Abstract: Stable, topically applicable oil-in-water bioaffecting emulsions having intermediate viscosity, characteristically ranging from 3 to 10 Pa.multidot.s, comprise (a) from 30% to 50% by weight of at least one pro-penetrating glycol, (b) at least one emulsifying agent, advantageously an anionic amphiphilic polymer, and (c) at least one biologically active agent, for example an active agent that modulates skin differentiation and/or proliferation and/or pigmentation, an anti-inflammatory, an antibacterial, an antifungal, etc.

Abstract: Methods of treating a host suffering from neuroma pain are provided. In the subject methods, a topical local anesthetic composition is applied to a keratinized skin site of the host proximal to the neuroma responsible for the neuroma pain. Preferably, the topical local anesthetic composition comprises eucalyptol in addition to an effective amount of a local anesthetic. The subject methods find particular use in the treatment of pain associated with Morton's neuroma.

Abstract: Anesthetic compositions that achieve enhanced anesthesia of the peripheral nerves located in the mouth region of a subject or patient are provided. Such anesthetic compositions comprise water, a local anesthetic agent, and a sugar alcohol at a concentration of at least 0.1 moles/L i.e., at least 0.1 M. A method of anesthetizing a peripheral nerve of the mouth region is also provided. The method comprises: providing an anesthetic composition comprising water, a local anesthetic agent, and a sugar or, preferably, a sugar alcohol at a concentration of at least 0.1 M; and administering said anesthetic composition to a site proximate to said peripheral nerve.

Abstract: A method of relieving neuropathic pain uses moxonidine and its physiologically compatible acid-addition salts for the treatment and/or prophylaxis of neuropathic pain. A composition comprising an effective amount of moxonidine, or a pharmaceutically acceptable salt thereof, in a pharmaceutically acceptable carrier, is administered to a subject in need of such treatment. The composition may be administered intrathecally.

Abstract: The use of glucocorticosteroids in methods and formulations for prolonging and/or reactivating local anesthesia or local anesthesia previously induced by a local anesthetic agent, is disclosed.

Abstract: A method of producing local anesthesia in a mammal experiencing pain in an epithelial tissue region is described. The method includes topically administering to the region, in a suitable pharmaceutical vehicle, an effective dose of a long-acting sodium channel blocking compound.

Abstract: The invention is directed to a novel pharmaceutical composition comprising one or more local anaesthetics in oil form, one or more surfactants, water and optionally a taste masking agent. The novel composition is advantageously used as a local anaesthetic for pain relief within the oral cavity.

Abstract: A composition for local anesthesia which comprises (A) lidocaine, (B) a catecholamine such as epinephrine in an amount of, for example, 1/200,000 (g/ml) based on the volume of the composition, and (C) one or more amino acids such as glycine, glutamic acid, and L-glutamic acid-L-lysine or one or more hydroxycarboxylic acids such as lactic acid, glycolic acid, and citric acid, which has a duration suitable for short-time dental operations such as tooth extraction and excellent storage stability.

Abstract: Methods of inducing genetic material into cells of an individual and compositions and kits for practicing the same are disclosed. The methods comprise the steps of contacting cells of an individual with a polynucleotide function enhancer and administering to the cells, a nucleic acid molecule that is free of retroviral particles. The nucleic acid molecule comprises a nucleotide sequence that encodes a protein that comprises at least one epitope that is identical or substantially similar to an epitope of a pathogen antigen or an antigen associated with a hyperproliferative or autoimmune disease, a protein otherwise missing from the individual due to a missing, non-functional or partially functioning gene, or a protein that produces a therapeutic effect on an individual. Methods of prophylactically and therapeutically immunizing an individual against HIV are disclosed. Pharmaceutical compositions and kits for practicing methods of the present invention are disclosed.

Abstract: The present invention is a method for enhancing the analgesic efficacy of a locally applied opioid analgesic or local anesthetic agent in a mammal having an impermeable perineurium barrier sheet about the peripheral sensory nerves at the site of action of the analgesic or anesthetic agent. The method involves applying to that site an effective amount of the analgesic or anesthetic agent dissolved in a hyperosmolar solution having an osmolality of above 300 mOsm/l.

Abstract: A formulation and methods for inducing sustained regional local anesthesia in a patient comprising a substrate comprising a local anesthetic and an effective amount of a biocompatible, biodegradable, controlled release material prolonging the release of the local anesthetic from the substrate to obtain a reversible local anesthesia when implanted or injected in a patient, and a pharmaceutically acceptable, i.e., non-toxic, non-glucocorticoid augmenting agent effective to prolong the duration of the local anesthesia for a time period longer than that obtainable from the substrate without the augmenting agent.

