Zoloft pills 50mg, 28pcs

Composition

Active ingredient:

sertraline (in the form of hydrochloride)50 mg;

Auxiliary substances:

calcium phosphate;

MCC;

hydroxypropylcellulose;

sodium starch glycolate;

magnesium stearate;

hydroxypropylmethylcellulose;

polyethylene glycol;

polysorbates;

titanium dioxide (E171)

Pharmacological action

of Zoloft – antidepressant.

Pharmacodynamics

Sertraline is an antidepressant, a powerful specific inhibitor of serotonin reuptake (5-HT) in neurons. It has very little effect on the reuptake of norepinephrine and dopamine. In therapeutic doses, sertraline blocks the uptake of serotonin in human platelets. It does not have a stimulating, sedative or anticholinergic effect. Due to the selective inhibition of 5-HT uptake, sertraline does not increase adrenergic activity. Sertraline has no affinity for muscarinic (cholinergic), serotonergic, dopaminergic, adrenergic, histaminergic, GABA or benzodiazepine receptors.

Sertraline does not cause drug dependence, and an increase in body weight with prolonged use.

Pharmacokinetics

Absorption is high (but at a slow rate). Bioavailability increases with food intake by 25%. Food increases cmax by 25% and shortens tmax. In humans, when treated with sertraline at a dose of 50 to 200 mg once a day for 14 days, the plasma tmax is 4.5-8.4 hours after use. _Cmax and AUC are proportional in the dose range of 50-200 mg of sertraline once a day for 14 days, and a linear pharmacokinetic relationship is revealed. The pharmacokinetic profile in adolescents and the elderly does not differ from that in patients aged 18 to 65 years. The average T_1/2 of sertraline in young and elderly men and women is 22-36 h. Accordingly, the final T_1/2 is approximately twice the accumulation of the drug before the onset of_CSSS after 1 week of treatment (taking the dose — 1 time per day). Binding to plasma proteins is approximately 98%. The pharmacokinetics of sertraline in children with obsessive-compulsive disorder (OCD, see below) have been shown to be similar to those in adults (although sertraline metabolism is somewhat more active in children). 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 lower dose to avoid excessive plasma levels.

Sertraline undergoes active biotransformation during its first passage through the liver. The main metabolite found in plasma, N-desmethylsertraline, is significantly inferior (approximately 20 times) to sertraline in vitro activity and is virtually inactive in in vivo models of depression. T_1/2 of N-desmethylsertraline varies within 62-104 hours. Sertraline and N-desmethylsertraline are actively biotransformed; the resulting metabolites are excreted in equal amounts in the feces and urine. Unchanged sertraline is excreted in the urine in a small amount (1/2 of the drug and AUC compared to those in healthy people.

Indications

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

Use during pregnancy and lactation

Zoloft is contraindicated during pregnancy and lactation.

Contraindications

• : hypersensitivity to sertraline;
• concomitant use of inhibitors MAO and pimozide;
• pregnancy;
• breast-feeding period (see “Use during pregnancy and lactation”);
• children under 6 years of age.

With caution:  organic diseases of the brain (including mental retardation); epilepsy; liver and / or kidney failure; severe weight loss.

Side effects

From the digestive system:  dyspeptic disorders (flatulence, nausea, vomiting, diarrhea, constipation), abdominal pain, pancreatitis, dry mouth.

From the CCC side:  rapid heartbeat, tachycardia, arterial hypertension.

From the musculoskeletal system:  arthralgia, muscle cramps.

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

Respiratory system disorders:  bronchospasm, yawning.

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

From the side of the reproductive system and breast:  sexual dysfunction (delayed ejaculation, decreased potency), galactorrhea, gynecomastia, menstrual disorders, priapism.

From the side of the visual organs:  visual impairment, mydriasis.

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

From the side of the hepatobiliary system:  hepatitis, jaundice, liver failure.

Allergic reactions:  urticaria, pruritus, anaphylactoid reaction.

Other services:  weakness, redness of the skin or flushes of blood to the face, ringing in the ears, alopecia, angioedema, facial edema, periorbital edema, photosensitization reaction, purpura, increased sweating, decreased appetite (rarely increased), up to anorexia, weight loss or increase, bleeding (including nasal, gastrointestinal or hematuria), peripheral edema, occasionally Stevens — Johnson syndrome and epidermal necrolysis.

Laboratory analysis data:  rarely, with prolonged use, there is an asymptomatic increase in the activity of transaminases in the blood serum. Withdrawal of the drug in this case leads to normalization of enzyme activity.

Interaction

Pimozide. When sertraline and pimozide were co-administered, an increase in pimozide levels was observed with a single low dose (2 mg). Increased pimozide levels were not associated with any ECG changes. Since the mechanism of this interaction is unknown, and pimozide has a narrow therapeutic index, simultaneous use of pimozide and sertraline is contraindicated.

