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Paxil

Information about the drug Paxil, 20mg tablet number 30

Pharmacological effect of Paxil

Antidepressant. Refers to a group of selective serotonin reuptake inhibitors. The mechanism of action Paxila based on its ability to selectively block the reuptake Serotonin (5HT) presynaptic membrane, what has caused this increase in free content neurotransmitter in the synaptic cleft and enhancing serotoninergic actions in the CNS, responsible for the development timoanalepticheskogo (antidepressant) effect. Paroxetine has low afffinitetom to the m-cholinergic receptors, a-and b-adrenoreceptors, as well as dopamine, 5HT1-like, 5HT2-like and histamine H1-receptors. According to the study of behavior and EEG of paroxetine revealed weak activating properties when it is administered in doses higher than those required to inhibit the capture of 5HT. Y healthy volunteers, it does not cause significant changes in the level of blood pressure, heart rate and EEG. The main constituents of the profile of psychotropic activity Paxila are antidepressant and protivotrevozhnoe a moderate stimulatory effect (activated) effect.

Pharmacokinetics Paxil

After receiving Paxila inside paroxetine is well absorbed from the gastrointestinal tract. Food intake did not affect the absorption. Css is set to the 7-14 day since the start of therapy. Clinical effects of paroxetine (Side effects and efficacy) did not correlate with its concentration in plasma. Paroxetine is extensively distributed in tissues, and pharmacokinetic calculations indicate that only 1% of its present in plasma, and in therapeutic concentrations in 95% associated with protein form. The major metabolites of paroxetine are polar and conjugated products of oxidation and methylation. Due to the low pharmacological activity of metabolites, their effects on therapeutic efficacy is unlikely. Because the metabolism of paroxetine includes the step of first passage through the liver, it amount, as determined in the systemic circulation is less than that which is absorbed from the gastrointestinal tract. When increasing the dose of paroxetine or multiple dosing, when the load on the organism, there is partial absorption of the effect of the first passage through the liver and decreased plasma clearance of paroxetine. As a result, may increase the concentration of paroxetine fluctuations in the plasma and pharmacokinetic parameters that can be observed only in those patients, who when taking low doses of reach of low levels of the drug in plasma. Excreted in the urine (as unchanged - less than 2% of the dose in the form of metabolites - 64%) or bile (Unchanged - 1%, as metabolites - 36%). T1 / 2 varies, but averages 16-24 hours Excretion of paroxetine is biphasic in nature, including the primary metabolism (first phase) and following the systemic elimination of them. With long-term continuous employment drug pharmacokinetic parameters were not changed. Pharmacokinetics in special clinical situations In elderly patients, as well as for violations expressed in liver and kidney function, the concentration paroxetine in plasma increased, and the range of plasma concentrations had almost identical to range of healthy adult volunteers.

Indications for use of the drug Paxil, 20mg tablet number 30

Depression of all types, including reactive depression, severe depression and endogenous depression accompanied by anxiety (the results of studies in which patients received drug for up to 1 year show that it is effective in preventing recurrence depression); - Obsessive-compulsive disorder (OCD) (proved to preserve the efficacy of the drug in the treatment of OCD for at least 1 year and in preventing recurrence ROC); - Panic disorder with agoraphobia and without it (the effectiveness of the drug remains in 1 year, preventing relapse of panic disorder); - Social anxiety disorder / social phobia (efficacy is preserved under long-term treatment of this disorder); - Generalized anxiety disorder (efficacy persists during long-term treatment of this disorder); - Post Traumatic Stress Disorder.

Dosing regimen of the drug Paxil, 20mg tablet number 30

When depression is the average therapeutic dose is 20 mg / day. In case of insufficient effective dose may be increased to a maximum of 50 mg / day. Increasing the dose should be spent gradually - by 10 mg at intervals of 1 week. Paxila dose should be reviewed and if necessary, to change within 2-3 weeks of therapy and continue until obtain an adequate clinical effect. For obsessive-compulsive disorder, the average therapeutic dose is 40 mg / day. To start treatment should be with 20 mg / day, then gradually increase the dose of 10 mg every week. In case of insufficient clinical effect dose may be increased to 60 mg / day. In panic disorder average therapeutic dose is 40 mg / day. Treatment should be start with the drug at a dose of 10 mg / day. The drug used in a low initial dose with To minimize the possible risk of exacerbation of panic symptoms, which may occur in the initial phase of therapy. In a subsequent dose increase to 10 mg weekly until effect. In case of insufficient effective dose can be increased to 60 mg / day. In social anxiety disorder / social phobia average therapeutic dose is 20 mg / day. In case of insufficient clinical effect dose may be increased gradually to 10 mg weekly to 50 mg / day. When generalized anxiety disorder average therapeutic dose is 20 mg / day. In case of insufficient clinical effect dose may be increased gradually to 10 mg weekly to a maximum dose of 50 mg / day. Post-traumatic stress disorder, the average therapeutic dose is 20 mg / day. In case of insufficient clinical effect dose may be increased gradually to 10 mg weekly maximum of 50 mg / day. In elderly patients treatment should begin with a starting dose for adults, what dose may be increased to 40 mg / day. In patients with severe liver and kidney function (creatinine clearance below 30 ml / min) dose should be lowered to the bottom of the range of doses. The course of treatment must be long enough. Patients with depression or OCD should receive treatment for a period of time sufficient for the disappearance of all symptoms. This period can take several months for depression, while OCD and panic disorder - more long term. Paxil taken 1 time per day in the morning with food. Tablet should be swallowed whole, without chewing, drinking water.

