Saroten

Saroten is an antidepressant. It belongs to the group of non-selective monoamine reuptake inhibitors.

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Indications Saroten

Main indications for use:

• depressive states, especially those accompanied by anxiety, sleep problems, and agitation;
• endogenous type of depression (mono-, and also bipolar), masked, as well as climacteric and, at the same time, involutional forms of depressive states;
• dysphoria, as well as alcohol-induced depressive syndrome;
• reactive type of depression;
• neuroses caused by depression;
• schizophrenic forms of depressive syndrome (used in combination with neuroleptics);
• pain syndrome in the chronic stage.

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Release form

Available in capsule or tablet form. One package contains 100 tablets.

Pharmacodynamics

Amitriptyline is a tricyclic. It is a tertiary amine that is the central substance in the tricyclic category because it is almost equally active in vivo as an inhibitor of serotonin and norepinephrine uptake by presynaptic nerve receptors.

The main breakdown product of the substance, nortriptyline, is a fairly powerful inhibitor of norepinephrine uptake, but is also capable of blocking serotonin uptake. Amitriptyline has powerful anticholinergic, sedative and antihistaminergic properties, and in addition, it is capable of potentiating the effects of catecholamines.

Suppression of the REM phase of sleep is a sign of the active effect of antidepressants. Tricyclics, as well as selective serotonin reuptake inhibitors, as well as MAOIs, suppress the process of the REM phase and also improve the stage of deep sleep (slow-wave).

Amitriptyline improves depressed mood due to illness.

The sedative effect of amitriptyline is an important aspect of the treatment of depressions, which are characterized by increased agitation, anxiety, restlessness, and sleep problems. The antidepressant effect begins to manifest itself after 2-4 weeks from the start of treatment, while the sedative effect of the drug does not decrease.

The analgesic properties of the drug are not related to antidepressant properties, since the analgesic effect begins much earlier than changes in mood occur. Often, a much lower dose is sufficient to achieve this effect than to ensure changes in the patient's mood.

Pharmacokinetics

After oral administration, the bioavailability of amitriptyline is approximately 60%. The plasma protein binding rate is approximately 95%. The active ingredient reaches its peak concentration in the blood serum approximately 4-10 hours after administration and remains fairly stable.

The process of metabolism of the active component occurs by hydroxylation and demethylation. The main decay product is nortriptyline.

The half-life of amitriptyline is between 16-40 hours (average 25 hours), and the half-life of nortriptyline is approximately 27 hours. Steady-state concentrations of the therapeutic element are established after 1-2 weeks.

Amitriptyline is excreted mainly in the urine, and in addition, in small quantities, it is excreted in the feces.

Amitriptyline, and along with it nortriptyline, are able to pass through the placenta and in small doses penetrate into breast milk.

Dosing and administration

The medicine should be taken orally with water. You can also open the capsule and drink the granules inside with water (they must not be chewed).

In the process of getting rid of depressive states, it is necessary to take the medicine once a day, before going to bed (3-4 hours). The dosage corresponds to 2/3 of the dose of the medicine in tablets.

At the beginning of the treatment course, adults are required to take 1 capsule (50 mg) in the evening. After 1-2 weeks, the daily dosage may be increased to 2-3 capsules (100-150 mg) in the evening, if necessary. After obtaining the desired result, the daily dosage may be reduced to the minimum effective (usually 1-2 capsules or 50-100 mg).

In this case, it is necessary to continue treatment with antidepressants (such as Saroten Retard) for about 4-6 months after receiving a noticeable positive result. Maintenance doses of Saroten Retard (they have anti-relapse properties) are allowed to be taken for a long time - up to several subsequent years.

Elderly patients are recommended to start therapy with tablets - the daily dose is 30 mg (three times a day, 10 mg). After a few days, you can start taking capsules. You should take 1-2 pieces per day (dosage 50-100 mg) - in the evenings before bedtime.

In case of chronic pain syndrome, the daily dosage for adults is 1-2 capsules (50-100 mg) before bedtime. At the initial stage of treatment, it is allowed to take Saroten tablets (25 mg) 1 time in the evening.

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Use Saroten during pregnancy

It is not recommended to take the drug during pregnancy, except in cases where the potential benefit to the mother is greater than the risk of developing potentially negative consequences for the fetus.

Contraindications

Among the contraindications:

• a recent history of myocardial infarction;
• disorder of the intracardiac conduction process;
• acute intoxication with opiates, alcoholic beverages or barbiturates;
• closed-angle glaucoma;
• combination with MAO inhibitors, as well as in the period of time after completing their intake (at least 2 weeks);
• individual intolerance to amitriptyline.

Side effects Saroten

Due to the anticholinergic effect of the drug, the following side effects may occur: sour-bitter taste along with dryness in the mouth, and in addition, stomatitis. Visual disturbances, cholestatic jaundice, tachycardia, increased intraocular pressure, and constipation occasionally develop. Urinary retention occurs sporadically. All these reactions mainly develop at the initial stage of treatment, and then decrease and disappear.

Among other (systemic) reactions:

• cardiovascular system: development of arrhythmia or tachycardia, and in addition to this, intracardiac conduction disorders (recorded only on ECG, not clinically manifested) and orthostatic hypotension;
• CNS organs: a feeling of weakness or drowsiness, and in addition to this, a disorder of concentration and dizziness with headaches. These problems mainly develop at the initial stage of treatment, and then decrease. Rarely, usually in cases where increased initial dosages are used, reactions such as disorientation, a feeling of confusion, drowsiness, strong excitement, and the development of hallucinations are possible. In addition, convulsions, tremors, and extrapyramidal disorders may also appear. In rare cases, a feeling of anxiety appears;
• allergy: skin rashes and itching;
• Others: increased sweating, nausea, weight gain, and decreased libido may occur.

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Overdose

Overdose manifests itself in excitation or suppression of the central nervous system. This is expressed in the form of significant cardiotoxic (low blood pressure, arrhythmia, development of heart failure), as well as cholinolytic (drying of mucous membranes, tachycardia, and urinary retention) symptoms. Hyperthermia and the appearance of convulsions are also observed.

Therapy is symptomatic. It should be carried out in a hospital. After oral administration of amitriptyline, the patient's stomach should be washed as quickly as possible and activated carbon should be given to drink. It is also necessary to provide support for the functioning of the cardiovascular and respiratory systems. It is recommended to monitor the heart for 3-5 days. Adrenaline is not prescribed in such cases. Diazepam can be used to eliminate convulsions.

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Interactions with other drugs

Amitriptyline enhances the effectiveness of ethanol, and in addition to this, barbiturates together with other drugs that suppress the function of the central nervous system. When combined with MAO inhibitors, a hypertensive crisis may develop.

Since amitriptyline increases the effect of anticholinergic drugs, combining these drugs is not recommended.

Increases the effectiveness of sympathomimetics, such as adrenaline and noradrenaline. Therefore, local anesthetics containing these components should not be combined with amitriptyline.

The drug can weaken the hypotensive effect of such drugs as betanidine, clonidine, and guanethidine.

In case of combination with neuroleptics, it is necessary to take into account the fact that tricyclics and neuroleptics mutually slow down each other's metabolic processes, as a result of which the limit of convulsive readiness is lowered.

The combined use of the drug with cimetidine can inhibit the process of amitriptyline metabolism, as well as increase its concentration in the blood plasma - as a result of which a toxic effect develops.

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Storage conditions

The medicine should be kept in the original medicinal packaging under conditions standard for medicines. Temperature conditions – no more than 25°C.

Shelf life

Saroten is permitted to be used for 5 years from the date of manufacture of the drug.