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PRESCRIBING INFORMATION
For the use of a Registered Medical Practitioner only

Difnal OD
(Diclofenac Sodium Sustained Release Tablets 100 mg)

WARNING

CARDIOVASCULAR RISK
NSAIDs may cause an increased risk of serious cardiovascular thrombotic events, myocardial infarction, and stroke, which can be fatal. This risk may increase with duration of use. Patients with cardiovascular disease or risk factors for cardiovascular disease may be at greater risk.

Diclofenac sodium is contraindicated for the treatment of perioperative pain in the setting of coronary artery bypass graft (CABG) surgery.

RISK OF GI ULCERATION, BLEEDING AND PERFORATION WITH NSAID
Serious GI toxicity such as bleeding, ulceration and perforation can occur at any time, with or without warning symptoms, in patients treated with NSAID therapy. Although minor upper GI problems (e.g. dyspepsia) are common, usually developing early in therapy, prescribers should remain alert for ulceration and bleeding in patients treated with NSAIDs even in the absence of previous GI tract symptoms.

Studies to date have not identified any subset of patients not at risk of developing peptic ulceration and bleeding. Patients with prior history of serious GI events and other risk factors associated with peptic ulcer disease (e.g. alcoholism, smoking, and corticosteroid therapy) are at increased risk. Elderly or debilitated patients seem to tolerate ulceration or bleeding less than other individuals and account for most spontaneous reports for fatal GI events.

Composition:
Each film-coated sustained release tablet contains
Diclofenac sodium 100 mg

Excipients: Lactose, Hydroxypropyl Methylcellulose (Methocel-K 100MCR), Hydroxypropyl Cellulose (HPC-L), Sodium Lauryl Sulphate, Colloidal Silicon Dioxide, Purified Talc, Magnesium stearate, Hydroxypropyl Methylcellulose, Titanium Dioxide, Ponceau 4R Lake, Polyethlene Glycol-400, Purified Water

PRODUCT DESCRIPTION
Pink coloured, round biconvex, film coated tablets.

DESCRIPTION
DIFNAL OD contains diclofenac sodium which is a benzene-acetic acid derivative. Diclofenac sustained release tablets have prolonged release profile. The chemical name is 2-[(2,6-dichlorophenyl)amino] benzeneacetic acid, monosodium salt. The molecular weight is 318.14. Its molecular formula is C14H10CI2NNaO2, and it has the following structural formula:


PHARMACODYNAMIC AND PHARMACOKINETIC PROPERTIES
• Pharmacodynamics
Mechanism of action
Diclofenac sodium is a non-steroldal compound with pronounced antlrheumatic, anti-inflammatory, analgesic and antipyretic properties. Inhibition of prostaglandin biosynthesis, which has been demonstrated in experiments, is considered fundamental to its mechanism of action. Prostaglandins play a major role in causing inflammation, pain and fever. Diclofenac sodium in vitro does not suppress proteoglycan biosynthesis in cartilage at concentrations equivalent to those reached in humans.

Pharmacodynamic effects
In rheumatic diseases, the anti-inflammatory and analgesic properties of diclofenac sodium elicit a clinical response characterised by marked relief from signs and symptoms such as pain at rest, pain on movement, morning stiffness, and swelling of the joints, as well as by an improvement in function.

In post-traumatic and post-operative inflammatory conditions, diclofenac sodium relieves both spontaneous pain and pain on movement and reduces inflammatory swelling and wound edema. The possibility of prescribing the medicinal product in a single daily dose considerably simplifies long-tern treatment and helps to avoid the possibility of dosage errors.

• Pharmacokinetics
Absorption
Judged by urinary recovery of unchanged diclofenac and its hydroxylated metabolites, the same amount of diclofenac is released and absorbed from Diclofenac sodium SR tablets as from enteric-coated tablets. However, the systemic availability of diclofenac from Diclofenac sodium SR tablets is on average about 82% of that achieved with the same dose of diclofenac sodium enteric-coated tablets (possibly due to release-rate dependent "first-pass" metabolism). As a result of a slower release of the active substance from Diclofenac sodium SR tablets, peak concentrations attained are lower than those observed following the administration of gastro-resistant tablets.

