Ingredients and mechanism of Drug Action

Opioid overdose is a serious issue that has gained immediate medical attention worldwide. Naloxene which is popularly sold under the medicine brand name of Narcan is widely prescribed by the medical experts in order to block the effect of opioid (Walley et al., 2013,p. 346). Naloxene has been reported to be extremely effective in case of drug overdose resulting due to over-consumption of opioid. Naloxene is administered to the patients either intravenously or injected into the muscles. Scientific evidences have reported that the time required to elicit the effect of the drug when administered intravenously is equivalent to 2 minutes (Wermeling, 2015,p.27). On the other hand the time required to elicit an effective response of the drug when administered into the muscle is roughly around 5 minutes (Wermeling, 2015,p.27).

The effects of administering the drug includes generating the withdrawal effect. The withdrawal effect comprises of elements such as accelerated heart-beat, profuse sweating, agitation, nausea and vomiting tendencies (Wheeler,Jones, Gilbert & Davidson, 2015, p. 634). In order to combat the side effects aligned with the administration of the drug, it is widely prescribed by the clinicians that small doses are administered at a specific time duration. Scientific literatures have also stated that the use of Naloxene by patients who are prone to cardiovascular problems often lead to severe complications and hence should be avoided. This essay would focus on the efficacy of the drug Naloxene as a take home drug to save critical conditions that might take away the life of patients who resort to opiate abuse. This essay would delve deeper into the positive effect of the drug and further argue upon the effectiveness of the drug in being prescribed commonly to help patients who are frequent opiate users.

In order to develop a clear understanding about the mechanism of drug action, it is important to first acquire an insight about the ingredients present in the drug. Each millilitre of the drug comprises of the ingredients, 0.4 milligram of Naloxene hydrochloride and 8.9 milligram of sodium chloride is order to substantially balance the tonicity of water to administer the injection with precision (Mueller, Walley, Calcaterra, Glanz & Binswanger, 2015, p. 242). The pH of the drug has been reported to be around 4.0 and it has been stated that the drug comprises a certain proportion of Hydrochloric acid in order to adjust and maintain the pH of the drug. Naloxene has been categorised as a lipophilic compound that has the ability to act as a competitive opioid receptor antagonist and reverse the action of the opioid overdose. Two isomeric forms of the drug have been reported to exist the positive form and the negative form which is also the pharmacologically active form. Studies reveal that there are four subtypes of opioid receptors, namely the µ-opioid receptor, the δ-opioid receptor, nociception receptor and k-opioid receptor (Robinson & Wermeling, 2014, p. 2130). The binding receptor affinity in decreasing order can be stated as: µ-opioid receptor> δ-opioid receptor> k-opioid receptor and nociception receptor (Rudd et al., 2016, p. 1325).

Administration and Effects of Naloxone

Although there are no substantial evidences on the mode of action of the drug, however researchers have stated that the drug proceeds with eliciting an effect of withdrawal. The manifestation of the withdrawal symptoms is produced by the action of competitive inhibition where the molecules of the drug compete to occupy the opiate receptor site that are primarily placed in the central nervous system. On binding with the receptors, the drug molecules effectively prevent the action of opiates that are endogenous and xenobiotic in origin at the receptor sites without generating a direct impact. The drug was patented in the year 1961 by a two eminent scientists, namely Jack Fishman and Mozes J. Lewenstein who worked for the reputed pharmaceutical company Sankyo. The drug was approved in the year 1971 (Parchman et al., 2017, p. 48). The approval was dispensed by the FDA that initiated the distribution of abuse prevention kits to common people during the year 1996 (Parchman et al., 2017, p. 49). The time period of 1996-2014, witnessed approximately a total of 26,000 cases that were successfully reversed using the abuse-prevention kits (Parchman et al., 2017, p. 51).

Take home Naloxone has been prescribed as an anecdote world-wide to deal with the negative impact of the drug. Research papers have revealed that opioid overdose can lead to fatal consequences if not controlled on immediate basis. Naloxone has been discovered to be an effective antidote that has the potential to reverse the adverse effect of opioid. Opioid drug overuse leads to major pre-mature deaths across the world. Most of the death cases have been reported in drug users who use syringes to inject drugs into their body (Sairam Alturi & Manchikant, 2014, p. 120).

