Composition, form of production and packaging
The tablets covered with a film membrane of white or almost white color, round, biconcave, with a risk on one side and the inscription "P20" - on the other.
1 tab.
paroxetine hydrochloride 22.22 mg,
which corresponds to the content of paroxetine 20 mg
Auxiliary substances: magnesium stearate 2255 - 4.5 mg, sodium carboxymethyl starch - 6 mg, mannitol DC - 133.64 mg, microcrystalline cellulose - 133.64 mg, methyl methacrylate copolymer, dimethylaminoethyl methacrylate and butyl methacrylate (eudragit E100) - 1.8 mg, opaline AMB white (aqueous solution): polyvinyl alcohol partially hydrolyzed - 5.46 mg, titanium dioxide (E171) 3.84 mg, talc 2.4 mg, soy lecithin (E322) 0.24 mg, xanthan gum (E415) 0.06 mg.
10 pieces. - blisters (3) - packs of cardboard.
The tablets covered with a film cover of blue color, round, biconcave, with a risk on 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
Auxiliary substances: Magnesium stearate 2255 - 6.75 mg, sodium carboxymethyl starch - 9 mg, mannitol DC - 200.46 mg, microcrystalline cellulose - 200.46 mg, methyl methacrylate copolymer, dimethylaminoethyl methacrylate and butyl methacrylate (eudragit E100) 2.7 mg, opaline AMB blue (aqueous solution): polyvinyl alcohol partially hydrolyzed - 8.19 mg, titanium dioxide (E171) 4.93 mg, talc 3.6 mg, indigocarmine (E132) 0.83 mg, soy lecithin (E322) 0.36 mg, xanthan gum (E415) 0.086 mg, dye solar sunset yellow (E110) - 0.002 mg, dye quinoline yellow (E104) - 0.002 mg.
10 pieces. - blisters (3) - packs of cardboard.
The tablets covered with a film membrane of white or almost white color, round, biconcave, with a risk on one side and the inscription "P20" - on the other.
1 tab.
paroxetine hydrochloride 22.22 mg,
which corresponds to the content of paroxetine 20 mg
Auxiliary substances: magnesium stearate 2255 - 4.5 mg, sodium carboxymethyl starch - 6 mg, mannitol DC - 133.64 mg, microcrystalline cellulose - 133.64 mg, methyl methacrylate copolymer, dimethylaminoethyl methacrylate and butyl methacrylate (eudragit E100) - 1.8 mg, opaline AMB white (aqueous solution): polyvinyl alcohol partially hydrolyzed - 5.46 mg, titanium dioxide (E171) 3.84 mg, talc 2.4 mg, soy lecithin (E322) 0.24 mg, xanthan gum (E415) 0.06 mg.
10 pieces. - blisters (3) - packs of cardboard.
The tablets covered with a film cover of blue color, round, biconcave, with a risk on 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
Auxiliary substances: magnesium stearate 2255 - 6.75 mg, sodium carboxymethyl starch - 9 mg, mannitol DC - 200.46 mg, microcrystalline cellulose - 200.46 mg, methyl methacrylate copolymer, dimethylaminoethyl methacrylate and butyl methacrylate (eudragit E100) 2.7 mg, opaline AMB blue (aqueous solution): polyvinyl alcohol partially hydrolyzed - 8.19 mg, titanium dioxide (E171) 4.93 mg, talc 3.6 mg, indigocarmine (E132) 0.83 mg, soy lecithin (E322) 0.36 mg, xanthan gum (E415) 0.086 mg, dye solar sunset yellow (E110) - 0.002 mg, dye quinoline yellow (E104) - 0.002 mg.
10 pieces. - blisters (3) - packs of cardboard.
INSTRUCTION FOR THE SPECIALIST.
Description of the drug approved by the manufacturer for the printed edition of 2011.
PHARMACHOLOGIC EFFECT
Antidepressant. Paroxetine is a potent and selective inhibitor of the capture of serotonin (5-hydroxytryptamine, 5-HT) by neurons of the brain, which determines its antidepressant effect and effectiveness in treating obsessive-compulsive and panic disorder.
The main metabolites of paroxetine are polar and conjugated oxidation and methylation products that are rapidly eliminated from the body, have weak pharmacological activity and do not affect the therapeutic effect. In the metabolism of paroxetine, the selective uptake of 5-HT neurons due to its action is not impaired.
