Seralin

Seralin is an antidepressant in the IOZS drug category.

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Indications Serinalina

The drug should be used for depression, and in addition, with a feeling of anxiety and the presence / absence of references to mania in the individual history of the patient. The drug can also be administered with maintenance treatment after improvement in the patient's condition (to prevent a relapse of the initial depressive episode).

It is also possible to use capsules during therapy in people with OCD. After receiving the initial drug exposure, long-term (up to 2 years) supportive therapy can be performed using Seralin (most patients tolerate such treatment without complications).

Capsules can also be used in the treatment of people with panic disorders (accompanied by agoraphobia or not), and in addition with PTSD.

Release form

The release of the substance is made in capsules, in the amount of 7 pieces inside a blister pack. The box contains 2 such packages.

Pharmacodynamics

The drug contains sertraline - an active element that significantly slows down the process of reverse serotonin uptake inside the synapses. In in vitro tests, this component significantly weakened the reverse serotonin uptake of 5-hydroxytryptamine inside neurons.

The drug has some effects on the re-uptake of other intermediaries, among which is norepinephrine with dopamine. In therapeutic portions, it blocks the process of serotonin uptake inside platelets.

Seralin does not have a cardiotoxic, sedative, and anticholinergic effect, and in addition does not stimulate the activity of the central nervous system and does not cause changes in psychomotor activity.

Selective locking of the 5-HT reuptake ensures no potentiation of catecholaminergic effects. The drug has no direct effect on muscarinic, benzodiazepine, GABA, dopamine and histamine endings, as well as adrenergic receptors. Testing has shown that prolonged use of Seralin led to a certain weakening of the activity of noradrenalinergic brain endings, and with it to a decrease in mental and motor responses.

The medicine differs from tricyclics in that it does not cause weight changes in people with obsessive and depressive states.

Physical or mental addiction to the drug during the treatment was not observed.

Pharmacokinetics

Pharmacokinetic parameters of sertraline in the range of portions of 0.05-0.2 g are determined by the size of the dosage. The Cmax values of sertraline after ingestion of a portion of 0.05-0.2 g (1-fold per day in a 14-day period) are noted after 4.5-8.6 hours. The average half-life is 22-36 hours and varies with the age of the patient. Considering the half-life, there may be an approximately 2-fold accumulation of the drug; equilibrium values are observed after 7 days from the beginning of the application (1-time use per day).

About 99% of the active ingredient is synthesized with plasma protein.

After the 1st hepatic passage, an active metabolism of the drug substance is observed. The degree of activity of the main metabolic product (N-desmethyl sertraline) is approximately 20% lower compared with sertraline in an unchanged state (with in vitro tests). It should be noted that during in vivo tests, N-desmethyl sertraline showed almost no activity in depressive state models.

The half-life of the main metabolic product is in the range of 62–104 hours. There is a subsequent metabolism of sertraline with N-desmethylsertraline inside the body; its derivatives are equally excreted through the intestines and kidneys. Unchanged sertraline is poorly excreted through the urethra (maximum 0.2% of the dosage used).

Dosing and administration

Capsules must be taken orally, without reference to food intake. Daily dosage is often used for 1 reception (in the morning or in the evening). Portion sizes and duration of treatment should be determined by the physician, taking into account the tolerance of the drug and the nature of the pathology.

People with episodes of depression, as well as OCD, are often prescribed 50 mg of the drug per day. After 7 days from the start of treatment, the dosage can be increased to 0.1 g per day (if there is a good tolerance of the drug and a weak therapeutic effect).

In case of PTSD and panic disorders, treatment should be started with 25 mg of the drug per day (1-fold administration of a 50-mg capsule with 48-hour intervals is performed 1x). If required, the portion can be increased after 7 days from the moment of initiation of therapy.

Individuals may need to take up to 0.2 g of sertraline per day. It is necessary to increase the portion gradually, with a 7-day interval and a one-time increase to a maximum of 50 mg.

Drug treatment often develops after 7 days, reaching its maximum level by the 2nd-4th week of treatment. To get the final effect, often requires a long treatment cycle. It is not recommended to stop the use of drugs without a doctor's recommendation (due to the risk of relapse).

The size of portions of drugs in children 6-12 years of age, as well as adolescents over 12 years of age.

In the treatment of OCD and depressive conditions in adolescents from the age of 12, Seralin is often used in portions intended for an adult.

In depressive situations, children 6-12 years old should use the drug in a 25 mg dose per day (1 capsule of 50 mg is taken 1 time in 48 hours).

