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The Opiates or Opioids

Module Six Lecture The second category of psychoactive drugs discussed are the Narcotics or Opioids. Again, in many ways they are similar acting as to the CNS Depressants, but there are some major differences in terms of drug effects and withdrawal symptoms. Therefore they are in put into their own category. Sometimes they are also called opioid analgesics as each drug in this category can be used to alleviate pain. Another characteristic these drugs have is paralysis of intestinal muscles, thus many of them are used for diarrhea relief, saving lives of millions of people around the world suffering with dysentery. Some of them are also useful for suppression of the cough reflex, as many of us know who have ever taken cough medicine with codeine in it. All of these drugs characteristically are also soporific or hypnotic, meaning they can induce sleep when taken. Recreational users of these drugs take them for their euphoria inducing properties when injected. This is especially true of narcotics like heroin and oxycontin. After the euphoric feeling is over, the person tends to fall into a dream like state with the sensation of total well being. Even though these drugs do create an intoxication similar to depressant drugs, they don't typically cause staggering walk, slurring of words, and impulsivity that the depressant drugs do. These drugs constrict (narrows) the pupils of the eyes and can be extremely psychologically and physically dependency producing. Most of these drugs, except for heroin, which is a Schedule One drug, are used for medical purposes as indicated above, but they also can produce unwanted side effects or adverse effects. These include constipation, depression of respiration which can be fatal in an overdose, nausea and vomiting, itching, and again, dependency. Your book does a wonderful job of describing the historical implications regarding the use of each one of these drugs, and I would certainly encourage you to study some of these details as outlined by the authors. Suffice it to say, the use of opium and opiate

derived drugs has been around for thousands of years. There is even evidence of prehistoric use of opium. Even thousands of years ago the drug was used for its medicinal properties. Opium use was so widespread around the world two countries went to war over it. In the middle 1800's China and Britain actually fought two wars called the Opium Wars. China rulers were concerned with opium use in their country and the problems it was causing, thus they outlawed its importation from other countries. Britain was a chief supplier of opium to China and saw the economic hardship it would cause not to be able to export it into China. Hence, the two countries went to war. Britain eventually “won” the war and as a result was given the island of Hong Kong from China. China has since been given Hong Kong back from Great Britain. Prominent use in the United States of opium started in the early 1800's. By the late 1800's the government was becoming concerned with how many people were becoming dependent upon opium based patented medicines and morphine. As a result of the availability and accessibility of these drugs, a number of people were becoming dependent upon them. It was estimated that around the turn of the century, that 2% of the adult population was “addicted” to opium or morphine. The typical “addict” being a white, middle-class, middleaged woman. One of the outcomes of the Civil War in this country were numerous combat veterans becoming dependent upon morphine. Morphine was used on the battlefield for pain relief with wounds and was also used for dysentery. Just prior to the Civil War, the hypodermic syringe had been invented making it easy to administer the drug. It was with the Harrison Act that the government began to enforce legislation to curb non-medical opium and morphine use. Narcotic or opiate drugs are categorized based upon how much of the narcotic is natural or man made. The first category of narcotic drugs are the natural occurring narcotics. The drugs in this category would include opium, morphine, and codeine. Opium itself is derived from the opium producing poppy plant. The residue from cutting an unripe poppy plant is collected and dried. Opium is typically smoked but it can also be eaten. Back in the 19th Century, an elixir called Laudanum

