ZOLOFT PILLS COATED 100MG

Indications

- Depression of various etiologies (treatment and prevention);

- obsessive compulsive disorder (OCD);

- panic disorders;

- posttraumatic stress disorder (PTSD);

- social phobia.

Dosage and administration

The drug is used orally, 1 time per day in the morning or in the evening. pills can be taken regardless of the meal.

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

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

With insufficient effect of sertraline in patients at a dose of 50 mg / day, the daily dose can be increased. The dose should be increased at intervals of no more than 1 time per week to the maximum recommended dose of 200 mg / day.

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

At long-term maintenance therapy the drug is prescribed in the minimum effective dose, which subsequently change depending on the clinical effect.

Have children and adolescents aged 13-17 with OCD Zoloft treatment® should start with a dose of 50 mg / day. Have 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 between the ages of 6 and 17 years, it was shown that the pharmacokinetic profile of sertraline was similar to that in adults. To avoid overdose, increasing the dose of more than 50 mg should take into account the lower body weight in children compared with adults.

T1/2 sertraline is approximately 1 day, so the dose change should occur at intervals of at least 1 week.

Have 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. Have patients with hepatic insufficiency should use smaller doses or increase the interval between doses of the drug.

The drug is largely metabolized in the body. Unchanged in the urine displays only a small amount of the drug. As expected, taking into account the slight renal excretion of sertraline, correction of its dose depending on the severity renal failure not required.

Adverse effects

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

Cardiovascular: palpitations, tachycardia, arterial hypertension.

Musculoskeletal system: arthralgia, muscle cramps.

Nervous system: extrapyramidal disorders (dyskinesias, akathisia, gnashing of teeth, gait disturbance), involuntary muscle contractions, paresthesias, fainting, drowsiness, headache, migraine, dizziness, tremor, insomnia, anxiety, agitation, hypomania, mania, hallucinations, ephritia, insomnia, anxiety, agitation, hypomania, mania, hallucinations, ephritia, insomnia, anxiety, agitation, hypomania, mania, hallucinations, ephria psychosis, decreased libido, suicide, coma.

Respiratory: bronchospasm, yawning.

Urogenital: enuresis, incontinence or urinary retention.

From the reproductive system: violation of sexual function (delayed ejaculation, reduced potency), galactorrhea, gynecomastia, menstrual disorders, priapism.

Special senses: blurred vision, mydriasis, tinnitus.

On the part of the endocrine system: hyperprolactinemia, hypothyroidism, inadequate secretion syndrome ADH.

Dermatologic: reddening of the skin or "flushes" of blood to the face, alopecia, photosensitization reaction, purpura, increased sweating.

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

Hemic and lymphatic: possible development of leukopenia and thrombocytopenia.

Other: decrease or increase in body weight, peripheral edema, increased serum cholesterol, weakness, bleeding (including nasal, gastrointestinal, or hematuria). When discontinuing treatment with sertraline, rare cases of withdrawal syndrome are described. Paresthesias, hypoesthesia, symptoms of depression, hallucinations, aggressive reactions, agitation, anxiety, or symptoms of psychosis, which cannot be distinguished from the symptoms of the underlying disease, may appear.

Contraindications

- simultaneous administration 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 in organic brain diseases (including mental retardation), epilepsy, liver and / or renal failure, marked weight loss.

Use during pregnancy and lactation

Pregnant women do not have controlled results of sertraline, therefore, to prescribe Zoloft® 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 should use effective methods of contraception.

Sertralin 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.

When using sertraline during pregnancy and during breastfeeding in some newborns whose mothers took antidepressants from the group of selective serotonin reuptake inhibitors, including serotonin, symptoms similar to the reaction to discontinuation of the drug may be observed.

Application for violations of the liver

The drug should be used with caution in patients with liver disease. Have patients with hepatic insufficiency should use smaller doses or increase the interval between doses of the drug.

WITH caution should be prescribed the drug for liver failure.

Application for violations of kidney function

Taking into account the slight renal excretion of sertraline, the correction of its dose depending on the severity renal failure not required.

WITH caution It should appoint a drug for renal failure.

