Drug Eruption and Interactions - PHARMACEUTICAL REVIEW

TACROLIMUS
Synonym: FK506
Trade names: Prograf (Astellas); Protopic (Astellas)
Indications: Prophylaxis of organ rejection, atopic dermatitis
(topical)
Category: Calcineurin inhibitor; Immunosuppressant;
Macrolactam
Half-life: ~8.7 hours
Clinically important, potentially hazardous interactions
with: amiodarone, beta-blockers, caspofungin, cyclosporine,
dairy products, danazol, erythromycin, etoricoxib, grapefruit
juice, hemophilus B vaccine, HMG-CoA reductase inhibitors,
ibuprofen, immunosuppressants, ketoconazole, lovastatin,
mycophenolate, peanuts, potassium, potassium-sparing diuretics,
rifabutin, rifampin, rifapentine, simvastatin, St John’s wort,
telithromycin, vaccines
Reactions
Skin
Angioedema
(2003): Lykavieris P+, Transplantation 75(1), 152
Burning (46%)
(2005): Ashcroft DM+, BMJ 330(7490), 516
(2005): Hanifin JM+, JAmAcadDermatol53(2 Suppl 2), S186
(2005): Harper J+, J Invest Dermatol 124(4), 695
(2004): Lampropoulos CE+, Rheumatology (Oxford)
43(11), 1383
(2004): Pascual JC+, Skin Therapy Lett 9(9), 1
(2002): Rozycki TW+, JAmAcadDermatol46, 27
(2002): Russell JJ, Am Fam Physician 66(10), 1899
(2001): Goldman D, JAmAcadDermatol44, 995 (transient,
localized)
(2000): Reitamo S+, Arch Dermatol 136, 999 (46.8%)
(1999): Ruzicka R+, Arch Dermatol 135, 574
(1998): Alaiti S+, JAmAcadDermatol38, 69
Dermatitis
(2007): Shaw DW+, JAmAcadDermatol56(2), 342
Diaphoresis (>3%)
Edema (>10%)
Erythema (12%)
(2005): Hanifin JM+, JAmAcadDermatol53(2 Suppl 2), S186
(2001): Bohannon JS, Midlothian, VA (facial) (from topical)
(following wine) (from Internet) (observation)
(2000): Reitamo S+, Arch Dermatol 136, 999 (12.3%)
Exanthems (4%)
(2001): Takamatsu Y+, Bone Marrow Transplant 28(4), 421 (with
cyclosporine)
(2000): Reitamo S+, Arch Dermatol 136, 999 (4.1%)
Exfoliative dermatitis
(2004): Lampropoulos CE+, Rheumatology (Oxford)
43(11), 1383
Folliculitis (10%)
(2006): Singalavanija S+, J Med Assoc Thai 89(11), 1915 (2%)
(2000): Reitamo S+, Arch Dermatol 136, 999 (10.8%)
Graft-versus-host reaction
(2004): Tamaki H+, Int J Hematol 80(3), 291
(2003): Bunetel L+, JPeriodontol74(4), 552
Herpes simplex (13%)
(2005): Joseph MA+, Cornea 24(4), 417
(2005): Lonsdale-Eccles AA+, Clin Exp Dermatol 30(1), 95
(vulva)
(2004): Furue M+, JDermatol31(4), 277
(2000): Reitamo S+, Arch Dermatol 136, 999 (13%)
Irritation
TACROLIMUS 519
(2002): Rozycki TW+, JAmAcadDermatol46(1), 27
Kaposi’s sarcoma
(2006): Chua R+, Heart Lung Circ 15(5), 340
(2006): Schmutz JL+, Ann Dermatol Venereol 133(3), 303 (from
topical)
Kaposi’s varicelliform eruption
(2004): Miyake-Kashima M+, Cornea 23(2), 190
Lentigo
(2005): Hickey JR+, Br J Dermatol 152(1), 152
Melanoma
(2005): Hickey JR+, Br J Dermatol 152(1), 152 (3 cases)
Molluscum contagiosum
(2004): Wilson LM+, Australas J Dermatol 45(3), 184
Nevi
(1999): Reed BR, Denver, CO (from Internet) (observation)
Peripheral edema (26%)
Photosensitivity (>3%)
Pigmentation
(2002): Phillips R, Melbourne, Australia (from Internet)
(observation)
Pruritus (25–36%)
(2005): Hanifin JM+, JAmAcadDermatol53(2 Suppl 2), S186
(2004): Pascual JC+, Skin Therapy Lett 9(9), 1
(2002): Russell JJ, Am Fam Physician 66(10), 1899
(2000): Emre S+, Transpl Int 13, 73
(2000): Reitamo S+, Arch Dermatol 136, 999 (25.3%)
Purpura
(1996): Nash RA+, Blood 88, 3634
Pustules (6%)
(2000): Reitamo S+, Arch Dermatol 136, 999 (6.3%)
Rash (sic) (24%)
Rosacea
(2004): Antille C+, Arch Dermatol 140(4), 457
(2003): Bernard LA+, Arch Dermatol 139(2), 229
(granulomatous)
Squamous cell carcinoma
(2001): Otley CC+, Arch Dermatol 137, 459
Urticaria
(2001): Takamatsu Y+, Bone Marrow Transplant 28(4), 421 (with
cyclosporine)
Mucosal
Gingival hyperplasia/hypertrophy
(2006): de Oliveira Costa F+, JPeriodontol77(6), 969
(2000): Schmutz J+, Ann Dermatol Venereol (French) 127, 646
(1998): Basile C+, NephrolDialTransplant13, 2980
Oral candidiasis (>3%)
Oral pigmentation
(2005): Fricain JC+, Dermatology 210(3), 229
(2004): Shen JT+, JAmAcadDermatol50(2), 326
Oral ulceration
(2001): Hernandez G+, Oral Surg Oral Med Oral Pathol Oral
Radiol Endod 92(5), 526
(2001): Macario-Barrel A+, Ann Dermatol Venereol
128(12), 1327
Hair
Hair – alopecia (>3%)
(1999): Ushigome H+, Transplant Proc 31, 2885 (2 cases)
(1998): Shapiro R+, Transplantation 65, 1284
(1997): Talbot D+, Transplantation 64, 1631
Hair – hirsutism
Hair – hypertrichosis
(2005): Prats Caelles I+, Pediatr Dermatol 22(1), 86
(1994): Yamamoto S+, JDermatolSci7, S47
Eyes
Vision loss
(2004): Tamaki H+, Int J Hematol 80(3), 291