Griseofulvin Ultr 250mg Tablets
It is used to treat fungal infections.
Drug Class
Antifungal
Pharmacologic Class
Antifungal, Systemic; Mitotic Inhibitor
Pregnancy Category
Category X
FDA Approved
Sep 1959
DEA Schedule
Not Controlled
Overview
What is this medicine?
Griseofulvin is an antifungal medication used to treat fungal infections of the skin, hair, and nails. It works by stopping the growth of the fungus.
How to Use This Medicine
Taking Your Medication
To use this medication correctly, follow your doctor's instructions and read all the information provided. Discuss with your doctor or pharmacist whether to take this medication with food. Continue taking the medication as directed, even if your symptoms improve.
To take the medication:
- Swallow the tablet whole with a full glass of water.
- Alternatively, you can crush the tablet and mix it with 1 tablespoon (15 mL) of applesauce. Swallow the mixture immediately without chewing.
Storing and Disposing of Your Medication
Store the medication at room temperature in a dry place, avoiding bathrooms. Keep all medications in a safe location, out of the reach of children and pets. Dispose of unused or expired medications properly. Do not flush them down the toilet or pour them down the drain unless instructed to do so. If you have questions about disposing of your medication, consult your pharmacist. You may also want to check if there are drug take-back programs available in your area.
Missing a Dose
If you miss a dose, take it as soon as you remember. However, if it's close to the time for your next dose, skip the missed dose and resume your regular schedule. Avoid taking two doses at the same time or taking extra doses.
To use this medication correctly, follow your doctor's instructions and read all the information provided. Discuss with your doctor or pharmacist whether to take this medication with food. Continue taking the medication as directed, even if your symptoms improve.
To take the medication:
- Swallow the tablet whole with a full glass of water.
- Alternatively, you can crush the tablet and mix it with 1 tablespoon (15 mL) of applesauce. Swallow the mixture immediately without chewing.
Storing and Disposing of Your Medication
Store the medication at room temperature in a dry place, avoiding bathrooms. Keep all medications in a safe location, out of the reach of children and pets. Dispose of unused or expired medications properly. Do not flush them down the toilet or pour them down the drain unless instructed to do so. If you have questions about disposing of your medication, consult your pharmacist. You may also want to check if there are drug take-back programs available in your area.
Missing a Dose
If you miss a dose, take it as soon as you remember. However, if it's close to the time for your next dose, skip the missed dose and resume your regular schedule. Avoid taking two doses at the same time or taking extra doses.
Lifestyle & Tips
- Take with a fatty meal (e.g., milk, ice cream, fatty foods) to improve absorption and effectiveness.
- Avoid alcohol during treatment and for several days after, as it can cause a disulfiram-like reaction (flushing, nausea, vomiting, headache) and increase CNS depression.
- Protect skin from sun exposure (wear protective clothing, use sunscreen) as griseofulvin can cause photosensitivity.
- Treatment duration is long; continue taking the medication for the full prescribed period, even if symptoms improve, to prevent recurrence.
- For nail infections, it may take many months for new, healthy nails to grow out.
Available Forms & Alternatives
Dosing & Administration
Adult Dosing
Standard Dose:
250 mg once daily or 125 mg twice daily (ultramicrosize formulation)
Dose Range:
125 - 500 mg
Condition-Specific Dosing:
tineaCorporis:
250 mg once daily
tineaCruris:
250 mg once daily
tineaPedis:
250-500 mg once daily
tineaCapitis:
250-500 mg once daily
onychomycosis:
250-500 mg once daily
Pediatric Dosing
Neonatal:
Not established
Infant:
Not established
Child:
10-15 mg/kg/day (ultramicrosize) as a single dose or divided doses
Adolescent:
10-15 mg/kg/day (ultramicrosize) as a single dose or divided doses, up to 250-500 mg/day
Dose Adjustments
Renal Impairment:
Mild:
No adjustment needed
Moderate:
No adjustment needed
Severe:
No adjustment needed
Dialysis:
Not significantly removed by dialysis; no supplemental dose needed.
