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Active ingredients
Paroxetine
Release form
Pills
Composition
Active ingredient: Paroxetine. Concentration of active ingredient (mg): 20 mg
Pharmacological effect
The drug affects the central nervous system and is used to treat depression and related anxiety, as well as for the treatment of obsession, panic disorders, social phobia and post-traumatic stress disorders (for example, traffic accidents, injuries, natural disaster), as well as for the treatment of generalized anxiety frustration. The drug can be effectively used in agoraphobia (in the form of panic disorders, when the patient is afraid of the crowd). The concentration of serotonin in the body determines the mood of a person. Decreased serotonin levels in the brain can lead to depression. The active ingredient of the drug Rexetin normalizes the level of serotonin in the central nervous system. Lack of addiction to the drug means that you will not be dependent on the drug for its long-term use.
Pharmacokinetics
Absorption: After oral administration, paroxetine is well absorbed and undergoes primary metabolism. Due to the presystemic metabolism of the drug, the amount of active substance that has entered the systemic circulation is less than the amount of the drug that has been absorbed in the digestive tract, therefore, the absolute bioavailability is different. The use of higher single doses or repeated use leads to a partial saturation of the primary metabolism and a decrease in plasma clearance. Simultaneous administration of the drug with food does not affect its absorption and further drug pharmacokinetics. When taken regularly at a dose of 20 mg / day, the plasma concentration is 12–90 ng / ml (on average, 41 ng / ml), and the time to reach the maximum concentration is 3–7 hours (on average, 5 hours). Distribution: Paroxetine is extensively distributed in body tissues, including the central nervous system (the average volume of distribution is 10–20 l / kg, only 1% of the drug remains in the blood plasma). Paroxetine passes into breast milk and through the placenta. At therapeutic concentrations of paroxetine in the blood, binding to plasma proteins is 95%.No correlation was found between the plasma concentration of paroxetine and the clinical effect (side effects). Biotransformation: Paroxetine is metabolized mainly in the liver. The main metabolites are polarized and associated products of oxidation and methylation. The forms associated with the glucuronic acid or sulfate group predominate. The pharmacological activity of the main metabolite is about 1/50 of the activity of the parent compound: thus, the metabolite shows practically no biological activity. Paroxetine metabolism is associated with the cytochrome P450 2D6 system. Elimination: T1 / 2 paroxetine ranges from 6 to 71 hours, an average of about 1 day. Equilibrium plasma concentration is reached 7–14 days after the start of therapy, and the pharmacokinetics do not change with long-term therapy. About 64% of paroxetine is excreted in the urine (2% - unchanged, 62% - in the form of metabolites); approximately 36% - with feces (presumably with bile), mainly in the form of metabolites, less than 1% is excreted in feces in unchanged form.
Indications
Use strictly as prescribed by a doctor to avoid complications! Depression of various etiologies, including anxiety-related conditions. Obsessive compulsive disorder (obsessive syndrome). Panic disorders, including fear of being in a crowd (agoraphobia). Social phobia Generalized Anxiety Disorder (GAD). Post-traumatic stress disorder. It is also used as part of anti-relapse treatment.
Contraindications
Hypersensitivity to the components of the drug in history. Therapy with monoamino oxidase (MAO) inhibitors and the period after cessation of treatment with MAO inhibitors for two weeks. Pregnancy and lactation. The safety of paroxetine during pregnancy has not been studied, so it should not be used during pregnancy and lactation, except when medically the potential benefits of treatment outweigh the possible risk associated with taking the drug. Children's age up to 18 years (due to the lack of clinical experience).
Precautionary measures
The effect of the drug on the ability to drive and other mechanisms.At the beginning of treatment with Rexetin, you cannot drive a car or work on dangerous machines until your doctor has allowed it.
Use during pregnancy and lactation
If you are pregnant or breastfeeding, consult your doctor before taking the drug. If you take Rexetin and wish to become pregnant, consult a psychiatrist.
Dosage and administration
Rexetin should be taken once a day, preferably in the morning, during meals, without chewing. As with other antidepressants, depending on the clinical condition of the patient, the dosage of the drug can be changed after two to three weeks. For depressions, the recommended daily dose is 20 mg. As with the use of other antidepressants, the effect in most cases develops gradually. In some patients, you may need to increase the dose of the drug. Depending on the patient's response to therapy, the daily dose may be increased by 10 mg at intervals of one week, until a therapeutic effect is achieved. the maximum daily dose is 50 mg. In obsessive-compulsive disorders (obsessive syndrome), the initial dose is 20 mg per day. The dose may be increased by 10 mg weekly, until a desired therapeutic response is achieved. The maximum daily dose is usually 40 mg, but should not exceed 60 mg. For panic disorders, the recommended therapeutic dose is 40 mg per day. Therapy should be started with a small dose (10 mg per day), with a weekly increase in dosages by 10 mg per day until the desired effect is achieved. The maximum daily dose should not exceed 60 mg. The recommended low initial dose of the drug is due to the possibility of a temporary increase in the intensity of symptoms of the disease at the beginning of therapy. With social phobia therapy can be started with a dose of 20 mg per day. If after a two-week course of treatment there is no significant improvement in the patient's condition, the dose of the drug can be increased weekly by 10 mg to achieve the desired effect. The maximum daily dose should not exceed 50 mg. For maintenance therapy, a daily dose of 20 mg is usually sufficient. For generalized anxiety disorder: The recommended therapeutic dose is 20 mg per day.Depending on the patient's response to therapy, the daily dose may be increased gradually in 10 mg. the maximum daily dose is 50 mg. For post-traumatic stress disorders: The recommended therapeutic dose is 20 mg per day. Depending on the patient's response to therapy, the daily dose may be increased periodically by 10 mg, the maximum daily dose is 50 mg. Depending on the clinical condition of the patient, to prevent the possibility of relapse, it is necessary to carry out maintenance therapy. This course after the disappearance of the symptoms of depression can be 4-6 months, and with obsessive and panic disorders, and more. As with the use of other psychotropic drugs, you should avoid abrupt termination of the course of treatment. (See: Side Effects). In debilitated and elderly patients, the level of the drug in the serum may rise above the usual level, therefore the recommended initial dose is 10 mg per day. This dose can be increased by 10 mg weekly, depending on the condition of the patient. The maximum dose should not exceed 40 mg per day. Children due to lack of clinical experience the drug is not shown. With renal (creatinine clearance less than 30 ml per minute) or liver failure, the concentration of paroxetine in the blood plasma increases, therefore the recommended daily dose of the drug in these cases is 20 mg. This dose can be increased depending on the condition of the patient, but it is necessary to strive to keep the dose at the lowest possible level.
