Abstract: The application provides compounds of Formula I and pharmaceutically acceptable salts and solvates thereof, wherein R1, R2, R3, R4, R5, dash line a, dash line b, W, Z, X, and m are defined as set forth in the specification. The invention is also directed to use of the compounds of Formula I and the pharmaceutically acceptable salts and solvates thereof to treat disorders responsive to the modulation of one or more opioid receptors, or as synthetic intermediates. In certain embodiments, the Compounds of the Invention are useful for treating pain.

Abstract: In one aspect, the invention provides compounds of Formula (I) or (II): (I) or (II) and pharmaceutically acceptable salts and solvates thereof, wherein R1, R2a, R2b, R3, R4, Z and G are defined as set forth in the disclosure. The invention also provides compounds of Formulae A and B and pharmaceutically acceptable salts and solvates thereof. Other aspects of the invention include the use of compounds of Formulae I, II, A, and B, and pharmaceutically acceptable salts and solvates thereof for the treatment of disorders responsive to modulation of one or more opioid receptors. In certain embodiments, the Compounds of the Invention are useful for treating pain.

Abstract: A method for cleansing and treating skin exposed to a capsaicin or derivative thereof so as to inhibit capsaicin reactivation includes: providing a subject having exposure to capsaicin, oleoresin capsicum, or other capsaicinoid derivative; cleansing capsaicin, oleoresin capsicum, or other capsaicinoid derivative from skin of the subject with a cleansing composition having: a carrier; a surfactant and/or detergent; a chelating agent; and salicylic acid, acetylsalicylic acid, or ibuprofen; and treating the skin of the subject with a therapeutic composition so as to inhibit reactivation of effects of capsaicin, oleoresin capsicum, or other capsaicinoid derivative exposure, the therapeutic composition having: a carrier; aloe; a thickening agent; and salicylic acid, acetylsalicylic acid, or ibuprofen.

Abstract: Compositions and methods for enhancing heavy metal detoxification are described. The compositions and methods described provide enhanced activity of key detoxification systems including that the induction of phase II detoxification enzymes, such as glutathione S-transferases (GSTs), and NADPH quinone reductase (NQO1) activity.

Abstract: An antimicrobial and chemical deactivating composition for use in a liquid medium or for incorporation into a coating, structural plastic materials, thin microporous membranes, textiles and sponges. The composition includes macrosize or submicron particles of silver, platinum with silver and their salts with parabens, oxide, salicylate, acetate, citrate, benzoate and phosphate along with copper and zinc salts of the same.

Abstract: A pest-combating composition including sodium lauryl sulfate and one or more of C6-12 fatty acids, preferably lauric and/or capric and/or caprylic acid, soy methyl ester, and 2-undecanone, and methods of combating pests utilizing same, are disclosed. The compositions can include a carrier oil such as silicon oil, soy methyl ester, or a vegetable oil, and can be in the form of an emulsion. The composition may be constituted as a spray composition, an aerosol, a lotion, a paste, or another compositional form. Pests that may be usefully combated with such composition include flying insects, including flies, mosquitoes, and wasps, ants, including arthropods such as fire ants, ticks, fleas, cockroaches, silver fish, thrips, gnats, aphids, Japanese beetles, and agricultural and horticultural arthropods and insects including beetles (potato and bean), flea beetles, fleahoppers, squash bugs, slugs, leaf hoppers, harlequin bugs, milk weed bugs, spiders, mites, lice, rodents, and deer.

Abstract: An antimicrobial and chemical deactivating composition for use in a liquid medium or for incorporation into a coating, structural plastic materials, thin microporous membranes, textiles and sponges. The composition includes macrosize or submicron particles of silver, platinum with silver and their salts with parabens, oxide, salicylate, acetate, citrate, benzoate and phosphate along with copper and zinc salts of the same.

Abstract: The present invention relates to the use of the dye methylene blue (MB) or a related compound to prevent or reverse an exaggerated hemodynamic reaction in animals in need thereof, including humans. More specifically, the present invention concerns the use of MB or a related compound to prevent or reverse hypotension, unstable angina, myocardial infarction or shock caused by the concomitant ingestion of a phosphodiesterase inhibitor, such as sildenafil citrate, and a NO-donor, such as L-arginine, or an organic nitrate, such as nitroglycerin.

