Composition, structure and packing
Tablets, film-coated white or almost white, round, biconvex, with risks on both sides and the side of risk, with the inscription "P" on one side and "20" - on the other.
1 tab. paroxetine hydrochloride 22.22 mg, which corresponds to the content of paroxetine 20 mg.
Excipients: magnesium stearate, karboksimetilkrahmal sodium (sodium starch glycolate), mannitol DC, microcrystalline cellulose, polymethacrylates, Opadry white AMB (aqueous solution), polyvinyl alcohol (partially hydrolyzed), titanium dioxide (E171), talc, soya lecithin (E322) , Gum Xanthan (E415); Opadry AMB blue (aqueous solution): alcohol polyvinyl (partially hydrolyzed), titanium dioxide (E171), talc, lecithin soya (E322), Gum Xanthan (E415); FD & C blue-indigo carmine lake (E132 ), FD & C yellow-6/sunset yellow lake (E110), Qunoline yellow lake (E104).
Tablets, film-coated blue, round, biconvex, with risks on the one side and the inscription "P30" - on the other.
1 tab. paroxetine hydrochloride 33.33 mg, which corresponds to the content of paroxetine 30 mg.
Excipients: magnesium stearate, karboksimetilkrahmal sodium (sodium starch glycolate), mannitol DC, microcrystalline cellulose, polymethacrylates, Opadry white AMB (aqueous solution), polyvinyl alcohol (partially hydrolyzed), titanium dioxide (E171), talc, soya lecithin (E322) , Gum Xanthan (E415); Opadry AMB blue (aqueous solution): alcohol polyvinyl (partially hydrolyzed), titanium dioxide (E171), talc, lecithin soya (E322), Gum Xanthan (E415); FD & C blue-indigo carmine lake (E132 ), FD & C yellow lake (E110), Qunoline yellow lake (E104). 10 pcs. - Blisters (3) - packs cardboard. Clinico-pharmacological group: Antidepressants. Mechanism of action of antidepressants.
Paroxetine is a potent and selective inhibitor of serotonin (5-hydroxytryptamine, 5-HT) neurons of the brain that determines its antidepressant action and effectiveness in the treatment of obsessive-compulsive and panic disorder. The main metabolites of paroxetine are polar and conjugated products of oxidation and methylation, which are rapidly cleared from the body, have weak pharmacological activity and not affect the therapeutic effect.
When the metabolism of paroxetine is not disturbed due to the operation of selective serotonin neurons. Paroxetine has low affinity to m-cholinergic receptors. With a selective action, in contrast to tricyclic antidepressants, paroxetine has a low affinity to α1, α2, β-adrenoceptors, as well as dopamine, 5-HT1 like, 5-HT2 and histamine H1 like-receptors.
Paroxetine does not affect psychomotor function and potentiates the inhibitory effect of ethanol on them. According to the study of behavior and EEG in patients taking paroxetine, it is proved that the appointment at doses higher than those required for inhibition of serotonin, paroxetine at the weak-activating properties. In healthy volunteers it causes no significant change in the level of blood pressure, heart rate and EEG. Unlike antidepressants, which inhibit the capture of norepinephrine, paroxetine is much weaker inhibits the antihypertensive effect guanetidina.
Pharmacokinetics
Absorption
After oral administration of paroxetine is well absorbed from the gastrointestinal tract. Treated metabolism during "first pass" through the liver. Clinical effects of paroxetine (side-effects and efficacy) did not correlate with its concentration in plasma.
Distribution
Css achieved for 7-14 days after initiation of treatment, pharmacokinetics during prolonged treatment does not change. At therapeutic concentrations of paroxetine binding to plasma proteins is 95%. Paroxetine is extensively distributed in tissues, and pharmacokinetic calculations indicate that only 1% of it is present in the plasma.
