Rexetin - instructions for use, dose, side effects, contraindications

Paroxetine hydrochloride hemihydrate 22.76 mg (equivalent to 20 mg of paroxetine). Excipients: hypromellose, calcium hydrophosphate dihydrate, carboxymethyl starch sodium, magnesium stearate.

Shell composition: hypromellose, macrogol 400, macrogol 6000, polysorbate 80, titanium dioxide.

One Rexetin 30 mg film coated tablet contains: Active substance:

Paroxetine hydrochloride hemihydrate 34.14 mg (equivalent to 30 mg of paroxetine). Excipients: hypromellose ,. calcium hydrogen phosphate dihydrate, carboxymethyl starch sodium, magnesium stearate.

Shell composition: hypromellose, macrogol 400, macrogol 6000, polysorbate 80, titanium dioxide.

Description:

Tablets 20 mg - White or almost white round biconvex tablets, covered with a film membrane. With a risk on one side, and with engraving X20 - another.

Tablets 30 mg - White or almost white round biconvex tablets, covered with a film membrane. With a risk on one side, and with engraving CHO - another.

Pharmacotherapeutic group:antidepressant.

ATX: & nbsp

N.06.A.B Selective serotonin reuptake inhibitors

N.06.A.B.05 Paroxetine

Pharmacodynamics:

Inhibits in the central nervous system an inverse neuronal seizure of serotonin. Little affects the neuronal seizure of norepinephrine and dopamine. It also has an anxiolytic and psychostimulating property.

Pharmacokinetics:

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

The half-life of paroxetine is in the range from 6 up to 71 hours, but an average of one day. Dynamic equilibrium in the blood plasma is achieved 7-14 days after the initiation of therapy, further pharmacokinetics with prolonged therapy does not change. Approximately 64% of paroxetine is excreted in the urine (2 % in unchanged form, 62% in the form of metabolites); about 36% is released through the gastrointestinal tract mainly in the form of metabolites, less 1 % is excreted with feces unchanged.

The concentration of paroxetine in the blood plasma increases with a violation of the liver and kidneys, as well as in old age.

Indications:

Use strictly according to the doctor's prescription to avoid complications!

- Depression of different etiology, incl. states accompanied by anxiety;

- Obsessive-compulsive disorder (obsessive-compulsive disorder);

- Panic disorders, including fear of being in a crowd (agoraphobia);

- Sociophobia;

- Generalized anxiety disorder;

- Post-traumatic stress disorders.

- It is also used in the context of anti-relapse treatment.

Contraindications:

- Hypersensitivity to the components of the drug in the anamnesis.

- Therapy with monoamine oxidase inhibitors (MAO) and the period after discontinuation of treatment MAO inhibitors for two weeks.

- Pregnancy and lactation. Safety of paroxetine for. of pregnancy not studied, so it should not be used during pregnancy and lactation, behind except in cases where, from a medical point of view, the potential benefit of treatment exceeds the possible risk associated with taking the drug.

- Children under 18 years of age (due to lack of clinical experience).

Rexetin should not be used in combination with thioridazine, because, like other drugs that inhibit hepatic isoenzyme CYP2D6, paroxetine can also increase plasma levels of thioridazine (see section Interactions with other drugs and other forms of interaction). The administration of a single thioridazine may result in lengthening of the interval QT on an ECG with concomitant severe ventricular arrhythmias, such as torsades de pointes (pirouette ventricular tachycardia), and cause sudden death.

Carefully:

Carefully should apply the drug for violations of the cardiovascular system, hepatic failure, chronic renal disease deficiency, prostatic hyperplasia, as well as in old age.

Like other antidepressants, paroxetine should be used with caution when presence of epilepsy in the anamnesis. According to clinical

observations, paroxetine the 0,1 % of patients causes epileptiform seizures. It is necessary to interrupt the course of treatment of patients who have developed similar disorders!

Like other selective serotonin reuptake inhibitors (SSRI), paroxetine causes mydriasis, so if there is glaucoma, the drug should be used with caution.

When paroxetine is used together with benzodiazepines (oxazepam), barbiturates, antipsychotics data on the enhancement of the inherent sedative effect (drowsiness) was not observed. There is little experience of the joint use of paroxetine with neuroleptics, so in these cases, the drug should be used with caution (See: Side effects: extrapyramidal disorders}.

Sufficient experience in the combined use of lithium with paroxetine or with other serotonin reuptake inhibitors has not yet been accumulated, so it should be used with caution, under regular control of lithium levels in the blood.

Pregnancy and lactation:

Dosing and Administration:

- Rexetin should be taken once a day, preferably in the morning, while eating, without chewing.

