What is griseofulvin used to treat. How should griseofulvin be taken. What are the potential side effects of griseofulvin. What precautions should be followed when taking griseofulvin.

Understanding Griseofulvin: A Powerful Antifungal Medication

Griseofulvin is a widely prescribed antifungal medication used to treat various fungal infections affecting the skin, hair, and nails. This powerful drug, pronounced as (gri see oh ful’ vin), has been a staple in dermatological treatments for decades. But what exactly does griseofulvin treat, and how does it work?

Primary Uses of Griseofulvin

Griseofulvin is primarily used to treat the following conditions:

• Jock itch
• Athlete’s foot
• Ringworm
• Fungal infections of the scalp
• Fingernail infections
• Toenail infections

These infections are caused by dermatophytes, a group of fungi that thrive on keratin, a protein found in skin, hair, and nails. Griseofulvin works by inhibiting the growth of these fungi, allowing the body to naturally eliminate the infection over time.

Dosage and Administration: How to Take Griseofulvin Effectively

Griseofulvin comes in various forms, including tablets, capsules, and liquid. The dosage and duration of treatment depend on the type and severity of the infection. How often should griseofulvin be taken? It’s typically administered once daily or divided into two to four doses throughout the day.

Treatment Duration for Different Infections

The duration of griseofulvin treatment varies depending on the infection:

• Skin infections: 2 to 4 weeks
• Hair and scalp infections: 4 to 6 weeks
• Foot infections: 4 to 8 weeks
• Fingernail infections: 3 to 4 months
• Toenail infections: At least 6 months

Why does the treatment duration vary so much? The answer lies in the growth rate of different body tissues. Nails, especially toenails, grow much slower than skin, requiring a longer treatment period to ensure complete eradication of the fungal infection.

Potential Side Effects and Risks of Griseofulvin

Like all medications, griseofulvin can cause side effects. While many people tolerate the drug well, it’s essential to be aware of potential adverse reactions. What are the most common side effects of griseofulvin?

• Headache
• Upset stomach
• Vomiting
• Diarrhea or loose stools
• Thirst
• Fatigue
• Dizziness
• Faintness

Most of these side effects are mild and tend to subside as your body adjusts to the medication. However, there are some more serious side effects that require immediate medical attention. These include:

• Fever
• Sore throat
• Skin rash
• Mouth soreness or irritation

If you experience any of these severe symptoms, it’s crucial to contact your healthcare provider immediately. They may need to adjust your dosage or switch you to an alternative treatment.

Precautions and Interactions: Ensuring Safe Use of Griseofulvin

Before starting griseofulvin treatment, it’s essential to inform your healthcare provider about your medical history and any medications you’re currently taking. Why is this step so important? Griseofulvin can interact with various drugs and may not be suitable for people with certain medical conditions.

Key Precautions to Consider

• Allergies: Inform your doctor if you’re allergic to griseofulvin or any other medications.
• Existing medical conditions: Mention if you have liver disease, porphyria, lupus, or a history of alcohol abuse.
• Pregnancy and breastfeeding: Griseofulvin may not be safe during pregnancy or while breastfeeding. Discuss this with your doctor.
• Alcohol consumption: Alcohol may interact with griseofulvin, so it’s best to avoid or limit intake during treatment.
• Sun sensitivity: Griseofulvin can increase your skin’s sensitivity to sunlight. Take precautions to avoid excessive sun exposure.

Potential Drug Interactions

Griseofulvin may interact with several medications, including:

• Anticoagulants (blood thinners) like warfarin
• Oral contraceptives
• Cyclosporine
• Phenobarbital
• Certain vitamins

Always provide your healthcare provider with a complete list of your medications, including over-the-counter drugs and supplements, to avoid potential interactions.

Proper Storage and Disposal of Griseofulvin

Proper storage and disposal of griseofulvin are crucial for maintaining its effectiveness and ensuring safety. How should griseofulvin be stored?

• Keep the medication in its original container, tightly closed.
• Store at room temperature, away from excess heat and moisture.
• Keep liquid formulations away from light and do not freeze them.
• Store all forms of griseofulvin out of reach of children.

When it comes to disposal, it’s important to follow proper procedures. Do not flush griseofulvin down the toilet. Instead, utilize a medicine take-back program or consult your pharmacist for the best disposal method in your area.

