COMPOSITION
Each capsule contains 50mg of Diclofenac Sodium.
One gram of Gel contains 11.5mg of Diclofenac Diethylamine, which is equivalent to 10mg Diclofenac Sodium.
CLINICAL PHARMACOLOGY
Pharmacodynamic Properties:
Diclofenac Sodium is a non- steroidal anti-inflammatory (NSAIDs) agent which has analgesic and anti-pyretic properties. It inhibits prostaglandin synthesis by decreasing the activity of the enzyme cyclo-oxygenase, which results in decreased formation of prostaglandin precursors.
Pharmacokinetic properties:
Diclofenac Sodium Capsule is completely absorbed from the intestinal tract but undergoes first pass metabolism and peak plasma concentration occurs in about 2 to 4 hours; at therapeutic concentrations it is more than 99% bound to plasma proteins. Diclofenac is almost entirely metabolized in the liver and the terminal plasma half-life is about 1-2 hours, with metabolic excretion mainly via the kidneys and also in the bile.
Diclofenac Gel is absorbed through the skin. In healthy volunteers approximately 6% of the dose applied is absorbed, as determined by urinary excretion of Diclofenac and its hydroxylated metabolites.
Findings in patients confirm that Diclofenac penetrates inflamed areas following local application. After topical administration of the gel to hand and knee joints, Diclofenac can be measured in plasma, synovial tissue and synovial fluid
INDICATIONS:
For rheumatoid arthritis; osteoarthritis; low back pain; acute musculo-skeletal disorders and trauma such as periarthritis (especially frozen shoulder), tendonitis, tenosynovitis, bursitis, sprains and dislocations; relief of pain in fractures; ankylosing spondylitis; acute gout; control of pain and inflammation in orthopaedic, dental and other minor surgery.
Diclofenac Gel is used for the local symptomatic relief of pain and inflammation in:
– Trauma of the tendons, ligaments, muscles and joints e. g sprains, strains
and bruises.
– Localized forms of soft tissue rheumatism.
– For the treatment of osteoarthritis of ultrasound and may be used as a
couplant.
CONTRAINDICATIONS:
Hypersensitivity to any of the constituents.
Non steroidal anti-inflammatory drugs (NSAIDs) should not be administered to patients with a history of active peptic ulceration.
NSAIDs are contraindicated in patients who have previously shown hypersensitivity reactions (e.g asthma, rhinitis or urticaria) in response to ibuprofen, aspirin or other non-steroidal anti-inflammatory drugs.
DRUG INTERACTIONS
– The anti-hypertensive effect of anti-hypertensive drugs may be reduced when taken concomitantly with Diclofenac Sodium.
– Increase risk of hemorrhages when non-steroidal anti-inflammatory agents are used in conjunction with anticoagulants has been reported.
– Increased risk of hypoglycemic effect when non steroidal anti-inflammatory agents are used in conjunction with anti diabetic agents.
– Concomitant use of two or more NSAIDs (including aspirin) should be avoided.
– There is an increased risk of GI bleeding when NSAIDs are administered concomitantly with corticosteroids.
– Patients taking NSAIDs and quinolones may have an increased risk of developing convulsions.

WARNINGS/PRECAUTIONS
– Caution is required if administered to patients suffering from, or with a
previous history of bronchial asthma since NSAIDs have been reported
to cause bronchospasm in such patients.
– Patient on long term treatment should be monitored and patients with severe hepatic, cardiac or renal insufficiency should be kept under close surveillance as the use of NSAIDs may result in deterioration of renal function.
– NSAIDs should only be given with care to patients with a history of gastrointestinal disease.
– Diclofenac Gel should not be co-administered with other products
containing Diclofenac.
– Diclofenac Gel should be applied only to intact and not to broken skin or
open wounds.
– It should not be allowed to come into contact with the eyes or mucous membranes and should never be taken by mouth.
PREGNANCY AND LACTATION
Diclofenac Sodium should be used in pregnancy only if the benefits outweigh the risks. Use of Diclofenac Sodium in the last trimester of pregnancy is not recommended as regular use of NSAIDs may result in closure of the fetal ductus arteriosus in utero and possibly persistent pulmonary hypertension of the new-born, delay onset and increase duration of labour.
Diclofenac may be excreted in human milk; use with caution in breastfeeding women.

KEEP OUT OF THE REACH OF CHILDREN
SIDE/ADVERSE EFFECTS:
Gastro-intestinal disorders such as nausea, vomiting, diarrhea, dyspepsia, abdominal pain and gastrointestinal hemorrhages, in some cases exacerbation of existing condition such as ulcerative colitis may occur.
LOCAL REACTIONS: Diclofenac Gel is usually well tolerated but occasionally, there may be allergic or non allergic contact dermatitis (with symptoms and signs such as itching, reddening, oedema, and scaling of skin).
SYSTEMIC REACTIONS: Isolated cases: generalized skin rash, hypersensitivity reactions (e.g. Asthmatic attacks, angio-oedema) and photosensitivity reactions. Avoid excessive exposure to sunlight in other to reduce the incidence of photosensitivity.
SYMPTOMS OF OVERDOSE AND ANTIDOTE
Symptoms include headache, vomiting, drowsiness, dizziness and fainting.
Treatment should be symptomatic and supportive. Gastric lavage and treatment with activated charcoal as soon as possible, to prevent absorption together with symptomatic measures to treat gastro-intestinal irritation and other complications.
DOSAGE AND ADMINISTRATION:
-Analgesia/primary dysmenorrhea: starting dose: 50mg three times daily; maximum dose 150mg/day
-Rheumatoid arthritis: 150-200mg /day in 2- 4 divided doses
-Osteoarthritis: 100 -150mg/day in 2-3 divided doses
Diclofenac Gel should be rubbed gently into the skin. Depending on the size of the affected site to be treated 2-4g(a circular shaped mass approximately 2.0 – 2.5cm in diameter) should be applied 3 -4 times daily.
STORAGE
Store below 300C.
PRESENTATION
Diclofenac Sodium is presented as a 50mg Capsules in a blister of 1 x 10’s and 10 x 10’s per pack.
Diclofenac Gel is available in tube of 20g.