Metabolism
Because the metabolism of paroxetine includes "first passage" through the liver, its amount, as determined in the systemic circulation is less than that which is absorbed from the gastrointestinal tract. With increasing doses of paroxetine or multiple dosing, which increases the load on the body, has been partially reduced the effect of "first pass" through the liver and reduced plasma clearance of paroxetine. As a result, may increase the concentration of paroxetine in plasma and variations of pharmacokinetic parameters that can be observed only in those patients in whom the drug in low doses are reached low concentrations of paroxetine in plasma.
Withdrawal
T1 / 2 varies, but usually is about 1 day. Withdrawal from the body of metabolites of paroxetine biphasic, initially as a result of metabolism during first passage through the liver, then it is controlled by systemic elimination. Paroxetine appears mainly in the form of metabolites: 64% of metabolites excreted in urine and 36% of the bile through the intestines. In the unaltered output of 2% in the urine and 1% bile.
Pharmacokinetics in special clinical situations
In elderly patients, as well as in patients with renal and hepatic insufficiency of severe degree, the concentration of paroxetine in plasma increased, and the range of plasma concentrations had almost coincides with the range in healthy adult volunteers.
Statement
depression of all types (incl. reactive, severe endogenous depression and depression accompanied by anxiety);
obsessive-compulsive disorder;
panic disorder, including with agoraphobia;
social anxiety disorder / social phobia;
generalized anxiety disorder;
treatment of posttraumatic stress disorder.
Dosage regimen
Drugs are taken by mouth 1 time per day, morning, during a meal. Swallow the tablet whole, washed down with water. The dose selected individually for the first 2-3 weeks after initiation of therapy and subsequently, if necessary, corrected.
For the treatment of depression prescribed drug in a dose of 20 mg 1 time per day. If necessary, gradually increase the dose of 10 mg / day, maximum daily dose - 50 mg.
In obsessive-compulsive disorders initial therapeutic dose is 20 mg / day, followed by a weekly increase of 10 mg.
The recommended average therapeutic dose - 40 mg / day, if necessary, the dose may be increased to 60 mg / day.
In panic disorder Aktaparoksetin appointed at the initial dose of 10 mg / day (to reduce the possible risk of exacerbation of panic symptoms), followed by a weekly increase of 10 mg. The average therapeutic dose - 40 mg / day. The maximum dose - 50 mg / day.
When social anxiety disorder / social phobia initial dose is 20 mg / day, with no effect for at least 2 weeks may increase the dose to a maximum of 50 mg / day.
The dose should be increased to 10 mg at intervals of not less than 1 week in accordance with the clinical effect.
In post-traumatic mental disorder for the majority of patients starting and therapeutic dose is 20 mg / day. In some cases, we recommend increasing the dose to a maximum of 50 mg / day.
The dose should be increased to 10 mg per week according to the clinical effect.
When generalized anxiety disorder and recommended starting dose - 20 mg / day.
In renal and / or hepatic insufficiency the recommended daily dose is 20 mg.
For elderly patients daily dose should not exceed 40 mg. In order to prevent the development of withdrawal symptoms on discontinuing treatment is carried out gradually.
The use of paroxetine in children is not recommended because of its safety and efficacy in this patient is not installed.
Side effect
From the CNS: drowsiness, tremor, asthenia, insomnia, dizziness, fatigue, cramps, ekstrapiramidiye disorders, serotonin syndrome, hallucinations, mania, confusion, agitation, anxiety, depersonalization, panic attacks, nervousness.
The part of the musculoskeletal system: arthralgia, myalgia.
On the part of the organ of vision: visual impairment.
On the part of the reproductive system: disorders of sexual function (including impotence and ejaculation disorders), hyperprolactinaemia / galactorrhoea, anorgasmia.
From the urinary system: urinary retention.
On the part of the digestive system: loss of appetite, nausea, vomiting, dry mouth, constipation or diarrhea; very rarely - hepatitis.
Since the cardiovascular system: orthostatic hypotension.