Abstract: The present invention relates to an injectable solution for administration of one or more active compounds. According to the invention the active compound, which is in its neutral form, is dissolved in a biologically acceptable solvent whereby the active compound by administration precipitates, forming a solid phase of the solution in situ. Thus, said solution, which is easy to sterilize, is acting like a suspension when injected.

Abstract: A water-based topical analgesic and method of application wherein the analgesic contains capsicum, capsicum oleoresin and/or capsaicin. This analgesic is applied to the skin to provide relief for rheumatoid arthritis, osteoarthritis, and the like.

Abstract: Prilocaine base, in liquid and micro rod crystal form, can be solubilized within hydrofluorocarbon propellants to produce a stable, oily liquid. The prilocaine base can be used to solubilize additional medicaments within hydrofluorocarbon propellants that are not ordinarily soluble. The combination of prilocaine base and hydrofluorocarbon propellant can be used as an aerosolized spray to provide topical anesthesia.

Abstract: New combination of a .beta.-receptor blocker, an enantiomer thereof, and a local anesthetic, administered simultaneously or sequentially, giving excellent pain relief. Also comprised in the invention is the use of a non-selective .beta.-receptor blocker alone, especially a non-selective .beta.-receptor blocker giving pain relief.

Abstract: A method of immunizing an individual against pathogen is disclosed. Also disclosed is a method of treating an individual who has a hyperproliferative disease, or of treating an individual who is infected by a pathogen. Specifically, the individual is injected with bupivacaine along with DNA in an expressible form, the DNA encoding an antigen. The encoded antigen can be from a protein from the pathogen or from a protein associated with the hyperproliferative disease.

Abstract: Medicated plasters composed of a flexible support and a pressure-sensitive adhesive layer laminated thereon, in which said pressure-sensitive adhesive layer has an exposed surface with pH of 7 or higher and contains one of the following three components:i) a basic physiologically active agent and an acidic substance,ii) a salt of a basic physiologically active agent and a basic substance, andiii) a basic physiologically active agent and a salt of a basic physiologically active agent.

Abstract: Infusions of brain-derived neurotrophic factor, neurotrophin-3 or neurotrophin-4 are used to produce analgesia in mammals. In addition, these neurotrophins are used to treat other diseases or disorders mediated by serotonin.

Abstract: Methods of prophylactic and therapeutic immunization of an individual against pathogen infection, diseases associated with hyperproliferative cells and autoimmune diseases are disclosed. The methods comprise the steps of administering to cells of an individual, a nucleic acid molecule that comprises a nucleotide sequence that encodes a protein which comprises at least one epitope that is identical or substantially similar to an epitope of a pathogen antigen, a hyperproliferative cell associated protein or a protein associated with autoimmune disease respectively. In each case, nucleotide sequence is operably linked to regulatory sequences to enable expression in the cells. The nucleic acid molecule is free of viral particles and capable of being expressed in said cells. The cells may be contacted cells with a cell stimulating agent. Methods of prophylactically and therapeutically immunizing an individual against HIV are disclosed.

Abstract: A composition for topical therapy for symptoms of back pain, muscle tension or myofascial pain or a combination thereof, which comprises a topical carrier system for intact skin of the back or outer synovial membranes or both, which comprises a therapeutic dose of a local anesthetic, and which applies the local anesthetic to a region of skin lying beneath the topical carrier system.

Abstract: A formulation for inducing sustained regional local anesthesia in a patient comprising a substrate comprising a local anesthetic and an effective amount of a biocompatible, biodegradable, controlled release material prolonging the release of the local anesthetic from the substrate to obtain a reversible nerve blockade when implanted or injected in a patient, and an amount of colchicine effective to prolong the duration of the local anesthesia for a time period longer than that obtainable from the substrate without colchicine.

Abstract: Biodegradable controlled release microspheres for the prolonged administration of a local anesthetic agent, and a method for the manufacture thereof are disclosed. The microspheres are formed of a biodegradable polymer degrading significantly within a month, with at least 50% of the polymer degrading into non-toxic residues which are removed by the body within a two week period. Useful polymers include polyanhydrides, polylactic acid-glycolic acid copolymers and polyorthoesters containing a catalyst; polylactic acid-glycolic acid copolymers are preferred. Local anesthetics are incorporated into the polymer using a method that yields a uniform dispersion, preferably solvent casting. Prolonged release is obtained by incorporation of a glucocorticoid into the polymeric matrix or by co-administration of the glucocorticoid with the microspheres. The type of anesthetic and the quantity are selected based on the known pharmaceutical properties of these compounds.

