Fungolon 100mg Uses

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What is Fungolon 100mg?

Fungolon 100mg injection is used to treat serious fungal or yeast infections, such as vaginal candidiasis, oropharyngeal candidiasis (thrush, oral thrush), esophageal candidiasis (candida esophagitis), other candida infections (including urinary tract infections, peritonitis [inflammation of the lining of the abdomen or stomach], and infections that may occur in different parts of the body), or fungal (cryptococcal) meningitis. Fungolon 100mg works by killing the fungus or yeast, or preventing its growth.

Fungolon 100mg injection is also used to prevent candidiasis in patients having bone marrow transplants, who receive cancer or radiation treatment.

Fungolon 100mg is to be given only by or under the direct supervision of a doctor.

Fungolon 100mg indications

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Fungolon 100mg tablets, USP are indicated for the treatment of:

  1. Vaginal candidiasis (vaginal yeast infections due to Candida).
  2. Oropharyngeal and esophageal candidiasis. In open noncomparative studies of relatively small numbers of patients, Fungolon 100mg tablets, USP were also effective for the treatment of Candida urinary tract infections, peritonitis and systemic Candida infections including candidemia, disseminated candidiasis and pneumonia.
  3. Cryptococcal meningitis. Before prescribing Fungolon 100mg tablets, USP for AIDS patients with cryptococcal meningitis, please see CLINICAL STUDIES section. Studies comparing Fungolon 100mg to amphotericin B in non-HIV infected patients have not been conducted.

Prophylaxis. Fungolon 100mg tablets, USP are also indicated to decrease the incidence of candidiasis in patients undergoing bone marrow transplantation who receive cytotoxic chemotherapy and/or radiation therapy.

Specimens for fungal culture and other relevant laboratory studies (serology, histopathology) should be obtained prior to therapy to isolate and identify causative organisms. Therapy may be instituted before the results of the cultures and other laboratory studies are known; however, once these results become available, anti-infective therapy should be adjusted accordingly.

How should I use Fungolon 100mg?

Use Fungolon 100mg solution as directed by your doctor. Check the label on the medicine for exact dosing instructions.

Ask your health care provider any questions you may have about how to use Fungolon 100mg solution.

Uses of Fungolon 100mg in details

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Use: Labeled Indications

Treatment of candidiasis (esophageal, oropharyngeal, peritoneal, urinary tract, vaginal); systemic candida infections (eg, candidemia, disseminated candidiasis, pneumonia); and cryptococcal meningitis; and antifungal prophylaxis in allogeneic hematopoietic cell transplant recipients

Off Label Uses

Blastomycosis

Data from a randomized, multicenter, open-label study comparing Fungolon 100mg 400 mg versus 800 mg suggest that the use of Fungolon 100mg at each of these doses is effective for the treatment of non-life-threatening blastomycosis.

Fungolon 100mg description

A semisynthetic antibiotic produced from Streptomyces mediterranei. It has a broad antibacterial spectrum, including activity against several forms of Mycobacterium. In susceptible organisms it inhibits DNA-dependent RNA polymerase activity by forming a stable complex with the enzyme. It thus suppresses the initiation of RNA synthesis. Fungolon 100mg is bactericidal, and acts on both intracellular and extracellular organisms. (From Gilman et al., Goodman and Gilman&

Fungolon 100mg dosage

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Dosage and Administration in Adults

Single Dose: Vaginal Candidiasis: The recommended dosage of Fungolon 100mg for vaginal candidiasis is 150 mg as a single oral dose.

Multiple Dose: SINCE ORAL ABSORPTION IS RAPID AND ALMOST COMPLETE, THE DAILY DOSE OF Fungolon 100mg IS THE SAME FOR ORAL (TABLETS AND SUSPENSION) AND INTRAVENOUS ADMINISTRATION. In general, a loading dose of twice the daily dose is recommended on the first day of therapy to result in plasma concentrations close to steady-state by the second day of therapy.

