3-Substituted GABA analogs with central nervous system activity: A review

Bryans, Justin S.; Wustrow, David

doi:10.1002/(sici)1098-1128(199903)19:2<149::aid-med3>3.0.co;2-b

Cited by 281 publications

(162 citation statements)

References 91 publications

(95 reference statements)

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“…17 In healthy volunteers peak plasma concentrations are achieved within one hour after the administration of pregabalin, whereas maximum plasma concentrations for gabapentin are attained after 3-4 hours. 10,17 The bioavailability of pregabalin is high and exceeds 90 percent irrespective of the dosage, whereas the bioavailability of gabapentin drops from 60 percent to 33 percent as the dosage increases from 900 mg to 3600 mg daily (149). Pregabalin has a favourable pharmacokinetic profile compared with gabapentin.…”

Section: 6mentioning

confidence: 99%

See 1 more Smart Citation

Comparative efficacious study between preoperative pregabalin and gabapentin on postoperative pain in abdominal hysterectomy: an institutional experience

Gayathri¹,

Swaroop²,

G³

et al. 2017

Int J Reprod Contracept Obstet Gynecol

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Background: Pain is a consistent and predominant complaint following surgical intervention including abdominal open hysterectomy. A multimodal approach has been suggested to improve postoperative analgesia and to reduce opioid related side effects. In this context we conducted a comparative study on efficacy between gabapentin and pregabalin on postoperative pain relief.Methods: In this prospective randomised study, 60 patients were divided in to two arms group G and group P. 900 mg of gabapentin and 300 mg of pregabalin were administered orally one hour before spinal anaesthesia to respective groups. Hemodynamic parameters such as heart rate, mean arterial pressure, respiratory rate was monitored pre, per and postoperatively. Also, the need for first analgesic dose and visual analog pain score were documented in all subjects of both groups. Statistical analysis with SPSS 16.0 performed.Results: There was significant fall in mean arterial pressure in group G than group P patients. Further the fall in mean pulse rate was more in group G compared to group P throughout pre, per and post-operative phases. In terms of mean postoperative time required for first dose of analgesic drug, pregabalin and gabapentin was required after 7 and 5 hours respectively. There was a statistically significant change in Visual Analogue Scale, showing pregabalin as better drug than gabapentin in post operative pain control with score 5 and 7 respectively.Conclusions: Pre-emptive analgesia with pregabalin appears to be superior to gabapentin as a part of multimodal perioperative pain management in abdominal hysterectomy.

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Section: 6mentioning

confidence: 99%

“…Pregabalin has a favourable pharmacokinetic profile compared with gabapentin. 10,17 When studied in non-humans pregabalin appears to be 3 to 10 times more potent as an anticonvulsant than gabapentin. 18,19 Pregabalin is 2 to 4 times more potent as an analgesic than gabapentin.…”

Section: 6mentioning

confidence: 99%

Comparative efficacious study between preoperative pregabalin and gabapentin on postoperative pain in abdominal hysterectomy: an institutional experience

Gayathri¹,

Swaroop²,

G³

et al. 2017

Int J Reprod Contracept Obstet Gynecol

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“…Similar to gabapentin, pregabalin was developed as a treatment for epileptic seizures, but it has evolved to include other indications, such as neuropathic pain [50,51]. Their mechanisms of action require the binding to the high affinity α2-delta subunit protein of the voltagegated Ca 2+ channels [52], thereby reducing release of excitatory neurotransmitters in the central nervous system [53]. To our knowledge, there has only been one retrospective case study that has examined the effects of pregabalin on spasticity [54].…”

Section: Pregabalinmentioning

confidence: 99%

Latest Approaches for the Treatment of Spasticity and Autonomic Dysreflexia in Chronic Spinal Cord Injury

Rabchevsky

Kitzman

2011

Neurotherapeutics

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Summary: Two of the most prevalent secondary complications following spinal cord injury (SCI), besides loss of function and/ or sensation below the level of injury, are uncontrolled muscle spasticity and hypertensive autonomic dysreflexia. Despite the desires of the SCI community, there have been few advances in the treatment and/or management of these fundamental impediments to the quality of life associated with chronic SCI. Therefore, the purpose of this review is to focus on current drug treatment strategies that alleviate symptoms of spasticity and autonomic dysfunction. Subsequently, looking ahead, we discuss whether individuals suffering from autonomic dysreflexia and/or muscle spasms can take certain compounds that specifically and rapidly block the neurotransmission of pain into the injured spinal cord to get rapid relief for both aberrant reflexes for which painful stimuli below the level of SCI are common precipitants.

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“…GABA deficiency has been associated with several neurodegenerative disorders such as Parkinson's disease,2 Huntington's disease,[2b], 3 and Alzheimer's disease4 in addition to psychiatric disorders including depression,5 alcoholism,6 and anxiety. [5b], [5c], 7 Over the past few decades, a number of GABA derivatives showing biological activities have been developed as potential drugs for the treatment of neurological disorders 8, 9. It has been shown that the biological activities of these compounds are largely dependent on the configuration of the chiral center.…”

Section: Introductionmentioning

confidence: 99%

“…The asymmetric synthesis of GABA derivatives has therefore attracted considerable attention, and several methodologies involving the use of metal catalysts, organocatalysts, and biocatalysts, or their combinations, to construct these chiral molecules have been established. [8a]…”

Section: Introductionmentioning

confidence: 99%

Stereochemical Control of Enzymatic Carbon–Carbon Bond‐Forming Michael‐Type Additions by “Substrate Engineering”

et al. 2016

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The enzyme 4‐oxalocrotonate tautomerase (4‐OT) promiscuously catalyzes the Michael‐type addition of acetaldehyde to β‐nitrostyrene derivatives to yield chiral γ‐nitroaldehydes, which are important precursors for pharmaceutically active γ‐aminobutyric acids. In this study, we investigated the effect of different substituents at the aromatic ring of the Michael acceptor on the catalytic efficiency and stereoselectivity of the 4‐OT‐catalyzed acetaldehyde addition reactions. Highly enantioenriched (R)‐ and (S)‐γ‐nitroaldehydes and 4‐substituted chroman‐2‐ol could be obtained in good to excellent yields by applying different substituents at appropriate positions of the aromatic substrate. Stereochemical control of these enzymatic Michael‐type additions by “substrate engineering” allowed the enantioselective synthesis of valuable γ‐aminobutyric acid precursors. In addition, the results suggest a novel enzymatic synthesis route towards precursors for chromans and derivatives, which are valuable scaffolds for preparing biologically active natural products.

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3-Substituted GABA analogs with central nervous system activity: A review

Cited by 281 publications

References 91 publications

Comparative efficacious study between preoperative pregabalin and gabapentin on postoperative pain in abdominal hysterectomy: an institutional experience

Comparative efficacious study between preoperative pregabalin and gabapentin on postoperative pain in abdominal hysterectomy: an institutional experience

Latest Approaches for the Treatment of Spasticity and Autonomic Dysreflexia in Chronic Spinal Cord Injury

Stereochemical Control of Enzymatic Carbon–Carbon Bond‐Forming Michael‐Type Additions by “Substrate Engineering”

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