Zoloft - instructions for use, reviews, analogs and formulations (50 mg and 100 mg tablets) of an antidepressant drug for the treatment of depression and phobia in adults, children and pregnancy. Alcohol and withdrawal syndrome after taking

In this article, you can read the instructions for using the drug Zoloft. There are reviews of visitors to the site - consumers of this medication, as well as opinions of doctors of specialists on the use of Zoloft in their practice. A big request is to actively add their feedback on the drug: the medicine helped or did not help get rid of the disease, which were observed complications and side effects, possibly not declared by the manufacturer in the annotation. Analogues Zoloft in the presence of existing structural analogs. Use to treat depression and phobia in adults, children, as well as during pregnancy and lactation.Interaction with alcohol, manifestations and fight with withdrawal syndrome after the end of the drug.

Zoloft - antidepressant, a powerful specific inhibitor of reuptake of serotonin (5-HT) in neurons. Has a very weak effect on the re-uptake of norepinephrine and dopamine. In therapeutic doses, it blocks the seizure of serotonin in human platelets. It has no stimulating, sedative or anticholinergic action. Due to the selective inhibition of 5-HT capture, sertraline (an active substance of Zoloft) does not increase adrenergic activity. Sertraline does not have an affinity for muscarinic cholinergic receptors, serotonin, dopamine, histamine, GABA-, benzodiazepine and adrenoreceptors.

Zoloft does not cause drug dependence, does not cause an increase in body weight with prolonged admission.

Composition

Sertraline (in the form of hydrochloride) + auxiliary substances.

Pharmacokinetics

Absorption is high, but at a slow rate. When taking the drug simultaneously with food bioavailability increases by 25%. Binding to plasma proteins is about 98%.Sertraline undergoes active biotransformation at the "first pass" through the liver. The main metabolite found in plasma, N-desmethylsertralin, is significantly inferior (about 20 times) to sertraline by activity and is in fact not active in depression models. Sertraline and N-desmethylsertralin are actively biotransformed. 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.

The pharmacokinetic profile in adolescents and the elderly is not significantly different from that in patients aged 18 to 65 years.

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

Indications

• depression of different etiology (treatment and prevention);
• obsessive-compulsive disorder (OCD);
• panic disorder;
• post-traumatic stress disorder (PTSD);
• social phobia.

Forms of release

Tablets coated with 50 mg and 100 mg.

Instructions for use and dosage

Zoloft is prescribed 1 time per day in the morning or evening. Tablets can be taken regardless of food intake.

With depression and OCD, treatment starts with a dose of 50 mg per day.

Treatment of panic disorders, PTSD and social phobia begin with a dose of 25 mg per day, which is increased after 1 week to 50 mg per day. The use of the drug in this scheme allows you to reduce the frequency of early undesirable effects of treatment, characteristic of panic disorder.

With an insufficient effect of sertraline in patients at a dose of 50 mg per day, the daily dose can be increased. The dose should be increased at intervals not more than once a week to the maximum recommended dose of 200 mg per day.

The initial effect can be observed 7 days after the start of treatment, but the overall effect is usually achieved in 2-4 weeks (or even for a longer time with OCD).

In the case of prolonged maintenance therapy, the drug is administered at the lowest 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 be started at a dose of 50 mg per day. In children aged 6-12 years, OCD therapy begins with a dose of 25 mg per day, after 1 week it is increased to 50 mg per day. In the following, if the effect is insufficient, the dose can be increased stepwise by 50 mg per day to 200 mg per day as needed. In clinical trials in patients with depression and OCD at the age of 6 to 17 years, it was shown that the pharmacokinetic profile of sertraline was similar to that in adults. To avoid an overdose, with a dose increase of more than 50 mg, it is necessary to take into account the smaller body weight in children compared to adults.

The half-life of sertraline is approximately 1 day, so the dose change should occur at intervals of not less than 1 week.

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

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

The drug is largely metabolized in the body. In an unchanged form, only a small amount of the drug is excreted in the urine.As expected, taking into account the minor renal excretion of sertraline, correction of its dose depending on the severity of renal failure is not required