The daily dose of Fungolon 100mg for the treatment of infections other than vaginal candidiasis should be based on the infecting organism and the patient’s response to therapy. Treatment should be continued until clinical parameters or laboratory tests indicate that active fungal infection has subsided. An inadequate period of treatment may lead to recurrence of active infection. Patients with AIDS and cryptococcal meningitis or recurrent oropharyngeal candidiasis usually require maintenance therapy to prevent relapse.

Oropharyngeal Candidiasis: The recommended dosage of Fungolon 100mg for oropharyngeal candidiasis is 200 mg on the first day, followed by 100 mg once daily. Clinical evidence of oropharyngeal candidiasis generally resolves within several days, but treatment should be continued for at least 2 weeks to decrease the likelihood of relapse.

Esophageal Candidiasis: The recommended dosage of Fungolon 100mg for esophageal candidiasis is 200 mg on the first day, followed by 100 mg once daily. Doses up to 400 mg/day may be used, based on medical judgment of the patient’s response to therapy. Patients with esophageal candidiasis should be treated for a minimum of three weeks and for at least two weeks following resolution of symptoms.

Systemic Candida Infections: For systemic Candida infections including candidemia, disseminated candidiasis, and pneumonia, optimal therapeutic dosage and duration of therapy have not been established. In open, noncomparative studies of small numbers of patients, doses of up to 400 mg daily have been used.

Urinary Tract Infections and Peritonitis: For the treatment of Candida urinary tract infections and peritonitis, daily doses of 50 to 200 mg have been used in open, noncomparative studies of small numbers of patients.

Cryptococcal Meningitis: The recommended dosage for treatment of acute cryptococcal meningitis is 400 mg on the first day, followed by 200 mg once daily. A dosage of 400 mg once daily may be used, based on medical judgment of the patient’s response to therapy. The recommended duration of treatment for initial therapy of cryptococcal meningitis is 10 to 12 weeks after the cerebrospinal fluid becomes culture negative. The recommended dosage of Fungolon 100mg for suppression of relapse of cryptococcal meningitis in patients with AIDS is 200 mg once daily.

Prophylaxis in Patients Undergoing Bone Marrow Transplantation: The recommended Fungolon 100mg daily dosage for the prevention of candidiasis in patients undergoing bone marrow transplantation is 400 mg, once daily. Patients who are anticipated to have severe granulocytopenia (less than 500 neutrophils per cu mm) should start Fungolon 100mg prophylaxis several days before the anticipated onset of neutropenia, and continue for 7 days after the neutrophil count rises above 1000 cells per cu mm.

Dosage and Administration in Children

The following dose equivalency scheme should generally provide equivalent exposure in pediatric and adult patients:

Experience with Fungolon 100mg in neonates is limited to pharmacokinetic studies in premature newborns. Based on the prolonged half-life seen in premature newborns (gestational age 26 to 29 weeks), these children, in the first two weeks of life, should receive the same dosage (mg/kg) as in older children, but administered every 72 hours. After the first two weeks, these children should be dosed once daily. No information regarding Fungolon 100mg pharmacokinetics in full-term newborns is available.

Oropharyngeal Candidiasis: The recommended dosage of Fungolon 100mg for oropharyngeal candidiasis in children is 6 mg/kg on the first day, followed by 3 mg/kg once daily. Treatment should be administered for at least 2 weeks to decrease the likelihood of relapse.

Esophageal Candidiasis: For the treatment of esophageal candidiasis, the recommended dosage of Fungolon 100mg in children is 6 mg/kg on the first day, followed by 3 mg/kg once daily. Doses up to 12 mg/kg/day may be used based on medical judgment of the patient’s response to therapy. Patients with esophageal candidiasis should be treated for a minimum of three weeks and for at least 2 weeks following the resolution of symptoms.

Systemic Candida Infections: For the treatment of candidemia and disseminated Candida infections, daily doses of 6 to 12 mg/kg/day have been used in an open, noncomparative study of a small number of children.

Cryptococcal Meningitis: For the treatment of acute cryptococcal meningitis, the recommended dosage is 12 mg/kg on the first day, followed by 6 mg/kg once daily. A dosage of 12 mg/kg once daily may be used, based on medical judgment of the patient’s response to therapy. The recommended duration of treatment for initial therapy of cryptococcal meningitis is 10 to 12 weeks after the cerebrospinal fluid becomes culture negative. For suppression of relapse of cryptococcal meningitis in children with AIDS, the recommended dose of Fungolon 100mg is 6 mg/kg once daily.

