Pharmacological properties of the drug Zoloft
Pharmacodynamics. Sertraline is a potent and nonspecific inhibitor of serotonin (5-HT) reuptake in neurons. Very little effect on the reuptake of norepinephrine and dopamine. At therapeutic doses, sertraline blocks the uptake of serotonin into human platelets. It does not have a stimulating, sedative or anticholinergic effect, and also does not exhibit a cardiotoxic effect in the experiment. In controlled trials in healthy volunteers, sertraline did not cause sedation or affect psychomotor performance. Consistent with its selectivity for (5-HT) reuptake inhibition, sertraline does not stimulate catecholaminergic activity. Sertraline does not show affinity for muscarinic, serotonergic, dopaminergic, adrenergic, histaminergic, GABAergic and benzodiazepine receptors. Long-term use of sertraline in animals led to a decrease in the activity of brain adrenergic receptors; Other antidepressants and anti-obsessive drugs exhibit a similar effect. Sertraline does not cause drug dependence; does not have the stimulant and anxiety effects of d-amphetamine or the sedation and psychomotor effects of alprazolam. Pharmacokinetics. In the dose range of 50–200 mg, the pharmacokinetics of sertraline are dose dependent. When sertraline was administered orally at a dose of 50–200 mg once a day for 14 days, the concentration of the drug in the blood plasma reached its maximum level 4.5–8.4 hours after administration. The pharmacokinetic profile in adolescents and the elderly does not differ significantly from that in adult patients aged 18–65 years. The half-life of sertraline in young and old men and women is 22–36 hours. In accordance with the terminal half-life, a double cumulation is observed upon reaching an equilibrium concentration, which is achieved after 1 week of treatment (use once a day). Plasma protein binding is 98%. Animal studies have demonstrated a large apparent volume of distribution for sertraline. The pharmacokinetics of sertraline in children with obsessive-compulsive disorder (OCD) are the same as in adults (although sertraline is metabolized somewhat more rapidly in children). However, it may be appropriate to use it at lower doses in children, given their lower body weight and the need to prevent excessive plasma concentrations. Sertraline undergoes biotransformation during its initial passage through the liver. Its major plasma metabolite is Ν-desmethylsertraline, which has much lower activity (approximately 20-fold) than sertraline in vitro in vivo models of depression . The half-life of N-desmethylsertraline is 62–104 hours. Sertraline and N-desmethylsertraline undergo intensive biotransformation in the human body, and the final metabolites are excreted in feces and urine in equivalent amounts. Only a small portion of sertraline (≤0.2%) is excreted unchanged in the urine. Concomitant food intake does not significantly affect the bioavailability of sertraline.
special instructions
Zoloft 100 mg, buy in Moscow or other cities, only with a prescription. The tablets are packaged in blisters and placed in cardboard boxes along with instructions. It is important to understand that if you take Zoloft, the side effects of which are extensive, without following the doctor's recommendations, it can cause serious consequences.
The drug does not affect psychomotor reactions. This means that there are no restrictions on driving a car during the treatment period.
The price of the drug Zoloft is affordable. In most cases, one package is enough for a course of treatment. The exception is complex pathological conditions that require long-term therapy. Cheaper analogues of Zoloft can be purchased in pharmacies. The most famous of them are Stimuloton and Surlift.
Indications for use of the drug Zoloft
Depression (including accompanied by anxiety) with or without a history of mania. OCD in adults and children. Panic disorders, with or without agoraphobia. Post-traumatic stress disorder (PTSD). Social phobia (social anxiety disorder). If the treatment outcome is satisfactory, continuation of sertraline therapy is an effective means of preventing recurrence of the initial episode of depression and its development in the future; relapse of an initial episode of OCD; panic disorder, initial episode of PTSD, social phobia.