Side effect

• dyspeptic symptoms (flatulence, nausea, vomiting, diarrhea, constipation);
• abdominal pain;
• pancreatitis;
• dry mouth;
• jaundice;
• liver failure;
• decreased appetite (rarely - increase), up to anorexia;
• a feeling of palpitations;
• tachycardia;
• arterial hypertension;
• arthralgia;
• muscle cramps;
• extrapyramidal disorders (dyskinesias, akathisia, gnashing of teeth, violation of gait);
• involuntary muscle contractions;
• paresthesia;
• fainting;
• drowsiness;
• headache;
• migraine;
• dizziness;
• tremor;
• insomnia;
• anxiety;
• hallucinations;
• euphoria;
• nightmares;
• psychosis;
• decreased libido;
• suicide;
• coma;
• bronchospasm;
• yawn;
• urinary incontinence or retention;
• violation of sexual function (delay in ejaculation, decreased potency);
• gynecomastia;
• violation of the menstrual cycle;
• priapism;
• impaired vision;
• tinnitus;
• redness of the skin or "tides" of blood to the face;
• alopecia;
• photosensitivity reaction;
• increased sweating;
• hives;
• itching;
• anaphylactoid reaction;
• angioedema;
• swelling of the face;
• possibly development of leukopenia and thrombocytopenia;
• decrease or increase in body weight;
• weakness;
• bleeding (including nasal, gastrointestinal or hematuria).

When treatment with sertraline is discontinued, rare cases of withdrawal syndrome are described. There may be paresthesia, hypoesthesia, symptoms of depression, hallucinations, aggressive reactions, psychomotor agitation, anxiety or symptoms of psychosis that can not be distinguished from the symptoms of the underlying disease.

Contraindications

• simultaneous administration of MAO inhibitors and pimozide;
• pregnancy;
• lactation period (breastfeeding);
• children's age till 6 years;
• hypersensitivity to the components of the drug.

Application in pregnancy and lactation

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

Female reproductive age during treatment with sertraline should use effective methods of contraception.

Sertraline is found in breast milk, and therefore the use of Zoloft during lactation is not recommended. In this case there are no reliable data on the safety of its application. If the purpose of the drug is necessary, then breastfeeding should be discontinued.

In the case of sertraline during pregnancy and during breastfeeding, some newborns whose mothers were taking antidepressants from the group of selective serotonin reuptake inhibitors, including serotonin, may have symptoms similar to the response to drug withdrawal.

Application in elderly patients

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

Use in children

Contraindicated in children under 6 years.

In children and adolescents aged 13-17 years suffering from OCD, treatment with Zoloft should be started with a dose of 50 mg per day. In children aged 6-12 years, OCD therapy begins with a dose of 25 mg per day, after 1 week it is increased to 50 mg per day. In the following, if the effect is insufficient, the dose can be increased stepwise by 50 mg per day to 200 mg per day as needed.To avoid an overdose, with a dose increase of more than 50 mg, it is necessary to take into account the smaller body weight in children compared to adults. Change the dose should be at intervals of not less than 1 week.

special instructions

Sertraline should not be administered together with MAO inhibitors, but also within 14 days after discontinuation of treatment with MAO inhibitors. Similarly, after the withdrawal of sertraline within 14 days, MAO inhibitors are not prescribed.

Serotonin syndrome and malignant neuroleptic syndrome

With the use of selective serotonin reuptake inhibitors (SSRIs), cases of the development of serotonin syndrome and malignant neuroleptic syndrome (SNS) are described, the risk of which increases when SSRIs are combined with other serotonergic agents (including triptans), as well as drugs affecting serotonin metabolism (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 gastrointestinal disorders (nausea, vomiting and diarrhea). Some manifestations of serotonin syndrome, incl. hyperthermia, rigidity of muscles, vegetative lability with the possibility of rapid fluctuations in the parameters of vital functions, as well as changes in mental status, can resemble the symptoms developing in the NSA. It is necessary to monitor patients for the development of clinical manifestations of serotonin syndrome and ZNS.

Other serotonergic agents

Caution should be exercised with the simultaneous administration of Zoloft with other drugs that enhance serotonergic neurotransmission, such as tryptophan, fenfluramine or 5-HT-agonists. Such a joint appointment, if possible, should be ruled out, given the likelihood of pharmacodynamic interaction.

Transition from other selective serotonin reuptake inhibitors (SSRIs), antidepressants or anti-obsessive drugs

The experience of clinical studies, the purpose of which was to determine the optimal time required for transferring patients from taking other antidepressant and anti-obsessive agents to sertraline, is limited.Care must be taken in this transition, especially with long-acting drugs, for example, with fluoxetine. The necessary interval between the cancellation of one selective serotonin reuptake inhibitor and the start of administration of another similar preparation has not been established. It should be noted that in patients undergoing electroconvulsive therapy, there is no sufficient experience with sertraline.

The possible success or risk of such a combined treatment has not been studied. There is no experience with sertraline in patients with convulsive syndrome, therefore, its use in patients with unstable epilepsy should be avoided, and patients with controlled epilepsy should be carefully observed during treatment. When the seizures appear, the drug should be discontinued.

Patients with depression are at risk for suicide attempts. This danger persists until the development of remission. Therefore, from the beginning of treatment and until the optimal clinical effect is achieved, patients should be provided with permanent medical supervision.

