Drug Interaction:
Azole anti-fungals include- Fluconazole, Itraconazole, Ketoconazole, Miconazole, Econazole, Terconazole
Interacting drugs- summary
+ Fluconazole
Cimetidine
fluconazole plasma levels reduced, possibly due to decreased absorption
Hydrochlorthiazide
concomittant use resulted in significant increase in fluconazole Cmax
and AUC which can be attributed to reduced renal clearance
Rifampin
a single oral fluconazole dose after chronic rifampin resulted in decrease
in AUC and a shorter half-life of fluconazole
Fluconazole +
Antihistamines Non sedating
although terfenadine levels were not affected by fluconazole, terfenadine
metabolite AUC increased
Contraceptives Oral
concurrent use with an OC containing ethinyl estradioal/levenogestrel
produced an overall mean increase in the levels of the OC components
Cyclosporine
significant increases in cyclosporine Cmax, Cmin.and AUC values occurred
following use.
Phenytoin
coadministration resulted in an increase of phenytoin AUC values
Theophylline
theophylline AUC , Cmax, and half-life were significantly increased and
clearance was decreased
Sulfonylureas
Fluconazole resulted in significant increases in Cmax and AUC of
tolbutamide, glyburide, and glipizide. Several subjects experienced
symptoms with hypoglycemia, requiring oral glucose treatment
Warfarin
a single warfarin dose of fluconazole resulted in an increase
in the PT response (area under the prothombin time-time curve).
Zidovudine
there was a significant increase in zidovudine AUC following fluconazole
administration
Indication:
U.S FDA APPROVED DRUGS FROM 01-01-08 TO 31-12-08
Drug name Indication Date of Approval
116. Fluconazole Dispersible tablets 50mg 22-04-08
haemagglutinin complex
(Addl.indication)
For the treatment of systemic candidiatis,
mucosal candidiasis, prevention of fungal infections
in patients with malignancy
199. Fluconazole 15-09-08
+ Zinc Pyrethrone (Each 30/60ml
bottle contains: 2% +1%) Lotion
For the treatment of seborrhoeic dermatitis
Azole anti-fungals include- Fluconazole, Itraconazole, Ketoconazole, Miconazole, Econazole, Terconazole
U.S FDA APPROVED DRUGS DURING 2004
222. Flucanazole Gel (0.5%) 12-08-2004
Anti-fungal
Approved by (DCI) Drug Controller GENERAL - India For Marketing
(Ref- IDMA Publication)
Name of Drug Indication Date of Approval
Fluconazole Systemic Antifungals January 1993
FIXED DOSE COMBINATIONS APPROVED BY DCG(I)
FROM JANUARY 1961 TILL NOVEMBER 2014
Name of Drug Indication Date of Approval
1.Combipack of 1 tablet of Fluconazole 150mg 07-06-1999
1 Film coated tablet of Azithromycin dihydrate eq.to
Azithomycin 1gm &
2 Film coated tablet of Secnidazole 1gm
2. Fluconazole 2% + 22-02-2005
Zinc Pyrethione 1% suspension
For seborrhic dermatitis
3.Fluconazole + 15-09-2008
Zinc Pyrethionone
Each 30/60ml bottle contain: 2% + 1% lotion
For the treatment of seborrhoeic dermatitis
Patent Expiry Date of drugs (Ref - IDMA Publication)
Chemical Category Manufacturer/ US Patent
Ingredient- Marketer Expiration Date
Fluconazole Antibiotics/ Pfizer Inc. 03-07-2005
and Antifungals
Adverse Reaction:
Nausea, headache, abdominal pain, diarrhoea,dyspepsia, dizziness, taste perversion Angioedema Anaphylactic reactions( rare)
Most reactions were mild to moderate in severity.
Others reported
Exfoliative skin disorders, including- Stevens-Johnson syndrome and toxic epidermal necrolysis. alopecia, leukopenia, thrmbocytopenia, hypercholesterolemia, hyperglyceridemia, hypokalemia, serious hepatic reactions
Lab test abnormalities- Increase in AST levels from baseline value of 30 to 41IU/L Overall rate of serum transminase elevations of more than 8 times the upper limit of normal was approximately 1% in fluconazole treated patients in clinical trials.
