Pharmacological properties of the drug Serlift
Sertraline is a potent selective serotonin reuptake inhibitor. Almost no effect on the reuptake of norepinephrine and dopamine. Sertraline has no affinity for cholinergic, dopamine, histamine, benzodiazepine and adrenergic receptors. Sertraline does not have a sedative, stimulant or anticholinergic effect, and does not enhance catecholaminergic stimulation. The use of sertraline does not lead to weight gain. Sertraline does not cause physical or mental dependence. Sertraline is slowly absorbed from the gastrointestinal tract. Food intake does not have a significant effect on the bioavailability of the drug. Sertraline undergoes extensive metabolism during its first passage through the liver. The main metabolite, N-desmethylsertraline, has virtually no antidepressant effect. The maximum concentration in blood plasma is achieved 4.5–8.4 hours after taking the drug. Equilibrium concentration is achieved after 1 week of therapy (when taken once a day). The degree of binding to plasma proteins is 98%. The half-life of sertraline is 22–36 hours, N-desmethylsertraline is 62–104 hours. Sertraline and N-desmethylsertraline are actively biotransformed, and the resulting metabolites are excreted in feces and urine in equal quantities. The pharmacokinetics of the drug in elderly and young patients does not differ significantly. With simultaneous ingestion of food and sertraline, the time to reach maximum concentration in the blood serum is reduced, and the maximum concentration increases by 25%.
pharmachologic effect
Antidepressant, a powerful specific inhibitor of serotonin (5-HT) reuptake in neurons.
It has a very weak effect on the reuptake of norepinephrine and dopamine. In therapeutic doses, it blocks the uptake of serotonin in human platelets. Does not have a stimulating, sedative or anticholinergic effect. Due to the selective inhibition of 5-HT uptake, sertraline does not enhance adrenergic activity. Sertraline has no affinity for muscarinic cholinergic receptors, serotonin, dopamine, histamine, GABA, benzodiazepine and adrenergic receptors. Sertraline does not cause drug dependence and does not cause weight gain with long-term use.
Use of the drug Serlift
For adults with depression and obsessive-compulsive disorder, the drug is usually prescribed at a dose of 50 mg once a day at any time, regardless of meals. For patients with panic disorder, post-traumatic stress disorder, and social anxiety, treatment is recommended to begin with a dose of 25 mg. After a week, the dose can be increased to 50 mg. If the therapeutic effect is insufficient, the dose of sertraline can be increased by 50 mg every week until a maximum daily dose of 200 mg is reached. At the same time, the drug is well tolerated. A satisfactory therapeutic result is usually achieved within 7 days from the start of treatment, however, regular use of the drug is necessary to achieve the full therapeutic effect. Patients with obsessive-compulsive disorder may require 8–12 weeks to achieve good results. For premenstrual dysphoric disorder, treatment with Sirlift should begin with a dose of 50 mg/day, which is taken daily throughout the entire menstrual cycle or limited to the luteal phase. For patients in whom the use of the drug at a dose of 50 mg is not effective enough, the dose can be increased to 150 mg / day (50 mg every week) if the drug is taken daily throughout the menstrual cycle, or to 100 mg / day if the drug is limited. only in the luteal phase. Maintenance therapy is subsequently carried out at the minimum effective dose. In children aged 6–12 years with obsessive-compulsive disorder, treatment with sertraline begins with a dose of 25 mg 1 time per day, in adolescents aged 13–17 years - with a dose of 50 mg 1 time per day. The maximum daily dose is 200 mg, which should be increased at intervals of more than 1 week.
Side effects of the drug Serlift
They usually occur rarely and disappear quickly after discontinuation of the drug. Cardiovascular system : changes in blood pressure, tachycardia. CNS : amnesia, headache, insomnia, drowsiness, movement disorders, paresthesia, hypoesthesia, symptoms of depression, hallucinations, aggressive reaction, agitation, anxiety, psychosis, depersonalization, increased excitability, panic reaction, as well as signs and symptoms that are associated with serotonin syndrome, which includes fever, rigidity, confusion, agitation, and hyperhidrosis. Gastrointestinal tract : nausea, diarrhea, vomiting, anorexia, dyspepsia, abdominal pain. Allergic reactions : rash (including isolated reports of erythema multiforme and photosensitivity), angioedema, ecchymosis, pruritus and anaphylactoid reactions. Musculoskeletal system : arthralgia, myalgia. Other : blurred vision, hyponatremia, urinary retention, general malaise, dry mouth, sexual dysfunction (mainly delayed ejaculation in men).
Side effects
From the digestive system:
dyspeptic symptoms (flatulence, nausea, vomiting, diarrhea, constipation), abdominal pain, pancreatitis, dry mouth, hepatitis, jaundice, liver failure, decreased appetite (rarely increased), even anorexia; rarely, with long-term use - an asymptomatic increase in transaminase activity in the blood serum occurs. Discontinuation of the drug in this case leads to normalization of enzyme activity.
From the cardiovascular system:
palpitations, tachycardia, arterial hypertension.
From the musculoskeletal system:
arthralgia, muscle cramps.
From the central nervous system and peripheral nervous system:
extrapyramidal disorders (dyskinesia, akathisia, teeth grinding, gait disturbance), involuntary muscle contractions, paresthesia, fainting, drowsiness, headache, migraine, dizziness, tremor, insomnia, anxiety, agitation, hypomania, mania, hallucinations, euphoria, nightmares, psychosis, decreased libido, suicide, coma.
