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Opiates derived from

P-Endorphin. A peptide corresponding to the 31 C-terminal amino acids of P-LPH was first discovered in camel pituitary tissue (10). This substance is P-endorphin, which exerts a potent analgesic effect by binding to cell surface receptors in the central nervous system. The sequence of P-endorphin is well conserved across species for the first 25 N-terminal amino acids. Opiates derived from plant sources, eg, heroin, morphine, opium, etc, exert their actions by interacting with the P-endorphin receptor. On a molar basis, this peptide has approximately five times the potency of morphine. Both P-endorphin and ACTH ate cosecreted from the pituitary gland. Whereas the physiologic importance of P-endorphin release into the systemic circulation is not certain, this molecule clearly has been shown to be an important neurotransmitter within the central nervous system. Endorphin has been invaluable as a research tool, but has not been clinically useful due to the avadabihty of plant-derived opiates. [Pg.175]

Morphine, an opiate derived from the opium poppy (genus Papaver), has the molecular formula CyHipNOj. It is a weakly basic amine, with a AJ, of 1.6 X 10. What is the pH of a 0.0045 M solution of morphine ... [Pg.527]

In the strict sense, opiates are drugs which are derived from opium and include the natural products morphine, codeine, thebaine and many semi-synthetic congeners derived from them. In the wider sense, opiates are morphine-like drugs with non-peptidic structures. The old term opiates is now more and more replaced by the term opioids which applies to any substance, whether endogenous or synthetic, pqrtidic or non-peptidic, that produces morphine-like effects through an action on opioid receptors. [Pg.903]

When Montgomery and I published our article, we thought we had disproven another theory of placebo effects - the theory that placebo effects are produced by the release of endorphins in the brain. In 1978 researchers at the University of California in San Francisco discovered that when placebos reduce pain, they may stimulate the release of endorphins.18 Endorphins, the existence of which had only been discovered a few years earlier, are opioids that are produced naturally by the brain. Just like the opiates that are derived from opium - morphine and codeine, for example - endorphins reduce the sensation of pain. The University of California researchers reasoned that if placebos can mimic the effects of opiate drugs, maybe they do so by stimulating the release of the brain s endogenous opioids. [Pg.138]

Opiate A drug related to morphine, derived from opium. [Pg.247]

The pleasure derived from using tobacco is linked to the stimulation of dopamine-dependent neurotransmitter pathways in the brain, particularly in the meso-limbic system. The precise nature of this link remains controversial, but many of the neurophysiological processes underlying nicotine addiction are common to other addictive drugs with diverse pharmacological actions such as opiates, cannabis, alcohol and cocaine. [Pg.443]

Opiates are drugs derived from opium, including morphine and heroin 914... [Pg.911]

The chemical structures and biological activities of hundreds of opioid analgesics derived from the prototype opioid drug morphine are most comprehensively described in two books published in 1986, one entitled Opioid Analgesics, Chemistry and Receptors by Casy and Parfitt [1] and the other entitled Opiates by Lenz et al. [2]. Follow-up articles include those by Casy in 1989, entitled Opioid Receptors and their Ligands Recent Developments [3] which also includes sections on opioid peptides, affinity labelling and opioid receptor subtypes Rees and Hunter in 1990 [4] covering the... [Pg.110]

Pharmacology Buprenorphine is a semisynthetic centrally acting opioid analgesic derived from thebaine a 0.3 mg dose is approximately equivalent to 10 mg morphine in analgesic effects. Buprenorphine exerts its analgesic effect via high affinity binding of CNS opiate receptors. [Pg.898]

The enkephalins, derived from pro-enkephalin, are distributed much more widely in the CNS both in local circuit neurons and projection neurons, a distribution generally paralleling to that of the opiate receptors. Leu-enkephalin predominates over Met-enkephalin and both peptides are inhibitory. Enkephalin containing neurons are sparsely distributed in upper lay-... [Pg.19]

For centuries opium was used for both medicinal and recreational purposes. Derived from the poppy Papaver somniferum, it contains numerous opiates, the primary one of which is morphine. The term opiate has largely been replaced by opioid, which represents all compounds with morphinelike activity and includes morphine, morphine derivatives, and peptides. Opiate is used to refer to morphinelike drugs derived from the plant and structurally similar analogues. These drugs are frequently referred to as narcotics, a Greek term for stupor, which is scientifically obsolete. Even in its early history, opium presented a problem when it was smoked or taken orally. The introduction of the hypodermic needle and syringe, however, drastically enhanced the euphoric properties of opioids and thereby altered their abuse liability. In addition, the synthesis of heroin resulted in an opioid that was more potent than morphine and ideally suited for intravenous administration. [Pg.409]

Opiate refers to any drug derived from opium. Opiates inciude codeine, morphine, and papaverine. [Pg.13]

