Medochemie #The_nervous_system #Stimulants #Antidepressants #HEALTH_CARE
Indications
Treatment of major depressive episodes, panic disorders, including agoraphobia, social anxiety disorders (social phobia), generalized anxiety disorders, obsessive-compulsive disorders.
Application
Medopram is used in adults inside 1 time per day, regardless of food intake.
major depressive episode. Usually prescribed 10 mg 1 time per day. Depending on the individual sensitivity of the patient, the dose may be increased to 20 mg.
The antidepressant effect usually occurs within 2-4 weeks. After the disappearance of symptoms, treatment should be continued usually for 6 months in order to strengthen the effect.
Panic disorder with or without agoraphobia. During the first week, an initial dose of 5 mg/day is recommended, after which the dose can be increased to 10 mg/day. In the future, the dose can be increased to 20 mg / day, depending on the individual sensitivity of the patient.
The maximum effect in the treatment of panic disorders is achieved after 3 months. The duration of treatment is several months and depends on the severity of the disease.
Social anxiety disorders (social phobia). Usually prescribed 10 mg 1 time per day. Depending on the individual sensitivity of the patient, it is recommended to increase the dose to 20 mg / day.
Reducing the severity of symptoms, as a rule, occurs after 2-4 weeks of treatment. It is recommended to continue treatment for 3 months. Long-term treatment for 6 months is prescribed to prevent relapse, taking into account the individual manifestations of the disease; regularly evaluate the effectiveness of treatment.
Generalized anxiety disorders. Usually prescribed 10 mg 1 time per day. Depending on individual sensitivity, the dose may be increased to a maximum of 20 mg / day.
It is recommended to continue treatment for 3 months. Long-term treatment for 6 months is prescribed to prevent relapse, taking into account the individual manifestations of the disease; the effectiveness of treatment is regularly evaluated.
Obsessive Compulsive Disorder (OCD). Usually prescribed 10 mg 1 time per day. Depending on individual sensitivity, the dose may be increased to 20 mg / day. OCD is a chronic disease and treatment should be continued for a sufficient period to ensure complete resolution of symptoms, which may be several months or even longer.
Elderly patients (over 65 years of age). The initial dose should be half the usual recommended dose. The recommended daily dose for elderly patients is 5 mg. Depending on individual sensitivity and severity of depression, the dose may be increased to a maximum of 10 mg / day.
Renal failure. In the presence of mild to moderate renal insufficiency, there are no restrictions. The preparation should be used with caution in patients with severe renal insufficiency (creatinine clearance 30 ml / min).
Decreased liver function. The recommended starting 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.
Reduced activity of the cytochrome isoenzyme CYP 2C19. For patients with weak activity of the CYP 2C19 isoenzyme, the recommended initial dose during 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.
Termination of treatment. When stopping treatment with escitalopram, the dose should be gradually reduced over 1-2 weeks to avoid a reaction to discontinuation of the preparation.
Contraindications
Hypersensitivity to escitalopram or other components of the preparation, simultaneous treatment with MAO inhibitors or pimozide.
Side effects
Escitalopram is usually transient and minor. they are observed during the 1-2nd week of treatment and gradually disappear as the patient recovers.
Side effects that are common to all preparations of the class of selective serotonin reuptake inhibitors (SSRIs) and escitalopram, which were observed in placebo-controlled studies and in therapeutic use, are listed by organ system.
From the blood and lymphatic system: thrombocytopenia.
From the immune system: anaphylactic reactions.
Endocrine disorders: disorders of the secretion of antidiuretic hormone.
Nutritional and metabolic disorders: decreased or increased appetite, hyponatremia.
Mental disorders: anxiety, restlessness, abnormal dreams, decreased libido, anorgasmia (in women), teeth grinding during sleep, agitation, nervousness, panic attacks, confusion, aggression, depersonalization, hallucinations, suicidal cases, mania.
From the nervous system: insomnia, drowsiness, dizziness, paresthesia, tremor, taste disturbance, sleep disturbance, loss of consciousness, serotonin syndrome, dyskinesia, movement disorders, convulsions.
On the part of the organ of vision: dilated pupil, blurred vision.
On the part of the organ of hearing: ringing in the ears.
From the cardiovascular system: tachycardia, bradycardia, orthostatic hypotension.
From the respiratory system: sinusitis, yawning, epistaxis.
From the digestive tract: nausea, diarrhea, constipation, vomiting, dry mouth, gastrointestinal bleeding (including rectal).