From the respiratory system:
bronchospasm, yawning.
From the urinary system:
enuresis, incontinence or urinary retention.
From the reproductive system:
sexual dysfunction (delayed ejaculation, decreased potency), galactorrhea, gynecomastia, menstrual irregularities, priapism.
From the senses:
blurred vision, mydriasis, ringing in the ears.
From the endocrine system:
hyperprolactinemia, hypothyroidism, syndrome of inappropriate ADH secretion.
Dermatological reactions:
redness of the skin or flushing of the face, alopecia, photosensitivity reaction, purpura, increased sweating.
Allergic reactions:
urticaria, pruritus, anaphylactoid reaction, angioedema, periorbital edema, facial edema, rarely Stevens-Johnson syndrome and epidermal necrolysis.
From the hematopoietic system:
possible development of leukopenia and thrombocytopenia.
Other:
weight loss or gain, peripheral edema, increased serum cholesterol levels, weakness, bleeding (including nasal, gastrointestinal or hematuria). Rare cases of withdrawal syndrome have been described when stopping treatment with sertraline. Paresthesia, hypoesthesia, symptoms of depression, hallucinations, aggressive reactions, psychomotor agitation, anxiety, or symptoms of psychosis may appear that cannot be distinguished from the symptoms of the underlying disease.
Special instructions for the use of the drug Serlift
Sudden discontinuation of sertraline should be avoided. It is recommended to gradually reduce the dose, avoiding sudden discontinuation of the drug. If severe symptoms develop after a dose reduction or discontinuation, the previous dose may be resumed. Then the dose reduction can be continued, but more gradually. Due to the fact that the drug is intensively metabolized in the liver, caution must be exercised when prescribing Sirlift to patients with impaired liver function (a reduction in the daily dose or an increase in the interval between doses of the drug is indicated). Renal elimination of the drug is negligible, so there is no need to adjust the dose in patients with renal failure. Careful monitoring of patients with convulsive syndrome is necessary when prescribing Sirlift. Its use should be avoided in patients with unstable epilepsy. Careful monitoring of patients with a tendency to suicide attempts is necessary at the beginning of treatment until the full clinical effect of the drug is manifested. Some patients who took sertraline experienced a slight decrease in body weight. Cases of bleeding from the upper gastrointestinal tract have been described in patients who took psychotropic drugs that affect the reuptake of serotonin. Sertraline is associated with an average reduction in serum uric acid levels of approximately 7%. Such a minor uricosuric effect has no clinical significance. There are no results from the controlled use of sertraline in pregnant women, so the drug can be prescribed during pregnancy only if the expected therapeutic effect for the mother outweighs the potential risk to the fetus. It is unknown whether sertraline and its metabolites are excreted into breast milk, therefore it is not recommended to prescribe the drug during breastfeeding. When using the drug, you should refrain from driving vehicles and working with potentially dangerous mechanisms.
Interactions of the drug Serlift
Cases of severe reactions, sometimes fatal, have been described in patients who took sertraline in combination with an MAO inhibitor. Sirlift should not be prescribed within 14 days after stopping treatment with a MAO inhibitor. MAO inhibitors are also prescribed no earlier than 14 days after stopping sertraline. When taking sertraline and warfarin simultaneously, a slight increase in prothrombin time is possible. It is necessary to monitor these indicators at the beginning of treatment with sertraline and after its discontinuation. Patients should be informed of the possible risk of bleeding associated with the simultaneous use of Sirlift and NSAIDs. Concomitant use of sertraline with diazepam or tolbutamide may lead to changes in the serum levels of these drugs. Caution must be exercised when using Sirlift and other drugs acting on the central nervous system simultaneously. With simultaneous use of sertraline with cimetidine, the maximum plasma concentration and half-life of sertraline increase. It is recommended to monitor the level of lithium in the blood plasma after starting treatment with sertraline with dose adjustment of lithium preparations. When using sertraline and methadone simultaneously, it is necessary to monitor the level of methadone in the blood plasma. Sertraline and most tricyclic antidepressants inhibit the activity of the cytochrome P450 2D6 isoenzyme and thus may increase the plasma concentrations of drugs that are metabolized by this isoenzyme. With the simultaneous use of sertraline and sumatriptan, weakness, hyperreflexia, and loss of coordination may occur. If concomitant treatment with sumatriptan and sertraline is clinically justified, patient monitoring is recommended.
Overdose of the drug Serlift, symptoms and treatment
Symptoms: drowsiness, nausea, vomiting, tachycardia, dizziness, agitation, tremor, bradycardia, coma, convulsions, delirium, hallucinations, hypertension (arterial hypertension) or hypotension, manic reaction, pancreatitis, prolongation of the QT interval on the ECG, serotonin syndrome, stupor. Treatment: there is no specific antidote; To reduce absorption, gastric lavage and the administration of activated charcoal are indicated. It is necessary to ensure airway patency, adequate ventilation and oxygenation, monitor the function of vital organs, and provide symptomatic and supportive therapy.
Overdose
Symptoms:
no severe symptoms were detected in case of an overdose of sertraline even when using the drug in high doses. However, when administered simultaneously with other drugs or alcohol, severe poisoning can occur, including coma and death.
In case of overdose, manifestations of serotonin syndrome are possible (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, and therefore increased diuresis, dialysis, hemoperfusion or blood transfusion may be ineffective.