Use of the drug Zoloft
Orally 1 time per day in the morning or evening, regardless of meals. Beginning of treatment For depression and OCD : treatment should begin with a dose of 50 mg/day. Panic disorders, PTSD and social phobia : start with a dose of 25 mg/day, after 1 week the dose of the drug is increased to 50 mg/day. This dosage regimen reduces the incidence of side effects at the initial stage of treatment of panic disorders. Dose titration Depression, OCD, panic disorder, PTSD : if the effect of the 50 mg dose is insufficient, the dose can be increased. Dose adjustment should begin no earlier than after 1 week of treatment, titration dose - 50 mg per week. The dose should not exceed 200 mg/day. Dose adjustments should be made no more than once a week, taking into account the half-life of sertraline, which is 24 hours. The first manifestations of the clinical effect are observed within 7 days of treatment. However, a longer period is required for its full development, especially in OCD. Maintenance dose When carrying out long-term treatment, the dose should be minimally effective; it is subsequently adjusted depending on the response to treatment (therapeutic effect). Use in children The safety and effectiveness of sertraline have been established for children and adolescents with OCD aged 13–18 years. There is no experience with the use of sertraline in children under 6 years of age, as well as in other pathologies. When using sertraline in children with OCD (age 13–18 years), a dose of 50 mg/day should be used. If there is no effect when taking the drug at a dose of 50 mg/day, if necessary, it may be further increased to 200 mg/day. In clinical trials in children aged 13 to 18 years with depression or OCD, the pharmacokinetic profile of sertraline was similar to that in adults. However, in pediatrics, when increasing the dose of 50 mg, the lower body weight in children compared to adults should be taken into account. Dose titration in children The half-life of sertraline is about 24 hours. Dose adjustments should not be made more than once a week. Use in elderly people In elderly people (over 65 years of age), the drug is used in the same doses as in younger people (up to 65 years of age). Side effects and their frequency were the same as in younger patients. Use in patients with liver failure In patients with liver disease, sertraline is used with caution. In patients with liver failure, the dose or frequency of administration should be reduced. Use in patients with renal failure Sertraline is intensively metabolized in the body, so a small amount of the drug is excreted unchanged in the urine. Due to the insignificant renal excretion of sertraline, there is no need to change the dose of the latter in patients with renal failure.
Zoloft®
Sertraline should not be co-administered with MAOIs, within 14 days before starting an IMAO 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 golbutamide simultaneously, it is necessary to monitor blood glucose levels (see section “Interaction with other drugs”).
Serotonin syndrome
Cases of the development of serotonin syndrome (SS) and neuroleptic malignant syndrome (NMS) have been described with the use of SSRIs. The risk of these complications increases with simultaneous use of SSRIs with other serotonergic drugs (including trintanes and fentanyl and their analogues, tramadol, dexomstorphan, 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 signs, as well as changes in mental status, may resemble symptoms that develop in NMS. It is necessary to monitor patients for the development of clinical manifestations of SS and PVD.
Prolongation of the OTc interval or arrhythmia ventricular tachysystolic tina “pirouette” (torsade de pointes)
During post-marketing use of sertraline, cases of prolongation of the QTc interval on the ECG and the development of ventricular tachysystolic arrhythmia of the torsades de pointes type 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 prolongation of the QTc interval on the ECG or the development of torsade dc pointes.
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
The simultaneous use of sertraline with other drugs with a pronounced effect on neurotransmitter transmission (such as tryptophan, fenfluramine, 5-HT agonists or herbal medicines, St. John's wort) should be used with caution and, if possible, avoided, given the potential pharmacodynamic interaction.
Suicidal behavior
Depression is associated with an increased risk of suicidal ideation, self-harm, and suicide. This risk persists until stable remission. Given that improvement in the patient's condition may not occur 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 in the treatment of 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.
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 growth, puberty and cognitive and behavioral development of the child 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/nsychomotor agitation
The use of sertraline 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, hypomania and mania 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 anti-depressive or anti-obsessive 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 or 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 automatic hyonatremia 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, when treating patients with OCD, panic disorders, PTSD and social phobia, the same precautions should be taken 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 is not different. In old age, the drug should be used with caution due to the increased risk of developing hyponatremia.
Diabetes mellitus/impaired blood glucose control When using SSRIs, including Zoloft®, cases of exacerbation of diabetes mellitus and/or impaired glucose control (hyperglycemia and hypoglycemia) have been reported 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 closed-angle 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
The simultaneous use of sertraline and grapefruit juice is not recommended.
