An Old-But-New Treatment for Opioid Addiction

by | Apr 1, 2021

Lucy’s addiction to heroin began over 25 years ago. “It was a slow creep,” she says, “and then all of a sudden I was doing an eight ball a day and living on the street.”

Over the years, Lucy has tried to overcome opioid use disorder (OUD) through a variety of methods, including hospital detox and methadone maintenance. She is now taking frequent, high doses of buffered vitamin C to try and kick her addiction.

Lucy’s curiosity in trying the vitamin C regimen was rooted in desperation. Even after enrolling in an outpatient injectable opioid agonist therapy (iOAT) program through which she received high doses of opiates twice a day, every day, Lucy was still plagued by drug cravings and breakthrough withdrawal symptoms. She controlled these symptoms with street drugs—about 300 mg a day of fentanyl, a synthetic opioid pain reliever 50 to 100 times more potent than morphine,1 or “whatever I could get my hands on.”

Lucy was flung into the throes of withdrawal, however, when she could no longer afford her $50 to $75-a-day fentanyl habit. “I was so sick I was blacking out – they wanted to call an ambulance,” she says of the staff at the nearby health clinic. As a last-ditch attempt, a nurse suggested calling Trevor Millar, a local health advocate well versed in supporting those with opioid addiction.

Millar met Lucy that night with a bottle of sodium ascorbate, a buffered form of vitamin C, and instructed her to take 2 grams of the vitamin every two waking hours.

“The next morning, I woke up and I had no withdrawal symptoms,” Lucy tells me. “I felt better than I had in years. Had I had to do that come down on my own, it would have killed me.”

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The Epidemic Rages On

Lucy isn’t the only North American living with opioid use order (OUD). OUD refers to a problematic pattern of opioid drug use that leads to serious harm (or risk of harm) for a person. (The condition is also known simply as “opioid addiction.”) While OUD used to be centered on heroin, the use of prescription opioids pain relievers—drugs like fentanyl, oxycodone (OxyContin®), hydrocodone (Vicodin®), codeine, and morphine—is now on the rise. Opioids are implicated in overdose deaths more than any other drug class, claiming more lives than guns, breast cancer, or car accidents.2

The prescribing practices of healthcare providers are implicated: opioid misuse often begins with a legally acquired prescription.3

OUD used to be associated with poor, inner-city neighborhoods. Since the 1980s, however, the epidemic has infiltrated all strata of society, including suburbanites and the upper class. OUD now affects more Caucasians than any other race, with women comprising the fastest growing demographic afflicted. This may be because women might be more sensitive to pain than men, and thus more susceptible to cravings and relapse.4

Simply put: OUD is the deadliest drug crisis in American history,5 and it has only gotten worse since the onset of the COVID-19 global pandemic6: Opioid withdrawal-related emergencies and opioid-related deaths have increased since the SARS-CoV-2 virus erupted on the scene.7 Lockdown has pushed more people into isolation and toward addictive behavior, and the closure of treatment facilities and the interruption of care has pushed those with OUD to the point of crisis.8

A Slow and Steady Taper

A good night’s sleep after taking vitamin C was just the beginning of Lucy’s recovery: Within a week of starting the vitamin C regimen, she was off all street drugs, save for a single dose in the morning. “That morning dose was really hard to kick,” she explains, but within eight weeks she had successfully done so and has been entirely off of fentanyl ever since.

Fueled by her success in quitting fentanyl, Lucy continues taking vitamin C daily and working closely with her physician to steadily decrease her opioid usage. She has gradually dropped her iOAT dose of hydromorphone from 170 mL twice daily to 30 mL twice daily (the exact mg/mL potency of her preparation could not be confirmed). Her dose of morphine sulfate has likewise slid downward from 1,800 mg daily to now 30 mg daily—and she’s still lowering her doses.

She attributes her drop in opioid dependency entirely to vitamin C. “I wish I could give the whole world vitamin C, it just works so well,” she says, “I’m flabbergasted.”

