Consumer medicine information

Loceryl NAIL LACQUER

Amorolfine

BRAND INFORMATION

Brand name

Loceryl Nail Lacquer

Active ingredient

Amorolfine

Schedule

S2

 

Consumer medicine information (CMI) leaflet

Please read this leaflet carefully before you start using Loceryl NAIL LACQUER.

What is in this leaflet

This leaflet answers some common questions about LOCERYL nail lacquer.

It does not take the place of talking to your doctor or pharmacist.

All medicines have risks and benefits. If you have any concerns about using this medicine, ask your doctor or pharmacist.

Keep this leaflet with the medicine.

What LOCERYL is used for

LOCERYL contains the active ingredient amorolfine. It is used to treat fungal infections of the nails.

LOCERYL belongs to a family of medicines called anti-fungal drugs. These medicines work by killing a wide variety of fungi that can cause nail infections.

This medicine is available from a pharmacy. A doctor’s prescription is not required.

LOCERYL treatment alone is not suitable for use in severe infections where the lunula is affected. In this case, you should talk to your healthcare practitioner. The lunula is the crescent-shaped area at the base of the nail – see the illustration on the LOCERYL carton.

Because fungal nail infections are hard to treat, treatment may be required for 6-12 months or longer and a full cure cannot be expected in all cases. After 6 months of treatment, improvement can be expected in 70% to 80% of people, with full cure expected in approximately one in three people.

Before you use LOCERYL

When you must not use it

Do not use LOCERYL if:

  1. you have had an allergic reaction to LOCERYL or any ingredients listed at the end of this leaflet.
  2. the package shows signs of tampering.
  3. the expiry date (EXP) printed on the pack has passed.
  4. you are pregnant or breast-feeding or intend to become pregnant or breast-feed.

The safety of LOCERYL in pregnancy and breast-feeding has not been established.

If you are not sure if you should start using LOCERYL, talk to your doctor or pharmacist.

Use in children.

Do not use in children under 12 years. The safety and effectiveness of LOCERYL in children have not been established.

Before you start to use LOCERYL

Check with your doctor or pharmacist if:

  1. you are allergic to any other medicines, foods, dyes or preservatives.
  2. you have any other health problems.
  3. you are taking any other medicines.

LOCERYL treatment alone is not suitable for use in severe infections where the lunula is affected. In this case, you should talk to your healthcare practitioner. The lunula is the crescent-shaped area at the base of the nail – see the illustration on the LOCERYL carton.

How to use LOCERYL

LOCERYL is for external use only, do not swallow LOCERYL. Apply only to finger nails and toe nails, avoid the surrounding skin.

How to apply the nail lacquer:

Follow these instructions each time the lacquer is used

  1. Place everything you need for the LOCERYL treatment within easy reach:
  • LOCERYL nail lacquer.
  • nail file (supplied).
  • cleaning pad (supplied).
  • reusable spatula (supplied).

First application of LOCERYL:

  1. Before painting with LOCERYL nail lacquer, file down the infected areas of the nail (particularly the nail surfaces) as thoroughly as possible using the nail file.
    CAUTION: Nail files used on an infected nail must not be used on healthy nails.
  1. Clean the surface of the infected nail with a cleaning pad. Put the cleaning pad aside, do not discard.
  1. Dip one of the reusable spatulas into the lacquer. Do not wipe it on the neck of the bottle.
    Note: the spatula provides a measured dose of LOCERYL.
  1. Using the spatula, paint LOCERYL nail lacquer over the entire surface of the infected nail.
  1. When you have finished treating all of your infected nails, clean the spatula and the neck of the bottle with the same cleaning pad that was used during the treatment.
  1. To avoid evaporation, close the bottle tightly.
  1. Allow time for the nails to dry (3 to 5 minutes).
  1. Discard used cleaning pad and nail file. Stow spatula and nail lacquer for next treatment.

Subsequent applications of LOCERYL:
File the infected areas of the nail using the nail file as required to remove any remaining lacquer, ensure that you do not over-file to avoid damage to the nail and surrounding area. Repeat steps 3-9.

How often to apply LOCERYL

Paint LOCERYL once or twice weekly onto the infected fingernails or toenails or as otherwise directed by your doctor or pharmacist.

