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Sertraline, film-coated tablets. Medicinal reference book geotar

Instructions for medical use

medicine

SERTRALINE

Trade name

Sertraline

International nonproprietary name

Sertraline

Dosage form

Film-coated tablets 25 mg, 50 mg, 100 mg

Compound

One film-coated tablet contains

active substance - sertraline hydrochloride 27.98 mg (equivalent to sertraline 25 mg),

Shell: Opadry green 15 B11947 (for a dosage of 25 mg).

active substance - sertraline hydrochloride 55.95 mg (equivalent to sertraline 50 mg)

excipients: hydroxypropylcellulose, microcrystalline cellulose, sodium starch glycolate, calcium hydrogen phosphate dihydrate, magnesium stearate

Shell: Opadry blue YS-1-10748-A (for 50 mg dosage).

active substance - sertraline hydrochloride 111.9 mg (equivalent to sertraline 100 mg)

excipients: hydroxypropylcellulose, microcrystalline cellulose, sodium starch glycolate, calcium hydrogen phosphate dihydrate, magnesium stearate

Shell: Opadry yellow YS-1-12524-A (for a dosage of 100 mg).

Description

The tablets are oval-shaped, light green, biconvex, film-coated, with a score line on one side. To the left of the marks is the marking “I”, to the right of the marks is the marking “G”. On the back of the tablet is marked “212” (for a dosage of 25 mg).

The tablets are oval, blue, biconvex, film-coated, with a score line on one side. To the left of the marks is the marking “I”, to the right of the marks is the marking “G”. On the back of the tablet is marked “213” (for a dosage of 50 mg).

The tablets are oval, light yellow, biconvex, film-coated, scored on one side. To the left of the marks is the marking “I”, to the right of the marks is the marking “G”. On the back of the tablet is marked “214” (for a dosage of 100 mg).

Farmacotherapy group

Psychoanaleptics. Antidepressants. Selective serotonin reuptake inhibitors. Sertraline

ATX code N06AB06

Pharmacological properties

Pharmacokinetics

When taking sertraline in a dose of 50 to 200 mg once a day for 14 days, the concentration of sertraline in plasma reached a maximum (C m ax) 4.5-8.4 hours after taking the drug. The pharmacokinetic profile of the drug in adolescents and the elderly does not differ significantly from the pharmacokinetic profile of adult patients aged 18 to 65 years. The pharmacokinetics of sertraline in children are similar to those in adults (although sertraline is metabolized slightly more efficiently in children). The average half-life of sertraline from blood plasma in young and elderly people varies from 22 to 36 hours. The binding of the drug to plasma proteins is approximately 98%.

Sertraline is extensively biotransformed during its first passage through the liver. The main metabolite found in plasma, N-desmethylsertraline, is significantly inferior in activity to sertraline. The half-life of N-desmethylsertraline varies between 62-104 hours. Sertraline and N-desmethylsertraline are extensively biotransformed in humans; the resulting metabolites are excreted in feces and urine in equal quantities. Unchanged sertraline is excreted in the urine in small amounts (<0,2%).

Food intake does not have a significant effect on the bioavailability of sertraline.

Pharmacodynamics

Sertraline is a potent and selective inhibitor of serotonin reuptake in neurons. It has a very weak effect on the reuptake of norepinephrine and dopamine. At clinical doses, sertraline blocks the uptake of serotonin into human platelets. Due to the selective inhibition of 5-HT uptake, sertraline does not enhance catecholaminergic activity. Sertraline has no affinity for muscarinergic (cholinergic), serotonergic, dopaminergic, adrenergic, histaminergic, GABA or benzodiazepine receptors.

Sertraline does not cause physical or mental dependence.

Indications for use

depression of various etiologies
obsessive-compulsive disorder (OCD)
panic disorder with or without agoraphobia
disorders caused by post-traumatic stress (PTS)

Directions for use and doses

Sertraline should be taken once a day in the morning or evening. Sertraline tablets can be taken with or without food

Initial therapy

Depression and OCD: Sertraline is prescribed at a dose of 50 mg/day.

Panic disorder disorders caused by post-traumatic stress (PS): Treatment should begin with a dose of 25 mg per day. After a week, the dose should be increased to 50 mg per day. This dosage regimen reduces the incidence of side effects in the early stages of treatment, especially in panic disorders.

If a dose of 50 mg is insufficient in the treatment of depression, OCD, panic disorder and PS, the effect can be achieved by increasing the dose. Dosage increases should be carried out at intervals of 1 week, if necessary, the dose can be increased up to a maximum dose of 200 mg per day.

The initial effect can be observed no later than 7 days. However, a longer period is required for the full therapeutic effect to occur, especially in OCD.

Maintenance therapy

The dosage for long-term treatment should be maintained at the minimum effective level with subsequent adjustment depending on the therapeutic effect.

Use in children

The safety and effectiveness of the drug in children with OCD (aged 6 to 17 years) has been established. In adolescents (aged 13-17 years) suffering from OCD, treatment should begin with a dose of 50 mg/day. In children (aged 6-12 years), treatment for OCD begins with a dose of 25 mg/day, after one week it is increased to 50 mg/day. Subsequently, if the effect is insufficient, the dose can be increased in steps of 50 mg/day up to 200 mg/day as needed. In clinical trials in patients with depression and OCD aged 6 to 17 years, it was shown that the pharmacokinetic profile of sertraline was similar to that in adults. However, to avoid overdose, when increasing the dose above 50 mg, it is necessary to take into account the lower body weight in children compared to adults.