Millar is pleased with Lucy’s progress as well, noting her absence of withdrawal symptoms despite the speediness of her taper. “And that’s using nothing but sodium ascorbate in the poorest costal code in Canada,” he says, pointing out that Lucy cannot afford to engage in psychotherapy, trigger avoidance, healthy eating, or other supportive services typically recommended to those battling substance use disorders.

But is Lucy’s steady improvement on account of the vitamin C?

“I honestly cannot say,” says her physician, who asked not to be named. The MD confirms that Lucy is, indeed, tapering down faster than is typically seen at the clinic. The doctor points out, however, that Lucy has had to increase her dosages a couple of times during periods of acute stress—like when the pandemic began and Lucy feared contracting the viral respiratory illness on top of her pre-existing asthma and chronic obstructive pulmonary disease (COPD). Nevertheless, Lucy says the nurses at her iOAT program “can’t believe I’ve pulled off the taper I have.”

Lucy has some ground to cover before she’s free of OUD. After several months of using vitamin C, she is still dependent upon opioids, albeit at much lower doses. Being spared withdrawal symptoms is not quite the same thing as overcoming a 25-year addiction or staying clean for the long haul, after all.

But even if Lucy never entirely stops using opioids, she has at least reeled in her drug use, saved taxpayers thousands of dollars, and significantly improved her quality of life since adding vitamin C into her treatment plan.

In addition to working with Lucy, Millar—who is also chair of the board for the Multidisciplinary Association for Psychedelic Studies (MAPS) Canada—has helped numerous other clients across North America successfully taper down their opioid use without having to suffer the horrific symptoms of opioid withdrawal. In fact, Millar says, “they feel pretty great.”

Millar pulls out his phone and reads me a text sent by a client less than one day after starting vitamin C: “Dude I made it longer today with less stuff than I can remember.” Millar explains that in fewer than three weeks this client dropped his daily buprenorphine (Subutex) use from 12 mg to 2 mg, without experiencing a single craving or side effect.

Millar also shares with me the success story of an Alaska couple who received his vitamin C protocol via e-mail: “Within three months they were both entirely off of all opioids and are still doing well.”

What the Research Shows

Millar and Lucy’s claims, as unusual as they may seem, are supported by research. The body of scientific evidence regarding vitamin C’s efficacy in dampening opioid addiction is compelling—though somewhat patchy.

Much of the peer-reviewed data comes from animal studies, which may or may not translate into outcomes in humans. Nevertheless, the findings are consistent: Vitamin C supplementation makes animals take fewer “hits” of morphine and clearly mitigates opioid tolerance and dependency.9,10,11,12 The vitamin has also been shown to reduce the number of opioid binding sites in the brains of guinea pigs.

Whereas most mammals synthesize vitamin C within their bodies, humans and other primates, bats, and guinea pigs are the exceptions to this rule. Vitamin C is thus an essential nutrient in humans—meaning we must take it in through the diet and/or supplements to ensure proper health, whether or not we suffer from substance use disorder.13

High doses of oral vitamin C have eased the symptoms of opiate withdrawal in at least a couple of human studies. A 2000 study by Evangelou et al,14 for example, found that supplementation with vitamins C and E reduced opioid withdrawal symptoms in 57% of patients—compared to just 7% of those in the placebo group. Another study by Newmeyer et al.15 found that just 1 to 3 grams of buffered vitamin C taken daily offset withdrawal symptoms for those in active detox as well as for those who had recently finished detoxing. The case reports of Schauss, Libby, and Stone (explained below) also support the case for using high dose vitamin C to abort opioid withdrawal symptoms.

I sent some of these studies over to Wesley Ryan, MD, a physician board-certified in both general and addiction psychiatry. “At first I thought it was probably ridiculous,” Ryan admits, “but after skimming the studies, it seems like there’s some real effect there.”

