Oxycodone
Oxycodone is one of the powerful analgesics in the market. The drug has been used for more than a century in the treatment of postoperative pain and pain resulting from chronic conditions such as cancer. The development of oxycodone in the early 1900s was seen as a major hallmark in establishing an opioid with a lower risk of user addiction. In the recent period, however, oxycodone has been classified as a highly potent drug with stronger addiction potency than morphine. In addition, the drug has been largely abused leading to serious health concerns.
History
Oxycodone is a narcotic painkiller developed in 1916. The drug was first manufactured in Germany in 1916. Clinical use of the drug began in 1917 in Germany. The drug is derived by modifying some elements of an organic compound known as thebaine, which naturally occurs in opium (Kalso, 2005). Oxycodone is used in moderating post-operative and acute pain. The drug may be used alone or in combination with others to moderate pain. The development of the drug arose out of the need to create a non-addictive painkiller. Heroin, clinically used at the time as a clinical painkiller, was found to be highly addictive. Heroin had been introduced into the market in the 1890s. However, it was banned for use in the U.S. in the late 1890s. Other common opiates during this period were laudanum and morphine (Frankenburg, 2014). Other countries also saw the need to develop a non-addictive painkiller. This led to the creation of oxycodone by two German scientists as a possible replacement for the addictive heroin.
Oxycodone was introduced to the U.S. market in 1939. In 1950, Percodan, made by combining aspirin and oxycodone, was used as a prescription drug for moderate pain. In 1963, Percodan was recognized as responsible for about one-third of all drug abuse cases in California. Just like other opiates, oxycodone is addictive and thus subject to abuse by drug users. In 1970, oxycodone became recognized as a Schedule II drug. Schedule II drugs are those drugs or substances that are subject to abuse by drug users, have reduced abuse potential compared with Schedule I drugs, and whose continued use can lead to serious psychological issues (Frankenburg, 2014).
In 1995, a time-release version was introduced into the market. This was known as OxyContin, which replaced oxycodone. The time-release version was meant to eliminate the growing issue of oxycodone abuse (Frankenburg, 2014). However, this has not been successful in curbing the issue of abuse. Crashing the drug and snorting it inhibits the time-release mechanism, meaning that the new drug is still susceptible to abuse. Drug users are able to obtain OxyContin as prescription for pain from doctors or pharmaceuticals. This has become a major concern as deaths from the drug overdose have increased significantly (Frankenburg, 2014). It is worth noting that oxycodone, just like other opiates, is likely to be abused.
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The Pharmacology
Oxycodone works by binding onto opioid receptors within the central nervous system. The receptors include kappa, delta, and mu receptors (Smith, Pappagallo, & Stahl, 2012). Specifically, oxycodone reduces the number of calcium ions (Ca2+) among the pain receptors. This leads to declining levels of neurotransmitter within the central nervous system. Oxycodone also causes the outflow of potassium ions (K+) within the postsynaptic level (Smith, Pappagallo, & Stahl, 2012). This results in heavy polarization of pain receptor neurons within the central nervous system. This reduces pain perception among individuals. Oxycodone, just like other opioids also produces an analgesic effect on the peripheral sites. All these actions cause the user to experience significant reduction in pain.
Oxycodone and other opioids also instill an emotional response among users. Oxycodone and other opioids cause a euphoric feeling among users by stimulating the pleasure points found on the brain (Webster & Dove, 2007). In addition, taking oxycodone activates the pathways that control the additive processes in the body. Oxycodone works with mu receptors in the brain to control the rewarding feeling of drugs (Webster & Dove, 2007). By working on the mu receptors, individuals develop oxycodone receptors. Research has shown that knockout mice do not become physically dependent on opioids because they lack mu-opioid receptors.