Paroxetine has a low affinity for m-cholinergic receptors. Having a selective effect, unlike tricyclic antidepressants, paroxetine is characterized by low affinity to? 1 -,?2 -,? -adrenoceptors, as well as to dopamine, 5-HT 1 -like, 5-HT 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 patients taking paroxetine, it is proved that when administered at doses higher than those required to inhibit the capture of 5-HT, weak activation properties are revealed in paroxetine. In healthy volunteers, it does not cause a significant change in the level of blood pressure, heart rate and EEG.
Unlike antidepressants, which inhibit the capture of norepinephrine, paroxetine much less suppresses the antihypertensive effects of guanethidine.
PHARMACOKINETICS
Suction
After ingestion paroxetine is well absorbed from the digestive tract. It is metabolized by the "first pass" through the liver.
The clinical effects of paroxetine (side effect and efficacy) do not correlate with its concentration in the plasma.
Distribution
C ss is reached by 7-14 days after the start of treatment, pharmacokinetics during prolonged treatment does not change.
In therapeutic concentrations, the binding of paroxetine to plasma proteins is 95%.
Paroxetine is extensively distributed in tissues, and pharmacokinetic calculations show that only 1% of it is present in the plasma.
Metabolism
Because the metabolism of paroxetine involves the effect of "first passage" through the liver, its quantity, determined in the systemic blood flow, is less than that absorbed from the digestive tract. With increasing dose of paroxetine or with multiple dosing, when the load on the body increases, a partial absorption of the effect of "first passage" through the liver and a decrease in plasma clearance of paroxetine occur. As a result, it is possible to increase the concentration of paroxetine in the plasma and fluctuations in the pharmacokinetic parameters, which can be observed only in those patients who, when taking the drug at low doses, achieve low concentrations of paroxetine in the plasma.
Excretion
T 1/2 varies, but usually is about 1 day. Excretion of metabolites of paroxetine from the body is biphasic, first as a result of metabolism during the first passage through the liver, and then it is controlled by systemic elimination.
Paroxetine is excreted mainly in the form of metabolites: 64% of metabolites are excreted in the urine and 36% with bile through the intestine. Unchanged, 2% of urine and 1% of bile are excreted.
Pharmacokinetics in special clinical cases
In elderly patients, as well as in patients with severe and severe renal and hepatic insufficiency, the concentration of paroxetine in plasma is increased, and the range of plasma concentrations in them almost coincides with the range in healthy adult volunteers.
INDICATIONS
- depression of all types (including reactive, severe endogenous depression and depression, accompanied by anxiety);
- obsessive-compulsive disorder;
- panic disorder, incl. with agoraphobia;
- social anxiety disorder / social phobia;
generalized anxiety disorder;
- treatment of post-traumatic stress disorder.
DOSING MODE
The drug is taken orally 1 time / day, in the morning, while eating. The tablet is swallowed whole, washed down with water.
The dose is selected individually during the first 2-3 weeks after the initiation of therapy and subsequently, if necessary, adjusted.
To treat depression, prescribe a drug at a dose of 20 mg 1 time / day. If necessary, the dose is gradually increased by 10 mg / day, the maximum daily dose is 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, Aktaparoxetine is prescribed at an initial dose of 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-anxiety disorders / social phobia, 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 not less than 1 week in accordance with the clinical effect.
For posttraumatic disorders of the psyche for most patients, the initial and therapeutic doses are 20 mg / day. In some cases, a dose increase of up to 50 mg / day is recommended. The dose should be increased by 10 mg every week in accordance with the clinical effect.
In generalized anxiety disorders, the initial and recommended dose is 20 mg / day.
In renal and / or liver failure, the recommended daily dose is 20 mg.
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 is carried out gradually.
SIDE EFFECT
From the side of the central nervous system: drowsiness, tremor, asthenia, insomnia, dizziness, fatigue, seizures, extrapyramidal disorders, serotonin syndrome, hallucinations, mania, confusion, agitation, anxiety, depersonalization, panic attacks, increased nervous excitability, paresthesia, decreased ability to concentrate attention.
From the musculoskeletal system: arthralgia, myalgia, myasthenia gravis, myoclonia, myopathic syndrome.
From the sense organs: visual disturbances, changes in taste.
On the part of the reproductive system: violations of sexual function (including impotence and ejaculation disorders), hyperprolactinaemia / galactorrhea, anorgasmia.
From the urinary system: urinary retention, increased frequency of urination.
On the part of the digestive system: decreased appetite, nausea, vomiting, dry mouth, constipation or diarrhea; very rarely - hepatitis.
