Serenata, 50 mg 30 pcs

Serenate is an antidepressant.

Sertraline is a selective serotonin reuptake inhibitor (5-NT). It has a very weak effect on norepinephrine and dopamine reuptake. In therapeutic doses, sertraline blocks serotonin uptake by human platelets. It has no stimulant, sedative or anticholinergic effects. Sertraline has no affinity for muscarinic (cholinergic), serotoninergic, dopaminergic, adrenergic, histaminergic, GABA or benzodiazepine receptors.

Antidepressant effect is noted by the end of the second week of regular Sertraline administration, while the maximum effect is reached only after 6 weeks. Unlike tricyclic antidepressants, there is no increase in body weight when prescribed sertraline. Sertraline does not cause mental or physical drug dependence.

Pharmacokinetics

Sertraline absorption from the gastrointestinal tract is significant but slow. The maximum plasma concentration is reached 4.5-8.4 hours after oral administration. Equilibrium plasma concentration of Sertraline is reached within a week with a single daily dose. Bioavailability during food intake is increased by 25%, while the time to reach maximum concentration is shortened.

Distribution. Total binding of sertraline to plasma proteins is 98%. The volume of distribution is >20 l/kg.

Metabolism and excretion. Sertraline undergoes intensive metabolism during its first passage through the liver, undergoing N-demethylation. Its main metabolite, N-desmethylsertraline, is less active than the original compound. Metabolites are excreted with urine and feces in equal amounts. About 0.2% of sertraline is excreted unchanged by the kidneys. The half-life of the drug is 22-36 hours and does not depend on age or sex. For N-desmethylsertraline this figure is 62-104 hours.

The half-life of sertraline and the area under the plasma concentration curve (AUC) increases with impaired hepatic function. Regardless of the severity of renal impairment, the pharmacokinetics of sertraline does not change with its continuous use.

Sertraline penetrates into breast milk. There is no data on its ability to pass through the blood-brain barrier. Sertraline is not dialyzed.

Indications

Active ingredient

Composition

1 film-coated tablet contains:

the active ingredient:

sertraline hydrochloride in terms of sertraline 50 or 100 mg;

excipients:

Microcrystalline cellulose,

sodium carboxymethyl starch,

calcium hydrophosphate dihydrate,

polysorbate,

magnesium stearate;

hypromellose,

propylene glycol,

titanium dioxide.

How to take, the dosage

Depression and OCD
Adults
The initial dose is 50 mg of Sertraline once daily, morning or evening. The daily dose can be gradually increased from 50 mg to a maximum daily dose of 200 mg, at the earliest after one week.

Panic Disorders and PTSD
The initial dose is 25 mg of Serenate once daily, morning or evening. After a week, the doctor may increase the dose to 50 mg of Sertraline once daily, and then gradually, at the earliest after a week, the daily dose may be gradually increased from 50 mg to a maximum daily dose of 200 mg.

Satisfactory therapeutic results are usually achieved after 7 days from the start of treatment. However, regular use of the drug for 2-4 weeks is required to achieve full therapeutic effect. In patients with obsessive-compulsive disorders, it may take 8-12 weeks to achieve a good result. The minimum dose that provides a therapeutic effect is maintained thereafter as a maintenance dose.

Children with OCD
For children 6 to 12 years of age, the starting dose is 25 mg of sertraline once daily, in the morning or evening. After a week, the dose can be increased to 50mg once daily.

For children 12 to 17 years of age, the starting dose is 50 mg once daily, morning or evening. The daily dose can be gradually increased from 50 mg to a maximum daily dose of 200 mg, at the earliest after a week. To avoid overdose, the lower body weight in children compared to adults should be taken into account, and if the dose is increased beyond 50 mg/day, this category of patients should be closely monitored and the drug should be discontinued at the first signs of overdose.

There is no need for special dose selection in elderly patients.

Patients with hepatic dysfunction require special attention during treatment with sertraline. In severely impaired liver function, the dose of Serenat should be reduced or the intervals between doses should be increased. In patients with impaired renal function, there is no need to specifically adjust the dose.

Interaction

Monoamine oxidase inhibitors (MAOIs). Severe complications have been reported with concomitant use of sertraline and IMAOs (including selectively acting (selegiline) IMAOs and with reversible type of action (moclobemide). The development of serotonin syndrome is possible. Similar complications, sometimes fatal, occur when prescribing IMAOs during treatment with antidepressants that inhibit neuronal takeover of monoamines or immediately after their withdrawal.

The simultaneous use of selective serotonin reuptake inhibitors and IMAO can cause: hyperthermia, rigidity, myoclonus, lability of the autonomic nervous system (rapid fluctuations of respiratory and cardiovascular system parameters), changes in mental status, including increased irritability, pronounced agitation, confusion of consciousness, which in some cases can turn into a delirium or coma.

Drugs that depress the central nervous system and ethanol. The combined use of sertraline and central nervous system depressants requires close attention, and drinking alcohol during treatment with sertraline is prohibited.
Coumarin derivatives – when combined with sertraline, a significant increase in prothrombin time has been noted – in these cases, it is recommended that the prothrombin time be monitored at the start of treatment with sertraline and after 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, tolbutamide and warfarin).

Cimetidine: concomitant use significantly reduces the clearance of sertraline.

Drugs metabolized by cytochrome P450 isoenzyme 2D6: prolonged treatment with sertraline at a dose of 50 mg per day is accompanied by increased concentration of desipramine.

