Application of imatinib and derivative thereof and analgesic in combined medication or compound preparation in treatment of pain

Abstract

The invention discloses an application of imatinib and a derivative thereof and an analgesic drug in combined medication or compound preparation in treatment of pain, and belongs to the technical field of medicines. The medicine provided by the invention is a composition containing imatinib and a derivative thereof and an analgesic in a dosage ratio of more than or equal to 2:1, and can be used for preparing a medicine for treating pain and a medicine for preventing analgesic tolerance and addiction side effects; and when the composition is used for preparing the medicine, the dosage of the imatinib and the derivative thereof is 100-400mg / day, and the imatinib and the derivative thereof and the analgesic medicine can be simultaneously, separately or sequentially applied. The imatinib and the derivative thereof and the analgesic are combined or compounded according to the dosage ratio of more than or equal to 2:1 for medication, so that the analgesic effect of the analgesic can be effectively exerted, meanwhile, the serious side effects of opioid drugs can be effectively prevented, and the analgesic effect of the opioid drugs is not influenced; and the clinical indications of the addictive analgesic analgesic are further expanded.

Description

technical field [0001] The invention belongs to the technical field of medicine, and specifically relates to the application of imatinib and its derivatives in combination with opioid drugs or prepared as a compound preparation in pain treatment. Background technique [0002] At present, the commonly used analgesics in clinical practice are mainly opioid analgesics represented by morphine, non-steroidal anti-inflammatory analgesics represented by aspirin, and other analgesics. Act on the central or peripheral nervous system, peripheral tissue inflammation, etc. to selectively reduce and eliminate various pains to achieve analgesic effect. [0003] Opioid analgesics exert analgesic effect mainly by stimulating opioid receptors. Opioid receptors are distributed in a high density in the medial thalamus, spinal cord glial area, and ventricle, and are related to the afferent pain stimulus, the integration and perception of pain signals, Including μ, δ, and κ receptors, all of wh...

AI Technical Summary

Problems solved by technology

[0004] Non-steroidal anti-inflammatory analgesics, represented by aspirin, have analgesic effects mainly in the periphery, and the central analgesic effect is weak, mainly for pain caused by tissue damage or inflammation, by inhibiting the cyclooxygenase in the peripheral lesion (COX), which reduces the synthesis of PGS and relieves pain, has only a moderate analgesic effect, and has a good analgesic effect, but it is not effective for severe pain such as acute sharp pain, sharp pain caused by severe trauma, and smooth muscle colic

[0005] Other analgesics mainly act on receptors other than opioid receptors, such as NMDA receptors, NK1 receptors, purine and pyrimidine receptors, cannabinoid receptors and other drugs, and their analgesic effects are not strong, such as rotundine It has a good effect on chronic persistent dull pain, and its analgesic effect is weaker than that of meperidine, but stronger than that of antipyretic, analgesic and anti-inflammation drugs; gaurine can be used as an alternative drug for mild to moderate pain, but none of them can meet the current requirements. Treatment needs for severe pain

[0006] However, severe pain such as cancer pain, burns, knife wounds, etc. is caused by multiple factors, and the mechanism of pain is complicated. Only the use of peripheral analgesics cannot prevent severe pain, and central analgesia must be used.

Opioid analgesics such as morphine have powerful analgesic effects and are effective for all kinds of pain. They are in an irreplaceable position in clinical practice, but their side effects such as addiction and tolerance greatly limit their application.

At present, it is necessary to transform a single compound to solve the problem of having a strong analgesic effect while preventing serious side effects such as addiction and tolerance. Indeed, no good drug or compound has been found, and there is no drug or compound that can eliminate opioids in clinical practice. Better approaches to addiction and tolerance and treatments to reduce or delay the onset of drug addiction and tolerance, which can be difficult to treat in severe pain

On the other hand, although opioids have strong analgesic effects, their severe side effects such as addiction and tolerance also severely limit the scope of indications for the powerful analgesic effects of opioids

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