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Lurasidone is a medication prescribed to treat schizophrenia and bipolar disorder. It belongs to the benzisothiazole class of medicines. This activity covers the indications, actions, and contraindications of lurasidone, which is a useful medicine for treating schizophrenia and bipolar depression. It was approved by the US FDA for the treatment of schizophrenia on October 29, 2010, and is currently being considered for the treatment of bipolar disorder in the United States.

BRAND NAMES

Latuda: It contains the active ingredient of lurasidone. It is available in the form of tablets used to treat schizophrenia and bipolar depression.

MECHANISM OF ACTION

Lurasidone belongs to the benzisothiazole class. Although the mechanism of action for lurasidone is not fully understood, it is thought to target both dopamine and serotonin receptors. Lurasidone completely blocks the dopamine D2 and serotonin 5-HT2A and 5-HT7 receptors. It is a partial agonist of the serotonin 5-HT1A receptor. When compared to other atypical antipsychotics, lurasidone has the strongest binding affinity for the 5-HT7 receptor. Lurasidone's atypical antipsychotic characteristics are caused by its blockage of D2 and 5-HT2A receptors. Lurasidone's antidepressant properties are attributed to its 5-HT7 receptor antagonist and modest 5-HT1A agonism.

PHARMACOKINETICS

Absorption

Taking lurasidone with food doubles exposure and extends the time to peak concentration by 0.5-1.5 hours. Lurasidone is rapidly absorbed and reaches maximum concentrations within 1-4 hours. 

Distribution 

The apparent volume of distribution was approximately 17.2 L. 

Metabolism 

Lurasidone is largely metabolized by the cytochrome P450 enzyme CYP3A4. When used with mild CYP3A4 inhibitors, it is recommended to reduce the lurasidone dose to half of the original amount, with a starting dose of 20 mg and a maximum dose of 80 mg per day. Similarly, when paired with mild CYP3A4 inducers, the lurasidone dose might be increased roughly. 

Elimination

Lurasidone is excreted 9% through urine and 80% in feces.

PHARMACODYNAMINCS

Lurasidone is an atypical antipsychotic that stimulates D2 and 5-HT2A receptors to improve cognition. Antagonism of serotonin receptors is expected to relieve unpleasant symptoms of psychoses while reducing the extrapyramidal adverse effects commonly associated with standard antipsychotics. 

ADMINISTRATION

Lurasidone is available as a pill that can be taken orally. It is typically consumed with a meal once a day. Take Lurasidone at about the same time every day. Lurasidone treats schizophrenia and depression in patients with bipolar illness but does not cure them.

DRUG INTERACTIONS

Other drugs can interact with the clearance of lurasidone from the body, reducing its effectiveness. It consists Antifungal medications include ketoconazole and itraconazole, as well as HIV protease inhibitors like nelfinavir. 

  • Antibiotic: clarithromycin. 
  • Cough relievers: hydrocodone, codeine. 
  • Anxiety medications: alprazolam, lorazepam. 
  • Cyclobenzaprine is a muscle relaxer. 
  • Antihistamines: cetirizine. 

CONTRAINDICATIONS

Hypersensitivity to lurasidone or any other component of the medication when combined with effective CYP3A4 inhibitors and inducers

SIDE EFFECTS

Lurasidone may produce adverse effects. 

Symptoms may include dizziness, weakness, tiredness, restlessness, slow movement, nausea, vomiting, appetite loss, breast enlargement, and decreased sexual capacity. 

Some severe side effects may include seizures, swelling, hoarseness, shortness of breath, irregular heartbeat, sore throat, fever, cough, chills, unusual facial or body movements, and falling. 

Overdose

Symptoms caused by overdose can include

  • Irregular heartbeat
  • Low blood pressure
  • Seizures
  • Decreased alertness

Toxicity

Lurasidone increases the toxicity of methotrexate intranasal through pharmacodynamic synergy. Avoid or utilize an alternative drug. Potential for additive effects, including increased frequency and severity of tardive dyskinesia, other extrapyramidal symptoms, and neuroleptic malignant syndrome.

Storage

Keep out of the reach of children.

Store at room temperature

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Lurasidone
Lurasidone HCl

Lurasidone HCl

CAS Number
367514-88-3