was popular. It was a combination of opium and alcohol, and was used to treat pain. But as it is true today, back then many used the drug recreationally. The poets, musicians, and artists hailed the concoction as opening up their creative spirit. Morphine is directly derived from opium and is the main active ingredient in opium. Its name comes from Morpheus, the ancient god of dreams. Since the early 1800's to today, it has been used for its analgesic properties. In fact, it’s probably the most powerful natural analgesic available. Many of us have had morphine, especially with episodes of acute pain due to injury or surgery. In terms of how it addresses pain, it does not actually take the pain away, but its strong sedative characteristic relaxes the person in pain to the point that he or she is not as aware of the pain and can thus cope better. The route of administration with morphine is oral, rectal, or by injection. It is metabolized by the liver quickly so its duration within the body is only 4 to 5 hours. For this reason, if the person is in pain or using the morphine for its sedative characteristic, they will need to readminister the drug frequently, and because the body adapts to its presence quickly, it eventually takes more of the drug to have the desired effect. This of course, leads to dependency upon the drug. Some individuals report hallucinatory experiences under the drug’s influence along with nausea and vomiting. Another interesting side effect is itching. This is probably due to increased amounts of histamines being produced. Codeine is also derived from opium and is the secondary active agent in opium. Codeine is not as powerful as morphine in terms of pain relief, but is commonly prescribed for its analgesic property by both doctors and dentists. Tylenol Number Three is an example of a codeine based analgesic. Codeine is also used for its cough suppressant property in treatment of unproductive coughs. At one time, in a number of states, codeine was known as an “exempt” narcotic, meaning you did not need a doctor’s prescription to obtain it. Since many cough syrups had codeine in them, the individual could purchase the medicine over-the- counter after signing their name to ensure they weren’t coming in too often.

Speaking of cough syrup, one current disturbing trend among young people is the use of dextromethorphan (DXM for short) found in the cough suppressant Robitussin. Ingesting preparations known as robocop and robotripping can produce effects such as tactile, auditory, and visual hallucinations, paranoia, altered time perception and disorientation. There's evidence of a withdrawal syndrome that features craving, insomnia, and dysphoria. Of course there is also the danger of overdose. A second category of narcotics or opiates are the semi-synthetic narcotics. This means some of the original opium is still present, but has been altered or combined with other drugs. The most well known drug in this category would be heroin. This drug was developed around 1900 by the Bayer Company, as a more potent substitute pain reliever for codeine, but less addictive. Of course, today we know that when heroin is regularly injected, it can quickly lead to physical dependence. Morphine is a powerful pain reliever, but heroin is estimated to be three times as powerful as morphine. Heroin accounts for about 90% of all narcotic substance abuse. Since 1970 is has been a Schedule One drug meaning it has high abuse potential with no medical usefulness, thus making it an illegal drug to produce of possess. There are those who take issue with heroin having little or no medical usefulness, as it is a powerful pain reliever that if used appropriately could be of great assistance in those dying of terminal illness in making them more comfortable. Unfortunately, heroin has a horrible public relations image in terms of the stereotypical picture associated with a heroin user. Also, the pendulum of doctors prescribing narcotic pain medication swings from one extreme to another. Early in the 20th Century, the criticism of doctors was they were over prescribing opiate derived drugs leading to the Harrison Act, to today where doctors are probably overly concerned with prescribing such drugs to treat pain for fear of the patient becoming dependent upon them, but in cases of extreme pain with a person dying, or pain so bad that a person has little quality of life, what other alternatives exist? Heroin is typically injected directly into a vein (mainlining), although it can be smoked and snorted. When injected it produces a euphoria in

some people, but not all people, followed by a state of well being, a literal “feeling no pain.” But like morphine, heroin has a short duration or half-life leading to a need to inject more heroin more often to have the desired effect. Sometimes this can lead to injecting the drug anywhere from 3 to 4 times during the day. This then can lead to quick physical dependence upon the drug. Once physically dependent, the person suffers withdrawal symptoms including a strong craving for the drug. Not everyone, however, who uses heroin becomes dependent upon it, in fact, just like there are social drinkers, there are also social heroin users called “chippers.” Those individuals who do use a needle to inject the drug often started out by “skin popping” or injecting the drug into a pinch of skin as opposed to directly into a vein. There are many problems associated with mainlining heroin. One of the biggest concerns is overdose. When a drug is used intravenously the effects will be felt much more quickly than when the drug is orally administered, but the possibility of a fatal overdose also increases. Buying a dime bag of heroin off the street is a gamble. The actual amount of heroin in the purchase or its purity is unknown. Thus one bag may have a few grams of heroin in it, then the next has ten times that amount. Another problem with injecting drugs is contracting infectious disorders from sharing “dirty” needles. Infectious disorders like HIV and hepatitis are quite common with regular needle sharers. Then there’s the problem of running out of available veins to inject the heroin, or veins that won’t leave “tracks” for others to see. Some needle users then get quite desperate and creative as to where they stick their needles. So then the question becomes why? Why do the users use needles to inject the drug when there are safer ways to administer the drug? Part of the answer probably has to do with the ritual of intravenous drug use, where the needle becomes representative of the culture of its use and the process of bonding that takes place between users. This tends to be true with any drug where it is intravenously used, the “addiction” is not only to the drug but to the needle itself. Another semi-synthetic narcotic or opiate is oxycodone (Percodan). Oxycodone is a strong analgesic used in treating moderate to severe