Side effects of the drug Paxil, 20mg tablet number 30

Side effects of the drug Paxil, 20mg tablet number 30, as a rule, moderately expressed. When continuation of therapy side effects are reduced in intensity and frequency of occurrence and usually do not lead to the cessation of treatment. From the digestive system: nausea, dry mouth, constipation, diarrhea, decreased appetite, increase in liver enzymes, very rarely - hepatitis, liver failure. The nervous system: drowsiness, tremor, fatigue, insomnia, dizziness, agitation, reduction of concentration, anxiety, rarely - serotonin syndrome, confusion consciousness, convulsions, and in rare cases - extrapyramidal disorders with oro-facial dystonia (patients with movement disorders or those taking antipsychotics). On the part of the vision: rarely - acute glaucoma, in rare cases - blurred vision. With the urinary system: rarely - retention of urine, frequent urination. Cardio-vascular system: transient increase or decrease in blood pressure (usually patients with hypertension and anxiety), rarely - sinus tachycardia, peripheral edema. From the blood coagulation system: rarely - thrombocytopenia, increased bleeding and skin mucous membranes (ecchymosis). On the part of the endocrine system: rarely - gipoprolaktinemiya / galactorrhea and hyponatremia (mostly in older patients), which is sometimes caused by inadequate secretion syndrome antidiuretic hormone. Allergic reactions: seldom - angioedema, hives, skin rash. Other: increased sweating, ejaculation disorders, rarely - photosensitivity reaction.

Contraindications of the drug Paxil, 20mg tablet number 30

Concomitant use of MAO inhibitors and the period of 14 days after their withdrawal; - Concomitant use of thioridazine; - Concomitant use of drugs containing tryptophan; - Pregnancy; - Lactation (breastfeeding); - Hypersensitivity to paroxetine and other ingredients.

Pregnancy and lactation

Health & Safety Paxila during pregnancy has not been studied, so it should not be used during pregnancy and lactation (breastfeeding), except in cases where a medical point of view of the potential benefits of treatment outweigh the risks associated with drug intake.

Cautions Paxil

The drug should be used with caution in hepatic failure, renal disease, angle-closure glaucoma, prostatic hyperplasia, maniyah, pathology heart, epilepsy, convulsive states, in the presence of risk factors for increased bleeding and predisposing to this disease, in combination with cardioversion and with oral anticoagulants. With a sharp lifting Paxila may develop symptoms such as dizziness, paresthesia, sleep disturbances, agitation, anxiety, nausea and sweating. If the observed against the background of Paxila increase in liver enzymes retained long, the drug should be discontinued. Paxil did not potentiate the effect of alcohol on psychomotor function, however patients taking Paxil, should refrain from drinking alcohol. Use in pediatrics The use of paroxetine in children is not recommended, since safety and efficacy of its use in children have not been established. Effects on ability to drive vehicles and management mechanisms Paxilom therapy does not cause cognitive impairment, or psychomotor retardation. None However, as in the treatment of any psychotropic drugs, patients should exercise caution while driving and working with moving machinery.

An overdose of the drug Paxil, 20mg tablet number 30

Symptoms: increased above side effects, as well as vomiting, headache, increased pupils, fever, change in blood pressure, involuntary muscle contractions, agitation, anxiety, tachycardia. Patients usually do not develop serious complications, even when taking 200 mg paroxetine. Sometimes it develops a coma and EEG changes, very rarely occurs fatal the combined use of paroxetine with psychotropic drugs with alcohol or without it. Treatment: Standard measures used with an overdose of antidepressants (purification stomach by vomiting or artificial irrigation, the appointment of 20-30 mg of activated charcoal every 4-6 hours during the first days after the overdose). The specific antidote is known. Requires careful monitoring and control of vital functions.

Drug Interactions Paxil

Absorption and pharmacokinetics of paroxetine did not change at all or changes only partially under the influence of food, antacids, digoxin, propranolol and ethanol. Combined therapy with drugs Paxila lithium should be undertaken with caution and under supervision lithium concentration in the blood, as experience combined use of paroxetine and lithium is limited. Metabolism and pharmacokinetic parameters Paxila may change while the application drugs that induce or inhibit the protein metabolism. While the application Paxila with drugs that inhibit the metabolism of enzymes (cimetidine), the dose should confined to the lower boundary of the normal level. The combined use of drugs, induce metabolism enzymes (carbamazepine, phenytoin, sodium valproate) is not required changes in the initial dose Paxila. Subsequent dose adjustments should be made depending on clinical effect. While the application Paxila with drugs metabolized by cytochrome P450 CYP2D6 (tricyclic antidepressants (amitriptyline, nortriptyline, imipramine, desipramine), fenotiazinovyh neuroleptics (thioridazine, perphenazine), and class IC antiarrhythmic drugs (Propafenone, flecainide) and metoprolol) marked increase in their concentrations in blood plasma. Paxila combination with terfenadine and other drugs that are substrates for the isoenzyme CYP3A4, does not cause adverse reactions. The simultaneous use of Paxila with MAO inhibitors, tryptophan can cause the development serotonin syndrome, which manifests itself agitation, anxiety, disorders of the gastrointestinal tract, including diarrhea. Daily appointment Paxila significantly increases protsiklidina in plasma. In the presence of anticholinergic symptoms protsiklidina dose should be reduced. In the interaction Paxila with warfarin may increase bleeding time when unaltered prothrombin time. Paxil did not potentiate the action of ethanol on psychomotor function, however patients taking Paxil, should refrain from taking etanolsoderzhaschih drugs. Unlike antidepressants, which inhibit the capture of norepinephrine, paroxetine much suppresses the weaker antihypertensive effects guanetidina.