Side effects

Infections and infestations

Often (>1/100,<1/10)

pharyngitis

Rarely (>1/1000,<1/100)

upper respiratory tract infections
rhinitis

Sometimes (>1/10000,<1/1000)

diverticulitis
gastroenteritis
inflammation of the middle ear Benign tumors Rarely (>1/1000,<1/100)

Disorders of the circulatory and lymphatic system

lymphadenopathy

Metabolic and digestive disorders Often (>1/100,<1/10)

anorexia
increased appetite

Sometimes (>1/10000,<1/1000)

hypercholesterolemia
hypoglycemia

Mental disorders

Very common (>1/10)

insomnia

Often (>1/100,<1/10)

depression
depersonalization
nightmares
anxiety
excitement
nervousness
decreased libido
bruxism

Rarely (>1/1000,<1/100)

hallucinations

Euphoria

unusual thoughts

Sometimes (>1/10000,<1/1000)

speech disorders
drug addiction

Psychotic disorder

Aggression

Paranoia

Suicidal thoughts

Sleepwalking

Prospermia

Nervous system disorders

Often (>1/100,<1/10)

Dizziness

Drowsiness

headache

Often (>1/100,<1/10)

Paresthesia

Hypertension

Perversion of taste

attention disorder

Rarely (>1/1000,<1/100)

Convulsions

Involuntary muscle contractions

Loss of coordination

Hyperkinesia

Amnesia

Hypesthesia

Speech disorders

Migraine

Sometimes (>1/10000,<1/1000)

Choreoathetosis

Dyskinesia

Hyperesthesia

Sensory impairment

Visual impairment

Often (>1/100,<1/10)

visual impairment

Sometimes (>1/10000,<1/1000)

Glaucoma

Lacrimal disorder

Scotoma

Diplopia

Photophobia

Hemorrhage into the anterior chamber of the eye

myadriasis

Hearing impairment

Often (>1/100,<1/10)

Tinnitus

Rarely (>1/1000,<1/100)

ear pain

Heart disorders

Often (>1/100,<1/10)

Increased heart rate

Rarely (>1/1000,<1/100)

Tachycardia

Sometimes (>1/10000,<1/1000)

Myocardial infarction

bradycardia

Vascular disorders

Often (>1/100,<1/10)

feeling of heat

Rarely (>1/1000,<1/100)

Hypertension

facial redness

Sometimes (>1/10000,<1/1000)

Peripheral ischemia

Respiratory disorders

Often (>1/100,<1/10)

Rarely (>1/1000,<1/100)

Bronchospasms

nosebleed

Sometimes (>1/10000,<1/1000)

Hyperventilation

Hypoventilation

Hissing

Deterioration in sound reproduction

Gastrointestinal disorders

Very common (>1/10)

Nausea

Dry mouth

Often (>1/100,<1/10)

Abdominal pain

Dyspepsia

Flatulence

Rarely (>1/1000,<1/100)

Inflammation of the esophagus

Dysphagia

Haemorrhoids

Increased salivation

Changing the language

Belching

Sometimes (>1/10000,<1/1000)

Tarry stool

Bloody stool

Stomatitis

Ulceration of the tongue

Dental changes

Inflammation of the tongue

oral ulceration

Hepatobiliary disorders

Sometimes (>1/10000,<1/1000)

Liver dysfunction

Skin and subcutaneous tissues

Often (>1/100,<1/10)

Hyperhidrosis

Rarely (>1/1000,<1/100)

Periorbital edema

Purpura

Alopecia

Cold sweat

Dry skin

Hives

Sometimes (>1/10000,<1/1000)

Dermatitis

Bullous dermatitis

Follicular rash

Hair structure disorder

unusual skin odor

Musculoskeletal disorders

Often (>1/100,<1/10)

Myalgia

Rarely (>1/1000,<1/100)

Ostearthritis

Muscle weakness

Back pain

muscle twitching

Sometimes (>1/10000,<1/1000)

Bone diseases

Renal and genitourinary disorders

Very common (>1/10)

Inability to ejaculate

Often (>1/100,<1/10)

Sexual dysfunction

Erectile dysfunction

Rarely (>1/1000,<1/100)

Frequent urination at night

Urinary retention

Polyuria

Pollakiuria

Urination disorder

Vaginal hemorrhage

Female sexual dysfunction

Sometimes (>1/10000,<1/1000)

Menorrhagia

Atopic vulvovaginitis

Balanoposthitis

Diseases of the genital organs

Priapism

Galactorrhea

General disorders

Very common (>1/10)

Often (>1/100,<1/10)

Chest pain

Rarely (>1/1000,<1/100)

Malaise

fever
asthenia
thirst

Sometimes (>1/10000,<1/1000)

hernia

Fibrosis at the injection site

Decreased drug tolerance

Gait disturbance

Consequences

Rarely (>1/1000,<1/100)

Weight loss

weight gain

Sometimes (>1/10000,<1/1000)

Increased aminotransferase levels

Increased levels of aspartate aminotransferase

sperm production disorders

Surgical and medical procedures

Sometimes (>1/10000,<1/1000)

vasodilation

Contraindications

known hypersensitivity to sertraline or other components of the drug

Children under 6 years old

pregnancy and lactation

Unstable epilepsy

the drug should not be prescribed to patients simultaneously receiving monoamine oxidase inhibitors (MAOIs) (or within 14 days after stopping use) and pimozide. It is recommended to stop taking sertraline 7 days before starting treatment with MAO inhibitors.