Hepatic Impairment:
Mild:
Use with caution; monitor liver function
Moderate:
Use with caution; monitor liver function
Severe:
Contraindicated in severe liver disease
Pharmacology
Mechanism of Action
Griseofulvin is a fungistatic agent that deposits in keratin precursor cells. It binds to keratin, making it resistant to fungal invasion. It also interferes with fungal mitosis by disrupting the mitotic spindle structure and inhibiting nucleic acid synthesis.
Pharmacokinetics
Absorption:
Bioavailability:
Approximately 25-70% (ultramicrosize formulation has better absorption than microsize); significantly enhanced by fatty meals.
Tmax:
Approximately 4 hours
FoodEffect:
Absorption is significantly increased (up to 1.5 to 2.5 times) when taken with a high-fat meal.
Distribution:
Vd:
Not readily available, but widely distributed in keratinized tissues (skin, hair, nails).
ProteinBinding:
Approximately 80%
CnssPenetration:
Limited
Elimination:
HalfLife:
Approximately 9-24 hours
Clearance:
Not readily available
ExcretionRoute:
Primarily renal (as metabolites), small amount in feces
Unchanged:
Less than 1% excreted unchanged in urine
Pharmacodynamics
OnsetOfAction:
Clinical improvement may take weeks to months, depending on the site of infection (e.g., nails may take 4-6 months).
PeakEffect:
Not applicable for fungistatic action; effect is cumulative.
DurationOfAction:
Persists in keratinized tissues as long as the drug is administered and for some time after discontinuation.
Safety & Warnings
Side Effects
Urgent Side Effects: Seek Medical Help Right Away
Although rare, some people may experience severe and potentially life-threatening side effects while taking this medication. If you notice any of the following symptoms, contact your doctor or seek immediate medical attention:
Signs of an allergic reaction, such as:
+ Rash
+ Hives
+ Itching
+ Red, swollen, blistered, or peeling skin (with or without fever)
+ Wheezing
+ Tightness in the chest or throat
+ Trouble breathing, swallowing, or talking
+ Unusual hoarseness
+ Swelling of the mouth, face, lips, tongue, or throat
Signs of lupus, including:
+ A rash on the cheeks or other body parts
+ Easy sunburn
+ Muscle or joint pain
+ Chest pain or shortness of breath
+ Swelling in the arms or legs
Signs of liver problems, such as:
+ Dark urine
+ Tiredness
+ Decreased appetite
+ Upset stomach or stomach pain
+ Light-colored stools
+ Vomiting
+ Yellow skin or eyes
Feeling confused
Abnormal burning, numbness, or tingling sensations
Redness or white patches in the mouth or throat
A severe skin reaction (Stevens-Johnson syndrome/toxic epidermal necrolysis), which can cause:
+ Red, swollen, blistered, or peeling skin (with or without fever)
+ Red or irritated eyes
+ Sores in the mouth, throat, nose, or eyes
Other Possible Side Effects
Like all medications, this drug can cause side effects. While many people experience no side effects or only mild ones, others may have more bothersome symptoms. If you experience any of the following side effects or any other unusual symptoms, contact your doctor for advice:
Headache
Dizziness, tiredness, or weakness
Diarrhea
Stomach pain
Upset stomach
Vomiting
Trouble sleeping
Reporting Side Effects
This list is not exhaustive, and you may experience other side effects not mentioned here. If you have questions or concerns about side effects, contact your doctor. You can also report side effects to the FDA at 1-800-332-1088 or online at https://www.fda.gov/medwatch.