Abstract: The present invention relates to a pharmaceutical composition and the method for the preparation thereof. The composition comprises 1.5˜6.9% (w/v) of one or more substances selected from sodium chloride, sodium bicarbonate, potassium chloride, magnesium sulfate, calcium chloride, calcium gluconate, and the like, and 3˜18% (w/v) of one or more substances selected from hydroxyethylstarch, dextran, carboxymethylstarch, polyvinyl-pyrrolidone, gelatin derivatives, and the like as well as the remainder of conventional injections, as long as sodium chloride is not less than 1.5% (w/v). The pharmaceutical composition of the present invention is used to treat and save the wounded and patients, as well as to treat shock, its advantages include safe and convention use, rapid and good curative effect, long time maintenance, extensive uses and the like.

Abstract: Polyoxometalate topical compositions for removing contaminants from an environment and methods of use thereof are disclosed. An embodiment of the polyoxometalate topical composition includes a topical carrier and at least one polyoxometalate, with the proviso that the polyoxometalate is not H5PV2Mo10O40; K5Si(H2O)MnIIIW11O39; K4Si(H2O)MnIVW11O39; or K5CoIIIW12O40. Another embodiment relates to a method for removing a contaminant from an environment, including contacting the polyoxometalate topical composition with the environment containing the contaminant for a sufficient time to remove the contaminant from the environment.

Abstract: The present invention relates to a pharmaceutical composition and the method for the preparation thereof, The composition comprises 1.5˜6.9% (w/v) of one or more substances selected from sodium chloride, sodium bicarbonate, potassium chloride, magnesium sulfate, calcium chloride, calcium gluconate, and the like, and 3˜18% (w/v) of one or more substances selected from hydroxyethylstarch, dextran, carboxymethylstarch, polyvinyl-pyrrolidone, gelatin derivatives, and the like as well as the remainder of conventional injections, as long as sodium chloride is not less than 1.5% (w/v). The pharmaceutical composition of the present invention is used to treat and save the wounded and patients, as well as to treat shock, its advantages include safe and convenient use, rapid and good curative effect, long time maintenance, extensive uses and the like.

Abstract: The invention relates to a polyoxometalate topical composition for removing a contaminant from an environment, comprising a topical carrier and at least one polyoxometalate, with the proviso that the polyoxometalate is not H5PV2Mo10O40; K5Si(H2O)MnIIIW11O39; K4Si(H2O)MnIVW11O39; or K5CoIIIW12O40. The invention further relates to a method for removing a contaminant from an environment, comprising contacting the polyoxometalate topical composition of the present invention with the environment containing the contaminant for a sufficient time to remove the contaminant from the environment. The invention further relates to a modified polyoxometalate, wherein the modified polyoxometalate comprises the admixture of (1) a polyoxometalate and (2) a cerium compound, a silver compound, a gold compound, a platinum compound, or a combination thereof.

Abstract: A composition is prepared by extracting phytochemicals from plant matter. This composition is enriched preferably in isoflavones, lignans, saponins, catechins and phenolic acids. Soy is the preferred source of these chemicals; however, other plants may also be used, such as red clover, kudzu, flax, and cocoa. The composition is a dietary supplement for treatment of various cancers, pre- and post-menstrual syndromes, and various other disorders.

Abstract: A pharmaceutical formulation for the prophylaxis and preliminary treatment of a poisoning caused by organophosphorus cholinesterase inhibitors is characterized in that it consists of an active substance combination of at least one parasympathomimetic and at least one parasympatholytic.

Abstract: The present invention concerns composition, kits and methods for reducing the flushing effect (cutaneous erythema) of an antilipemic drug, for treating hyperlipemia, for improving the effectiveness of an anti-platelet aggregating drug (e.g., in nonresponders) and for treating thrombosis. The present compositions and kits for reducing the flushing effect and for treating hyperlipemia contain an antilipemic drug (such as niacin) and either a sustained release NSAID (such as aspirin) or an NSAID and a carboxylic acid compound other than the NSAID and antilipemic drug. The kits contain (a) pre-dosages of the NSAID and optional carboxylic acid compound and (b) an antilipemic dosage of the antilipemic drug, which optionally may be combined with NSAID and optional carboxylic acid compound in an amount effective to maintain the reduction of the flushing effect.

