Pregabalin epilepsy

Gabapentin and pregabalin are prescribed in certain epileptic diseases such as absence epilepsy and in neuropathic pain. Their therapeutic target for pain suppression is the a2S-l subunit. 

In addition to being a first-line treatment for neuropathic pain and anxiety disorders, pregabalin is itself an augmenting agent to numerous other anticonvulsants in treating epilepsy... 

An attractive feature of this two-step one-pot reaction is that it not only incorporates an innovative technique for site-isolation but also produces enantiomerically enriched useful intermediates. Indeed the Michael adducts that are produced represent precursors to y-amino acids, allowing access to y-amino butyric acid analogues. Pregabalin (145) is one such analogue that is approved for the treatment of both epilepsy and neuropathic pain. Following this one-pot synthetic strategy there is no need for nitroalkene isolation and byproduct formation can be avoided. Scheme 3.42 depicts the total synthesis of pregabalin. 

Taylor, C. R, Angelotti, T., Eauman, E. Pharmacology and mechanism of action of pregabalin the calcium channel al[ a2-delta (alpha2-delta) subunit as a target for antiepileptic drug discovery. Epilepsy Res. 2007, 73c, 137—150. 

Brodie MJ, Wilson EA, Wesche DL, Alvey CW, F dinitis EJ, Posvar EL, Hounslow NJ, Bron NJ, Gibson GL, Bockbrader HN Pregabalin drug intemction studies lack of effect on the pharmacokinetics of carbamazepine, phenytoin, lamotrigine, and val M oate in patients with p ial epilepsy. Epilepsia (2005) 46, 1407-13. 

Baulac M, Leon T, O Brien TJ, Whalen E, Barrett J. A comparison of pregabalin, lamotrigine, and placebo as adjunctive therapy in patients with refractory partial-onset seizures. Epilepsy Res 2010 91(1) 10-9. 

Calabro RS, Bramanti P. Pregabalin-induced severe delayed ejaculation. Epilepsy Behav 2010 19(3) 543. 

Yuen AW, Singh R, Bell GS, Bhattachaijee A, Neligan A, Heaney DC, Duncan JS, Sander JW. The long-term retention of pregabalin in a large cohort of patients with epilepsy at a tertiary referral centre. Epilepsy Res 2009 87(2-3) 120-3. 

A method for the analysis of the basic antiepileptic compounds felbamate, lamotrigine, carbamazepine, carbamazepine-10,11-epoxide, gabapentin, pregabalin, levetiracetam, and oxcarbazepine monohydroxy derivative (oxcarb MHD) in human plasma is described. This protocol incorporates a simplified sample preparation step followed by quantitative high performance chromatography-tandem mass spectrometry detection of commonly prescribed and monitored anticonvulsant drugs. Since polytherapy is common in epilepsy patients, use of a multiconstituent assay can improve laboratory efficiency and reduce required analytical time. 

Of 25 patients receiving pregabalin as add-on therapy in tumor-related epilepsy, only two reported adverse events one reported dizziness and one reported dr5mess of the eyes. Both of these patients dropped out of the study [141 ]. 

Maschio M, Dinapoli L, Sperati F, Pace A, Fabi A, Vidiri A, et al. Effect of pregabalin add-on treatment on seizure control, quality of life, and anxiety in patients with brain tumour-related epilepsy a pilot study. Epileptic Disord December 2012 14(4) 388-97. 

S)-(+)-3-aminomethyl-5-methylhexanoic add (Pregabalin) 1 (Figure 11.1) is a lipophilic GABA (y-aminobutyric add) analog devdoped for the treatment of several central nervous system disorders induding epilepsy, neuropathic pain, anxiety, and sodal phobia [29,30]. Recent studies have shown that pregabalin... 

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