Use in children

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

Have children and adolescents aged 13-17suffering from OCD, treatment with Zoloft® should start with a dose of 50 mg / day. Have 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, increasing the dose to more than 50 mg should take into account the lower body weight in children compared with adults. Change the dose should be at intervals of at least 1 week.

Use in elderly patients

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

Special notes

Sertralin should not be prescribed in conjunction with MAO inhibitors, as well as within 14 days after stopping treatment with MAO inhibitors. Similarly, after the abolition of sertraline, no MAO inhibitors are prescribed for 14 days.

Serotonin syndrome and neuroleptic malignant syndrome

When using selective serotonin reuptake inhibitors (SSRIs), cases of the development of serotonin syndrome and malignant neuroleptic syndrome (MNS) are described, the risk of which increases with the combination of SSRIs with other serotonergic drugs (including triptans), as well as drugs that affect serotonin metabolism (includingMAO inhibitors), antipsychotics and other dopamine receptor antagonists. 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 neuro-muscular transmission (hyperreflexia, impaired coordination of movements) and / or disorders of the gastrointestinal tract ( nausea, vomiting and diarrhea). Some manifestations of serotonin syndrome, including hyperthermia, muscle stiffness, vegetative lability with the possibility of rapid fluctuations in the parameters of vital functions, as well as changes in mental status, may resemble symptoms that develop in MPS. It is necessary to monitor patients for the development of clinical manifestations of serotonin syndrome and MNS.

Other serotonergic drugs

Care must be taken when prescribing sertraline with other drugs that enhance serotonergic neurotransmission, such as tryptophan, fenfluramine or 5-HT agonists. If possible, such a joint appointment should be excluded, given the likelihood of pharmacodynamic interaction.

Transition from other SSRIs, antidepressants or anti-obsessive drugs

The experience of clinical studies, the purpose of which was to determine the optimal time required for the transfer of patients from taking other anti-depressive and anti-obsessive drugs to sertraline, is limited.Care must be taken in such a transition, especially with long-acting drugs, such as Fluoxetine . The required interval between the cancellation of one SSRI and the start of taking another similar drug has not been established. It should be noted that in patients undergoing electroconvulsive therapy, there is no adequate experience with sertraline.

The possible success or risk of such a combination treatment has not been studied. There is no experience with 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.

Depressed patients are at risk for suicidal attempts. This danger persists until the development of remission. Therefore, from the start of treatment and until the optimum clinical effect is achieved, patients should be provided with constant medical supervision.

Activation of mania / hypomania

During clinical studies prior to the introduction of sertraline into the market, hypomania and mania were observed in about 0.4% of patients receiving sertraline. Cases of activation of mania / hypomania are also described in a small proportion of patients with manic-depressive psychosis who received other anti-depressive or anti-obsessive drugs.

Use for liver failure

Sertralin is actively biotransformed in the liver.According to a pharmacokinetic study, with repeated administration of sertraline in patients with stable cirrhosis of the lungs, an increase in T was observed.1/2 drug and almost triple increase in AUC and Cmax drug compared with those in healthy people. There were no significant differences in plasma binding in the two groups. Sertraline should be used with caution in patients with liver disease. In appointing the drug to a patient with impaired liver function, it is necessary to discuss the feasibility of reducing the dose or increasing the interval between taking the drug.

Use in renal failure

Sertralin 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 failure (CC 10-29 ml / min) pharmacokinetic parameters (AUC0-24 and Cmax) sertraline with its repeated administration did not significantly differ from the control group. In all groups T1/2 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, given the negligible renal excretion of sertraline, its dose is not adjusted depending on the severity of renal failure.

Pathological bleeding / hemorrhage

It is recommended to use caution when prescribing selective serotonin reuptake inhibitors in combination with drugs that have an established ability to change platelet functions, as well as in patients with a history of hemorrhagic diseases.

Hyponatremia

During treatment with sertraline, transient hyponatremia may occur. This most often develops in elderly patients, as well as when taking diuretics or a number of other drugs. This side effect is associated with the syndrome of inadequate secretion of ADH. With the development of symptomatic hyponatremia, sertraline should be discontinued and appropriate therapy should be appointed to correct the sodium level in the blood. Signs and symptoms of hyponatremia include headache, impaired concentration, memory impairment, weakness and instability, which can lead to falls. In more severe cases, hallucinations, syncope, convulsions, coma, respiratory arrest and death may occur.