Abstract: A composition containing capsaicin together with another ingredient to neutralize the discomfort resulting from the application of capsaicin to the skin can be used to treat many types of discomforts, including arthritis pain, hemorrhoid pain and itching, and poison ivy itching, without the discomfort normally associated with the topical application of capsaicin.

Abstract: An improved process for the production of a pharmaceutical composition comprising p-hydroxyacetanilide and L-cysteine or a compound which is converted thereto in vivo comprises mixing p-hydroxyacetanilide and L-cysteine or its precursor in the solid state and then shaping the solid mixture.

Abstract: An opiate analgesic drug formulation which induces minimal respiratory dession is provided which contains a homogeneous mixture of an opiate agonist drug component and an opiate antagonist drug component in an aqueous medium, the opiate agonist component and the opiate antagonist component being present in the mixture in a molar ratio, wherein when the drug formulation is administered to a patient in an amount sufficient for the opiate agonist drug component to induce analgesia in the patient, substantially no respiratory depression is induced in the patient.

Abstract: A concentrated, stable solution, especially an injection solution, which comprises water and either sodium-leucovorin or potassium-leucovorin or sodium-N(5)-methyl-5,6,7,8-tetrahydrofolic acid or potassium-N(5)-methyl-5,6,7,8-tetrahydrofolic acid. Also described is a process for the preparation of the solution, as well as its uses.

Abstract: The combined use of opiate antagonists and of calcium salts for the preparation of medicaments for the treatment of endorphin-mediated pathologies is described.

Abstract: An antidotal food product containing activated charcoal is provided for ingestion into the gastro-intestinal tract of a user. The antidotal food product is orally administered having the visual appearance and physical properties which enables the desire on the part of young children to chew and ingest the food product. The food product in a preferred embodiment includes a substantially dry friable wafer which is adapted to be chewed by the user for ingestion. The dry friable wafer has a wafer mixture composition formed by blending a first predetermined weight of sorbent particulate composition having an initial adsorption value with respect to a toxin to a second predetermined weight of a substantially non-interfering flavored binding composition which provides for a creamy and sweet tasting food product.

Abstract: The present invention concerns methods for reducing cutaneous flushing in a patient to whom niacin is administered. According to the present method, two or more doses of a nonsteroidal anti-inflammatory drug are administered to a patient prior to administering niacin. Alternatively, the nonstcroidal anti-inflammatory drug can be administered concurrently with niacin administration. The nonstcroidal anti-inflammatory drug can be aspirin, ibuprofen, indomethacin, phenylbutazone, or naproxen. The nonsteroidal anti-inflammatory drug is administered in an amount effective to reduce cutaneous flushing caused by the niacin, and is administered in an amount up to 160 mg for aspirin and ibuprofen, 10 mg for indomethacin, and 100 mg for phenylbutazone and naproxen.

Abstract: An improved process for the production of a pharmaceutical composition comprising p-hydroxyacetanilide and L-cysteine or a compound which is converted thereto in vivo comprises mixing p-hydroxyacetanilide and L-cysteine or its precursor in the solid state and then shaping the solid mixture.

Abstract: To provide a therapeutic dose of an aqueous slurry of activated charcoal to a poisoning victim, an opaque straw is coated internally with a viscous flavoring solution and the slurry is sucked up from an opaque container using the straw. The use of natural and/or artificial sweeteners in the slurry masks the gritty particles and improves the taste.

Abstract: 2-oxopropanedioic acid is an extremely effective antidote for cyanide poisoning even at low doses.

Abstract: A method for accumulating drugs or other chemicals within synthetic, lipid-like vesicles by means of a pH gradient imposed on the vesicles just prior to use is described. The method is suited for accumulating molecules with basic or acid moieties which are permeable to the vesicles membranes in their uncharged form and for molecules that contain charge moieties that are hydrophobic ions and can therefore cross the vesicle membranes in their charged form.The method is advantageous over prior art methods for encapsulating biologically active materials within vesicles in that it achieves very high degrees of loading with simple procedures that are economical and require little technical expertise, furthermore kits which can be stored for prolonged periods prior to use without impairment of the capacity to achieve drug accumulation are described.

