Grisoral

Grisoral Uses, Dosage, Side Effects, Food Interaction and all others data.

Grisoral is fungistatic, however the exact mechanism by which it inhibits the growth of dermatophytes is not clear. It is thought to inhibit fungal cell mitosis and nuclear acid synthesis. It also binds to and interferes with the function of spindle and cytoplasmic microtubules by binding to alpha and beta tubulin. It binds to keratin in human cells, then once it reaches the fungal site of action, it binds to fungal microtubes thus altering the fungal process of mitosis.

Grisoral is a mycotoxic metabolic product of Penicillium spp. It was the first available oral agent for the treatment of dermatophytoses and has now been used for more than forty years. Grisoral is fungistatic with in vitro activity against various species of Microsporum Epidermophyton, and Trichophyton. It has no effect on bacteria or on other genera of fungi. Following oral administration, griseofulvin is deposited in the keratin precursor cells and has a greater affinity for diseased tissue. The drug is tightly bound to the new keratin which becomes highly resistant to fungal invasions. Once the keratin-Grisoral complex reaches the skin site of action, it binds to fungal microtubules (tubulin) thus altering fungal mitosis.

Trade Name Grisoral
Availability Prescription only
Generic Griseofulvin
Griseofulvin Other Names Amudane, Griseofulvin, Griseofulvina, Griséofulvine, Griseofulvinum
Related Drugs clotrimazole topical, ketoconazole topical, terbinafine, itraconazole, miconazole topical, Lamisil, ciclopirox topical, Jublia, Penlac, Sporanox
Type Tablet
Formula C17H17ClO6
Weight Average: 352.766
Monoisotopic: 352.071365983
Groups Approved, Investigational, Vet approved
Therapeutic Class Other Antifungal preparations
Manufacturer Bal Pharma Limited
Available Country India
Last Updated: September 19, 2023 at 7:00 am
Grisoral
Grisoral

Uses

Major indications for griseofulvin are:

  • Tinea capitis (ringworm of the scalp)
  • Tinea corporis (ringworm of the body)
  • Tinea pedis (athlete's foot)
  • Tinea unguium (onychomycosis; ringworm of the nails)
  • Tinea cruris (ringworm of the thigh)
  • Tinea barbae (barber's itch)

Grisoral inhibits the growth of those genera of fungi that commonly cause ringworm infections of the hair, skin, and nails, such as:

  • Trichophyton rubrum
  • Trichophyton tonsurans
  • Trichophyton mentagrophytes
  • Trichophyton interdigitalis
  • Trichophyton verrucosum
  • Trichophyton sulphureum
  • Trichophyton schoenleini
  • Microsporum audouini
  • Microsporum canis
  • Microsporum gypseum
  • Epidermophyton floccosum
  • Trichophyton megnini
  • Trichophyton gallinae
  • Trichophyton crateriform

Note: Prior to therapy, the type of fungi responsible for the infection should be identified. The use of the drug is not justified in minor or trivial infections which will respond to topical anti-fungal agents alone.

Grisoral is also used to associated treatment for these conditions: Tinea Capitis, Tinea Corporis, Tinea Cruris, Tinea Pedis, Tinea Unguium, Tinea barbae

How Grisoral works

Grisoral is fungistatic, however the exact mechanism by which it inhibits the growth of dermatophytes is not clear. It is thought to inhibit fungal cell mitosis and nuclear acid synthesis. It also binds to and interferes with the function of spindle and cytoplasmic microtubules by binding to alpha and beta tubulin. It binds to keratin in human cells, then once it reaches the fungal site of action, it binds to fungal microtubes thus altering the fungal process of mitosis.

Dosage

Grisoral dosage

Accurate diagnosis of the infecting organism is essential. Identification should be made either by direct microscopic examination of a mounting of infected tissue in a solution of potassium hydroxide or by culture on an appropriate medium.

Medication must be continued until the infecting organism is completely eradicated as indicated by appropriate clinical or laboratory examination. Representative treatment periods are tinea capitis, 4 to 6 weeks; tinea corporis, 2 to 4 weeks; tinea pedis, 4 to 8 weeks; tinea unguium- depending on rate of growth- fingernails, at least 4 months; toenails, at least 6months.