- As with other antidepressant medications, depending on the clinical condition of the patient after two to three weeks, the dosage of the drug can be changed.

With depression the recommended daily dose is 20 mg. As with the use of other antidepressants, the effect in most cases develops gradually. Some patients may need to increase the dose of the drug. Depending on the response of the patient to therapy, the daily dose can be increased by 10 mg with an interval of one week, until the therapeutic effect is achieved; the maximum daily dose is 50 mg.

In obsessive-compulsive disorders (obsessive-compulsive disorder), the initial dose is 20 mg per day. The dose may be increased by GO mg weekly, until the required therapeutic response is achieved. The maximum daily dose is usually 40 mg, but should not exceed 60 mg.

In panic disorders the recommended therapeutic dose is 40 mg per day. Therapy should be started with a small dose (10 mg / day), with a weekly increase in dosages for 10 mg per 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 the symptoms of the disease at the beginning of therapy.

With social phobia Therapy can be started with a dose of 20 mg per day. If after a two-week course of treatment there is no significant improvement in the patient's condition, the dose of the drug can be increased weekly to 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.

With generalized anxiety disorder: The recommended therapeutic dose is 20 mg per day. Depending on the response of the patient to therapy, the daily dose can be increased gradually by 10 mg; the maximum daily dose is 50 mg.

With post-traumatic stress disorders: Recommended The therapeutic dose is 20 mg per 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 clinical condition of the patient, to prevent the possibility of relapses, it is necessary to carry out maintenance therapy. This course after the disappearance of the symptoms of depression can be 4-6 months, and with obsessional and panic disorders and more. As with the use of other psychotropic drugs, sudden termination of the course of treatment should be avoided. (Cm.: Side effects)

Weakened and elderly patients may rise above the usual level of the drug in the serum, so the recommended initial dose is 10 mg per day. This dose can be increased by 10 mg weekly, depending on the patient's condition.

The maximum dose should not exceed 40 mg per day.

Children due to lack of clinical experience, the drug is not shown.

In renal (creatinine clearance <30 ml per minute) or liver failure increases the concentration of paroxetine in the blood plasma, so the recommended daily dose of the drug in these cases is 20 mg.This dose can be increased depending on the patient's condition, but it is necessary to strive to maintain the dose at the lowest possible level.

Side effects:

- The frequency of manifestation and the intensity of side effects in the therapy process is reduced, so when they develop in most cases it is possible to continue taking the drug.

- Side effects on organs and systems (in percent of the revealed ratio of the total number of patients receiving this treatment);

- From the digestive tract, liver: Nausea (12%); sometimes constipation, diarrhea, decreased appetite. Rarely increased hepatic functional tests; sometimes severe dysfunction of the liver. Between the reception of paroxetine and changes in the activity of liver enzymes, causality has not been proven, but in the event of a violation of liver function, it is recommended that paroxetine be discontinued.

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

- From the side of the autonomic nervous system: increased sweating (9%), dry mouth (7%).

- From the sense organs: In some cases, visual impairment, mydriasis; rarely - an attack of acute glaucoma.

- From the cardiovascular system: B 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 a difficulty urinating.

- Violation of the electrolyte balance: In some cases, it is marked hyponatremia with the development of peripheral edema, a violation of consciousness or epileptiform symptoms. After drug cancellation, the sodium level in the blood is normalized.In some cases, this condition developed due to hyperproduction of antidiuretic hormone. The majority of such cases were observed in elderly patients who, in addition to paroxetine, received diuretics and other medications.

- Dermatological reactions and hypersensitivity reactions:

In rare cases, skin hyperemia, subcutaneous hemorrhage, edema in the face and limbs, anaphylactic reactions (urticaria, bronchospasm, angioedema), itchy skin.

- Others: In isolated cases, myopathy, myalgia, myasthenia gravis, myoclonia, hyperglycemia, rarely hyperprolactinemia, galactorrhea, hypoglycemia, temperature increase and development of influenza-like condition, taste change.

Rarely, thrombocytopenia develops, but the cause-and-effect relationship with taking the drug has not been proven. Paroxetine may be accompanied by an increase or decrease in body weight. Several cases of increased bleeding have been described. Warnings).

- Paroxetine, in comparison with tricyclic antidepressants, less often causes dry mouth, constipation and drowsiness.Sudden abolition of the drug may cause dizziness, impaired sensitivity (eg, paresthesia), a sense of fear, sleep disturbance, agitation, tremor, nausea, increased sweating and confusion, so stop the therapy with the drug gradually, it is advisable to reduce dosage every second day.

