Add to favorites

Sertraline, film-coated tablets. Medicinal reference book geotar

Instructions for medical use

medicinal product

SERTRALINE

Tradename

Sertraline

International non-proprietary 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),

Sheath: 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

Sheath: Opadry blue YS-1-10748-A (for a dosage of 50 mg).

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

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

Description

Oval-shaped, light green, biconvex, film-coated tablets, scored on one side. To the left of the risk mark "I", to the right of the risk mark "G". On the reverse side of the tablet, the marking "212" (for a dosage of 25 mg).

Oval-shaped, blue, biconvex, film-coated tablets, scored on one side. To the left of the risk mark "I", to the right of the risk mark "G". On the reverse side of the tablet, the marking "213" (for a dosage of 50 mg).

Tablets are oval-shaped, light yellow, biconvex, film-coated, scored on one side. To the left of the risk mark "I", to the right of the risk mark "G". On the reverse side of the tablet, the marking "214" (for a dosage of 100 mg).

Farmacotherapeutic group

Psychoanaleptics. Antidepressants. Selective serotonin reuptake inhibitors. Sertraline

ATX code N06AB06

Pharmacological properties

Pharmacokinetics

When taking sertraline at a dose of 50 to 200 mg once a day for 14 days, the plasma concentration of sertraline reached a maximum (Cmax) 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 is similar to that 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 pass 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 the feces and urine in equal amounts. Unchanged sertraline is excreted in the urine in small amounts (<0,2%).

Eating does not significantly affect the bioavailability of sertraline.

Pharmacodynamics

Sertraline is a potent and selective neuronal serotonin reuptake inhibitor. It has very little effect on the reuptake of norepinephrine and dopamine. At clinical doses, sertraline blocks the uptake of serotonin in human platelets. Due to selective inhibition of 5-HT uptake, sertraline does not enhance catecholaminergic activity. Sertraline does not have affinity for muscarinergic (cholinergic), serotonergic, dopaminergic, adrenergic, histaminergic, GABA or benzodiazepine receptors.

Sertraline does not cause physical and mental dependence.

Indications for use

depression of various etiologies
obsessive-compulsive disorder (OCD)
panic disorder with or without agoraphobia
post-traumatic stress disorder (PS)

Dosage and administration

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 given at a dose of 50 mg/day.

panic disorder, post-traumatic stress disorder (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 frequency 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. Dose increases should be made at 1-week intervals, if necessary, dose increases up to a maximum dose of 200 mg per day.

The initial effect can be observed no later than after 7 days. However, the full therapeutic effect, especially in OCD, requires a longer period of time.

Supportive care

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 efficacy of the drug in children with OCD (aged 6 to 17 years) have been established. In adolescents (aged 13-17 years) with OCD, treatment should begin with a dose of 50 mg/day. In children (aged 6-12 years), OCD therapy is started at a dose of 25 mg/day, increased to 50 mg/day after one week. Subsequently, with insufficient effect, the dose can be increased in steps of 50 mg / day 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, in order to avoid overdose, when increasing the dose of more than 50 mg, it is necessary to take into account the lower body weight in children compared with adults.

Side effects

Infections and infestations

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

pharyngitis

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

upper respiratory infections
rhinitis

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

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

Disorders of the circulatory and lymphatic system

lymphadenopathy

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

anorexia
increased appetite

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

hypercholesterolemia
hypoglycemia

Mental disorders

Very often (>1/10)

insomnia

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

depression
depersonalization
nightmares
anxiety
excitement
nervousness
decreased libido
bruxism

