Lenuxin® (Lenuxin®)

Composition Pharmacodynamics Indications Carefully Contraindications Dosing and Administration Side effects Form release / dosage
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Active substanceEscitalopramEscitalopram
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    • Dosage form: & nbspfilm-coated tablets
    Composition:

    1 tablet contains:

    Dactive substance:

    Escitalopram oxalate

    6.3875 mg

    12.7750 mg

    25.55 mg

    (equivalent to escitalopram)

    5 mg

    10 mg

    20 mg

    Excipients:

    Microcrystalline cellulose

    16.4125 mg

    32.8250 mg

    65.65 mg

    Croscarmellose sodium

    3,1250 mg

    6,2500 mg

    12.50 mg

    Talc

    0.6250 mg

    1.2500 mg

    2.50 mg

    Siliconized microcrystalline cellulose 90 (Prosolv 90)

    17.6625 mg

    35.3250 mg

    70.65 mg

    Siliconized microcrystalline cellulose HD90 (Prosolv HD90)

    17.6625 mg

    35.3250 mg

    70.65 mg

    Magnesium stearate

    0.6250 mg

    1.2500 mg

    2.50 mg

    Shell composition:

    Opadry II white 33G 28523

    (Gipromellose 6sP (2910) 40%, titanium dioxide (E 171) 25%, lactose monohydrate 21%, macrogol 3350 8%, glycerol triacetate (triacetin) 6%).

    1.25 mg

    2.50 mg

    5.00 mg
    Description:

    Dosage of 5 mg: Round biconvex tablets coated with a film shell, white or almost white, engraved "No. 53" on one side, on a transverse section of white or almost white.

    Dosage of 10 mg: Round biconvex tablets covered with a film shell, white or almost white, engraved "No. 54" on one side and risky on the other side, on a transverse section of white or almost white color.

    Dosage of 20 mg: Round biconvex tablets covered with a film shell, white or almost white, engraved "No. 56" on one side and risky on the other side, on a transverse section of white or almost white color.

    Pharmacotherapeutic group:antidepressant
    ATX: & nbsp

    N.06.A.B.10   Escitalopram

    Pharmacodynamics:

    Antidepressant, selective serotonin reuptake inhibitor (SSRI); increases the concentration of the neurotransmitter in the synaptic cleft, enhances and prolongs the action of serotonin on postsynaptic receptors. Escitalopram practically does not bind to serotonin (5-HT), dopamine (D1 and D2), alpha-adrenergic, histamine, m-cholinergic receptors, as well as benzodiazepine and opioid receptors.

    The antidepressant effect usually develops in 2-4 weeks after the beginning of admission. The maximum therapeutic effect of treatment of panic disorders is reached approximately 3 months after the start of treatment.

    Pharmacokinetics:

    Suction and distribution: absorption is not dependent on food intake. The kinetics of escitalopram is linear for a single and regular admission in the dosage range of 10 to 30 mg / day. Bioavailability of about 80%. The time to reach the maximum concentration in the blood plasma of the TCmOh - 4 hours. Equilibrium concentration in blood plasma (Css) is achieved after 1 week. average value Css is 50 nmol / l (20 to 125 nmol / l) with a daily dose of 10 mg. The average volume of distribution is from 12 to 26 l / kg. The connection with plasma proteins is about 56%.

    Metabolism and excretion: is metabolized in the liver to active demethylated and demodetylated metabolites. With a regular intake of the drug, the steady-state concentration of demethyl- and didemetylmetabolites is 28-31% and less than 5%, respectively, of the concentration of escitalopram.Metabolism of escitalopram in the demethylated metabolite occurs mainly with the help of cytochrome P450 isoenzymes: CYP2C19, CYP3A4 and CYP2D6. The half-life of excretion T1/2 after repeated use - 30 hours. The main metabolites of escitalopram T1/2 more prolonged. The total ground clearance is 0.6 l / min. Escitalopram and its major metabolites are excreted by the liver and most of it by the kidneys, partially excreted in the form of glucuronides.

    With hepatic insufficiency The clearance of escitalopram is reduced by 37% and T1/2 doubled.

    In patients with low isoenzyme activity CYP2C19 the concentration of escitalopram can be 2 times higher. Significant changes in drug concentration with a weak isoenzyme activity CYP2D6 is not observed.

