Paxil
Paxil: instructions for use and reviews
- 1. Release form and composition
- 2. Pharmacological properties
- 3. Indications for use
- 4. Contraindications
- 5. Method of application and dosage
- 6. Side effects
- 7. Overdose
- 8. Special instructions
- 9. Application during pregnancy and lactation
- 10. Use in childhood
- 11. In case of impaired renal function
- 12. For violations of liver function
- 13. Use in the elderly
- 14. Drug interactions
- 15. Analogs
- 16. Terms and conditions of storage
- 17. Terms of dispensing from pharmacies
- 18. Reviews
- 19. Price in pharmacies
Latin name: Paxil
ATX code: N06AB05
Active ingredient: paroxetine (paroxetine)
Manufacturer: GlaxoSmithKline Pharmaceuticals, S. A. (GlaxoSmithKline Pharmaceuticals, SA) (Poland); Glaxo Wellcome Production (France); Es. C. Evrofarm Es. A. (SCEuropharm SA) (Romania)
Description and photo update: 2019-20-08
Prices in pharmacies: from 617 rubles.
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Paxil is a drug with an antidepressant effect.
Release form and composition
The dosage form of Paxil is film-coated tablets: white, biconvex, oval; on one side - risk, on the other - engraving "20" (10 pcs. in blisters, 1, 3 or 10 blisters in a cardboard box).
Composition of 1 tablet:
- Active ingredient: paroxetine - 20 mg (paroxetine hydrochloride hemihydrate - 22.8 mg);
- Additional components and shell: Opadry white - 7 mg (macrogol 400 - 0.6 mg, hypromellose - 4.2 mg, titanium dioxide - 2.2 mg, polysorbate 80 - 0.1 mg), magnesium stearate - 3.5 mg, calcium hydrogen phosphate dihydrate - 317.75 mg, sodium carboxymethyl starch (type A) - 5.95 mg.
Pharmacological properties
Pharmacodynamics
The active ingredient of Paxil is paroxetine, an antidepressant, the effect of which is due to the specific inhibition of serotonin reuptake in the neurons of the brain.
Paroxetine has a low affinity for muscarinic cholinergic receptors. Its anticholinergic properties, according to animal studies, are weak. In vitro studies have shown that the substance has a weak affinity for alpha1-, alpha2- and beta-adrenergic receptors, as well as for serotonin 5-HT1- and 5-HT2-, histamine (H1) and dopamine (D2) receptors. The lack of interaction with postsynaptic receptors in vitro was confirmed by in vivo studies, in which it was found that paroxetine does not have the ability to inhibit the central nervous system (CNS) and cause the development of arterial hypotension. Paxil does not violate the psychophysical functions of a person, does not enhance the depressing effect of ethanol on the central nervous system.
Paroxetine is a selective serotonin reuptake inhibitor (SSRI) that, when administered to animals previously treated with tryptophan or monoamine oxidase inhibitors, causes symptoms of 5-HT receptor overstimulation.
In the study of behavior and changes in the electrocardiogram (ECG), it was found that the drug has weak activating effects if used in doses that exceed those required to inhibit serotonin reuptake. Its activating properties are not amphetamine-like in nature.
Animal studies show that paroxetine has no effect on the cardiovascular system. In healthy volunteers, it does not cause clinically significant changes in blood pressure, heart rate and ECG.
When Paxil is taken in the morning, paroxetine does not adversely affect sleep duration or sleep quality. Moreover, as the clinical effect of the drug manifests itself, sleep may improve. In the case of additional use of a short-acting hypnotic, side effects, as a rule, do not occur.
In the first few weeks of treatment, Paxil effectively reduces symptoms of depression and suicidal thoughts. According to the results of studies that lasted 1 year, the drug effectively prevents relapses of depression.
In controlled clinical trials for the treatment of depression in children aged 7 to 17 years, the efficacy of paroxetine has not been proven. However, Paxil is effective in patients in this age group in the treatment of obsessive-compulsive disorder.
It has been found that the addition of Paxil to cognitive behavioral therapy in adult patients with panic disorder significantly increases the effectiveness of treatment.
Studies have shown that paroxetine is able to slightly inhibit the hypotensive effect of guanethidine.
