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Rexetin (Paroxetinum, Paroxetine, Reksetin) - an antidepressant. Inhibits reverse neuronal uptake of serotonin in the central nervous system. Little effect on the neuronal uptake of norepinephrine and dopamine. It has also anxiolytic and psychoactive effect.
It is also used as part of anti-treatment.
Pregnancy and breast-feeding:
The safety of paroxetine during pregnancy has not been studied, so it should not be used during pregnancy and lactation, except when medically potential benefit of treatment exceeds potential risks associated with taking the drug.
If necessary, use during lactation should decide the issue of termination of breastfeeding.
During the period of preparation of women of childbearing age should avoid conception (use reliable methods of contraception).
Contraindications receiving paroxetine simultaneously with MAO inhibitors and within 14 days after their cancellation. In the future, paroxetine should be used with extreme caution, since treatment with small doses and gradually increasing the dosage to achieve the desired therapeutic effect. After treatment with paroxetine for 14 days, you can not start a course of treatment MAO inhibitors.
If the patient has previously been in a manic state, while taking paroxetine should be considered the possibility of occurrence of relapse (as when taking other antidepressants). In case of violation of the cardiovascular system of the drug should be used with caution.
Paroxetine should be used with caution in the presence of a history of epilepsy (and other antidepressants). According to clinical observations in 0.1% of patients, paroxetine causes epileptiform seizures. In this case it is necessary to interrupt the course of therapy. There is little experience of simultaneous use of ECT and paroxetine.
In connection with a predisposition to suicidal attempts in patients with depression and patients with drug addiction during abstinence for this group of patients should be closely monitored during treatment. In many cases, there is hyponatremia, especially in elderly patients receiving diuretics. After the abolition of paroxetine in blood sodium levels to normal. In some cases, during treatment with paroxetine occurred increased bleeding (mostly ecchymosis and purpura).
The drug is prescribed with caution in glaucoma, as paroxetine (and other selective serotonin reuptake inhibitors) cause mydriasis. Against the background of paroxetine rarely observed hyperglycemic state.
The tablets should be taken 1 time / day., Preferably in the morning, while eating, not chewing. As with other antidepressant therapy, depending on the clinical condition of the patient after 2-3 weeks of therapy, the dose can be changed.
In depression the recommended daily dose is 20 mg. The effect develops more gradually. Possible to increase the dose. The daily dose may be increased to 10 mg per week to achieve a therapeutic effect; The maximum daily dose is 50 mg / day.
With obsessive-compulsive disorder (obsessions syndrome) initial dose is 20 mg / day. The dose may be increased to 10 mg to achieve a therapeutic response. The maximum daily dose is usually 40 mg, but should not exceed 60 mg.
In panic disorder the recommended therapeutic dose is 40 mg / day. Therapy should be initiated with a small (10 mg / day.) Dose with a weekly increase of 10 mg per week until the desired effect. The maximum daily dose should not exceed 60 mg. The recommended initial dose is low due to the possibility of a temporary increase of the intensity of the symptoms at the start of therapy.
With social phobia therapy can be initiated with a dose of 20 mg / day. If after two weeks of treatment, no significant improvement in the condition of the patient, the dose can be increased by 10 mg weekly until the desired effect. The maximum daily dose should not exceed 50 mg. For maintenance medication therapy is used in a dose of 20 mg / day.
In generalized anxiety disorder, the recommended therapeutic dose is 20 mg / day. Depending on the patient's response to therapy daily dose can be gradually increased by 10 mg per week; the maximum daily dose - 50 mg.
In post-traumatic stress disorders, the recommended therapeutic dose is 20 mg / day. The daily dose may be increased to 10 mg / week, the maximum daily dose is 50 mg.
Depending on the clinical condition of the patient to prevent the possibility of recurrence is necessary supportive therapy. Course maintenance therapy after the disappearance of the symptoms of depression may reach 4-6 months, and for panic disorders and obsessive - more. As with other psychotropic drugs, to avoid abrupt withdrawal of the drug.
In debilitated patients, and the elderly in the serum concentration of paroxetine may increase faster than usual, so the recommended starting dose is 10 mg / day. This dose may be increased to 10 mg at intervals of 1 week according to the patient's condition. The maximum dose should not exceed 40 mg / day.
Adverse reactions are detected percent ratio of the total number of patients receiving this treatment.
From the digestive system: nausea (12%); sometimes - constipation, diarrhea, loss of appetite; rarely - increased rates of liver function tests; in some cases - severe liver dysfunction. Between taking paroxetine and the change has not been proven activity of liver enzymes, a causal relationship, but in the case of abnormal liver function is recommended discontinuation of paroxetine.
From the central and peripheral nervous system: somnolence (9%); tremor (8%); general weakness and fatigue (7%), insomnia (6%); in some cases - headache, irritability, paresthesia, dizziness, somnambulism, decreased concentration; rarely - extrapyramidal disorders, orofacial dystonia. Extrapyramidal disorder observed primarily during the previous intensive use of neuroleptics. Rarely observed epileptiform seizures (which is characteristic of other antidepressants and therapy); increased intracranial pressure.
Since the autonomic nervous system: sweating (9%), xerostomia (7%).
From a sight organ: in some cases - blurred vision, mydriasis; rarely - an attack of acute glaucoma.
Cardio-vascular system: in some cases - tachycardia, ECG changes, labile blood pressure, fainting.
From the reproductive system: ejaculation disorder (13%), in some cases - changes in libido.
