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What medications should not be taken with Zoloft? Zoloft: instructions for use and what it is for, price, reviews, analogues. Post Traumatic Stress Disorder

Antidepressant

Active substance

Sertraline (as hydrochloride) (sertraline)

Release form, composition and packaging

Coated tablets white, oblong, with the inscription "Pfizer" embossed on one side, with a line and the inscription "ZLT50" embossed on the other side of the tablet.

14 pcs. - blisters (1) - packs of cardboard.

Coated tablets white, oblong, with "Pfizer" embossed on one side and "ZLT100" on the other side of the tablet.

Excipients: calcium phosphate, microcrystalline cellulose, hydroxypropyl cellulose, sodium starch glycolate, magnesium stearate, hydroxypropyl methylcellulose, polyethylene glycol, polysorbates, titanium dioxide (E171).

14 pcs. - blisters (2) - packs of cardboard.

pharmachologic effect

Antidepressant, a potent specific reuptake inhibitor (5-HT) in neurons. It has a very weak effect on the reuptake of norepinephrine and dopamine. In therapeutic doses, it blocks the uptake of serotonin in human platelets. It does not have a stimulating, sedative or anticholinergic effect. Due to selective inhibition of 5-HT uptake, sertraline does not enhance adrenergic activity. Sertraline has no affinity for muscarinic cholinergic receptors, serotonin, dopamine, histamine, GABA-, benzodiazepine and adrenoreceptors.

Sertraline does not cause drug dependence, does not cause weight gain with long-term use.

Pharmacokinetics

Suction

Absorption is high, but at a slow rate. When taking the drug simultaneously with food, bioavailability increases by 25%, C max increases by 25% and T max decreases.

In humans, when taking sertraline at a dose of 50 to 200 mg 1 time / day for 14 days, Cmax was reached 4.5-8.4 hours after administration. C max and AUC are proportional to the dose in the range of 50-200 mg of sertraline 1 time / day for 14 days, while the linear nature of the pharmacokinetic dependence is revealed.

Distribution

When they are co-administered with sertraline, there is a slight but statistically significant increase in prothrombin time. In these cases, it is recommended to control the prothrombin time at the beginning of treatment with sertraline and after its withdrawal.

Pharmacokinetic interaction

Sertraline binds to plasma proteins. Therefore, it is necessary to consider the possibility of its interaction with other drugs that bind to proteins (for example, with diazepam and tolbutamide).

Simultaneous use significantly reduces the clearance of sertraline.

Drugs metabolized by CYP2D6

Long-term treatment with sertraline at a dose of 50 mg / day increases the plasma concentration of concomitantly used drugs in the metabolism of which this enzyme is involved (tricyclic antidepressants, class IC antiarrhythmic drugs - propafenone, flecainide).

Drugs metabolized by other cytochrome P450 enzyme systems

In vitro interaction studies have shown that beta-hydroxylation of endogenous cortisol, carried out by the CYP3A3 / 4 isoenzyme, as well as the metabolism of carbamazepine and terfenadine, do not change with long-term administration of sertraline at a dose of 200 mg / day. The concentration in the blood plasma of tolbutamide (when taken simultaneously reduces the clearance of tolbutamide - it is necessary to control blood glucose with simultaneous use), phenytoin and warfarin with long-term administration of sertraline at the same dose also does not change. Thus, it can be concluded that sertraline does not inhibit the CYP2C9 isoenzyme.

Sertraline does not affect the concentration of diazepam in the blood serum, which indicates the absence of inhibition of the CYP2C19 isoenzyme. According to in vitro studies, sertraline has little or no effect on the CYP1A2 isoenzyme.

Lithium preparations

The pharmacokinetics of lithium does not change with the concomitant administration of sertraline. However, tremor is observed more often when they are used together. As well as the appointment of other selective serotonin reuptake inhibitors, the combined use of sertraline with drugs that affect serotonergic transmission (for example, with lithium preparations) requires increased caution.

Drugs affecting serotonergic transmission

When replacing one neuronal serotonin reuptake inhibitor with another, there is no need for a "washout period". However, caution is required when changing the course of treatment. Co-administration of tryptophan or fenfluramine with sertraline should be avoided.

Induction of microsomal liver enzymes

Sertraline causes minimal induction of liver enzymes. The simultaneous appointment of sertraline at a dose of 200 mg and antipyrine leads to a small (5%), but significant decrease in T 1/2 of antipyrine.

Atenolol

With the joint introduction of sertraline does not change its beta-adrenergic blocking effect.

Glibenclamide and digoxin

With the introduction of sertraline in a daily dose of 200 mg, drug interactions with these drugs have not been identified.

