Zoloft 50mg №28 pills
A specific serotonin (5-HT) reuptake inhibitor in neurons in vitro that enhances the effects of 5-HT in animals. It has a very weak effect on the reuptake of norepinephrine and dopamine. In clinical doses, it blocks serotonin uptake in human platelets. It has no stimulating, sedative or anticholinergic effects and does not have cardiotoxicity in animals. In controlled trials in healthy volunteers, sertraline did not sedate and did not alter the psychomotor function. Due to the selective inhibition of seizure of 5-HT sertraline does not enhance catecholaminergic activity. Sertralin has no affinity for muscarinic cholinergic receptors, serotonin, dopamine, histamine, GABA, benzodiazepine and adrenergic receptors. Prolonged use of sertraline in animals led to a decrease in the activity of brain norepinephrine receptors; other clinically effective anti-depressive and anti-obsessive drugs have a similar effect.
Unlike tricyclic antidepressants, in the treatment of depression or obsessive-compulsive disorders (obsessive state) with sertraline, weight gain does not occur; in some patients, it even decreases.
Sertralin did not cause physical or psychological dependence.
In the range of 50 to 200 mg, sertraline pharmacokinetics are dose dependent.
Suction and distribution
In humans, when treated with sertraline at a dose of 50 to 200 mg 1 time / day for 14 days, Cmax was achieved 4.5–8.4 h after administration. Accordingly, T1 / 2 (in young and elderly men and women is 22-36 hours), there is approximately two-fold cumulation of the drug to achieve Css after 1 week of treatment (receiving the dose 1 time / day).
Food intake does not significantly affect the bioavailability of sertraline pills.
Plasma protein binding is about 98%. According to animal studies, sertraline has a large apparent volume of distribution.
Metabolism and excretion
Sertralin is actively biotransformed when it first passes through the liver. The main metabolite found in plasma, N-desmethyl sertraline, is significantly inferior in sertraline activity (approximately 20 times) in vitro and is actually not active in in vivo depression models. The average T1 / 2 of sertraline in young and elderly men and women is 22–36 h. T1 / 2 of N-desmethyl sertraline varies from 62–104 h.Sertralin and N-desmethylsertraline are actively biotransformed in humans; formed metabolites are excreted in feces and urine in equal amounts. Only a small part of the drug (less than 0.2%) is excreted in the urine unchanged.
Pharmacokinetics in special clinical situations
The pharmacokinetics of sertraline in the elderly and adolescents are similar.
Indications for use of the drug Zoloft pills 50mg №28
- treatment of depressive states (including those accompanied by anxiety), in the presence and absence of mania in history;
- treatment of obsessive compulsive disorder (OCD) in children and adults;
- treatment of panic disorders, accompanied or not accompanied by agoraphobia;
- posttraumatic stress disorder (PTSD).
Dosing regimen of the drug Zoloft, pills 50mg №28Zoloft is prescribed 1 time per day in the morning or in the evening. pills can be taken regardless of the meal.
For depression and OCD, treatment begins with a dose of 50 mg / day.
With insufficient effect, the daily dose can be increased gradually (by 50 mg), over several weeks, up to a maximum dose of 200 mg / day.
The initial effect can be observed 7 days after the start of treatment, however, the full effect is usually achieved in 2-4 weeks.
Treatment of panic disorders and PTSD begin with a dose of 25 mg / day, which is increased after 1 week to 50 mg / day. The use of the drug according to this scheme allows to reduce the frequency of early undesirable effects of treatment characteristic of panic disorder.
When conducting long-term maintenance therapy, the drug is prescribed in the minimum effective dose, which is subsequently changed depending on the clinical effect.
In the elderly, the drug is used in the same doses as in younger patients.
In children and adolescents aged 13-17 years suffering from OCD, treatment with Zoloft should be started with a dose of 50 mg / day. In children aged 6-12 years, OCD therapy begins with a dose of 25 mg / day, after 1 week it is increased to 50 mg / day. Subsequently, with insufficient effect, the dose can be increased in steps of 50 mg / day to 200 mg / day as needed. However, in order to avoid overdose, with increasing doses of more than 50 mg, it is necessary to take into account the lower body weight in children compared with adults.Change the dose should be at intervals of at least 1 week.