Allergic reactions: rash, urticaria, ekhimatozy, itching, angioedema.
Other: increased sweating, hyponatremia, violation of secretion of ADH, withdrawal syndrome with abrupt cancellation of the drug.
Contraindications
simultaneous reception of MAO inhibitors and the period to 14 days after their removal;
simultaneous reception tioridazina;
unstable epilepsy;
Pregnancy
Lactation (breastfeeding);
Hypersensitivity to the drug's components.
Precautions should be prescribed drug in the liver and kidney failure, angle-closure glaucoma, prostatic hyperplasia, mania, heart disease, epilepsy, convulsive states, with an electric pulse therapy, while taking drugs that increase the risk of bleeding, the presence of risk factors for bleeding disorders and diseases, increase the risk of bleeding.
Pregnancy and lactation
Aktaparoksetin drug is contraindicated during pregnancy and lactation (breastfeeding).
Application for violations of liver function
When liver failure Aktaparoksetin used with caution.
Recommended daily dose is 20 mg.
Application for violations of renal function
In renal insufficiency drug Aktaparoksetin used with caution. Recommended daily dose is 20 mg.
Cautions
To avoid the development of CSN patients taking neuroleptics, a drug used with caution. Treatment of paroxetine prescribed after 2 weeks after discontinuation of MAO inhibitors. Elderly patients during the administration of the drug can hyponatraemia. In some cases, while application Aktaparoksetina with insulin and / or oral hypoglycemic agents require dosage adjustment of the latter.
With the development of seizures paroxetine treatment should be discontinued.
When the first signs of mania should be abolished paroxetine therapy. During the first few weeks should carefully monitor the condition of the patient in connection with possible suicide attempts. Patients should be informed that during the period of treatment should refrain from alcohol.
Effects on ability to drive vehicles and management mechanisms
Paroxetine does not impair cognitive and psychomotor function. Nevertheless, as in the treatment of other psychotropic drugs, patients should exercise caution when driving and drivers.
During the period of treatment should refrain from the study of potentially hazardous activities that require high concentration and speed of psychomotor reactions.
Overdose
Symptoms: nausea, dilated pupils, fever, changes in blood pressure, headache, involuntary muscle contractions, agitation, anxiety, tachycardia is very rare - ECG changes, coma (while also taking other psychotropic drugs and / or alcohol).
Treatment: gastric lavage, activated charcoal, symptomatic therapy. No specific antidote.
Drug Interactions
Acceptance of food and antacid did not affect the absorption and pharmacokinetic parameters of the drug. Paroxetine is incompatible with MAO inhibitors. In case of simultaneous appointment with paroxetine increases the concentration of protsiklidina.
During paroxetine therapy should refrain from alcohol intake in connection with the intensification of the toxic effect of alcohol. Because inhibition of cytochrome P450 paroxetine may gain of barbiturates, phenytoin, indirect anticoagulants, tricyclic antidepressants, phenothiazine neuroleptics, a class 1C antiarrhythmic drugs, metoprolol, and increased risk of side effects, while the appointment of these medicines.
In case of simultaneous appointment with drugs that inhibit liver enzymes may require reducing the dose of paroxetine. Paroxetine increases bleeding time in the background receiving warfarin at constant prothrombin time. In case of simultaneous appointment of paroxetine with atypical antipsychotic means, phenothiazines, tricyclic antidepressants, acetylsalicylic acid, NSAIDs should be cautious in connection with possible bleeding disorders.
Simultaneous with the appointment of serotoninergic drugs (tramadol, sumatriptan) may lead to increased serotonergic effect.
It is marked synergism tryptophan, drugs lithium and paroxetine. In case of simultaneous appointment of paroxetine with phenytoin and other anticonvulsant may decrease the concentration of paroxetine in plasma and increased frequency of side effects.
Terms and Conditions of storage
The drug should be stored out of reach of children at or above 25 ° C. Shelf life - 3 years.
