Abstract
The paper is going to talk about the drug Tramadol. Tramadol is an opioid drug that relieves pain and is usually known and marketed under the trade names Ultram and Ultracet. The paper will give a description of the type of disease the drug was invented for. It is meant to relieve different types of pains like neuropathy in both its chronic and acute form and dental pain. The Tramadol drug is also associated with treating cancer pain in an estimated period of not more than three months. The paper is also going to talk about the detailed explanation of the process involved in the discovery of the drug Tramadol. The synthetic route that was used to make the drug active will also be discussed in this paper. Reports on ADME and toxicology will also be included to show how they came about with the Tramadol drug, how they discovered it and also how they tested it to make sure it is an active drug. The paper will also feature the clinical trial data which will include details of the post-launch market information. It will feature the data to prove to the market how the trial was successful in getting to know how the drug works. Lastly, the paper will discuss how Tramadol drug compares with others on the market like morphine that are used to treat the same disease or other different treatments.
Introduction
Tramadol is an opioid drug that is used as a pain reliever. It is similar to morphine in the sense that it is also a pain relieving drug. The mechanism that tramadol uses in pain relieving is that of binding opioid receptors in the brain that are vital in the transmission of pain throughout the body to the brain. By so doing, the pain is either stopped or lessened. Tramadol is also linked to forms of abuse and addiction by patients who tend to use it without the recommendation of their doctor. The fact that tramadol is linked to potential abuse and addiction makes it tightly regulated. Regardless of the fact that it is prone to abuse, it is the safest method of pain relief compared to heroin and oxycontin which have both abuse potential and no acceptable medical use.
The Disease for which Tramadol was invented
The drug Tramadol was invented for the disease known as osteoarthritis. Osteoarthritis mostly affects older people than younger people. The risk of death associated with people dying of osteoarthritis is linked to older people than younger ones. Osteoarthritis is a form of arthritis that is common among millions of people in the world. It is a disorder that occurs when the protective cartilage that cushions the bone ends wears down over a long period of time. The condition mostly affects the joints in the hands, spine, hips and knees (Kaye, Allan, 397).
Osteoarthritis is a disease that is mostly associated with aging. It starts by pain, some tenderness, stiffening of the joints and the hips might begin to hurt after any strenuous activity. The aging aspect that contributes to osteoarthritis comes about as a result of the protein composition of the cartilage decreasing and the water content of the cartilage increasing. Consistent use of the cartilage leads to the joint pains and the swelling. The pain associated with these areas are mostly felt during and after an activity that required use of these body parts.
Osteoarthritis is usually associated with a lot of pain in the joints around the knee, hip, spine and the hands. The pain comes about as a result of the cartilage in a joint stiffening and losing its elasticity, which makes it more prone to damage caused by various activities. The tendons and ligaments stretch over time which causes a lot of pain. The more the ligaments and tendons stretch, the more the pain around the areas associated with the pain. It might lead to loss of movement in severe cases (Raffa, Robert, 1443).
Tramadol is used in the treatment of osteoarthritis since it associated with treating moderate to chronic pains. In this case, osteoarthritis is a chronic case due to the pain associated with it. The drug is also used to treat for extended time frames and for a continuous period for effective results. The fact that it is used continuously for long, makes it the recommended type of drug for the treatment of osteoarthritis. It is because tramadol is not recommended to children less than eighteen years, overweight children, and children with breathing disorders (Wright, Curtis, Robert, Raymond).
Tramadol is recommended for the treatment of osteoarthritis since it is a fast pain relief method. It begins relieving the pain approximately within an hour of administration of the drug and then it continues for a further three hours. Due to the fact that it relieves the osteoarthritis pain in a faster way, it is the safest and easiest drug to use when in extreme pain. Older people require this fast pain relief drug since they cannot bear the pain for a longer time. In this manner, the drug improves the situation and pain associated with osteoarthritis to the affected patients involved (Kaye, Alan, 397).
Despite the fact that Tramadol is the suitable drug for osteoarthritis, it also has its negative symptoms and side effects. The symptoms associated with Tramadol drug are dizziness, sweating, constipation, nausea, among others which are also similar to other opioids. The difference between tramadol and morphine is that, morphine causes the release of histamine while tramadol does not release histamine. Tramadol has no effect on the heart rate or on the cardiac index at the therapeutic dosages to its patients.
The Process Involved in the Invention of Tramadol
Tramadol was invented after other medicinal drugs had already been invented. A German drug company which majored in pain treatment in 1962 invented the drug. Before it was approved for use in the foreign market, tramadol was tested for 15 years in Germany (Elkalioubie & Ahmed, 855-858). When it was approved for use, the name tramal was used to refer to tramadol as from 1977. Tramadol was termed as a success for this company when it come to relieving pain. Pain-relieving among patients undergoing various types of treatment was the initial reason that necessitated the German company to come up with a medication that could cure pain.
