Thorin - instructions for use, dose, side effects, contraindications

Name	Amount, mg
	Tab 50 mg	Tab. 100 mg
Sertraline hydrochloride	56	112
in terms of sertraline	50	100
Excipients
Calcium phosphate dihydrate	77,6	155,2
Sodium carboxymethyl starch (primogel)	4,8	9,6
Microcrystalline cellulose	11,2	22,4
Silica colloidal dioxide (aerosil)	0,8	1,6
Povidone (polyvinylpyrrolidone)	8	16
Calcium stearate	1,6	3,2
Shell
Hepromellosis	2,15	4,3
(hydroxypropylmethylcellulose)
Povidone (polyvinylpyrrolidone)	1,35	2,7
Macrogol 4000 (polyethylene glycol 4000)	0,45	0,9
Titanium dioxide	0,45	0,9
Talc	0,6	1,2

Description:

tablets covered with a film shell of white or almost white color, 'round, biconvex.

Pharmacotherapeutic group:antidepressant

ATX: & nbsp

N.06.A.X Other antidepressants

N.06.A Antidepressants

N.06.A.B Selective serotonin reuptake inhibitors

Pharmacodynamics:Mechanism of action. Sertraline is a selective serotonin reuptake inhibitor (5-HT). It has very little effect on the re-uptake of norepinephrine and dopamine. In therapeutic doses sertraline blocking, seizure of serotonin by human platelets. It does not have a stimulating, sedative or v anticholinergic action. Sertraline does not have an affinity for muscarinic - (cholinergic), 1 serotonergic, dopaminergic, adrenergic; , histaminergic, GABA or benzodiazepine receptors. Antidepressant. the effect is noted towards the end of the second week of regular sertraline intake, whereas the maximum effect is achieved only after 6 weeks. Unlike tricyclic * antidepressants, sertraline does not increase body weight. Sertraline does not cause mental or physical drug dependence.

Pharmacokinetics:

Absorption of sertraline from the gastrointestinal tract is high, but it is slow. The maximum concentration in the blood plasma is achieved in 4,5-8,4 hours after taking the drug inside.The equilibrium concentration of sertraline in blood plasma is reached, within a week with a single daily intake. Bioavailability during reception - food rises by 25%, while the time to reach maximum concentration is shortened.

Distribution. The total binding of sertraline to plasma proteins is 98%. Volume - distribution> 20l / kg.

Metabolism and excretion. Sertraline is subjected to intensive metabolism during the first passage through the liver, undergoing N-demethylation. Its main metabolite is 1 N-desmethylsertralin is less active than the parent compound. Metabolites are excreted through the kidneys and intestines in equal amounts. About 0.2% sertraline

is excreted by the kidneys unchanged. The average half-life (T1 / 2) of sertraline in young and elderly men and women is 22-36 hours. According to the final T1 / 2, approximately twice the cumulation of the drug is observed before the onset of equilibrium concentrations after 1 week of treatment (dose intake once a day). The pharmacokinetics of sertraline in children with OCD (see below) 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.

The half-life of sertraline and the area under the plasma concentration curve (AUC) increase with liver function impairment. Regardless of the severity of renal failure, the pharmacokinetics of sertraline when it is used consistently

does not change. Sertraline penetrates into breast milk. Sertraline not dialyziruetsya.

Indications:

Depression of various etiologies (treatment and prevention);

Obsessive-compulsive disorder (ROC);

Panic disorders;

Post-traumatic stress disorder (PTSD);

Social phobia.

Contraindications:

Hypersensitivity to sertraline or other components of the drug;

Simultaneous administration of monoamine oxidase (MAO) inhibitors and pimozide;

Unstable epilepsy;

Children under 6 years;

Pregnancy and lactation. .

Carefully:

: organic brain diseases (including mental retardation), epilepsy, hepatic and / or renal failure, marked weight loss, in children older than 6 years.

Pregnancy and lactation:

Controlled results of the use of sertraline in pregnant women are not, therefore ' - ’

, it is only necessary to prescribe a drug if the expected benefit for the mother

exceeds the potential risk for. the fetus. Women of reproductive age, *

which are supposed to be appointed sertraline, it should be recommended to use effective contraceptives. Sertraline is found in breast milk, and therefore treatment with this drug during breastfeeding is not recommended. If the treatment is still the same. it is necessary, then it is better to stop breastfeeding. Some newborns whose mothers during pregnancy took antidepressants from the group of selective serotonin reuptake inhibitors (SSRIs), including serotonin, there may be symptoms similar to the response to drug withdrawal.