Abstract: A method and topical pharmaceutical composition for treating respiratory allergies, allergic rhinitis, allergic conjunctivitis, allergic asthma, and allergy to fur and dust, in which free ion calcium plays a role in a subject. The composition is in the form of oral local and/or nasal liquid solution or suspension for instillation, inhalation or insufflation and includes as active agent, at least one compound selected from the group consisting of: DL-.alpha.-glycerophosphoric acid, glutaric acid and their sodium or potassium salts as the essential active agent. The active agent, when supplied in a sufficient amount, being effective to enable by a reduction in free ion calcium concentration the removal or improvement in symptoms of allergy amenable to said free calcium ion concentration reduction.

Abstract: A method for inhibiting the metabolism of methanol in a human is disclosed. The method comprises administering a source of ethanol introduced into the respiratory tract of a human being, permitting the gradual time release of ethanol from the dietary vaccine into the respiratory tract for absorption into the blood stream of an individual.

Abstract: A method of preventing acetaminophen (APAP)-induced hepatotoxicity utilizing diallyl sulfide (DAS) and diallyl sulfone (DASO.sub.2) is disclosed. DAS and DASO.sub.2 are prepared as an oral dosage form or injected. In a preferred embodiment, diallyl sulfone is added to a dosage form of acetaminophen in an amount effective to prevent the metabolism of said unit dose of acetaminophen into its hepatotoxic metabolites. In certain preferred embodiments, the above formulations further include an effective amount of N-acetylcysteine to detoxify hepatotoxic metabolites of acetaminophen.

Abstract: Disclosed is a pharmaceutical composition comprising a dextrin derivative in which a proportion of the hydroxyl groups of dextrin are replaced by basic groups. Such compositions are useful for the treatment of acidic conditions.

Abstract: A prophylactic pretreatment for nerve gas and pesticide poisons which can be administered orally and which comprises the following agents, in combination: a. Pyridostigmine (pyridostigmine bromide) b. Diazepam c. N-methyl-4-pipyridinyl phenylcyclopentanecarboxylateThese agents may be administered in the form of a capsule which contains, for example, tablets, one a normal release dosage form and one or two in a slow release dosage form.

Abstract: A prophylactic pretreatment for nerve gas and pesticide poisons which can be administered orally and which comprises the following agents, in combination:a. Pyridostigmine (pyridostigmine bromide) or physostigmineb. Diazepam or clonazepamc. G 3063, Arpenal, Sycotrol (pipetabanate hydrochloride), caramiphen (caramiphene hydrochloride) or benactyzine (benactyzine hydrochloride).These agents may be administered in the form of a capsule which contains, for example, tablets, one a normal release dosage form and one or two in a slow release dosage form.

Abstract: A method of treating acid poisoning in mammals or of lowering blood cholesterol levels in mammals, which involves administering to the mammals a pharmaceutically effective amount of an aminated dextrin where amine groups or residues are present in an amount of from 0.5 to 2 groups per glucose unit.

Abstract: Products for cutaneous application with cosmetic and/or therapeutic effects, containing one or more active substances. This or these substances are carried by the microspheres of a polymer, dispersed in a liquid in which this polymer is not soluble.

Abstract: A dextrin derivative, in which a proportion of the hydroxyl groups in the dextrin have been replaced by strongly acidic groups, is useful in treatment of poisoning or drug overdose, particularly by compounds having basic groups. Dextrin sulphate is a preferred derivative for use in the treatment of paraquat poisoning.

Abstract: Disclosed herein are vesicle compositions for controlled sustained release of an encapsulated therapeutic agent after parenteral administration. By adjusting the osmolarity between the suspending solution and the solution within the vesicles by adjusting the concentration of the suspending solution, the rate of release of the therapeutic agent after parenteral administration can be varied. The compositions can be effectively administered by intramuscular, subcutaneous injection or other means.

