Last Updated on February 19, 2017 by Dr.Derek Fhisher

Paxil Paroxetine 10, 20, 30, 40, 12,5, 25, 37,5 mg
Most popular brand: Paxil
Active ingredient: Paroxetine
Available dosage forms: 10, 20, 30, 40, 12,5, 25, 37,5 mg
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Paroxetine general information

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Active – active substance / start: Paroxetine

Adepress; Aktaparoksetin; Apo – Paroxetine; Paxil; Paroxetine; Paroxetine hydrochloride; pliz; Reksetin; Sirestill.

Paroxetine – an antidepressant, selective serotonin reuptake inhibitor. It is used in depressive states of various etiologies (reactive depression, dysthymia, atypical depression, postpsihoticheskih depression), obsessive – compulsive disorder (obsessions syndrome), panic disorder (agoraphobia, social phobia), etc. .

Active – active substance:
Paroxetine / Paroxetine.

Dosage Forms:
Tablets.

Paroxetine

Properties / Action:
Paroxetine – is an antidepressant. It belongs to the group of selective inhibitors of reverse neuronal capture of serotonin in the central nervous system. It has a complex bicyclic structure different from that of other known antidepressants.
The main components of psychotropic activity profile of paroxetine are antidepressant and antianxiety (anxiolytic) action at a sufficiently pronounced stimulatory (activates) the effect. Furthermore, paroxetine causes reduction obsessive – compulsive disorders.
The mechanism of action of paroxetine based on its ability to selectively block the reuptake of serotonin (5HT) presynaptic membrane, what has caused the increase of the free content of this neurotransmitter in the synaptic cleft and enhancing the action of serotonin in the central nervous system, responsible for the development timoanalepticheskogo effect. Paroxetine is a potent and more specific blocker of serotonin reuptake among selective serotonergic antidepressant.
The effect of paroxetine on muscarinic, alpha – and beta – adrenergic receptors is insignificant, that determines the extremely weak intensity of anticholinergic, sedative and cardiovascular side effects. Paroxetine has little effect on the neuronal uptake of norepinephrine and dopamine as well.
In animal experiments paroxetine negative impact on reproduction and fetal development, as well as carcinogenic and mutagenic properties not found.

Pharmacokinetics:
Paroxetine after oral administration is well adsorbed. Simultaneous food intake does not affect the absorption and pharmacokinetics of paroxetine. Paroxetine binds to plasma proteins by 93 – 95%. Half-life varies but averages 16 – 24 hours. The equilibrium concentration is set to 7 – 14 day from the beginning of therapy. Prolonged continuous reception pharmacokinetics unchanged. Metabolized mainly in the liver to form predominantly inactive metabolites. The principal metabolites of paroxetine are polar and conjugated products of oxidation and methylation which are rapidly cleared. In view of their pharmacological activity the low impact on the therapeutic efficacy of paroxetine unlikely.
Less than 2% of the applied dose of paroxetine is released unchanged in the urine; the rest is allocated as metabolites or the urine (64%) or through the bile. In humans, urinary paroxetine is biphasic in nature, including the primary metabolism (first phase) and the subsequent systematic elimination.

Indications:

  • depressive conditions of various etiologies, including anxiety accompanied (reactive depression, dysthymia, atypical depression, depression or other postpsihoticheskih depression in schizophrenia, organic CNS disorders, alcoholism, etc.);
  • obsessive – compulsive disorder (obsessions syndrome);
  • panic disorder, including with the fear of staying in a crowd (agoraphobia);
  • social phobia;
  • Post-traumatic stress disorder.
    It is also used as part of anti-treatment.

