Tacrolimus drug by Ray Sahelian, M.D. Tacrolimus side effects - Brand name Prograf for oral version

Tacrolimus is an immunosuppressive drug that has been used widely in organ transplantation and topically for atopic dermatitis. Tacrolimus exerts its immunosuppressive effects by the inhibition of calcineurin, leading to interference with T-cell activation. As T-cell activation plays a major role in the pathogenesis of rheumatoid arthritis, there has been an interest in the use of tacrolimus for the treatment of rheumatoid arthritis. The pharmacological properties of tacrolimus have the potential of suppressing the production of inflammatory cytokines, improvement of joint inflammation, improvement of bone and cartilage destruction, improvement of functional status and relief from arthritic pain. There are natural options to the treatment of rheumatoid arthritis.

Tacrolimus for liver transplant
Tacrolimus is used to prevent rejection of liver transplants. Sometimes it is used to prevent rejection of other types of organ transplants.

Tacrolimus for Lichen Sclerosus
Topical tacrolimus may be helpful in the management of lichen sclerosus. The effective management of vulval lichen sclerosus currently depends upon the use of topical steroids and emollients. There are concerns with regard to the long-term toxicity of potent steroids and therefore is a need to consider effective alternatives. Immunomodulatory macrolactams offer an alternative to steroids in the management of some other inflammatory skin disorders and it would seem reasonable therefore to assess their activity in lichen sclerosus. A pilot study of 16 histologically confirmed cases of lichen sclerosus suggests that macrolactams have a positive pharmacological effect.

PROTOPIC (tacrolimus) Ointment contains tacrolimus, a macrolide immunosuppressant produced by Streptomyces tsukubaensis. It is for topical dermatologic use only.

Tacrolimus for skin conditions

Tacrolimus is an immunosuppressant that acts by inhibiting T-cell activation and cytokine release. Tacrolimus is approved for the treatment of atopic dermatitis. Since its introduction, anecdotal reports and case series have found topical tacrolimus to perhaps be useful in patients with a variety of other skin disorders, including other types of eczema, papulosquamous disorders, disorders of cornification, rosacea, other inflammatory skin conditions, vesiculobullous diseases, vitiligo, connective-tissue diseases, graft-versus-host disease, and follicular disorders. However, more research is needed to determine the long term safety and side effects.
     Topical tacrolimus seems to be a therapeutic alternative for resistant skin lesions of dermatomyositis.

Tacrolimus side effects used topically - Tacrolimus is sold as Protopic ointment

Topical tacrolimus ointment was approved for the treatment of atopic dermatitis in Japan in 1999, the United States in 2000, and Europe in 2001. Pimecrolimus and tacrolimus are two topical calcineurin inhibitors used in pediatric patients with atopic dermatitis. Tacrolimus side effects include infections, pyrexia, burning, pruritus, erythema, and papules in the application area. In suckling babies tacrolimus side effects include dry skin, pruritus, infections, constipation, erythema, and papules.

Tacrolimus side effects used orally
Common tacrolimus side effects include upset stomach, stomach discomfort, diarrhea, vomiting, insomnia and loss of appetite.

Tacrolimus for Lichen Sclerosus
Multicentre, phase II trial on the safety and efficacy of topical tacrolimus ointment for the treatment of lichen sclerosus.
Br J Dermatol. 2006 Nov;155(5):1021-8. Department of Andrology and Venereology, Philipps-University Marburg, Marburg, Germany.
Lichen sclerosus is a chronic inflammatory autoimmune disease causing significant sclerosis, atrophy and pruritus. Treatment remains unsatisfactory, with potent corticosteroids being the most effective therapy. We conducted a multicentre, phase II trial to assess the safety and efficacy of tacrolimus ointment 0.1% for the treatment of lichen sclerosus with a follow-up period of 18 months at 10 university and teaching hospitals in Germany and Austria. Methods Eighty-four patients (49 women, 32 men and three girls) aged between 5 and 85 years with long-standing, active lichen sclerosus (79 with anogenital and five with extragenital localization) were treated with topical tacrolimus ointment 0.1% twice daily for 16 weeks. Results: The primary endpoint (clearance of active lichen sclerosus) was reached by 43% of patients at 24 weeks of treatment. Partial resolution was reached in 34% of patients. Maximal effects occurred between week 10 and 24 of therapy. Tacrolimus reatment led to a significant reduction of the total lesional area and to a significant decline in the total symptom score. Symptoms (e.g. itching) and findings (erythema, erosions and induration) showed significant improvement. No serious tacrolimus side effects were observed. There were three (9%) recurrences during the follow-up period. Conclusions Topical tacrolimus ointment 0.1% was safe and effective for the treatment of long-standing active lichen sclerosus.

Topical Tacrolimus for Nickel Allergy

Protopic, also known as tacrolimus 0.1 percent ointment, suppresses the signs and symptoms of skin allergy resulting in contact dermatitis among individuals who are sensitive to nickel and who continue to be exposed to this metal. Allergic contact dermatitis -- characterized by inflammation, rash, itching and blistering -- is one of the most common occupationally related conditions in the United States, costing an estimated $1 billion annually due to lost work, reduced productivity, medical care and disability payments. Nickel induces allergic reactions in roughly 5.8 percent of the U.S. population, making it an appropriate model for studying allergic contact dermatitis.

Tacrolimus for Kidney Transplantation

Tacrolimus is superior to cyclosporin in improving graft survival and preventing acute rejection after kidney transplantation, but increases post-transplant diabetes, neurological and gastrointestinal side effects.