Adult: Dosage is individualised and adjusted according to the disease being treated, the severity of the condition, patient response and tolerability. Use the lowest effective dose. Acute disorders: Initially, up to 120 mg daily. Maintenance dose in most conditions: 3-18 mg daily. Severe cases may require higher doses. Refer to the disease-specific product guidelines for detailed dosage recommendations. Child: Dosage is individualised and adjusted according to the disease being treated, the severity of the condition, patient response and tolerability. Use the lowest effective dose. Usual range: 0.25-1.5 mg/kg daily or on alternate days. Refer to the disease-specific product guidelines for detailed dosage recommendations.
Oral Duchenne muscular dystrophy
Adult: 0.9 mg/kg once daily. Round up to the nearest possible dose (tab); round up to the nearest tenth of mL (susp). Treatment guidelines may vary among individual products or between countries (refer to local product-specific recommendations). Child: ≥2 years Same as adult dose.
Nhóm bệnh nhân đặc biệt
Duchenne muscular dystrophy:
Patient taking concurrent moderate or strong CYP3A4 inhibitors: Decrease dose to 1/3 of the recommended dosage (e.g. a 36 mg daily dose would be reduced to 12 mg daily).
Suy gan
Allergic and inflammatory disorders: Dose adjustment may be required (minimum effective dose).
Chống chỉ định
Systemic infection (unless specific anti-infective therapy is given). Concomitant administration with live vaccines (especially in patients with impaired immune response, or receiving immunosuppressive doses).
Thận trọng
Patient with hypertension, cardiac disease or CHF (except in the presence of active rheumatic carditis), recent MI, thromboembolic disorders, gastrointestinal disease (e.g. gastritis, oesophagitis, diverticulitis, ulcerative colitis, fresh intestinal anastomoses, active or latent peptic ulcer, abscess or other pyogenic infections), diabetes mellitus (including family history), phaeochromocytoma, thyroid disease, active or latent TB, TB reactivity, ocular herpes simplex, glaucoma, strongyloidiasis, osteoporosis, myasthenia gravis, history of corticosteroid-induced myopathy, history of seizure disorder, emotional instability or psychotic tendency, existing or history of severe affective disorders (e.g. previous steroid-induced psychosis, depressive or manic-depressive illness); systemic sclerosis, haematological malignancies. Avoid exposure to chickenpox or measles. Patient subjected to stress conditions (e.g. trauma, severe infection, surgery). When used for Duchenne muscular dystrophy: Patient taking concurrent moderate or strong CYP3A4 inhibitors. Avoid abrupt withdrawal (particularly during prolonged therapy). Renal and hepatic (e.g. hepatic failure, cirrhosis) impairment. Children. Pregnancy and lactation.
Tác dụng không mong muốn
Significant: Adrenal suppression (e.g. adrenal cortical atrophy, hypercortisolism, hypothalamic-pituitary-adrenal [HPA] axis suppression), immunosuppression (prolonged use), Kaposi’s sarcoma (prolonged-use), visual disturbances (e.g. cataract, glaucoma, central serous chorioretinopathy, posterior subcapsular cataracts [prolonged-use], increased intraocular pressure), hypertension, electrolyte disturbance, salt and water retention, increased K excretion, left ventricular free wall rupture, thromboembolism, hyperglycaemia, acute myopathy, osteoporosis, tendonitis and tendon rupture, growth suppression (in children), psychiatric disturbances (e.g. depression, suicidal ideation, euphoria, insomnia, mood swings, personality changes), scleroderma renal crisis; toxic epidermal necrolysis, withdrawal syndrome. Rarely, anaphylaxis. Blood and lymphatic system disorders: Leucocytosis. Ear and labyrinth disorders: Vertigo. Eye disorders: Corneal or scleral thinning. Gastrointestinal disorders: Dyspepsia, abdominal pain, peptic ulceration, nausea. General disorders and administration site conditions: Oedema, impaired healing. Infections and infestations: Opportunistic infections, dormant TB recurrence. Investigations: Weight gain. Metabolism and nutrition disorders: Cushingoid appearance, increased appetite. Musculoskeletal and connective tissue disorders: Vertebral and long bone fractures, avascular necrosis. Rarely, muscle wasting. Nervous system disorders: Headache. Psychiatric disorders: Irritability, hallucination. Reproductive system and breast disorders: Amenorrhoea, irregular menstruation. Renal and urinary disorders: Pollakiuria. Respiratory, thoracic and mediastinal disorders: Cough, upper respiratory tract infection, nasopharyngitis. Skin and subcutaneous tissue disorders: Acne, skin atrophy, telangiectasia, hirsutism, erythema, striae. Rarely, bruising. Potentially Fatal: Acute adrenal insufficiency, phaeochromocytoma crisis.
Chỉ số theo dõi
Monitor blood pressure, blood glucose, electrolytes, weight. For prolonged use: Monitor bone mineral density, HPA axis suppression (e.g. ACTH stimulation test, morning plasma cortisol test, urinary free cortisol test), growth in children. Perform ophthalmic exam for >6 weeks therapy. Assess for signs and symptoms of infection, formation of cataract, elevated intraocular pressure, volume overload, and depressed mood or suicidal ideation.
Tương tác
May increase risk of tendonitis and tendon rupture with quinolones. May antagonise the effects of hypoglycaemic agents (e.g. insulin), antihypertensives, diuretics. Enhances hypokalaemic effects of acetazolamide, loop and thiazide diuretics, β2-agonists, xanthines and carbenoxolone. May enhance the therapeutic effect of coumarin anticoagulants. May lead to prolonged relaxation and acute myopathy when given with non-depolarising relaxants. May increase the renal clearance of salicylates. May increase deflazacort plasma concentration with oral contraceptives and estrogens. May have reduced bioavailability with antacids. Increased risk of systemic side effects with CYP3A inhibitors, including cobicistat-containing products. Decreased exposure to the active metabolite of deflazacort with moderate or strong CYP3A4 inducers (e.g. rifampicin, efavirenz, carbamazepine, phenytoin). Increased total exposure to deflazacort active metabolite with moderate or strong CYP3A4 inhibitors (e.g. clarithromycin, fluconazole, diltiazem, verapamil). Potentially Fatal: May diminish the serum antibody response to live vaccines.
Tương tác với thức ăn
May increase the total exposure to deflazacort active metabolite with grapefruit juice.
Ảnh hưởng đến kết quả xét nghiệm
May suppress reactions to skin tests.
Tác dụng
Description: Mechanism of Action: Deflazacort, a derivative of prednisolone, is a synthetic corticosteroid prodrug converted to its active metabolite. The active metabolite acts on the glucocorticoid receptors to exert potent anti-inflammatory and immunosuppressive effects. Its exact mechanism of action is unknown in the management of Duchenne muscular dystrophy. Pharmacokinetics: Absorption: Well absorbed from the gastrointestinal tract. Time to peak plasma concentration: 1.5-2 hours. Distribution: Crosses the placenta and enters breast milk. Plasma protein binding: Approx 40%. Metabolism: Rapidly converted by esterases into the active metabolite, 21-desacetyldeflazacort (21-desDFZ) or D 21-OH in some references; further metabolised into several inactive metabolites. Excretion: Mainly via urine (70%; 18% as active metabolite); faeces (30%). Elimination half-life: 1.1-1.9 hours.
Đặc tính
Deflazacort Source: National Center for Biotechnology Information. PubChem Compound Summary for CID 189821, Deflazacort. https://pubchem.ncbi.nlm.nih.gov/compound/Deflazacort. Accessed June 24, 2021.
Đăng xuất