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

hallucinations

Euphoria

unusual thoughts

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

speech disorders
drug dependence

Psychotic disorder

Aggression

Paranoia

Suicidal thoughts

Sleepwalking

Prospermia

Disorders of the nervous system

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

Dizziness

Drowsiness

headache

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

paresthesia

Hypertension

perversion of taste

attention disorder

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

Convulsions

involuntary muscle contractions

Impaired coordination

Hyperkinesia

Amnesia

hypoesthesia

Speech disorders

Migraine

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

Choreoathetosis

Dyskinesia

Hyperesthesia

Sensory disturbance

visual impairment

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

visual impairment

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

Glaucoma

Lacrimal disorder

scotoma

Diplopia

Photophobia

Hemorrhage in the anterior chamber of the eye

myadriasis

Hearing disorders

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

Tinnitus

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

ear pain

Heart disorders

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

Increased heart rate

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

Tachycardia

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

myocardial infarction

bradycardia

Vascular disorders

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

sensation of heat

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

hypertension

redness of the face

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

Peripheral ischemia

Respiratory disorders

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

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

Bronchospasms

nose bleed

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

Hyperventilation

hypoventilation

hissing

Loss of sound reproduction

Gastrointestinal Disorders

Very often (>1/10)

Nausea

Dry mouth

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

Abdominal pain

Dyspepsia

Flatulence

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

Inflammation of the esophagus

Dysphagia

Haemorrhoids

Increased salivation

Language change

Belching

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

Tar stool

Bloody stool

Stomatitis

Ulceration of the tongue

Tooth changes

Inflammation of the tongue

ulceration of the mouth

Hepatobiliary disorders

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

Liver dysfunction

Skin and subcutaneous tissues

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

Hyperhidrosis

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

Perorbital edema

Purpura

Alopecia

Cold sweat

Dry skin

Hives

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

Dermatitis

bullous dermatitis

Follicular rash

Violation of the hair structure

unusual skin odor

Musculoskeletal disorders

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

Myalgia

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

Ostearthritis

muscle weakness

Backache

muscle twitches

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

Bone diseases

Kidney and urinary disorders

Very often (>1/10)

Inability to ejaculate

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

sexual dysfunction

erectile disfunction

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

Frequent nighttime urination

urinary retention

Polyuria

Pollakiuria

urinary disorder

Vaginal hemorrhage

Female sexual dysfunction

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

menorrhagia

Atopic vulvovaginitis

Balanoposthitis

Diseases of the genital organs

Priapism

Galactorrhea

General Condition Disorders

Very often (>1/10)

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

Chest pain

Rare (>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

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

Weight loss

weight gain

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

Increasing aminotransferase levels

Increased aspartate aminotransferase levels

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's age up to 6 years

pregnancy and lactation

Unstable epilepsy

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

Drug Interactions

With simultaneous treatment with sertraline in combination with lithium preparations, which can act through serotonergic mechanisms, patients should be under appropriate supervision.

Co-administration with phenytoin may cause a decrease in plasma sertraline levels.

With the simultaneous administration of sertraline with warfarin, a slight but statistically significant increase in prothrombin time was observed.

Simultaneous administration 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 they are used together.

Sertraline promotes cumulation (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 from the connection with proteins) H 2 blockers, tricyclic antidepressants, sulfonylurea derivatives, anxiolytics, digoxin.

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

There is variability among serotonin reuptake inhibitors in terms of clinically important CYP 2 D6 inhibition. Long-term administration of sertraline results in a minimal increase in persistent plasma levels of desipramine.

If co-administration 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 it is necessary to prescribe simultaneously with triptans, 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 hepatic insufficiency, when taking 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 disease. 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 moderately severe renal insufficiency (creatinine clearance 20-50 ml / min) and patients with severe renal insufficiency (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 effect of alcohol, carbamazepine, haloperidol, or phenytoin on cognitive and psychomotor function in healthy individuals, 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 does not affect psychomotor function. However, since psychotropic drugs may impair the mental or physical activity required to perform "potentially" hazardous activities such as driving or operating machinery, the patient should be informed about this.

Overdose

Cases of overdose with one sertraline at a dose of up to 13.5 g are known. There are also cases of death in case of an overdose of sertraline in the first place in combination with other drugs and / or alcohol. In this regard, in all cases, an overdose requires intensive treatment.

