Identification | |||||||
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Name | gabapentin enacarbil | ||||||
Accession Number | DB08872 | ||||||
Type | small molecule | ||||||
Description | Gabapentin enacarbil is marketed under the name Horizant(R). It is a prodrug of gabapentin, and indicated in adults for the treatment of Restless Legs Syndrome (RLS) and postherpetic neuralgia (PHN). | ||||||
Structure |
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Categories (*) | |||||||
Molecular Weight | Not Available | ||||||
Groups | approved | ||||||
Monoisotopic Weight | Not Available | ||||||
Pharmacology | |||||||
Indication | For the treatment of adult Restless Legs Syndrome (RLS) and postherpetic neuralgia (PHN). | ||||||
Mechanism of action | Although the exact mechanism of action of gabapentin in RLS and PHN is unknown, it is presumed to involve the descending noradrenergic system, resulting in the activation of spinal alpha2-adrenergic receptors. | ||||||
Absorption | Gabapentin enacarbil is absorbed in the intestines by active transport through the proton-linked monocarboxylate transporter, MCT-1. | ||||||
Protein binding | Gabapentin plasma protein binding is less than 3%. | ||||||
Biotransformation | Gabapentin enacarbil does not interact with any of the major cytochrome P450 enzymes. | ||||||
Route of elimination | Gabapentin enacarbil is eliminated primarily in the urine (94%) and to a lesser extent in the feces (5%). | ||||||
Toxicity | Most common adverse reactions are headache, dizziness, and somnolence. | ||||||
Affected organisms |
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Interactions | |||||||
Drug Interactions |
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Food Interactions |
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Sodium-coupled monocarboxylate transporter 1 | |
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Name | Sodium-coupled monocarboxylate transporter 1 |
Gene Name | Not Available |
Actions | substrate |
References |
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DTHybrid score | Not Available |
Sodium-dependent multivitamin transporter | |
Name | Sodium-dependent multivitamin transporter |
Gene Name | SLC5A6 |
Actions | substrate |
References |
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DTHybrid score | 0.8652 |
Id | Partner name | Gene Name | Score |
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45 | Lipoyltransferase 1, mitochondrial | LIPT1 | 0.1647 |
4079 | Lipoic acid synthetase, mitochondrial | LIAS | 0.1647 |
4120 | NADPH--cytochrome P450 reductase | POR | 0.0829 |
81 | Methylcrotonoyl-CoA carboxylase beta chain, mitochondrial | MCCC2 | 0.0659 |
547 | Propionyl-CoA carboxylase alpha chain, mitochondrial | PCCA | 0.0658 |
495 | Methylcrotonoyl-CoA carboxylase subunit alpha, mitochondrial | MCCC1 | 0.0658 |
177 | Biotin--protein ligase | HLCS | 0.0658 |
690 | Acetyl-CoA carboxylase 1 | ACACA | 0.0658 |
601 | Propionyl-CoA carboxylase beta chain, mitochondrial | PCCB | 0.0534 |
771 | Pyruvate carboxylase, mitochondrial | PC | 0.0484 |
775 | Acetyl-CoA carboxylase 2 | ACACB | 0.04 |
1898 | Cytochrome P450 1B1 | CYP1B1 | 0.0268 |