Pub Date : 2024-01-18DOI: 10.3390/futurepharmacol4010007
Christian Bailly
The white berry bush, officially Flueggea virosa (Roxb. ex Willd.) Royle is a medicinal plant distributed throughout tropical areas and traditionally used in Africa, India and China. Root decoctions are used to treat abdominal pain, whereas extracts from the aerial parts serve to treat liver and urinary diseases, inflammatory pathologies and diabetes, among other pathologies. Plant extracts have revealed antiparasitic, antimicrobial, antiepilepsy, antidiabetic, anticancer and analgesic effects. Three main categories of phytochemicals were isolated from F. virosa: polyphenols, with the lead product bergenin; terpenoids, such as the flueggenoids and related podocarpane-type diterpenoids; and many alkaloids derived from securinine and norsecurinine. A remarkable feature of S. virosa is the production of norsecurinine oligomers, including macromolecular tetramers and pentamers, such as fluevirosinines. The most potent anticancer alkaloid in the family is the dimeric indolizidine flueggine B, which was identified as a potential binder to α/β-tubulin dimer, which is a known target for securinine. This review highlights the diversity of phytochemicals identified from S. virosa and the potential therapeutic benefits of dimeric alkaloids. Studies are encouraged to further investigate the therapeutic properties of the lead compounds but also define and finesse the nutritional profile of the edible fruit.
{"title":"Traditional Uses, Pharmacology and Phytochemistry of the Medicinal Plant Flueggea virosa (Roxb. ex Willd.) Royle","authors":"Christian Bailly","doi":"10.3390/futurepharmacol4010007","DOIUrl":"https://doi.org/10.3390/futurepharmacol4010007","url":null,"abstract":"The white berry bush, officially Flueggea virosa (Roxb. ex Willd.) Royle is a medicinal plant distributed throughout tropical areas and traditionally used in Africa, India and China. Root decoctions are used to treat abdominal pain, whereas extracts from the aerial parts serve to treat liver and urinary diseases, inflammatory pathologies and diabetes, among other pathologies. Plant extracts have revealed antiparasitic, antimicrobial, antiepilepsy, antidiabetic, anticancer and analgesic effects. Three main categories of phytochemicals were isolated from F. virosa: polyphenols, with the lead product bergenin; terpenoids, such as the flueggenoids and related podocarpane-type diterpenoids; and many alkaloids derived from securinine and norsecurinine. A remarkable feature of S. virosa is the production of norsecurinine oligomers, including macromolecular tetramers and pentamers, such as fluevirosinines. The most potent anticancer alkaloid in the family is the dimeric indolizidine flueggine B, which was identified as a potential binder to α/β-tubulin dimer, which is a known target for securinine. This review highlights the diversity of phytochemicals identified from S. virosa and the potential therapeutic benefits of dimeric alkaloids. Studies are encouraged to further investigate the therapeutic properties of the lead compounds but also define and finesse the nutritional profile of the edible fruit.","PeriodicalId":12592,"journal":{"name":"Future Pharmacology","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2024-01-18","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"139615878","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Pub Date : 2024-01-17DOI: 10.3390/futurepharmacol4010006
T. M. Vieira, Lívia S. Tanajura, V. C. Heleno, Lizandra G. Magalhães, A. E. M. Crotti
Curcumin (or diferuloylmethane), a component of Curcuma longa L. rhizomes, displays various biological and pharmacological activities. However, it is poorly bioavailable and unstable in physiological pH. In this review, we cover papers published between 2019 and 2023 on the synthesis and biological activities of more stable and effective curcumin analogs known as monoketone curcuminoids (MKCs) or “monocarbonyl curcuminoids.” Recent advances in Claisen–Schmidt condensation, the standard procedure to synthesize MKCs, including the use of ionic liquids, are addressed. MKCs’ antimicrobial, anticancer, antioxidant, and antiparasitic actions, as well as other less common MKC biological and pharmacological activities, have been shown to be similar or higher than curcumin. The promising biological and pharmacological activities, combined with the attractive synthetic aspects (e.g., good yields and an easiness of product isolation) to obtain MKCs, make this class of compounds an interesting prospect for further antimicrobial, anticancer, and antiparasitic drug discovery.