Dosage in Patients with Impaired Renal Function

Fungolon 100mg is cleared primarily by renal excretion as unchanged drug. There is no need to adjust single dose therapy for vaginal candidiasis because of impaired renal function. In patients with impaired renal function who will receive multiple doses of Fungolon 100mg, an initial loading dose of 50 to 400 mg should be given. After the loading dose, the daily dose (according to indication) should be based on the following table:

Patients on regular dialysis should receive 100% of the recommended dose after each dialysis; on non-dialysis days, patients should receive a reduced dose according to their creatinine clearance.

These are suggested dose adjustments based on pharmacokinetics following administration of multiple doses. Further adjustment may be needed depending upon clinical condition.

When serum creatinine is the only measure of renal function available, the following formula (based on sex, weight, and age of the patient) should be used to estimate the creatinine clearance in adults:

Females: 0.85 x above value

Although the pharmacokinetics of Fungolon 100mg has not been studied in children with renal insufficiency, dosage reduction in children with renal insufficiency should parallel that recommended for adults. The following formula may be used to estimate creatinine clearance in children:

(Where K=0.55 for children older than 1 year and 0.45 for infants.)

Administration

Fungolon 100mg for

Oral Suspension USP is administered orally. Fungolon 100mg can be taken with or without food.

Directions for Mixing the

Oral Suspension

Prepare a suspension at time of dispensing as follows: tap bottle until all the powder flows freely. To reconstitute, add 24 mL of distilled water or Purified Water (USP) to Fungolon 100mg bottle and shake vigorously to suspend powder. Each bottle will deliver 35 mL of suspension. The concentrations of the reconstituted suspensions are as follows:

Note: Shake oral suspension well before using. Before Reconstitution: Store at 20° to 25°C (68° to 77°F). After Reconstitution: Store suspension at 5° to 25°C (41° to 77°F). Discard unused portion after 2 weeks. Protect from freezing.

Fungolon 100mg interactions

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What other drugs will affect Fungolon 100mg?

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Anticoagulants: Bleeding events (bruising, epistaxis, gastrointestinal bleeding, hematuria, and melena), have been reported, in association with increases in prothrombin time in patients receiving Fungolon 100mg concurrently with warfarin. Prothrombin time in patients receiving coumarin-type anticoagulant should be carefully monitored.

Azithromycin: There was no significant pharmacokinetic interaction between Fungolon 100mg and Azithromycin.

Benzodiazepines (Short Acting): Following oral administration of midazolam, Fungolon 100mg resulted in substantial increases in midazolam concentrations and psychomotor effects. This effect on midazolam appears to be more pronounced following oral administration of Fungolon 100mg than with Fungolon 100mg administered intravenously. If concomitant benzodiazepine therapy is necessary in patients being treated with Fungolon 100mg, consideration should be given to decreasing the benzodiazepine dosage, and the patients should be appropriately monitored.

Cisapride: Cisapride increased risk of ventricular arrhythmia troubles notably torsades de pointes. The interaction between Fungolon 100mg and cisapride yielded significant increase in cisapride plasma levels and prolongation of QTc interval. Coadministration of cisapride is contraindicated in patients receiving Fungolon 100mg.

Cyclosporin: Fungolon 100mg slowly increase cyclosporin concentrations in renal transplant patients. Fungolon 100mg did not affect cyclosporine levels in patients with bone marrow transplants. Cyclosporin plasma concentration monitoring in patients receiving Fungolon 100mg is recommended.

Hydrochlorothiazide: Interaction between multiple-dose hydrochlorothiazide and Fungolon 100mg has increased plasma concentrations of Fungolon 100mg by 40%. An effect of this magnitude should not necessitate a change in the Fungolon 100mg dose regimen in subjects receiving concomitant diuretics, although the prescriber should bear it in mind.

