Griseofulvin Ultr 125mg Tablets
It is used to treat fungal infections.
Drug Class
Antifungal
Pharmacologic Class
Antifungal, Systemic
Pregnancy Category
X
FDA Approved
Aug 1982
DEA Schedule
Not Controlled
Overview
What is this medicine?
Griseofulvin is an antifungal medicine used to treat fungal infections of the skin, hair, and nails. It works by stopping the growth of the fungus. It's important to take this medicine for the full duration prescribed, even if your symptoms improve, to ensure the infection is completely cleared.
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 disposal, 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 disposal, 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, peanut butter, fatty meat) to help your body absorb the medicine better.
- Avoid alcohol while taking this medicine, as it can cause unpleasant side effects like flushing, rapid heartbeat, and nausea.
- Protect your skin from the sun (wear protective clothing, use sunscreen) as this medicine can make you more sensitive to sunlight.
- If you are a woman of childbearing potential, use effective non-hormonal birth control during treatment and for at least one month after stopping the medicine, as it can make hormonal birth control less effective and can cause severe birth defects.
- If you are a man, use effective birth control during treatment and for at least 6 months after stopping the medicine, as there is a theoretical risk of genetic damage to sperm.
Available Forms & Alternatives
Dosing & Administration
Adult Dosing
Standard Dose:
For Tinea corporis, cruris, pedis: 250 mg once daily or 125 mg twice daily. For Tinea capitis, unguium: 375 mg once daily or 187.5 mg twice daily.
Dose Range:
125 - 750 mg
Condition-Specific Dosing:
Tinea corporis/cruris/pedis:
250 mg once daily or 125 mg twice daily
Tinea capitis/unguium:
375 mg once daily or 187.5 mg twice daily
Max daily dose:
750 mg
Pediatric Dosing
Neonatal:
Not established
Infant:
Not established
Child:
5.5 mg/kg/day to 7.3 mg/kg/day (ultramicrosize) given once daily or in divided doses. Max 750 mg/day.
Adolescent:
5.5 mg/kg/day to 7.3 mg/kg/day (ultramicrosize) given once daily or in divided doses. Max 750 mg/day. Or adult dosing if weight appropriate.
Dose Adjustments
Renal Impairment:
Mild:
No adjustment generally needed
Moderate:
No adjustment generally needed
Severe:
No adjustment generally needed
Dialysis:
Not significantly removed by dialysis; no specific dose adjustment recommended, but monitor for adverse effects.
Hepatic Impairment:
Mild:
Use with caution; monitor liver function.
Moderate:
Use with caution; monitor liver function. Dose reduction may be considered.
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:
Variable, enhanced by fat. Ultramicrosize formulation has approximately 1.5 times greater absorption than microsize.
Tmax:
Approximately 4 hours (ultramicrosize)
FoodEffect:
Absorption is significantly increased when taken with a high-fat meal.
Distribution:
Vd:
Not readily available, but widely distributed to keratinized tissues (skin, hair, nails).
ProteinBinding:
Approximately 80%
CnssPenetration:
Limited
Elimination:
HalfLife:
9 to 24 hours
Clearance:
Not readily available
ExcretionRoute:
Mainly via urine (metabolites) and feces. Less than 1% excreted unchanged in urine.
Unchanged:
<1%
Pharmacodynamics
OnsetOfAction:
Clinical improvement may be seen within days to weeks, but full effect (e.g., for nail infections) can take months due to slow growth of keratinized tissues.
PeakEffect:
Dependent on the site of infection and tissue turnover (e.g., weeks for skin, months for nails).
DurationOfAction:
Persists in keratinized tissues as long as new keratin is formed, providing prolonged antifungal activity.
