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

Active substance: sertraline hydrochloride 55.96 mg, equivalent to 50 mg sertraline Excipients: calcium hydrophosphate, microcrystalline cellulose (Avicel PH 101), microcrystalline cellulose (Avicel PH 102), giprollos-L, sodium carboxymethyl starch, magnesium stearate, purified water (evaporates in the process production).

Sheath: opedray white OY-S-58910, purified water (evaporates during production). The composition of dye opiate white OY-S-58910: hypromellose, titanium dioxide, macrogol 400, talc.

Tablets 100 mg

Active ingredient: sertraline hydrochloride 111.92 mg, equivalent to 100 mg sertraline Excipients: calcium hydrophosphate, microcrystalline cellulose (Avicel PH 101), microcrystalline cellulose (Avicel PH 102), giprollos-L, sodium carboxymethyl starch, magnesium stearate, purified water (evaporates in the process production).

Sheath: opedray white OY-S-58910, purified water (evaporates during production). The composition of dye opiate white OY-S-58910: hypromellose, titanium dioxide, macrogol 400, talc.

Description:

Tablets 50 mg: white or almost white oval-shaped tablets coated with a film shell engraved with the inscription "50" on one side and with a risk on the other.

Tablets of 100 mg: white or almost white oval-shaped tablets coated with a film shell engraved with the inscription "100" on one side and with a risk on the other.

Pharmacotherapeutic group:antidepressant

ATX: & nbsp

N.06.A.X Other antidepressants

N.06.A Antidepressants

N.06.A.B Selective serotonin reuptake inhibitors

Pharmacodynamics:

Antidepressant, a selective serotonin reuptake inhibitor, enhances its effects, has little effect on the reuptake of norepinephrine and dopamine; in therapeutic doses blocks the seizure of serotonin in human platelets.

Suppression of serotonin reuptake activity increases serotonergic transmission, which leads to a subsequent inhibition of adrenergic activity in the bluish locus (locus ceruleus). Sertraline inhibits also the excitation of serotonin neurons in the seam region (median line of the medulla oblongata); which leads to an initial increase in the activity of the bluish place, followed by a decrease in the activity of postsynaptic beta adrenoreceptors and presynaptic alpha-2-adrenergic receptors.

Does not cause drug dependence, does not have m-holinoblokiruyuschego and cardiotoxic effect. Does not increase the activity of the sympathetic nervous system.

Has no affinity for m-cholino, serotonin, dopamine, adreno, histamine, GABA or benzodiazepine receptors; does not inhibit monoamine oxidase (MAO).

Unlike tricyclic antidepressants in the treatment of depression or obsessive-compulsive disorder (obsessive-compulsive disorder) does not increase body weight. The initial effect is observed for 7 days, full - in 2-4 weeks.

Pharmacokinetics:

Absorption of sertraline is high, but 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 meals increases by 25%, while the time to reach maximum concentration is shortened.

Distribution. The total binding of sertraline to plasma proteins is 98%. The volume of 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, N-desmethylsertralin, is less active than the parent compound. Metabolites vschelyayutsya with urine and feces in equal amounts. About 0.2% sertraline is excreted by the kidneys unchanged. The half-life of the drug is 22-36 hours, regardless of age and sex. For N-desmethylsertraline, this indicator is 62-104 hours.

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 does not change with its constant application. Sertraline penetrates into breast milk. Data on its ability to pass through the hematoplacental barrier is not present. Sertraline not dialyziruetsya.

Indications:

Depressive conditions of various etiologies, including those accompanied by a sense of anxiety (treatment and prevention)

Panic disorders with agoraphobia and without agoraphobia

Obsessive-compulsive disorder (OCD)

Post-traumatic stress disorder (PTSD)

Contraindications:

Hypersensitivity to the active substance or other ingredients included in the preparation

Joint use of sertraline and MAO inhibitors

The combined use of sertraline with tryptophan or phenylfluoramine

Combined use with pimozide

Epilepsy during an exacerbation

Children under 6 years old

Pregnancy and lactation

Carefully:

organic brain diseases (including mental retardation), manic conditions, epilepsy (in anamnesis and without exacerbation), hepatic and / or renal failure, weight loss, in children older than 6 years.

Pregnancy and lactation:

Controlled trials of sertraline in pregnant women have not been carried out, therefore, during pregnancy, the drug can be prescribed only if the intended benefit to the mother exceeds the possible risk to the fetus.