Pharmacokinetics
When Paxil is taken internally, paroxetine is well absorbed in the gastrointestinal tract (GIT). During the first passage through the liver, it undergoes metabolism, as a result of which a smaller amount of the drug enters the systemic circulation compared to that which is absorbed from the gastrointestinal tract.
With an increase in the concentration of paroxetine in the case of repeated administration of usual doses or a single administration of a large dose, the metabolic pathway of the first passage is partially saturated, and the clearance of the substance from the plasma decreases. As a result, the concentration of the drug increases disproportionately. Thus, the pharmacokinetic parameters of paroxetine are unstable, and its kinetics is not linear. However, nonlinearity is usually weak and is observed only in patients who, when taking Paxil in low doses, have low plasma concentrations of paroxetine.
Time to reach equilibrium plasma concentration is 7-14 days. The active substance of the drug is well distributed in tissues. According to pharmacokinetic calculations, only 1% of the total paroxetine present in the human body remains in plasma.
When Paxil is taken in therapeutic doses, the connection of paroxetine with plasma proteins is high - about 95%. There was no connection between the concentration of the drug in the blood plasma and its clinical properties (efficacy and side effects).
In small amounts, paroxetine penetrates into embryos and fetuses of laboratory animals, as well as into the breast milk of women.
Biotransformation by oxidation and methylation results in the formation of inactive polar and conjugated products.
The half-life (T 1/2) may differ in different patients, usually 16-24 hours. The drug is excreted: with urine - about 64% in the form of metabolites, no more than 2% unchanged; with feces - the rest in the form of metabolites, no more than 1% unchanged. Excretion of metabolites is biphasic in nature, including primary metabolism (first phase) and systemic elimination.
Indications for use
- Depression of all types, including severe and reactive depression, and depression with anxiety. In terms of effectiveness, the action of Paxil is similar to tricyclic antidepressants. There is evidence that it gives good results in patients with the ineffectiveness of standard antidepressant treatment. With prolonged therapy, Paxil is effective in preventing recurrence of depression;
- Panic disorder with and without agoraphobia - as a means of supportive and preventive therapy; the drug is most effective when used in combination with cognitive-behavioral treatment;
- Obsessive-compulsive disorder (OCD) - as supportive and preventive therapy; Paxil is effective when used prophylactically to prevent relapse;
- Social phobia - as a supportive and preventive therapy;
- Generalized anxiety disorder - as long-term supportive and preventive therapy; Paxil is effective in preventing relapse;
- Post-traumatic stress disorder - treatment.
Contraindications
- Combined use with methylene blue, pimozide, thioridazine and monoamine oxidase inhibitors (with the latter, an interval of at least 14 days must be observed);
- Age up to 18 years - with depression, up to 8 years - with social phobia, up to 7 years - with obsessive-compulsive disorder;
- Hypersensitivity to drug components.
If it is necessary to use Paxil for pregnant women, as well as when planning pregnancy, it is recommended to consider the possibility of prescribing an alternative treatment.
Instructions for use of Paxil: method and dosage
Paxil tablets should be taken orally, without chewing, whole, preferably in the morning at the same time as eating.
Adults are advised to observe the following dosing regimen (daily dose with a frequency of taking 1 time per day):
- Depression: 20 mg (starting dose). If necessary, it is possible to gradually increase the dose (10 mg 1 time in 7 days) until the maximum - 50 mg is reached. Evaluation of the effectiveness of Paxil for dose adjustment should be performed after 2-3 weeks of therapy. The duration of the course is determined by the indications (up to several months);
- Panic disorder: 10 mg (starting dose). If necessary, it is possible to gradually increase the dose (10 mg 1 time in 7 days) to the recommended or maximum (40/60 mg). The duration of the course is several months or longer;
- OCD: 20 mg (starting dose). If necessary, it is possible to gradually increase the dose (10 mg 1 time in 7 days) to the recommended or maximum (40/60 mg). The duration of the course is several months or longer;
- Social phobia, generalized anxiety and post-traumatic stress disorder: 20 mg (starting dose). If necessary, a phased increase in the dose (10 mg 1 time in 7 days) up to 50 mg is possible.
