Pharmacokinetics, metabolism and drug-abuse potential of nabilone

Lemberger, Louis; Rubin, Alan; Wolen, Robert L.; DeSante, Karl A.; Rowe, Howard; Forney, Robert B.; Pence, P. J.

doi:10.1016/s0305-7372(82)80031-5

Cited by 51 publications

(34 citation statements)

References 7 publications

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“…31 One laboratory study showed that the euphoric effects of single doses of intravenously (0.25 mg) and orally (2 mg) administered nabilone were less pronounced than for $ 9 -THC (17.5 mg oral and 2.2 mg intravenous). 33 Similarly, another laboratory study showed that smoked cannabis (1.83% $ 9 -THC), but not 2 mg oral nabilone, increased elation factor scores on the Profile of Mood States. 34 In the present study, however, a range of doses of nabilone administered to regular cannabis users generated positive self-reported effects such as good drug effects and like the drug effects, comparable to what has been demonstrated for oral $ 9 -THC and smoked cannabis.…”

Section: Discussionmentioning

confidence: 95%

“…Clinical studies that have tested nabilone for therapeutic indications suggest that it does not typically engender positive mood effects in nonYcannabis users. 28Y32 Two studies in cannabis users suggest also that nabilone is less effective than $ 9 -THC at enhancing mood 33 and that nabilone is less reinforcing than $ 9 -THC and smoked cannabis, 34 although these laboratory studies have tested only single doses.…”

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confidence: 99%

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Substitution Profile of the Cannabinoid Agonist Nabilone in Human Subjects Discriminating Δ9-Tetrahydrocannabinol

Lile

Kelly²,

Hays³

2010

Clinical Neuropharmacology

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These data demonstrate that the interoceptive effects of nabilone are similar to Δ-THC in cannabis users. The overlap in their behavioral effects is likely due to their shared mechanism as CB1 receptor agonists. Given the relative success of agonist replacement therapy to manage opioid, tobacco, and stimulant dependence, these results also support the evaluation of nabilone as a potential medication for cannabis-use disorders.

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Section: Discussionmentioning

confidence: 95%

mentioning

confidence: 99%

Substitution Profile of the Cannabinoid Agonist Nabilone in Human Subjects Discriminating Δ9-Tetrahydrocannabinol

Lile

Kelly²,

Hays³

2010

Clinical Neuropharmacology

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“…However, after intravenous tracer administration, the disappearance of total radioactivity, parent nabilone and the alcohol metabolite was biphasic, with the first phase (half-life approximately 10 min) attributed to distribution into tissue and the slower phase to elimination (61,63).…”

Section: Distributionmentioning

confidence: 99%

Pharmacokinetics of Cannabinoids

McGilveray

2005

Pain Research and Management

166

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Delta-9-tetrahydrocannabinol (∆-9-THC) is the main psychoactive ingredient of cannabis (marijuana). The present review focuses on the pharmacokinetics of THC, but also includes known information for cannabinol and cannabidiol, as well as the synthetic marketed cannabinoids, dronabinol (synthetic THC) and nabilone. The variability of THC in plant material (0.3% to 30%) leads to variability in tissue THC levels from smoking, which is, in itself, a highly individual process. THC bioavailability averages 30%. With a 3.55% THC cigarette, a peak plasma level of 152±86.3 ng/mL occured approximately 10 min after inhalation. Oral THC, on the other hand, is only 4% to 12% bioavailable and absorption is highly variable. THC is eliminated from plasma in a multiphasic manner, with low amounts detectable for over one week after dosing. A major active 11-hydroxy metabolite is formed after both inhalation and oral dosing (20% and 100% of parent, respectively). THC is widely distributed, particularly to fatty tissues, but less than 1% of an administered dose reaches the brain, while the spleen and body fat are long-term storage sites. The elimination of THC and its many metabolites (from all routes) occurs via the feces and urine. Metabolites persist in the urine and feces for several weeks. Nabilone is well absorbed and the pharmacokinetics, although variable, appear to be linear from oral doses of 1 mg to 4 mg (these doses show a plasma elimination half-life of approximately 2 h). As with THC, there is a high first-pass effect, and the feces to urine ratio of excretion is similar to other cannabinoids. Pharmacokineticpharmacodynamic modelling with plasma THC versus cardiac and psychotropic effects show that after equilibrium is reached, the intensity of effect is proportional to the plasma THC profile. Clinical trials have found that nabilone produces less tachycardia and less euphoria than THC for a similar antiemetic response.Key Words: Cannabinoids; Inhalation; Nabilone; Pharmacodynamics; Pharmacokinetics Pharmacocinétique des cannabinoïdesLe delta-9-tétrahydrocannabinol (∆-9-THC) est le principal ingrédient psychoactif du cannabis (marijuana). Le présent article de synthèse s'attarde à la pharmacocinétique du THC, mais inclut également des données sur le cannabinol et le cannabidiol, de même que sur les cannabinoïdes de synthèse sur le marché, soit le dronabinol (THC synthétique) et le nabilone. La variabilité des taux de THC dans la substance végétale (0,3 % à 30 %) donne lieu à des taux tissulaires variables de THC après l'inhalation, qui en soi, est déjà un processus hautement individuel. La biodisponibilité du THC est en moyenne de 30 %. Avec une cigarette dont la teneur en THC est de 3,55 % un pic plasmatique de 152 ± 86,3 ng/mL s'obtient environ 10 minutes après l'inhalation. D'autre part, le THC oral n'est biodisponible que dans une proportion de 4 à 12 % et son absorption est très variable. Le THC est éliminé du plasma de façon multiphasique, de faibles quantités étant décelables encore dans les sept jours suivant ...

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“…Utilizing pseudoscientific labeling that recalled the Periodic Table of The Current Armamentarium At the time of this writing, there are two FDAapproved cannabinoid drugs available for prescription in the United States: dronabinol, a synthetic THC compound, and nabilone, a semisynthetic analog of THC approximately 10 times more potent than dronabinol. 4 Both are approved for chemotherapy-associated nausea and vomiting; dronabinol is also approved for HIVassociated anorexia/wasting, although the evidence for the latter indication is slim and the problem is much rarer since the advent of antiretroviral drugs. Both dronabinol and nabilone have been studied as possible treatments for other symptoms; although each has shown some efficacy as an adjuvant analgesic, the sedating and psychotropic properties of both agents tend to limit their utility.…”

Section: Definition Of Termsmentioning

confidence: 99%

Cannabinoids in Medical Practice

Strouse¹

2016

Alternative and Complementary Therapies

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Many patients with chronic medical illnesses use cannabinoids. There are two FDA-approved cannabinoid products, whereas medical marijuana purchased at legal dispensaries is not FDA regulated and may contain uncertain concentrations of various compounds. Cannabinoids have shown efficacy in treating chemotherapy-related nausea and vomiting, poor appetite in advanced HIV, some pain states, and multiple sclerosis-associated spasticity. Recreational cannabinoid use has many known potential serious harms. Physicians should be knowledgeable about cannabinoids and should inquire with their patients about cannabinoid use. Practical suggestions for clinical approaches are included.

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Pharmacokinetics, metabolism and drug-abuse potential of nabilone

Cited by 51 publications

References 7 publications

Substitution Profile of the Cannabinoid Agonist Nabilone in Human Subjects Discriminating Δ9-Tetrahydrocannabinol

Substitution Profile of the Cannabinoid Agonist Nabilone in Human Subjects Discriminating Δ9-Tetrahydrocannabinol

Pharmacokinetics of Cannabinoids

Cannabinoids in Medical Practice

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