Drug interactions

When concomitantly treated with sertraline in combination with lithium preparations, which may act through serotonergic mechanisms, patients should be under appropriate supervision.

Concomitant use with phenytoin may cause a decrease in sertraline plasma levels.

When sertraline was taken simultaneously with warfarin, a small but statistically significant increase in prothrombin time was observed.

Concomitant use of sertraline with diazepam or tolbutamide leads to a small but statistically significant change in some pharmacokinetic parameters.

Cimetidine causes a significant decrease in the clearance of sertraline when used together.

Sertraline promotes the accumulation (blocks biotransformation) of H1-blockers (astemizole, terfenadine, cisapride) with prolongation of the QT interval and the possible development of fatal ventricular arrhythmias of the “pirouette” type. Increases the plasma level of the free fraction (displaces H 2 -blockers, tricyclic antidepressants, sulfonylurea derivatives, anxiolytics, digoxin) from binding with proteins.

Sertraline may inhibit the metabolism of tricyclic antidepressants, so caution should be exercised when using these drugs concomitantly.

There is variability among serotonin reuptake inhibitors to the extent of clinically important CYP2D6 inhibition. Long-term administration of sertraline results in minimal increases in steady-state plasma levels of desipramine

If concomitant use of sertraline and sumatriptan is clinically indicated, the patient's condition should be monitored.

The simultaneous administration of sertraline and substances that enhance serotonergic neurotransmission should be avoided due to the possibility of developing pharmacodynamic interactions

Concomitant use of sertraline and alcohol should be avoided

Do not use simultaneously with pimozide, monoamine oxidase inhibitors

If concomitant use with triptans is necessary, the patient should be monitored

When taken simultaneously with drugs that affect platelet function (acetylsalicylic acid and ticlopidine), the risk of bleeding increases

Special instructions

In patients with mild chronic liver failure, when taking the drug Sertraline, a decrease in clearance was observed, leading to an increase in the half-life. Therefore, the drug should be used with caution in patients with liver diseases. If the drug is prescribed to a patient with impaired liver function, it is necessary to discuss the advisability of reducing the dose or increasing the interval between taking the drug.

Sertraline undergoes active biotransformation, therefore, unchanged in the urine, it is excreted in small quantities. In patients with initial and moderate renal failure (creatinine clearance 20-50 ml/min) and patients with severe renal failure (creatinine clearance<20 мл/мин) фармакокинетические параметры препарата при однократном его приеме существенно не отличались от контроля. Однако, фармакокинетика сертралина в равновесном состоянии у этой категории больных изучена недостаточно, поэтому при лечении больных почечной недостаточностью следует соблюдать осторожность.

Co-administration of sertraline does not enhance the effects of alcohol, carbamazepine, haloperidol or phenytoin on cognitive and psychomotor function in healthy people, but concomitant use of sertraline and alcohol is not recommended.

Features of the effect of the drug on the ability to drive vehicles and potentially dangerous mechanisms

Clinical and pharmacological studies have shown that sertraline has no effect on psychomotor function. However, because psychotropic drugs may impair the mental or physical performance required to perform “potentially” hazardous activities such as driving or operating machinery, the patient should be informed of this.

Overdose

There are known cases of overdose with sertraline alone in a dose reaching 13.5 g. There are also known cases of death with an overdose of sertraline, primarily in combination with other drugs and/or alcohol. In this regard, in all cases, overdose requires intensive treatment.

Overdose symptoms: drowsiness, gastrointestinal disorders (such as nausea, vomiting), tachycardia, tremor, agitation and dizziness. Cases of coma were recorded much less frequently.

Treatment. Sertraline does not have a specific antidote. Normal airway patency and oxygenation should be ensured, as well as ventilation of the lungs if necessary. Gastric lavage, taking emetics, activated charcoal with sorbitol. It is advisable to monitor the performance of the heart and other vital organs and carry out symptomatic and supportive measures. Given the large volume of distribution of sertraline, forced diuresis, dialysis, hemoperfusion and exchange transfusion are ineffective

Release form and packaging

10 tablets in a blister pack made of polyvinyl chloride / polyvinyl dichloride film and aluminum foil.

2 strip packaging with instructions for medical use in the state and Russian languages are placed in a cardboard box

Storage conditions

Store in a dry place, protected from light, at a temperature not exceeding 25 °C.

Keep out of the reach of children!

