| Composition |
| Each suppository contains (12.5-25-50-100) mg of Diclofenac sodium. |
| Properties |
Diclofenac is non-steroidal anti-inflammatory, with marked analgesic actions.
It is suitable for use in inflammatory conditions.
It has properties give an adequate activity in the treatment of rheumatic and inflammatory pain. |
| Pharmacokinetics |
Diclofenac100 mg suppositories, the rectal absorption of diclofenac was almost immediate (Tmax 0.62hr and the Cmax was lower but more sustained. The t½ was significantly longer for the suppository).
Following oral or rectal administration, about half the active substance is metabolised during its first passage through the liver ("first pass" effect).
Diclofenac becomes bound to serum proteins to the extent of 99.7%, chiefly to albumin (99.4%). The terminal half-life in plasma is 1 to 2 hours. |
| Therapeutic indications |
– Inflammatory forms of rheumatoid, osteoarthritis, ankylosing spondylitis and sondyloarthritis.
– Non articular forms of rheumatism.
– Post-operative pain and post –traumatic inflammation and swelling.
– Treatment of primary dysmenorrhoea.
– As an adjuvant in severe painful infections of the ear, nose, or throat. |
| Side effect |
Occasionally, gastro-intestinal disorders (gastrointestinal ulcer, gastrointestinal haemorrhage)
headache, dizziness, or vertigo, rash, hypersensitivity reaction. |
| Warnings and precautions |
Gastrointestinal effects: To reduce the risk of GI toxicity in patients with a history of ulcer, particularly if complicated with haemorrhage or perforation, and in the elderly, the treatment should be initiated and maintained at the lowest effective dose.
Gastrointestinal bleeding, ulceration and perforation in general have more serious consequences in the elderly.
They can occur at any time during treatment with or without warning symptoms or a previous history.
This drug should be taken carefully in hypertension patients and Cardiovascular events.
Elevations of one or more of liver enzymes (ALT or AST) may occur during drug therapy.
Physicians should inform patients of the warning signs and symptoms of hepatic damage (e.g., nausea, fatigue, pruritus, jaundice, "flu-like" symptoms).Monitoring of renal function as a precautionary measure is therefore recommended when using this drug in advanced renal disease. |
| Contraindication |
Diclofenac is contraindicated in:
Peptic ulcer, hypersensitivity to the product or other NSAIDs e.g aspirin, and it hould not be taken by asthmatics especially when sensitive symptoms appeared e.g., swelling face, tongue, dyspnea and Proctitis. |
| Pregnancy and lactation |
Use in Pregnancy:
category c: No enough data available to use during pregnancy, this drug and NSAIDs should be avoided during late pregnancy, because it may cause closure of the foetal ductus arteriosus, and delay labour and birth.
Use in Lactation:
Following oral doses of 50 mg administered every 8 hours, the active substance, diclofenac, passes into the breast milk. This drug is not recommended for use in nursing women. |
| Drug interactions |
– Co-administration of diclofenac with aspirin should be avoided.
– Caution should be exercised when diclofenac is administered with methotrexate, anti-coagulants,
and oral antidiabetic agents.
– Combination with preparations containing lithium or digoxin, diclofenac may raise their plasma
concentration. |
| Dosage & administration |
adults:
Initial dosage is 75 to 150 mg daily.
For long-term therapy, 75 to 100 mg daily is usually sufficient.
The daily dosage should generally be prescribed in 2 or 3 fractional doses.
To suppres snocturnal pain and morning stiffness, treatment with tablets during the day can be supplemented by the administration of a suppository at bedtime (up to a maximum daily dose of 150 mg).
In primary dysmenorrhoea the daily dosage, which should be individually adapted, is generally
50 to 150 mg. Initially a dose of 50 to 100 mg should be given and, if necessary,raised in the course of several menstrual cycles up to a maximum of 200 mg/day.
Post-operative analgesia in children (6–12 year):
A first dose of 1–2 mg/kg followed by 1 mg/kg three times daily for a maximum of three days total therapy. The maximum daily dose is 3 mg/kg. |
| Overdose |
Management of acute poisoning with NSAIDS, including diclofenac, consists essentially of supportive measures and symptomatic treatment.
There is no typical clinical picture resulting from an overdosage of diclofenac. Overdosage can cause symptoms such as vomiting, gastrointestinal haemorrhage, diarrhea, dizziness, tinnitus or convulsions.
In the event of significant poisoning, acute renal failure and liver damage are possible.
The therapeutic measures to be taken in cases of overdosage are as follows: Absorption should
be prevented as soon as possible after the overdosage by treatment with activated charcoal.
Supportive and symptomatic treatment should be given for complications such as hypotension, renal failure, convulsions, gastrointestinal disorder, and respiratory depression. Haematological
and biochemical parameters, and the presence or absence of blood in the stools, should be monitored.
Specific therapies such as forced diuresis, dialysis, or haemoperfusion are probably of no help in eliminating NSAIDS. |
| Package |
| 10 Suppositories in two blisters packed in carton box. |
| Storage |
| Store below 25°C. |