If you forget to paint on the LOCERYL nail lacquer, use it as soon as you remember. Then go

back to using LOCERYL as you would normally.

How long LOCERYL should be used

Treatment should be continued until the infected nails are completely cured and re-grown.

Usually, treatment of fungal infections of the nails takes around six months for the fingernails

and nine to twelve months for the toenails.

Don’t be discouraged if after several weeks of therapy no improvement is visible. A healthy nail only grows by approximately 2mm per month.

Because fungal nail infections are hard to treat, treatment may be required for 6-12 months or longer and a full cure cannot be expected in all cases. After 6 months of treatment, improvement can be expected in 70% to 80% of people, with full cure expected in approximately one in three people.

If symptoms persist or improvement is not observed, see your doctor or pharmacist.

In case of accidental swallowing

Immediately telephone your doctor or Poisons Information Centre (Australia 13 11 26, New Zealand 0800 POISON or 0800 764 766) for advice or go to Accident and Emergency at your nearest hospital if you think that you or anyone else may have swallowed LOCERYL, even if there are no signs of discomfort or poisoning. You may need urgent medical attention.

While you are using LOCERYL

Things you must do

Tell your doctor or pharmacist that you are using Loceryl if you are about to be started on a new medicine.

Wear gloves to protect the coat of nail lacquer on your fingernails if you work with solvents (e.g. paint thinners, turpentine substitute, petrol, paraffin etc.).

Things you must not do

Do not use nail files for infected nails on healthy nails.

Do not use artificial nails during treatment with LOCERYL.

Do not apply cosmetic nail varnish or other medication(s) on the nail(s) being treated.

Do not give LOCERYL to anyone else to use, even if they have the same condition as you.

Do not use LOCERYL to treat other complaints unless your doctor says to.

Side effects

All medicines can have side effects. LOCERYL helps most people with fungal infections of the nails but it may have unwanted side effects in a few people.

Tell your doctor, or pharmacist if you notice any of the following and they worry you:

  • burning feeling in the area surrounding the treated nail(s). This is usually mild and short-lasting.
  • itching or redness of the skin.
  • rare cases of nail disorder (nail discolouration, brittle or broken nails) have been reported during treatment with LOCERYL nail lacquer. However these reactions may also be linked to the nail infection itself.

After using LOCERYL

Storage

Screw the bottle top of the LOCERYL nail lacquer tightly immediately after use.

Keep LOCERYL in a cool dry place where the temperature stays below 30°C. Heat and dampness can destroy some medicines.

Do not store it, or any other medicine, in a bathroom or near a sink.

Do not leave it in the car or on window sills.

Keep LOCERYL where young children cannot reach it.

A locked cupboard at least one-and-a-half metres above the ground is a good place to store medicines.

Product description

What it looks like

LOCERYL nail lacquer comes in one strength, 5% amorolfine (50 mg/ mL) in an amber glass bottle.

LOCERYL comes in a pack containing:

  • 1 bottle of 2.5mL or 5 mL nail lacquer
  • 10 spatulas
  • 30 cleaning pads saturated with 70%
    Isopropyl alcohol in foil packets
  • 30 nail files

Ingredients

Active - amorolfine Each 2.5mL or 5 mL bottle contains 125mg or 250mg of amorolfine as the hydrochloride.

Inactives - methacrylic acid copolymer, glycerol triacetate, butyl acetate, ethyl acetate, absolute ethanol.

If you require extra nail files or cleaning pads they will be supplied free of charge. In Australia contact Galderma toll free on 1800 800 765.
In New Zealand contact Galderma free-phone on 0800 174 104.

LOCERYL has been clinically tested.

Distributor

Galderma Australia Pty Ltd
13B Narabang Way
Belrose NSW 2085
Australia
Call 1800 800 765 (Australia)

Healthcare Logistics’
58 Richard Pearce Drive
Airport Oaks
Auckland New Zealand
Call 0800 174 104 (New Zealand)

Australian Registration Number: AUST R 57051

Date of preparation of this leaflet, 19 June 2012

BRAND INFORMATION

Brand name

Loceryl Nail Lacquer

Active ingredient

Amorolfine

Schedule

S2

 

Name of the medicine

Amorolfine (as hydrochloride).

