Naloxone Naltrexone

Alfentanil, codein, dihydromorphine, etor-phine, fentanyl, heroin, hydromorphone, levo-methadone, morphine, oxycodone, pethidine, piritramide, remifentanil, sufentanil, tilidine, tramadol Buprenorphine, pentazocine Naloxone, naltrexone... 

Several narcotic antagonists, including naloxone, naltrexone, L-methadone, and cyclazocine, have been incorporated in lactide homopolymers and lactide/glycolide copolymers. Cyclozocine was incorporated in poly(L-lactide) in the form of films (81,82). Lamination of drug-polymer films with a drug-free film created a reservoir device and eliminated the burst observed with the monolithic films originally tested. 

Naltrexone and nalmefene are structurally related to naloxone. Naltrexone is the /V-cyclopropy I methyl analogue of oxymorphone while nalmefene is the /V-allyl analogue. They have similar pharmacological properties to naloxone but with longer durations of action, with elimination half-lives in excess of 8 hours. They also have significant oral availability. They are used mainly in the management of addicts. 

The pure opioid antagonist drugs naloxone,naltrexone, and nalmefene are morphine derivatives with bulkier substituents at the l l17 position. These agents have a relatively high affinity for - opioid binding sites. They have lower... 

Buccal delivery of opioid analgesics and antagonists can improve bioavailability relative to the oral route. Esterification of the 3-pheno-lic hydroxyl group in opioid analgesics such as nalbuphine, naloxone, naltrexone, oxymorphone, butorphanol, and levallorphan improved bioavailability and eliminated the bitter taste. The prodrug of morphine,... 

OH-, and 4-OH-biphenyl, buprenorphine (low), morphine (low), naloxone, naltrexone, ciprofibrate, diflunisal, diphenylamine, furosemide,... 

A number of narcotic antagonists based on the morphinan stmcture have been marketed—for example, Buprenorphine, Naloxone, Naltrexone, and Nalorfine. Nalmefene is being pursued for the treatment of alcohol abuse. Oxycodone, and its precursor Codeine, are marketed, with restrictions, as analgesics. noSee Chapter 9, Table 3. 

Pure competitive opioid antagonists, e.g. naloxone, naltrexone, block all opioid receptors while exerting no activating effect. 

Intoxication Sedation, respiratory depression Naloxone, naltrexone... 

Other efforts have been under way to develop narcotic antagonists that can be u.sed to treat narcotic addiction. The continuous administration of an antagonist will block the euphoric effects of heroin, thereby aiding rehabilitation of an addict. The cyclopropylmethyl derivative of naloxone, naltrexone, has been marketed for this purpose. The oral dose of 100 to ISO mg 3 limes a week suffices to block several usual doses of heroin. Long-acting preparations Kerc once also under study... 

Antidotes opioid antagonists nalmefene naloxone naltrexone... 

Full agonists morphine, meperidine, methadone, fentanyl, and heroin Partial agonists buprenorphine, codeine, propoxyphene Mixed agonist-antagonists nalbuphine, pentazocine Antagonists naloxone, naltrexone Phenothiazines chlorpromazine, fluphenazine, thioridazine Others haloperidol, clozapine, risperidone, olanzapine... 

Effects of morphine, naloxone, naltrexone and. beta.-endorphin on monoamine synthesis in rat brain Ahtee, Liisa Garcia-Sevilla, J. A. Magnusson, T. Carlsson, A. 

---