Overdose:

Paroxetine therapy is safe in a wide range of doses. Signs of an overdose were manifested in a one-stage application 2000 mg paroxetine, or when taking a large dose of paroxetine with other drugs, or with alcohol. Signs of an overdose: nausea, vomiting, tremor, pupil dilated, dry mouth, general arousal, increased sweating, drowsiness, dizziness, redness of the facial skin. No coma or convulsions were noted. The fatal outcome was rarely observed, usually with a simultaneous overdose of paroxetine and another drug that causes adverse interactions. There is no specific antidote. In case of overdose, it is necessary to ensure the release of the respiratory tract, if necessary, oxigenization, gastric lavage or vomiting, giving 20-30 g of activated carbon every 4-6 hours during the first 24-48 hours.It is recommended to constantly monitor cardiac and other vital functions. Forced diuresis, hemodialysis or hemoperfusion are not very effective, if a large dose of paroxetine comes from the blood in the tissue.

Interaction:

Food, antacids: Food and antacids do not affect absorption and pharmacokinetics of paroxetine.

MAO inhibitors: Like other serotonin reuptake inhibitors, an undesirable interaction between MAO inhibitors and paroxetine has been observed in animal experiments (See: Special instructions).

Tryptophan: In patients with the simultaneous use of tryptophan and paroxetine, headache, nausea, increased sweating and dizziness were noted, so joint use of paroxetine and tryptophan should be avoided.

Warfarin: Between paroxetine and warfarin is expected pharmacodynamic interaction (with unchanged prothrombin time marked increased bleeding). therefore paroxetine it is necessary to appoint with special caution to patients taking oral anticoagulants.

Sumatriptan: In a few cases of joint use general weakness, hyperreflexia, and coordination disorders were noted. If it is necessary to simultaneously use sumatriptan and a serotonin reuptake inhibitor, the latter must be performed under strict medical supervision.

Tricyclic antidepressants (TCAs): As with the joint use of other serotonin reuptake inhibitors with TCA preparations, caution is necessary, since paroxetine can inhibit the metabolism of TCAs, carried out with the participation of isoenzyme (CYP) IID₆. Therefore, the dose of TCA should be reduced. (Cm.: Joint application with preparations, inducing and inhibiting the metabolic enzyme system) Joint use with drugs inducing and inhibiting the metabolic enzyme system:

Drugs that increase or inhibit the activity of enzymes in the liver systems can affect the metabolism and pharmacokinetics of paroxetine. When combined with inhibitors of liver metabolic enzymes, the lowest effective dose of paroxetine should be used. A joint application with inducers of hepatic enzymes does not require correction of the initial dose of paroxetine; further changes in dosage depend on the clinical effect (efficacy and tolerability).

Drugs metabolized by isoenzyme CYP 2D6.

Paroxetine significantly inhibits the activity of this enzyme. Therefore, special care requires its simultaneous use with drugs, the metabolism of which occurs with the participation of this isoenzyme, including: some antidepressants (for example, nortriptyline, amitriptyline, imipramine, desipramine and fluoxetine), phenothiazines (e.g., thioridazine), antiarrhythmic drugs of the group 1C (eg, propafenone, flecainide and enkinide), or which block its action (for example, quinidine, cimetidine, codeine).

Drugs metabolized by isoenzyme CYP FOR4:

Reliable clinical data on paroxetine inhibition of isoenzyme CYP No 4, therefore, with drugs that inhibit this enzyme (eg, terfenadine), it can probably be used without problems.

Cimetidine: Cimetidine inhibits some isoenzymes of cytochrome P450. Because of this, when combined, the level of paroxetine concentration in the blood plasma increases at the stage of dynamic equilibrium.

Phenobarbital: Phenobarbital increases the activity of some cytochrome P isoenzymes450. When combined, the concentration of paroxetine in the blood plasma decreases, and the half-life is shortened.

Anticonvulsant drugs (Phenytoin): With the combined use of paroxetine and phenytoin, the concentration of paroxetine in the blood plasma decreases, but an increase in the frequency of side effects of phenytoin is possible. When using other anticonvulsants, the frequency of their side effects may also increase. In patients with epilepsy, treated for a long time with carbamazepine, phenytoin, or sodium valproate, the additional administration of paroxetine did not cause changes in the pharmacokinetic and pharmacodynamic properties of anticonvulsants; increased paroxysmal convulsive readiness was not noted.

Drugs that bind to plasma proteins:

Paroxetine is largely associated with blood plasma proteins. With simultaneous use with drugs that also bind to plasma proteins, against the background of increased concentrations of paroxetine in the blood plasma may increase the side effects.