General measures in regard to hygiene should be observed to control sources of infection or reinfection. Concomitant use of appropriate topical agents is usually required, particularly in treatment of tinea pedis since in some forms ofathlete's foot, yeasts and bacteria may be involved. Grisoral will not eradicate the bacterial or monilial infection.

Adults:A daily dose of 500 mg will give a satisfactory response in most patients with tinea corporis, tinea cruris, and tinea capitis. For those fungus infections more difficult to eradicate such as tinea pedis and tinea unguium, a daily dose of 1.0gmis recommended.

Children: Approximately 5 mg per pound of body weight per day is aneffective dosefor most children. On this basis the following dosage schedule for children is suggested:

  • Children weighing 30 to 50 pounds:125 mg to 250 mg daily.
  • Children weighing over 50 pounds:250 mg to 500 mg daily.

Should be taken with food. Take immediately after meals.

Side Effects

When adverse reactions occur, they are most commonly of the hypersensitivity type such as skin rashes, urticaria and rarely, angioneurotic edema or erythemamultiforme-like drug reaction, and may necessitate withdrawal of therapy and appropriate countermeasures. Paresthesias of the hands and feet have been reported rarely after extended therapy. Other side effects reported occasionally are oral thrush, nausea, vomiting, epigastric distress, diarrhea, headache, fatigue, dizziness, insomnia, mental confusion and impairment of performance of routine activities.

Proteinuria and leukopenia have been reported rarely. Administration of the drug should be discontinued if granulocytopenia occurs. When rare, serious reactions occur with griseofulvin, they are usually associated with high dosages, long periods of therapy, or both.

Toxicity

Side effects are minor: headaches, gastrointestinal reactions and cutaneous eruptions

Precaution

Patients on prolonged therapy with any potent medication should be under close observation. Periodic monitoring of organ system function, including renal, hepaticand hemopoietic, should be done.

Since griseofulvin is derived from species of penicillin, the possibility of cross sensitivity with penicillin exists; however, known penicillin-sensitive patients have been treated without difficulty.

Since a photosensitivity reaction is occasionally associated with griseofulvin therapy, patients should be warned to avoid exposure to intense natural or artificial sunlight. Should a photosensitivity reaction occur, lupus erythematosus may be aggravated.

Interaction

Patients on warfarin-type anticoagulant therapy may require dosage adjustment of the anticoagulant during and after griseofulvin therapy. Concomitant use of barbiturates usually depresses griseofulvin activity and may necessitate raising the dosage.

The concomitant administration of griseofulvin has been reported to reduce the efficacy of oral contraceptives and to increase the incidence of breakthrough bleeding.

Food Interaction

  • Avoid alcohol.
  • Take with a high fat meal.

[Moderate] MONITOR: Isolated case reports have suggested that the ingestion of alcohol during griseofulvin therapy may rarely cause disulfiram-like reactions, flushing, tachycardia, or increased effects of alcohol.

The mechanism is unknown.

MANAGEMENT: Patients should be advised of the possibility of increased adverse effects or a disulfiram-like reaction.

Elimination Route

Poorly absorbed from GI ranging from 25 to 70% of an oral dose. Absorption is significantly enhanced by administration with or after a fatty meal.

Half Life

9-21 hours

Pregnancy & Breastfeeding use

Pregnancy Category C. Either studies in animals have revealed adverse effects on the foetus (teratogenic or embryocidal or other) and there are no controlled studies in women or studies in women and animals are not available. Drugs should be given only if the potential benefit justifies the potential risk to the foetus.

Contraindication

This drug is contraindicated in patients with porphyria, hepatocellular failure, and in individuals with a history of hypersensitivity to griseofulvin.

Two cases of conjoined twins have been reported in patients taking griseofulvin during the first trimester of pregnancy. Grisoral should not be prescribed to pregnant patients.

Storage Condition

Store between 15-30° C.

Innovators Monograph

You find simplified version here Grisoral

Grisoral contains Griseofulvin see full prescribing information from innovator Grisoral Monograph, Grisoral MSDS, Grisoral FDA label

FAQ

What is Grisoral used for?

