Serlift
Monoamine oxidase inhibitors (MAOIs).
Severe complications have been observed with the simultaneous use of sertraline and MAOIs, including selectively acting (selegiline) MAOIs and those with a reversible type of action (moclobemide). The development of serotonin syndrome is possible (see section “Overdose”).
Medicines that depress the central nervous system and ethanol.
The combined use of sertraline and substances that depress the central nervous system requires monitoring. Not compatible with ethanol.
Coumarin derivatives:
when they are co-administered with sertraline, a significant increase in prothrombin time is observed - in these cases it is recommended to monitor the prothrombin time at the beginning of treatment with Sirlift and after its discontinuation.
Cimetidine.
When used simultaneously, it significantly reduces the clearance of sertraline.
Drugs metabolized by cytochrome P450 isoenzyme 2D6.
Although sertraline has only the potential to cause clinically significant suppression of the 2D6 isoenzyme of cytochrome P450, however, when used together with drugs metabolized by this isoenzyme (desipramine, tricyclic antidepressants, class I antiarrhythmic drugs - propafenone and flecanaid), lower doses of sertraline are used, and when Increased doses of these drugs may be required when discontinuing sertraline.
Drugs metabolized by other cytochrome P450 enzyme systems.
Experiments to study the interaction
in vitro
showed that the beta-hydroxylation of endogenous cortisol carried out by the isoenzyme CYP 3A3/4, as well as the metabolism of carbamazepine and terfenadine, do not change with long-term administration of sertraline at a dose of 200 mg per day. Plasma concentrations of phenytoin and warfarin also do not change with long-term administration of sertraline at the same dose. Thus, we can conclude that sertraline does not inhibit CYP2C9.
Sertraline does not affect the concentration of diazepam in the blood serum, which indicates the absence of inhibition of the CHZ 2C19 isoenzyme. Based on in vitro
Sertraline has virtually no effect or minimal inhibition of the CYP1A2 isoenzyme.
Sumatriptan.
If combined with sertraline, patients experienced weakness, hyperreflexia, and impaired coordination of movements, therefore, if such a combination is necessary, patients should be monitored.
Tolbutamide:
sertraline reduces the clearance of tolbutamide (monitoring of blood glucose is necessary during simultaneous use)
Lithium.
The pharmacokinetics of lithium do not change with concomitant treatment with sertraline. However, tremor is more often observed when they are used together.
Drugs affecting serotonergic transmission
. When replacing one serotonin reuptake inhibitor with another, there is no need for a washout period. However, caution is required when doing this. Incompatible with tryptophan and phenifluramine.
Induction of microsomal liver enzymes.
Sertraline causes minimal induction of liver enzymes. The simultaneous administration of sertraline and antipyrine at a dose of 200 mg leads to a significant decrease in the half-life of antipyrine, although this occurs in only 5% of cases.
Atenolol.
When administered together, sertraline does not change the 13-adrenergic blocking effect of atenolol.
Glibenclamide and digoxin.
When sertraline was administered in a daily dose of 200 mg, no drug interactions with these drugs were detected.
Nonsteroidal anti-inflammatory drugs, acetylsalicylic acid:
When used together, the risk of bleeding increases.
Sirlift tablets ppo 50mg No. 28
Compound
Active substance: sertraline - 50 mg.
Excipients: calcium hydrogen phosphate - 16.00, microcrystalline cellulose (Avicel PH 101) - 51.54, microcrystalline cellulose (Avicel PH 102) - 15.00, hyprollose-L - 4.00, sodium carboxymethyl starch - 6.00, purified water - qs (consumed during the production process), magnesium stearate-1.50.
Pharmacokinetics
When sertraline is taken orally in doses of 50-200 mg 1 time / day for 14 days, Cmax in blood plasma is achieved in 4.5-8.4 hours. The average T1/2 in young and elderly men and women is 22-36 hours. According to the half-life, observed approximately twofold cumulation of the active substance until an equilibrium state is achieved after 1 week of treatment. Plasma protein binding is about 98%, Vd is 20 l/kg. Intensively metabolized during the first passage through the liver. The main metabolite found in plasma, N-desmethylsertraline, has weak pharmacological activity.
T1/2 of N-desmethylsertraline varies between 62-104 hours. It is excreted mainly through the intestines and urine in equal amounts in the form of metabolites, less than 0.2% is excreted unchanged in the urine.
Indications for use
- Depressive states of various etiologies, including those accompanied by feelings of anxiety (treatment and prevention).
- Panic disorders with and without agoraphobia.
- Obsessive-compulsive disorder (OCD).
- Post-traumatic stress disorder (PTSD).
Contraindications
- Hypersensitivity to the active substance or other ingredients included in the drug.
- Combined use of sertraline and MAO inhibitors.
- Combined use of sertraline with tryptophan or phenylfluramine.
- Combined use with pimozide.
- Epilepsy during an exacerbation.
- Children's age up to 6 years.
- Pregnancy and lactation period.
With caution:
Organic diseases of the brain (including mental retardation), manic states, epilepsy (with a history and without exacerbation), liver and/or renal failure, weight loss, in children over 6 years of age.
Directions for use and doses
Depression and OCD:
Adults
Inside. 50 mg 1 time per day in the morning or evening, regardless of meals. If there is no effect, a gradual (over several weeks) dose increase to 200 mg/day (by 50 mg per week) is possible. Some clinicians recommend an initial dose of 25 mg/day for 1-2 days.
In patients with OCD, 8-12 weeks of therapy may be required to achieve good results.
