Consumer medicine information

Grisovin

Griseofulvin

BRAND INFORMATION

Brand name

Grisovin

Active ingredient

Griseofulvin

Schedule

S4

 

Consumer medicine information (CMI) leaflet

Please read this leaflet carefully before you start using Grisovin.

What is in this leaflet

This leaflet answers some common questions about GRISOVIN.

It does not contain all the available information.

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

All medicines have risks and benefits. Your doctor has weighed the risks of treating you with GRISOVIN against the benefits it is expected to have for you.

If you have any concerns about this medicine, ask your doctor or pharmacist.

Keep this leaflet with your medicine. You may need to read it again.

What is GRISOVIN

The name of your medicine is GRISOVIN.

GRISOVIN contains the antifungal griseofulvin.

This medicine is available in two strengths: Grisovin 125 mg uncoated tablets and Grisovin 500 mg uncoated tablets.

What is it used for

GRISOVIN is used to treat tinea, a fungal infection.

It is only used when other antifungal treatments, such as tinea creams or powders, have not worked.

GRISOVIN will not work for bacterial or viral infections.

Tinea may occur in the skin of the body, scalp, hair or nails. GRISOVIN works by helping newly formed skin, hair and nails to resist attack by fungi. As the new tissue (keratin) grows, the old infected keratin is cast off. That is why it is important to continue treatment until all the old infected tissue is gone.

Ask your doctor or pharmacist if you have any questions about why GRISOVIN has been prescribed for you. This medicine is available only with a doctor’s prescription.

Before you take it

Before taking GRISOVIN, you must tell your doctor if you:

  • have ever had an allergic reaction to any of the ingredients listed at the end of this leaflet
  • are or may become pregnant
  • are breast-feeding
  • planning to father a child
  • are on a low fat diet
  • have any other health problems, especially liver disease, lupus (systemic lupus erythematosis) or porphyria (a blood disease)

GRISOVIN may reduce the effectiveness of oral contraceptives. Extra contraceptive precautions (e.g. condom) should be used during your treatment and for a month after stopping GRISOVIN.

This medicine may cause birth defects. It must not be used during pregnancy. If you intend to become pregnant, you should delay pregnancy until one month after stopping treatment.

GRISOVIN may cause abnormalities in sperm cells. Men should not father children until at least six months after stopping treatment.

Do not use GRISOVIN if the packaging shows sign of tampering or the seal is broken.

Do not use it after the expiry date printed on the pack has passed. It may have no effect at all, or worse, it may give an entirely unexpected effect if you use after the expiry date.

Taking other medicines

Tell your doctor if you are taking the following medicines:

  • Barbiturates
  • Warfarin
    (an anticoagulant)
  • Oral contraceptives

Tell your doctor or pharmacist if you are taking any other medicines. This includes any that you buy without a prescription from a pharmacy, supermarket or health food shop.

Some medicines may affect the way other's work. Your doctor or pharmacist can tell you what to do when taking GRISOVIN with other medicines.

How to take it

How much to take

The following information lists the usual dose of GRISOVIN.

Adults - The usual dose is 500 mg per day. For nail infections, your doctor may prescribe up to 1000 mg daily until a response is apparent, at which time the dose may be reduced to 500 mg per day.

Children - The usual dose is 10 mg/kg body weight daily, taken in divided doses.

The dose will depend on the type of treatment required for a patient.

Your doctor will decide the number of doses needed each day and how long you will need to take GRISOVIN. These doses may differ from the usual doses shown in this leaflet.

If your dose is different to that described in this leaflet do not change it unless your doctor tells you to.

How to take it

Follow the instructions given by your doctor and pharmacist and read the label carefully.

Ask your doctor or pharmacist if you do not understand the instructions on the box or bottle.

When to take it

GRISOVIN tablets should always be taken after meals. They will work better if some fat is included in the meal (for example milk or ice cream).

You should tell your doctor if you are on a fat reduced diet.

How long to take it

Your doctor will advise you how long you will need to take GRISOVIN.

Generally, hair or skin infections need at least 4 weeks treatment. Infection of the toenails or fingernails may need 6 to 12 months treatment. Treatment should be continued for at least 2 weeks after all signs of the infection have disappeared.

If you forget to take it

If you forget to take GRISOVIN, take it as soon as possible with food.

If it is almost time for your next dose, skip the missed dose, and take the next dose at the usual time.