People with disorders of renal filtration processes.

This group of drugs should be prescribed very carefully. It is possible that in such a case, a change in the mode of use (extension of the interval between uses) or a reduction in single dosages will be needed.

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Use Serinalina during pregnancy

Seralin is forbidden to prescribe pregnant.

If you need the use of medication for lactation, you must first stop breastfeeding (for the duration of therapy).

If the drug is used in women who are in reproductive age, it is necessary to select a reliable means of contraception. Planning a pregnancy with Seralin should not be.

Contraindications

Main contraindications:

• the presence of hypersensitivity to sertraline, as well as additional elements of the drug;
• use while receiving IMAO;
• the patient has strong changes in the urethra and liver;
• convulsive states (epilepsy, having an unstable character).

Side effects Serinalina

With placebo-controlled tests, sertraline often showed nausea, drowsiness, upset stools, dyspepsia, tremor, dizziness, insomnia, sleep disorders, hyperhidrosis, sexual dysfunction (also delayed ejaculation), and dry oral mucosa.

In addition, the use of Seralina may lead to an asymptomatic increase in the activity of ALT / AST elements. Changes in the transaminase activity of the liver were often noted on the 1-9th week of treatment. The indicators self-stabilized after the correction of single servings or withdrawal of the drug.

There are isolated reports of the development of hyponatremia after the use of drugs (this effect is treatable, and after withdrawal of the drug, sodium levels return to normal). Most likely, hyponatremia when using Seralina develops due to inadequate release of antidiuretic hormone. The risk of developing hyponatremia is higher in people over 65 years of age, as well as those using medications that affect renal activity.

People with strong sensitivity may develop manifestations of an allergic origin.

Occasionally the use of the drug causes the appearance of hyperthermia and disorders of motor activity.

There is also information about the deterioration of dynamics in people with hypomania or mania caused by taking the drug.

There are no significant differences in the profile of adverse signs of the drug in individuals with obsessive and depressive states.

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Overdose

The drug has a fairly large range of security. But at the same time there are reports of cases with a fatal outcome due to sertraline poisoning - with complex treatment or combination with alcoholic beverages.

The medication does not have an antidote. In case of overdose, gastric lavage is required, and then appoint sorbent intake. In case of drug poisoning, you also need to monitor the work of the vital systems of the body.

In addition, it is necessary to ensure the free flow of air and adequate pulmonary ventilation (if necessary, artificial respiration can be performed). At the same time, supportive procedures and drugs are prescribed to reduce the severity of symptoms of poisoning.

When sertraline intoxication dialysis procedures will be ineffective.

Interactions with other drugs

Care should be taken to replace treatment with a variety of SSRIs for sertraline therapy. In addition, the transition to Seralin with antidepressants or anti-obsessive drugs is carried out with great care (especially if these medicines have a long half-life - for example, such as fluoxetine).

You can not combine the drug with an MAOI (because it can lead to the development of extrapyramidal disorders), and in addition to take for 2 weeks from the date of application of the last dosage of MAOI.

The drug should be carefully combined with hypoglycemic drugs for oral administration (sulfonylurea derivatives), because sertraline may affect serum glucose levels. You may also need to change the dosage of antidiabetic drugs (especially at the initial stage of use of sertraline or when it is canceled).

The combination of the drug with tricyclics and tranquilizers may change the pharmacokinetic parameters of these agents.

Combination with substances that block the activity of histamine H1- and H2-terminations leads to a decrease in the clearance of Seralin.

It is necessary to very carefully combine the drug with digoxin.

The drug should be used with extreme caution in people who are treated with drugs that can develop indirectly (through serotonergic mechanisms — for example, such as lithium).

During treatment can not take alcoholic beverages.

Use of the drug is prohibited for people receiving electroconvulsive therapy.

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Storage conditions

Seralin is required to be kept in a place closed to prevent access by small children.

Shelf life

Seralin can be used within 24 months of the release of the therapeutic agent.

Application for children

It is forbidden to prescribe medication in pediatrics - children under 6 years of age.

Analogs

Analogues of the medication are drugs Zoloft, Fluanksol, Velafax, Torin, Truksal with Stimuloton, and in addition Simbalta, Serlift, Lerivon, Serenata, Risperidone and Pulsatilla compositum with Tsipramil. In addition, Melipramin, Noben, Ignatia-homaccord, Velaksin, Adepress, Tazepam, Lamotrigine, Plizil and Lyudomil with Velafax MV are on the list.