Generic Name : ( Methylprednisolone )
Therapeutic Group : Anti-inflammatory
Overview:
Methylprednisolone is a corticosteroid medicine that prevents the release of substances in the body that cause inflammation.
Methylprednisolone is used to treat many different inflammatory conditions such as arthritis, lupus, psoriasis, ulcerative colitis, allergic disorders, gland (endocrine) disorders, and conditions that affect the skin, eyes, lungs, stomach, nervous system, or blood cells.
Presentation
Tablet : 2, 4, 8 & 16 mg
Injection : 500 & 1000 mg IM/IV
Melpred 2 tablet :
Each tablet contains Methylprednisolone USP 2 mg.
Melpred 4 tablet :
Each tablet contains Methylprednisolone USP 4 mg.
Melpred 8 tablet :
Each tablet contains Methylprednisolone USP 8 mg.
Melpred 16 tablet :
Each tablet contains Methylprednisolone USP 16 mg.
Melpred 500 mg Injection :
Each vial contains 500 mg of Methylprednisolone USP as Methylprednisolone Sodium Succinate USP.
Melpred 1 g Injection :
Each vial contains 1 gm of Methylprednisolone USP as Methylprednisolone Sodium Succinate USP.
Methylprednisolone is a potent anti-inflammatory steroid with greater anti-inflammatory potency than prednisolone and even less tendency than prednisolone to induce sodium and water retention. When given parenterally and in equimolar quantities, the two compounds are equivalent in biologic activity.
Endocrine Disorders, Dermatologic Diseases, Gastrointestinal Diseases, Neoplastic Diseases, Rheumatic Disorders, Allergic States, Respiratory Diseases, Edematous States Disease, Collagen Diseases, Ophthalmic Diseases, Hematologic Disorders, Nervous System Disorder.
Melpred tablet: The usual range is 2-48 mg daily in divided doses, depending on the specific disease being treated. As anti-inflammatory/immunosuppressive initial dosage: As anti-inflammatory/ immunosuppressive, the initial dosage of Methylprednisolone tablets may vary from 4-48 mg per day depending on the specific disease entity being treated. In situations of less severity lower doses will generally suffice while in selected patients higher initial doses may be required. The initial dosage should be maintained or adjusted until a satisfactory response is noted. If after a reasonable period of time there is a lack of satisfactory clinical response, Methylprednisolone should be discontinued and the patient transferred to other appropriate therapy. It should be emphasized that dosage requirements are variable and must be individualized on the basis of the disease under treatment and the response of the patient.
As anti-inflammatory/immunosuppressive maintenance dosage: After a favorable response is noted, the proper maintenance dosage should be determined by decreasing the initial drug dosage in small decrements at appropriate time intervals until the lowest dosage which will maintain an adequate clinical response is reached. It should be kept in mind that constant monitoring is needed in regard to drug dosage. If after long-term therapy the drug is to be stopped, it is recommended that it be withdrawn gradually rather than abruptly.