Shelf life

Do not use after expiration date

Conditions for dispensing from pharmacies

By prescription

Manufacturer

Hetero Labs Limited, India

22-110, I.D.A. Dzhidimetla

Hyderabad-500 055, India

Registration Certificate Holder

ABMG Expert LLP, Kazakhstan

Address of the organization that receives claims from consumers regarding the quality of products (products) on the territory of the Republic of Kazakhstan

ABMG Expert LLP Almaty, st. Gogol, 86 t.2508-445

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Sertraline INN

International name: Sertraline

Dosage form: film-coated tablets

Chemical name:

(1S, 4S) - 4 - (3, 4 - dichlorophenyl) - 1, 2, 3, 4 - tetrahydro - N - methyl - 1 - naphthylamine (as hydrochloride)

Pharmacological action:

An antidepressant, a specific serotonin reuptake inhibitor, enhances its effects and has a weak effect on the reuptake of norepinephrine and dopamine; in therapeutic doses it blocks the uptake of serotonin in human platelets. Inhibition of serotonin reuptake activity increases serotonergic transmission, which leads to subsequent inhibition of adrenergic activity at the locus ceruleus. Sertraline also inhibits the excitation of serotonin neurons in the raphe region (midline of the medulla oblongata); which leads to an initial increase in locus coeruleus activity followed by a decrease in the activity of postsynaptic beta-adrenergic receptors and presynaptic alpha2-adrenergic receptors. Does not cause drug dependence, does not have psychostimulating, sedative, m-anticholinergic and cardiotoxic effects, does not change psychomotor activity. Due to the selective inhibition of serotonin uptake, it does not enhance the activity of the sympathetic nervous system. Has no affinity for m-cholinergic, serotonin (5-HT1A, 5-HT1B, 5-HT2), dopamine, adrenergic, histamine, GABA or benzodiazepine receptors; does not inhibit MAO. Unlike tricyclic antidepressants in the treatment of depression or obsessive-compulsive disorders (obsessive states), it does not increase body weight. The initial effect develops within 7 days, the full effect takes 2-4 weeks.

Pharmacokinetics:

Absorption is high (but at a slow rate). Bioavailability increases by 25% with food. TCmax when taken orally 50-200 mg 1 time per day for 14 days - 4.5-8.4 hours. Cmax and AUC are proportional to the dose within 50-200 mg of sertraline 1 time per day for 14 days, while the linear nature of the pharmacokinetic dependence is revealed . Food increases Cmax by 25% and slightly - AUC, shortens TCmax. Communication with plasma proteins - 98%. Metabolized during the "first pass" through the liver. The main metabolite, N-desmethylsertraline, is 20 times less active than sertraline in vitro and is virtually inactive in in vivo models of depression. Both sertraline and N-desmethylsertraline undergo oxidative deamination followed by reduction, hydroxylation, and glucuronide coupling. T1/2 of sertraline - 22-36 hours, metabolite - 62-104 hours. There is a twofold cumulation of the drug before the onset of Css after 1 week of treatment. In patients with liver cirrhosis, T1/2 of the drug and AUC increase compared to those in healthy people. Excreted through the gastrointestinal tract, by the kidneys.

Indications:

Depressive states (including those accompanied by feelings of anxiety); prevention of initial or chronic episodes of depression; obsessive-compulsive disorders; panic disorders.

Contraindications:

Hypersensitivity, pregnancy; lactation period, simultaneous administration of MAO inhibitors. Caution. Neurological disorders (including mental retardation), manic states, epilepsy, liver and/or kidney failure, weight loss, childhood.

Dosage regimen:

Orally, 50 mg, 1 time per day in the morning or evening, regardless of meals. If there is no effect, a gradual (over several weeks) dose increase to 200 mg/day (by 50 mg/week) is possible. Some clinicians recommend an initial dose of 25 mg/day for 1-2 days. Panic disorders: initial dose - 25 mg/day, followed by an increase to 50 mg/day for 1 week. When conducting long-term maintenance therapy, the minimum effective dose is prescribed, which is subsequently changed depending on the effect. Obsessive-compulsive disorders: in children and adolescents 13-17 years old, the initial dose is 50 mg/day; in children 6-12 years old, the initial dose is 25 mg/day, followed by an increase over 1 week to 50 mg/day. If the effect is insufficient, the dose can be increased in steps of 50 mg/day up to 200 mg/day, with an interval of at least 1 week. In elderly patients, the initial dose is 25 mg/day (morning or evening), followed by a gradual increase. VSD-0.2

Side effects:

Allergic reactions, bleeding (including nosebleeds), palpitations, dry mouth, decreased appetite. Rarely - increased appetite (possibly as a consequence of eliminating depression), nausea, vomiting, unstable stools, diarrhea, stomach or abdominal cramps, flatulence or pain, weight loss; headache, dizziness, insomnia, drowsiness, tremor, movement disorders (extrapyramidal symptoms, changes in gait), akathisia, convulsions, paresthesia, symptoms of depression, hallucinations, aggressiveness, agitation, anxiety, psychosis, skin flushing or flushing of the face, visual impairment (including blurred vision), yawning, increased sweating, sexual dysfunction (delayed ejaculation, decreased potency and/or libido, anorgasmia), dysmenorrhea, galactorrhea, hypomania, mania, hyponatremia (syndrome of inappropriate ADH secretion), hyperprolactinemia, "syndrome" withdrawal", exudative erythema multiforme, skin rash and itching. Overdose. Symptoms: anxiety, drowsiness, ECG changes, mydriasis, nausea, vomiting, tachycardia. Treatment: ensuring normal airway patency (oxygenation and ventilation), gastric lavage, administration of emetic drugs, activated carbon with sorbitol. Monitoring of heart and liver function is necessary. Forced diuresis, dialysis, hemoperfusion and exchange transfusion are ineffective (given the large volume of distribution).