From the cardiovascular system: orthostatic hypotension.
Allergic reactions: rashes, hives, ecchymoses, itching, angioedema.
Other: increased sweating, hyponatremia, violation of ADH secretion, withdrawal syndrome with abrupt withdrawal of the drug, rhinitis.
CONTRAINDICATIONS
- simultaneous administration of MAO inhibitors and a period of up to 14 days after their cancellation;
- simultaneous reception of thioridazine;
- Unstable epilepsy;
- Pregnancy;
- the period of lactation (breastfeeding);
- children and adolescence under 18;
- Hypersensitivity to the components of the drug.
With caution , the drug should be prescribed for hepatic and renal failure, zakratougolnoy glaucoma, prostatic hyperplasia, mania, cardiac pathology, epilepsy, convulsive states, during electropulse therapy, when taking drugs that increase the risk of bleeding, if there are risk factors for increased bleeding and diseases, increasing the risk of bleeding, elderly patients.
PREGNANCY AND LACTATION
Aktaparoxetine is contraindicated for use in pregnancy and lactation (breastfeeding).
APPLICATION FOR FUNCTIONS OF THE LIVER
With renal failure, the drug Aktaparoxetine is administered with caution. The recommended daily dose is 20 mg.
APPLICATION FOR VIOLATIONS OF THE FUNCTION OF KIDNEYS
With hepatic failure, Aktaparoxetine is administered with caution. The recommended daily dose is 20 mg.
APPLICATION FOR CHILDREN
Contraindicated: children and adolescence under 18 years.
APPLICATION IN ELDERLY PATIENTS
Caution should be given to elderly patients.
SPECIAL INSTRUCTIONS
To avoid the development of ZNS patients taking antipsychotics, the drug is prescribed with caution.
Treatment with paroxetine is prescribed 2 weeks after the abolition of MAO inhibitors.
In elderly patients during the administration of the drug, hyponatremia is possible.
In some cases, with the simultaneous use of Aktaparoxetine with insulin and / or oral hypoglycemic drugs, a dose adjustment of the latter is required.
With the development of seizures, treatment with paroxetine should be discontinued.
At the first sign of mania, therapy with paroxetine should be discontinued.
During the first few weeks, the patient's condition should be carefully monitored in connection with possible suicidal attempts.
The patient should be informed that during the treatment period it is necessary to refrain from drinking alcohol.
Impact on the ability to drive vehicles and manage mechanisms
Paroxetine does not impair cognitive and psychomotor functions. Nevertheless, as with other psychotropic medications, patients should be careful when driving and moving machinery. During the treatment period, the patient should refrain from engaging in potentially dangerous activities that require an increased concentration of attention and speed of psychomotor reactions.
OVERDOSE
Symptoms: nausea, dilated pupils, fever, increased blood pressure, headache, involuntary muscle contractions, agitation, anxiety, sinus tachycardia, bradycardia, nodal rhythm; very rarely - oppression of consciousness up to coma (with simultaneous reception with other psychotropic drugs and / or alcohol).
Treatment: gastric lavage, activated charcoal, symptomatic therapy. There is no specific antidote.
DRUG INTERACTION
The intake of food and antacid agents does not affect the absorption and pharmacokinetic parameters of the drug.
Paroxetine is incompatible with MAO inhibitors.
With simultaneous administration with paroxetine, the concentration of procyclidine increases.
During therapy with paroxetine, one should refrain from taking alcohol because of the increased toxic effect of alcohol.
In connection with the inhibition of cytochrome P450 by paroxetine, it is possible to increase the action of barbiturates, phenytoin, indirect anticoagulants, tricyclic antidepressants, phenothiazine antipsychotics, antiarrhythmics of class I C, metoprolol, and an increased risk of side effects with concomitant administration of these drugs.
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 taking warfarin, with the same prothrombin time.
With the simultaneous administration of paroxetine with atypical antipsychotic agents, phenothiazines, tricyclic antidepressants, acetylsalicylic acid, NSAIDs, caution should be exercised in connection with possible bleeding disorders.
Simultaneous administration 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 anticonvulsants, a decrease in paroxetine concentration in the plasma and an increase in the frequency of side effects are possible.
TERMS OF RELEASE FROM PHARMACY
The drug is released by prescription.
TERMS AND CONDITIONS OF STORAGE
The drug should be stored out of reach of children at a temperature of no higher than 25 В° C. Shelf life - 3 years.
