Золофт

Золофт – drug with antidepressive action.

Form of release and structure

Золофт release in the form of tablets, coated: oblong, white color, on one of the parties the text of "Pfizer", on other party for a dose of 50 mg - "ZLT|50", for a dose of 100 mg - "ZLT|100" is squeezed out (on 14 pieces in blisters from aluminum foil and opaque polypropylene, on 1 or 2 blisters in a cardboard pack).

Structure of 1 tablet:

• Active ingredient: sertraline – 50 or 100 mg (in the form of a sertraline hydrochloride);
• Auxiliary components: microcrystallic cellulose, phosphate calcium, hydroxypropyl cellulose, magnesium stearate, glikolit starch of sodium, a gidroksipropilmetiltsellyuloz, polysorbates, polyethyleneglycol, dioxide of titanium (E171).

Indications to use

• Sociophobia (social alarming frustration);
• OCF (obsessivno-compulsive frustration);
• PTSR (posttraumatic stressorny frustration);
• Incidental paroxysmal uneasiness (panic frustration);
• Depressions of various etiology (prevention and therapy).

Contraindications

Absolute:

• Simultaneous use of sertraline with monoamine oxidase inhibitors (MAO) and Pimozidum;
• Age up to 6 years;
• Hypersensitivity to drug components.

With care (because of the increased probability of complications):

• Epilepsy;
• The expressed decrease in body weight;
• Organic lesions of a brain (including a delay of intellectual development);
• Renal and/or liver failure.

Controlled researches on use of sertraline during pregnancy were not conducted therefore to appoint drug to pregnant women it is allowed only in case the expected advantage for mother considerably exceeds potential risk of development of pathologies of a fruit. Women at reproductive age which supposes Zoloft's appointment for therapy should use effective contraceptive remedies.

Sertraline gets into breast milk. Administration of drug during breastfeeding is not recommended as safety of use in this case is authentically not confirmed. If treatment is necessary, then for a while it is necessary to stop feeding by a breast.

As a result of use of sertraline at pregnancy and during breastfeeding in a complex with antidepressants from the SIOZS group (selective serotonin reuptake inhibitors), including serotonin, at some newborns the symptoms similar to cancellation reaction can be shown.

Route of administration and dosage

Золофт accept inside, irrespective of meal, 1 times a day, in the morning or in the evening:

• ROC and depressions of various etiology: an initial dose – 50 mg a day;
• PTSR, sociophobia, panic frustration: an initial dose – 25 mg a day, in 1 week increase a dose to 50 mg a day (such scheme allows to reduce the frequency of the early undesirable effects of therapy characteristic of panic frustration).

If use of sertraline in a dose of 50 mg a day is insufficiently effective, the dose can be increased. It is recommended to raise a dose with an interval not more often than once a week, without exceeding the maximum recommended – 200 mg a day.

In 7 days after the beginning of administration of drug the initial result can be observed, however the maximum effect is usually reached 2-4 weeks (in case of ROC for this purpose longer time usually is required) later.

For carrying out a course of the long supporting treatment of Zoloft appoint in a minimal effective dose which is allowed to be changed depending on the achieved clinical result.

The recommended dosing mode for therapy of ROC at children and teenagers, depending on age:

• 6-12 years: an initial dose – 25 mg a day, 1 week later increase it to 50 mg a day; further, if the effect is insufficient, the dose can be increased in steps on 50 mg to 200 mg a day;
• 13-17 years: an initial dose – 50 mg a day.

By results of clinical trials of a pharmacokinetic profile of sertraline at patients with a depression and ROC aged from 6 years up to 17 years it was revealed that it was similar to that at adults. To avoid overdose, increasing a dose more than 50 mg, it is necessary to consider that children have a body weight less, than at adults.

Sertraline elimination half-life about days therefore change of a dose it is necessary to spend not less than a week with an interval.

At advanced age dose adjustment of Zoloft is not required.

