Composition, structure and packing
Tablets, coated in white or almost white, round, biconvex.
1 tab. paroxetine (in the form gemigidrata hydrochloride) 20 mg.
Excipients: calcium hydrophosphate (calcium disodium phosphate), corn starch, sodium karboksimetilkrahmal (primogel), magnesium stearate.
The composition of the shell: Opadry II (gipromelloza, lactose monohydrate, macrogol / polyethylene glycol 3350, polyethylene 4000 /, titanium dioxide).
Clinico-pharmacological group: Antidepressants.
Pharmacological action
Antidepressant. Is a selective serotonin reuptake inhibitors (5-hydroxytryptamine, 5-HT) neurons of the brain that determines its antidepressant action and effectiveness in treating obsessive-compulsive (OCD) and panic disorder.
Paroxetine has low affinity to m-cholinergic receptors (has a weak anticholinergic effect), α1-, α2-and β-adrenoceptors, as well as dopamine (D2), 5HT1-like, 5HT2-like and histamine H1-receptors. Paroxetine does not affect psychomotor function and potentiates the inhibitory effect of ethanol on them.
According to the study of behavior and EEG paroxetine the weak activating properties when it is administered in doses higher than those required for inhibition of serotonin. In healthy volunteers it causes no significant change in levels of blood pressure, heart rate and EEG.
Pharmacokinetics
Absorption
After oral administration of paroxetine is well absorbed from the gastrointestinal tract. Simultaneous food intake does not affect the absorption and pharmacokinetics of paroxetine.
Distribution
The equilibrium state is reached in 7-14 days after initiation of therapy, further pharmacokinetics during prolonged treatment does not change.
Clinical effects of paroxetine (side-effects and efficacy) did not correlate with its concentration in plasma.
Since the effect of paroxetine being the "first pass" through the liver, its amount, as determined in systemic circulation is less than that which is absorbed from the gastrointestinal tract. With increasing doses of paroxetine or when multiple dosing 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 achieved low levels of paroxetine in plasma.
Paroxetine is extensively distributed in tissues, and pharmacokinetic calculations indicate that only 1% of it is present in plasma, with therapeutic concentrations of 95% associated with plasma proteins.
Metabolism
The main metabolites of paroxetine are polar and conjugated products of oxidation and the methylation, which are rapidly cleared from the body, have weak pharmacological activity and do not affect its therapeutic effect. Withdrawal from the body of metabolites of paroxetine biphasic, initially as a result of "first pass" through the liver, then it is controlled by systemic elimination.
Withdrawal
T1 / 2 of paroxetine is in the range of 6 to 71 h, but the average is 24 hours about 64% of paroxetine is excreted in the urine (2% - unchanged, 64% - in the form of metabolites), approximately 36% is excreted in the bile through intestine, mainly in the form of metabolites, less than 1% - unchanged.
Pharmacokinetics in special clinical situations
The concentration of paroxetine in plasma increases with abnormal liver function and kidney, as well as in the elderly, with a range of plasma concentrations of nearly coincides with the range of concentrations in healthy adult volunteers.
Statement
depression of all types, including reactive, severe endogenous depression and depression accompanied by anxiety;
obsessive-compulsive disorder (OCD);
panic disorder, including fear stay in the crowd (agoraphobia);
social anxiety disorder / social phobia;
generalized anxiety disorder;
PTSD.
Dosage regimen
Tablets should be taken 1 time per day in the morning, while eating, not chewing, drinking water. The dose is individually during the first 2-3 weeks after starting therapy and subsequently, if necessary, corrected. The effect in most cases develops gradually. For depression the recommended dose is 20 mg 1 time / day. If necessary, gradually increase the dose to 10 mg at intervals of 1 week to achieve a therapeutic effect, the maximum daily dose should not exceed 50 mg / day.
