Lenuxin, pills 10mg, 28pcs

Composition

Active ingredient:

escitalopram oxalate – 10 mg;

Auxiliary substances:

MCC;

croscarmellose sodium;

Talc;

Siliconized MCC 90 (Prosolv 90);

Siliconized MCC HD90 (Prosolv HD90);

magnesium stearate;

Film shell:

Opadry II white 33G28523 (hypromellose 6 cP (2910) – 40%, titanium dioxide (E 171) – 25%, lactose monohydrate-21%, macrogol 3350-8%, glycerol triacetate (triacetin) — 6%)

Pharmacological action

Lenuxin is an antidepressant.

Pharmacodynamics

Antidepressant, SSRI; increases the concentration of 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-holinoreceptors, as well as benzodiazepine and opioid receptors. The antidepressant effect usually develops 2-4 weeks after the start of use. The maximum therapeutic effect of treatment of panic disorders is achieved approximately 3 months after the start of treatment.

Pharmacokinetics

Suction and distribution

Absorption is independent of food intake. The kinetics of escitalopram is linear with a single and regular dose in the dosage range from 10 to 30 mg / day. Bioavailability is about 80%. Tmax — 4 h. Css in blood plasma is reached after 1 week. The average Css value is 50 nmol / l (20 to 125 nmol/L) at a daily dose of 10 mg. The average Vd is from 12 to 26 l / kg. Binding to plasma proteins is about 56%.

Metabolism and elimination

It is metabolized in the liver to active demethylated and didemethylated metabolites. With regular use of the drug, the steady-state concentration of demethyl-and didemethylmetabolites is 28-31% and less than 5%, respectively, of the concentration of escitalopram. Escitalopram is metabolized to a demethylated metabolite mainly by cytochrome P 450 isoenzymes: CYP2C19, CYP3A4, and CYP2D6. T1 / 2 after repeated use — 30 hours. In the main metabolites of escitalopram, T1 / 2 is longer. Total ground clearance-0.6 l / min.

Escitalopram and its major metabolites are excreted by the liver and most of them by the kidneys, partly in the form of glucuronides. In hepatic insufficiency, the clearance of escitalopram is reduced by 37%, and T1 / 2 is doubled. In patients with low activity of the CYP2C19 isoenzyme, the concentration of escitalopram may be 2 times higher. There are no significant changes in the drug concentration with weak activity of the CYP2D6 isoenzyme.

In patients with moderate renal insufficiency, the clearance of escitalopram decreases by 17%. Data on the pharmacokinetics of escitalopram in patients with severe renal insufficiency (creatinine clearance below 20 ml/min) are not available. Escitalopram is excreted more slowly in the elderly (over 65 years of age) than in younger patients. AUC increases by 50% in the elderly.

Indications

• moderate to severe depression;
• panic disorders with or without agoraphobia;
• social anxiety disorder (social phobia);
• generalized anxiety disorder.

Use during pregnancy and lactation

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

During the use of the drug, breastfeeding should be discontinued.

Contraindications

• hypersensitivity to the drug or its components;
• concomitant use with inhibitors MAO;
• sucrose/isomaltase deficiency, fructose intolerance and glucose-galactose malabsorption, since the drug contains sucrose;
• children and adolescents (up to 18 years).

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

With caution:  renal failure (Cl creatinine less than 30 ml/min); hypomania, mania; pharmacologically uncontrolled epilepsy; depression with suicidal attempts; diabetes mellitus; elderly age; liver cirrhosis; bleeding tendency; simultaneous use of drugs that reduce the seizure threshold and cause hyponatremia; ethanol; drugs metabolized by the isoenzyme CYP2C19.

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

Side effects

From the central nervous system:  often — headache, dizziness, weakness, insomnia or drowsiness, convulsions, tremor, motor disorders, serotonin syndrome (agitation, tremor, myoclonus, hyperthermia, see “Special instructions”); less often — 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 side of the skin:  often — increased sweating; less often-skin rash, pruritus, ecchymosis, purpura, angioedema.

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

From the urinary system:  often-urinary retention.

From the body as a whole:  often-weakness; less often-hyperthermia.

Metabolic disorders:  rarely-insufficient ADH secretion.