Multiple Sclerosis: In the treatment of acute exacerbations of multiple sclerosis, daily doses of 160 mg of Methylprednisolone for a week followed by 64 mg every other day for 1 month have been shown to be effective. Methylprednisolone 4 mg tablet can be used to treat and to control severe allergy and dermatitis. Following the guideline listed below to minimize the steroid withdrawal syndromes:
• Day 1: 2 tablets before breakfast + 1 tablet after lunch + 1 tablet after dinner + 2 tablets at bedtime
• Day 2: 1 tablet before breakfast + 1 tablet after lunch + 1 tablet after dinner + 2 tablets at bedtime
• Day 3: 1 tablet before breakfast + 1 tablet after lunch + 1 tablet after dinner + 1 tablet at bedtime
• Day 4: 1 tablet before breakfast + 1 tablet after lunch + 1 tablet at bedtime
• Day 5: 1 tablet before breakfast + 1 tablet at bedtime
• Day 6: 1 tablet before breakfast
Alternate-day therapy (ADT): Alternate-day therapy is a corticosteroid dosing regimen in which twice the usual daily dose of corticoid is administered every other morning. The purpose of this mode of therapy is to provide the patient requiring long-term pharmacologic dose treatment with the beneficial effects of corticoids, while minimizing certain undesirable effects, including pituitary-adrenal suppression, Cushingoid state, Corticoid withdrawal symptoms, and growth suppression in children. The following should be kept in mind when considering alternate-day therapy: (a) Basic principles and indications for corticosteroid therapy should be applied. (b) ADT is a therapeutic technique primarily designed for patients in whom long-term pharmacologic corticoid therapy is anticipated. In less severe disease processes in which corticoid therapy is indicated, it may be possible to initiate treatment with ADT. More severe disease states usually will require daily divided high dose therapy for initial control of the disease process. The initial suppressive dose level should be continued until satisfactory clinical response is obtained, usually four to ten days in the case of many allergic and collagen diseases. Once control has been established, two courses are available: (a) change to ADT and then gradually reduce the amount of corticoid given every other day or (b) following control of the disease process reduce the daily dose of corticoid to the lowest effective level as rapidly as possible and then change over to an alternate day schedule.
Melpred Injection
Rheumatoid arthritis:
1 g/day IV for 1, 2, 3 or 4 days or 1 g/month IV for 6 months.
The regimen should be administered over at least 30 minutes and may be repeated if no improvement has been reported within one week after therapy or if the patient’s condition dictates.
Mild to moderately emetogenic chemotherapy:
Administer Methylprednisolone IV over at least 5 minutes and one hour before chemotherapy, at the initiation of chemotherapy and at the time of discharge.
Severely emetogenic chemotherapy :
Administer Methyprednisolone IV over at least 5 minutes with appropriate doses of metoclopramide or a butyrophenone one hour before chemotherapy, then Methylprednisolone IV at the initiation of therapy and at time of discharge.
Acute Spinal Cord Injury:
The treatment should begin within eight hours of injury.
For patients initiated on treatment within 3 hours of injury:
Start with an IV bolus dose of 30 mg methylprednisolone per kilogram of body weight over a 15-minute period under continuous medical supervision. This administration rate of the bolus injection may only be used for this indication, under ECG monitoring and with an available defibrillator. The administration of high doses of methylprednisolone in bolus intravenously (doses of more than 500 mg over a period of less than 10 minutes) may cause arrhythmias, circulatory collapse and cardiac arrest. After the bolus injection comes a 45-minute pause, followed by a continuous infusion of 5.4 mg/kg per hour for 23 hours.
For patients initiated on treatment within 3 to 8 hours of injury:
Administer 30 mg/kg as an IV bolus over a 15-minute period, followed by a 45-minute pause, and then a continuous IV infusion of 5.4 mg/kg/h for 47 hours. For the infusion pump, one should preferably choose another intravenous site than for the bolus injection.
Special Risk Groups
Patients belonging to the following special risk groups should be under strict medical surveillance and should be treated during as short period as possible.
Children
Growth may be suppressed in children receiving long-term, daily divided doses glucocorticoid therapy. The use of such a regimen should be restricted to those most serious indications.
Diabetics
Manifestations of latent diabetes mellitus or increased requirements for insulin or oral hypoglycemic agents.
Hypertensive patients
Aggravation of arterial hypertension.
Patients with psychiatric antecedents
Existing emotional instability or psychotic tendencies may be aggravated by corticosteroids.