Side effects

• Cardiovascular system (CCC): tachycardia, tachycardia, arterial hypertension;
• Alimentary system: an abdominal pain, dryness in a mouth, pancreatitis, dispepsichesky frustration (nausea, vomiting, a meteorism, diarrhea, a lock);
• Musculoskeletal system: muscular spasms, arthralgia;
• System of breath: yawning, bronchospasm;
• Central and peripheral nervous system: paresthesias, faint, migraine, headache, dizziness, tremor, drowsiness, sleeplessness, alarm, hypomania, mania, agitation, hallucinations, euphoria, psychosis, decrease libido, nightmares, suicide, coma, extrapyramidal frustration (akathisias, bruxism, dyskinesia, gait disturbance);
• Urinary system: enuresis, delay or incontience of urine;
• Reproductive system and mammary gland: galactorrhoea, gynecomastia, disturbance of sexual function (decrease in a potentiality, ejaculation delay), disturbance of a menstrual cycle, priapism;
• Organs of sight: mydriasis, vision disorder;
• Endocrine system: hypothyroidism, giperprolaktinemiya, syndrome of inadequate secretion of antidiuretic hormone (ADG);
• Gepatobiliarny system: jaundice, hepatitis, liver failure;
• Allergic reactions: itch, urticaria, anaphylactoid reaction;
• Others: weakness, a ring in ears, "inflows" of blood to the person or erubescence, an alopecia, a face edema, a Quincke's disease, periorbital hypostasis, reaction of a photosensitization, the increased sweating, a purpura, a loss of appetite, up to anorexia (it is rare – increase), increase or decrease in body weight, bleeding (including gastrointestinal, nasal or a hamaturia), peripheral hypostases, occasionally Stephen-Johnson's syndrome and an epidermal necrolysis;
• Data of laboratory researches: in case of prolonged use seldom there is a symptomless increase in blood serum of activity of transaminases (at drug withdrawal activity of enzymes is normalized); development of thrombocytopenia and a leukopenia, increase in cholesterol level blood serum is possible; the therapy termination by sertraline in rare instances can become the reason of the withdrawal which is followed by paresthesias, hypesthesias, depression symptoms, hallucinations, aggressive reactions, psychomotor excitement, concern or symptoms of psychosis which cannot be distinguished from signs of a basic disease.

At overdose of sertraline considerable side effects, even in case of use of high doses are not revealed. Zoloft's use with other substances / drugs or alcohol can become the reason of a serious poisoning, up to a coma and a lethal outcome.

Overdose signs – the serotoninovy syndrome which is followed by psychomotor excitement, nausea, vomiting, tachycardia, agitation, drowsiness, the dizziness, diarrhea raised by sweating, a hyperreflexia and a myoclonus. Specific antidotes do not exist, the intensive maintenance therapy with continuous monitoring of the vital functions is necessary. To provoke vomiting not effectively, reception of absorbent carbon can be more productive than a gastric lavage. It is important to maintain passability of respiratory tracts. Because of the large volume of distribution of sertraline, and strengthening thereof diuresis, carrying out dialysis or hemoperfusion, and also hemotransfusion, can be not productive.

Special instructions

Sertraline is not applied together with MAO inhibitors, between courses of reception of these substances it is necessary to observe a break at least 2 weeks.

At use of SIOZS cases of development of a serotoninovy syndrome and MAS (malignant antipsychotic syndrome) which probability increases at the combined use of antidepressants of the third generation with other serotonergic substances (including triptanes), and also the drugs exerting impact on serotonin metabolism (including MAO inhibitors), neuroleptics and other antagonists of dopamine receptors are described. Signs of a serotoninovy syndrome can become: changes of the mental status (hallucinations, agitation, a coma), vegetative lability (fluctuations of arterial pressure, tachycardia, a hyperthermia), changes of neuromuscular transfer (a lack of coordination of movements, a hyperreflexia) and/or disturbances from digestive tract (diarrhea, nausea, vomiting). Some symptoms of a serotoninovy syndrome, including a hyperthermia, muscle tension, vegetative lability with a possibility of frequent fluctuations of parameters of the vital functions, and changes of the mental status, are similar to the symptomatology developing at ZNS. Observation of development in patients of clinical effects of a serotoninovy syndrome and ZNS for the purpose of providing timely medical care is necessary.

It is necessary to apply sertraline along with other drugs which strengthen serotonergic neurotransmission (for example, фенфлурамин, tryptophane or 5-NT-agonisty) with care as there is a probability of their pharmakodinamichesky interaction.

The patients who are exposed to electroconvulsive therapy have no sufficient experience of simultaneous use of sertraline. There are no data, both about positive takes, and about undesirable effects of similar combinations. Also there is no experience of use of Zoloft for treatment of a convulsive syndrome therefore it is impossible to use drug at unstable epilepsy, and in case of controlled epilepsy careful monitoring of patients (at emergence of spasms means should be cancelled) is necessary.

Upon transition to Zoloft from others of SIOZS, antiobsessivny drugs or antidepressants it is necessary to be careful, especially in case of use before drugs of the prolonged effect, for example, of fluoxetine. Data on the size of a necessary interval which needs to be observed between cancellation of one of drugs SIOZS and the beginning of reception of other similar drug, no.

Continuous monitoring from the beginning of a course till the period of steady remission is necessary at therapy of patients by Zoloft with a depression, in view of the increased risk of a suicide.

There is an insignificant probability of activation of a mania/hypomania at the patients receiving sertraline and at the patients with maniac-depressive psychosis applying other antiobsessivny or antidepressive medicines.

