Olanzapine pills 5 mg 30 pcs
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Active ingredients
Olanzapine
Release form
Pills
Composition
Olanzapine 5 mg; Excipients: lactose monohydrate - 50.6 mg, microcrystalline cellulose - 51.4 mg, pregelatinized starch - 51.4 mg, colloidal silicon dioxide - 0.8 mg, magnesium stearate - 0.8 mg.
Pharmacological effect
Olanzapine is an antipsychotic (neuroleptic); in preclinical studies, an affinity for 5-НТ2А / 2С-, 5-НТ3-, 5-НТ6-serotonin receptors, D1, D2, D3, D4, D5-dopamine receptors , m-holinoblokiruyuschie effects due to blockade of M1-5-cholinergic receptors; also has affinity for 1-adreno and H1-histamine receptors. In animal experiments, antagonism was revealed in relation to serotonin, dopamine and m-cholinergic receptors. In vivo and in vitro, olanzapine has a more pronounced affinity and activity for 5-HT2-serotonin receptors compared with D2-dopamine receptors. According to electrophysiological studies, olanzapine selectively reduces the excitability of mesolimbic dopaminergic neurons, and at the same time has a slight effect on the striatal pathways involved in the regulation of motor functions. Olanzapine reduces the conditioned defensive reflex (a test that characterizes antipsychotic activity) at doses lower than the doses that cause catalepsy (a disorder reflecting a side effect on motor function). Unlike other neuroleptics, olanzapine enhances the anti-anxiety effect when conducting an "anxiolytic" test.; Olanzapine provides a statistically significant response to both productive (delusions, hallucinations, etc.) and negative disorders. With a single dose of 10 mg of olanzapine through positron emission tomography (PET) on healthy volunteers showed a greater affinity of olanzapine for 5 HT2A- than for D2-dopamine receptors. On tomograms of patients with schizophrenia, it is shown that in patients sensitive to treatment with olanzapine, affinity for striatal D2 receptors is comparable to the effect in patients sensitive to receiving clozapine and lower than in patients sensitive to treatment with other antipsychotic drugs and risperidone. Clinical efficacy ; In the international, double-blind,a comparative study of patients with schizophrenia, schizoaffective or similar disorders of varying severity of depressive symptoms (average baseline value of 16.6 on the Montgomery-Asberg scale for assessing depression), a prospective secondary analysis on the mood scale from baseline to endpoint control was found statistically significant (p = 0.001) improvement with olanzapine (-6.0) compared with haloperidol (-3.1); in patients with manic or mixed episodes of bipolar disorder compared with placebo and the drug m valproic acid (divalproate) has been shown to be highly effective in reducing manic symptoms for 3 weeks. Comparable results of the effectiveness of olanzapine and haloperidol were observed in patients with symptomatic remission of mania and depression after 6-12 weeks. In the therapy of patients who took lithium or valproic acid for at least 2 weeks, an additional dose of 10 mg of olanzapine (therapy with lithium or valproic acid) led to a significant reduction in the symptoms of mania compared with monotherapy with lithium or valproic acid for 6 weeks. In a 12-month study of the prevention of maniac relapse In episodes in patients who achieved remission while taking olanzapine and then randomly assigned to the group of the drug olanzapine, a statistically significant advantage over placebo was found in the main criterion for controlling the occurrence of bipolar disorder and in terms of preventing relapse or relapse of depression. In the second 12-month period a study on the prevention of recurrent manic episodes in patients who achieved remission when co-administering olanzapine with a lithium drug, and then randomized h olanzapine monotherapy group or mixture of lithium. The effectiveness of olanzapine was statistically insignificant compared with the lithium drug by the main criterion for control of bipolar disorder recurrence (olanzapine 30.0%, lithium 38.3%, p = 0.055); mood stabilizing drugs (lithium or valproic acid),Long-term combined therapy with olanzapine with lithium or valproic acid was not statistically significant compared with monotherapy with lithium or valproic acid in order to delay the onset of relapse of bipolar disorder, which is determined by diagnostic signs.
