Tox Tuesday: Nalbuphine

January 19, 2016

Prescribed by doctors for pain relief, usually after surgery or childbirth, nalbuphine, which is sold under trade names that include Nubain, is a semi-synthetic opioid drug that is often used in place of other powerful pain medication, such as morphine. While available by prescription only, reports of this drug being abused date back several decades and today is responsible for a new HIV epidemic and has also been found in the professional bodybuilding world.

Nalbuphine is explained as essentially the same potency as morphine, but nalbuphine has less potential for abuse as it exhibits a “ceiling effect,” meaning a dose over 30 milligrams does not produce further

results once metabolized by the body. Nalbuphine has also been found to work better for some who do not respond to morphine, or who develop adverse reactions after being treated with it. This includes pruritus, a condition of intensely itchy skin that can occur after being treated with morphine as well as after kidney dialysis treatment. Nalbuphine has shown to be effective in relieving symptoms in both these cases.

Compared to morphine, Nalbuphine works a bit differently after being metabolized, as it is an opioid agonist-antagonist of the phenanthrene series and binds to different opioid receptors in the brain than morphine and other similar prescription pain medication. Because of this, nalbuphine has also been used to help treat cocaine abuse and other opioid drug dependence issues. However, as of late, nalbuphine has gained more popularity for quiet the opposite of drug treatment, including issues of abuse and addiction.

Cebu City in the Philippines is currently the epicenter of many of these issues as people have turned to abusing the drug in “shooting galleries,” a place where people gather to purchase and inject the drug. According to a recent article, the effects of the drug can be felt within two to three minutes after intravenous administration and is available in the country at about $3 per milliliter. Smaller quantities can often be purchased for as little as 50 cents.

In addition, unused needles sell for another 50 cents, but as the article explains, few people who come through the shooting gallery choose to purchase one. Instead, the dealer in these shooting galleries will supply free “service needles,” which can be new and slightly used syringes on rotation that any customer can use. In fact, it’s common for groups of customers to split the cost of a vial of nalbuphine between them, and share a service needle.

The Philippine Department of Health (DOH) said that the typical shooting gallery has three to five service needles on rotation at a time, each of which can be used four to six times before it becomes too blunt to use. According to Genesis Samonte, the head of the department’s HIV surveillance unit, one shared needle can infect four to six people with HIV or hepatitis C and is to blame for the high rate of these diseases, especially HIV, at a time when new infections have declined worldwide.

Injecting pure nalbuphine is not all that worries government officials in the city. Known to create an even more dangerous and faster addiction is “Milkshake,” a drug combination of nalbuphine and crack cocaine. While users report that the combination of the drugs enhances their high, studies have shown that scientifically this may not be true.

Regardless, stopping the drug from entering into the city in the first place, or spreading to other areas, has become a top priority in the city along with increased access to drug treatment, clean needle exchange programs, contraceptives and sexual health education. Tracking the drug down, however, has proven difficult as many officials have traced it back to the black market with origins in Pakistan and throughout India.

The article explains that once a user in the Philippines is caught with the drug, they can be arrested immediately and forced to undergo a rehabilitation program. Second time offenders face six years imprisonment, with more grave penalties for repeat offenses. In the U.S., however, nalbuphine is currently not a controlled substance under the Controlled Substances Act.

That is one reason the misuse of nalbuphine also has been reported among bodybuilders around the world. Allegedly able to help one train twice as hard for twice as long, the drug limits an athlete’s ability to feel pain. Once athletes develop a pattern of use, they can also become addicted to the “high” it produces, the article explains.

Extreme muscle tears have been reported from training while using nalbuphine and it has been described as a cousin of heroin, in terms of its addictive nature. The article goes on to explain that as many as 80% of those involved in bodybuilding competitions have used nalbuphine, or a combination of nalbuphine and other performance enhancing drugs, at some point in their career.

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Category: Toxicology, Toxicology, Toxicology