Caffeine Augments the Lactate and Interleukin-6 Response to Moderate-Intensity Exercise.

INTRODUCTION: The release of interleukin (IL)-6 from contracting skeletal muscle is thought to contribute to some of the health benefits bestowed by exercise. This IL-6 response seems proportional to exercise volume and to lactate production. Unfortunately, high volumes of exercise are not feasible for all people. Caffeine augments the magnitude of increase in circulating IL-6 in response to high-intensity and long-duration exercise. Caffeine also increases circulating concentrations of lactate during exercise. We hypothesized that caffeine, ingested before short-duration, moderate-intensity exercise, would lead to greater circulating concentrations of lactate and IL-6 in a study population comprising both male and female individuals. METHODS: Twenty healthy adults (10 men and 10 women age 25 ± 7 yr (mean ± SD)) completed 30 min of moderate-intensity cycle ergometer exercise, at an intensity corresponding to 60% peak oxygen uptake, after ingesting either caffeine (6 mg·kg -1 ) or placebo. Arterialized-venous blood was collected throughout each of the exercise sessions. RESULTS: Compared with placebo, caffeine increased circulating concentrations of lactate at the end of exercise (5.12 ± 3.67 vs 6.45 ± 4.40 mmol·L -1 , P < 0.001) and after 30 min of inactive recovery (1.83 ± 1.59 vs 2.32 ± 2.09 mmol·L -1 , P = 0.006). Circulating IL-6 concentrations were greatest after 30 min of inactive recovery ( P < 0.001) and higher with caffeine (2.88 ± 2.05 vs 4.18 ± 2.97, pg·mL -1 , P < 0.001). Secondary analysis indicated sex differences; caffeine increased the IL-6 response to exercise in men ( P = 0.035) but not in women ( P = 0.358). CONCLUSIONS: In response to moderate-intensity exercise, caffeine evoked greater circulating lactate concentrations in men and women but only increased the IL-6 response to exercise in men. These novel findings suggest that for men unwilling or unable to perform high-intensity and/or long-duration exercise, caffeine may augment the health benefits of relatively short, moderate-intensity exercise.

Edible marijuana and cycle ergometer exercise.

Purpose: There is extensive public and scientific interest in the influence of cannabis and the psychoactive cannabinoid, delta-9-tetrahydrocannabinol (THC), on exercise performance. Unfortunately, recent, up-to-date studies are lacking. The aim of the current study was to address the hypothesis that ingestion of edible marijuana, prior to exercise, would have unfavorable effects on the physiological response to exercise and on exercise performance. Methods: 17 Healthy adult male and female habitual exercisers, who were regular users of cannabis products, were screened for study participation. 10 were enrolled, and data from 9 [8 males, 1 female, aged 25±3 years, with peak oxygen uptake of 56.5±11.7 ml/kg/min (mean ± SD)] were retained. Participation included two exercise sessions, each preceded by self-administration and ingestion of either edible marijuana (containing 10 mg THC) or placebo. Cardio-respiratory responses (via indirect calorimetry) to stationary cycle ergometer exercise (8 min at 50, 100 and 150 W) were recorded before completion of a 20-min Functional Threshold Power test (FTP20) and a sprint test involving maximal effort until volitional fatigue. Results: Edible marijuana increased the concentration of circulating THC and THC metabolites, and evoked sensations of intoxication and altered psychoactive state. Cardio-respiratory responses to staged cycle ergometer exercise were normal and were unaffected by edible marijuana. Compared with placebo, edible marijuana did not influence FTP20 (Placebo 253±75 vs THC: 251±72 W (mean±SD); p > 0.45) or peak power output during the sprint test (Placebo: 710±201 vs. THC: 732±136 W; p = 0.864). Conclusion: 10 mg of THC, when ingested prior to exercise by regular exercisers and habitual users of cannabis, had little effect on the physiological response to standardized cycle ergometer exercise, and was neither ergogenic nor ergolytic.

Cannabidiol and Cannabidiol Metabolites: Pharmacokinetics, Interaction with Food, and Influence on Liver Function.

