Nalbuphine or Nubain: A Widely Abused Narcotic in Weight-Lifters

Nalbuphine is an addictive injectable narcotic manufactured by Endo Pharmaceuticals, the company with the most different forms of narcotics on the market.  Endo claims "Nubain is is a potent analgesic" (PDR 2003), but it is no more potent than the average opiate, which isn't saying much.  It is related to both naloxone and oxymorphone chemically.  It has antagonist effects mainly at low doses, although it can block other opioid drugs precipitating withdrawal.  It is sold for moderate to severe pain.  According to the manufacturer, it has a low abuse potential, less than that of codeine or propoxyphene, but addiction has occurred.  It is a kappa agonist-antagonist opioid (Neurosci Lett 2003;345:165-8).  In this respect, it is similar to pentazocine (Talwin), which is widely abused.

Sadly, the FDA allows nalbuphine to be unscheduled which means there are no narcotic controls on it whatsoever and it is widely abused by body-builders.  It is definitely addictive and dangerous, although probably not as bad as full agonist narcotics.  It should be listed as schedule III.  It is probably preferable to other narcotics if a narcotic is going to be used.  Most studies find nalbuphine as effect at pain relief as other narcotics.  Like all other narcotics, nalbuphine appears inferior to non-narcotic pain relievers, although few comparative studies have been done.

I was able to find only three studies comparing nalbuphine to a non-narcotic and two of these were against the weaker pain releiver, acetaminophen (Tylenol).  In no study did nalbuphine do better than the non-narcotic. Nalbuphine's record is 0 wins, 0 losses, and 3 ties. Choose the non-narcotic and, if your having surgery, ask for a non-narcotic which is stronger than 650 mg of Tylenol.

Low dose nalbuphine reportedly provided poor pain relief in 115 patients being brought to the hospital by paramedics, although it was not a controlled study (Emerg Med J 2002;19:565-70).  IV nalbuphine provided poor analgesia for children in sickle-cell crisis (J Pain Symptom Manage 2000;19:6372) although this was not a controlled study.  Nalbuphine was equal to meperidine in a DB study of 150 children undergoing tonsillectomy (Eur J Anaesth 1999;16:186-94)(Nalbuphine is widely used on children.  What an abuse of children! Needless narcotics).  Similar results occurred for women having abdominal hysterectomies (Acta Anaest Sin 1998;36:65-70).  When nalbuphine is used pre-hospital, it increases resistance to opiates after arrival at the hospital, leading to higher doses of morphine, etc. bieng given (J Accid Emerg Med 1999;16:29-31)(Why were narcotics used at all?).

Despite the manufacturer's claim, the Alcohol and Drug Abuse Research Center at Harvard-McLean reported interviewing 11 body builders who have used nalbuphine, an unscheduled narcotic.  Eight were clinically dependent on nalbuphine and seven had experienced tolerance and withdrawal. Eight, who had never used IV drugs before, reported using nalbuphine IV.  Morbidity was "extensive" with medical and psychiatric complications. All reported awidespread nalbuphine use in gums they frequented.  Authors (JD Wines Jr, et al) call for a re-evaluation of the scheduling status of nalbuphine (Am J Addict 1999;8:161-4).

Doctors are so insensitive to the narcotics issue that there are many studies comparing nalbuphine to other narcotics, but only the below comparing it to non-narcotics.  Shame on the entire field of medicine and our corrupt FDA.

Children Dental Surgery: Narcotic Nalbuphine No Better than Non-Narcotic Diclofenac: In a DB study of 60 chidren having extractions under general anesthesia, children received either IV nalbuphine 0.3 mg/kg or diclofenac suppositories 12.5 mg to a dose of 1-2 mg/kg or placebo.  Duration of anesthesia was longer with diclofenac (9.6 min vs. 7.2 for placebo and 6.9 for nalbuphine).  There was no difference in post-op pain scores. Littlejohn IH, et al. London Hospital Medical College, UK. Post-operative pain relief in children following extraction of carious deciduous teeth under general anaesthesia: a comparison of nalbuphine and diclofenac. Eur J Anaesthesiol 1996;13:359-63. Ed: The non-narcotic was also much less expensive.

Headaches: Neither Nalbuphine Nor Hydroxyzine Nor the Combination Did Better than Placebo: In a study of 94 patients with severe headaches, nalbuphine 10 mg. vs. hydroxyzine 50 mg. vs. the combination vs. placebo, no treatment did better than placebo for classic migraines.  Tek S, et al. Ann Emerg Med 1987;16:308-13.  Ed: Nalbuphine may have helped headaches other than classic migraines, but this was a post-hoc analysis in a very small study to be breaking it up into 8 different treatment groups.  Also, hydroxyzine is rarely considered an appropriate treatment by itself for headaches, thus, this study is more a placebo vs. narcotic study. Narcotics do help headaches, but the trigger addiction and help headaches less than standard non-narcotic pain relievers.  This study was not counted in my overall tabulation.

OB-GYN Surgery: Acetaminophen Cut Nalbuphine Dose in Half and Still Resulted in Better Pain Relief: In a single-blind study of 152 women, post-op pain was treated with IV acetaminophen 2000 mg with nalbuphine 10 mg or nalbuphine 20 mg.  The acetaminophen group had significantly better pain at one and two hours, despite half the narcotic level. Monrigal C, et al. Angers, France. Ann Fr Anesth Reanim 1994;13:153-7. Ed: This is not a study comparing a non-narcotic to a narcotic.  But it repeated an almost universal finding that adding a non-narcotic to a narcotic results in a considerable decrease in the amount of narcotic needed to achieve the same effect and usually results in better pain control.  In fact, not giving a non-narcotic, in view of the research, mistreats patients, causing them to suffer unnecessary pain and to be subjected to excessive doses of narcotics (if the narcotics are needed at all, which is extremely doubtful).

Post-Op Pain: Nalbuphine No Better Than Acetaminophen Although Combination Somewhat Better: In a DB PC study of 126 patients with post-op pain, a single dose of nalbuphine 30 mg orally was not significantly better than acetaminophen 650 mg at any point from 1-6 hours for pain relief.  However, the combination was better at hours 4, 5, and 6.  All did better than placebo. Comparison of oral nalbuphine, acetaminophen, and their combination in postoperative pain. Jain AK, et al. Clin Pharmacol Ther 1986;39:295-9.

Post-Op Pain: Nalbuphine No Better Than Acetaminophen Although Combination Somewhat Better: In a DB PC study of 129 patients with post-operative pain, nalbuphine 30 mg orally did no better than acetaminophen 650 mg, but the combination did better.  All were better than placebo. Nalbuphine, acetaminophen, and their combination in postoperative pain. Nalbuphine, acetaminophen, and their combination in postoperative pain. Forbes JA, et al. Clin Pharmacol Ther 1984;35:843-51. Ed: This study is virtually identical to the one above.  I imagine it was funded by a manufacturer thinking of introducing the combination.  Certainly, by choosing one of the weakest pain relievers for a comparator, the manufacturer was avoided the embarassment of its narcotic being shown inferior. 

Study unavailable to me: IM ketorolac vs. nalbuphine in orthopedic surgery. Munguia-Fajardo Y, et al. Proc West Pharmacol Soc. 1992;35:195-9.

Labor and Delivery: Nalbuphine and Butorphanol Caused Infants Not to Initiate Breast-Feeding as Readily: Compared to 22 mothers who did not have labor analgesia, infants whose mothers received analgesia more than one hour before birth initiated breast feeding later, and establied effective feeding significantly later. Crowell MK, et al. Univ of Illinois at Chicago. J Nurse Midwifery 1994;39:150-6.