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Screening and Pharmacological Management of Neuropathic Pain
Published in Suvardhan Kanchi, Rajasekhar Chokkareddy, Mashallah Rezakazemi, Smart Nanodevices for Point-of-Care Applications, 2022
Manu Sharma, Ranju Soni, Kakarla Raghava Reddy, Veera Sadhu, Raghavendra V. Kulkarni
Meprobamate, an anxiolytic drug, exhibits affinity to bind GABA receptors to pepper the neuronal transmission in the spinal cord. This symptomatically lessens pain sensation and produces sedation. Similarly, methocarbamol, a central muscle relaxant, is used to treat skeletal muscle spasms caused by musculoskeletal disorders, tetanus, and injury [42]. The GABA-derivative drug, baclofen, is mainly effective in managing muscle spasticity associated with spinal cord injury. Metaxalone is extensively used to relax muscle during strains, sprains, and other musculoskeletal conditions, although its mechanism of action is unclear [43]. Dantrolene is a hydantoin derivative. It produces muscle relaxation by dissociating excitation-contraction coupling possibly by restricting secretion of Ca+2 from sarcoplasmic reticulum by binding to ryanodine receptor1. It has been found suitable for the treatment of fulminant hypermetabolism of skeletal muscles [44].
Acquired Brain Injury Rehabilitation: What Can HRV Tell You?
Published in Herbert F. Jelinek, David J. Cornforth, Ahsan H. Khandoker, ECG Time Series Variability Analysis, 2017
Ian J. Baguley, Melissa T. Nott
Baclofen is a GABA B analog medication that decreases spasticity through its action on inhibitory interneurons in the spinal cord. Oral baclofen has limited efficacy due to its inability to penetrate the blood–brain barrier. In cases of severe spasticity, baclofen can be injected directly into the cerebrospinal fluid of the spinal cord, thereby bypassing the blood–brain barrier. Injected in this way, ITB is said to have maximal effect around 90–180 minutes postinjection. A single bolus produces a direct pharmacological effect for approximately 24 hours.
Ene-Reductases in Pharmaceutical Chemistry
Published in Peter Grunwald, Pharmaceutical Biocatalysis, 2019
Chiral γ-amino acids and their derivatives are important building blocks in organic synthesis and constitute the active pharmaceutical ingredients in a variety of drugs used to treat central nervous system disorders. Baclofen, a γ -aminobutyric acid derivative, sold under the brand name Lioresal® is used in the treatment of spastic movement. In 1962, Heinrich Keberle was the first to synthesize the compound, which in 1968 was patented by CIBA (Keberle and Faigle, 1968). The drug acts as a central nervous system depressant and skeletal muscle relaxant by activating (or agonizing) GABA receptors, specifically the GABAB receptors (Yogeeswari et al., 2006). In addition, there is evidence that baclofen administration reduces alcohol craving and intake (Addolorato et al., 2000). The (S)-enantiomer is the physiological active form, yet drugs contain the racemate. To obtain the pure (S)-Baclofen, a chemo-enzymatic synthesis approach was applied using crude microbial extracts derived from three anaerobic species, namely Clostridium sporogenes, Ruminococcus productus and Acetobacterium woodii (Fryszkowska et al., 2010). The crude enzyme preparations were investigated for the asymmetric double bond reduction in potassium (Z)-3-cyano-3-phenylacrylate and its derivatives (Scheme 10.7). The crude extract from Clostridium sporogenes containing a 2-enoate reductase gave the best enantioselectivity and the synthesis of the (S)-enantiomer of Baclofen was achieved with high specificity in four steps (>99% ee, overall yield 43%). A drawback is the oxygen-sensitivity of the enzyme involved. Whole cell extracts containing ene-reductases catalyze an asymmetric double bond reduction in the synthesis of (S)-Baclofen. X = −H, −F, −Cl, −OMe. Data from Fryszkowska et al. (2010).
Neuromodulatory effect of repetitive transcranial magnetic stimulation pulses on functional motor performances of spastic cerebral palsy children
Published in Journal of Medical Engineering & Technology, 2018
Meena Gupta, Bablu Lal Rajak, Dinesh Bhatia, Arun Mukherjee
Cerebral Palsy (CP) is common developmental disability occurring in paediatric population which is caused by injury to the developing brain that affects their posture and movement. CP is a condition with multiple etiologies in the natal, antenatal and postnatal period from conception to three years of life. Hence, it is regarded as a heterogeneous spectrum disorder represented by different clinical types, co-morbidities, pathways and genetic variants [6]. CP results in different movement patterns which includes spastic, hypotonic, ataxic and dyskinetic [7]; among which spastic CP is most common. Though CP is not fully curable, several interventions are employed such as medication [8], surgical intervention [9,10] baclofen pump [11] and rhizotomy [12] which prevent development of secondary deformities but do not improve functional abilities. Additionally, these treatment regimes provide temporary relief from spasticity, instead a better treatment option would be to treat CP with neuromodulatory device that can elicit muscle response for faster achievement of developmental milestone.