Selektra - instructions for use, doses, side effects, contraindications

Excipients: salted SMCC®90/HD90 73.71 mg (microcrystalline cellulose 72.24 mg + silicon dioxide 1.47 mg); sodium croscarmellose 4.5 mg, talc 4.5 mg, magnesium; stearate 0.9 mg;

film coating: opadrai white (Opadry 03F28446 White) about 2.7 mg: hypromellose 6 cp 1.64 mg, titanium dioxide 0.66 mg, macrogol 6000 0.4 mg.

1 tablet, film-coated, 10 mg contains:

active substance: escitalopram oxalate 12.78 mg corresponding to 10 mg escitalopram base;

Excipients: SMCC®90 / HD90 prosalt 147.42 mg (microcrystalline cellulose 144.47 mg + silicon dioxide 2.95 mg); sodium croscarmellose 9 mg, talc 9 mg, magnesium stearate 1.8 mg;

film coating: opada white (Opadry 03F28446 White) about 5.4 mg: hypromellose 6cP 3.29 mg, titanium dioxide 1.31 mg, macrogol 6000 0.8 mg.

1 tablet, film-coated, 15 mg contains:

active substance: escitalopram oxalate 19.17 mg corresponding to 15 mg escitalopram base;

Excipients: salted SMCC®90/HD90 221.13 mg (microcrystalline cellulose 216.71 mg + silicon dioxide 4.42 mg); sodium croscarmellose 13.5 mg, talc 13.5 mg, magnesium stearate 2.7 mg;

film coating: fall off white (Opadry 03F28446 White) about 18.1 mg: hypromellose 6 cp 4,931 mg, titanium dioxide 1.97 mg, macrogol 6000 1.2 mg.

1 tablet, film-coated, 20 mg contains:

active substance: escitalopram; oxalate 25.56 mg corresponding 20 mg escitalopram base;

Excipients: salted SMCC®90/HD90 294.84 mg (microcrystalline cellulose 288.94 mg + silicon dioxide 5.9 mg); sodium croscarmellose 18 mg, talcum 18 mg, magnesium stearate 3.6 mg;

film coating: opada white (Opadry 03F28446 White) about 10.8 mg: hypromellose 6cP 6.57 mg, titanium dioxide 2.63 mg, macrogol 6000 1.6 mg.

Description:

Tablets 5 mg: round biconvex tablets covered with a white film shell with an engraved 'E' on one side.

Tablets 10 mg: oval biconvex tablets coated with a white film shell, engraved with 'E' on the one hand, risky on the other side and lateral risks.

Tablets 15 mg: oval biconvex tablets coated with a white film shell with an engraved 'E' on the one hand, risk on the other hand and lateral risks.

Tablets of 20 mg: oval biconvex tablets coated with a white film shell with an engraved 'E' on the one hand, risk on the other hand and lateral risks.

Pharmacotherapeutic group:antidepressant

ATX: & nbsp

N.06.A.B.10 Escitalopram

Pharmacodynamics:

Escitalopram is an antidepressant, a selective serotonin reuptake inhibitor (SSRI). Inhibition of reuptake of serotonin leads to an increase in the concentration of this neurotransmitter in the synaptic cleft, enhances and prolongs its effect on postsynaptic receptor sites.

Escitalopram does not have at all or has a very weak ability to bind to a number of receptors, including: serotonin 5-HT_1A, 5-HT₂ receptors, dopamine D₁ and D₂receptors, α₁-, α₂-, β-adrenergic receptors, histamine H₁, muscarinic cholinergic, benzodiazepine and opiate receptors.

Pharmacokinetics:

Absorption is not dependent on food intake. Bioavailability of escitalopram is about 80%. The mean time to reach the maximum concentration in the blood plasma (T_mOh) is about 4 hours. Apparent volume of distribution (V_d_,_β/F) after oral administration is from 12 to 26 l / kg. The binding of escitalopram and its major metabolites to blood plasma proteins is about 80%. Escitalopram is metabolized in the liver to demethylated and demodetylated metabolites. They are both pharmacologically active. The basic substance and its metabolites are partially isolated in the form of glucuronides.

