INFORMATION FOR HEALTH PROFESSIONALS
Home | Consumers | Health Professionals | Regulatory | Other | Hot Topics | Search
Home | Consumers | Health Professionals | Regulatory | Other | Hot Topics | Search
The faintly yellowish cream is an oil in water emulsion containing approximately 70% water.
1 g NERISONE C contains 1 mg (0.1 %) diflucortolone valerate and 10 mg (1 %) chlorquinaldol.
Diflucortolone valerate suppresses inflammation in inflammatory and allergic skin conditions and alleviates the subjective complaints, such as itching, burning and pain. Capillary dilatation, intercellular oedema and tissue infiltration regress; capillary proliferation is suppressed. This leads to fading of inflamed skin surfaces.
Chlorquinaldol inhibits the growth of bacteria, yeasts, dermatophytes and moulds.
In order to display its therapeutic effects it is necessary that diflucortolone valerate diffuses out of the formulation into the skin. In vitro investigations with human skin showed a rapid penetration of diflucortolone valerate into the horny layer. Four hours after application of the cream; maximum corticosteroid levels of approx. 500 mcg/ml have been measured in the horny layer. The concentration in the horny layer decreased from distal to proximal by approximately 1.5-2 degrees. After application to stripped skin - as a model for diseased skin -local concentrations in the living skin were distinctly higher than after application to healthy skin.
Diflucortolone valerate is partly hydrolysed in the skin to the likewise effective diflucortolone. The portion of the corticosteroid, which is percutaneously absorbed, is low. Within four hours exposure time, less than 1 % of the topically applied dose have been percutaneously absorbed.
Entering the systemic circulation, diflucortolone valerate is hydrolysed to diflucortolone and the corresponding fatty acid within minutes. Besides diflucortolone 11-keto-diflucortolone and two further metabolites have been detected in the plasma. All metabolites are eliminated from the plasma with half-lives of 4 - 5 hours and approx. 9 hours, respectively (half-lives after iv. injection) and are excreted in a ratio of 75:25 with urine and faeces.
Chlorquinaldol was percutaneously absorbed through intact skin only to a minor extent. It is anticipated that no more than 10 % of the dose become systemically available after application to diseased skin.
After entering the organism, chlorquinaldol is rapidly and nearly exclusively excreted as glucuronide with the urine. Since the conversion of chlorquinaldol in excretable metabolites involves only conjugation and no oxidative reactions, interactions of simultaneously given drug with enzyme of the P450 system seem to be improbable.
Initial and interim treatment of bacterially and/or mycotically infected skin diseases as long as inflammatory concomitant symptoms predominate and in which a cream is indicated. They include:
Eczemas with bacterial and/or mycotic superimposition, such as nummular, seborrhoeic and dyshidrotic eczema; eczema in varicose syndrome (but not directly onto lower limb ulcers); bacterid; eczematid;
Skin infections, such as pyodermia (folliculitis, impetigo), erythrasma;
Dermatomycoses (tinea, candidiasis, pityriasis versicolor).
NERISONE C is also used to prevent the above-mentioned bacterial and fungal infections in inflammatory and allergic skin diseases.
At the beginning of treatment, NERISONE C is applied thinly twice or, perhaps, three times per day. Once the clinical picture has improved, one application per day usually suffices.
Babies and children up to the age of 4 years should not be treated with NERISONE C for longer than three weeks, particularly on skin areas covered by nappies. If the skin dries out too much under protracted use of NERISONE C, a neutral fatty preparation (e.g. NERISONE Ointment or Fatty Ointment) is to be applied additionally or alternately.
Tuberculous or syphilitic processes in the area to be treated; virus diseases (e.g. vaccinia, chickenpox, shingles).
NERISONE C should not be allowed to come into contact with the eyes when being applied to the face. If rosacea or perioral dermatitis is present, NERISONE C must not be applied to the face.
In systemic tolerance studies following repeated dermal and subcutaneous administration the effect of diflucortolone valerate was that of a typical glucocorticoid. It can be derived from these results that no side effects further to those that are typical of glucocorticoids are to be expected following therapeutic use of NERISONE C under extreme conditions such as application over large areas and/or occlusion.
The results from systemic tolerance studies following repeated dermal administration of chlorquinaldol suggest that no systemic effects of this active substance be to be expected in the case of therapy with NERISONE C.
Specific embryotoxicity studies with diflucortolone valerate following subcutaneous and dermal administration led to results typical of glucocorticoids, i.e. following sufficiently high exposure embryolethal and/or teratogenic effects could be induced given the appropriate test systems.
Following dermal administration of the maximum practical dose of chlorquinaldol no embryotoxic/teratogenic effects were observed. Since epidemiological studies have as yet given no indications of embryotoxic effects due to systemic glucocorticoid therapy, no embryotoxic effects are to be expected following the therapeutic use of NERISONE C. However, taking animal-experimental results into consideration, particular care should be taken when prescribing NERISONE C.
In vitro investigations for detection of gene mutations in bacteria and mammalian cells as well as in vitro and/or in vivo examinations for detection of chromosome and gene mutations have not given any indications of a mutagenic potential of diflucortolone valerate or chlorquinaldol.
Specific tumorigenicity studies have not been carried out whether with diflucortolone valerate or with chlorquinaldol. On the basis of the pharmacodynamic action pattern, the lack of evidence of a genotoxic profile, the structural properties and the results of chronic toxicity tests (no indication of proliferative changes), there is no suspicion of a tumorigenic potential of either of the active substances. Since systemically effective immuno-suppressive dosages are not reached after dermal application of NERISONE C, no influence on the occurrence of tumours is to be expected.
According to the results from local tolerance studies following repeated dermal administration of diflucortolone valerate, chlorquinaldol or the combination no dermal changes further to the side-effects already known for topical preparations containing glucocorticoids are to be expected from therapy with NERISONE C.
As a general rule, topical preparations containing corticoids should not be applied during the first trimester of pregnancy. In particular, application to large areas of the body or for prolonged periods must be avoided.
The following reactions may occur when NERISONE C is applied to large areas of the body (about 10 % and more) and/or for long periods of time (more than 4 weeks): local concomitant symptoms such as atrophy of the skin, telangiectasia, striae, acneform changes of the skin, perioral dermatitis, increased growth of body hair (hypertrichosis) and systemic effects of the corticoid due to absorption. In rare cases allergic skin reactions may occur.
Side effects cannot be excluded in neonates whose mothers have been treated extensively or for a prolonged period of time during pregnancy or while lactating (for example, reduced adrenocortical function, when applied during the last weeks of pregnancy).
None so far known.
On the basis of results from acute toxicity studies with diflucortolone valerate, chlorquinaldol and NERISONE C: no acute risk of intoxication is to be expected either after a single dermal application of an overdose (application over a large area under conditions favouring resorption) or even after inadvertent oral intake of a whole package.
Prescription Medicine
Tubes made of pure aluminium, interior wall coated with epoxy resin, and with a polyester-based external coating, fold seal ring is made of polyamide based heat sealable material. The screw cap is made of high-density polyethylene.
Presentation: 15g tubes
White soft paraffin, liquid paraffin, and steryl alcohol, polyoxyl 40
stearate
polyacrylic acid (Carbopol 934), sodium hydroxide, disodium edetate dihydrate,
purified water.
Store all drugs properly and keep them out of reach of children.
Schering NZ Ltd.,
5 William Pickering Drive, Albany
P.O. Box 65-051, Mairangi Bay
AUCKLAND
Telephone: (09) 415-2850
Facsimile: (09) 415-6497
Toll free 0800- 80-45 45
9th December, 1998