Rexetine, pills 20mg, 30pcs

Composition

1 coated tablet contains:

Active ingredient:

paroxetine hydrochloride hemihydrate 22.76 mg, which corresponds to the content of paroxetine 20 mg. ;

Auxiliary substances:

hypromellose-15 mg;

calcium hydrophosphate dihydrate-244.24 mg;

sodium carboxymethyl starch-15 mg;

magnesium stearate-3 mg

Film shell:

hypromellose-7.2 mg;

macrogol 400-0.07 mg; macrogol 6000-0.956 mg;

polysorbate 80-0.044 mg;

titanium dioxide-1.03 mg

Pharmacological action

Rexetine has an antidepressant effect.

Pharmacodynamics

Inhibits reverse neuronal uptake of serotonin in the central nervous system. It has little effect on neuronal uptake of norepinephrine and dopamine. It also has anxiolytic and psychostimulating properties.

Pharmacokinetics

After oral use, paroxetine is well absorbed. It is mainly metabolized in the liver, with the formation of mainly inactive metabolites. Simultaneous food intake does not affect the absorption and pharmacokinetics of paroxetine. Paroxetine binds to plasma proteins by 93-95%.

The half-life of paroxetine ranges from 6 to 71 hours, but on average is one day.

Dynamic equilibrium in blood plasma is reached 7-14 days after the start of therapy, and the pharmacokinetics do not change further with long-term therapy. Approximately 64% of paroxetine is excreted in the urine (2% unchanged,62% as metabolites); approximately 36% is excreted mainly as metabolites through the gastrointestinal tract, and less than 1% is excreted unchanged in the faeces. The concentration of paroxetine in the blood plasma increases with impaired liver and kidney function, as well as in the elderly.

Indications

• Depression of various etiologies, including conditions accompanied by anxiety;
• Obsessive-compulsive disorder (obsessive compulsive disorder).
• Panic disorders, including fear of being in a crowd (agoraphobia);
• Social phobia.
• Generalized anxiety disorder (GAD)
• Post-traumatic stress disorders.
• It is also used as part of anti-relapse treatment.

Use during pregnancy and lactation

The safety of using paroxetine during pregnancy has not been studied, so it should not be used during pregnancy and lactation, except in cases where from a medical point of view the potential benefit of treatment outweighs the possible risk associated with taking the drug.

If it is necessary to use the drug during lactation, the question of stopping breastfeeding should be decided.

During the period of use of the drug, women of childbearing age should avoid conception (use reliable methods of contraception).

Contraindications

• Hypersensitivity to the components of the drug in the anamnesis.
• Monoamine oxidase (MAO) inhibitor therapy and the period after discontinuation of treatment with MAO inhibitors for two weeks.
• Pregnancy and lactation. The safety of using paroxetine during pregnancy has not been studied, so it should not be used during pregnancy and lactation, except in cases where from a medical point of view the potential benefit of treatment outweighs the possible risk associated with taking the drug.
• Children under 18 years of age (due to lack of clinical experience).

Side effects

From the gastrointestinal tract, liver:  Nausea (12%); sometimes constipation, diarrhea, decreased appetite. Rarely increased hepatic function tests; sometimes severe hepatic impairment. There is no proven causal relationship between paroxetine intake and changes in liver enzyme activity, but discontinuation of paroxetine is recommended in cases of impaired liver function.

From the central nervous system:  Drowsiness (9%); tremor (8%); general weakness and fatigue (7%); insomnia (6%); in some cases, headache, increased irritability, paresthesia, dizziness, somnambulism. Extrapyramidal disorders and orophacial dystonia were rarely observed. Extrapyramidal disorders are noted mainly with the previous intensive use of neuroleptics. Epileptiform seizures were rarely observed, which is also typical for therapy with other antidepressants; increased intracranial pressure.

From the autonomic nervous system:  Increased sweating (9%), dry mouth (7%).

From the side of the senses:  In some cases, visual impairment, mydriasis are noted; rarely-an attack of acute glaucoma.