Do not take a double dose to make up for the missed dose.

If you have trouble remembering to take or give GRISOVIN, ask your pharmacist for some hints.

You should follow all advice from your doctor when being treated with this medicine. This information is not intended to replace your doctor's advice.

If you take too much (overdose)

Telephone your doctor or the Poisons Information Centre (Telephone 131126) for advice or go to Accident and Emergency at the nearest hospital if you think that you or anyone else may have taken too much GRISOVIN. Do this even if there are no signs of discomfort or poisoning. You may need urgent medical attention.

Keep the telephone numbers of these places handy.

There are unlikely to be any serious problems from an overdose of GRISOVIN.

But you must consult your doctor or Poisons Information Centre.

While you are using it

Things you must do

GRISOVIN can increase the sensitivity of the skin to sunlight. Avoid direct sunlight and artificial UV light. When outside, wear protective clothing, hat and sunglasses, and use a sunblock that is at least SPF15.

Oral contraceptives (birth control pills) containing oestrogen may not work properly if you take them while you are taking GRISOVIN. If you are taking oral contraceptives, you should use a different or additional means of birth control while you are this medicine and until one month after stopping treatment.

If you become pregnant while you are taking GRISOVIN tell your doctor.

If you are about to start taking any new medicine, tell your doctor and pharmacist that you are taking GRISOVIN.

Tell your doctor if, for any reason, you have not used this medicine exactly as prescribed. Otherwise, your doctor may think that the medicine was not effective and change your treatment unnecessarily.

Things you must not do

Do not stop taking GRISOVIN until it is finished. Your infection and symptoms may not clear completely.

Do not give your medicine to anyone else even if his or her symptoms seem similar to yours.

Things to be careful of

GRISOVIN may cause some people to feel drowsy or dizzy. Make sure you know how you react to this medicine before you drive a car, use machinery, or do anything else that could be dangerous if you are dizzy or are not alert.

GRISOVIN may increase the effects of alcohol. If taken with alcohol it may also cause fast heartbeat, flushing, increased sweating, or redness of the face. If you have this reaction, do not drink alcoholic beverages without first checking with your doctor.

To avoid reinfection, any clothes, towels, bed linen, shoes, headwear etc. that has come into contact with the affected area, should be cleaned thoroughly or disposed of. Where possible, clothing and linen should be washed with detergent and hot water and dried in the sun. You may use a tinea powder or cream to help reduce the spread of infected clothing and linen.

Side Effects

All medicines, including GRISOVIN, may cause unwanted side effects in some people.

If any of the following side effects are severe or are worrying you, tell your doctor:

  • headache, which may be severe, but usually disappears as treatment is continued
  • tiredness, drowsiness
  • dizziness
  • nausea, vomiting or thirst
  • diarrhoea
  • insomnia (trouble in sleeping)
  • heartburn or flatulence (“wind”)
  • skin rash and skin eruptions

If you have any of the following side effects, tell your doctor as soon as possible, as you may need medical attention:

  • mental confusion
  • skin rash, hives or itching
  • soreness or irritation of the mouth or tongue
  • sore, creamy-yellow, raised patches in mouth
  • numbness, tingling, pain or weakness in hands or feet
  • sore throat and fever
  • yellow eyes or skin
  • swelling in the throat
  • menstrual irregularities

GRISOVIN may cause other side effects not listed above. If you have any other side effects, tell your doctor.

Do not be alarmed by this list of possible side effects. You may not experience any of them.

After using it

Storage

Keep GRISOVIN 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.

Store GRISOVIN tablets in a dry place below 30°C.

Do not leave it in the car or on windowsills. Heat and dampness can destroy some medicines.

Disposal

If your doctor tells you to stop using GRISOVIN or it has passed its expiry date, ask your pharmacist what to do with any left over.

Further Information

This is not all the information that is available on GRISOVIN. If you need more information, ask a doctor or pharmacist.

Product Description

What it looks like

Grisovin 125 mg tablets are a white to off white, scored, uncoated tablet engraved with “G125” on one side, that contains 125 mg of griseofulvin. They are available in bottles of 100 tablets.

Grisovin 500 tablets are a white to off white uncoated tablet engraved with “G500” on one side, that contains 500 mg of griseofulvin. They are available in blister packs of 28 tablets.