Side effects
The frequency of manifestation and intensity of side effects in the process of therapy is reduced, therefore, with their development, in most cases it is possible to continue taking the drug. Side effects on organs and systems (as a percentage of the detected ratio of the total number of patients receiving this treatment). On the part of the digestive tract, liver: Nausea (12%). sometimes constipation, diarrhea, loss of appetite. Rare increase in liver function tests. sometimes severe liver dysfunction. Between taking paroxetine and a change in the activity of liver enzymes, a causal relationship has not been proven, but in case of abnormal liver function, discontinuation of paroxetine is recommended. From the side of the central nervous system: Drowsiness (9%). tremor (8%).general weakness and fatigue (7%). insomnia (6%). in some cases, headache, irritability, paresthesia, dizziness, somnambulism. Extrapyramidal disorders and orofacial dystonia have rarely been observed. Extrapyramidal disorders occur predominantly in the prior intensive use of neuroleptics. Rarely observed epileptiform seizures, which is characteristic of treatment with other antidepressants. increased intracranial pressure. On the part of the autonomic nervous system: Increased sweating (9%), dry mouth (7%). From the senses: In some cases, visual disturbances, mydriasis. rarely an attack of acute glaucoma. Since the cardiovascular system: In some cases, described tachycardia, ECG changes, blood pressure lability, fainting. Genital and urinary system disorders: Ejaculation disorder (13%), in some cases, a change in libido, rarely difficulty urinating. Electrolyte imbalance: In some cases, marked hyponatremia with the development of peripheral edema, impaired consciousness or epileptiform symptoms. After discontinuation of the drug, the level of sodium in the blood is normalized. In some cases, this condition has developed due to overproduction of antidiuretic hormone. Most of these cases were observed in elderly patients who, in addition to paroxetine, received diuretic and other drugs. Dermatological and hypersensitivity reactions: In rare cases skin hyperemia, subcutaneous hemorrhages, edema in the face and extremities, anaphylactic reactions (urticaria, bronchospasm, angioedema), skin itch are described. Others: In isolated cases, myopathies, myalgia, hyperglycemia, rarely hyperprolactinemia, galactorrhea, hypoglycemia, fever and the development of a flu-like state were noted. Thrombocytopenia rarely develops, but a causal relationship with taking the drug has not been proven. Reception of paroxetine may be accompanied by an increase or decrease in body weight. Several cases of increased bleeding have been described (See Warnings). Paroxetine, compared with tricyclic antidepressants, is less likely to cause dry mouth, constipation and drowsiness.Sudden withdrawal of the drug can cause dizziness, sensitivity disorders (eg, paresthesia), fear, sleep disturbance, agitation, tremor, nausea, sweating and confusion, therefore, discontinuation of drug therapy should be made gradually, it is advisable to reduce the dosage every second day.
Overdose
The drug is well tolerated by patients, however, when taking the drug in a dose of more than 2000 mg or in combination with drugs that increase the plasma concentrations of paroxetine and its toxicity, the development of acute poisoning is possible. In patients with acute poisoning, nausea, vomiting, trembling of limbs, mydriasis, dry mouth are observed. In addition, there may be a state of excitement or, on the contrary, drowsiness, dizziness, reddening of the skin of the face and upper part of the body. With drug monotherapy, no effects that threaten the patient’s life were observed, even with a significant excess dose. There is no specific antidote. Symptomatic treatment. It is necessary to monitor vital functions, to ensure the airway is permeable. Showing gastric lavage, taking enterosorbents and oxygen therapy.
Interaction with other drugs
Always inform the doctor if you are taking other medications along with Rexetin, as this may significantly change the effectiveness of the drugs. Therefore, you can not take other medications without a doctor's prescription. We draw your attention to the fact that when a skin rash or shortness of breath appears, you should stop taking the drug and immediately consult a doctor. Taking Rexetin with food and drink. When treating Rexetin, alcohol should be avoided.
special instructions
The use of the drug in children and adolescents up to 18 years. Usually, Rexetin is not used to treat children and adolescents under 18 years of age. It is important to note that the use of drugs belonging to this group in patients under 18 years of age is accompanied by an increased risk of thoughts and attempts to commit suicide, as well as hostile behavior (characterized by rudeness, resistance, anger). Despite this, the doctor in the interests of the patient may appoint Rexetin patients under 18 years of age. If your doctor prescribed Rexetin to a patient under the age of 18 and you have any questions in this regard, then ask your doctor for any questions.Notify your doctor if a patient under 18 years old who is taking Rexetin develops or worsens the above symptoms. In addition, it should be noted that the effect of long-term administration of the drug Rexetin on the growth, development, behavior and thinking of children and adolescents in this age group has not yet been proven.