11 results about "Opioid analgesics" patented technology

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 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.

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.

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.

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 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.

In certain embodiments, the present invention is directed to a solid controlled release dosage form comprising: a core comprising a first portion of an opioid analgesic dispersed in a first matrix material; and a shell encasing the core and comprising a second portion of the opioid analgesic dispersed in a second matrix material; wherein the amount of opioid analgesic released from the dosage form is proportional within 20% to elapsed time from 8 to 24 hours, as measured by an in-vitro dissolution in a USP Apparatus 1 (basket) at 100 rpm in 900 ml simulated gastric fluid without enzymes (SGF) at 37 C.