Cannabidiol (CBD) is widely available and marketed as having therapeutic properties. Over-the-counter CBD is unregulated, many of the therapeutic claims lack scientific support, and controversy exists as to the safety of CBD-liver interaction. The study aims were to compare the pharmacokinetics of commercial CBD and CBD metabolites following the ingestion of five different CBD formulations, determine the influence of CBD on food induced thermogenesis, determine the influence of food on CBD pharmacokinetics, and determine the influence of CBD on markers of liver function. Fourteen males (body mass index ≥ 25 kg/m2) were studied in a placebo-controlled, randomized, crossover design. On five occasions, different CBD formulations were ingested (one per visit). On two additional occasions, CBD or placebo was ingested following a meal. CBD servings were standardized to 30 mg. Considerable pharmacokinetic variability existed between formulations; this pharmacokinetic variability transferred to several of the metabolites. CBD did not influence food induced thermogenesis but did favorably modify early insulin and triglyceride responses. Food appreciably altered the pharmacokinetics of CBD. Finally, CBD did not evoke physiologically relevant changes in markers of liver function. Collectively, these data suggest that consumers should be aware of the appreciable pharmacokinetic differences between commercial CBD formulations, CBD is unlikely to influence the caloric cost of eating but may prove to be of some benefit to initial metabolic responses, consuming CBD with food alters the dynamics of CBD metabolism and increases systemic availability, and low-dose CBD probably does not represent a risk to normal liver function.

Pharmacokinetic Investigation of Commercially Available Edible Marijuana Products in Humans: Potential Influence of Body Composition and Influence on Glucose Control.

The purpose of the study was to describe and compare the pharmacokinetics of five commercial edible marijuana products, determine the influence of body composition on pharmacokinetics, and, in light of epidemiology suggesting marijuana may offer diabetes protection, explore the influence of edible marijuana on glucose tolerance. Seven regular users of marijuana self-administered five edible products in a randomized crossover design; each product contained 10 mg of delta-9-tetrahydrocannabinol (THC). Thirty minutes following marijuana ingestion, participants imbibed a 75 g glucose beverage. Time-to-peak plasma THC concentration ranged between 35 and 90 min; maximal plasma THC concentration (Cmax) ranged between 3.2 and 5.5 ng/mL. Differences between products in plasma THC concentration during the first 20-30 min were detected (p = 0.019). Relations were identified between body composition and pharmacokinetic parameters for some products; however, none of these body composition characteristics were consistently related to pharmacokinetics across all five of the products. Edible marijuana had no effect on oral glucose tolerance compared with a marijuana-free control (Matsuda Index; p > 0.395). Commercially available edible marijuana products evoke different plasma THC concentrations shortly after ingestion, but do not appear to influence acute glucose regulation. These data may allow recreational marijuana users to make informed decisions pertaining to rates of edible marijuana ingestion and avoid overdose.

Comparison of Five Oral Cannabidiol Preparations in Adult Humans: Pharmacokinetics, Body Composition, and Heart Rate Variability.

Data supporting the physiological effects of cannabidiol (CBD) ingestion in humans are conflicting. Differences between CBD preparations and bioavailability may contribute to these discrepancies. Further, an influence of body composition on CBD bioavailability is feasible, but currently undocumented. The aims of this study were to: (1) compare the pharmacokinetics of five oral CBD preparations over 4 h; (2) examine the relationship between body composition and CBD pharmacokinetics; and, (3) explore the influence of CBD on heart rate variability. In total, five preparations of CBD, standardized to 30 mg, were orally administered to 15 healthy men and women (21-62 years) in a randomized, crossover design. Prior to and 60 min following CBD ingestion, heart rate variability was determined. Body composition was assessed using dual energy X-ray absorptiometry. Peak circulating CBD concentration, time to peak concentration, and area under the curve was superior in a preparation comprising 5% CBD concentration liquid. Fat free mass was a significant predictor (R 2 = 0.365, p = 0.017) of time to peak concentration for this preparation. Several heart rate variability parameters, including peak frequency of the high frequency band, were favorably, but modestly modified following CBD ingestion. These data confirm an influence of CBD preparation and body composition on CBD bioavailability, and suggest that acute CBD ingestion may have a modest influence on autonomic regulation of heart rate.