Oral Contraceptives:

Multiple dose use of Fungolon 100mg at these doses is unlikely to have an effect on the efficacy of the combined oral contraceptive.

Phenytoin: Concomitant administration of Fungolon 100mg and phenytoin may increase the levels of phenytoin to a clinically significant degree. If it is necessary to administer both drugs concomitantly, phenytoin levels should be monitored and the phenytoin dose adjusted to maintain therapeutic levels.

Pimozide: Combination of Fungolon 100mg will increase the risk of ventricular arrhythmia troubles notably torsades de pointes.

Rifabutin: An interaction exists when Fungolon 100mg is administered concurrently with rifabutin, leading to increased serum levels of rifabutin. There have been reports of uveitis in patients to whom Fungolon 100mg and rifabutin were coadministered. Patients receiving rifabutin and Fungolon 100mg concomitantly should be carefully monitored.

Rifampicin: Concomitant administration of Fungolon 100mg and rifampicin resulted in a 25% decrease in the AUC and a 20% shorter half-life of Fungolon 100mg. In patients receiving concomitant rifampicin, an increase of the Fungolon 100mg dose should be considered.

Sulfonylureas: Fungolon 100mg has been shown to prolong the serum half-life of concomitantly administered oral sulfonylureas (chlorpropamide, glibenclamide, glipizide and tolbutamide) in healthy volunteers. Fungolon 100mg and oral sulfonylureas may be coadministered to diabetic patients, but the possibility of a hypoglycemic episode should be borne in mind.

Tacrolimus: An interaction exists when Fungolon 100mg is administered concomitantly with tacrolimus, leading to increased serum levels of tacrolimus. There have been reports of nephrotoxicity in patients also. Patients receiving tacrolimus and Fungolon 100mg concomitantly should be carefully monitored.

Terfenadine: Concomitant Fungolon 100mg and terfenadine causes palpitations, tachycardia, dizziness, and chest pain where the relationship of the adverse events to drug therapy or underlying medical condition was not clear. Because of the potential seriousness of such an interaction, it is recommended that terfenadine not be taken in combination with Fungolon 100mg.

Theophylline: Patients who are receiving high dose theophylline or who are otherwise at increased risk for theophylline toxicity should be observed for signs of theophylline toxicity while receiving Fungolon 100mg, and therapy modified appropriately it signs of toxicity develop.

Zidovudine: Increased levels of zidovudine most likely caused by the decreased conversion of zidovudine to its major metabolite. Patients receiving this combination of Fungolon 100mg and zidovudine should be monitored for the development of zidovudine-related adverse reaction.

Use of Fungolon 100mg in combination with astemizole or other drugs metabolized by the cytochrome P-450 system may be associated with elevations in serum levels of these drugs.

Oral Fungolon 100mg is coadministered with food, cimetidine, antacids or following total body irradiation for bone marrow transplantation. No clinically significant impairment of Fungolon 100mg absorption.

Fungolon 100mg side effects

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What are the possible side effects of Fungolon 100mg?

Fungolon 100mg is generally well tolerated.

In some patients, particularly those with serious underlying diseases such as AIDS and cancer, changes in renal and hematological function test results and hepatic abnormalities have been observed during treatment with Fungolon 100mg and comparative agents, but the clinical significance and relationship to treatment is uncertain.

In Patients Receiving a Single Dose for Vaginal Candidiasis

During comparative clinical studies conducted in the United States, 448 patients with vaginal candidiasis were treated with Fungolon 100mg, 150 mg single dose. The overall incidence of side effects possibly related to Fungolon 100mg was 26%. In 422 patients receiving active comparative agents, the incidence was 16%. The most common treatment-related adverse events reported in the patients who received 150 mg single dose Fungolon 100mg for vaginitis were headache (13%), nausea (7%), and abdominal pain (6%). Other side effects reported with an incidence equal to or greater than 1% included diarrhea (3%), dyspepsia (1%), dizziness (1%), and taste perversion (1%). Most of the reported side effects were mild to moderate in severity. Rarely, angioedema and anaphylactic reaction have been reported in marketing experience

In Patients Receiving Multiple Doses for Other Infections

Sixteen percent of over 4000 patients treated with Fungolon 100mg in clinical trials of 7 days or more experienced adverse events. Treatment was discontinued in 1.5% of patients due to adverse clinical events and in 1.3% of patients due to laboratory test abnormalities.