Maximizing the Effectiveness of Griseofulvin Treatment

To get the most out of your griseofulvin treatment, consider the following tips:

1. Take the medication exactly as prescribed, even if symptoms improve.
2. Complete the full course of treatment to prevent recurrence of the infection.
3. Take griseofulvin with a fatty meal to enhance absorption.
4. Be patient, as it may take several weeks to see significant improvement.
5. Practice good hygiene to prevent reinfection or spreading the infection to others.

Remember, consistency is key when it comes to antifungal treatments. Skipping doses or stopping the medication prematurely can lead to treatment failure and potential antibiotic resistance.

When to Seek Medical Attention During Griseofulvin Treatment

While griseofulvin is generally well-tolerated, there are instances where you should seek immediate medical attention. When should you contact your healthcare provider?

• If you experience severe side effects such as persistent nausea, vomiting, or abdominal pain
• If you develop signs of an allergic reaction, including rash, itching, or difficulty breathing
• If your symptoms worsen or do not improve after the prescribed treatment duration
• If you suspect an overdose

In case of a suspected overdose, contact the poison control helpline at 1-800-222-1222 immediately. Prompt medical attention can prevent serious complications and ensure the best possible outcome.

Alternative Treatments and Future Perspectives in Antifungal Therapy

While griseofulvin has been a mainstay in antifungal treatment for decades, research into new and improved therapies continues. What are some alternatives to griseofulvin for treating fungal infections?

• Terbinafine: Often used for nail infections, particularly effective against dermatophytes
• Itraconazole: A broad-spectrum antifungal that can treat a wide range of fungal infections
• Fluconazole: Commonly used for yeast infections but also effective against some dermatophytes
• Topical treatments: Including creams, ointments, and nail lacquers for localized infections

The choice of treatment depends on various factors, including the type of fungus, the location of the infection, and individual patient characteristics. Your healthcare provider will determine the most appropriate treatment based on your specific situation.

Emerging Therapies and Research

The field of antifungal therapy is evolving, with researchers exploring new avenues for more effective and targeted treatments. Some areas of ongoing research include:

• Novel antifungal compounds with improved efficacy and safety profiles
• Combination therapies to enhance treatment outcomes
• Nanotechnology-based drug delivery systems for improved penetration and targeting
• Immunotherapies to boost the body’s natural defenses against fungal infections

These advancements hold promise for the future of antifungal treatments, potentially offering more effective options with fewer side effects and shorter treatment durations.

Living with Fungal Infections: Beyond Medication

While griseofulvin and other antifungal medications play a crucial role in treating fungal infections, lifestyle modifications and preventive measures are equally important. How can you reduce your risk of fungal infections and prevent recurrence?

• Maintain good personal hygiene, especially in areas prone to fungal growth
• Keep your skin clean and dry, particularly after sweating or swimming
• Wear breathable fabrics and avoid tight-fitting shoes or clothing
• Use antifungal powders or sprays in shoes and on feet regularly
• Avoid walking barefoot in public areas like locker rooms or swimming pools
• Don’t share personal items like towels, combs, or nail clippers
• Manage underlying conditions that may increase your risk, such as diabetes

By combining proper medication use with these preventive strategies, you can effectively manage fungal infections and improve your overall skin health.

The Importance of Patient Education

Understanding your condition and treatment is crucial for successful management of fungal infections. Don’t hesitate to ask your healthcare provider questions about your diagnosis, treatment options, and expected outcomes. Being well-informed empowers you to take an active role in your health and make informed decisions about your care.

Griseofulvin in Special Populations: Considerations for Specific Groups

While griseofulvin is widely used, its use may require special considerations in certain populations. How does griseofulvin treatment differ for various groups?

Pediatric Use

Griseofulvin is approved for use in children, but dosing is typically based on body weight. Children may also be more susceptible to certain side effects, so close monitoring is essential.

Geriatric Use

Older adults may be more sensitive to the effects of griseofulvin and may require dose adjustments. They may also be at higher risk for drug interactions due to concurrent medications.

Pregnancy and Breastfeeding

Griseofulvin is generally not recommended during pregnancy due to potential risks to the fetus. It’s also not advised during breastfeeding as it can pass into breast milk. Alternative treatments should be considered for pregnant or breastfeeding individuals.

Patients with Liver Disease

Since griseofulvin is metabolized in the liver, patients with liver disease may require dose adjustments or closer monitoring during treatment.

