Ziconotide (Molecule of the Month for August 2006)
Prialt, Conotoxin
Ziconotide is a non-opioid, non-local anesthetic used for the treatment of chronic pain. Ziconotide is the synthetic form of the cone snail (Conus magus) peptide ?-conotoxina which is a N-type calcium channel blocker. Ziconotide is a peptide with the amino acid sequence H-Cys-Lys-Gly-Lys-Gly-Ala-Lys-Cys-Ser-Arg-Leu-Met-Tyr-Asp-Cys-Cys-Thr-Gly-Ser-Cys-Arg-Ser-Gly-Lys-Cys-NH2
Ziconotide is derived from the toxin of the cone snail species Conus magus. Scientists have been intrigued by the effects of the thousands of chemicals in marine snail toxins since the initial investigations in the late 1960s by Baldomero Olivera, who remembered the deadly effects from his childhood in the Philippines. Ziconotide was discovered in the early 1980s by Michael McIntosh working with Baldomero Olivera. It was developed into an artificially manufactured drug by Elan Corporation. It was approved for sale under the name Prialt by the U.S. Food and Drug Administration and by the European Commission in 2004.
Ziconotide must be administered intrathecally (directly into the fluid surrounding the spinal cord through a small pump worn by the patient), this is by far the most expensive and invasive method of drug delivery and involves additional risks of its own. However, this must be weighed against the high level of pain management, both in terms of degree and length, and the apparent lack of tolerance and other signs of addiction even after extended treatment along with the need for alternatives to other therapies that have not worked for the patient.
Update by Karl Harrison
(Molecule of the Month for
August 2006
)
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