Side effect of the drug Zoloft pills 50mg №28
In controlled trials with repeated use of the drug in different doses compared with placebo, sertraline often caused the following adverse reactions:
On the part of the digestive system: nausea, diarrhea, unstable stool, lack of appetite, dyspepsia, dry mouth. An asymptomatic increase in the activity of aminotransferases (AST and ALT) in the treatment with sertraline occurred infrequently (approximately in 0.8% of cases). These disorders were usually observed during the first 1–9 weeks of treatment and quickly disappeared after discontinuation of the drug.
From the side of the central nervous system: tremor, dizziness, insomnia, drowsiness.
From the side of water and electrolyte balance: in some cases - hyponatremia (after stopping the treatment, the sodium level returned to normal); in some cases, hyponatremia may have been associated with inadequate secretion of antidiuretic hormone. In most cases, a decrease in sodium levels was observed in patients of more advanced age, as well as patients receiving diuretics and other drugs.
On the part of the blood coagulation system: transient thrombocytopenia, atypical bleeding and hemorrhagic rash, the causal relationship with the administration of the drug has not been established.
Other: increased sweating, impaired sexual function in men (mainly delayed ejaculation).
The adverse reaction profile encountered during double-blind, placebo-controlled trials in patients with an obsessive state was similar to that in patients with depression.
After the drug was introduced to the market, the following reports were noted in the submitted reports, which were sometimes observed when using the drug but could not be associated with it: vomiting, abdominal pain, movement disorders (extrapyramidal symptoms and gait disorders) cycle, hyperprolactinemia, galactorrhea, rash (including rare cases of erythema multiforme), rarely - pancreatitis and severe liver dysfunction (including hepatitis, jaundice and liver failure). Rare cases of withdrawal syndrome have been described. In rare cases, the following side effects were noted that could not be distinguished from the manifestations of the natural course of the underlying disease: paresthesia, hypoesthesia, symptoms of depression, hallucinations, aggressive reactions, agitation, anxiety, and psychosis.
Contraindications drug Zoloft pills 50mg №28- simultaneous administration of MAO inhibitors;
- Hypersensitivity to the drug.
Pregnancy and lactation
In pregnancy, sertraline should be prescribed only if the expected benefit outweighs the possible risk, since adequate well-controlled trials of the drug in pregnant women have not been carried out, and the results of studies in animals do not always allow us to predict the effect of the drug on the human reproductive function.
Information on the penetration of sertraline into breast milk is not available, so it is not recommended to prescribe the drug during lactation. There is limited information about the concentration of sertraline in mother's milk. Separate studies on a small number of lactating mothers and their children showed that sertraline level in the blood serum of children was insignificant or not determined, while its amounts in milk exceeded sertraline level in the mother's blood.
Women of childbearing age should use adequate methods of contraception during sertraline treatment.
In experimental studies with the administration of sertraline to rats and rabbits in doses approximately 20 and 10 times higher than the maximum daily doses for humans (in mg / kg), no signs of teratogenic action were found. Sertralin had no mutagenic action. Nevertheless, sertraline in doses of approximately 2.5-10 times the maximum daily doses for a person (in mg / kg) caused a delay in ossification of the fetal bone tissue, possibly as a result of the effect on the maternal individual. With the introduction of sertraline in doses of about 5 times the maximum dose for a person (in mg / kg), a decrease in the survival rate of newborns was observed.
Zoloft can be administered no earlier than 14 days after discontinuation of MAO inhibitors. MAO inhibitors can also be administered no earlier than 14 days after Zoloft is discontinued.
Care must be taken when prescribing Zoloft with other drugs that enhance serotonergic neurotransmission, such as tryptophan or fenfluramine. Until more data is available, serotonergic agents should not be used in combination with sertraline.