Although rare, some people may experience severe and potentially life-threatening side effects while taking this medication. If you notice any of the following symptoms, contact your doctor or seek immediate medical attention:
Signs of an allergic reaction, such as:
+ Rash
+ Hives
+ Itching
+ Red, swollen, blistered, or peeling skin (with or without fever)
+ Wheezing
+ Tightness in the chest or throat
+ Trouble breathing, swallowing, or talking
+ Unusual hoarseness
+ Swelling of the mouth, face, lips, tongue, or throat
Signs of lupus, including:
+ A rash on the cheeks or other body parts
+ Easy sunburn
+ Muscle or joint pain
+ Chest pain or shortness of breath
+ Swelling in the arms or legs
Signs of liver problems, such as:
+ Dark urine
+ Tiredness
+ Decreased appetite
+ Upset stomach or stomach pain
+ Light-colored stools
+ Vomiting
+ Yellow skin or eyes
Feeling confused
Abnormal burning, numbness, or tingling sensations
Redness or white patches in the mouth or throat
A severe skin reaction (Stevens-Johnson syndrome/toxic epidermal necrolysis), which can cause:
+ Red, swollen, blistered, or peeling skin (with or without fever)
+ Red or irritated eyes
+ Sores in the mouth, throat, nose, or eyes
Other Possible Side Effects
Like all medications, this drug can cause side effects. While many people experience no side effects or only mild ones, others may have more bothersome symptoms. If you experience any of the following side effects or any other unusual symptoms, contact your doctor for advice:
Headache
Dizziness, tiredness, or weakness
Diarrhea
Stomach pain
Upset stomach
Vomiting
Trouble sleeping
Reporting Side Effects
This list is not exhaustive, and you may experience other side effects not mentioned here. If you have questions or concerns about side effects, contact your doctor. You can also report side effects to the FDA at 1-800-332-1088 or online at https://www.fda.gov/medwatch.
Seek Immediate Medical Attention If You Experience:
- Signs of liver problems: yellowing of skin or eyes (jaundice), dark urine, persistent nausea/vomiting, severe stomach pain, unusual tiredness.
- Signs of blood problems: fever, sore throat, easy bruising or bleeding, unusual weakness.
- Severe skin rash, blistering, peeling, or widespread redness.
- Signs of an allergic reaction: rash, itching, swelling (especially of face/tongue/throat), severe dizziness, trouble breathing.
- Numbness or tingling in hands or feet (paresthesia).
- Confusion or difficulty concentrating.
Before Using This Medicine
Before Taking This Medication: Important Information to Share with Your Doctor
It is essential to inform your doctor about the following:
Any allergies you have, including allergies to this medication, its components, or other substances, such as foods or drugs. Be sure to describe the allergic reaction you experienced, including any symptoms that occurred.
Certain health conditions, including liver disease or porphyria, as these may affect your ability to take this medication safely.
If you are pregnant or planning to become pregnant, please note:
Do not take this medication if you are pregnant, as it may harm your unborn baby.
If you plan to become pregnant within 1 month after your last dose, you should not take this medication.
Additionally, if you are breast-feeding or plan to breast-feed, inform your doctor, as this medication may pass into breast milk and affect your baby.
To ensure your safety, it is crucial to provide your doctor and pharmacist with a comprehensive list of:
All prescription and over-the-counter medications you are taking
Any natural products or vitamins you are using
* Any health problems you have, as these may interact with this medication
Before starting, stopping, or changing the dose of any medication, including this one, always consult with your doctor to confirm it is safe to do so. This will help prevent potential interactions and ensure your well-being.
It is essential to inform your doctor about the following:
Any allergies you have, including allergies to this medication, its components, or other substances, such as foods or drugs. Be sure to describe the allergic reaction you experienced, including any symptoms that occurred.
Certain health conditions, including liver disease or porphyria, as these may affect your ability to take this medication safely.
If you are pregnant or planning to become pregnant, please note:
Do not take this medication if you are pregnant, as it may harm your unborn baby.
If you plan to become pregnant within 1 month after your last dose, you should not take this medication.