    With an average degree of severity of renal failure clearance of escitalopram decreased by 17%. Data on the pharmacokinetics of escitalopram in patients with severe renal insufficiency (creatinine clearance below 20 ml / min) are absent.

    The elderly (over 65 years of age) escitalopram is slower than in younger patients. The area under the concentration-time curve in the elderly is increased by 50%.
    Indications:

    - Depression of moderate or severe severity;

    - panic disorder with or without agoraphobia;

    - social anxiety disorder (social phobia);

    - generalized anxiety disorder.

    Contraindications:

    - Hypersensitivity to the drug or its components;

    - children's and adolescence (up to 18 years);

    - simultaneous administration with monoamine oxidase (MAO) inhibitors;

    - deficiency of sugar / isomaltase, intolerance to fructose and glucose-galactose malabsorption, since the preparation contains sucrose.

    If you have one of the listed conditions and / or diseases before taking the drug, be sure to consult a doctor.

    Carefully:

    Renal failure (creatinine clearance below 30 ml / min), hypomania, mania, pharmacologically uncontrolled epilepsy, depression with suicidal attempts, diabetes, elderly age, cirrhosis, tendency to bleeding; simultaneous reception with drugs (LS), reducing the threshold of convulsive readiness and causing hyponatremia, with ethanol, as well as with drugs metabolized by isoenzyme CYP2C19.

    If you have one of the listed conditions and / or diseases before taking the drug, be sure to consult a doctor.

    Pregnancy and lactation:

    The use of the drug during pregnancy is not recommended due to the lack of data on efficacy and safety.

    During the application of the drug, breastfeeding should be discarded.

    Dosing and Administration:

    The drug is taken orally 1 time per day, regardless of food intake.

    Depression of moderate to severe severity

    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 should continue therapy to fix the effect for at least 6 months.

    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.

    Social anxiety disorder (social phobia)

    Usually prescribe 10 mg once a day. Symptom weakening usually develops 2-4 weeks after the start of treatment. Depending on the individual reaction of the patient, the dose can subsequently be reduced to 5 mg / day. or increased to a maximum of 20 mg / day. Because social anxiety disorder is a disease with chronic course, the minimum recommended duration of a therapeutic course is 12 weeks. To prevent recurrence of the disease, repeat therapy may be given for 6 months or longer depending on the individual response of the patient.

    Before prescribing the drug, it is necessary to differentiate the social phobia with "ordinary" shyness or shyness.

    Generalized anxiety disorder

    The recommended initial dose is 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.A prolonged prescription of the drug (6 months and longer) at a dose of 20 mg / day is allowed.

    Elderly patients (over 65 years of age): it is recommended to use half of the usual recommended dose - 5 mg / day. The maximum dose is 10 mg / day.

    Decreased kidney function: with moderate severity of renal failure, dose adjustment is not required. Patients with severe renal insufficiency (creatinine clearance below 30 ml / min) the drug is administered with caution.

    Decreased liver function: with mild and moderate hepatic insufficiency, 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. With severe hepatic insufficiency, care must be taken when titrating.

    Reduced isoenzyme activity CYP2C19: for patients with low isoenzyme activity CYP2C19 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.

    Discontinuation of treatment: at the end of treatment the dose should gradually decrease within 1-2 weeks in order to avoid the occurrence of the "withdrawal" syndrome.

    Side effects:

    Side effects most often occur in the first or second week of treatment with the drug and then usually become less intense and occur less frequently with continued therapy.

    WHO classification of unwanted adverse reactions according to the frequency of development:

    Very frequent - 1/10 appointments (> 10%)

    Frequent - 1/100 appointments (> 1% and <10%)

    Infrequent - 1/1000 appointments (> 0.1% and <1%)

    Rare - 1/10000 appointments (> 0.01% and <0.1%)

    Very rare - 1/10000 prescriptions (<0.01%)

    From the side of the central nervous system: often - headache, dizziness, weakness, insomnia or drowsiness, convulsions, tremor, motor disorders, serotonin syndrome (agitation, tremor, myoclonus, hyperthermia, see section "Special instructions"); less hallucinations, mania, confusion, agitation, anxiety, depersonalization, panic attacks, increased irritability, visual disturbances.

    From the digestive system: very often - nausea, vomiting; often - diarrhea, dry mouth, taste disorders, decreased appetite or vice versa, constipation.

    From the skin: often - excessive sweating, less often - skin rash, itching, ecchymosis, purpura, angioedema.