From the side of the liver and biliary tract: hepatitis.
From the skin and subcutaneous tissue: increased sweating, rash, baldness, itching, bruising, swelling.
From the musculoskeletal system: arthralgia, myalgia.
From the side of the kidneys and urinary tract: urinary retention.
From the reproductive system and mammary glands: ejaculatory disorders, impotence, priapism, galactorrhea (men), metrorrhagia, menorrhagia (women).
General disorders: fatigue, pyrexia, edema.
Investigations: weight gain, abnormal liver function tests.
There are reports of such side effects with the use of preparations of the SSRI class, such as anorexia and akathisia. Cases of prolongation of the QT interval were observed during use, mainly in patients with existing heart disease, a causal relationship has not been established.
Withdrawal symptoms usually occur within the first few days after abrupt discontinuation of treatment and resolve within 2 weeks in most cases. Dizziness, headache, sensory disturbances, sleep disturbances, anxiety, nausea and/or vomiting, tremors, confusion, sweating, headache, diarrhea, tachycardia, emotional instability, irritability, and visual disturbances were observed more frequently. Most of these symptoms are minor and transient, but may be severe and/or prolonged in some patients. To avoid withdrawal symptoms, gradual discontinuation of the preparation over 1-2 weeks is recommended.
special instructions
paradoxical anxiety. some patients with panic disorder may experience an increase in anxiety at the start of treatment with SSRIs. this paradoxical reaction usually disappears within 2 weeks of treatment. to reduce the likelihood of an anxiogenic effect, low initial doses are recommended.
Convulsive seizures. It is necessary to cancel the preparation in case of development of convulsive seizures.
Mania. SSRIs should be used with caution in patients with a history of mania/hypomania. When a manic state occurs, SSRIs should be discontinued.
Diabetes. In diabetic patients, SSRI treatment may affect glycemic control (hypoglycemia or hyperglycemia). Dosage of insulin and/or oral hypoglycemic agents may require adjustment.
Suicide. Suicidal attempts are characteristic of people in a state of depression, their threat may exist up to the achievement of a stable remission, both spontaneously and as a result of therapy. Patients taking antidepressants should be carefully monitored, especially at the beginning of therapy, for clinical deterioration and/or the appearance of suicidal thoughts and behavior.
Such caution is also appropriate in the treatment of patients with other psychiatric disorders due to the possible presence of concomitant major depressive disorder.
Akathisia. The use of SSRIs/SNRIs has been associated with the development of akathisia, a condition characterized by an unpleasant, debilitating feeling of restlessness and need to move, 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 treatment. Increasing the dose may harm patients who develop such symptoms.
Hyponatremia. Hyponatremia may be associated with impaired secretion of antidiuretic hormone while taking SSRIs, occurs rarely and usually disappears when therapy is discontinued. SSRIs should be used with caution in patients at risk (older age, presence of cirrhosis of the liver, or concomitant treatment with preparations that cause hyponatremia).
Hemorrhages. When taking SSRIs, hemorrhages (ecchymosis and purpura) may develop. SSRIs should be used with caution in patients with a bleeding tendency, as well as in patients taking anticoagulants and preparations that affect blood clotting.
ECT (electro-convulsive therapy). Clinical experience with concomitant use of SSRIs and ECT is limited, hence caution is advised.
Reverse selective MAO inhibitors type A Combining escitalopram and MAO type A inhibitors is not recommended due to the risk of serotonin syndrome.
serotonin syndrome. In patients taking SSRIs concomitantly with serotonergic preparations, in rare cases, serotonin syndrome may develop. It is necessary to use escitalopram with caution simultaneously with preparations that have a serotonergic effect. A combination of symptoms such as agitation, tremor, myoclonus, hyperthermia may indicate the development of serotonin syndrome. If such a situation arose, then SSRIs and serotonergic preparations should be urgently canceled and symptomatic treatment prescribed.
St. John's wort. The simultaneous use of SSRIs and herbal remedies containing St. John's wort may lead to an increase in the frequency of adverse reactions.
Use during pregnancy and lactation. Clinical data on the use of escitalopram in the treatment of pregnant women are limited. Escitalopram should not be given to pregnant women. The exceptions are cases where, after careful consideration of all risks and benefits, the need to prescribe the preparation has been clearly proven. A thorough examination of newborns whose mothers took escitalopram during pregnancy, especially in the third trimester, is recommended. Avoid abrupt discontinuation of the preparation during pregnancy.