Excipients

Lacquer base consisting of methacrylic acid copolymer, glycerol triacetate, butyl acetate, ethyl acetate, ethanol.

Description

Chemical name: cis-4-[(RS)-3-[4-(1, 1-dimethylpropyl)phenyl]- 2-methylpropyl]-2, 6-dimethyl morpholine hydrochloride. Molecular formula: C21H35NO.HCl. MW: 353.98. CAS: 78613-38-4.
Amorolfine hydrochloride is a white to off-white powder, having at most a slight odour. It has a very high lipophilicity with a partition coefficient of > 1,000 in n-octanol buffer (pH 7.5). Amorolfine hydrochloride is slightly soluble in water (932 mg/100 mL at 23°C). It is less soluble in hydrochloric acid due to a common ion effect (solubility 320 mg/100 mL in artificial gastric fluid, pH 1.2 at 37°C). Amorofline hydrochloride is practically insoluble in artificial intestinal juice at pH 7.4. The pKa of amorolfine hydrochloride is 6.6.

Pharmacology

Actions.

Class.

Amorolfine is a topical antimycotic. Amorolfine belongs to a new chemical class. Its fungistatic or fungicidal effect is based on an alteration of the fungal cell membrane targeted primarily on sterol biosynthesis. The ergosterol content is reduced and, at the same time, unusual, sterically nonplanar sterols accumulate.

Site and mode of action.

Amorolfine has a broad spectrum of action. It is effective against the following.

Yeasts.

Candida, Cryptococcus.

Dermatophytes.

Tricophyton, Microsporum, Epidermophyton.

Moulds.

Alternaria, Hendersonula, Scopulariopsis.

Dermatiacea.

Cladosporium, Fonsecaea, Wangiella.

Dimorphic fungi.

Coccidioides, Histoplasma, Sporothrix.
With the exception of some Actinomyces, bacteria are not sensitive to amorolfine. Propionibacterium acnes is only slightly sensitive.
In rats, progressive cataract formation was seen after high oral doses (40 and 60 mg/kg/day in 26 and 13 week studies respectively). Females were more affected than males. In both sexes, further deterioration occurred during the recovery period. Cataract formation also became apparent after 26 weeks in dogs treated orally with 40 mg/kg/day. The mechanism of cataract formation is unknown.
Additional data from a study in pigmented rats with dermal application of amorolfine cream 0.25% indicated neither a direct cataractogenic nor a cocataractogenic potential. The systemic exposure of the rats during this study resulted in plasma concentrations seven to tenfold greater than those expected in humans.

Pharmacokinetics.

Amorolfine from nail lacquer penetrates and diffuses through the nail plate.
In one clinical study, patients being treated for a large number of infected nails tended to have measurable levels of amorolfine between 0.1 and 0.5 nanogram/mL whereas other patients had levels below the level of quantification (0.1 nanogram/mL). In this study, nails were not filed before application of the lacquer. One patient consistently had greater than 0.5 nanogram/mL (maximum 1.05 nanogram/mL).

Clinical Trials

Clinical efficacy of amorolfine has been demonstrated in three main multicentre studies in around 700 patients. The percentage of clinical responders (cure/ improvement) ranged from 70 to 80% in all these studies.
In an open comparative, randomised clinical study conducted in 340 patients with severe infections involving mainly toenails, clinical efficacy has been demonstrated when amorolfine 5% nail lacquer was applied twice weekly in conjunction with griseofulvin 500 mg twice daily for the first two months of a 12 month treatment course. The reduction in treatment with griseofulvin decreased the risk of intolerance to griseofulvin. Clinical efficacy has not been demonstrated in severe onychomycosis (involving the lunula) for amorolfine 5% nail lacquer when used alone.
Data directly comparing efficacy of once versus twice weekly application of Loceryl is not available. Two studies on a related formulation have suggested a slight increase in mycological and clinical cure rates when lacquer was applied twice weekly rather than once weekly, but increases were not statistically significant.

Indications

Onychomycoses caused by dermatophytes, yeasts and moulds.

