31 results about "OPIOID TOLERANCE" patented technology

The invention provides methods and compositions for inhibiting opioid tolerance by administering an A₃AR agonist to a subject receiving opiate therapy for nociceptive pain. Also provided are methods of treating opiate withdrawal using an A₃AR agonist.

The invention relates to BCAT inhibitors and the use thereof for treating or preventing neuronal loss associated with stroke, ischemia, CNS trauma, hypoglycemia and surgery, as well as treating neurodegenerative diseases including Alzheimer's disease, amyotrophic lateral sclerosis, Huntington's disease and Down's syndrome, treating or preventing the adverse consequences of the overstimulation of the excitatory amino acids, treating anxiety, psychosis, convulsions, aminoglycoside antibiotics-induced hearing loss, migraine headache, chronic pain, neuropathic pain, Parkinson's disease, diabetic retinopathy, glaucoma, CMV retinitis, urinary incontinence, opioid tolerance or withdrawal, and inducing anesthesia, as well as for enhancing cognition.

The present invention provides composition of matter for and methods of treating pain and drug abuse using novel chimeric hybrid molecules containing an opioid moiety of chemically modified morphine (3) that binds to and activates the human mu (μ) opioid receptor, with the opioid moiety linked through a novel linker-hinge (4) to a substance P peptide fragment moiety (5) that binds to and activates the human substance P receptor. The hybrid alkaloid/peptide chimeric molecules produce clinically efficacious opioid analgesia with little or no development of opioid tolerance or formation of opioid dependence. The hybrid alkaloid/peptide analgesics may be administered intrathecally, systemically or orally.

The invention discloses novel application of stilbene glycoside to the field of analgesic medicine, and particularly discloses application of stilbene glycoside to preparing medicine for enhancing analgesic effects of opioid medicine and delaying or relieving opioid tolerance. The application has the advantages that the stilbene glycoside is used with the opioid medicine, or compound preparations are made of the stilbene glycoside and the opioid medicine, so that the analgesic time can be prolonged, the analgesic efficacy can be enhanced, and opioid tolerance during chronic opioid medicine treatment procedures can be delayed or relieved; excessive activation of spinal glial cells induced by the opioid medicine is particularly suppressed by the stilbene glycoside, so that effects can be realized.

The invention relates to BCAT inhibitor compounds of formula (I) and use thereof for treating or preventing neuronal loss associated with stroke, ischemia, CNS trauma, hypoglycemia and surgery, as well as treating neurodegenerative diseases including Alzheimer's disease, amyotrophic lateral sclerosis, Huntington's disease and Down's syndrome, treating or preventing the adverse consequences of the overstimulation of the excitatory amino acids, treating anxiety, psychosis, convulsions, aminoglycoside antibiotics-induced hearing loss, migraine headache, chronic pain, neuropathic pain, Parkinson's disease, diabetic retinopathy, glaucoma, CMV retinitis, urinary incontinence, opioid tolerance or withdrawal, and inducing anesthesia, as well as for enhancing cognition.

The invention discloses novel application of paeoniflorin in the field of analgesics, and in particular relates to application of paeoniflorin in preparation of a medicine for reinforcing the analgesic effect of opioid medicines, and retarding or reducing the opioid tolerance. The application of paeoniflorin matched with opioid medicines or compound preparation prepared from paeoniflorin and opioid medicines can be used for prolonging the analgesic time of opioid medicines and strengthening the analgesic effect of opioid medicines, and can retard or reduce the opioid tolerance phenomenon in the treatment process of opioid medicines. The effect can be realized by using p-P38 of paeoniflorin in inhibiting opioid medicine induced over activation of spinal microglial cells and inhibiting opioid induced over up-regulation.

The present invention discloses the new application of Corydalis CDL (CDL) in the field of analgesic drugs, and specifically discloses the application of CDL in the preparation of drugs for preventing or treating analgesic tolerance of opioid analgesic drugs. The corydalis dammine is used in combination with opioids, or used in compound preparations with opioids, which can enhance its analgesic effect and prevent or alleviate opioid tolerance in the course of chronic opioid treatment. This effect is achieved by inhibiting opioid-induced excessive activation of spinal cord microglial cells, and inhibiting opioid-induced excessive up-regulation of p-P38, p-ERK and p-JNK.

The present invention relates to compositions and methods for managing opioid tolerance and reducing opioid withdrawal. More specifically, the present invention provides for endothelin, endothelin receptors, and endothelin receptor antagonists and agonists as a means for managing G-protein activity in the context of opioid tolerance and withdrawal.

