56 results about "Alpha-2 adrenergic receptor" patented technology

The present invention relates to a method of treating, reducing, inhibiting, preventing and / or reversing cutaneous facial flushing caused by abnormal, endogenously-induced vasomotor instability associated with, but not limited to acne rosacea, menopause-associated hot flashes, hot flashes resulting from orchiectomy or ingestion of substances capable of inducing a cutaneous facial flushing reaction (e.g.: alcohol, chocolate, spices) by topical dermatological application of an effective dose of a composition comprising at least one α2 adrenergic receptor agonist (such as a (2-imidazolin-2-ylamino) quinoxaline derivative such as brimonidine tartrate)and a suitable carrier.

Biocompatible intraocular microspheres and implants include an alpha-2 adrenergic receptor agonist and a polymer associated with the alpha-2 adrenergic receptor agonist to facilitate release of the alpha-2 adrenergic receptor agonist into an eye for an extended period of time. The alpha-2 adrenergic receptor agonist may be associated with a biodegradable polymer matrix, such as a matrix of a two biodegradable polymers. The implants may be placed in an eye to treat or to prevent the occurrence of one or more ocular conditions, to reduce one or more symptoms of an ocular condition, such as an ocular neurosensory disorder and the like, to enhance normal retinal function and / or to lower intraocular pressure.

Methods and compositions for the treatment of pain using thiourea derivatives. Particularly disclosed are new compositions for the treatment of chronic pain, and methods for their use.

This document relates to methods and materials involved in treating skin disorders. For example, methods and materials for using an alpha adrenergic receptor agonist (e.g., midodrine) to treat mammals having a skin disorder are provided.

Compositions, and methods of use thereof, are provided for the prevention or treatment of side effects associated with the use of drugs that act as 5HT2 / 5HT3 serotonin receptor antagonists and alpha-2 adrenergic receptor antagonists (5HT2 / 5HT3 antagonist / alpha-2 antagonist). The method involves using dopamine-releasing compounds, such as amantadine, anticonvulsants, such as zonisamide, or dopamine / norepinephrine reuptake inhibitors, such as bupropion, in combination with 5HT2 / 5HT3 antagonist / alpha-2 antagonists, such as mirtazapine, to reduce the excessive daytime drowsiness and / or weight gain associated with 5HT2 / 5HT3 antagonist / alpha-2 antagonist use for the treatment of disorders, such as, depression, schizophrenia, anxiety disorders, sleep-related breathing disorders, insomnia, migraine headache, chronic tension-type headache, hot flashes, lower back pain, neuropathic pain and functional somatic syndromes. Formulations of dopamine-releasing compounds or anticonvulsants with 5HT2 / 5HT3 antagonist / alpha-2 antagonists are provided. In particular embodiments, combination therapy with mirtazapine and zonisamide provides relief from chronic low back pain, while reducing or avoiding side effects associated with monotherapy with mirtazapine or zonisamide.

The present study demonstrates that brimonidine tartrate, an alpha-2 adrenergic receptor agonist, can prevent photoreceptor cell degeneration and the associated Muller cell degenerative signs in an in vitro model of retinal degeneration and retinal detachment (separation of the neuroretina from the retinal pigment epithelium). Similar to control conditions, brimonidine allowed for the formation of highly structured photoreceptor outer segments, prevented the expression of stress markers in Müller cells and preserved the expression patterns of Muller cell markers of proper cell-cell contact and differentiation. Ultrastructural studies also indicated that brimonidine favored the formation of cell-cell junctions between photoreceptor cells and Müller cells, indicating that this phenomenon is associated with the exertion of the neuroprotective effect. The results suggest that brimonidine compounds may be utilized as an effective therapeutic agent for early and late onset retinal degenerations caused by defects in photoreceptor cells, Müller cells or both, and as an adjuvant to therapeutic success in retinal detachment surgery or macular translocation surgery for age-related macular degeneration.