Contraindications

Reuse by patients who have shown hypersensitivity to the treatment.
Since there are no data on the use of Loceryl in pregnant and lactating women, the use of Loceryl nail lacquer should be avoided during pregnancy and lactation.

Precautions

Occasionally, a slight, transient burning sensation in the area of the nails was observed after application of nail lacquer. The application of lacquer to skin areas surrounding the nails should be avoided.

Use in pregnancy.

(Category B3)
Exposure of pregnant rats and rabbits to systemic amorolfine (≥ 10 mg/kg/day orally) resulted in increased resorptions (embryotoxicity). The significance of these findings to human embryotoxicity is not known. There are no data on the use of amorolfine in pregnant women.

Use in lactation.

In a perinatal and postnatal study in rats, an increased mortality of newborn pups was observed at 10 mg/kg/day orally. There is no information on whether amorolfine passes into human breast milk. There are no data on the use of amorolfine in lactating women.

Use in children

Owing to the lack of clinical experience available to date, children, particularly young children and infants, should not be treated with amorolfine.

Carcinogenicity and genotoxicity.

No animal carcinogenicity studies have been conducted on amorolfine. Amorolfine was not shown to be genotoxic in a standard battery of assays for gene mutations and chromosomal changes.

Adverse Effects

Of the 502 patients treated with amorolfine nail lacquer monotherapy, three (0.6%) experienced local adverse events such as itching and erythema. Of the 172 patients evaluated for safety in the combination group during the monotherapy period, three (1.8%) experienced the following adverse reactions: pruritus and vesicles (one), periungual scaling (one) and nail discolouration (one). In a sensitisation study involving 122 subjects, about one-tenth of patients experienced delayed hypersensitivity skin reactions.
Rare cases of nail disorder (nail discolouration, brittle nails (onychorrhexis) or broken nails) have been reported during treatment with Loceryl nail lacquer. However these reactions may also be linked to the onychomycosis itself.
Very rarely (≤ 1/10000) burning sensation and contact dermatitis.

Dosage and Administration

The patient should apply the nail lacquer to affected fingernails or toenails once or twice weekly. Twice weekly application may be more effective, see Clinical Trials. Application is as follows.
Before the first application of Loceryl Nail Lacquer, it is essential that the affected areas of nail (particularly the nail surfaces) be filed down as thoroughly as possible using the nail file supplied. The surface of the nail should then be cleansed and degreased using a cleaning pad (as supplied). Before repeat application of Loceryl Nail Lacquer, the affected nails should be filed down again as required and, in any case, they must first be cleansed with a cleaning pad to remove any remaining lacquer.

Caution.

Nail files used for affected nails must not be used for healthy nails.
With one of the reusable spatulas supplied, apply the nail lacquer to the entire surface of the affected nails. For each nail to be treated, dip the spatula into the nail lacquer without wiping off any of the lacquer on the bottle neck. After use, clean the spatula as well as the neck of the bottle with the same cleaning pad used before for nail cleaning. Immediately after application, the bottle should be tightly closed. Allow the nails to dry.
When working with organic solvents (e.g. thinners, white spirit) wear impermeable gloves in order to protect the Loceryl lacquer on the nails.
Treatment should be continued without interruption until the nail is regenerated and the affected areas are finally cured. The required duration of treatment depends essentially on the intensity and localisation of the infection. In general, it is six months for fingernails. Longer periods are probably required for toenails.
Cosmetic lacquers, artificial nails or occlusive dressings should not be used during treatment with Loceryl Nail Lacquer.
Because fungal nail infections are hard to treat, treatment may be required for 6-12 months or longer and a full cure cannot be expected in all cases. After 6 months of treatment, improvement can be expected in 70% to 80% of people, with full cure expected in approximately one in three people.
Clinical efficacy has not been demonstrated in severe onychomycosis (involving the lunula) for amorolfine 5% nail lacquer when used alone.

Overdosage

No information is available concerning overdosage in humans.

Presentation

Kit containing nail lacquer, 5%: 2.5 mL or 5 mL plus 30 cleaning pads impregnated with 70% isopropyl alcohol (foil packets), 10 spatulas and 30 nail files.

Storage

Keep in a cool dry place. Store below 30°C.

Poison Schedule

S2.