Special instructions:

During the treatment period, it is necessary to strictly monitor the behavior of patients in a state of depression (risk of suicide attempts) until significant improvement occurs as a result of the treatment. Sertraline is prescribed no earlier than 14 days after discontinuation of MAO inhibitors. Women of childbearing potential should use adequate contraception during treatment. During the treatment period, care must be taken when driving vehicles and engaging in other potentially hazardous activities that require increased concentration and speed of psychomotor reactions.

Interaction:

Capable of displacing other drugs from binding to plasma proteins. It enhances the effect of indirect anticoagulants (increased prothrombin time), blocks cytochrome CYP2D6, increasing the plasma concentration of simultaneously used drugs in the metabolism of which this enzyme takes part (tricyclic antidepressants, class I antiarrhythmic drugs - propafenone, flecainide). Reduces the clearance of tolbutamide (monitoring of blood glucose is necessary during simultaneous use). MAO inhibitors increase the risk of side effects (hyperthermia, rigidity, convulsions, changes in mental status, confusion, irritability, excessive agitation with the development of delirium and coma). Incompatible with ethanol. Cimetidine reduces the AUC, Cmax and T1/2 of sertraline by 50, 24 and 26%, respectively. When used simultaneously with Li+ drugs, the risk of developing tremor increases.

Sertraline is an antidepressant (antidepressant), a specific serotonin reuptake inhibitor. Well tolerated, does not have stimulating, sedative or anticholinergic effects.

Selectively inhibits the reuptake of serotonin by the presynaptic membrane of brain neurons and platelets. Inhibition of serotonin reuptake activity increases serotonergic transmission.

It has a very weak effect on the reuptake of norepinephrine and dopamine. Sertraline does not have a stimulant, sedative or anticholinergic effect, does not alter psychomotor activity, does not enhance the activity of the sympathetic nervous system and does not have cardiotoxicity.

The initial antidepressant effect develops within 7-14 days of regular use of Sertraline and reaches a maximum after 6 weeks.

The drug does not cause physical or mental dependence.

Extensive safety studies of its long-term use in animals at doses several times higher than therapeutic doses have shown good tolerability.

Sertraline is the active substance, not the name of the drug. The original medicine is.

Indications for use

What is Sertraline used for? According to the instructions, the drug is prescribed in the following cases:

depressive states (including those accompanied by feelings of anxiety);
prevention of initial or chronic episodes of depression;
obsessive-compulsive disorders;
panic disorders.

Instructions for use Sertraline, dosage

Tablets are taken 1 time per day in the morning or evening, regardless of meals. The standard therapeutic dose is 1 Sertraline 50 mg tablet per day.

For depressive conditions and obsessive-compulsive disorders, the dosage is 50 mg/day. The effect of the drug appears already on the 7th day of treatment, and the full effect is achieved in 2-4 weeks. If no therapeutic effect is observed, the dose can be gradually increased to 200 mg/day.

Treatment of panic attacks and post-traumatic stress disorder begins with a dosage of 25 mg/day, and after a week the dose is increased to 50 mg of Sertraline. According to the instructions, this reduces the likelihood of side effects at the initial stage of therapy if the patient has mental disorders.

If the use of the drug requires a long period, then the dosage should be minimal, which subsequently varies depending on the therapeutic effect.

The dosage of the drug in elderly people does not differ from the standard one.

The optimal dosage for children 6-12 years old diagnosed with obsessive-compulsive disorder is 25 mg/day, followed by an increase in dose to 50 mg/day.

In adolescents 13-17 years old, you can start using the drug at 50 mg/day. If there is no clinical effect, the dosage can be increased by 50 mg/day to a maximum of 200 mg/day. Each dose increase should be at intervals of at least 1 week, taking into account the child’s body weight.

The use of the drug in children under 6 years of age has not been established. There is also no data on the safety of treatment for depression and panic disorders in children.

Side effects

The instructions warn about the possibility of developing the following side effects when prescribing Sertraline:

From the side of the central nervous system: dizziness, drowsiness, headache, insomnia, feeling of fatigue, weakness, tremor; rarely - manic or hypomanic state, anxiety, restlessness, visual impairment.
From the cardiovascular system: rarely - redness of the skin with a feeling of heat or warmth, a feeling of heartbeat.
From the digestive system: loss of appetite, diarrhea, dry mouth, nausea, cramps in the stomach or intestines, flatulence; rarely - constipation, vomiting.
Metabolism: increased sweating.
From the reproductive system: rarely - decreased potency.
Allergic reactions: rarely - fever, skin rash, urticaria or itching.

Use with caution if there is a history of drug abuse or dependence, impaired liver function, impaired renal function, epileptic seizures, or weight loss.

Contraindications

Sertraline is contraindicated in the following cases:

individual hypersensitivity to the components of the drug,
simultaneous use of MAO inhibitors, tryptophan or fenfluramine,
unstable epilepsy,
children under 6 years of age.

During pregnancy, it is possible if the expected benefit to the mother outweighs the potential risk to the fetus. FDA category of effect on the fetus is C.

Breastfeeding should be stopped during treatment (discovered in breast milk).

Overdose

Symptoms of overdose are serotonin syndrome - nausea, vomiting, drowsiness, ECG changes, mydriasis, tachycardia, agitation, dizziness, anxiety, psychomotor agitation, diarrhea, increased sweating, myoclonus and hyperreflexia.

It is necessary to prescribe activated carbon, symptomatic therapy, and maintain vital functions.

