Instructions for medical use of the drug Enterosgel®
Registration number: LP-N_(000036)-(RG-RU)
Trade name: Enterosgel®.
Group name: polymethylsiloxane polyhydrate.
Chemical name: nonlinear polycondensation product
1,1,3,3-tetrahydroxy-1,3-dimethyldisiloxane polyhydrate.
Dosage form: paste for oral administration.
Pharmacological properties
Enterosgel® has a porous structure of an organosilicon matrix (molecular sponge) of a hydrophobic nature, which is characterized by a sorption effect in relation only to medium-molecular toxic metabolites (mm from 70 to 1000). Enterosgel® has pronounced sorption and detoxification properties. In the lumen of the gastrointestinal tract, the drug binds and removes from the body endogenous and exogenous toxic substances of various natures, including bacteria and bacterial toxins, antigens, food allergens, drugs and poisons, heavy metal salts, radionuclides, alcohol. The drug also absorbs some metabolic products of the body, including excess bilirubin, urea, cholesterol and lipid complexes, as well as metabolites responsible for the development of endogenous toxicosis. Enterosgel® does not reduce the absorption of vitamins and microelements, helps restore disturbed intestinal microflora and does not affect its motor function.
Pharmacokinetics
The drug is not absorbed from the gastrointestinal tract and is excreted unchanged within 12 hours.
Indications for use
In adults and children as a detoxifying agent:
- acute and chronic intoxications of various origins;
- acute poisoning with potent and toxic substances, including drugs and alcohol, alkaloids, salts of heavy metals;
- acute intestinal infections of any origin as part of complex therapy (toxic infections, salmonellosis, dysentery, diarrheal syndrome of non-infectious origin, dysbacteriosis);
- purulent-septic diseases accompanied by severe intoxication, as part of complex therapy;
- food and drug allergies;
- hyperbilirubinemia (viral hepatitis) and hyperazotemia (chronic renal failure);
- for the purpose of preventing chronic intoxication for workers in hazardous industries (occupational intoxication with chemical agents of polytropic action, xenobiotics, incorporated radionuclides, compounds of lead, mercury, arsenic, petroleum products, organic solvents, oxides of nitrogen, carbon, fluorides, salts of heavy metals).
Contraindications
Individual intolerance to the drug, intestinal atony.
Use during pregnancy and breastfeeding
Enterosgel® is not contraindicated during pregnancy and breastfeeding.
Directions for use and doses
Enterosgel® paste is taken orally 1-2 hours before or after meals or taking other medications with water.
It is recommended to mix the required amount of the drug in a glass with three times the volume of water at room temperature or take it orally with water.
- Dosage for adults: 15 g – 22.5 g (1 – 1.5 tablespoons) 3 times a day. Daily dose 45 g – 67.5 g.
- Children aged 5 to 14 years – 15 g (1 tablespoon) 3 times a day. Daily dose 45 g.
- Children under 5 years of age – 7.5 g (0.5 tablespoon) 3 times a day. Daily dose 22.5 g.
- It is recommended for infants to mix 2.5 g (0.5 teaspoon) of the drug in three times the volume of breast milk or water and give it before each feeding (6 times a day).
- For the prevention of chronic intoxication - 22.5 g 2 times a day for 7-10 days monthly. In case of severe intoxication, the dose of the drug can be doubled during the first three days.
The duration of treatment for acute poisoning is 3-5 days, and for chronic intoxication and allergic conditions 2-3 weeks. Repeated course on doctor's recommendation.
Side effect
Possible nausea and constipation. In case of severe renal and/or liver failure, a feeling of disgust towards the drug may occur.
Overdose
No cases of overdose have been identified.
Interaction with other drugs
The absorption of other drugs may be reduced when taken simultaneously with Enterosgel®.
special instructions
The drug can be used in complex therapy with other drugs, subject to the rule of taking it separately in time, 1-2 hours before or after taking other drugs.
Impact on the ability to drive vehicles and machinery
No influence of Enterosgel® on the ability to drive vehicles or operate machinery has been identified.
Release form
Paste for oral administration
90 g and 225 g in laminated tubes made of combined materials.
22.5 g in bags made of a combined two-layer material based on aluminum foil and film.
Each tube of 90 g and 225 g or 2, 10, 20 bags of 22.5 g together with instructions for use are placed in a cardboard pack.