List of inactive ingredients

Grisovin 125 mg tablets contain the following inactive ingredients:

  • maize starch
  • povidone
  • sodium lauryl sulfate
  • potato starch
  • magnesium stearate

Grisovin 500 tablets contain the following inactive ingredients:

  • maize starch
  • povidone
  • sodium lauryl sulfate
  • potato starch
  • microcrystalline cellulose
  • magnesium stearate

The Australian Product Registration numbers are:

  • AUST R 12512 for GRISOVIN 125 mg tablets
  • AUST R 157849 for GRISOVIN 500 mg tablets

Sponsor

Aspen Pharmacare Australia Pty Ltd
34-36 Chandos Street
St Leonards NSW 2065
Australia

This leaflet was revised in December 2022.

Published by MIMS February 2023

BRAND INFORMATION

Brand name

Grisovin

Active ingredient

Griseofulvin

Schedule

S4

 

1 Name of Medicine

Griseofulvin.

2 Qualitative and Quantitative Composition

Each Grisovin 125 mg and 500 mg tablet contains either 125 mg or 500 mg of griseofulvin B.P (fine particle).
For the full list of excipients, see Section 6.1 List of Excipients.

3 Pharmaceutical Form

Grisovin "500" mg.

Round, white to off white, biconvex, uncoated tablets engraved with "G500" on one side and on the other.

Grisovin "125" mg.

Round, white to off white, bevel edged tablets engraved with a breakline on one side and "G125" on the other.

4 Clinical Particulars

4.1 Therapeutic Indications

Griseofulvin is indicated in the treatment of fungal infections of the skin, scalp, hair or nails, where topical therapy is considered inappropriate or has failed.
When griseofulvin is given orally for systemic treatment of fungal infections, it enables newly formed keratin of the skin, hair and nails to resist attack by the fungi. As the new keratin extends, the old infected keratin is shed.

4.2 Dose and Method of Administration

Adults.

The usual recommended dosage is 500 mg per day. However, in certain infections higher doses are necessary. For nail infections some patients may require up to 1000 mg daily until a response is apparent, at which time the dose may be reduced to 500 mg per day.

Children.

The usual dose for children is 10 mg/kg bodyweight daily, in divided doses. Doses should be taken after meals, otherwise absorption is likely to be inadequate. Absorption is increased when Grisovin is taken with a high fat meal.

Duration of treatment.

This depends upon the thickness of keratin at the site of infection. For hair or skin at least four weeks treatment is required, whereas toe or fingernails may need six to twelve months treatment. Therapy should be continued for at least two weeks after all signs of infection have disappeared.
Patients on prolonged therapy should be under close observation. Organ system function including renal, hepatic and haemopoietic should be monitored periodically.

General measures.

Customary hygienic measures should be adopted to minimise the risk of reinfection, and concurrent use of a topical fungicide may be helpful to minimise any spread of infective material.
Footwear and, in case of scalp ringworm, headwear, pillows, etc. should be regarded as possible reservoirs of infection.

4.3 Contraindications

Hypersensitivity to any ingredient of the preparation.
Grisovin is contraindicated in pregnancy and in women intending to become pregnant within one month following cessation of treatment. Griseofulvin is teratogenic in animals and some case reports suggest that it produces human foetal abnormalities (see Section 4.4 Special Warnings and Precautions for Use).
Men should not father children within six months of treatment (see Section 4.4 Special Warnings and Precautions for Use).
Griseofulvin is contraindicated in established porphyria and systemic lupus erythematosus.
Severe liver disease, hepatocellular failure. Griseofulvin may cause liver disease to worsen and liver function should be monitored in such conditions.
Prophylactic use of griseofulvin is contraindicated (see Section 4.4 Special Warnings and Precautions for Use).

4.4 Special Warnings and Precautions for Use

Use with caution in the following circumstances.

Concurrent treatment with griseofulvin may reduce the effectiveness of oral contraceptives, so additional non-hormonal contraceptive precautions should be taken during griseofulvin treatment and for a month after stopping griseofulvin.
Since a photosensitivity reaction is occasionally associated with griseofulvin therapy, patients should be warned to avoid exposure to intense natural or artificial sunlight.

Use in the elderly.

No data available.

Paediatric use.

No data available.

Effects on laboratory tests.

No data available.