In obsessive-compulsive disorders initial therapeutic dose is 20 mg / day, followed by a weekly increase of 10 mg to achieve a therapeutic response. Recommended mean therapeutic dose - 40 mg / day, if necessary, the dose may be increased to 60 mg / day. When panic disorders initial dose - 10 mg / day (to reduce the possible risk of worsening of panic symptoms) followed by a weekly increase of 10 mg. The average therapeutic dose - 40 mg / day. The maximum daily dose should not exceed 60 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 a week in accordance with the clinical effect.
Post-traumatic stress disorder for most patients starting and therapeutic doses are 20 mg / day. In some cases, we recommend an increase in the maximum dose to 50 mg / day. The dose should be increased to 10 mg per week according to the clinical effect.
When generalized anxiety disorder and the initial therapeutic dose is 20 mg / day.
In renal and / or hepatic insufficiency the recommended dose is 20 mg / day. For elderly patients daily dose should not exceed 40 mg. To prevent recurrence should be carried out by maintenance therapy. With the disappearance of the symptoms of depression, this course can be 4-6 months, and for obsessive and panic disorders - more than 4-6 months. Should avoid abrupt withdrawal of the drug. In order to prevent the development of withdrawal symptoms discontinuing treatment should be gradual.
Side effect
From the CNS and the peripheral nervous system: Frequently - drowsiness or insomnia, tremor, asthenia, dizziness, anxiety, and sometimes - confusion, hallucinations, extrapyramidal disorder, paresthesia, reduced capacity to concentrate; rarely - seizures, mania, and very rarely - serotonin syndrome (agitation, hyperreflexia, diarrhea), panic disorder.
On the part of the organ of vision: in some cases - blurred vision, mydriasis.
On the part of the musculoskeletal system: rarely - myasthenia gravis, myoclonia, arthralgia, myalgia.
From the urinary system: frequent urination; rarely - urinary retention.
On the part of the reproductive system: disorders of ejaculation, libido disorders, seldom - hyperprolactinaemia / galactorrhoea, anorgasmia.
On the part of the digestive system: loss of appetite, nausea, vomiting, dry mouth, and sometimes - constipation or diarrhea, and in some cases - hepatitis.
Since the cardiovascular system: orthostatic hypotension.
Allergic reactions: seldom - rash, urticaria, ekhimatozy, pruritus, angioedema.
Other: increased sweating, in rare cases - hyponatremia, violation of secretion of antidiuretic hormone.
Contraindications
simultaneous reception of MAO inhibitors and the period of 14 days after their removal;
unstable epilepsy;
Pregnancy
Lactation (breastfeeding);
Hypersensitivity to the drug's components.
Precautions should be prescribed the drug for hepatic failure, renal insufficiency, angle-closure glaucoma, prostatic hyperplasia, mania, heart disease, epilepsy, convulsive states, while the appointment of electro therapy, simultaneous intake of drugs that increase risk of bleeding, the presence of risk factors for bleeding disorders and diseases, increase the risk of bleeding, as well as elderly patients.
Pregnancy and lactation
The drug is contraindicated during pregnancy and lactation.
Application for violations of liver function
Precautions should be prescribed the drug for hepatic failure. In liver failure the recommended dose is 20 mg / day.
Application for violations of renal function
Precautions should be prescribed the drug in renal failure. In renal insufficiency the recommended dose is 20 mg / day.
Cautions
In order to avoid the development of neuroleptic malignant syndrome should be prescribed with caution Adepress patients taking neuroleptics.
Treatment Adepressom appoint 2 weeks after discontinuation of MAO inhibitors. Elderly patients on a background of reception Adepressa possible hyponatremia. In some cases a dose correction applied simultaneously insulin and / or oral hypoglycemic agents.
With the development of seizures treatment Adepressom stop.
When the first signs of mania should be abolished Adepressom therapy. During the first few weeks of therapy Adepressom should carefully monitor the condition of the patient in connection with possible suicide attempts. During therapy Adepressom should refrain from taking alcohol in relation to increasing its toxic effect.
Use in Pediatrics
Application Adepressa in children is not recommended because of its safety and efficacy in this group of patients is not installed.