Tablets, film-coated white or almost white, round, biconvex, with risks on both sides and the side of risk, with the inscription "P" on one side and "20" - on the other.
1 tab. paroxetine hydrochloride 22.22 mg, which corresponds to the content of paroxetine 20 mg.
Excipients: magnesium stearate, karboksimetilkrahmal sodium (sodium starch glycolate), mannitol DC, microcrystalline cellulose, polymethacrylates, Opadry white AMB (aqueous solution), polyvinyl alcohol (partially hydrolyzed), titanium dioxide (E171), talc, soya lecithin (E322) , Gum Xanthan (E415); Opadry AMB blue (aqueous solution): alcohol polyvinyl (partially hydrolyzed), titanium dioxide (E171), talc, lecithin soya (E322), Gum Xanthan (E415); FD & C blue-indigo carmine lake (E132 ), FD & C yellow-6/sunset yellow lake (E110), Qunoline yellow lake (E104).
Tablets, film-coated blue, round, biconvex, with risks on the one side and the inscription "P30" - on the other.
1 tab. paroxetine hydrochloride 33.33 mg, which corresponds to the content of paroxetine 30 mg.
Excipients: magnesium stearate, karboksimetilkrahmal sodium (sodium starch glycolate), mannitol DC, microcrystalline cellulose, polymethacrylates, Opadry white AMB (aqueous solution), polyvinyl alcohol (partially hydrolyzed), titanium dioxide (E171), talc, soya lecithin (E322) , Gum Xanthan (E415); Opadry AMB blue (aqueous solution): alcohol polyvinyl (partially hydrolyzed), titanium dioxide (E171), talc, lecithin soya (E322), Gum Xanthan (E415); FD & C blue-indigo carmine lake (E132 ), FD & C yellow lake (E110), Qunoline yellow lake (E104). 10 pcs. - Blisters (3) - packs cardboard. Clinico-pharmacological group: Antidepressants. Mechanism of action of antidepressants.
Paroxetine is a potent and selective inhibitor of serotonin (5-hydroxytryptamine, 5-HT) neurons of the brain that determines its antidepressant action and effectiveness in the treatment of obsessive-compulsive and panic disorder. The main metabolites of paroxetine are polar and conjugated products of oxidation and methylation, which are rapidly cleared from the body, have weak pharmacological activity and not affect the therapeutic effect.
When the metabolism of paroxetine is not disturbed due to the operation of selective serotonin neurons. Paroxetine has low affinity to m-cholinergic receptors. With a selective action, in contrast to tricyclic antidepressants, paroxetine has a low affinity to α1, α2, β-adrenoceptors, as well as dopamine, 5-HT1 like, 5-HT2 and histamine H1 like-receptors.
Paroxetine does not affect psychomotor function and potentiates the inhibitory effect of ethanol on them. According to the study of behavior and EEG in patients taking paroxetine, it is proved that the appointment at doses higher than those required for inhibition of serotonin, paroxetine at the weak-activating properties. In healthy volunteers it causes no significant change in the level of blood pressure, heart rate and EEG. Unlike antidepressants, which inhibit the capture of norepinephrine, paroxetine is much weaker inhibits the antihypertensive effect guanetidina.
Pharmacokinetics
Absorption
After oral administration of paroxetine is well absorbed from the gastrointestinal tract. Treated metabolism during "first pass" through the liver. Clinical effects of paroxetine (side-effects and efficacy) did not correlate with its concentration in plasma.
Distribution
Css achieved for 7-14 days after initiation of treatment, pharmacokinetics during prolonged treatment does not change. At therapeutic concentrations of paroxetine binding to plasma proteins is 95%. Paroxetine is extensively distributed in tissues, and pharmacokinetic calculations indicate that only 1% of it is present in the plasma.
