Lenuxin, 10 mg 28 pcs

Lenuxin is an antidepressant.

Pharmacodynamics

Antidepressant, SSRI; increases the concentration of neurotransmitter in the synaptic cleft, increases and prolongs the effect of serotonin on postsynaptic receptors. Estcitalopram binds to serotonin (5-NT), dopamine (D1 and D2), α-adrenergic, histamine, m-cholinoreceptors, and benzodiazepine and opioid receptors. Antidepressant effect usually develops 2-4 weeks after the start of treatment. Maximum therapeutic effect of treatment of panic disorder is reached approximately 3 months after the beginning of treatment.

Pharmacokinetics

Intake and distribution

Intake is not dependent on food intake. The kinetics of escitalopram are linear with single and regular administration in a dosage range of 10 to 30 mg/day. Bioavailability is about 80%.Tmax is 4 h. Css in plasma is reached after 1 week. The average Css is 50 nmol/L (20 to 125 nmol/L) at a daily dose of 10 mg. The average Vd is 12 to 26 l/kg. Binding to plasma proteins is about 56%.

Metabolism and excretion

Metabolized in the liver to active demethylated and didemethylated metabolites. When the drug is taken regularly, the steady-state concentration of demethyl and didemethyl metabolites is 28-31% and less than 5%, respectively, of the concentration of escitalopram. Metabolism of escitalopram to demethylated metabolite occurs primarily via cytochrome P450 isoenzymes: CYP2C19, CYP3A4 and CYP2D6. T1/2 after multiple administration is 30 h. The main metabolites of escitalopram have a longer T1/2. Total clearance is 0.6 l/min.

Escitalopram and its major metabolites are excreted by the liver and most of them by the kidneys, partially excreted as glucuronides. In hepatic insufficiency, the clearance of escitalopram is decreased by 37% and the T1/2 is doubled. In patients with low activity of CYP2C19 isoenzyme, the concentration of escitalopram may be 2 times higher. No significant changes in drug concentrations are observed in patients with low activity of CYP2D6 isoenzyme.

In moderate renal failure, the clearance of escitalopram is reduced by 17%. There are no data on the pharmacokinetics of escitalopram in patients with severe renal impairment (creatinine Cl below 20 ml/min). In the elderly (over 65 years), escitalopram is excreted slower than in younger patients. The AUC in the elderly is increased by 50%.

Indications

Active ingredient

Composition

Active substance:

Escitalopram oxalate – 10 mg;

Associate Ingredients:

MCC;

croscarmellose sodium;

How to take, the dosage

Overly, once daily regardless of meals.

Moderate to severe depression

In general, 10 mg once daily is prescribed. Depending on the individual response of the patient, the dose may be increased to a maximum of 20 mg/day. Antidepressant effect usually develops 2-4 weeks after the start of treatment. After the symptoms of depression disappear, it is necessary to continue therapy to consolidate the effect for at least 6 months.

Panic disorder with or without agoraphobia

In 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 response of the patient, the dose may be increased to a maximum of 20 mg/day. Maximum therapeutic effect is achieved about 3 months after the start of treatment. Therapy lasts for several months.

Social anxiety disorder (social phobia)

Prescription is usually 10 mg once daily. Relief of symptoms usually develops in 2-4 weeks after the start of treatment. Depending on the patient’s individual response, the dose may subsequently be reduced to 5 mg/day or increased to a maximum of 20 mg/day. Since social anxiety disorder is a disease with a chronic course, the minimum recommended duration of therapy is 12 weeks. To prevent recurrence of the disorder, repeated therapy for 6 months or longer may be prescribed, depending on the individual patient’s response.

Before prescribing the drug, it is necessary to differentiate social phobia from everyday shyness or timidity.

Generalized anxiety disorder

The recommended starting dose is 10 mg once daily. Depending on the individual response of the patient, the dose may be increased to a maximum of 20 mg/day. Long-term prescription of the drug (6 months and longer) in a dose of 20 mg/day is allowed.

Patient special groups

The elderly (over 65 years). Half of the usual recommended dose of 5 mg/day is recommended. The maximum dose is 10 mg/day.

Decreased renal function. No dose adjustment is required in moderately severe renal failure. In patients with severe renal insufficiency (creatinine Cl below 30 ml/min) the drug is administered with caution.

Limited liver function. In mild to moderate hepatic insufficiency, the recommended initial dose for the first 2 weeks of treatment is 5 mg/day. Depending on the individual response of the patient, the dose may be increased to 10 mg/day. In severe hepatic insufficiency, caution should be exercised when titrating.

Decreased activity of CYP2C19 isoenzyme. For patients with reduced CYP2C19 isoenzyme activity, the recommended initial dose for the first 2 weeks of treatment is 5 mg/day. Depending on the individual response of the patient, the dose may be increased to 10 mg/day.