Oxycodone causes the release dopamine into the nucleus accumbens of the brain, the part of the brain that controls positive behavioral reinforcement (Webster & Dove, 2007). Drugs such as oxycodone cause a significant increase in the level of dopamine in the nucleus accumbens. The increase of dopamine in the nucleus accumbens causes the pleasurable feelings experienced by users. Any subsequent decrease in the level of dopamine in the hippocampus leads to cravings and feelings of anxiety. Oxycodone also acts by activating another region of the brain known as the ventral tegmental area (Webster & Dove, 2007). Other chemicals also contribute to addiction apart from dopamine. These include norepinephrine, glutamate, serotonin, gamma-amino butyric acid, and acetylcholine. Glutamine shapes the reward pathway. Glutamine also helps in reinforcing pleasant or euphoric memories among users, leading to cravings for similar experiences (Webster & Dove, 2007). This contributes to addiction.
Related: Health Care Issue Analysis
Growth, Manufacture, Transportation, and Marketing of Oxycodone
As earlier mentioned, oxycodone is derived from an organic compound known as thebaine. Thebaine occurs in opium. Opium is derived from Papaver somniferum, commonly known as the opium poppy plant. The opium poppy plant gives different types of alkaloids. These are thebaine, morphine, oripavine, and codeine. The opium poppy plant is mainly cultivated in Europe and other parts of the world such as India. In the United States, there are strict regulations concerning how the plant may be grown (UNODC, 2018). In the 1940s, farmers in California had begun growing opium poppy plant, but the government outlawed the growing of the plant due to incidences of abuse. The Poppy Control Act of 1942 required farmers to obtain licenses for growing the plant (UNODC, 2018). In the latter years, growing of opium poppy plant reduced significantly as fewer licenses were issued to farmers. Currently, there is no commercial cultivation of opium poppy plant in the U.S. following a national policy directive.
The manufacture of oxycodone begins with the extraction of two main raw materials from the opium poppy plant. These are poppy straw and opium (INCB, 2014). From these raw materials, it is possible to extract alkanoids including thebaine. Poppies from the opium poppy plant can be used to produce alkaloids and for seed production. During manufacturing, thebaine goes through a process of oxidation, hydrogenation, and lastly purification to form oxycodone. India accounts for about 96.8 percent of total global production of opium poppy plant. About 99.2 percent of the plant grown in India is meant for exports (INCB, 2014). The U.S. exports vast of the opium poppy plant product from India. This is used in the manufacture of oxycodone and other pain relievers. The manufacture and consumption of oxycodone has tremendously increased over the last two decades (INCB, 2014). From the 1990s to 2012, the demand for oxycodone has increased driven by high prescription rates.
Oxycodone manufacturers market the drug to physicians. The current drug in the market, OxyContin, is marketed as an effective painkiller with minimal risk of developing dependency among users. The common marketing techniques has been the sending of direct sales force to doctors countrywide in an effort to convince them of the effectiveness of OxyContin. Purdue Pharma is one of the largest drug makers in the U.S. that produces OxyContin (Associated Press, 2018). In the recent past, however, the production and marketing of OxyContin has come under pressure from lobby groups who claim that OxyContin has been largely responsible for the current drug abuse menace. This has prompted Purdue Pharma to withdraw its direct sales representatives from the market and shift to a new opioid drug, which could replace OxyContin.
Dosage, Expected Effects, side Effects, and Potential for Overdose
Oxycodone is a powerful drug compared to other opioid drugs in the market. According to Lew (2014), oxycodone is 1.5-2.0 times more potent than morphine, and approximately 12 times potent compared to codeine. The dosage depends on the particular patients’ needs. Patients who are using oxycodone for the first time should take 5 mg within a span of 4 to 6 hours. The dosage should be adjusted depending on the pain severity as reported by the patient or as per historical records. The maximum dosage per day is about 400 mg.
There are several expected effects. One of the key effects is pain relief. Oxycodone is a powerful analgesic (Frankenburg, 2014). Another effect is decreased pain awareness among patients. Continued use can lead to higher pain sensitivity (Frankenburg, 2014). Another effect is constipation. Oxycodone affects the nerves that control bowel movement, slowing them down. This leads to higher water reabsorption in the body causing constipation. Another effect is on the endocrine system. Oxycodone reduces stress hormones. It also reduces sex hormones, where users report lower libido (Frankenburg, 2014). Oxycodone relieves anxiety. It can also induce hallucinations and cause users to engage in fantasies. When given in high doses oxycodone can affect breathing.
