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2. Gabapentinoid - Wikipedia

   en.wikipedia.org/wiki/Gabapentinoid

   Major gabapentinoid compound structures compared to GABA and L-leucine. The gabapentinoids are 3-substituted derivatives of GABA; hence, they are GABA analogues , as well as γ-amino acids . [ 3 ] [ 4 ] Specifically, pregabalin is ( S )-(+)-3-isobutyl-GABA, phenibut is 3-phenyl-GABA, [ 28 ] and gabapentin is a derivative of GABA with a ...

3. Gabapentin - Wikipedia

   en.wikipedia.org/wiki/Gabapentin

   Gabapentin, like other gabapentinoid drugs, acts by decreasing activity of the α 2 δ-1 protein, coded by the CACNA2D1 gene, first known as an auxiliary subunit of voltage gated calcium channels. [13] [14] [15] However, see Pharmacodynamics, below.

4. Gabapentin enacarbil - Wikipedia

   en.wikipedia.org/wiki/Gabapentin_enacarbil

   Gabapentin enacarbil (Horizant (ER) (U.S. Tooltip United States), Regnite (in Japan)) is an anticonvulsant and analgesic drug of the gabapentinoid class, and a prodrug to gabapentin. [1] It was designed for increased oral bioavailability over gabapentin, [ 2 ] [ 3 ] and human trials showed it to produce extended release of gabapentin with ...

5. Mirogabalin - Wikipedia

   en.wikipedia.org/wiki/Mirogabalin

   Mirogabalin (brand name Tarlige; developmental code name DS-5565) is a gabapentinoid medication developed by Daiichi Sankyo. Gabapentin and pregabalin are also members of this class. As a gabapentinoid, mirogabalin binds to the α 2 δ subunit of voltage-gated calcium channel ( 1 and 2 ), but with significantly higher potency than pregabalin.

6. Pharmacokinetics - Wikipedia

   en.wikipedia.org/wiki/Pharmacokinetics

   The number of time points available in order to perform a successful NCA analysis should be enough to cover the absorption, distribution and elimination phase to accurately characterize the drug. Beyond AUC exposure measures, parameters such as Cmax (maximum concentration), Tmax (time to maximum concentration), CL and Vd can also be reported ...

7. Pregabalin - Wikipedia

   en.wikipedia.org/wiki/Pregabalin

   Pregabalin is a gabapentinoid medication, ... In contrast, this is not the case for pregabalin, which shows linear pharmacokinetics and no saturation of absorption.

8. Distribution (pharmacology) - Wikipedia

   en.wikipedia.org/wiki/Distribution_(pharmacology)

   Distribution in pharmacology is a branch of pharmacokinetics which describes the reversible transfer of a drug from one location to another within the body.. Once a drug enters into systemic circulation by absorption or direct administration, it must be distributed into interstitial and intracellular fluids.

9. Bioavailability - Wikipedia

   en.wikipedia.org/wiki/Bioavailability

   Although knowing the true extent of systemic absorption (referred to as absolute bioavailability) is clearly useful, in practice it is not determined as frequently as one may think. The reason for this is that its assessment requires an intravenous reference ; that is, a route of administration that guarantees all of the administered drug ...