The Codeine Controversy – How Safe and Effective is Tylenol® #1 Compared to Other Over-The-Counter Products?

Ethos Ho, BSc Pharm Candidate

A Painful Dilemma

Are you experiencing pain that just won’t go away despite taking medications like Tylenol^® or Advil^®? Perhaps a headache, migraine, swollen joint, or an aching muscle is keeping you up at night, or preventing you from participating in your daily activities.  You may be thinking about using something with a little extra “kick” than your typical medications, and maybe you’ve heard about over-the-counter Tylenol^® #1, also known as acetaminophen with codeine. Would this convenient, non-prescription medication provide the relief that you need? How effective is it compared to regular pain medications?

What is Tylenol® #1?

Tylenol^® #1’s, commonly known as “number ones” or simply “T1’s,” is a combination product containing acetaminophen, caffeine, and codeine that’s intended for mild to moderate pain. Note that generic versions of this product also exist, which do not carry the brand name Tylenol® but contain the same ingredients in the same amounts.¹

The signature ingredient in all regular Tylenol® is acetaminophen, which belongs to a family of medications known as analgesics which reduce pain. Therefore, the main difference in T1’s are the other two ingredients:¹

• Caffeine: used to increase the effects of acetaminophen
• Codeine: for added pain control

Together, these ingredients have something called synergy, which means that when taken together, they have a higher effect than when taken separately.

This may sound great at first, but in reality, the addition of codeine introduces an added risk of side effects and other complications, that can far outweigh the benefits of T1’s.

The Risks of Opioid Medications

Codeine belongs to a family of medications called opioids, which includes morphine, oxycodone, and many other medications used for moderate to severe pain. Side effects of opioids can range from minor inconveniences like constipation and dizziness to more severe issues like drowsiness, unconsciousness, and potentially coma. At extremely high doses, opiate toxicity can occur in the form of respiratory depression, where the body’s breathing rate becomes especially low – this can be life-threatening. When misused, opioids also have the potential to cause dependence, and possibly even addiction.²

Codeine is often used because it’s seen as a weaker opioid, and thus, safer to use. However, it’s important to know that the body metabolizes codeine into morphine, which is actually responsible for its effect. The problem lies in that not everybody metabolizes codeine the same. The majority of us are “slow metabolizers,” where we only convert roughly 10% of codeine into morphine. However, a small part of the population are “fast metabolizers,” who generate much greater amounts of morphine from the same dose of codeine.²

Fast metabolizers are at added risk of side effects and toxicity of opioids. In 2006, one case was published where a breastfeeding infant died from morphine poisoning: the mother was unknowingly a fast metabolizer of codeine and was transferring high doses of medication through breast milk.³ This is only one case, but the risk is still very real, as there is no practical way test if someone is a fast metabolizer of codeine.

Are the Benefits Worth the Risks?

All the risks aside, is there any benefit at all to using over-the-counter codeine products? Numerous studies have compared the effectiveness of regular pain medications against different strengths of codeine. So far, the results have been consistent: regular ibuprofen (Advil^®, Motrin^®)  is just as effective as acetaminophen with codeine in providing pain relief. This includes pain following childbirth, surgery, headache, osteoarthritis, and post-traumatic pain.^4-7

It’s important to mention that most of these studies used prescription strength codeine products, which contain about twice the amount that’s found in non-prescription acetaminophen and codeine – and regular analgesics still performed just as good. Also, regular analgesics had fewer side effects and constipation.

The Bottom Line

In short, there is no added benefit from using non-prescription acetaminophen and codeine products, but there are greater side effects – this means that T1’s are actually the least attractive option when choosing non-prescription analgesics. Instead, Advil^® (Ibuprofen), Tylenol^® (Acetaminophen), and Aleve^® (Naproxen) should always be considered first for pain management, as they provide the same or better benefit, with fewer risks.

This is not to say that codeine and opiates have no place in pain management. That being said, you should always consult a healthcare provider if you have any questions or concerns or what medications are best for you.

We hope that you were able to take away some tips to manage your pain in this article. Questions or concerns? Reach out to us over Instagram, Facebook, or at ask@orbishealth.ca.  

RESOURCES

1. Lexicomp
2. Dynamed
3. Madadi, P., Koren, G., Cairns, J., Chitayat, D., Gaedigk, A., Leeder, J. S., … Aleksa, K. (2007). Safety of codeine during breastfeeding: Fatal morphine poisoning in the breastfed neonate of a mother prescribed codeine. Canadian Family Physician, 53(1), 33–35.
4. Peter, E. A., Janssen, P. A., Grange, C. S., & Douglas, M. J. (2001). Ibuprofen versus acetaminophen with codeine for the relief of perineal pain after childbirth: a randomized controlled trial. CMAJ: Canadian Medical Association Journal, 165(9), 1203–1209.
5. Friday, J., Kanegaye, J., McCaslin, I., Zheng, A., & Harley, J. (2009). Ibuprofen Provides Analgesia Equivalent to Acetaminophen-Codeine in the Treatment of Acute Pain in Children with Extremity Injuries: A Randomized Clinical Trial. Academic Emergency Medicine, 16(8), 711-716. http://dx.doi.org/10.1111/j.1553-2712.2009.00471.x
6. Chen, T., Adamson, P.A. (2009). Comparison of Ibuprofen and Acetaminophen with Codeine Following Cosmetic Facial Surgery. Journal of Otolaryngology — Head & Neck Surgery, 38(5), 580-586.
7. Nauta, M., Landsmeer, M., & Koren, G. (2009). Codeine-acetaminophen versus nonsteroidal anti-inflammatory drugs in the treatment of post–abdominal surgery pain: a systematic review of randomized trials. The American Journal Of Surgery, 198(2), 256-261. http://dx.doi.org/10.1016/j.amjsurg.2008.11.044