Sertraline-apo

Sertralin-apo is an antidepressant, which is included in the group of drugs SSRIs.

The sertraline component is a potent, highly selective substance that slows down the process of serotonin reuptake within the body.

The drug has a very low impact on the processes of dopamine and norepinephrine reuptake. When using Sertralina-apo in medicamentous portions, serotonin uptake is blocked by human platelets.

[1]

Indications Serralina-apo

It is used for such painful conditions:

• depression, as well as the kind of depression in which there is a feeling of anxiety (a history of mania may be present (or not));
• panic disorders (against which may be noted (or not) agoraphobia);
• OCD or PTSD;
• social phobia.

Release form

The release of the medication is realized in capsules - 28 pieces inside a can of polyethylene.

[2]

Pharmacodynamics

Like many other antidepressants with clinical influence, sertraline weakens the activity of serotonin and noradrenaline endings inside the brain. At the same time, the component does not have significant affinity with respect to adrenergic (α-1 and α-2, as well as β), GABA, cholinergic with histaminergic, dopaminergic, serotonergic (such as 5-HT1A with 5-HT1B and 5-HT2) or benzodiazepine endings.

The drug has no sedative properties and does not affect the psychomotor activity.

[3]

Pharmacokinetics

The pharmacokinetic characteristics of sertraline are linear with a pharmaceutical range of 50–200 mg per day.

After repeated use of drugs in a dose of 0.2 g 1-time per day, the Cmax values of sertraline inside the blood plasma are on average 0.19 µg / ml; it takes 6-8 hours to get this figure. The AUC level is 2.8 mg · h / l, and the term half-life at the terminal stage is about 26 hours. The Cmax level of the metabolic element N-desmethyl sertraline is 0.14 µg / ml, the half-life term is 65 hours, and the AUC values are 2.3 mg · h / l.

Foods increase sertraline bioavailability by approximately 40%. The substance undergoes extensive metabolic processes with the formation of N-desmethyl sertraline, which has almost no therapeutic activity. Both sertraline and the element N-desmethyl sertraline participate in the processes of oxidative deamination with further hydroxylation, reduction, and besides this, glucuronic conjugation. A large number of metabolic elements are excreted in the bile.

98% synthesized with blood intraplasma protein.

Indicators of N-desmethyl sertraline in the elderly in the case of multiple use of drugs three times higher, although the clinical significance of this factor is not defined.

[4], [5]

Dosing and administration

Sertralin-Apo should be taken in conjunction with food, one time a day, it is recommended in the evening (or with breakfast, if it is needed in the morning).

The initial stage of treatment.

People with OCD or depression should first use 50 mg of medication per day.

Persons with PTSD, panic disorders and social phobia are recommended to first take 25 mg of the drug per day. After the first week of treatment, the portion is increased to 50 mg 1-fold per day, taking into account the course tolerance and medication effects.

In the absence of drug exposure, the portion is gradually increased by titration, with intervals of at least 7 days (because studies related to pharmacokinetics showed that the equilibrium intraplasma level of sertraline is recorded after the 1st week when using the drug 1 time per day). It is forbidden to exceed the maximum permissible portion size limit of 0.2 g per day.

The drug usually reaches full-fledged drug exposure after the 1st month of therapy and more. Accelerated elevation of servings often does not allow reducing the specified latent term, but at the same time it can increase the intensity of negative symptoms.

Supporting activities.

With prolonged treatment, the minimum effective portions of drugs are used. Periodic examination of patients is required to clarify the need for continuation of therapy.

It is forbidden to abruptly stop treatment with the use of the drug, because it can lead to the appearance of withdrawal syndrome. When discontinuing therapy, a gradual reduction in dosage is performed.

Therapy in individuals with problems in the liver.

It is required to use the drug with caution in people with hepatic diseases. If a patient has severe disorders, the dosage of the drug should be reduced or the frequency of its intake should be reduced.

[7]

Use Serralina-apo during pregnancy

There is no evidence of whether sertraline is safe to use during breastfeeding or pregnancy, which is why it is not used during these periods. Exceptions are possible only in situations where the benefits of its administration are more expected than the risk of a negative impact on the fetus.

Contraindications

The main contraindications:

• severe intolerance associated with the active ingredient or other elements of the drug;
• combined use with MAOI;
• liver failure.

