Composition
Each vial (1 ml) contains: Methylprednisolone acetate 40 mg.
- For Intramuscular, Intrasynovial and Soft Tissue Injection.
- Not For I.V. Use
Properties
Methylprednisolone, a potent synthetic glucocorticoid is 6-methyl derivative of prednisolone.
It has four to five times the anti-inflammatory activity as that of hydrocortisone and lacks significant mineralocorticoid activity.
Methylprednisolone acetate is less soluble and slowly metabolized which explains its prolonged effect (elimination half life is 139 hours, i.e. about 6 days).
Indications
M.P.A. is recommended for intra-articular, periarticular administration, or intralesional injection in various dermatologic conditions for local effect and for intramuscular administration for systemic effect.
For Local Effect
Intrasynovial and intralesional or soft tissue administration
- Rheumatoid arthritis, osteoarthritis
- Bursitis
- Miscellaneous: Ganglion, tendonitis and epicondylitis.
Dermatologic conditions
- Keloids
- Hypertrophic lichen planus
- Neurodermatitis
- Discoid lupus erythematosus
- Necrobiosis lipoidica diabeticorum
- Alopecia areata
Instillation for local effect in patients with ulcerative colitis
For Systemic Effect
Intramuscular Administration
- Adrenogenital syndrome
- Rheumatoid arthritis
- Dermatologic conditions: Acute and chronic contact dermatitis, including poison ivy dermatitis and seborrheic dermatitis
- Bronchial asthma
- Perennial allergic rhinitis
- Patients with esophageal burns due to caustic ingestion
Contraindications
Acute infectious conditions, herpes simplex keratitis, acute psychoses, systemic fungal infections, viral infections (as vaccinia and varicella), tuberculosis (if used, it must be combined with an appropriate antituberculous regimen).
Relative Contraindications: Peptic ulcer, osteoporosis, recent intestinal anastmosis, renal insufficiency, thromboembolic tendencies, diabetes mellitus and hypertension.
Pregnancy and Lactation
If it is necessary to give corticosteroids during pregnancy, the potential risks should be carefully considered.
Infants born of mothers who have received substantial corticosteroid doses during pregnancy should be carefully observed for signs of hypoadrenalism. Advise mothers taking corticosteroid not to nurse their infants.
Adverse Effects
Include cushingoid state (moonface, supraclavicular fat pad), suppression of growth in children, secondary adrenocortical insufficiency particularly in times of stress, decreased glucose tolerance with hyperglycemia and glycosuria, manifestations of latent diabetes mellitus, negative nitrogen balance due to protein catabolism, hirsutism, fluid and electrolyte disturbance, steroid myopathy, osteoporosis and spontaneous fractures, pancreatitis, peptic ulcer with perforation and hemorrhage, purpura, striae, petechiae, convulsions, increased intracranial pressure with papilledema, posterior subcapsular cataract, increased intraocular pressure, aggravation and masking of infections, aggravations of hypertension, hyperpigmentation, subcutaneous and cutaneous atrophy.
When adverse effects occur, they are usually reversible and disappear when the drug is discontinued.
Precautions
Drug-induced secondary adrenocortical insufficiency may be avoided by gradual reduction of dosage. This type of relative insufficicency may persist for months after discontinuation of therapy; therefore, in any situation of stress occurring during that period, hormonal therapy should be reinstituted.
Growth and development of infants and children on prolonged corticosteroid therapy should be carefully observed.
Steroids may mask signs of infections, and new infections may appear during their use, if an infection occurs during therapy, it should be promptly controlled by suitable antimicrobial therapy.
Average and large doses of steriods may cause elevation of blood pressure, salt and water retention and increased potassium excretion. Dietary salt restriction and potassium supplementation may be necessary.
Corticosteroids aggravate diabetes mellitus, if steriods are required in patients with diabetes mellitus, changes in dose of insulin or oral antidiabetic drugs may be necessary.
Intrasynovial injection of corticosteroid drugs may produce systemic as well as local effects.
A marked increase in pain accompanied by local swelling, further restriction of joint motility, fever and malaise are suggestive of septic arthritis. If this complication occurs and the diagnosis of sepsis is confirmed, appropriate antimicrobial therapy should be instituted.
Warnings
This preparation should not be administered intravenously.
In order to minimize the incidence of dermal and subdermal atrophy, care must be exercised not to exceed recommended doses in injections. Multiple small injections into the area of the lesions should be made whenever possible.
The technique of intrasynovial and intramuscular injections should include precautions against injection or leakage into the dermis. Injection into the deltoid muscle should be avoided because of the high incidence of subcutaneous atrophy.
Dosage and Administration
M.P.A. sterile aqueous suspension should not be diluted or mixed with other solutions.
Administration for local effect
Rheumatoid and osteoarthritis
The dose for intra-articular administration depends on the size of the joint (large joints 20-80 mg, medium joints 10-40 mg, small joints 4-10 mg) and varies with severity of the condition.
In chronic cases injections may be repeated at intervals of 1-5 or more weeks depending on the degree of relief obtained from the initial injection.
Repeated intra-articular injection may result on joint instability. X-ray follow-up is suggested in selected cases to detect deterioration.