pain. It is typically orally administered in pill form. A commonly prescribed analgesic is Percocet which is Percodan combined with acetaminophen (Tylenol). Another pain reliever that has oxycodone in it is Oxycontin. Oxycontin is quite potent as it is oxycodone in timerelease form. In other words, when it is prescribed for pain relief, it is with the idea that its onset of action is periodic over a set time. Thus this drug has become a popular recreational drug, especially with young people. It too can be intravenously injected like heroin to produce an intense eupohoria. Hydrocodone is another semi-synthetic narcotic used to treat moderate to severe pain. It too is typically orally administered. The popular analgesic Vicodin is hydrocodone combined with acetaminophen. Over the last ten years, our country has seen an increase (some say to epidemic proportions) in use of opiate derived pain relievers. Many have called for less prescribing of these drugs and use of other ways to manage pain. There are those, who when the Oxycontin, or the Vicodin can no longer be obtained, or the drugs are no longer producing the desired effect, have switched over to the use of heroin. The third category of narcotic drugs are the synthetic narcotics. These are narcotics that do not have any opium derived drugs in them, but have been laboratory created to have a similar chemistry and thus similar effect. A synthetic narcotic many of us might be familiar with is the drug Demerol which is a trade name for meperidine. This drug is used to treat moderate to severe pain and is typically injected into the blood stream. One concern with meperidine is it can cause seizures in high doses. Another commonly prescribed analgesic used to treat more minor pain is propoxyphene, known better by the trade name Darvon. It typically is orally administered. When combined with acetaminophen it is called Darvocet. Studies seem to indicate that this drug is a poor analgesic, and not much more effective than acetaminophen alone. The last synthetic narcotic important to discuss is methadone, because of its use in treating other narcotic addictions. Methadone resembles morphine and heroin, thus it is a narcotic agonist, though

its analgesic properties are probably not as powerful. It’s a drug that was developed in Germany and used by the Germans in World War II after supplies of morphine had been cut off by the Allied forces. Its duration in the body is longer than morphine and heroin, thus it's used to curb withdrawal and craving with a person withdrawing from heroin. It is typically orally administered. Narcotic withdrawal, especially heroin withdrawal with heavy heroin users, can be extremely unpleasant. Think of the worst flu you’ve ever had and magnify it a number of times. Withdrawal includes agitation, craving, sweating, anxiety, fever, projectile vomiting, “goose flesh” (going “cold turkey”), stomach cramping, insomnia, and aches and pains. The more severe withdrawal typically depends upon large amounts of heroin being used over a longer period of time. Although the person in withdrawal is very “sick,” withdrawal is seldom life threatening. A recent movie entitled “Trainspotting” is an excellent movie to watch in terms of the life of a heroin user. It tends to be realistic in its depiction of young people in Scotland living their lives around the use of heroin. Graphically it shows them “shooting up” together, the protagonist going through withdrawal, and overdosing prior to his withdrawal. In the movie, after a period of abstinence, he mainlines the heroin leading to an overdose. In the emergency room he is given an injection by a nurse which brings him out of his overdose. The drug that is used to treat overdose victims is the narcotic antagonist Naloxone. Remember that antagonistic drugs work against the effect of the drug. Another narcotic antagonist is naltrexone. One of the trade names for naltrexone is ReVia. ReVia has shown promise in the treatment of narcotic or opiate dependency in helping to prevent withdrawal and in preventing the high if heroin is injected, thus eliminating the primary reinforcement. ReVia has also shown to be effective in the treatment of alcohol dependency in the same manner. Treatment of narcotic dependency has taken a number of forms over the years. Back in the late 1950's a group of recovering heroin addicts in San Francisco banded together to create what is now called a therapeutic community. The name of this therapeutic community was Synanon. Those heroin users who came to the community were counseled, primarily group counseling was the primary modality of

