Brand Name : CORTILONE
Generic Name : Prednisolone
Preparations : 2.5 mg / 5 mg / 10 mg / 20 mg / 30 mg / 40 mg Tablets
Pharmacological Category : Corticosteroid
Mechanism of Action (MOA)
CORTILONE (Prednisolone) diffuses into the cell, and then binds noncovalently and with high affinity to the cytoplasmic glucocorticoid receptor (GR) and forms a complex. This activated steroid-receptor complex translocates to the nucleus, binds to specific DNA sequences called glucocorticoid-responsive elements (GREs), and alters the transcription rate of specific genes associated with the GRE. This increases the synthesis of phospholipase A2 inhibitory proteins, lipocortins, which control the biosynthesis of potent mediators of inflammation such as prostaglandins and leukotrienes. In addition, CORTILONE inhibits leukocyte infiltration at the site of inflammation, suppression of humoral immune responses, and reduction in edema or scar tissue.
- Absorption : Absorbed from the gastrointestinal tract
- Peak Plasma Time : 1 hour
- Protein Binding : 65 to 91% (lower in elderly)
- Metabolism : Extensively in liver
- Elimination Half-life : 3.6 hours; End-stage renal disease: 3 to 5 hours
- Excretion : Primarily urine
Indications and Dosage
- Mysthenia Gravis : CORTILONE 5 to 20 mg daily or on alternative days to reduce the risk of steroid induced exacerbations of weakness and increase the dose slowly thereafter according to response
- Auto-immune Haemolytic Anaemia : CORTILONE 1 to 1.5 mg per kg daily
- Prostate Cancer : One tablet of CORTILONE 5 mg twice daily in combination with anticancer drug (docetaxel)
- Bone Disorders, Non-malignant : CORTILONE 20 to 30 mg daily in 7-day courses every 2 months along with chemotherapy (melphalan)
- Giant Cell Arteritis (Temporal Arteritis, Cranial Arteritis) : CORTILONE 40 to 60 mg daily
- Polyarteritis Nodosa : CORTILONE 40 to 60 mg daily
- Microscopic Polyangiitis : CORTILONE 1 mg per kg with cyclophosphamide
- Hypersensitivity Vasculitis : CORTILONE 60 mg or CORTILONE 1 mg per kg daily, tapered rapidly until therapy can be stopped
- Non-necrotising Scleritis : CORTILONE 60 to 80 mg daily
- Optic Neuropathies : CORTILONE 80 to 400 mg daily
- Corneal Graft Rejection : CORTILONE 60 to 80 mg daily
- Pemphigus and Pemphigoid : CORTILONE 1 mg per kg daily is continued until new blister stops forming then gradually decreases
- Polymyositis and Dermatomyositis : CORTILONE 40 to 60 mg daily or CORTILONE 1 to 2 mg per kg daily
- Rheumatoid Arthritis : CORTILONE 5 to 7.5 mg daily, not exceeding CORTILONE 15 mg daily
- Polymyalgia Rheumatic: CORTILONE 10 to 20 mg daily
- Sarcoidosis : CORTILONE 30 to 40 mg daily
- Chronic Active Hepatitis : CORTILONE 20 to 30 mg daily or CORTILONE 60 mg daily then is slowly tapered over several months to the minimum required for maintenance
- Inflammatory Bowel Disease (IBD) : CORTILONE 10 to 40 mg daily
- Bell’s Palsy : CORTILONE 60 mg daily for 5 days then taper down by CORTILONE 10 mg daily for 5 days for total duration of 10 days
- Multiple Sclerosis : CORTILONE 200 mg per day for 1 week then CORTILONE 80 mg every other day for 1 month
- Acute Severe Asthma : CORTILONE 40 to 50 mg daily for 5 to 10 days
- Chronic Asthma : CORTILONE 7.5 to 10 mg daily
- Acute Exacerbation of Chronic Obstructive Pulmonary Disease (AECOPD) : CORTILONE 30 to 50 mg daily for 7 to 14 days
- Croup requiring Intubation : CORTILONE 1 mg per kg
- Cluster Headache Attacks : CORTILONE 20 to 40 mg daily
Fluid and electrolyte disturbances, osteoporosis, muscle weakness, cushingoid state, menstrual irregularities, facial erythema, convulsions, impaired wound healing, increased sweating, decreased carbohydrate tolerance, glaucoma, posterior subcapsular cataracts, vertigo, headache, abdominal distention
Hypersensitivity to prednisolone, superficial herpes simplex keratitis, varicella, systemic fungal infections
Warnings / Precautions
- Dose may need to be increased before, during, and after stressful situation.
- May mask signs of infection or cause new infections.
- Possible benefits should be weighed against potential hazards if used during pregnancy / nursing.
- Prolonged use may produce posterior subcapsular cataracts, glaucoma, optic nerve damage, and secondary ocular infections.
- May cause BP elevation, increased K+ / Ca2+ excretion, and salt / water retention.
- Dietary salt restriction and K+ supplementation may be necessary when used in large doses.
- More serious / fatal course of infections reported with chickenpox and measles; avoid exposure.
- Reactivation of disease may occur with latent TB or tuberculin reactivity.
- Caution with hypothyroidism, cirrhosis, ocular herpes simplex, hypertension, diverticulitis, fresh intestinal anastomoses, nonspecific ulcerative colitis, osteoporosis, myasthenia gravis, renal insufficiency, and active or latent peptic ulcer.
- Growth and development of children on prolonged therapy should be monitored.
- May cause psychic derangements or aggravate existing emotional instability or psychotic tendencies.
- Avoid abrupt withdrawal.
- Prednisolone reduces plasma-salicylate concentration when taken along with aspirin.
- Rifampin accelerates the metabolism of prednisolone.
- Phenytoin / Phenobarbital / carbamazepine reduce the efficacy of prednisolone.
- Ketoconazole reduces the clearance of prednisolone.
- Oral contraceptives increase the plasma concentration of prednisolone.
- Ritonavir increases the plasma concentration of prednisolone.
- Potassium-depleting diuretics (thiazides or frusemide) may increase the potassium loss when taken along with prednisolone.
Pregnancy Category : C
CORTILONE 2.5 mg : A box of 20 blisters, each blister of 10 tablets
CORTILONE 5 mg : A box of 20 blisters, each blister of 10 tablets
CORTILONE 10 mg : A box of 20 blisters, each blister of 10 tablets
CORTILONE 20 mg : A box of 20 blisters, each blister of 10 tablets
CORTILONE 30 mg : A box of 20 blisters, each blister of 10 tablets
CORTILONE 40 mg : A box of 10 strips, each strip of 10 tablets