From the CCC side:  infrequently-orthostatic hypotension.

Laboratory parameters:  often — changes in laboratory parameters of liver function, hyponatremia and ECG changes (prolongation of the QT interval, expansion of the QRS complex, changes in the ST segment and T wave).

Musculoskeletal disorders:  infrequently-arthralgia, myalgia.

Allergic reactions:  in some cases — anaphylactic reactions.

Interaction

To avoid possible drug interactions with the drug Lenuxin®, you can use other drugs only after consultation with your doctor.

Pharmaceutical interaction

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

Drugs that reduce the threshold of convulsive readiness. Escitalopram may lower the seizure alert threshold. Caution should be exercised when concomitantly 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. With the simultaneous use of escitalopram and lithium or tryptophan, cases of increased drug action have been reported.

St. John’s wort (Hypericum perforatum). Concomitant use of escitalopram and St. John’s wort may lead to an increase in the number of side effects.

Anticoagulants and other drugs that affect blood clotting. Concomitant use of escitalopram with indirect anticoagulants and other agents that affect blood clotting (for example, atypical antipsychotics and phenothiazine derivatives, most tricyclic antidepressants, acetylsalicylic acid and NSAIDs, ticlopidine and dipyridamole) blood clotting disorders may occur. In such cases, regular monitoring of blood clotting is necessary at the beginning or end of escitalopram therapy.

Pharmacokinetic interaction

Effect of other drugs on the pharmacokinetics of escitalopram. Concomitant use of escitalopram and omeprazole (an inhibitor of the CYP2C19 isoenzyme) at a dose of 30 mg once a day leads to a moderate (approximately 50%) increase in the concentration of escitalopram in blood plasma.

Concomitant use of escitalopram and cimetidine (an inhibitor of the isoenzymes CYP2D6, CYP3A4 and CYP1A2) at a dose of 400 mg 2 times a day leads to an increase (approximately 70%) in the concentration of escitalopram in blood plasma.

Therefore, escitalopram should be administered with caution concomitantly with CYP2C19 inhibitors (e. g. omeprazole, esomeprazole, fluvoxamine, lansoprazole, ticlopidine) and cimetidine. When escitalopram and the above medications are co-administered, it may be necessary to reduce the dose of escitalopram based on monitoring of side effects.

Effect of escitalopram on the pharmacokinetics of other drugs. Escitalopram is an inhibitor of the CYP2D6 isoenzyme. Caution should be exercised when using escitalopram concomitantly with drugs that are metabolized by this isoenzyme and have a low therapeutic index, for example, flecainide, propafenone and metoprolol (in cases of use in heart failure), or drugs that are mainly metabolized by the CYP2D6 isoenzyme and act on the central nervous system, for example, antidepressants — desipramine, clomipramine, nortriptyline — or neuroleptics — risperidone, thioridazine, haloperidol. In these cases, a dose adjustment may be necessary.

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

Escitalopram may slightly inhibit the CYP2C19 isoenzyme. Therefore, caution is recommended when using escitalopram concomitantly with drugs that are metabolized by CYP2C19.

How to take, course of use and dosage

Inside,1 time a day, regardless of food intake.

Moderate to severe depression

Usually prescribed 10 mg once a day. Depending on the individual response of the patient, the dose can be increased to a maximum of 20 mg/day. The 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 disorders with or without agoraphobia

During the 1st 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 can 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 prescribed 10 mg 1 time a day. Relief of symptoms usually develops 2-4 weeks after the start of treatment. Depending on the individual response of the patient, the dose can then be reduced to 5 mg / day or increased to a maximum of 20 mg / day. Since social anxiety disorder is a chronic disease, the minimum recommended duration of treatment is 12 weeks. To prevent relapses of the disease, repeated therapy may be prescribed for 6 months or longer, depending on the individual response of the patient.

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

Generalized anxiety disorder

The recommended starting dose is 10 mg once a day. Depending on the individual response of the patient, the dose can be increased to a maximum of 20 mg/day. Long-term use of the drug (6 months or longer) at a dose of 20 mg/day is allowed.

Special patient groups

Elderly (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.

Reduced kidney function. No dose adjustment is required for moderate renal insufficiency. Patients with severe renal insufficiency (creatinine clearance below 30 ml/min) should be treated with caution.