    Dosage and administration:
    Paroxetine is assigned to a single daily dose (intake with food in the morning). Tablets should be swallowed whole, washed down with liquid water.
    Depression:
    The initial dose is 20 mg / day. The same dose is the optimal therapeutic. The effect develops more gradually. In case of insufficient effectiveness of the dose can be increased to 50 mg / day (maximum daily dose). Increasing the dose gradually carried – 10 mg at intervals of one week. For elderly and debilitated patients, as well as the presence of functional disorders of the liver and kidneys – starting dose is 10 mg / day, the maximum – 40 mg / day. The course of treatment should be long enough. To assess the effectiveness of therapy requires 6 – 8 weeks. The total duration of treatment is determined by the general rules for all antidepressants.
    Obsessive – compulsive disorder
    The initial dose is 20 mg / day. The dose may be increased to 10 mg / week to achieve a therapeutic response. The average therapeutic dose of 40 mg / day. The maximum daily dose is 60 mg.
    Panic disorder:
    Treatment should begin with 10 mg / day. Subsequently, the dose is increased by 10 mg weekly depending upon the therapeutic effect. The average therapeutic dose – 40 mg / day. A low starting dose is appointed in order to minimize the possible risk of worsening of panic symptomatology, which may occur in the initial phase of therapy. In case of insufficient effectiveness of the dose may be increased to 60 mg / day.
    Social phobia:
    With social phobia therapy can be initiated with a dose of 20 mg / day. If after two weeks of treatment, no significant improvement in the condition of the patient, the dose can be increased by 10 mg weekly until the desired effect. The maximum daily dose should not exceed 50 mg.
    Post-traumatic stress disorder:
    With PTSD the recommended therapeutic dose is 20 mg / day. The daily dose may be increased to 10 mg / week, the maximum daily dose is 50 mg.
    In order to prevent relapse:
    To prevent relapses necessary supportive therapy. For maintenance medication therapy is used in a dose of 20 mg / day. After the disappearance of the symptoms of depression, this course can be 4 – 6 months, and for panic disorders and obsessive – over 4 – 6 months. Avoid abrupt withdrawal of the drug.
    In frail and elderly patients the recommended starting dose is 10 mg / day. This dose can be increased by 10 mg weekly, depending on the patient. The maximum dose should not exceed 40 mg / day. In renal
    (CC less than 30 ml / min) or hepatic deficiency increases the concentration of paroxetine in blood plasma, therefore, the recommended daily dose is 20 mg in these cases. Depending on the condition of the patient the dose can be increased, however, should strive to keep it at a minimum.

    Overdose:
    The symptoms of paroxetine overdose include nausea, vomiting, tremors, dilated pupils, dry mouth, irritability, general excitement, sweating, drowsiness, dizziness, flushing of the skin. Experience overdose – described in patients who took 850 mg paroxetine alone or in combination with other drugs. Notification of change of ECG, coma or convulsive disorders associated with an overdose of paroxetine, are absent. No clinically relevant effects of an overdose in the long term was not observed.
    Treatment: gastric lavage, 20 – 30 g of activated charcoal every 4 – 6 hours for the first 24 – 48 hours is necessary to free the respiratory tract, conduct oxygenation if required. Monitor vital body functions and common activities aimed at maintaining them. Forced diuresis, hemodialysis or hemoperfusion are ineffective if a large dose of paroxetine came from the blood into the tissues. A specific antidote is not known.

    Contraindications:
    The existing hypersensitivity to paroxetine.
    Paroxetine should not be used in combination with monoamine oxidase inhibitors (MAOIs), and within two weeks after discontinuation of MAO inhibitors; later, at the beginning of treatment should be careful doses should gradually built up. MAO inhibitors should not be administered within two weeks of discontinuation of paroxetine.
    Pregnancy, lactation (breastfeeding).
    Children and teens under 18 years of age.

    Use during pregnancy and lactation:
    The safety of paroxetine in pregnant women has not been studied, so it should not be used during pregnancy and breast-feeding, except when medically the potential benefits of treatment exceed the possible risks associated with taking the drug.
    During the period of paroxetine women of childbearing age should avoid conception (use reliable methods of contraception).
    If necessary, the use of paroxetine during lactation should decide the issue of termination of breastfeeding.

    Side effects:
    Side effects of paroxetine are rare, their manifestations are minor and do not affect the social life of patients. The severity and frequency of side effects may decrease over time. Drug withdrawal, usually not required.
    From the digestive system: nausea; occasional constipation, diarrhea, loss of appetite; rarely – increased liver enzymes, severe impairment of liver function (connection to the intake of the drug has not been proven).
    From the CNS: drowsiness, tremor; weakness and fatigue; insomnia; in some cases – headache, irritability, paresthesia, somnabulizm; rarely – extrapyramidal disorders (mainly at the previous intensive use of neuroleptics), oro – facies dystonia, epileptiform seizures, increased intracranial pressure.
    On the part of the autonomic nervous system: increased sweating, dry mouth.
    From the senses: in some cases – blurred vision, mydriasis; rarely – an attack of acute glaucoma.
    Cardio – vascular system: in some cases – tachycardia, ECG changes, labile blood pressure, fainting.
    part of the reproductive and urinary system: ejaculation disorder, rarely – dysuria, in some cases – changes in libido.
    From the water – electrolyte balance: in some cases – hyponatremia (peripheral edema, impaired consciousness or epileptiform symptoms).
    Dermatological reactions: seldom – flushing of the skin, subcutaneous hemorrhage.
    Allergic reactions: rare – swelling of the face and limbs, urticaria, bronchospasm, angioedema, pruritus.
    Other: in rare cases – myopathy, myalgia, hyperglycaemia; rarely – gipoprolaktinemiya, galactorrhea, hypoglycemia, fever and flu-like syndrome develop. Rarely – thrombocytopenia (cause – effect relationship with the administration of the drug has not been proven), increased bleeding (ecchymosis and purpura), increased or decreased body weight.