Many patients used to undergo different types of pains. The pains by these patients to some extent made some to fear treatment. Some of the minor pains for which tramadol was invented to cure was dental, osteoporosis, and neuropathy in their various forms of development. After its invention, it was realized that the drug could also cure the pain related to cancer when it is still in its development stages.
In its invention, it was realized that a fully synthetic drug was necessary for to relief pain. It was one instance that led to research so as to develop such a drug. In comparison with other types of opiates like morphine and codeine, tramadol is man-made. Some other forms of opiates which were also manufacture in the laboratory were found to retain some natural characteristics. Examples of such drugs are hydromorphone, hydrocodone, and oxycodone. An opium drug that was fully synthetic was necessary to aid the investigations being undertaken by the German company in relation to pain relieving.
Moreover, a drug that could offer more benefits rather than relieving the pain was needed. A drug that could cause some relaxation feelings through the brain when a patient was going a treatment like an operation was necessary. Tramadol was therefore found to be the best recommendation for this as it has been incorporated with different transmitter chemicals for the brain. The two chemicals that were included in this drug to realize this condition were norepinephrine and serotonin. These chemicals are known for their capabilities to enhance concentration and that they could manage other body functions like mood and sleep.
Even though tramadol acted like an opiate, it was not classified as one when it was approved for usage in 1995 (Robert). It was used for a long period until in 2014 when the FDA classified it under controlled substances as a result of the rampant abuse. It was regulated to control the high-level of abuse it had encountered. In terms of spectrum, tramadol was found to offer safer results as compared to other drugs in the market. As a result, tramadol was listed under the schedule Ⅳ drugs for the reason that as it could be abused, it had some potential benefits as compared to other drugs like Heroine which were on the high verge of being abused but do not have medicinal properties.
Despite the concerns discussed about this drug, it still has benefit in the modern world. It was realized that the drug could also aid in the treatment of osteoarthritis and other types of pains in the modern era. Many agencies came together to determine other illnesses which the drug could aid in treatment, the recent one being the American Academy of Orthopaedic Surgeons which recommended tramadol in osteoarthritis treatment.
Fig1: Tramadol Use in the USA in 2012 and 2013
In the modern research, tramadol was linked to some death cases. Among the 90,000 patients who participated in the research, it was established that tramadol accounted for a higher level of death as compared to other types of pain-relievers. For example, it was established that 2.2% of the patients who were given tramadol as a pain-reliever died as compared to the 1.3% of patients who died after being given naproxen (Robert). The challenge in this research was that the research could not ascertain whether the deaths were as a result of the injected tramadol or the natural death due to the illness of the patient.
Since its invention, the use of this drug has been on the rise. May countries have joined hands to incorporate the drug in their medication systems so as to relief the pain felt by many people undergoing treatment. Although the use of this drug has been gaining usage, some people are abusing its use. It has been reported that many governments, as a result of the many cases of drug abuse reported in relation to tramadol, have resorted in burning the usage. Other governments have allowed it to be used but under strict regulation, being considered for medicinal purposes.
As all medications come with a risk dose, tramadol was weight and the risks related to it found to be negligible. As compared to the other forms of pain-relieving drugs, tramadol was invented so that it could reduce the dangers imposed to the patients by the use of drugs whose risks were high. Risk dose was also one reason that necessitated the scientists to come up with this type of drug. It was seen that it could reduce some of the deaths associated with extreme pains and also it could make the work of doctors attending to various patients easy (Elkalioubie & Ahmed, 857).
Elkalioubie, Ahmed, et al. “Near-fatal tramadol cardiotoxicity in a CYP2D6 ultrarapid metabolizer.” European journal of clinical pharmacology 67.8 (2011): 855-858.
Kaye, Alan David. “Tramadol, pharmacology, side effects, and serotonin syndrome: a review.” Pain physician 18 (2015): 395-400.
Raffa, Robert B., et al. “Mechanistic and functional differentiation of tapentadol and tramadol.” Expert opinion on pharmacotherapy 13.10 (2012): 1437-1449.
Robert H. Shmerling, MD. “Is Tramadol A Risky Pain Medication? – Harvard Health Blog”. Harvard Health Blog, 2019, https://www.health.harvard.edu/blog/is-tramadol-a-risky-pain-medication-2019061416844.
Wright, Curtis, Robert Colucci, and Raymond Sanchez. “Titration dosing regimen for controlled release tramadol.” U.S. Patent No. 8,722,087. 13 May 2014.
