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for the synthesis of Lurasidone, ..

5,532,372 describe a process for the synthesis of Lurasidone, which is illustrated below in Scheme-I

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Synthesis of Lurasidone hydrochloride

Given these considerations, LATUDA should be prescribed in a manner that is most likely to minimize the occurrence of tardive dyskinesia. Chronic antipsychotic treatment should generally be reserved for patients who suffer from a chronic illness that (1) is known to respond to antipsychotic drugs, and (2) for whom alternative, equally effective, but potentially less harmful treatments are not available or appropriate. In patients who do require chronic treatment, the smallest dose and the shortest duration of treatment producing a satisfactory clinical response should be sought. The need for continued treatment should be reassessed periodically.

Lurasidone is an atypical antipsychotic developed by Dainippon Sumitomo Pharma

Lurasidone was administered orally to female rats at doses of 0.1, 1.5, 15, or 150 mg/kg/day for 15 consecutive days prior to mating, during the mating period, and through day 7 of gestation. Estrus cycle irregularities were seen at 1.5 mg/kg and above; the no-effect dose of 0.1 mg/kg is approximately 0.01 times the maximum recommended human dose (MRHD) of 80 mg/day based on body surface area. Fertility was reduced only at the highest dose and this was shown to be reversible after a 14 day drug-free period. The no-effect dose for reduced fertility was 15 mg/kg, which is 1.8 times the MRHD based on body surface area.

Sulpiride can be synthesized from 5-aminosulfosalicylic acid

SAR Study, Synthesis, and Biological Activity of Lurasidone Hydrochloride : A New Drug for Treating Schizophrenia.

Lifetime carcinogenicity studies were conducted in ICR mice and Sprague-Dawley rats. Lurasidone was administered orally at doses of 30, 100, 300, or 650 (the high dose was reduced from 1200 in males) mg/kg/day to ICR mice and 3, 12, or 36 (high dose reduced from 50) mg/kg/day to Sprague-Dawley rats.

Lurasidone is absorbed and reaches peak serum concentrations in approximately 1-3 hours. It is estimated that 9-19% of an administered dose is absorbed. Following administration of 40 mg of LATUDA, the mean (%CV) apparent volume of distribution was 6173 (17.2) L. Lurasidone is highly bound (~99%) to serum proteins.

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It is recommended that LATUDA dose should not exceed 40 mg/day in patients with moderate and severe hepatic impairment (Child-Pugh Class B and C). In a single-dose study of LATUDA 20 mg, lurasidone mean AUC was 1.5-times higher in subjects with mild hepatic impairment (Child-Pugh Class A), 1.7-times higher in subjects with moderate hepatic impairment (Child-Pugh Class B) and 3-times higher in subjects with severe hepatic impairment (Child-Pugh Class C) compared to the values for healthy matched subjects. Mean C was 1.3, 1.2 and 1.3-times higher for mild, moderate and severe hepatically impaired patients respectively, compared to the values for healthy matched subjects.

The figures in the tables and tabulations cannot be used to predict the incidence of side effects in the course of usual medical practice where patient characteristics and other factors differ from those that prevailed in the clinical studies. Similarly, the cited frequencies cannot be compared with figures obtained from other clinical investigations involving different treatment, uses and investigators. The cited figures, however, do provide the prescriber with some basis for estimating the relative contribution of drug and nondrug factors to the adverse reaction incidence in the population studied.

Drug Patents International: Lurasidone
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  • Lurasidone hydrochloride synthesis essay

    Lurasidone - Wikipedia


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Category:Lurasidone - Wikimedia Commons

Non-stimulants Atomoxetine (Strattera) Inhibits norepinephrine reuptake Treatment for ADHD/ADD Black Box Warning: increased risk of suicidality Side effects: dry mouth, abdominal pain, nausea/vomiting, insomnia, abnormal dreams, appetite decrease, somnolence, fatigue, blood pressure and heart rate increase. Serious reactions: psychosis, aggressive behavior, stroke, seizures, liver toxicity, myocardial infarction (heart attack)

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Benadryl Antihistamine - antagonizes histamine receptors Has a sedative effect - used for insomnia/agitation Used as a PRN (as-needed) in hospital settings Side effect: drowsiness, dizziness, incoordination, headache, palpitations Paradoxical effect Tolerance issues

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