Sertraline analogues, price in pharmacies

Preparations containing sertraline as an active ingredient:

Aleval,
Asentra,
Deprefault,
Seralin,
Serenata,
Sirlift,
Stimuloton,
Thorin.

When choosing analogues, it is important to understand that the instructions for use, price and reviews do not apply to drugs with similar effects. It is important to consult a doctor and not change the drug yourself.

The price in Russian pharmacies for the original drug Zoloft (Sertraline) is 50 mg (30 tablets) from 2100 rubles, 50 mg (60 tablets) – from 3400 rubles. A cheap analogue is Torin (from 250 rubles), made in Russia.

Store in a dry place, out of reach of children, at a temperature not lower than 25*C. Shelf life – 3 years. Sale in pharmacies with a doctor's prescription.

Sertraline is a drug belonging to the group of antidepressants used to treat depression of various etiologies.

What is the composition and release form of the drug Sertraline?

The active substance of the pharmaceutical drug Sertraline is represented by sertraline hydrochloride, the content of which is 55.95, 27.98 and 111.9 milligrams per tablet. Auxiliary components: microcrystalline cellulose, sodium glycolate, calcium dihydrate, magnesium stearate, hydroxypropylcellulose, opadry yellow.

The medicine Sertraline is available in green, film-coated tablets. On one side of the dosage form there are markings “I” and “G”, on the other there is a designation of the dosage of the active substance. Supplied in blister packs of 10 pieces. The drug is dispensed with a prescription.

What is the effect of Sertraline?

Sertraline hydrochloride belongs to the group of antidepressants and has the ability to suppress the processes of serotonin reuptake, which leads to increased effects of the latter. The action of the drug is carried out not in the structures of the central nervous system, but in human platelets.

Increasing the amount of serotonin improves the transmission of electrical impulses in the nervous system, especially in a formation called locus coeruleus.

The drug has almost no effect on the reuptake of dopamine and norepinephrine, but is able to suppress the activity of the adrenergic system, blocking electrical activity on postsynaptic membranes.

Using the medicine leads to a significant improvement in mood, reduces anxiety, helps eliminate manic states, stimulates memory and gets rid of phobias.

In addition, unlike many other antidepressants, the drug is not addictive, does not affect m-cholinergic receptors, and does not have a cardiotoxic effect. It should also be noted that there is no effect on carbohydrate and fat metabolism, and this is extremely important because it prevents the development of obesity.

After taking the drug, the therapeutic concentration in the blood plasma is formed after 4.5 – 8 hours. The bioavailability coefficient is low, due to the effect of the first passage through the liver. Eating does not change this indicator.

Metabolization of the active substance occurs in the liver, with the formation of several less active metabolites. The half-life ranges from 60 to 100 hours or more. The drug is excreted from the body in urine and stool in approximately equal proportions.

What are the indications for use of the drug Sertraline?

Sertraline can be prescribed in the presence of the following diseases:

Depressive states of various etiologies;
Obsessive-compulsive disorders;
Stressful conditions of various origins.

It should be noted that the drug, as well as any other representative of the antidepressant group, should be taken only when its use is approved by a specialist.

What are the contraindications for use of Sertraline?

Taking Sertraline is contraindicated in the presence of the following conditions:

Pregnancy;
Lactation period;
The need to take monoamine oxidase inhibitors.

The drug is not prescribed for children under 6 years of age.

What are the uses and dosage of Sertraline?

The choice of dosage is determined by the diagnosis. You can take the medicine regardless of food, but it is strongly recommended to carry out this procedure at regular intervals.

In the absence of clinically significant improvement, the dosage can be increased every week until a maximum of 200 milligrams per day is reached.

The first positive changes should be expected no earlier than a week from the start of treatment. The maximum therapeutic effect is in about a month. Treatment is long-term.

Overdose from Sertraline

Symptoms are: drowsiness, nausea, vomiting, abdominal pain, tremors of the limbs, agitation, dizziness, tachycardia, headache. When combined with alcohol, the likelihood of an overdose increases significantly.

There is no specific antidote. Symptomatic treatment aimed at maintaining the performance of vital organs is indicated. Hemodialysis and blood transfusions are not effective.

What are the side effects of Sertraline?

From the digestive system: cramping abdominal pain, manifestations of flatulence, damage to the pancreas, nausea, vomiting, diarrhea.

From the nervous system: convulsions, drowsiness, changes in gait, hallucinations, paresthesia, acute psychomotor agitation, aggressiveness.

Other side effects: increased sweating, decreased libido and sexual dysfunction, acyclic bleeding in women, flushing of the face, visual disturbances, weight loss, peripheral edema, allergic and anaphylactic reactions.

Special instructions

In the presence of severe liver diseases occurring against the background of decreased function of this organ, the half-life of the drug may increase. To avoid the development of side effects, the dosage should be reduced.

Sertraline, as confirmed in clinical trials, does not have the ability to change the speed of psychomotor reactions. However, patients are advised to refrain from operating potentially dangerous machinery.

How to replace Sertraline, what analogues?

The drug Thorin, Stimuloton, Sertraline hydrochloride, Serenata, Seralin, Serlift, Zoloft, Asentra, Deprefolt, Aleval are analogues.

Conclusion

We reviewed the drug Sertraline, instructions for use. Treatment of depressive conditions should be carried out under constant supervision by a psychiatrist.