Women of childbearing age who are treated with Sellyft should apply adequate methods of contraception. Sertraline is found in breast milk, so the use of Sellyft in lactating women is not recommended. If treatment is necessary, then breast-feeding should be stopped.

Dosing and Administration:

Depression and OCD:

Adults

Inside. 50 mg once a day in the morning or evening, regardless of food intake. In the absence of effect, a gradual (within several weeks) dose increase up to 200 mg / day (at 50 mg per week) is possible. Some clinicians recommend prescribing a dose of 25 mg / day for 1-2 days.

In patients with OCD, it may take 8-12 weeks of therapy to achieve a good result.

Panic disorder and PTSD: the initial dose is 25 mg / day in the morning or evening, followed by an increase in 1 week to 50 mg / day, and then gradually to 50 mg per week, you can increase the dose to 200 mg / day. Therapeutic effect is usually achieved after 7 days from the beginning of treatment. However, in order to achieve a complete therapeutic effect, the drug should be taken regularly for 2-4 weeks.

In the case of prolonged maintenance therapy, a minimum effective dose is prescribed, which is subsequently changed depending on the effect.

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

Patients with a dysfunction of the liver require special attention in the treatment of Sellyft. If the liver function is severely impaired, the dose of the drug should be reduced or the intervals between doses should be increased. In patients with impaired renal function, no special dose is required.

Children with 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, the dose can be increased to 50 mg once a day.

In adolescents 13-17 years, the initial dose is 50 mg / day in the morning or evening once. The daily dose can be gradually increased by 50 mg per week to a maximum dose of 200 mg / day. It is necessary to take into account the lower body weight in children compared to adults and when administering a dose of more than 50 mg / day, children should be carefully monitored in order to cancel the drug at the first signs of an overdose.

To achieve a good result, it may take 8-12 weeks of therapy.

Side effects:

From the side of the cardiovascular system: postural hypotension, tachycardia, skin hyperemia or "tides" of blood to the face.

On the part of the senses: impaired vision

From the gastrointestinal tract: rarely anorexia, increased appetite

(Possibly as a result of elimination of depression), dry mouth, nausea, vomiting, diarrhea, stomach cramps or abdominal bloating or pain.

From the nervous system: headache, dizziness, insomnia, somnolence, tremor, movement disorders (extrapyramidal symptoms, changes in gait), akathisia, convulsions, paresthesia, hypoesthesia, amnesia, depressive symptoms, hallucinations, aggression, anxiety, agitation, psychosis, depersonalization, nervousness, hypomania, mania, panic reactions, yawning, serotonin syndrome (see. in "Overdose").

From the side of the musculoskeletal system, arthralgia, myalgia

On the part of hepato-biliary system: the rare pancreatitis, hepatitis, jaundice, liver failure, asymptomatic increased activity of "liver" transaminases (aspartate aminotransferase and alanine aminotransferase).

From the urinary system, urinary retention and urinary incontinence.

On the part of the reproductive system: sexual dysfunction (delayed ejaculation, decreased potency and / or libido, anorgasmia), dysmenorrhea, galactorrhea.

On the side of the skin, a rash (rarely - multiforme exudative erythema, photosensitivity), angioedema, ecchymosis, pruritus and anaphylactoid reactions.

From the side of metabolism and endocrine system ', hyponatremia (syndrome of inadequate secretion of antidiuretic hormone (ADH), hyperprolactinaemia.

From the hemopoietic system: thrombocytopenia, bleeding (including nasal), purpura. Others: rarely - withdrawal syndrome, increased sweating; malaise.

Overdose:

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

Overdose can cause serotonin syndrome.

The initial manifestations of serotonin syndrome are observed from the side of the nervous system (extrapyramidal symptoms such as tremor, disorientation, restlessness, muscle hypertonia, hyperreflexia, myoclonic twitchings first in the feet, then spread throughout the body, ataxia, disturbance of coordination samples) and from the gastrointestinal tract spasms in the abdomen, flatulence, diarrhea, nausea,vomiting, indigestion).

When the condition becomes heavier, a manic-like state develops.

The final stage resembles a malignant neuroleptic syndrome: fever, profuse sweat, masklike face, greasiness of the face.

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. Sertraline has a large volume of distribution, in connection with this, increased diuresis, dialysis, hemolul- susion, or blood transfusion may be unsuccessful.

Interaction:

Inhibitors of monoamine oxidase (MAOI). Serious complications are noted with the simultaneous use of sertraline and MAOI, including selective (selegiline) MAAO and with a reversible type of action (moclobemide). Perhaps the development of serotonin syndrome (see the section "Overdose").

