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Opiate or narcotic drugs have a tremendous potential to alleviate chronic pain, pain associated with surgery, and other forms of pain; however, they are also drugs that are highly prone to abuse, the development of physical dependence, and the development of addictions.
Pharmaceutical companies realized that the development of a very effective pain-relieving drug that would not have a high potential for abuse or for the development of physical dependence could be very profitable. One of the drugs developed in the 1970s in the quest for this type of drug was nalbuphine (Nubain).
Nalbuphine is chemically related both to the opioid antagonist naloxone (blocks the effects of opioid receptors in the brain) and the opioid agonist Opana (oxymorphone; an opioid agonist activates endogenous opioid receptors in the brain, leading to their effects). Nalbuphine was originally classified as a Schedule II controlled substance by the US Drug Enforcement Administration (DEA); however, its manufacturer petitioned the DEA to remove it from drug schedules associated with the Controlled Substances Act, and they were successful in doing so. Thus, nalbuphine remains the only narcotic medication of its type that is not listed in the DEA’s Schedule of Controlled Substances.
According to a number of professional sources, including the DEA and academic texts such as Foye’s Principles of Medicinal Chemistry,nalbuphine is not considered to be a drug with a serious abuse potential, although there are cases where the drug is abused.
The drug is primarily used in hospitals as an injectable and prescribed by physicians.
Because of its very potent antagonistic effects, an individual who has an opioid use disorder will most likely experience withdrawal symptoms upon using it. Nonetheless, individuals with chronic substance abuse issues often abuse any drug. Both of the above sources report that there are case reports of nalbuphine being abused by some healthcare professionals and even anabolic steroid abusers (Some say it can improve fat burning and reduce muscle pains associated with heavy training.); however, it is not considered to be a drug with a potential for abuse.
All opiate drugs carry the potential to develop physical dependence; however, not everyone who uses these drugs will develop significant physical dependence on them. The syndrome of physical dependence consists of the development of tolerance and withdrawal.
Detox refers to a natural process the body uses to rid foreign substances and waste materials from the system. This is primarily accomplished via the liver. Drugs in an individual’s system are systematically metabolized and removed from the system. If an individual has developed physical dependence on a drug such as nalbuphine and does not replenish the amounts of the drug in the system, the detox process will reduce the level of the drug, such that the individual will experience withdrawal symptoms.
According to the book Opioids, nalbuphine has a half-life of about 3-6 hours. The half-life is the time that the concentration of the drug in an individual’s system is reduced by half due to normal metabolic processes (detox). Withdrawal symptoms from nalbuphine appear to occur within 24 hours of discontinuation and peak within 24-48 hours following discontinuation. During this time, individuals may experience varying levels of joint pain, nausea, vomiting, diarrhea, appetite loss, abdominal cramps, joint pain, weakness, irritability, runny nose, teary eyes, dry mouth, increased blood pressure, increased breathing, increased heart rate, irritability, anxiety, depression, and cravings to take more of the drug. These symptoms will typically subside substantially within 72 hours following discontinuation but may remain at a much lower level for a week or more.
Individuals who are able to negotiate withdrawal symptoms without relapsing may still experience much longer periods of time (months to years in some cases) of cravings that often appear due to stressful situations, environmental conditions that remind them of drug use, and other seemingly nondescript situations that trigger memories of the individual’s experiences on drugs.
The individual experience of withdrawal will depend on several factors, including the length of time the individual used the drug, the amount the individual typically used, how often the individual took the drug (e.g., once a day, twice a day, etc.), and how the individual took the drug (e.g., injecting, snorting, etc.). As a general rule, individuals who used the drug for longer periods of time, took it in higher doses, took it more frequently, and injected or snorted it will experience longer withdrawal periods and more severe withdrawal symptoms than individuals who used the drug in lower doses, for shorter periods of time, and/or who took drugs orally. Of course, an important factor in the subjective experience of withdrawal is the individual. Often, differences in the length of the withdrawal symptoms and the severity of the symptoms are due to individual differences in metabolism, other physiological factors, and psychological and emotional stability.
Treatment for withdrawal from nalbuphine can be accomplished by using a tapering strategy, using other drugs to alleviate symptoms (e.g., Clonidine for anxiety), and, in some cases, the use of opioid replacement medications, such as Suboxone. Because this drug is most often administered in a clinical setting and often administered by injection, individuals who have developed physical dependence on it can be given subsequently lower doses of the drug at specific time intervals to slowly and very carefully wean them off the drug. This tapering strategy results in the individual experiencing minimal withdrawal symptoms.
Any withdrawal symptoms that the individual does experience can be controlled by the administration of other medications that can specifically address symptoms, such as headache, nausea, anxiety, etc. Anyone who is taking the drug without being under the supervision of a physician should not attempt to initiate a tapering strategy on their own. Medical detox is recommended.