Phycotoxins and Uses Thereof

a technology of phycotoxins and toxins, applied in the field of phycotoxins, can solve the problems of causing death in mammals via respiratory arrest and cardiovascular shock, blocking neuronal transmission,

Inactive Publication Date: 2008-01-24
PHYTOTOX LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The high toxicity of the PSP toxins is due to the reversible binding to a receptor site on the voltage-gated sodium channel on excitable cells, thus blocking the influx of sodium ions and preventing nerve and muscle cells from producing action potentials, thereby blocking neuronal transmission and causing death in mammals via respiratory arrest and cardiovascular shock.

Method used

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  • Phycotoxins and Uses Thereof
  • Phycotoxins and Uses Thereof
  • Phycotoxins and Uses Thereof

Examples

Experimental program
Comparison scheme
Effect test

example 1

[0079] One unit of activity corresponds to an amount of the composition of the invention necessary to block the muscular contractions of the crural biceps of a 20 gram CF1 albino BALB-C strain mouse leg for 1.5 to 2.0 hours. The toxin was intramuscularly injected in the crural biceps of the mouse right leg in a volume of 0.5 ml. The left leg is used as a control. This was done in three mice and the paralyzing effect was tested every 30 minutes for the first two hours, and then every 2, 4, 8 hours and overnight. Depending on the dose injected, the paralyzing effect can last 24 hours or longer. This example confirms the reversible nature of the effect of the toxins of the present invention and demonstrates that the duration of the effect can be controlled by varying the dosage of the toxins.

example 2

Fibromyalgia

[0080] Each dose of toxin contains from 10 to 400 units of activity of a mixture of gonyautoxins (GTX2 / GTX3) and is intramuscularly infiltrated locally in 2 to 20 muscle points according to the diagram shown in FIG. 1. Each injection point receives 0.1 to 0.2 ml (10 to 20 units) of toxin solution, which contains 100 units of activity of the mixture of GTX2 / GTX3 per milliliter of solution. The carrier is 0.9% sodium chloride in sterile solution, without preservatives. This dose may be repeated, for example, every four weeks, as prescribed by the physician, or according to the patient's requirements in order to minimize pain.

[0081] 10 patients have been enrolled in an open label study. The patients need to fulfill specified clinical criteria. Upon evaluation and admission to the study, the patients are administered the toxin as described above. Depending on the symptomatology and local painful points of each patient, the physician determines the number of infiltration po...

example 3

Tension Headache (tension cefelea)

[0082] Each dose of toxin contains from 10 to 400 units of activity of a mixture of gonyautoxins (GTX2 / GTX3) and is intramuscularly infiltrated locally in 2 to 10 muscle points according to the diagram shown in FIG. 2. Each injection point receives 0.1 ml (10 units) of a toxin solution, which contains 100 units of activity of the mixture of GTX2 / GTX3 per millilitre of solution. The carrier is 0.9% sodium chloride in a sterile solution, without preservatives. This dose may be repeated, for example, every four weeks, as prescribed by the physician, or according to the patient's requirements.

[0083] 20 patients have been enrolled in an open label study. The patients need to fulfil the following clinical criteria: they have to be chronic patients, that experience primary non vascular, tensional headache at least twice a week, and that have been treated previously for this condition with analgesics, systemic muscle relaxants, local corticosteroid infilt...

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Abstract

Pharmaceutical compositions comprising tricyclic 3,4-propinoperhydropurines and uses thereof for blocking neuronal transmission which are useful in treating anal fissure and other wounds and muscle disorders are provided. Also provided are methods of treating wounds and muscle disorders by administering the composition of the invention to a muscle or in the vicinity of a muscle either topically or by injection.

Description

FIELD OF THE INVENTION [0001] This invention relates to methods of treating muscle disorders and to pharmaceutical compositions containing heterocyclic guanidine-type compounds which can be used in the methods, as well as for other purposes. BACKGROUND OF THE INVENTION [0002] Paralytic shellfish poisoning (PSP) results from a mixture of phycotoxins that bind reversibly to a receptor site on the voltage-gated sodium channel found in excitable cells. The primary clinical symptom is an acute paralytic illness. Phycotoxins or algal toxins are produced by microscopic planktonic algae. These toxins accumulate on filter feeders such as bivalves. Consumption of phycotoxin-contaminated shellfish results in six diseases in humans: PSP, amnesic shellfish poisoning (ASP), Diarrheic shellfish poisoning (DSP), neurotoxic shellfish poisoning (NSP), ciguatera poisoning (CP), and cyanobacterial poisoning (CNP). [0003] The phycotoxins that produce PSP have a common structure of 3,4,6-trialquil tetrah...

Claims

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Application Information

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Patent Type & Authority Applications(United States)
IPC IPC(8): A61K31/519A61P19/00A61P21/00A61F2/00A61K31/505
CPCA61K31/505A61P1/00A61P1/04A61P9/14A61P13/10A61P15/00A61P17/00A61P17/02A61P19/00A61P19/02A61P19/10A61P21/00A61P21/02A61P23/00A61P25/00A61P25/02A61P25/04A61P25/06A61P25/08A61P27/02A61P29/00Y02A50/30
Inventor WILSON, NESTOR ANTONIO LAGOS
Owner PHYTOTOX LTD
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