Universal reference book for medicines
Product name: REXETIN ® (REXETIN ® )

Active substance: paroxetine

Type: Antidepressant

Manufacturer: GEDEON RICHTER (Hungary)
Composition, form of production and packaging
Tablets covered with a film coat of white or almost white color, round, biconcave, with a risk on one side and engraved "X20" - on the other.
1 tab.
paroxetine hydrochloride hemihydrate 22.76 mg,
which corresponds to the content of paroxetine 20 mg
[PRING] hypromellose, calcium hydrophosphate dihydrate, carboxymethyl starch sodium, magnesium stearate.
Sheath composition: hypromellose, macrogol 400, macrogol 6000, polysorbate 80, titanium dioxide.
10 pieces. - blisters (3) - packs of cardboard.
The tablets covered with a film cover of white or almost white color, round, biconcave, with risk on one side and engraving "X30" - on another.
1 tab.
paroxetine hydrochloride hemihydrate 34.14 mg,
which corresponds to the content of paroxetine 30 mg
[PRING] hypromellose, calcium hydrophosphate dihydrate, carboxymethyl starch sodium, magnesium stearate.
Sheath composition: hypromellose, macrogol 400, macrogol 6000, polysorbate 80, titanium dioxide.
10 pieces. - blisters (3) - packs of cardboard.
INSTRUCTION FOR THE SPECIALIST.
Description of the drug approved by the manufacturer for the printed edition of 2011.
PHARMACHOLOGIC EFFECT
Antidepressant. Inhibits reverse neuronal seizure of serotonin in the central nervous system. Little affects the neuronal seizure of norepinephrine and dopamine. It also has anxiolytic and psychostimulating action.
PHARMACOKINETICS
Suction
After ingestion paroxetine is well absorbed from the digestive tract. Simultaneous food intake does not affect the absorption and pharmacokinetics of paroxetine.
Distribution
Paroxetine binds to plasma proteins by 93-95%. The equilibrium state is reached after 7-14 days after the start of therapy, further pharmacokinetics with prolonged therapy does not change.
Metabolism
Metabolized mainly in the liver with the formation of predominantly inactive metabolites.
Excretion
T 1/2 of paroxetine is in the range of 6 to 71 hours, but an average of 24 hours. About 64% of paroxetine is excreted in the urine (2% in unchanged form, 62% in the form of metabolites); approximately 36% is released through the intestine, mainly in the form of metabolites, less than 1% - unchanged with feces.
Pharmacokinetics in special clinical cases
The concentration of paroxetine in the blood plasma increases with the violation of the liver and kidneys, as well as in the elderly.
INDICATIONS
- Depression of various etiologies, incl. states accompanied by anxiety;
- obsessive-compulsive disorder (obsessive-compulsive disorder);
- panic disorder, incl. with fear of being in the crowd (agoraphobia);
- social phobia;
- generalized anxiety disorder (GAD);
- Post-traumatic stress disorders.
It is also used in the context of anti-relapse treatment.
DOSING MODE
Tablets should be taken 1 time / day, preferably in the morning, while eating, without chewing.
As with other antidepressants, depending on the clinical condition of the patient after 2-3 weeks of therapy, the dose of the drug can be changed.
With depression, the recommended daily dose is 20 mg. The effect in most cases develops gradually. In some patients, an increase in the dose of the drug is possible. The daily dose can be increased by 10 mg per week until the therapeutic effect is achieved; the maximum daily dose is 50 mg / day.
In obsessive-compulsive disorders ( obsessive-compulsive disorder ), the initial dose is 20 mg / day. The dose may be increased by 10 mg until a therapeutic response is obtained. The maximum daily dose is usually 40 mg, but should not exceed 60 mg.
In 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 of 10 mg per week to achieve the desired effect. 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 / 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 by 10 mg until the desired effect is achieved. The maximum daily dose should not exceed 50 mg. For maintenance therapy, the drug is used at a dose of 20 mg / day.
With a generalized anxiety disorder, the recommended therapeutic dose is 20 mg / day. Depending on the patient's response to therapy, the daily dose may be increased gradually by 10 mg per week; the maximum daily dose is 50 mg.
In 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 by 10 mg, the maximum daily dose is 50 mg.
Depending on the clinical condition of the patient, maintenance therapy is necessary to prevent the possibility of relapses . The course of maintenance therapy after the disappearance of symptoms of depression can be 4-6 months, and with obsessional and panic disorders and more. As with other psychotropic drugs, the drug should be abruptly discontinued.
In weakened patients and the elderly, the concentration of paroxetine in the blood serum can grow faster 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.
Children due to lack of clinical experience, the drug is not shown.
With renal (CC <30 ml / min) or liver failure , the concentration of paroxetine in the blood plasma increases, 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 EFFECT