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

Treatment. There is no specific antidote for sertraline. 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 blister packs with instructions for medical use in the state and Russian languages are put into a cardboard box

Storage conditions

Store in a dry, dark place at a temperature not exceeding 25 °C.

Keep out of the reach of children!

Shelf life

Do not use after expiration date

Terms of dispensing from pharmacies

On prescription

Manufacturer

Hetero Labs Limited, India

22-110, I.D.A. jidimetla

Hyderabad-500 055, India

Registration certificate holder

ABMG Expert LLP, Kazakhstan

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

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

Have you taken sick leave due to back pain?

How often do you experience back pain?

Can you handle pain without taking painkillers?

Find out more how to deal with back pain as quickly as possible

Sertraline INN

International name: Sertraline

Dosage form: coated tablets

Chemical Name:

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

Pharmachologic effect:

Antidepressant, a specific serotonin reuptake inhibitor, enhances its effects, has little effect on the reuptake of norepinephrine and dopamine; in therapeutic doses blocks the uptake of serotonin in human platelets. Suppression of serotonin reuptake activity increases serotonergic transmission, which leads to subsequent inhibition of adrenergic activity in the bluish locus (locus ceruleus). Sertraline also inhibits the excitation of serotonin neurons in the suture area (midline of the medulla oblongata); which leads to an initial increase in the activity of the locus coeruleus, followed by a decrease in the activity of postsynaptic beta-adrenergic receptors and presynaptic alpha2-adrenergic receptors. It does not cause drug dependence, does not have a psychostimulating, sedative, m-anticholinergic and cardiotoxic effect, does not change psychomotor activity. Due to the selective inhibition of serotonin uptake, it does not increase the activity of the sympathetic nervous system. Does not have affinity for m-cholinergic, serotonin (5-HT1A, 5-HT1B, 5-HT2), dopamine, adreno-, histamine, GABA- or benzodiazepine receptors; does not inhibit MAO. Unlike tricyclic antidepressants, in the treatment of depression or obsessive-compulsive disorders (obsessive-compulsive disorders), it does not increase body weight. The initial effect develops within 7 days, full - after 2-4 weeks.

Pharmacokinetics:

Absorption is high (but at a slow rate). Bioavailability is increased by 25% during meals. 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 in the range of 50-200 mg sertraline 1 time per day for 14 days, while a linear 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 actually inactive in in vivo models of depression. Both sertraline and N-desmethylsertraline undergo oxidative deamination followed by reduction, hydroxylation, and glucuronide binding. T1 / 2 sertraline - 22-36 hours, metabolite - 62-104 hours. There is a two-fold cumulation of the drug before the onset of Css after 1 week of treatment. In patients with cirrhosis of the liver, T1 / 2 of the drug and AUC increase compared to those in healthy people. It is excreted through the gastrointestinal tract, by the kidneys.

Indications:

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

Contraindications:

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

Dosing regimen:

Inside, 50 mg, 1 time per day in the morning or evening, regardless of the meal. If there is no effect, a gradual (over several weeks) increase in the dose 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, it is prescribed in the minimum effective dose, 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 within 1 week to 50 mg / day. With insufficient effect, the dose can be increased in steps of 50 mg / day 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 nasal), palpitations, dry mouth, loss of appetite. Rarely - increased appetite (possibly as a result of elimination of depression), nausea, vomiting, unstable stools, diarrhea, cramps in the stomach or abdomen, flatulence or pain, weight loss; headache, dizziness, insomnia, drowsiness, tremor, movement disorders (extrapyramidal symptoms, change in gait), akathisia, convulsions, paresthesias, symptoms of depression, hallucinations, aggressiveness, agitation, anxiety, psychosis, flushing of the skin or flushing of blood to 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 " cancellation", erythema multiforme exudative, skin rash and itching. Overdose. Symptoms: anxiety, drowsiness, ECG changes, mydriasis, nausea, vomiting, tachycardia. Treatment: ensuring normal airway patency (oxygenation and ventilation of the lungs), gastric lavage, administration of emetic drugs, activated charcoal with sorbitol. It is necessary to control the function of the heart and liver. Forced diuresis, dialysis, hemoperfusion and exchange transfusion are ineffective (given the large volume of distribution).