After repeated use, the average concentration of demethyl- and didemethyl metabolites is usually 28-31% and less than 5%, respectively, of the concentration of escitalopram. The biotransformation of escitalopram in the demethylated metabolite occurs mainly with the help of cytochrome CYP2C19. Some participation of isoenzymes is possible CYP3A4 and CYP2D6. In persons with weak activity CYP2C19 the concentration of escitalopram can be twice as high as in cases with high activity of this isoenzyme.Significant changes in drug concentration in cases with a weak isoenzyme activity CYP2D6 was not found.

Half-life (T_1/2) after repeated use is about 30 hours. The clearance for oral administration is about 0.6 l / min. The main metabolites of escitalopram have a longer half-life. Escitalopram and its main metabolites are excreted by the liver (the metabolic pathway) and the kidneys.

The kinetics of escitalopram are linear. The equilibrium concentration (C_ss) is reached after about 1 week. Average C_ss - 50 nmol / l (20 to 125 nmol / l) is achieved with a daily dose of 10 mg.

In the elderly (over 65) escitalopram is slower than in young patients. The amount of the substance in the systemic circulation, calculated using the pharmacokinetic index, the area under the concentration-time curve (AUC) in the elderly is 50% more than in young healthy volunteers.

Indications:

- Depressive disorders of any severity;

- panic disorder with / without agoraphobia.

Contraindications:

Hypersensitivity to the drug or its components,children and adolescents (up to 18 years), simultaneous reception with monoamine oxidase (MAO) inhibitors, pregnancy, the period of breastfeeding.

Carefully:

Pabnormal insufficiency (creatinine clearance below 30 ml / min), hypomania, manic disorders, pharmacologically uncontrolled epilepsy, depression with suicidal attempts, diabetes mellitus, advanced age, cirrhosis, tendency to bleeding; simultaneous reception with drugs that reduce the threshold of convulsive readiness, causing hyponatremia; ethanol; drugs metabolized by the system CYP2C19.

Dosing and Administration:

Inside. The drug is prescribed to adults once a day, regardless of food intake.

Depressive disorders

Usually prescribe 10 mg once a day. Depending on the individual reaction of the patient, the dose may be increased to a maximum of 20 mg / day. The antidepressant effect usually develops in 2-4 weeks after the start of treatment. After the disappearance of the symptoms of depression, at least for another 6 months, it is necessary to continue therapy to fix the effect.

Panic disorder with or without agoraphobia

During the first week of treatment, a dose of 5 mg / day is recommended, which is then increased to 10 mg / day. Depending on the individual reaction of the patient, the dose may be increased to a maximum of 20 mg / day.

The maximum therapeutic effect is achieved approximately 3 months after the start of treatment. The therapy lasts for several months.

Elderly patients (over 65 years of age)

It is recommended to use half of the usually recommended dose (ie, only 5 mg / day) and a lower maximum dose (10 mg / day).

Decreased kidney function

With mild and moderate renal failure, dose adjustments are not required. Patients with severe renal insufficiency (QC below 30 ml / min) should be prescribed the drug with minimal therapeutic doses, gradually increasing them taking into account the tolerability and effectiveness of the drug.

Decreased liver function

The recommended initial dose for the first two weeks of treatment is 5 mg / day. Depending on the individual reaction of the patient, the dose may be increased to 10 mg / day.

Reduced activity of cytochrome CYP2C19

For patients with a weak isoenzyme activity CYP2C19 The recommended starting dose for the first two weeks of treatment was 5 mg / day. Depending on the individual reaction of the patient, the dose may be increased to 10 mg / day.

Discontinuation of treatment

At termination of treatment with the dose should decline gradually over 1-2 weeks in order to avoid a withdrawal syndrome.

Side effects:

Side effects most often occur at 1 or 2 week of treatment, then typically become less intense and less likely to occur with continued therapy.

From the central nervous system (CNS): dizziness, weakness, insomnia or drowsiness, convulsions, tremor, movement disorders, serotonin syndrome (agitation, tremor, myoclonus, hyperthermia), hallucinations, manic disorder, confusion, agitation, anxiety, depersonalisation, panic attacks, irritability, visual disturbances.

From the digestive system: nausea, vomiting, dry mouth, taste disorders, decreased appetite, diarrhea, constipation.

From the cardiovascular system: orthostatic hypotension.

From the endocrine system: decrease in the secretion of antidiuretic hormone (ADH), galactorrhea.

From the genitourinary system: decreased libido, impotence, ejaculation, anorgasmia (in women), urinary retention.

