What is opioid? Opium, a poppy plant or the “joy plant” as known in earliest civilizations, is accountable for furnishing a number of drugs to mankind that serve as sedatives, tranquillizers and painkillers due to their euphoric effects.

The drugs belonging to this class are also termed as “narcotics” and are chiefly prescribed for severe pain incidents such as in cancer patients and after surgical trauma. Although the history dates back to 3400 BC, ever since it was unveiled to mankind, its euphoric effects have been misused and have become the cause of abuse.

Opioid addiction is one of the strongest obsessions to fight against, driving a person to frenzy. The drugs belonging to opioid class primarily include morphine, heroin, codeine, hydrocodone, oxycodone and fentanyl, to name a few. Since, these drugs are highly abusive due to their strong addictive properties, they are categorized into different schedule of drugs.

Scheduling Of Opioids By FDA

Drugs bearing a strong potential for abuse are termed as “controllable” drugs and have been sorted out into different categories or schedules by FDA depending on their abusive potential.

The scheduling is from 1 to 5 with the drugs bearing strongest potential are graded as schedule 1 drugs and the ones with lowest potential are then graded down the schedule.

Heroin belongs to schedule 1 drug – with a high potential for abuse it has no accepted medical use and lacks a safety data. Furthermore, it cannot be prescribed in any case nor can it be available for clinical trials.

Morphine on the other hand along with its synthetic and semi synthetic analogues (fentanyl, hydromorphone, hydrocodone, methadone, meperidine, oxycodone, oxymorphone) is categorized as schedule 2 drug, bearing a strong potential for abuse but still have limited medical use and can only be dispensed on prescription.

Opioid Addiction

Considering the fact that these are highly abusive drugs and a lot is known about their addictive potential, still people fall prey to their snare.

The abusive potential is related to the tolerance, psychological and physical dependence on the drug, that is, a person addicted to any opioid will develop tolerance for the drug — requiring more of the drug with the passage of time to produce the same effect, will crave for the drug and won’t be able to run any errands until the drug is present in sufficient quantities in the blood.

Moreover, these opioids or narcotics produce addiction overtime — a compulsive drug seeking behavior, that is, the addict despite knowing the harmful effects of the drug, still keeps on seeking for it.

Addiction is a community infliction in terms that not only the addict is subjected to the deleterious effects of the drug but also shares his addiction habits with his friends, family members and other acquaintances.

Thus, a single person can become a source of addiction for tens or hundreds of individuals. The most frequently abused opioid is the heroin and since it is abused either in inject-able form or sniffing it as a powder, the inject-able form is accountable for a number of blood borne infectious diseases such as HIV, hepatitis C and tuberculosis due to needle sharing habit amongst the addicts.

How Does Addiction Or Dependence Develop?

Dependence is a learning process, that is by repeatedly performing a certain task the brain starts learning about that particular task and it eventually becomes a habit. Same learning process holds true for substance abuse dependence.

Substance abuse or abusive substances are connected or interlinked with “pleasure” — the euphoria. The brain “realizes” that the substance abuse is somehow related to “pleasure”, and therefore, craving or desire starts developing gradually for that substance abuse. This means that whenever an individual initiates the use of an addictive substance, he /she will drive pleasure from that substance abuse.

This phenomenon has a neurobiological basis, that is the pleasure is actually related to the rise or surge of a specific neurotransmitter — the dopamine, in the pleasure center (nucleus accumbens) of the brain.

The dopamine is a neurotransmitter that is related to pleasure. Whenever a task that is pleasurable for an individual is performed such as eating or sex, the levels of this neurotransmitter escalate and starts binding to the nucleus accumbens – the pleasure center. The same happens when opioids or narcotics are taken in since addicts seek narcotics for pleasure or recreational purposes.

The opioids bind to their receptors in the brain and these receptors are abundant in the mesolimbic dopamine pathway – the reward pathway. The reward pathway is responsible for our desires, pleasures and cravings. Whenever we want, desire or crave for something, that specific object or stimulus (in this case substance abuse) triggers or activates the reward pathway, thus making us crave or desire more for that object or thing /stimulus.

The more this pathway is activated the more we crave or desire for it and this leads to our dependency and finally addiction for that particular substance/object, making it our habit.

How To Counter Addiction?

Although various opioid antagonists or blockers have been synthesized with the passage of time, the problem still persists as they are also subject to addiction. The commonly employed antagonists are buprenorphine (Buprenex), buprenorphine + naloxone (Suboxone), naloxone (Narcan), naltrexone (Vivitrol) and methadone (Dolophine).

These antagonists eliminate withdrawal symptoms and diminish craving for the narcotics by acting on the same receptors as opioids, produce the same pain relieving effect but are not addictive as opioids, thus free of abusive potential when taken as directed under the surveillance and monitoring of rehabilitation centers.

However, since these blockers or antagonists are analogous to the natural or synthetic or semi-synthetic opioids, they also possess abusive potential if used for prolonged periods and in large quantities.

