Brand Name : METHAPRED
Generic Name : Methylprednisolone
Preparations : 2 mg / 4 mg / 8 mg / 16 mg / 32 mg Tablets
Pharmacological Category : Glucocorticoids
Mechanism of Action (MOA)
METHAPRED (Methylprednisolone) is a synthetic corticosteroid with mainly glucocorticoid activity and minimal mineralocorticoid properties. METHAPRED following systemic absorption diffuse across cell membranes and complex with specific cytoplasmic receptors. These complexes enter the cell nucleus, bind to DNA and stimulate transcription of mRNA. Subsequent cellular responses result in a variety of local and systemic effects. By this mechanism METHAPRED can inhibit leukocyte infiltration at the site of inflammation, interferes with mediators of inflammatory response, and suppresses humoral immune responses. The anti-inflammatory actions of corticosteroids are thought to involve phospholipase A2 inhibitory proteins, lipocortins, which control the biosynthesis of potent mediators of inflammation such as prostaglandins and leukotrienes.
- Absorption : Readily absorbed from the gastrointestinal tract
- Onset of Action : 1 to 2 hours
- Duration of Action : 30 to 36 hours
- Distribution : Distributed to all body tissues
- Metabolism : Mainly in liver but also in other tissues
- Elimination Half-life : 3 to 3.5 hours
- Excretion : Urine (mainly, as metabolites), faeces (minimally)
Indications and Dosage
Anti-inflammatory : METHAPRED 4 mg to METHAPRED 48 mg daily
Immunosuppression : METHAPRED 4 mg to METHAPRED 48 mg daily
Asthma – Acute
Asthma Exacerbations (Emergency Medical Care or Hospital Doses): METHAPRED 40 to 80 mg once a day or equally divided into 2 times a day until peak expiratory flow is 70% of predicted or personal best
Short-course “burst” (acute asthma) : METHAPRED 40 to 60 mg once a day or equally divided into 2 times a day for 3 to 10 days
Note : Burst should be continued until symptoms resolve and peak expiratory flow is at least 80% of personal best; usually requires 3 to 10 days of treatment (approximately 5 days on average); longer treatment may be required
Asthma – Maintenance : METHAPRED 7.5 to 60 mg daily given as a single dose in the morning or every other day as needed for asthma control
Allergic Conditions :
Day 1 : One tablet of METHAPRED 8 mg before breakfast, one tablet of METHAPRED 4 mg after lunch & dinner and one tablet of METHAPRED 8 mg at bed time
Day 2 : One tablet of METHAPRED 4 mg before breakfast, after lunch & after dinner and one tablet of METHAPRED 8 mg at bed time
Day 3 : One tablet of METHAPRED 4 mg before breakfast, after lunch, dinner and at bed time
Day 4 : One tablet of METHAPRED 4 mg before breakfast, after lunch and bedtime
Day 5 : One tablet of METHAPRED 4 mg before breakfast and at bedtime
Day 6 : One tablet of METHAPRED 4 mg before breakfast
May be tapered over 12 days to decrease chance of dermatitis flare-up
Vestibular Neuritis : METHAPRED 100 mg for 3 days then gradually taper as
Days 4 to 6 : METHAPRED 80 mg
Days 7 to 9 : METHAPRED 60 mg
Days 10 to 12 : METHAPRED 40 mg
Days 13 to 15 : METHAPRED 20 mg
Days 16 to 18 : METHAPRED 10 mg
Days 20 and 22 : METHAPRED 10 mg
Ulcerative Colitis : METHAPRED 40 to 60 mg per day
Acute Exacerbation of Multiple Sclerosis : METHAPRED 160 mg a day for one week, followed by METHAPRED 64 mg every other day for one month
Little or no mineralocorticoid activity, osteoporosis, spontaneous fractures, muscle wasting, nitrogen depletion, hyperglycaemia with accentuation or precipitation of the diabetic state, increased appetite, delayed wound healing, increased susceptibility to infection, menstrual irregularities, amenorrhoea, hyperhidrosis, skin thinning, glaucoma and cataract, mental and neurological disturbances, benign intracranial hypertension, acute pancreatitis, avascular necrosis of bone, peptic ulceration, adrenal atrophy, Cushingoid symptoms
Untreated serious infections, documented hypersensitivity, systemic fungal infections, traumatic brain injury (high doses), administration of live or attenuated vaccines
Warnings / Precautions
- Caution in cirrhosis, ocular herpes simplex, hypertension, diverticulitis, hypothyroidism, myasthenia gravis, peptic ulcer disease, osteoporosis, ulcerative colitis, psychotic tendencies, renal insufficiency, pregnancy, diabetes mellitus, thromboembolic disorders, myocardial infraction.
- Long term treatment is associated with osteoporosis, myopathy, delayed wound healing.
- Use in septic shock or sepsis syndrome has not proven effective.
- Dose adjustment may be necessary in hyperthyroid and hypothyroid patients.
- Patients receiving corticosteroids should avoid chicken pox or measles-infected persons if unvaccinated.
- Latent tuberculosis may be reactivated (patients with positive tuberculin test should be monitored).
- Some suggestion (not fully substantiated) of slightly increased cleft palate risk if corticosteroids are used in pregnancy.
- May cause hypothalamic-pituitary-adrenal (HPA) axis suppression, Cushing syndrome, or hyperglycemia.
- Prolonged corticosteroid use may result in elevated Intra Ocular Pressure, glaucoma, or cataracts.
- Killed or inactivated vaccines may be administered. However, the response to such vaccines cannot be predicted.
- Immunization procedures may be undertaken in patients who are receiving corticosteroids as replacement therapy in physiologic doses (e.g. for Addison’s disease).
- Aminoglutethimide may result in a loss of corticoid-induced adrenal suppression.
- Concomitant use of methylprednisolone with anticholinesterase may lead to severe weakness in patients with myasthenia gravis.
- Methylprednisolone may decrease the hypoglycaemic effects of antidiabetic agents.
- Barbiturates increase the clearance of methylprednisolone.
- Carbamazepine may enhance metabolism of corticosteroids.
- Cholestyramine causes increased clearance of corticosteroids.
- Contraceptives (oral) may decrease hepatic metabolism of some corticosteroids thus increasing their effects.
- Plasma concentrations of cyclosporine may be increased during concomitant therapy with methylprednisolone.
- Methylprednisolone with digitalis glycosides as there is increased risk of arrhythmias associated with hypokalemia.
- Methylprednisolone may decrease serum isoniazid concentration.
- Ketoconazole decreases metabolism of certain corticosteroids.
- Macrolide antibiotics decrease clearance of methylprednisolone.
- Methylprednisolone increases the risk of adverse GI effects with NSAIDs.
- Phenytoin may enhance metabolism of corticosteroids.
- Potassium-depleting diuretics enhance the potassium-wasting effects of glucocorticoids.
- Rifampin may enhance metabolism of corticosteroids.
- Methylprednisolone may cause a diminished response to toxoids and live or inactivated vaccines and may potentiate replication of some organisms contained in live, attenuated vaccines.
Pregnancy Category : C
METHAPRED 2 mg : A box of 10 blisters, each blister of 10 tablets
METHAPRED 4 mg : A box of 20 blisters, each blister of 10 tablets
METHAPRED 8 mg : A box of 10 strips, each strip of 10 tablets
METHAPRED 16 mg : A box of 5 strips, each strip of 10 tablets
METHAPRED 32 mg : A box of 3 strips, each strip of 10 tablets