Phenytoin

Long-term use of sertraline at a dose of 200 mg / day does not have a clinically significant effect and does not suppress the metabolism of phenytoin. Despite this, careful monitoring of the content of phenytoin in the blood plasma is recommended from the time of the appointment of sertraline with an appropriate dose adjustment of phenytoin.

Sumatriptan

Extremely rare cases of weakness, increased tendon reflexes, confusion, anxiety and agitation have been reported in patients taking sertraline and sumatriptan at the same time. If necessary, the simultaneous use of sertraline and sumatriptan is recommended to monitor patients.

special instructions

Sertraline should not be administered in conjunction with MAO inhibitors, and within 14 days after stopping treatment with MAO inhibitors. Similarly, after the abolition of sertraline, MAO inhibitors are not prescribed for 14 days.

Serotonin syndrome and neuroleptic malignant syndrome

With the use of selective inhibitors of the reverse capture of serotonin (SIOS), cases of the development of serotonin syndrome and malignant antipsychotic syndrome (BLS) are described, the risk of which increases when combining SIOOS with other serotonergic agents (including triptans), as well as drugs affecting the metabolism of serotonin (including MAO inhibitors) , antipsychotic agents and other antagonists of dopamine receptors. Manifestations of serotonin syndrome can be changes in mental status (in particular, agitation, hallucinations, coma), autonomic lability (tachycardia, fluctuations in blood pressure, hyperthermia), changes in neuromuscular transmission (hyperreflexia, impaired coordination of movements) and / or disorders of the gastrointestinal tract (nausea, vomiting and diarrhea). Some manifestations of serotonin syndrome, incl. hyperthermia, muscle rigidity, autonomic lability with the possibility of rapid fluctuations in vital signs, as well as changes in mental status, may resemble the symptoms that develop in NMS. It is necessary to monitor patients for the development of clinical manifestations of serotonin syndrome and NMS.

Other serotonergic agents

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, if possible, should be excluded, given the likelihood of pharmacodynamic interaction.

Switching from other SSRIs, antidepressants, or anti-obsessional drugs

The experience of clinical studies, the purpose of which was to determine the optimal time required to transfer patients from other antidepressant and anti-obsessional drugs to sertraline, is limited. Care must be taken when switching, especially from long-acting drugs such as fluoxetine. The necessary interval between the abolition of one SSRI and the start of another similar drug has not been established. It should be noted that there is no sufficient experience with sertraline in patients undergoing electroconvulsive therapy.

The possible success or risk of such combined treatment has not been studied. There is no experience with the use of sertraline in patients with convulsive syndrome, so its use in patients with unstable epilepsy should be avoided, and patients with controlled epilepsy should be carefully monitored during treatment. If convulsions occur, the drug should be discontinued.

Patients with depression are at risk for suicide attempts. This danger persists until remission develops. Therefore, from the beginning of treatment until the achievement of the optimal clinical effect, patients should be under constant medical supervision.

Activation of mania/hypomania

During clinical trials prior to the introduction of sertraline to the market, hypomania and mania were observed in approximately 0.4% of patients treated with sertraline. Cases of activation of mania/hypomania are also described in a small proportion of patients with manic-depressive psychosis treated with other antidepressant or anti-obsessional drugs.

Use in 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 T 1/2 of the drug and an almost threefold increase in AUC and C max 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 in renal failure

Sertraline undergoes active biotransformation, therefore, unchanged in the urine, it is excreted in small quantities. In patients with mild and moderate renal insufficiency (CC 30-60 ml / min) and patients with moderate or severe renal insufficiency (CC 10-29 ml / min), the pharmacokinetic parameters (AUC 0-24 and Cmax) of sertraline with repeated administration did not differ significantly from the control group. In all groups, T 1/2 of the drug was the same, as well as there were no differences in plasma protein binding. The results of this study suggest that, as expected, given the negligible renal excretion of sertraline, no dose adjustment is required depending on the severity of renal failure.

Pathological bleeding/hemorrhage

Caution is advised 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

During treatment with sertraline, transient hyponatremia may occur. It often develops in elderly patients, as well as when taking diuretics or a number of other drugs. A similar side effect is associated with the syndrome of inappropriate ADH secretion. With the development of symptomatic hyponatremia, sertraline should be discontinued and adequate therapy aimed at correcting the level of sodium in the blood should be prescribed. Signs and symptoms of hyponatremia include headache, difficulty concentrating, memory impairment, weakness, and unsteadiness, which can lead to falls. In more severe cases, hallucinations, fainting, convulsions, coma, respiratory arrest, and death may occur.

Influence on the ability to drive vehicles and control mechanisms

Appointment, sertraline, as a rule, is not accompanied by a violation of psychomotor functions. However, its use simultaneously with other drugs can lead to impaired attention and coordination of movements. Therefore, during treatment with sertraline, it is not recommended to drive vehicles, special equipment or engage in activities associated with an increased risk.

