Comparative Pharmacology of Δ9-Tetrahydrocannabinol and its Metabolite, 11-OH-Δ9-Tetrahydrocannabinol

Lemberger, Louis; Martz, Robert; Rodda, Bruce E.; Forney, Robert B.; Rowe, Howard

doi:10.1172/jci107431

Cited by 80 publications

(42 citation statements)

References 13 publications

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“…The time profile of the pharmacodynamic effects was more similar to the concentration curve of 11-OH-THC than that of THC. A previous study reported that 11-OH-THC induced a quicker onset of the pharmacodynamic effects compared with THC [34][35][36]. These results in this study are quite promising for a fast onset of the clinical effects in a patient population, although future studies should carefully investigate the relation between pharmacodynamic effects in healthy volunteers and clinical effects in patients.…”

Section: Pharmacodynamicsmentioning

confidence: 53%

“…Preclinical studies have found 11-OH-THC to be a highly potent CB1-agonist [14,15], and clinical studies also reported more rapid and larger effects after 11-OH-THC administration compared with THC [34][35][36]. In itself, this would have allowed us to predict the pharmacodynamic effects of higher doses in panel II, by reference to the results of other oral THC formulations in the literature which also produce high concentrations of 11-OH-THC.…”

Section: Pharmacodynamicsmentioning

confidence: 99%

See 1 more Smart Citation

Novel Δ9-tetrahydrocannabinol formulation Namisol® has beneficial pharmacokinetics and promising pharmacodynamic effects

Klumpers

Beumer

Hasselt

et al. 2011

British Journal of Clinical Pharmacology

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Section: Pharmacodynamicsmentioning

confidence: 53%

Section: Pharmacodynamicsmentioning

confidence: 99%

Novel Δ9-tetrahydrocannabinol formulation Namisol® has beneficial pharmacokinetics and promising pharmacodynamic effects

Klumpers

Beumer

Hasselt

et al. 2011

British Journal of Clinical Pharmacology

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“…One metabolite of 9-THC -11-OH-THC-has psychoactive effects by its own if injected pure intravenously, observing faster and stronger psychoactive effects than after the administration of 9-THC (Lemberger, Martz, Rodda, Forney, and Rowe, 1973). …”

Section: ) Naturally Present Cannabinoids Affecting Cannabis Psycho mentioning

confidence: 99%

Constituyentes psicoactivos del cannabis y sus implicaciones clínicas: una revisión sistemática

et al. 2018

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Objective This systematic review aims to summarize current evidence on which naturally present cannabinoids contribute to cannabis psychoactivity, considering their reported concentrations and pharmacodynamics in humans.Design Following PRISMA guidelines, papers published before March 2016 in Medline, Scopus-Elsevier, Scopus, ISI-Web of Knowledge and COCHRANE, and fulfilling established a-priori selection criteria have been included. ResultsIn 40 original papers, three naturally present cannabinoids and one human metabolite (11-OH-THC) had clinical relevance.Of these, the metabolite produces the greatest psychoactive effects. Cannabidiol (CBD) is not psychoactive but plays a modulating role on cannabis psychoactive effects. The proportion of 9-THC in plant material is higher (up to 40%) than in other cannabinoids (up to 9%). Pharmacodynamic reports vary due to differences in methodological aspects (doses, administration route and volunteers' previous experience with cannabis). (CBD) no es psicoactivo, pero sí ejerce un efecto modulador sobre los efectos psicoactivos del cannabis. La concentración 9-THC en derivados cannábicos (hasta 40%) supera en gran medida la de otros cannabinoides (hasta 9%). La farmacodinamia descrita varía, dada la heterogeneidad en aspectos clave de la metodología (dosis, rutas de administración y experiencia previa con cannabis de los participantes). ConclusionsConclusiones Los resultados evidencian que el 9-THC es el cannabinoide que más contribuye al efecto psicoactivo del cannabis.Otros cannabinoides psicoactivos contribuirían mínimamente, dada su menor potencia psicoactiva y su baja concentración en los derivados cannábicos. La falta de estándares metodológicos dificulta el avance en los conocimientos sobre los efectos del cannabis en la salud. Establecer una unidad estándar de cannabis basada en 9-THC ayudaría a superar estas limitaciones.

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“…This is readily detectable in plasma, faeces and urine of users and even non-users that are exposed [16,17]. 11-OH-THC levels peak later than THC levels after cannabis exposure [16,[18][19][20][21]. Metabolism of 11-OH-THC yields 11-nor-9-carboxy-delta-9-tetrahydrocannabinol (THC-COOH) which is non-psychoactive, but its long half-life of about 140 hours makes it a common biomarker in urine testing for cannabis use.…”

Section: Pharmacokinetic and Pharmacodynamic Considerationsmentioning

confidence: 99%

Does "Hotboxing?" Get You High and Can You Test Positive? - A Brief Review of Second-Hand Cannabis Exposure, Intoxication and Urine Drug Screens

Gnanasegaram¹,

Ganpat²,

Stanciu³

2017

J Alcohol Drug Depend

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Cannabis use is on the rise with higher and higher potencies of marijuana being cultivated. Current legislatures make it easier, and legal, for users to use, especially around nonusers. When such second-hand smoke occurs in poorly ventilated confinements, nonusers may inhale some of the smoke, resulting in absorption of cannabinoids. Some degree of intoxication may occur but most importantly, detectable levels of the drug in blood and urine. Often screening is used by employers, law enforcement agencies, physicians and substance abuse providers. Clinicians hence need to be mindful of such factors when patients deny use despite positive tests. Here we review available evidence, with emphasis on current data based on today's trends.Clinical background: "I have not smoked marijuana since before I was drafted" 23 year-old NFL player Josh Gordon stated as his explanation for testing positive above the 15 ng/mL THC threshold the NFL considers a failed test. In his appeal he stated he was around individuals using marijuana. His "A" sample tested at 16 ng/mL and his "B" sample tested at 13.63 ng/mL. The two should be consistent since it comes from the same specimen. His legal team was able to dispute the results and reduce his sentence to 8 months as he was the "victim of breathing second hand smoke" (ESPN, 2014).

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Comparative Pharmacology of Δ9-Tetrahydrocannabinol and its Metabolite, 11-OH-Δ9-Tetrahydrocannabinol

Cited by 80 publications

References 13 publications

Novel Δ9-tetrahydrocannabinol formulation Namisol® has beneficial pharmacokinetics and promising pharmacodynamic effects

Novel Δ9-tetrahydrocannabinol formulation Namisol® has beneficial pharmacokinetics and promising pharmacodynamic effects

Constituyentes psicoactivos del cannabis y sus implicaciones clínicas: una revisión sistemática

Does "Hotboxing?" Get You High and Can You Test Positive? - A Brief Review of Second-Hand Cannabis Exposure, Intoxication and Urine Drug Screens

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