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Active ingredients
Sertraline
Release form
Pills
Pharmacological effect
Absorption; Absorption is high, but at a slow rate. When taking the drug simultaneously with food, bioavailability increases by 25%, Cmax increases by 25% and Tmax decreases.; In humans, when taking sertraline at a dose of 50 to 200 mg 1 time / day for 14 days, Cmax was reached 4.5-8.4 hours after reception. Cmax and AUC are proportional to the dose within 50-200 mg of sertraline 1 time / day for 14 days, thus revealing the linear nature of the pharmacokinetic dependence.; Distribution; Binding to plasma proteins is about 98%; Accordingly, the final T1 / 2 is approximately double cumulation of the drug before the onset of equilibrium concentrations after 1 week of treatment (receiving the dose 1 time / day); Metabolism; Sertralin undergoes active biotransformation during the "first pass" through the liver. The main metabolite found in plasma, N-desmethyl sertraline, is significantly inferior (approximately 20 times) to sertraline in in vitro activity and is actually not active in in vivo depression models.; Sertralin and N-desmethyl sertraline are biotransformed actively.; Excretion; Medium T1 / 2 sertraline in young and old men and women is 22-36 hours. T1 / 2 N-desmethyl sertraline varies from 62-104 hours. Metabolites are excreted in feces and urine in equal amounts. Only a small part of the drug (less than 0.2%) is excreted in the urine unchanged.; Pharmacokinetics in special clinical situations; The pharmacokinetic profile in adolescents and elderly patients is not significantly different from that in patients aged 18 to 65 years. It was shown The pharmacokinetics of sertraline in children with OCD is similar to that in adults (although sertraline is slightly more active in children). However, given the lower body weight in children (especially at the age of 6-12 years), it is recommended to use the drug in a lower dose in order to avoid excessive plasma levels. T1 / 2 of the drug and AUC are increased in patients with liver cirrhosis compared with those in healthy people.
Pharmacokinetics
Ingredients; 1 tablet contains sertraline (in the form of; hydrochloride) 50 mg; excipients: calcium, phosphate, cellulose, microcrystalline,, hydroxypropylcellulose, sodium starch, glycolate, magnesium stearate,; hydroxypropylmethylcellulose,; polyethylene glycol, polysorbate, titanium, dioxide (E171).
Indications
Antidepressant, a powerful specific serotonin reuptake inhibitor (5-HT) in neurons.It has a very weak effect on the reuptake of norepinephrine and dopamine. At therapeutic doses, it blocks serotonin uptake in human platelets. It has no stimulating, sedative or anticholinergic effects. Due to the selective inhibition of the capture of 5-HT, sertraline does not enhance adrenergic activity. Sertralin has no affinity for muscarinic cholinergic receptors, serotonin, dopamine, histamine, GABA-, benzodiazepine and adrenergic receptors. Sertralin does not cause drug dependence, does not cause an increase in body weight during long-term use.
Contraindications
Zoloft appoint 1 time / day. in the morning or evening. Tablets can be taken regardless of the meal.; For depression and OCD, treatment begins with a dose of 50 mg / day. Treatment of panic disorders, PTSD and; social phobias start with a dose of 25 mg / day, which is increased after 1 week to 50 mg / day; The use of the drug according to this scheme reduces the incidence of early adverse effects, treatment characteristic of panic disorder. With insufficient effect of sertraline, in patients at a dose of 50 mg / day. daily dose can be increased. The dose should be increased at intervals not more often than once a week to the maximum recommended dose of 200 mg / day. The initial effect can be observed 7 days after the start of treatment, but the full effect is usually achieved in 2-4 weeks (or even for a longer time with OCD). When conducting; long-term maintenance therapy, the drug is prescribed in the minimum effective dose, which is then modified according to the clinical effect. In children and adolescents aged 13-17; years old with OCD, treatment with Zoloft should be started with a dose of 50 mg / day. In children aged 6-12 years, OCD therapy begins with a dose of 25 mg / day, after 1 week it is increased to 50 mg / day. In; subsequent with insufficient effect, the dose can be increased in steps of 50 mg / day. up to 200 mg / day; as needed. To avoid overdose, increasing the dose to more than 50 mg is necessary; take into account the lower body weight in children compared with adults. Change the dose should be with; an interval of at least 1 week. In elderly patients, the drug is used in the same doses as in younger patients.
