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Naloxone is a non-selective and competitive opioid receptor antagonist. [6] [17] It reverses the depression of the central nervous system and respiratory system caused by opioids. [13] Naloxone was patented in 1961 and approved for opioid overdose in the United States in 1971. [18] [19] It is on the World Health Organization's List of Essential ...
An equianalgesic chart can be a useful tool, but the user must take care to correct for all relevant variables such as route of administration, cross tolerance, half-life and the bioavailability of a drug. [5] For example, the narcotic levorphanol is 4–8 times stronger than morphine, but also has a much longer half-life. Simply switching the ...
(+)-Naloxone (dextro-naloxone) is a drug which is the opposite enantiomer of the opioid antagonist drug (−)-naloxone. Unlike (−)-naloxone, (+)-naloxone has no significant affinity for opioid receptors , [ 1 ] but instead has been discovered to act as a selective antagonist of Toll-like receptor 4 .
Buprenorphine/naloxone, sold under the brand name Suboxone among others, is a fixed-dose combination medication that includes buprenorphine and naloxone. [3] It is used to treat opioid use disorder, and reduces the mortality of opioid use disorder by 50% (by reducing the risk of overdose on full-agonist opioids such as heroin or fentanyl).
It has a slow onset of activity, with a long duration of action, and a long half-life of 24 to 60 hours. Once a patient has stabilised on the (buprenorphine) medication and programme, three options remain - continual use (buprenorphine-only medication), switching to a buprenorphine/naloxone combination, or a medically supervised withdrawal. [32]
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Tianeptine/naloxone (developmental code names TNX-601, TNX-601-CR, TNX-601-ER), or naloxone/tianeptine, is an extended-release combination of tianeptine, an atypical μ-opioid receptor agonist, and naloxone, an orally inactive μ-opioid receptor antagonist, which was under development for the treatment of major depressive disorder, post-traumatic stress disorder (PTSD), and neurocognitive ...