Metabolism
Because the metabolism of paroxetine includes "first passage" through the liver, its amount, as determined in the systemic circulation is less than that which is absorbed from the gastrointestinal tract. With increasing doses of paroxetine or multiple dosing, which increases the load on the body, has been partially reduced the effect of "first pass" through the liver and reduced plasma clearance of paroxetine. As a result, may increase the concentration of paroxetine in plasma and variations of pharmacokinetic parameters that can be observed only in those patients in whom the drug in low doses are reached low concentrations of paroxetine in plasma.
Withdrawal
T1 / 2 varies, but usually is about 1 day. Withdrawal from the body of metabolites of paroxetine biphasic, initially as a result of metabolism during first passage through the liver, then it is controlled by systemic elimination. Paroxetine appears mainly in the form of metabolites: 64% of metabolites excreted in urine and 36% of the bile through the intestines. In the unaltered output of 2% in the urine and 1% bile.
Pharmacokinetics in special clinical situations
In elderly patients, as well as in patients with renal and hepatic insufficiency of severe degree, the concentration of paroxetine in plasma increased, and the range of plasma concentrations had almost coincides with the range in healthy adult volunteers.
Statement
depression of all types (incl. reactive, severe endogenous depression and depression accompanied by anxiety);
obsessive-compulsive disorder;
panic disorder, including with agoraphobia;
social anxiety disorder / social phobia;
generalized anxiety disorder;
treatment of posttraumatic stress disorder.
Dosage regimen
Drugs are taken by mouth 1 time per day, morning, during a meal. Swallow the tablet whole, washed down with water. The dose selected individually for the first 2-3 weeks after initiation of therapy and subsequently, if necessary, corrected.
For the treatment of depression prescribed drug in a dose of 20 mg 1 time per day. If necessary, gradually increase the dose of 10 mg / day, maximum daily dose - 50 mg.
In obsessive-compulsive disorders initial therapeutic dose is 20 mg / day, followed by a weekly increase of 10 mg.
The recommended average therapeutic dose - 40 mg / day, if necessary, the dose may be increased to 60 mg / day.
In panic disorder Aktaparoksetin appointed at the initial dose of 10 mg / day (to reduce the possible risk of exacerbation of panic symptoms), followed by a weekly increase of 10 mg. The average therapeutic dose - 40 mg / day. The maximum dose - 50 mg / day.
When social anxiety disorder / social phobia initial dose is 20 mg / day, with no effect for at least 2 weeks may increase the dose to a maximum of 50 mg / day.
The dose should be increased to 10 mg at intervals of not less than 1 week in accordance with the clinical effect.
In post-traumatic mental disorder for the majority of patients starting and therapeutic dose is 20 mg / day. In some cases, we recommend increasing the dose to a maximum of 50 mg / day.
The dose should be increased to 10 mg per week according to the clinical effect.
When generalized anxiety disorder and recommended starting dose - 20 mg / day.
In renal and / or hepatic insufficiency the recommended daily dose is 20 mg.
For elderly patients daily dose should not exceed 40 mg. In order to prevent the development of withdrawal symptoms on discontinuing treatment is carried out gradually.
The use of paroxetine in children is not recommended because of its safety and efficacy in this patient is not installed.
Side effect
From the CNS: drowsiness, tremor, asthenia, insomnia, dizziness, fatigue, cramps, ekstrapiramidiye disorders, serotonin syndrome, hallucinations, mania, confusion, agitation, anxiety, depersonalization, panic attacks, nervousness.
The part of the musculoskeletal system: arthralgia, myalgia.
On the part of the organ of vision: visual impairment.
On the part of the reproductive system: disorders of sexual function (including impotence and ejaculation disorders), hyperprolactinaemia / galactorrhoea, anorgasmia.
From the urinary system: urinary retention.
On the part of the digestive system: loss of appetite, nausea, vomiting, dry mouth, constipation or diarrhea; very rarely - hepatitis.
Since the cardiovascular system: orthostatic hypotension.