The experience of clinical trials, the purpose of which was to determine the optimal time required for transferring patients from taking other anti-depressant drugs to sertraline, is limited.Care must be taken with this transition, especially with long-acting drugs. The required interval between the cancellation of one selective serotonin reuptake inhibitor and the start of taking another similar drug has not been established.
Sertralin undergoes active metabolism in the liver. According to a pharmacokinetic study, with a single dose of sertraline in patients with stable liver cirrhosis, an increase in T1 / 2 of the drug and AUC (area under the concentration-time curve) was observed compared with those in healthy people. Caution should be used with sertraline in patients with liver disease; It is necessary to discuss the feasibility of reducing the dose or increasing the interval between taking the drug.
Sertralin unchanged is excreted in the urine in small quantities. In patients with primary and moderately severe renal insufficiency (CC 20-50 ml / min) and patients with severe renal insufficiency (CC less than 20 ml / min), the pharmacokinetic parameters of sertraline did not differ significantly from the control when taken once. However, the pharmacokinetics of sertraline in an equilibrium state in this category of patients has not been studied sufficiently, therefore caution should be exercised in treating patients with renal insufficiency.
In patients with convulsive syndrome, Sertralin has not been studied, therefore, its use in unstable epilepsy should be avoided, and patients with controlled epilepsy should be carefully monitored during treatment. In the event of convulsions in all cases, the drug must be discontinued.
When testing sertraline, hypomania and mania were observed in about 0.4% of patients receiving sertraline. Cases of activation of mania / hypomania are also described in a small proportion of patients with major depression who received other anti-depressive or anti-obsessive drugs.
The risk or benefit of combined use of electroconvulsive therapy and sertraline has not been studied in clinical studies.
Depression patients tend to attempt suicide, which persists until a significant improvement in their condition as a result of treatment. In this regard, at the beginning of treatment of patients must be carefully monitored.
In clinical studies on the effectiveness of sertraline in the elderly, its effectiveness in patients in this group was demonstrated in over 700 patients over 65 years of age. The profile and frequency of adverse reactions in elderly and younger patients were the same.
While taking Zoloft, they do not recommend drinking alcohol.
Use in pediatrics
In completed and ongoing studies, sertraline received more than 250 children with OCD. The safety of sertraline in these studies was comparable to that in studies in adult OCD patients. The effectiveness of sertraline in depression or panic disorder in children in controlled studies has not been established.
The safety and efficacy of sertraline in children less than 6 years old have not been proven.
Influence on ability to drive motor transport and control mechanisms
Studies have shown that sertraline does not affect the psychomotor function. However, anti-depressive or anti-obsessive drugs can impair mental or physical activity necessary to perform potentially dangerous functions, such as driving a car or controlling machinery, which is necessary to warn the patient.
An overdose of the drug Zoloft pills 50mg №28
Toxicological studies in various animal species have demonstrated a good tolerability of sertraline.
Available data suggest a wide range of safety of sertraline in case of overdose. Reported cases of overdose with sertraline monotherapy in a dose of up to 13.5 g. There have been cases of death in overdose of sertraline in combination with other drugs and / or alcohol. In this regard, in all cases, overdose requires intensive treatment.
Treatment. Recommendations for specific treatment of overdose, as well as specific antidotes, are not available. It is necessary to ensure normal airway, oxygenation and ventilation of the lungs. Activated carbon, which can be used in combination with sorbitol, may be even more effective than vomiting or gastric lavage. It is advisable to monitor the performance of the heart and other vital organs and to carry out symptomatic and supportive therapy.The use of forced diuresis and hemodialysis is impractical because of the large volume of distribution of the drug.
Cases of serious adverse reactions in patients who received sertraline in combination with MAO inhibitors, including selective inhibitors of MAO (selegilin) and reversible inhibitors of MAO (moclobemide). Symptoms of this interaction include: hyperthermia, rigidity, muscle cramps, changes in the mental state, which include confusion, irritability and excessive agitation with the development of delirium and coma.