Pregnancy and lactation

There are no controlled results of the use of sertraline in pregnant women, therefore Zoloft can be prescribed during pregnancy only if the expected benefit to the mother outweighs the potential risk to the fetus.

Women of reproductive age during treatment with sertraline, effective methods of contraception should be used.

Sertraline is found in breast milk, and therefore the use of Zoloft during lactation is not recommended. There is no reliable data on the safety of its use in this case. If the appointment of the drug is necessary, then breastfeeding should be stopped.

In the case of the use of sertraline during pregnancy and during breastfeeding, some newborns whose mothers took antidepressants from the group of selective serotonin reuptake inhibitors, including serotonin, may experience symptoms similar to the reaction to drug withdrawal.

Application in childhood

The use of the drug in children under 6 years of age is contraindicated.

At children and adolescents aged 13-17 years patients suffering from OCD, treatment with Zoloft should begin with a dose of 50 mg / day. At 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. To avoid overdose, when increasing the dose of more than 50 mg, it is necessary to take into account the lower body weight in children compared to adults. The dose should be changed at intervals of at least 1 week.

For impaired renal function

Given the slight renal excretion of sertraline, adjusting its dose depending on the severity Conditions for dispensing from pharmacies

The drug is dispensed by prescription.

Terms and conditions of storage

List B. The drug should be stored out of the reach of children at a temperature not exceeding 30°C. Shelf life - 5 years.

Content

Zoloft tablets are part of a group of antidepressants with the active substance sertraline. It is a selective serotonin reuptake inhibitor (SSRI) suitable for long-term use in adults and children over six years of age. From the instructions for using the medication, you can learn about its indications, side effects, method of use, special instructions.

Antidepressant Zoloft

The drug belongs to antidepressants that can selectively suppress the reuptake of serotonin. The effectiveness of the drug is confirmed by comparative clinical trials of several new generation antidepressants. Zoloft is able to quickly relieve symptoms in the form of phobias, anxiety, melancholy and other deviations from the norm of psychological stability. Taking the drug against the background of cognitive-behavioral psychotherapy gives very good results in the treatment of obsessive-compulsive disorder (OCD).

Composition and form of release

The drug is available in the form of oblong white tablets. On one side of the surface there is an embossed inscription, on the other side the dosage of the active substance is indicated. In addition to the active component, the composition contains a number of auxiliary elements.

Pharmacodynamics and pharmacokinetics

The drug has the property of a strong suppression of the reuptake of serotonin (5-HT) in neurons, while exerting a subtle effect on the reuptake of dopamine and norepinephrine. In a therapeutically significant dosage, the drug counteracts the capture of serotonin in platelets. The advantage of Zoloft is that it does not have side effects in the form of anticholinergic, sedative or stimulant effects. In connection with the selective suppression of the capture of serotonin receptors, the drug does not increase adrenergic activity.

The active substance of the drug - sertraline has no affinity for serotonergic histaminergic, dopaminergic, muscarinic (cholinergic), adrenergic, GABA or benzodiazepine receptors. The drug does not create dependence, does not lead to an increase in body mass index even with prolonged course intake, does not affect the secretion of hormones.

The drug has a high degree of absorption (at a slow pace). The bioavailability of the active substance increases by 25% during meals. Taking the drug at a dosage of 50-200 mg once a day for two weeks allows you to reach the maximum plasma concentration after 4.5-8.5 hours after administration. The age of the patient does not significantly affect the pharmacological profile. Elimination half-life: 22 to 36 hours.

Sertraline is 98% bound to plasma proteins. Active biotransformation of sertraline occurs in the liver, the main metabolite in plasma is N-desmethylsertraline. Excretion occurs in equal proportions with urine and feces. Sertraline in its original form is excreted in the urine in very small amounts (less than 0.2%). In patients with cirrhosis of the liver, the half-life increases.

Indications for use

Zoloft is prescribed for depression and for the prevention of episodes of depression. In severe cases, the drug can be combined with antidepressants from other groups. List of main indications:

depression of various origins (both prevention and treatment);
panic states;
post-traumatic states of stress;
different kinds of social phobias.

How to take Zoloft

Zoloft is taken orally once a day in the morning or evening, without strict attachment to food intake. In the treatment of obsessive-compulsive disorder or depression, therapy begins with a dose of 50 mg per day. With panic disorders, social phobias, psychotraumatic situations, the dosage starts at 25 mg per day with a gradual increase after a week to 50 mg. In the absence or weak effect of a dose of 50 mg, an increase with an interval of at least one week is acceptable. The maximum dosage is 200 mg. The recommendations are valid for young and elderly patients.

