Effect of a high-protein meal on gabapentin pharmacokinetics

Gidal, Barry E.; Maly, Melissa M.; Budde, J.A.; Lensmeyer, Gary L.; Pitterle, Michael E.; Jones, John C.

doi:10.1016/0920-1211(95)00051-8

Cited by 41 publications

(22 citation statements)

References 13 publications

Supporting

Mentioning

Contrasting

Unclassified

Order By: Relevance

“…This study was not designed to specifically test if food by-products might interfere with the absorption of gabapentin in a clinical setting but to elucidate, in vivo, a mechanism-based interaction by which intestinal drug absorption can be influenced by a component of the meal. Indeed, Gidal et al (24) reported that the C max of gabapentin was significantly enhanced (by 38%) when the drug was administered after a high-protein meal. At the time, they speculated that the large amino acid load delivered with the meal enhanced gabapentin absorption via trans-stimulation of the amino acid transport system in intestine.…”

Section: Discussionmentioning

confidence: 97%

In Vivo Effects of Glycyl-Glutamate and Glycyl-Sarcosine on Gabapentin Oral Absorption in Rat

2007

View full text Add to dashboard Cite

show abstract

Section: Discussionmentioning

confidence: 97%

In Vivo Effects of Glycyl-Glutamate and Glycyl-Sarcosine on Gabapentin Oral Absorption in Rat

2007

View full text Add to dashboard Cite

show abstract

“…Although food did not alter the absorption of gabapentin in preapproval pharmacokinetic studies (40), Gidal and colleagues found that meals rich in neutral amino acids enhanced mean plasma levels by 36% and the area under the curve by 12% (45,46). These findings suggest that gabapentin uptake can be stimulated under certain conditions.…”

Section: S42 M J Mcleanmentioning

confidence: 89%

Gabapentin in the Management of Convulsive Disorders

McLean

1999

Epilepsia

View full text Add to dashboard Cite

Summary: Gabapentin, in clinical use since 1993, is indicated as an adjunctive antiepileptic drug (AED) for treatment of complex partial seizures, with or without secondary generalization, in patients over 12 years of age. Although several cellular actions have been described in the literature, the molecular mechanism(s) of action responsible for the anticonvulsant effect of gabapentin has not been conclusively determined. It is likely that gabapentin has multiple concentration-dependent actions that combine in a unique manner to produce antiepileptic efficacy. The pharmacokinetic properties of this water-soluble, amino-acid AED are generally favorable. Absorption appears to be dependent on transport by the L-system amino acid transporter. Elimination of unmetabolized drug occurs by the renal route. Although its therapeutic range is not well characterized, gabapentin has a broad therapeutic index. This implies that a wide range of doses can be used, based on individual patientThe structure of gabapentin combines an inhibitory amino acid, y-aminobutyric acid (GABA) and a cyclohexane ring. Gabapentin appears to be actively transported by the L-system amino acid transporter across the gut wall and the blood-brain barrier (1,2). The same transporter recognizes naturally occurring, bulky, neutral amino acids such as L-leucine, L-isoleucine, L-valine, and L-phenylalanine. Gabapentin is freely soluble in water (3) and is available for clinical use in 100-, 300-, and 400-mg capsules. Tablets containing 600 mg or 800 mg of gabapentin are in late stages of stability testing. A liquid preparation is also in development. However, a bitter taste and prolonged aftertaste of gabapentin have slowed the development of a palatable elixir.Although gabapentin was originally synthesized as a baclofen analog for spasmolytic effects, more favorable anticonvulsant properties were recognized in the course of testing in standard laboratory models. This led to clinical trials against partial and secondarily generalized seizures that resulted in licensing.

show abstract

“…yields average bioavailability of 29.2 ± 16.2% and 35.6 ± 17.6% (p = 0.006), respectively [4]. Despite this, administration with foods, including those high in protein and enteral nutrition supplements, does not decrease absorption [5,6]. Inter-and intrapatient variability in absorption is present however and interpatient variability can be quite pronounced [7].…”

Section: Absorption and Distributionmentioning

confidence: 91%

Drug interactions in epilepsy care: perspective on the newer generation antiepileptic drugs

Gidal¹,

Nemergut²,

French³

2002

Expert Review of Neurotherapeutics

View full text Add to dashboard Cite

Pharmacokinetic interactions involving the antiepileptic drugs have long been considered to be an unavoidable component of epilepsy treatment. Many of the 'older' generation of antiepileptic drugs, including carbamazepine, phenytoin and phenobarbital, are recognized to cause hepatic induction of drug-metabolizing enzyme systems, such as the cytochrome P450 and UDP-gluculronyltransferase. Such interactions are not uncommonly implicated in resulting in clinically significant treatment complications. During the latter half of 1990s, a number of new antiepileptic drugs have become available to clinicians. Generally speaking, a common feature of these 'newer' generation medications are improved pharmacokinetic characteristics, including an improved drug interaction profile. The aim of this review is to summarize the data, both experimental and clinical, regarding pharmacokinetic interactions with the newer antiepileptic drugs.

show abstract

Effect of a high-protein meal on gabapentin pharmacokinetics

Cited by 41 publications

References 13 publications

In Vivo Effects of Glycyl-Glutamate and Glycyl-Sarcosine on Gabapentin Oral Absorption in Rat

In Vivo Effects of Glycyl-Glutamate and Glycyl-Sarcosine on Gabapentin Oral Absorption in Rat

Gabapentin in the Management of Convulsive Disorders

Drug interactions in epilepsy care: perspective on the newer generation antiepileptic drugs

Contact Info

Product

Resources

About