Simultaneous administration of Zolofta in a dose of 200 mg / day does not enhance the effect of ethanol, carbamazepine, haloperidol or phenytoin on cognitive and psychomotor function in healthy people.
Sertralin binds to plasma proteins, so you need to consider the possibility of its interaction with other drugs that bind to proteins. However, when conducting 3 official studies on the interaction with diazepam, tolbutamide and warfarin, no significant effect on the binding of drugs to proteins was found.
Simultaneous administration of Zolofta at a dose of 200 mg / day with diazepam or tolbutamide led to a small, but statistically significant change in some pharmacokinetic parameters.
Cimetidine caused a significant decrease in sertraline clearance when used in combination with Zoloft.
With the simultaneous use of sertraline had no effect on the beta-adrenoceptor blocking activity of atenolol.
Signs of interaction of Zoloft 200 mg / day with glibenclamide and digoxin were not detected.
While taking Zoloft 200 mg / day with warfarin, a small but statistically significant increase in prothrombin time was observed. In this regard, you should carefully monitor the prothrombin time at the beginning of sertraline therapy and after its cancellation.
Many antidepressants, for example, selective serotonin reuptake inhibitors, including sertraline, and most tricyclic antidepressants, inhibit the biochemical activity of the drug metabolizing enzyme, cytochrome P450 2D6 (debrisoquine hydroxylase), and as a result, can increase plasma concentration of other drugs that are biotransformed in the plasma form of other cells that are biotransformed. have a narrow therapeutic index, for example, tricyclic antidepressants and class 1 antiarrhythmic drugs (propafenone and flecainide). Antidepressants differ in the degree of inhibiting effect on P450 2D6.In two clinical studies of the interaction of desipramine and serotonin reuptake inhibitors in recommended doses in healthy volunteers, the effect of Zoloft and two other selective serotonin reuptake inhibitors was compared. In the first study, the average area under AUC0-24 of desipramine in an equilibrium state increased by 23% and 380% with simultaneous use with Zoloft and the comparator, respectively. In the second study, when using another selective serotonin reuptake inhibitor as a comparison drug, the average AUC0-24 of desipramine in the equilibrium state increased by 37% and 421% with simultaneous use with Zoloft and the comparator respectively. The results of these studies suggest that the Zoloft effect compared with the other two selective serotonin reuptake inhibitors was significantly less pronounced. However, with the simultaneous use of a drug that undergoes biotransformation of P450 2D6, and Zoloft, it may be necessary to prescribe the first one in a lower dose than usual. In addition, if Zoloft is canceled, it may be necessary to increase the dose of another drug.
Prolonged use of Zolofta at a dose of 200 mg / day did not significantly affect plasma levels of carbamazepine as compared with placebo (marker activity of P450 3A3 / 4 isoenzyme). In vitro studies indicate that sertraline does not inhibit or inhibits little activity of P450 1A2. The clinically insignificant effect of long-term use of Zolofta at a dose of 200 mg / day on the concentration of tolbutamide, phenytoin and warfarin in the blood plasma suggests that sertraline does not have a clinical effect of inhibiting CYP 2C9. The clinically insignificant effect of long-term use of Zolofta at a dose of 200 mg / day on plasma diazepam concentration suggests that sertraline does not have a clinical effect of inhibiting CYP 2C19.
Judging by the decrease in T1 / 2 of antipyrine, sertraline induces hepatic enzymes, but this does not represent any clinical significance.
In placebo-controlled trials in healthy volunteers, sertraline did not significantly affect the pharmacokinetics of lithium, however, compared with placebo, increased tremor, indicating a possible pharmacodynamic interaction.In this regard, while simultaneous treatment with sertraline, as well as other selective serotonin reuptake inhibitors, in combination with other drugs such as lithium, which can act through serotonergic mechanisms, care must be taken.
Terms and conditions of storage
The drug should be stored at a temperature not higher than 30 ° C.
Shelf life - 5 years.
Pharmacy sales terms
The drug is available on prescription.
It is a drug. Consultation with a doctor is required.