Special instructions:

During the period of treatment, it is necessary to exercise strict control of the behavior of patients in a state of depression (risk of suicidal attempts) until there is a significant improvement as a result of the treatment. Sertraline is prescribed no earlier than 14 days after the abolition of MAO inhibitors. Women of childbearing age during treatment should use adequate methods of contraception. During the period of treatment, care must be taken when driving vehicles and engaging in other potentially hazardous activities that require an increased concentration of attention and speed of psychomotor reactions.

Interaction:

Able to displace other drugs from the connection with plasma proteins. It enhances the effect of indirect anticoagulants (an increase in prothrombin time), blocks the cytochrome CYP2D6, increasing the plasma concentration of simultaneously used drugs in the metabolism of which this enzyme is involved (tricyclic antidepressants, antiarrhythmic drugs of class Ic - propafenone, flecainide). Reduces the clearance of tolbutamide (blood glucose control is necessary with 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. With simultaneous use with Li + preparations, the risk of developing tremor increases.

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

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

It has a very weak effect on the reuptake of norepinephrine and dopamine. Sertraline has no stimulant, sedative, or anticholinergic effects, does not alter psychomotor activity, does not enhance sympathetic nervous system activity, and is not cardiotoxic.

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 and mental dependence.

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

Sertraline is the active ingredient, 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 anxiety);
prevention of initial or chronic episodes of depression;
obsessive-compulsive disorders;
panic disorder.

Instructions for use Sertraline, dosage

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

In depressive states and obsessive-compulsive disorders, the dosage is 50 mg / day. The effect of the drug appears already on the 7th day of treatment, and in 2-4 weeks the full effect is achieved. If a therapeutic effect is not 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 in the presence of mental disorders in the patient.

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 the elderly does not differ from the standard.

The optimal dosage in children 6-12 years of age 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 with 50 mg / day. In the absence of clinical effect, the dosage can be increased by 50 mg/day up to a maximum of 200 mg/day. Each dose increase should be at least 1 week apart, 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 are also no data on the safety of treating children with depression and panic disorders.

Side effects

The instruction warns of the possibility of developing the following side effects when prescribing Sertraline:

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

Use with caution in case of drug abuse or dependence on them in history, liver dysfunction, kidney dysfunction, epileptic seizures, 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's age up to 6 years.

During pregnancy, it is possible if the expected benefit to the mother outweighs the potential risk to the fetus. Category of action on the fetus according to the FDA - C.

At the time of treatment should stop breastfeeding (found in breast milk).

Overdose

Overdose symptoms 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 charcoal, symptomatic therapy, maintenance of vital functions.

Sertraline analogues, price in pharmacies

Preparations containing sertraline as an active ingredient:

Aleval,
Asentra,
Depreflot,
Seralyn,
Serenata
Sirlift,
Stimuloton,
Thorin.

When choosing analogues, it is important to understand that instructions for use, price and reviews for drugs of similar action do not apply. It is important to consult a doctor and not to make an independent replacement of the drug.

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

Store in a dry place, out of the reach of children, at a temperature not lower than 25*C. Shelf life - 3 years. Sale in pharmacies by prescription.

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

What is the composition and form of the drug Sertraline?

The active substance of the pharmaceutical product 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, hydroxypropyl cellulose, opadry yellow.

Sertraline is available in green coated tablets. On one side of the dosage form there is a marking "I" and "G", on the other side there is a designation of the dosage of the active substance. Supplied in cell packs of 10 pieces. The release of the drug is carried out with a prescription.

What is the effect of Sertraline?

Sertraline hydrochloride belongs to the group of antidepressants and has the ability to inhibit the reuptake of serotonin, which leads to an increase in the 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.

