Lyrica (Pregabalin)
Alias: C1-1008
Chemical name: (3S) -3-aminomethyl-5-methylcaproic acid
Chemical name: (+) -4-amino -3(S)-isobutylbutyric acid
Molecular formula: C8H17NO2
CAS number: 148553-50-8
Molecular weight: 159.23
Route of administration: oral administration
Properties: white crystalline powder
Mechanism of action: γ-aminobutyric acid analogues, treatment of epilepsy, neuropathic pain and anxiety.
ATC Classification: Other labor and antipyretic Agents (N02B)/Antiepileptic agents (N03A)/Other antianxiety Agents (N05B-X)
Indications: pregabalin for epilepsy, neuropathic pain and anxiety
1. Generalized Anxiety Disorder GAD
2. Diabetic Peripheral Neuropathy DPN
3. Post-herpetic Neuralgia PHN
4. Fibromyaigia Syndrome FMS
5. Adjuvant therapy for epilepsy
Pharmacological effect
Pregabalin is a novel gamma-aminobutyric acid (GABA) receptor agonist, which can block voltage-dependent calcium channels and reduce the release of neurotransmitters. It is mainly used in the treatment of peripheral neuralgia and adjuvant treatment of localized partial epilepsy.
Pharmacology and toxicology
Pharmacological Action
Pregabalin has a high affinity for the α2-δ site (a helper subunit of voltage-gated calcium channels) in the central nervous system. The mechanism of action of pregabalin is unclear, but the results of studies in transgenic mice and structure-related compounds such as gabapentin suggest that the analgesic and anticonvulsive effects of pregabalin in animal models may be related to the binding of pregabalin to the α2-δ subunit. In vitro studies have shown that pregabalin may reduce calcium-dependent release of some neurotransmitters by regulating the function of calcium channels.
Although pregabalin is a structural derivative of the inhibitory neurotransmitter G-aminobutyric acid (GABA), it does not directly bind to GABAA, GABAB or benzodiazepine receptors, does not increase the GABAA response of cultured neurons in vitro, does not change the concentration of GABA in the rat brain, and has no acute effect on the uptake or degradation of GABA. However, prolonged exposure to pregabalin in cultured neurons increased the density of GABA transporters and the functional GABA transport rate. Pregabalin does not block sodium channels, has no activity on opioid receptors, does not change cyclooxygenase activity, has no activity on dopamine and serotonin receptors, and does not inhibit the reuptake of dopamine, serotonin or norepinephrine.
Toxicological studies
Genetic toxicity:
In vitro studies showed that pregabalin had no mutagenic effect on bacteria and mammalian cells, in vivo and in vitro studies showed that pregabalin did not cause mammalian chromosome aberration, and did not induce extra-programmed DNA synthesis in hepatocytes in rats or mice.