Naloxone has been found to be effective in treating respiratory complications and related depression arising due to the use of opioid over-use. Researches state that the first intervention that was developed to reverse the effect of opioid is dated back to the 1990s era. The intervention strategies included spreading awareness about the negative use of opioid and at the same time popularising the use of Naloxone. Access to Naloxone is guaranteed through the use of rescue kits handed over to the opiate users. It should be critically noted that within the past 15 years, ‘Take Home Naloxone’ has been highly popularised in numerous countries across the continents of Europe, North America, Asia and Australia (Mehendale, Goldman & Mehendale, 2013, p. 438). The efficacy of the drug had been analysed thoroughly on the basis of the literary evidences furnished by the scientific studies conducted so far. Naloxone has been reported to minimise the prevalence of death among drug users.

The Role of Naloxone in Reducing Mortality Rate

Statistics obtained from research studies have revealed that ‘Take Home Naloxone’ has reduced the death rate to a considerable extent. Research studies have also reported that administration of Naloxone has helped in the reversal of 2249 drug overdose reversals. Naloxone elicits the effect by binding to the µ-opioid receptor and inhibits the binding ability of all competing agents including heroin which is believe to be a strong drug (Krieter et al.,2016, p. 1245). ‘Take Home Naloxone’ was introduced in Australia in the year 2011. Reports suggest that the administration of Naloxone has led to the reduction of the mortality rate in Australia. However, it should be noted that Naloxone is extremely drug specific and has not been found effective in cases where subjects were intoxicated with high doses of cocaine (Kolondy et al., 2015, p. 560).

Recent studies have effectively highlighted the efficacy of Naloxone to treat drug-overdose. Statistical evidences have stated the prevalence of increased number of deaths due to drug overdose. It has been estimated that every year almost 41,340 deaths occur due to drug overdose (Rudd, 2016, p.65). Further research studies have also revealed that 1 out of 6 individuals indulge in drug abuse in the United States of America (Rudd, 2016, p.65). In this context, it can also be stated that the primary target audience engaging in drug abuse is the adolescent group. In most of the cases, it has been reported that individuals involve in non-prescribed opioid overuse. In order to deal with the problem of drug abuse Naloxone has been found to be an effective anecdote. Naloxone has excellent pharmacological property to actively inhibit the action of opioid by binding to the receptor sites. Scientific studies state that Naloxone possesses the ability to bind to the Mu-receptor sites present in the opioid substance and elicit a negative effect by reversing the overdose and the cascade of fatal consequences involved (Straus, Ghitza & Tai,2013,p.68). The efficacy of the drug made it the first anecdote to be legalised. The legalisation of the drug proceeded with directly handing over the drug to the drug-abusers to reverse the action of overdose in Chicago (Straus et al.,2013,p.67). The initiative was further strengthened by including community based programs that involved distribution of Naloxone to common people. Interestingly, it was found that between the time period of 1996 to 2010, there were approximately 10,171 successful cases of drug overdose reversal (Straus et al., 2013,p.71).

Prevalence of Drug Abuse and Misuse

Opioids can be defined as a class of drugs that occur naturally and are derived from the poppy plant. It is important to note here that opioids have medicinal properties that can effectively treat pain and relax the tensed muscles in order to provide quick relief. The prescription of opioids in order to effectively treat pain and administer relief to patients experiencing muscular spasms or pain fall under the category of prescription opioids. Opioids have also been reported to possess medicinal properties that can effectively cure diarrhoea and cough. In addition to the positive uses, it is important to note that Opioids are often consumed for the wrong purpose on account of the severe addictive properties of the compound (Hser et al., 2014, p. 82). The most common prescription Opioids include the formulations, such as Oxymorphone, Fentanyl, Codeine and Morphine. A common trend prevalent among individuals to misuse opioids have been seen among people especially among the group of teenagers. Misuse of prescription opioids is mainly done by individuals by the virtue of three ways. Either individuals misusing the drug take in the drug in a different manner or enhance the dose levels on their own which is completely different from what has been prescribed by the physician (Gellad, Good & Shulkin, 2017, p. 611).