Abstract: This invention relates to a mixture of homologous narrow range lauryl polyglycol ethers, to its use as a local anaesthetic agent.

Abstract: The present invention relates to an anaesthetic veterinary pharmaceutical composition, comprising a general anaesthetic selected from phencyclidine derivatives such as ketamine or tiletamine, as well as 0.015 to 1.25 molar equivalents of selegiline, combined in a single pharmaceutical composition or presented separately.

Abstract: The present invention relates to stabilized topical pharmaceutical preparations. More specifically the present invention relates to a stabilized topical pharmaceutical preparation, based on the solubilization of a eutectic mixture of local anesthetic agents, in base form, which when combined in the presence of a surfactant and water produce a single phase hydrated polymer to be used in obtaining topical anesthesia and also relates to a stabilized antimicrobial topical pharmaceutical preparation.

Abstract: An improved biodegradable controlled release system consisting of a polymeric matrix incorporating a local anesthetic for the prolonged administration of the local anesthetic agent, and a method for the manufacture thereof, are disclosed. The polymers and method of manufacture used to form the PLAMs are selected on the basis of their degradation profiles: release of the topical anesthetic in a linear, controlled manner over a period of preferably two weeks and degradation in vivo with a half-life of less than six months, more preferably two weeks, to avoid localized inflammation. Alternatively, a non-inflammatory can be incorporated into the polymer with the local anesthetic to prevent inflammation.

Abstract: Methods of prophylactic and therapeutic immunization of an individual against pathogen infection, diseases associated with hyperproliferative cells and autoimmune diseases are disclosed. The methods comprise the steps of administering to cells of an individual, a nucleic acid molecule that comprises a nucleotide sequence that encodes a protein which comprises at least one epitope that is identical or substantially similar to an epitope of a pathogen antigen, a hyperproliferative cell associated protein or a protein associated with autoimmune disease respectively. In each case, nucleotide sequence is operably linked to regulatory sequences to enable expression in the cells. The nucleic acid molecule is free of viral particles and capable of being expressed in said cells. The cells may be contacted cells with a cell stimulating agent. Methods of prophylactically and therapeutically immunizing an individual against HIV are disclosed.

Abstract: An article of manufacture in the form of a gel pharmaceutical formulation for local anesthesia is prepared by a process comprising: coating a supporting substrate, which preferably is porous, e.g., a non-woven fabric, and has an impervious backing sheet, with a matrix of a copolymer of alkyl (meth)acrylates and (meth)acrylic acid and a local anesthetic whereby the matrix penetrates the substrate, crosslinking the copolymer in the matrix to form a polymer/drug matrix, and coating the surface of the matrix with an aqueous fluid, thereby converting the matrix into a gel and preferably covering the gel matrix with an impervious protective sheet. The product has excellent percutaneous absorption, provides local anesthesia easily just by attaching the formulation to the skin, enables elimination of various kinds of pain, such as the pain at the time of hypodermic injection, can be removed easily from the skin, and causes no soiling of fingers, hands or cloths.

Abstract: Aerosol compositions used for anesthetizing mammals in both human and veterinary applications include prilocaine base solubilized in the hydrofluorocarbon (HFC) propellants 1,1,1,2-tetrafluoroethane and 1,1,1,2,3,3,3-heptafluoropropane. Prilocaine base has been found to be readily soluble in HFC propellants when combined in liquid or micro rod form, and a solution stable to temperatures as low as -82.degree. C. is formed upon combination of the two components. In the aerosol compositions, the HFCs are the only propellants used. Additional pharmaceutical constituents can also be combined the the prilocaine base/HFC composition to provide a multi-component anesthetic, and it has been found that the presence of prilocaine in the combination can assist in solubilizing and/or suspending these pharmaceutical consituents.

Abstract: The present invention provides a topical anesthetic gel composition, comprising: (a) one or more topical anesthetic agents; (b) an adrenergic sympathomimetic compound; and (c) a pharmaceutical gel component. The present invention also provides a topical anesthetic gel composition, comprising: (a) tetracaine HCl, wherein said tetracaine HCl is contained in said composition in an amount of from about 0.01% to about 1.0% by weight, based upon the total weight of said composition; (b) epinephrine HCl topical solution, wherein said epinephrine HCl is contained in said composition in an amount of from about 0.04% to about 0.1% by weight, based upon the total weight of said composition; (c) cocaine HCl, wherein said cocaine HCl is contained in said composition in an amount of from about 3.0% to about 12.0% by weight, based upon the total weight of said composition; and (d) GELFOAM.RTM., wherein said Gelfoam.RTM. is contained in said composition in an amount of from about 6.0% to about 9.

