Expiration date: 05/2022
Release form and composition:
Tablets, film-coated white color, round, lenticular, film-coated, scored, with a rough surface.
Excipients: calcium hydrogen phosphate, cellulose microcrystalline, crospovidone, copovidone, silica colloidal anhydrous, magnesium stearate, talc.
The composition of the shell: hypromellose, macrogol 6000, talc, titanium dioxide.10 PCs. - blisters (3) - packs cardboard.
1 tablet contains:
paroxetine hydrochloride 22.76 hemihydrate the mg,
EMCO corresponds to the content of paroxetine 20 mg
Pharmacological action:Antidepressant. Is a selective reuptake inhibitor of serotonin (5-hydroxytryptamine, 5-HT) neurons in the brain, that determines its antidepressant action and effectiveness in treating obsessive-compulsive (OCD) and panic disorder.Paroxetine has a low affinity for m-cholinergic receptors (it has a weak anticholinergic effect), apha1-, apha2 and beta-adrenergic receptors and dopaminovykh (D2), 5HT1-like, 5HT2-like and histamine H1-receptors. Paroxetine does not violate the psychomotor function and potentiates the depressing action of ethanol.According to the study of behavior and EEG in paroxetine identifies weak trigger properties, when he is assigned to doses higher than those needed to inhibit capture of serotonin. Does not cause significant changes in blood pressure, heart rate and EEG.
Pharmacokinetics:Vsasavayasi intake of paroxetine is well absorbed from the gastrointestinal tract and undergoes first pass metabolism through the liver.Raspredelenie achieved through 7-14 days after the start of therapy. If you increase the dose and/or duration of treatment observed nonlinear dependence of pharmacokinetic parameters on dose.Paroxetine extensively distributed in the tissues, only 1% is present in plasma.Associated with a protein of 95%.Metabolicmetabolic in the liver to form inactive metabolites. Is an inhibitor of the isoenzyme CYP2D6.The main metabolites of paroxetine represent the polar and conjugated products of oxidation and methylation, which are rapidly eliminated from the body, have a weak pharmacological activity and do not affect its therapeutic action. The metabolism of paroxetine is not broken due to its effects of the selective serotonin uptake by neurons.Vvedeniem 64% of the paroxetine is excreted with urine (2% - unchanged, 64% - as metabolites) of approximately 36% is excreted in bile through the intestine, mainly in the form of metabolites, less 1% - unaltered.Excretion of metabolites of paroxetine biphasic, first as a result of first pass metabolism through the liver, and then it is controlled by systemic elimination. T1/2 of paroxetine varies, but the average is 24 h. Pharmacokinetics in special clinical locaconcentrated of paroxetine in plasma increases with abnormal liver function and kidney , as well as the elderly.
Indications: depression of all types, including reactive, severe endogenous depression and depression, accompanied by anxiety - obsessive-compulsive disorder (OCD)- panic disorder including with agoraphobia - social anxiety disorder/social phobia - generalised anxiety disorder.
The dosage:the Tablets should be taken orally, 1 time/day, in the morning, while eating, swallowing whole with water.Dose is selected individually during the first 2-3 weeks after initiation of therapy and subsequently corrected if necessary.
In depression the recommended dose is 20 mg 1 time/day. If necessary, gradually increase the dose to 10 mg/day, the maximum daily dose should not exceed 50 mg.
Probressive-compulsive disorders initial therapeutic dose is 20 mg/day, with subsequent weekly increase 10 mg. the recommended average therapeutic dose - 40 mg/day, if necessary dose can be increased to 60 mg/day.
Panic disorder initial dose - 10 mg/day (to reduce the possible risk of acute panic symptoms), with the subsequent weekly increase 10 mg. the Average therapeutic dose - 40 mg/day. The maximum dose of 50 mg/day.
When social anxiety disorder/sociophobia initial dose is 20 mg/day, with no effect for at least 2 weeks to increase doses up to 50 mg/day. The dose should be increased by 10 mg at intervals of at least weeks according to clinical effect.
In generalized anxiety disorders the initial therapeutic dose is 20 mg/day.
Renal and/or hepatic insufficiency the recommended dose is 20 mg/day.
For elderly patients the daily dose should not exceed 40 mg. To prevent development of the syndrome, discontinuation of the drug should be gradual.
CNS and peripheral nervous system: drowsiness, tremor, asthenia, insomnia, dizziness, fatigability, seizures, extrapyramidal disorders, serotonin syndrome, hallucinations, mania, confusion, agitation, anxiety, depersonalization, panic attacks, nervousness, amnesia, myoclonia.
