Composition, form of production and packaging
The tablets covered with a film cover of white color, round, biconcave, covered with a shell, with a risk, with a rough surface.
1 tab.
paroxetine hydrochloride hemihydrate 22.76 mg,
which corresponds to the content of paroxetine 20 mg
Excipients: calcium hydrophosphate, microcrystalline cellulose, crospovidone, copovidone, silicon dioxide colloid, magnesium stearate, talc.
Composition of the membrane: hypromellose, macrogol 6000, talc, titanium dioxide.
10 pieces. - blisters (3) - packs of cardboard.
The tablets covered with a film membrane of white color, round, biconcave, with a risk, with a rough surface.
1 tab.
paroxetine hydrochloride hemihydrate 34.14 mg,
which corresponds to the content of paroxetine 30 mg
Excipients: calcium hydrophosphate, microcrystalline cellulose, crospovidone, copovidone, silicon dioxide colloid, magnesium stearate, talc.
Composition of the membrane: hypromellose, macrogol 6000, talc, titanium dioxide.
10 pieces. - blisters (3) - packs of cardboard.
INSTRUCTION FOR THE SPECIALIST.
Description of the drug approved by the manufacturer for the print edition of 2007.
PHARMACHOLOGIC EFFECT
Antidepressant. It is a selective inhibitor of reuptake of serotonin (5-hydroxytryptamine, 5-HT) by neurons of the brain, which determines its antidepressant effect and effectiveness in the treatment of obsessive-compulsive (OCD) and panic disorder.
Paroxetine has a low affinity for m-holinoretseptoram (has a weak anticholinergic effect),? 1 -,? 2 - and? -adrenoceptors, as well as to dopaminovym (D 2 ), 5HT 1 -like, 5HT 2 -like and histamine H 1 -receptors. Paroxetine does not impair psychomotor functions and does not potentiate the inhibitory effect of ethanol on them.
According to the study of behavior and EEG in paroxetine, weak activating properties are revealed when it is administered at doses higher than those required to inhibit the capture of serotonin. Does not cause a significant change in blood pressure, heart rate and EEG.
PHARMACOKINETICS
Suction
After ingestion paroxetine is well absorbed from the digestive tract and is metabolized first pass through the liver.
Distribution
C ss is achieved 7-14 days after the start of therapy. With increasing dose and / or duration of treatment, non-linear dependence of pharmacokinetic parameters on dose is observed.
Paroxetine is extensively distributed in tissues, only 1% of it is present in the plasma.
It binds to proteins by 95%.
Metabolism
Metabolized in the liver with the formation of inactive metabolites. It is an inhibitor of the isoenzyme CYP2D6.
The main metabolites of paroxetine are polar and conjugated products of oxidation and methylation, which are rapidly excreted from the body, have weak pharmacological activity and do not affect its therapeutic effect. In the metabolism of paroxetine, the selective seizure of serotonin due to its action by neurons is not impaired.
Excretion
About 64% of paroxetine is excreted in urine (2% in unchanged form, 64% in the form of metabolites); approximately 36% is secreted with bile through the intestine, mainly in the form of metabolites, less than 1% - in unchanged form.
Derivation of metabolites of paroxetine biphasic, first as a result of the metabolism of the first passage through the liver, and then it is controlled by systemic elimination. T 1/2 of paroxetine varies, but on average is 24 hours.
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 all types, including reactive, severe endogenous depression and depression, accompanied by anxiety;
- obsessive-compulsive disorder (ROC);
- panic disorder, incl. with agoraphobia;
- social anxiety disorder / social phobia;
generalized anxiety disorder.
DOSING MODE
Tablets should be taken orally, 1 time / day, in the morning, while eating, swallowing whole, with water.
The dose is selected individually during the first 2-3 weeks after the start of therapy and is subsequently adjusted if necessary.
With depression, the recommended dose is 20 mg 1 time / day. If necessary, the dose is gradually increased by 10 mg / day, the maximum daily dose should not exceed 50 mg.
In obsessive-compulsive disorders, the initial therapeutic dose is 20 mg / day, followed by a weekly increase of 10 mg. The recommended average therapeutic dose is 40 mg / day, if necessary, the dose may be increased to 60 mg / day.
In panic disorders, the initial dose is 10 mg / day (to reduce the possible risk of developing panic symptoms) followed by a weekly increase of 10 mg. The average therapeutic dose is 40 mg / day. The maximum dose is 50 mg / day.
With socially-disturbing disorders / social phobias, the initial dose is 20 mg / day, in the absence of effect for at least 2 weeks, an increase in the dose to a maximum of 50 mg / day is possible. The dose should be increased by 10 mg at intervals of at least a week in accordance with the clinical effect.
In generalized anxiety disorders, the initial and therapeutic doses are 20 mg / day.
With renal and / or liver failure the recommended dose is 20 mg / day.
For elderly patients, the daily dose should not exceed 40 mg.
In order to prevent the development of withdrawal syndrome, the discontinuation of taking the drug should be gradual.
SIDE EFFECT
From the central nervous system and peripheral nervous system: drowsiness, tremor, asthenia, insomnia, dizziness, fatigue, seizures, extrapyramidal disorders, serotonin syndrome, hallucinations, mania, confusion, agitation, anxiety, depersonalization, panic attacks, nervousness, amnesia, myoclonia.
From the senses: a blurred vision.
