Intrasphincteric Neosaxitoxin Injection: Evidence of Lower Esophageal Sphincter Relaxation in Achalasia

Rodriguez-Navaro, Alberto J; Lagos, Néstor; Lagos, Marcelo E.; Braghetto, Italo; Csendes, Attila; Hamilton, James; Berger, Zoltán; Wiedmaier, Gonzalo; Henríquez, A

doi:10.1111/j.1572-0241.2006.00809_6.x

Cited by 13 publications

(5 citation statements)

References 5 publications

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“…For TTH, the treatment was by intramuscular injections, causing an immediate muscle relaxation and pain reduction that lasted for more than 2 months in some cases [ 144 ]. Pain blockage for TKA was achieved by local infiltration, and there were no side effects or adverse reactions without the use of opioids [ 145 ]. Neosaxitoxin, an N-1 hydroxylated STX analog (see Figure 2 ), has been used in the treatment of achalasia, a gastrointestinal motility disorder resulting from a failure of the lower esophageal sphincter that causes dysphagia or chest pain.…”

Section: Guanidinium Toxins As Ion Channel Research Subjects and Tmentioning

confidence: 99%

Guanidinium Toxins and Their Interactions with Voltage-Gated Sodium Ion Channels

Durán-Riveroll

Cembella

2017

Marine Drugs

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Guanidinium toxins, such as saxitoxin (STX), tetrodotoxin (TTX) and their analogs, are naturally occurring alkaloids with divergent evolutionary origins and biogeographical distribution, but which share the common chemical feature of guanidinium moieties. These guanidinium groups confer high biological activity with high affinity and ion flux blockage capacity for voltage-gated sodium channels (NaV). Members of the STX group, known collectively as paralytic shellfish toxins (PSTs), are produced among three genera of marine dinoflagellates and about a dozen genera of primarily freshwater or brackish water cyanobacteria. In contrast, toxins of the TTX group occur mainly in macrozoa, particularly among puffer fish, several species of marine invertebrates and a few terrestrial amphibians. In the case of TTX and analogs, most evidence suggests that symbiotic bacteria are the origin of the toxins, although endogenous biosynthesis independent from bacteria has not been excluded. The evolutionary origin of the biosynthetic genes for STX and analogs in dinoflagellates and cyanobacteria remains elusive. These highly potent molecules have been the subject of intensive research since the latter half of the past century; first to study the mode of action of their toxigenicity, and later as tools to characterize the role and structure of NaV channels, and finally as therapeutics. Their pharmacological activities have provided encouragement for their use as therapeutants for ion channel-related pathologies, such as pain control. The functional role in aquatic and terrestrial ecosystems for both groups of toxins is unproven, although plausible mechanisms of ion channel regulation and chemical defense are often invoked. Molecular approaches and the development of improved detection methods will yield deeper understanding of their physiological and ecological roles. This knowledge will facilitate their further biotechnological exploitation and point the way towards development of pharmaceuticals and therapeutic applications.

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Section: Guanidinium Toxins As Ion Channel Research Subjects and Tmentioning

confidence: 99%

Guanidinium Toxins and Their Interactions with Voltage-Gated Sodium Ion Channels

Durán-Riveroll

Cembella

2017

Marine Drugs

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“…Indeed, the use of outer pore blockers in different clinical settings is becoming more widely applied. No reports are available showing side effects produced by the applied doses (see Garrido et al 2004Garrido et al , 2005Garrido 2005;Rodriguez-Navarro et al 2006).…”

Section: Discussionmentioning

confidence: 97%

Potentiation of Local Anesthetic Activity of Neosaxitoxin with Bupivacaine or Epinephrine: Development of a Long-Acting Pain Blocker

et al. 2009

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Local anesthetics effectively block and relieve pain, but with a relatively short duration of action, limiting its analgesic effectiveness. Therefore, a long-acting local anesthetic would improve the management of pain, but no such agent is yet available for clinical use. The aim of this study is to evaluate the potentiation of the anesthetic effect of neosaxitoxin, with bupivacaine or epinephrine in a randomized double-blind clinical trial. Ten healthy males were subcutaneously injected into the left and right forearms with a randomized pair of the following treatments: (i) bupivacaine (5 mg); (ii) neosaxitoxin (10 microg); (iii) neosaxitoxin (10 microg) plus bupivacaine (5 mg), and (iv) neosaxitoxin (10 microg) plus epinephrine (1:100.000), but all participant received all four formulations (in 2 ml; s.c.), with 1 month elapsing between the two round of experiments. A validated sensory and pain paradigm was used for evaluating the effect of the treatment 0-72 h after the injections, measuring sensory, pain, and mechanical touch perception threshold. The duration of the effect produced by combined treatments was longer than that by the single drugs. In conclusion, bupivacaine and epinephrine potentiate the local anesthetic effect of neosaxitoxin in humans when co-injected subcutaneously. The present results support the idea that neosaxitoxin is a new long-acting local pain blocker, with highly potential clinical use.

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“…Several previous approaches to prolonged-duration local anesthesia have been investigated in animal models 3Y11 and in humans. 6,9,10,12,27,28 We believe that site 1 sodium-channel toxins have several potentially attractive features as candidates for prolonged-duration local anesthesia. They appear to produce far less neurotoxicity or myotoxicity 28 than amino-amide local anesthetics such as lidocaine or bupivacaine.…”

Section: Discussionmentioning

confidence: 99%

Comparison of Neosaxitoxin Versus Bupivacaine via Port Infiltration for Postoperative Analgesia Following Laparoscopic Cholecystectomy

Rodríguez-Navarro

Berde

Wiedmaier³

et al. 2011

Regional Anesthesia and Pain Medicine

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Intrasphincteric Neosaxitoxin Injection: Evidence of Lower Esophageal Sphincter Relaxation in Achalasia

Cited by 13 publications

References 5 publications

Guanidinium Toxins and Their Interactions with Voltage-Gated Sodium Ion Channels

Guanidinium Toxins and Their Interactions with Voltage-Gated Sodium Ion Channels

Potentiation of Local Anesthetic Activity of Neosaxitoxin with Bupivacaine or Epinephrine: Development of a Long-Acting Pain Blocker

Comparison of Neosaxitoxin Versus Bupivacaine via Port Infiltration for Postoperative Analgesia Following Laparoscopic Cholecystectomy

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