Effects on ability to drive vehicles and management mechanisms
In spite of the fact that paroxetine did not affect cognitive and psychomotor function, patients should avoid or exercise extreme caution when driving and when engaging in other potentially hazardous activities that require high concentration and quickness of psychomotor reactions.
Overdose
Symptoms: nausea, dilated pupils, fever, changes in blood pressure, headache, involuntary muscle contractions, agitation, anxiety, tachycardia. In very rare cases, while taking other psychotropic drugs and / or ethanol (alcohol), there are ECG changes, coma.
Treatment: gastric lavage, activated charcoal method. If necessary, a symptomatic therapy. No specific antidote.
Drug Interactions
Simultaneous reception antacid did not affect the absorption and pharmacokinetic parameters Adepressa. Because inhibition of cytochrome P450 paroxetine may strengthen the effect of barbiturates, phenytoin, indirect anticoagulants, tricyclic antidepressants, neuroleptics and fenotiazinovogo 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 dose reduction Adepressa.
Between paroxetine and warfarin expected pharmacodynamic interaction (with unaltered prothrombin time was an increase in bleeding). At the same time appointing Adepressa with atypical neuroleptics, tricyclic antidepressants, drugs phenothiazine series, acetylsalicylic acid, NSAIDs may be in breach of the process of blood clotting.
Simultaneous with the appointment Adepressa serotoninergic drugs (tramadol, sumatriptan) may lead to increased serotoninergic effect.
It is marked synergism tryptophan, drugs lithium and paroxetine.
At the same time appointing Adepressa with phenytoin and other anticonvulsant drugs may reduce the concentration of paroxetine in plasma and increased frequency of side effects.
Paroxetine is much weaker than inhibits the antihypertensive effect guanetidina compared with antidepressants, which inhibit the capture of norepinephrine.
Terms and Conditions of storage
List B. The drug should be kept dry, out of reach of children, at a temperature not above 25 ° C.
Shelf life - 2 years.
Tablets, coated in white or almost white, round, biconvex.
1 tab. paroxetine (in the form gemigidrata hydrochloride) 20 mg.
Excipients: calcium hydrophosphate (calcium disodium phosphate), corn starch, sodium karboksimetilkrahmal (primogel), magnesium stearate.
The composition of the shell: Opadry II (gipromelloza, lactose monohydrate, macrogol / polyethylene glycol 3350, polyethylene 4000 /, titanium dioxide).
Clinico-pharmacological group: Antidepressants.
Pharmacological action
Antidepressant. Is a selective serotonin reuptake inhibitors (5-hydroxytryptamine, 5-HT) neurons of the brain that determines its antidepressant action and effectiveness in treating obsessive-compulsive (OCD) and panic disorder.
Paroxetine has low affinity to m-cholinergic receptors (has a weak anticholinergic effect), α1-, α2-and β-adrenoceptors, as well as dopamine (D2), 5HT1-like, 5HT2-like and histamine H1-receptors. Paroxetine does not affect psychomotor function and potentiates the inhibitory effect of ethanol on them.
According to the study of behavior and EEG paroxetine the weak activating properties when it is administered in doses higher than those required for inhibition of serotonin. In healthy volunteers it causes no significant change in levels of blood pressure, heart rate and EEG.
Pharmacokinetics
Absorption
After oral administration of paroxetine is well absorbed from the gastrointestinal tract. Simultaneous food intake does not affect the absorption and pharmacokinetics of paroxetine.
Distribution
The equilibrium state is reached in 7-14 days after initiation of therapy, further pharmacokinetics during prolonged treatment does not change.
Clinical effects of paroxetine (side-effects and efficacy) did not correlate with its concentration in plasma.
Since the effect of paroxetine being the "first pass" through the liver, its amount, as determined in systemic circulation is less than that which is absorbed from the gastrointestinal tract. With increasing doses of paroxetine or when multiple dosing 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 achieved low levels of paroxetine in plasma.