Abstract: Controlled-release particles containing biologically effective agents such as therapeutic drugs and local anesthetics are suspended in a liquid suspending vehicle which has an elevated viscosity, the viscosity being substantially higher than that of water. Preferred vehicles are non-aqueous liquids and aqueous media which contain a dissolved polymer to increase the viscosity of the vehicle. Regardless of the composition of the media, however, the increased viscosity permits the use of particles of a relatively large size without a loss of suspension stability or localized application. The large particles offer the advantage of a longer release profile, and thus more prolonged activity of the agent.

Abstract: Clear and stable aerosol formulations including both lidocaine base and vasoconstricting agents have been produced. This combination of medicaments are dissolved in suitable hydrofluorocarbon propellants with additional organic solvent as required. The lidocaine base serves to improve the solubility of the vasoconstricting agent and reduce the concentration of organic solvent required. This aerosol combination is designed for nasal application to cause topical anesthesia and concomitant vasoconstriction in preparation for nasal examination or instrumentation. It is also suitable for application to other anatomical sites such as the upper airway, anus and genital tract.

Abstract: The present invention is directed to a method for anesthetizing teeth which does not require an injection into the gum in order to anesthetize a tooth (or teeth) which requires attention. The method comprises the step of applying a composition having a high concentration of potassium to a tooth requiring caries removal or manual manipulation thereof. The composition is adapted to anesthetize the tooth so that the tooth may be drilled or manually manipulated. It has been discovered that the potassium enters the dentinal tubules and odontoblastic fibrils and penetrates the pulpal tissues of the tooth for anesthetizing the tooth without having to inject anesthetics into the gum surrounding the tooth.

Abstract: An anesthetic pharmaceutical combination comprising the combination of a local anesthetic and lithium ions present in an amount effective to lower the amount of the local anesthetic necessary to achieve equivalent anesthetic effect in a patient and a method of use of the anesthetic pharmaceutical combination.

Abstract: Non-volatile general anesthetics are advantageously provided to patients in aerosolized form using a metered dose inhaler. The anesthetics are highly lipophilic in character and are rapidly absorbed through the nasal, oral, and lung mucosa. Experiments have shown that propofol is readily soluble in hydrofluorocarbon propellants without the use of surfactants and co-solvents. The solubility allows for the controlled delivery of concentrated pure anesthetic agents like propofol to the airway mucosa of human and animal patients to cause rapid onset of sedation or anesthesia without the requirement of prior intravenous access.

Abstract: A method is provided for loading a delivery system for a chemical repellant composition. An aqueous mixture comprising one part water-soluble isothiuronium salt and two parts weak base is prepared. Capsaicin is added to the aqueous mixture before it is loaded into the delivery system. A fluorescent compound, such as dichlorofluorescine, may also be added to the aqueous mixture and capsaicin before loading the delivery system.

Abstract: A composition for topical application comprising a therapeutically effective amount of a pharmaceutical agent(s), a flexible, finite, pharmaceutically acceptable, bioadhesive carrier, and a solvent for the pharmaceutical agent(s) in the carrier and a method of administering the pharmaceutical agent to a mammal are disclosed.

Abstract: A method for treatment of ulcerative colitis (and sequelae to surgically treated colitis, for instance ileal pouchiris) and ulcerative proctitis comprising administration to a patient suffering therefrom of a therapeutically effective amount of a local anaesthetic or a pharmaceutically acceptable salt thereof, preferably lidocaine hydrochloride in the form of a pharmaceutically acceptable preparation.

Abstract: A method of using veratridine to inhibit nerve impulses, and a composition of matter including veratridine and epinephrine, is provided. Application of veratridine proximal to a nerve causes depolarization of the nerve membrane, thereby blocking transmission of nerve impules. C-fiber selectivity is demonstrated in vitro in rabbit vagus nerves. Veratridine displays extended anesthetic activity over long periods of time when compared to similar local anesthetics, with no local toxicity. Systemic toxicity is reduced by co-injection with epinephrine.

Abstract: Disclosed are hybrid paucilamellar lipid vesicles containing a phospho- or glycolipid and a nonionic, anionic, or zwitterionic surfactant in the lipid bilayers. The paucilamellar vesicles may have either an aqueous or oil-filled central cavity. A method of manufacture for these vesicles is also disclosed.