Side effects of the drug Zoloft
From the gastrointestinal tract: diarrhea/fecal incontinence, dry mouth, dyspepsia, nausea, abdominal pain, constipation, pancreatitis, vomiting. Metabolic disorders: anorexia; increased appetite, hyponatremia. From the central nervous system and peripheral nervous system: dizziness, drowsiness and tremor, coma, convulsions, headache, hypoesthesia, migraine, movement disorders (including extrapyramidal symptoms, including hyperkinesia, jaw muscle spasms or gait disturbances), involuntary muscle contractures, paresthesia and loss of consciousness. The development of manifestations of serotonergic syndrome, in some cases associated with the use of serotonergic drugs, has also been recorded, namely: agitation, confusion, increased sweating, diarrhea, fever, hypertension (arterial hypertension), rigidity and tachycardia. Mental disorders: insomnia, aggressive reactions, agitation, anxiety, depressive symptoms, euphoria, hallucinations, decreased libido in men and women, nightmares and psychosis. From the reproductive system: sexual dysfunction (primarily delayed ejaculation in men), galactorrhea, gynecomastia, irregular menstrual cycle and priapism. From the skin and subcutaneous tissues: increased sweating, alopecia, angioedema, facial edema, periorbital edema, photosensitivity skin reactions, itching, skin rash (including isolated cases of exfoliative skin lesions - Stevens-Johnson syndrome and epidermal necrolysis), urticaria. From the blood system: leukopenia and thrombocytopenia. From the cardiovascular system: palpitation and tachycardia, pathological bleeding (for example, nosebleeds, gastrointestinal bleeding or hematuria), flushing (sudden redness of the skin) and hypertension (arterial hypertension). From the hearing organs/vestibular system: ringing in the ears. From the endocrine system: hyperprolactinemia, hypothyroidism, hypoaldosteronism syndrome; From the organs of vision: mydriasis and visual impairment. Body as a whole: asthenia, chest pain, peripheral edema, fatigue, fever, malaise. From the hepatobiliary system: severe liver dysfunction (hepatitis, jaundice, liver failure) and asymptomatic increase in the level of transaminases in the blood plasma (ALAT and AST). From the immune system: allergic reactions, anaphylactic reactions. Laboratory indicators: false results of clinical laboratory tests, changes in platelet function, increased cholesterol concentration in the blood serum, increase or decrease in body weight. From the musculoskeletal system: arthralgia and muscle spasms. From the urinary system: urinary incontinence, urinary retention. From the respiratory system: bronchospasm and yawning. The range of side effects most commonly observed in studies of patients with OCD, panic disorder, PTSD, and social phobia were similar to those observed in clinical studies of patients with depression. Other: manifestations of withdrawal syndrome when stopping treatment with sertraline, in particular agitation, anxiety, dizziness, headache, nausea and paresthesia.
Negative effects
Negative reactions when taking the drug were observed in various systems of the human body. But most often problems arise with the digestive system. Dyspeptic disorders, abdominal pain, and dry mouth are observed. In severe cases, pancreatitis may develop.
During treatment, disturbances in the functioning of the central nervous system may also occur, which are expressed by headaches, dizziness, insomnia and other unpleasant symptoms. Dangerous reactions include disruptions in the functioning of the cardiovascular system, such as arterial hypertension or tachycardia. Sometimes taking medication provokes muscle cramps.
The instructions for using Zoloft focus on the risks of many other side effects. Warnings should be read carefully before starting treatment. If any negative manifestations occur, the antidepressant should be discontinued.