Dosing and Administration:

The drug is administered orally, once a day in the morning or in the evening, regardless of food intake. „

Adult patients

Initial dose

Depression and OCD: The initial dose is 50 mg of thorin once a day, in the morning or in the evening.

Panic disorder and PTSD, social phobia: The initial dose is 25 mg of thorin once a day, in the morning or in the evening. After a week, you can increase the dose to 50 mg -

, ' 1 < ' * * 4 \

sertraline once a day%

Dose selection

Depression, OCD, panic disorder, PTSD, social phobia: The daily dose can be gradually, not earlier than a week increased from 50 mg to a maximum dose of 200 mg / day. The initial therapeutic effect may appear within 7 days, the full effect in 2-4 weeks. In patients with obsessive-compulsive disorders, it may take 8-12 weeks to achieve a good result. Supportive therapy - , : , *

The minimum dose providing the therapeutic effect is preserved as a supporting one in the future.

Children and adolescents OCD

For children from 6 to 12 years, the initial dose is 25 mg sertraline once a day, in the morning or in the evening. After a week, you can increase the dose to 50 mg once a day. For adolescents from 13 to 17 years, the initial dose is 50 mg once a day, in the morning or in the evening. The daily dose can be gradually, not earlier than a week, increase from 50 mg to a maximum daily dose of 200 mg. To avoid overdosing should take into account the smaller body weight in children compared to adults, and, 'increasing doses greater than 50 mg / day should be closely monitored for this category of patients and remove the drug at the first sign of overdose.

Selection of dose in children and adolescents

The half-life of sertraline is! approximately 1 day, therefore the dose change should occur with an interval of not less than 1 week.

In elderly patients, there is no need for a special dose selection.

Patients with impaired liver function require special attention in the treatment of sertraline. In case of severe disorder of the liver function, the dose of the drug should be reduced, or the intervals between doses should be increased.

In patients with impaired renal function, there is no need to select a dose. '

Precautions for use

Sertraline should not be administered simultaneously with monoamine oxidase (MAOI) inhibitors, and also within 14 days after discontinuation of MAOI treatment. Similarly, after the withdrawal of sertraline within 14 days, no MAOI is prescribed.

Serotonin syndrome and malignant neuroleptic syndrome. With the use of selective serotonin uptake inhibitors (SSRIs), cases of the development of serotonin syndrome (SS) and malignant neuroleptic syndrome

(NSA). Manifestations of the SS can be changes in mental status (agitation,

hallucinations, coma), autonomic lability (tachycardia, fluctuations in blood pressure, hyperthermia), changes in neuromuscular transmission (hyperreflexia, impaired coordination of movements) and / or gastrointestinal disturbances (nausea, vomiting and diarrhea). Some manifestations of SS, including hyperthermia, rigidity of muscles, vegetative 'lability with the possibility of rapid fluctuations - - parameters of vital functions, as well as changes in mental status, can' resemble symptomatology developing under NSA.

Other serotonergic agents

Care must be taken when concurrently administering sertraline with other drugs that enhance serotonergic neurotransmission, such as tryptophan, fenfluramine, or 5-HT agonists. Such a joint appointment for> opportunity should be ruled out, given the possibility of pharmacodynamic interaction.

Transition from other SSRIs, antidepressants or anti-obsessive drugs. \ Care must be taken when. such a transition, especially with long-acting drugs, for example, with fluoxetine.

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, it should be avoided in patients with unstable epilepsy, and patients with controlled epilepsy should be carefully observed during treatment. When the seizures appear, the drug should be discontinued.

Patients with major depressive disorder, (MDD), adults and children, may experience aggravation - depression and / or the appearance of suicidal thoughts and - suicidal behavior. A combined analysis of clinical trials of antidepressants (SSRIs - etc.) has shown that these drugs increase the risk

the emergence of suicidal thoughts and suicidal behavior in children, adolescents and young adults (aged 18-24 years) with major depressive disorder and other mental disorders. This danger persists until the development of remission. Therefore, from the beginning of treatment and until the optimal clinical effect is reached, patients should be provided with permanent medical supervision.