therapy, by other recovering addicts. The type of counseling offered tended to be highly confrontational with the idea of “stripping” away the unhealthy defense mechanisms of the individual in order to help them. The recovering individual stayed in the community for a period of months helping out in the day-to-day functions of running things, eventually to also be vocationally rehabilitated in order to find employment outside of the community and return to the community as a productive citizen. Other therapeutic communities started up across the United States, with one of the more famous being the Phoenix House in New York City. Here in Omaha there is a therapeutic community called NOVA which abides by many of the same principles of the classic therapeutic community. In the 1960's, maintenance programs started, with the use of methadone to treat the heroin dependent individual. The concept of methadone maintenance as a treatment approach is to encourage the person to come in for treatment, knowing that with a prescribed amount of methadone, the withdrawal from the heroin will be avoided, including the relapse trigger of the strong craving for drug. As methadone stays in the body for about 24 hours, the person will hopefully not feel a need to administer heroin. Then over a period of time, the methadone will gradually be reduced to the point of not needing the methadone any longer. For some heroin users, this might have been possible, but for many the need for the methadone lasted for years. Some would say, all that has been done is switching the addiction from the narcotic heroin to the narcotic methadone. However, in many cases the heroin user goes from being unemployed, not able to fulfill other major role obligations in life, perhaps stealing in order to have money to purchase the heroin, and not using or sharing “dirty” needles, to being able to have a healthy and productive lifestyle. Another maintenance drug that is now being used is Levo-Alpha-Acetyl-Methadol or LAAM. The advantage with LAAM is that its duration in the body can be up to 72 hours, thus eliminating the need for the person to come in every day for a dose of methadone. Other maintenance drugs being used in a similar fashion are buprenorphine and ibogaine.

It’s important to note that with these maintenance drugs, the type of dependency being managed is physical dependency, but what about the psychological or behavioral component of dependency. It would be hoped that counseling to help individuals change unhealthy lifestyle patterns would be incorporated along with the treatment of the physical dependency. Methadone maintenance is a type of a harm reduction model of treatment. This model supposes that for some individuals, mandating abstinence from the drug in order to receive treatment for a drug abuse problem is not realistic. That it would be better to help them manage their drug use to avoid undesired outcomes to the individual him or herself and to society. Another example of harm reduction as it applies to heroin use are needle exchange or give away programs so users will not use infected needles to administer the heroin. The harm reduction model is also being studied as a treatment for adolescents, knowing that life long abstinence from alcohol or other drugs is in all likelihood, not going to happen. Of course some might say, the other side of the argument against harm reduction is, when does harm reduction become enabling. Back in the 1950's recovering heroin addicts who wanted to attend a 12-Step support group had no option but to attend Alcoholics Anonymous, even though their drug of choice was not alcohol. Unfortunately back then, and to some extent today, recovering alcoholics looked down upon recovering drug addicts, not taking into account that a recovering alcoholic is a recovering drug addict. This caused a lot of distress for those recovering heroin dependent people looking for what the recovering alcoholics had with AA. It was at that time that this need for a 12-Step program and the discomfort with AA gave birth to Narcotics Anonymous, a 12-Step program based upon the steps and traditions of AA with the substitution of the word drug for alcohol. Today there are numerous NA groups in the United States and the world. Research indicates that the best or most effective treatment approach for narcotic depe...