These special considerations highlight the importance of personalized treatment plans. Your healthcare provider will take into account your individual circumstances when prescribing griseofulvin or any other antifungal treatment.

The Role of Griseofulvin in Modern Antifungal Therapy

Despite the development of newer antifungal agents, griseofulvin continues to play a significant role in modern antifungal therapy. Why does griseofulvin remain a valuable treatment option?

• Proven efficacy: Griseofulvin has a long history of successful use against various dermatophyte infections.
• Oral administration: Unlike some newer treatments that are only available topically, griseofulvin can be taken orally, allowing for systemic treatment of widespread or deep infections.
• Cost-effectiveness: As a generic medication, griseofulvin is often more affordable than some newer antifungal drugs.
• Well-established safety profile: With decades of clinical use, the side effects and potential risks of griseofulvin are well understood.

However, the choice between griseofulvin and newer antifungal agents depends on various factors, including the specific type of fungus, the location and severity of the infection, and individual patient characteristics. Your healthcare provider will consider these factors when determining the most appropriate treatment for your condition.

The Future of Antifungal Therapy

As research in antifungal therapy progresses, we may see new treatments that offer advantages over existing options, including griseofulvin. These advancements may include:

• More targeted therapies with fewer systemic side effects
• Treatments with shorter durations, improving patient compliance
• Combination therapies that enhance efficacy and reduce the risk of drug resistance
• Novel drug delivery methods for improved penetration into affected tissues

While these developments are exciting, griseofulvin is likely to remain an important tool in the antifungal arsenal for the foreseeable future, particularly for certain types of dermatophyte infections.

Conclusion: Griseofulvin as a Cornerstone of Antifungal Treatment

Griseofulvin has stood the test of time as an effective treatment for various fungal infections affecting the skin, hair, and nails. Its ability to target dermatophytes systemically makes it a valuable option for widespread or deep-seated infections. While it requires a longer treatment duration compared to some newer antifungals, its proven efficacy and well-established safety profile continue to make it a go-to choice for many healthcare providers.

As with any medication, the key to successful treatment with griseofulvin lies in proper use, adherence to the prescribed regimen, and open communication with your healthcare provider. By understanding how griseofulvin works, its potential side effects, and necessary precautions, patients can maximize the benefits of this time-tested antifungal medication.

Remember, fungal infections can be persistent and may require patience during treatment. With the right approach, combining medication like griseofulvin with proper hygiene and preventive measures, most fungal infections can be effectively managed and overcome. Always consult with your healthcare provider for personalized advice and treatment plans tailored to your specific condition and needs.

Griseofulvin: MedlinePlus Drug Information

pronounced as (gri see oh ful’ vin)

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Griseofulvin is used to treat skin infections such as jock itch, athlete’s foot, and ringworm; and fungal infections of the scalp, fingernails, and toenails.

This medication is sometimes prescribed for other uses; ask your doctor or pharmacist for more information.

Griseofulvin comes as a tablet, capsule, and liquid to take by mouth. It is usually taken once a day or can be taken two to four times a day. Although your symptoms may get better in a few days, you will have to take griseofulvin for a long time before the infection is completely gone. It 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. Follow the directions on your prescription label carefully, and ask your doctor or pharmacist to explain any part you do not understand. Take griseofulvin exactly as directed. Do not take more or less of it or take it more often than prescribed by your doctor.

Shake the liquid well before each use to mix the medication evenly.

Continue to take griseofulvin even if you feel well. Do not stop taking griseofulvin without talking to your doctor.

Before taking griseofulvin,

• tell your doctor and pharmacist if you are allergic to griseofulvin, or any other medications.
• tell your doctor and pharmacist what prescription and nonprescription medications you are taking, especially anticoagulants (‘blood thinners’) such as warfarin (Coumadin), oral contraceptives, cyclosporine (Neoral, Sandimmune), phenobarbital (Luminal), and vitamins.
• tell your doctor if you have or have ever had liver disease, porphyria, lupus, or a history of alcohol abuse.
• tell your doctor if you are pregnant, plan to become pregnant, or are breast-feeding. If you become pregnant while taking griseofulvin, call your doctor.
• tell your doctor if you drink alcohol.
• you should plan to avoid unnecessary or prolonged exposure to sunlight and to wear protective clothing, sunglasses, and sunscreen. Griseofulvin may make your skin sensitive to sunlight.

Take the missed dose as soon as you remember it. However, if it is almost time for the next dose, skip the missed dose and continue your regular dosing schedule. Do not take a double dose to make up for a missed one.

