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Penfluridol is an organic compound with the chemical formula C28H27ClF5NO, CAS 26864-56-2. At room temperature and pressure, it is a white solid powder, odorless and tasteless. Easy to dissolve in methanol, ethanol, acetone, or chloroform, almost insoluble in water. It is a long-acting antipsychotic drug that is difficult to dissolve in water but has some solubility in acidic aqueous solutions. Moderate density is beneficial for its uniform distribution and stability in the formulation. When preparing solid formulations, density can serve as an important reference for designing drug dosage and formulation form. One of the important indicators for drug purity testing. By measuring the refractive index of a drug, its purity and crystal state can be preliminarily determined. In the process of drug quality control, refractive index data can be used for inter batch comparison and analysis to ensure the consistency and stability of the drug.
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Chemical Formula |
C28H27ClF5NO |
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Exact Mass |
523.17 |
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Molecular Weight |
523.97 |
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m/z |
523.17 (100.0%), 525.17 (32.0%), 524.17 (30.3%), 526.17 (9.7%), 525.18 (4.4%), 527.17 (1.4%) |
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Elemental Analysis |
C, 64.18; H, 5.19; Cl, 6.77; F, 18.13; N, 2.67; O, 3.05 |
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Penfluridol is an oral long-acting antipsychotic drug mainly used to treat schizophrenia and its related symptoms.
Main therapeutic effects
(1) Illusion and delusion:
By blocking the D2 receptor in the central nervous system, the activity of neurotransmitter dopamine is reduced, thereby alleviating or eliminating psychiatric symptoms such as hallucinations and delusions. These symptoms are common positive symptoms in patients with schizophrenia, and pentafluorouracil can effectively control these symptoms and improve the quality of life of patients.
(2) Emotional apathy and delayed thinking:
It has a highly selective antagonistic effect on dopamine D2 receptors in the midbrain limbic system, which can effectively combat behavioral disorders in schizophrenia. For patients with symptoms such as emotional apathy, slow thinking, and reduced speech and movement, it can help alleviate these symptoms and improve their social skills and daily life functions.
(3) Stable condition:
It can effectively control the symptoms of schizophrenia, help stabilize the patient's condition, and prevent the condition from worsening. Through continuous treatment, pentafluoropropane can maintain the mental health status of patients and reduce the adverse effects caused by fluctuations in the condition.
(4) Preventing recurrence:
It has a good anti recurrence effect, mainly due to its longer duration of action. Pentafluorouracil can maintain an effective blood drug concentration for a long time, thereby effectively preventing the recurrence of schizophrenia. For patients with stable conditions, long-term use of pentafluorouracil can significantly reduce the risk of recurrence and decrease social dysfunction caused by the disease.
(5) Improving behavioral abnormalities:
Not only does it treat psychiatric symptoms, but it can also improve patients' behavioral abnormalities. For example, symptoms such as loneliness and withdrawal that may occur in patients with schizophrenia can help alleviate these symptoms and improve their social and self-care abilities.
Applicable population and disease types
1. Applicable population
Schizophrenia patients:
Mainly used to treat schizophrenia, including acute, chronic, and remission patients. For patients with different types of schizophrenia, it has shown good therapeutic effects.
Other psychiatric patients:
In addition to schizophrenia, it is also applicable to other psychiatric patients with positive and/or negative symptoms. For example, for patients with psychotic symptoms such as mania and depression, it can also be used as an adjuvant therapy drug.
2. types of diseases
Acute schizophrenia:
For patients in the acute phase, the condition can be quickly controlled to alleviate their pain. Doctors may increase the dosage to quickly control the condition, and then gradually reduce it to the maintenance dosage.
Chronic schizophrenia:
For patients with chronic schizophrenia, it can be used as a long-term treatment drug to stabilize the condition and prevent recurrence. Through continuous treatment, pentafluorouracil can significantly improve the quality of life and social function of patients.
Schizophrenia remission period:
During the remission period of schizophrenia, it can be used as a maintenance therapy drug to help patients maintain a stable condition. By maintaining treatment, the risk of recurrence can be reduced and social dysfunction caused by the disease can be minimized.
3. Security
Penfluridol is a relatively safe medication, but potential adverse reactions should still be noted during use. Common side effects include inability to sit still, acute muscle tone disorders, and extrapyramidal reactions. In addition, long-term extensive use may also lead to adverse reactions such as delayed onset motor disorders.
When using, medication dosage should be adjusted according to medical advice and potential side effects should be monitored. For patients who experience adverse reactions, doctors will adjust the drug dosage or choose other suitable drugs for alternative treatment based on the specific situation.
Precautions for drug use
Follow the doctor's advice to take medication
When using, patients should strictly follow the doctor's instructions for medication. Doctors will develop personalized treatment plans based on the patient's specific condition (such as severity, age, weight, liver and kidney function, etc.) and inform patients on how to use medication correctly.
Patients should take medication on time and in the appropriate amount, and should not change the dosage or stop taking medication at will. If it is necessary to adjust the dosage of medication or change the treatment plan, it should be done under the guidance of a doctor.
Monitoring drug efficacy and adverse reactions
During use, patients should regularly monitor the efficacy and adverse reactions of the medication. Doctors will evaluate the patient's specific condition and adjust the treatment plan based on the evaluation results.
For patients who experience adverse reactions, doctors will take corresponding treatment measures based on the specific situation, such as adjusting drug dosage, replacing other drugs, etc.
Pay attention to drug interactions
When using, patients should inform their doctors of other medications they are currently taking, including prescription drugs, over-the-counter drugs, herbs, and health supplements. Doctors will assess the risk of drug interactions based on the patient's specific condition and develop corresponding preventive measures.