{"title":"Monoketone Curcuminoids: An Updated Review of Their Synthesis and Biological Activities","authors":"T. M. Vieira, Lívia S. Tanajura, V. C. Heleno, Lizandra G. Magalhães, A. E. M. Crotti","doi":"10.3390/futurepharmacol4010006","DOIUrl":"https://doi.org/10.3390/futurepharmacol4010006","url":null,"abstract":"Curcumin (or diferuloylmethane), a component of Curcuma longa L. rhizomes, displays various biological and pharmacological activities. However, it is poorly bioavailable and unstable in physiological pH. In this review, we cover papers published between 2019 and 2023 on the synthesis and biological activities of more stable and effective curcumin analogs known as monoketone curcuminoids (MKCs) or “monocarbonyl curcuminoids.” Recent advances in Claisen–Schmidt condensation, the standard procedure to synthesize MKCs, including the use of ionic liquids, are addressed. MKCs’ antimicrobial, anticancer, antioxidant, and antiparasitic actions, as well as other less common MKC biological and pharmacological activities, have been shown to be similar or higher than curcumin. The promising biological and pharmacological activities, combined with the attractive synthetic aspects (e.g., good yields and an easiness of product isolation) to obtain MKCs, make this class of compounds an interesting prospect for further antimicrobial, anticancer, and antiparasitic drug discovery.","PeriodicalId":12592,"journal":{"name":"Future Pharmacology","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2024-01-17","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"139527361","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Pub Date : 2024-01-12DOI: 10.3390/futurepharmacol4010005
B. Covella, M. Giliberti, Adriano Montinaro, Luigi Rossi, Vincenzo Montinaro
Hereditary angioedema (HAE) is a rare disease caused by a genetic alteration of the SERPING1 gene and characterized by recurrent attacks of angioedema that involve the skin, and the mucosae of the gastrointestinal tract and upper airways, which significantly affect the quality of life of patients. Nowadays there are effective drugs for both 1. treating acute attacks and 2. preventing attacks with a long-term prophylaxis. However, there are some unmet needs for HAE treatment, and therefore several novel molecules are under active testing for this clinical condition. Novel drugs will simplify the mode of administration (oral versus parenteral for both on demand treatment or long-term prophylaxis), prolong the interval between administrations (up to 3–6 months of efficacy with a single administration), target more specifically the central enzymes involved in the generation of bradykinin, the ultimate mediator of angioedema (prekallikrein, activated plasma kallikrein or activated factor XII), and potentially determine a definitive cure for the disease by genetic manipulation of the altered gene (SERPING1) or other downstream genes (KLKB1). In this review we provide a panoramic view of all new medications that are under active experimentation and will probably transform and enrich all of the therapeutic armamentarium for treating this disease.
{"title":"Hereditary Angioedema: Novel Molecules for Treatment of Acute Attacks and Long-Term Prophylaxis","authors":"B. Covella, M. Giliberti, Adriano Montinaro, Luigi Rossi, Vincenzo Montinaro","doi":"10.3390/futurepharmacol4010005","DOIUrl":"https://doi.org/10.3390/futurepharmacol4010005","url":null,"abstract":"Hereditary angioedema (HAE) is a rare disease caused by a genetic alteration of the SERPING1 gene and characterized by recurrent attacks of angioedema that involve the skin, and the mucosae of the gastrointestinal tract and upper airways, which significantly affect the quality of life of patients. Nowadays there are effective drugs for both 1. treating acute attacks and 2. preventing attacks with a long-term prophylaxis. However, there are some unmet needs for HAE treatment, and therefore several novel molecules are under active testing for this clinical condition. Novel drugs will simplify the mode of administration (oral versus parenteral for both on demand treatment or long-term prophylaxis), prolong the interval between administrations (up to 3–6 months of efficacy with a single administration), target more specifically the central enzymes involved in the generation of bradykinin, the ultimate mediator of angioedema (prekallikrein, activated plasma kallikrein or activated factor XII), and potentially determine a definitive cure for the disease by genetic manipulation of the altered gene (SERPING1) or other downstream genes (KLKB1). In this review we provide a panoramic view of all new medications that are under active experimentation and will probably transform and enrich all of the therapeutic armamentarium for treating this disease.","PeriodicalId":12592,"journal":{"name":"Future Pharmacology","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2024-01-12","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"139531955","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Pub Date : 2024-01-09DOI: 10.3390/futurepharmacol4010004