It has also been observed that individuals misuse the prescriptions of other patients who have been prescribed opioids or there have also been incidences where individuals have deliberately taken high doses of medicine in order to feel elated or get high. Hence, these have been the major contributing factors that have been associated with the misuse of prescribed drugs. Scientific evidences have further revealed that there are various forms in which the drug is taken (Garland et al., 2014, p. 448). For instance, the drugs can either be swallowed in complete form or snort the powdered form of the drug. There have also been reported instances where individuals have crushed the opioid tablets and dissolved it in water and proceeded with injecting the fluid intravenously. The feeling of pleasure associated with the intake of the drug is testified by the ability of the drug to synthesise the hormone dopamine in excess and elicit feelings of momentary euphoria. In order to deal with the problem of opioid misuse, Naloxone has been reported to be extremely effective. ‘Take Home Naloxone’ has been documented to work spontaneously and inhibit the effect and reverse the drug overuse activity. The activity of the drug proceeds with the dearth of withdrawal symptoms that causes initial symptoms of discomfort but ultimately leads to the prevention of the development of fatal symptoms.

The anecdote to the drug overuse of Opioid has been found in the pharmaceutical drug ‘Naloxone’. The anecdote has been found to be extremely effective and can either be injected intravenously, inhaled or be administered in the body with the help of hand-held auto injector (Coffin & Sullivan, 2013, p. 5). It is commonly suggested that the concerned family members of the individuals practicing drug-overuse must get in touch with medical experts to administer Naloxone, however recent studies have shown the popularity of ‘Take Home Naloxone’. Naloxone now a days are directly handed over to the immediate care providers of the affected individuals in order to provide instant relief and save someone who is overdosing and about to die (Clark, Wilder & Winstanley, 2014, p. 158).

Conclusion

Hence, to conclude it can be said that over use of opioid is a major issue all over the world. Evidences have revealed that almost 44 people in the United States of America die on account of opioid overuse every year. Statistical evidences have further revealed that there were almost 5.1% of deaths per 100,000 individuals all over the world. On account of the revelations made by the statistical evidences, it can be said that there is a major issue with the problem of drug use. Researches have unanimously agreed upon the effectiveness of the take home Naloxone drugs to deal with the problems of drug overuse. Hence, Naloxone has been prescribed all over the world as an over the counter medication that is available conveniently and can effectively reverse the effect of opiate overuse.

Literary evidences have further revealed that the mechanism of the drug action proceeds with the blocking of the receptor sites that help in weakening the negative effect of the opioid drug. Studies have revealed that Naloxone possesses of an effective binding ability to bind with the µ-opioid receptor type which is also the most active form of receptor. The drug has been documented to be administered in three ways that include either administering the drug intravenously, intra muscularly or by virtue of inhalation. It has been noticed that the  mode of action is fastest in case of administering the drug intravenously as it facilitates the entry of the drug into the blood stream of the individual and proceeds with eliciting the withdrawal effect. The time frame considered for eliciting the effect is around two minutes. On the other hand, the time taken to generate a response when the drug is injected intra-muscularly is around 5 minutes. Once inside the body, the drug starts its mode of action by manifesting the withdrawal symptoms. The withdrawal symptoms include, profuse sweating, feelings of nausea, weakness, restlessness and mild shivering in individuals who have traces of opioids present in their system. Researchers have commented that the use of Naloxone in individuals who have health issues related to over use of opioids is effective and safe. Initially, the idea of ‘Take Home Naloxone Drugs’ started during the year 1970s. It gradually gained popularity over the years on account of the success rate of the drug. The efficiency of the drug led to the introduction of the drug as an authentic treatment intervention in more than 15 countries all over the world. In addition it should be noted that the drug was introduced across all the major countries with the introduction of the drug in Australia being recent. Global reports have also revealed that the effective administration of the drug at the correct time has helped in the reduction of mortality cases to an impressive extent. Therefore it can be concluded that the use of the ‘Take Home Naloxone’ has been found to be efficient in light of the global scenario.

References

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