After the end of therapy, in order to reduce the likelihood of a withdrawal syndrome, the dose of the drug must be reduced in stages until it reaches 20 mg - 10 mg per week. After 7 days, Paxil can be completely canceled. If withdrawal symptoms are observed with dose reduction or after drug withdrawal, it is advisable to resume therapy at the previously prescribed dose, and then reduce the dose more slowly.
In elderly patients, therapy should be started with the recommended starting dose, which can be gradually increased to 40 mg per day. Patients with severe functional impairment of the kidneys (creatinine clearance less than 30 ml per minute) should be prescribed reduced doses (in the lower part of the therapeutic range).
Children 7-17 years old with obsessive-compulsive disorder and children 8-17 years old with social phobia at the beginning of treatment Paxil is prescribed in a daily dose of 10 mg. If necessary, the dose is increased by 10 mg weekly. The maximum allowable daily dose is 50 mg.
Side effects
The frequency and intensity of some of the following disorders associated with taking Paxil may decrease as therapy continues. In this case, drug withdrawal is usually not required.
During treatment, the following side effects may occur (> 1/10 - very often;> 1/100, 1/1000, 1/10 000, <1/1000 - rarely; <1/10 000, taking into account individual cases - very seldom):
- Respiratory system: often - yawning;
- Nervous system: often - dizziness, tremors, headache; infrequently - extrapyramidal disorders; rarely - akathisia, convulsions, restless legs syndrome; very rarely - serotonin syndrome (in the form of hallucinations, agitation, confusion, increased sweating, hyperreflexia, myoclonus, tachycardia with tremors and tremors); in rare cases, with simultaneous use with antipsychotics or impaired motor functions - extrapyramidal symptoms, incl. orofacial dystonia;
- Cardiovascular system: infrequently - postural hypotension, sinus tachycardia;
- Hepatobiliary system: rarely - an increase in the level of liver enzymes; very rarely - liver failure and / or hepatitis, accompanied in some cases by jaundice; sometimes - increased levels of liver enzymes; in very rare cases (based on the results of post-marketing observations) - liver damage (in the form of liver failure and / or hepatitis, sometimes with jaundice);
- Hematopoietic system: infrequently - abnormal bleeding, mainly in the mucous membranes and skin (in most cases - bruising); very rarely - thrombocytopenia;
- Gastrointestinal tract: very often - nausea; often - dry mouth, vomiting, diarrhea, constipation; very rarely - gastrointestinal bleeding;
- Immune system: very rarely - allergic reactions (including angioedema, urticaria);
- Psyche: often - agitation, insomnia, drowsiness, unusual dreams (including nightmares); infrequently - hallucinations, confusion; rarely - manic reactions (these disorders can also be associated with illness);
- Urinary system: rarely - urinary retention, urinary incontinence;
- Endocrine system: very rarely - syndrome of impaired secretion of antidiuretic hormone;
- Nutrition and metabolism: often - decreased appetite, increased cholesterol; rarely - hyponatremia (in most cases - in elderly patients);
- Vision: often - blurred vision; infrequently - mydriasis; very rarely - acute glaucoma;
- Reproductive system and mammary glands: very often - sexual dysfunction; rarely - hyperprolactinemia / galactorrhea;
- Subcutaneous tissue and skin: often - sweating; infrequently - skin rashes; very rarely - severe skin reactions, photosensitivity reactions;
- Others: often - weight gain, asthenia; very rarely - peripheral edema.
When you cancel taking Paxil, the following disorders may develop:
- Often: sleep disturbances, anxiety, sensory disturbances, headache, dizziness;
- Uncommon: confusion, diarrhea, nausea, sweating, agitation, tremors.
Taking Paxil in children can lead to the following side effects: emotional lability (including suicidal attempts and thoughts, mood swings, self-harm, tearfulness), sweating, hyperkinesia, decreased appetite, hostility, agitation, tremor.
Overdose
According to the available information on overdose, due to its high therapeutic index, paroxetine has a wide range of safety.
Symptoms: increased side effects, fever, dilated pupils, vomiting, involuntary muscle contractions, changes in blood pressure, tachycardia, anxiety, agitation. The condition of patients usually stabilized without serious complications even with a single dose of up to 2000 mg. Some reports describe the development of ECG changes and coma. Fatalities are very rare and were noted, as a rule, in situations where patients took Paxil simultaneously with other psychotropic drugs or alcohol.