Cessation of treatment. When discontinuing treatment, the dose should be gradually reduced over 1-2 weeks to avoid withdrawal syndrome.

Interaction

In order to avoid possible drug interactions with the drug Lenuxin®, other drugs may be used only after consultation with a physician.

Pharmaceutical interactions

Serotonergic drugs. Concomitant use with serotonergic drugs (e.g., tramadol, sumatriptan and other triptans) may lead to serotonin syndrome.

The drugs that lower the seizure threshold. Excitalopram may decrease the seizure threshold. Caution is required with concomitant use of other drugs which decrease the threshold of seizure susceptibility (tricyclic antidepressants, SSRIs, neuroleptics – phenothiazine derivatives, tioxanthene and butyrophenone, mefloquine and tramadol).

Lithium and tryptophan. When concomitant use of escitalopram and lithium or tryptophan there have been recorded cases of increasing the effect of the drug.

Wort (Hypericum perforatum). Simultaneous use of escitalopram and Hypericum perforatum preparations may lead to an increase in the number of side effects.

Anticoagulants and other agents that affect blood clotting. When concomitant use of escitalopram with indirect anticoagulants and other drugs affecting blood clotting (e.g. atypical neuroleptics and phenothiazine derivatives, most tricyclic antidepressants, acetylsalicylic acid and NSAIDs, ticlopidine and dipyridamole) may cause clotting disorders. In such cases, regular monitoring of blood clotting is necessary at the beginning or end of therapy with escitalopram.

Pharmacokinetic interaction

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

The simultaneous use of escitalopram and cimetidine (an inhibitor of CYP2D6, CYP3A4 and CYP1A2 isoenzymes) in a dose of 400 mg twice daily leads to increased (about 70%) plasma concentrations of escitalopram.

Thus, caution should be exercised when prescribing escitalopram concomitantly with CYP2C19 isoenzyme inhibitors (e.g., omeprazole, esomeprazole, fluvoxamine, lansoprazole, ticlopidine) and cimetidine. Concomitant use of escitalopram and the above drugs may require reduction of the dose of escitalopram based on monitoring of side effects.

The effect of escitalopram on the pharmacokinetics of other drugs. Excitalopram is an inhibitor of CYP2D6 isoenzyme. Caution should be exercised when concomitant use of escitalopram and drugs that are metabolized with this isoenzyme and have a low therapeutic index, such as flecainide, propafenone and metoprolol (in cases of use in heart failure) or drugs mainly metabolized by CYP2D6 isoenzyme and acting on CNS, such as antidepressants – desipramine, clomipramine, nortriptyline – or neuroleptics – risperidone, thioridazine, haloperidol. Dose adjustments may be necessary in these cases.

The simultaneous use of escitalopram and desipramine or metoprolol leads to a twofold increase in concentrations of the latter two drugs.

Escitalopram may slightly inhibit the CYP2C19 isoenzyme. Therefore, caution is recommended when concomitant use of escitalopram and drugs metabolized by CYP2C19.

Special Instructions

Escitalopram should not be prescribed concomitantly with MAO inhibitors (because of the risk of serotonin syndrome).

Escitalopram may be prescribed 14 days after stopping treatment with irreversible MAO inhibitors and at least 1 day after stopping therapy with reversible type A MAO inhibitors (moclobemide). At least 7 days must pass after stopping escitalopram before treatment with non-selective MAO inhibitors can be started.

In children, adolescents, and young adults (younger than 24 years) with depression and other psychiatric disorders, antidepressants increase the risk of suicidal ideation and suicidal behavior compared to placebo. Therefore, when prescribing Lenuxin® or any other antidepressant medication in children, adolescents, and young adults (under 24 years of age), the risk of suicide should be weighed against the benefit of the medication. If the decision is made to initiate antidepressant therapy, the patient should be closely monitored for the early detection of impairment or behavioral changes, as well as suicidal tendencies.

When using drugs belonging to the therapeutic group of SSRIs, including escitalopram, the following should be considered – some patients with panic disorder may experience an increase in anxiety at the beginning of SSRI treatment. This paradoxical reaction usually disappears within the first 2 weeks of treatment. To reduce the likelihood of an anxiogenic effect, low initial doses are recommended. The drug should be discontinued if seizures develop. Use in patients with unstable epilepsy is not recommended; in controlled seizures, close monitoring is necessary. If seizure frequency increases, SSRIs, including escitalopram, should be discontinued.

The use of SSRIs and SSRIs is associated with the development of akathisia, a condition characterized by an unpleasant debilitating feeling of restlessness and hyperactivity and often accompanied by an inability to sit or stand in one place. This condition is most likely to occur during the first few weeks of therapy. Increasing the dose may be detrimental to patients who experience these symptoms.

