CBD
CannabinoidesC42-[(1R,6R)-3-methyl-6-prop-1-en-2-ylcyclohex-2-en-1-yl]-5-pentylbenzene-1,3-diol
Estructura molecular
Datos: PubChem CID 644019 — National Library of Medicine
Efectos
Mecanismo de acción
El mecanismo exacto no está completamente elucidado. Actúa sobre receptores cannabinoides CB1 (modulador alostérico negativo) y CB2 (agonista inverso). Es agonista del receptor 5-HT1A serotoninérgico. Inhibe la recaptación de anandamida (endocannabinoide). Antagonista del receptor GPR55. Agonista de receptores TRPV1 y PPAR-γ. Modula canales de calcio y sodio.
Vida media
Vida media de eliminación de 18-32 horas por vía oral. Altamente lipofílico, se acumula en tejido adiposo con administración repetida. La vida media efectiva puede ser más larga con uso crónico.
Toxicidad
In prelicensure studies, serum aminotransferase elevations arose during cannabidiol therapy for epilepsy in 34% to 47% of patients compared to 18% of controls who were receiving other anticonvulsant medications. Elevations above 3 times ULN occurred in 13% of cannabidiol treated compared to 1% on placebo. ALT and AST elevations were more frequent with higher doses and were particularly common (and sometimes delayed) in patients who were receiving valproate and clobazam. The aminotransferase elevations typically arose within the first two months of treatment and were transient, mild-to-moderate in severity, and not associated with symptoms or jaundice. There have been no convincing reports of clinically apparent liver injury with jaundice attributable to prescription forms of cannabidiol, but it has had very limited general use. There have been few studies of liver test abnormalities during therapy with lower doses of CBD or with commercially available, over-the-counter CBD products. In doses between 200 and 400 mg daily, mild-to-moderate serum aminotransferase elevations have occasionally been reported, but there have been no reports of clinically apparent liver injury. Furthermore, liver injury arising in persons taking supplements with CBD must also consider the possibility of contaminants in the products or other herbal and dietary supplement use. Likelihood score: E* (unproven but suspected rare cause of clinically apparent liver injury, particularly with high doses). Drug Induced Liver Injury Rank (DILIrank 2.0) Cannabidiol
Farmacología
Cannabinoide no psicoactivo con perfil farmacológico complejo. Aprobado (como Epidiolex) para epilepsias refractarias (Lennox-Gastaut, Dravet). Propiedades antiinflamatorias, ansiolíticas y antipsicóticas en estudios preclínicos. No produce euforia ni dependencia. Interacciones farmacológicas significativas como inhibidor de CYP3A4 y CYP2C19.
Efectos en el organismo
Farmacocinética
Vida media de eliminación de 18-32 horas por vía oral
1-4 horas
6-12 horas
15-45 minutos (sublingual), 30-90 minutos (oral)
6-19% (oral), hasta 31% (inhalado)
Hígado (CYP3A4, CYP2C19)
Fecal (principal), renal (secundaria)
20-30 L/kg
Cronología farmacocinética
Riesgos para la salud — Calculadora de dosis
Advertencias
- Consultar con médico si se toman otros medicamentos (interacciones CYP450)
- Monitorizar función hepática con uso prolongado a dosis altas
Combinaciones peligrosas
Riesgo Individual (IPRS)
Bajo
IPRS v4 · escalar normalizado [0, 1]
BajoModelo IPRS calculado: 20 de octubre de 2018
Fuentes de datos de dosificación
Los rangos de dosificación fueron compilados a partir de Goodman & Gilman's (14ª ed.), Rang & Dale (9ª ed.) y publicaciones indexadas en PubMed. Los valores representan promedios poblacionales para la vía de administración principal y no consideran variabilidad individual, tolerancia, peso corporal ni interacciones.