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1: Arch Pharm (Weinheim). 2005 Aug;338(8):358-64.Click here to read Links

Design, synthesis, and preliminary evaluation of gabapentin-pregabalin mutual prodrugs in relieving neuropathic pain.

Shi W, Liu H, Zhang Y, Zhong B, Yang H.

Bejing Institute of Pharmacology and Toxicology, Bejing, China.

As a part of a program for the development of specific analgesics in relieving neuropathic pain, the purpose of the present study was to investigate a new concept that involves the conjugation of two drugs, gabapentin and pregabalin, as mutual prodrugs using a chemical modification approach. A series of gabapentin-pregabalin diester compounds were synthesized using linear or branch bis-hydroxyl linkers. Their pharmacological properties for treating neuropathic pain were investigated in a rat model of chronic sciatic nerve constriction injury (CCI). In-vivo evaluation demonstrated that 1a and 1b composed of two gabapentin molecules as well as 3a composed of gabapentin and pregabalin with the short linear linker, were effective in reversing tactile allodynia in CCI rats. Compounds with longer or side-branched linkers showed lower efficiencies and severe adverse effects.

PMID: 16041834 [PubMed - indexed for MEDLINE]

Patient Drug Information

  • Gabapentin (Gabarone® , Neurontin® )

    Gabapentin is used to help control certain types of seizures in patients who have epilepsy. Gabapentin is also used to relieve the pain of postherpetic neuralgia (PHN; the burning, stabbing pain or aches that may last fo...

  • Pregabalin (Lyrica® )

    Pregabalin is used to relieve neuropathic pain (pain from damaged nerves) that can occur in your arms, hands, fingers, legs, feet, or toes if you have diabetes or in the area of your rash if you have had shingles (a pain...

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