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

Drugs that depress the central nervous system, and ethanol. The combined use of sertraline and substances that depress the central nervous system requires close attention; the use of alcoholic beverages and drugs containing alcohol during treatment with sertraline is also prohibited. No potentiation of the effect of ethanol, carbamazepine, haloperidol, or phenytoin on cognitive and psychomotor function in healthy individuals has been observed; however, concomitant use of sertraline and alcohol is not recommended.

Indirect anticoagulants (warfarin). When they are co-administered with sertraline, there is a slight but statistically significant increase in PV (in these cases, it is recommended to monitor PV at the beginning of sertraline treatment 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, diazepam and tolbutamide).

Cimetidine. Concomitant use significantly reduces the clearance of sertraline.

Drugs metabolized by cytochrome P 2D6 isoenzyme%^%450. 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 participates (tricyclic antidepressants, antiarrhythmic drugs of the IC class — propafenone, flecainide).

Drugs metabolized by other cytochrome P%^%450 enzyme systems. In vitro interaction experiments have shown that the endogenous cortisol beta-hydroxylation carried out by the CYP3A3/4 isoenzyme, as well as the metabolism of carbamazepine and terfenadine, do not change with long-term use of sertraline at a dose of 200 mg/day. Plasma concentrations of tolbutamide (but with simultaneous use reduces the clearance of tolbutamide-it is necessary to control blood glucose with simultaneous use), phenytoin and warfarin with prolonged use of sertraline in the same dose also do not change. Thus, it can be concluded that sertraline does not inhibit the CYP2%^%C%^%9 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 virtually no effect or minimal inhibition of the CYP1A2 isoenzyme.

Lithium. The pharmacokinetics of lithium do not change with concomitant use of sertraline. However, tremor is observed more often when they are used together. As with other SSRIs, the concomitant use of sertraline with drugs that affect serotonergic transmission (for example, lithium) requires increased caution.

Drugs that affect serotonergic transmission. When replacing one inhibitor of neuronal serotonin uptake with another, there is no need for a washing period. However, caution should be exercised when changing the course of treatment. Co-use of tryptophan or fenfluramine with sertraline should be avoided.

Induction of microsomal liver enzymes. Sertraline causes minimal induction of liver enzymes. Simultaneous use 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. When co-administered, sertraline does not alter its beta-blocking effect.

Glibenclamide and digoxin. When sertraline was administered at a daily dose of 200 mg, no drug interaction with these drugs was detected.

Phenytoin. Long-term use of sertraline at a dose of 200 mg / day does not have a clinically significant effect and does not inhibit the metabolism of phenytoin. Despite this, careful monitoring of the level of phenytoin in blood plasma is recommended from the moment of sertraline use, with appropriate adjustment of phenytoin doses.

Sumatriptan. There are extremely rare cases of weakness, increased tendon reflexes, confusion, anxiety and agitation in patients taking sertraline and sumatriptan at the same time. Monitoring of patients with appropriate clinical grounds for concomitant use of sertraline and sumatriptan is recommended.

How to take, course of use and dosage

Inside,1 time a day, in the morning or in the evening, regardless of food intake.

Initial dose

Depression and OCD: Treatment with sertraline should start at a dose of 50 mg / day.

Panic disorders, PTSD, and social phobia. Treatment begins 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 treatment effects characteristic of panic disorder.

Dose selection

Depression, OCD, panic disorders, PTSD, and social phobia. If the effect of using sertraline in patients at a dose of 50 mg/day is insufficient, its daily dose can be increased. The dose should be increased at intervals of no more than once a week, up to the maximum recommended dose of 200 mg/day.

The initial therapeutic effect may occur within 7 days, but the full effect is usually achieved after 2-4 weeks (or even for a longer time in OCD).

Maintenance therapy

The maintenance dose for long-term treatment should be the minimum effective-with appropriate changes, depending on the therapeutic effect.

Application for the treatment of children

The safety and efficacy of sertraline have been established in children with OCD (aged 6 to 17 years). In adolescents (aged 13-17 years) suffering from OCD, treatment with sertraline 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, if the effect is insufficient, the dose can be increased stepwise,50 mg / day, up to 200 mg/day, as needed. In clinical trials in patients with depression and OCD aged 6 to 17 years, the pharmacokinetic profile of sertraline was shown to be similar to that in adults. However, to avoid overdose, when increasing the dose more than 50 mg, it is necessary to take into account the lower body weight in children compared to adults.

Dose selection in children and adolescents. T_1/2 of sertraline is approximately 1 day, so dose changes should occur at intervals of at least 1 week.

Special patient groups

Elderly people. In the elderly, the drug is used in the same dose range as in younger people.

Impaired liver function. Sertraline should be used with caution in patients with liver disease. In patients with hepatic insufficiency, use smaller doses or increase the interval between doses of the drug.

Impaired renal function. Sertraline is largely metabolized in the body. Only a small amount of the drug is excreted unchanged in the urine. As expected, given the low renal excretion of sertraline, no dose adjustment is required depending on the severity of renal failure

Overdose

Symptoms: severe symptoms of sertraline overdose were not detected even when the drug was prescribed in large doses. However, when administered concomitantly with other drugs or alcohol, severe poisoning can occur, up to coma and death.

