lecture om opoids

1. Morphine

15. Heroin

16. Codeine

19. Hydrogenation of morphine’s C=C produced dihydromorphine Dihydromorphine is slightly stronger than morphine as an analgesic with a nearly identical side-effect profile, and is a somewhat more active euphoriant -- therefore making it theoretically a bit superior in alleviating suffering -- and perhaps in a way subjectively closer to that of morphine than hydromorphone, other morphine derivatives, the codeine-based series, or the synthetics. Like metopon, dihydromorphine may be less addictive overall and have better bioavailability after oral administration than morphine. The onset of action is more rapid than morphine and it also tends to have a longer duration of action, generally 4-7 hours.

20. However, this led to a cmpd with improved activity Hydromorphone is a drug developed in Germany in the 1920s and introduced to the mass market beginning in 1926. It is used to relieve moderate to severe pain and severe, painful dry coughing. Hydromorphone is known by the trade names Hydal , Sophidone , Hydrostat , and most famously, "Dilaudid ｨ " , though an extended-release version called Palladone ｨ SR was available for a short time in the United States before being voluntarily withdrawn from the market after an FDA advisory released in July 2005 warned of a high overdose potential when taken with alcohol; it is still available in the United Kingdom as of March 2007. Another extended-release version called Hydromorph Contin ｨ , manufactured as controlled release capsules, continues to be produced and distributed in Canada by Purdue Pharma Inc. in Pickering, Ontario.

22. Similar synthetic manipulations make hydrocodone more potent than codeine Hydrocodone or dihydrocodeinone (marketed as Vicodin , Anexsia , Dicodid , Hycodan , Hycomine , Lorcet , Lortab (or Loritab ), Norco , Novahistex , Hydroco , Tussionex , Vicoprofen , Xodol ) is a semi-synthetic opioid derived from two of the naturally occurring opiates , codeine and thebaine . Hydrocodone is an orally active narcotic analgesic and antitussive . Sales and production of this drug have increased significantly in recent years, as have diversion and illicit use. Hydrocodone is commonly available in tablet, capsule and syrup form.

23. Oxycodone

29. Oxymorphone

31. Thebaine Thebaine (paramorphine) is an opiate alkaloid . A minor constituent of opium , thebaine is chemically similar to both morphine and codeine , but produces stimulatory, with strychnine-like convulsions, rather than depressant effects. Thebaine is not used therapeutically, but is converted industrially into a variety of compounds including oxycodone , oxymorphone , nalbuphine , naloxone , naltrexone , buprenorphine and etorphine . It is controlled in Schedule II of the Controlled Substances Act as well as under international law. Thebaine is listed as a Class A drug under the Misuse of Drugs Act 1971 in the United Kingdom .

32. Changing substitutents on nitrogen can either improve agonist activity…or create antagonists! Nalorphine , derivative of morphine that acts to reverse the effects of morphine and other narcotics . It counteracts narcotic-induced nervous system and respiratory system depression but is not effective against depression induced by other sedatives such as barbiturates . Nalorphine and other narcotic antagonists are useful in reversing the effects of narcotic overdoses. Because nalorphine causes withdrawal symptoms in addicts, it is administered to apparent ex-addicts to determine if they have returned to drug use. Nalorphine is marketed under the trade name Nalline.

33. Still more potent antagonists can be made by incorporating the same structural changes used to make morphine a more potent analgesic Naloxone is a drug used to counter the effects of opioid overdose , for example heroin or morphine overdose. Naloxone is specifically used to counteract life-threatening depression of the central nervous system and respiratory system. It is marketed under various trademarks including Narcan , Nalone , and Narcanti , and has sometimes been mistakenly called "naltrexate." It is not to be confused with Naltrexone , another opioid receptor antagonist with qualitatively different effects.