Abstract: A method is provided for preventing reducing or reversing adverse reactions, such as pulmonary hypertension produced when protamine interacts with heparin, by administering a thromboxane A.sub.2 receptor antagonist.

Abstract: Calcium modulators can be effectively used to treat cardiovascular and cerebral toxicity induced by materials that alter the normal interaction of neurotransmitters with the calcium transport mechanisms of myocardial and cerebral cells. For example, calcium modulators can be used as an antidote to the lethal and chronic toxicity of cocaine and related indirectly acting sympathomimetic amines, imipramine and other tricyclic antidepressants, ganglionic stimulating drugs, and other toxic substances such as organophosphorus compounds that cause accumulations of neurotransmitters. Calcium modulators can also be used as an antidote to substances whose toxicity is based upon anticholinesterase activity. In addition, calcium modulators can be used as antagonists to the various types of toxic substances.

Abstract: Various types of biological treatments, including antineoplastic treatments with antineoplastic drugs, can result in damage to the blood-forming function of the bone marrow. This damage can be reversed, at least to some degree, with an effective amount (preferably an extremely low dose) of a pharmaceutically acceptable dithiocarbamic compound, including a compound of the formula R.sub.1 R.sub.2 NCSSM or R.sub.1 R.sub.2 NCSS-SCSNR.sup.3 R.sup.4, wherein R.sup.1, R.sup.2, R.sup.3, and R.sup.4 are the same or different aliphatic or cycloaliphatic or heterocycloaliphatic groups, unsubstituted or substituted by hydroxyl, or one of R.sup.1 and R.sup.2 and one of R.sup.3 and R.sup.4 can be H, or R.sup.1 and R.sup.2 or R.sup.3 and R.sup.

Abstract: An opiate antagonist or a pharmaceutically acceptable salt thereof is used to treat emotional numbness associated with Post Traumatic Stress Disorder and other psychopathologic conditions.

Abstract: Antidotes to the rat poison flupropadine and substances acting in the same way include compounds which modulate (e.g. inhibit) aminergic systems in the gut or adrenal tissues. Such compounds include tricyclic anti-depressants (e.g. chlorpromazine) and many others.

Abstract: Use of a physiologically inert hydrophobic molecular sieve material to lower the blood alcohol level in the human body in the form of an edible composition or a suppository, the material having a pore size permitting the absorption of ethanol but preventing the absorption of larger molecules with lipophilic character. The material may be a crystalline zeolitic material such as Silicalite or ZSM5.

Abstract: A botulinus toxin neutralizer comprising heat-treated fat globule membranes of animal milk or gangliosides isolated from fat globule membranes of animal milk. The neutralizer of the former nature is prepared from a material containing fat globules of animal milk by fractionating the material for separating the membranes of the fat globules from the rest of the material, and subjecting the separated fat globule membranes to heat treatment. The neutralizer of the former nature is prepared from a material containing fat globules by fractionating the material for separating the membranes of the fat globules from the rest of the material, and isolating gangliosides from the globule membranes.

Abstract: A means of aiding in the prevention of Sudden Infant Death Syndrome (SIDS) is disclosed. The means comprises administering a pharmaceutically effective amount of the drug 6-methylene-6-desoxy-N-cylopryplymethyl-14-hydroxydihydronormorphone to an infant determined to be susceptible to SIDS. The drug is preferably administered bi-daily via the GI tract. The drug attaches to the nerve receptor sites responsible for the actuation of respiration thus blocking the attachment of endogenous endorphins which, if present in high levels, prevents such actuation resulting in apnea and SIDS. A suppository containing the drug for use in carrying out the method is also disclosed.

Abstract: New tetrazole derivatives, characterized in that they correspond to the formula: ##STR1## in which R.sub.1 represents: either a hydrogen atom in any one of the positions 1 to 5 of the tetrazole nucleus, R designating a branched alkyl group comprising at least 5 carbon atoms or a branched alkenyl group, or a methyl group in position 2(3) of the tetrazole nucleus, R representing the (1-propyl)n butyl chain.These new derivatives are useful as medicaments, more especially for their anti-epileptic action.