Sertraline-apo

Sertraline-apo is an antidepressant that belongs to the SSRI group of drugs.

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

The drug has an extremely weak effect on the processes of reverse dopamine and norepinephrine uptake. When using Sertraline-apo in medicinal doses, serotonin uptake is blocked by human platelets.

[ 1 ]

Indications Sertraline-apo

It is used for the following painful conditions:

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

Release form

The medicinal product is released in capsules - 28 pieces inside a polyethylene jar.

[ 2 ]

Pharmacodynamics

Like many other clinically active antidepressants, sertraline attenuates the activity of serotonin and norepinephrine terminals within the brain. However, it has no significant affinity for 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 terminals.

The medication does not have sedative properties and does not affect psychomotor activity.

[ 3 ]

Pharmacokinetics

The pharmacokinetic characteristics of sertraline are linear over the pharmaceutical dose range of 50-200 mg per day.

After repeated administration of the drug in a 0.2 g dose once a day, the Cmax values of sertraline in blood plasma average 0.19 μg/ml; it takes 6-8 hours to obtain this value. The AUC level is 2.8 mg h/l, and the half-life term at the terminal stage is about 26 hours. The Cmax level of the metabolic element N-desmethylsertraline is 0.14 μg/ml, the half-life term is 65 hours, and the AUC values are 2.3 mg h/l.

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

98% is synthesized with blood intraplasmic protein.

N-desmethylsertraline levels in elderly people are three times higher in the case of repeated use of the drug, although the clinical significance of this factor has not been determined.

[ 4 ], [ 5 ]

Dosing and administration

Sertraline-Apo should be taken with food, once a day, preferably in the evening (or with breakfast if taken in the morning).

Initial stage of treatment.

People with OCD or depression are initially required to take 50 mg of the drug per day.

People with PTSD, panic disorders and social phobia are recommended to initially take 25 mg of the drug per day. After the first week of treatment, the dose is increased to 50 mg once a day, taking into account the tolerability of the course and the drug effect.

If there is no medicinal effect, the dose is gradually increased by titration, with intervals of at least 7 days (because studies related to pharmacokinetics have shown that the equilibrium intraplasmic level of sertraline is recorded after 1 week when taking the drug once a day). It is prohibited to exceed the maximum permissible dose limit of 0.2 g per day.

The drug usually achieves its full medicinal effect after 1 month of therapy or more. Accelerated increase in doses often does not allow to reduce the specified latent term, but at the same time it can increase the intensity of negative symptoms.

Supporting activities.

In long-term treatment, minimally effective doses of drugs are used. Periodic examination of patients is required to determine the need for continued therapy.

It is forbidden to abruptly stop treatment with the drug, because this can lead to withdrawal syndrome. When stopping therapy, a gradual reduction in dosage is performed.

Therapy for people with liver problems.

The drug should be used with caution in people with liver disease. If the patient has severe disorders, the dosage of the drug should be reduced or the frequency of its administration should be reduced.

[ 7 ]

Use Sertraline-apo during pregnancy

There is no data on 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 benefit from its administration is more expected than the risk of negative effects on the fetus.

Contraindications

Main contraindications:

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

[ 6 ]

Side effects Sertraline-apo

Side effects include:

• disorders affecting the autonomic nervous system: hyperhidrosis and dryness of the oral mucosa;
• CVS-related lesions: chest pain or palpitations;
• disorders of the PNS and CNS: dizziness, hypoesthesia, increased blood pressure, headaches, paresthesia 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 system: arthralgia or myalgia;
• symptoms associated with mental activity: agitation, mania or hypomania, insomnia, a feeling of restlessness or nervousness, drowsiness, and in addition yawning, depersonalization, sexual dysfunction (usually delayed ejaculation in men), problems with concentration, decreased libido and nightmares;
• problems related to the reproductive organs: menstrual irregularities;
• Respiratory system disorders: pharyngitis or runny nose;
• disorders of the sense organs: tinnitus, visual disturbances or taste disturbances;
• urinary dysfunction: difficulty or increased frequency of urination;
• deviation of laboratory test results: occasionally, asymptomatically, the activity of liver transaminases in the blood serum 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 the drug is discontinued, the values quickly return to normal), the total cholesterol level increases slightly (by approximately 3%), as well as triglycerides (about 5%), the serum uric acid level decreases slightly (about 7%, this phenomenon has no clinical consequences).

Overdose

Sertraline has a wide safety profile; poisoning has been reported with doses up to 6 g. Symptoms of sertraline-only intoxication include nausea, anxiety, tachycardia, drowsiness, ECG changes, vomiting, and pupil dilation. While no deaths have been reported from sertraline-only overdoses, there have been reports of fatalities with sertraline in combination with other drugs and alcoholic beverages. Therefore, intensive therapy is required in cases of sertraline-only intoxication.

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

It is necessary to monitor the main physiological parameters and carry out general supportive and symptomatic procedures.

There is no data on the antidote of the drug. Hemoperfusion, forced diuresis and exchange blood transfusion do not give a noticeable effect, because sertraline has large distribution volume indices.

When providing assistance to 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

Concomitant administration with MAOIs is prohibited.

Pimozide values increase when combined with sertraline. Due to the narrow limits of the drug index of pimozide, these drugs cannot be combined.

Combination with lithium agents may affect serotonergic neurotransmission; therefore, appropriate monitoring should be ensured when this combination is used.

At the initial stage of treatment with Sertraline-Apo, plasma phenytoin levels should be monitored, adjusting the dose if necessary. This is due to the fact that phenytoin can reduce plasma sertraline levels.

Combination of the drug with sumatriptan causes incoordination, anxiety, hyperreflexia and delirium with agitation. If such a combination is clinically necessary, it is necessary to ensure the necessary monitoring.

Because the drug is synthesized with intraplasmic protein, it is necessary to take into account the possibility of interaction with other drugs that are also subject to this process.

When administered with warfarin, PT values are increased; this parameter should be continuously monitored at the beginning and end of the therapeutic course using sertraline.

Combination with tolbutamide or diazepam causes changes in individual pharmacokinetic characteristics.

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

Chronic use of sertraline causes minimal increases in steady-state plasma levels of desipramine.

[ 11 ]

Storage conditions

Sertraline-Apo must be stored in a place closed to children. Temperature values - not higher than 25°C.

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

Shelf life

Sertraline-Apo is approved for use for a period of 3 years from the date of sale of the drug.

[ 16 ], [ 17 ]

Application for children

There is no information regarding drug efficacy and safety when used in pediatrics, which is why Sertraline-apo is not prescribed to children.

[ 18 ], [ 19 ]

Analogues

The analogs of the drug are Sertraloft, A-Depresin, Stimuloton, Adjuvin with Zalox and Asentra with Solotik. In addition, the list includes Debitum-Sanovel, Emothon, Depralin with Misol, Serlift with Zoloft and Sertralux.

[ 20 ], [ 21 ]