The key difference between cyclosporine and tacrolimus is that cyclosporine is a cyclic endecapeptide in its chemical structure, while tacrolimus is a macrocyclic lactone in its chemical structure.
Cyclosporine and tacrolimus are the two main types of calcineurin inhibitors. Calcineurin inhibitors are immunosuppressants used to control autoimmune conditions. They differ in their chemical structure, but both act in a similar manner. Their mechanism of action involves the inhibition of phosphatase. Cyclosporine and tacrolimus are cornerstone immunosuppressive agents administered to solid organ transplant recipients or patients in order to prevent allograft rejection.
CONTENTS
1. Overview and Key Difference
2. What is Cyclosporine
3. What is Tacrolimus
4. Similarities – Cyclosporine and Tacrolimus
5. Cyclosporine vs Tacrolimus in Tabular Form
6. Summary – Cyclosporine vs Tacrolimus
What is Cyclosporine?
Cyclosporine is a calcineurin inhibitor. It is a cyclic endecapeptide in its chemical structure. It is an immunosuppressant used to manage autoimmune conditions that were discovered in 1971. Cyclosporine was the most successful antirejection drug discovered to date. This is because it has radically improved the chance of survival for transplant recipients. Other than solid organ transplantation, it can also be prescribed for liver, intestinal, lung, and heart transplant recipients and to manage severe autoimmune conditions such as atopic dermatitis and rheumatoid arthritis.
Figure 01: Cyclosporine
Cyclosporine is a natural product produced from the fungus Tolypocladium inflatum. Normally, it is taken intravenously for rheumatoid arthritis, psoriasis, Crohn’s disease, nephritic syndrome, and in organ transplantation. Moreover, it can also be used as an eye drop for keratoconjunctivitis sicca (dry eyes). The common side effects include high blood pressure, headache, kidney problems, increased hair growth, and vomiting. The severe side effects may include an increased risk of infection, liver problems, and an increased risk of lymphoma. In addition, usage of this drug during pregnancy may cause preterm birth, but it does not appear to cause any birth defects. Furthermore, it is also on the World Health organization’s List of Essential Medicines.
What is Tacrolimus?
Tacrolimus is an immunosuppressive drug sold under the brand name Prograf. It is mainly used for allogeneic organ transplants to prevent rejection. Tacrolimus can also be used as a topical medication in order to treat T-cell-mediated diseases like eczema and psoriasis. Other than that, it is also prescribed to treat severe refractory uveitis after bone marrow transplant, exacerbations of minimal change disease, Kimura’s disease, vitiligo, and dry eye syndrome in cats and dogs.
Figure 02: Tacrolimus
In its function, this drug inhibits calcineurin, which is involved in the production of interleukin-2. Interleukin-2 is important in the development and proliferation of T cells, which are the main agents of autoimmune conditions. Tacrolimus was discovered in 1987 from the fermentation broth of a Japanese soil sample that contained Streptomyces tsukubensis bacterium. The common side effects may include headache, diarrhoea, nausea/vomiting, upset stomach, loss of appetite, trouble sleeping, and numbness of hands and feet. The more serious side effects may include mood changes, dizziness, kidney problems, pounding heartbeat, heart failure, swelling of ankles/feet, unusual tiredness, unusual weight gain, hearing problems, pain, redness and swelling of arms or legs, easy bruising, muscle cramps or weakness, yellowing of skin, eyes, dark urine, severe stomach/abdominal pain severe leg pain, brain infection, clumsiness, loss of coordination, sudden changes of thinking, difficulty moving the muscles, problems with speech, seizure and vision changes. Furthermore, tacrolimus is also present on the World Health organization’s List of Essential Medicines.
What are the Similarities Between Cyclosporine and Tacrolimus?
- Cyclosporine and tacrolimus are two main types of calcineurin inhibitors and are immunosuppressants used to control autoimmune conditions.
- Both drugs work by decreasing the function of lymphocytes by blocking the phosphatase activity of calcineurin, which in turn decreases the production of inflammatory cytokines.
- Both drugs are natural products.
- They are on the World Health organization’s List of Essential Medicines.
- Both drugs have common and serious drug effects.
What is the Difference Between Cyclosporine and Tacrolimus?
Cyclosporine is a cyclic endecapeptide in its chemical structure, while tacrolimus is a macrocyclic lactone in its chemical structure. Thus, this is the key difference between cyclosporine and tacrolimus. Furthermore, cyclosporine was discovered in 1971 and produced from the fungus Tolypocladium inflatum. On the other hand, tacrolimus was discovered in 1987 and produced from the fermentation broth of a Japanese soil sample that contained the Streptomyces tsukubensis bacterium.
The below infographic presents the differences between cyclosporine and tacrolimus in tabular form for side-by-side comparison.
Summary – Cyclosporine vs Tacrolimus
Cyclosporine and tacrolimus are the two main calcineurin inhibitors and immunosuppressants used to control autoimmune conditions. They are mainly administered to solid organ transplant recipients or patients in order to prevent allograft rejection. However, cyclosporine is a cyclic endecapeptide in its chemical structure, while tacrolimus is a macrocyclic lactone in its chemical structure. So, this summarizes the difference between cyclosporine and tacrolimus.
Reference:
1. Barbarino, Julia M, et al. “PharmGKB Summary: Cyclosporine and Tacrolimus Pathways.” Pharmacogenetics and Genomics, U.S. National Library of Medicine, Oct. 2013.
2. “Tacrolimus Oral: Uses, Side Effects, Interactions, Pictures, Warnings & Dosing.” WebMD.
Image Courtesy:
1. “Cyclosporine 3D” By Ph.David – Own work (CC BY-SA 3.0) via Commons Wikimedia
2. “Tacrolimus-2D-skeletal” By Fuzzform (talk) – English Wikipedia (CC BY-SA 3.0) via Commons Wikimedia