32 results about "Opioid analgesics" patented technology

Described are compositions and methods for increasing opioid therapy efficacy and ameliorating opioid use disorder. The compositions and methods target Ptchd1 or neuronal cholesterol.

The present invention relates to pharmaceutical dosage forms, for example to a tamper resistant dosage form including an opioid analgesic, and processes of manufacture, uses, and methods of treatment thereof.

The invention belongs to the technical field of biological medicines, and particularly relates to a microneedle of a drug with a short half-life period as well as a preparation method and application of the microneedle. The bipolar controllable release microneedle is provided for drugs with short half-life periods, long-acting percutaneous minimally invasive drug delivery is achieved, the convenience and comfort of a patient in drug use are greatly improved, controllable plasma concentration maintaining time can be achieved by adjusting the proportion of the first-stage release phase and the second-stage release phase, and the personalized analgesic drug delivery requirement is met. Besides, by taking an opioid analgesic administration strategy as an entry point, the precise controllable two-stage release microneedle of the biphasic matrix carried medicine is innovatively provided, a new dosage form is developed for the opioid analgesic medicine, and compared with an existing intravenous injection administration mode, the analgesic time can be prolonged by 24 times, and the analgesic effect of the medicine is greatly improved.

The present invention relates to novel somatostatin 4 (SST4) selective agonists as non-opioid analgesics. In particular, the present invention relates to peptides having strong SST4-selectivity for use in treatment of pain or inflammation.

The present invention relates to pharmaceutical dosage forms, for example to a tamper resistant dosage form including an opioid analgesic, and processes of manufacture, uses, and methods of treatment thereof.

Provided is a use of an oncolytic virus in the treatment of pain, especially in the treatment of cancer while relieving cancer pain. The drug effect time of the oncolytic virus for relieving cancer pain is obviously longer than that of the existing opioid analgesic, and the dual effects of treating cancer and easing pain are achieved at the same time.

The invention relates to (i) the prevention or treatment of a sleep disturbance, preferably in a patient having neuropathic pain; and / or (ii) the prevention or treatment of neuropathic pain in a patient having a sleep disturbance; and / or (iii) the prevention or treatment of neuropathic pain in a patient having been treated previously and / or being treated concomitantly with an analgesic medication for relief of neuropathic pain, preferably selected from antiepileptics, antidepressants and opioid analgesics, wherein the patient preferably has a sleep disturbance; in either cases by means of one or more high-concentration capsaicin and / or capsaicinoid topical dose units, preferably pharmaceutical patches, comprising capsaicin and / or capsaicinoid at a concentration of at least 2.5 wt.-%, relative to the total weight of dose unit.

The present invention relates to pharmaceutical compositions comprising etoricoxib and tramadol, or a pharmaceutically acceptable salt thereof, for the treatment of pain, which in addition to offering the possibility of an analgesic effect with a decrease in adverse events due to the reduction of the dose of one or both compounds, presents an improved stability, maintaining the dissolution and bioavailability of the composition to be administered; The composition manages to overcome the technological complexity that lies in having a drug with high sensitivity to light and humidity (tramadol), together with another fat-soluble drug with poor flow and excessive adhesiveness (etoricoxib), in a dispensing media in which their absorption is not affected through a water-free process, without affecting the release of both drugs.

The present invention relates to pharmaceutical dosage forms, for example to a tamper resistant dosage form including an opioid analgesic, and processes of manufacture, uses, and methods of treatment thereof.

The invention relates to the technical field of gene detection, in particular to an opioid analgesic drug gene detection method based on multiple targeted amplification, which comprises the following steps: extracting DNA from a peripheral blood sample; the method comprises the following steps: setting a primer pool aiming at a preset site of a specific gene related to opioid drugs, and carrying out multi-targeted amplification sequencing by using the primer pool to obtain sequencing data; comparing the sequencing data with a human reference genome to obtain a data comparison rate, and judging the eligibility of the multi-target amplification sequencing process according to the data comparison rate; performing variation detection on the qualified sequencing data, identifying the base type of each SNP site, and determining the genotype of the subject in combination with a dbSNP database; and inputting the genotype and clinical data into a pre-trained multi-gene prediction model, and obtaining the medication guidance of the subject for using the opioid drugs. The gene detection efficiency is improved.