Griseofulvin may cause side effects. Tell your doctor if any of these symptoms are severe or do not go away:

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

If you experience any of the following symptoms, call your doctor immediately:

• fever
• sore throat
• skin rash
• mouth soreness or irritation

If you experience a serious side effect, you or your doctor may send a report to the Food and Drug Administration’s (FDA) MedWatch Adverse Event Reporting program online (http://www.fda.gov/Safety/MedWatch) or by phone (1-800-332-1088).

Keep this medication in the container it came in, tightly closed, and out of reach of children. Store it at room temperature and away from excess heat and moisture (not in the bathroom). Keep the liquid away from light. Do not freeze.

Unneeded medications should be disposed of in special ways to ensure that pets, children, and other people cannot consume them. However, you should not flush this medication down the toilet. Instead, the best way to dispose of your medication is through a medicine take-back program. Talk to your pharmacist or contact your local garbage/recycling department to learn about take-back programs in your community. See the FDA’s Safe Disposal of Medicines website (http://goo.gl/c4Rm4p) for more information if you do not have access to a take-back program.

It is important to keep all medication out of sight and reach of children as many containers (such as weekly pill minders and those for eye drops, creams, patches, and inhalers) are not child-resistant and young children can open them easily. To protect young children from poisoning, always lock safety caps and immediately place the medication in a safe location – one that is up and away and out of their sight and reach. http://www.upandaway.org

In case of overdose, call the poison control helpline at 1-800-222-1222. Information is also available online at https://www. poisonhelp.org/help. If the victim has collapsed, had a seizure, has trouble breathing, or can’t be awakened, immediately call emergency services at 911.

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Last Revised – 06/15/2017

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Griseofulvin Oral: Uses, Side Effects, Interactions, Pictures, Warnings & Dosing

Uses

This medication is used to treat fungal infections of the skin, hair, and nails that do not respond to creams/lotions. Clearing such infections will get rid of symptoms such as itching, red/peeling/scaly skin, and discolored nails. This medication works by stopping the growth of fungi. It does not treat infections due to bacteria or yeast.

How to use Griseofulvin 250 Mg Tablet

Take this medication by mouth as directed by your doctor. For the best absorption, it is best taken with or after a meal containing a moderate amount of fat. Talk to your doctor or pharmacist about specific dietary instructions, especially if you are on a low-fat diet.

The dosage is based on your medical condition and response to therapy. In children, dosage is also based on weight. The length of treatment depends on the type of infection you have. It may take several weeks to months to complete treatment for infections of the scalp, feet, and body. Nail infections may require several months to a year or longer to treat.

Antifungal medications work best when the amount of medicine in your body is kept at a constant level. Take this drug at evenly spaced intervals.

Continue to take this medication for the full prescribed length of treatment even if symptoms improve after a few days. Stopping the medication too early may allow the fungus to continue to grow, which may result in a relapse of the infection.

Inform your doctor if your condition lasts or gets worse.

Side Effects

Headache, nausea, vomiting, diarrhea, stomach upset, tiredness, dizziness, or trouble sleeping may occur. If any of these effects last or get worse, tell your doctor or pharmacist promptly.

Remember that this medication has been prescribed because your doctor has judged that the benefit to you is greater than the risk of side effects. Many people using this medication do not have serious side effects.

Tell your doctor right away if you have any serious side effects, including: numbness/tingling of the hands/feet, mental/mood changes (such as confusion, trouble doing normal activities), hearing changes, butterfly-shaped facial rash (around the nose and cheeks), joint/muscle pain, signs of liver disease (such as nausea/vomiting that doesn’t stop, stomach/abdominal pain, yellowing eyes/skin, dark urine), signs of kidney problems (such as change in the amount of urine, frothy urine), signs of infection (such as sore throat that doesn’t go away, fever).

Use of this medication for prolonged or repeated periods may result in oral thrush or a new vaginal yeast infection (oral or vaginal fungal infection). Contact your doctor if you notice white patches in your mouth, a change in vaginal discharge, or other new symptoms.

A very serious allergic reaction to this drug is rare. However, get medical help right away if you notice any symptoms of a serious allergic reaction, including: rash, itching/swelling (especially of the face/tongue/throat), severe dizziness, trouble breathing.

This is not a complete list of possible side effects. If you notice other effects not listed above, contact your doctor or pharmacist.