Grisoral is an antifungal medicine that is used to treat infections such as ringworm, athlete's foot, jock itch, and fungal infections of the scalp, fingernails, or toenails. Grisoral may also be used for purposes not listed in this medication guide. Grisoral used to treat a number of types of dermatophytoses. This includes fungal infections of the nails and scalp, as well as the skin when antifungal creams have not worked.

How safe is Grisoral?

All five drugs appear relatively safe, however, only Grisoral has a long track record of safety, is Food and Drug Administration (FDA) approved for the treatment of tinea capitis in children, and has the least known drug interactions.

How does Grisoral work?

Grisoral works to interfere with fungal mitosis by preventing fungal cells from dividing and multiplying, ultimately causing the infection to die off. By clearing the infections and fungus, symptoms such as itching, red, peeling, scaly skin, and discolored nails will subside.

What are the common side effects of Grisoral?

Common side effects of Grisoral are include:

  • headache.
  • upset stomach.
  • vomiting.
  • diarrhea or loose stools.
  • thirst.
  • fatigue.
  • dizziness.
  • faintness.

Is Grisoral safe during pregnancy?

Grisoral should never be used during pregnancy.

Is Grisoral safe during breastfeeding?

Grisoral may pass into breast milk and cause side effects in a child who is breastfed. Talk to your doctor if you breastfeed your child. You may need to decide whether to stop breastfeeding or stop taking this medication.

Can I drink alcohol with Grisoral?

Grisoral 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 these symptoms, do not drink alcoholic beverages while you are taking this medicine, unless you have checked first with your doctor.

What is the best time to take Grisoral?

Grisoral is best taken with or after meals, especially fatty ones (e.g., whole milk or ice cream). This lessens possible stomach upset and helps to clear up the infection by helping your body absorb the medicine better. However, if you are on a low-fat diet, check with your doctor.

How many time can I take Grisoral daily?

Grisoral is usually taken once a day or can be taken two to four times a day.

How long does Grisoral take to work?

Grisoral usually takes about two to four weeks for skin infections and four to six weeks for hair and scalp infections to be completely gone.

How long does Grisoral take to work?

Half the medication is cleared from the blood stream in 10 to 20 hours; the rest is eliminated in urine and faeces. This means the medication can be taken once daily.

When should I stop taking Grisoral?

This Grisoral can cause skin reactions. These may be serious and life threatening. Symptoms can include hives, fever, swelling of your tongue and face, and peeling or blistering of your skin. If you have signs of a skin reaction, stop taking the drug and call your doctor right away.

How long can I take Grisoral?

Grisoral is usually taken for 2 to 4 weeks for skin infections, 4 to 6 weeks for hair and scalp infections, 4 to 8 weeks for foot infections, 3 to 4 months for fingernail infections, and at least 6 months for toenail infections.

Can Grisoral cause liver damage?

This Grisoral can cause serious liver damage.

Who should not take Grisoral?

You should not use Grisoral if you have porphyria or liver failure. Taking Grisoral during the first 3 months of pregnancy may harm the unborn baby.

What happens if I miss a dose?

Take the medicine as soon as you can, but skip the missed dose if it is almost time for your next dose. Do not take two doses at one time.

Can I overdose on Grisoral?

The likely symptoms of any overdose would be nausea, nomiting, headache, numbness and tingling, confusion, and vertigo. Urticaria or porphyria could occur. Treatment: There is no specific antidote to Grisoral.

What happen If I stop taking Grisoral?

If you stop taking the drug suddenly or don't take it at all: Your infection will continue to grow. It may also spread to other parts of your body.

Will Grisoral affect my fertility?

Grisoral is contraindicated in pregnancy (class C). As Grisoral induces abnormalities in murine sperm, fertile men should be advised not to father children during therapy or for six months after the drug is stopped.

Can Grisoral affects my heart ?

It may be inferred from these experiments that Grisoral has a direct action on the cardiovascular system rather than one mediated through neurogenic or hormonal mechanisms. 

*** Taking medicines without doctor's advice can cause long-term problems.
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