Disprelone D Tablets
1) Company name :
AI Andalous medical Company
2) Trade name :
Disprelone D Tablets
3) Generic name :
Prednisolone sodium metasulphobenzoate
4) Composition :
a- Active Ingredients: Prednisolone sodium metasulphobenzoate 31.4 mg equivalent to 20mg Prednisolone base.
b- Inactive ingredients: microcrystalline cellulose, lactose, colloidal silicon dioxide, crosscarmellose sodium, magnesium stearate ,cinnamon flavour.
5) Pharmaceutical form :
6) Pharmacological action :
Prednisolone decreases inflammation by suppression of migration of polymorphonuclear leukocytes and reversal of increased capillary permeability, suppress the immune system by reducing activity and volume of the lymphatic system.
7) Pharmacokinetics :
– The peak plasma concentration -by oral route – is reached within 5 hours.
– P rotein binding: 65-91%, decreased in elderly.-
– T he metabolism: Primary hepatic but also metabolized in most tissues, to inactive compounds.
– T he half -life elimination: 3.6 hours,End stage renal disease: 3-5 hours
– B iological half-life: 18-36 hours. – E xcretion is primary urinary.
8) Therapeutic indications :
Rheumatic fever, rheumatoid arthritis and other rheumatic affections, gouty arthritis, psoriasis arthropathica .Severe bronchial asthma. Allergic states of all kinds such as drug sensitivity, transfusion reactions, serum sickness, severe hay fever. Generalized eczema and dermatitis, urticaria, pruritis, lupus erythematosus ,pemphigus, exfoliative dermatitis, dermatomyositis.
Agranulocytosis, thrombocytopenia, hemolytic anemia myeloblastosis , various forms of leukemia, Hodgkin’s disease, inoperable malignant disease (for palliative treatment and to support cytostatic and radiotherapy). Nephrosis, hepatitis, ulcerative colitis, polyarteritis nodosa, encephalitis .Severe infection (to counteract toxic and severe allergic reactions only for short-term therapy and in conjunction with an effective antibiotic and chemotherapeutic cover). Anterior pituitary and adrenal insufficiency.
9)Dosage & Administration :
The dose is variable according to the diagnosis, the severity of the affection, the prognosis, the response of the patient and the tolerance to the treatment.
Initial dose: 10-20 mg (up to 60 mg in severe disease) preferably taken in the morning after breakfast. The dose can be often reduced within a few days, but may need to be continued for several weeks or months. Maintenance usual range: 2.5 -15 mg daily, but higher doses may be needed.
10) Contra lndications :
Glucocorticoids are contraindicated in peptic ulcer. Patients suffering from infectious disease, and particularly tuberculosis require special care. An effective cover of antituberculous drugs should be maintained throughout the period of treatment and for some days after. Diabetic and mentally unbalanced patients
require particularly careful monitoring. Avoid live virus vaccines (serum antibody response diminished).
11 ) Side effects :
Cardiovascular: Cardiomyopathy, CHF, edema, facial edema, hypertension Central nervous system: Convulsions, headache, insomnia, nervousness & psychic disorders.
Dermatologic: Facial erythema, hirsutism, urticaria Endocrine & metabolic: Carbohydrate tolerance decreased, Cushing’s syndrome, diabetes mellitus, growth suppression, hyperglycemia, hypernatremia, hypokalemia & menstrual irregularities
Gastrointestinal: Abdominal distention, increased appetite, indigestion, nausea, pancreatitis, peptic ulcer, ulcerative esophagitis, weight gain Hepatic: LFTs increased (usually reversible) Neuromuscular & skeletal: Arthralgia, fractures, muscle mass decreased, muscle weakness, osteoporosis, tendon rupture, weakness
Ocular: Cataracts, exophthalmus, eyelid edema, glaucoma, intraocular pressure increased, irritation
Miscellaneous: impaired wound healing
12) Drug interactions :
Prednisolone (corticosteroids) increases:
– The adverse effects of acetylcholinestrase inhibitors.
– Cyclosporine concentration.
– Hypokalemic effect of loop and thiazide diuretics.
– Adverse effects of NSAIDs.
– Anticoagulant effect.
– Side effects of vaccines (live organisms)
Prednisolone (corticosteroids) decrease:
– Hypoglycemic effect of antidiabetic agents.
– Therapeutic effect of calcitriol.
– Serum concentration of isoniazid.
– Therapeutic effect of vaccines (dead).
Corticosteroid effect (prednisolone) may be decreased by:
– Bile acid sequestrants.
– Rifamycin derivatives.
Corticosteroid effect (prednisolone) may be increased by:
– Calcium channel blockers.
– Estrogen derivatives.
– Many macrolide antibiotics.
Corticosteroid side effect (prednisolone) may be increased by:
– Quinolone antibiotics.
– Neuromuscular-blocking agent
13)Pregnancy and lactation :
Disprelone -D should not be given during pregnancy or lactation.
14) Precautions and warnings :
Long use of corticosteroids (prednisolone) may lead to adrenal suppression & immune suppression with increased risk to secondary infections. Also long use of corticosteroids (prednisolone) may lead to myopathy & psychotic disturbances.
• Cardiovascular disease: Use with caution in patients with HF; long-term use has been associated with fluid retention and hypertension.
• Diabetes: Use with caution in patients with diabetes mellitus; may alter glucose production/regulation leading to hyperglycemia.
• Gastrointestinal disease: Use with caution in patients with GI diseases (diverticulitis, peptic ulcer, ulcerative colitis) due to perforation risk.
• Hepatic impairment: Use with caution in patients with hepatic impairment, including cirrhosis; long-term use has been associated with fluid retention.
• Myasthenia gravis: Use with caution in patients with myasthenia gravis; exacerbation of symptoms has occurred especially during initial treatment with corticosteroids.
• Myocardial infarction (MI): Use with caution following acute MI; corticosteroids have been associated with myocardial rupture.
• Osteoporosis: Contraindicated in patients with osteoporosis; high doses and/or long-term use of corticosteroids have been associated with increased bone loss and osteoporotic fractures.
• Renal impairment: Use with caution in patients with renal impairment; fluid retention may occur.
• Seizure disorders: Use with caution in patients with a history of seizure disorder; seizures have been reported with adrenal crisis.
• Thyroid disease: Changes in thyroid status may necessitate dosage adjustments; metabolic clearance of corticosteroids increases in hyperthyroid patients and decreases in hypothyroid ones.
15) Package & Storage :
Package: Carton box of 1, 2 or 3 (AUPVC) strips, each strip contains 10 tablets & an inner leaflet
Storage: Store below 25° C in dry place.
16) Information to patients :
-Should be taken after meals or with food or milk to decrease GI effects; increase dietary intake of pyridoxine, vitamin C, vitamin D, folate, calcium, and phosphorus. A diet low in sugars and higher in proteins must be associated.
-The addition of potassium is justified only for high doses treatments, prescribed during long duration or in case of rhythm disorders or associations to a hypokaliemiant treatment.
-Inform prescriber if you are or intend to become pregnant Consult prescriber if breast-feeding.
-If you have diabetes, monitor glucose levels closely (antidiabetic medication may need to be adjusted
-You may be more susceptible to infection (avoid crowds and exposure to infection).
-Inform prescriber if you are experiencing greater-than-normallevels of stress (medication may need adjustment)
-Report promptly any symptom or signs of overdose.
– Keep all medicines out of reach of children.
Manufactured by :
Al Andalous for Pharmaceutical
Industries for Al Andalous medical Company – Egypt