Heroin morphine

Alkaloids range from the belladonna alkaloids, such as atropine and scopalomine—which are used as poisons, cold remedies, and truth serums —to dextromethorphan, a cough suppressant (anti-tussive). But the most widely known alkaloids are the opiates, such as morphine, heroin, fentanyl, oxycodone, and methadone. These act on... 

Dioctyl sulfo-succinate codeine, morphine, monoacetyl-morphine, heroin stabilization dipping solution, 20 /o in ethanol [94]... 

The use of prodrugs with higher lipophrlicity compared to the parent molecule is realized in the classical example of heroin and morphine. Heroin, the di-acetyl derivative of morphine, penetrates the BBB by one log order better than morphine and is cleaved by tissue esterases to release the active parent drug. As follows from fhe pharmacokinetic principles shown in Section 2.3.2.1 (Eq. 2.3), brain concentration is a function of bofh BBB permeability, reflected by and plasma area under the curve ... 

Schedule 2 includes drugs such as dia-morphine (heroin), morphine, pethidine, quin-albarbitone, glutethimide, amphetamine and cocaine and which are subject to the full controlled drug requirements relating to prescriptions, safe custody (except for quinalbarbitone), the need to keep registers, etc. (unless exempted in Schedule 5). 

The chemical transmitters may be small molecules— notably acetylcholine, norepinephrine, epinephrine, serotonin, dopamine, or histamine. Acetylcholine and norpeinephrine are the dominant neurotransmitters in the parasympathetic and sympathetic nervous systems, respectively. Dopamine and serotonin are employed primarily in the central nervous system. Neurotransmitters may also be more complex peptides (small proteins) such as substance P, vasopressin, endorphins, and enkephalins. The latter agents are of particular importance to our considerations of opium since they represent the endogenous opiates—agents that exist within the body whose actions are mimicked by exogenous, or outside, agents such as morphine, heroin, codeine, and so on. These neurotransmitters serve to convey information between neurons across the synaptic cleft (the junction where two neurons meet) or at the neuroeffector junction (the site between neuron and an innervated organ such as muscle or secretory gland). 

Diamorphine (3,6-diacetyl morphine, heroin) is a semi-synthetic derivative of morphine. It was first synthesised in 1874 and put on the market in 1898 as a non-habit-forming alternative to morphine ... 

Opioids (opium, morphine, heroin, meperidine, methadone, etc) are common drugs of abuse (see Chapters 31 and 32), and overdose is a common result of using the poorly standardized preparations sold on the street. See Chapter 31 for a detailed discussion of opioid overdose and its treatment. 

More than half (57 %) of all seizure cases involved cannabis (herb, resin, oil, plants and seeds). Opiates (opium, morphine, heroin, synthetic opiates and poppy seeds), accounted for 17 per cent, with heroin alone accounting for 14 per cent of the total. This is followed by seizures of the amphetamine-type stimulants (12 %). About half of these seizures (or 5.5 % of the total) is accounted for by methamphetamine, followed by amphetamine (2.5 %) and ecstasy (2%) the rest (2 %) includes Captagon tablets (Near East) and Maxiton Forte (Egypt), ephedrone (methcathinone) and various undefined amphetamines. Coca products account for 9 percent of global seizure cases the bulk of coca related seizure cases concern cocaine (8 % of total). 

Narcotics Demerol Morphine Heroin Others Natural and synthetic opioids analgesics Oral or injected (IM, IV) Relaxation euphoria feelings of tranquility prevent onset of opiate withdrawal Physical dependence respiratory depression high potential for death due to overdose See Chapter 14... 

In addition, the purveyors of thousands of patent medicines—containing drugs such as opium, morphine, heroin, and cocaine—sold them without restriction. The makers of these medicines, who regularly made false claims about their therapeutic value, did not even list ingredients or warnings on the labels. 

Opium traders buy the raw opium from farmers. In Southeast Asia, the price for raw opium in 1999-2000 ranged from 150 to 350 per kilogram. The price is marked up as the opium goes through each stage of processing and refinement. For example, the DEA reports that cooked opium is usually marked up approximately 20%. The price is then marked up again as the opium is refined into morphine base, morphine, heroin base, and heroin. 

In recent years there has been a major research effort, so far without success, to produce potent, centrally acting analgesics that do not have an abuse potential. The discovery of various types of opioid receptor, which may have different effects on central neurotransmitter function, may ultimately lead to the development of such a drug. In the meantime, the most widely used opioids, for example morphine, heroin (also called diacetylmorphine) and codeine are therapeutically effective but are liable to be abused and produce dependence. The structure of some of the morphine-like analgesics and their antagonists are shown in Figure 15.2. 

Drugs in this therapeutic group include morphine, heroin, pethidine, methadone, codeine, dihydrocodeine, dextropropoxyphene, pentazocine, phenazocine, levorphanol and buprenorphine. The principal antagonists in clinical use are naloxone and naltrexone (see Figure 15.3). 

As seen in Figure 3.7, the most widely abused opiate pain relievers are Darvocet , Darvon , and Tylenol with codeine , followed by Vicodin, Lortab , and Lorcet . Methadone is the least addicting of the opiate pain relievers and stays in the body the longest. Because of this, methadone is often used as a substitute for morphine, heroin, and other more addictive opiates to wean people off the drug to which they are addicted. 

It has long been known that only morphine and codeine possess analgesic properties, whereas thebaine acts as a convulsant, similar to strychnine [16]. However, analogues produced from thebaine have provided some of the more interesting and clinically useful dmgs such as buprenorphine (see Section 11.5). Indeed, an early structure-activity relationship was realized between morphine and its methylated phenolic relative, codeine. Codeine (see below) is known to have about one-tenth the analgesic activity of morphine, and was also less likely to produce addiction. Additionally, an early diacetylated analogue of morphine, heroin (6) (Fig. 11.2), demonstrated an increased potency but also an increased addictive potential. 

Many opium-derived and other IQs are psychoactive, the best known being the analgesic, addictive, narcotic, opium-derived morphinan alkaloids codeine and morphine (heroin being the semi-synthetic diacetate of morphine). The tertiary or quaternary amine structural component is important for the activity of some Erytkrina alkaloids and bisbenzyliso-quinolines (notably the major curare component (+)-tubocurarine) as antagonists of the nACh-R involved in neuronal excitation of skeletal muscle. The planar disposition of some polycyclic benzophenanthridines enables intercalation (parallel interleaving) between the base pairs of DNA. A variety of naturally occurring and synthetic IQ compounds are protein kinase inhibitors. 

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