Naloxone
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| Non-proprietary name | Naloxone | ||||||||||||
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| Molecular formula | C 19 H 21 NO 4 | ||||||||||||
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whitish solid |
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| Molar mass | 327.37 g · mol -1 | ||||||||||||
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Water: 1.4 g l −1 (25 ° C) |
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| As far as possible and customary, SI units are used. Unless otherwise noted, the data given apply to standard conditions . | |||||||||||||
Naloxone is an opioid - antagonist and, with naltrexone to the pure opioid antagonist , as competitive antagonists at all opioid receptors act. In doing so, they partially or completely cancel out the effects that are caused by opiates and opioids . Naloxone is used as a medicinal substance in human medicine .
Naloxone has a duration of action of about 30 minutes and is therefore shorter than most opiates and opioids. To prevent a rebound effect , it may have to be administered repetitively or intramuscularly for intravenous administration.
The name naloxone is derived from N-Al lyl and Ox ymorph on .
application
Monotherapy
Naloxone is used in emergency medicine as an antidote for opiate overdoses caused by appropriate drugs or medication such as heroin and methadone . Used in connection with respiratory depression or respiratory arrest, naloxone (when given intravenously) works within seconds. In anesthesia it can also be used in the case of a relative opiate overdose to accelerate the waking up phase and relieve respiratory depression, and in regional anesthesia to relieve opiate pruritus .
Combination therapy
Since naloxone triggers a withdrawal syndrome in opiate addicts, it is used in low doses to diagnose such addiction. In addition, it is combined with some centrally acting analgesics ( tilidine , buprenorphine), among other things, to prevent improper use.
- Combination with tilidine
- Naloxone is subject to a high first-pass effect , which means that it cannot develop its antagonistic effect when used orally . In patients with liver damage, naloxone is no longer largely broken down during the first passage through the liver and thus weakens the effect of the tilidine . In the event of improper parenteral use, naloxone is also not broken down and unfolds its effect: Tilidine remains ineffective.
- For this reason, this combination was not subject to the Narcotics Act for some time . Since January 2013, however, the combination in the form of drops has again been subject to BtM in Germany. The prolonged-release tablets are not affected.
- Combination with oxycodone
- The same mechanism also comes into play in the combination of naloxone with oxycodone in a ratio of 1: 2. Due to the low bioavailability after oral administration, there is largely no systemic effect. Naloxone acts locally through competitive binding to the opioid receptors of the intestinal wall and reduces the symptoms of constipation typically triggered by opioids.
- Combination with buprenorphine
- Suboxone is a combination preparation of buprenorphine with naloxone in a ratio of 4: 1. With appropriate, d. H. In this case of sublingual use, naloxone is not absorbed and buprenorphine unfolds its effect as a substitute for opioid addiction, while intravenous or nasal administration ("sniffing") leads to withdrawal symptoms, because not only the opioid (buprenorphine) but also the antidote ( Naloxone) enters the blood.
history
Naloxone was patented in New York in 1961. It has been approved in the United States for the treatment of opiate overdoses since 1971. In the 1990s, opiate abuse increased in the USA and was ultimately perceived as an “opioid crisis” , which is why the use of naloxone preparations was expanded there. The patent has now expired and naloxone is available as a generic from various manufacturers.
Trade names
- Monopreparations : Nexodal (A), Narcanti (D), Narcan or Naloxon OrPha (CH), Nyxoid (D)
- Combination preparations: Andolor (D), Celldolor (D), Suboxone (D, A), Targin (D), Tilidin (D), Valoron N (D)
Ready- made naloxone injections are offered in the USA under the trade name Evzio , and their use should also be possible without medical supervision. In the wake of the drug crisis in the USA, Kaleo Pharma came under fire in 2016/2017 for increasing the price of a two-pack of the preparation from US $ 690 in 2014 to US $ 4,500 in January 2017.
Individual evidence
- ↑ a b c d e f Entry on naloxone. In: Römpp Online . Georg Thieme Verlag, accessed December 10, 2014.
- ↑ a b M. Carmichael, FF Cantwell: Measurement of self-association and ion-pair dissociation constants by solvent extraction using a membrane phase separator . In: Canadian Journal of Chemistry . 60, 1982, pp. 1286-1290, doi : 10.1139 / v82-189 .
- ^ Entry on naloxone in the ChemIDplus database of the United States National Library of Medicine (NLM) .
- ↑ a b Data sheet Naloxone hydrochloride dihydrate from Sigma-Aldrich , accessed on October 20, 2016 ( PDF ).
- ↑ Der Tagesspiegel: Without pain and understanding. Berlin Crimes (December 22, 2007).
- ↑ Targin®: Oxycodone and naloxone as a fixed combination in pain therapy, 2006 ( Memento from August 28, 2011 in the Internet Archive ) In: medknowledge.de
- ↑ The History of Naloxone - Cordant Solutions. In: cordantsolutions.com. Retrieved April 7, 2018 .
- ↑ Shefali Luthra: The $ 4,500 injection to stop heroin overdoses. In: Washington Post , January 27, 2017