Historically, plant-based natural products have been a source of useful drugs. The analgesic opiates come from the poppy plant. Digitalis for congestive heart failure was first isolated from the foxglove plant. Various antibiotics (penicillin) and anticancer agents (taxol) are derived from natural product sources. There are numerous other examples. [Pg.115]

It is centrally acting synthetic analgesic compound that is not derived from natural sources nor is chemically related to opiates. It acts via opioid receptors in CNS to produce analgesia and has no abuse potential. It also inhibits the reuptake of noradrenaline and serotonin. [Pg.79]

Opiates abuse is basically stable or declining in West and Central Europe. The annual prevalence rate remained close to 0.5 per cent of the population aged 15-64 (1.5 million people). Major opiates markets in Western Europe are the United Kingdom (some 350,000 persons) and Italy (300,000), followed by France (170,000), Germany (120,000) and Spain (70,000). Data for Spain suggest that opiates abuse has declined in recent years. These data are derived from problem drug use estimates. Household survey results in all of the countries mentioned above show substantially lower figures (with prevalence rates typically around 0.2%). Household surveys, however, may not provide the optimal measure of the number of opiates abusers as many heroin addicts do not have a fixed or permanent residence. [Pg.55]

This was derived from an estimate of the total number of drug users in the Russian Federation of 2.3 million (UNODCCP, Country Profile on Drugs and Crime in the Russian Federation, 2002) and estimates of the proportion of registered opiate users among all registered drug users. [Pg.55]

Morphine and codeine as well as their natural and synthetic derivatives ultimately derived from opium ( opiates )... [Pg.151]

Opiates act on a variety of receptors. The three most important subtypes are the mu, delta, and kappa opiate receptors (Fig. 13—25). The brain makes its own endogenous opiate-like substances, sometimes referred to as the brain s own morphine. They are peptides derived from precursor proteins called pro-opiomelanocortin (POMC), proenkephalin, and prodynorphin. Parts of these precursor proteins are cleaved off to form endorphins or enkephalins, stored in opiate neurons, and presumably released during neurotransmission to mediate endogenous opiate-like actions (Fig. 13-25). However, the precise number and function of endogenous opiates and their receptors and their role in pain relief and other central nervous system (CNS) actions remain largely unknown. [Pg.521]

OPIATES AND OPIATE-LIKE NEUROTRANSMITTERS The euphoric and sleep-producing effects of opiates, which are derived from the poppy plant, were well-known to ancient civilizations. Around 4000 BCE, for example, the Sumerians... [Pg.133]

How does aspirin differ from morphine Aspirin has three main beneficial effects in your body. It blocks pain in the mild-to-moderate range, and it reduces both inflammation and fever. Its effects on pain derive from its actions not on neuropeptides, such as the endogenous opiates in the brain, but on a local hormone called prostaglandin that is released at the site of bodily pain. When a cell in your body is damaged or injured, prota-glandins are rapidly synthesized and released from the injured cells. Prostaglandins help mediate pain in the injured areas. They sensitize your pain-sensing neurons to mechanical stimulation,... [Pg.139]

All drugs derived from opium poppy are called opiates. Of the opiates, heroin (diacetylmorphine) is the most potent and fast-acting. Though heroin is no longer used in medical settings, its less potent cousins— codeine, liquid morphine, pethidine, and methadone— are found in clinics and hospitals all over the world. But it wasn t until the early 1970s that scientists began to understand the real reasons behind heroin s propensity for abuse and addiction. [Pg.236]

Hydromorphone and its natural opioid relatives have been used to relieve pain, treat a variety of ailments, and create euphoric feelings at least as far back as the time of the ancient Greeks. In early Greek history, the priests controlled the use of opium and ascribed to it supernatural powers. In the fifth century bc, Hippocrates, the father of medicine, dismissed the supernatural attributes of opium. Hippocrates believed opium had cathartic, narcotic, hypnotic, and styptic properties. He believed that all diseases had a natural origin and could be cured by natural therapies. All of the natural opiates historically were derived from opium poppy plants. The liquid extracted from the poppy seeds was typically dried to create a concentrated powder. These extracts were then smoked, eaten, or drank. [Pg.245]

The opiates and their semi-synthetic and synthetic relatives have long been among the most important drugs in the world because of their ability to alleviate the most severe forms of pain. Often, this pain is derived from invasive surgical procedures or from advanced cancer pain that is virtually unbeatable without this family of drugs. A clear majority of persons who use opiates and their relatives never develop an addiction problem. However, addiction can develop quickly in those with a propensity for these drugs. This can occur in those who are using them for medical reasons as well as in those who use them recreationally. [Pg.252]


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Opiate

Papaver somniferum opiates derived from

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