Special instructions for the use of Zoloft
MAO inhibitors. Cases of serious side effects, sometimes fatal, have been reported in patients using sertraline in combination with MAO, in particular with the selective MAO inhibitor selegiline and the reversible MAO inhibitor moclobemide. In some cases, serotonergic syndrome developed with the appearance of symptoms such as hyperthermia, rigidity, myoclonus, autonomic dysfunction with the possibility of sudden disturbances in vital functions. Mental disorders in this case are manifested by delirium, irritability and severe agitation, which progresses to a state of delirium and coma. Therefore, sertraline should not be prescribed concomitantly with MAO inhibitors or within 14 days after stopping treatment with this class of drugs. Also, treatment with MAO inhibitors should not be started earlier than 14 days after the end of treatment with sertraline. Other serotonergic agents. The combined use of sertraline and other drugs that stimulate serotonergic neuromediation, in particular tryptophan, fenfluramine or 5-HT agonists, should be carried out with caution and, if possible, excluded (given the risk of pharmacodynamic interaction). Switching from selective serotonin reuptake inhibitors, antidepressants or anti-obsessive drugs. There is limited controlled experience in calculating the optimal timing of switching from selective serotonin reuptake inhibitors, antidepressants or anti-obsessive medications to sertraline. Caution should be exercised when switching from selective serotonin reuptake inhibitors and other antidepressants and anti-obsessive medications, especially long-acting ones (for example, fluoxetine), to sertraline. The duration of the break when switching from treatment with one drug to another has not been established. Increased manic/hypomanic symptoms. During pre-marketing trials of sertraline, increased manic/hypomanic symptoms were observed in approximately 0.4% of patients. Isolated cases of increased mania/hypomania have been described in patients with significantly severe affective disorder who received other antidepressant or antiobsessive drugs. Convulsive seizures. Seizures are a potential complication of therapy with antidepressants or anti-obsessive medications. Seizures were reported in approximately 0.08% of patients treated with sertraline during the depression treatment program. No cases of seizures have been reported during the treatment of panic disorders with sertraline. During treatment with sertraline in 1800 patients with OCD, only 4 of them had seizures (about 0.2%). Three of these patients were children, two had existing seizure pathology, and one had a family history of seizure pathology. However, none of them used anticonvulsants. In all of these cases, a causal relationship with sertraline therapy is unlikely. Since sertraline has not been studied in patients with seizure disorders, it should not be used in patients with uncontrolled epilepsy, and patients with controlled epilepsy should be monitored during treatment. If seizures develop, the drug must be discontinued. Suicides. Patients with depression have a tendency to attempt suicide, which persists until remission occurs. For this reason, patients should be monitored at the beginning of treatment. Given the established fact of increased co-occurrence rates of OCD and depression, panic disorder and depression, and PTSD and depression, similar precautions should be taken when treating patients with OCD, panic disorder, and PTSD. Use for liver failure. Sertraline is actively biotransformed in the liver. According to a multidose pharmacokinetic study, with repeated use of sertraline in patients with compensated mild liver cirrhosis, an increase in the half-life of the drug, an almost 3-fold increase in AUC and an increase in the maximum concentration of the drug in the blood plasma were observed compared with the same values in healthy individuals. There were no significant differences in the level of binding to plasma proteins in patients of these 2 groups. Sertraline should be prescribed with caution to patients with liver disease. If liver function is impaired, it is necessary to reduce the dose and reduce the interval between doses of the drug. Use for renal failure. Sertraline undergoes active biotransformation in the body, so a small part of the drug is excreted unchanged in the urine. In studies of patients with mild and moderate renal failure (drug clearance 30–60 ml/min) and patients with severe renal failure (drug clearance 10–29 ml/min), the main pharmacokinetic parameters of sertraline when taken repeatedly in patients of these groups were not reliably were different. The half-life was the same and no differences in binding to plasma proteins were detected in patients of the study groups. Research data indicate that, given the low rates of sertraline excretion by the kidneys, drug doses may not be adjusted depending on the degree of renal impairment. Children: see APPLICATION section. During pregnancy and breastfeeding. Sertraline can be used during pregnancy and lactation only if the expected benefit to the mother outweighs the likely risk to the fetus and newborn. Women of reproductive age must use effective contraception during treatment. The ability to influence reaction speed when driving vehicles or working with other mechanisms. Clinical and pharmacological studies indicate that sertraline has no effect on psychomotor functions. However, patients should be careful when driving or operating machinery, as the drug may interfere with mental or physical reactions.
Zoloft: contraindications
A contraindication to taking the drug is hypersensitivity to sertraline and other components that make up the drug. Their list is indicated in the instructions for use.
Drug treatment is not prescribed for people under 18 years of age. The exception is cases of treatment of obsessive-compulsive disorders. In such cases, it is allowed to use the medicine after 6 years. Treatment with the drug is contraindicated during pregnancy and lactation, since studies that confirm the absence of a negative effect of the drug on the fetus and newborn child have not been conducted.
