Pregabalin

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. 

Outside of the evidence-based guidelines, other pharmacologic treatments are commonly used or avoided. For initial treatment of absence seizures, ethosuximide and valproate are commonly used, not only in the United Kingdom, but also in the United States. Zonisamide may be also used for initial treatment of absence and myoclonic seizures. In absence and myoclonic seizures, carbamazepine, oxcarbazepine, gabapentin, tiagabine, and pregabalin should be avoided, as they have been associated with an exacerbation of these types of seizures. 

Long-acting Opioids (e.g., MS Contin, Oxycontin) SSRI/SNRI Pregabalin... 

Gabapentin, a non-benzodiazapine GABA analog, was modestly effective in a 14-week controlled trial in SAD. Most patients were titrated to a maximal dose of 3600 mg/day.58 Pregabalin 600 mg/day was effective for social anxiety, fear, and avoidance behavior in a 10-week controlled trial.63 Pregabalin was well tolerated, and the most common side effects were somnolence and dizziness. 

Peripheral neuropathy is the most common complication reported in type 2 DM. This complication generally presents as pain, tingling, or numbness in the extremities. The feet are affected more often than the hands and fingers. A number of treatment options have been tried with mixed success. Current options include pregabalin, gabapentin, low-dose tricyclic antidepressants, duloxetine, venlafaxine, topiramate, non-steroidal anti-inflammatory drugs, and topical capsaicin. 

An excellent example for an enzymatic resolution process is reported for production of Pregabalin. This drug was approved by the US Food and Drug Administration (FDA) in 2004 against neurophatic pain associated with diabetic peripheral neuropathy and postherpetic neuralgia. Several different routes have been developed based on asymmetric hydrogenation, crystallization and biocatalytic resolutions [16-20]. The most powerful and currently applied process is based on a lipase resolution, shown in Figure 14.3. This process is one of the very few... 

Figure 14.3 Route to Pregabalin based on a lipase-based resolution...

Pregabalin Dizziness Pedal edema Weight gain... 

Pregabalin binds to the subunit of the voltage-gated Ca channel, resulting in a decrease in the release of several excitatory neurotransmitters. 

Pregabalin produced anxiolytic effects similar to lorazepam, alprazolam, and venlafaxine in acute trials. Sedation and dizziness were the most common adverse effects, and the dose should be tapered over 1 week upon discontinuation. 

Generalized anxiety Duloxetine Escitalopram Paroxetine Venlafaxine XR Benzodiazepines Buspirone Imipramine Sertraline Hydroxyzine Pregabalin... 

Social anxiety disorder Escitalopram Fluvoxamine Paroxetine Sertraline Venlafaxine XR Citalopram Clonazepam Buspirone Gabapentin Miitazapine Phenelzine Pregabalin... 

Scheme 10. Chemoenzymatic synthesis of pregabalin by overcoming product inhibition...

Scheme 13. Nitrilase-catalyzed synthesis of pregabalin by ePCR...

Hu S, Martinez CA, Tao J, Tully W, Kelleher P, Dumond Y (2005) An efficient method for the production of enantiopure pregabalin. US Pat Appl Publ US 2005283023... 

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