Pharmacokinetics
After oral administration, olanzapine is well absorbed, Cmax in plasma is reached after 5–8 hours. The absorption of olanzapine does not depend on food intake. Studies with different doses in the range of 1–20 mg showed that plasma concentration of olanzapine varies linearly and proportionally to the dose. Olanzapine is metabolized in the liver as a result of conjugation and oxidation. The major circulating metabolite is 10-N-glucuronide, which theoretically does not penetrate the blood-brain barrier. CYP1A2 and CYP2D6 isoenzymes are involved in the formation of N-desmethyl- and 2-hydroxymethylmetabolites of olanzapine. Both metabolites in animal studies had significantly less pronounced pharmacological activity in vivo than olanzapine. The main pharmacological activity of the drug is due to the parent compound, olanzapine, which has the ability to penetrate the blood-brain barrier. In healthy volunteers, after ingestion, the average T1 / 2 was 33 hours (21–54 hours for 5–95%), and the average plasma olanzapine clearance was 26 l / h (12–47 l / h for 5–95%); However, the degree of changes in the half-life and clearance under the influence of each of these factors is significantly lower than the degree of differences in these indicators between individuals. Pharmacokinetics in adolescents (13-17 years) and in adults are similar. According to clinical studies, the amount of exposure in adolescents is 27% higher than in adults. The difference in demographic parameters between the population of adults and adolescents was that there were fewer smokers among adolescents and lower average body mass indexes were observed. Significant differences between the mean half-life and plasma clearance of olanzapine in individuals with severe renal impairment, compared with persons with normal renal function, not established. About 57% of radioactively labeled olanzapine is excreted in the urine mainly as metabolites. In smokers with minor hepatic impairment, the clearance of olanzapine is lower than in non-smokers without impaired liver function; plasma proteins is about 93%. Olanzapine is mainly associated with albumin and with acidic 1-glycoprotein.In a study involving people of European, Japanese and Chinese origin, differences in the pharmacokinetics of olanzapine related to race were not established. The activity of the isoenzyme CYP2D6 does not affect the metabolism of olanzapine.
Indications
- for the treatment of schizophrenia. Olanzapine is effective in maintaining clinical improvement in ongoing treatment of patients with schizophrenia who responded to initial treatment ;; - to treat a moderate to severe manic episode; - to prevent recurrences in patients with bipolar disorder, in whom it has proven effective in treating manic phases ;; - therapeutically resistant depression. In combination with fluoxetine, olanzapine is indicated for the treatment of therapeutically resistant depression in adult patients (major depressive episodes if there is a history of ineffective use of two antidepressants with respect to the dose and duration of therapy appropriate to this episode). Olanzapine in monotherapy is not indicated for the treatment of therapeutically resistant depression.
Contraindications
- hypersensitivity to any of the components of the drug ;; - contraindicated for persons under 18 years old ;; - lactase deficiency ;; - lactose intolerance ;; - glucose-galactose malabsorption.
Dosage and administration
Inside Olanzapine can be taken regardless of the meal, as food does not affect the absorption of olanzapine. Schizophrenia; The recommended initial dose of olanzapine is 10 mg once a day. Therapeutic doses of olanzapine range from 5 mg to 20 mg per day. The daily dose must be selected individually depending on the patient’s clinical condition. Increasing the dose above the standard daily dose (10 mg) is recommended only after evaluating the clinical picture. When using the drug, it is necessary to regularly assess the need to continue therapy.; Bipolar disorder; For the treatment of a manic episode, the recommended initial dose of olanzapine is 15 mg once a day as monotherapy or 10 mg once a day in combination with lithium preparations or valproic acid. Therapeutic doses of olanzapine range from 5 mg to 20 mg per day. The daily dose must be selected individually, depending on the clinical condition of the patient.Increasing the dose above the standard daily is recommended only after evaluating the clinical picture and with an interval of at least 24 hours. Supportive therapy for bipolar disorder: Patients who take olanzapine to treat a manic episode should continue maintenance therapy at the same dose. In patients in remission, the recommended initial dose of olanzapine is 10 mg once a day. In the future, the daily dose must be selected individually; depending on the clinical condition of the patient, ranging from 5 mg to 20 mg per day. For the treatment of a depressive episode, olanzapine should be administered in combination with fluoxetine 1 time per day, in the evening, regardless of the meal. As a rule, the initial dose is 5 mg of olanzapine and 20 mg of fluoxetine. Antidepressant activity was confirmed with the use of olanzapine in a dose of 6–12 mg (average daily dose - 7.4 mg) and fluoxetine in a dose of 25–30 mg (average daily dose - 39.3 mg). If necessary, change the dose of both olanzapine and fluoxetine. When using the drug, it is necessary to regularly assess the need for continued therapy.; Therapeutically resistant depression; Olanzapine should be prescribed in combination with fluoxetine 1 time per day, in the evening, regardless of the meal. As a rule, the initial dose is 5 mg of olanzapine and 20 mg of fluoxetine. If necessary, change the dose of both olanzapine and fluoxetine. Antidepressant activity was confirmed when using olanzapine in a dose of 6–12 mg and fluoxetine in a dose of 25–30 mg. When using the drug, it is necessary to regularly assess the need for continued therapy.; General rules for choosing a daily dose for special groups of patients when taken orally; Reducing the initial dose to 5 mg per day is recommended for elderly patients or patients with other clinical risk factors, including severe renal failure or liver failure. moderate severity. Reducing the initial dose to 5 mg can be recommended for patients with a combination of factors (female gender, old age and no smoking habits) that can reduce the metabolism of olanzapine (see table 1) .; The use of olanzapine has not been studied in persons younger than 13 years.