Children and adolescents 13 to 17 years of age with OCD are given a dosage of 50 mg per day. In children with OCD 6 to 12 years of age, therapy begins at 25 mg per day, increasing to 50 mg a week later. Depending on the clinical effect, the dosage may increase up to 200 mg (taking into account body weight). Caution must be exercised in patients with liver disease (lower doses or extended intervals between doses).

When it starts to work

The first effect begins to be felt a week after the start of the intake. A significant and marginal effect is usually achieved two to four weeks after the start of the course. With obsessive-compulsive disorder, it may sometimes take longer to reach the maximum effect (much depends on the simultaneous psychological impact).

special instructions

The drug is prescribed with caution in combination with certain drugs, it is forbidden to combine it with monoamine oxidase inhibitors. Other items from the special instructions section of the instructions for use read:

Against the background of drug treatment, the development of serotonin syndrome and a malignant neuroleptic state is possible, the risk increases when combined with triptans, antipyrine and antipsychotics. Signs of manifestation of these deviations are tachycardia, pressure fluctuations, hyperthermia, hyperreflexia.
0.4% of patients develop hypomania and mania.
With cirrhosis of the liver, the elimination period of the drug increases. Zoloft should be used with caution in liver diseases and with correction of the interval of administration. With kidney failure, the dosage and regimen do not change.
Transient hyponatremia may occur during sertraline therapy. When it appears, treatment is canceled, adequate therapy is prescribed. Signs of hyponatremia are headache, impaired concentration and memory, fainting, hallucinations, weakness.
It is not recommended to drive cars or dangerous machinery while taking the medicine, as the speed of psychomotor reactions decreases.

During pregnancy and lactation

Studies on the safety and efficacy of sertraline in pregnant and breastfeeding women have not been conducted. You can prescribe a medicine if the potential benefit to the mother outweighs the risk to the fetus. Women of reproductive age during treatment with Zoloft should be effectively protected. Sertraline passes into breast milk, so it should not be used during lactation. Newborns whose mothers received Zoloft develop signs of a withdrawal syndrome.

In childhood

Zoloft is contraindicated for use under the age of six years. Children and adolescents 13-17 years old with obsessive-compulsive disorder are prescribed 50 mg / day, 6-12 years old - 25 mg / day. After a week, the dosage is increased to 50 mg / day. To obtain the effect, the dose is gradually increased by 50 mg / day to 200 mg. The dosage change occurs once / week.

Zoloft and alcohol

Alcohol should not be taken while taking SSRIs, because ethanol itself prolongs the action of intracerebral serotonin. Plus, alcohol is an inducer of dopamine synthesis, so this enhances the side effects of Zoloft and there is competition for the substrate (metabolism in the liver). As a result, intoxication, disruption of the liver and excretion of the substance can occur.

drug interaction

While taking Zoloft, the use of MAO inhibitors is prohibited. Other drug interactions of the drug:

the combination with pimozide, selegiline, moclobemide, linezolid, propafenone is contraindicated - the development of serotonin syndrome and changes in mental status are possible, up to delirium and extremely serious consequences;
in healthy people there is no potentiation of the effect of ethanol, carbamazepine, phenytoin, haloperidol;
increases the prothrombin time of anticoagulants of indirect action, Warfarin;
lowers the effectiveness of diazepam, tolbutamide, increases the concentration of tricyclic antidepressants, antiarrhythmic drugs, flecainide, reduces the elimination time of Aspirin, acts on liver cytochrome enzymes;
cimetidine reduces the clearance of creatinine and sertraline, lithium preparations cause tremor;
combinations with tryptophan, fenfluramine are prohibited;
Sumatriptan causes weakness, confusion, anxiety, and increased tendon reflexes.

Side effects

Side effects may occur while taking Zoloft. Patients indicate these factors:

dyspepsia, flatulence, diarrhea, constipation, vomiting;
pancreatitis, hepatitis, hypesthesia;
decreased or increased appetite, anorexia;
palpitations, tachycardia, arterial hypertension;
muscle cramps, arthralgia, dyskinesia, akathisia, hematuria;
teeth grinding, gait problems, paresthesia;
fainting, drowsiness, migraine, dizziness, tremor;
agitation, decreased libido, insomnia, psychosis, coma;
bronchospasm, yawning, enuresis, impotence, menstrual disorders;
priapism, gynecomastia, visual impairment;
hypothyroidism, hyperprolactinemia, skin redness;
alopecia, increased sweating, leukopenia;
allergic reactions, urticaria, itching, angioedema;
bleeding, depression, aggressive behavior.

withdrawal syndrome

Discontinuation of an antidepressant should always be done gradually, reducing the dose so that a withdrawal syndrome does not occur. The smooth completion of treatment lasts several months. If you stop taking the drug quickly, there will be a "breaking" - the body will not have time to adapt. Doctors advise to reduce the dose of Zoloft according to the schedule - by 25 g at a time with an interval of two weeks. Withdrawal symptoms:

nausea, cramps, diarrhea, vomiting;
insomnia, nightmares, dizziness, fainting;
numbness of the extremities, tingling, trembling;
lack of coordination, anxiety.