From the skin: skin rash, itching, ecchymosis, purpura, angioedema.

Allergic reactions: anaphylactic reactions.

Laboratory indicators: hyponatremia, changes in laboratory parameters of liver function.

Other: increased sweating, hyperthermia, sinusitis, arthralgia, myalgia.

In addition, after prolonged use, a sharp cessation of SELECTRA therapy in some patients may lead to withdrawal. With a sharp discontinuation of escitalopram, unwanted reactions such as dizziness, headaches and nausea, which are not significant, and duration - are limited.

Overdose:

Symptoms. Dizziness, tremor, agitation, drowsiness, confusion, convulsive seizures, tachycardia, changes in the ECG (segment change S-T, T wave, expansion of the complex QRS, elongation QT interval), arrhythmias, respiratory depression, vomiting, rhabdomyolysis, metabolic acidosis, hypokalemia, very rarely acute renal failure.

Treatment. There is no specific antidote. Treatment is symptomatic and supportive: gastric lavage, adequate oxygenation. Monitoring the function of the cardiovascular and respiratory systems.

Interaction:

Inhibitors of monoamine oxidase (MAO)

There may be serious adverse reactions with the simultaneous administration of SELECTRA and MAO inhibitors, as well as with the administration of MAO inhibitors to patients who had stopped taking the drug shortly before. In such cases, a serotonin syndrome may develop.

Escitalopram can not be administered simultaneously with MAO inhibitors. Escitalopram can be appointed 14 days after cessation of treatment by irreversible MAO inhibitors and at least 1 day after discontinuation of therapy with a reversible MAO inhibitor of type A - moclobemide. At least 7 days must pass after the end of taking escitalopram before treatment with non-selective MAO inhibitors can begin.

Serotonergic drugs

Joint use with serotonergic drugs (eg tramadol, sumatriptan and other triptans) can lead to the development of serotoninsyndrome.

Drugs that reduce the threshold of convulsive readiness

SELECTRA can reduce the threshold of convulsive readiness. Care should be taken when concomitantly with other drugs that reduce the threshold of convulsive readiness (tricyclic antidepressants, other SSRIs, neuroleptics (phenothiazines, thioxanthene derivatives and butyrophenone), mefloquine and tramadol).

Lithium, tryptophan

Escitalopram enhances the pharmacological effects of tryptophan (increased serotonergic effect) and the toxic effects of lithium preparations.

St. John's wort perforated (Hypericum perforatum)

Simultaneous administration of escitalopram and preparations containing St. John's Wort (Hypericum perforatum), can lead to an increase in the number of side effects.

Anticoagulants and other drugs that affect blood coagulability

Violation of blood clotting can occur with the simultaneous administration of escitalopram with oral anticoagulants and other drugs that affect blood clotting (for example, atypical antipsychotics and phenothiazines,most tricyclic antidepressants, acetylsalicylic acid and non-steroidal anti-inflammatory drugs, ticlopidine and dipyridamole). In such cases, control of blood clotting parameters is necessary.

Ethanol

Escitalopram does not enter with pharmacodynamic or pharmacokinetic interaction with ethanol. However, as with other psychotropic drugs, simultaneous use of escitalopram and alcohol is not recommended.

The effect of other drugs on the pharmacokinetics of escitalopram

Joint use with drugs that inhibit cytochrome CYP2C19, can increase the concentration of escitalopram in blood plasma. Caution should be exercised while using escitalopram with similar drugs, for example, omeprazole. A decrease in the dose of escitalopram may be required.

Caution should be given to high doses of escitalopram simultaneously with high doses of cimetidine, which is a strong inhibitor of cytochromes CYP2D6, CYP3A4 and CYP1A2.

The effect of escitalopram on the pharmacokinetics of other drugs

Escitalopram is an inhibitor of the isoenzyme CYP2D6. Caution should be exercised when concomitant administration of escitalopram and drugs metabolized by this isoenzyme and having a small therapeutic index, for example, flecainide, propafenone and metoprolol (in cases of heart failure), or medicines, mainly metabolized by CYP2D6 and acting on the central nervous system, for example, antidepressants - desipramine, clomipramine, nortriptyline, or antipsychotic agents - risperidone, thioridazine, haloperidol. In these cases, dose adjustment may be required, as the concentration of escitalopram in the blood plasma increases.