Considering active biotransformation of sertraline in a liver and data of a pharmacokinetic research, it is necessary to apply it at abnormal liver functions with care: it is recommended to reduce doses or to increase an interval between administrations of drug.

By results of researches of use of Zoloft for patients with a renal failure it is revealed that taking into account insignificant renal excretion of sertraline dose adjustment depending on expressiveness of a renal failure is not required.

Pathological hemorrhages / bleedings at purpose of selective serotonin reuptake inhibitors with the drugs having the established ability to change of functions of thrombocytes are possible and also at patients with hemorrhagic pathologies in the anamnesis.

The Tranzitorny hyponatremia develops at patients at advanced age more often, and also at reception of sertraline with diuretics or some other drugs. Similar side reaction is connected with a syndrome of inadequate secretion of ADG. At the same time it is necessary to cancel Zoloft and to appoint the corresponding therapy for correction of level of sodium in blood. Symptoms and signs of a hyponatremia: a headache, memory disturbance, disturbance of concentration of attention, weakness and disturbances of a vestibular mechanism that can lead to falling; in more difficult episodes are possible: faint, spasms, hallucinations, coma, apnoea and lethal outcome.

Therapy by sertraline, usually, is not followed by disturbance of concentration and reduction in the rate of psychomotor reactions, but its use with other substances / drugs can lead to a lack of coordination and attention. Therefore, at Zoloft's reception it is not recommended to manage the special equipment, vehicles or to be engaged in the activity connected with the increased risk.

Medicinal interaction

• Antiarrhytmic drugs IC of a class (флекаинид, пропафенон), tricyclic antidepressants: long reception of sertraline in a dose of 50 mg a day increases their concentration in plasma as CYP2D6 isoenzyme takes part in metabolism;
• Anticoagulants of indirect action (warfarin): insignificant, but statistically reliable increase in a prothrombin time is noted, in these cases it is necessary to control a prothrombin time in an initiation of treatment sertraline and after its cancellation;
• Antipyrine: at joint reception with sertraline (a day) brings in a dose of 200 mg to insignificant (5%), but to reliable reduction ^{of T1/2} of antipyrine;
• Atenolol: sertraline does not exert impact on its β-adrenoceptor blocking action;
• Digoxin and glibenclamide: medicinal interaction with sertraline (in a dose of 200 mg a day) is not revealed;
• Selective inhibitors of the return neyronalny serotonin reuptake (including lithium drugs): the increased care at combined use with sertraline is required (the pharmacokinetics of lithium does not change, but at patients the tremor is more often observed);
• IMAO, including with reversible type of action (линезолид, моклобемид) and selectively acting (селегилин): heavy complications (development of a serotoninovy syndrome with rigidity, a myoclonus, a hyperthermia, lability of the autonomic nervous system (bystry fluctuations of parameters of cardiovascular and respiratory activity)), changes of the mental status are possible (including the expressed excitement, an acrimony, confusion of consciousness which in some episodes can pass into a delirium or a coma). Similar complications, sometimes from the death, arise at purpose of IMAO against the background of treatment by the antidepressants oppressing neyronalny capture of monoamines or right after their cancellation;
• Medicinal substances, metaboliziruyemy isoenzymes of CYP3A3/4, CYP2C9, CYP2C19, CYP1A2: sertraline minimum oppresses or practically does not influence these isoenzymes;
• Pimozidum: increase in its level at single appointment in a low dose (2 mg) is possible. As the mechanism of this interaction is not defined, and Pimozidum differs in a target therapeutic index, the concomitant use of Pimozidum with sertraline is contraindicated;
• The drugs contacting blood proteins (diazepam, Tolbutamidum): sertraline influences their concentration in a blood plasma, reducing clearance (it is required to control the content of glucose in blood);
• Sumatriptan: in extremely rare episodes weakness, increase in tendon jerks, confusion of consciousness, alarm and excitement is noted; in case of simultaneous use with sertraline observation of patients is recommended;
• Tryptophane, фенфлурамин: it is necessary to avoid simultaneous use with sertraline;
• Phenytoinum: sertraline (in a dose of 200 mg a day) does not suppress metabolism, does not make clinically significant impact on Phenytoinum, but, despite it, from the beginning of their simultaneous use it is required to control carefully in a blood plasma the maintenance of Phenytoinum for the purpose of the subsequent dose adjustment;
• Cimetidinum: significantly reduces clearance of sertraline;
• The ethanol and substances/drugs oppressing the central nervous system: potentiation of effect of carbamazepine, Phenytoinum, a haloperidol or ethanol on psychomotor and cognitive functions at healthy people is noted, but combined use of Zoloft and alcohol is not recommended.

Terms and storage conditions

To store in the place, unavailable to children, at a temperature not above 30 °C.

Period of validity – 5 years.