From the musculoskeletal system: arthralgia, myalgia, muscle weakness, myopathy.
From the urinary system: urinary retention, frequent urination.
On the part of the reproductive system: violations of sexual function, including impotence and ejaculation disorders, hyperprolactinemia / galactorrhea, anorgasmia.
On the part of the digestive system: a decrease or increase in appetite, a change in taste, nausea, vomiting, dry mouth, constipation or diarrhea; in some cases - hepatitis.
From the cardiovascular system: orthostatic hypotension.
Allergic reactions: rash, hives, ecchymosis, itching, angioedema.
Other: increased sweating, rhinitis, hyponatremia, a violation of the secretion of antidiuretic hormone.
CONTRAINDICATIONS
- simultaneous administration of MAO inhibitors and a period of 14 days after their withdrawal;
- Unstable epilepsy;
- Pregnancy;
- the period of lactation (breastfeeding);
- childhood;
- Hypersensitivity to the components of the drug.
With caution , the drug should be prescribed for liver failure, renal insufficiency, closed-angle glaucoma, prostatic hyperplasia, mania, cardiac pathology, epilepsy, convulsive conditions, simultaneous appointment of electropulse therapy, simultaneous use of drugs that increase the risk of bleeding, the presence of risk factors for increased bleeding and diseases, increasing the risk of bleeding.
PREGNANCY AND LACTATION
The drug is contraindicated for use in pregnancy and lactation.
APPLICATION FOR FUNCTIONS OF THE LIVER
With caution should prescribe the drug for kidney failure. In renal failure, the recommended dose is 20 mg / day.
APPLICATION FOR VIOLATIONS OF THE FUNCTION OF KIDNEYS
With caution should prescribe the drug for liver failure. In liver failure, the recommended dose is 20 mg / day.
APPLICATION FOR CHILDREN
The drug is contraindicated in childhood.
APPLICATION IN ELDERLY PATIENTS
For elderly patients, the daily dose should not exceed 40 mg.
SPECIAL INSTRUCTIONS
To avoid the development of a malignant neuroleptic syndrome, with caution should be prescribed Paroxetine to patients taking antipsychotics.
Treatment with Paroxetine is prescribed 2 weeks after the abolition of MAO inhibitors.
In elderly patients with the administration of Paroxetine, hyponatremia is possible.
In some cases, a dose adjustment of simultaneously used insulin and / or oral hypoglycemic drugs is required.
With the development of seizures, treatment with Paroxetine is stopped.
At the first sign of mania, it is necessary to cancel therapy with Paroxetine.
During the first few weeks of therapy, Paroxetine should carefully monitor the patient's condition in connection with possible suicidal attempts.
During therapy, Paroxetine should refrain from taking alcohol because of the increased toxic effect.
Use in Pediatrics
The use of Paroxetine in children is not recommended, since its safety and effectiveness in this group of patients are not established.
Impact on the ability to drive vehicles and manage mechanisms
Although paroxetine does not impair cognitive and psychomotor functions, patients should abstain or observe extreme caution when driving and engaging in other potentially dangerous activities requiring increased attention and speed of psychomotor reactions.
OVERDOSE
Symptoms: nausea, vomiting, tremor, mydriasis, dry mouth, irritability, nystagmus, agitation, sweating, drowsiness, sinus tachycardia, convulsions, bradycardia, increased blood pressure, nodal rhythm. In very rare cases, while taking with other psychotropic drugs and / or alcohol, ECG, coma changes are possible. With severe overdose - serotonin syndrome, rarely - rhabdomyolysis.
Treatment: gastric lavage, reception of activated charcoal. If necessary, conduct symptomatic therapy. There is no specific antidote.
DRUG INTERACTION
Simultaneous administration of antacid agents does not affect the absorption and pharmacokinetic parameters of Paroxetine.
Contraindicated concurrent use of Paroxetine with MAO inhibitors.
With concomitant administration with Paroxetine, the concentration of procyclidine increases.
In connection with the inhibition of paroxetine cytochrome P 450 , the effect of barbiturates, phenytoin, indirect anticoagulants, tricyclic antidepressants, phenothiazine antipsychotics and antiarrhythmics of class 1C, metoprolol, and an increased risk of side effects with the simultaneous administration of these medicines may be enhanced.
At simultaneous appointment with the preparations, inhibiting enzymes of a liver, the dose of Paroxetine can be required.
Paroxetine increases bleeding time against the background of a single-dose warfarin (with unchanged prothrombin time).
With the simultaneous administration of paroxetine with atypical antipsychotics, tricyclic antidepressants, phenothiazine drugs, NSAIDs (including acetylsalicylic acid), it is possible that the blood coagulation process is violated.
Simultaneous administration of Paroxetine with serotonergic drugs (tramadol, sumatriptan) may lead to an increase in the serotonergic effect.
Mutual enhancement of the action of tryptophan, lithium and paroxetine preparations was noted.
With the simultaneous administration of paroxetine with phenytoin and other anticonvulsant drugs, an increase in the incidence of side effects is possible.
Paroxetine much less suppresses the antihypertensive effects of guanethidine compared with antidepressants that inhibit the seizure of norepinephrine.
TERMS OF RELEASE FROM PHARMACY
The drug is released by prescription.
TERMS AND CONDITIONS OF STORAGE
The drug should be stored in a dry, protected from light, out of reach of children at a temperature of no higher than 25 В° C. Shelf life - 3 years.
