Index of drugs

Treatment: major depressive episode, obsessive-compulsive disorder, panic disorder with or without agoraphobia, social phobia, generalized anxiety disorder, post-traumatic stress disorder.

1 tabl powl. contains 20 mg of paroxetine in the form of a hydrochloride semiplatelet. The preparation contains lactose.

Antidepressant - a strong and selective serotonin reuptake inhibitor in brain neurons. Paroxetine has a low affinity for cholinergic muscarinic receptors, for α receptors₁, α₂ and β-adrenergic, dopaminergic receptors (D2), 5HT₁-like 5-HT₂ and histamine (H₁). This lack of interaction with postsynaptic receptors has been reflected in researchin vivothat showed no depressive effect on o.u.n. and no hypotensive effect. The drug is well absorbed from the digestive tract and is subject to first-pass metabolism. In the case of a greater load on the body, following the administration of a higher single dose or multiple doses, partial absorption of the first pass effect and decreased plasma clearance result in a disproportionate increase in paroxetine concentration. Dynamic balance is achieved within 7-14 days of starting treatment. Paroxetine undergoes extensive tissue distribution, only 1% of paroxetine present in the body is found in plasma. At therapeutic concentrations, approximately 95% of the drug binds to plasma proteins. The main metabolites of paroxetine are polar and conjugated oxidation and methylation products, which are easily excreted and have no pharmacological activity. Less than 2% of the dose of paroxetine administered is excreted unchanged in the urine and about 64% of the dose in the form of metabolites. About 36% of the dose is excreted in the faeces, probably through bile, of which unchanged paroxetine accounts for less than 1%. Excretion of metabolites is two-phase. Initially, it is the result of first-pass metabolism, and later associated with the systemic elimination of paroxetine. T_0,5 it is variable, but is usually about 1 day.

Hypersensitivity to paroxetine or to any of the excipients. Paroxetine is contraindicated for concomitant use with MAO inhibitors. Under exceptional circumstances, linezolid (an antibiotic that is a reversible, non-selective MAO inhibitor) can be administered in combination with paroxetine, as long as it is possible to closely observe the symptoms of serotonin syndrome and control blood pressure. Treatment with paroxetine can be started: 2 weeks after the end of irreversible MAO inhibitors; at least after 24 hours from the end of the use of reversible MAO inhibitors (eg moclobemide, linezolid, methylthioninium chloride (methylene blue, a color used for pre-operative visualization, being a reversible, non-selective MAOI) From the moment of discontinuation of paroxetine treatment to another MAO inhibitor At least one week should be taken Paroxetine should not be used together with thioridazine - paroxetine may increase thioridazine plasma concentrations. Administration of thioridazine alone may lead to QTc prolongation and associated severe ventricular arrhythmias, such astorsade de pointesand sudden death. Paroxetine should not be used together with pimozide.

The drug should not be used in children and adolescents under 18 years of age. In clinical trials with children and adolescents treated with antidepressants, suicide-related behaviors (suicide attempts and suicidal thoughts) and hostility (mostly aggression, opposing behavior and anger) were observed more frequently than in patients receiving placebo. If a decision to use the drug is made in connection with the clinical indication, the patient should be closely monitored for signs of suicide. In addition, long-term safety data in children and adolescents regarding growth, maturation and development of cognitive and behavioral abilities are lacking.Depression is accompanied by an increased risk of suicidal thoughts, self-harm and suicide (suicide related events). The risk persists until significant remission occurs. Patients should be closely monitored until improvement occurs and in the early stages of recovery (increased risk of suicide). Patients with other than depression should be treated with similar precautions when treating patients with a major depressive episode. It is known that patients with a history of suicide or a significant degree of suicidal ideation are at greater risk of suicidal thoughts or attempted suicide prior to commencement of treatment and should be closely monitored during treatment, particularly in patients below 25 years of age. Close observation of patients, especially those at increased risk, should accompany treatment especially in the initial phase and after dose adjustment. In patients who develop symptoms of akathisia, increasing the dose may be harmful. If symptoms of serotonin syndrome or neuroleptic malignant syndrome occur, treatment with paroxetine should be discontinued and symptomatic supportive treatment initiated. Due to the risk of serotonin syndrome, paroxetine should not be used in combination with serotonin precursors (such as L-tryptophan, oxytryptan). Caution should be exercised when using paroxetine in patients with a history of mania. Paroxetine should be discontinued in any patient who begins the manic phase. Caution is advised in patients with severe renal insufficiency or hepatic insufficiency. Treatment of patients with diabetes with SSRIs may change the degree of glycemic control - adjustment of insulin dose and / or oral antidiabetic agents may be required. Caution should be exercised when using paroxetine in patients with epilepsy. The drug should be discontinued in any patient who has had a seizure. There is little clinical experience regarding the concomitant use of paroxetine and electroconvulsive therapy. Paroxetine may cause mydriasis; it should be used with caution in patients with narrow-angle glaucoma or glaucoma. Normal precautions should be observed in patients with cardiac disorders. Precautions should be taken in patients at risk for hyponatremia, e.g. due to concomitant medications and liver cirrhosis. Because of the risk of abnormal bleeding, caution should be exercised when administering SSRIs with oral anticoagulants, platelets or other drugs that may increase the risk of bleeding (eg atypical antipsychotics, such as clozapine, phenothiazines, most tricyclic drugs). antidepressants, Acetylsalicylic acid, NSAIDs, COX-2 inhibitors), as well as in patients with a history of bleeding or conditions that may predispose to bleeding. Avoid using paroxetine during treatment with tamoxifen. The preparation contains lactose - should not be used in patients with rare hereditary galactose intolerance, lactase deficiency (Lapp type) or malabsorption of glucose-galactose.