Overdose can cause SS with nausea, vomiting, drowsiness, tachycardia, agitation, dizziness, psychomotor agitation, diarrhea, increased sweating, myoclonus and hyperreflexia.

Treatment: There is no specific antidote to the drug. Intensive maintenance therapy and constant monitoring of vital body functions are required. It is not recommended to induce vomiting. Prescribing activated charcoal may be more effective than gastric lavage. It is necessary to maintain the patency of the respiratory tract. Sertraline has a largeVd, and therefore increased diuresis, dialysis, hemoperfusion, or blood transfusion may be ineffective.

Special instructions

Sertraline should not be co-administered with MAO inhibitors, nor should it be administered for 14 days after discontinuation of treatment with MAO inhibitors. Similarly, after sertraline is discontinued for 14 days, no MAO inhibitors are prescribed.

SS and neuroleptic malignant syndrome (NMS). When applying SSRIs cases of SS and NMS are described, the risk of which increases when combined SSRIs with other serotonergic agents (including triptans), as well as drugs that affect serotonin metabolism (including MAO inhibitors), antipsychotics, and other dopamine receptor antagonists. Symptoms 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 coordination of movements), and/or gastrointestinal disorders (nausea, vomiting, and diarrhea). Some manifestations of SS, including hyperthermia, muscle rigidity, vegetative lability with the possibility of rapid fluctuations in the parameters of vital functions, 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 SS and NMS.

Other serotonergic agents. Caution should be exercised when concomitantly prescribing sertraline with other drugs that enhance serotonergic neurotransmission, such as tryptophan, fenfluramine or 5-HT agonists. If possible, such co-use should be excluded, taking into account the likelihood of pharmacodynamic interaction.

Switching from other SSRIs, antidepressants, or anti-obsessive medications. The experience of clinical trials aimed at determining the optimal time required to transfer patients from taking other antidepressants and anti-obsessive drugs to sertraline is limited. Caution should be exercised during this transition, especially with long-acting medications such as fluoxetine. The necessary interval between discontinuing one SSRI and starting another similar drug has not been established.

In patients undergoing electroconvulsive therapy, there is no sufficient experience of using sertraline. The possible success or risk of such combination treatment has not been studied.

There is no experience of using sertraline in patients with convulsive syndrome, so it 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.

Patients suffering from depression are at risk for suicide attempts. This danger persists until remission develops. Therefore, from the beginning of treatment until the optimal clinical effect is achieved, patients should be constantly monitored.

Activation of mania / hypomania. During clinical trials prior to the introduction of sertraline on the market, hypomania and mania were observed in approximately 0.4% of patients treated with sertraline. Cases of mania/hypomania activation have also been reported in a small proportion of patients with manic-depressive psychosis treated with other antidepressant or anti-obsessive medications.

Use in patients with hepatic insufficiency. Sertraline is actively biotransformed in the liver. According to a pharmacokinetic study, repeated use of sertraline in patients with stable mild cirrhosis showed an increase in T_1/2 of the drug and an almost threefold increase in AUC and_cmax of the drug compared to those in healthy people.There were no significant differences in plasma protein binding in 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 feasibility of reducing the dose or increasing the interval between taking the drug.

Use in patients with renal insufficiency. Sertraline undergoes active biotransformation, so it is excreted unchanged in the urine in small amounts. In patients with mild to moderate renal insufficiency (Creatinine clearance 30-60 ml/min) and patients with moderate or severe renal insufficiency (creatinine clearance 10-29 ml/min), the pharmacokinetic parameters (AUC_0-24 and_cmax) of sertraline with repeated use 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 binding to plasma proteins. The results of this study indicate that, as expected, given the low renal excretion of sertraline, no dose adjustment is required depending on the severity of renal failure.

Pathological bleeding/hemorrhage. It is recommended to use caution when prescribing SSRIs in combination with drugs that have a proven ability to alter platelet function, as well as in patients with a history of hemorrhagic diseases.

Hyponatremia. Transient hyponatremia may occur during sertraline treatment. This is more common in elderly patients, as well as when taking diuretics or a number of other medications. This side effect is associated with the syndrome of inadequate ADH secretion. If symptomatic hyponatremia develops, sertraline should be discontinued and adequate therapy should be prescribed to correct the level of sodium in the blood. Signs and symptoms of hyponatremia include headache, impaired concentration, memory impairment, weakness and unsteadiness, which can lead to falls. In more severe cases, hallucinations, fainting, seizures, coma, respiratory arrest, and death may occur.

Influence on the ability to drive vehicles and work with mechanisms. use of sertraline, as a rule, is not accompanied by a violation of psychomotor functions. However, its use simultaneously with other medications can lead to impaired attention and coordination of movements. Therefore, it is not recommended to drive vehicles, special equipment, or engage in high-risk activities during sertraline treatment.

Tablet Form of production

Storage conditions

At a temperature not exceeding 30 °C

Shelf life

5 years

Active ingredient

Sertraline

Conditions of release from pharmacies

By prescription

Dosage form

Tablets