Although methadone had long been used as a maintenance therapy in addicts, suboxone is superior to methadone in countering the addiction or dependence on the opioids. This is because methadone, like heroin, is an agonist of the opioid receptors, that is, it activates the receptors in the same way as heroin, leads to a stronger dependence if used for prolonged periods and is fatal in overdoses, especially if accidently ingested by children.

Methadone worked as a maintenance therapy in addicts by being present in the addicts blood for longer periods of time, therefore, only once daily dose of methadone was required. It was a substitute of heroin but with less abusive potential. The patient had to be on maintenance therapy for months or years, gradually weaning off from the methadone.

But it was found that being on maintenance therapy on methadone for longer periods actually resulted in severe dependence on methadone and made the detoxification process – a drug free state, even more difficult. Moreover, its overdosage is responsible for respiratory depression resulting in death.

Suboxone contains naloxone plus buprenorphine. It is superior to methadone and now widely used as a counter addiction therapy. This is because it is administered sublingually — under the tongue — in contrast to intravenous use of methadone which requires injection.

Moreover, studies have demonstrated that buprenorphine blocks the effects of heroin and withdrawal from heroin is easy when Suboxone is substituted than compared to methadone.

Additionally, it has less potential for dependence on long term use as a maintenance therapy, it has no evidence for development of tolerance, and is much safer in overdoses and has a ceiling effect to respiratory depression.

The addition of naloxone makes the drug less liable to be abused as an injectable since naloxone produces severe withdrawal symptoms when Suboxone is injected intravenously, thus deterring the opioid addicts to abuse. Furthermore, detoxification is achieved far more easily as compared to methadone.

Is Suboxone Also Addictive?

However, recently a news was published in New York Times regarding fatalities due to Suboxone overdosage. According to the New York Times report, after a decade of ruling the opioid addiction market as an antidote to opioids, its benefits have been tampered due to illicit prescribing by doctors and utilizing it as a dope by addicts, drug dealers and addicts undergoing rehabilitation process.

The social benefit that had been associated with its authorized and “as directed” use had been messed around with or manipulated. The report/news documented a number of stories of patients that had been succumbed to death due to overdosage of Suboxone.

The drug has become a profitable or high income asset for manufacturers, doctors, drug dealers and even patients who pass on the drug to friends and family members or acquaintances. The plausible cause of death might be that since the drug was known to have a plateau effect — milder and less likely to be overdosed and deadly — this apparently “safety factor” led to its over dosage in addicts, not expecting it to be fatal in overdosage.

Moreover, the drug is also available in a filmstrip form which is easily dissolvable, melting it right away once the drug is in the mouth, leaving no trace of its use. Although the drug is to be prescribed by only federally authorized licensed practitioners and that too to only a certain number of patients per month to avoid and discourage its misuse, yet this stringent federal policy has still led to its abuse.

A volatile subculture has risen due to this restriction, due to resurfacing of mushroom clinics that would deliver the drug on cash payment, feeding a thriving underground market. Addicts undergoing withdrawal symptoms due to heroin discontinuation or those that were not able to pay the federally licensed doctors or the ones using the drug as a dope would benefit from these underground markets.

According to the report, “At least 1,350 of 12,780 buprenorphine doctors have been sanctioned nationally for offenses that include excessive narcotics prescribing and practicing medicine while impaired. Some have been suspended or arrested, leaving patients in the lurch.”

According to the statistics released by the law enforcement authorities, buprenorphine abuse has markedly escalated as reported by poison centers in emergency visits to hospital due to illicit use or accidental ingestions by children.

Cause Behind Illicit Use?

According to Senator Hatch, the problem with overdosage fatalities resulted when the patient load was hiked from 30 to 100 per year as initially the federally licensed doctors were allowed to prescribe Suboxone to only 30 patients per year but due to lobbying by the health officials and the manufacturer (Reckitt Benckiser) of the Suboxne regarding its restricted access to the patients, an amendment was passed in 2006, allowing doctors to increase the prescription number from 30 to 100 patients per year. This set the stage for misuse due to more prescriptions and patients.

Possible Solution For The Problem

Although the reports regarding expiry of patients regarding Suboxone overdosage may hold truth, the rule of thumb is that excess of everything is detrimental, even if it is water. Since drugs are inherently associated with side effects, their overdosage is link to mortality is a reality. Addicts or any patient who is dependent on drugs must bear this in mind that illicit/non–medical use or self-administration of drugs is a path that can lead to dangerous results.

Moreover, narcotics or anti-narcotics are associated with high potential for abuse and are always weaned off in a tapering manner so that a limited amount of the opioid or the blocker is always present in the blood to satisfy the craving for the drug. Furthermore, drugs are always labelled to be used “as directed” by physician. This becomes even more necessary in the case of narcotic or opioid blocker use.

The safety factor for narcotics and opioid blockers lie in the fact that they must be used “as directed” and should never be discontinued abruptly but in a tapering manner — gradually over a period of time that might last for years, eventually detoxifying the patient of the drug. Moreover, they should never be overdosed. Following safety principles would never bring adverse events, whatever the drug.