methoxsalen
Sources réglementaires consultées
Indications approuvées
- Contrôle symptomatique du psoriasis sévère, récalcitrant et invalidant ne répondant pas suffisamment aux autres traitements, avec UVA contrôlés et diagnostic étayé par biopsie.
Contre-indications
Absolues
- Réaction idiosyncrasique aux psoralènes, maladie photosensible, mélanome actuel ou antérieur, carcinome épidermoïde invasif ou aphakie.
Mises en garde cliniques
- Mise en garde majeure · Utilisation réservée aux spécialistes de la PUVA. Les risques majeurs sont les brûlures graves, les cataractes, le photovieillissement et les cancers cutanés, dont le mélanome. Ne pas s’exposer volontairement au soleil pendant les 24 heures précédant la prise. Pendant l’exposition aux UVA, protéger les organes génitaux masculins non atteints et les zones sensibles jusqu’au bronzage. Porter des lunettes enveloppantes absorbant les UVA pendant 24 heures, éviter le soleil au moins 8 heures et ne pas s’exposer volontairement pendant 48 heures après ; surveillance cutanée à vie. — DailyMed methoxsalen capsules set ID a6ec8292-9189-4ebd-862a-e1725eb29eef
Interactions médicamenteuses
- SévèreMédicaments photosensibilisants
Mécanisme: Ils peuvent augmenter les réactions phototoxiques sous PUVA.
Recommandation: Redoubler de prudence, ajuster la dosimétrie UVA et maintenir une surveillance étroite en cas d’utilisation d’anthraline, de goudron, de griséofulvine, de phénothiazines, de quinolones, de sulfamides, de tétracyclines ou de thiazidiques.
https://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?setid=a6ec8292-9189-4ebd-862a-e1725eb29eef
Effets indésirables
Communs (≥1%)
Nausées · Prurit sous PUVA · Érythème après PUVA
Rares mais graves
Brûlure phototoxique grave · Cataracte ou cancer cutané
Grossesse et allaitement
N’utiliser pendant la grossesse qu’en cas de nécessité manifeste. Pendant l’allaitement, arrêter soit le méthoxsalène, soit l’allaitement.
Bibliographie récente (PubMed)
Alzheimer's disease (AD) presents a growing global health concern. In recent decades, natural and synthetic chromenone have emerged as promising drug candidates due to their multi-target potential. Natural chromenone, quercetin, scopoletin, esculetin, coumestrol, umbelliferone, bergapten, and methoxsalen (xanthotoxin), and synthetic chromenone hybrids comprising structures like acridine, 4-aminophenyl, 3-arylcoumarins, quinoline, 1,3,4-oxadiazole, 1,2,3-triazole, and tacrine, have been explored for their potential to combat AD. Key reactions used for synthesis of chromenone hybrids include Perkin and Pechmann condensation. The activity of chromenone hybrids has been reported against several drug targets, including AChE, BuChE, BACE-1, and MAO-A/B. This review comprehensively explores natural, semisynthetic, and synthetic chromenone, elucidating their synthetic routes, possible mode of action/drug targets and structure-activity relationships (SAR). The acquired knowledge provides valuable insights for the development of new chromenone hybrids against AD.
We aimed to summarize the cancer risk among patients with indication of group I pharmaceuticals as stated in monographs presented by the International Agency for Research on Cancer working groups. Following the PRISMA guidelines, a comprehensive literature search was conducted using the PubMed database. Pharmaceuticals with few studies on cancer risk were identified in systematic reviews; those with two or more studies were subjected to meta-analysis. For the meta-analysis, a random-effects model was used to calculate the summary relative risks (SRRs) and 95% confidence intervals (95% CIs). Heterogeneity across studies was presented using the Higgins I square value from Cochran's Q test. Among the 12 group I pharmaceuticals selected, three involved a single study [etoposide, thiotepa, and mustargen + oncovin + procarbazine + prednisone (MOPP)], seven had two or more studies [busulfan, cyclosporine, azathioprine, cyclophosphamide, methoxsalen + ultraviolet (UV) radiation therapy, melphalan, and chlorambucil], and two did not have any studies [etoposide + bleomycin + cisplatin and treosulfan]. Cyclosporine and azathioprine reported increased skin cancer risk (SRR = 1.32, 95% CI 1.07-1.62; SRR = 1.56, 95% CI 1.25-1.93) compared to non-use. Cyclophosphamide increased bladder and hematologic cancer risk (SRR = 2.87, 95% CI 1.32-6.23; SRR = 2.43, 95% CI 1.65-3.58). Busulfan increased hematologic cancer risk (SRR = 6.71, 95% CI 2.49-18.08); melphalan was associated with hematologic cancer (SRR = 4.43, 95% CI 1.30-15.15). In the systematic review, methoxsalen + UV and MOPP were associated with an increased risk of skin and lung cancer, respectively. Our results can enhance persistent surveillance of group I pharmaceutical use, establish novel clinical strategies for patients with indications, and provide evidence for re-categorizing current group I pharmaceuticals into other groups.
Natural products have always served as an important source of drugs for treating various diseases. Among various privileged natural product scaffolds, the benzopyrone class of compounds has a substantial presence among biologically active compounds. One of the pioneering anticoagulant drugs, warfarin approved in 1954 bears a benzo-α-pyrone (coumarin) nucleus. The widely investigated psoriasis drugs, methoxsalen, and trioxsalen, also contain a benzo-α-pyrone nucleus. Benzo-γ-pyrone (chromone) containing drugs, cromoglic acid, and pranlukast were approved as treatments for asthma in 1982 and 2007, respectively. Numerous other small molecules with a benzopyrone core are under clinical investigation. The present review discusses the discovery, absorption, distribution, metabolism, excretion properties, and synthetic approaches for the Food and Drug Administration-approved and clinical-stage benzopyrone class of compounds. The role of the pyrone core in biological activity has also been discussed. The present review unravels the potential of benzopyrone core in medicinal chemistry and drug development.