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Q: Does naloxone (in any brand name) come in orally active tablets? Is it possible to crush up and inject a naloxone tablet if needed during an OD?

A: The short answer is "no". Naloxone for reversing an overdose is currently only available in liquid form, which can be injected or administered via a nasal spray.1 (While nasal spray is part of the local standard of care in many areas, it has not been approved by the Food and Drug Administration in the United States.)

It's possible you're thinking of naltrexone, a related opioid antagonist that is orally active, but is not generally used to treat opioid overdoses (ODs). Naltrexone can be used to treat alcohol and opiate addiction and is produced in pill, subcutaneous implant, and monthly injection form. Naltrexone, like naloxone, is an opiate antagonist and blocks the effects of opiates/opioids in the body and therefore should work to reverse the effects of an opiate overdose. There are a few reports on the use of naltrexone during an accidental methadone overdose with opioid-naive people (non-regular users for pain or other reasons)2, but its use is contraindicated for people who are habituated to opiates. The reason is that naltrexone lasts much longer in the body, with a half-life of 13 hours compared to naloxone's 30-80 minute half-life, resulting in uncomfortable withdrawal symptoms for people who have an opioid tolerance (including those who use opioids for pain). Attempts to alleviate those withdrawal symptoms by using more opiates would further put a person at risk for re-overdosing. In addition, crushing up and filtering a tablet to prepare an injection when someone is in respiratory distress from an opiate/opioid overdose would take a dangerously long time.

Or, you may be thinking of Suboxone, a prescription tablet that contains buprenorphine and naloxone (at a 4:1 ratio), and which is meant to be taken sublingually (dissolved under the tongue). Suboxone is used to treat addiction to opiates/opioids (morphine, heroin, hydrocodone, etc.) either via tapered doses in a medically supervised withdrawal (detox) program, or as substitution therapy in office-based treatment via an ongoing prescription from a doctor. Since Suboxone consumption is not always directly supervised (like the consumption of methadone in maintenance programs is), naloxone is combined with the buprenorphine in order to prevent people from injecting or snorting Suboxone. Because naloxone is not orally active, it does not block buprenorphine if taken in pill form, but when injected or snorted it will.

Both the buprenorphine and the naloxone in Suboxone may help to reverse an overdose, dependent upon how they are administered.
  • Using sublingual Suboxone to reverse an overdose has not been studied scientifically, although it was reported to work in one case3, most likely because buprenorphine binds more tightly to the opioid receptors than the opiates/opioids that it displaces, but it is much less potent--a "partial agonist"--thereby lifting the respiratory suppression. (Again, since the naloxone is not absorbed sublingually, it has no effect in reversing an overdose when taken this way.)
  • There are no published reports of injecting Suboxone to reverse an overdose, but there are anecdotal reports that it also works when administered this way. This makes more sense, since both the buprenorphine acting as a partial agonist and the naloxone acting as a receptor blocker will decrease the effects of opiates/opioids. In sublingual tablet form, Suboxone contains buprenorphine/naloxone at the following doses: 0.2/0.05 mg, 0.4/0.1 mg, 2/0.5 mg, and 8/2 mg (the last two are the most common). Naloxone sold under the trade name Narcan to reverse opiate/opioid overdose is available as a sterile solution for intravenous, intramuscular, subcutaneous, and intranasal (common, though not FDA-approved) administration in three concentrations: 0.02 mg/mL, 0.4 mg/mL, and 1 mg/mL. Those intending to crush and inject Suboxone pills to treat an overdose should know that although there are anecdotal reports that 0.5 mg injected naloxone is enough to reverse an overdose in some people, other people need a higher dose; and because naloxone has a shorter half-life than almost all opiates/opioids, repeated injections might be needed to keep the overdoser from lapsing back into an overdose. So keeping a single 2/0.5 mg Suboxone tablet handy for an emergency may not be enough naloxone. And again, remember that when someone stops breathing, time is of the essence; the time spent crushing a Suboxone and dissolving it into water for injection is time not spent summoning medical help and providing oxygen by rescue breathing.
The best preparation for responding to an opiate/opioid overdose is to obtain naloxone and learn how to administer it from a naloxone distribution program. Nasal naloxone kits are available that repurpose injectable naloxone, allowing it to be administered to an overdose victim without requiring a needle. Naloxone is not risk-free: it can cause hypertension, tachycardia, cardiovascular collapse, and pulmonary edema. But in the face of respiratory arrest, these risks are usually worth it, and naloxone has saved the lives of countless overdose victims. Websites advertise naloxone distribution programs in the United States<4 and other countries.5

Please note that there are documented cases of fatal Suboxone overdoses among children and adults, particularly when combined with other sedating medications such as benzodiazepines. Also, Subutex--used much less often than Suboxone in the United States--contains only buprenorphine and no naloxone.

References #
  1. Kerr D, Kelly A-M, Dietze P, Jolley D, Barger B. "Randomized Controlled Trial Comparing the Effectiveness and Safety of Intranasal and Intramuscular Naloxone for the Treatment of Suspected Heroin Overdose". Addiction 2009 Nov;104(12):2067-74.
  2. Dhopesh V, Yu E, Fudala, P. "Conservative Management With Naltrexone of an Iatrogenic Methadone Overdose in an Opiate-Naive Patient". Journal of Clinical Psychopharmacology 2002 Apr; 22(2):231-2.
  3. Welsh C, Sherman SG, Tobin KE. "A Case of Heroin Overdose Reversed by Sublingually Administered Buprenorphine/Naloxone (Suboxone)". Addiction 2008 Jul;103(7):1226-8.
  4. South Boston Hope & Recovery Coalition, http://hopeandrecovery.org/overdose/
  5. Take-Home Naloxone, http://www.take-homenaloxone.org/

Asked By : AC
Answered By : Maya
Edited By : Andrew Sewell, the Erowid Crew
Published Date : 1 / 18 / 2012
Last Edited Date : 2 / 7 / 2012
Question ID : 3175

Categories: [ Naltrexone ] [ Naloxone ] [ Effects ] [ Heroin ] [ Opiates ] [ Buprenorphine ] [ Overdose ] [ Addiction ]




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