Methods of reversing local anesthesia are disclosed. The methods comprise administering a local anesthetic and alpha adrenergic receptor agonist to induce local anesthesia followed by reversing anesthesia with a low dose of an alpha adrenergic receptor antagonist. Also disclosed are kits comprising a local anesthetic, an alpha adrenergic receptor agonist and a low dose of an alpha adrenergic receptor antagonist.

Combination therapies of an alpha-2 adrenergic receptor agonist and an alpha-2 adrenergic receptor antagonist at a concentration effective to potentiate but not antagonize a therapeutic effect of the alpha-2 adrenergic receptor agonist are provided. Also provided are methods for use of these combination therapies in potentiating the therapeutic effects of alpha-2 adrenergic receptor agonists, inhibiting development of acute and / or chronic tolerance to alpha-2 adrenergic receptor agonists and treating conditions treatable by alpha-2 adrenergic receptor agonist therapy in a subject. In addition, a method for reversing alpha-2 adrenergic receptor agonist tolerance and / or restoring therapeutic effect of an alpha-2 adrenergic receptor agonist in a subject via administration of an alpha-2 adrenergic receptor antagonist at a concentration effective to potentiate, but not antagonize, the therapeutic effect of the alpha-2 adrenergic receptor agonist is provided.

Methods and compositions for the treatment of pain and intraocular pressure. Particularly disclosed are new compositions for the treatment of chronic pain, glaucoma and methods for their use.

The invention generally relates to compositions and methods for treating and / or preventing an allergic response with reduced rebound hyperemia, comprising highly selective alpha-2 adrenergic receptor agonists, at low concentrations, such as below 0.05% weight by volume, and histamine antagonists. The compositions preferably comprise brimonidine. The compositions preferably have pH between about 5.5 and about 6.5.

The invention generally relates to compositions for inducing vasoconstriction. The compositions comprise highly selective alpha-2 adrenergic receptor agonists, at low concentrations, such as below 0.05% weight by volume. The compositions preferably comprise brimonidine. The compositions preferably have pH between about 5.5 and about 6.5.

The invention generally relates to compositions and methods for preferential vasoconstriction of smaller blood vessels relative to larger blood vessels. The compositions comprise highly selective alpha-2 adrenergic receptor agonists, at low concentrations, such as below 0.05% weight by volume. The compositions preferably comprise brimonidine. The compositions preferably have pH between about 5.5 and about 6.5.

The present invention concerns a pharmaceutical composition comprising an alpha-2 adrenergic receptor agonist for preventing or treating inflammatory pain and diseases in mucosa of oral cavity, pharynx and larynx. Inanother aspect the present invention provides mucosal bioadhesive slow release carriers for the extended and controlled release of alpha-2 adrenergic receptor agonists that can be used on mucosal surfaces for preventing or treating inflammatory pain and diseases in mucosa of oral cavity.

A compound having selective modulating activity at the alpha 2B and / or alpha 2C adrenergic receptor subtypes is represented by the general Formula 1:whereinn=1-4;X is C or N;R1-R6 can be the same or different and are independently selected from the group consisting of H, C1-6 alkyl, OCH3, OH, F, Cl, Br, CH2OH, CH2N(R7)2, C(O)R8, CH2CN, CF3;wherein R7 is H or C1-6 alkyl; andR8 is C1-6 alkyl or aryl.The compounds of Formula 1 can be incorporated in pharmaceutical compositions and used in methods of treatment of alpha 2 receptor mediated diseases and conditions.

The present invention includes polymorphisms in nucleic acids encoding the alpha-2B, alpha-2A, and alpha-2C adrenergic receptor and expressed alpha-2B, alpha2A and alpha-2C adrenergic receptor molecule. The invention also pertains to methods and molecules for detecting such polymorphisms. The invention further pertains to the use of such molecules and methods in the diagnosis, prognosis, and treatment of diseases such as cardiovascular and central nervous system disease.