Panic disorders and PTSD: initial dose - 25 mg / day in the morning or evening, followed by an increase over 1 week to 50 mg / day, and then gradually by 50 mg per week the dose can be increased to 200 mg / day. The therapeutic effect is usually achieved within 7 days from the start of treatment. However, to achieve the full therapeutic effect, regular use of the drug is required for 2-4 weeks.
When conducting long-term maintenance therapy, the minimum effective dose is prescribed, which is subsequently changed depending on the effect.
In elderly patients there is no need for special dose selection.
Patients with impaired liver function require special attention when treated with Sirlift. In case of severe liver dysfunction, the dose of the drug should be reduced or the intervals between doses should be increased. In patients with impaired renal function, a special dose adjustment is not required.
Children with OCD
For children 6 to 12 years of age, the starting dose is 25 mg sertraline once daily, morning or evening. After a week, the dose can be increased to 50 mg once a day.
In adolescents 13-17 years old, the initial dose is 50 mg/day in the morning or evening once. The daily dose can be gradually increased by 50 mg per week to a maximum dose of 200 mg/day. The lower body weight of children compared to adults should be taken into account, and when prescribing a dose of more than 50 mg/day, children should be carefully monitored in order to discontinue the drug at the first sign of overdose.
To achieve a good result, 8-12 weeks of therapy may be required.
Storage conditions
Store out of the reach of children at a temperature not exceeding 25°C.
Best before date
3 years. Do not use after the expiration date stated on the packaging.
special instructions
Sirlift should not be prescribed in conjunction with an MAOI, or within 14 days after stopping treatment with an MAOI. Similarly, after discontinuation of Sirlift, no MAOIs are prescribed for 14 days.
There is no sufficient experience with the use of sertraline in patients undergoing electroconvulsive therapy.
It is necessary to strictly monitor the behavior of patients in a state of depression (risk of suicide attempts) until significant improvement occurs as a result of treatment.
Description
Antidepressant.
Dosage form
White or almost white oval-shaped film-coated tablets with the inscription “50” engraved on one side and scored on the other.
Use in children
Safety for use in pediatrics has not been established.
Pharmacodynamics
Antidepressant, naphthylamine derivative. Selective blocker of neuronal reuptake of serotonin in the brain. The neuronal uptake of norepinephrine and dopamine is practically unaffected. It does not have a specific affinity for adrenergic and m-cholinergic receptors, GABA receptors, dopamine, histamine, serotonin or benzodiazepine receptors. Does not inhibit MAO. Causes anorexia, effective in obsessive states.
Side effects
From the side of the central nervous system: dizziness, drowsiness, headache, insomnia, feeling of fatigue, weakness, tremor; rarely - manic or hypomanic state, anxiety, restlessness, visual impairment.
From the cardiovascular system: rarely - redness of the skin with a feeling of heat or warmth, a feeling of heartbeat.
From the digestive system: loss of appetite, diarrhea, dry mouth, nausea, cramps in the stomach or intestines, flatulence; rarely - constipation, vomiting.
Metabolism: increased sweating.
From the reproductive system: rarely - decreased potency.
Allergic reactions: rarely - fever, skin rash, hives or itching.
Use during pregnancy and breastfeeding
Controlled trials of sertraline in pregnant women have not been conducted; therefore, during pregnancy, the drug can be prescribed only if the expected benefit to the mother outweighs the possible risk to the fetus.
Women of childbearing potential receiving treatment with Sirlift should use adequate methods of contraception. Sertraline is found in breast milk, so the use of Surlift in nursing women is not recommended. If treatment is necessary, it is better to stop breastfeeding
Interaction
When used simultaneously with anticoagulants, coumarin derivatives significantly increase the prothrombin time.
With simultaneous use, sertraline can displace other drugs from binding to plasma proteins, as a result of which the plasma concentration of the corresponding active substance increases and the risk of side effects increases.
When used simultaneously with drugs whose metabolism occurs with the participation of the CYP2D6 isoenzyme, it is possible to increase the plasma concentration of these drugs due to inhibition of the CYP2D6 isoenzyme under the influence of sertraline.
With the simultaneous use of MAO inhibitors (including selegiline, moclobemide), the development of serotonin syndrome (hyperthermia, muscle rigidity, myoclonus, as well as manifestations of instability of the mental and physiological state of the body, up to the development of delirium and coma) is possible.
When used simultaneously with lithium salts, tremor may increase. When used simultaneously with desipramine, it is possible to increase the concentration of desipramine in the blood plasma; with cimetidine - a significant decrease in the clearance of sertraline.
Overdose
Severe symptoms from an overdose of sertraline have not been identified, even when the drug is prescribed in large doses. However, when used simultaneously with other drugs or ethanol, severe poisoning may occur.
Overdose can cause serotonin syndrome.
The initial manifestations of serotonin syndrome are observed from the nervous system (extrapyramidal symptoms - tremor, disorientation, restlessness, muscle hypertonicity; hyperreflexia; myoclonic twitching first in the feet, then spreading throughout the body; ataxia; impaired coordination tests) and from the gastrointestinal tract ( abdominal cramps, flatulence, diarrhea, nausea, vomiting, dyspepsia).
As the condition worsens, a manic-like state develops.
The final stage resembles neuroleptic malignant syndrome: fever, profuse sweat, mask-like face, greasy face.
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 volume of distribution, and therefore increased diuresis, dialysis, hemoperfusion or blood transfusion may not be effective.
Release form
Film-coated tablets, 50 mg No. 28.
Impact on the ability to drive vehicles and operate machinery
During the treatment period, activities that require increased attention and high speed of psychomotor reactions should be avoided.