In the US – Call your doctor for medical advice about side effects. You may report side effects to FDA at 1-800-FDA-1088 or at www.fda.gov/medwatch.

In Canada – Call your doctor for medical advice about side effects. You may report side effects to Health Canada at 1-866-234-2345.

Precautions

Before taking griseofulvin, tell your doctor or pharmacist if you are allergic to it; or if you have any other allergies. This product may contain inactive ingredients, which can cause allergic reactions or other problems. Talk to your pharmacist for more details.

Before using this medication, tell your doctor or pharmacist your medical history, especially of: a certain blood disorder (porphyria), liver disease, lupus.

This drug may make you dizzy or less alert. Alcohol or marijuana (cannabis) can make you more dizzy or much less alert. Do not drive, use machinery, or do anything that needs alertness until you can do it safely. Avoid alcoholic beverages while you are taking this drug unless your doctor gives permission. Drinking alcohol during treatment with this drug could result in a fast heartbeat and flushing of the skin. Talk to your doctor if you are using marijuana (cannabis).

This medication may make you more sensitive to the sun. Limit your time in the sun. Avoid tanning booths and sunlamps. Use sunscreen and wear protective clothing when outdoors. Tell your doctor right away if you get sunburned or have skin blisters/redness.

Tell your doctor if you are pregnant or plan to become pregnant. You should not become pregnant while using griseofulvin. Griseofulvin may harm an unborn baby. Ask about reliable forms of birth control while using this medication and for 1 month after the last dose. If you become pregnant, talk to your doctor right away about the risks and benefits of this medication. (See also Drug Interactions section.)

The effects of this drug on human sperm are unknown. However, based on animal cell studies, the manufacturer recommends waiting for a period of time after completing griseofulvin treatment before trying to father a child. Discuss the risks and benefits with your doctor, and ask how long to wait after your last dose before trying to father a child.

It is unknown if this drug passes into breast milk. Consult your doctor before breast-feeding.

Interactions

Drug interactions may change how your medications work or increase your risk for serious side effects. This document does not contain all possible drug interactions. Keep a list of all the products you use (including prescription/nonprescription drugs and herbal products) and share it with your doctor and pharmacist. Do not start, stop, or change the dosage of any medicines without your doctor’s approval.

Some products that may interact with this drug are: barbiturates (such as phenobarbital), warfarin.

This medication may decrease the effectiveness of hormonal birth control such as pills, patch, or ring. This could cause pregnancy. Discuss with your doctor or pharmacist if you should use additional reliable birth control methods while using this medication. Also tell your doctor if you have any new spotting or breakthrough bleeding, because these may be signs that your birth control is not working well.

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Overdose

If someone has overdosed and has serious symptoms such as passing out or trouble breathing, call 911. Otherwise, call a poison control center right away. US residents can call their local poison control center at 1-800-222-1222. Canada residents can call a provincial poison control center.

Do not share this medication with others.

This medication has been prescribed for your current condition only. Do not use it later for another infection unless your doctor tells you to.

Lab and/or medical tests (such as kidney/liver function, complete blood count) should be done while you are taking this medication. Keep all medical and lab appointments. Consult your doctor for more details.

Ask your doctor or pharmacist about ways to control the infection and to prevent re-infection. Fungus spreads easily in warm, moist areas. Follow good hygiene (for example wash and dry the infected area completely, and do not share articles of clothing or objects that come in contact with the infected area).

If you miss a dose, take it as soon as you remember. If it is near the time of the next dose, skip the missed dose. Take your next dose at the regular time. Do not double the dose to catch up.

Store at room temperature away from light and moisture. Do not store in the bathroom. Keep all medications away from children and pets.

Do not flush medications down the toilet or pour them into a drain unless instructed to do so. Properly discard this product when it is expired or no longer needed. Consult your pharmacist or local waste disposal company.

Selected from data included with permission and copyrighted by First Databank, Inc. This copyrighted material has been downloaded from a licensed data provider and is not for distribution, except as may be authorized by the applicable terms of use.

CONDITIONS OF USE: The information in this database is intended to supplement, not substitute for, the expertise and judgment of healthcare professionals. The information is not intended to cover all possible uses, directions, precautions, drug interactions or adverse effects, nor should it be construed to indicate that use of a particular drug is safe, appropriate or effective for you or anyone else. A healthcare professional should be consulted before taking any drug, changing any diet or commencing or discontinuing any course of treatment.