Erick Turner, MD, a psychiatrist with Oregon Health and Science University, however, is not so easily convinced. “On the face of it, it doesn’t seem biologically plausible,” Turner writes to me in an email. “How/why would vitamin C affect opioid receptors? Even if there were some plausible sounding mechanism, that’s no substitute for rigorous data.”

There’s no way around it: there aren’t many—or even any—double blind, placebo-controlled clinical trials published in peer-reviewed medical journals assessing vitamin C’s potential anti-addictive effect in humans.

There are, however, a number of studies and monographs in the literature postulating the mechanisms by which vitamin C may curb addiction. Many of these focus on vitamin C’s antioxidant properties.

Free radicals—and the subsequent oxidative stress they cause – have been implicated in a number of mental illnesses, including opioid addiction. Antioxidants like vitamin C, however, have been shown to prevent that damage, thus easing the symptoms of opioid withdrawal and supporting mental health.16,17,18

Vitamin C’s anti-inflammatory properties19 may further protect the brain and nervous system against injury and stress.20 The concentration of vitamin C (ascorbic acid) in the cerebrospinal fluid (CSF) that bathes the brain and spinal cord is two to four times higher than in the blood plasma.21

We now know that substance use disorders are incited and perpetuated at least in part by a dysfunctional response to stress.22 Vitamin C may help, as it is essential for healthy recovery after stress exposure, helping bring the body back to homeostasis after the cortisol rush that accompanies stress and pain.23,24

The vitamin also has merit as a treatment for depression and anxiety. This could be because vitamin C supports the production of the feel-good neurotransmitters serotonin and dopamine.25 (Dopamine is a particularly important chemical when it comes to addiction: We get addicted not merely to a substance itself, but to the dopamine hit that rewards us when we satisfy a craving.26) The vitamin has also been shown to protect the brain in neurodegenerative disorders like Alzheimer’s and Parkinson’s diseases.27

Vitamin C may also reduce opioid dependency by mitigating pain. Human studies have shown that giving vitamin C—in as low of a dose as 2 grams by mouth one hour before surgery—reduces the need for opioid analgesics post-op.28,29,30 Vitamin C also has positive effects on collagen synthesis and wound healing, making it of further value in surgical settings.31

Vitamin C interacts positively with harder-hitting pain medications like morphine, yielding additive pain-relieving effects and thus allowing for lower doses of narcotics (in mice).32 Considering that 75% of heroin users in treatment state that their opioid addiction began with a legal prescription33 and that those undergoing even minor surgery (including outpatient and elective procedures) are at increased risk of persistent opioid use,34 the potential positive impact of vitamin C is immense.

In addition, vitamin C supports the immune system and reduces the risk of infections.35,36 It has also been shown to shorten the duration of ICU stays and the need for ventilation,37 and is thus being investigated as a potential treatment for the serious complications of COVID-19. Considering that those with opioid addiction are at high risk for poor COVID-19 outcomes, vitamin C may serve a dual purpose for this population.38

These effects could be why Lucy tells me: “Vitamin C has saved me from a lot of pain and misery. I feel a lot better, a lot healthier in general.”

High Doses in Harlem: Alexander Schauss, PhD

While Millar supports clients in slowly and gradually tapering down their opioid use, Alexander Schauss, PhD, advocates for a bolder approach: taking mega-doses of vitamin C and quitting cold turkey.

Intrigued by a paper by Becket and Casey arguing that vitamin C occupies opioid receptor sites in the brain,39 Schauss conducted a study through the City University of New York in 1969. He instructed 20 study participants—all of whom were addicted to heroin and had unsuccessfully attempted cold turkey withdrawals prior to enrolling—to drink a mixture of diluted fruit juice and powdered sodium ascorbate throughout the day, for several days. Schauss reports that the cocktail aborted the signs and symptoms of opioid withdrawal in 100% of the participants.40 (The full details of Schauss’ dosing regimen, which includes dosages of 1 to 7.5 grams of sodium ascorbate taken every two hours, can be found in his 2012 paper in the Journal of Orthomolecular Medicine.)