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
+ Difficulty breathing, swallowing, or talking
+ Unusual hoarseness
+ Swelling of the mouth, face, lips, tongue, or throat
Signs of lupus, including:
+ 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
+ Fatigue
+ Decreased appetite
+ Upset stomach or stomach pain
+ Light-colored stools
+ Vomiting
+ Yellow skin or eyes
Confusion
Abnormal burning, numbness, or tingling sensations
Redness or white patches in the mouth or throat
Severe skin reaction (Stevens-Johnson syndrome/toxic epidermal necrolysis), characterized by:
+ 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 may not experience any side effects or only minor ones, it's essential to discuss any concerns with your doctor. If you experience any of the following side effects or any other unusual symptoms, contact your doctor for advice:
Headache
Dizziness, fatigue, or weakness
Diarrhea
Stomach pain
Upset stomach
Vomiting
Difficulty 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
+ Difficulty breathing, swallowing, or talking
+ Unusual hoarseness
+ Swelling of the mouth, face, lips, tongue, or throat
Signs of lupus, including:
+ 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
+ Fatigue
+ Decreased appetite
+ Upset stomach or stomach pain
+ Light-colored stools
+ Vomiting
+ Yellow skin or eyes
Confusion
Abnormal burning, numbness, or tingling sensations
Redness or white patches in the mouth or throat
Severe skin reaction (Stevens-Johnson syndrome/toxic epidermal necrolysis), characterized by:
+ 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 may not experience any side effects or only minor ones, it's essential to discuss any concerns with your doctor. If you experience any of the following side effects or any other unusual symptoms, contact your doctor for advice:
Headache
Dizziness, fatigue, or weakness
Diarrhea
Stomach pain
Upset stomach
Vomiting
Difficulty 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:
- Severe headache, dizziness, confusion
- Numbness or tingling in hands or feet
- Yellowing of skin or eyes (jaundice), dark urine, pale stools, severe fatigue, persistent nausea/vomiting (signs of liver problems)
- Fever, sore throat, mouth sores, unusual bruising or bleeding (signs of blood problems)
- Severe skin rash, blistering, peeling skin, or swelling of the face/lips/tongue
- Severe sunburn reaction after sun exposure
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. Describe the allergic reaction you experienced, including the symptoms that occurred.
Certain health conditions, including liver disease or porphyria, as these may affect your ability to take this medication safely.
Additionally, women should discuss the following with their doctor:
If you are pregnant or think you may be pregnant. Do not take this medication if you are pregnant.
If you plan to become pregnant within 1 month after your last dose of this medication.
If you are breast-feeding or plan to breast-feed, as this may affect your ability to take this medication.
This medication may interact with other drugs or health conditions. Therefore, it is crucial to:
Inform your doctor and pharmacist about all medications you are taking, including prescription and over-the-counter drugs, natural products, and vitamins.
Discuss all your health problems with your doctor to ensure it is safe to take this medication.
Never start, stop, or change the dose of any medication without first consulting your doctor to avoid potential interactions or adverse effects.
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. Describe the allergic reaction you experienced, including the symptoms that occurred.
Certain health conditions, including liver disease or porphyria, as these may affect your ability to take this medication safely.
Additionally, women should discuss the following with their doctor:
If you are pregnant or think you may be pregnant. Do not take this medication if you are pregnant.
If you plan to become pregnant within 1 month after your last dose of this medication.
If you are breast-feeding or plan to breast-feed, as this may affect your ability to take this medication.
This medication may interact with other drugs or health conditions. Therefore, it is crucial to:
Inform your doctor and pharmacist about all medications you are taking, including prescription and over-the-counter drugs, natural products, and vitamins.
Discuss all your health problems with your doctor to ensure it is safe to take this medication.
Never start, stop, or change the dose of any medication without first consulting your doctor to avoid potential interactions or adverse effects.
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 exceed the recommended duration of treatment, as this may lead to a secondary infection. If you have a history of lupus, this medication can 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 contraceptives may be less effective in preventing pregnancy. To minimize the risk of unplanned pregnancy, use an additional form of birth control, such as condoms, 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 effective birth control methods while taking this medication and for 6 months after the final 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 exceed the recommended duration of treatment, as this may lead to a secondary infection. If you have a history of lupus, this medication can 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 contraceptives may be less effective in preventing pregnancy. To minimize the risk of unplanned pregnancy, use an additional form of birth control, such as condoms, 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 effective birth control methods while taking this medication and for 6 months after the final 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
- Oral Contraceptives (decreased efficacy of contraceptives, leading to breakthrough bleeding or pregnancy)
- Warfarin (decreased anticoagulant effect of warfarin)
- Barbiturates (e.g., Phenobarbital - decreased griseofulvin levels)
Moderate Interactions
- Alcohol (disulfiram-like reaction, tachycardia, flushing, nausea, vomiting)
- Cyclosporine (decreased cyclosporine levels)
- Salicylates (decreased griseofulvin absorption)
- Theophylline (decreased theophylline levels)
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) with differential
Rationale: To assess for baseline hematologic abnormalities, as rare cases of leukopenia or neutropenia have been reported.