An increase in the amount of serotonin improves the transmission of electrical impulses in the nervous system, especially in the formation called the 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 by blocking electrical activity on postsynaptic membranes.

The use of the drug leads to a significant improvement in mood, reduces anxiety, helps eliminate manic states, stimulates memory and relieves 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, since 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, since the effect of the first passage through the liver affects. 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 with urine and stool in approximately equal proportions.

What are the indications for Sertraline?

Appointment of Sertraline can be carried out in the presence of the following diseases:

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

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

What are the contraindications for Sertraline?

Sertraline is contraindicated in the presence of the following conditions:

Pregnancy;
lactation period;
Need for monoamine oxidase inhibitors.

Do not prescribe a remedy at the age of less than 6 years.

What are the uses and dosages 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 a 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 about a month later. The treatment is long-term.

Overdose from sertraline

Symptoms are: drowsiness, nausea, vomiting, abdominal pain, tremor of the extremities, 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 shown. Hemodialysis and blood transfusion are not effective.

What are the side effects of sertraline?

On the part of the digestive system: spastic pain in the abdomen, 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, visual disturbances, weight loss, peripheral edema, allergic and anaphylactic reactions.

special instructions

In the presence of severe liver diseases occurring against the background of a decrease in the function of this organ, an increase in the half-life of the drug is possible. In order to avoid the development of side effects, the dosage should be reduced.

Sertraline, as it was 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 Torin, Stimuloton, Sertraline hydrochloride, Serenata, Seralin, Serlift, Zoloft, Asentra, Deprefolt, Aleval are analogues.

Conclusion

We have reviewed the drug Sertraline, instructions for use for it. Treatment of depressive conditions should be carried out with constant monitoring by a psychiatrist.

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

Antidepressant

Active substance

Sertraline (as hydrochloride) (sertraline)

Release form, composition and packaging

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, hydroxypropyl cellulose, polysorbate, magnesium stearate.

Shell composition: hypromellose, propylene glycol, titanium dioxide.

10 pieces. - blisters (3) - packs of cardboard.
10 pieces. - blisters (5) - packs of cardboard.

pharmachologic effect

Antidepressant. Selective reuptake inhibitor (5-HT). It has little 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. It does not have a stimulating, sedative or anticholinergic effect.

The antidepressant effect is noted 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 inside, the absorption of sertraline from the gastrointestinal tract is significant, but occurs slowly. C max in the blood is reached in 4.5-8.4 hours. Bioavailability during meals increases by 25%, while the time to reach C max is shortened.

Distribution

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

Sertraline is excreted in breast milk. There are 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 amounts. About 0.2% of sertraline is excreted by the kidneys unchanged. T 1/2 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

In case of impaired liver function, T 1/2 and AUC increase.

Regardless of the severity of renal insufficiency, the pharmacokinetics of sertraline does not change with its constant use.

Sertraline is not subject to dialysis.

Indications

- depression of various etiologies (treatment and prevention);

- obsessive-compulsive disorders (OCD);

- panic disorder (with or without agoraphobia);

- post-traumatic stress disorder (PTSD).

Contraindications

- unstable epilepsy;

- children's age up to 6 years;

- pregnancy;

- lactation period;

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

- the 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, weight loss.

Dosage

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 increased gradually, not earlier than a week later, from 50 mg to a maximum daily dose of 200 mg.

At panic disorder 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, not 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 after 7 days from the start of treatment. However, to achieve the full therapeutic effect, regular administration of the drug for 2-4 weeks is required. At treatment of OCD it may take 8-12 weeks to achieve a good result. The minimum dose that provides a therapeutic effect is maintained in the future as a maintenance dose.

children at OKR

At elderly patients

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

At patients with impaired renal function special dose selection is not required.

Side effects

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

From the side of the central nervous system and peripheral nervous system: drowsiness, headache, dizziness, tremor, insomnia, anxiety, agitation, hypomania, mania, gait disturbances, weakness. Movement disorders were more often observed in patients with indications of their presence in history or with concomitant use of antipsychotics.