It is prohibited to use Zoloft, the instructions emphasize this, in combination with MAO inhibitors. This may cause serotonin toxicity. This syndrome leads to malfunctions in many systems of the human body and can be fatal.
Contraindications also include the combination of the drug with the psychotropic drug pimozide.
The drug should be taken with extreme caution when diagnosing epilepsy and organic diseases of the brain. Their development can be caused by both congenital pathologies and various negative external influences, in particular injury or infection.
Zoloft drug interactions
MAO inhibitors. The combined use of sertraline with MAO inhibitors is contraindicated (see SPECIAL INSTRUCTIONS). Other serotonergic drugs (see SPECIAL INSTRUCTIONS). Switching from taking selective serotonin reuptake inhibitors, antidepressants or anti-obsessive drugs (see SPECIAL INSTRUCTIONS). Pimozide. In a study of the combined use of a low dose of pimozide (2 mg once) and sertraline at a dose of 200 mg/day, an increase in the level of pimozide in the blood plasma was noted without any changes in the ECG. Since the mechanism of this interaction has not been established, and given the narrow therapeutic index of pimozide, the simultaneous use of sertraline and pimozide is contraindicated. CNS depressants and alcohol. The combined use of sertraline (200 mg/day) did not potentiate the effect of alcohol, carbamazepine, haloperidol or phenytoin on cognitive and psychomotor performance in healthy individuals; however, the simultaneous use of sertraline and alcohol is not recommended. Lithium. The combined use of sertraline and lithium did not significantly change the pharmacokinetics of lithium, however, tremor increased, which may indicate a pharmacodynamic interaction. With the simultaneous use of sertraline and lithium preparations, which affect serotonergic neuromediation, it is necessary to ensure appropriate control. Phenytoin. Long-term use of sertraline at a dose of 200 mg/day does not lead to clinically significant inhibition of phenytoin metabolism. Despite this, monitoring of phenytoin plasma concentrations during the initial phase of sertraline therapy with appropriate adjustment of the phenytoin dose should be recommended. In addition, concomitant use of phenytoin may cause a decrease in sertraline plasma concentrations. Sumatriptan. There are reports of isolated cases of the development of general weakness, hyperreflexia, impaired coordination, confusion, anxiety and agitation, which were observed after the simultaneous use of sertraline and sumatriptan. If it is necessary to prescribe sertraline and sumatriptan simultaneously, the patient should be under medical supervision. Drugs that bind to blood plasma proteins. Since sertraline binds to plasma proteins, it is necessary to consider the possibility of its interaction with other drugs that also bind to plasma proteins. However, in 3 studies, no significant effect of sertraline on the binding of diazepam, tolbutamide and warfarin to plasma proteins was detected. Warfarin. With simultaneous use of sertraline at a dose of 200 mg/day with warfarin, a slight but statistically significant increase in prothrombin time was observed; the clinical significance of this effect is unknown. In this regard, prothrombin time should be carefully monitored at the beginning of sertraline therapy and after its discontinuation. Interaction with other means. A number of studies have examined the interaction of sertraline with various drugs. The simultaneous use of sertraline at a dose of 200 mg/day with diazepam and tolbutamide led to a slight but statistically significant change in some pharmacokinetic parameters. Cimetidine caused a significant decrease in the clearance of sertraline when used simultaneously. The clinical significance of these changes is unknown. Sertraline did not affect the β-adrenergic blocking activity of atenolol. There were no signs of interaction of sertraline (at a dose of 200 mg/day) with glibenclamide and digoxin. Electroconvulsive therapy . The safety and effectiveness of the combined use of electroconvulsive therapy and sertraline have not been studied in clinical studies. Drugs metabolized with the participation of cytochrome P450 CYP 2D6. Antidepressant drugs have varying abilities to inhibit the activity of the 2D6 isoenzyme of cytochrome P450 CYP 2D6. The clinical significance of this depends on the degree of inhibition and the therapeutic index of the drug prescribed. CYP2D6 substrates with a low therapeutic index