Additionally, if you are breast-feeding or plan to breast-feed, inform your doctor, as this medication may pass into breast milk and affect your baby.
To ensure your safety, it is crucial to provide your doctor and pharmacist with a comprehensive list of:
All prescription and over-the-counter medications you are taking
Any natural products or vitamins you are using
* Any health problems you have, as these may interact with this medication
Before starting, stopping, or changing the dose of any medication, including this one, always consult with your doctor to confirm it is safe to do so. This will help prevent potential interactions and ensure your well-being.
Precautions & Cautions
It is essential to inform all your healthcare providers, including doctors, nurses, pharmacists, and dentists, that you are taking this medication. If you are taking this drug for an extended period, your doctor may recommend regular blood tests to monitor your condition.
Before consuming alcohol, discuss the potential risks with your doctor. Additionally, be aware that this medication can increase your sensitivity to the sun, making you more prone to sunburn. To minimize this risk, avoid exposure to direct sunlight, sunlamps, and tanning beds, and use protective measures such as sunscreen, clothing, and eyewear that provide adequate sun protection.
Do not take this medication for longer than prescribed, as this can increase the risk of a second infection. If you have a history of lupus, this drug may cause your condition to become active or worsen. Immediately report any new or worsening symptoms to your doctor.
When taking this medication, be aware that birth control pills and other hormone-based birth control methods may be less effective in preventing pregnancy. To minimize the risk of unintended pregnancy, use an additional form of birth control, such as a condom, while taking this drug.
This medication can pose a risk to the unborn baby if taken during pregnancy. If you are pregnant or planning to become pregnant, discuss the potential risks with your doctor. If your partner may become pregnant, use birth control while taking this medication and for 6 months after your last dose. If your partner becomes pregnant, notify your doctor immediately.
Before consuming alcohol, discuss the potential risks with your doctor. Additionally, be aware that this medication can increase your sensitivity to the sun, making you more prone to sunburn. To minimize this risk, avoid exposure to direct sunlight, sunlamps, and tanning beds, and use protective measures such as sunscreen, clothing, and eyewear that provide adequate sun protection.
Do not take this medication for longer than prescribed, as this can increase the risk of a second infection. If you have a history of lupus, this drug may cause your condition to become active or worsen. Immediately report any new or worsening symptoms to your doctor.
When taking this medication, be aware that birth control pills and other hormone-based birth control methods may be less effective in preventing pregnancy. To minimize the risk of unintended pregnancy, use an additional form of birth control, such as a condom, while taking this drug.
This medication can pose a risk to the unborn baby if taken during pregnancy. If you are pregnant or planning to become pregnant, discuss the potential risks with your doctor. If your partner may become pregnant, use birth control while taking this medication and for 6 months after your last dose. If your partner becomes pregnant, notify your doctor immediately.
Overdose Information
Overdose Symptoms:
- Nausea
- Vomiting
- Diarrhea
- Headache
- Confusion
What to Do:
Seek immediate medical attention or call a Poison Control Center (1-800-222-1222). Treatment is generally supportive.
Drug Interactions
Major Interactions
- Warfarin (decreased anticoagulant effect)
- Oral Contraceptives (decreased efficacy, leading to breakthrough bleeding or pregnancy)
Moderate Interactions
- Barbiturates (e.g., phenobarbital) (decreased griseofulvin levels)
- Cyclosporine (decreased cyclosporine levels)
- Salicylates (decreased griseofulvin levels)
- Alcohol (disulfiram-like reaction, increased CNS depression)
Monitoring
Baseline Monitoring
Liver Function Tests (LFTs)
Rationale: To assess baseline hepatic function, as griseofulvin is hepatically metabolized and can cause hepatotoxicity.
Timing: Prior to initiation of therapy.
Complete Blood Count (CBC)
Rationale: To assess baseline hematologic status, as rare cases of leukopenia or neutropenia have been reported.