Griseofulvin – description of the substance, pharmacology, use, contraindications, formula

Contents

• Structural formula

• Russian name

• English title

• Latin name

• chemical name

• Gross formula

• Pharmacological group of the substance Griseofulvin

• Nosological classification

• CAS code

• pharmachologic effect

• Characteristic

• Pharmacology

• Application of the substance Griseofulvin

• Contraindications

• Application restrictions

• Use during pregnancy and lactation

• Side effects of the substance Griseofulvin

• Interaction

• Dosage and administration

• Precautionary measures

• Trade names with the active substance Griseofulvin

Structural formula

Russian name

Griseofulvin

English name

Griseofulvin

Latin name

Griseofulvinum (genus Griseofulvini)

Chemical name

(1’S-trans)-7-Chloro-2′,4,6-trimethoxy-6′-methylspiro[benzofuran-2(3H),1′-[2]cyclohexene]-3,4′-dione

Gross formula

C ₁₇ H ₁₇ ClO ₆

Pharmacological group of the substance Griseofulvin

Antifungals

Nosological classification

ICD-10 code list

CAS code

126-07-8

Pharmacological action

Pharmacological action 9 0095-

antifungal , fungistatic .

Feature

Antifungal. Antibiotic produced by the fungus Penicillium nigricans (griseofulvum). White or white with a yellowish tint, the smallest crystalline powder with a slight specific (mushroom) odor. Practically insoluble in water and petroleum ether, slightly soluble in ethanol, methanol, acetone, benzene, ethyl acetate, acetic acid. Solubility in DMF at 25°C: 12-14 g/100 ml. Stable at high temperature, incl. when autoclaving. Molecular weight 352.77.

Pharmacology

Fungistatic effect is associated with the effect on the microtubular proteins of the fungal cell, resulting in the rupture of spindle-shaped mitotic structures and the arrest of mitotic division of fungal cells in metaphase, inhibits protein synthesis, disrupts the formation of the cell wall in chitin-containing fungi. It has a greater affinity for affected tissues: it selectively accumulates in the precursors of keratinocytes of the skin, hair and nails, strongly binds to the newly formed keratin, providing it with high resistance to fungal invasion (thus preventing fungal infection of new emerging cells). Gradually, the structures containing keratin are sloughed off. The cure occurs after the complete replacement of the infected keratin, so the therapeutic effect develops slowly.

Active against dermatomycetes, including Trichophyton 62 , Trichophyton verrucosum , Trichophyton sulphureum , Trichophyton menginii , Trichophyton gallinae , Trichophyton schoenleini , Tri chophyton crateriforme ), Microsporum ( Microsporum audouinii , Microsporum canis , Microsporum gypseum ), Epidermophyton ( Epidermophyton floccosum ). The fungistatic concentration for most griseofulvin-sensitive fungal species is 0.5–3 µg/ml. Yeast-like fungi (genus Candida ) and molds are resistant to griseofulvin. It does not have antibacterial activity.

When taken orally, the absorption of griseofulvin depends on the dispersion of its crystals: the amount of absorption of the microcrystalline form varies from 25 to 70%, the ultramicrocrystalline form is absorbed almost completely. Absorption from the gastrointestinal tract varies greatly from person to person, mainly due to the insolubility of the substance in the aquatic environment of the upper GI tract. From _max in the blood of adults on an empty stomach after ingestion of 0.5 g of griseofulvin is 0.5–2.0 μg / ml and is reached after 4 hours. It should be noted that in some patients there is a tendency to create low levels of the substance in the blood, regardless of time. This may explain the unsatisfactory therapeutic effect in some patients. Bioavailability in most patients increases when taken together with fatty foods. After ingestion, it accumulates in the stratum corneum and its appendages, as well as in the liver, adipose tissue, and skeletal muscles. Minor amounts enter liquid media and other tissues of the body. Biotransformation occurs in the liver, the main metabolites are 6-methylgriseofulvin and a glucuronide derivative. T _1/2 – about 24 hours, does not change in renal failure. Excreted in faeces (36% unchanged) and urine (less than 1% unchanged).

When applied topically, griseofulvin has little effect.

Toxicology in Animals

In long-term studies in animals fed griseofulvin with food (0.5-2.5% of the feed), hepatoma formation was noted in several strains of mice, especially in males. This effect was higher when griseofulvin particles were used in a smaller size. Subcutaneous administration of relatively smaller doses of griseofulvin once a week during the first three weeks of life also led to the formation of hepatomas in mice.