Clinical adverse events were reported more frequently in HIV infected patients (21%) than in non-HIV infected patients (13%); however, the patterns in HIV infected and non-HIV infected patients were similar. The proportions of patients discontinuing therapy due to clinical adverse events were similar in the two groups (1.5%).

The following treatment-related clinical adverse events occurred at an incidence of 1% or greater in 4048 patients receiving Fungolon 100mg for 7 or more days in clinical trials: nausea 3.7%, headache 1.9%, skin rash 1.8%, vomiting 1.7%, abdominal pain 1.7%, and diarrhea 1.5%.

Hepatobiliary: In combined clinical trials and marketing experience, there have been rare cases of serious hepatic reactions during treatment with Fungolon 100mg.. The spectrum of these hepatic reactions has ranged from mild transient elevations in transaminases to clinical hepatitis, cholestasis and fulminant hepatic failure, including fatalities. Instances of fatal hepatic reactions were noted to occur primarily in patients with serious underlying medical conditions (predominantly AIDS or malignancy) and often while taking multiple concomitant medications. Transient hepatic reactions, including hepatitis and jaundice, have occurred among patients with no other identifiable risk factors. In each of these cases, liver function returned to baseline on discontinuation of Fungolon 100mg.

In two comparative trials evaluating the efficacy of Fungolon 100mg for the suppression of relapse of cryptococcal meningitis, a statistically significant increase was observed in median AST (SGOT) levels from a baseline value of 30 IU/L to 41 IU/L in one trial and 34 IU/L to 66 IU/L in the other. The overall rate of serum transaminase elevations of more than 8 times the upper limit of normal was approximately 1% in Fungolon 100mg-treated patients in clinical trials. These elevations occurred in patients with severe underlying disease, predominantly AIDS or malignancies, most of whom were receiving multiple concomitant medications, including many known to be hepatotoxic. The incidence of abnormally elevated serum transaminases was greater in patients taking Fungolon 100mg concomitantly with one or more of the following medications: rifampin, phenytoin, isoniazid, valproic acid, or oral sulfonylurea hypoglycemic agents.

Post-Marketing Experience

In addition, the following adverse events have occurred during post-marketing experience.

Immunologic: In rare cases, anaphylaxis (including angioedema, face edema and pruritus) has been reported.

Body as a Whole: Asthenia, fatigue, fever, malaise.

Cardiovascular: QT prolongation, torsades de pointes.

Central Nervous System: Seizures, dizziness.

Hematopoietic and Lymphatic: Leukopenia, including neutropenia and agranulocytosis, thrombocytopenia.

Metabolic: Hypercholesterolemia, hypertriglyceridemia, hypokalemia.

Gastrointestinal: Cholestasis, dry mouth, hepatocellular damage, dyspepsia, vomiting.

Other Senses: Taste perversion.

Musculoskeletal System: Myalgia.

Nervous System: Insomnia, paresthesia, somnolence, tremor, vertigo.

Skin and Appendages: Acute generalized exanthematous-pustulosis, drug eruption, increased sweating, exfoliative skin disorders including Stevens-Johnson syndrome and toxic epidermal necrolysis, alopecia.

Adverse Reactions in Children

The pattern and incidence of adverse events and laboratory abnormalities recorded during pediatric clinical trials are comparable to those seen in adults.

In Phase II/III clinical trials conducted in the United States and in Europe, 577 pediatric patients, ages 1 day to 17 years were treated with Fungolon 100mg at doses up to 15 mg/kg/day for up to 1,616 days. Thirteen percent of children experienced treatment-related adverse events. The most commonly reported events were vomiting (5%), abdominal pain (3%), nausea (2%), and diarrhea (2%). Treatment was discontinued in 2.3% of patients due to adverse clinical events and in 1.4% of patients due to laboratory test abnormalities. The majority of treatment-related laboratory abnormalities were elevations of transaminases or alkaline phosphatase.