Contra-Indications:
Hypersens,advanced liver disease,lactation.
Special precautions:
Pregnancy, renal/liver disease. Immunosupressive disease.
Single-dose use- Weigh the convenience and efficacy of the single dose regimen for treatment of vaginal yeast infections against the acceptability of a higher incidence of adverse reactions with fluconazole (26%) vs intravaginal agents (16%)
Warnings-
Causative organisms- obtain specimen for fungal culture and other relevant laboratories studies ( seriology, histopathology) prior to therapy and identify causative organisms. Therapy may be instituted before the results are known, however, once the results become avilable, adjust anti-infective therapy accordingly.
Hepatic injury-
Fluconazole has been associated with rare cases of serious hepatic injury. Patients who develop abnormal liver function tests during fluconazole therapy should be monitored for development of more severe hepatic injury.
Fluconazole should be discontinued if clinical signs and symptoms consistent with liver disease develop that may be attributable to fluconazole.
Anaphylaxis- in rare cases, anphylaxis has occurred.
Dermatologic changes- patients have rarely developed exfoliative skin disorders during treatment with fluconazole.
Pregnancy- use in pregnancy only if the potential benefits justifies the possible risk to the fetus.
Lactation- Use of fluconazole in nursing mothers is not recommended
Children- Safety and efficacy of the single-dose regimen for vaginal candidiasis in patients < 18 years
of age has not been established
Dosages/ Overdosage Etc:
For the treatment of seborrhoeic dermatitis
Dosage-
Single dose-
Vaginal candiadiasis- 150mg as a single oral dose
Multiple dose-
Individualise dose.
Orapharyngeal candiadiasis- 200mg on first day ,followedby 100mg once daily.
Esophagealcandidiasis- 200mg on first day followed by 100mg once daily
Candiadiasis- for candial UTIs and peritonitis- 50 to 200mg/ day has beenused.
Prevention of candiadiasis- bone marrow transplant- 400mg once daily
Pediatric patients-
3mg/kg
6mg/kg
12mg/kg per day
Overdosage-
Symptoms
Onereported case of overdosage
Decreased motility, and respiration, ptosis,lacrimation, salivation, urinary incontinence,loss of righting reflex andcyanosis,death was sometimes preceded by clonic convulsions.
Treatment
1. Institute symptomatic treatment with suppoprtive measures and gastric lavage if clinically indicated.
Missed dose-
1. If you miss a dose of this medicine, take it as soon as possible.
2. However, if it is almost time for next dose, skip the missed dose and go back to your regular dosing schedule.
3. Do not double doses.
Other Information:
For Availability/supplies
Contact -
1.Indian Drug Manufacturers Association (IDMA)
Phone- 022- 24944624/ 24974308
Fax- 022- 24950723
Email- idma@vsnl.com
Website: www.idma-assn.org
2.Bulk Drug Manufacturers Association (India)(BDMA)
Phone - 040-23703910/ 23706718
Fax- 040-23704804
Email- info@bdmai.org
Website: www.info@bdmai.org
Patient Information:
Refer Ketoconazole
Pharmacology/ Pharmacokinetics:
Pharmacology:
Fluconazole a synthetic broad spetrum bis-triazole antifungal agent, is a selective inhibitor of fungal P-450 and strol C-14 alpha demethylation.
Pharmacokinetics:
Peak plasma concentrations occur between 1 and 2 hours with a terminal plasma elimination half-life of about 30 hours (range 20 to 50) after oral admin. Fluconazole is cleared primarily by renal excretion with about 80% ot the dose appearing in the urine unchanged, and about 11% as metabolites.
Interaction with Food:
Not significant
Pregnancy and lactation:
Pregnancy:
Use in pregnancy only if the potential benefits justifies the potential risk to the fetus.
Lactation:
Use not reccommended in nursing mothers.
Children-
Safety and efficacy of the single-dose regimen for vaginal candidiasis in patients < 18 years of age has not been established
Manufacturer Details