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BIVATE™ Cream: A smooth white glossy cream containing 0.1% w/w betamethasone as the valerate.
BIVATE™ Ointment: A semi-transparent unctuous white ointment containing 0.1% w/w betamethasone as the valerate.
Both Bivate™ cream and ointment contain 0.12%w/w betamethasone-17-valerate, this is equivalent to 0.1%w/w betamethasone.
Betamethasone valerate is a potent topical corticosteroid. Topical corticosteroids have anti-inflammatory, antipruritic and vasoconstrictive actions when administered topically.
Betamethasone is a group II (potent) topical corticosteroid. This classification ranks the potency of topical corticosteroids from I to IV, with I being the most potent. The more potent the topical corticosteroid the greater the efficacy of the preparation, however, this also increases the risk of any systemic side effects associated with the topical absorption of the corticosteroid.
Sufficient corticosteroids may be absorbed through the skin to give rise to systemic side effects. The extent of absorption is determined by many factors including the vehicle, the presence of broken skin and the use of occlusive dressings. Topical corticosteroids can be absorbed through normal intact skin.
The esterification of the betamethasone steroid nucleus at the C17 position with valerate minimises the absorption of the molecule through the skin. This increase the topical potency of the steroid whilst decreasing the possibility of absorption through the skin and any systemic side effects.
It is possible that topically administered betamethasone valerate can produce systemic side effects mimicking those of the orally administered parent compound betamethasone.
Betamethasone has relatively high glucocorticoid activity (anti-inflammatory effects) with insignificant mineralocorticoid activity (effects on the fluid and electrolyte balance). Systemic glucocorticoid effects are described under ADVERSE EFFECTS.
The risk of systemic glucocorticoid effects is significantly less with topically administered betamethasone valerate than with the oral administration of the parent compound (betamethasone). It has been estimated the application of more than 100g of 0.1%w/w betamethasone valerate to the skin in one week is likely to cause adrenal suppression.
The systemic absorption of betamethasone valerate can occur in situations when it is applied to large areas of the body, thin skin, open lesions, or is covered by an occlusive dressing.
Once absorbed through the skin the pharmacokinetics of topical corticosteroids are similar to those of the systemically administered parent compound. Betamethasone valerate is metabolised in the liver to yield the parent compound.
Corticosteroids are bound to plasma proteins in varying degrees, mainly to globulin and to a lesser extent to albumin. Betamethasone is 64% bound to plasma proteins. Only the unbound form of betamethasone valerate has pharmacological effects, or is metabolised.
The half life of orally administered betamethasone is 5.6 hours. Betamethasone is primarily metabolised in the liver, and then excreted via the kidneys, only 5% of betamethasone is excreted unchanged in the urine.
Bivate™ cream and ointment are indicated for the treatment of corticosteroid responsive dermatoses including the conditions:
Eczema including atopic, infantile, stasis and discoid eczemas.
Atopic dermatitis, contact dermatitis, seborrhoeic dermatitis, and contact sensitivity reactions.
Apply sparingly to the affected area two to three times daily until an improvement occurs, then twice daily or less.
If the condition does not improve or worsens, seek further medical advice.
The usual maximum duration of therapy is three weeks.
The use of Bivate™ cream or ointment is contraindicated in the presence of the following conditions:
The use of Bivate™ cream and ointment is not indicated in the treatment of primarily infected skin lesions caused by an infection with fungi or bacteria or in dermatoses in children under one year of age, including dermatitis or napkin eruptions.
Long term continuous topical therapy with topical corticosteriods should be avoided where possible, particularly in children as adrenal suppression can occur even without occlusion of the skin.
As with all topical corticosteroids, when extensive areas are treated sufficient systemic absorption can occur to produce symptoms of hypercorticoticalism. This effect is more likely if occlusive dressings are used, or if the treatment is prolonged.
Rarely, local atrophy or striae may occur after prolonged treatment.
The face or other areas of the body may exhibit atrophic changes after prolonged treatment with potent topical corticosteroids. This must be borne in mind when treating conditions such as severe eczema and seborrhoeic dermatitis. If applied to the eyelids care is needed to ensure that the preparation does not enter the eye, as glaucoma might result. Appropriate antimicrobial therapy should be used whenever treating inflammatory conditions which have been infected.