    On the part of the reproductive system: often - violation of ejaculation, impotence, possible violations of the menstrual cycle.

    From the urinary system: often - urinary retention.

    On the part of the body as a whole: often - weakness, less often hyperthermia.

    Metabolic disorders: rarely - insufficient secretion of antidiuretic hormone (ADH).

    From the cardiovascular system: infrequently - orthostatic hypotension. Laboratory indicators: often - changes in laboratory parameters of liver function, hyponatremia and changes in the electrocardiogram (prolongation of the Q-T interval, expansion of the QRS complex, change in the S-T segment and T wave).

    From the musculoskeletal system: infrequently - arthralgia, myalgia.

    Allergic reactions: in some cases, anaphylactic reactions are possible.

    If any of the side effects indicated in the manual are aggravated, or if you notice any other side effects not listed in the instructions, report this doctor.

    Overdose:

    Symptoms: dizziness, tremor, agitation, drowsiness, confusion, convulsions, tachycardia, ECG changes (segment change S-T, T wave, expansion of the complex QRS, lengthening the interval Q-T), arrhythmias, respiratory depression, vomiting, rhabdomyolysis, metabolic acidosis, hypokalemia.

    Coma and fatal cases of escitalopram overdose are extremely rare, most of them include a simultaneous overdose with other medicines. Taking a dose of 400-800 mg of escitalopram did not cause severe symptoms.

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

    Interaction:To avoid possible drug interactions with the drug Lenuksin® apply other medications only after consultation with your doctor.

    Pharmaceutical interaction

    Serotonergic drugs: simultaneous use with serotonergic drugs (for example, tramadol, sumatriptan and other triptans) may lead to the development of serotonin syndrome.

    Drugs that reduce the threshold of convulsive readiness: escitalopram can reduce the threshold of convulsive readiness.Care should be taken when using other drugs that reduce the threshold of convulsive readiness (tricyclic antidepressants, SSRIs, neuroleptics - derivatives of phenothiazine, thioxanthene and butyrophenone, mefloquine and tramadol).

    Lithium and tryptophan: while concomitant use of escitalopram and lithium or tryptophan reported cases of increased drug effects.

    St. John's wort Perforated (Hypericum perforatum): simultaneous application escitalopram and preparations of St. John's wort can lead to an increase in the number of side effects.

    Anticoagulants and other means that affect blood clotting: at concomitant use of escitalopram with indirect anticoagulants and other agents that affect blood clotting (eg, atypical antipsychotics and phenothiazine derivatives, most tricyclic antidepressants, acetylsalicylic acid and non-steroidal anti-inflammatory drugs, ticlopidine and dipyridamole) may result in a clotting disorder. In such cases, when initiating or completing therapy with escitalopram, regular monitoring of blood clotting is necessary.

    Pharmacokinetic interaction

    The effect of other drugs on the pharmacokinetics of escitalopram: simultaneous use of escitalopram and omeprazole (inhibitor of isoenzyme CYP2C19) at a dose of 30 mg once a day leads to a moderate (about 50%) increase in the concentration of escitalopram in blood plasma.

    Simultaneous use of escitalopram and cimetidine (inhibitor of isoenzymes CYP2D6, CYP3A4 and CYP1A2) at a dose of 400 mg twice a day leads to an increase (approximately 70%) of the concentration of escitalopram in the blood plasma.

    Therefore, it should be administered with caution escitalopram simultaneously with inhibitors of isoenzyme CYP2C19 (for example, omeprazole, esomeprolol, fluvoxamine, lansoprazole, ticlopidine) and cimetidine. When concomitantly using escitalopram and the above drugs, a dose reduction of escitalopram may be required based on monitoring of side effects.

    The effect of escitalopram on the pharmacokinetics of other drugs: escitalopram is an inhibitor of the isoenzyme CYP2D6. Caution should be exercised when concomitant use of escitalopram and drugs,metabolized with this isoenzyme and having a small therapeutic index, for example, flecainide, propafenone and metoprolol (in cases of heart failure) or drugs that are mainly metabolized by isoenzyme CYP2D6 and acting on the central nervous system, for example, antidepressants: desipramine, clomipramine, nortriptyline, or Neuroleptics: risperidone, thioridazine, haloperidol. In these cases, dose adjustment may be required.

