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| http://linked.open...gbank/description
| - Pregabalin is an anticonvulsant drug used for neuropathic pain, as an adjunct therapy for partial seizures, and in generalized anxiety disorder. It was designed as a more potent successor to gabapentin. Pregabalin is marketed by Pfizer under the trade name Lyrica. It is considered to have a dependence liability if misused, and is classified as a Schedule V drug in the U.S. [Wikipedia] (en)
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| http://linked.open...y/drugbank/dosage
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| http://linked.open...generalReferences
| - # : Schedules of controlled substances: placement of pregabalin into schedule V. Final rule. Fed Regist. 2005 Jul 28;70(144):43633-5. "Pubmed":http://www.ncbi.nlm.nih.gov/pubmed/16050051 # Su TZ, Feng MR, Weber ML: Mediation of highly concentrative uptake of pregabalin by L-type amino acid transport in Chinese hamster ovary and Caco-2 cells. J Pharmacol Exp Ther. 2005 Jun;313(3):1406-15. Epub 2005 Mar 15. "Pubmed":http://www.ncbi.nlm.nih.gov/pubmed/15769862 # Li Z, Taylor CP, Weber M, Piechan J, Prior F, Bian F, Cui M, Hoffman D, Donevan S: Pregabalin is a potent and selective ligand for alpha(2)delta-1 and alpha(2)delta-2 calcium channel subunits. Eur J Pharmacol. 2011 Sep 30;667(1-3):80-90. doi: 10.1016/j.ejphar.2011.05.054. Epub 2011 Jun 1. "Pubmed":http://www.ncbi.nlm.nih.gov/pubmed/21651903 (en)
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| http://linked.open...gy/drugbank/group
| - approved (en)
- illicit (en)
- investigational (en)
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| http://linked.open...drugbank/halfLife
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| http://linked.open...ugbank/indication
| - Pregabalin is used for the management of neuropathic pain associated with diabetic peripheral neuropathy or spinal cord injury, and postherpetic neuralgia. It is also used as adjunctive therapy for adult patients with partial onset seizures and management of fibromyalgia. (en)
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| http://linked.open...bank/manufacturer
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| sameAs
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| Title
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| adms:identifier
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| http://linked.open...mechanismOfAction
| - Pregabalin binds with high affinity to the alpha2-delta site (an auxiliary subunit of voltage-gated calcium channels) in central nervous system tissues. Although the mechanism of action of pregabalin is unknown, results with genetically modified mice and with compounds structurally related to pregabalin (such as gabapentin) suggest that binding to the alpha2-delta subunit may be involved in pregabalin's antinociceptive and antiseizure effects in animal models. In vitro, pregabalin reduces the calcium-dependent release of several neurotransmitters, possibly by modulation of calcium channel function. Studies also suggest that the descending noradrenergic and serotonergic pathways originating from the brainstem may be involved with the mechanism of pregabalin. Interestingly, although pregabalin is a structural derivative of inhibitory neurotransmitter gamma-aminobutyric acid (GABA), it does not bind directly to GABA or benzodiazepine receptors. The sodium channels, opiate receptors, and cyclooxygenase enzymes are not involved with the mechanism of pregabalin. It is also inactive at serotonin and dopamine receptors and does not inhibit dopamine, serotonin, or noradrenaline reuptake. (en)
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| http://linked.open...drugbank/packager
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| http://linked.open...y/drugbank/patent
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| http://linked.open...outeOfElimination
| - 90% of the dose was recovered in the urine as the parent compound. The N-methylated derivative of pregabalin, the major metabolite was found in the urine and accounted for 0.9% of the dose. Pregabalin (S-enantiomer) did not undergo racemization to the R-enantiomer. (en)
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| http://linked.open.../drugbank/synonym
| - Lyrica (en)
- (S)-3-Isobutyl gaba (en)
- 3-Isobutyl gaba (en)
- CI-1008 (en)
- S-(+)-3-isobutylgaba (en)
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| http://linked.open...drugbank/toxicity
| - Most common adverse reactions (≥5% and twice placebo) are dizziness, somnolence, dry mouth, edema, blurred vision, weight gain and thinking abnormal (primarily difficulty with concentration/attention). (en)
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| http://linked.open...umeOfDistribution
| - Apparent volume of distribution, oral administration = 0.5 L/kg. Pregabalin has been shown to cross the placenta in rats and is present in the milk of lactating rats. (en)
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| http://linked.open.../drug/hasAHFSCode
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| http://linked.open...k/foodInteraction
| - Avoid alcohol (may increase CNS effects). (en)
- When taken with food, Cmax decreases, while Tmax is prolonged. Despite these observations, the total absorption of pregabalin is not effected to a clinically relevant degree. Pregabalin can be taken with or without food. (en)
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| http://linked.open...nk/proteinBinding
| - Pregabalin does not bind to plasma proteins. (en)
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| http://linked.open...ynthesisReference
| - Mark Burk, "Asymmetric synthesis of pregabalin." U.S. Patent US20030212290, issued November 13, 2003. (en)
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| foaf:page
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| http://linked.open...ugbank/IUPAC-Name
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| http://linked.open...gy/drugbank/InChI
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| http://linked.open...Molecular-Formula
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| http://linked.open.../Molecular-Weight
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| http://linked.open...noisotopic-Weight
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| http://linked.open...y/drugbank/SMILES
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| http://linked.open.../Water-Solubility
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| http://linked.open...ogy/drugbank/logP
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| http://linked.open...ogy/drugbank/logS
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| http://linked.open...logy/drugbank/pKa
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| http://linked.open...l/drug/hasATCCode
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| http://linked.open...nd-Acceptor-Count
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| http://linked.open...-Bond-Donor-Count
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| http://linked.open...drugbank/InChIKey
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| http://linked.open...urface-Area--PSA-
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| http://linked.open...nk/Polarizability
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| http://linked.open...bank/Refractivity
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| http://linked.open...atable-Bond-Count
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| http://linked.open...ugbank/absorption
| - Pregabalin is well absorbed after oral administration. When an oral administration of pregabalin under fasting conditions is given, the pharmacokinetic parameters are as follows: Tmax = 1.5 hours; Oral bioavailability = >90% (independent of dose); Time to steady state = 24-48 hours. It is also a substrate for the L-type transport system. (en)
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| http://linked.open.../affectedOrganism
| - Humans and other mammals (en)
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