Overdose

Even high doses of sertraline do not result in severe overdose symptoms. But if you take the remedy at the same time as alcohol or other medicines, coma and the risk of death are possible. Typical signs of an overdose are vomiting, tachycardia, drowsiness, nervous excitement, diarrhea, hyperreflexia. There is no specific antidote, dialysis, hemoperfusion or blood transfusion are ineffective. It is not recommended to induce vomiting, it is better to give the patient activated charcoal and maintain airway patency.

Contraindications

The drug is prescribed with caution for organic diseases of the brain, mental retardation, epilepsy, renal or hepatic insufficiency, severe weight loss. Contraindications are:

pregnancy, lactation;
children's age up to six years;
hypersensitivity to components;
combination with MAO inhibitors and pimozide.

Terms of sale and storage

You can buy an antidepressant with a prescription. Its storage involves protection from children and a temperature not higher than 30 degrees. The shelf life is five years.

Analogues

Zoloft can be replaced by both its direct analogues and other selective serotonin reuptake inhibitors. Analogues of the drug include:

Asentra is a drug based on sertraline, 50 mg tablets, used to treat depression and panic disorders;
Serlift - tablets 50 and 100 mg with the same active substance, treats depression in patients with mono- and bipolar affective disorders;
Stimuloton is a Hungarian drug in the form of tablets based on sertraline.

Zoloft price

The cost of drugs differs depending on the concentration of the active substance, the number of tablets in a pack, the pricing policy of the pharmacy. In the pharmacy chains of Moscow and St. Petersburg, the approximate prices for the medicine will be.

Antidepressant, a potent specific serotonin (5-HT) reuptake inhibitor in neurons. It has a very weak effect on the reuptake of norepinephrine and dopamine. In therapeutic doses, it blocks the uptake of serotonin in human platelets. It does not have a stimulating, sedative or anticholinergic effect. Due to selective inhibition of 5-HT uptake, sertraline does not enhance adrenergic activity. Sertraline has no affinity for muscarinic cholinergic receptors, serotonin, dopamine, histamine, GABA-, benzodiazepine and adrenoreceptors.

Sertraline does not cause drug dependence, does not cause weight gain with long-term use.

Pharmacokinetics

Suction

Absorption is high, but at a slow rate. When taking the drug simultaneously with food, bioavailability increases by 25%, C max increases by 25% and T max decreases.

Distribution

Plasma protein binding is about 98%.

According to the final T 1/2, approximately two-fold cumulation of the drug is observed before the onset of equilibrium concentrations after 1 week of treatment (dosing 1 time / day).

Metabolism

Sertraline undergoes active biotransformation during the "first pass" through the liver. The main metabolite found in plasma, N-desmethylsertraline, is significantly inferior (about 20 times) to sertraline in activity in vitro and is actually not active in models of depression in vivo.

Sertraline and N-desmethylsertraline are actively biotransformed.

breeding

The average T 1/2 sertraline in young and elderly men and women is 22-36 hours. T 1/2 N-desmethylsertraline varies within 62-104 hours. 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 pharmacokinetic profile in adolescents and elderly patients does not differ significantly from that in patients aged 18 to 65 years.

The pharmacokinetics of sertraline in children with OCD has been shown to be similar to that in adults (although sertraline metabolism is somewhat more active in children). However, given the lower body weight in children (especially those aged 6-12 years), the drug is recommended to be used at a lower dose in order to avoid excessive plasma levels.

In patients with cirrhosis of the liver, T 1/2 of the drug and AUC increase compared to those in healthy people.

Release form

White film-coated tablets, oblong, debossed with "Pfizer" on one side and "ZLT100" on the other side of the tablet.

14 pcs. - blisters (2) - packs of cardboard.

Dosage

The drug is used orally, 1 time / day in the morning or evening. The tablets can be taken with or without food.

For depression and OCD, treatment begins with a dose of 50 mg/day.

Treatment of panic disorder, PTSD and social phobia is started 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 can reduce the frequency of early undesirable effects of treatment, characteristic of panic disorder.

With insufficient effect of the use of sertraline in patients at a dose of 50 mg / day, the daily dose can be increased. The dose should be increased at intervals no more than once a week to the maximum recommended dose of 200 mg / day.