Allergic reactions: rash, urticaria, ekhimatozy, itching, angioedema.
Other: increased sweating, hyponatremia, violation of secretion of ADH, withdrawal syndrome with abrupt cancellation of the drug.
Contraindications
simultaneous reception of MAO inhibitors and the period to 14 days after their removal;
simultaneous reception tioridazina;
unstable epilepsy;
Pregnancy
Lactation (breastfeeding);
Hypersensitivity to the drug's components.
Precautions should be prescribed drug in the liver and kidney failure, angle-closure glaucoma, prostatic hyperplasia, mania, heart disease, epilepsy, convulsive states, with an electric pulse therapy, while taking drugs that increase the risk of bleeding, the presence of risk factors for bleeding disorders and diseases, increase the risk of bleeding.
Pregnancy and lactation
Aktaparoksetin drug is contraindicated during pregnancy and lactation (breastfeeding).
Application for violations of liver function
When liver failure Aktaparoksetin used with caution.
Recommended daily dose is 20 mg.
Application for violations of renal function
In renal insufficiency drug Aktaparoksetin used with caution. Recommended daily dose is 20 mg.
Cautions
To avoid the development of CSN patients taking neuroleptics, a drug used with caution. Treatment of paroxetine prescribed after 2 weeks after discontinuation of MAO inhibitors. Elderly patients during the administration of the drug can hyponatraemia. In some cases, while application Aktaparoksetina with insulin and / or oral hypoglycemic agents require dosage adjustment of the latter.
With the development of seizures paroxetine treatment should be discontinued.
When the first signs of mania should be abolished paroxetine therapy. During the first few weeks should carefully monitor the condition of the patient in connection with possible suicide attempts. Patients should be informed that during the period of treatment should refrain from alcohol.
Effects on ability to drive vehicles and management mechanisms
Paroxetine does not impair cognitive and psychomotor function. Nevertheless, as in the treatment of other psychotropic drugs, patients should exercise caution when driving and drivers.
During the period of treatment should refrain from the study of potentially hazardous activities that require high concentration and speed of psychomotor reactions.
Overdose
Symptoms: nausea, dilated pupils, fever, changes in blood pressure, headache, involuntary muscle contractions, agitation, anxiety, tachycardia is very rare - ECG changes, coma (while also taking other psychotropic drugs and / or alcohol).
Treatment: gastric lavage, activated charcoal, symptomatic therapy. No specific antidote.
Drug Interactions
Acceptance of food and antacid did not affect the absorption and pharmacokinetic parameters of the drug. Paroxetine is incompatible with MAO inhibitors. In case of simultaneous appointment with paroxetine increases the concentration of protsiklidina.
During paroxetine therapy should refrain from alcohol intake in connection with the intensification of the toxic effect of alcohol. Because inhibition of cytochrome P450 paroxetine may gain of barbiturates, phenytoin, indirect anticoagulants, tricyclic antidepressants, phenothiazine neuroleptics, a class 1C antiarrhythmic drugs, metoprolol, and increased risk of side effects, while the appointment of these medicines.
In case of simultaneous appointment with drugs that inhibit liver enzymes may require reducing the dose of paroxetine. Paroxetine increases bleeding time in the background receiving warfarin at constant prothrombin time. In case of simultaneous appointment of paroxetine with atypical antipsychotic means, phenothiazines, tricyclic antidepressants, acetylsalicylic acid, NSAIDs should be cautious in connection with possible bleeding disorders.
Simultaneous with the appointment of serotoninergic drugs (tramadol, sumatriptan) may lead to increased serotonergic effect.
It is marked synergism tryptophan, drugs lithium and paroxetine. In case of simultaneous appointment of paroxetine with phenytoin and other anticonvulsant may decrease the concentration of paroxetine in plasma and increased frequency of side effects.
Terms and Conditions of storage
The drug should be stored out of reach of children at or above 25 ° C. Shelf life - 3 years.
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