Use during pregnancy and lactation
Sertralin should not be prescribed in conjunction with MAO inhibitors, as well as within 14 days after stopping treatment with MAO inhibitors. Similarly, after the cancellation of sertraline, no MAO inhibitors are prescribed for 14 days.; Serotonin syndrome and neuroleptic malignant syndrome; With the use of selective serotonin reuptake inhibitors (SSRIs), the development of serotonin syndrome and malignant neuroleptic syndrome (SNS) with other serotonergic drugs (including triptans), as well as drugs that affect the metabolism of serotonin (including MAO inhibitors), antipsychotic cf food and other dopamine receptor antagonists. Manifestations of serotonin syndrome can be changes in mental status (in particular, agitation, hallucinations, coma), autonomic lability (tachycardia, fluctuations in blood pressure, hyperthermia), changes in neuro-muscular transmission (hyperreflexia, impaired coordination of movements) and / or impaired gastrointestinal nausea, vomiting and diarrhea). Some manifestations of serotonin syndrome, including hyperthermia, muscle stiffness, vegetative lability with the possibility of rapid fluctuations in the parameters of vital functions, as well as changes in mental status, may resemble symptoms that develop in MPS. Patients should be monitored for the development of the clinical manifestations of serotonin syndrome and NNS.; Other serotonergic drugs; Care should be taken when administering sertraline with other drugs that increase serotonergic neurotransmission, such as tryptophan, fenfluramine or 5-HT-agonists. Such a joint appointment, if possible, should be excluded, given the likelihood of pharmacodynamic interaction.; The transition from other SSRIs, antidepressants or antiobsessive drugs; Experience in clinical studies, the purpose of which was to determine the optimal time required to transfer patients from taking other antidepressive and antiobsessive drugs to sertraline, limited Care must be taken in such a transition, especially with long-acting drugs, such as fluoxetine.The required interval between the cancellation of one SSRI and the start of taking another similar drug has not been established. It should be noted that in patients undergoing electroconvulsive therapy, there is no adequate experience with sertraline. The possible success or risk of such combined treatment has not been studied. There is no experience with sertraline in patients with convulsive syndrome, so its use should be avoided in patients with unstable epilepsy, and patients with controlled epilepsy should be carefully monitored during treatment. If seizures occur, the drug should be discontinued.; Depressed patients are at risk for suicidal attempts. This danger persists until the development of remission. Therefore, from the start of treatment and until the optimum clinical effect is reached, patients should be constantly monitored.; Activation of mania / hypomania; During clinical studies to market sertraline, hypomania and mania were observed in about 0.4% of patients receiving sertraline. Cases of activation of mania / hypomania are also described in a small proportion of patients with manic-depressive psychosis who received other anti-depressive or anti-obsessive drugs; use for deficient liver function; Sertralin is actively biotransformed in the liver. According to a pharmacokinetic study, with repeated administration of sertraline in patients with stable cirrhosis of the mild liver, an increase in the T1 / 2 of the drug and an almost threefold increase in the AUC and Cmax of the drug were observed compared with those in healthy people. There were no significant differences in plasma binding in the two groups. Sertraline should be used with caution in patients with liver disease. When prescribing a drug to a patient with impaired liver function, it is necessary to discuss the feasibility of reducing the dose or increasing the interval between taking the drug.; Use in case of kidney failure; Sertralin undergoes active biotransformation, therefore, in an unchanged form with urine, it is eliminated in small quantities. In patients with mild and moderate renal insufficiency (CC 30-60 ml / min) and patients with moderate or severe renal insufficiency (CC 10-29 ml / min) serroralin pharmacokinetic parameters (AUC0-24 and Cmax) with its repeated use did not significantly differ from the control group. In all groups T1 / 2 of the drug was the same, as well as there were no differences in binding to plasma proteins.The results of this study suggest that, as expected, given the negligible renal excretion of sertraline, its dose adjustment depending on the severity of renal insufficiency is not required; with drugs that have an established ability to change platelet functions, as well as in patients with a history of hemorrhagic diseases.; Gipon atriemia; transient hyponatremia may occur during sertraline treatment. This most often develops in elderly patients, as well as when taking diuretics or a number of other drugs. This side effect is associated with the syndrome of inadequate secretion of ADH. With the development of symptomatic hyponatremia, sertraline should be discontinued and appropriate therapy should be prescribed to correct the sodium level in the blood. Signs and symptoms of hyponatremia include headache, impaired concentration, memory impairment, weakness and instability, which can lead to falls. In more severe cases, hallucinations, fainting, convulsions, coma, respiratory arrest and death may occur. Influence on the ability to drive vehicles and control mechanisms; Appointment, sertralina, 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 increased risk.
Dosage and administration
Depression of various etiologies (treatment and prevention); obsessive compulsive disorder (OCD); panic disorder; post-traumatic stress disorder (PTSD); social phobia.