An initial effect may be seen as early as 7 days after the start of treatment, however, the full effect is usually achieved in 2-4 weeks (or even longer in OCD).

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 children and adolescents aged 13-17 years with OCD, treatment with Zoloft ® should begin 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. In clinical trials in patients with depression and OCD aged 6 to 17 years, it was shown that the pharmacokinetic profile of sertraline was similar to that in adults. To avoid overdose, when increasing the dose of more than 50 mg, it is necessary to take into account the lower body weight in children compared to adults.

T 1/2 sertraline is approximately 1 day, so dose changes should occur at intervals of at least 1 week.

The drug is largely metabolized in the body. Only a small amount of the drug is excreted unchanged in the urine. As expected, given the negligible renal excretion of sertraline, no dosage adjustment is required based on the severity of renal failure.

Overdose

Symptoms: Sertraline overdose has not shown severe symptoms, even when the drug is used in high doses. However, with simultaneous administration with other drugs or alcohol, severe poisoning can occur, up to coma and death.

In case of overdose, manifestations of serotonin syndrome (nausea, vomiting, drowsiness, tachycardia, agitation, dizziness, psychomotor agitation, diarrhea, increased sweating, myoclonus and hyperreflexia) are possible.

Treatment: There are no specific antidotes. Intensive maintenance therapy and constant monitoring of vital body functions are required. Inducing vomiting is not recommended. The introduction of activated charcoal may be more effective than gastric lavage. The airway must be maintained. Sertraline has a large V d , in connection with this, increased diuresis, dialysis, hemoperfusion or blood transfusion may be ineffective.

Interaction

With the combined use of sertraline and pimozide, there was an increase in the levels of pimozide when administered once at a low dose (2 mg). The increase in pimozide levels was not associated with any ECG changes. Since the mechanism of this interaction is not known, and pimozide has a narrow therapeutic index, the simultaneous use of pimozide and sertraline is contraindicated.

MAO inhibitors

Severe complications have been noted with the simultaneous use of sertraline and MAO inhibitors (including selectively acting (selegiline) MAO inhibitors and with a reversible type of action (moclobemide, as well as linezolid). Serotonin syndrome may develop (hyperthermia, rigidity, myoclonus, autonomic nervous system lability (rapid fluctuations in respiratory and cardiovascular system parameters), changes in mental status, including increased irritability , marked agitation, confusion, which in some cases can turn into a delirious state or coma).Similar complications, sometimes fatal, occur when prescribing MAO inhibitors during treatment with antidepressants that inhibit neuronal uptake of monoamines or immediately after their withdrawal.

CNS depressants and ethanol

The combined use of sertraline and CNS depressants requires close attention. It is forbidden to drink alcohol and preparations containing ethanol during treatment with sertraline. There was no potentiation of the effect of ethanol, carbamazepine, haloperidol or phenytoin on cognitive and psychomotor function in healthy people; however, co-administration of sertraline and alcohol is not recommended.

Indirect anticoagulants (warfarin)

Pharmacokinetic interaction

Sertraline binds to plasma proteins. Therefore, it is necessary to consider the possibility of its interaction with other drugs that bind to proteins (for example, with diazepam and tolbutamide).

Cimetidine

Simultaneous use significantly reduces the clearance of sertraline.

Drugs metabolized by CYP2D6

Drugs metabolized by other cytochrome P450 enzyme systems

Lithium preparations

Drugs affecting serotonergic transmission

Induction of microsomal liver enzymes

Atenolol

With the joint introduction of sertraline does not change its beta-adrenergic blocking effect.

Glibenclamide and digoxin

With the introduction of sertraline in a daily dose of 200 mg, drug interactions with these drugs have not been identified.

Phenytoin

Sumatriptan

Side effects

From the digestive system: dyspeptic symptoms (flatulence, nausea, vomiting, diarrhea, constipation), abdominal pain, pancreatitis, dry mouth, hepatitis, jaundice, liver failure, decreased appetite (rarely - increased), up to anorexia; rarely, with prolonged use, an asymptomatic increase in serum transaminase activity occurs. Cancellation of the drug in this case leads to the normalization of enzyme activity.

From the side of the cardiovascular system: palpitations, tachycardia, arterial hypertension.

From the musculoskeletal system: arthralgia, muscle cramps.

From the side of the central nervous system and peripheral nervous system: extrapyramidal disorders (dyskinesia, akathisia, teeth grinding, gait disturbance), involuntary muscle contractions, paresthesia, fainting, drowsiness, headache, migraine, dizziness, tremor, insomnia, anxiety, agitation, hypomania, mania, hallucinations, euphoria, nightmares, psychosis, decreased libido, suicide, coma

From the respiratory system: bronchospasm, yawning.

