Pregabalin
Pregabalin product information:
| Product Name: | Pregabalin |
| Synonyms: | 3(S)-(AMINOMETHYL)-5-METHYLHEXANOIC ACID;(3S)-3-(AMINOMETHYL)-5-METHYLHEXANOIC ACID;PREGABALIN;Pregablin;3-(Aminomethyl)-5-methyl-hexanoic acid;PREDNISOLONESODIUMPHOSPHATE;(R)-Pregabalin;(S)-Pregabalin |
| CAS: | 148553-50-8 |
| MF: | C8H17NO2 |
| MW: | 159.23 |
| EINECS: | 604-639-1 |
| Pregabalin Chemical Properties | |
| Melting point | 194-196°C |
| alpha | D23 +10.52° (c = 1.06 in water) |
| Boiling point | 274.0±23.0 °C(Predicted) |
| density | 0.997±0.06 g/cm3(Predicted) |
| Fp | 9℃ |
| storage temp. | 2-8°C |
| solubility | deionized water: ≥10mg/mL |
| pka | 4.23±0.10(Predicted) |
| form | white powder |
| Uses | Pregabalin is an anticonvulsant drug used for neuropathic pain, as an adjunct therapy for partial seizures, and in generalized anxiety disorder. It was designed as a more potent successor to gabapentin. Pregabalin is marketed by Pfizer under the trade nam |
pregabalin side effects
Commonly reported side effects of pregabalin include: infection, ataxia, blurred vision, constipation, diplopia, dizziness, drowsiness, fatigue, headache, peripheral edema, tremor, weight gain, visual field loss, accidental injury, and xerostomia. Other side effects include: abnormal gait, abnormality in thinking, amnesia, arthralgia, asthenia, cognitive dysfunction, confusion, edema, neuropathy, sinusitis, speech disturbance, vertigo, visual disturbance, myasthenia, amblyopia, increased appetite, and twitching. Continue reading for a comprehensive list of adverse effects.
pregabalin vs gabapentin
Though pregabalin and gabapentin have somewhat similar pharmacokinetic and pharmacodynamic profiles, there are clearly significant differences. Overall, pregabalin has more predictable pharmacokinetics, and it also shows a stronger binding affinity to its target receptor, increased potency, and a steeper dose-response curve in neuropathic pain that does not plateau over recommended dosing levels.
A few studies have found that pregabalin has fewer side effects and may be more efficacious for neuropathic pain than gabapentin. Several studies reviewing conversion of gabapentin to pregabalin predict that a rough ratio for conversion is about 6:1 gabapentin to pregabalin. In addition, a direct switch from gabapentin to pregabalin seems to be well tolerated, making the conversion simple.
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pregabalin mechanism of action
Pregabalin (Lyrica) is a new antiepileptic drug that is active in animal seizure models. Pregabalin is approved in US and Europe for adjunctive therapy of partial seizures in adults, and also has been approved for the treatment of pain from diabetic neuropathy or post-herpetic neuralgia in adults. Recently, it has been approved for treatment of anxiety disorders in Europe.
Although the mechanism of action has not been fully elucidated, studies involving structurally related drugs suggest that presynaptic binding of pregabalin to voltage-gated calcium channels is key to the antiseizure and antinociceptive effects observed in animal models.
By binding presynaptically to the alpha2-delta subunit of voltage-gated calcium channels in the central nervous system, pregabalin modulates the release of several excitatory neurotransmitters including glutamate, substance-P, norepinephrine, and calcitonin gene related peptide. In addition, pregabalin prevents the alpha2-delta subunit from being trafficked from the dorsal root ganglia to the spinal dorsal horn, which may also contribute to the mechanism of action.
Although pregabalin is a structural derivative of the inhibitory neurotransmitter gamma-aminobutyric acid (GABA), it does not bind directly to GABA or benzodiazepine receptors.