The patient must independently study the instructions for use of the prescribed drug. Be healthy!

Antidepressant

Active ingredient

Sertraline (as hydrochloride)

Release form, composition and packaging

Film-coated tablets white or almost white, capsule-shaped, biconvex, with a dividing line on one side; at the break - white or almost white.

Excipients: microcrystalline cellulose, sodium carboxymethyl starch, calcium hydrogen phosphate dihydrate, hydroxypropylcellulose, polysorbate, magnesium stearate.

Shell composition: hypromellose, propylene glycol, titanium dioxide.

10 pcs. - blisters (3) - cardboard packs.
10 pcs. - blisters (5) - cardboard packs.

Pharmacological action

Antidepressant. Selective reuptake inhibitor (5-HT). It has a weak effect on the reuptake of norepinephrine and dopamine. At therapeutic doses, sertraline blocks the uptake of serotonin by human platelets. Sertraline has no affinity for muscarinic, serotonin, dopamine, adrenergic, histamine, GABA or benzodiazepine receptors. Does not have a stimulating, sedative or anticholinergic effect.

The antidepressant effect is observed by the end of the second week of regular use of sertraline, while the maximum effect is achieved only after 6 weeks.

Unlike tricyclic antidepressants, sertraline does not cause weight gain. Sertraline does not cause mental or physical drug dependence.

Pharmacokinetics

Suction

After taking the drug orally, the absorption of sertraline from the gastrointestinal tract is significant, but occurs slowly. Cmax in the blood is reached after 4.5-8.4 hours. Bioavailability during meals increases by 25%, while the time to reach Cmax is shortened.

Distribution

With a single daily dose, C ss in blood plasma is achieved within a week. The binding of sertraline to plasma proteins is 98%. V d >20 l/kg.

Sertraline is excreted in breast milk. There is no data on its permeability through the placental barrier.

Metabolism and excretion

Sertraline is extensively metabolized during the “first pass” through the liver, undergoing N-demethylation. Its main metabolite, N-desmethylsertraline, is less active than the parent compound. Metabolites are excreted in urine and feces in equal quantities. About 0.2% of sertraline is excreted unchanged by the kidneys. T1/2 is 22-36 hours and does not depend on age or gender. For N-desmethylsertraline this figure is 62-104 hours.

Pharmacokinetics in special clinical situations

If liver function is impaired, T1/2 and AUC increase.

Regardless of the severity of renal failure, the pharmacokinetics of sertraline does not change with its continuous use.

Sertraline is not dialyzable.

Indications

— depression of various etiologies (treatment and prevention);

— obsessive-compulsive disorders (OCD);

- panic disorders (with or without agoraphobia);

- post-traumatic stress disorder (PTSD).

Contraindications

- unstable epilepsy;

- children under 6 years of age;

- pregnancy;

- lactation period;

- combined use of sertraline and MAO inhibitors (when replacing one drug with another, you should refrain from taking antidepressants for 14 days);

- combined use of sertraline with tryptophan or fenfluramine;

- hypersensitivity to the components of the drug.

WITH caution The drug should be used for organic diseases of the brain (including mental retardation), manic states, epilepsy, liver and/or kidney failure, and weight loss.

Dosage

For adults at depression and OCD the drug is prescribed at an initial dose of 50 mg 1 time/day in the morning or evening. The daily dose can be gradually, no earlier than a week later, increased from 50 mg to a maximum daily dose of 200 mg.

At panic disorders and PTSD The initial dose is 25 mg 1 time / day in the morning or evening. After a week, you can increase the dose to 50 mg 1 time / day, and then gradually, no earlier than a week later, the daily dose can be increased from 50 mg to a maximum daily dose of 200 mg.

A satisfactory therapeutic result is usually achieved within 7 days from the start of treatment. However, to achieve the full therapeutic effect, regular use of the drug is required for 2-4 weeks. At OCD treatment It may take 8-12 weeks to achieve good results. The minimum dose that provides a therapeutic effect is subsequently maintained as a maintenance dose.

For children at OCD

U elderly patients

At severe liver dysfunction the dose of the drug should be reduced or the intervals between doses increased.

U patients with impaired renal function no special dose selection is required.

Side effects

From the digestive system: dry mouth, decreased appetite (rarely increased), up to anorexia, dyspeptic disorders (flatulence, nausea, vomiting, diarrhea), ; with long-term use in 0.8% of cases - an asymptomatic increase in transaminase activity in the blood serum (when the drug is discontinued, enzyme activity normalizes).

From the central nervous system and peripheral nervous system: drowsiness, headache, dizziness, tremor, insomnia, anxiety, agitation, hypomania, mania, gait disturbances, weakness. During treatment with sertraline, extrapyramidal disorders, dyskinesias, tremor, convulsions, and visual disturbances were noted. Motor disorders were more often observed in patients with indications of their presence in the anamnesis or with concomitant use of antipsychotic drugs.

From the endocrine system: ejaculation disorders, decreased libido, menstrual irregularities, hyperprolactinemia, galactorrhea.

From the side of metabolism: increased sweating, weight loss; 0.8% (more often in elderly patients, as well as when taking diuretics or a number of other drugs) - transient hyponatremia (this side effect is associated with the syndrome of inappropriate ADH secretion).

Dermatological reactions: redness of the skin, skin rash; rarely - erythema multiforme.

