Oxycodone Research Paper

An Opioid such as morphine act by attaching to specific proteins called opioid receptors, which are found in the mainly in the brain, spinal

The binding could only occur in the receptors active site if the size, shape and charge of the morphine’s meet the requirement of the receptor. Once the match is identified, the following binding process would take place. The flat benzene ring in morphine would fit securely in the flat surface of the receptor’s active site to allow the rest of the molecule to fall in place easily. The adjacent carbon atoms would fit into a nearby groove, while the nitrogen atom would attach to the negatively charged group receptor, hence joining the two together. After the binding occurred, the morphine would be able to block the sending of the painful information from the pre-synaptic neuron on the nociceptor. This is because, it caused a reactionary changed in the cell which blocks its ability to produces the substance that causes the feeling of pain during and/or after an operation and injury.

For thousands of years, opiates have been used in the treatment of pain. Opium is believed to have been discovered 6000 BC, and since then, it has had a huge impact on both medicine and the recreations of those seeking euphoria. More recent than the ancient discovery of natural opium are the derivatives of opium, such as the alkaloids morphine, codeine, and thebaine. From these alkaloids, semi-synthetic opiates can by synthesized, such as hydrocodone, and oxycodone. Synthetic opioids are also quite prevalent, which include fentanyl and tramadol. Opium can also be processed into heroin, a morphine derivative. As advancements were made in science and engineering to allow for a wider distribution and usage of opiates, the problems of dependence and overdose also increased drastically. According to Hart and Ksir (2013, p. 302), the invention of the hypodermic needle for intravenous administration of morphine and other drugs allowed for a much faster and more potent dose of the drug. With this increased potency came an increase in the possibility of a recreational intravenous user to overdose. Hart also mentions that some of the wars surrounding the era of the synthesis of morphine may have contributed to the rise of morphine, seeing as a medic soldier’s motto was always “first provide relief” (2013). This relief-driven attitude and extensive use of opioid analgesics in medicine during the time, in addition to the large amount of patent medicines and remedies on the market may

Next, there is an extensive history of opioid use for pain management, and other symptom management as well. Morphine can be traced back to Civil War veterans trying to manage pain and, consequently, being addicted. “‘Drugs were already on the scene and being consumed at alarming rates long before the start of the war,’ said Mark A Quinoes, a scholar who studied drug abuse during the Civil War.” It was not until 1898 that heroin was on the market for commercial sale, considered a “wonder drug,” it began to spread in use along with users that found out injecting it would increase its effects. There was little known about these new opioids, they were even used as cough suppressants. Heroin worked for what is was being used as, a pain suppressant, and there were few other options. In 1914 the Harrison Narcotics Tax Act imposed a tax on importing and selling opium or coca leaves. In 1924 doctors were avoiding using opioids after being aware of their addictive nature which lead heroin becoming illegal. Without this opioid, doctors had to get creative when treating World War II soldiers, this sparked research into nerve blockers. These nerve blockers managed pain without the use of surgery. This was, unfortunately, not the end of the opioid. While these results were shocking the pharmaceutical industry still faces much leniency from the federal

Oxycontin is classified as an opioid or narcotic pain relieving medication, called opioid analgesics. The Oxycontin molecules work by changing the pain response generated by the central nervous system. It works by interacting with specific proteins called receptors as shown in Figure 1. These receptors are found on cell surface, in the brain, gastrointestinal tract, spinal cord and other organs in the body (Columbus, 2008).

The pharmacokinetics of opioids begins with the type of route of administration. The faster the opioid reaches the blood stream the quicker the effects of the opioid will reach the brain. Only about 50% of orally administered morphine passes through the blood brain barrier. Heroine is more lipid soluble than morphine therefore has an easier time of crossing the blood brain barrier. It is the fact that heroine has two acetyl groups attached to it that helps it be more lipid-soluble. This makes heroine 2 to 3 times more potent than morphine. Opioids bind to opioid receptors in the brain. There are 3 types of opioid receptors. There are Mu, Delta, and Kappa receptors. The Mu receptors are highly concentrated in the nucleus accumbens, the reward center of the brain, which explains why opioids are highly addictive. Opioids are eventually metabolized by the liver and

When it comes to measuring the potency of opiates, morphine remains the measuring stick: all other opiates are described as more potent than morphine or less. There 's a simple reason for that: morphine is the actual active ingredient in the opium plant. It is, in effect, the substance that causes an opiate to be an opiate. And pure morphine remains potent.