4.5 Interactions with Other Medicines and Other Forms of Interactions

Barbiturates may reduce the effectiveness of griseofulvin by interference with the gastrointestinal absorption of griseofulvin. The concurrent use of substances such as phenylbutazone and sedative and hypnotic drugs which induce metabolizing enzymes should be avoided as the blood level, and hence efficacy, of griseofulvin may be reduced.
Griseofulvin may decrease the response to coumarin anticoagulants administered concomitantly. Dosage adjustment of the anticoagulant may be required during therapy and after griseofulvin therapy.
Griseofulvin has also been reported to interfere with the efficacy of oral contraceptives. Amenorrhoea, breakthrough bleeding and failure of contraceptive therapy have been reported when griseofulvin has been used concomitantly with oral contraceptives.
Patients should be warned that an enhancement of the effects of alcohol by griseofulvin has been reported.

4.6 Fertility, Pregnancy and Lactation

Effects on fertility.

No data available.
(Category D)
Drugs which have caused, are suspected to have caused or may be expected to cause, an increased incidence of human fetal malformations or irreversible damage. These drugs may also have adverse pharmacological effects. Accompanying texts should be consulted for further details.
Grisovin is contraindicated in pregnancy and in women intending to become pregnant within one month following cessation of treatment. Griseofulvin is teratogenic in animals and some case reports suggest that it produces human foetal abnormalities. As griseofulvin is capable of inducing aneuploidy (abnormal segregation of chromosomes following cell division) in mammalian cells exposed to the compound in vitro and in vivo, women should not take the drug during pregnancy or become pregnant within one month following cessation of treatment (see Section 4.3 Contraindications).
 There is no information available as to whether griseofulvin passes into the breast milk. The safety in children of mothers who are breastfeeding has therefore not been established.

Use in men.

Griseofulvin is capable of inducing aneuploidy (abnormal segregation of chromosomes following cell division) in mammalian cells exposed to the compound in vitro. In the absence of the relevant in vivo data, it is prudent to warn men that they should not father children within six months of treatment.

4.7 Effects on Ability to Drive and Use Machines

The effects of this medicine on a person's ability to drive and use machines were not assessed as part of its registration.

4.8 Adverse Effects (Undesirable Effects)

Among the minor effects, the incidence of which may be as high as 15%, is headache that is sometimes severe and usually disappears as therapy is continued.

Nervous system.

Peripheral neuritis, lethargy, mental confusion, impairment of performance of routine efforts, fatigue, vertigo and drowsiness. In those rare cases where individuals are affected by drowsiness whilst taking griseofulvin, they should not drive vehicles or operate machinery. Patients should be warned that an enhancement of the effects of alcohol by griseofulvin has been reported.

Gastrointestinal tract.

Nausea, vomiting, diarrhoea, heartburn, flatulence, thirst, oral thrush and gastrointestinal bleeding.

Haematological effects.

Include leukopenia and neutropenia; these often disappear despite continuation of therapy. Blood studies should be carried out at least once a week during the first month of treatment or longer. Administration of the drug should be discontinued if granulocytopenia occurs.

Renal effects.

Include albuminuria without evidence of renal insufficiency.
Reactions involving the skin are skin rash, and cold and warm urticaria, photosensitivity, erythema and vesicular and morbilliform eruptions.
Proteinuria, nephrosis, hepatotoxicity and menstrual irregularities have been reported rarely in patients receiving griseofulvin.
Toxic epidermal necrolysis and erythema multiforme have been reported.
Oestrogen-like effects have been observed in children.
The incidence of serious reactions associated with the use of griseofulvin is very low.
Serum sickness syndromes and severe angioedema develop rarely during treatment with griseofulvin.
There have been rare reports of precipitation of systemic lupus erythematosus, occurrence of lupus-like syndromes, or exacerbation of existing lupus in patients receiving griseofulvin.
A moderate but inconsistent increase of faecal protoporphyrins has been noted when the drug is used for a long period of time.
Although the source of griseofulvin is a Penicillium, cross sensitisation of patients to penicillin has not yet been observed.
Candida intertrigo may complicate griseofulvin therapy.

Reporting suspected adverse effects.

Reporting suspected adverse reactions after registration of the medicinal product is important. It allows continued monitoring of the benefit-risk balance of the medicinal product. Healthcare professionals are asked to report any suspected adverse reactions at http://www.tga.gov.au/reporting-problems.