Paroxetine is extensively distributed in tissues, and pharmacokinetic calculations indicate that only 1% of it is present in plasma, with therapeutic concentrations of 95% associated with plasma proteins.
Metabolism
The main metabolites of paroxetine are polar and conjugated products of oxidation and the methylation, which are rapidly cleared from the body, have weak pharmacological activity and do not affect its therapeutic effect. Withdrawal from the body of metabolites of paroxetine biphasic, initially as a result of "first pass" through the liver, then it is controlled by systemic elimination.
Withdrawal
T1 / 2 of paroxetine is in the range of 6 to 71 h, but the average is 24 hours about 64% of paroxetine is excreted in the urine (2% - unchanged, 64% - in the form of metabolites), approximately 36% is excreted in the bile through intestine, mainly in the form of metabolites, less than 1% - unchanged.
Pharmacokinetics in special clinical situations
The concentration of paroxetine in plasma increases with abnormal liver function and kidney, as well as in the elderly, with a range of plasma concentrations of nearly coincides with the range of concentrations in healthy adult volunteers.
Statement
depression of all types, including reactive, severe endogenous depression and depression accompanied by anxiety;
obsessive-compulsive disorder (OCD);
panic disorder, including fear stay in the crowd (agoraphobia);
social anxiety disorder / social phobia;
generalized anxiety disorder;
PTSD.
Dosage regimen
Tablets should be taken 1 time per day in the morning, while eating, not chewing, drinking water. The dose is individually during the first 2-3 weeks after starting therapy and subsequently, if necessary, corrected. The effect in most cases develops gradually. For depression the recommended dose is 20 mg 1 time / day. If necessary, gradually increase the dose to 10 mg at intervals of 1 week to achieve a therapeutic effect, the maximum daily dose should not exceed 50 mg / day.
In obsessive-compulsive disorders initial therapeutic dose is 20 mg / day, followed by a weekly increase of 10 mg to achieve a therapeutic response. Recommended mean therapeutic dose - 40 mg / day, if necessary, the dose may be increased to 60 mg / day. When panic disorders initial dose - 10 mg / day (to reduce the possible risk of worsening of panic symptoms) followed by a weekly increase of 10 mg. The average therapeutic dose - 40 mg / day. The maximum daily dose should not exceed 60 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 a week in accordance with the clinical effect.
Post-traumatic stress disorder for most patients starting and therapeutic doses are 20 mg / day. In some cases, we recommend an increase in the maximum dose to 50 mg / day. The dose should be increased to 10 mg per week according to the clinical effect.
When generalized anxiety disorder and the initial therapeutic dose is 20 mg / day.
In renal and / or hepatic insufficiency the recommended dose is 20 mg / day. For elderly patients daily dose should not exceed 40 mg. To prevent recurrence should be carried out by maintenance therapy. With the disappearance of the symptoms of depression, this course can be 4-6 months, and for obsessive and panic disorders - more than 4-6 months. Should avoid abrupt withdrawal of the drug. In order to prevent the development of withdrawal symptoms discontinuing treatment should be gradual.
Side effect
From the CNS and the peripheral nervous system: Frequently - drowsiness or insomnia, tremor, asthenia, dizziness, anxiety, and sometimes - confusion, hallucinations, extrapyramidal disorder, paresthesia, reduced capacity to concentrate; rarely - seizures, mania, and very rarely - serotonin syndrome (agitation, hyperreflexia, diarrhea), panic disorder.
On the part of the organ of vision: in some cases - blurred vision, mydriasis.
On the part of the musculoskeletal system: rarely - myasthenia gravis, myoclonia, arthralgia, myalgia.
From the urinary system: frequent urination; rarely - urinary retention.
On the part of the reproductive system: disorders of ejaculation, libido disorders, seldom - hyperprolactinaemia / galactorrhoea, anorgasmia.
On the part of the digestive system: loss of appetite, nausea, vomiting, dry mouth, and sometimes - constipation or diarrhea, and in some cases - hepatitis.