I. Maray, Cristina Álvarez-Asteinza, Lola Macia-Rivas, C. L. Fernández-Laguna, Miguel Alaguero-Calero, Pablo Valledor, Javier Fernández
The objective was to evaluate the incidence of nephrotoxicity related to vancomycin and other anti-MRSA antibiotics (linezolid and daptomycin). Patients receiving any of these drugs between July 2014 and December 2020 at a tertiary hospital were included. Renal failure was evaluated using the acute renal injury (AKIN) system. Univariate analysis was conducted on the 5806 patients who were included. Among them, 1023 patients (17.62%) developed renal failure. The renal damage incidence was 14.74% (496/3365) for vancomycin, 19.13% (367/1918) for linezolid, and 30.59% (160/523) for daptomycin. Patients with lower basal glomerular filtration had a higher risk of AKIN. In the vancomycin group, the risk factors were high creatinine and urea serum basal values, duration of treatment (DOT), body mass index (BMI), ICU stay, age, and low CKDEPI and albumin levels. In the linezolid group, AKIN was linked to high creatinine and urea levels, BMI, age, and ICU stay and to low CKDEPI levels; for daptomycin, AKIN was associated with low CKDEPI and albumin levels and a long DOT. Patients with AKIN showed higher mortality rates. Vancomycin-associated nephrotoxicity remains a great concern. However, linezolid and daptomycin could also cause nephrotoxicity. Bearing in mind risk factors that may prompt nephrotoxicity in hospitalized patients taking anti-staphylococcal antibiotics will result in better pharmacotherapeutic management.
{"title":"Real-World Data Study on Risk Factors Associated with Acute Kidney Damage in Patients Treated with Anti-MRSA Antibiotics","authors":"I. Maray, Cristina Álvarez-Asteinza, Lola Macia-Rivas, C. L. Fernández-Laguna, Miguel Alaguero-Calero, Pablo Valledor, Javier Fernández","doi":"10.3390/futurepharmacol4010004","DOIUrl":"https://doi.org/10.3390/futurepharmacol4010004","url":null,"abstract":"The objective was to evaluate the incidence of nephrotoxicity related to vancomycin and other anti-MRSA antibiotics (linezolid and daptomycin). Patients receiving any of these drugs between July 2014 and December 2020 at a tertiary hospital were included. Renal failure was evaluated using the acute renal injury (AKIN) system. Univariate analysis was conducted on the 5806 patients who were included. Among them, 1023 patients (17.62%) developed renal failure. The renal damage incidence was 14.74% (496/3365) for vancomycin, 19.13% (367/1918) for linezolid, and 30.59% (160/523) for daptomycin. Patients with lower basal glomerular filtration had a higher risk of AKIN. In the vancomycin group, the risk factors were high creatinine and urea serum basal values, duration of treatment (DOT), body mass index (BMI), ICU stay, age, and low CKDEPI and albumin levels. In the linezolid group, AKIN was linked to high creatinine and urea levels, BMI, age, and ICU stay and to low CKDEPI levels; for daptomycin, AKIN was associated with low CKDEPI and albumin levels and a long DOT. Patients with AKIN showed higher mortality rates. Vancomycin-associated nephrotoxicity remains a great concern. However, linezolid and daptomycin could also cause nephrotoxicity. Bearing in mind risk factors that may prompt nephrotoxicity in hospitalized patients taking anti-staphylococcal antibiotics will result in better pharmacotherapeutic management.","PeriodicalId":12592,"journal":{"name":"Future Pharmacology","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2024-01-09","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"139442406","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Pub Date : 2024-01-09DOI: 10.3390/futurepharmacol4010003
N. Matsubara, J. E. da Silva-Santos
