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Gabapentin: Difference between revisions
>DXMethorphan mNo edit summary |
>DiphenylHydra m Added what is very clearly missing info about the bioavailability drop-off of gabapentin—which should have been included when the bioavailability percentage drop-off info was first added to the pharmacology section since it is information found in the end of the sentence which was paraphrased from page 3, 1st paragraph of this reference: http://www.accessdata.fda.gov/drugsatfda_docs/nda/2002/21-397.pdf_Neurontin_BioPharmr.pdf |
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The bioavailability of gabapentin is relatively low and is inversely proportional to the dose (i.e. higher doses have lower bioavailability than lower doses). The bioavailability of gabapentin is approximately 60%, 47%, | The bioavailability of gabapentin is relatively low and is inversely proportional to the dose (i.e. higher doses have lower bioavailability than lower doses). The bioavailability of gabapentin is approximately 60%, 47%, | ||
34%, 33%, and 27% following 900, 1200, 2400, 3600, and 4800 mg/day.<ref>Neurontin Clinical Pharmacology Biopharmaceutics Review | http://www.accessdata.fda.gov/drugsatfda_docs/nda/2002/21-397.pdf_Neurontin_BioPharmr.pdf</ref> Gabapentin is highly lipophilic, making unsaturated fats such as vegetable oil and olive oil significantly boost the total amount of absorption. This means that eating a high fat meal substantially increases gabapentin's bioavailability, due to the fact that unsaturated fats bind to gabapentin to allow for absorption, and that meals slow down and thus increase gabapentin absorption by decreasing gabapentin transporter saturation.<ref>Gabapentin datasheet | http://reference.medscape.com/drug/neurontin-gralise-gabapentin-343011#showall</ref> | 34%, 33%, and 27% following 900, 1200, 2400, 3600, and 4800 mg/day, given in divided doses of one pill per every 8 hours.<ref>Neurontin Clinical Pharmacology Biopharmaceutics Review | http://www.accessdata.fda.gov/drugsatfda_docs/nda/2002/21-397.pdf_Neurontin_BioPharmr.pdf</ref> Gabapentin is highly lipophilic, making unsaturated fats such as vegetable oil and olive oil significantly boost the total amount of absorption. This means that eating a high fat meal substantially increases gabapentin's bioavailability, due to the fact that unsaturated fats bind to gabapentin to allow for absorption, and that meals slow down and thus increase gabapentin absorption by decreasing gabapentin transporter saturation.<ref>Gabapentin datasheet | http://reference.medscape.com/drug/neurontin-gralise-gabapentin-343011#showall</ref> | ||
Gabapentin transporter saturation occurs when large enough doses of gabapentin are consumed in a short enough period of time to result in the body being unable to absorb any more gabapentin, causing a significant reduction in bioavailability, which largely accounts for the drop in bioavailability seen with increasing doses. | Gabapentin transporter saturation occurs when large enough doses of gabapentin are consumed in a short enough period of time to result in the body being unable to absorb any more gabapentin, causing a significant reduction in bioavailability, which largely accounts for the drop in bioavailability seen with increasing doses. | ||