Earlier this year, the pharmaceutical giant AbbVie announced some news that made patients feel relief and anticipation: a citrate-free version of Humira (adalimumab), its widely used biologic drug, would soon be available.
Humira and other similar drugs can be life-changing for patients who take them to manage such chronic inflammatory diseases as rheumatoid arthritis, Crohn’s disease, or psoriasis. An immunosuppressive biologic, Humira binds to a protein called tumor necrosis factor (TNF) that contributes to over-activation of the immune system and inflammation. People with autoimmune inflammatory disease produce too much TNF, so taking drugs in this class (called TNF blockers) can help stop inflammation and even disease progression.
But even though Humira, which was first FDA-approved in 2002 for treating rheumatoid arthritis, can provide significant symptom relief, many patients who take it complain that it burns upon injection. In some cases, very badly.
“The feeling when the medication entered my body was like nothing I had ever felt before,” wrote Crohn’s disease patient Natalie Hayden on her blog Lights Camera Crohn’s. “It was an unthinkable amount of pain. It was overwhelming knowing that for the rest of my life, I would endure this same pain, multiple times a month.”
The citrate-free version of Humira is still rolling out. If you haven’t heard about it or spoken with your doctor about it yet, here’s what you need to know.
What is citrate?
Citrate is a buffer, or a chemical that’s used to help maintain the stability of medications, explains James Wu, PharmD, a pharmacist and manager of a Walgreens community pharmacy in Chicago. “It’s commonly found in injectable medications such as Humira to help it keep its chemical and physical properties,” he says. Changes in pH can adversely affect the proteins used in biologic medications.
What about the new formulation is better for patients?
Citrate-free Humira uses a different buffer to help stabilize and preserve the drug, and this buffer doesn’t cause the same burning and pain that patients commonly report experiencing, says Doug Roberts, MD, a rheumatologist in Sacramento. The pen has a smaller needle (29 gauge versus 27 gauge) and contains 50 percent less volume (but the amount of medication is the same). So you’re injecting less fluid to begin with, the needle is smaller, and the fluid is less painful.
How does citrate-free Humira compare with the formulations of other TNF blockers?
All biologic drugs need buffers to help stabilize and preserve their chemical makeup. “Most contain some form of buffer that can create some burning,” says rheumatologist Vinicius Domingues, MD, CreakyJoints medical advisor. “However others, including Enbrel (etanercept), Cimzia (certolizumab pegol), and Simponi (golimumab), have also made modifications in their formulas.”
What else do patients need to know about the citrate-free version of Humira?
The drug is administered the exact same way as the original version. The only other thing to know is that the packaging looks slightly different. As circled in the photo above, the numbers on the caps are now white. There’s a larger viewing window on the pen. And the drug comes in a blue box instead of a red one.
What does it feel like to use the citrate-free Humira?
CreakyJoints community member Eddie Applegate, from the Atlanta area, learned about citrate-free Humira at his last rheumatologist visit, a usual check-up for his psoriatic arthritis. “The burning sensation [on Humira] is something I have experienced, but I’ve heard and read from others how much worse it was for them,” he says. Due for a drug refill anyway, he decided to try the new formulation.
Applegate had to call his specialty pharmacy to change the prescription instead of scheduling delivery online as he usually does.
His first injection, which he administered last week, went off without a hitch. “I did not experience any burning. The claims online were not overstated,” he says. “I hope this allays any fears or worries from other Humira patients.”
For her part, Natalie Hayden says it was difficult to fathom the impact of switching to the citrate-free version. But she knew right away the new version made a huge difference.
“I’m here to tell you it’s completely painless. Less pain than a blood draw. Less than a flu shot. You feel nothing,” she wrote on her blog. “It’s emotional and overwhelming in the best way. I cried for a good half hour after my first one, happy tears. Tears of joy from a woman who now knows her children will never see their mom struggle in pain. Tears of joy from someone who is eternally grateful for a medication that keeps a painful and debilitating chronic illness at bay. Tears of joy knowing that I will never have to feel that awful pain again. A pain that’s too much to put into words, that was part of my life for so long.”
Keep Reading
- 50+ Arthritis Research Updates Patients Need to Know About
- Is It Safe to Taper Biologics in Rheumatoid Arthritis Once You Achieve Low Disease Activity?
- The 4 Factors that Affect Whether or Not You Hit Remission in RA
My son was tortured for the last year of taking Humira. We had his first citrate free injection last week and he was so excited. Couldn’t believe it. He said he felt nothing!! I’m glad they finally decided to remove the preservative. So excited my son gets to feel better and not have complete anxiety about taking his meds.
The new citrate free pen is where it’s at!!! Absolutely love it. No pain AT ALL!
I’m glad the new formulation of Humira is helping patients, but it should be noted here that it is also less costly to manufacture, and the drug company is still charging patients the same amount. So for patients such as myself, who experience little to no pain from the original version, please consider avoiding this switch…. because why should they benefit off of us any further than they already are?
It’s all about the Benjamins…
Humira was the best biologic for my RA, but it gave me psoriasis,pustular. I was hoping it was the citrate so I could take it again. No pain, just blisters.
Actemra is not stopping progression of my RA. I inject 4x a month. I’m miserable.
I was on the citrate free version in UK and am now back to the old citrate formula because we moved to Australia. It all seems 10 years behind and I can’t wait for it to catch up. I still disagree with lights camera crohns in that yea it’s a bit painful but come on its way less painful than a year long flare or surgery. I’m just glad kids don’t have to suffer the stinging of the liquid going in any more.
I absolutely hated taking my shots, I would constantly push it off till the very end of the day or sometimes not do it at all and just say “ill do it tomorrow” well tomorrow would come and I still wouldn’t do my shot. Last night I went and opened up the package and noticed a difference, the packaging looked more up to date with times. I proceeded to prepare myself to do my shot and I did it… I felt no pain whatsoever and immediately knew somethings had changed. I am very glad that they decided to make the switch, the side effects of Citrate are just as bad as having Crohn’s Disease.
My husband had same issues.
He is on cosentyx now 1x mo 2– 150 ml injections
Blisters gone
The old Humira pain was unbearable for me. Had to have someone else give me the injections.
I can’t believe it I did my second shot without the citratre. Can’t feel any psin hsve been on Humira sbout 3 years dreaded every time I had to do the shot. Thank you so much I sm 71 and so hsppy now.
not feel same more weak and tire, with the new humira citrate free want to know if somebody feel the same . humor user for the last 11 years
Yes, my doctor switched me to the citrate free HUMIRA and it’s been about 3 months and it doesn’t work as well for me as the old formula. Weak, tired and my joint pain is mild but coming back and getting worse.
Not only was I in remission but I felt the best I had ever felt since I got Crohn’s 2 1/2 years ago. Until I started taking the new formula……It might be a coincidence, So I had some blood work done I’m waiting for the results of the blood test
You are not alone, I was feeling the best I had felt since I was diagnosed with Crohn’s 2 1/2 years ago but when I started taking the new formula I went downhill fast
I, just like Miguel am not feeling as good as I felt with the original Humira.. I obviously appreciate less pain with the injection but I will take that to feel better.. I am thinking about going back to the original formula.
I just switched to citrate and I have been in pain and feeling terrible every since. I’m going back to the other