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      Pharmacokinetics of Caffeine following a Single Administration of Coffee Enema versus Oral Coffee Consumption in Healthy Male Subjects

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          Abstract

          The objective of this study was to determine the pharmacokinetics of caffeine after single administration of a coffee enema versus coffee consumed orally in healthy male subjects. The study design was an open-label, randomized two-phase crossover study. Eleven healthy subjects were randomly assigned either to receive 500 mL of coffee enema for 10 minutes or to consume 180 mL of ready-to-drink coffee beverage. After a washout period of at least 10 days, all the subjects were switched to receive the alternate coffee procedure. Blood samples were collected immediately before and at specific time points until 12 hours after coffee administration in each phase. The mean caffeine content in both the coffee solution prepared for the coffee enema and the ready-to-drink coffee beverage was not statistically different. The C max and AUC of caffeine obtained from the coffee enema were about 3.5 times significantly less than those of the coffee consumed orally, despite having slightly but statistically faster T max. The t 1/2 of caffeine obtained following both coffee procedures did not statistically differ. In summary, the relative bioavailability of caffeine obtained from the coffee enema was about 3.5 times significantly less than those of the coffee consumed orally.

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          The rate of absorption and relative bioavailability of caffeine administered in chewing gum versus capsules to normal healthy volunteers.

          Thomas J Balkin, Adrienne D. Cox, Gary Kamimori … (2002)
          The purpose of this study was to evaluate the rate of absorption and relative bioavailability of caffeine from a Stay Alert chewing gum and capsule formulation. This was a double blind, parallel, randomized, seven treatment study. The treatment groups were: 50, 100, and 200 mg gum, 50, 100, and 200 mg capsule, and a placebo. Subjects consisted of 84 (n=12 per group); healthy, non-smoking, males who had abstained from caffeine ingestion for at least 20 h prior to dosing and were randomly assigned to the treatment groups. Blood samples were collected pre-dose and at 5, 15, 25, 35, 45, 55, 65, 90 min and 2, 3, 4, 6, 8, 12, 16 and 29 h post administration. Plasma caffeine levels were analyzed by a validated UV-HPLC method. Mean Tmax for the gum groups ranged from 44.2 to 80.4 min as compared with 84.0-120.0 min for the capsule groups. The Tmax, for the pooled data was significantly lower (P<0.05) for the gum groups as compared with the capsule groups. Differences in Tmax were significant for the 200 mg capsule versus 200 mg gum (P<0.05). The mean ka values for the gum group ranged from 3.21 to 3.96 h-1 and for the capsule groups ranged from 1.29 to 2.36 h-1. Relative bioavailability of the gum formulation after the 50, 100 and 200 mg dose was 64, 74 and 77%, respectively. When normalized to the total drug released from the gum (85%), the relative bioavailability of the 50, 100 and 200 mg dose were 75, 87, and 90%, respectively. No statistical differences were found for Cmax and AUCinf for comparisons of the gum and capsule formulations at each dose. Within each dose level, there were no significant formulation related differences in Cmax. No significant differences were observed in the elimination of caffeine after the gum or capsule. The results suggest that the rate of drug absorption from the gum formulation was significantly faster and may indicate absorption via the buccal mucosa. In addition, for the 100 and 200 mg groups, the gum and capsule formulations provide near comparable amounts of caffeine to the systemic circulation. These findings suggest that there may be an earlier onset of pharmacological effects of caffeine delivered as the gum formulation, which is advantageous in situations where the rapid reversal of alertness and performance deficits resulting from sleep loss is desirable.
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            Caffeine: a double-blind, placebo-controlled study of its thermogenic, metabolic, and cardiovascular effects in healthy volunteers.

            A Astrup, S Toubro, S. Cannon … (1990)
            In humans caffeine stimulates thermogenesis by unknown mechanisms and its effect on body weight has not been studies. The effect of placebo and 100, 200, and 400 mg oral caffeine on energy expenditure, plasma concentrations of substrates and hormones, blood pressure, and heart rate was investigated in a double-blind study in healthy subjects who had a moderate habitual caffeine consumption. Caffeine increased energy expenditure dose dependently and the thermogenic response was positively correlated with the response in plasma caffeine (r = 0.52; p less than 0.018), plasma lactate (r = 0.79; p less than 0.000001), and plasma triglyceride (r = 0.53; p less than 0.02). Stepwise regression analysis with the thermogenic response as the dependent variable excluded plasma caffeine and yielded the following equation: thermic effect (kcal/3 h) = -0.00459 X heart rate + 0.30315 X (triglyceride) + 0.53114 X (lactate) + 15.34 (r = 0.86; p = 0.0001). The results suggest that lactate and triglyceride production and increased vascular smooth muscle tone may be responsible for the major part of the thermogenic effect of caffeine.
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              Are we dependent upon coffee and caffeine? A review on human and animal data.