Paroxetine should be used during pregnancy only when there are strict indications for its use. The prescribing doctor should consider the possibility of alternative treatment for pregnant women or those planning to become pregnant. Avoid sudden interruption of treatment during pregnancy. Some epidemiological results indicate an increased risk of malformations, in particular of the circulatory system (eg ventricular defects or atrial septum) associated with the use of paroxetine in the third trimester of pregnancy. Newborns should be observed whose mothers continued to take paroxetine in late pregnancy, especially in the third trimester. When the mother uses paroxetine in late pregnancy, the following symptoms may occur in the newborn: respiratory distress syndrome, cyanosis, apnea, fits, temperature fluctuations, feeding difficulties, vomiting, hypoglycaemia, hypertonia, hypotonia, hyperreflexia, tremor, nervousness, irritability, lethargy, constant crying, drowsiness and difficulty sleeping.The above symptoms may be caused both by serotoninergic effects and discontinuation of the drug. In most cases, complications appear immediately or soon (<24 hours) after delivery. Epidemiological data indicate that the use of SSRI during pregnancy, especially in late pregnancy, may increase the risk of persistent pulmonary hypertension in the newborn (PPHN). Small amounts of paroxetine are excreted in human milk. Paroxetine should not be used during lactation unless the expected benefit to the mother justifies the potential risk to the child. As no effects on the infant are to be expected, breast-feeding may be considered. Paroxetine may affect the quality of semen; this action is reversible. No effects on human fertility have been observed so far.

Very common: nausea, sexual dysfunction. Common: decreased appetite, increased cholesterol, drowsiness, insomnia, agitation, sleep disturbances (including nightmares), dizziness, tremor, headache, decreased concentration, blurred vision, yawning, constipation, diarrhea, vomiting, dry mucous membrane mouth, sweating, asthenia, weight gain, dizziness, disturbances of sensation, sleep disturbances, anxiety, headache. Uncommon: abnormal bleeding, usually affecting the skin and mucous membranes (most likely ecchymosis), confusion, hallucinations, extrapyramidal symptoms, mydriasis, sinus tachycardia, transient decrease or increase in blood pressure, hypotension associated with tilting the body, rash, pruritus, urinary retention , urinary incontinence, agitation, nausea, tremors, confusion, sweating, emotional instability, blurred vision, palpitations, diarrhea, irritability. Rare: hyponatraemia (mainly in elderly patients and sometimes associated with the syndrome of inappropriate antidiuretic hormone secretion), manic reactions, anxiety, depersonalization, panic attacks, akathisia, convulsions, restless legs syndrome, bradycardia, increased liver enzymes, joint pain, pain muscle, hyperprolactinemia and (or) milking. Very rare: thrombocytopenia, allergic reactions (including urticaria and angioneurotic edema), syndrome of abnormal secretion of antidiuretic hormone (ADH), serotonin syndrome (symptoms may include: agitation, confusion, excessive sweating, hallucinations, hyperreflexia, muscle climacteric convulsions, chills, tachycardia and tremor), acute glaucoma, gastrointestinal bleeding, abnormal liver function (such as hepatitis, sometimes associated with jaundice and / or liver failure), serious skin-related adverse events (including erythema multiforme, Stevens-Johnson syndrome and toxic epidermal necrolysis), hypersensitivity to light, priapism, peripheral edema. Not known: suicidal thoughts and suicidal behavior, tinnitus. Data from epidemiological studies, mainly in patients aged 50 and older, indicate an increased risk of bone fractures in patients taking SSRIs and TCAs. The mechanism leading to this risk is unknown. Discontinuation of treatment with paroxetine (especially sudden) often leads to withdrawal symptoms: dizziness, sensory disturbances (including paresthesia, feelings of electric shock and tinnitus), sleep disturbances (including intense dreams), agitation or anxiety, nausea, tremors, confusion, sweating, headaches, diarrhea, palpitations, emotional instability, irritability and blurred vision. Adverse reactions observed in pediatric clinical trials: increased suicidal behavior (including suicidal ideation and attempts), self-harm and increased hostility (suicidal thoughts and attempts were mainly observed in clinical studies involving adolescents with major depressive disorder; increased hostility occurred especially in children with obsessive-compulsive disorders, especially in children under 12 years of age). In addition, events such as decreased appetite, tremor, sweating, hyperkinesia, agitation, emotional instability (including crying and mood swings) were observed, adverse events associated with bleeding, especially from the skin and mucous membranes.Events observed after discontinuation or reduction of paroxetine dose are: emotional instability (including crying, mood swings, self-injury, suicidal thoughts and attempts), nervousness, dizziness, nausea and abdominal pain.