Adverse reactions are presented with percentages of the revealed ratio of the total number of patients receiving this treatment.
From the digestive system: nausea (12%); sometimes - constipation, diarrhea, decreased appetite; rarely - increase in liver function tests; in some cases - a serious violation of liver function. Between the reception of paroxetine and changes in the activity of liver enzymes, a cause-and-effect relationship 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 and the peripheral nervous system: drowsiness (9%); tremor (8%); general weakness and increased fatigue (7%), insomnia (6%); in some cases - headache, increased irritability, paresthesia, dizziness, somnambulism, decreased concentration of attention; rarely - extrapyramidal disorders, orofacial dystonia. Extrapyramidal disorders are noted mainly with the previous intensive use of neuroleptics. Rarely observed epileptiform seizures (which is typical of other antidepressant therapy); increased intracranial pressure.
On the part of the autonomic nervous system: increased sweating (9%), dry mouth (7%).
From the side of the organ of vision: in some cases - visual impairment, mydriasis; rarely - an attack of acute glaucoma.
From the cardiovascular system: in some cases - tachycardia, ECG changes, lability of blood pressure, syncope.
On the part of the reproductive system: an ejaculation disorder (13%), in some cases - a change in libido.
From the urinary system: rarely - difficulty urinating.
From the side of water-electrolyte balance: in some cases - hyponatremia with the development of peripheral edema, a violation of consciousness or epileptiform symptomatology. 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 people who, in addition to paroxetine, received diuretics and other medications.
Allergic reactions: rarely - skin hyperemia, subcutaneous hemorrhage, edema in the face and limbs, anaphylactic reactions (urticaria, bronchospasm, angioedema), itchy skin.
Other: in isolated cases - myopathies, myalgia, myasthenia gravis, myoclonia, hyperglycemia; rarely - hyperprolactinaemia, galactorrhea, hypoglycemia, fever and development of influenza-like state, taste change. Rarely developed thrombocytopenia (cause-and-effect relationship with taking the drug is not proven). Paroxetine may be accompanied by an increase or decrease in body weight. Several cases of development of increased hemorrhage are described.
Paroxetine, in comparison with tricyclic antidepressants, less often causes dry mouth, constipation and drowsiness. Sudden abolition of the drug may cause dizziness, impaired sensation (eg, paresthesia), a sense of fear, sleep disturbance, agitation, tremor, nausea, increased sweating and confusion, so stopping therapy with the drug should be gradual (it is advisable to reduce dosages every second day).
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.
CONTRAINDICATIONS
- simultaneous administration of MAO inhibitors and a period of 14 days after their withdrawal;
- Pregnancy;
- lactation (breastfeeding);
- children and adolescence under 18 (due to lack of clinical experience);
- Hypersensitivity to the components of the drug.
Rexetin ® should not be used in combination with thioridazine because, like other drugs that inhibit the CYP2D6 isoenzyme, paroxetine can increase plasma levels of thioridazine. The administration of a single thioridazine can lead to an elongation of the QT interval on the ECG with concomitant severe ventricular arrhythmias, such as torsades de pointes (pirouette ventricular tachycardia), and cause sudden death.
With caution should apply the drug for violations of the cardiovascular system, liver failure, chronic kidney failure, prostatic hyperplasia, as well as in elderly patients.
Paroxetine should be used with caution in the presence of epilepsy in an anamnesis. According to clinical observations, paroxetine causes epileptiform seizures in 0.1% of patients. It is necessary to interrupt the course of treatment of patients who have developed similar disorders.
Paroxetine causes mydriasis, so if there is glaucoma, the drug should be used with caution.
When combined use of paroxetine with benzodiazepines (oxazepam), barbiturates, neuroleptics, data on the enhancement of the inherent sedative effect (drowsiness) was not observed. There is little experience sharing the use of paroxetine with neuroleptics, so in these cases, use the drug with caution.
Sufficient experience in the combined use of lithium with paroxetine or with other serotonin reuptake inhibitors has not yet been accumulated, so this combination should be used with caution, under regular control of lithium levels in the blood.
PREGNANCY AND LACTATION
The safety of paroxetine during pregnancy and during lactation has not been studied, so the drug should not be used during pregnancy and lactation, except when, from a medical point of view, the potential benefit of treatment exceeds the potential risk associated with taking the drug.
Women of childbearing age are recommended contraception during paroxetine therapy.
APPLICATION FOR FUNCTIONS OF THE LIVER
In renal (CC <30 ml / min) 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

