Rexetine

Rexetin is an antidepressant that belongs to the SSRI class of drugs.

Indications Rexetine

It is used in the following conditions:

• a state of depression of various origins (especially pathologies in which a regular feeling of anxiety is observed);
• episodes with the development of depression or bipolar disorder as a consequence of schizophrenia;
• therapy for OCD or its prevention (the medication can prevent the development of active relapses even in the case of a long treatment cycle);
• lesions in the central nervous system that are organic in nature (this includes lesions affecting deep brain structures);
• rehabilitation in case of episodic occurrence of manic-depressive syndrome (during the depressive phase);
• social phobia or generalized symptoms observed in persistent anxiety syndrome;
• PTSD, which often occurs in connection with a disaster or extremely life-threatening situation;
• disorders of a neuropsychiatric nature in which panic or agoraphobia develops.

Release form

The substance is released in tablets of 20 or 30 mg, which are packed in blisters in the amount of 10 pieces. The box contains 3 such blisters.

Pharmacodynamics

The active element of the drug, paroxetine, is a complex organic compound with a bicyclic structure. It slows down the ability of presynaptic wall vesicles to replenish the loss of active serotonin mediators, causing it to linger inside the synaptic cleft. As a result, along with the main therapeutic effect, it has a pronounced activating effect on the central nervous system - because the mediator of nerve impulses has a longer effect (stimulates the serotonergic system).

It should be noted that the active component of the drug, being its chemical base, also has an anxiolytic effect, because the state of anxiety is largely associated with increased excitability of the structures of the subcortex of the brain, which are affected by the drug. Suppression of these parts of the central nervous system (thalamus, limbic formation and hypothalamus) leads to a weakening of the symptoms of anxiety syndrome.

The use of Rexetin also leads to a decrease in the severity of OCD.

Paroxetine has a high specificity of therapeutic effect. It does not affect the activity of opioid, muscarinic or nicotinic endings, as well as adrenergic receptors, due to which it does not lead to the development of drug dependence and addiction of a generalized nature. In addition, there is no change in the intensity of the reuptake of some mediators (dopamine and norepinephrine).

Pharmacokinetics

After oral administration, the drug is absorbed at high speed in the gastrointestinal tract. Food intake does not significantly affect the degree of absorption of the substance. The drug has high protein synthesis rates (approximately 93-95% of paroxetine), due to which its active elements circulate in the main bloodstream for a long time.

Rexetin undergoes intrahepatic metabolism, during which inactive metabolic products are formed. After transformation, the drug in the form of metabolic products is excreted in the urine through the kidneys (mainly). The half-life varies in the range of 15-24 hours (a more accurate indicator depends on the individual rate of metabolic processes).

With a short-term conservative therapy cycle, the drug accumulates slightly, reaching equilibrium values after 7 days of continuous tablet intake. But with prolonged use, the drug does not accumulate.

Dosing and administration

The tablets are taken orally, in the morning, with food. They do not need to be chewed, so as not to damage the tablet shell. Taking into account the clinical condition of the person, the portion size can be adjusted after 2-3 weeks from the start of the treatment cycle.

The dosage sizes of the drug vary significantly depending on the diagnosis given to the patient.

In depressive states, 20 mg of the substance is taken per day. The therapeutic effect develops rather gradually, which is why in extremely severe conditions it may be necessary to increase the dose. At 1-week intervals, the dosage can be increased by 10 mg until the desired result is achieved. A maximum of 50 mg of the drug is allowed per day.

People with OCD should initially take 20 mg of the drug per day. As with depression, the drug effect does not develop immediately, so the dose can be increased by 10 mg at 1-week intervals. In this case, a maximum of 60 mg of the drug is allowed per day.

It is necessary to start treating panic disorders with a small daily dose (10 mg), and then increase it every week until the required sanative effect is achieved. The use of such a small initial dose is due to the fact that the intensity of the manifestations of the main disease can increase due to side effects (negative reactions are most pronounced at the initial stage of the conservative cycle). The maximum permissible daily dose is 60 mg.