The administration of the α2-adrenergic receptor agonist clonidine via intracerebroventricular route produces hypotension in pentobarbital-anesthetized rats and pressor responses in conscious normotensive rats. We explored the impact of different anesthetics on the central nervous system-dependent cardiovascular effects of clonidine. Normotensive male Wistar rats with guide cannulas previously implanted in the cerebroventricular system were anesthetized with pentobarbital or ketamine/xylazine and prepared for blood pressure measurement. The animals received intracerebroventricular injections of 10 μg clonidine or 0.6 μg dexmedetomidine, and the effects on the systolic, diastolic, mean arterial pressure, and heart rate were evaluated. The influence of 5 μg yohimbine, a selective α2-adrenergic receptor antagonist, was also assessed. The i.c.v. microinjection of clonidine decreased all three components of systemic arterial pressure and the heart rate of pentobarbital-anesthetized rats. On the other hand, clonidine increased the blood pressure and generated a less intense reduction in the heart rate of ketamine/xylazine-anesthetized rats. The pressor and bradycardic effects of clonidine in ketamine/xylazine-anesthetized animals were reproduced by dexmedetomidine, a more selective α2-adrenergic receptor agonist. Notably, the previous intracerebroventricular injection of yohimbine significantly inhibited the hypertensive effect of clonidine and dexmedetomidine. This study discloses that while normotensive rats anesthetized with pentobarbital show hypotensive responses, the stimulation of α2-adrenergic receptors increases the blood pressure in rats under ketamine/xylazine-induced anesthesia, reproducing the effects seen in conscious normotensive animals. Recognizing the mechanisms involved in these differences may allow us to understand better the final effects of clonidine and other α2-adrenergic receptor agonists in the central nervous system, contributing to the repurposing of these drugs.
{"title":"The Dual Cardiovascular Effect of Centrally Administered Clonidine: A Comparative Study between Pentobarbital- and Ketamine/Xylazine-Anesthetized Rats","authors":"N. Matsubara, J. E. da Silva-Santos","doi":"10.3390/futurepharmacol4010003","DOIUrl":"https://doi.org/10.3390/futurepharmacol4010003","url":null,"abstract":"The administration of the α2-adrenergic receptor agonist clonidine via intracerebroventricular route produces hypotension in pentobarbital-anesthetized rats and pressor responses in conscious normotensive rats. We explored the impact of different anesthetics on the central nervous system-dependent cardiovascular effects of clonidine. Normotensive male Wistar rats with guide cannulas previously implanted in the cerebroventricular system were anesthetized with pentobarbital or ketamine/xylazine and prepared for blood pressure measurement. The animals received intracerebroventricular injections of 10 μg clonidine or 0.6 μg dexmedetomidine, and the effects on the systolic, diastolic, mean arterial pressure, and heart rate were evaluated. The influence of 5 μg yohimbine, a selective α2-adrenergic receptor antagonist, was also assessed. The i.c.v. microinjection of clonidine decreased all three components of systemic arterial pressure and the heart rate of pentobarbital-anesthetized rats. On the other hand, clonidine increased the blood pressure and generated a less intense reduction in the heart rate of ketamine/xylazine-anesthetized rats. The pressor and bradycardic effects of clonidine in ketamine/xylazine-anesthetized animals were reproduced by dexmedetomidine, a more selective α2-adrenergic receptor agonist. Notably, the previous intracerebroventricular injection of yohimbine significantly inhibited the hypertensive effect of clonidine and dexmedetomidine. This study discloses that while normotensive rats anesthetized with pentobarbital show hypotensive responses, the stimulation of α2-adrenergic receptors increases the blood pressure in rats under ketamine/xylazine-induced anesthesia, reproducing the effects seen in conscious normotensive animals. Recognizing the mechanisms involved in these differences may allow us to understand better the final effects of clonidine and other α2-adrenergic receptor agonists in the central nervous system, contributing to the repurposing of these drugs.","PeriodicalId":12592,"journal":{"name":"Future Pharmacology","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2024-01-09","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"139443662","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Pub Date : 2024-01-02DOI: 10.3390/futurepharmacol4010001
Fabrizio Schifano
The end of any year provides an opportunity to reflect on the past, and in particular, the past twelve months [...]
任何一年的结束都为反思过去，特别是过去的十二个月提供了机会 [...]