Influence on ability to drive motor transport and control mechanisms

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

Overdose

Symptoms: severe symptoms of sertraline overdose were not detected even with the use of the drug in high doses. However, with the simultaneous introduction with other drugs or alcohol can cause severe poisoning, even coma and death.

Overdose may cause manifestations of serotonin syndrome (nausea, vomiting, drowsiness, tachycardia, agitation, dizziness, psychomotor agitation, diarrhea, sweating, myoclonus, and hyperreflexia).

Treatment: there are no specific antidotes. Requires intensive supportive care and constant monitoring of vital body functions. Vomiting is not recommended. The introduction of Activated carbon may be more effective than gastric lavage. It is necessary to maintain airway patency. Sertraline big vdIn this regard, increased diuresis, dialysis, hemoperfusion, or blood transfusion may be unsuccessful.

Drug interaction

Pimozide

With the joint use of sertraline and pimozide, there was an increase in the levels of pimozide with its single appointment in a low dose (2 mg). An 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, the simultaneous administration of pimozide and sertraline is contraindicated.

MAO inhibitors

Severe complications are observed with 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 (hyperthermia, rigidity, myoclonus, lability of the autonomic nervous system (rapid parameters of the respiratory and cardiovascular systems), changes in mental status, including increased irritability, marked excitement, confusion, which cases may become delirious or coma.) Similar complications, sometimes fatal, occur when prescribing MAO inhibitors during treatment with antidepressants that suppress the neuronal seizure of monoamines or immediately after their withdrawal.

CNS depressant drugs and ethanol

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

Indirect anticoagulants (warfarin)

With their joint appointment 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 cancellation.

Pharmacokinetic interaction

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

Cimetidine

Simultaneous use significantly reduces the clearance of sertraline.

Drugs metabolized by CYP2D6 isoenzyme

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

Drugs metabolized by other cytochrome P450 enzyme systems

Experiments to study the interaction in vitro showed that the beta-hydroxylation of endogenous cortisol carried out by the CYP3A3 / 4 isoenzyme, as well as the metabolism of carbamazepine and terfenadine with a long-term administration of sertraline at a dose of 200 mg / day do not change. The concentration of tolbutamide in the blood plasma (while taking it decreases the clearance of tolbutamide - control of blood glucose is necessary when used simultaneously), phenytoin and Warfarin with the long-term administration of sertraline in the same dose also does not change.Thus, it can be concluded that sertraline does not inhibit the CYP2C9 isoenzyme.

Sertralin does not affect the concentration of diazepam in the serum, which indicates the absence of inhibition of the CYP2C19 isoenzyme. According to in vitro studies, sertraline has virtually no effect or is minimally inhibited by the CYP1A2 isoenzyme.

Lithium preparations

The pharmacokinetics of lithium do not change with the concomitant administration of sertraline. However, tremor occurs more often with their combined use. As well as the appointment of other selective serotonin reuptake neuronal 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 inhibitor of neuronal seizure of serotonin with another, there is no need for a “laundering period”. However, care is required when changing the course of treatment. Co-administration of tryptophan or fenfluramine with sertraline should be avoided.

Induction of Liver Microsomal Enzymes

Sertralin causes minimal induction of liver enzymes. The simultaneous appointment of sertraline 200 mg and antipyrine leads to a small (5%) but significant decrease in T1/2 antipyrine

Atenolol

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

Glibenclamide and Digoxin

With the introduction of sertraline in a daily dose of 200 mg of drug interaction with these drugs is not detected.

Phenytoin

Prolonged use of sertraline at a dose of 200 mg / day has no clinically significant effect and does not inhibit the metabolism of phenytoin. Despite this, careful monitoring of the plasma phenytoin content since the administration of sertraline with the appropriate dose adjustment of phenytoin is recommended.

Sumatriptan

There are extremely rare cases of weakness, increased tendon reflexes, confusion, anxiety and arousal in patients simultaneously taking sertraline and Sumatriptan . If simultaneous use of sertraline and sumatriptan is necessary, patient monitoring is recommended.

Terms and conditions of storage

List B. The drug should be kept out of the reach of children at a temperature not exceeding 30 ° C.