Sierestill - instructions for use, dose, side effects, contraindications

Excipients: hydroxypropyl betacode (hydroxypropyl-beta-cyclodextrin), sucrose, anise flavoring (ethyl alcohol, water, natural anethole), sodium benzoate, purified water.

Description:

A clear, colorless or slightly pink solution with a characteristic taste of anise.

Pharmacotherapeutic group:antidepressant.

ATX: & nbsp

N.06.A.B Selective serotonin reuptake inhibitors

N.06.A.B.05 Paroxetine

Pharmacodynamics:

Paroxetine is a potent and selective inhibitor of the capture of 5-hydroxytryptamine (5-HT, serotonin) by neurons of the brain, which determines its antidepressant effect and effectiveness in the treatment of obsessive-compulsive (OCD) and panic disorder.

The main metabolites of paroxetine are polar and conjugated products of oxidation and methylation, which are rapidly excreted from the body, have weak pharmacological activity and do not affect its therapeutic effect. In the metabolism of paroxetine, the selective uptake of 5-HT neurons due to its action is not impaired.

Paroxetine has low affinity for muscarinic cholinergic receptors. Having selective action, in contrast to tricyclic antidepressants, paroxetine showed a low affinity for α-1, α-2, β-adrenoreceptors, as well as for dopamine, 5-HT1 like, 5-HT2-like and histamine (H1) receptors. Paroxetine does not violate psychomotor functions and does not potentiate the inhibitory effect of ethanol on them.

According to the behavioral and EEG studies, paroxetine reveals weak activating properties when it is administered at doses higher than those required to inhibit 5-HT capture. In healthy volunteers, it does not cause a significant change in blood pressure, heart rate and EEG.

In contrast to antidepressants, which inhibit the seizure of norepinephrine, paroxetine much weaker suppresses the antihypertensive effects of guanethidine.

Pharmacokinetics:

Paroxetine is well absorbed after ingestion and is metabolized first pass through the liver. Excretion of unchanged paroxetine in the urine is usually less than 2% of the dose, with metabolites accounting for about 64% of the dose. The intestine excretes about 36% of the dose, probably through bile, in which the unchanged paroxetine is less than 1% of the dose. In this way, paroxetine is excreted mainly as a result of metabolism.

Excretion of metabolites of paroxetine from the body is 2-phase, first as a result of metabolism of the first passage through the liver, and then it is controlled by systemic elimination.The half-life period varies, but usually is about one day. Stable systemic concentrations are achieved by 7-14 days after the start of treatment, and pharmacokinetics during prolonged treatment does not change. The clinical effects of paroxetine (side effect and efficacy) do not correlate with its concentration in the plasma.

Since the metabolism of paroxetine involves the stage of the first passage through the liver, its quantity, determined in the systemic circulation, is less than that which is absorbed from the gastrointestinal tract. With an increase in the dose of paroxetine or with multiple dosing, when the load on the body increases, a partial absorption of the effect of the first "passage through the liver" occurs and a decrease in the plasma clearance of paroxetine. As a result, an increase in the plasma paroxetine concentration and fluctuations in the pharmacokinetic parameters is possible, which can be observed only in those patients who, when taking low doses, reach low plasma levels of the drug. Paroxetine extensively distributed in tissues, and pharmacokinetic calculations show that only 1% of it is present in the plasma, and at therapeutic concentrations 95% is associated with plasma proteins.

In elderly patients, as well as in severe renal and hepatic insufficiency, the concentration of paroxetine in plasma is increased, and the range of plasma concentrations practically coincides with the range in healthy adult volunteers.

Indications:

- depression of all types, including reactive, severe endogenous depression and depression, accompanied by anxiety;

- obsessive-compulsive disorder (OCD);

- panic disorder, including agoraphobia;

- social anxiety disorder / social phobia;

- generalized anxiety disorder;

Contraindications:

- hypersensitivity to the components of the drug, including sucrose;

- simultaneous administration with MAO inhibitors and within 14 days after their cancellation;

- unstable epilepsy;

- pregnancy and lactation;

- children under 18 years of age

Carefully:liver failure; kidney failure; angle-closure glaucoma; hyperplasia of the prostate; mania; pathology of the heart; epilepsy; convulsive conditions; the appointment of electropulse therapy; taking drugs that increase the risk of bleeding; presence of risk factors for increased bleeding and diseases that increase the risk of bleeding.

Dosing and Administration:

The bottle is equipped with a dispensing cap-pipet, tared to extract 0.5 ml, 1 ml, 1.5 ml, 2 ml of a solution corresponding to 10. 20. 30. 40 drops, respectively.

1 ml of solution corresponds to 20 drops, which is equivalent to 10 mg of paroxetine.

One drop corresponds to 0.5 mg of paroxetine.

Drops are taken orally, once a day, in the morning, while eating. Dilute the drops with water. The dose is selected individually during the first two to three weeks after the start of therapy and is subsequently adjusted if necessary.

With depression - 20 mg once a day. If necessary, the dose is gradually increased by 10 mg / day, the maximum daily dose should not exceed 50 mg.

With obsessively-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 may be increased to 60 mg / day.

In panic disorders the initial dose is 10 mg / day (to reduce the possible risk of developing panic symptoms), followed by a weekly increase of 10 mg. The average therapeutic dose is 40 mg / day.The maximum dose is 60 mg / day.

Socially-disturbing disorders / social phobia: the initial dose is 20 mg per day, in the absence of effect for at least two weeks, an increase in the dose to a maximum of 50 mg per day is possible. The dose should be increased by 10 mg at intervals of at least a week in accordance with the clinical effect.