Storage conditions
Store at a temperature not lower than 4 °C and not higher than 30 °C. Keep out of the reach of children. Protect from drying out after opening the package. Protect from freezing.
Best before date
3 years. Do not use after the expiration date stated on the package. .
Vacation conditions
Available without a prescription.
Manufacturer: TNK SILMA LLC
399851, Russia, Lipetsk region, Dankov, st. L. Tolstoy, 32/2 Tel./fax, www.enterosgel.ru, e-mail: [email protected]
Name and address of the owner of the registration certificate: FARMASIL LLC, 115573, Russia, Moscow, st. Shipilovskaya, 50 bldg. 1, p. 2, floor 1, room. I, room 5 Tel./fax, www.enterosgel.ru, e-mail
Organization accepting complaints:
TNK SILMA LLC, 115573, Russia, Moscow, st. Shipilovskaya, 50 bldg. 1, p. 2 Tel./fax, www.enterosgel.ru, e-mail
Instructions for use Enterosgel (sweet paste)
Aleval
Sertraline should not be co-administered with MAOIs, within 14 days before starting MAOIs and for 14 days after their discontinuation.
Blood concentrations of tricyclic antidepressants should be monitored to assess the need for dose adjustment.
When using sertraline and tolbutamide simultaneously, it is necessary to monitor blood glucose levels.
Serotonin syndrome
With the use of selective serotonin reuptake inhibitors (SSRIs), cases of the development of serotonin syndrome (SS) and neuroleptic malignant syndrome (NMS) have been described. The risk of these complications increases with the simultaneous use of SSRIs with other serotonergic drugs (including amphetamines, triptans and fentanyl and their analogues, tramadol, dexomethorphan, tapentadol, meperedine, methadone, pentazocine), as well as drugs that affect the metabolism of serotonin (including monoamine oxidase inhibitors), antipsychotics and other dopamine receptor antagonists. Manifestations of SS may include changes in mental status (in particular, agitation, hallucinations, coma), autonomic lability (tachycardia, blood pressure fluctuations, hyperthermia), changes in neuromuscular transmission (hyperreflexia, impaired motor coordination) and/or gastrointestinal disorders (nausea, vomiting and diarrhea).
Some manifestations of SS. including hyperthermia, muscle rigidity, autonomic lability with possible rapid fluctuations in vital function parameters, as well as changes in mental status, may resemble the symptoms that develop with NMS. It is necessary to monitor patients for the development of clinical manifestations of SS and NMS.
Prolongation of the QTc interval or ventricular tachysystolic arrhythmia of the “torsade de pointes” type (TdP)
During post-marketing use of sertraline, ECG QTc prolongation and torsade de pointes (TdP) have been reported. Most cases were observed in patients with risk factors for developing such conditions. Therefore, caution should be exercised when using sertraline in patients with risk factors for ECG QTc prolongation or torsade de pointes (TdP).
Switching from other SSRIs, antidepressants or anti-obsessive medications
The required interval between stopping one SSRI and starting another similar drug has not been established. Caution should be exercised when switching to sertraline from other SSRIs, antidepressants or anti-obsessive medications, especially from long-acting medications such as fluoxetine.
When replacing one neuronal serotonin uptake inhibitor with another, there is no need for a washout period. However, caution is required when changing the course of treatment.
Other serotonergic drugs, such as tryptophan, fenfluramine and 5-HT agonists Concomitant use of sertraline with other drugs with significant effects on neurotransmitter transmission (such as amphetamines, tryptophan, fenfluramine, 5-HT agonists or herbal medicines, St. John's wort) should use with caution and, if possible, avoid due to potential pharmacodynamic interactions.
Suicidal behavior
Depression is associated with an increased risk of suicidal ideation, self-harm, and suicide.
This risk persists until stable remission. Given that the patient's condition may not improve in the first few weeks of therapy or longer, patients should be closely monitored until such improvement occurs. It is also common for the risk of suicide to increase during the early stages of recovery.
Other medical conditions for which sertraline may be prescribed may also be associated with an increased risk of suicidal events. In addition, these diseases may accompany major depressive disorder. In this regard, the same precautions should be taken as when treating major depressive disorder.
Patients with a history of suicidal tendencies or patients prone to suicidal ideation before starting therapy have a higher risk of suicidal thoughts or suicide attempts. Such patients should also be under close medical supervision during therapy.