From the cardiovascular system:  In some cases, tachycardia, ECG changes, lability of blood pressure, fainting states are described.

From the genital area and urinary system:  Ejaculation disorder (13%), in some cases a change in libido, rarely difficulty urinating.

Electrolyte imbalance:  In some cases, hyponatremia with the development of peripheral edema, impaired consciousness or epileptiform symptoms was noted. After discontinuation of the drug, the level of sodium in the blood returns to normal. In some cases, this condition developed due to hyperproduction of antidiuretic hormone. Most of these cases were observed in elderly patients who received diuretics and other medications in addition to paroxetine.

Dermatological reactions and hypersensitivity reactions:  In rare cases, hyperemia of the skin, subcutaneous hemorrhage, edema in the face and extremities, anaphylactic reactions (urticaria, bronchospasm, angioedema), pruritus are described.

Other:  Isolated cases of myopathy, myalgia, hyperglycemia, rarely hyperprolactinemia, galactorrhea, hypoglycemia, fever and the development of a flu-like condition were noted. Rarely develops thrombocytopenia, but the causal relationship with taking the drug is not proven. Taking paroxetine may be accompanied by an increase or decrease in body weight. Several cases of increased bleeding have been described (See Warnings). Paroxetine is less likely to cause dry mouth, constipation, and drowsiness than tricyclic antidepressants. Sudden withdrawal of the drug can cause dizziness, sensitivity disorders (for example, paresthesia), a feeling of fear, sleep disturbance, agitation, tremor, nausea, increased sweating and confusion. Therefore, discontinuation of therapy with the drug should be carried out gradually, it is advisable to reduce the dosage every second day.

Interaction

Food and antacids do not affect the absorption and pharmacokinetics of paroxetine.

Similar to other serotonin reuptake inhibitors, an undesirable interaction between MAO inhibitors and paroxetine was observed in animal experiments.

Concomitant use of paroxetine with tryptophan leads to headache, nausea, increased sweating and dizziness, so the use of this combination should be avoided.

A pharmacodynamic interaction is expected between paroxetine and warfarin (with the prothrombin time unchanged, increased bleeding is noted); the use of such a combination requires caution.

When paroxetine is co-administered with sumatriptan, general weakness, hyperreflexia, and coordination disorders are noted. If it is necessary to use them simultaneously, special care should be taken (medical supervision is required).

When used concomitantly, paroxetine may inhibit the metabolism of tricyclic antidepressants (due to inhibition of the CYP2D6 isoenzyme), so the use of such a combination requires caution and a reduction in the dose of tricyclic antidepressants.

Drugs that enhance or inhibit the activity of liver enzyme systems may affect the metabolism and pharmacokinetics of paroxetine. When co-administered with liver metabolic enzyme inhibitors, the lowest effective dose of paroxetine should be used. Co-use with inducers of hepatic enzymes does not require correction of the initial dose of paroxetine; further dosage changes depend on the clinical effect (efficacy and tolerability).

Paroxetine significantly inhibits the activity of the CYP2D6 isoenzyme. Therefore, special care should be taken when using paroxetine concomitantly with drugs that are metabolized with the participation of this isoenzyme, including certain antidepressants (for example, nortriptyline, amitriptyline, imipramine, desipramine and fluoxetine), phenothiazines (for example, thioridazine), Class 1 C antiarrhythmic drugs (for example, propafenone, flecainide and encainide) or with those drugs that block its action (for example, quinidine, cimetidine, codeine).

There are no reliable clinical data on paroxetine inhibition of the CYP3A4 isoenzyme, so it can be used with drugs that inhibit this enzyme (for example, terfenadine).

Cimetidine inhibits some cytochrome P450 isoenzymes. As a result, the combined use of paroxetine with cimetidine increases the level of paroxetine in the blood plasma at the equilibrium stage.