For social phobia, 20 mg of Rexetin is taken per day at first. If there is no improvement in the person's condition after 14 days of treatment, the dose of the drug should be increased by +10 mg every week until the desired effect is achieved or the maximum permissible dose of 50 mg per day. The standard maintenance dose for sanitation is usually 20 mg.

In case of generalized anxiety syndrome or PTSD, the conservative treatment regimen is similar to the scheme used in the treatment of social phobia.

Once the active stage of conservative treatment is completed (the severity of all leading symptoms of the underlying CNS disease is significantly reduced), maintenance treatment is required to prevent relapses. Such cycles often last 4-6 months. In addition, when completing therapy, the risk of withdrawal syndrome should be taken into account, and therefore the use of drugs should be discontinued gradually.

In people with kidney or liver failure (with a CC level below 30 ml/min), the ability to metabolize paroxetine is sharply weakened, which is why they are allowed to take no more than 20 mg of the drug per day. In the presence of strict vital indications, the dose can be increased, but it is still recommended to maintain it within the minimum.

Use Rexetine during pregnancy

The drug can be used during pregnancy only if there are strict vital indications, because its use can have a significant impact on the development of the fetus in the womb. For example, in the 1st trimester, the likelihood of developing a congenital defect of the cardiovascular system increases greatly (very often, defects appear in the area of the septum between the atrium and ventricle). In the case of using the drug in the 3rd trimester, premature birth may occur or other prenatal complications may develop (such as extensive cyanosis, RDS syndrome, lethargy, hyperreflexia, epilepsy and decreased blood pressure).

If there is a need to conduct a conservative treatment cycle using Rexetin during lactation, it is necessary to discuss with the attending physician the issue of temporary cessation of breastfeeding, because the active components of the drug cannot be used in children, and a small portion of paroxetine is excreted with breast milk.

Contraindications

Main contraindications:

• the presence of intolerance, idiosyncrasy, and also acquired or hereditary hypersensitivity to the components of the drug;
• use in combination with MAOI drugs (their use is permitted only after 3 weeks from the end of the treatment cycle using antidepressants);
• conservative treatment using tryptophan or its derivatives;
• prolonged QT syndrome;
• liver failure;
• closed-angle glaucoma (in this case, excessive increase in IOP values may occur);
• arrhythmia of ventricular origin;
• prostate hyperplasia;
• appointment for elderly people.

Side effects Rexetine

During active conservative therapy using the drug, the following side effects may be observed:

• disorders affecting the functioning of the PNS or CNS: headaches or dizziness, tremor, circadian rhythm disorder, trembling of the extremities, increased fatigue, irritability, hyperhidrosis, paresthesia, and also visual impairment of nervous origin and dry mouth. In addition, there is information about the development of oromandibular dystonia or extrapyramidal symptoms, but this happens only occasionally;
• problems with digestive function: bowel disorders (both diarrhea and constipation may be observed), dyspepsia, loss of appetite, and in addition, increased activity of liver enzymes, resulting in impaired liver function;
• disorders in the cardiovascular system: decrease or increase in blood pressure (depending on the patient's predisposition), heart rhythm disorders, changes in ECG values and vasodilation, which can lead to fainting due to acute circulatory failure;
• lesions affecting the urogenital system: decreased libido, problems with urination and disorders of active ejaculation;
• other manifestations: skin redness, appearing due to hyperemia of the vascular bed, salt imbalance disorder (hyponatremia), hematomas, increased production and secretion of vasopressin (antidiuretic hormone), hypo- or hyperglycemia, thrombocytopenia, pain in the muscles, myopathy and flu-like symptoms (rhinorrhea, increased temperature, etc.).

In addition, allergy symptoms may be observed, manifested in the form of epidermal rashes, urticaria, itching, bronchospasm, swelling of the upper body (arms and face), and Quincke's edema.

It is necessary to pay attention to the fact that negative manifestations when using drugs are more pronounced at the initial stage of therapy, and as it progresses, they usually weaken significantly.

Abrupt discontinuation of the drug may result in withdrawal symptoms, which include vomiting, confusion, severe tremor, peripheral sensory disturbances, nausea, and circadian rhythm disturbances.