All patients, especially those at risk, receiving sertraline therapy should be carefully monitored to detect the development or worsening of symptoms of suicidal behavior. Patients, their relatives and guardians should be warned of the need to monitor the condition for the emergence or worsening of depression, the emergence of suicidal thoughts or behavior, as well as for any changes in behavior, especially at the beginning of therapy and with any change in the dose of the drug. The risk of suicide attempts should also be kept in mind, especially in patients with depression. In this regard, in order to reduce the risk of overdose, it is necessary to take the minimum dose of the drug that provides a sufficient therapeutic effect.
Patients with depression and other mental disorders are at risk of suicidal behavior. These diseases themselves are strong predisposing factors for such behavior. In children, adolescents and young adults (ages 18–24 years) with depression or other mental disorders, antidepressants (SSRIs and others) have been found to increase the risk of suicidal ideation and behavior compared with placebo. Therefore, when using sertraline or any other antidepressants in children, adolescents and young adults (under 24 years of age), the risk of suicide should be weighed against the benefits of their use. In addition, there was no increase in the risk of suicidal behavior in adult patients over 24 years of age, and a decrease in this risk was noted in patients aged 65 years and older.
Sexual dysfunction
Selective serotonin reuptake inhibitors (SSRIs) may cause symptoms of sexual dysfunction. There have been reports of long-term sexual dysfunction, symptoms of which persisted despite discontinuation of SSRIs.
Use in children and adolescents under 18 years of age
Sertraline should not be used to treat children and adolescents under the age of 18 years, with the exception of patients with OCD aged 6-17 years. Suicidality (suicide attempts or suicidal thoughts) and hostility (primarily aggressiveness, oppositional behavior and anger) were observed more often in patients receiving antidepressant therapy than in patients receiving placebo. If a decision is made to proceed with therapy based on the clinical assessment of the patient, the patient should be carefully monitored for symptoms of suicidal behavior. In addition, it should be borne in mind that data on the effect of the drug on child growth, puberty and cognitive behavioral development are limited.
During long-term therapy of pediatric patients, clinicians should monitor for abnormal developmental abnormalities.
Withdrawal syndrome
When stopping a drug, withdrawal symptoms often occur, especially if the drug is stopped abruptly. Withdrawal symptoms were observed in 23% of patients who stopped taking sertraline and in 12% of patients who continued taking the drug.
The risk of these symptoms depends on several factors, including the duration of therapy and dosage, and the rate of dose reduction. The most common reactions are dizziness, sensory disturbances (including paresthesia), sleep disturbances (including insomnia and deep sleep), agitation or anxiety, nausea and/or vomiting, tremor and headache. These symptoms are usually mild to moderate in severity; however, in some cases they can be severe. Typically, these symptoms occur during the first few days of discontinuation of therapy, but there are very rare reports of the development of such symptoms in patients who inadvertently missed a dose. Typically these symptoms do not get worse and resolve within two weeks, except in some cases where they may last longer (2-3 months or more). In this regard, it is recommended to discontinue the drug gradually, reducing the dose over several weeks or months, depending on the patient's condition.
Akathisia/psychomotor agitation
Sertraline use may be associated with the development of akathisia, characterized by a subjective feeling of discomfort or restlessness and a need to move, accompanied by an inability to sit or stand still. Most often, such symptoms are observed in the first weeks of treatment. Increasing the dose in these patients may be harmful.
Liver dysfunction
If it is necessary to use sertraline in patients with impaired liver function, consider reducing the dose of the drug or the frequency of administration. Sertraline should not be taken in patients with severe hepatic impairment.
Renal dysfunction
It was found that, as expected, given the insignificant renal excretion of sertraline, no dose adjustment is required depending on the severity of renal failure.
Electroconvulsive therapy
The possible success or risk of this combination treatment has not been studied (clinical data are not available).
Convulsions
There is no experience with the use of sertraline in patients with convulsive syndrome, so its use should be avoided in patients with unstable epilepsy, and patients with controlled epilepsy should be carefully monitored during treatment. If seizures occur, the drug should be discontinued.
Activation of mania/hypomania
During clinical studies prior to the marketing of sertraline, mania and hypomania were observed in approximately 0.4% of patients receiving sertraline. Cases of activation of mania/hypomania have also been described in a small proportion of patients with manic-depressive psychosis who received other antidepressant or antiobsessive drugs. Sertraline should be used with caution in patients with a history of mania or hypomania. Close medical supervision is necessary and sertraline should be discontinued if the patient exhibits any signs of mania.