An abuse deterrent and misuse deterrent transdermal patch comprising aversive agents incorporated in the backing layer of the patch. The aversive agents can exhibit biphasic or sustained kinetics of release with an immediate portion released rapidly and an extended portion released in a prolonged manner when exposed to a dissolution medium. The prolonged aversive agent release provides deterrence against extraction of drug from fresh and used patches and serves to prevent accidental misuse of used patches by children. The abuse deterrent and misuse deterrent patch systems can be used for transdermal delivery of therapeutically active agents and particularly those drugs that are highly prone to abuse such as opiate and opioid analgesics and stimulants.

The present disclosure provides methods and compositions for reducing the addictive liability of opioid analgesics in a subject, for example, by co-administering to the subject the opioid and a serotonin receptor type 2 (5HT2) agonist or a serotonin (5HT) releasing agent. The disclosed methods include methods for preventing opioid abuse, methods for reducing the rewarding effect of an opioid, methods for reducing the addictive liability of an opioid, methods for eliminating or substantially reducing the tendency for a subject to develop physical dependence, tolerance, and / or withdrawal symptoms with respect to an opioid, and methods for eliminating or substantially reducing the tendency for a subject to use opioids in ways not prescribed, take opioids more often or in larger amounts than prescribed, and / or use opioids recreationally. The methods can be performed on a subject, such as a patient (e.g., a human patient).

Provided are a pharmaceutical composition of an analgesic compound and a preparation method therefor. The pharmaceutical composition can be prepared into a liquid injection or a lyophilized powder. The pharmaceutical composition has a controllable particle size and a narrow distribution range, features good stability, and can be used for intravenous injection and achieves a rapid onset of action, thereby effectively replacing the use of opioid analgesics and reducing addiction. In addition, the composition does not contain excipients having a sustained-release function, thereby providing higher safety.

A class of competitive and reversible GlyT2 inhibitors is provided that demonstrate a differentiated pharmacological profile from earlier inhibitors, such as ORG25543. ORG25543 and genetic GlyT2 knockout paradigms can elicit neuromotor or excitatory adverse effects. To overcome these challenges, SAR- and SKR-driven hit-to-lead campaigns were used to design improved, competitive and reversible GlyT2 inhibitors with improved drug-like characteristics and demonstrates a differentiated pharmacological profile. These improved GlyT2 inhibitors include indole, indoline, or indazole cores substituted with a variety of groups to modify the reversible binding activity thereof. The compounds described herein are shown to possess properties useful for safe, efficacious, and orally bioavailable non-opioid analgesics for the treatment of neuropathic pain.

The present invention belongs to the technical field of medicine. Provided are a compound, and a preparation method therefor and the use thereof. The compound has a structure as shown in formula I. The compound of the present invention not only has efficient sedative, hypnotic and / or anesthetic effects, and the ability to control status epilepticus, but also exhibits an analgesic effect, and can reduce or avoid the use of opioid analgesics such as fentanyl, alfentanil, sufentanil or remifentanil in clinical application, thereby reducing the occurrence of adverse reactions such as circulatory depression, respiratory depression, urinary retention and pruritus caused by opioid analgesics.

The invention relates to the technical field of medicines, and particularly discloses application of 9-anthraformic acid in preparation of a non-addictive peripheral analgesic medicine. It is proved for the first time that 9-anthracene formic acid has a remarkable analgesic effect and can effectively relieve inflammatory pain, the action target is a peripheral part, central side effects such as addiction and respiratory depression of traditional opioid analgesic are avoided, gastrointestinal injury, cardiovascular risk and curative effect capping effect of non-steroidal anti-inflammatory drugs are also overcome, and the 9-anthracene formic acid can be applied to preparation of anti-inflammatory drugs. Animal experiments prove that the analgesic effect of the compound is comparable with that of classical opioid drug morphine, and a brand new candidate drug and an application direction are provided for developing novel non-addiction analgesic drugs.

Compositions and methods are presented that include exosomes from stem cells and / or tumor cells that were previously exposed to an inflammatory stimulus. Advantageously, such exosomes exhibit anti-inflammatory and analgesic effect when administered to an individual. Therefore, a preferred use of such exosomes will reduce the need for opioid analgesics, and reduce pain and inflammation.