Medicines that depress the central nervous system and ethanol. The combined use of sertraline and substances that depress the central nervous system requires observation. Not compatible with ethanol.

Coumarin derivatives: when combined with sertraline, there is a significant increase in prothrombin time - in these cases it is recommended that prothrombin time be monitored at the beginning of treatment by Sirleft and after its withdrawal.

Cimetidine. With simultaneous use, significantly reduces the clearance of sertraline.

Drugs metabolized by isoenzyme 2D6 cytochrome P450. Although sertraline has only a potential property to cause clinically significant suppression of isoenzyme 2D6 cytochrome P450, however, when combined with drugs metabolized by this isoenzyme (desipramine, tricyclic antidepressants, antiarrhythmic drugs 1c grade - propafenone and fllekanaid), lower doses of sertraline are used, and with the withdrawal of sertraline, higher doses of these drugs may be required.

Drugs metabolized by other enzymatic systems of cytochrome P450. Experiments on the study of interaction in vitro have shown,that the isoenzyme CYP ZAZ / 4 beta-hydroxylation of endogenous cortisol, as well as the metabolism of carbamazepine and terfenadine with long-term administration of sertraline at a dose of 200 mg per day do not change. Concentration in blood plasma of phenytoin and warfarin with long-term administration of sertraline in the same dose also does not change. Thus, it can be concluded that sertraline Do not depress CYP2C9.

Sertraline does not affect the concentration of diazepam in the serum, indicating that there is no inhibition of isoenzyme СНЗ 2С19. According to in vitro studies sertraline practically does not influence or minimally inhibits the isoenzyme CYP1A2.

Sumatriptan. Jari joint use with sertraline in patients had weakness, hyperreflexia, impaired coordination of movements, so if necessary, such a combination of patients should be monitored.

Tolbutamide: sertraline reduces the clearance of tolbutamide (requires monitoring of glucose in the blood with simultaneous application)

Lithium. The pharmacokinetics of lithium does not change with concomitant treatment with sertraline. However, tremor is more often observed when they are used together.

Drugs affecting serotonergic transmission. When replacing one serotonin reuptake inhibitor with another, there is no need for a "washing period". However, care must be taken. Not compatible with tryptophan and fenifluramine.

Induction of microsomal liver enzymes. Sertraline causes minimal induction of liver enzymes. Simultaneous administration of sertraline and antipyrin 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. When co-introduced sertraline does not change the 13-adrenergic blocking effect of atenolol.

Glibenclamide and digoxin. With the introduction of sertraline in a daily dose of 200 mg of drug interaction with these drugs is not revealed.

Non-steroidal anti-inflammatory drugs, acetylsalicylic acid: at

joint use increases the risk of bleeding.

Special instructions:

Serlift should not be administered in conjunction with MAOI, nor within 14 days after discontinuation of MAOI treatment. Similarly, after the cancellation of Selifta, no MAOI is prescribed for 14 days.

In patients undergoing electroconvulsive therapy, sufficient experience with sertraline is absent.

It is necessary to exercise strict control over the behavior of patients in a state of depression (risk of suicide attempts) until there is a significant improvement as a result of the treatment.

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

Influence on the ability to drive vehicles and control mechanisms. The appointment of Sirleft can be accompanied by a violation of psychomotor functions. Therefore, during

Serlift treatment should be careful when driving vehicles and taking other potentially dangerous activities that require increased concentration and speed of psychomotor reactions.

Form release / dosage:

Film coated tablets 50 mg and 100 mg.

Packaging:

For 10 pieces in a blister of aluminum foil and PVC / PVDH film; 1 or 3 blisters with instructions for use in a cardboard bundle

For 14 pieces in a blister of aluminum foil and PVC / PVC film; 1 or 2 blisters with instructions for use in a cardboard bundle.

Storage conditions:

List B.

Store in a dry place at a temperature of no higher than 25 ° C.

Keep out of the reach of children.

Shelf life:

3 years.

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

Terms of leave from pharmacies:On prescription

Registration number:П N012258 / 01

Date of registration:24.12.2007

The owner of the registration certificate:Ranbaxy Laboratories LimitedRanbaxy Laboratories Limited India

Manufacturer: & nbsp

RANBAXY LABORATORIES, Ltd. India

Representation: & nbspRABBAYS LABORATORY LIMITEDRABBAYS LABORATORY LIMITED

Information update date: & nbsp20.09.2015

Illustrated instructions

Instructions

Sirlift® (Serlift®)