Schizophrenia
Patients with schizophrenia may experience exacerbation of psychotic symptoms.
Pathological bleeding/hemorrhage
There are reports of the development of bleeding or hemorrhage from ecchymosis and purpura to life-threatening bleeding/hemorrhage) during the use of SSRIs. Caution should be exercised when prescribing SSRIs in combination with drugs that have an established ability to affect platelet function (for example, atypical antipsychotics and phenothiazines, most tricyclic antidepressants, acetylsalicylic acid and non-steroidal anti-inflammatory drugs), as well as in patients with a history of hemorrhagic diseases.
In addition, when using sertraline with indirect anticoagulants, it is recommended to monitor the prothrombin time at the beginning of treatment with sertraline and after its discontinuation.
Hyponatremia
Transient hyponatremia occurs more often in older patients, in patients with dehydration, or when taking diuretics. This side effect is associated with the syndrome of inappropriate secretion of antidiuretic hormone.
Cases of decreased plasma sodium concentrations below 110 mmol/L have been reported. If symptomatic hyponatremia develops, sertraline should be discontinued and adequate therapy aimed at correcting the concentration of sodium in the blood should be prescribed. Signs and symptoms of hyponatremia include headache, difficulty concentrating, memory loss, weakness and unsteadiness, which can lead to falls. In more severe cases, hallucinations, fainting, seizures, coma, respiratory arrest, and death may occur.
Due to the fact that there is a clear relationship between the development of depression and OCD, depression and panic disorders, depression and PTSD, depression and social phobia, in the treatment of patients with OCD. Panic disorders, PTSD and social phobia should take the same precautions as when treating depression.
Fractures
Based on epidemiological studies, it has been established that the use of serotonin reuptake inhibitors, including sertraline, increases the risk of fractures. The mechanism leading to the increased risk is not completely clear.
Elderly patients
The profile of adverse reactions in elderly and young patients does not differ. In old age, the drug should be used with caution due to the increased risk of developing hyponatremia.
Diabetes mellitus/impaired blood glucose control
Exacerbation of diabetes mellitus and/or impaired glucose control (hyperglycemia and hypoglycemia) have been reported with the use of SSRIs, including sertraline, in patients with or without diabetes mellitus. In this regard, glucose levels should be monitored. Particular attention is required in patients with diabetes mellitus, as they may require dose adjustment of oral hypoglycemic agents and/or insulin. Angle-closure glaucoma
SSRIs, including sertraline, affect pupil size, leading to mydriasis. In this case, a narrowing of the angle of the eye is observed, which leads to an increase in intraocular pressure and the development of angle-closure glaucoma, especially in patients with a predisposition. The drug should be used with caution in patients with angle-closure glaucoma or a history of glaucoma.
Laboratory methods
False-positive urine immunoassays for benzodiazepines have been reported in patients taking sertraline. This is due to the low specificity of screening tests. False-positive results may also occur for several days after discontinuation of sertraline therapy. Additional tests such as gas chromatography and mass spectrometry can help distinguish sertraline from benzodiazepines.
Grapefruit juice
Concomitant use of sertraline and grapefruit juice is not recommended.
Aleval, 50 mg, film-coated tablets, 28 pcs.
Sertraline should not be co-administered with an MAOI, or within 14 days of stopping treatment with an MAOI. Similarly, after discontinuation of sertraline, no MAOIs are prescribed for 14 days.
Serotonin syndrome and neuroleptic malignant syndrome
When using selective serotonin reuptake inhibitors (SSRIs), cases of the development of serotonin syndrome (SS) and neuroleptic malignant syndrome (NMS) have been described, the risk of which increases when combining SSRIs with other serotonergic drugs (including triptans), as well as drugs that affect metabolism serotonin (including monoamine oxidase inhibitors), antipsychotics and other dopamine receptor antagonists. Manifestations of SS may include changes in mental status (in particular, agitation, hallucinations, coma), autonomic instability (tachycardia, blood pressure fluctuations, hyperthermia), changes in neuromuscular transmission (hyperreflexia, incoordination) and/or gastrointestinal disorders (nausea, vomiting and diarrhea). Some manifestations of SS, including hyperthermia, muscle rigidity, autonomic instability with the possibility of rapid fluctuations in vital signs, and changes in mental status, may resemble symptoms that develop in NMS.