Phenobarbital increases the activity of some cytochrome P450 isoenzymes. When paroxetine is co-administered with phenobarbital, the concentration of paroxetine in the blood plasma decreases, and its T1 / 2 is shortened.

When paroxetine and phenytoin are used together, the concentration of paroxetine in the blood plasma decreases and the frequency of side effects of phenytoin may increase. Other anticonvulsant medications may also increase the frequency of their side effects.In patients with epilepsy treated for a long time with carbamazepine, phenytoin or sodium valproate, additional use of paroxetine did not cause changes in the pharmacokinetic and pharmacodynamic properties of anticonvulsants; no increase in paroxysmal convulsive readiness was observed.

Paroxetine is largely bound to plasma proteins. When used concomitantly with drugs that also bind to plasma proteins, against the background of an increase in the concentration of paroxetine in blood plasma, side effects may increase.

Due to the lack of sufficient clinical experience with the combined use of digoxin with paroxetine, the appointment of such a combination requires caution.

Diazepam does not affect the pharmacinetics of paroxetine during the course of treatment.

Paroxetine significantly increases the concentration of procyclidine in blood plasma, so if anticholinergic side effects occur, it is necessary to reduce the dose of procyclidine.

In clinical trials, paroxetine did not affect the level of propranolol in the blood.

In some cases, an increase in the concentration of theophylline in the blood is noted. Although the interaction between paroxetine and theophylline has not been proven in clinical studies, regular monitoring of theophylline levels in the blood is recommended.

No increase in the effect of ethanol when used concomitantly with paroxetine was detected. However, due to the effect of paroxetine on the liver enzyme system, it is necessary to exclude the use of alcoholic beverages during treatment with paroxetine.

How to take, course of use and dosage

Inside,1 time a day, preferably in the morning, with meals, without chewing.

As with other antidepressants, depending on the patient’s clinical condition, the dosage of the drug can be changed after 2-3 weeks.

For depression: The recommended daily dose is 20 mg. As with the use of other antidepressants, the effect in most cases develops gradually. In some patients, it may be necessary to increase the dose of the drug. Depending on the patient’s response to therapy, the daily dose can be increased by 10 mg at intervals of 1 week, until a therapeutic effect is achieved; the maximum daily dose is 50 mg.

Obsessive-compulsive disorder (obsessive compulsive disorder): the initial dose is 20 mg / day. The dose can be increased by 10 mg weekly, until the required therapeutic response is achieved. The maximum daily dose is usually 40 mg, but should not exceed 60 mg.

For panic disorders: the recommended therapeutic dose is 40 mg / day. Therapy should be started with a small (10 mg/day) dose, with a weekly increase in dosages by 10 mg / day, until the desired effect is achieved. The maximum daily dose should not exceed 60 mg. The recommended low initial dose of the drug is due to the possibility of a temporary increase in the intensity of symptoms of the disease at the beginning of therapy.

For social phobias: therapy can be started with a dose of 20 mg / day. If after a 2-week course of treatment there is no significant improvement in the patient’s condition, the dose of the drug can be increased weekly by 10 mg until the desired effect is achieved. The maximum daily dose should not exceed 50 mg. For maintenance therapy, a daily dose of 20 mg is usually sufficient.

For generalized anxiety disorder: the recommended therapeutic dose is 20 mg / day. Depending on the patient’s response to therapy, the daily dose can be increased gradually by 10 mg; the maximum daily dose is 50 mg.

For post-traumatic stress disorders: the recommended therapeutic dose is 20 mg / day. Depending on the patient’s response to therapy, the daily dose can be increased periodically by 10 mg, the maximum daily dose is 50 mg.

Depending on the patient’s clinical condition, maintenance therapy is necessary to prevent possible relapses. This course after the disappearance of symptoms of depression can be 4-6 months, and for obsessive and panic disorders and more. As with other psychotropic medications, abrupt discontinuation of treatment should be avoided. In debilitated and elderly patients, the level of the drug in the blood serum may increase higher than usual, so the recommended initial dose is 10 mg / day. This dose can be increased by 10 mg weekly, depending on the patient’s condition.