Digoxin: Since there is not sufficient clinical experience for joint application, caution is advised when they are used simultaneously.

Diazepam: Diazepam with course use does not affect the pharmacokinetics of paroxetine.

Procyclidine: Paroxetine significantly increases the concentration of pro-cyclidine in the blood plasma, therefore, when anticholinergic side effects appear, it is necessary to reduce the dose of procyclidine.

Beta-blockers: In clinical trials paroxetine did not affect level of propranolol in the blood.

Theophylline: In some cases, increased the concentration of theophylline in the blood. Despite the fact that during clinical trials the interaction between paroxetine and theophylline is not proven, regular monitoring of the level of theophylline in the blood is recommended.

Alcohol: The increase in the effect of alcohol with simultaneous use with paroxetine was not revealed. However, due to the effect of paroxetine on the enzyme system of the liver, it is necessary to exclude the use of alcoholic beverages during treatment with paroxetine.

Special instructions:

1. Contraindicated taking paroxetine simultaneously with MAO inhibitors and within two weeks after their withdrawal.Further, paroxetine should be used with extreme caution, starting a course of treatment with small doses and gradually increasing dosages to achieve the desired therapeutic effect. After the end of paroxetine therapy for two weeks, treatment with MAO inhibitors should not be started.

2. The presence of a manic condition in the history: As with the reception other antidepressants, if the patient was previously in a manic state, during the reception of paroxetine, the possibility of relapse should be taken into account.

3. Electroconvulsive therapy (ECT): There is not enough experience concurrent use of ECT and paroxetine therapy.

4. In connection with the predisposition to suicide attempts in patients with depression and patients with drug abuse in withdrawal, in the treatment of this category of patients need careful monitoring.

5. Hyponatremia: In many cases, hyponatremia has been noted, especially in elderly patients who receive diuretics. After the withdrawal of paroxetine, the level of sodium in the blood is normalized.

6. Increased bleeding: In some cases, paroxetine treatment resulted in bleeding (mainly ecchymosis and purpura).

7. Rarely were there hyperglycemic conditions during the adoption of paroxetine.

Suiyid / Suiidal thinking

Depression is associated with an increased risk of suicidal thoughts, autoaggression and suicide. This risk persists until a remission occurs. Because the improvement may not occur within the first few weeks or more from the start of treatment, patients should be carefully monitored until such an improvement occurs. The current clinical experience indicates that when treating 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 associated with a major depressive disorder. The same precautions as for the treatment of patients with major depressive disorder should be observed when it comes to treating patients with other psychiatric disorders. Patients with an anamnesis of suicidal behavior or thoughts, or demonstrating a significant degree of suicidal thinking before starting treatment,are at greater risk of suicidal thoughts or suicide attempts, and should be carefully observed during treatment.

In such patients aged 18-29 years there is an increased risk of suicide, so treatment with the drug should be carefully monitored.

Patients (and those who provide care to patients) should be prepared for the need for monitoring in emergencies - suicidal intent / behavior or thoughts about autoaggression, in order to seek medical help immediately if these symptoms are present.

Edit Warnings

Women of childbearing age are recommended contraception during paroxetine therapy.

Effect on the ability to drive transp. cf. and fur:Controlled studies have not revealed a negative effect of paroxetine on the psychomotor or cognitive function. Despite this, at the beginning of the course of therapy, for an individually defined period, you can not drive a car or work in an environment of increased danger requiring quick reaction. The degree of restriction is determined individually.

Form release / dosage:

20 mg or 30 mg of paroxetine (as paroxetine hydrochloride hemihydrate) in each film-coated tablet. 10 tablets in a blister pack of AL / PVC. 3 blisters with instructions for use in a cardboard bundle.

Packaging:(1) - polyethylene double-layered bags (1) - polypropylene boxes
(10) - packings of cellular contour - boxes made of cardboard
(10) - packings, cellular, outline (3) - packs, cardboard

Storage conditions:

Store at a temperature of 15-30 ° C.

Keep the drug in a place inaccessible to children!

Shelf life:

5 years.

Use the product only with the expiration date printed on the package.

Terms of leave from pharmacies:On prescription

Registration number:П N015052 / 01

Date of registration:01.10.2008

The owner of the registration certificate:GEDEON RICHTER, OJSC GEDEON RICHTER, OJSC Hungary

Manufacturer: & nbsp

GEDEON RICHTER-RUS, CJSC Russia

Representation: & nbspGEDEON RICHTER OJSC GEDEON RICHTER OJSC Hungary

Information update date: & nbsp21.08.2015

Illustrated instructions

Instructions

Rexetin® (Rexetin®)