Oxycodone has a number of side effects even when taken under physician prescription. The side effects include nausea, vomiting, constipation, stomach pain, sweating, weakness, dry mouth, mood changes, loss of appetite, headache, flushing, difficulty breathing, drowsiness, and irregular heart rhythm. Some of the side effects could require intervention by the physician as they might be fatal, for instance, difficulty in breathing.
There is a high potential for oxycodone overdose. Due to the high potency of the drugs, those who abuse the drug are likely to overdose. This is worsened by the fact that oxycodone is highly addictive. Continued use of oxycodone leads to dependency. In relation to this, continued use of oxycodone or any other opioids leads to development of a tolerance level. As such, the users will always user higher dosage in order to achieve some meaningful drug effect on the body. This increases the risk of overdose. According to Frankenburg (2014), deaths from overdose of opioids administered through doctors’ prescription surpassed deaths caused by heroin abuse in 2010. This shows the magnitude of the problem and the potential for overdose.
Possible Treatments in Rehabilitation
Continued use of oxycodone leads to addition. An appropriate treatment plan can enable addicted people to get back to their normal lives free of opioid dependence. Individuals addicted to oxycodone will exhibit similar addiction symptoms to those of other addictive drugs, for instance, failed attempts to quit the drug. Attempts to quit may be thwarted by various withdrawal symptoms such as diarrhea, nausea, anxiety, agitation, vomiting, and body tremors. A user is likely to experience severe withdrawal symptoms if he/she was taking large doses of the drug (Lew, 2014). In addition, quickly withdrawing the drug from an addict may lead to serious withdrawal symptoms.
It is possible to help patients quit dependence of oxycodone by providing lower doses successively. This helps in avoiding serious withdrawal symptoms among users. A common medication used to prevent withdrawal symptoms is buprenorphine (Lew, 2014). This drug inhibits the same receptors as oxycodone but with marginal effects. This ensures that the patient does not experience strong cravings. Another drug that can help in recovery is naloxone. Methadone has similar effects as naloxone. This drug ensures that the patient does not become dependent on buprenorphine (Lew, 2014). Medical treatment should be used in combination with effective therapies such as cognitive-behavioral therapy and group counselling.
In summary, oxycodone is a powerful analgesic that helps in pain relief. The drug is susceptible to abuse and is highly addictive if frequently used. In the recent period, incidences of oxycodone overdose has increased raising concerns among policymakers. The rime-release version of the drug has been ineffective in curbing abuse since users can crash the drug hence causing rapid absorption of the chemical elements in the bod
References
Associated Press. (2018, Feb. 10). OxyContin maker will stop marketing opioids to doctors, company says. The Guardian. Retrieved https://www.theguardian.com/us- news/2018/feb/10/oxycontin-maker-purdue-marketing-opioids-painkillers
Frankenburg, F. R. (2014). Brain-robbers: How alcohol, cocaine, nicotine, and opiates have changed human history. Santa Barbara, California : Praeger.
International Narcotics Control Board (INCB). (2014). Comments on the reported statistics on narcotic drugs. Retrieved from https://www.incb.org/documents/Narcotic-Drugs/Technical- Publications/2014/ND_TR_2014_2_Comments_EN.pdf
Kalso, E. (2005). Oxycodone. Journal of Pain and Symptom Management, 29(5), 47-56. doi:10.1016/j.jpainsymman.2005.01.010
Lew, K. (2014). The Truth About Oxycodone and Other Narcotics (e-Book PDF). New York: Rosen Digital.
Smith, H. S., Pappagallo, M., & Stahl, S. M. (2012). Essential pain pharmacology: The prescriber’s guide. Cambridge: Cambridge University Press.
United Nations Office on Drugs and Crime (UNODC). (2018). The suppression of poppy cultivation in the United States. Retrieved from https://www.unodc.org/unodc/en/data- and-analysis/bulletin/bulletin_1950-01-01_3_page003.html#s001
Webster, L. R., & Dove, B. (2007). Avoiding Opioid Abuse While Managing Pain: A Guide for Practitioners. North Branch: Sunrise River Press.