4.9 Overdose

There is no specific antidote. Treatment is unlikely to be required in cases of acute overdoses; however, consider using activated charcoal and contact the Poisons Advisory Centre for further advice.
For information on the management of overdose, contact the Poisons Information Centre on 13 1126 (Australia).

5 Pharmacological Properties

5.1 Pharmacodynamic Properties

Mechanism of action.

Griseofulvin is active in exceedingly low concentrations in vitro against dermatophytes that are the cause of tinea of the hand, feet, nails, body and scalp. This group includes: Epidermophyton floccosum; Microsporum audouinii; Microsporum canis; Microsporum gypseum; Trichophyton concentricum; Trichophyton mentagrophytes; Trichophyton versicolor; Trichophyton rubrum; Trichophyton schoenleinii; Trichophyton sulphureum; Trichophyton tonsurans; Trichophyton verrucosum; Trichophyton violaceum.
The activity in vivo of griseofulvin against this group of fungi is highly specific.
Griseofulvin has no effect on Candida, Cryptococcus, Sporotrichum, Blastomyces, Histoplasma, Coccidioides, Aspergillus, Geotrichum, Malassezia, Phialophora, Saccharomyces, Zygosaccharomyces, other genera of fungi Actinomyces and Nocardia.
Griseofulvin has no antibacterial activity thus oral administration is unlikely to change the gastrointestinal flora.

Clinical trials.

No data available.

5.2 Pharmacokinetic Properties

The absorption of griseofulvin from the gastrointestinal tract is variable and incomplete. On average, less than 50% of the oral dose is absorbed, but fatty foods and a reduction in particle size will increase the rate and extent of the absorption.
After oral dosing there is a phase of rapid absorption followed by slower prolonged absorption. Peak plasma levels (0.5-1.5 microgram/mL after a 500 mg oral dose) are achieved by 4 hours and are maintained for 10-20 hours. The terminal plasma half-life ranges from 9.5-21 hours, there being considerable inter-subject variability. In plasma, griseofulvin is approximately 84% bound to plasma proteins, predominantly albumin.
The absorbed griseofulvin is excreted in the urine mainly as 6-desmethylgriseofulvin or its glucuronide conjugate.
There is selective deposition of griseofulvin in newly formed keratin of hair, nails and skin, which gradually moves to the surface of these appendages.

5.3 Preclinical Safety Data

Genotoxicity.

No data available.

Carcinogenicity and mutagenicity.

Long-term administration of griseofulvin with food has been reported to induce hepatomas in mice and thyroid tumours in rats but not in hamsters. The clinical significance of these findings in man is not known. In view of these data, griseofulvin should not be used prophylactically.

6 Pharmaceutical Particulars

6.1 List of Excipients

Grisovin 125 mg tablets.

Potato starch, povidone, sodium lauryl sulfate, maize starch, magnesium stearate.

Grisovin 500 mg tablets.

Microcrystalline cellulose, potato starch, povidone, sodium lauryl sulfate, maize starch, magnesium stearate.

6.2 Incompatibilities

Incompatibilities were either not assessed or not identified as part of the registration of this medicine.
See Section 4.5 Interactions with Other Medicines and Other Forms of Interactions.

6.3 Shelf Life

In Australia, information on the shelf life can be found on the public summary of the Australian Register of Therapeutic Goods (ARTG). The expiry date can be found on the packaging.

6.4 Special Precautions for Storage

Store below 30°C in a dry place.

6.5 Nature and Contents of Container

Grisovin 500 mg available in a blister strip of 28 tablets.
Grisovin 125 mg available in HDPE bottles of 100 tablets.

6.6 Special Precautions for Disposal

In Australia, any unused medicine or waste material should be disposed of by taking to your local pharmacy.

6.7 Physicochemical Properties

Chemical structure.

Grisovin contains as the active ingredient griseofulvin (fine particle) an antifungal produced by Penicillium griseofulvum and other species of Penicillium. Griseofulvin is stable to heat and in water.
Chemically, griseofulvin is (1'S,6'R)-7-chloro- 2',4,6-trimethoxy- 6'-methylspiro[benzofuran- 2(3H'),1'-[2]cyclohexene]-3,4'-dione.
The structural formula of griseofulvin is:
Molecular formula C17H17ClO6 and molecular weight 352.80.

CAS number.

126-07-8.

7 Medicine Schedule (Poisons Standard)

S4.

Summary Table of Changes