Other serotonergic drugs - Caution should be exercised when sertraline is co-administered with other drugs that enhance serotonergic neurotransmission, such as tryptophan, fenfluramine or 5-HT agonists. Such co-administration should be avoided whenever possible, given the potential for pharmacodynamic interactions.
Switching from other selective serotonin reuptake inhibitors (SSRIs), antidepressants, or medications used for OCD.
The experience of clinical studies aimed at determining the optimal time required to transfer patients from taking other antidepressants and drugs used for OCD to sertraline is limited. Caution must be used when switching, especially from long-acting drugs such as fluoxetine. The required interval between stopping one selective serotonin reuptake inhibitor and starting another similar drug has not been established.
It should be noted that there is no sufficient experience with the use of sertraline in patients undergoing electroconvulsive therapy. The possible success or risk of this combination treatment has not been studied.
There is no experience with the use of sertraline in patients with seizure disorders, so its use should be avoided in patients with unstable epilepsy, and patients with controlled epilepsy should be carefully monitored during treatment. If seizures occur, the drug should be discontinued.
Patients with depression are at risk for suicide attempts. This danger persists until remission develops. Therefore, from the start of treatment until the optimal clinical effect is achieved, patients should be under constant medical supervision.
Activation of manic disorders. During clinical studies prior to the marketing of sertraline, manic episodes were observed in approximately 0.4% of patients taking sertraline. Cases of activation of manic disorders have also been described in a small proportion of patients with manic-depressive psychosis who received other antidepressants or drugs used for OCD.
Use for liver failure. Sertraline is actively biotransformed in the liver. According to a pharmacokinetic study, with repeated administration of sertraline in patients with stable mild liver cirrhosis, an increase in the half-life of the drug and an almost threefold increase in AUC (area under the concentration-time curve) and maximum concentration of the drug were observed compared with those in healthy people. There were no significant differences in plasma protein binding between the two groups. Sertraline should be used with caution in patients with liver disease. When prescribing the drug to a patient with impaired liver function, it is necessary to discuss the advisability of reducing the dose or increasing the interval between taking the drug.
Use for renal failure. Sertraline undergoes active biotransformation, so it is excreted unchanged in the urine in small quantities. In patients with mild to moderate renal failure (creatinine clearance 30–60 ml/min) and patients with moderate or severe renal failure (creatinine clearance 10–29 ml/min or less), pharmacokinetic parameters (AUC0-24 and Cmax) of sertraline with repeated administration did not differ significantly from the control group. In all groups, the half-life of the drug was the same, and there were no differences in plasma protein binding. The results of this study suggest that, as expected given the low renal excretion of sertraline, no dosage adjustment is required based on the severity of renal impairment.
Pathological bleeding/hemorrhage. It is recommended to exercise caution when prescribing selective serotonin reuptake inhibitors in combination with drugs that have an established ability to alter platelet function, as well as in patients with a history of hemorrhagic diseases.
Hyponatremia. Transient hyponatremia may occur during treatment with sertraline. This develops more often in older patients, as well as when taking diuretics or a number of other drugs. This side effect is associated with the syndrome of inappropriate secretion of antidiuretic hormone. If symptomatic hyponatremia develops, sertraline should be discontinued and adequate therapy aimed at correcting the concentration of sodium in the blood should be prescribed. Signs and symptoms of hyponatremia include headache, difficulty concentrating, memory problems, weakness and unsteadiness, which can lead to falls. In more severe cases, hallucinations, fainting, seizures, coma, respiratory arrest, and death may occur.
Use in children. In children, adolescents and young adults (under 24 years of age) with depression and other mental disorders, antidepressants, compared with placebo, increase the risk of suicidal thoughts and suicidal behavior. Therefore, when prescribing Aleval or any other antidepressants in children, adolescents and young adults (under 24 years of age), the risk of suicide should be weighed against the benefits of their use. In short-term studies, the risk of suicide did not increase in people over 24 years of age, but it decreased slightly in people over 65 years of age. Any depressive disorder itself increases the risk of suicide. Therefore, during treatment with antidepressants, all patients should be monitored for early detection of disturbances or changes in behavior, as well as suicidality.
Impact on the ability to drive vehicles and operate machinery
During treatment with sertraline, driving vehicles, special equipment or engaging in activities associated with increased risk is not recommended.