When stopping treatment: rarely - withdrawal syndrome: possible paresthesia, hypoesthesia, symptoms of depression, hallucinations, aggressive reactions, psychomotor agitation, anxiety or symptoms of psychosis that cannot be distinguished from the symptoms of the underlying disease.

Overdose

Symptoms: no severe symptoms of sertraline overdose were detected even when the drug was prescribed in high doses. However, when taken simultaneously with other drugs or ethanol, severe poisoning may occur. Overdose can 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 care and constant monitoring of vital body functions are required. Inducing vomiting is not recommended. The administration of activated carbon may be more effective than gastric lavage. The airway must be maintained. Sertraline has a large Vd, so increasing diuresis, dialysis, hemoperfusion, or blood transfusion may not be effective.

Drug interactions

With the simultaneous use of the drug Serenata and MAO inhibitors, both selectively acting (selegiline) and with a reversible type of action (moclobemide), severe complications may develop, including serotonin syndrome. Similar complications, sometimes fatal, occur when MAO inhibitors are prescribed during treatment with antidepressants that inhibit the neuronal uptake of monoamines or immediately after their withdrawal. With the simultaneous use of selective neuronal reuptake inhibitors of serotonin and MAO inhibitors, the following occur: 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, severe agitation, confusion, which in some cases can progress to delirium or coma.

When coumarin derivatives and sertraline are administered together, a significant increase in prothrombin time is observed (it is recommended to monitor the prothrombin time at the beginning of treatment with Serenata and after its discontinuation).

Pharmacokinetic interaction

Sertraline binds to plasma proteins. Therefore, the possibility of its interaction with other protein-binding drugs (for example, diazepam, tolbutamide, etc.) should be taken into account.

When used simultaneously with cimetidine, a significant decrease in the clearance of sertraline is observed. With long-term treatment with sertraline at a dose of 50 mg/day, in case of simultaneous use, an increase in the plasma concentration of desipramine, which is metabolized with the participation of the CYP2D6 isoenzyme, is observed.

In experimental studies of drug interactions in vitro, it was shown that metabolic processes occurring with the participation of CYP3A3/4 isoenzymes - beta-hydroxylation of endogenous cortisol and metabolism of terfenadine - do not change with long-term administration of sertraline at a dose of 200 mg / day. The plasma concentrations of tolbutamide, phenytoin and warfarin also do not change with long-term administration of sertraline at the same dose. Thus, we can conclude that sertraline does not inhibit the activity of the CYP2C9 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.

The pharmacokinetics of lithium does not change with simultaneous use of sertraline, however, in such cases, tremor is more often observed. As with the administration of other selective neuronal serotonin reuptake inhibitors, the combined use of sertraline with drugs that affect serotonergic transmission (for example, lithium) requires increased caution. When replacing one neuronal serotonin uptake inhibitor with another, there is no need for a washout period. However, caution is required when changing the course of treatment.

Co-administration of tryptophan or fenfluramine with sertraline should be avoided.

Sertraline causes minimal induction of liver microsomal enzymes. The simultaneous administration of sertraline and antipyrine at a dose of 200 mg leads to a significant decrease in T1/2 of antipyrine, although this occurs in only 5% of cases.

When used concomitantly, sertraline does not change the beta-adrenergic blocking effect.

With simultaneous use of sertraline at a dose of 200 mg/day with glibenclamide or digoxin, no drug interactions were detected.

Special instructions

Sertraline should not be administered within 14 days of stopping treatment with MAO inhibitors. MAO inhibitors are not prescribed within 14 days after discontinuation of sertraline.

Patients receiving electroconvulsive therapy do not have sufficient experience with the use of the drug Serenata. The possible success or risk of this combination treatment has not been studied.

Patients suffering from depression are at risk for suicide attempts. This danger persists until remission develops. Therefore, from the start of treatment until the optimal clinical effect is achieved, patients should be under constant medical supervision.

When using the drug Serenata simultaneously with drugs that have a depressant effect on the central nervous system, special caution and careful monitoring of the patient's condition are required.

Use in pediatrics

During the treatment period, alcohol consumption is prohibited.

Impact on the ability to drive vehicles and operate machinery

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

Pregnancy and lactation

Adequate and strictly controlled clinical studies of the safety of Serenata during pregnancy have not been conducted. Prescribing the drug to pregnant women is contraindicated.

Women of reproductive age Patients who are expected to undergo treatment with Serenata should use effective methods of contraception.

Sertraline is excreted in breast milk. There are no reliable data on the safety of sertraline use during lactation. Therefore, if it is necessary to prescribe the drug, breastfeeding should be stopped.

Use in childhood

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

The drug should be used with caution in children over 6 years of age.

For children at OCD the drug is prescribed depending on age. For children aged 6 to 12 years The initial dose is 25 mg 1 time / day in the morning or evening. After a week, the dose can be increased to 50 mg 1 time / day. For children and adolescents aged 12 to 17 years The initial dose is 50 mg 1 time/day, morning or evening. The daily dose can be gradually, no earlier than a week later, increased from 50 mg to a maximum daily dose of 200 mg. To avoid an overdose, one should take into account the lower body weight in children compared to adults, and when increasing the dose to more than 50 mg/day, it is necessary to carefully monitor this category of patients and, at the first signs of an overdose, discontinue the drug.