{"title":"2023: The Best Year Ever for Future Pharmacology (and Even Better Years to Come)","authors":"Fabrizio Schifano","doi":"10.3390/futurepharmacol4010001","DOIUrl":"https://doi.org/10.3390/futurepharmacol4010001","url":null,"abstract":"The end of any year provides an opportunity to reflect on the past, and in particular, the past twelve months [...]","PeriodicalId":12592,"journal":{"name":"Future Pharmacology","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2024-01-02","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"139390624","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Pub Date : 2023-12-04DOI: 10.3390/futurepharmacol3040057
R. Payan-Carreira
Feline population control remains a concern as to whether it is intended for the short- or long-term. Induced sterilization of felids is critical in the case of feral, free-roaming cats, or the management of wild populations in Zoos or sanctuaries. This narrative review explores the shifting paradigm in induced sterilization methods, driven by the development of gene editing approaches recently applied to control felid reproductive activity. Although gene therapy approaches have gained attention as alternatives to more traditional methods, their clinical applications remain in the realm of thought. The objective of this study was to provide a comprehensive overview of the current state and most recent advances in gene-based contraception options, consolidate current research and evidence, and share some considerations on its potential effectiveness, advantages or limitations, and implications for animal welfare and population control strategies. Gene-based contraception therapy tested in felines, targeting the AMH pathway, was unable to suppress the estrous cycle and follicular development. However, at an experimental level, preliminary results hint at the need to change towards different molecular targets. Moreover, their side effects remain largely unknown, and several questions remain unanswered, such as the regularity of treatment applications or cost.
{"title":"Gene-Based Therapy: A New Approach to Feline Induced Sterilization?","authors":"R. Payan-Carreira","doi":"10.3390/futurepharmacol3040057","DOIUrl":"https://doi.org/10.3390/futurepharmacol3040057","url":null,"abstract":"Feline population control remains a concern as to whether it is intended for the short- or long-term. Induced sterilization of felids is critical in the case of feral, free-roaming cats, or the management of wild populations in Zoos or sanctuaries. This narrative review explores the shifting paradigm in induced sterilization methods, driven by the development of gene editing approaches recently applied to control felid reproductive activity. Although gene therapy approaches have gained attention as alternatives to more traditional methods, their clinical applications remain in the realm of thought. The objective of this study was to provide a comprehensive overview of the current state and most recent advances in gene-based contraception options, consolidate current research and evidence, and share some considerations on its potential effectiveness, advantages or limitations, and implications for animal welfare and population control strategies. Gene-based contraception therapy tested in felines, targeting the AMH pathway, was unable to suppress the estrous cycle and follicular development. However, at an experimental level, preliminary results hint at the need to change towards different molecular targets. Moreover, their side effects remain largely unknown, and several questions remain unanswered, such as the regularity of treatment applications or cost.","PeriodicalId":12592,"journal":{"name":"Future Pharmacology","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2023-12-04","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"138604363","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Pub Date : 2023-12-01DOI: 10.3390/futurepharmacol3040054
Andrea Miuli, Carlotta Marrangone, Ornella Di Marco, A. Pasino, G. Stigliano, A. Mosca, M. Pettorruso, Fabrizio Schifano, Giovanni Martinotti
This case report was conducted by searching for the following keywords on PubMed: High Functioning Autism, Autism Spectrum Disorder, cariprazine, aripiprazole, partial agonist antipsychotic, DRD2/DRD3. High Functioning Autism (HFA) is a neurodevelopmental disorder characterized by the core symptoms of autism spectrum disorder (ASD) with average intellectual abilities, behavioral symptoms such as irritability, hyperactivity, aggressiveness and mood symptoms. HFA is not a term used in the Diagnostic and Statistical Manual of mental disorders (DSM), but it is commonly used to identify patients diagnosed with Autistic Disorder (AD) or Pervasive Developmental Disorder-Not Otherwise Specified (PDD-NOS) with average or above average intellectual abilities. Several factors are involved in HFA development, including environmental and genetic factors. In particular, over the last several decades, dopaminergic signaling system dysfunction has been highlighted as being responsible for behavioral patterns. Nowadays, symptoms of ASD lack a specific pharmacological treatment. The only medications approved by the Food and Drug Administration (FDA) for symptoms associated with ASD, in particular the irritability, are risperidone and aripiprazole. According to the hypothesis that dopamine receptor DRD2 and DRD3 might be involved in impulsive behavior, stereotypy, repetitive behaviors and language impairment, cariprazine could be a therapeutic option. This molecule is primarily characterized by DRD3 partial agonism and serotonin 5-HT1A partial agonism, with a lower ability to activate DRD2 than other third-generation antipsychotics, such as aripiprazole. We have reported here a case study of treatment of HFA with cariprazine.