Schauss tells me that his work caught the attention of two-time Nobel Laureate Linus Pauling, PhD, who developed a similar vitamin C protocol, to which he added niacin.

Schauss tells me that some of participants in his study started using heroin again after discontinuing the vitamin C supplementation. “There were all these fights on the street about the heroin being fake and not working,” he explains, “but the reason it wasn’t working was because these people were saturated in vitamin C, which was blocking the effects of the heroin.”

His observations were echoed in the later work of Drs. Alfred F. Libby and Irwin Stone,41 who, in their 1977 pilot study, supplemented heroin-addicted individuals with a whopping 25 to 85 grams of sodium ascorbate daily along with other nutrients in divided doses. (For comparison, most vitamin C supplements contain 0.5 gram per dose.) They report that 30 out of 30 (100%) of their patients were successfully treated with this regimen.

Like Schauss, Libby and Stone observed that heroin didn’t seem to have much of an effect in patients who first took mega doses of vitamin C. They write this of a 24-year-old patient: “On a Sunday he first took 45 g of sodium ascorbate and then in the space of five hours he ‘shot-up’ $300-$400 worth of heroin, and he felt no effect from this large amount of heroin.”

As compelling as these reports may seem, they are both old and anecdotal. Why haven’t there been more studies on vitamin C’s potential value in the treatment of opioid dependency since the 1970’s?

“One thing that comes to mind,” offers Ryan, “is that vitamin C has been around for a while. There’s not as much financial incentive for a pharmaceutical company to research it. So it falls on governmental funding to pay for this kind of research, and getting that funding is a really competitive process.”

In other words: Nobody stands to make money or look particularly flashy by conducting studies on a vitamin that is old, affordable, and widely available.

There’s also an elephant in the room here: bias. When I asked Schauss why his 1969 study wasn’t published until very recently, and why he didn’t follow it up with more studies, he said, “Anybody doing this type of nutritional research was categorically getting rejected by medical journals.” While thankfully most clinicians no longer believe that nutritional supplements just make expensive urine, allopathic medicine is still dismissive of orthomolecular therapies like vitamin C.

Current, Conventional Treatment of Opioid Use Disorder

“Nothing has been done for the addict in the 117 years since morphine was first introduced in the United States, except to substitute one addicting drug (like methadone) for another (like Heroin),” said Dr. Alfred F. Libby In 1977.42

Thankfully, much has been done to better support those with OUD since Libby’s time. We nevertheless have ways to go.

While opioid maintenance treatment can truly be helpful—over 100 randomized studies report benefits for those in treatment—the drugs used in the protocols are themselves opioids and thus come with the associated laundry list of serious and sometimes fatal side effects.43 Unlike vitamin C, methadone and buprenorphine—the pharmaceuticals often used in conventional OUD treatment—do not confer any known health-promoting benefits.

As useful as it may be, the duration of treatment with a replacement opioid is unclear, furthermore. “There’s research that suggests people who stay on suboxone longer have better outcomes,” says Ryan. He explains that while some people are able to eventually taper off of their opioid replacement medications, many stay on them indefinitely.

Although opioid maintenance therapy is a worthwhile investment from a societal standpoint – it is cheaper to treat somebody with addiction than it is to incarcerate them, for example – the financial cost is nevertheless considerable. According to drugabuse.gov, the cost of methadone treatment is $126.00 per week, the cost of buprenorphine for a stable patient is $115.00 per week, and the cost of naltrexone is $1,176.50 per month (pre-COVID-19 statistics).44 These medications must be administered by a licensed healthcare provider on a weekly or even daily basis.

Vitamin C, on the other hand, may be purchased over the counter at most pharmacies and supermarkets for a modest price. Lucy, for example, spends under $15 per week on sodium ascorbate.

Vitamin C mega-dosing is not without its risks, however. Although studies evaluating the claim that vitamin C causes kidney stones have yielded contradictory findings,45 one analysis46 reports an association between vitamin C intake and kidney stone risk in men – though not in women. The safety of vitamin C supplementation in the settings of hemochromatosis and other rare iron overload diseases is likewise a topic of debate.47,48

One Piece of the Puzzle

“Anything that can address withdrawal will help pull people in the right direction, but we can’t view that as the whole puzzle,” states Ryan.