Activation of mania / hypomania.During clinical trials, hypomania and mania were observed in approximately 0.4% of patients who received sertraline.

Application in the failure of liver function. With repeated administration of sertraline in patients with stable hepatic cirrhosis, an increase in T1 / 2 'was observed and a tripling increase in AUC (area under, curve concentration / time) was observed. and Stach in comparison with those of healthy people. When 'appointment sertralina to a patient with impaired liver function should discuss

? * s

the advisability of reducing the dose or increasing the interval between taking the drug. -

Application in renal failure. Correction of sertraline dose depending on the severity of renal failure is not required.

Pathological bleeding / hemorrhage. It is advisable to use caution in the appointment of selective serotonin reuptake inhibitors in combination with drugs with established ability to change the function of platelets, as well as in patients with hemorrhagic diseases in history.

Hyponatremia

During treatment with sertraline, transient hyponatremia may occur,especially in elderly patients or when taking diuretics, a number of other drugs. With the development of symptomatic hyponatraemia sertraline should be abolished and an appropriate therapy aimed at correcting the sodium level in the blood should be prescribed. Symptoms of hyponatremia: headache, impaired concentration, memory impairment, weakness and instability, falls; in severe cases, hallucinations, fainting, convulsions, coma, respiratory arrest may occur.

Side effects:

From the gastrointestinal tract: dryness of the oral mucosa,; dyspeptic disorders (flatulence, nausea, vomiting, diarrhea), abdominal pain. ' . '

From the cardiovascular system: heart palpitations. * '.

From the musculoskeletal system: arthralgia, muscle cramps. '-

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

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

On the part of the reproductive system: disorders of ejaculation, decreased libido, -

From the endocrine system: a menstrual cycle, galactorrhea, hyperprolactinaemia,

Allergic reactions: urticaria, pruritus, anaphylactoid reaction. ,

Laboratory test data: rarely - in 0.8% of observations, with long-term use there is an asymptomatic increase in the activity of transaminases in the blood serum. , Cancellation of the drug in this case leads to a normalization of enzyme activity. Possible development of leukopenia, thrombocytopenia, hypercholesterolemia. During treatment with sertraline, transient hyponatremia may occur; "This is more often developed in elderly patients, as well as with the intake of diuretics or a number of other drugs. A similar side effect is associated with the syndrome of inadequate secretion of antidiuretic hormone.

Other: weakness, redness of the skin or "tides" of blood to the face, ringing in the ears, alopecia, ;

increased sweating, decreased appetite (rarely - increased), - up to anorexia, bleeding (incl.nasal, gastrointestinal, hematuria), Stephen-Johnson syndrome and epidermal necrolysis.

When treatment with sertraline is discontinued, rare cases of withdrawal syndrome are described / May

appear paresthesia, gipostezii, depressive symptoms, hallucinations, aggressive reaction, agitation, anxiety or psychotic symptoms that are indistinguishable from symptoms of the underlying disease.

Overdose:

Severe symptoms with an overdose of sertraline was not detected even with the administration of the drug in large doses. However, with simultaneous administration with other drugs or ethanol, severe poisoning can occur, up to coma. ' ,

Overdose can cause serotonin syndrome with nausea, vomiting, somnolence, tachycardia, agitation, dizziness, -psihomotornym agitation, diarrhea, sweating, myoclonus and hyperreflexia.

Treatment: there are no specific antidotes. It requires intensive maintenance therapy and constant monitoring of vital body functions. It is not recommended to induce vomiting. The introduction of activated carbon can be more effective than gastric lavage.It is necessary to maintain airway patency. U. sertraline a large volume of distribution, 'in connection with this, increased diuresis, dialysis, hemoperfusion or blood transfusion may not be successful:; ", '

Interaction:

Pimozide. With the simultaneous use of sertraline and pimozide, there was an increase in the concentration of pimozide with its single administration in a dose of 2 mg. Because pimozide has a narrow therapeutic index, simultaneous administration of pimozide and sertraline is contraindicated.