Simultaneous administration of escitalopram and desipramine or metoprolol leads to a twofold increase in the concentration of the last two drugs, which should be taken into account when choosing doses.

Escitalopram may slightly inhibit the isoenzyme CYP2C19. Therefore, caution should be exercised while using escitalopram and medications that are metabolized CYP2C19.

Special instructions:

When using drugs belonging to the therapeutic group of SSRIs, including escitalopram, the following should be considered:

Some patients with panic disorder at the beginning of SSRI treatment may experience increased anxiety. A similar paradoxical reaction usually disappears within two weeks of treatment. To reduce the likelihood of an anxiogenic effect, it is recommended to use low initial doses.

It is necessary to cancel the drug in case of convulsive seizures. It is not recommended to use in patients with uncontrolled epilepsy; with controlled seizures careful monitoring is necessary. With an increase in the frequency of convulsive seizures of SSRIs, including escitalopram, should be canceled.

Escitalopram should be used with caution in patients with a history of mania / hypomania. With the development of the manic state escitalopram should be canceled.

In patients with diabetes, treatment with escitalopram can alter blood glucose levels (both hypoglycemia and hyperglycemia are possible). Therefore, the dosage of insulin and / or oral hypoglycemic agents may need to be adjusted.

The risk of committing suicide is inherent in depression and can persist until a significant improvement in the condition occurs spontaneously or as a result of ongoing therapy. Careful observation of patients on antidepressant medication is necessary, especially at the beginning of treatment because of the possibility of clinical deterioration and / or the appearance of suicidal manifestations (thoughts and behavior). This precaution should be followed in the treatment of other mental disorders due to the possibility of simultaneous development of depression.

In a number of cases, in the treatment of antidepressants, the SSRI group was noted highernorNo risk of developing suicidal thoughts and behavior in children, adolescents and young people younger than 24 years compared with placebo.

Hyponatremia, possibly associated with a violation of ADH secretion, against the background of taking escitalopram occurs rarely and usually disappears when therapy is withdrawn. Caution should be manifested in the appointment of escitalopram and other SSRIs to persons at risk of developing hyponatremia: the elderly, the patient with cirrhosis of the liver and taking drugs that can cause hyponatraemia.

When taking escitalopram, subcutaneous hemorrhage (ecchymosis and purpura) can develop. It is necessary to use caution escitalopram in patients with a tendency to bleeding, and also taking oral anticoagulants and other drugs that affect blood clotting.

Since the clinical experience of simultaneous use of escitalopram and electroconvulsive therapy is limited, caution should be exercised in such cases.

Combine escitalopram and MAO type A inhibitors are not recommended because of the risk of developing a serotonin syndrome.

In patients receiving escitalopram and other SSRIs simultaneously with serotonergic drugs, in rare cases, a serotonin syndrome may develop. It is necessary to use caution escitalopram simultaneously with drugs that have a serotonergic effect. The combination of such symptoms as agitation, tremor, myoclonus, hyperthermia, may indicate the development of serotonin syndrome. If this occurs, SSRIs and serotonergic drugs should be immediately withdrawn and symptomatic treatment is prescribed.

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

During the treatment of the drug, patients should avoid performing potentially dangerous activities requiring high rates of psychomotor reactions, such as driving a car or controlling machinery.

Form release / dosage:

Tablets, film-coated, 5 mg, 10 mg, 15 mg and 20 mg.

Packaging:

For 10 or 14 tablets per blister PVC / PVDC / aluminum foil.

1, 2, 3 blisters for 10 tablets or 1, 2, 4 blisters for 14 tablets together with instructions for use in a cardboard pack.

For 10 blisters together with instructions for use in a cardboard box (for hospitals).

Storage conditions:

At a temperature of no higher than 25 ° C.

Keep out of the reach of children.

Shelf life:

24 months.

Do not use after the expiration date printed on the package.

Terms of leave from pharmacies:On prescription

Registration number:LSR-008205/09

Date of registration:16.10.2009

The owner of the registration certificate:Abbott Productions AJAbbott Productions AJ Switzerland

Manufacturer: & nbsp

ACTAVIS, Ltd. Iceland

Representation: & nbspABBOTT LABORATORIES LLC ABBOTT LABORATORIES LLC Russia

Information update date: & nbsp04.10.2015

Illustrated instructions

Instructions

Selectra (Selectra)