Suitable sites for injection are the knee, ankle, wrist, elbow, shoulder, hip and phalangeal joints. Since difficulty is frequently encountered in entering the hip joint, precautions should be taken to avoid any large blood vessels in the area. Joints not suitable for injection are those that are anatomically inaccessible and devoid of synovial space such as the spinal joints and the sacroiliac joints.
Treatment failures frequently results from failure to enter the joint space, little or no benefit follows injection into the surrounding tissue. If failures occur when injections into the synovial spaces are certain, as determined by aspiration of fluid, repeated injections are usually of no benefit.
Local therapy does not alter the underlying disease process, whenever possible, employ comprehensive therapy including physiotherapy and orthopedic correction.
Following intra-articular steroid therapy, care should be taken to avoid overuse of joints in which symptomatic benefit has been obtained. Negligence in this matter may permit an increase in joint deterioration that will be more than offset the beneficial effects of the steroid.
Procedure
It is recommended that the anatomy of the joint involved should be reviewed before attempting intra-articular injection. In order to obtain the full anti-inflammatory effect, it is important that the injection be made into the synovial space.
Employing the same sterile technique as for a lumbar puncture, a sterile 20-24 gauge needle (on a dry syringe) is quickly inserted into synovial cavity. Procaine infiltration is elective. The aspiration of only few drops of joint fluid to prove the joint space has been entered by the needle.
The injection site for each joint is determined by that location where the synovial cavity is most superficial and most free of large vessels and nerves.
With the needle in space, the aspirating syringe is removed and replaced by a second syringe containing the desired amount of M.P.A. suspension. The plunger is then pulled outward slightly to aspirate synovial fluid and to make sure the needle is still in the synovial space.
After injection, the joint is moved gently a few times to aid mixing the synovial fluid and the suspension. The site is covered with a small sterile dressing.
Bursitis
The area around the injection site is prepared in a sterile way and a wheal at the site made with 1% Procaine hydrochloride solution. A 20-24 gauge needle attached to a dry syringe is inserted into the bursa and the fluid aspirated. The needle is left in place and the aspirating syringe changed for a small syringe containing the desired dose. After injection, the needle is withdrawn and a small dressing applied.
Tendonitis, epicondylitis, ganglion
In the treatment of conditions such as tendinitis or tenosynovitis, care should be taken, following application of a suitable antiseptic to the overlying skin, to inject the suspension into the tendon sheath rather than into the substance of the tendon.
When treating conditions such as epicondylitis, outline the area of greatest tenderness and infiltrate the drug into this area. For ganglia of the tendon sheath, inject the drug directly into the cyst. The dose ranges from 4-30 mg. In recurrent or chronic conditions, repeated injections may be needed.
Injections for local effect in dermatologic conditions
Avoid injection of sufficient material to cause blanching, since this may be followed by a small slough. Following cleansing with an appropriate antiseptic such as 70% alcohol, 20-60 mg of the suspension is injected into the lesion.
It may be necessary to distribute doses ranging from 20-40 mg by repeated local injections in the case of large lesions. 1-4 injections are usually employed, intervals between injections vary with the type of lesion being treated and duration of improvement produced by initial injection.
Instillation for local effect in patients with ulcerative colitis
A dose of 40 mg administered as a retention enema or by continuous drip 3-7 times a week for 2 or more weeks.
Administration for systemic effect
Intramuscular injections of M.P.A. suspension should be made deeply into the gluteal muscle. Repeated intramuscular injections at the same site should be avoided, and should not be administered subcutaneously.
Dosage must be individualized and readjusted according to the severity of the disease, stress and patient’s responsiveness.
For infants and children the recommended dosage should be governed by the same considerations rather than by strict adherence to the ratio indicated by age or body weight.
If spontaneous remission occurs in a chronic condition, discontinue treatment gradually.
Routine laboratory studies such as urine analysis, two-hour postprandial blood sugar, determination of blood pressure and body weight, and a chest x-ray should be made at regular intervals during prolonged therapy. Upper gastrointestinal x-ray are desirable in patients with an ulcer history or significant dyspepsia.
In patients with adrenogenital syndrome, a single intramuscular injection of 40 mg every two weeks may be adequate.
In rheumatoid arthritis: Weekly, intramuscular dose will vary from 40-120 mg.
In dermatologic lesions 40-120 mg intramuscularly at weekly intervals for 1-4 weeks. In acute severe dermatitis due to poison ivy, relief may result within 8-12 hours following intramuscular injection of single dose of 80-120 mg. In chronic contact dermatitis repeated injections at 5-10 days interval may be necessary.
In seborrheic dermatitis, a weekly dose of 80 mg may be adequate to control the condition.
In asthmatic patients, injection of 80-120 mg may result in relief of symptoms within 6-48 hours and persist for several days to two weeks.
In patients with allergic rhinitis (hay fever) an intramuscular dose of 80-120 mg may be followed by relief of coryzal symptoms within 6 hours persisting for several days of 3 weeks.
Withdrawal of therapy
If, after long-term therapy, the drug is to be stopped, it must be withdrawn gradually.
How to Supplied
Vials of 1 ml in packs of 1 vial.
N.B.: Shake well before using.
Keep all medicaments out of reach of children
Product of: AMOUN PHARMACEUTICAL CO. El-Obour City, Cairo, Egypt. ATC Code: H02AB04