Fungolon 100mg contraindications

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What is the most important information I should know about Fungolon 100mg?

Fungolon 100mg is contraindicated in patients who have shown hypersensitivity to Fungolon 100mg or to any of its excipients. There is no information regarding cross-hypersensitivity between Fungolon 100mg and other azole antifungal agents. Caution should be used in prescribing Fungolon 100mg to patients with hypersensitivity to other azoles. Coadministration of terfenadine is contraindicated in patients receiving Fungolon 100mg at multiple doses of 400 mg or higher based upon results of a multiple dose interaction study. Coadministration of other drugs known to prolong the QT interval and which are metabolized via the enzyme CYP3A4 such as cisapride, astemizole, erythromycin, pimozide and quinidine are contraindicated in patients receiving Fungolon 100mg.

Active ingredient matches for Fungolon 100mg:

Fluconazole in Bulgaria.


List of Fungolon 100mg substitutes (brand and generic names)

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Unit description / dosage (Manufacturer)Price, USD
FUNGONIL TABLET 1 strip / 1 tablet each (Mars Therapeutics & Chemicals Ltd)$ 0.15
Fungout 150 mg Tablet (Indamed Pharmaceuticals Pvt. Ltd)$ 0.17
Fungoz 150 mg Tablet (Klintoz Pharmaceuticals Pvt Ltd)$ 0.29
Funiz 150 mg Tablet (Anikem Laboratories)$ 0.20
Funmax 150 mg Tablet (Elcure Pharmaceuticals)$ 0.19
Funmax 50 mg Tablet (Elcure Pharmaceuticals)$ 0.12
Funnie 50mg DT-TAB / 2 (Invision (Infalife))$ 0.27
50 mg x 2's (Invision (Infalife))$ 0.27
FUNNIE dispertab 50 mg x 2's (Invision (Infalife))$ 0.27
Funnie DT 50 mg Tablet (Infalife (Invision Medi Sciences))$ 0.13
Funo 150 mg Tablet (Pentamark Organics)$ 0.04
FUNSPOR Capsule/ Tablet / 150mg / 1 units (DWD Pharmaceuticals Ltd.)$ 0.18
150 mg x 1's (DWD Pharmaceuticals Ltd.)$ 0.18
Funspor 150mg TAB / 1 (DWD Pharmaceuticals Ltd.)$ 0.18
Funspor 150 mg Tablet (DWD Pharmaceuticals Ltd.)$ 0.18
FUNSPOR 150MG TABLET 1 strip / 1 tablet each (DWD Pharmaceuticals Ltd.)$ 0.18
FUNSPOR tab 150 mg x 1's (DWD Pharmaceuticals Ltd.)$ 0.18
Funspor 150mg TAB / 1 (DWD Pharmaceuticals Ltd.)$ 0.18
Funspor 150mg Tablet (DWD Pharmaceuticals Ltd.)$ 0.18
Funtin 150 mg Tablet (Indoss Life Sciences (Oscar Remedies Pvt. Ltd))$ 0.18
Funzela 50 mg x 20's (Biofemme)$ 48.21
Funzela 150 mg x 1's (Biofemme)$ 7.29
Funzela 200 mg x 10's (Biofemme)$ 186.69
Funzela 150 mg x 4's (Biofemme)$ 18.60
Capsule; Oral; Fluconazole 100 mg (Avyukt)
Capsule; Oral; Fluconazole 150 mg (Avyukt)
Capsule; Oral; Fluconazole 50 mg (Avyukt)

References

  1. DailyMed. "FLUCONAZOLE: DailyMed provides trustworthy information about marketed drugs in the United States. DailyMed is the official provider of FDA label information (package inserts).". https://dailymed.nlm.nih.gov/dailyme... (accessed September 17, 2018).
  2. PubChem. "fluconazole". https://pubchem.ncbi.nlm.nih.gov/com... (accessed September 17, 2018).
  3. DrugBank. "fluconazole". http://www.drugbank.ca/drugs/DB00196 (accessed September 17, 2018).

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