From the urinary system: enuresis, incontinence or urinary retention.

From the reproductive system: sexual dysfunction (delayed ejaculation, decreased potency), galactorrhea, gynecomastia, menstrual irregularities, priapism.

From the senses: blurred vision, mydriasis, tinnitus.

From the endocrine system: hyperprolactinemia, hypothyroidism, syndrome of inappropriate ADH secretion.

Dermatological reactions: reddening of the skin or flushing of the face, alopecia, photosensitivity reaction, purpura, increased sweating.

Allergic reactions: urticaria, pruritus, anaphylactoid reaction, angioedema, periorbital edema, facial edema, occasionally Stevens-Johnson syndrome and epidermal necrolysis.

On the part of the hematopoietic system: leukopenia and thrombocytopenia may develop.

Others: weight gain or decrease, peripheral edema, increased serum cholesterol levels, weakness, bleeding (including nasal, gastrointestinal or hematuria). With the termination of treatment with sertraline, rare cases of withdrawal syndrome have been described. Paresthesias, hypesthesias, symptoms of depression, hallucinations, aggressive reactions, psychomotor agitation, anxiety, or symptoms of psychosis that cannot be distinguished from the symptoms of the underlying disease may appear.

Indications

depression of various etiologies (treatment and prevention);
obsessive-compulsive disorders (OCD);
panic disorder;
post-traumatic stress disorder (PTSD);
social phobia.

Contraindications

simultaneous appointment of MAO inhibitors and pimozide;
pregnancy;
lactation period (breastfeeding);
children's age up to 6 years;
hypersensitivity to sertraline.

With caution, the drug should be used for organic diseases of the brain (including mental retardation), epilepsy, liver and / or kidney failure, a pronounced decrease in body weight.

Application features

Use during pregnancy and lactation

There are no controlled results of the use of sertraline in pregnant women, therefore Zoloft ® can be prescribed during pregnancy only if the expected benefit to the mother outweighs the potential risk to the fetus.

Women of childbearing age should use effective contraception during treatment with sertraline.

Sertraline is found in breast milk, and therefore the use of the drug Zoloft ® during lactation is not recommended. There is no reliable data on the safety of its use in this case. If the appointment of the drug is necessary, then breastfeeding should be stopped.

Application for violations of liver function

The drug should be used with caution in patients with liver disease. In patients with hepatic insufficiency, smaller doses should be used or the interval between doses should be increased.

With caution, the drug should be prescribed for liver failure.

Application for violations of kidney function

Given the insignificant renal excretion of sertraline, its dose adjustment, depending on the severity of renal failure, is not required.

With caution, the drug should be prescribed for renal failure.

Use in children

The use of the drug in children under 6 years of age is contraindicated.

In children and adolescents aged 13-17 years with OCD, treatment with Zoloft ® should begin 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. To avoid overdose, when increasing the dose of more than 50 mg, it is necessary to take into account the lower body weight in children compared to adults. The dose should be changed at intervals of at least 1 week.

Use in elderly patients

In elderly patients, the drug is used in the same doses as in younger patients.

special instructions

Serotonin syndrome and neuroleptic malignant syndrome

Other serotonergic agents

Switching from other SSRIs, antidepressants, or anti-obsessional drugs

Activation of mania/hypomania

Use in liver failure

Use in renal failure

Pathological bleeding/hemorrhage

Hyponatremia

Influence on the ability to drive vehicles and control mechanisms

Additional components: calcium phosphate, hydroxypropyl cellulose, MCC, sodium starch glycolate, hydroxypropyl methylcellulose, magnesium stearate, polyethylene glycol, titanium dioxide, polysorbates.

Release form

Zoloft is produced in the form of coated tablets of 50 mg and 100 mg, 14 pieces in a blister, 1-2 blisters per pack.

pharmachologic effect

The drug has antidepressant pharmacological action.

Pharmacodynamics and pharmacokinetics

Substance sertraline is the strongest antidepressant, with a powerful specific serotonin reuptake inhibitor in neurons. At the same time, there is a slight effect on the reuptake and norepinephrine . Therapeutic dosages sertraline block the uptake of serotonin within platelets. This drug does not have a stimulating, sedative or anticholinergic effect, and does not increase adrenergic activity. Besides, sertraline does not contribute to the emergence of drug dependence, weight gain and other undesirable effects.

The drug has a fairly high, but slow absorption. An increase in bioavailability occurs when taken with food. Thus, food may increase the maximum concentration, but reduce the healing effect. Almost 98% of the active substance binds to proteins. undergoing biotransformation in the liver, sertraline forms the main metabolite N-desmethylsertraline , which is less active. Excretion from the body occurs in the composition of urine and feces.

