Pregabalin Cas:148553-50-8
Pregabalin, a structural analogue of gamma-aminobutyric acid, acts as a ligand of the α2⁃δ subunit of the voltage-gated calcium channel of the nervous system to induce a depolarization-induced reduction of calcium inflow, thereby reducing the release of excitatory neurotransmitters such as glutamine, norepinephrine, dopamine and serotonin. At present, it is widely used in the treatment of a variety of diseases including neuropathic pain, generalized anxiety disorder, epilepsy, etc
Pregabalin is an analogue of the neurotransmitter gamma-aminobutyric acid (GABA), sold under the trade name Lyrica. In December 2004, the FDA approved Pregabalin for the treatment of diabetic neuralgia and herpes zoster neuralgia. Pregabalin is the first drug approved in the United States and Europe for the treatment of both types of pain. In June 2005, Pregabalin was approved for the adjuvant treatment of adult partial seizure epilepsy. In March 2006, the European Union approved Pregabalin for the treatment of generalized anxiety disorder (GAD) and social anxiety disorder (SAD).
Indication
Pregabalin is used primarily for the treatment of peripheral neuralgia and for adjuvant treatment of localized partial seizures
Pharmacological action
Pregabalin has a good therapeutic effect on epilepsy, and various animal epilepsy model studies have shown that pregabalin can significantly prevent seizures, and the dose of its active effect is 3-10 times lower than gabapentin. Pregabalin was found to reduce sensory and motor spinal reflexes in rat clamp toe stimulation, reduce behaviors associated with diabetes, peripheral nerve injury, or chemotherapy in neuropathic animal pain models, and inhibit or reduce pain-related behaviors caused by spinal administered stimuli. Animal studies have found that pregabalin may have advantages in combination with opioids. Pregabalin provides a new option for the clinical treatment of neuropathic pain.