Mean peak concentrations of 0.5 micrograms/mL or 0.4 micrograms/mL (1.6 or 1.25 micro mol/L) are reached on average 4 hours after ingestion of a prolonged-release tablet of 100 mg or 75 mg. Food has no clinically relevant influence on the absorption and systemic availability of Diclofenac sodium SR tablets.

On the other hand, mean plasma concentrations of 13 ng/mL (40 nmol/L) can be recorded at 24 hours (16 hours) after administration of prolonged-release tablet of 100 mg (75 mg). The amount absorbed is linearly related to the dose strength.

Since about half of diclofenac is metabolised during its first passage through the liver ("first pass" effect), the area under the concentration curve (AUC) following oral or rectal administration is about half that following en equivalent parenteral dose.

Pharmacokinetic behaviour does not change after repeated administration. No accumulation occurs provided the recommended dosage intervals are observed.

Trough concentrations are around 22 ng/mL or 25 ng/mL (70 nmol/L or 80 nmol/L) during treatment with Diclofenac sodium prolonged-release tablets 100 mg once dally or 75 mg twice daily.

Distribution
99.7% of diclofenac is bound to serum proteins, mainly to albumin (99.4%). The apparent volume of distribution calculated is 0.12 to 0.17 L/kg. Diclofenac enters the synovial fluid, where maximum concentrations are measured 2 to 4 hours after peak plasma values have been attained. The apparent half-life for elimination from the synovial fluid is 3 to 6 hours. Two hours after reaching peak plasma values, concentrations of the active substance are already higher in the synovial fluid than in the plasma, and they remain higher for up to 12 hours.

Biotransformation
Biotransformation of diclofenac takes place partly by glucuronidation of the intact molecule, but mainly by single and multiple hydroxylation and methoxylation, resulting in several phenolic metabolites (3'-hydroxy-,4'-hydroxy-,5-hydroxy-,4',5-dihydroxy-and 3'-hydroxy-4'-methoxy-diclofenac), most of which are converted to glucuronide conjugates. Two of these phenolic metabolites are biologically
active, but to a much smaller extent Than diclofenac.

Elimination
Total systemic clearance of diclofenac from plasma is 263 ±56 mL/min (mean value ±SD). The terminal half-life in plasma is 1 to 2 hours. Four of the metabolites, including the two active ones, also have short plasma half-lives of 1 to 3 hours. One metabolite, 3'-hydroxy-4'-methoxy-diclofenac has a much longer plasma half-life. However, this metabolite is virtually inactive.

About 60% of the administered dose is excreted in the urine as the glucuronide conjugate of the intact molecule and as metabolites, most of which are also converted to glucuronide conjugates. Less than 1% is excreted as unchanged substance. The rest of the dose is eliminated as metabolites through the bile in the feces.

Elderly
No relevant age-dependent differences in the drug's absorption, metabolism or excretion have been observed.

Renal impairment
In patients suffering from renal impairment, no accumulation of the unchanged active substance can be inferred from the single-dose kinetics when applying the usual dosage schedule. At a creatinine clearance of <10 mL/min, the calculated steady-state plasma levels of the hydroxy metabolites are about 4 times higher than in normal subjects. However, the metabolites are ultimately cleared through the bile.

Hepatic impairment
In patients with chronic hepatitis or non-decompensated cirrhosis, the kinetics and metabolism of diclofenac are the same as in patients without liver disease.

 

INDICATIONS
Treatment of:
• Inflammatory and degenerative forms of rheumatism: rheumatoid arthritis, ankylosing spondylitis, osteoarthritis and spondylarthritis, painful syndromes of the vertebral column, non-articular rheumatism.

• Painful post-traumatic and post-operative inflammation and swelling.

• Primary dysmenorrhoea.

 

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