Indeed, addiction is complicated and multi-factorial. No one agent can alone take the place of a multi-faceted treatment plan that includes counseling, exercise, rest, stress management, meaningful social connections, trauma integration, physical safety, and kinship with nature.

Nevertheless, medications and vitamins can have profound effects on the neurochemical aspects of addiction, and a substance that curbs opioid withdrawal symptoms can make or break a person’s attempts to get clean.

That’s why we need more clinical trials evaluating vitamin C’s potential in the treatment of opiate use disorder. Ryan agrees: “This topic strikes me as meriting more investigation, particularly since vitamin C is so benign.” But we both know that those trials are not likely to come any time soon, given the paucity of incentives for performing such research.

As a physician, I must weigh the risk-to-benefit of any treatment. When I consider the cost of opioid use disorder both to the individual and to society, along with the long list of vitamin C’s proven health benefits,49 sodium ascorbate strikes me as a rather low-stakes wager.

In the face of the opioid epidemic, which rages on with indiscriminate ferocity, I’m willing to take an educated guess and give vitamin C a chance.

Have you used vitamin C to treat addiction?

I am compiling data from real people on their experiences using vitamin C (and other remedies) to treat addiction. Have you (or a patient, or a loved one) tried using mega doses of vitamin C to treat a drug or alcohol use disorder? If so, please tell me about it at: www.SimbaHealth.com/surveys

Are you an addiction researcher?

As mentioned in the article above, we need more modern-day case reports and studies on vitamin C’s effects in those with opioid use disorder. I hope to address this gap in the research – and you can help. Please contact Research@SimbaHealth.com if you are willing to help fund research, if you are a researcher interested authoring (or co-authoring) a study, or if you can help in any other way.


References

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12. Khanna NC, Sharma SK. Megadoses of vitamin C prevent the development of tolerance and physical dependence on morphine in mice. Life Sci. 1983;33:401-4.↩︎

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16. Buettner GR. The pecking order of free radicals and antioxidants: lipid peroxidation, alpha-tocopherol, and ascorbate. Arch Biochem Biophys. 1993;300(2):535-43.↩︎

17. Mori T, Ito S, Matsubayashi K, Sawaguchi T. Comparison of nitric oxide synthase inhibitors, phospholipase A2 inhibitor and free radical scavengers as attenuators of opioid withdrawal syndrome. Behav Pharmacol. 2007 Dec;18(8):725-9.↩︎

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19. Mikirova N, et al. Effect of high-dose intravenous vitamin C on inflammation in cancer patients. J Transl Med. 2012;10:189.↩︎

20. Vogelzangs N, et al. Anxiety disorders and inflammation in a large adult cohort. Transl Psychiatry. 2013 Apr 23;3:e249.↩︎

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24. Hooper MH, Carr A, Marik PE. The adrenal-vitamin C axis: from fish to guinea pigs and primates. Crit Care. 2019;23:29.↩︎

25. Ward MS, et al. Behavioral and monoamine changes following severe vitamin C deficiency. J Neurochem. 2013;124(3):363-75.↩︎

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28. Kanazi GE, et al. Effect of vitamin C on morphine use after laparoscopic cholecystectomy: A randomized controlled trial. Can J Anesth. 2012;59(6):538-43.↩︎

29. Jeon Y, et al. Effect of intravenous high dose vitamin C on postoperative pain and morphine use after laparoscopic colectomy: a randomized controlled trial. Pain Res Manag. 2016;2016.↩︎

30. Ayatollahi V, et al. Effect of intravenous vitamin C on postoperative pain in uvulopala- topharyngoplasty with tonsillectomy. Clin Otolaryngol. 2017;42(1):139-43.↩︎