[6]

Side effects Serralina-apo

Among the adverse events:

• disorders affecting vegetative NA: hyperhidrosis and dryness of the oral mucosa;
• lesions associated with cardiovascular disease: pain in the sternum or palpitation;
• disorders in the PNS and CNS: dizziness, hypesthesia, increased blood pressure values, headaches, paresthesias and convulsions, as well as tremor;
• epidermal signs: rash;
• problems with digestive function: diarrhea, bloating, vomiting, increased appetite, constipation, nausea, abdominal pain and dyspepsia;
• manifestations of a systemic nature: fever, fatigue, pain in the back and flushing of the face;
• metabolic disorders: feeling of thirst;
• disorders of the musculoskeletal structure: arthralgia or myalgia;
• symptoms associated with mental activity: agitation, mania or hypomania, insomnia, anxiety or nervousness, drowsiness, and besides this yawning, depersonalization, sexual disorders (usually delayed ejaculation in men), problems with concentration, weakening of libido and nightmares;
• problems associated with reproductive organs: menstrual disorders;
• lesions of the respiratory system: pharyngitis or runny nose;
• disorders in the work of the sense organs: ear noise, visual disturbance or taste disturbance;
• disorders of urinary function: disorder or increased urination;
• laboratory test deviation: the activity of liver transaminases inside blood serum rarely asymptomatically increases (approximately three times higher than the maximum permissible limit of the norm; this mainly occurs during the first 1-9 weeks of therapy, after discontinuation of drugs, the values quickly return to normal), insignificantly the indicator of total cholesterol increases (by about 3%), as well as triglycerides (about 5%), the serum value of uric acid decreases slightly (about 7%, this phenomenon has no clinical consequences nd).

Overdose

Sertraline has a wide range of safety; poisoning reported in the case of the use of up to 6 g of drugs. In the case of sertraline-only intoxication, the following symptoms were observed: nausea, anxiety, tachycardia, drowsiness, altered ECG readings, vomiting, and pupillary dilation. Given that deaths due to an overdose of sertraline alone were not noted, there are reports of a fatal outcome in case of sertraline poisoning in combination with other drugs and alcoholic beverages. Because of this, it is necessary to conduct intensive therapy in case of intoxication with the indicated drugs.

It is required to ensure the free passage of air into the respiratory tract, and in addition, adequate ventilation with oxygenation. In addition, laxatives, activated charcoal are used, or gastric lavage is performed (activated charcoal used in combination with sorbitol is considered to be as effective (or even more effective) as gastric lavage and vomiting).

It is required to control the main physiological parameters and conduct general supportive and symptomatic procedures.

No data regarding antidote medication. Hemoperfusion, the forced form of diuresis and exchange blood transfusion do not give a noticeable effect, because sertraline has large indicators of distribution volume.

While assisting the victim, the possibility of poisoning by several drugs at the same time should also be taken into account.

[8], [9], [10]

Interactions with other drugs

Prohibited simultaneous introduction with MAOI.

Pimozide values increase when combined with sertraline. Due to the narrow borders of the drug index of pimozide, it is forbidden to combine these drugs.

The combination with lithium drugs can affect serotonergic neuromediation; therefore, with this combination, it is necessary to ensure adequate monitoring.

At the initial stage of treatment with Sertralin-Apo, plasma indicators of phenytoin need to be monitored, adjusting its portion, if necessary. This is due to the fact that phenytoin is able to reduce the plasma values of sertraline.

Combining drugs with sumatriptan causes discoordination, anxiety, hyperreflexia, and delirium with agitation. With a clinical need for such a combination, the necessary monitoring is required.

Because the drug is synthesized with intraplasma protein, it is necessary to take into account the possibility of developing interaction with other drugs, which are also subjected to this process.

When administered with warfarin, the PTV values increase; this indicator must be constantly monitored at the beginning and end of a therapeutic course using sertraline.

The combination with tolbutamide or diazepam causes a change in individual pharmacokinetic characteristics.

When combined with cimetidine, a decrease in drug clearance is noted.

Prolonged use of sertraline causes a minimal increase in the equilibrium plasma values of desipramine.

[11],

Storage conditions

Sertralin-Apo is required to be kept in a place closed from the penetration of children. Temperature values - not higher than 25 ° C.

[12], [13], [14], [15]

Shelf life

Sertralin-Apo is allowed to apply for a 3-year period from the date of sale of the drug.

[16], [17],

Application for children

Information regarding drug efficacy and safety when used in pediatrics is missing, which is why Sertralin-apo is not prescribed to children.

[18], [19]

Analogs

Analogues of the medication are the means Sertraloft, A-Depresin, Stimuloton, Adjuvin with Zalox and Ascentr with Solotok. In addition, the list is Debitum-Sanovel, Emoton, Depralin with Misal, Serlift with Zoloft and Sertralux.

[20], [21]