Opioid receptors are members of the G-protein-coupled receptors (GPCRs) family, which consists of 7 transmembrane domains linked together by 3 extracellular and 3 intracellular loops (Trescot et al., 2008). The three different classes of opioid receptors are: -opioid receptor, -opioid receptor and -opioid receptor, which are distributed throughout the central and peripheral nervous systems (Trescot et al., 2008). -opioid receptors are associated with analgesia, euphoria and physical dependence and are predominately located in the brainstem and thalamus (Trescot et al., 2008). -opioid receptors, on the other hand, are primarily found in limbic brain topography, brain stem and spinal cord, and are related to dysphoria and analgesia (Trescot et al., 2008). Although -opioid receptor mechanisms are poorly understood, it has been indicated to also have psychomimetic effects (Trescot et al., 2008).

Once an individual receives extreme amounts on morphine, the body will not be able to manage the activation or deactivation of the -opioid receptor. This leads to adverse effects on the individual which includes asphyxia, hallucinations, confusion, delirium, suppressive breathing, and eventually death[18]. Further, it was determine that the on average the minimum lethal dose for morphine is 200 mg which can lead to life threatening respiratory

In their article, “The Effects of Pharmacological Opioid Blockade on Neural Measures of Drug Cue-Reactivity in Humans,” Courtney et al. investigates the role of opioid blockade on neural systems underlying drug craving. They tested whether blockade of opioid receptors can actually reduce the salience of the methamphetamine cues.

An increase in endogenous opioids can act upon the ON/OFF cells in the RVM, which can in effect turn “off” the pain signal, or dampen it dramatically, hence the use of opioids as pain killers. Proving the presence of opioids within the placebo mechanism was determined by using an opioid antagonist naloxone3, which was able to reduce the placebo effect if there were strong expectation cues, but not as effectively when the expectation

Opioids are important for pleasurable experience . If we observe a hedonic spectrum, we sould see, that opioids shift it in positive direction : while sweat tastes seem sweater , bitter tastes and pain seem less aversive. Blocking of opioid-mediated signalling results in decreased pleasantness of rewards. Recent studies have shown, that there is a dissotiation between the way how µ-opioid and κ-opioid – receptor related signalls modulate the perception of pain.( µ and κ come from the name of the first discoverd ligand that attach to this receptors: µ stands for morphine and κ for ketocyclazocine ). The activation of µ-opioid receptors induces

Through the use of social construction of expertise, OxyContin became a medicine for daily use similar to taking an aspirin. The fame of OxyContin did not arise overnight and it was not natural. Accredited pain specialists spoke describing that there was few long term side effects and that OxyContin was a gift from nature, and that it was a medical myth about concerns of addiction. Seeing qualified doctors in lab coats promote a drug, people began to believe that this drug was not only a viable option but also safe. Additionally, the Sackler family created many advertisements designed to create more widespread use of OxyContin by introducing it as a great acute pain drug. The result of targeted advertising combined with backing by doctors created

OxyContin is the brand name for a formula of oxycodone, first developed in 1995. It is an opioid pain medication, which is also known as a narcotic. OxyContin can prescribed to dull severe pain that is expected to last for an extended period of time. It is typically given to patients with arthritis, cancer, or for post-operative pain. OxyContin is not to be used as an as needed drug; it is used for around the clock treatment. OxyContin contains between 10 and 80 milligrams of oxycodone. Because it is a time release formula, OxyContin allows up to 12 hours of relief. Originally it was just a blessing for patients who needed round the clock relief. Soon it began being abused. What was once just helpful to one became detrimental to another.

The dose of Naloxone is influenced by the dose of opioids taken; thus, the higher the dose of opioids is, the higher dose of naloxone required to reverse the narcotic effects. Nevertheless, higher doses of naloxone produce more severe withdrawal symptoms in dependent patients.