Avoid driving or operating machinery
During use, patients should avoid tasks that require high concentration, such as driving vehicles or operating machinery. Because pentafluorouracil may have an impact on patients' attention, reaction ability, and increase the risk of accidents.
Regular follow-up
During use, patients should regularly follow up with doctors to promptly understand changes in their condition and adjust treatment plans. The doctor will develop a follow-up plan based on the specific situation of the patient and inform them on how to cooperate with the follow-up work.
Penfluridol, a traditional antipsychotic drug, exhibits antitumor activity in multiple cancers through a multi-target mechanism of action, including AMPK activation, mitochondrial metabolism inhibition, and glycolysis blockade. This "repurposing" strategy not only offers a novel perspective for cancer treatment but also shortens the drug development cycle. Future large-scale clinical trials are needed to determine the optimal dosage, administration regimen, and target patient populations for penfluridol across different tumors. Concurrently, exploring synergistic mechanisms with other anticancer drugs, optimizing combination therapies, and developing novel derivatives or nanomedicines will further enhance efficacy while reducing side effects. Penfluridol holds promise as a model for repurposing existing drugs in oncology, offering patients expanded treatment options.
Prospects for drug development and clinical application
Drug development
With the continuous in-depth research on the pathogenesis of schizophrenia and the emergence of new drugs, their position in clinical application may be affected to some extent. However, due to its unique pharmacological effects and long-term clinical experience, pentafluorolide will still be one of the important drugs for treating schizophrenia.
In the future, drug development may focus more on reducing its side effects and improving its efficacy. By optimizing the drug structure and improving the preparation process, the safety and efficacy of pentafluorolide can be further enhanced.
Clinical application prospects
Despite the continuous emergence of new antipsychotic drugs, they still have broad clinical application prospects. Especially in primary healthcare institutions and remote areas, pentafluoropropane is favored by doctors and patients due to its moderate price and precise efficacy.
In addition, with the increasing awareness of mental illnesses such as schizophrenia, the demand for mental health services in society is also constantly increasing. Therefore, the demand for antipsychotic drugs such as pentafluorouracil in clinical applications will continue to grow.
This substance is an oral long-acting antipsychotic drug mainly used to treat schizophrenia and its related symptoms. By blocking D2 receptors in the central nervous system, it is possible to alleviate or eliminate psychiatric symptoms such as hallucinations and delusions, stabilize the condition, and prevent recurrence. At the same time, pentafluorouracil can improve patients' behavioral abnormalities and social functioning, and enhance their quality of life. When using 5-fluorouracil, patients should strictly follow the doctor's advice, pay attention to monitoring the efficacy and adverse reactions of the drug, and avoid interactions with other drugs. In the future, with the continuous progress of drug development and the expansion of clinical applications, penfluridol is expected to play a more important role in the treatment of mental illnesses such as schizophrenia.
Emerging Roles in Oncology
Anticancer Activity
Recent discoveries position Penfluridol as a potential anticancer agent. In vitro studies demonstrate its cytotoxicity against multiple cancer cell lines, including:
MDA-MB-231 (breast cancer): IC50 values ranging from 2.3–6.1 μM after 24–72 hours of exposure.
Lewis lung carcinoma (LLC): IC50 values of 3.2–6 μM, suggesting efficacy against lung cancer.
NIH/3T3 fibroblasts: IC50 values around 6 μM, indicating selectivity for cancerous over normal cells.
Mechanistically, Penfluridol induces apoptosis and autophagy, disrupting cancer cell survival pathways. It also inhibits TNFα-induced NF-κB activation, a pro-survival signal in tumors. These effects collectively suppress tumor growth and metastasis.
Specific Cancer Applications
Esophageal Cancer: A 2024 patent application highlights Penfluridol's ability to inhibit esophageal cancer cell proliferation, offering a novel therapeutic option for this aggressive malignancy.
Antimicrobial Effects: Penfluridol exhibits antibacterial activity against Enterococcus faecalis (MIC = 7.81 µg/ml), suggesting potential in treating drug-resistant infections, a growing concern in cancer patients.
Frequently Asked Questions
What drugs interact with Penfluridol?
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The notable drug Interactions include: orthostatic hypotension with MAOIs; may increase sedation with alcohol, hypnotics, antihistamines, opiates; antacids containing aluminum salts may decrease absorption; additive antimuscarinic effects with TCAs; may reduce bromocriptine's ability to reduce serum prolactin.
What are the side effects of the drug Penfluridol?
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Penfluridol may cause certain common side effects such as nausea, vomiting, headache, dizziness, and sleepiness. Most of these side effects may not require medical attention and gradually resolve over time. Take Penfluridol as prescribed by your doctor. Do not take Penfluridol if you are pregnant or breastfeeding.
What is another name for Penfluridol?
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Penfluridol is a long-acting antipsychotic medication that has been utilized primarily for the treatment of chronic schizophrenia and other psychotic disorders. It was first introduced in the late 1960s and is known by various trade names such as Semap, Longoperidol, and Micefal.
What is Penfluridol used for?
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Penfluridol is an unusual, potent, long-acting, first-generation, oral antipsychotic agent indicated for the treatment of chronic schizophrenia, acute psychosis, and Tourette syndrome. It may be considered a depot medication, as it is administered once a week.
What is the mechanism of action of penfluridol?
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The mechanism of penfluridol action against the positive symptoms of schizophrenia and other psychotic disorders is thought to be blockade of dopamine receptors, especially to postsynaptic D2 receptor (Figure 1). Penfluridol also acts as a T-type calcium- channel blocker (Kd value ≈ 70–100 nM)
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