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

Generalized anxiety disorders: the initial and recommended dose is 20 mg per day, in the absence of effect for at least two weeks, an increase in the dose to a maximum of 50 mg per day is possible. The dose should be increased by 10 mg at intervals of at least a week in accordance with the clinical effect.

With renal and / or hepatic insufficiency the recommended dose is 20 mg per day.

For elderly patients daily dose should not exceed 40 mg.

In order to prevent the development of withdrawal syndrome, the discontinuation of taking the drug is carried out gradually.

Paroxetine application in children is not recommended, since its safety and effectiveness in this population are not established.

Side effects:

From the sidess nervous system: drowsiness or insomnia, tremor, asthenia, dizziness, extrapyramidal disorders, serotonin syndrome, manic disorders, confusion, agitation, anxiety, depersonalization, paresthesia, increased nervous excitability, rarely hallucinations, convulsions.

From the sides: the musculoskeletal system: arthralgia, myalgia, myasthenia gravis, myoclonia, myopathic syndrome.

From the sidess sense organs: change of taste, impaired vision.

From the genitourinary system: violations of sexual function, including impotence and disorders ejaculation, decreased libido, urinary retention, increased urination, hyperprolactinaemia / galactorrhea, anorgasmia.

From the side digestive system: decreased or increased appetite, nausea, vomiting, dry mouth, constipation or diarrhea, in very rare cases - hepatitis.

From the side, the cardiovascular system: orthostatic hypotension.

Other: rhinitis, increased sweating, allergic reactions (rash, urticaria, ecchymatosis, itching, angioedema, hyponatremia, impaired secretion antidiuretic hormone, withdrawal syndrome with a drastic withdrawal of the drug (dizziness, sensory disturbances (paresthesia, sensations resembling exposure to electric current), sleep disorder, psychomotor agitation, anxiety, nausea and sweating).

Overdose:

Symptoms: nausea, dilated pupils, fever, changes in blood pressure, headache, involuntary muscle contractions, agitation, anxiety, tachycardia. In rare cases, with simultaneous reception with other psychotropic drugs and / or alcohol, changes in the electrocardiogram, coma are possible.

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

Interaction:

The intake of food and antacid agents does not affect the absorption and pharmacokinetic parameters of the drug.

Paroxetip is incompatible with MAO inhibitors.

With simultaneous administration with paroxetine, the concentration of procyclidine increases. During therapy with paroxetine, one should refrain from taking alcohol because of the increased toxic effect of alcohol.

In connection with the death of the paroxetine cytochrome P450, the effect of the effect of barbiturium, phenytoin, indirect anticoagulants, tricyclic antidepressants, phenotyzatic antipsychotics and antiarrhythmics of the class 1C, metoprolol and an increased risk of developing side effects with the simultaneous administration of these medicines.

At simultaneous appointment with the preparations, inhibiting enzymes of a liver, the dose of paroxetine can be required.

Paroxep increases the time of bleeding against the background of taking warfarin, with the same prothrombin time.

With the simultaneous administration of paroxetine with atypical antipsychotic agents, phenothiazines, tricyclic antidepressants, acetylsalicylic acid, nonsteroidal anti-inflammatory agents, caution should be exercised in connection with possible bleeding disorders.

Simultaneous appointment with serotonergic drugs (tramadol, sumatriptan) can lead to an increase in the serotonergic effect.

Mutual enhancement of the action of tryptophan, lithium and paroxetine preparations was noted.

When simultaneous the administration of paroxetine with phenytoin and other anticonvulsants may reduce the concentration of paroxetine in the plasma and increase the incidence of side effects.

Special instructions:

To avoid development of a malignant neuroleptic syndrome with caution prescribed to patients taking antipsychotics.

Treatment with suxetine is prescribed 2 weeks after the abolition of MAO inhibitors.

In elderly patients, hyponatremia is possible.

In thethecases require correction of the dose of insulin and / or oral hypoglycemic drugs.

With the development of seizures, paroxetine treatment is discontinued.

When the first signs of mania should be canceled therapy with paroxetine.

During the first few weeks, the patient's condition should be carefully monitored in connection with possible suicidal attempts.

Effect on the ability to drive transp. cf. and fur:

Paroxetype does not impair cognitive and psychomotor functions, however, as with other psychotropic medications, patients should be careful when driving and moving machinery.

During the treatment period, one should refrain from using ethanol and from practicing potentially dangerous activities,requiring increased concentration of attention, rapidity of psychomotor reactions.

Form release / dosage:

Drops for ingestion 10 mg / ml in a bottle of dark glass type III with aluminum with a cap, covered from the inside with polyethylene. Each 30 ml bottle or 60 ml complete with a dosing lid-pipet, removal of the aluminum cap, and instructions for use in cardboard pack. Dosing pipette made of transparent glass type III is tared to extract 0.5 ml, 1 ml, 1.5 ml, 2 ml of a solution, corresponding to 10, 20, 30, 40 drops, respectively.

Packaging:(1) - bottles of dark glass (1) / complete with a pipette / - packs of cardboard

Storage conditions:

Store at a temperature not exceeding 25 ° C, in the place protected from light.

Store 30 days after first opening vial.

Keep out of the reach of children.

Shelf life:3 years. Not use the product with expired shelf life.

Terms of leave from pharmacies:On prescription

Registration number:LSR-000834/08

Date of registration:18.02.2008

The owner of the registration certificate:Italfarmaco SpAItalfarmaco SpA Italy

Manufacturer: & nbsp

ITALFARMACO, S.p.A. Italy

Representation: & nbspITALFARMAKO SpA ITALFARMAKO SpA Italy

Information update date: & nbsp21.08.2015

Illustrated instructions

Instructions

Searestill (Serestill)