There is no specific antidote to paroxetine. Standard measures are taken in case of overdose of any antidepressant. If necessary, gastric lavage is performed, activated charcoal is prescribed (20–30 mg every 4–6 hours on the first day after taking an extremely high dose of Paxil) and supportive therapy. Constant monitoring of vital body functions is required.
special instructions
In patients at a young age, especially during the treatment of major depressive disorders, taking Paxil may increase the risk of developing suicidal behavior.
An exacerbation of symptoms with depression and / or the emergence of suicidal thoughts and suicidal behavior may occur regardless of whether the patient is receiving antidepressants. The likelihood of their development remains until the onset of pronounced remission. Due to the fact that the improvement of the condition of patients, as a rule, occurs after several weeks of taking Paxil, during this period they need to ensure careful monitoring of the condition, especially at the beginning of the treatment course.
It should be borne in mind that in other mental disorders for which Paxil is indicated, there is also a high risk of suicidal behavior.
In some cases, most often in the first few weeks of therapy, the use of the drug can lead to akathisia (manifests itself in the form of internal anxiety and psychomotor agitation, when the patient cannot be in a calm state - to sit or stand).
Disorders such as agitation, akathisia or mania can be manifestations of the underlying disease or develop as a side effect of taking Paxil. Therefore, in cases where the existing symptoms worsen, or with the development of new ones, it is necessary to consult a specialist for advice.
Sometimes, most often during combined use with other serotonergic drugs and / or neuroleptics, it is possible to develop serotonin syndrome or symptoms that are similar to neuroleptic malignant syndrome. If symptoms such as autonomic disorders, myoclonus, hyperthermia, muscle stiffness appear, accompanied by rapid changes in the indicators of vital functions, as well as changes in mental status, including confusion and irritability, treatment is canceled.
Major depressive episodes are in some cases the initial manifestation of bipolar disorder. It is believed that Paxil monotherapy may increase the likelihood of accelerated development of a manic / mixed episode in patients at risk of developing this condition. Before prescribing Paxil to assess the risk of developing bipolar disorder, a thorough screening should be performed, including a detailed psychiatric family history with data on cases of depression, suicide and bipolar disorder. Paxil is not intended for the treatment of a depressive episode in bipolar disorder. It should be used with caution in patients with anamnestic data indicating the presence of mania. Also, the appointment of the drug requires caution against the background of epilepsy, angle-closure glaucoma, predisposing diseases to bleeding,including the use of substances / drugs that increase the likelihood of bleeding.
The development of withdrawal symptoms (in the form of suicidal thoughts and attempts, mood swings, nausea, tearfulness, nervousness, dizziness, pain in the abdomen) does not mean that Paxil is addictive or abused.
If convulsive seizures develop during treatment, Paxil is discontinued.
Influence on the ability to drive vehicles and complex mechanisms
Due to the existing risk of side effects on the part of the psyche and the nervous system, patients must be especially careful while working with mechanisms and when driving vehicles.
Application during pregnancy and lactation
In animal studies, no teratogenic or selective embryotoxic activity of paroxetine has been identified. According to data from a small number of women who received paroxetine during pregnancy, the drug did not increase the risk of developing congenital anomalies in children. There are reports of preterm birth in women who received paroxetine or other drugs from the SSRI group during pregnancy, but a causal relationship with the intake of an antidepressant has not been established.
There are also known individual cases of development in newborns whose mothers in the third trimeter of pregnancy took paroxetine or other SSRIs, the following clinical complications: difficulties with eating, vomiting, instability of body temperature, respiratory distress, constant crying, drowsiness, lethargy, irritability, tremors, tremors, convulsive seizures, hyperreflexia, apnea, cyanosis, hypoglycemia, arterial hypertension / hypotension. In some reports, symptoms have been described as neonatal withdrawal symptoms. In most cases, these disorders occurred immediately after childbirth or soon after (within 24 hours). However, it is worth noting that, in this case, the causal relationship of the described complications with antidepressant therapy has not been established.
Thus, during pregnancy, Paxil can be used only if the expected benefits are higher than the possible risks. Newborns whose mothers have taken paroxetine during pregnancy (especially in later stages) should be closely monitored.