Since complications of treatment with glucocorticoids are dependent on the size of the dose and the duration of treatment, a risk/benefit decision must be made in each individual case as to dose and duration of treatment and as to whether daily or intermittent therapy should be used. In patients on corticosteroid therapy subjected to unusual stress, increased dosage of rapidly acting glucocorticosteroids before, during and after the stressful situation is indicated. Glucocorticosteroids may mask some signs of infection and new infections may appear during their use. There may be decreased resistance and inability to localize infection when corticosteroids are used. Data from a clinical study conducted to establish the efficacy of methylprednisolone sodium succinate in septic shock, suggest that a higher mortality occurred in subsets of patients who entered the study with elevated serum creatinine levels or who developed a secondary infection after therapy began. The use of methylprednisolone sodium succinate in active tuberculosis should be restricted to those cases ofulminating or disseminated tuberculosis in which the glucocorticosteroid is used for the management of the disease in conjunction with an appropriate antituberculous regimen. If glucocorticosteroids are indicated in patients with latent tuberculosis or tuberculin reactivity, close observation is necessary as reactivation of the disease may occur. During prolonged corticosteroid therapy, these patients should receive chemoprophylaxis. Because rare instances of anaphylactic (e.g. bronchospasm) reactions have occurred in patients receiving parenteral corticosteroid therapy, appropriate precautionary measures should be taken prior to administration, especially when the patient has a history of allergy to any drug. Drug-induced secondary adrenocortical insufficiency may be minimized by gradual reduction of dosage. This type of relative insufficiency may persist for months after discontinuation of therapy; therefore, in any situation of stress occurring during that period, hormone therapy should be reinstituted. Since mineralocorticoid secretion may be impaired, salt and/or a mineralocorticoid should be administered concurrently. There is an enhanced effect of glucocorticosteroids on patients with hypothyroidism and in those with cirrhosis. Glucocorticosteroids should be used cautiously in patients with ocular herpes simplex because of possible corneal perforation. Glucocorticosteroids should be used with caution in nonspecific ulcerative colitis. Growth and development of infants and children on prolonged corticosteroid therapy should be carefully observed. Methylprednisolone sodium succinate should not be used routinely to treat head injury as demonstrated by the results of a multicenter study. The study results revealed an increased mortality in the 2 weeks after injury in patients administered methylprednisolone sodium succinate compared to placebo (1.18 relative risk). A causal association with methylprednisolone sodium succinate treatment has not been established. Some of these presentations contain benzyl alcohol. Benzyl alcohol has been reported to be associated with a fatal “gasping syndrome” (respiratory disorder characterized by a persistent gasping for breath) in premature infants. Corticotherapy has to be considered when interpreting a whole series of biological tests and parameters (e.g. skin tests, thyroid hormone levels). The duration of the treatment should in general be kept as short as possible. The discontinuation of a chronic treatment should also occur under medical surveillance (gradual discontinuation, evaluation of the adrenocortical function). The most important symptoms of adrenocortical insufficiency are asthenia, orthostatic hypotension and depression.
Combination of glucocorticosteroids with ulcerogenic drugs (e.g. salicylates and NSAIDs) increases the risk of gastrointestinal complications.
• Combination of glucocorticosteroids with thiazide diuretics increases the risk of glucose intolerance.
• Glucocorticosteroids can increase the requirements for insulin or oral hypoglycemic agents in diabetics.
• While on corticosteroid therapy, patients should not be vaccinated against smallpox. Other immunization procedures should not be undertaken in patients who are on corticosteroids, especially on high doses, because of possible hazards of neurological complications and/or lack of antibody response.
• Acetylsalicylic acid should be used cautiously in conjunction with corticosteroids in hypoprothrombinemia.
• Convulsions have been reported with concurrent use of methylprednisolone and cyclosporin. Concurrent administration of these agents results in a mutual inhibition of metabolism. Therefore it is possible that convulsions and other adverse events associated with the individual use of either drug may be more apt to occur.
The duration of the treatment should in general be kept as short as possible. Medical surveillance is recommended during chronic treatment. The discontinuation of a chronic treatment should also occur under medical surveillance (gradual discontinuation, evaluation of the adrenocortical function). The most important symptoms of adrenocortical insufficiency are asthenia, orthostatic hypotension and depression. Injection into the deltoid muscle should be avoided because of the high incidence of subcutaneous atrophy.