{"title":"Could Cariprazine Be a Possible Choice for High Functioning Autism? A Case Report","authors":"Andrea Miuli, Carlotta Marrangone, Ornella Di Marco, A. Pasino, G. Stigliano, A. Mosca, M. Pettorruso, Fabrizio Schifano, Giovanni Martinotti","doi":"10.3390/futurepharmacol3040054","DOIUrl":"https://doi.org/10.3390/futurepharmacol3040054","url":null,"abstract":"This case report was conducted by searching for the following keywords on PubMed: High Functioning Autism, Autism Spectrum Disorder, cariprazine, aripiprazole, partial agonist antipsychotic, DRD2/DRD3. High Functioning Autism (HFA) is a neurodevelopmental disorder characterized by the core symptoms of autism spectrum disorder (ASD) with average intellectual abilities, behavioral symptoms such as irritability, hyperactivity, aggressiveness and mood symptoms. HFA is not a term used in the Diagnostic and Statistical Manual of mental disorders (DSM), but it is commonly used to identify patients diagnosed with Autistic Disorder (AD) or Pervasive Developmental Disorder-Not Otherwise Specified (PDD-NOS) with average or above average intellectual abilities. Several factors are involved in HFA development, including environmental and genetic factors. In particular, over the last several decades, dopaminergic signaling system dysfunction has been highlighted as being responsible for behavioral patterns. Nowadays, symptoms of ASD lack a specific pharmacological treatment. The only medications approved by the Food and Drug Administration (FDA) for symptoms associated with ASD, in particular the irritability, are risperidone and aripiprazole. According to the hypothesis that dopamine receptor DRD2 and DRD3 might be involved in impulsive behavior, stereotypy, repetitive behaviors and language impairment, cariprazine could be a therapeutic option. This molecule is primarily characterized by DRD3 partial agonism and serotonin 5-HT1A partial agonism, with a lower ability to activate DRD2 than other third-generation antipsychotics, such as aripiprazole. We have reported here a case study of treatment of HFA with cariprazine.","PeriodicalId":12592,"journal":{"name":"Future Pharmacology","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2023-12-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"138620581","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Pub Date : 2023-12-01DOI: 10.3390/futurepharmacol3040056
Antonia Stamatiou, T. Nguyen-Ngoc, Laureline Wetterwald, Ana Dolcan, Giovanni Dei Tos, S. Cherix, Patrick Omoumi, A. Digklia
Tenosynovial giant cell tumor (TGCT) is a rare and locally aggressive benign tumor arising from the synovium of joints, bursae, and tendon sheaths. It is classified into localized (L-TGCT) and diffuse (D-TGCT) forms based on the extent of involvement. Surgical resection is the primary treatment, though achieving a definitive cure remains challenging due to the high recurrence rates, especially in D-TGCT. Systemic therapies targeting the CSF1-CSF1R axis have emerged as promising treatment options. CSF1R tyrosine kinase inhibitors (TKIs) such as imatinib, nilotinib, pexidartinib, and vimseltinib, alongside anti-CSF1R antibodies like emactuzumab, cabiralizumab, and lacnotuzumab, have shown encouraging results in managing TGCT, particularly when surgery is not feasible or poses significant morbidity. Other potential therapies, including local treatments and anti-inflammatory drugs, are being explored for TGCT management. This review provides an overview of systemic treatment options for D-TGCT, highlighting emerging therapeutic modalities and their potential implications. Effective management is crucial due to TGCT’s significant morbidity despite its non-life-threatening nature, necessitating novel approaches to improve patient prognosis and quality of life.
