(+)-Naloxone (dextro-naloxone) is a drug which is the "unnatural" enantiomer of the opioid antagonist drug (−)-naloxone. Unlike "normal" naloxone, (+)-naloxone has no significant affinity for opioid receptors, but instead has been discovered to act as a selective antagonist of Toll-like receptor 4. This receptor is involved in immune system responses, and activation of TLR4 induces glial activation and release of inflammatory mediators such as TNF-α and Interleukin-1.
Relation of TLR4 to opioid drugs
Both "normal" and "unnatural" enantiomers of various opioid analgesic drugs including morphine, meperidine, fentanyl, methadone and buprenorphine, as well as some otherwise inactive metabolites like morphine-3-glucuronide, have been found to act as agonists of TLR4, and chronic use of these drugs consequently causes constant low-level release of TNF-α and IL-1β as well as other downstream effects. This is thought to be involved in various adverse properties of opioid analgesic drugs, such as loss of efficacy with extended use and the associated development of tolerance and dependence, as well as the development of side effects such as hyperalgesia and allodynia, which can cause long-term use of opioid analgesics to not only fail to treat neuropathic pain, but ultimately exacerbate it.
Naloxone, sold under the brandname Narcan among others, is a medication used to reverse the effects of opioids, especially in overdose. Naloxone may be combined within the same pill as an opioid to decrease the risk of misuse. When given intravenously, it works within two minutes, and when injected into a muscle, it works within five minutes. The medication may also be used in the nose. The effects of naloxone last about half an hour to an hour. Multiple doses may be required, as the duration of action of most opioids is greater than that of naloxone.
Administration to opioid-dependent individuals may cause symptoms of opioid withdrawal, including restlessness, agitation, nausea, vomiting, a fast heart rate and sweating. To prevent this, small doses every few minutes can be given until the desired effect is reached. In those with previous heart disease, further heart problems have occurred. It appears to be safe in pregnancy, after having been given to a limited number of women. Naloxone is a pure opioid antagonist. It works by reversing the depression of the central nervous system and respiratory system caused by opioids.
That’s why proposals to provide Medication Assisted Treatment, or to buy naloxone — the medication that be used in the event of an overdose — and other harm reduction supplies have been successful.
the overdose antidote naloxone. James “Sleaze” Morgan says naloxone has saved him after overdosing – as many as 20 times in the last several years ...Food and Drug Administration’s move in March 2023 to allow the sale of naloxone without a prescription.
(MENAFN - The Conversation) Opioids are some of the most widely used and misused drugs in the world. Opioids are central nervous system depressants, meaning they slow down brain activity and ... .
A Vancouver pharmacist has been fined $20,000 and suspended for six months for dispensing naloxone without consent of patients ... But the naloxone did not go to those patients.
Preliminary research shows people are using fentanyl, a lab-made opioid over 30 times as potent as heroin, responsible for thousands of deaths in the US ... .
A Vancouver pharmacist has been suspended six months, ordered to pay a $20,000 fine and directed to take remedial courses after admitting to misconduct in a consent order agreement with his professional college ... .
She and others in the non-profit train and hand out naloxone and drug test strips to students and social organizations on and off campus. "We hear testimonies all the time about people who use naloxone ...
Faced with the risk of fentanyl intoxication -- a highly lethal opioid -- in the general population, Urgences-Sant� is in favour of 'everyone' having the antidote commonly known as naloxone in their possession ... .
Telegraph Herald
26 Dec 2024
Telegraph Herald
26 Dec 2024