Reduced liver function. In patients with 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 can be increased to 10 mg/day. In case of severe hepatic insufficiency, care should be taken when titrating.

Reduced activity of the CYP2C19 isoenzyme. For patients with low activity of the CYP2C19 isoenzyme, 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 can be increased to 10 mg/day.

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

Overdose

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

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

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

Special instructions

Escitalopram should not be administered concomitantly with MAO inhibitors (due to the risk of serotonin syndrome).

Escitalopram may be prescribed 14 days after discontinuation of treatment with irreversible MAO inhibitors and at least 1 day after discontinuation of therapy with reversible MAO type A inhibitors (moclobemide). At least 7 days should elapse after the end of escitalopram before treatment with non-selective MAO inhibitors can be initiated.

In children, adolescents, and young adults (under 24 years of age) with depression and other psychiatric disorders, antidepressants increase the risk of suicidal thoughts and behavior compared to placebo. Therefore, when prescribing the drug Lenuxin®or any other antidepressants to children, adolescents and young people (under 24 years of age), the risk of suicide and the benefits of their use should be correlated. If a decision is made to start antidepressant therapy, the patient should be closely monitored for early detection of behavioral disorders or changes, as well as suicidal tendencies.

When using drugs belonging to the SSRI therapeutic group, including escitalopram, the following should be considered — in some patients with panic disorder at the beginning of treatment An SSRI may cause increased anxiety. This paradoxical reaction usually disappears within the first 2 weeks of treatment. To reduce the likelihood of an anxiogenic effect, it is recommended to use low initial doses. The drug should be discontinued in case of convulsive seizures. It is not recommended for use in patients with unstable epilepsy; for controlled seizures, careful monitoring is necessary. If the frequency of seizures increases, SSRIs, including escitalopram, should be discontinued.

Application SSRIs and An SSRI is associated with the development of akathisia, a condition characterized by an unpleasant, debilitating feeling of anxiety 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 harmful to patients who experience such symptoms.

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

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

The risk of suicide is associated with depression and may persist until significant improvement occurs spontaneously or as a result of ongoing therapy. Patients treated with antidepressants should be carefully monitored, especially at the beginning of treatment (due to the possibility of clinical deterioration and / or the appearance of suicidal thoughts and behaviors). This precaution should also be observed in the treatment of other mental disorders (due to the possibility of simultaneous illness with a depressive episode).

Hyponatremia, possibly associated with impaired ADH secretion while taking escitalopram, occurs rarely and usually disappears when therapy is discontinued. Caution should be exercised when prescribing escitalopram and other SSRIs to people at risk for hyponatremia — such as the elderly, patients with cirrhosis of the liver, and those taking medications that may cause hyponatremia.

When taking escitalopram, skin hemorrhages (ecchymosis and purpura) may develop. Escitalopram should be used with caution in patients with a tendency to bleed, as well as taking oral anticoagulants and medications that affect blood clotting.

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

In patients taking escitalopram and other medications SSRIs are taken simultaneously with serotonergic drugs, and in rare cases serotonin syndrome may develop. Escitalopram should be used with caution simultaneously with medications that have a serotonergic effect.

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

After prolonged use, abrupt discontinuation of escitalopram therapy may lead to withdrawal reactions in some patients. Adverse reactions such as dizziness, headaches, and nausea may occur. The severity of these reactions is usually insignificant, and the duration is limited. To avoid the occurrence of withdrawal reactions, it is recommended to gradually cancel the drug for 1-2 weeks.

Interaction with alcohol. Escitalopram does not interact pharmacodynamically or pharmacokinetically with alcohol. However, as with other antidepressants, you should refrain from drinking alcohol during the entire period of treatment with the drug.

Influence on the ability to drive vehicles and engage in potentially dangerous activities. During the treatment period, it is necessary to refrain from driving vehicles and engaging in potentially dangerous activities that require increased concentration of attention and speed of psychomotor reactions.

Composition

Tablet Form of production

Storage conditions

In a dark place, at a temperature not exceeding 30 °C

Shelf life

2 years

Active ingredient

Escitalopram

Conditions of release from pharmacies

By prescription

Dosage form

Tablets