Inhibitors of monoamine oxidase (MAOI). Severe complications are noted in the simultaneous use of sertraline and MAOI (including selectively acting (selegiline) MAAO and with a reversible type of action (moclobemide, linezolid). Perhaps the development of serotonin syndrome. Similar complications, sometimes with fatal, outcome, arise when MAOI is prescribed against a background of treatment with antidepressants,., Oppressing neuronal capture of monoamines or immediately after their withdrawal.

With simultaneous application of selective inhibitors of reverse neuronal, seizure of serotonin and MAOA, hyperthermia, rigidity,myoclonus lability of the autonomic nervous system (rapid fluctuations in the parameters of the respiratory and cardiovascular system), changes in mental status, including increased irritability, marked agitation, confusion, which in some cases can go into a delirious state or to whom.

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, and the use of alcoholic beverages during the treatment with sertraline is banned.

Anticoagulants of indirect action (warfarin) - with their simultaneous use there is an increase in prothrombin time, in these cases it is recommended to monitor prothrombin time at the beginning of treatment with sertraline and after its withdrawal. ' Pharmacokinetic interaction �?

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

Cimetidine: simultaneous use significantly reduces the clearance of sertraline.

Drugs metabolized by isoenzyme 2D6 cytochrome. P450:

long-term treatment with sertraline at a dose of 50 mg per day is accompanied by an increase in the concentration of desipramine. '

Drugs metabolized by other enzymatic systems of cytochrome P450. Experiments on the study of interaction in vitro have shown that

isoenzyme CYP ZAZ / 4 beta-hydroxylation of endogenous cortisol, as well as the metabolism of carbamazepine and terfenadine for long-term sertraline administration

the dose of 200 mg per day does not change. The concentration in the blood plasma of tolbutamide, phenytoin and warfarin in the long-term administration of sertraline in the same dose also does not change.

. Thus, it can be concluded that sertraline Do not depress isoenzyme CYP 2C9.

Sertraline does not affect the concentration of diazepam in the serum, indicating that there is no inhibition of isoenzyme SNZ 2S19. According to in vitro studies sertraline practically does not influence or minimally inhibits isoenzyme CYP 1A2.

Lithium] The pharmacokinetics of lithium does not change with the concomitant administration of sertraline.

However, tremor is observed more often with their, joint-application.As well as the appointment of other selective inhibitors of reverse neuronal seizure of serotonin, the joint use of sertraline with drugs that affect serotonergic transmission (eg, with -, lithium) requires

increased caution.

Drugs affecting serotonergic transmission. When replacing one inhibitor of neuronal seizure of serotonin with another, there is no need for a "period of washing".

However, care must be taken when changing the course of treatment. Tryptophan or fenfluramine should be avoided together with sertraline.

Induction of microsomal liver enzymes. .Sertraline causes. minimal ', induction of liver enzymes. Simultaneous 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 cases.

Atenolol: with co-administration sertraline does not change its beta-adrenoblocking 'effect.

Glibenclamide and digoxin: when sertraline was administered in a daily dose, 200 mg of drug interaction with these drugs was not detected. <

Effect on the ability to drive transp. cf. and fur:

The appointment of sertraline, as a rule, is not accompanied by a violation of 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.

Form release / dosage:

Tablets, film-coated 50 mg and 100 mg.

Packaging:

For 7 tablets (for a dosage of 50 mg) or for 10 tablets (for a dosage of 100 mg) in a contour cell pack. For 28 tablets (for a dosage of 50 mg) or 30 tablets (for a dosage of 100 mg) in a can of polymeric materials. Each bank or 2 or 4 contiguous packaged packs of 7 tablets (for a dosage of 50 mg) or 3 contour packs of 10 tablets (for a dosage of 100 mg), together with the instruction for use, is placed in a pack of cardboard.

Storage conditions:In a place inaccessible to children at a temperature not exceeding 25 ° C

Shelf life:

2 years.

Do not use the product after the expiry date printed on the package.

Terms of leave from pharmacies:On prescription

Registration number:P N003379 / 01

Date of registration:17.03.2009

The owner of the registration certificate:VEROPHARM SA VEROPHARM SA Russia

Manufacturer: & nbsp

VEROPHARM SA Russia

Information update date: & nbsp20.09.2015

Illustrated instructions

Instructions

Torin® (Torin)