              A Nehlig (1999)
              Caffeine is the most widely used psychoactive substance and has been considered occasionally as a drug of abuse. The present paper reviews available data on caffeine dependence, tolerance, reinforcement and withdrawal. After sudden caffeine cessation, withdrawal symptoms develop in a small portion of the population but are moderate and transient. Tolerance to caffeine-induced stimulation of locomotor activity has been shown in animals. In humans, tolerance to some subjective effects of caffeine seems to occur, but most of the time complete tolerance to many effects of caffeine on the central nervous system does not occur. In animals, caffeine can act as a reinforcer, but only in a more limited range of conditions than with classical drugs of dependence. In humans, the reinforcing stimuli functions of caffeine are limited to low or rather moderate doses while high doses are usually avoided. The classical drugs of abuse lead to quite specific increases in cerebral functional activity and dopamine release in the shell of the nucleus accumbens, the key structure for reward, motivation and addiction. However, caffeine doses that reflect the daily human consumption, do not induce a release of dopamine in the shell of the nucleus accumbens but lead to a release of dopamine in the prefrontal cortex, which is consistent with caffeine reinforcing properties. Moreover, caffeine increases glucose utilization in the shell of the nucleus accumbens only at rather high doses that stimulate most brain structures, non-specifically, and likely reflect the side effects linked to high caffeine ingestion. That dose is also 5-10-fold higher than the one necessary to stimulate the caudate nucleus, which mediates motor activity and the structures regulating the sleep-wake cycle, the two functions the most sensitive to caffeine. In conclusion, it appears that although caffeine fulfils some of the criteria for drug dependence and shares with amphetamines and cocaine a certain specificity of action on the cerebral dopaminergic system, the methylxanthine does not act on the dopaminergic structures related to reward, motivation and addiction.
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                Author and article information

                Journal
                Journal ID (nlm-ta): ISRN Pharmacol
                Journal ID (iso-abbrev): ISRN Pharmacol
                Journal ID (publisher-id): ISRN.PHARMACOLOGY
                Title: ISRN Pharmacology
                Publisher: Hindawi Publishing Corporation
                ISSN (Print): 2090-5165
                ISSN (Electronic): 2090-5173
                Publication date Collection: 2013
                Publication date (Electronic): 4 March 2013
                Volume: 2013
                Electronic Location Identifier: 147238
                Affiliations
                1Department of Pharmacology, Faculty of Medicine, Chiang Mai University, Chiang Mai 50200, Thailand
                2Center of Thai Traditional and Complementary Medicine, Faculty of Medicine, Chiang Mai University, Chiang Mai 50200, Thailand
                3Phisaleeh Hospital, Nakhon Sawan 60220, Thailand
                4Department of Biochemistry, Faculty of Medicine, Chiang Mai University, Chiang Mai 50200, Thailand
                Author notes
                *Supanimit Teekachunhatean: steekach@ 123456med.cmu.ac.th

                Academic Editors: K. N. Klotz, T. Kumai, and T. W. Stone

                Author information
                https://orcid.org/0000-0003-1329-379X
                Article
                DOI: 10.1155/2013/147238
                PMC ID: 3603218
                PubMed ID: 23533801
                SO-VID: cd8f4277-2521-48b0-b886-513e4eb5edec
                Copyright © Copyright © 2013 Supanimit Teekachunhatean et al.
                License:

                This is an open access article distributed under the Creative Commons Attribution License, which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited.

                History
                Date received : 8 January 2013
                Date accepted : 30 January 2013
                Categories
                Subject: Clinical Study

                ScienceOpen disciplines: Pharmacology & Pharmaceutical medicine
                Data availability:
                ScienceOpen disciplines: Pharmacology & Pharmaceutical medicine

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