Timing: Prior to initiation of therapy.
Routine Monitoring
Liver Function Tests (LFTs)
Frequency: Periodically (e.g., monthly or every 2-3 months) during prolonged therapy.
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) with differential
Frequency: Periodically (e.g., every 1-2 months) during prolonged therapy, especially if patient develops fever, sore throat, or other signs of infection.
Target: Within normal limits
Action Threshold: Discontinue if significant leukopenia or neutropenia develops.
Renal Function (BUN, Creatinine)
Frequency: Periodically, especially in patients with pre-existing renal impairment.
Target: Within normal limits
Action Threshold: Not a primary concern for dose adjustment, but monitor for overall health.
Symptom Monitoring
- Signs of liver injury (e.g., persistent nausea, anorexia, fatigue, jaundice, dark urine, right upper quadrant pain)
- Signs of hematologic abnormalities (e.g., fever, sore throat, unusual bleeding or bruising, pallor)
- Severe skin reactions (e.g., rash, blistering, peeling skin)
- Neurological symptoms (e.g., headache, dizziness, confusion, paresthesias)
- Gastrointestinal upset (e.g., nausea, vomiting, diarrhea)
- Photosensitivity (severe sunburn reaction)
Special Patient Groups
Pregnancy
Contraindicated in pregnancy due to potential for severe teratogenic effects (e.g., conjoined twins, skeletal and renal anomalies). Women of childbearing potential must use effective non-hormonal contraception during and for at least one month after treatment.
Trimester-Specific Risks:
First Trimester:
High risk of teratogenicity, especially during organogenesis.
Second Trimester:
Risk of fetal harm still present.
Third Trimester:
Risk of fetal harm still present.
Lactation
Griseofulvin is excreted into breast milk. Due to potential for serious adverse effects in the infant and lack of definitive safety data, breastfeeding is generally not recommended during treatment.
Infant Risk:
Potential for gastrointestinal upset, rash, and theoretical risk of carcinogenicity or other long-term effects. Risk category L4 (Potentially Hazardous).
Pediatric Use
Griseofulvin ultramicrosize is commonly used in pediatric patients for tinea capitis and other fungal infections. Dosing is weight-based. Safety and efficacy are established for children.
Geriatric Use
No specific dose adjustment is generally required based on age alone. However, geriatric patients may be more susceptible to adverse effects (e.g., CNS effects, liver dysfunction) and may have comorbidities or polypharmacy that require careful monitoring.
Clinical Information
Clinical Pearls
- Griseofulvin must be taken with a fatty meal to maximize absorption and efficacy.
- Treatment duration is often prolonged (weeks to months) depending on the infection site (e.g., 4-8 weeks for skin, 6-12 months for nails). Patient adherence is crucial.
- Advise patients about the importance of using effective non-hormonal contraception during and after treatment due to teratogenicity and interaction with oral contraceptives.
- Warn patients about photosensitivity and the need for sun protection.
- Educate patients about the disulfiram-like reaction with alcohol and advise strict avoidance.
- Regular monitoring of liver function tests is important, especially during long-term therapy.
Alternative Therapies
- Terbinafine (oral)
- Itraconazole (oral)
- Fluconazole (oral)
- Ketoconazole (oral - less common due to hepatotoxicity concerns)
- Topical antifungals (e.g., clotrimazole, miconazole, terbinafine cream) for localized, superficial infections.
Cost & Coverage
Average Cost:
$30 - $150 per 30 tablets (125mg ultramicrosize)
Generic Available:
Yes
Insurance Coverage:
Tier 1 or Tier 2 (Generic)
General Drug Facts
If your symptoms or health issues persist or worsen, it is essential to contact your doctor promptly. To ensure your safety, never share your medication with others or take someone else's medication. Some medications may come with an additional patient information leaflet, so it's a good idea to check with your pharmacist. If you have any questions or concerns about this medication, don't hesitate to discuss them with your doctor, nurse, pharmacist, or other healthcare provider. 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 information about the medication taken, the amount, and the time it happened.