Methylprednisolone is a cytochrome P450 enzyme (CYP) substrate and is mainly metabolized by the CYP3A4 enzyme. CYP3A4 is the dominant enzyme of the most abundant CYP subfamily in the liver of adult humans. It catalyzes 6β-hydroxylation of steroids, the essential Phase I metabolic step for both endogenous and synthetic corticosteroids.CYP3A4 SUBSTRATES - Many compounds are also substrates of CYP3A4, some of which (as well as other drugs) have been shown to alter glucocorticoid metabolism by induction (upregulation) or inhibition of the CYP3A4 enzyme. In the presence of another CYP3A4 substrate,the hepatic clearance of methylprednisolone may be affected, with corresponding dosage adjustments required. It is possible that adverse events associated with the use of either drug alone may be more likely to occur with coadministration. CYP3A4 INHIBITORS - Drugs that inhibit CYP3A4 activity, such as ketoconazole,erythromycin, clarithromycin, diltiazem, and cyclosporine generally decrease hepatic clearance and increase the plasma concentration of CYP3A4 substrate medications, such as methylprednisolone. In the presence of a CYP3A4 inhibitor, a lower dose of methylprednisolone may be required to avoid toxicity.CYP3A4 INDUCERS - Drugs that induce CYP3A4 activity, such as Phenobarbital, rifampin, carbamazepine, and phenytoin generally increase hepatic clearance, resulting in decreased plasma concentration of medications that are substrates for CYP3A4. Coadministration may require an increase in methylprednisolone dosage to achieve the desired result. Withdrawal of these inhibitors or inducers reverses these clinical changes and may require careful dosage re-adjustment.
Pregnancy & Lactation
Some animal studies have shown that corticosteroids, when administered to the mother at high doses, may cause fetal malformations. Since adequate human reproduction studies have not been done with glucocorticosteroids, the use of these drugs in pregnancy, nursing mothers or women of childbearing potential, requires that the possible benefits of the drug be weighed against the potential hazards to the mother, embryo or fetus. Glucocorticoids should be used during pregnancy only if clearly needed. If a chronic treatment with corticosteroids has to be stopped during pregnancy (as with other chronic treatments), this should occur gradually. In some cases (e.g. substitution treatment of adrenocortical insufficiency), however, it can be necessary to continue treatment or even to increase dosage. Corticosteroids readily cross the placenta. New born infants born of mothers who have received substantial doses of glucocorticosteroids during pregnancy should be carefully observed and evaluated for signs of adrenal insufficiency. In the case of labor and delivery no effects are known. Corticosteroids are excreted in breast milk.
In patients with known hypersensitivity to any components of the product
• In patients with systemic fungal infections
• In patients administered with live or live, attenuated vaccines while receiving immunosuppressive doses of corticosteroids
• In herpes simplex of the eye, except when used for short-term or emergency therapy as in acute sensitivity reactions
• In patients with vaccinia and varicella, except when used for short-term or emergency therapy as in acute sensitivity reactions.
Protect from light. Store unreconstituted product at controlled room temperature 20°C to 25° C.
Melpred 2 Tablet : Each box contains 2 x 15 tablets in Alu-Alu blister pack.
Melpred 4 Tablet : Each box contains 2 x 15 tablets in Alu-Alu blister pack.
Melpred 8 Tablet : Each box contains 3 x 10 tablets in Alu-Alu blister pack.
Melpred 16 Tablet : Each box contains 3 x 10 tablets in Alu-Alu blister pack.
Melpred 500 mg Injection : Each combipack contains 1vial with 1 ampoule of 10 ml water for injection BP in blister pack, one 10 ml sterile disposable syringe, one butterfly needle & one alcohol pad.
Melpred 1 gm Injection : Each combipack contains 1vial with 2 ampoules of 10 ml water for injection BP in blister pack, 20 ml sterile disposable syringe, one butterfly needle & one alcohol pad.
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