The invention discloses an all-hydrocarbon cyclized endomorphin 2 as well as a preparation method and application thereof, natural endomorphin EM-2 (YPFF) is selected as a template, and a series of analogues (21 pieces) are designed and synthesized by adopting closed-loop olefin metathesis reaction through a chemical modification strategy. In-vivo and in-vitro analgesic activity and side effect fall experiments show that the total hydrocarbon cyclization binding endomorphin 2 analogue (EM2-5 / EM2-6) is a novel efficient and lasting analgesic with low side effect, and a new lead compound is provided for solving the problems of large side effect and the like of opioid analgesic clinically.

This invention relates to crystal- line salts of naloxone and of naltrexone and their use as opioid antagonists. The crystalline salts of the invention include naloxone saccharinate, nal- trexone succinate and a methanol solvate of nal- trexone succinate. A drug-in-adhesive trans- dermal patch containing the opioid analgesic fentanyl or an analog thereof and a crystalline salts of naloxone or naltrexone is disclosed. Also disclosed is a method of treating pain, such as acute, chronic or intermittent pain, by applying a drug-in-adhesive transdermal patch of the inven- tion to the skin of a patient in need thereof.

The present application discloses a method and system for individualized analgesia evaluation of opioid drugs based on gene polymorphism, which relates to the field of digital medical technology. An evidence-based evaluation is carried out on SNP loci related to opioid analgesia to establish a recommendation strength standard; SNP loci related to the analgesic effect of opioid drugs detected in all databases and samples are screened, and pain influence parameters of SNPs in different levels are respectively set according to the classification levels of the recommendation strength standard; a drug dosage prediction scheme is established according to the pain influence parameters and the number of SNP variations, and the drug dosage prediction scheme is adjusted based on the analgesic attribute characteristics corresponding to the patient to be evaluated determined by the overall score of the patient to be evaluated under different clinical variables. By incorporating the individualized information of the patient and the pain assessment data and adjusting the drug dosage according to the SNP locus variation situation, the clinical medication decision-making of opioid analgesic drugs based on gene polymorphism is realized, and intelligent medication decision support for drug dosage can be provided according to the detection results.

The present invention belongs to the technical field of medicine. Provided are a compound, and a preparation method therefor and the use thereof. The compound has a structure as shown in formula I. The compound of the present invention not only has efficient sedative, hypnotic and / or anesthetic effects, and can control status epilepticus, but also has an analgesic effect, and can reduce or avoid the use of opioid analgesics such as fentanyl, alfentanil, sufentanil or remifentanil in clinical application, thereby reducing the occurrence of adverse reactions such as circulatory inhibition, respiratory inhibition, urinary retention and pruritus caused by opioid analgesics.

The invention discloses an opioid individualized analgesia evaluation method and system based on gene polymorphism, relates to the technical field of digital medical treatment, and comprises the following steps: evaluating opioid analgesia related SNP sites according to evidence to establish a recommendation intensity standard; screening all detected SNP sites related to the analgesic effect of the opioid drugs in the database and the sample, and respectively setting pain influence parameters of SNP in different levels according to classification levels of recommended intensity standards; and establishing an administration dosage prediction scheme according to the pain influence parameters and the SNP variation number, and adjusting the dosage prediction scheme based on analgesia attribute characteristics corresponding to a to-be-evaluated patient determined by overall scores of the to-be-evaluated patient under different clinical variables. According to the method, individual information and pain assessment data of a patient are introduced, the administration dosage is adjusted according to SNP locus variation conditions, clinical medication decision-making of opioid analgesic drugs based on gene polymorphism is realized, and intelligent medication decision-making support of the administration dosage can be provided according to a detection result.

The invention belongs to the technical field of biological medicines, and particularly relates to application of an O-GlcNAc glycosyl hydrolase inhibitor in preparation of a medicine for treating depression caused by opioid withdrawal. Experimental research shows that after being used for a long time, the opioids are abstinged, so that the glycosylation modification of dopaminergic neurons O-GlcNAc in a covered region on the abdominal side of a mouse is reduced, and the phenotypes of pleasant sensation loss and despair-like depression are caused. Intracranial sustained release and intraperitoneal injection of the O-GlcNAc glycosyl hydrolase inhibitor MK-8719 can recover the glycosylation modification level of dopaminergic neurons O-GlcNAc, can significantly improve pleasant sensation loss and despair symptoms caused by withdrawal of opioid analgesic drugs, and has an anti-depression curative effect. Therefore, the O-GlcNAc glycosyl hydrolase inhibitor MK-8719 can effectively reduce pleasant sensation loss and despair-like behaviors, the inhibition effect is clear in target and remarkable in effect, and the O-GlcNAc glycosyl hydrolase inhibitor MK-8719 can be applied to preparation of drugs for treating depression caused by withdrawal of opioid analgesic drugs.

