity of some cytochrome P450 isoenzymes. When used in combination, the plasma concentration of paroxetine is reduced and the half-life is shortened. With simultaneous use of paroxetine and phenytoin, the concentration of paroxetine in the blood plasma decreases, and side effects may increase. When using other antiepileptic drugs, clinical side effects may also increase. Paroxetine is highly bound to plasma proteins. When used simultaneously with drugs that also bind to plasma proteins, it is possible to increase the concentration of paroxetine and increase the severity of side effects. Paroxetine increases the concentration of procyclidine in the blood plasma, therefore, if anticholinergic side effects occur, it is necessary to reduce the dose of procyclidine. An increase in the concentration of theophylline in the blood is possible, therefore it is recommended to regularly monitor the concentration of theophylline in the blood serum when used simultaneously with paroxetine. An increase in the effect of alcohol on the central nervous system when used simultaneously with paroxetine was not detected, however, due to the effect of paroxetine on liver enzyme systems, it is necessary to avoid drinking alcohol during treatment with this drug.

Side effects of the drug Rexetine

The incidence and severity of side effects during therapy are reduced, so in most cases they do not require discontinuation of the drug. From the digestive tract: nausea (12%), sometimes - constipation, diarrhea, anorexia, rarely - increased liver function tests, extremely rarely - severe liver dysfunction. A cause-and-effect relationship between paroxetine and liver damage has not been proven, however, in case of liver dysfunction, it is recommended to discontinue use of paroxetine. From the side of the central nervous system : drowsiness (9%), tremor (8%), general weakness and increased fatigue (7%), insomnia (6%), in some cases - headache, increased irritability, paresthesia, confusion, somnambulism, rarely - extrapyramidal disorders and orofacial dystonia. Extrapyramidal disorders are noted mainly in cases where movement disorders are a symptom of an underlying disease, or with previous intensive use of antipsychotics. Epileptiform seizures, which are also common with other antidepressants, have been reported rarely. From the autonomic nervous system : sweating (9%), feeling of dryness in the mouth (7%). From the senses : in some cases - visual impairment, mydriasis, attacks of acute glaucoma. From the cardiovascular system: in some cases - tachycardia, ECG changes, vasodilation, blood pressure changes, fainting. From the genitourinary system: ejaculation disorders (13%), in some cases - other manifestations of sexual dysfunction, rarely - difficulty urinating. Electrolyte disturbances: hyponatremia with the development of edema, impaired consciousness or epileptiform symptoms was sometimes noted. After discontinuation of the drug, the level of sodium in the blood serum normalizes. In some cases, this condition developed due to overproduction of antidiuretic hormone. Most of these cases were observed in elderly patients who, in addition to paroxetine, received diuretics and other drugs. Dermatological reactions and hypersensitivity reactions: isolated cases of skin hyperemia, subcutaneous hemorrhages, swelling of the face and extremities, anaphylactic reactions (urticaria, bronchospasm, angioedema), itching have been described. Other: myopathy, myalgia, hyperglycemia, galactorrhea, hypoglycemia, fever and the development of influenza-like conditions were sometimes noted. Extremely rarely - thrombocytopenia; a cause-and-effect relationship with taking the drug has not been proven. Several cases of increased bleeding have been described. Taking paroxetine may be accompanied by an increase or decrease in body weight. Paroxetine is less likely to cause dry mouth, constipation, and drowsiness than tricyclic antidepressants. Sudden withdrawal of the drug can cause dizziness, sensory disturbances (paresthesia), a feeling of fear, sleep disturbances, agitation, tremor, nausea, sweating and confusion, so the drug should be discontinued gradually, and it is advisable to reduce the dose every other day.

Pharmacological properties of the drug Rexetine

Paroxetine is a selective 5-hydroxytryptamine (serotonin) reuptake inhibitor. The mechanism of therapeutic action of paroxetine for depression, obsessive compulsive disorders, and panic disorders is based on inhibition of neuronal reuptake of serotonin. The chemical structure of paroxetine differs from tricyclic, tetracyclic and other antidepressants. After oral administration, paroxetine is well absorbed and undergoes first-pass metabolism. Absolute bioavailability due to saturation of primary metabolic pathways varies. Simultaneous administration with food does not affect the pharmacokinetics of the drug. When taken regularly at a dose of 20 mg/day, the concentration in the blood plasma is 12–90 ng/ml (average 41 ng/ml), and the time to reach maximum concentration is 3–7 hours (average 5 hours). Paroxetine is extensively distributed in body tissues, including central nervous system tissues (average volume of distribution is 10–20 l/kg body weight, only 1% of the drug remains in the blood plasma). At blood concentrations ranging from 100 to 400 ng/ml, about 93–95% of paroxetine is bound to plasma proteins. Metabolized mainly in the liver. The main metabolites are polarized and associated products of oxidation and methylation. The predominant forms are those associated with glucuronic acid or the sulfate group. The pharmacological activity of the main metabolite is about 1/50 of the activity of the parent compound. The metabolism of paroxetine is associated with the cytochrome P450 IID6 system. In some individuals, due to a genetic defect, the activity of this isoenzyme may be reduced. The nonlinearity of the pharmacokinetics of paroxetine is due to the saturation of the cytochrome P450 IID6 enzyme system. The half-life of paroxetine ranges from 6 to 71 hours, with an average of 1 day. Equilibrium concentration in the blood plasma is achieved 7–14 days after the start of therapy; subsequently, the pharmacokinetics do not change with prolonged therapy. About 64% of paroxetine is excreted in the urine (2% unchanged, 62% as metabolites); approximately 36% - with feces (bile), mainly in the form of metabolites, ≤1% - with feces unchanged.