Nowadays, medical science offers numerous remedies for alleviating pain, ranging from regular painkillers to ‘The Simpsons’, but opioids have been alleged to be the most effective in this regard. Opioids have also been suspected of providing euphoric entertainment (sometimes unintended) to people who are into using the drugs for non-medical purposes, i.e. abusing the drugs. The use of opioids as a painkiller and source of unmatched euphoria can be dated back to antiquity.
Actor Bela Lugosi, writer Charles Dickens, poet Elizabeth Barrett Browning, Kurt Cobain, and Dr. John Pembert (inventor of Coca Cola) were all regular users of opioids (in one form or the other), although, several experts have refuted the claims regarding the link between their creative genius and the noted drug use. Opioids have come a long way from being used as Mrs. Winslow’s Soothing Syrup to put babies to sleep to being used as a pain-relieving agent in palliative care. To ascertain the positive and negative effects of opioids, the composition, use and abuse of the drug has to be understood (in relevant detail).

An opioid is one of the commonly used analgesics (painkillers) – a property attributed to its ability to ‘decrease the perception of pain and also increase pain tolerance’. Contrastingly, prolonged use of opioids has also been linked to side effects such as constipation, sedition and respiratory depression. Other adverse effects due to the use of opioids can be the over-dependence on the drug, which might result in severe complications when the drug is abruptly discontinued. Our nervous system and certain parts of the small intestine possess specific receptors, generally referred to as opium receptors, which mediate these ‘benefits as well as side-effects’. Opioids have specific chemicals that can stimulate these receptors, thereby leading to a decreased perception of pain.

The use of opioids has been recommended by the World Health Organization (WHO) as one of the best pain-relieving treatments. In spite of this, only six countries in the world are using nearly 80 percent opioid and related medications signifying that other countries largely lack such pain-relief drugs. The supply chain of poppy based drugs is monitored by the International Narcotics Control Board, which is bound to the terms and provisions of Single Convention on Narcotic Drugs (1961). The supply of these drugs to all the countries in the world is strictly scrutinized, which has resulted in under-prescription of these pain relieving drugs in some developing countries. In response to this, World Health Organization (WHO) is considering training health workers to facilitate an increased use of these poppy based drugs for pain relieving purposes. The stringent rules and regulations against these drugs were developed with the course of time. It started with the Harrison Narcotics Tax (1914) that criminalized non-clinical use of poppy related drugs. After this act, different countries in the world came up with their own laws to monitor the use of these drugs. A report developed by the Royal College of Physicians in UK reasserted that medical use of these drugs is essential but should be properly monitored. Since then, the controlled medical use of these drugs has been recommended time and again.
The ‘Drug Facts and Comparisons, 2005’ suggested that Opioids could be used for a wide range of purposes – as pain relievers (mainly post-operative pain), curing cough and diarrhea and as anxiety relievers. Lady Day (Billie Holliday) had contested the fact by claiming that it gave her anxiety rather than alleviating it. She emphasized by quoting her $750 tabloid fee that she could not pay till death due to the lack of funds in her bank account ($0.70 at the time of her demise). Analysts have attributed the lack of funds in the jazz queen’s account to ‘God Bless the Child’, which sold over a million copies and the excessive spending on drugs and alcohol.
Opioids can relieve pain of moderate and severe intensity and can be used for maintaining anesthesia during surgery. Opioids can be more effective than diazepam (used for treating insomnia and anxiety) in relieving pain. Opioids can also be used as intra-spinal injection and can also be used in surgical procedures where normal procedures cannot be used due to allergy or related reasons. Opioids are also used in cough syrups – the basic cough relieving opioids are codeine and hydrocodone and morphine for more complicated cases. In addition to this, opioids can also be used to treat severe cases of diarrhea. Some of the best known opioids that have been used to treat diarrhea are loperamide and difenoxin, but in some complicated cases, powdered opium is also used. Diarrhea related to IBS (Irritable Bowel Syndrome) can also be treated with the help of opioids, such as Codeine, paregoric and laudanum. Opioids can also effectively treat anxiety linked to the shortness of breath. Opioids are generally used for psychological relief, which helps us in overcoming our physiological troubles as well. One of the best examples of pain-relieving ability of opioids is in ‘palliative care’, where it is used for treating pain due to cancer and rheumatoid arthritis.

Like several other miraculous drugs, numerous side-effects have been attributed to opioids as well. Some of the most common side-effects attributed to the use of opioids are nausea and vomiting, dry mouth, itching, drowsiness and constipation. Some of the side-effects that are not common but more severe than the common ones include anxiety linked to shortness of breath, hallucinations, dizziness, biliary spasm, urinary retention and muscle rigidity.
Hyperalgesia, induced by the intake of Opioids, has been reported in some of the patients. In this type of disorder, instead of relieving pain more pain is experienced due to the rapid escalation of the dose in some palliative care patients. In some cases, the use of Opioids can result in suppression of the immune system as they can inhibit the migration of infection fighting leucocytes. The use of opioids can facilitate the increase in testosterone levels. This can be fatal to our bones as it can cause severe osteoporosis and weakness in muscles. This condition needs to be properly monitored (by monitoring testosterone levels and prostate-related antigens) as it can cause problems in body movements.

As the use of these opioids cannot be sidelined, it is important to have a well-developed strategy to overcome the adverse effects associated to their use. Experts have suggested some common strategies that should be followed while using these opioids. In addition to these specific measures for each of the side-effects, generally opioid effects can be reversed with the help of opioid antagonists such as naxalone, among others. These antagonists bind to the opioid receptors forcing the opioid to leave the receptor. This results in diminishing the effect of opioids but the affinity of the antagonist for the receptor remains for a short period thus, in order to maintain the antagonist effect, repetitive doses of naxalone might be required. Naxalone and other antagonists are usually required to overcome breathing problems developed on account of over-dose of opioids.

In spite of these adverse effects caused due to opioids abuse, experts in UK, over the course of last two decades, have repeatedly observed that opioids are safe when taken in a controlled manner. Researchers in UK have found that even double dose of morphine didn’t increase the risk of overnight death. Researchers claim that cautiously titrating the dose of opioid can help in overcoming pain and that too with minimal side-effects. In addition to this, experts have failed to prove any link between opioid usage and organ toxicity as has been proved in case of drugs such as aspirin and acetaminophen. If the opioid supply chains are properly regulated and if administration of the drug is properly monitored by the experts, opioids can be used to eliminate human pain and anxiety without any related adverse effects.
The very important thing to note about opioids is that if taken in regular moderation and on exact time’s as prescribed by the doctor, it can be very effective in relieving pain. Deviation from the prescribed time may alleviate the pain as it takes at least 2 hours for opioids to take effect. In contrast, if the drug is taken too often, it may result in amplified sensory perceptions resulting in hallucinations and euphoria, which might actually help in relieving pain but may not be exactly what one wants. So, a boxer might risk taking opioids two hours before a fight in order to prevent the expected pain, but it may also lead to an altered state of consciousness, which can result in a very gleeful knockout (his) that would be both unexpected and unwanted.
Although the use and abuse of the drug has been dated back to 4000 BC and 2000 BC in Sumerians and Egyptians respectively, the importance and negative effective effects of the drug still make a controversial commodity. The use of opioids can be conclusively linked to the old saying about science – it is an obedient servant, but it can be a very bad master.