Paroxetine penetrates into breast milk in insignificant quantities, however, during lactation, it is not recommended to use Paxil, unless the expected benefit of therapy is higher than the potential risks.
Pediatric use
Paroxetine is not recommended for children under 7 years of age, as no studies have been conducted on its effectiveness and safety.
In clinical trials in children and adolescents aged 7–17 years, adverse events associated with hostility (mainly aggression, anger, deviant behavior) and suicidality (suicidal thoughts and actions) were observed more often than in children who received placebo. There are currently no data on the long-term safety of paroxetine for children and adolescents with regard to growth, maturation, behavioral and cognitive development.
According to the instructions, Paxil is prohibited for use under the age of 18 for depression, up to 8 years for social phobia, and up to 7 years for obsessive-compulsive disorder.
With impaired renal function
In severe renal dysfunction (creatinine clearance <30 ml / min), the concentration of paroxetine in the plasma increases, therefore it is recommended to prescribe Paxil in the lowest therapeutic dose; treatment should be carried out under close medical supervision.
For violations of liver function
In case of impaired liver function, the concentration of paroxetine in the plasma increases, therefore it is recommended to prescribe Paxil in the lowest therapeutic dose, the treatment should be carried out under close medical supervision.
Use in the elderly
In elderly patients, an increase in the plasma concentration of paroxetine is possible, but the concentration range coincides with that in younger patients. Therefore, correction of the initial dosage regimen of Paxil is not required; if necessary, the daily dose can be increased to 40 mg.
Drug interactions
Absorption (absorption) and pharmacokinetics of Paxil when taking alcohol, food, digoxin, antacids, propranolol does not change, however, it is not recommended to consume alcoholic beverages during therapy.
With the combined use of Paxil with certain substances / drugs, the following effects may develop:
- Pimozide: its blood level rises, the QT interval lengthens (such a combination of drugs is contraindicated; if combined use is necessary, care must be taken and careful monitoring of the condition must be carried out);
- Serotonergic drugs (including lithium, triptans, fentanyl, L-tryptophan, SSRI drugs, tramadol and herbal remedies containing perforated St. John's wort): the likelihood of developing serotonin syndrome increases (the combined use of Paxil with monoamine oxidase inhibitors and linezolid is contraindicated);
- Ritonavir and / or fosamprenavir: the concentration of Paxil in the blood plasma is significantly reduced;
- Inhibitors and enzymes that take part in the metabolism of drugs: the pharmacokinetics and metabolism of paroxetine changes;
- Drugs that are metabolized by the hepatic enzyme CYP2D6 (tricyclic antidepressants, thioridazine, perphenazine and other neuroleptic drugs of the phenothiazine series, atomoxetine, risperidone, flecainide, propafenone and some other class 1 C antiarrhythmics): their concentration in plasma increases;
- Procyclidine: its concentration in blood plasma increases (with the development of anticholinergic effects, its dose should be reduced).
Analogs
Paxil's analogues are: Paroxetine, Paroxin, Plizil N, Reksetin, Adepress.
Terms and conditions of storage
Keep out of reach of children at temperatures up to 30 ° C.
The shelf life is 3 years.
Terms of dispensing from pharmacies
Dispensed by prescription.
Reviews about Paxil
Reviews of Paxil on specialized medical forums are contradictory. Some patients describe it as an effective drug that helped them cope with depression, improved sleep, normalized mood and literally brought them back to life. Other patients write that Paxil not only did not help, but, on the contrary, worsened the state of depression and caused side effects in the form of mental depression, apathy, and uncontrollable anger. Many complain about the development of withdrawal syndrome after the end of the course of treatment.
The high cost of the drug, which many consider unjustified, is also considered a significant disadvantage.
The price of Paxil in pharmacies
Approximate prices for Paxil (20 mg tablets): pack of 30 pcs. - 670–710 rubles, pack of 100 pcs. - 1960–2125 rubles.
Paxil: prices in online pharmacies
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Anna Kozlova Medical journalist About the author
Education: Rostov State Medical University, specialty "General Medicine".
Information about the drug is generalized, provided for informational purposes only and does not replace the official instructions. Self-medication is hazardous to health!