The maximum dose should not exceed 40 mg / day.

The drug is not indicated for children due to lack of clinical experience.

With renal (Cl creatinine

Overdose

Symptoms: nausea, vomiting, tremor, dilated pupils, dry mouth, general agitation, increased sweating, drowsiness, dizziness, flushing of the facial skin. No comatose state or convulsions were observed. Fatal outcome was observed rarely, usually with simultaneous overdose of paroxetine and another drug, causing adverse interactions. Signs of overdose occur with simultaneous use of 2 g of paroxetine or when taking a large dose of paroxetine with other drugs or with alcohol. Paroxetine therapy is safe in a large dose range.

Treatment: gastric lavage,20-30 g of activated charcoal every 4-6 hours for the first 24-48 hours; the airways should be cleared, and oxygenation should be performed if necessary. Vital functions of the body are monitored and general measures are taken to maintain them. There is no specific antidote. Forced diuresis, hemodialysis, or hemoperfusion are ineffective if a large dose of paroxetine is delivered from the blood to the tissues.

Special instructions

It is contraindicated to take paroxetine simultaneously with MAO inhibitors and for 14 days after their withdrawal. In the future, paroxetine should be used with extreme caution, starting the course of treatment with small doses and gradually increasing the dosage until the desired therapeutic effect is achieved. After the end of paroxetine therapy, you should not start a course of treatment with MAO inhibitors for 14 days.

If the patient has previously been in a manic state, the possibility of relapse should be considered while taking paroxetine (as with other antidepressants).

There is insufficient experience with the simultaneous use of electroconvulsive therapy and paroxetine.

Due to the predisposition to suicide attempts in patients with depression and drug addiction during abstinence, this category of patients should be carefully monitored during treatment.

Hyponatremia has been reported in many cases, especially in elderly patients receiving diuretics. After the withdrawal of paroxetine, the level of sodium in the blood returns to normal.

In some cases, increased bleeding occurred during treatment with paroxetine (mainly ecchymosis and purpura).

Hyperglycemic conditions were rarely observed during the use of paroxetine.

Suicide/Suicidal thinking

Depression is associated with an increased risk of suicidal thoughts, autoaggression, and suicide. This risk persists until remission occurs. Since improvement may not occur within the first few weeks or more of starting treatment, patients should be carefully monitored until such improvement occurs. Existing clinical experience suggests that when treated with antidepressants, the risk of suicide may increase in the early stages of recovery.

Other psychiatric conditions for which Rexetin is prescribed may also be associated with an increased risk of suicidal behavior. In addition, these conditions can be concomitant with major depressive disorder. The same precautions as in the treatment of patients with major depressive disorder should be followed when it comes to the treatment of patients with other psychiatric disorders. Patients with a history of suicidal behavior or thoughts, or who demonstrate a significant degree of suicidal thinking prior to treatment, are at greater risk of suicidal thoughts or suicide attempts, and should be carefully monitored during treatment. Such patients aged 18-29 years have an increased risk of suicide, so treatment with the drug should be carefully monitored.

Patients (and those who care for patients) should be prepared for the need for monitoring in emergency situations – the appearance of suicidal intentions/behaviors or thoughts of auto-aggression, in order to seek medical help immediately if these symptoms are present.

Influence on the ability to drive motor vehicles and manage mechanisms

Controlled studies have not shown any negative effects of paroxetine on psychomotor or cognitive function. Despite this, at the beginning of the course of therapy, during an individually set period, you can not drive a car or work in conditions of increased danger that require quick reaction. The degree of restriction is determined individually.

Composition

Tablet Form of production

Storage conditions

At a temperature of 15-30 °C

Shelf life

5 years

Active ingredient

Paroxetine

Conditions of release from pharmacies

By prescription

Dosage form

Tablets

Purpose

For adults as directed by your doctor

Indications

Depression, Phobias and Panic Attacks, Mental disorders