The invention provides an opioid and ghrelin receptor multi-target peptide molecule as well as a preparation method and application thereof, and relates to the technical field of biochemistry. According to the present invention, G (1-5)-EM2 is adopted as a basic peptide, L-amino acids at the 5th site, the 7th site and the 9th site of G (1-5)-EM2 and isomer D-amino acids of G (1-5)-EM2 are modified to obtain the multi-target peptide molecule, and the multi-target peptide molecule has the multi-target agonistic activity of an opioid receptor and a ghrelin receptor, can pass through the blood brain barrier, can be used for relieving various pain symptoms such as acute pain or pathological pain, and can be used for preparing the multi-target peptide molecule, meanwhile, side effects caused by traditional opioid analgesic drugs can be reduced.

Dosage forms containing nefopam, nefopam metabolite, nefopam prodrug, isomers thereof or combinations of the foregoing, optionally an acid, and optionally an opioid analgesic and / or NSAID, and associated methods for treating various types of pain in patients.

There is provided an intraoral composition comprising an alkaline active pharmaceutical agent, or a salt thereof, and a chemically bonded ceramic system formed from a substance selected from the group consisting of calcium aluminates, calcium silicates, calcium phosphates and mixtures thereof. The intraoral composition may be held in the mouth where it releases the alkaline active pharmaceutical agent and contributes to providing an environment that facilitates uptake into the blood stream. Active pharmaceutical agents of particular interest include nicotine and opioid analgesics.

To provide a pharmaceutical composition for treatment of pain.SOLUTION: The present invention relates to pharmaceutical compositions comprising etoricoxib and tramadol, or a pharmaceutically acceptable salt thereof, for the treatment of pain. In addition to offering the possibility of an analgesic effect with a decrease in adverse events due to the reduction of the dose of one or both compounds, this presents an improved stability and maintains the dissolution and bioavailability of the composition to be administered. The composition succeeds to overcome the technological complexity when making a drug (tramadol) with high sensitivity to light and humidity and another fat-soluble drug (etoricoxib) with poor flowability and excessive adhesiveness exist in a dispersed medium in which their absorption is not affected through a water-free process, without affecting the release of both drugs.SELECTED DRAWING: None

An abuse deterrent and misuse deterrent transdermal patch comprising aversive agents incorporated in the backing layer of the patch. The aversive agents can exhibit biphasic or sustained kinetics of release with an immediate portion released rapidly and an extended portion released in a prolonged manner when exposed to a dissolution medium. The prolonged aversive agent release provides deterrence against extraction of drug from fresh and used patches and serves to prevent accidental misuse of used patches by children. The abuse deterrent and misuse deterrent patch systems can be used for transdermal delivery of therapeutically active agents and particularly those drugs that are highly prone to abuse such as opiate and opioid analgesics and stimulants.

The present invention relates to the field of pharmaceutical technology, and particularly to the application of jujuboside in the preparation of analgesic drugs / drugs for reducing addiction; the solution includes: using jujuboside as an adjuvant drug and compounding it with opioid analgesics to form a compound analgesic drug, or using jujuboside as an active ingredient for separate preparation to reduce the addiction caused by opioid analgesics. Experiments have shown that jujuboside can effectively enhance the analgesic effect of opioid analgesics, prolong the analgesic duration, inhibit the formation of opioid analgesic addiction memory, and jujuboside itself has no addiction. Therefore, the present invention can provide better analgesic efficacy while reducing the dosage of opioid analgesics, prolonging the drug administration interval, eliminating / reducing the addiction of opioid analgesics, improving the drug safety of opioid analgesics, and reducing various side effects caused by the overdose of opioid analgesics.

The present invention relates to pharmaceutical dosage forms, for example to a tamper resistant dosage form including an opioid analgesic, and processes of manufacture, uses, and methods of treatment thereof.