31. Ringsdorf WM, Cheraskin E. Vitamin C and human wound healing. Oral Surgery, Oral Med Oral Pathol. 1982;53(3):231-236.↩︎

32. Zeraati F, Araghchian M, Farjoo MH. Ascorbic acid interaction with analgesic effect of morphine and tramadol in mice. Anesthesiol Pain Med. 2014;4(3).↩︎

33. Cicero TJ, et al. The changing face of heroin use in the United States a retrospective analysis of the past 50 years. JAMA Psychiatry. 2014;71(7):821-6.↩︎

34. Brummett CM, Waljee JF, Goesling J, et al. New persistent opioid use after minor and major surgical procedures in us adults. JAMA Surg. 2017;152(6).↩︎

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36. Hemilä H. Vitamin C and infections. Nutrients. 2017 Mar 29;9(4):339.↩︎

37. Hemilä H, Chalker E. Vitamin C Can Shorten the Length of Stay in the ICU: A Meta-Analysis. Nutrients. 2019 Apr;11(4):708.↩︎

38. Dubey MJ, Ghosh R, Chatterjee S, Biswas P, Chatterjee S, Dubey S. COVID-19 and addiction. Diabetes Metab Syndr. Sep-Oct 2020;14(5):817-23.↩︎

39. Beckett AH, Casey AF. Synthetic analgesics: stereochemical considerations. J Pharm Pharmacol. 1954;6:986-1001.↩︎

40. Schauss AG. Attenuation of heroin withdrawal syndrome by the administration of high-dose vitamin C. J Orthomol Med. 2012;27(4);189-97↩︎

41. Libby AF, Stone I. The hypoascorbemia-kwashiorkor approach to drug addiction therapy: a pilot study. J. Orthomol Psychiatry. 1977;6:300-8.↩︎

42. Shwartz M. Vitamin C a new cure for drug addicts? Synapse – The UCSF Student Newspaper. 13 October 1977. https://synapse.library.ucsf.edu/?a=d&d=ucsf19771013-01.2.9&e=–––-en–20–1–txt–––txIN–↩︎

43. WHO Collaborative Research Project on Drug Dependence Treatment and HIV/AIDS. Accessed November 3, 2020. https://www.who.int/substance_abuse/activities/substituion_therapy_opioid_dependence_general_protocol%20_v2.pdf?ua=1↩︎

44. How much does opioid treatment cost? National Institutes of Health. June 2018. Accessed November 3, 2020. https://www.drugabuse.gov/publications/research-reports/medications-to-treat-opioid-addiction/how-much-does-opioid-treatment-cost↩︎

45. Traxer O, Pearle MS, Gattegno B, Thibault P. [Vitamin C and stone risk. Review of the literature]. Prog Urol. 2003 Dec;13(6):1290-4.↩︎

46. Ferraro PM, et al. Total, dietary, and supplemental vitamin C intake and risk of incident kidney stones. Am J Kidney Dis. 2016 Mar;67(3):400-7.↩︎

47. Gerster H. High-dose vitamin C: A risk for persons with high iron stores? Int J Vitam Nutr Res. 1999;69(2):67-82.↩︎

48. Bendich A, Langseth L. The health effects of vitamin C supplementation: a review. J Am Coll Nutr. 1995 Apr;14(2):124-36.↩︎

49. Vitamin C. Linus Pauling Institute, Micronutrient Information Center. Oregon State University. https://lpi.oregonstate.edu/mic/vitamins/vitamin-C↩︎

Author

  • Erica Zelfand, ND, is a licensed family physician specializing in functional medicine and integrative mental health. In addition to supporting patients with their physical wellbeing, Erica facilitates psycho-spiritual experiences for individuals and groups across the globe. She regularly lectures on entheogenic science and trains aspiring psychedelic therapists in person and through her online CME-approved course, ScienceOfPsychedelics.com. When she isn’t trying to save the world, Erica can be found forest bathing, eating chocolate, and initiating group hugs (all of which, she would argue, may also help save the world). To learn more and connect, visit DrZelfand.com.

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