Saroten

Saroten is an antidepressant. It is part of a group of non-selective inhibitors of reverse monoamine capture.

[1]

Indications Saroten

The main indications for the appointment:

• Depressive conditions, especially those accompanied by anxiety, sleep problems, and excitement;
• endogenous type of depression (mono- and, in addition, bipolar), masked, as well as menopausal and, at the same time, involutionary 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 a chronic stage.

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Release form

Produced in the form of capsules or tablets. One package contains 100 tablets.

Pharmacodynamics

Amitriptyline belongs to the tricyclic group. It is an amine of the tertiary type, which is the central substance in the tricyclic category, because it is practically equally active in vivo as an inhibitor of serotonin and noradrenaline seizure by presynaptic nerve receptors.

The main product of the decay of the substance, nortriptyline, is a potent inhibitor of noradrenaline capture, but it is also capable of blocking serotonin capture. Amitriptyline has powerful cholinolytic, sedative and antihistaminergic properties, and besides this it is capable of potentiating the effects of catecholamines.

The suppression of BDG sleep phase is a sign of the active effect of antidepressants. Tricyclics, and in addition to them selective inhibitors of reverse serotonin capture, as well as MAO, inhibit the process of the BDG phase, and also improve the stage of deep sleep (slow wave).

Amitriptyline improves mood lowered due to illness.

The sedative effect of amitriptyline is an important aspect of the treatment of depression, in which there is increased excitement, anxiety, anxiety, and sleep problems. Antidepressant effects begin to appear after 2-4 weeks from the start of treatment, while the sedative effect of the drug does not decrease.

The analgesic properties of drugs are not associated with antidepressant drugs, since anesthesia begins much earlier than changes in mood occur. Often, a much lower dose is sufficient to obtain this effect than to provide a change in the mood of the patient.

Pharmacokinetics

After internal reception, the bioavailability of amitriptyline is approximately 60%. The binding index for plasma proteins is approximately 95%. The peak concentration in the blood serum of the active ingredient reaches approximately 4-10 hours after use and remains fairly stable.

The process of metabolism of the active component occurs by hydroxylation, as well as demethylation. The main product of decomposition is nortriptyline.

The half-life of amitriptyline is in the range of 16-40 hours (the average is 25 hours), and the half-life of nortriptyline is approximately 27 hours. The steady-state concentration of the therapeutic element is established after 1-2 weeks.

The excretion of amitriptyline occurs for the most part with urine, and in addition, in small amounts, is excreted with feces.

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

Dosing and administration

The medicine should be taken orally, washed down with water. You can also open the capsule and drink with water the granules inside (they are forbidden to chew).

In the process of getting rid of depressive states, you need to take the medicine 1 time per day, before going to bed (3-4 hours). The dosage corresponds to 2/3 of the drug dose 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, daily dosage is allowed to increase until evening use of 2-3 capsules (100-150 mg) - if necessary. After obtaining the desired result, the daily dosage can be reduced to the minimum effective (mostly 1-2 capsules or 50-100 mg).

It should be about 4-6 months to continue treatment with antidepressants (such as Saroten Retard), after receiving a noticeable positive result. The maintenance dosages of Saroten Retard (they possess anti-relapsing properties) are allowed to take a long time - up to several years.

Elderly patients are advised to start therapy with tablets - the volume of a daily dose is 30 mg (three times a day for 10 mg). After a few days, it is allowed to start taking capsules. In a day should be taken 1-2 pieces (dosage 50-100 mg) - in the evenings before bedtime.

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

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Use Saroten during pregnancy

It is not recommended to take the medicine during pregnancy. Except where the possible benefits for the mother are higher than the risk of developing potentially negative consequences for the fetus.

Contraindications

Among the contraindications:

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

Side effects Saroten

Due to the anticholinergic effect of the drug, such adverse reactions may occur: an acid-bitter taste along with dryness in the oral cavity, and in addition stomatitis. Occasionally, visual disturbances develop, cholestatic form of jaundice, tachycardia, increased intraocular pressure, and constipation. Delayed urination is rare. All these reactions mainly develop at the initial stage of treatment, and subsequently decrease and disappear.

Among other (systemic) reactions:

• organs of the cardiovascular system: the development of arrhythmia or tachycardia, and in addition to this intracardiac conduction disorder (recorded only on the ECG, clinically does not manifest) and orthostatic form of hypotension;
• organs of the central nervous system: a feeling of weakness or drowsiness, and in addition, attention and dizziness disorder with headaches. These problems mainly develop at the initial stage of treatment, and then decrease. Occasionally, usually in cases where elevated initial dosages are used, reactions such as disorientation, a sense of confusion, drowsiness, strong arousal, the development of hallucinations are possible. In addition, convulsions, tremors and extrapyramidal disorders may also occur. In rare cases, there is a feeling of anxiety;
• allergies: skin rashes and itching;
• other: possibly increased sweating, nausea, weight gain, as well as decreased libido.

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Overdose

The manifestation of an overdose is the excitation or suppression of the CNS function. This is expressed in the form of significant cardiotoxic (lowering blood pressure, arrhythmia, the development of heart failure), as well as holinoliticheskih (overdrying of mucous membranes, tachycardia, as well as retention of urinary symptoms). There is also hyperthermia and the appearance of seizures.

Therapy is symptomatic. You need to spend it at the hospital. After oral administration of amitriptyline, the stomach should be rinsed as soon as possible and give an activated charcoal. It is also required to provide support for the functioning of the cardiovascular and respiratory systems. It is recommended 3-5 days to follow the work of the heart. Adrenaline is not prescribed in such cases. To eliminate seizures, you can use diazepam.

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Interactions with other drugs

Amitriptyline increases the effectiveness of ethanol, and in addition barbiturates, along with other drugs, suppressing the function of the central nervous system. When combined with MAO inhibitors, hypertensive crisis may develop.

Since amitriptyline increases the effect of cholinolytic drugs, it is not recommended to combine these medicines.

Increases the effectiveness of sympathomimetics - such as adrenaline and norepinephrine. Therefore, do not combine local anesthetics with amitriptyline, which contain these components.

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

In the case of a compound with neuroleptics, it is necessary to take into account the fact that tricycles with neuroleptics mutually slow each other's metabolic processes, thereby lowering the border of convulsive readiness.

Combined medication with cimetidine can inhibit the metabolism of amitriptyline, as well as increase the index of its concentration inside the blood plasma - as a result, the toxic effect develops.

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Storage conditions

Keep the medication in the original medicinal package under conditions that are standard for medications. Temperature regime - no more than 25 ° С.

Shelf life

Saroten is allowed to be used within 5 years from the date of manufacture of the medicinal product.