The invention discloses new application of puerarin to preparing a pain easing medicine, and particularly discloses the application of the puerarin to preparing the medicine for strengthening the opioid medicine pain easing effect and delaying or alleviating the opioid tolerance. When the puerarin is matched with an opioid medicine to be used, or the puerarin and the opioid medicine are prepared into a compound preparation to be used, the pain easing time of the medicine can be prolonged, the pain easing efficiency can be strengthened, and the opioid tolerance in the opioid medicine treatment process can be further delayed or alleviated. The effect is specifically achieved by restraining spinal glial cell overactivity induced by the opioid medicine through the puerarin.

Methods of preventing the development and reversing or partially reversing opioid tolerance in a subject are provided herein. Such methods include the step of administering to a subject in need thereof a therapeutically effective amount of a PDGFR modulator or EGFR modulator alone or together with an opiate analgesic. The methods can also be used for the treatment of refractory neuropathic pain, physical dependence or addiction.

The present disclosure is directed to a method of treating morphine tolerance and/or symptoms associated therewith by administration to a subject in need thereof a DN-TNF polypeptide that inhibits the activity of soluble TNF- but not transmembrane TNF-α.

The invention relates to BCAT inhibitors and the use thereof for treating or preventing neuronal loss associated with stroke, ischemia, CNS trauma, hypoglycemia and surgery, as well as treating neurodegenerative diseases including Alzheimer's disease, amyotrophic lateral sclerosis, Huntington's disease and Down's syndrome, treating or preventing the adverse consequences of the overstimulation of the excitatory amino acids, treating anxiety, psychosis, convulsions, aminoglycoside antibiotics-induced hearing loss, migraine headache, chronic pain, neuropathic pain, Parkinson's disease, diabetic retinopathy, glaucoma, CMV retinitis, urinary incontinence, opioid tolerance or withdrawal, and inducing anesthesia, as well as for enhancing cognition.

The invention discloses a new application of ligustrazine in the field of analgesic drugs, and particularly discloses an application of the ligustrazine in preparation of medicines for enhancing the analgesic effect of opioid agents, and delaying or relieving the opioid tolerance. The ligustrazine is matched with the opioid agents for use, or is prepared into a compound preparation together with the opioid agents for use; the analgesic time can be prolonged; the analgesic effect can be enhanced; the phenomenon of opioid tolerance caused in the treatment process of the chronic opioid agents can also be delayed or relieved; and the ligustrazine has the specific effects of inhibiting excessive activation of spinal microglia induced by the opioid agents through the ligustrazine and inhibiting realization of excessive increase p-P38 induced by opioid.

Opioid tolerance is reduced by treating the patient with a neurosteroid of formula (I) wherein R1 is H or methyl; R2 is OH and R3 is H, or R2 and R3 taken together are O; R4 is H or methyl; R5 and R6 are each H, or R5 and R5 taken together are O; R7 is H or methyl; and R8 is H, OH, —OC(═O)CH3, SH, —SC(═O)CH3, Cl, Br or F.

The invention discloses new application of matrine in the field of analgesic drugs, and particularly discloses application of matrine in preparing drugs enhancing the analgesic effect of opioid, and delaying or relieving opioid tolerance. The matrine is matched with the opioid for use, or the matrine and the opioid are prepared into compound preparations for use, the analgesia time of the opioid can be prolonged, the analgesic efficacy of the opioid can be enhanced, and the opioid tolerance phenomenon happening in the treating process of opioid slow in taking effect can also be delayed or relieved. Specifically, the effect is achieved in the mode that the matrine is used for inhibiting excessive activation, induced by the opioid, of spinal cord glial cells.

The invention provides a D-amino-acid oxidase inhibitor for preventing and/or reversing opioid tolerance and a method for preventing or reversing opioid tolerance by the use of the D-amino-acid oxidase inhibitor, and also provides a method for preventing and/or treating ache by the use of the D-amino-acid oxidase inhibitor and a method for identifying the compound for preventing and/or reversing opioid tolerance.

The invention discloses an application of seabuckthorn flavone in the preparation of compositions for enhancing the drug effect of opioids. Compared with applications in the prior art, the application has the advantages of substantial prolongation of the pain easing time of the opioids, enhancement of the pain easing effect of the opioids, and delaying of opioid tolerance caused by the opioids through synergism realized by common use of the seabuckthorn flavone and the opioids.

The present invention provides a method for treating cancer pain by administering to an individual in need of such treatment with a pharmaceutically effective amount of a blocking reagent for ephrinB-EphB signaling. Also provided is a method for reducing opioid tolerance in treating cancer pain thereby rescuing analgesic effect of morphine treatment of cancer pain by administering to an individual in need of such treatment with a pharmaceutically effective amount of a blocking reagent for ephrinB-EphB signaling. The blocking reagent can be an EphB receptor blocker such as EphB1-Fc and EphB2-Fc.