Timing: Prior to initiation of therapy.
Routine Monitoring
Liver Function Tests (LFTs)
Frequency: Periodically, especially during prolonged therapy (e.g., every 4-8 weeks for first few months, then less frequently).
Target: Within normal limits.
Action Threshold: Discontinue if significant elevation (e.g., >3x ULN) or clinical signs of liver injury occur.
Complete Blood Count (CBC)
Frequency: Periodically, especially during prolonged therapy.
Target: Within normal limits.
Action Threshold: Discontinue if significant leukopenia or neutropenia develops.
Symptom Monitoring
- Signs of liver dysfunction (e.g., persistent nausea, vomiting, abdominal pain, dark urine, jaundice, fatigue)
- Signs of blood dyscrasias (e.g., fever, sore throat, unusual bleeding or bruising, pallor)
- Severe skin reactions (e.g., rash, blistering, peeling)
- Photosensitivity (severe sunburn reaction)
- Neurological symptoms (e.g., headache, dizziness, confusion, paresthesia)
- Allergic reactions (e.g., hives, swelling, difficulty breathing)
Special Patient Groups
Pregnancy
Contraindicated in pregnancy (Category X) due to potential for teratogenicity. Women of childbearing potential should use effective contraception during treatment and for at least one month after the last dose.
Trimester-Specific Risks:
First Trimester:
High risk of teratogenicity; contraindicated.
Second Trimester:
Contraindicated.
Third Trimester:
Contraindicated.
Lactation
Use with caution. Griseofulvin is excreted into breast milk. The American Academy of Pediatrics considers it compatible with breastfeeding, but potential for adverse effects on the infant (e.g., gastrointestinal upset, photosensitivity) should be weighed against benefits.
Infant Risk:
L3 (Moderate risk - potential for adverse effects; monitor infant for GI upset, rash, photosensitivity).
Pediatric Use
Dosing is established for children. Generally well-tolerated, but monitor for adverse effects similar to adults. Duration of therapy depends on the site of infection.
Geriatric Use
No specific dose adjustments are typically required based on age alone. However, elderly patients may be more susceptible to adverse effects (e.g., CNS effects, liver dysfunction) and may have comorbidities or polypharmacy requiring careful monitoring.
Clinical Information
Clinical Pearls
- Griseofulvin ultramicrosize is preferred over microsize due to better absorption and lower dosing requirements.
- Always advise patients to take griseofulvin with a fatty meal to maximize absorption.
- Emphasize the importance of completing the full course of therapy, which can be very long (e.g., 6-12 months for toenail infections), to prevent relapse.
- Counsel patients on sun protection due to photosensitivity.
- Warn patients about potential interactions with alcohol and oral contraceptives.
- Regular monitoring of liver function tests is important, especially during prolonged treatment.
Alternative Therapies
- Terbinafine (oral)
- Itraconazole (oral)
- Fluconazole (oral)
- Topical antifungals (for superficial infections, less severe cases, or as adjunct therapy)
Cost & Coverage
Average Cost:
$20 - $80 per 30 tablets (250mg ultramicrosize)
Generic Available:
Yes
Insurance Coverage:
Tier 1 or Tier 2 (for generic)
General Drug Facts
If your symptoms or health condition do not improve or worsen over time, it is essential to contact your doctor for further evaluation and guidance. To ensure your safety and the effectiveness of your treatment, never share your medication with others or take someone else's medication. Some medications may come with an additional patient information leaflet, so it is a good idea to consult with your pharmacist to see if this applies to your prescription. If you have any questions or concerns about your medication, do not hesitate to reach out to your doctor, nurse, pharmacist, or other healthcare provider for clarification and guidance. In the event of a suspected overdose, immediately call your local poison control center or seek emergency medical attention. When seeking help, be prepared to provide detailed information about the overdose, including the name of the medication taken, the amount consumed, and the time it occurred.