Indications for the use of Zoloft

The main indications for the use of this drug:

various forms ;
obsessive-compulsive disorders;
panic disorder;
social phobia;
post-traumatic stress disorder.

Contraindications for use

The medicine is not prescribed for:

children under 6 years of age;
high sensitivity to sertraline;
concomitant treatment with MAO inhibitors and pimozide;
, .

Side effects of Zoloft

During therapy with this drug, side effects may occur that affect the functioning of the digestive system, which are manifested by dyspeptic disorders. For example: , nausea, vomiting, abdominal pain, and so on.

Disturbances in the work of the cardiovascular, nervous, motor, respiratory, urinary and other systems are also possible.

In addition, there may be deviations in the work of the organs of vision, the development of various forms and general unwanted symptoms.

Sometimes stopping treatment sertraline may be accompanied by the development of a withdrawal syndrome, with manifestations , hypoesthesia, depressive symptoms, , aggressive reactions, psychomotor agitation, anxiety or psychosis, complicating the possibility of making an accurate diagnosis.

Tablets Zoloft, instructions for use (Method and dosage)

According to the instructions for the use of Zoloft, the tablets should be taken daily, one at a time, in the morning or in the evening.

In this case, the initial dosage depends on the type of disorder, for example, with depression, a daily dose of 50 mg is immediately prescribed. Panic disorder and social phobia suggest initial therapy at 25 mg daily. This approach helps to prevent the development of early side effects inherent in panic disorder.

In the future, it is possible to increase the therapeutic dose, but not more than once a week. In this case, the maximum daily dosage should not exceed 200 mg. The manifestation of a therapeutic effect can be expected after 7 days, but usually the achievement of a full therapeutic effect occurs after 2-4 weeks.

When conducting long-term treatment, the minimum effective maintenance dose is prescribed, which is adjusted depending on the therapeutic effect.

Application in pediatrics

This drug is often used to treat children aged 6-17 who suffer from obsessive-compulsive disorders.

At the same time, adolescents aged 13–17 years at the beginning of treatment are prescribed a daily dosage of 50 mg. Children 6-12 years old are recommended to take 25 mg daily for the first week, then it is increased to 50 mg. After that, taking into account the therapeutic efficacy and characteristics of patients, the dose is adjusted upward or downward. In order to prevent overdose by increasing the dose from 50 mg, it should be remembered that children are lighter than adult patients.

Overdose

While taking Zoloft in high doses, the development of severe symptoms was not noted. But if at the same time treatment is carried out with other drugs, then it can develop: nausea, vomiting, agitation, psychomotor agitation, excessive sweating, myoclonus And hyperreflexia .

In such cases, symptomatic therapy is required, with careful monitoring of important body functions, especially respiratory.

Interaction

Simultaneous use of this drug with pimozide can significantly increase its concentration in the body, and as for pimozide characterized by a narrow therapeutic index, their joint use is not recommended.

Combination with MAO inhibitors may lead to the development serotonin syndrome With hyperthermia, rigidity, myoclonus , lability of the autonomic nervous system and so on. Such symptoms can occur with serious complications and be a threat to the health and life of patients.

Combinations with cimetidine significantly lower ground clearance sertraline.

Tricyclic antidepressants or antiarrhythmic drugs , For example, And flecainide can lead to a mutual increase in the concentration of these substances in the body.

Taking drugs containing lithium can increase the manifestations of other disorders of the nervous system, so you need to be extra careful.

Should not be combined with sertraline accept , fenfluramine and, since it can cause liver malfunction and nervous system disorders.

With prolonged use phenytoin And sertraline at dosages up to 200 mg, clinically significant undesirable symptoms usually do not occur. However, the dosage and level must be carefully controlled. phenytoin in plasma, with each dose adjustment of these drugs.

Combined treatment and sertraline can lead to the development of weakness, increased tendon reflexes, impaired consciousness, anxiety and agitation. Therefore, it is necessary to carefully monitor the condition of patients with clinical grounds for the joint intake of these substances.

Terms of sale

Zoloft in pharmacies can be purchased with a prescription.

Storage conditions

Best before date

Zoloft's analogs

Coincidence in the ATX code of the 4th level:

The main analogues of this drug: Serenata, Solotik, Aleval, Sertralux, Sertraloft, Deprefolt, Depralin, Seralin, Sertraline hydrochloride, Zalox, Torin, A-depresin, Aduvin, Sertraline, and so on.

Zoloft and alcohol

The simultaneous use of this drug and alcohol-containing drugs can potentiate the inhibitory effect on the nervous system. In addition, alcohol can lead to severe poisoning, and even a coma and death.