Sodium channel blocker for treatment of loss of superficial sensitivity

Abstract

The invention concerns a sodium channel blocker for the treatment of a reduction or loss of superficial sensitivity or sense of touch of a human being or another mammal

1 - 19 . (canceled) 
     
     
         20 . A method of treatment of a reduction or loss of superficial sensitivity or sense of touch of a human being or another mammal in need thereof, the method comprising topically administering a composition comprising 1 to 100 μg/ml of a sodium channel blocker (SCB) to the human being or other mammal, thereby treating the reduction or loss of superficial sensitivity or sense of touch of the human being or other mammal, wherein the SCB is neosaxitoxin, descarbamoylsaxitoxin, gonyautoxin 1 (GTX-1), gonyautoxin 2 (GTX-2), gonyautoxin 3 (GTX-3), gonyautoxin 4 (GTX-4), or gonyautoxin 5 (GTX-5), wherein the SCB is in the form of a racemate, a pure stereoisomer, or a mixture of stereoisomers, in neutral form, or in the form of an acid, a base, a salt, or a solvate. 
     
     
         21 . The method of  claim 20 , wherein the composition comprises 10 μg/ml of the SCB. 
     
     
         22 . The method of  claim 20 , wherein the composition comprises 1 to 10 μg/ml of the SCB. 
     
     
         23 . The method of  claim 20 , wherein the composition comprises 10 to 100 μg/ml of the SCB. 
     
     
         24 . The method of  claim 20 , wherein the composition is administered as a skin-patch, a cream, an ointment, or a spray. 
     
     
         25 . The method of  claim 20 , wherein the SCB is contained in a liposome or a microemulsion, or wherein the pharmaceutical composition further comprises at least one substance facilitating the transport of the SCB through the skin, wherein the substance is selected from the group consisting of alcohols, amines, amides, amino acids, amino acid esters, 1-substituted azacycloheptan-2-ones, pyrrolidones, terpenes, fatty acids, fatty acid esters, macrocyclic compounds, tensides, sulfoxides, liposomes, transferomes, lecithin vesicles, ethosomes, anionic, cationic and non-ionic surfactants, polyols, essential oils, dimethylsulfoxide, decylmethylsulfoxide, diethylene glycol monoethyl ether, diethylene glycol monomethyl ether, sodium laurate, sodium lauryl sulfate, cetyltrimethylammonium bromide, benzalkonium chloride, a poloxamer, polysorbate 20 (polyoxyethylene sorbitan monolaurate), polysorbate 40 (polyoxyethylene sorbitan monopalmitate), polysorbate 60 (polyoxyethylene sorbitan monostearate), polysorbate 80 (polyoxyethylene 5 sorbitan monooleate), lecithin, 1-n-dodecylcycla-zacycloheptan-2-one, ethanol, propanol, octanol, benzyl alcohol, lauric acid, oleic acid, valerie acid, isopropyl myristate, isopropyl palmitate, methylpropionate, ethyl oleate, sorbitan sesquioleate, propylene glycol, ethylene glycol, glycerol, butanediol, polyethylene glycol, poly-ethylene glycol monolaurate, urea, dimethylacetamide, dimethylformamide, 2-pyrrolidone, 1-methyl-2-pyrrolidone, ethanol amine, diethanol amine, triethanolamine, alkanones, salicylic acid, salicylates, citric acid and succinic acid. 
     
     
         26 . The method of  claim 20 , wherein the SCB is contained in a liposome or microemulsion. 
     
     
         27 . The method of  claim 20 , wherein the SCB is contained in a liposome. 
     
     
         28 . The method of  claim 20 , wherein the method comprises administering the composition in multiple treatment cycles. 
     
     
         29 . The method of  claim 20 , wherein the method comprises topically administering the composition one to four times a day. 
     
     
         30 . The method of  claim 20 , wherein the method comprises topically administering 10 to 1000 μg of the mixture per day. 
     
     
         31 . The method of  claim 20 , wherein the method comprises topically administering 10 to 100 μg of the SCB per day. 
     
     
         32 . The method of  claim 20 , wherein the reduction or loss of the superficial sensitivity or sense of touch is a side effect of a drug or of a medical treatment or is caused by diabetes mellitus, a viral infection, allodynia, causalgia, hyperalgesia, hyperesthesia, hyperpathia, neuralgia, neuritis, or neuropathy. 
     
     
         33 . The method of  claim 20 , wherein the administering is supported physically by UV light, ultrasound, iontophoresis, phonophoresis, or mechanical modulation. 
     
     
         34 . The method of  claim 20 , wherein each of the SCBs independently is synthetically synthesized or isolated from a biological source. 
     
     
         35 . The method of  claim 34 , wherein the biological source is cyanobacteria or contaminated shellfish. 
     
     
         36 . A method of treatment of a reduction or loss of superficial sensitivity or sense of touch of a human being in need thereof, the method comprising topically administering a composition comprising 1 to 10 μg/ml of a sodium channel blocker (SCB) to an area of the human being in which there is a reduction or loss of superficial sensitivity or sense of touch, thereby treating the reduction or loss of superficial sensitivity or sense of touch of the human being, wherein the SCB is neosaxitoxin, descarbamoylsaxitoxin, gonyautoxin 1 (GTX-1), gonyautoxin 2 (GTX-2), gonyautoxin 3 (GTX-3), gonyautoxin 4 (GTX-4), or gonyautoxin 5 (GTX-5), wherein the SCB is in the form of a racemate, a pure stereoisomer, or a mixture of stereoisomers, in neutral form, or in the form of an acid, a base, a salt, or a solvate. 
     
     
         37 . The method of  claim 36 , wherein the composition comprises 10 μg/ml of the SCB. 
     
     
         38 . The method of  claim 36 , wherein the composition is a cream composition and the SCB is contained in a liposome.