QUICKLINKS AND VIEW OPITONS
Meridia (sibutramine): Taking it with food increases absorption 5-fold
Sunday, December 05, 2004 9:14 pm Email this article
Taking the prescription diet pill Meridia (sibutramine) with food dramatically affects absorption according to a new study out of Canada. Food delays maxium blood levels of the drug by 2-4 hours
When six healthy non-smoking men, 24- to 59-years-old, were given Meridia (sibutramine) with food, maximum blood levels of the drug and its active metabolites, M1 and M2, were delayed 2 to 4 hours. This was previously known and is reflected in the product literature.
Food increases absorption of the drug 5-fold, increases peak blood levels 2.8 fold
However, in contrast to the product literature, this study found that the amount of Meridia (sibutramine) absorbed was 5.1 times greater when the drug was given with food than on a empty stomach, and peak blood levels were 2.8 times greater.
Food increases the amount of M1 produced 2.1 fold, and peak levels 1.7 fold
The amount of the active metabolite M1 produced over time was 2.1 times greater when Meridia (sibutramine) was given with food, and peak blood levels were 1.7 times greater.
Food did not significantly affect the amount of M2
Food did not significantly change the levels of the active metabolite M2. Levels of M2 were 1.1 times greater when Meridia was taken with food, and peak blood levels of M2 were 20 percent lower (0.8 times that of the levels seen when the drug was taken on a empty stomach.
Food increased the elimination half-life of Meridia 2.3 fold
The elimination half-life, that is the amount of time it takes for blood levels of the drug or its metabolites to fall to half of their peak levels, was also significantly increased when the drug was given with food. That is to say that the drug stayed in the body longer when it was given with food than when it was not.
The elimination half-life of Meridia (sibutramine) was 2.3 times longer when taken with food (19 hours versus 8 hours).
Food increased the elimination half-life of M1, 1.4 fold, M2, 1.2 fold
The elimination half-life of M1 was 1.4 times longer when taken with food (20 hours versus 14 hours), and the elimination half-life of M2 was 1.2 times longer with food (22 hours versus 18 hours).
These increases in levels of the drug and its metabolites could help to explain some adverse effects
The authors of the paper note that this effect of food on Meridia (sibutramine) might help to explain some of the recent safety concerns about the drug.
Meridia associated with 35 cases of amnesia
Yesterday, I reported that Meridia has been associated with 35 cases of amnesia world-wide. The possible reason for this, according to the authors of the report, is that Meridia increases serotonin.
M1 and M2 100 times more potent than Meridia at inhibiting reuptake of noradrenaline, serotonin, and dopamine
Meridia’s active metabolites, M1 and M2, are up to 100 times more potent than Meridia (sibutramine) at inhibiting reuptake of noradrenaline, serotonin, and dopamine according to a Luscombe et al (1987), although M1 and M2 inhibit dopamine reuptake 3 times less potently than they inhibit noradrenaline and serotonin according to the Meridia monograph (1998).
M1 and M2 as potent as Prozac at inhibiting serotonin reuptake
M1 and M2 inhibit reuptake of noradrenaline as potently as the antidepressant desipramine (Norpramine, Pertofrane), and inhibit serotonin reuptake as potently as Prozac (fluoxetine) according to Rolls et al (1997).
Meridia and M1 equally potent at inhibiting appetite, M2 slight more potent
Meridia (sibutramine) and M1 are equally potent at reducing appetite, while M2 is slightly more potent according to Fantino et al (1995) and Luscombe et al (1987).
Practical advice: Take with food to increase effectiveness, take on an empty stomach to reduce side effects
The results of this study suggest that people who find Meridia ineffective, might want to try taking it with food, and people who have side effects, might try taking it on an empty stomach.
People taking Meridia (sibutramine) should be made aware of this effect of food on the drug.
Abolfathi Z, Couture J, Vallee F, Lebel M, Tanguay M, Masson E. A pilot study to evaluate the pharmacokinetics of sibutramine in healthy subjects under fasting and fed conditions. J Pharm Pharm Sci. 2004 Nov 12, 7(3):345-49.
AUTHOR’S CONTACT INFORMATION
Fantino M, Souquet AM. Effects of metabolites 1 and 2 of sibutramine on the short-term control of food intake in the rat. International Journal of Obesity, May 1995, 19(suppl 2):145 abstract P400.
Luscombe GP, Hopcoft RH, Thomas PC, Buckett WR. Down-regulation of rat cortisol beta-adrenoreceptors by the putative antidepressant BTS 54 524: contribution of metabolites. British Journal of Pharmacology, 1987, 92(suppl):575P.
MERIDIA monograph dated Jan 1998. Knoll Pharmaceutical Company.
Rolls BJ, Shide DJ, Ulbrecht JS. Sibutramine and food intake in obese women. International Journal of Obesity, 1997 June, 21(Suppl 2):S31 abstract 70.
Articles on the same subject can be found here:
Please feel free to share your comments about this article.
© Copyright 2003-2017 - Larry Hobbs - All Rights Reserved.