From the urinary system: rarely - difficulty urinating.
From the water-electrolyte balance: in some cases - hyponatremia with the development of peripheral edema, impaired consciousness or epileptiform symptoms. After discontinuation of the drug in the blood level of sodium is normalized. In some cases, this condition develops as a result of overproduction of antidiuretic hormone. Most of these cases occurred in elderly persons who received diuretics and other medications in addition to paroxetine.
Allergic reactions: seldom - skin redness, bruising, swelling in the face and extremities, anaphylactic reactions (urticaria, bronchospasm, angioedema), itchy skin.
Other: in rare cases - myopathy, myalgia, myasthenia gravis, myoclonus, hyperglycemia; rarely - hyperprolactinemia, galactorrhea, hypoglycemia, fever and flu-like development of the state, a change of taste. Rarely has developed thrombocytopenia (causal relationship with the administration of the drug has not been proven). Paroxetine may be accompanied by an increase or decrease in body weight. Described several cases of increased bleeding.
Paroxetine compared with tricyclic antidepressants, rarely cause dry mouth, constipation and drowsiness. Sudden withdrawal of the drug may cause dizziness, sensory disturbances (eg, paresthesias), anxiety, sleep disturbances, agitation, tremor, nausea, sweating, and confusion, so the termination of drug therapy should be performed gradually (it is advisable to reduce the dosage every second day).
The incidence of side effects and intensity of treatment is reduced in the process, so their development in most cases possible to continue taking the drug.
Food and antacids do not affect the absorption and pharmacokinetics of paroxetine. Concomitant use of paroxetine with tryptophan leads to headache, nausea, sweating and dizziness. Between paroxetine and warfarin is expected pharmacodynamic interaction (with the unmodified prothrombin time marked by increased bleeding); the use of such combinations requires caution.
In a joint application with paroxetine sumatriptan there is a general weakness, hyperreflexia, incoordination. If necessary, they simultaneous application should take special care (medical supervision required). With simultaneous use of paroxetine and benzodiazepines (oxazepam), barbiturates, antipsychotics there were no gain sedation (sleepiness). Experience of the joint use of neuroleptics and paroxetine small, so this combination requires caution. With simultaneous use of paroxetine may inhibit the metabolism of tricyclic antidepressants (due to inhibition of isozyme CYP2D6), so the use of such a combination requires caution and reduce doses of tricyclic antidepressants.
Adequate experience simultaneous use of paroxetine and lithium drugs there, so the appointment of such a combination requires careful and regular monitoring of lithium levels in the blood. Drugs that enhance or inhibit the activity of the liver enzyme systems that can affect the metabolism and pharmacokinetics of paroxetine. In a joint application with inhibitors of liver metabolic enzymes necessary to use the lowest effective dose of paroxetine. The combined use of inducers of liver enzymes does not require correction of the initial dose of paroxetine; further change the dosage depends on the clinical effect (efficacy and tolerability).
Paroxetine significantly inhibits the activity of isozyme CYP2D6. Therefore, special care requires the simultaneous use of paroxetine with drugs whose metabolism occurs with the participation of isoenzyme, including with certain antidepressants (such as nortriptyline, amitriptyline, imipramine, desipramine and fluoxetine), phenothiazines (e.g., thioridazine), antiarrhythmics class 1C (e.g., propafenone, flecainide and encainide), or those drugs which inhibit its action (such as quinidine, cimetidine, codeine). No reliable clinical data on paroxetine inhibition of CYP3A4 is not.
In a joint application with cimetidine paroxetine paroxetine increases plasma level at the stage of equilibrium. In a joint application with phenobarbital paroxetine paroxetine reduced plasma concentration and shortened his T 1/2. When combined use of paroxetine and phenytoin decreases paroxetine plasma concentrations and possible increase in the frequency of side effects of phenytoin. When using other anticonvulsants may also increase the frequency of 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 the pharmacokinetic and pharmacodynamic properties of anticonvulsants; increasing paroxysmal seizure were noted.
With simultaneous use of paroxetine with drugs that are actively binding to plasma proteins, may increase side effects. Due to lack of sufficient clinical experience joint use of digoxin with paroxetine appointment of such a combination requires caution. Diazepam with exchange application does not affect the pharmacokinetics of paroxetine.
Paroxetine protsiklidina significantly increases the concentration in plasma, so the appearance of anticholinergic side effects should be reduced dose protsiklidina. In clinical trials of paroxetine is not influenced in blood levels of propranolol. In some cases, the observed increase in the concentration of theophylline in 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. Strengthening the action of ethanol have been identified while the use of paroxetine.
Symptoms include nausea, vomiting, tremors, dilated pupils, dry mouth, general excitement, sweating, drowsiness, dizziness, flushing of the skin. There was no coma or convulsions. The lethal outcome in this case was marked by rare, usually with simultaneous overdose of paroxetine and other drugs that cause adverse interactions. Symptoms of overdose appear at one-stage application of 2 g of paroxetine or receiving a large dose of paroxetine with other drugs or with alcohol. Treatment with paroxetine is safe in a wide range of doses.
Treatment: gastric lavage, 20-30 grams of activated charcoal every 4-6 hours during the first 24-48 hours; should free the airway, oxygenation hold if necessary. Monitor vital body functions and common activities aimed at maintaining them. No specific antidote. Forced diuresis, hemodialysis or hemoperfusion are ineffective if a large dose of paroxetine came from the blood into the tissues.
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