INDICATIONS     CONTRA-INDICATIONS     DOSAGE     SIDE-EFFECTS     PREGNANCY     OVERDOSE     IDENTIFICATION     PATIENT INFORMATION

Logo RELIFEN 500 (film coated tablet);
RELIFEN S500 (suspension).

SCHEDULING STATUS:
S3

PROPRIETARY NAMES
(and dosage form):

RELIFEN 500 (film coated tablet);
RELIFEN S500 (suspension).

COMPOSITION:
Relifen 500:
Each tablet contains 500 mg of 4-(6-methoxy-2-naphthyl) butan-2-one (
nabumetone).
Relifen S500: Each 5 mL suspension contains 500 mg nabumetone.
The suspension contains 0,1 % m/v sodium benzoate as preservative.

PHARMACOLOGICAL CLASSIFICATION:
A.3.1 Anti-rheumatics (anti-inflammatory agents).

PHARMACOLOGICAL ACTION:
Relifen is a member of a naphthalene series of synthetic compounds. Relifen has anti-inflammatory, analgesic and anti-pyretic properties but inhibits prostaglandin synthetase poorly and has no uricosuric activity. After oral administration, unaltered Relifen is only rarely detected in the serum as it is extensively metabolised to mainly 6-methoxy-2-naphthyl acetic acid, a more potent inhibitor of prostaglandin synthetase responsible for Relifen’s pharmacological activity. Steady state serum levels of 6-methoxy-2-naphthyl acetic acid are reached in 3 to 4 days with a serum half life of 20 to 23 hours. The absorption of Relifen is not impaired by food, but may be increased by taking it with milk. The main metabolite is distributed to all tissues, excreted in milk but shows no evidence of accumulation. The main method of excretion is via the urinary tract as a glucuronide conjugate of the metabolites.

INDICATIONS:
Relifen
is indicated for the symptomatic treatment of:
Rheumatoid arthritis
Osteo-arthritis/Osteo-arthrosis
Short-term treatment of soft-tissue injuries.

CONTRA-INDICATIONS:
Pregnancy and lactation. Active or recent history of peptic ulceration. History of analgesic induced asthma.
Use in children under the age of 12 years.
Hypersensitivity reactions to Relifen or other nonsteroidal anti-inflammatory drugs.

WARNINGS:
Nabumetone should not be used in patients with severe hepatic impairment and should be used with caution in patients with renal failure.

DOSAGE AND DIRECTIONS FOR USE:
ADULTS:
Rheumatoid Arthritis/Osteo-arthritis:
The recommended daily dosage is 2 tablets or 10 mL suspension (1 g) taken as a single night time dose.

Soft-tissue injuries:
The recommended dose is 2g per day taken in divided doses for a maximum of 7 days.

THE ELDERLY:
Blood levels are higher in elderly patients. In many cases 500 mg may give satisfactory relief.

It is recommended that a dose of 1 g daily should not be exceeded in elderly patients.

The total daily dosage should not exceed 2 g. Patients weighing under 50 kg may be less likely to require dosages beyond 1 g per day. Dosages over 2 g per day have not been studied. The lowest effective dose should be used for chronic treatment.

SIDE-EFFECTS AND SPECIAL PRECAUTIONS:
The incidence of episodes of gastro-intestinal bleeding, and peptic ulceration which have been reported in patients treated chronically with Relifen are low.

Gastro-symptoms including diarrhoea, dyspepsia, abdominal pain, constipation, flatulence, nausea, positive stool guaiac, dry mouth, gastritis, stomatitis and vomiting are the most commonly encountered side-effects.

Central nervous system symptoms such as dizziness, headaches, fatigue, increased sweating, insomnia, nervousness and somnolence have been reported.

Dermatologic reactions such as skin rashes and pruritus have also been reported.

Tinnitus, edema and jaundice may occur.

Hypersensitivity reactions such as bronchospasm and anaphylactoid reactions may occur.

Relifen is highly bound to plasma proteins and patients receiving simultaneous anti-diabetic sulphonylureas, other highly bound sulphonamides and hydantoins should be carefully observed for signs of overdosage to these drugs.

Although Relifen will displace warfarin from its serum protein binding sites in vitro this has little or no effect in vivo, but patients should be monitored for idiosyncratic reactions.

KNOWN SYMPTOMS OF OVERDOSAGE AND PARTICULARS OF ITS TREATMENT:
There are no specific known symptoms of overdosage. There is no specific antidote. Treatment is by gastric lavage and appropriate supportive therapy.

IDENTIFICATION:
Relifen 500: Dark red, film coated pillow shaped tablets engraved “RELIFEN”on one side and “500” on the other.
Relifen S500: A white to off-white suspension.
PRESENTATION:
Relifen 500 High density polyethylene bottles containing 60 tablets or blister packaging in strips of 10 tablets.
Relifen S500: High density polythene bottles containing 100 mL suspension.
STORAGE INSTRUCTIONS:
Store in a cool dry place (below 25°C) and protect from light.
KEEP OUT OF REACH OF CHILDREN.

REGISTRATION NUMBERS:
Relifen 500: R/3.1/265
Relifen S500: W/3.1/259
NAME AND BUSINESS ADDRESS OF THE APPLICANT:
SmithKline Beecham Pharmaceuticals (Pty) Ltd.
6 Carey Street, Wynberg Ext. 6,
Johannesburg 2090.

DATE OF PUBLICATION OF THIS PACKAGE INSERT:
15.12.1992

Relifen and the SB logo are trademarks.

        P1196

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