Tumors of the thyroid gland (usually adenomas, but sometimes carcinomas) developed in male rats fed griseofulvin with food (2.0; 1.0 and 0.2% of the feed), and in female rats with twice the griseofulvin content in the diet. In experiments on other animal species, no carcinogenic effects were found.

In oral subacute toxicity studies, griseofulvin caused hepatocellular necrosis in mice, but this effect was not observed in other animal species. In laboratory animals treated with griseofulvin, disturbances in the metabolism of porphyrin were observed. Griseofulvin had a colchicine-like effect on mitosis and contributed to the development of skin tumors in laboratory animals upon induction with methylcholanthrene.

Application of the substance Griseofulvin

Mycoses of the skin, scalp and nails: favus, trichophytosis, microsporia of the scalp, microsporia of smooth skin, ringworm of the beard and mustache, epidermophytosis of smooth skin, inguinal epidermophytosis, onychomycosis.

Contraindications

Hypersensitivity, porphyria, systemic lupus erythematosus, lupus-like syndrome, systemic blood diseases, leukopenia, organic diseases of the liver and kidneys, hepatocellular insufficiency, malignant neoplasms.

Restrictions for use

Children under 2 years of age (efficacy and safety of use have not been determined).

Use in pregnancy and lactation

There is evidence of teratogenic and embryotoxic effects of griseofulvin in animals (when administered orally in pregnant rats, pups with several disorders have been reported in the offspring). Griseofulvin has been shown to inhibit spermatogenesis in rats, although this has not been shown in human studies. Studies on dogs have shown that griseofulvin may cause adverse effects in offspring.

Contraindicated in pregnancy (griseofulvin crosses the placenta, adequate and well-controlled studies in pregnant women have not been conducted). Since 1977, two cases of conjoined twins have been reported in patients taking griseofulvin in the first trimester of pregnancy. If pregnancy occurs during treatment with griseofulvin, the patient should be informed of the potential risk to the fetus.

Use during lactation is not recommended (it is not known whether griseofulvin passes into breast milk). There are no adequate data.

Side effects of the substance Griseofulvin

On the part of the gastrointestinal tract: nausea, vomiting, dry mouth, diarrhea, abdominal pain, candidal stomatitis, increased activity of hepatic transaminases, jaundice, hepatitis.

From the nervous system and sensory organs: headache, dizziness, excessive fatigue or weakness, insomnia, peripheral neuropathy, paresthesia of the extremities, impaired coordination of movements, lethargy, disorientation, confusion, depression, impaired taste sensitivity.

From the side of the cardiovascular system and blood (hematopoiesis, hemostasis): granulocytopenia, agranulocytosis, leukopenia.

Allergic reactions: rash, pruritus, urticaria, angioedema, photosensitivity, lupus-like syndrome, erythema multiforme exudative, topical epidermal necrolysis (Lyell’s syndrome).

Interactions

Griseofulvin induces hepatic microsomal enzymes and as a result may increase hepatic metabolism and therefore reduce the activity of indirect anticoagulants (PT needs to be monitored, anticoagulant dose adjustment may be required), oral hypoglycemic agents (blood glucose control, antidiabetic dose adjustment possible), oral estrogen containing contraceptives, theophylline (monitoring of its concentration in the blood with possible dose adjustment). Inducers of microsomal enzymes (including barbiturates, rifampicin) can increase the metabolism of griseofulvin and reduce its fungistatic activity. Enhances the effect of ethanol.

Dosage and administration

Inside (during or immediately after a meal), in one or more divided doses. The daily dose for adults is 500 mg (in case of severe mycoses, the dose is increased), for children – 10 mg/kg. The highest daily dose is 1 g. The duration of treatment depends on the infection and on the thickness of the keratin at the site of infection and is: in case of damage to the skin of the scalp – 4-6 weeks, body – 2-4 weeks, feet – 4-8 weeks, fingers – at least 4 months, toes – at least 6 months.

Precautions

Before starting therapy with griseofulvin, the type of fungus causing the infection must be identified. Griseofulvin is not suitable for prophylactic use, it is not used to treat infections of mild severity, in which it is sufficient to prescribe only antifungal agents for external use. Griseofulvin is ineffective for the treatment of bacterial infections, candidiasis, histoplasmosis, actinomycosis, sporotrichosis, chromomycosis, coccidioidomycosis, North American blastomycosis, cryptococcosis, pityriasis versicolor and nocardiosis.