    Special instructions and precautions:
    Before treatment is necessary to find out whether there was a history of episodes of mania or seizures. If the patient previously was in a manic state, while taking paroxetine, you should consider the possibility of occurrence of relapse. In the event while taking paroxetine epileptiform seizures, the drug should be discontinued.
    With care use in patients with disturbance of function of the cardio – vascular system, as well as patients simultaneously receiving oral anticoagulants, antipsychotics, digoxin.
    There is not enough experience of the simultaneous use of electroconvulsive therapy and paroxetine therapy.
    In connection with a predisposition to suicidal attempts in patients with depression and drug addiction in patients with abstinence during the treatment of these patients should be closely monitored.
    In many cases, while taking paroxetine was marked hyponatremia, especially in elderly patients receiving diuretics. After the abolition of paroxetine in blood sodium levels to normal. In some cases, this condition develops as a result of overproduction of antidiuretic hormone.
    It should be used with caution in glaucoma medication because Paroxetine causes mydriasis.
    Cause – effect relationship between the intake of paroxetine and the change in liver enzyme activity is not proven, but in the case of abnormal liver function is recommended discontinuation of paroxetine.
    It should be an exception drinking during the use of paroxetine.
    The sudden cancellation of paroxetine may cause dizziness, sensory disturbances (eg, paresthesias), anxiety, sleep disturbances, agitation, tremor, nausea, sweating, and confusion, so the termination of drug therapy must be carried out gradually, it is advisable to reduce the dose every second day.
    The clinical data on the efficacy and safety of the drug paroxetine have no children.

    Effects on ability to drive vehicles and management mechanisms:
    Controlled studies did not reveal any adverse effect of paroxetine on psychomotor or cognitive function. Despite this, at the beginning of therapy with paroxetine is not recommended to perform work that requires attention and speed of psychomotor reactions. limitation period is determined based on the individual patient’s response to the drug.

    Drug Interactions:
    Food and antacids do not affect the absorption and pharmacokinetics of paroxetine.
    With the simultaneous use of paroxetine with drugs that are actively binding to plasma proteins, may increase side effects.
    Not recommended simultaneous reception of tryptophan. Interaction with tryptophan can cause the development of “serotonin syndrome,” manifested agitation, anxiety and gastro – intestinal disorders, including diarrhea.
    With the combined use of paroxetine with sumatriptan th there is a general weakness, hyperreflexia, incoordination. If necessary, they simultaneous application should be particularly careful.
    Paroxetine does not potentiate the effect of alcohol on psychomotor functions however, patients taking paroxetine to refrain from drinking alcohol.
    Paroxetine does not increase the sedation and drowsiness associated with haloperidol but amilobarbitona or oxazepam.
    Animal studies have shown the possibility of interaction MAO inhibitors and paroxetine, so you should observe the following precautions.
    paroxetine significantly increases the concentration Procyclidine plasma, so the appearance of anticholinergic side effects should be reduced dose Procyclidine.
    Combined with lithium paroxetine therapy should be used with caution under the control of the blood lithium levels, due to insufficient clinical experience and available data on the cases of lithium interaction with other serotonin reuptake inhibitors.
    The combined use of paroxetine and phenytoin is associated with a decrease in the concentration of paroxetine and an increase in the number of adverse events. Concomitant use of paroxetine with other anticonvulsants may also cause an increase in the number of adverse events. In a joint application with phenobarbital paroxetine paroxetine reduced plasma concentration and shortened its T1 / 2.
    In the interaction of paroxetine with vafarinom may increase bleeding at constant prothrombin time. Paroxetine should be administered with caution to patients receiving oral anticoagulants.
    Concomitant use of paroxetine with drugs that are metabolized by the cytochrome system, can lead to an increase in their concentration in blood plasma. Paroxetine significantly inhibits isoenzyme CYP 2D6. It is recommended to reduce the dose or combined with others. Antidepressant (nortriptyline, amitriptyline. Imipramine. Desipramine, fluoxetine), phenothiazine derivatives (thioridazine), antiarrhythmics class I (propafenone. Flecainide, encainide), quinidine, cimetidine, codeine. In a joint application with cimetidine paroxetine paroxetine increases plasma level at the stage of dynamic equilibrium.
    In some cases was an increase in the concentration of theophylline in the blood as well. Despite the fact that in the course of clinical studies the interaction between paroxetine and theophylline is not proven, it is recommended regular monitoring of theophylline in the blood.

    Storage:
    The drug should be stored at a temperature of 15 ° to 30 ° C.
    The expiration date on the package.
    Terms of pharmacy holiday – Prescription.

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