Literature DB >> 20133669

Prolonged sensory-selective nerve blockade.

Itay Sagie1, Daniel S Kohane.   

Abstract

Sensory-selective local anesthesia has long been a key goal in local anesthetic development. For example, it allows women to be pain-free during labor without compromising their ability to push. Here we show that prolonged sensory-selective nerve block can be produced by specific concentrations of surfactants-such as are used to enhance drug flux across skin-in combination with QX-314, a lidocaine derivative that has relative difficulty penetrating nerves. For example, injection of 25 mM QX-314 in 30 mM octyltrimethylammonium bromide (OTAB) lasted up to 7 h. Sensory selectivity was imparted to varying degrees by cationic, neutral, and anionic surfactants, and also was achieved with another lidocaine derivative, QX-222. Simultaneous injection of OTAB at a s.c. injection site remote from the sciatic nerve did not result in prolonged sensory-specific nerve blockade from QX-314, suggesting that the observed effect is due to a local interaction between the surfactant and the lidocaine derivative, not a systemic effect.

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Year:  2010        PMID: 20133669      PMCID: PMC2840479          DOI: 10.1073/pnas.0911542107

Source DB:  PubMed          Journal:  Proc Natl Acad Sci U S A        ISSN: 0027-8424            Impact factor:   11.205


  20 in total

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Journal:  Anesthesiology       Date:  1995-04       Impact factor: 7.892

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  14 in total

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Review 3.  Getting Drugs Across Biological Barriers.

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8.  Acid solution is a suitable medium for introducing QX-314 into nociceptors through TRPV1 channels to produce sensory-specific analgesic effects.

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10.  The quaternary lidocaine derivative QX-314 produces long-lasting intravenous regional anesthesia in rats.

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