Any spread of the infection requires withdrawal of topical corticosteroid therapy and the systemic administration of antimicrobial agents.
Bacterial infections are encouraged by the warm, moist conditions induced by occlusive dressings. If an occlusive dressing must be used the skin should be cleansed before a fresh dressing is applied.
To minimise the risk of systemic side effects the least potent corticosteroid which will control the disease should be selected.
In patients where there is an increased risk of systemic absorption should be regularly assessed for evidence of hypothalamic-pituitary-adrenal (HPA) axis suppression by using urinary free cortisol (hydrocortisone) tests and monitoring morning plasma cortisol levels. If there is evidence of suppression attempts should be made to slowly withdrawal the drug, use a less potent steroid or reduce the frequency of application..
Betamethasone containing creams and ointments are usually well tolerated, but if signs of hypersensitivity appear, application should be stopped and appropriate therapy initiated.
In pregnant animals, administration of corticosteroids can cause abnormalities of foetal development. The relevance of this finding to human beings has not been established. However, topical steroids should not be used extensively in pregnancy i.e. in large amounts or for long periods. As with the use of all medications in pregnancy the benefits that the mother may obtain from the use of the product should be weighed up against any harm which may come to the infant.
It is not known whether topical corticosteroids are absorbed sufficiently to be excreted in breast milk. The potential benefit should be weighed up against possible hazards to the nursing infant.
Children have a larger skin surface area to body weight ratio than adults. Hence the risk of systemic absorption/toxicity and HPA axis suppression (after the use of topical corticosteriods) is greater in children than in adults.
HPA axis suppression, Cushing's Syndrome and intracranial hypertension have been reported in children using topical corticosteroids.
The following local adverse reactions have been reported after the use of topical corticosteroids: dryness, itching, burning, skin thinning, local irritation, features of hypercorticalism, telangiectasia, striae, skin atrophy, hypertrichosis, change in pigmentation, secondary infection, perioral dermatitis, allergic contact dermatitis, maceration of the skin, acneform eruptions, exaberation of symptoms. In general creams and ointments containing betamethasone valerate are well tolerated. These reactions are more common with the use of high doses, long term use, and with the use of occlusive dressings.
Systemically administered betamethasone predominantly causes glucocorticoid effects (reduces inflammation etc. ).
Topically administered corticosteroids can be sufficiently absorbed to give rise to systemic side effects.
Systemic glucocorticoid adverse effects include:
Diabetes, osteoporosis, muscle wasting, depression (and paradoxically in some patients euphoria), paranoia, reduced ability to fight infection, Cushing's Syndrome (moon face, hump back, striae, acne - all of which are reversible on withdrawal of treatment), growth suppression in children, HPA axis suppression which may result in adrenal atrophy.
Nil
The percutaneous absorption of corticosteroids can occur when large amounts of corticosteroids are applied or when occlusive dressings are used. Toxic effects may include ecchymosis, peptic ulceration, hypertension, delayed wound healing, decreased resistance to infection, hirsutism, acne, oedema, and muscle weakness.
No specific antidote is available. Treatment should be the slow withdrawal of the drug bearing in mind the possibility of adrenal suppression.
Protect from light and moisture.
Bivate™ Ointment: Store below 30°C.
Bivate™ Cream: Store below 25°C
Keep out of the reach of children.
Prescription Medicine.
Bivate™ Cream: 15g, 30g and 100g tubes
Bivate™ Ointment: 15g, 30g and 100g tubes
Betamethasone-17- valerate is 9a-fluoro-11b, 21-dihydroxy-16b-methyl-3,20 dioxopregna-1,4-dien-17a-yl valerate. The molecular structure and weight of Betamethasone valerate are C27H37FO6 and 476.6 respectively.
Other ingredients are:
Bivate™ Cream: paraffin oil light, cetomacrogol 100, volpo CS6, cetyl alcohol 95%, glyceryl monostearate 400V, caprylic triglyceride, propyl paraben, methyl paraben, citric acid anhydrous, sodium citrate anhydrous, diazolidinyl urea, propylene glycol and water.
Bivate™ Ointment: white soft paraffin and paraffin oil light
7 December, 1998