    Simultaneous use of escitalopram and desipramine or metoprolol leads to a twofold increase in the concentration of the last two drugs.

    Escitalopram may slightly inhibit the isoenzyme CYP2C19. Therefore, caution should be exercised when concomitant use of escitalopram and drugs metabolized CYP2C19.

    Special instructions:

    - Escitalopram should not be administered simultaneously with MAO inhibitors because of the risk of developing serotonin syndrome. Escitalopram can be appointed 14 days after discontinuation of treatment with irreversible MAO inhibitors and at least 1 day after discontinuation of therapy with a reversible MAO type A inhibitormoclobemide).At least 7 days must pass after the end of taking escitalopram before treatment with nonselective MAO inhibitors can begin.

    - In children, adolescents and young adults (under 24 years) with depression and other mental disorders antidepressants compared to placebo, increased the risk of suicidal thoughts or suicidal behavior. Therefore, when appointing the drug Lenuksin® or any other antidepressant for children, adolescents and young people (under 24 years) should be related to the risk of suicide and the benefits of their use. In the case of the decision to initiate antidepressant therapy the patient should be monitored carefully for early detection of faults or changes in behavior, and suicidal tendencies.

    - When using drugs belonging to the therapeutic group of SSRIs, including escitalopram, the following should be considered: In some patients with panic disorder at the beginning of SSRI treatment, anxiety may be increased. A similar paradoxical reaction usually disappears during the first two weeks of treatment. To reduce the likelihood of an anxiogenic effect, it is recommendeduse low initial doses. It is necessary to cancel the drug in case of convulsive seizures. It is not recommended to use in patients with unstable epilepsy; with controlled seizures careful monitoring is necessary. With an increase in the frequency of convulsive seizures of SSRIs, including escitalopram, should be canceled.

    - The use of SSRIs and SSRIs (selective norepinephrine reuptake inhibitors) is associated with the development of akathisia, a condition characterized by an unpleasant debilitating anxiety and hyperactivity disorder and is often accompanied by an inability to sit or stand in one place. This condition most likely occurs during the first few weeks of therapy. Increasing the dose may harm patients who have experienced such symptoms.

    - 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 change the level of glucose in the blood. Therefore, it may be necessary to adjust the dosages of insulin and / or oral hypoglycemic drugs.

    - 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 concurrent depressive episode.

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

    - When taking escitalopram, it is possible to develop skin hemorrhages (ecchymosis and purpura). It is necessary to use caution escitalopram in patients with a tendency to bleeding, and also taking oral anticoagulants and drugs that affect blood coagulability.

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

    - 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.

    - Due to limited clinical experience, caution should be exercised when using the drug in patients with ischemic heart disease (CHD).

    - After prolonged use, a sharp discontinuation of escitalopram therapy in some patients may lead to a reaction of "withdrawal". There may be unwanted reactions such as dizziness, headaches and nausea. The severity of these reactions is usually insignificant, and the duration is limited.To avoid occurrence of reactions of "cancellation" the gradual cancellation of a preparation within 1-2 weeks is recommended.

    - Interaction with alcohol: escitalopram Do not enter with alcohol into pharmacodynamic or pharmacokinetic interaction. However, as with other antidepressants, you should refrain from drinking alcohol during the entire period of treatment with the drug.

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

    During the treatment period it is necessary to refrain from driving motor vehicles and practicing potentially dangerous activities that require an increased concentration of attention and speed of psychomotor reactions.

    Form release / dosage:

    Tablets, film-coated, 5 mg, 10 mg or 20 mg.

    Packaging:

    For 14 or 28 tablets, coated with a film shell, put in a polypropylene bottle, covered with a cover with silica gel.

    One bottle together with the instruction for use is placed in a cardboard box.

    Storage conditions:

    Store in a dark place at a temperature of no higher than 30 ° C.

    Keep out of the reach of children.

    Shelf life:

    2 years.

    Do not use the product after the expiry date printed on the package.

    Terms of leave from pharmacies:On prescription
    Registration number:LP-001456
    Date of registration:25.01.2012
    Date of cancellation:2017-01-25
    The owner of the registration certificate:GEDEON RICHTER, OJSC GEDEON RICHTER, OJSC Hungary
    Manufacturer: & nbsp
    Representation: & nbspGEDEON RICHTER OJSC GEDEON RICHTER OJSC Hungary
    Information update date: & nbsp04.10.2015
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