Drugs metabolized by other cytochrome P450 enzyme systems. Experiments on study of interaction in vitro showed that beta-hydroxylation of endogenous cortisol, as well as metabolism of carbamazepine and terfenadine by CYP 3A3/4 isoenzyme do not change with long-term administration of Sertraline at a dose of 200 mg per day. Plasma concentrations of tolbutamide, phenytoin and warfarin also do not change with long-term administration of Sertraline in the same dose. Thus, it can be concluded that sertraline does not inhibit CYP 2C9 isoenzyme.

Sertraline has no effect on the serum concentration of diazepam, indicating that it does not inhibit the CYP 2C19 isoenzyme. According to in vitro studies, Sertraline has little or no effect on the CYP 1A2 isoenzyme.

Lithium. The pharmacokinetics of lithium is not altered by concomitant administration of sertraline. However, tremor is observed more frequently when they are used together. As with the administration of other selective serotonin reuptake inhibitors, co-administration of sertraline with drugs that affect serotoninergic transmission (e.g., lithium) requires increased caution.

Drugs affecting serotonergic transmission. There is no need for a “washout period” when replacing one serotonin neuronal takeover inhibitor with another. However, caution is required when altering the course of treatment. Co-prescribing tryptophan or fenfluramine with sertraline should be avoided.

Induction of microsomal liver enzymes. Sertraline causes minimal induction of hepatic enzymes. Concomitant administration of sertraline and antipyrine at a dose of 200 mg leads to a significant decrease in the half-life of antipyrine, although this occurs in only 5% of observations.

Athenololol: when co-administered sertraline does not change its β-adrenoblocking effect.
Glibenclamide and digoxin: No drug interaction with these drugs was found when administering Sertraline in a daily dose of 200 mg.

Special Instructions

Serenate should not be coadministered with an IMAO or for 14 days after discontinuation of IMAO treatment. Similarly, no IMAO should be prescribed for 14 days after withdrawal of sertraline.

It should be noted that there is insufficient experience with the use of sertraline in patients undergoing electroconvulsive therapy. The possible success or risk of such combined treatment has not been studied.

Depressed patients are at risk for suicide attempts. This risk persists until remission develops. Therefore, ongoing medical monitoring of patients should be established from the beginning of treatment until optimal clinical effect is achieved.

The effect on the ability to drive and operate machinery:

Prescribing,sertraline is generally not accompanied by impairment of psychomotor functions. However, its use simultaneously with other drugs may lead to impairment of attention and coordination of movements. Therefore, during treatment with sertraline it is not recommended to drive vehicles, operate machinery, or engage in activities associated with increased risk.

Contraindications

With caution: organic brain disease (including mental retardation), manic states, epilepsy, hepatic and/or renal insufficiency, weight loss, in children over 6 years.

Side effects

Dry mouth, increased sweating, drowsiness, headache, dizziness, tremor, insomnia, anxiety, agitation, hypomania, mania, decreased appetite (rarely – increase), up to anorexia, dyspeptic disorders (flatulence, nausea, vomiting, diarrhea), abdominal pain, weight loss, gait disturbances.

Possible also weakness, redness of the skin, visual disturbances, ejaculation disorders, decreased libido.

During treatment with sertraline, extrapyramidal disorders, dyskinesias, tremors, seizures, menstrual disorders, hyperprolactinemia, galactorrhea, skin rash, and occasionally erythema multiforme were noted. Motor disorders were more frequently noted in patients with a history of such disorders or with concomitant use of antipsychotic agents.

Rare cases of withdrawal syndrome have been described when discontinuing treatment with sertraline. Paresthesias, hypoesthesias, symptoms of depression, hallucinations, aggressive reactions, psychomotor agitation, restlessness or symptoms of psychosis which cannot be distinguished from symptoms of the underlying disease may occur.

Laboratory test data: rarely – in 0.8% of observations, with long-term use – asymptomatic increase in serum transaminase activity occurs. Cancellation of the drug in this case leads to normalization of enzyme activity.
During treatment with sertraline, transient hyponatremia may occur. This occurs more often in elderly patients, as well as when taking diuretics or a number of other drugs. Such side effect is associated with the syndrome of inadequate secretion of antidiuretic hormone.

Overdose

Serious symptoms of Sertraline overdose have not been found, even when administered in high doses. However, severe poisoning may occur when administered concomitantly with other drugs or ethanol.

Overdose may cause serotonin syndrome with nausea, vomiting, drowsiness, tachycardia, agitation, dizziness, psychomotor agitation, diarrhea, increased sweating, myoclonus and hyperreflexia.

Treatment: there are no specific antidotes. Intensive supportive therapy and constant monitoring of vital body functions is required.

Inducing vomiting is not recommended. Administration of activated charcoal may be more effective than gastric lavage. Airway patency should be maintained. Sertraline has a large volume of distribution, so increasing diuresis, performing dialysis, hemoperfusion, or blood transfusion may be ineffective.

Pregnancy use

There are no controlled outcomes of Sertraline in pregnant women, so the drug should only be prescribed if the expected benefit to the mother outweighs the potential risk to the fetus.

Women of reproductive age who are to be prescribed sertraline should be advised to use effective contraception.

Sertraline is found in breast milk, so treatment with this drug during breastfeeding is not recommended.

There are no good safety data about its use in this case.

If treatment is still necessary, it is best to stop breastfeeding.

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