(and dosage form):
Contains metronidazole 7,5 mg per g, preserved with methylparaben 0,08% (m/m) and propylparaben 0,02% (m/m).
A 13.4.2 Dermatologicals - Other.
Metronidazole is an antiprotozoal and antibacterial agent which is active against a wide range of pathogenic micro-organisms. The mechanism of action in rosacea is unknown but is apparently not due to an antiparasitic effect on the mite Demodex folliculorum, found in hair follicles and sebaceous secretions, or to any effect on sebum production. Topical metronidazole may have an antioxidant effect. It has been shown to significantly reduce the concentrations of neutrophil-generated reactive oxygen species, hydroxyl radicals and hydrogen peroxide which are potent oxidants capable of causing tissue injury at the site of inflammation. Topical metronidazole may also have an effect on neutrophil cellular functions partly attributable to a direct anti-inflammatory effect.
Metronidazole is rapidly and nearly totally absorbed after oral administration. The agent is not significantly bound to serum proteins and distributes well to all body compartments with the lowest concentration found in the fat. Metronidazole is excreted primarily in the urine as parent agent, oxidative metabolites and conjugates. Bioavailability studies with ROZEX Gel in rosacea patients treated with 7,5 mg metronidazole applied topically to the face resulted in maximum serum concentrations of 66 nanograms per mL which is approximately 100 times less than those attained after a single oral dose of 250 mg. In most patients at most time points after ROZEX Gel application, serum concentrations of metronidazole were below the detectable limits of the assay (25 ng/mL).
ROZEX Gel is indicated for the treatment of inflammatory papules, pustules and erythema of rosacea.
ROZEX Gel has been reported to cause tearing of the eyes, therefore contact with the eyes should be avoided. If a reaction suggesting local irritation occurs, patients should be directed to use the medication less frequently, discontinue use temporarily or discontinue use until further instructions. Metronidazole is a nitroimidazole and should be used with care in patients with evidence of, or history of, blood dyscrasia.
ROZEX topical gel is contra-indicated in individuals with a history of hypersensitivity to metronidazole, parabens or other ingredients of the formulation.
Use in pregnancy and lactation: Metronidazole crosses the placental barrier and rapidly enters the foetal circulation. There is inadequate evidence of the safety of metronidazole in pragnancy.
Metronidazole is excreted in breast milk.
DOSAGE AND DIRECTIONS FOR USE:
For topical administration only. Adults: Apply and rub a thin film of ROZEX Gel twice daily, morning and evening, to entire affected areas after washing. Elderly: The dosage recommended in the elderly is the same as that recommended in adults. Children: Not recommended.
SIDE-EFFECTS AND SPECIAL PRECAUTIONS:
Because of the minimal absorption of metronidazole and consequently its insignificant plasma concentration after topical administration, the adverse experiences reported with the oral form of the agent have not been reported with ROZEX topical gel. Adverse reactions reported with ROZEX Gel include watery (tearing) eyes if the gel is applied too closely to this area, transient redness and mild dryness, burning and skin irritation.
Interactions with other medicines: Medicine interactions are less likely with topical administration but should be kept in mind when ROZEX Gel is prescribed for patients who are receiving anticoagulant treatment. Oral metronidazole has been reported to potentiate the anticoagulant effect of coumarin and warfarin resulting in a prolongation of prothrombin time.
KNOWN SYMPTOMS OF OVERDOSAGE AND PARTICULARS OF ITS TREATMENT:
There is no human experience with overdosage of ROZEX Gel. The acute oral toxicity of the ROZEX Gel is more than 5 g/kg (the highest dose given) in albino rats.
A clear, colourless to light yellow, viscous gel.
ROZEX Gel is packed in lined aluminium tubes containing 30 g gel.
Store at room temperature below 25°C, away from direct heat. Avoid exposure to temperatures below 4°C.
KEEP OUT OF REACH OF CHILDREN. FOR EXTERNAL USE ONLY.
NAME AND BUSINESS ADDRESS OF THE APPLICANT:
Alcon Laboratories (SA) (Pty) Ltd
DATE OF PUBLICATION OF THIS PACKAGE INSERT:
PROZ01 - 07/96
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