From the sensory organs: impaired vision.
From the side of musculoskeletal system: arthralgia, myalgia, muscular weakness, myopathy.From the urinary system: urinary retention, frequent urination.
From the reproductive system: sexual dysfunction, including impotence and ejaculation disorders, hyperprolactinemia/galactorrhea, anorgasmia.
From the digestive system: decreased or increased appetite, change of taste, nausea, vomiting, dry mouth, constipation or diarrhea in some cases - hepatitis.
Of the cardiovascular system: orthostatic hypotension.
Allergic reactions: rash, urticaria, ecchymosis, pruritus, angioedema.
Other: increased sweating, rhinitis, hyponatremia, disorders of secretion of antidiuretic hormone.
- the simultaneous admission of MAO inhibitors and period 14 days after their cancellation - unstable epilepsy - pregnancy - lactation (breast-feeding)- child age - hypersensitivity to the drug.
With caution should designate product in liver failure, kidney failure, angle-closure glaucoma, prostatic hyperplasia, mania, pathology of the heart, epilepsy, convulsive States, while the appointment of the EIT, concurrent use of drugs that increase the risk of bleeding, presence of risk factors for increased bleeding, and diseases that increase the risk of bleeding.
Pregnancy and lactation:
The drug is contraindicated during pregnancy and lactation.
In order to avoid the development of neuroleptic malignant syndrome with caution should designate Paroxetine patients receiving neuroleptics.Treatment with Paroxetine administered 2 weeks after the MAO inhibitors.The elderly patients in patients receiving Paroxetine possible hyponatremia.In some cases, dose adjustment is simultaneously applied insulin and/or oral hypoglycemic drugs.In the development convulsing with Paroxetine treatment is stopped.At the first signs of mania should cancel therapy with Paroxetine.During the first few weeks of therapy with Paroxetine should be carefully monitored patient in connection with possible suicidal attempts.During therapy The paroxetine should refrain from drinking alcohol in connection with the strengthening of its toxic effect.
Use pediatritions of Paroxetine in children is not recommended because its safety and efficacy in this group of patients is not established.
Effects on ability to drive vehicles and management mehanizmami.nelia that paroxetine does not impair cognitive and psychomotor function, patients should refrain or exercise extreme caution when driving and occupation of other potentially hazardous activities, require high concentration and psychomotor speed reactions.
Symptoms: nausea, vomiting, tremor, mydriasis, dry mouth, irritability, nystagmus, agitation, sweating, drowsiness, sinus tachycardia, convulsion, bradycardia, increased blood pressure, nodal rhythm. In very rare cases, when administered simultaneously with other psychotropic drugs and/or alcohol may ECG changes, coma. In severe overdose - serotonin syndrome, rare - rhabdomyolysis.Treatment: gastric lavage, administration of activated charcoal. If necessary, symptomatic therapy. There is no specific antidote.
Concurrent administration of antacids does not affect the absorption and pharmacokinetic parameters of Paroxetine.Contraindicated concomitant use of Paroxetine with MAO inhibitors.When concomitant administration with Paroxetine increases the concentration of procyclidine.In connection with paroxetine inhibition of cytochrome P450 may increase the effect of barbiturates, fenitoina, indirect anticoagulants, tricyclic antidepressants, phenothiazine neuroleptics and antiarrhythmic drugs of class 1C, metoprolol and increase the risk of side effects while appointing these medicines.In concurrent use with drugs that inhibit liver enzymes, may require dose reduction Paroxetine.Paroxetine increases bleeding time against the background odnovremennogo receiving warfarin (with unchanged prothrombin time).When concomitant administration of Paroxetine with atypical neuroleptics, tricyclic antidepressants, drugs phenothiazine series, NSAIDs (incl. acetylsalicylic acid) may be in breach of process blood clotting.Co-administration of Paroxetine with serotonergic drugs (tramadol, sumatriptan) may lead to increased serotonergic effect.Marked mutual potentiation of tryptophan, drugs lithium and paroxetine.When concomitant administration of Paroxetine with phenytoin and other anticonvulsants may increase the incidence of side effects.Paroxetine is much weaker suppresses antihypertensive effects of guanetidin compared with antidepressants that inhibit norepinephrine capture.
Terms and conditions of storage:
The drug should be stored in a dry, dark, inaccessible to children place at temperature not exceeding 25°C. shelf Life - 3 years.