Orally. Adults.Major depressive episodesThe recommended dose is 20 mg daily. In general, the improvement of the patient's condition begins after one week, but can be seen only from the second week of treatment. Dosage should be reviewed and, if necessary, adjusted to clinical needs within 3 to 4 weeks of starting treatment, and then re-evaluated and modified based on the results of treatment. In some patients with a 20 mg reaction, the dose may be increased by 10 mg depending on the patient's response, up to a maximum dose of 50 mg per day. Patients with depression should be treated for a sufficiently long period of at least 6 months to be sure that symptoms have subsided.Obsessive-compulsive disorderThe recommended dose is 40 mg daily. Patients should start treatment with 20 mg daily; the dose may be increased by 10 mg gradually to the recommended dose. If, after several weeks of using the recommended dose, the response to treatment is insufficient, some patients may benefit from a gradual increase in the dose up to a maximum dose of 60 mg per day. Patients with obsessive-compulsive disorder should be treated for a sufficiently long period to ensure that the symptoms have disappeared. Treatment can last several months or even longer.Panic disorderThe recommended dose is 40 mg daily. Treatment should start with a dose of 10 mg daily and increase it by 10 mg increments depending on the patient's response to the recommended dose. Starting treatment with a low starting dose is recommended to minimize the risk of exacerbating the symptoms of panic disorder, which is generally recognized to occur at the beginning of the treatment of the disease. If, after several weeks of using the recommended dose, the observed response to treatment is insufficient, some patients may benefit from a gradual increase in the dose up to a maximum dose of 60 mg per day. Patients with panic disorder should be treated for a sufficiently long time to ensure that the symptoms have subsided. Treatment can last several months or even longer.Social phobiaThe recommended dose is 20 mg daily. If, after several weeks of using the recommended dose, the observed response to treatment is inadequate, some patients may benefit from a gradual increase in the dose by 10 mg up to a maximum dose of 50 mg per day. Long-term therapy should be evaluated regularly.Generalized anxiety disorderThe recommended dose is 20 mg daily. If, after several weeks of using the recommended dose, the observed response to treatment is inadequate, some patients may benefit from a gradual increase in the dose every 10 mg up to a maximum dose of 50 mg per day. Long-term therapy should be evaluated regularly.Post-traumatic stress disorderThe recommended dose is 20 mg daily. If, after several weeks of using the recommended dose, the observed response to treatment is inadequate, some patients may benefit from a gradual increase in the dose every 10 mg up to a maximum dose of 50 mg per day. Long-term therapy should be evaluated regularly. In elderly patients, the starting dose should start with the starting dose recommended in adults; some patients may find it useful to increase the dose, but the maximum dose should not exceed 40 mg per day. In patients with severe renal impairment (creatinine clearance less than 30 ml / min) or in patients with hepatic impairment, the dosage should be limited to the lower dose range. The drug should be administered in the morning, during a meal. The tablet should be swallowed whole, not chewed.