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Introduction
Lurasidone is a novel antipsychotic drug that has been recently developed for the treatment of schizophrenia.
The drug is a serotonin D2 and dopamine D3/D4 receptor partial agonist, which means that it acts on certain receptors in the brain to regulate the levels of serotonin and dopamine, two neurotransmitters that play a crucial role in mood, emotions, and cognitive function.
Lurasidone has been found to be effective in treating the positive and negative symptoms of schizophrenia, as well as improving cognitive function.
Chemical Structure and Synthesis
Lurasidone is a synthetic compound that is structurally similar to clozapine, another antipsychotic drug.
It has a molecular formula of C28H28ClN3O2 and a molecular weight of 516.
99 g/mol.
The chemical synthesis of lurasidone involves a series of steps, including the preparation of several intermediates, such as 3-iodo-1,2,4-benzothiadiazine-7-carboxylic acid, 1,2,4-benzothiadiazine-7-carboxylic acid, and 4-chloro-1,2,4-benzothiadiazine-7-carboxylic acid.
The synthesis of lurasidone begins with the preparation of 3-iodo-1,2,4-benzothiadiazine-7-carboxylic acid, which is then treated with 4-amino-2,3-dihydro-1,5-benzoxazepine to form 1,2,4-benzothiadiazine-7-carboxylic acid.
This intermediate is then treated with hydrochloric acid to form 4-chloro-1,2,4-benzothiadiazine-7-carboxylic acid.
The final step involves the condensation of 4-chloro-1,2,4-benzothiadiazine-7-carboxylic acid with 2-methyl-2,3-dihydro-1H-indole-6-amine to form lurasidone.
Pharmacokinetics and Metabolism
Lurasidone is administered orally, and its bioavailability is around 70%.
It has a half-life of about 24 hours, and it is primarily metabolized by the liver enzyme CYP3A4.
The main metabolites of lurasidone are the N-desmethylated, N-oxidized, and O-desmethylated forms.
These metabolites are pharmacologically inactive, and their formation does not affect the efficacy of lurasidone.
Lurasidone is also a substrate of P-glycoprotein, a membrane transporter that pumps drugs out of cells, which may affect its brain penetration.
Indications and Usage
Lurasidone is indicated for the treatment of schizophrenia in adults.
It is generally recommended as a second-line treatment for patients who have not responded to or cannot tolerate other antipsychotic drugs.
Lurasidone has been found to be effective in improving negative symptoms, such as apathy and anhedonia, as well as cognitive function.
Contraindications and Precautions
Lurasidone is contraindicated in patients with a history of hypersensitivity to the drug or any of its components.
It should also be avoided in patients with a history of liver disease or severe hepatic impairment, as it may increase the risk of adverse effects.
Lurasidone should be used with caution in patients with a history of diabetes, as it may affect blood glucose levels.
The drug should also be used with caution in elderly patients, as they may be more susceptible to adverse effects, such as dizziness and orthostatic hypotension.
Dosage and Administration