Since the cardiovascular system: orthostatic hypotension.
Allergic reactions: seldom - rash, urticaria, ekhimatozy, pruritus, angioedema.
Other: increased sweating, in rare cases - hyponatremia, violation of secretion of antidiuretic hormone.
Contraindications
simultaneous reception of MAO inhibitors and the period of 14 days after their removal;
unstable epilepsy;
Pregnancy
Lactation (breastfeeding);
Hypersensitivity to the drug's components.
Precautions should be prescribed the drug for hepatic failure, renal insufficiency, angle-closure glaucoma, prostatic hyperplasia, mania, heart disease, epilepsy, convulsive states, while the appointment of electro therapy, simultaneous intake of drugs that increase risk of bleeding, the presence of risk factors for bleeding disorders and diseases, increase the risk of bleeding, as well as elderly patients.
Pregnancy and lactation
The drug is contraindicated during pregnancy and lactation.
Application for violations of liver function
Precautions should be prescribed the drug for hepatic failure. In liver failure the recommended dose is 20 mg / day.
Application for violations of renal function
Precautions should be prescribed the drug in renal failure. In renal insufficiency the recommended dose is 20 mg / day.
Cautions
In order to avoid the development of neuroleptic malignant syndrome should be prescribed with caution Adepress patients taking neuroleptics.
Treatment Adepressom appoint 2 weeks after discontinuation of MAO inhibitors. Elderly patients on a background of reception Adepressa possible hyponatremia. In some cases a dose correction applied simultaneously insulin and / or oral hypoglycemic agents.
With the development of seizures treatment Adepressom stop.
When the first signs of mania should be abolished Adepressom therapy. During the first few weeks of therapy Adepressom should carefully monitor the condition of the patient in connection with possible suicide attempts. During therapy Adepressom should refrain from taking alcohol in relation to increasing its toxic effect.
Use in Pediatrics
Application Adepressa in children is not recommended because of its safety and efficacy in this group of patients is not installed.
Effects on ability to drive vehicles and management mechanisms
In spite of the fact that paroxetine did not affect cognitive and psychomotor function, patients should avoid or exercise extreme caution when driving and when engaging in other potentially hazardous activities that require high concentration and quickness of psychomotor reactions.
Overdose
Symptoms: nausea, dilated pupils, fever, changes in blood pressure, headache, involuntary muscle contractions, agitation, anxiety, tachycardia. In very rare cases, while taking other psychotropic drugs and / or ethanol (alcohol), there are ECG changes, coma.
Treatment: gastric lavage, activated charcoal method. If necessary, a symptomatic therapy. No specific antidote.
Drug Interactions
Simultaneous reception antacid did not affect the absorption and pharmacokinetic parameters Adepressa. Because inhibition of cytochrome P450 paroxetine may strengthen the effect of barbiturates, phenytoin, indirect anticoagulants, tricyclic antidepressants, neuroleptics and fenotiazinovogo 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 dose reduction Adepressa.
Between paroxetine and warfarin expected pharmacodynamic interaction (with unaltered prothrombin time was an increase in bleeding). At the same time appointing Adepressa with atypical neuroleptics, tricyclic antidepressants, drugs phenothiazine series, acetylsalicylic acid, NSAIDs may be in breach of the process of blood clotting.
Simultaneous with the appointment Adepressa serotoninergic drugs (tramadol, sumatriptan) may lead to increased serotoninergic effect.
It is marked synergism tryptophan, drugs lithium and paroxetine.
At the same time appointing Adepressa with phenytoin and other anticonvulsant drugs may reduce the concentration of paroxetine in plasma and increased frequency of side effects.
Paroxetine is much weaker than inhibits the antihypertensive effect guanetidina compared with antidepressants, which inhibit the capture of norepinephrine.
Terms and Conditions of storage
List B. The drug should be kept dry, out of reach of children, at a temperature not above 25 ° C.
Shelf life - 2 years.
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