Декстромора мид: Құрамы, қолданылуы және шектеулер

Opioid analgesic drug
Drugbox
| Verifiedfields = changed
| Watchedfields = changed
| verifiedrevid = 460780572
| IUPAC name = (3S) 3 methyl 4 morpholin 4 yl 2,2 diphenyl 1 pyrrolidin 1 yl butan 1 one
| image = Dextromoramide2DACS. svg

| tradename = Palfium
| Drugs. com =
| pregnancy AU = C
| legal AU = S8
| legal BR = A1
| legal BR comment =
| legal CA = Schedule I
| legal US = Schedule I
| legal DE = Anlage II
| routes of administration = Oral, Rectal, Intravenous, Insufflation

| bioavailability = >75%
| protein bound = High (Palfium, Palphium, Jetrium, Dimorlin) is a powerful opioid analgesic approximately three times more potent than morphine but shorter acting. It is subject to drug prohibition regimes, both internationally through UN treaties and by the criminal law of individual nations, and is usually prescribed only in the Netherlands.

Dextromoramide was discovered and patented in 1956 by Paul Janssen at Janssen Pharmaceutica, who also discovered fentanyl, another important synthetic opioid, widely used to treat pain and in combination with other drugs as an anaesthetic, as well as haloperidol, piritramide, the loperamide diphenoxylate series and other important drugs. Dextromoramide was much favoured by drug users in Australia in the 1970s and the United Kingdom. It has the main proprietary name of Palfium amongst others, though as of mid 2004 the drug was discontinued in the UK due to limited supplies of precursor chemicals. Although this is true, it is believed there was an approximate one year shortage of Dextromoramide and the real reason that Palfium was not put back into production for the UK market is because of how addictive and potent it is as an oral painkiller. Dependence liability is similar to morphine, but with a less severe withdrawal syndrome. The only European countries that now use the brand Palfium are the Netherlands, Ireland and Luxembourg. It is presumably able to be imported into other Schengen zone countries under Title 76 of said treaty coming into force in 2002. It is a Schedule I Narcotic controlled substance in the United States, with a DEA ACSCN of 9613 and an annual aggregate manufacturing quota of zero as of 2013, and had been out of use in the United States for around a decade when the new Controlled Substances Act 1970 was promulgated. The salts of dextromoramide in use are the hydrochloride (free base conversion ratio 0.915) and tartrate (0.724). Racemoramide and moramide intermediate are also controlled.

The main advantage of this drug is that it has a fast onset of action when taken orally, and has a high bioavailability which means that oral dosing produces almost as much effect as injection. It also has a relatively low tendency to cause constipation which is a common problem with opioid analgesics used for cancer pain relief, and tolerance to the analgesic effects develops relatively slowly compared to most other short acting opioids.

Dextromoramide has a mean elimination half life of 215.3 ± 78.4 minutes and volume of distribution of 0.58 ± 0.20 L/kg. Peak plasma levels are reached within 0.5–4.0 h after dosing, decline of plasma concentrations after the peak follow a biphasic pattern, with half lives of 0.4–1.6 h for the first phase and 6.3–21.8 h for the terminal phase. While in about 40% of patients, half lives range from 1.5 to 4.7 h, in a monophasic manner. Less than 0.06% of the dose is excreted unchanged in urine within 8 h of administration.