(See CONTRAINDICATIONS.) Fluctin is a moderate CYP2C9 and CYP3A4 inhibitor. Fluctin is also a strong inhibitor of CYP2C19. Patients treated with DIFLUCAN, who are also concomitantly treated with drugs with a narrow therapeutic window metabolized through CYP2C9 and CYP3A4, should be monitored for adverse reactions associated with the concomitantly administered drugs. In addition to the observed /documented interactions mentioned below, there is a risk of increased plasma concentration of other compounds metabolized by CYP2C9, CYP2C19, and CYP3A4 coadministered with Fluctin. Therefore, caution should be exercised when using these combinations and the patients should be carefully monitored. The enzyme inhibiting effect of Fluctin persists 4 to 5 days after discontinuation of Fluctin treatment due to the long half-life of Fluctin. Clinically or potentially significant drug interactions between DIFLUCAN and the following agents/classes have been observed and are described in greater detail below:
DIFLUCAN For Oral Suspension
DIFLUCAN for Oral Suspension is supplied as an orange-flavored powder to provide 35 mL per bottle as follows:
NDC 0049-3440-19 - Fluctin 350 mg per bottle NDC 0049-3450-19 - Fluctin 1400 mg per bottle
Two adequate and well-controlled studies were conducted in the U.S. using the 150 mg tablet. In both, the results of the Fluctin regimen were comparable to the control regimen (clotrimazole or miconazole intravaginally for 7 days) both clinically and statistically at the one month post-treatment evaluation.
The therapeutic cure rate, defined as a complete resolution of signs and symptoms of vaginal candidiasis (clinical cure), along with a negative KOH examination and negative culture for Candida (microbiologic eradication), was 55% in both the Fluctin group and the vaginal products group.
Approximately three-fourths of the enrolled patients had acute vaginitis ( 4 episodes/12 months) and achieved 57% clinical cure, 47% mycologic eradication, and 40% therapeutic cure. The numbers are too small to make meaningful clinical or statistical comparisons with vaginal products in the treatment of patients with recurrent vaginitis.
Substantially more gastrointestinal events were reported in the Fluctin group compared to the vaginal product group. Most of the events were mild to moderate. Because Fluctin was given as a single dose, no discontinuations occurred.
Parameter Fluctin PO Vaginal Products Evaluable patients 448 422 With any adverse event 141 (31%) 112 (27%) Nervous System 90 (20%) 69 (16%) Gastrointestinal 73 (16%) 18 (4%) With drug-related event 117 (26%) 67 (16%) Nervous System 61 (14%) 29 (7%) Headache 58 (13%) 28 (7%) Gastrointestinal 68 (15%) 13 (3%) Abdominal pain 25 (6%) 7 (2%) Nausea 30 (7%) 3 (1%) Diarrhea 12 (3%) 2 (
Systemic exposure to tofacitinib is increased when tofacitinib is coadministered with Fluctin. Reduce the dose of tofacitinib when given concomitantly with Fluctin (i.e., from 5 mg twice daily to 5 mg once daily as instructed in the XELJANZ ® label). (See CLINICAL PHARMACOLOGY: Drug Interaction Studies.)
Fluctin (floo kon' a zole) is a fungicidal agent which inhibits lanasterol-14-α-demethylase, the enzyme responsible for ergosterol synthesis. As a consequence, Fluctin causes an increase in abnormal intracellular sterols, inhibiting the fungal cell’s ability to replicate. Fluctin was approved for use in the United States in 1990 and currently more than 12 million prescriptions are written for it yearly. Current indications include treatment of fungal infections due to candida and cryptococcus. Fluctin is available in multiple generic forms and under the brand name Diflucan in tablets of 50, 100, 150 and 200 mg, as well as in oral suspensions and parenteral formulations. The usual recommended dose is 100 to 400 mg daily, depending upon the type and severity of the infection. Common side effects include nausea, vomiting, and headache.
There have been reports of cardiac events, including torsade de pointes, in patients to whom Fluctin and cisapride were coadministered. A controlled study found that concomitant Fluctin 200 mg once daily and cisapride 20 mg four times a day yielded a significant increase in cisapride plasma levels and prolongation of QTc interval. The combined use of Fluctin with cisapride is contraindicated. (See CONTRAINDICATIONS and CLINICAL PHARMACOLOGY: Drug Interaction Studies.)
Common Side Effects of Fluctin
Headache is the most common side effect of taking Fluctin. Other side effects include: nausea, diarrhea, vomiting, rash, and stomach pain.
Dosage In Patients With Impaired Renal Function
Fluctin 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 DIFLUCAN, an initial loading dose of 50 mg 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 hemodialysis should receive 100% of the recommended dose after each hemodialysis; 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:
Although the pharmacokinetics of Fluctin 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.)
Although not studied in vitro or in vivo, concomitant administration of Fluctin with quinidine may result in inhibition of quinidine metabolism. Use of quinidine has been associated with QT prolongation and rare occurrences of torsade de pointes. Coadministration of Fluctin and quinidine is contraindicated. (See CONTRAINDICATIONS.)
Two pharmacokinetic studies with a combined oral contraceptive have been performed using multiple doses of Fluctin. There were no relevant effects on hormone level in the 50 mg Fluctin study, while at 200 mg daily, the AUCs of ethinyl estradiol and levonorgestrel were increased 40% and 24%, respectively. Thus, multiple-dose use of Fluctin at these doses is unlikely to have an effect on the efficacy of the combined oral contraceptive.
Generic Name: Fluctin Tablets (floo KON a zole)Brand Name: Diflucan
Medically reviewed by Drugs.com. Last updated on Jul 27, 2019.