The present invention includes polymorphisms in nucleic acids encoding the alpha-2B, alpha-2A, and alpha-2C adrenergic receptor and expressed alpha-2B, alpha-2A and alpha-2C adrenergic receptor molecule. The invention also pertains to methods and molecules for detecting such polymorphisms. The invention further pertains to the use of such molecules and methods in the diagnosis, prognosis, and treatment of diseases such as cardiovascular and central nervous system disease.

The invention generally relates to compositions and methods for reducing capillary permeability. The compositions comprise highly selective alpha-2 adrenergic receptor agonists, at low concentrations, such as below 0.05% weight by volume. The compositions preferably comprise brimonidine. The compositions preferably have pH between about 5.5 and about 6.5.

The present invention concerns a pharmaceutical composition comprising an alpha-2 adrenergic receptor agonist for preventing or treating inflammatory pain and diseases in mucosa of oral cavity, pharynx and larynx. In another aspect the present invention provides mucosal bioadhesive slow release carriers for the extended and controlled release of alpha-2 adrenergic receptor agonists that can be used on mucosal surfaces for preventing or treating inflammatory pain and diseases in mucosa of oral cavity.

The present invention includes polymorphisms in nucleic acids encoding the alpha-2B adrenergic receptor and expressed alpha-2B adrenergic receptor molecule. The invention also pertains to methods and molecules for detecting such polymorphisms. The invention further pertains to the use of such molecules and methods in the diagnosis, prognosis, and treatment of diseases such as cardiovascular and central nervous system diseases.

Methods and compositions for the treatment of pain. Particularly disclosed are new compositions for the treatment of chronic pain, and methods for their use.

The invention generally relates to compositions for inducing vasoconstriction. The compositions comprise highly selective alpha-2 adrenergic receptor agonists, at low concentrations, such as below 0.05% weight by volume. The compositions preferably comprise brimonidine. The compositions preferably have pH from about 4.0 to about 7.5.

The present invention includes polymorphisms in nucleic acids encoding the alpha-2A adrenergic receptor and expressed alpha-2A adrenergic receptor molecule. The invention also pertains to methods and molecules for detecting such polymorphisms and transgenic animals expressing alpha-2A adrenergic receptor molecules. The invention further pertains to the use of such molecules and methods in the diagnosis, prognosis, and treatment of diseases such as cardiovascular and central nervous system diseases.

The present invention relates to an ophthalmic composition comprising at least two active pharmaceutical ingredients. In particular, the active pharmaceutical ingredients are selected from the group consisting of: an alpha 2 adrenergic receptor agonist; a beta-adrenergic receptor agonist; an immunosuppressant; a lymphocyte associated antigen antagonist; an anti-inflammatory; a beta-blocker; a prostaglandin analog; a histamine receptor antagonist; a carbonic anhydrase inhibitor; and an antibiotic. In some embodiments, the composition of the invention is a nanoemulsion formulation. In one particular embodiment, the first active pharmaceutical ingredient is an alpha 2 adrenergic receptor agonist. The present invention also provides a method for treating various clinical conditions associated with an eye disorder or eye disease using the composition of the invention.

The invention relates to a method of treating capillary hemangiomas in a human in need thereof by topically administering an effective amount of one or more alpha-2 adrenergic receptors agonist to the site of the capillary hemangiomas on the skin of the human.

The invention provides well-defined heterocyclic compounds that are useful as subtype selective alpha 2 adrenergic agonists. As such, the compounds described herein are useful in treating a wide variety of disorders associated with selective subtype modulation of alpha 2 adrenergic receptors.

The present invention provides an aqueous ophthalmic composition comprising an alpha-2 adrenergic receptor agonist and a non-ionic cellulosic polymer, the solution having a pH less than 6.5. The present invention also provides an aqueous ophthalmic composition comprising an alpha-2 adrenergic receptor agonist and a benzododecinium halide. Also provided are methods of manufacture, use and method of reducing intraocular pressure in the patient in need thereof.