Index of drugs

Intensive treatment of depression (including severe) and maintenance treatment in patients who respond well to initial treatment.

1 tabl contains 4 mg of reboxetine (as methanesulfonate).

Antidepressant. Selective and strong norepinephrine reuptake inhibitor. It has only a small effect on the re-uptake of serotonin and has no effect on Dopamine uptake. There was no significant affinity of reboxetine for adrenergic receptors (α₁, α₂, β) and muscarinic receptors. Following oral administration of a single dose, the maximum plasma concentration is achieved after 2 hours. Total bioavailability is at least 60%. T_0,5 drug is about 13 hours. The steady state is achieved within 5 days. Reboxetine is distributed to all body fluids. Plasma proteins are 97% associated in young and 92% in elderly patients (with higher affinity for α₁ acid glycoprotein than albumin). It is metabolised mainly by CYP3A4. The drug is excreted in 78% in urine, 10% of the dose - unchanged. The major identified metabolic pathways are 2-O-dealkylation, hydroxylation of the ethoxyphenol ring, and oxidation of the morpholine ring, followed by partial or complete conjugation with glucuronic acid or sulfonate. The drug is available as a racemic mixture (both enantiomers are active).

Hypersensitivity to the active substance or to any of the excipients.

Reboxetine should not be used to treat children and adolescents under 18 years of age. During the clinical trials, suicide (suicide attempts and suicidal thoughts) and hostility (especially aggression, rebel behavior and anger) were observed more frequently in children and adolescents treated with antidepressants than in the placebo-treated groups. If, based on the existing clinical need, however, a decision to treat is made, the patient should be carefully monitored for suicidal behavior. In addition, there are no long-term data on the safety of use in children and adolescents regarding growth, maturation and development of cognitive functions and behavioral development. The drug should be used with extreme caution in patients with convulsive seizures; if seizures occur, treatment should be discontinued. Due to the risk of depression reaching a hypomanic or manic state, close observation of patients with bipolar disorder is recommended. Depression is associated with an increased risk of suicidal thoughts, self-harm and suicide (suicidal behavior) that may persist until remission of the disease. The patient should remain under strict control until significant improvement occurs and in the early stages of recovery (increased risk of suicide). Patients with a history of suicidal behavior and those who were more likely to develop suicidal ideation prior to treatment were more at risk of suicidal ideation and attempts and should remain under careful monitoring during treatment, particularly those under 25 years of age. During therapy, especially in its early stages and after dose adjustment, patients should be closely monitored, especially those at high risk. Patients with symptoms of urinary retention, prostatic hyperplasia, glaucoma and history of cardiac disease should be carefully observed. Because of the risk of orthostatic hypotension, caution should be exercised when using reboxetine with other medicines that lower blood pressure. There is limited clinical experience of long-term use of reboxetine in elderly patients. In this patient population, a reduction in mean values ​​of potassium concentration was observed starting from the 14th week of treatment; the reduction rate was never greater than 0.8 mmol / liter, and the potassium concentration never decreased below normal values.Due to the lack of appropriate studies, reboxetine should not be used in elderly patients over 65 years of age.

Reboxetine can be used during pregnancy only if the expected benefits of treating the mother outweigh the potential risk of fetal development. Reboxetine is excreted in breast milk. The expected concentration of active substance penetrating into breast milk is very low; however, the information available is not sufficient to rule out the risk to a breastfed child. The use of reboxetine during breastfeeding may be considered when the potential benefit outweighs the risk to the child.

Undesirable effects from clinical trials with a duration of ≤8 weeks. Very often: insomnia, dry mouth, constipation, increased sweating. Common: decreased appetite, akathisia, dizziness, dysgeusia, tachycardia, palpitations, vasodilation, orthostatic hypotension, hypotension, loss or loss of appetite, impaired urination, incomplete emptying of the bladder, urinary tract infection, painful urination , urinary retention, ejaculation and erectile dysfunction, ejaculation pain, ejaculation delay, testicular disorders (mainly testicular pain), chills. Uncommon: vertigo dizziness. During treatment with reboxetine, or shortly after cessation of use, cases of suicidal ideation and behavior were observed. In short-term studies in patients with depression, urological complications (such as the feeling of incomplete emptying of the bladder, impaired urination, and pollakiuria) were more frequently reported in men than in women. In short-term studies in patients with depression, reboxetine was associated with cardiac acceleration, compared to placebo, with an average of 6-12 beats per minute. Adverse reactions reported after placing reboxetine on the market. Very often: nausea. Common: agitation, anxiety, paresthesia, hypertension, vomiting. Frequency unknown: blood deficiency in sodium, hallucinations, aggressive behavior, peripheral cooling, Raynaud's syndrome, testicular pain, allergic dermatitis, rash, irritability. Several spontaneous reports of withdrawal symptoms, including headache, dizziness, nervousness and nausea, have been reported on the market.

Orally. Adults: the recommended therapeutic dose is 4 mg 2 times a day. The full therapeutic dose can be used from the beginning of treatment. In the case of incomplete clinical response after 3-4 weeks, this dose may be increased to 10 mg per day. The maximum daily dose should not exceed 12 mg. The minimum effective dose has not been established. The initial dose in patients with renal or hepatic impairment should be 2 mg 2 times a day; this dose may then be increased depending on the patient's response to the drug.