Opiate narcotics

Narcotics (opiates and opioids) are natural, semisynthetic, and synthetic derivatives of the opium poppy. Drugs such as morphine, codeine, heroin, methadone, Darvon, and Percodan fall into this category. They are all depressants, but they are also potent painkillers, and except for heroin (which is illegal) they are prescribed to relieve pain and to control coughing and diarrhea. But because of their pleasurable effects and addictive properties, they can cause problems when taken for nonmedical reasons. Most nonmedical users take these drugs to experience euphoria, to avoid pain, and to relieve withdrawal symptoms. —... 

Other narcotics, opiates (opium, morphine, codeine, methadone, Demerol, Darvon, etc.) A B C D E... 

Opiates are compounds extracted from the milky latex contained in the unripe seed pods of the opium poppy (Papaver somniferum). Opium, morphine, and codeine are the most important opiate alkaloids found in the opium poppy. Opium was used as folk medicine for hundreds, perhaps thousands of years. In the seventeenth century opium smoking led to major addiction problems. In the first decade of the nineteenth century, morphine was isolated from opium. About 20 years later, codeine, one-fifth as strong as morphine, was isolated from both opium and morphine. In 1898, heroin, an extremely potent and addictive derivative of morphine was isolated. The invention of the hypodermic needle during the mid-nineteenth century allowed opiates to be delivered directly into the blood stream, which increases the effects of these drugs. Synthetically produced drugs with morphine-like properties are called opioids. The terms narcotic, opiate, and opioid are frequently used interchangeably. Some common synthetically produced opioids include meperidine (its trade name is Demerol) and methadone, a drug often used to treat heroin addiction. 

On June 30, 1906, with the support of President Theodore Roosevelt, Congress passed the Pure Food and Drug Act of 1906. Because of this law, product labels now had to accurately list ingredients and ingredient strength. Medicine labels also had to declare the presence of narcotics, opiates, or other addictive dmgs. For the first time in American history, consumers would know what they were getting in the medicines they purchased. 

The Opiates. The International Narcotics Control Board—Vienna, tracks the tick production of narcotic dmgs and annually estimates world requkements for the United Nations. Thek most recent pubHcation (100) points out that more than 95% of the opium for Hcit medical and scientific purposes is produced by India and, in a declining trend, only about 600 t was utilized in 1988. This trend appears to be due to the fact that the United States, the largest user of opium for alkaloid extraction, reduced the amount of opium being imported from about 440 t in 1986 to 249 t in 1987 and 224 t in 1988. The United States used about 48 t of morphine (2, R = H) in 1988, most (about 90%) being converted to codeine (2, R = CH3) and the remainder being used for oral adrninistration to the terminally ill (about 2 t) and for conversion to other materials of minor commercial import which, while clearly alkaloid-derived, are not naturally occurring. 

Another agent of this general type is nalmefene (47) Despite their useful characteristics, opiates display tolerance, addiction, abuse, and some toxic side effects Antagonists combat some of these effects, most notably respiratory depression and addiction Nalmefene reputedly has significant oral activity as a narcotic antagonist The synthesis of nalmefine concludes by Wittig olefination of naltrexone (46) to nalmefene (47) This molecular transformation resulted in a significant increase in oral potency as well (141... 

These dm may produce withdrawal symptoms in those physically dependent on the narcotics. The patient must not have taken any opiate for the last 7 to 10 days. Naloxone may prevent die action of opioid antidiarrheals, antitussives, and analgesics. This drug is used cautiously during lactation. 

National Research Council Clinical evaluation of naltrexone treatment of opiate-dependent individuals report of the National Research Council Committee on Clinical Evaluation of Narcotic Antagonists. Arch Gen Psychiatry 35 335—340, 1978... 

Opiates and other narcotics and analgesic drugs may unpre-dicatably elevate the serum amylase. The elevation may last up to 24 hours. Therefore it is important that blood for amylase determination be drawn before giving the patient analgesic drugs for pain. Elevation of the enzyme in peritoneal fluid is strong... 

O DONAHUE has isolated a naturally occurring peptide from brain that can produce responses similar to PCP when administered to animals. The results are reminiscent of the early studies of the opiopeptides that interact with opiate receptors and produce effects like narcotic drugs when administered to animals. 

Epidural analgesia is frequently used for lower extremity procedures and pain (e.g., knee surgery, labor pain, and some abdominal procedures). Intermittent bolus or continuous infusion of preservative-free opioids (morphine, hydromorphone, or fentanyl) and local anesthetics (bupivacaine) may be used for epidural analgesia. Opiates given by this route may cause pruritus that is relieved by naloxone. Adverse effects including respiratory depression, hypotension, and urinary retention may occur. When epidural routes are used in narcotic-dependent patients, systemic analgesics must also be used to prevent withdrawal since the opioid is not absorbed and remains in the epidural space. Doses of opioids used in epidural analgesia are 10 times less than intravenous doses, and intrathecal doses are 10 times less than epidural doses (i.e., 10 mg of IV morphine is equivalent to 1 mg epidural morphine and 0.1 mg of intrathecally administered morphine).45... 

True narcotic allergies are rare and should not be confused with pruritus associated with opiate use. Cross-sensitivity between morphine-like, meperidine-like, and methadone-like agents is unlikely. Therefore, when an individual is allergic to one drug in a chemical class of opioids, it is reasonable to select... 

Opiates are narcotic analgesics (from the Greek narcotikos meaning benumbing and analgesia meaning painlessness), and they remain... 

Finally, intravenous drug administration and the sharing of needles and syringes is common among opiate addicts this creates a serious risk of cross-infection. Many studies have shown a high incidence of HIV and hepatitis B and C among heroin addicts. This risk is somewhat reduced in medically controlled narcotic prescription... 

Analgesic A drug that relieves pain by raising the pain threshold. In the case of the opiates or narcotic analgesics, it also produced a feeling of well-being and tranquillity. 

Loew, G., and D. S. Berkowitz. 1975. Quantum Chemical Studies of Morphinelike Opiate Narcotic Analgesics I. Effect of N-substituent Variations. J. Med. Chem. 18, 656. 

Dextromethorphan, contained in many nonprescription cough medicines, will produce a heavy psychedelic trip, but the nausea characteristic of the opiates may constitute a problem. Kosterlitz and Villareal (Eds.) AGONIST AND ANTAGONIST ACTIONS OF NARCOTIC ANALGESIC DRUGS (1972) and Braude et al. (Eds.) NARCOTIC ANTAGONISES (1973) are useful. 

The PE spectra of some other alkaloids like methadone and the opiate narcotics morphine, codeine and heroin have been investigated by Klasinc and coworkers95. Also in this study structure-activity relationships based on IPs were sought but not found. Since the interaction of the drug molecule with the receptor is highly specific, it is not unreasonable that the molecular rather than the electronic structure is more important for the physiological activity. 

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