APPLICATION FOR VIOLATIONS OF THE FUNCTION OF KIDNEYS
When 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

APPLICATION FOR CHILDREN
Contraindication: children and adolescence under 18 years (due to lack of clinical experience).
SPECIAL INSTRUCTIONS
Contraindicated taking paroxetine simultaneously with MAO inhibitors and within 14 days after their withdrawal. In the future, paroxetine should be used with extreme caution, starting a course of treatment with small doses and gradually increasing dosages until the desired therapeutic effect is achieved. After the end of paroxetine therapy for 14 days, treatment with MAO inhibitors should not be started.
If the patient was previously manic, during the reception of paroxetine, the possibility of relapse (as with other antidepressants) should be considered.
There is insufficient experience of simultaneous use of electroconvulsive therapy and paroxetine.
In connection with the predisposition to suicidal attempts in patients with depression and patients with drug abuse during the period of withdrawal, this category of patients requires careful monitoring during treatment.
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.
In some cases, against the background of paroxetine treatment, increased bleeding occurred (mainly ecchymosis and purpura).
Against the background of paroxetine, hyperglycemic conditions were rarely noted.
Suicide / Suicidal 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 shows that when treating with antidepressants, the risk of suicide may increase in the early stages of recovery.
Other psychiatric conditions for which Rexetin ® is administered 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 exhibiting 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. 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 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.
Impact on the ability to drive vehicles and manage mechanisms
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 that requires a quick response. The degree of restriction is determined individually.
OVERDOSE
Symptoms: Paroxetine therapy is safe in a wide range of doses. Signs of an overdose were manifested when using paroxetine at a dose of 2000 mg or more with other drugs or with alcohol: nausea, vomiting, tremor, pupil dilating, 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.
Treatment: gastric lavage, 20-30 g of activated carbon every 4-6 h for the first 24-48 h; it is necessary to release the airways, if necessary, to carry out oxygenation. Monitor the vital functions of the body and general measures aimed at their maintenance. It is recommended to constantly monitor cardiac and other vital functions. There is no specific antidote. Forced diuresis, hemodialysis or hemoperfusion are ineffective if a large dose of paroxetine comes from the blood in the tissue.
DRUG INTERACTION
Food and antacids do not affect the absorption and pharmacokinetics of paroxetine.
Like other serotonin reuptake inhibitors, undesirable interactions between MAO inhibitors and paroxetine have been observed in animal experiments.
The simultaneous use of paroxetine with tryptophan leads to the onset of headache, nausea, increased sweating and dizziness, therefore, this combination should be avoided.
Between paroxetine and warfarin is assumed pharmacodynamic interaction (with unchanged prothrombin time marked increased bleeding); The use of such a combination requires caution.
With the combined use of paroxetine with sumatriptan, general weakness, hyperreflexia, and coordination disorders are noted. If they need to be used together, special care should be taken (medical control is required).
With simultaneous use of paroxetine can inhibit the metabolism of tricyclic antidepressants (by inhibiting the isoenzyme CYP2D6), so the use of this combination requires caution and reduced doses of tricyclic antidepressants.
Drugs that enhance or inhibit the activity of the liver enzyme systems, can influence the metabolism and pharmacokinetics of paroxetine. When combined with inhibitors of hepatic metabolic enzymes necessary to use the lowest effective dose of paroxetine. Combined use with inducers of hepatic enzymes does not require correction of the initial dose of paroxetine; further change dosages depending on the clinical effect (efficacy and tolerability).
Paroxetine significantly inhibits isoenzyme CYP2D6. Therefore, special care requires the simultaneous use of paroxetine with drugs whose metabolism occurs with the participation of this isozyme, including with certain antidepressants (e.g., nortriptyline, amitriptyline, imipramine, desipramine and fluoxetine), phenothiazines (e.g., thioridazine), antiarrhythmics of class 1 C (e.g., propafenone, flecainide and encainide) or those drugs which inhibit its action (e.g. quinidine, cimetidine, codeine).
Reliable clinical data of paroxetine inhibiting CYP3A4 isozyme have therefore possible to use with drugs that inhibit this enzyme (e.g. terfenadine).
Cimetidine inhibits some isoenzymes of cytochrome P450. Consequently, when used in conjunction with cimetidine paroxetine paroxetine increases blood plasma at the stage of the equilibrium state.
Phenobarbital increases the activity of certain cytochrome P450 isoenzymes. In joint use of paroxetine with phenobarbital reduced concentration of paroxetine in blood plasma, and its shortened T 1/2 .
When the joint application of paroxetine and a paroxetine concentration of phenytoin decreases in plasma may increase and the incidence of side effects of phenytoin. When using other anticonvulsants may also increase the frequency of their side effects. In patients with epilepsy treated with long-term carbamazepine, phenytoin, or sodium valproate, the additional appointment of paroxetine did not cause changes in pharmacokinetic and pharmacodynamic properties of anticonvulsants; increasing paroxysmal seizure were noted.
Paroxetine is largely bound to plasma proteins. While the use of drugs that also bind to plasma proteins, accompanied by increased paroxetine concentrations in plasma may increase side effects.
Due to lack of sufficient clinical experience combined use of digoxin paroxetine purpose of this combination requires caution.
Diazepam with exchange application does not affect the farmakinetiku paroxetine.
Paroxetine significantly increases the concentration in blood plasma protsiklidina, so the appearance of anticholinergic side effects should be reduced dose protsiklidina.
In clinical trials of paroxetine did not affect the level of propranolol in the blood.
In some cases, there is an increased concentration of theophylline in the blood. Despite the fact that in the course of clinical studies, the interaction between paroxetine and theophylline is not proven, it is recommended regular monitoring of theophylline in the blood.
Potentiation of ethanol was not detected while the use of paroxetine. However, due to the effect of paroxetine on the enzyme system of the liver must be an exception drinking alcohol during treatment with paroxetine.
TERMS OF RELEASE FROM PHARMACY
The drug is released by prescription.
TERMS AND CONDITIONS OF STORAGE
The drug should be stored out of the reach of children at a temperature of 15 ° to 30 ° C. Shelf life - 5 years.
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