To avoid the development of addiction or withdrawal syndrome, it is necessary to discontinue the drug gradually and only after completing the full treatment cycle.

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Overdose

Often, the use of Rexetin does not lead to complications, because it has a wide range of safe dosages. But when using a 1-time portion, which is more than 2 g of the substance, or in combination with medications containing paroxetine, toxic properties of the active element may develop with subsequent acute intoxication, manifested by the following symptoms:

• dilation of pupils;
• vomiting with nausea;
• severe tremors in the limbs;
• dryness of the oral mucosa;
• feeling of drowsiness or excitement;
• dizziness or headaches;
• redness of the upper body, especially the skin on the face.

The drug has no antidote, so symptomatic procedures are used to eliminate the disorders. It is necessary to closely monitor the functioning of vital systems, as well as ensure free passage of the respiratory tract. As soon as possible after an overdose, it is necessary to perform gastric lavage and give the patient enterosorbents. Oxygen therapy is also considered effective.

Interactions with other drugs

It is forbidden to combine the drug with MAOIs, because with such a combination, mutual potentiation of negative manifestations occurs. If this prohibition is not observed, even a fatal outcome is possible.

Combination of the drug with drugs or dietary supplements containing tryptophan may lead to potentiation of the negative symptoms of therapy. Usually in such cases there are severe headaches, vomiting, regular dizziness and nausea. Such an effect when combined with Rexetin is exerted by anticonvulsants and antidepressants from various categories (amitriptyline, nortriptyline, as well as fluoxetine and others).

Concomitant use with sumatriptan is possible only under the condition of being under regular supervision of experienced medical workers, because with such a combination a feeling of weakness appears, reflexes are enhanced (hyperreflexia develops) and motor coordination is impaired. Therefore, if it is necessary to use a treatment regimen with the introduction of both of these drugs, therapy should be performed in a hospital.

The combination of the drug and oral anticoagulants may increase PT values and increase the risk of bleeding because the effect of anticoagulants is potentiated.

Medicines that stimulate the activity of liver enzymes (including the agent that induces the process of microsome oxidation – phenytoin) can lead to changes in the metabolism of paroxetine. The rate of decomposition of the component into inactive metabolic products increases and the half-life increases (as a result, the drug effect does not develop even in the case of a gradual increase in the dose of the drug).

Negative effects on the metabolic processes of the drug are also exerted by drugs from the phenobarbital category. But in this case, the elements of the drugs increase the rate of renal metabolism. Therefore, the bioactive components of the drug are excreted at a higher rate, due to which their plasma indicators are significantly reduced.

The drug increases the levels of theophylline and procyclidine in plasma, but the mechanism of this interaction could not be determined during clinical trials. Therefore, with such a combination, it is necessary to monitor the plasma levels of the active components of the drugs.

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Storage conditions

Rexetin should be kept in a place protected from moisture and access of small children. Temperature level – in the range of 15-30°C.

Shelf life

Rexetin is allowed to be used within 2-4 years from the date of release of the drug.

Application for children

The use of the drug in pediatrics is completely prohibited, because its use before the age of 18 can lead to changes in the development of internal organs and personality development.

Analogues

Analogues of the drug are such medications as Xet and Parelax with Luxotil.

Reviews

Rexetin generally receives positive reviews because it has a wide range of medicinal activity. Its components not only eliminate depression in a short period of time, but also eliminate such a complication of this disease as anxiety syndrome and prevent the development of a relapse.

In addition, those people who took the medicine say that after the course of therapy, the ability to solve difficult life situations was facilitated. There is no direct confirmation of this obtained during clinical tests, but when selecting medications used to treat nosological units related to the central nervous system and the peripheral nervous system, these subjective data cannot be completely rejected.

Doctors also speak positively about the drug. Although it has quite a large number of negative manifestations, their severity is significantly weakened after the first 7 days of conservative treatment. Among the advantages of the drug, doctors also note its anxiolytic properties and the ability to eliminate social phobia at the therapeutic level.