麻醉性镇痛药（Narcotic analgesics）.docVIP

麻醉性镇痛药（Narcotic analgesics） According to the type of analgesics and their antagonists and receptors, these drugs can be classified into four groups: Pure receptor agonists such as morphine, pethidine, droperidol, and fentanyl; Some agonists, such as buprenorphine, Bhutto, butorphanol, etc.; Mixed agonist - antagonist nalbuphine, such as (nalbuphine); Pure antagonists, such as naloxone and naltrexone. Classification of opioid receptors Mainly exists in neural tissues, such as brain, spinal cord, such as beta endorphin, enkephalin, dynorphin The mechanism of opioid action The relationship between drugs and receptors is like that of keys and locks, but opioid receptor agonists and antagonists differ in their roles in binding to receptors Only agonists can open their matching locks and produce an activating action, such as the combination of morphine with the Mu kappa receptor The antagonist naloxone only occupies the unlocked position and prevents the activation process after unlocking With high affinity receptor antagonists, but no intrinsic activity. Drug resistance and withdrawal phenomenon of opiates It is closely related to the existence of endogenous opioid substances in the body Endogenous opioids are ligands to opioid receptors, widely found in the brain, spinal cord, peripheral ganglia, autonomic nervous system, adrenal medulla, gastrointestinal tract, and plasma Drug resistance Receive continuous exogenous opioid substances in the body reaches a certain degree, the opioid receptor overload, the body through the negative feedback that endogenous opioid release to reduce or stop, it is required to use more opioid analgesic effect in order to maintain the original, this is on the clinical drug resistance. The dosage was increased and the time of drug action was shortened abstinence syndrome Physiological function disorder, a series of long-term continuous medication in a sudden stop of narcotic analgesics such as irritability, insomnia, muscle tremors, vomiting,