include tricyclic antidepressants and class Ic antiarrhythmics such as propafenone, flecainide. In studies of drug interactions with long-term use of sertraline at a dose of 50 mg/day, an increase (on average by 23–37%) in stable plasma levels of desipramine (a marker of CYP 2D6 activity) was detected. Drugs metabolized by other CYP isoenzymes (CYP 3A3/4, CYP 2C9, CYP 2C19, CYP 1A2). CYP 3A3/4: In vivo studies revealed that long-term use of sertraline at a dose of 200 mg/day does not inhibit CYP 3A3/4 dependent 6-β-hydroxylation of endogenous cortisol, or the metabolism of carbamazepine or terfenadine. In addition, long-term use of sertraline at a dose of 50 mg/day did not inhibit CYP 3A3/4, which is involved in the metabolism of alprazolam. The results of this study indicate that sertraline is not a clinically significant inhibitor of CYP3A3/4. CYP 2C9: Chronic use of sertraline 200 mg/day had no effect on plasma concentrations of tolbutamide, phenytoin, and warfarin, indicating that sertraline is not a clinically significant inhibitor of CYP 2C9. CYP 2C19: The use of sertraline at a dose of 200 mg/day did not affect the plasma concentrations of diazepam, indicating that sertraline is not a clinically significant inhibitor of CYP 2C19. CYP 1A2: In vitro studies indicate that sertraline has no or little effect on the activity of CYP 1A2.
Zoloft overdose, symptoms and treatment
Sertraline has a wide range of safety in overdose. Cases of drug overdose have been recorded when taken in doses of up to 13.5 g; Fatal outcomes from sertraline overdose were mainly observed when it was used in combination with other drugs and/or alcohol. In case of overdose, intensive therapy is necessary. Symptoms of overdose include serotonin-related effects such as drowsiness, digestive disturbances (nausea and vomiting), tachycardia, tremor, agitation and dizziness. Coma very rarely develops. Treatment: There is no specific antidote; treatment is symptomatic and supportive. It is necessary to ensure a patent airway and adequate levels of ventilation and oxygenation. Taking activated charcoal, which can be used as a laxative, may be more effective than gastric lavage. Inducing vomiting is not recommended. Monitoring of cardiac function and other vital signs should be ensured. Given the large volume of distribution of sertraline, forced diuresis, dialysis, hemoperfusion and exchange transfusion are unlikely to be effective.
Drug interactions
Do Zoloft and Anaprilin, Afobazol, Phenazepam combine: Is it possible to use Zoloft and Teraligen at the same time?
Combination of Zoloft and Anaprilin: the drugs can be taken together. What is the compatibility of Zoloft and Phenazepam? Combination with the drugs Afobazole, Phenazepam and Teraligen: interaction can lead to negative consequences for the patient’s health, consult a specialist. Zoloft and Paracetamol may be compatible. It is important to know that the drug in combination with MAO inhibitors (monoamine oxidase) contributes to the development of severe complications from human health, including death. When these drugs are used together, serotonin syndrome may occur, which is characterized by an increase in body temperature, disruptions in the functioning of the cardiovascular system, and the central nervous system. As mentioned earlier, Sertraline should not be combined with alcohol, since this substance inhibits the activity of the human central nervous system. The drug is eliminated from the body much more slowly if it was taken in combination with antihistamines.
Interaction with antipsychotics
Neuroleptics or antipsychotic drugs can only be prescribed by the attending physician. The specialist knows exactly what medications Zoloft is combined with and which medications should be avoided due to health risks. Psychotropic drugs in pharmacology are used for polytherapy of the disease. In what cases is this combination possible?
- To enhance the effect of the drug and provide a sedative effect, the use of drugs in combination can be prescribed for anxiety-anesthetic depression.
- To eliminate purely anesthetic depression with low effectiveness of monotherapy, a combination of Zoloft with antipsychotics is used.
- To enhance the serotonergic effect in the treatment of such a disorder as melancholy-anesthetic depression, antidepressants are used.
The combination of Zoloft and an antipsychotic helps to carry out complex treatment with a high level of effectiveness. However, it is important to know that antidepressants reduce the effect of antipsychotics.
