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Opioids, their analogues and antagonists
The groupThis group includes narcotic analgesics (from the Greek. Algos, pain and an-free) The expressed ability to reduce or eliminate a sense of pain.
Analgezirutuyu activism on the part substances with different chemical structure, and it is different mechanisms. Modern analgesics divided into two major groups : drug and nenarcoticeskie. Narcotic analgesics, with generally strong pain relieving effects are side effects, the most important of which is the development of addiction (drugs). Nenarcoticeskie analgesics are less severely than drugs, but not a drug addiction, drug addiction (see Nenarcoticeskie analgesics, including steroidal and �ротивовоспалительны�� means).
For opioids was very active analgezirutaya allowing their use as a highly effective painkillers in various fields of medicine, especially when injuries (operational intervention, injured, etc.) and a host of diseases involving expressed sore syndrome (malignant neoplasms, myocardial infarction, etc.). In particular impact on the central nervous system, opioids are euphoria, emotional change in the colour of pain and the reaction to it. The most significant of their disadvantage is the risk of psychological and physical dependence.
This group analgesics are natural alkaloids (morphine) and synthetic compounds (promedol, fentanyl, pentazuoqin, nalbufin etc.). Most synthetic drugs obtained in a modified molecules morphine to the preservation of its structure or its simplification. Through chemical modification of morphine molecules derived substances that were antagonists (naloxone, naltrexone).
On analgeticski symptoms and the side effects of different drugs vary among themselves, that due to their chemical structure and physico-chemical properties and the interactions with the receptor, involved in the exercise of their pharmacological effects.
It is the understanding of the neurochemical effect of opioids greater role has been played by the opening in the 1970s specific opioid receptors and endogenous peptide ligands, and enkefalinov endorfinov. Waismann receptors are concentrated mainly in the central nervous system, but also to be found in the peripheral organs and tissues. The Waismann brain receptors are mainly in the structures that are relevant to the transfer and coding pain signals. Depending on the sensitivity of different ligands of opioid receptors available route : 1-(mu), 2 - (kappa), and 3 (delta), 4 - (sigma), 5 - (epsilon) with a different functional significance.
The mechanism of action of opioids is the psychological impact on talamicakie points pain sensitivity conducting pain signals to the cortex.
The medical practice is the use of a variety of opioids. In addition to morfinu built prolongirovanne dosage forms. Received as a significant number of synthetic analgesics level of the group (promedol, fentanyl, buprenorphine, butorfanol, etc.) highly analgeticescoy activity with varying degrees of "abuse potential" (ability to create addicts).
If poisoning or overdose of narcotic analgesics used antagonists, which block all types of opioid receptors (naloxone and naltrexone).