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Lurasidone HCl – Precautions and side effects

by egpat         22 May 2024

Lurasidone is one of the medications that is classified as anti-psychotic. This is one of the second-generation antipsychotics, or what is also called an atypical antipsychotic. These are the new generation of antipsychotics with more effectiveness in relieving the symptoms of psychosis, so lurasidone can be indicated for the treatment of schizophrenia.

This is one of the common psychotic disorders that can be observed with different types of symptoms, like hallucinations, where patients can perceive auditory or visual hallucinations. They can also perceive some strange voice or light without their physical presence. Delusions are wrong judgments where one can perceive things in a different way. These two symptoms are commonly called positive symptoms of schizophrenia, and these symptoms can be treated by many of the antipsychotics.

But still, a few of the symptoms are resistant to many of the antipsychotics, and they are commonly known as negative symptoms. Among them, social withdrawal is one of the negative symptoms. Flattening of the emotional response or lack of any response in people is also a negative symptom of schizophrenia. These negative symptoms are not generally relieved by many of the typical antipsychotics.

However, lurasidone is an atypical antipsychotic, that is, a second-generation antipsychotic, that can relieve both positive and negative symptoms of schizophrenia. So lurasidone can be used for the long term to reduce the symptoms of hallucinations and delusions, reduce social withdrawal, and reduce the relapse of psychotic symptoms.

Apart from this clinical indication, lurasidone can also be used to treat bipolar disorder. This is one of the mood disorders where the mood of the person can swing between two phases: the depressive phase and the manic phase. Mood swings can range from depression to mania and vice versa. In such cases, to control the manic phase, lurasidone can be given. It can also be given as an adjunctive therapy along with other drugs like lithium carbonate, which is an anti-manic agent.

Similarly, valproate is another drug that can be used for bipolar depressive disorder. Lurasidone can be combined with these drugs as adjunctive therapy to control the manic phase of bipolar depressive disorder. Lurasidone has a few advantages: it is available for long-term use with less risk of relapse of psychosis, and it causes less weight gain in people, even though it has low cardiac effects.

Precautions

Just like many of the antipsychotics, lurasidone can also increase the risk of orthostatic hypotension, so people may have some dizziness, drowsiness, or lightheadedness, and they may also have an increase in their heart rate. They can also have palpitations and awareness of their heartbeats. Because of this orthostatic hypotension while using lurasidone, care should be taken while standing or changing positions. This drowsiness may impair the attention of a few people, so while driving vehicles or working with machinery, care should be taken.

Lurasidone can act by multiple mechanisms, so it can block one of the receptors, alpha-1 adrenergic receptors. These alpha-1 receptors are responsible for developing blood pressure while you are standing or changing positions. When these receptors are blocked, blood vessels are not receiving sufficient pressure, so you may experience orthostatic hypotension. Therefore, during the early days of therapy, dizziness and drowsiness may be produced by this medication.

The second important precaution is for the elders. Generally, in the elderly, we can observe some loss of memory called dementia. This dementia may be associated with psychotic symptoms. In the elderly, there may be a coexistence of dementia and psychosis. In such people, lurasidone can control the psychosis; however, it can cause cerebrovascular side effects. It can increase the risk of stroke in such a group of people.

If you observe that you have symptoms like high-grade fever, rapid heartbeat, excessive sweating, difficulty breathing, and some muscle rigidity in such conditions, lurasidone should be carefully used because all these symptoms are collectively called neuroleptic malignant syndrome. This is one type of syndrome commonly caused by many of the neuroleptics. Because of this muscle rigidity, it can reduce breathing, which is fatal to the patient. However, Lurasidone rarely produces this syndrome.

Another important precaution with this medication is involuntary movements. Even though this is a rare condition, with long-term treatment, few people can observe involuntary movements. Some shakiness can be observed at the hands and feet. Even the protrusion of the tongue can be observed. Lip smacking and twisting of the tongue can also be observed in such people.

These symptoms may indicate the development of tardive dyskinesia, a slowly developing disturbance in kinetic movements. Care should be taken to avoid further development of tardive dyskinesia, and the therapy may be stopped in order to avoid further involuntary movements. However, it is not common in all people and is observed only during long-term therapy.

Even though this medication causes fewer metabolic changes, with long-term use of lurasidone, we can observe a slight increase in glucose levels. Sometimes we can also observe increased weight gain, but all these side effects produced by lurasidone are somewhat less severe compared with other atypical antipsychotics. These symptoms may be observed after 4 weeks of treatment with lurasidone.

Side effects

With the use of lurasidone, somnolence is commonly observed, leading to sleepiness in people. Rhinitis-like symptoms, nausea, some dizziness, and drowsiness can also be produced. It can also cause orthostatic hypotension. Lurasidone can increase salivary secretion. Restlessness and involuntary movements are also observed. All these are the common side effects produced by lurasidone.

Mechanism of action

Lurasidone acts through multiple mechanisms. It can act on different types of receptors. It can affect D2 receptors, 5-HT2A receptors, and even 5-HT7 receptors. All these receptors are antagonized by lurasidone. Apart from these actions, lurasidone can also block muscarinic receptors, alpha-1 receptors, and histamine H1 receptors. But the anti-psychotic and anti-manic actions are mainly related to the blocking of D2 as well as 5-HT2A receptors.

Within the CNS, dopamine can be stored in the dopaminergic neurons and released by calcium-mediated exocytosis. Now this dopamine can act on dopamine D2 receptors, which are then activated. Upon activation, they can reduce the levels of cyclic AMP. The decrease in cyclic AMP levels may result in hallucinations and delusions in people. Now, lurasidone can block these D2 receptors as a full antagonist, thereby relieving the symptoms of psychosis. Similarly, lurasidone can block the 5HT-2A receptors, which may be responsible for its antimanic action.

Dosage forms

Lurasidone is available as a tablet in different strengths, starting at 20 mg, 40 mg, 80 mg, and 120 mg. The initial dose is started at 40 mg given once daily, and the dose may be slowly titrated such that the target dose may be variable from 40 mg to 160 mg per day. The total dose can be given in divided doses, but the starting dose is 40 mg given once daily.

Dose adjustment can also be done based on the patient's age as well as their health conditions. In people with any hepatic or renal impairment, the initial dose may be started at 20 mg given once daily. In this way, the dose of lurasidone can be customized based on the patient's conditions.

Conclusion

Lurasidone, which is one of the second-generation antipsychotics, is also called an atypical antipsychotic. This drug acts as a full antagonist at the D2 receptors, and it can be used for long-term therapy where it produces less relapse of psychosis. This medication has fewer cardiac effects and a low risk of weight gain. With such advantages, Lurasidone can be used to treat psychosis as well as to control the manic phase in bipolar disorder. Orthostatic hypotension is one of the important precautions that should be considered. Rarely can it produce neuroleptic malignant syndrome, and on long-term use, it can produce some involuntary movements.