If a low fat diet is used, griseofulvin should be taken with 1 tablespoon of vegetable oil. During treatment, you can not drink alcoholic beverages.

Treatment with griseofulvin should be discontinued if granulocytopenia develops. Since the therapy is long-term, periodic monitoring of the function of the liver, kidneys, and hematopoiesis is necessary.

In elderly patients, due to age-related changes in liver function, an increased risk of hepatotoxicity is possible (strict clinical and laboratory monitoring is required).

During treatment with griseofulvin, patients should avoid exposure to direct sunlight and UV radiation.

Men and women of childbearing age should use effective contraception during and for 6 months after treatment (adverse effects on reproductive function in both men and women).

Should not be administered as an outpatient to drivers of transport, as well as people whose professional activities require quick reactions and increased attention.

Trade names with active substance Griseofulvin

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Lek. form
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Dosage
All dosages 125 mg No dosage

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Griseofulvin (Griseofulvinum). Oral tablets Directory of drugs. Kyzyl (Republic of Tyva)

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Packaging

Oral tablets

Pharmacological action

Griseofulvin is an antibiotic produced by the fungus Penicillinum nigricans, a fungistatic agent active against various dermatomycetes (trichophytons, microsporums, epidermophytons). The drug inhibits the division of fungal cells in metaphase, disrupting the structure of the mitotic spindle. Griseofulvin accumulates to varying degrees in the cells of the skin, hair, nails, providing resistance to fungal infection. As the affected keratin dies off, it is replaced by a healthy one.

Indications for use

Trichophytosis, favus and microsporia of the scalp and smooth skin, epidermophytosis of the skin caused by trichophyton, as well as nail lesions (onychomycosis) caused by pathogenic fungi (trichophyton, red epidermophyton).

Release form

Tablets.

Pharmacokinetics

Metabolized in the liver with the formation of the main metabolites: 6-methylgriseofulvin and a glucuronide derivative. The half-life is 24 hours. Excreted by the kidneys. Less than 1% is excreted unchanged in the urine, 36% is excreted in the feces.

Contraindications for use

Hypersensitivity to the components of the drug, severe leukopenia and systemic blood diseases, organic lesions of the liver and kidneys, porphyria, malignant neoplasms, pregnancy, lactation, children under 3 years of age.

Side effects

From the digestive system: hepatitis, nausea, vomiting, diarrhea, epigastric pain.

Allergic reactions: urticaria, skin rashes, erythema multiforme, toxic epidermal necrosis.

From the side of the central nervous system and peripheral nervous system: peripheral neuropathy, dizziness, confusion.

From the hemopoietic system: granulocytopenia, leukopenia.

Others: candidal stomatitis, photosensitivity, sometimes lupus.

Method of administration and dosage

Tablets are taken during meals in three doses together with 1 teaspoon of vegetable oil. With microsporia, adults are prescribed 1 g of Griseofulvin per day, children (from 3 years old) – at the rate of 21-22 mg / kg per day. The drug is taken daily until the first negative result of mycological examination, then at the same dose for 2 weeks every other day and 4 times for 2 weeks.

With onychomycosis, trichophytosis, favus of the scalp, the daily dose of Griseofulvin for adults with a body weight of up to 50 kg is 625 mg (5 tablets), with a larger weight, an additional 125 mg is prescribed for every 10 kg. Children and adolescents are prescribed 16 mg / kg per day. With mycoses that are difficult to treat, the course of therapy can last up to 12 months.

Overdose

Clinical manifestations of an overdose of Griseofulvin are not known.

Interaction with other drugs

Due to the stimulation of microsomal liver enzymes by Griseofulvin, the effectiveness of indirect coagulants and oral contraceptives may decrease. Simultaneous reception with barbiturates leads to a weakening of the antifungal properties of Griseofulvin.

Special instructions for taking

With caution, the drug is prescribed for hypersensitivity to penicillins, with hypocoagulable conditions. Patients whose professional activities require a speed of reaction and increased attention, the drug is not prescribed. When using the drug, it is recommended to take vitamin preparations: ascorbic acid and vitamin preparations of group B. With candidiasis, the drug is ineffective. During treatment with Griseofulvin, it is necessary to refrain from drinking alcohol.