PLIZIL PILLS 20MG

Dosage form

Tablets, film coated from yellow to orange, round, engraved with “ROT 20” on one side and risky on both sides.

Composition

1 pill contains paroxetine mesylate 25.83 mg, which corresponds to a paroxetine content of 20 mg.

Excipients: anhydrous Calcium hydrophosphate, sodium carboxymethyl starch, Magnesium stearate.

The composition of the film shell: lactose monohydrate, hypromellose, titanium dioxide (E171), macrogol 4000, iron oxide yellow (E172), iron oxide red (E172).

Packaging

In carton packaging 30 pills of 20 mg.

Mechanism of action

Antidepressant. Paroxetine is a potent and selective serotonin reuptake inhibitor (5-hydroxytryptamine, 5-HT) brain neurons, which determines its antidepressant effect and effectiveness in treating obsessive-compulsive and panic disorder. The major metabolites of paroxetine are polar and conjugated oxidation and methylation products, which are rapidly excreted from the body, have weak pharmacological activity and do not affect the therapeutic effect. When paroxetine is metabolized, the selective capture of 5-HT neurons due to its action is not disturbed.

Paroxetine has a low affinity for m-cholinergic receptors.

Having a selective effect, unlike tricyclic antidepressants, paroxetine is characterized by a low affinity for α1, α2, β-adrenergic receptors, as well as dopamine, 5-HT1-like, 5-HT2-like and histamine H1-receptors. Paroxetine does not violate the psychomotor functions and does not potentiate the inhibitory effect of ethanol on them. Unlike antidepressants that inhibit norepinephrine uptake, paroxetine suppresses the antihypertensive effects of guanethidine much less.

Suction.

After oral administration, paroxetine is well absorbed from the gastrointestinal tract. Metabolized by "first pass" through the liver.

Distribution.

Css is achieved by 7-14 days after the start of treatment, the pharmacokinetics during long-term treatment does not change. The clinical effects of paroxetine (side effects and effectiveness) do not correlate with its concentration in plasma. Paroxetine is extensively distributed in the tissues, and pharmacokinetic calculations show that only 1% of it is present in the plasma. At therapeutic concentrations, the binding of paroxetine to plasma proteins is 95%.

Metabolism.

Since the metabolism of paroxetine includes the "first passage" through the liver, its amount, determined in the systemic circulation, is less than that absorbed from the gastrointestinal tract. With an increase in the dose of paroxetine or with repeated use, when the load on the body increases, there is a partial absorption of the effect of "first pass" through the liver and a decrease in the plasma clearance of paroxetine.As a result, it is possible to increase the concentration of paroxetine in the plasma and fluctuations in pharmacokinetic parameters, which can be observed only in those patients who, when taking the drug in low doses, achieve low concentrations of paroxetine in the plasma.

Inference.

T1 / 2 varies, but usually is about 16-21 hours. Excretion of paroxetine metabolites is bi-phase, first as a result of metabolism during the first passage through the liver, and then it is controlled by systemic elimination. Paroxetine is excreted primarily in the form of metabolites: 64% of metabolites are excreted in the urine and 36% through the intestine, probably, in the bile. Unchanged, less than 2% is excreted in the urine and less than 1% in the bile.

Indications and usage

Depression of various etiologies, obsessive compulsive states, panic disorders.

Contraindications

• simultaneous administration of MAO inhibitors and a period of up to 14 days after their withdrawal;
• pregnancy;
• lactation period (breastfeeding);
• children and adolescents under the age of 18 years (efficacy and safety have not been established);
• hypersensitivity to the drug.

The drug should be prescribed with caution in case of hepatic and renal failure, angle-closure glaucoma, prostatic hyperplasia, mania, heart disease, epilepsy (with unstable epilepsy, the drug should be avoided), convulsive states, during electropulse therapy, when taking drugs that increase the risk of bleeding, in the presence of risk factors for increased bleeding and diseases that increase the risk of bleeding; elderly patients.

Pregnancy and Breastfeeding

The drug is contraindicated in pregnancy and lactation (breastfeeding).

Dosage and administration

The drug is taken orally 1 time / day. in the morning while eating. The pill is swallowed whole with water. The dose is selected individually during the first 2-3 weeks after the start of therapy and subsequently adjusted if necessary.

Depressed the drug is prescribed in a dose of 20 mg 1 time / day. If necessary, gradually increase the dose by 10 mg / day. The maximum daily dose is 50 mg, depending on the response of the patient.

In obsessive compulsive disorders The initial therapeutic dose is 20 mg / day., followed by a weekly increase of 10 mg. The recommended average therapeutic dose is 40 mg / day. if necessary, the dose can be increased to 60 mg / day.

For panic disorders the drug is prescribed in the initial dose of 10 mg / day. (to reduce the possible risk of exacerbation of panic symptoms), followed by a weekly increase of 10 mg. The average therapeutic dose is 40 mg / day. The maximum dose is 50 mg / day.

Socio-anxiety disorders / social phobia: The initial dose is 20 mg / day. If there is no effect for at least 2 weeks, it is possible to increase the dose to a maximum of 50 mg / day. The dose should be increased by 10 mg at intervals of at least 1 week in accordance with the clinical effect.