Side effects
Pimozide; With the simultaneous use of sertraline and pimozide, there was an increase in the levels of pimozide when it was administered once at a low dose (2 mg). An increase in pimozide levels was not associated with any changes in the ECG.Since the mechanism of this interaction is not known, and pimozide has a narrow therapeutic index, simultaneous administration of pimozide and sertraline is contraindicated.; MAO inhibitors; Severe complications are noted with simultaneous use of sertraline and MAO inhibitors (including selectively acting MAO inhibitors and reversible type of (moclobemide, as well as linezolid). The development of serotonin syndrome (hyperthermia, rigidity, myoclonus, lability of the autonomic nervous system is possible (rapid fluctuations in ditch of the respiratory and cardiovascular systems), changes in mental status, including irritability, marked excitement, confusion, which in some cases can turn into a delirious state or coma.) Similar complications, sometimes fatal, occur when MAO inhibitors are prescribed for background treatment with antidepressants that inhibit the neuronal seizure of monoamines or immediately after their cancellation.; Medications that depress the central nervous system, and ethanol; Combined use of sertraline and substance CNS depressants, requires close attention. The use of alcoholic beverages and preparations containing ethanol during treatment with sertraline is prohibited. No potentiation of the effect of ethanol, carbamazepine, haloperidol, or phenytoin on cognitive and psychomotor function in healthy people; however, the combined use of sertraline and alcohol is not recommended.; Indirect anticoagulants (warfarin); When co-administered with sertraline, there is a slight but statistically significant increase in prothrombin time. In these cases, it is recommended to control the prothrombin time at the beginning of treatment with sertraline and after its cancellation.
Overdose
On the part of the digestive system: dyspeptic symptoms (flatulence, nausea, vomiting, diarrhea, constipation), abdominal pain, pancreatitis, dry mouth, hepatitis, jaundice, liver failure, loss of appetite (rarely - increased), up to anorexia; rarely, with long-term use, an asymptomatic increase in serum transaminase activity occurs. The abolition of the drug in this case leads to the normalization of the activity of enzymes. From the side of the cardiovascular system: a sensation of heartbeat,tachycardia, arterial hypertension. From the musculoskeletal system: arthralgia, muscle cramps. From the central nervous system and peripheral nervous system: extrapyramidal disorders (dyskinesias, akathisia, teeth grinding, gait disturbance), involuntary muscle contractions, paresthesias, fainting, sleepiness , headache, migraine, dizziness, tremor, insomnia, anxiety, agitation, hypomania, mania, hallucinations, euphoria, nightmares, psychosis, decreased libido, suicide, coma.; From the respiratory system: bronchospasm, yawning; With stor here urinary system: enuresis, incontinence or urinary retention. From the reproductive system: impaired sexual function (delayed ejaculation, reduced potency), galactorrhea, gynecomastia, menstrual disorders, priapism.; From the sense organs: visual impairment, mydriasis, ringing in the ears. On the part of the endocrine system: hyperprolactinemia, hypothyroidism, syndrome of inadequate secretion of ADH.; Dermatological reactions: reddening of the skin or "flushing" of the blood to the face, alopecia, photosensitization reaction, purpura, increased sweating ; Allergic reactions: urticaria, pruritus, anaphylactoid reaction, angioedema, periorbital edema, swelling of the face, occasionally Stevens-Johnson syndrome and epidermal necrolysis. From the hematopoietic system: leukopenia and thrombocytopenia may develop; body, peripheral edema, increased serum cholesterol, weakness, bleeding (including nasal, gastrointestinal or hematuria). When discontinuing treatment with sertraline, rare cases of withdrawal syndrome are described. Paresthesias, hypoesthesia, symptoms of depression, hallucinations, aggressive reactions, agitation, anxiety, or symptoms of psychosis, which cannot be distinguished from the symptoms of the underlying disease, may appear.
Interaction with other drugs
The drug should be used with caution in organic brain diseases (including mental retardation), epilepsy, liver and / or kidney failure, marked weight loss.
special instructions
Symptoms: severe symptoms of sertraline overdose have not been identified even with the use of the drug in high doses.However, in simultaneous administration with other drugs or alcohol may occur severe poisoning up to coma and death;. In overdose possible existence of serotonin syndrome (nausea, vomiting, drowsiness, tachycardia, agitation, dizziness, agitation, diarrhea, excessive sweating, myoclonus and hyperreflexia); Treatment: no specific antidotes. Requires intensive supportive care and constant monitoring of vital body functions. Vomiting is not recommended. The introduction of activated carbon may be more effective than gastric lavage. It is necessary to maintain airway patency. In sertraline large Vd, in this regard, increased diuresis, dialysis, hemoperfusion or blood transfusion may be unsuccessful.