{"title":"Overview of Pharmacological Therapies for Diffuse Tenosynovial Giant Cell Tumor","authors":"Antonia Stamatiou, T. Nguyen-Ngoc, Laureline Wetterwald, Ana Dolcan, Giovanni Dei Tos, S. Cherix, Patrick Omoumi, A. Digklia","doi":"10.3390/futurepharmacol3040056","DOIUrl":"https://doi.org/10.3390/futurepharmacol3040056","url":null,"abstract":"Tenosynovial giant cell tumor (TGCT) is a rare and locally aggressive benign tumor arising from the synovium of joints, bursae, and tendon sheaths. It is classified into localized (L-TGCT) and diffuse (D-TGCT) forms based on the extent of involvement. Surgical resection is the primary treatment, though achieving a definitive cure remains challenging due to the high recurrence rates, especially in D-TGCT. Systemic therapies targeting the CSF1-CSF1R axis have emerged as promising treatment options. CSF1R tyrosine kinase inhibitors (TKIs) such as imatinib, nilotinib, pexidartinib, and vimseltinib, alongside anti-CSF1R antibodies like emactuzumab, cabiralizumab, and lacnotuzumab, have shown encouraging results in managing TGCT, particularly when surgery is not feasible or poses significant morbidity. Other potential therapies, including local treatments and anti-inflammatory drugs, are being explored for TGCT management. This review provides an overview of systemic treatment options for D-TGCT, highlighting emerging therapeutic modalities and their potential implications. Effective management is crucial due to TGCT’s significant morbidity despite its non-life-threatening nature, necessitating novel approaches to improve patient prognosis and quality of life.","PeriodicalId":12592,"journal":{"name":"Future Pharmacology","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2023-12-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"138624338","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Pub Date : 2023-12-01DOI: 10.3390/futurepharmacol3040055
Eduardo Ladeia Leal, Paulo Caleb Júnior Lima Santos, T. S. Gonçalves, Mariana Martins Gonzaga Nascimento, Fábio Cardoso Cruz, Flávia Borelli Gomes do Nascimento, Carolina Paula Jesus Kasa
As one of the leading causes of death in childhood, cancer also causes discomfort to pediatric patients. Even with guidelines for pain management, more than half of hospitalized children have intense and unrelieved pain. The present work aims to describe the intensity of pain and its pharmacological management in a pediatric oncology population. Patients aged 0 to 17 years old, diagnosed with cancer, who were admitted to a children’s oncology hospital and had well-documented data on pain management in their medical records were included. A total of 333 patients were included, mostly male (55.8%) with a mean age of 7.9 years. A substantial portion of the patient cohort (51.4%) initially reported experiencing pain of moderate intensity during the first assessment. Subsequently, following the pharmacological intervention, a significant proportion of patients (90.1%) reported complete alleviation of pain. The predominant pharmaceutical agents utilized for pain management encompassed metamizole (76.6%) and morphine (10.2%). All pharmacological interventions used were able to significantly reduce patients’ pain. This study underscores the utilization of different pharmacological classes to achieve notable reductions in pain intensity among patients grappling with severe pain.
{"title":"Evaluations of NSAIDs and Opioids as Analgesics in Pediatric Oncology","authors":"Eduardo Ladeia Leal, Paulo Caleb Júnior Lima Santos, T. S. Gonçalves, Mariana Martins Gonzaga Nascimento, Fábio Cardoso Cruz, Flávia Borelli Gomes do Nascimento, Carolina Paula Jesus Kasa","doi":"10.3390/futurepharmacol3040055","DOIUrl":"https://doi.org/10.3390/futurepharmacol3040055","url":null,"abstract":"As one of the leading causes of death in childhood, cancer also causes discomfort to pediatric patients. Even with guidelines for pain management, more than half of hospitalized children have intense and unrelieved pain. The present work aims to describe the intensity of pain and its pharmacological management in a pediatric oncology population. Patients aged 0 to 17 years old, diagnosed with cancer, who were admitted to a children’s oncology hospital and had well-documented data on pain management in their medical records were included. A total of 333 patients were included, mostly male (55.8%) with a mean age of 7.9 years. A substantial portion of the patient cohort (51.4%) initially reported experiencing pain of moderate intensity during the first assessment. Subsequently, following the pharmacological intervention, a significant proportion of patients (90.1%) reported complete alleviation of pain. The predominant pharmaceutical agents utilized for pain management encompassed metamizole (76.6%) and morphine (10.2%). All pharmacological interventions used were able to significantly reduce patients’ pain. This study underscores the utilization of different pharmacological classes to achieve notable reductions in pain intensity among patients grappling with severe pain.","PeriodicalId":12592,"journal":{"name":"Future Pharmacology","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2023-12-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"138627424","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
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