With post-traumatic mental disorders for most patients, the initial and therapeutic doses are 20 mg / day. In some cases, it is recommended to increase the dose of paroxetine to a maximum of 50 mg / day. The dose should be increased by 10 mg every week in accordance with the clinical effect.

With generalized anxiety disorders Initial and recommended doses - 20 mg / day.

With renal and / or liver failure The recommended daily dose is 20 mg.

For elderly patients daily dose should not exceed 40 mg.

The dose of the drug should be evaluated and, if necessary, adjusted within 2-3 weeks at the beginning of therapy, and then as needed. Patients should continue treatment for a period sufficient to relieve symptoms for at least 4-6 months after recovery from depression and more if they have obsessive-compulsive and panic disorders. As with many other psychotropic drugs, abrupt withdrawal of the drug is not recommended.

Paroxetine in children not recommended because its safety efficacy in this population has not been established.

Adverse reactions

From the side of the central nervous system: drowsiness, tremor, asthenia, insomnia, dizziness, fatigue, convulsions, extrapyramidal disorders, hallucinations, mania, confusion, agitation, anxiety, depersonalization, panic attacks, nervousness, paresthesia, decreased ability to concentrate, serotonin syndrome.

Musculoskeletal system: arthralgia, myalgia, myopathy, myasthenia.

From the senses: visual impairment, change in taste.

Urogenital: urinary retention, increased urination, impaired sexual function, including impotence and ejaculation disorders, decreased libido, anorgasmia.

From the digestive system: decreased appetite, nausea, vomiting, dry mouth, constipation, or diarrhea; very rarely - hepatitis.

Cardiovascular: orthostatic hypotension.

Dermatological reactions: ecchymosis, increased sweating.

Allergic reactions: rash, urticaria, pruritus, angioedema.

Other: violation of ADH secretion, hyperprolactinemia / galactorrhea, hyponatremia, withdrawal syndrome with the abrupt cancellation of the drug.

Precautions should be prescribed the drug to patients receiving antipsychotic drugs (neuroleptics), in order to avoid the development of NNS. Plizil should be prescribed no earlier than 2 weeks after discontinuation of MAO inhibitors.

During the first few weeks of taking the drug, the patient’s condition should be carefully monitored due to possible suicidal attempts, because at this time, the adequate therapeutic effect of paroxetine is not yet achieved. Treatment with Plizil should be discontinued when seizures develop, as well as at the first symptoms of mania.

During the treatment period, patients with diabetes mellitus in some cases require dose adjustment of insulin and / or oral hypoglycemic drugs.

In elderly patients, hyponatremia is possible.

Influence on ability to drive motor transport and control mechanisms. Plizil does not impair cognitive and psychomotor functions, however, as with other psychotropic drugs, patients should refrain from driving and engaging in potentially hazardous activities that require increased concentration and psychomotor reactions.

Eating and antacid agents does not affect the absorption and pharmacokinetic parameters of the drug. Paroxetine is incompatible with MAO inhibitors, thioridazine.

With simultaneous appointment with paroxetine increases the concentration of procyclidine.

During the period of treatment, the patient should refrain from drinking alcohol, due to the possible increased toxic effect of ethanol.

When used simultaneously with liver enzyme inducers / inhibitors, changes in the metabolism and pharmacokinetics of paroxetine are possible.

Because inhibition of paroxetine isozymes of cytochrome P450 may enhance the effect of barbiturates, phenytoin, anticoagulants, tricyclic antidepressants (nortriptyline, Amitriptyline, imipramine, desipramine and fluoxetine), phenothiazine neuroleptics (thioridazine) and antiarrhythmics of class 1 P (including propafenone), Metoprolol and increased risk of side effects while prescribing these medicines.

If administered concurrently with drugs that inhibit liver enzymes, a reduction in the dose of paroxetine may be required.

Paroxetine increases bleeding time while taking Warfarin, while the prothrombin time does not change.

At simultaneous appointment of paroxetine with atypical antipsychotics, phenothiazines, tricyclic antidepressants, Acetylsalicylic acid, NSAIDs, caution is advised due to possible bleeding disorders.

With simultaneous appointment with serotonergic drugs (tramadol, sumatriptan) may increase serotonergic effect.

With simultaneous use, mutual enhancement of the action of tryptophan, lithium preparations and paroxetine was noted (as with the appointment of other selective serotonin reuptake inhibitors). Joint reception with lithium preparations should be carried out under the control of their concentration of lithium in the blood plasma. Not recommended for joint appointment with drugs containing tryptophan.

With the use of paroxetine (as well as other selective serotonin reuptake inhibitors) with neuroleptics, it is possible to develop NNS.

With the simultaneous appointment of paroxetine with phenytoin and other anticonvulsants, a decrease in the concentration of paroxetine in the plasma and an increase in the frequency of side effects is possible.

Symptoms: nausea, vomiting, tremor, dry mouth, dilated pupils, fever, changes in blood pressure, headache, involuntary muscle contraction, agitation, anxiety, sinus tachycardia, sweating, drowsiness, nystagmus, bradycardia, nodal rhythm.In very rare cases, while taking with other psychotropic drugs and / or alcohol, changes on the ECG, coma are possible.

Treatment: gastric lavage, the appointment of Activated carbon . If necessary, symptomatic therapy. There is no specific antidote.

List B. In a dry place, at a temperature not higher than 30 ° C.

3 years

Plizil