What is the Difference Between Cyclosporine and Tacrolimus

The main difference between cyclosporine and tacrolimus is that cyclosporine is more cost-effective as the primary prevention of graft rejection, whereas tacrolimus is effective and safe as an immunosuppressant. 

Generally, cyclosporine and tacrolimus are two calcineurin inhibitors. They are immunosuppressants necessary in the management of autoimmune conditions and in solid organ transplants.   

Key Areas Covered

1. What is Cyclosporine
– Definition, Facts, Importance
2. What is Tacrolimus
– Definition, Facts, Importance
3. Similarities Between Cyclosporine and Tacrolimus
– Outline of Common Features
4. Difference Between Cyclosporine and Tacrolimus
– Comparison of Key Differences

Key Terms 

Cyclosporine, Chlorophyta

What is Cyclosporine

Cyclosporine is an immunosuppressant essential to treat the rejection of the organ. It is vital in kidney, liver, and heart transplantation. It serves as an adjuvant to glucocorticoids in treating allogenic post-organ transplant rejection. Also, it is an approved drug by FDA. Modified formulations of cyclosporine with FDA approval are there too. They treat severe and active rheumatoid arthritis when the patient does not respond to methotrexate. It can be combined with methotrexate during the treatment of rheumatoid arthritis.

Figure 1: Cyclosporine

Furthermore, other cyclosporine modifications are important in treating adults with severe and recalcitrant plaque psoriasis when systemic therapy such as retinoids, PUVA, or methotrexate are failed to respond. Also, the FDA has approved an ophthalmic formulation of cyclosporine to increase tear production in patients with keratoconjunctivitis sicca due to ocular inflammation. It is used for vernal keratoconjunctivitis. Additionally, non-FDA-approved treatments are for allergic conjunctivitis, interstitial cystitis, chronic urticaria, alopecia, and aplastic anemia. Further, cyclosporine is important in treating ulcerative colitis, Sjogren disease, and systemic lupus erythematosus.

What is Tacrolimus

Tacrolimus is another medication in the treatment of solid organ transplant rejection. It is a drug in the calcineurin inhibitors. It is used to treat organ transplant rejection of the heart, kidney, and liver. Moreover, it is also given to lung-transplanted patients. Other conditions that use tacrolimus include Crohn’s disease, graft-versus-host disease, myasthenia gravis, and rheumatoid arthritis. Further, the oral formulation of tacrolimus is approved by the FDA, along with azathioprine and mycophenolate mofetil, in patients who have undergone kidney, heart, and liver transplants. The IV formulation of tacrolimus is there for patients that cannot take drugs orally.

Figure 2: Tacrolimus

Moreover, tacrolimus comes in two forms: 0.03% for children (2 to 15 years) and 0.1% for adults. Tacrolimus is approved as the second-line treatment in moderate to severe atopic dermatitis in children not responsive to other topical treatments. Also, tacrolimus is a prophylactic agent to prevent graft-vs-host disease and the transplant rejection of pancreatic, corneal, renal, and small intestines.

Similarities Between Cyclosporine and Tacrolimus

• Cyclosporine and tacrolimus are two calcineurin inhibitors.
• They are immunosuppressants important in managing autoimmune conditions and solid organ transplants.
• They are the principal drugs for immunosuppression in solid organ transplantation.
• They inhibit phosphatase.  

Difference Between Cyclosporine and Tacrolimus

Definition

Cyclosporine is an immunosuppressant used to prevent the rejection of grafts and transplants. In contrast, tacrolimus is a calcineurin inhibitor that prevents organ transplant rejection and treats moderate to severe atopic dermatitis.

Structure 

Cyclosporine is a cyclic decapeptide, while tacrolimus is a macrocyclic lactone. 

Significance

Cyclosporine is more cost-effective as the primary prevention of graft rejection, while tacrolimus is effective and safe as an immunosuppressant. 

Adverse Effects

Cyclosporine increases the risk of hypertension and the levels of LDL, while tacrolimus increases posttransplant diabetes and neurologic toxicity.

Conclusion

In brief, cyclosporine and tacrolimus are two immunosuppressant drugs important in treating autoimmune diseases and solid organ transplantation. Cyclosporine is a cyclic decapeptide, and it is cost-effective. Therefore, it is important for the primary prevention of graft rejection. However, it increases the risk of hypertension and LDL levels. In comparison, tacrolimus is a macrocyclic lactone that is more effective and safer as an immunosuppressant. However, it increases posttransplant diabetes and neurologic toxicity. 

References:

1. Tapia C, Nessel TA, Zito PM. Cyclosporine. [Updated 2023 Mar 7]. In: StatPearls [Internet]. Treasure Island (FL): StatPearls Publishing; 2023 Jan-.
2. Araya AA, Tasnif Y. Tacrolimus. [Updated 2023 May 29]. In: StatPearls [Internet]. Treasure Island (FL): StatPearls Publishing; 2023 Jan-.

Image Courtesy:

1. “Ciclosporin” By Yikrazuul – Own work (Public Domain) via Commons Wikimedia
2. “Tacrolimus2DCSD.” By Fuse809 – Own Work (Public Domain) via Commons Wikimedia