From the endocrine system: ejaculation disorders, decreased libido, menstrual disorders, 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: skin redness, skin rash; rarely - erythema multiforme.

When treatment is stopped: 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: severe symptoms of an overdose of sertraline were not detected even when the drug was administered 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 maintenance therapy and constant monitoring of vital body functions are required. Inducing vomiting is not recommended. The introduction of activated charcoal may be more effective than gastric lavage. The airway must be maintained. Sertraline has a large V d , so increased diuresis, dialysis, hemoperfusion, or blood transfusion may not be effective.

drug interaction

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, including serotonin syndrome, may develop. Similar complications, sometimes fatal, occur when prescribing MAO inhibitors during treatment with antidepressants that inhibit neuronal uptake of monoamines or immediately after their withdrawal. With the simultaneous use of selective serotonin reuptake inhibitors and MAO inhibitors, there are: hyperthermia, rigidity, myoclonus, lability of the autonomic nervous system (rapid fluctuations in the parameters of the respiratory and cardiovascular systems), changes in mental status, including increased irritability, severe agitation, confusion, which in some cases can go into a delirious state or coma.

With the joint appointment of coumarin and sertraline derivatives, there is a significant increase in prothrombin time (it is recommended to control prothrombin time at the beginning of treatment with Serenata and after its withdrawal).

Pharmacokinetic interaction

Sertraline binds to plasma proteins. Therefore, it is necessary to take into account the possibility of its interaction with other drugs that bind to proteins (for example, with diazepam, tolbutamide and).

With simultaneous use 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 the case of simultaneous use, an increase in plasma concentration of desipramine is observed, which is metabolized with the participation of the CYP2D6 isoenzyme.

In experimental studies on drug interactions in vitro, it has been shown that metabolic processes occurring with the participation of CYP3A3 / 4 isoenzymes - beta-hydroxylation of endogenous cortisol and metabolism and terfenadine - do not change with long-term administration of sertraline at a dose of 200 mg / day. Plasma concentrations of tolbutamide, phenytoin and warfarin also do not change with long-term administration of sertraline at the same dose. Thus, it can be concluded 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 practically does not affect or minimally inhibits the CYP1A2 isoenzyme.

The pharmacokinetics of lithium does not change with the simultaneous use of sertraline, however, in such cases, tremor is more often observed. As well as the appointment of other selective 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 reuptake 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 microsomal liver enzymes. The simultaneous appointment of sertraline and antipyrine at a dose of 200 mg leads to a significant decrease in T 1/2 of antipyrine, although this occurs in only 5% of cases.

With the simultaneous use of sertraline does not change the beta-adrenergic blocking effect.

With the simultaneous use of sertraline at a dose of 200 mg / day with glibenclamide or digoxin, drug interactions have not been identified.

special instructions

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

Patients receiving electroconvulsive therapy lack sufficient experience with Serenata. The possible success or risk of such combined treatment has not been studied.

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

With the simultaneous use of the drug Serenata and drugs that have a depressing effect on the central nervous system, special care and careful monitoring of the patient's condition are required.

Pediatric use

During the treatment period, alcohol is prohibited.

Influence on the ability to drive vehicles and control mechanisms

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 impaired attention and coordination of movements. Therefore, during treatment with sertraline, it is not recommended to drive vehicles, special equipment or engage in activities associated with an increased risk.

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 who are expected to be treated with Serenata should use effective contraceptive methods.

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

Application in childhood

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

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

children at OKR the drug is prescribed depending on age. For children aged 6 to 12 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, in the morning or in the evening. The daily dose can be gradually, not earlier than a week later, increased from 50 mg to a maximum daily dose of 200 mg. To avoid overdose, one should take into account the lower body weight in children compared to adults, and with an increase in the dose of more than 50 mg / day, careful monitoring of this category of patients is necessary and the drug should be discontinued at the first signs of an overdose.