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Clozapine, the most effective antipsychotic

Clozapine is an antipsychotic drug used in patients with schizophrenia resistant to other treatments. We are talking about a medication that has caused a lot of controversy, especially due to its side effects.

Clozapine, also known by the brand name Leponex, was the first licensed atypical antipsychotic.. It was marketed for the first time in Spain in 1993, although it had been approved before in other countries and withdrawn due to the appearance of serious side effects.

After several investigations, it was reintroduced to the market due to its high effectiveness. In United States, The Food and Drug Administration (FDA) approved it for the treatment of resistant schizophrenia. to other drugs in 1990.

What is clozapine?

Clozapine, as we have said, is an antipsychotic drug. It is used in patients with schizophrenia who are resistant to other types of treatments. We talk about a drug that has caused a lot of controversy, especially because of its side effects.

Nevertheless, Various studies recognize that it is the most effective antipsychotic in schizophrenia. And not only in resistant schizophrenia. However, he has been relegated only to the most extreme cases due to his security profile.

What is it for?

Clozapine, according to its technical information, is indicated in the following cases:

Schizophrenia resistant to other antipsychotic treatments. It is also indicated in patients in whom other drugs cannot be used due to the risk of serious neurological adverse reactions.Psychotic disorders in patients with Parkinson’swhen the usual treatments have not worked.

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Clozapine is currently the only drug indicated for resistant schizophrenia.. Its effectiveness has been proven in both the negative and positive symptoms of schizophrenia. It is especially useful in the treatment of auditory hallucinations, aggression and suicide risk.

Likewise, other studies affirm that clozapine also has a beneficial effect on cognitive functionthe affective symptoms, the feeling of well-being and the improvement in the quality of life of the patients treated with it.

Clozapine mechanism of action

Clozapine exerts a weak blocking action on dopamine receptors. D1, D2, D3 and D5, as well as strong blocking of the D4 receptors. It also exerts its effect on other receptors, including:

5-HT2 serotonin.Alpha-1 adrenergic: blocking these receptors produces effects such as sedation, muscle relaxation, hypotension and tachycardia.Muscarinic: this antagonistic effect is what causes some unwanted anticholinergic effects.Histamines H1.

Other notable effects of this drug are depression of the central nervous system.which leads to a reduction in the level of wakefulness, and a reduction in the seizure threshold.

Side effects

Clozapine can cause, such as serious adverse effects:

Agranulocytosis. Epileptic seizures. Cardiovascular effects. Fever.

However, the most common side effects are:

Drowsiness and sedation. Dizziness. Tachycardia. Constipation. Hypersalivation.

Since the beginning of its marketing, the adverse effect that has always been of most concern has been agranulocytosis. In severe cases, it can cause sepsis and lead to death of the patient. Because of this, monitoring of blood leukocyte count is necessary throughout the treatment.

The doctor who prescribes the drug must strictly follow all established safety measures. Likewise, patients should be alert for any signs of infection, especially symptoms such as fever or sore throat.

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Other adverse effects to watch for are cardiovascular disorders.. Orthostatic hypotension may occur, as well as myocarditis. In the latter case, cardiac signs must be monitored, such as arrhythmias, chest pain or dyspnea.

To conclude, we must remain with that Clozapine is an antipsychotic drug with a high index therapeutic. That is, the benefit of its clinical efficacy is far greater than the risk of adverse effects. Even so, it is necessary for the specialist to maintain close control and surveillance to avoid these possible reactions.

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All cited sources were reviewed in depth by our team to ensure their quality, reliability, validity and validity. The bibliography in this article was considered reliable and of academic or scientific accuracy.

Armendariz, JE (2008). Clozapine: a historical overview and current role in treatment-resistant schizophrenia. Ars Pharmaceutica (Internet), 49(2), 135-144.Huhn, M., Nikolakopoulou, A., Schneider-Thoma, J., Krause, M., Samara, M., Peter, N., … & Davis, J. (2019). Comparative efficacy and tolerability of 32 oral antipsychotics for the acute treatment of adults with multi-episode schizophrenia: a systematic review and network meta-analysis. The Lancet.Spanish Agency for Medicines and Health Products (2019). Data sheet. Leponex. Available at: https://cima.aemps.es/cima/dochtml/ft/59548/FT_59548.html

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