Activation of mania / hypomania

During clinical trials before the introduction of Zoloft on the market, hypomania and mania were observed in approximately 0.4% of patients receiving sertraline.The cases of activation of mania / hypomania are also described in a small part of patients with manic-depressive psychosis receiving other antidepressant or anti-obsessional drugs.

Application in case of insufficiency of liver function

Zoloft is actively biotransformed in the liver. According to the pharmacokinetic study, with multiple sertraline administration in patients with stable cirrhosis of the liver of the lung, there was an increase in the half-life of the drug and a nearly triple increase in the AUC and Cmax of the drug compared to those in healthy individuals. There were no significant differences in binding to plasma proteins in the two groups. Use sertralin in patients with liver disease with caution. When prescribing a 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.

Application for renal failure

Sertraline undergoes active biotransformation, so in unchanged form with urine it is excreted in a small amount. In patients with mild to moderate renal failure (CK 30-60 ml / min) and patients with moderate or severe renal diseaseinsufficiency (KK 10-29 ml / min) the pharmacokinetic parameters (AUC0-24 and Cmax) of sertraline at repeated administration did not differ significantly from the control group. In all the T1 / 2 groups of the drug was the same, as well as there was no difference in binding to plasma proteins. The results of this study suggest that, as expected, taking into account the minor renal excretion of sertraline, correction of its dose depending on the severity of renal failure is not required.

Pathological hemorrhages / hemorrhages

It is advisable to use caution in the appointment of selective serotonin reuptake inhibitors in combination with drugs with established ability to change the functions of platelets, as well as in patients with hemorrhagic diseases in the anamnesis.

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 inadequate secretion of antidiuretic hormone. With the development of symptomatic hyponatremia, sertraline should be abolished and an adequate therapy aimed at correcting the sodium level in the blood should be prescribed.Signs and symptoms of hyponatremia include headache, impaired concentration, memory impairment, weakness and instability, which can lead to falls. In more severe cases, hallucinations, fainting, convulsions, coma, respiratory arrest and death may occur.

Impact on the ability to drive vehicles and manage mechanisms

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

Drug Interactions

Pimozide

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

MAO inhibitors

There are serious complications with the simultaneous use of sertraline and MAO inhibitors (including selective-acting (selegiline) MAO inhibitors and reversible type of action (moclobemide, and also linezolid.) Serotonin syndrome (hyperthermia, rigidity, myoclonus, lability in the autonomic nervous system (rapid fluctuations parameters of the respiratory and cardiovascular system), changes in mental status, including increased irritability, marked exaltation, confusion, which in some In other cases, complications, sometimes fatal, occur with the appointment of MAO inhibitors against the background of treatment with antidepressants that inhibit neuronal capture of monoamines or immediately after their withdrawal.

Drugs that oppress the central nervous system, and ethanol

The combined use of Zoloft and substances depressing the central nervous system requires close attention, and the use of alcoholic beverages and preparations containing alcohol during sertraline treatment is prohibited. No potentiation of the effect of ethanol (alcohol), carbamazepine,Haloperidol or phenytoin on cognitive and psychomotor function in healthy people; however, the joint use of sertraline and alcohol is not recommended.

Anticoagulants of indirect action (warfarin)

When they are co-administered with sertraline, there is no significant but statistically significant increase in prothrombin time. In these cases, it is recommended to monitor prothrombin time at the beginning of sertraline treatment and after its withdrawal.

Analogues of the drug Zoloft

Structural analogs for the active substance:

• Aleval;
• Asentra;
• Deprefalt;
• Seralin;
• Serenata;
• Sirleft;
• Sertraline hydrochloride;
• Stimuloton;
• Thorin.

Analogues for the pharmacological group (antidepressants):

• Agomelatine;
• Aktaparoxetine;
• Alventa;
• Amizole;
• Amitriptyline;
• Valdoxane;
• Velaxin;
• Velafax;
• Venlafaxine hydrochloride;
• Heptor;
• Heptral;
• Daplex;
• Depres;
• Depenone;
• Deprim;
• Duloxetine;
• Ixelles;
• Clomipramine;
• Coaxyl;
• Mirzaten;
• Mirtazonal;
• Mirtalan;
• Nerustin;
• Neuroplant;
• Newvelong;
• Oprah;
• Paxil;
• Paroxetine;
• Pirazidol;
• Plizil;
• Portal;
• Prozac;
• Profluzak;
• Rexetin;
• Sedopram;
• Selektra;
• Seralin;
• Serenata;
• Sertraline hydrochloride;
• Stimuloton;
• Triptysole;
• Trittico;
• Umorap;
• Févarine;
• Fluval;
• Fluoxetine;
• Framex;
• Cipralex;
• Citalon;
• Citalopram;
• Citol;
• Elivel;
• Elicia;
• Esprital;
• Escitalopram;
• Ephevelone;
• Epevelon retard.

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