Abstract: Liposome encapsulated local anesthetic or analgesic agents when applied to skin or mucous membranes provided greater local anesthesia and analgesia than the same agents incorporated in conventional vehicles i.e., ointment, cream or lotion.

Abstract: There is disclosed an injectable anesthetic pharmaceutical composition which does not exhibit muscle rigidity and which includes an anesthetic effective amount of at least one substituted N-(4-piperidinyl)-N-amide and a muscle rigidity inhibiting effective amount of at least one alpha-2 adrenergic agonist as principle ingredients. Also disclosed are methods of inducing and maintaining anesthesia without muscle rigidity by administering said composition to warm blooded animals.

Abstract: Pharmaceutical compositions in the form of a buccal tablet comprising etorphine or a salt thereof, at least one monosaccharide, disaccharide or a mixture thereof, and a mixture of xanthan gum and locust bean gum in a weight ratio 3:1 to 1:1, wherein the total weight of the mono- and/or di-saccharides relative to the combined weight of the xanthan and locust bean gums is in the ratio of 20:1 to 3:1. The tablet affords improved bioavailability.

Abstract: A method of inducing analgesia or reducing pain is described. The method involves implanting in the central nervous system of a host susceptible to pain, living material capable of releasing effective amount of analgesic substance when interacted with a stimulus which induces said material to release analgesic amount of said substance. The procedure described herein reduces sensitivity to intractable pain.

Abstract: A composition and method of use for the treatment of pain and inflammation associated with lesions of the skin or mucus membrane, such as herpes simplex, herpes labialis, herpes progenitalis, chickenpox lesions, herpes genitalis, sensitivity of gingival tissue due to procedures for etching teeth with HCl, swollen gums, cheilosis, oral traumatic injuries, aphthous ulcer, by applying to the lesion an effective amount of a topical composition comprising diphenhydramine HCl, lidocaine HCl, aloe vera gel, propolis and sufficient base to raise the pH to 8-9.

Abstract: Microdroplets of water-insoluble drugs coated with a phospholipid are prepared by sonication. As an example, microdroplets of the general anesthetic methoxyfluorane coated by a unimolecular layer of dimysistoyl phosphatidylcholine are prepared by sonication. The microdroplets so prepared remain stable in physiologically-compatible solution, and are suitable for injection, typically intradermally or intraveneously, into a patient for inducing local anesthesia. These methoxyflurane-containing microdroplets have been demonstrated to cause long-term local anesthesia when injected intradermally, giving duration of anesthesia 28 times longer than with other anesthetics, such as lidocaine and 11 times longer than with bupivacaine. The latter is considered longest acting conventional local anesthetic.

Abstract: The local anesthetic, L-N-n-propylpipecolic acid-2,6-xylidide, namely: ##STR1## This compound is prepared by chlorinating L-pipecolic acid to yield the acid chloride, namely L-pipecolic acid chloride. The acid chloride is then reacted with 2,6-xylidine to yield L-pipecolic acid-2,6-xylidide. The L-N-pipecolic acid-2,6-xylidide is then propylated to yield the L-N-n-propylpipecolic acid-2,6-xylidide, which is a potent local anesthetic for humans and is of relatively low toxicity.

Abstract: Improved methods of anesthesia for mammals, especially humans, are provided wherein the prolonging effect upon local anesthesia which is exhibited by co-administration of vasoconstrictors, especially vasoconstrictors believed to act upon alpha adrenoreceptor sites on blood vessel walls, are provided. In accordance with a preferred embodiment, alpha adrenoreceptor blocking agents are aministered subsequent to the performance of surgery or dentistry under local anesthesia accomplished through co-administration of anesthesia and vasoconstrictor to cause reduction of prolonged anesthetic effect. Seriatim procedures are facilitated under local anesthesia through employment of the present invention. Improved patient aesthetics, diminution of self-inflicted trauma, and increased sensory feedback from patients are among the benefits conferred by the present invention.

Abstract: Local anesthesia is induced using microdroplets of a general anesthetic in liquid form. As an example, microdroplets of the general anesthetic methoxyfluorane coated by a unimolecular layer of dimysistoyl phosphatidylcholine are prepared by sonication. The microdroplets so prepared remain stable in physiologically-compatible solution, and are suitable for injection, typically intradermally or intraveneously, into a patient for inducing local anesthesia. These methoxyflurane-containing microdroplets have been demonstrated to cause long-term local anesthesia when injected intradermally, giving duration of anesthesia 28 times longer than with other anesthetics, such as lidocaine and 11 times longer than with bupivacaine.