Escitalopram should be used with caution in patients with a history of mania/hypomania. If a manic state develops, escitalopram should be withdrawn.

In patients with diabetes mellitus, treatment with escitalopram may alter blood glucose levels. Therefore, it may be necessary to adjust the doses of insulin and/or oral hypoglycemic drugs.

The risk of suicide is inherent in depression and may persist until significant improvement has occurred spontaneously or due to ongoing therapy. Close monitoring of patients on antidepressant therapy is necessary, especially at the beginning of treatment (because of the potential for clinical deterioration and/or suicidal ideation and behavior). This precaution should also be observed when treating other psychiatric disorders (because of the possibility of a concurrent depressive episode).

Hyponatremia, possibly associated with impaired ADH secretion during administration of escitalopram, is rare and usually disappears when therapy is discontinued. Caution should be used when prescribing escitalopram and other SSRIs for those at risk of hyponatremia – the elderly, those with cirrhosis of the liver, and those taking medications that can cause hyponatremia.

When taking escitalopram it is possible to develop skin bleeding (ecchymosis and purpura). It is necessary to use escitalopram with caution in patients who are prone to bleeding, as well as those who take oral anticoagulants and drugs affecting blood clotting.

Because clinical experience with concomitant use of escitalopram and electroconvulsive therapy is limited, caution should be exercised in such cases.

Patients taking escitalopram and other SSRIs concomitantly with serotonergic drugs may, in rare cases, develop serotonin syndrome. Caution is necessary when using escitalopram concomitantly with drugs with serotonergic effects.

Due to limited clinical experience, caution is recommended when using the drug in patients with CHD.

After long-term use, abrupt discontinuation of therapy with escitalopram in some patients may lead to withdrawal reactions. Undesirable reactions such as dizziness, headaches and nausea may occur. The severity of these reactions is usually mild and the duration is limited. To avoid the occurrence of withdrawal reactions, a gradual withdrawal of the drug over 1-2 weeks is recommended.

Interaction with alcohol. Excitalopram has no pharmacodynamic or pharmacokinetic interaction with alcohol. However, as with other antidepressants, you should refrain from drinking alcohol for the duration of treatment with the drug.

Impact on the ability to drive motor vehicles and engage in potentially hazardous activities. During treatment it is necessary to refrain from driving motor transport and engaging in potentially hazardous activities requiring increased concentration and quick psychomotor reactions.

Contraindications

If you have any of the above conditions and/or diseases, you should always consult your doctor before taking this medicine.

With caution: Renal insufficiency (creatinine Cl less than 30 ml/min); hypomania; mania; pharmacologically uncontrolled epilepsy; depression with suicide attempts; diabetes mellitus; advanced age; cirrhosis of the liver; susceptibility to bleeding; simultaneous use with drugs that reduce seizure threshold and cause hyponatremia; with ethanol; with drugs that are metabolized by CYP2C19 isoenzyme.

If any of the above conditions and/or diseases are present, always consult a physician before taking the drug.

Side effects

CNS disorders: often – headache, dizziness, weakness, insomnia or somnolence, seizures, tremor, motor disorders, serotonin syndrome (agitation, tremor, myoclonus, hyperthermia, see “Special Indications”); rarely – hallucinations, mania, confusion, agitation, anxiety, depersonalization, panic attacks, increased irritability, visual disturbances.

The digestive system: very frequently – nausea, vomiting; frequently – diarrhea, dry mouth, taste disorders, decreased appetite or increased appetite, constipation.

Skin disorders: frequently – increased sweating; less frequently – skin rash, itching, ecchymosis, purpura, angioedema.

With the reproductive system: often – disruption of ejaculation, impotence, menstrual disorders are possible.

Urinary system disorders: often – urinary retention.

The body in general: often – weakness; rarely – hyperthermia.

Metabolic disorders: rarely – insufficient secretion of ADH.

Particularly orthostatic hypotension.

Laboratory measures: frequently – changes of laboratory indexes of liver function, hyponatremia and changes of ECG (prolongation of QT interval, dilation of QRS complex, changes of ST segment and T wave).

Muscular system disorders: infrequent – arthralgia, myalgia.

Allergic reactions: in single cases – anaphylactic reactions.

Overdose

Symptoms: dizziness, tremor, agitation, drowsiness, confusion, convulsions, tachycardia, ECG changes (change of ST segment, T wave, widening of QRS complex, QT interval prolongation), arrhythmias, respiratory depression, vomiting, rhabdomyolysis, metabolic acidosis, hypokalemia.

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

Treatment: symptomatic and supportive. There is no specific antidote. Appointment of gastric lavage, adequate oxygenation. Monitoring of cardiac and respiratory system function. The outcome is favorable.

Pregnancy use

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

Breast-feeding should be stopped during the use of the drug.

Similarities