ABSTRACT
Synonym: FK506 Trade names: Prograf (Astellas), Protopic (Astellas) Indications: Prophylaxis of organ rejection, atopic dermatitis (topical) Class: Calcineurin inhibitor, Immunosuppressant, Macrolactam Half-life: ~8.7 hours Clinically important, potentially hazardous interactions with: abatacept, afatinib, alefacept, amiodarone, amprenavir, atazanavir, azacitidine, beta blockers, betamethasone, boceprevir, bosentan, cabazitaxel, caspofungin, cinacalcet, crizotinib, cyclosporine, CYP3A4 inhibitors and inducers, dabigatran, dairy products, danazol, darunavir, dasatinib, delavirdine, denileukin, dexlansoprazole, diclofenac, docetaxel, dronedarone, efavirenz, elvitegravir / cobicistat / emtricitabine / tenofovir, enzalutamide, erythromycin, etoricoxib, fingolimod, gefitinib, grapefruit juice, Hemophilus B vaccine, HMGCoA reductase inhibitors, ibuprofen, immunosuppressants, indinavir, irbesartan, itraconazole, ketoconazole, leflunomide, lenalidomide, lopinavir, lovastatin, meloxicam, mifepristone, mycophenolate, nelfinavir, nifedipine, olmesartan, omeprazole, oxaliplatin, pazopanib, pemetrexed, posaconazole, potassium, potassium-sparing diuretics, pralatrexate, rifabutin, rifampin, rifapentine, sevelamer, simvastatin, sirolimus, St John’s wort, telaprevir, telithromycin, temsirolimus, tinidazole, tipranavir, tofacitinib, triamcinolone, vaccines, voriconazole Pregnancy category: C
Skin Anaphylactoid reactions/Anaphylaxis (<1%) [2]
Angioedema [1] Burning (46%) [13] Dermatitis [1] Diaphoresis (>3%) Ecchymoses (>3%) Edema (>10%) Erythema (12%) [3] Exanthems (4%) [2] Exfoliative dermatitis [1] Fibrosis [1] Folliculitis (10%) [2] Graft-versus-host reaction [2] Herpes simplex (13%) [4] Herpes zoster [1] Human papilloma virus reactivation [1] Hypersensitivity [1] Kaposi’s sarcoma [2] Kaposi’s varicelliform eruption [2] Lentigo [1] Lymphoma [2] Melanoma [1] Melanosis [1] Molluscum contagiosum [1] Nevi [1] Peripheral edema (26%) Photosensitivity (>3%) Pigmentation [3] Pruritus (25-36%) [10] Purpura [1]
Pustules (6%) [1] Rash (24%) [1] Rosacea [4] Squamous cell carcinoma [1] Thrombocytopenic purpura [1] Toxicity [2] Tumors [1] Urticaria [1] Varicella zoster [1] Vasculitis [1]
Hair Alopecia (>3%) [5] Hirsutism [1] Hypertrichosis [2]
Mucosal Gingival hyperplasia/hypertrophy [6] Mucositis [1] Oral candidiasis (>3%) Oral pigmentation [2] Oral ulceration [2]
Cardiovascular Acute coronary syndrome Cardiomyopathy [3] Chest pain Flushing [4] Hypertension (49%) [6] QT prolongation [2] Torsades de pointes [1]
Central Nervous System Altered mental status [1] Catatonia [1] Encephalopathy [9] Fever (>10%) Headache [4] Hyperesthesia Intracranial pressure decreased [1] Leukoencephalopathy [13] Neurotoxicity [7] Pain [1] Paresthesias (40%) [3] Parkinsonism [2] Seizures (<10%) [4] Tremor (>10%) [6] Vertigo (dizziness) [1]
Neuromuscular/Skeletal Arthralgia (>10%) [1] Asthenia (fatigue) (>10%) Back pain (>10%) Bone or joint pain [1] Myalgia/Myositis/Myopathy/Myotoxicity (>3%)
Rhabdomyolysis [1]
Gastrointestinal/Hepatic Abdominal pain [3] Constipation (>10%) Diarrhea (>10%) [3] Dyspepsia (>10%) Dysphagia (>3%) [1] Gastroenteritis [1] Gastroesophageal reflux [1] Hepatotoxicity [6] Nausea (>10%) Pancreatitis [3] Vomiting (>10%)
Respiratory Cough (>10%) Dyspnea (>10%) Flu-like syndrome [1]
Pulmonary toxicity [1] Respiratory distress [1]
Endocrine/Metabolic Amenorrhea [1] Creatine phosphokinase increased (>10%) [2]
Diabetes mellitus [2] Diabetic ketoacidosis [2] Gynecomastia [2] Hyperglycemia [6] Hyperkalemia [2] Hyperlipidemia [1] Hypophosphatemia (>10%) Inappropriate secretion of antidiuretic hormone (SIADH) [2]
Genitourinary Priapism [1] Urinary tract infection [1]
Renal Nephrotoxicity [36] Renal failure [1] Renal function abnormal [2]
Hematologic Agranulocytosis [1] Anemia (>10%) Angiopathy [4] Hemolytic anemia [1] Hemolytic uremic syndrome [17] Hemorrhage [1] Hypomagnesemia (>10%) Leukopenia (>10%) [2] Myelosuppression [1] Neutropenia [2] Pancytopenia [1] Pure red cell aplasia Thrombocytopenia [1] Thrombotic complications [3]
Otic Ototoxicity [1] Tinnitus [2]
Ocular Diplopia [2] Hallucinations, visual [1] Maculopathy [1] Nystagmus [1] Ocular burning [2] Ophthalmoplegia [1] Optic neuropathy [2] Vision blurred [1] Vision loss [3] Visual disturbances [1]
Local Application-site burning [2] Application-site erythema [1] Application-site infection [2] Application-site pruritus [4] Application-site reactions [1]
Other Adverse effects [7] Cancer [2] Death [1] Infection (>10%) [8] Malakoplakia [1] Side effects [1]
