Oxycodone: Effects, Uses & Risks

Oxycodone is an opioid that is classified as a strong pain reliever. It is used for the treatment of intense pain.

What is oxycodone?

Oxycodone is an opioid that is classified as a strong pain reliever. Oxycodone is the name given to a strong-acting analgesic that belongs to the group of opioids. Opioids are generally considered the strongest and most effective analgesics. Oxycodone is produced semisynthetically. Its effect is even stronger than that of morphine. Oxycodone was developed in 1916 at the University of Frankfurt/Main by the German chemists Edmund Speyer (1878-1942) and Martin Freund (1863-1920), who synthesized the drug from thebaine. Just one year later, the drug was launched on the market by the Merck company and given the preparation name Eukodal. The drug was used to treat pain and cough. From 1919, it could also be used as a pure analgesic. Eukodal was available in Germany until 1990, when it disappeared from the market because of its high potential for abuse and addiction. The first cases of oxycodone abuse had already occurred in the early 1920s and were given the name eucodalism. Today, oxycodone is marketed in Germany and the USA under the names Oxygesic or Oxycontin. In the Federal Republic of Germany, the active ingredient falls under the Narcotics Act. In the USA, oxycodone was still one of the top-selling drugs until 2010. Since then, however, sales of the drug have declined. Since 2006, oxycodone has also been offered as a combination preparation with naloxone, an opioid antagonist, under the name Targin. The interaction of the two substances is intended to counteract constipation, which often occurs with opioid use. It also limits abusive administration.

Pharmacologic action

Oxycodone exerts its effects at different opioid receptors within the brain. In this process, the drug works as an agonist and does not exhibit any antagonistic property. The analgesic effect of oxycodone is two times greater than that of morphine. The effect is achieved by occupying the opioid binding sites, which leads to suppression of pain perception. Since the opioid exerts an additional effect at the K receptor, it is considered to be better tolerated than other strong painkillers. However, there is no confirmation of this effect from independent studies. Another positive effect of oxycodone is the attenuation of cough. For this reason, the drug was used in earlier years to treat cough disorders. When oxycodone is taken as a tablet, 60 to 85 percent of the drug enters the body’s bloodstream. It takes about an hour for the analgesic effect to set in. The effect of the drug lasts for about four hours. However, some preparations have a longer duration of effect (8 to 12 hours). Oxycodone is broken down by enzymes within the liver. From the body, the active ingredient passes through the kidneys.

Medical use and application

Because oxycodone is more potent than morphine, it is considered one of the strongest painkillers available. For this reason, it is used to treat severe or very severe pain. These include neuropathic pain, in which the nervous system has been severely damaged, pain caused by tumor diseases, and pain associated with bone loss (osteoporosis). Furthermore, the opioid can be used as an anesthetic during surgical procedures. In Germany, it is usually not used as a cough suppressant, since codeine and dihydrocodeine are more popular in this country. Oxycodone is usually taken orally in the form of capsules or tablets. Furthermore, there is the option of administering the active ingredient directly into a vein by intravenous injection. In the initial stages of oxycodone treatment, the opioid is taken twice daily. If needed, the dose can also be increased as therapy progresses.

Risks and side effects

The possible side effects of oxycodone include, first and foremost, the pain reliever’s potential for dependence. Thus, there is a risk of physical dependence from taking the opioid if it is administered over a long period of time. Furthermore, psychological dependence can occur. The side effects of oxycodone are similar to those of other opioids.These include headache, constipation, nausea, vomiting, dizziness, constriction of the pupils, spasmodic bronchoconstriction, suppression of the breathing process, reddened skin and itching. In addition, chills, changes in mood, sweating, a decrease in intellectual abilities, rapid fatigue, thirst, dry mouth, difficulty swallowing, hiccups, euphoria, confusion, depression, anxiety, diarrhea, stomach upset, abdominal pain, decreased appetite, and a drop in blood pressure are within the range of possibility. In case of hypersensitivity to oxycodone, the patient must not take the painkiller. The same applies to severe chronic lung disease due to obstruction or cramping of the airways, severe impairment of respiratory function, acute intestinal problems, intestinal paralysis or intestinal obstruction. Oxycodone should also not be used during pregnancy and breastfeeding. Thus, the opioid can penetrate the placenta and reach the unborn child. Likewise, breathing problems or withdrawal symptoms in the baby are conceivable. In children, oxycodone may only be administered after the age of 12. Interactions may occur due to the simultaneous use of oxycodone and other medicines. This includes the intensification of side effects when other opioids, antidepressants, drugs for Parkinson’s disease, neuroleptics, drugs for nausea and vomiting, sleeping pills, sedatives, and antihistamines are administered at the same time. Inhibition of oxycodone degradation is again possible through cimetidine.