Newborns of mothers taking SSRIs/SNRIs during late pregnancy may experience the following symptoms: respiratory distress, cyanosis, apnea, seizures, body temperature fluctuations, difficulty breastfeeding, vomiting, hypoglycemia, hypertension or hypotension, hyperreflexia, tremor, nervous agitation, irritability, apathy, constant crying, drowsiness and difficulty sleeping. These symptoms can develop as a result of both serotonergic effects and be signs of a withdrawal syndrome. In most cases, manifestations of complications occur immediately or soon (up to 24 hours) after childbirth.
Since escitalopram is excreted in breast milk, it is not recommended to prescribe the preparation during breastfeeding or breastfeeding should be discontinued.
Children. Use in children is contraindicated.
The ability to influence the reaction rate when driving vehicles or other mechanisms. In general, escitalopram does not affect the intellectual state or psychomotor functions, but the possible development of such adverse reactions from the nervous system as dizziness and drowsiness should be taken into account.
Interactions
Combinations are contraindicated
Non-selective MAO inhibitors. Escitalopram should not be used simultaneously with non-selective irreversible MAO inhibitors and within 2 weeks after stopping their use. Treatment with MAO inhibitors should begin no earlier than 7 days after discontinuation of escitalopram.
Pimozide. Due to the interaction of escitalopram with low doses of pimozide and the increased side effects of the latter, simultaneous use is contraindicated.
Unwanted Combinations
Moclobemide. Due to the risk of developing serotonin syndrome, the combination of escitalopram with the MAO-A inhibitor moclobemide is not recommended. If the use of this combination is considered necessary, then the minimum recommended doses are prescribed first under close medical supervision.
Combinations requiring caution
Selegilin. The combination with selegiline (an irreversible MAO inhibitor type B) requires caution. There is experience with the safe combination of selegiline up to 10 mg/day with racemic citalopram.
Serotonergic agents. Simultaneous use with serotonergic preparations (for example, with tramadol, sumatriptan and other triptans) can lead to the development of serotonin syndrome.
Preparations that lower the seizure threshold. SSRIs may lower the seizure threshold. Caution is advised when co-administering preparations that lower the seizure threshold (eg, antidepressants (tricyclics, SSRIs), neuroleptics (phenothiazines, thioxanthenes, butyrophenones), mefloquine, bupropion, and tramadol).
Lithium, tryptophan. Since cases of increased action have been reported with the combined use of SSRIs and lithium or tryptophan, it is recommended to prescribe these preparations with caution at the same time.
Anticoagulants. It is possible to change the effects of anticoagulants due to simultaneous use with escitalopram. In patients taking oral anticoagulants, it is necessary to carefully monitor the blood coagulation system before and after the use of escitalopram.
Alcohol. Escitalopram does not enter into a pharmacodynamic or pharmacokinetic interaction with alcohol.
Other preparations. The combined use of escitalopram and omeprazole (an inhibitor of CYP 2C19) increases the concentration of escitalopram in blood plasma by about 50%.
The combined use of escitalopram and cimetidine (a moderately strong main enzyme inhibitor) increases the concentration of escitalopram in blood plasma by about 70%.
Thus, when escitalopram is co-administered with CYP 2C19 inhibitors (eg, omeprazole, fluoxetine, fluvoxamine, lansoprazole, ticlopidine) and with cimetidine, caution should be exercised when prescribing upper dose limits of escitalopram. Dose reduction of escitalopram may be necessary depending on clinical judgment.
Overdose
Toxicity. Clinical data on escitalopram overdose are limited. many of the cases are caused by the simultaneous overdose of other preparations. in most cases, mild symptoms or asymptomatic overdose were observed. reports of death from escitalopram overdose are exceptional, most of them involving concurrent overdose of other preparations. taking doses of escitalopram in the range of 400-800 mg did not cause the development of any severe symptoms.
Symptoms. Signs of an overdose of escitalopram are mainly manifested by symptoms from the central nervous system (from dizziness, tremor and agitation to rare cases of serotonin syndrome, seizures and coma), the digestive tract (nausea / vomiting), the cardiovascular system (arterial hypotension, tachycardia, prolongation of the Q interval T, arrhythmia) and electrolyte imbalance (hypokalemia, hyponatremia).
Treatment. There is no specific antidote. Proper functioning of the respiratory system should be maintained, adequate oxygenation should be ensured, and gastric lavage should be applied as soon as possible. It is possible to use activated carbon. Vital signs should be monitored along with symptomatic supportive treatment.
Storage conditions
At a temperature not higher than 25 °C.
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