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Diflucan Review Article

 

urinary and vaginal infectionsDiflucan (generic name: fluconazole) is an antifungal drug used to treat the fungal infections like yeast infections of the vagina, throat, esophagus, lungs, mouth and other organs. It is also used to treat the meningitis caused by fungus. Diflucan (fluconazole) is also used to prevent the yeast infections in patients who are undergoing the treatment with the chemotherapy and radiotherapy before a bone marrow transplant as there is risk of yeast infections during this treatment. Diflucan (fluconazole) is used to prevent both the systemic as well as the superficial fungal infections. b>Mechanism of action Diflucan (fluconazole) inhibits the fungal cytochrome P450 enzyme 14α-demethylase. The demethylase enzyme which is present in the human body is less sensitive to the Diflucan (fluconazole) thus Diflucan (fluconazole) only inhibits the demethylase enzyme found in the fungus. The inhibition of fungal demethylase by Diflucan (fluconazole) ultimately leads to the inhibition of ergosterol synthesis from the lanosterol. As there is no ergosterol synthesis thus the fungal cytoplasmic membrane becomes weaken and the cellular permeability of fungus is increased and thus leakage of cellular components occurs which leads to the death of the fungus. (Borgers., et al 1980). Continue reading...

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CandidaIndications

Diflucan (fluconazole) can be used for both the prophylaxis and treatment of fungal infections including Tinea corporis, Candidiasis, tinea pedis, tinea cruris, Cryptococcal meningitis, Onychomycosis.

It can also be used as the first line treatment of Coccidioidomycosis, Histoplasmosis and Cryptococcosis.

Contraindications

Diflucan (fluconazole) is contraindicated in the patients who are hypersensitive to it. It is also contraindicated in the patients who are taking the terfenadine and quinidine. Similarly Diflucan (fluconazole) is also contraindicated in the pregnancy.
Warnings and precautions

There are no adequate studies of Diflucan (fluconazole) on the pregnant women. In a few published case reports it was revealed that when the Diflucan (fluconazole) is used during the pregnancy especially in high doses then it has the damaging effect on the fetus. Food and drug administration (FDA) is also saying that the treatment with the high doses i.e. about 400-800 mg/day of Diflucan (fluconazole) during the pregnancy (first trimester) may produce the birth defects in infants thus the use of Diflucan (fluconazole) during pregnancy should be avoided.

Diflucan (fluconazole) should be administered with caution in patients having proarrhythmic conditions. It should also be used with caution in patients having renal dysfunction.


Adverse drug reactions

The adverse drug reactions associated with the Diflucan (fluconazole) therapy includes the rash, dizziness, headache, diarrhea, stomach pain, heart burn, nausea, vomiting, anorexia, fatigue and constipation.


Over dosage

Overdose of the Diflucan (fluconazole) leads towards the paranoid behavior and hallucination. If the overdose of the Diflucan (fluconazole) occurs then immediately symptomatic treatment is given. In the symptomatic treatment gastric lavage is carried out and supportive therapy is given to the patient.

Clinical trials

In a study (Moorhead et al., 2011) it has been observed that the Diflucan (fluconazole) can treat the breast and nipple thrush. In this study the women suffering from nipple and breast Candida were treated with the 150mg capsules of the Diflucan (fluconazole) and it was observed in the study that the women having severe breast pain needed more than 3 capsules than the women with less severe pain.

In another study (Cordeiro Rde et al., 2011) it has been observed that the cotrimoxazole enhances the in vitro susceptibility of Coccidioides posadasii strains to antifungals like itraconazole, Diflucan (fluconazole), amphotericin B and voriconazole. It was also observed in this study that the cotrimoxazole itself inhibited the strains of Coccidioides posadasii.

In another study (Liu et al., 2011) it was also found that the corneal permeability of the Diflucan (fluconazole) eye drops can be increased by the permeability enhancers like menthol and borneol.

A study (Ascher et al., 2011) has also revealed that when the infants suffering from invasive candidiasis were treated with the amphotericin B lipid products then their mortality rate was high as compared to the infants treated with the Diflucan (fluconazole).

In a study (Lass-florl at al., 2011) different antifungal drugs are studied for the different types of fungal infections. In this study it was observed that the Diflucan (fluconazole) plays an excellent role in the prophylaxis, empirical therapy and the treatment of both invasive and superficial yeast fungal infections. In this study it was also observed that the voriconazole can be strongly recommended for the pulmonary invasive aspergillosis. Similarly itraconazole plays an important role in the treatment of the fungal skin and nail infections as well as helpful in the treatment of the dematiaceous fungi and endemic mycoses. In the same study it was also observed that the posaconazole may prove helpful in the treatment of the invasive aspergillosis and can also be used prophylactically in patients with neutropenia and haematopoietic stem-cell transplant recipients.

Drug interactions

Diflucan (fluconazole) has the drug-drug interactions with the different types of drugs. Hypoglycemic is precipitated by the concomitant use of Diflucan (fluconazole) with the oral hypoglycemic agents. Diflucan (fluconazole) increases the plasma concentration of phenytoin, theophylline, halofantrine and midazolam when used in combination with these drugs.


Dosage forms, Dose and administration

Diflucan (fluconazole) is available in different dosage forms. It is available in the form of tablets for the oral administration. It is also available in the form of oral suspension, and in the form of solution for the intravenous administration.

In the tablet dosage form it is available in the dose of 50,100,150 or 200 mg while in the case of oral suspension it is available in the dose of 10mg or 40 mg per ml. Similarly in case of injection it is available in the dose of 2mg per ml.

In case of Vaginal candidiasis Diflucan (fluconazole) is given as a single oral dose of 150mg. While in case of oropharyngeal candidiasis and esophageal candidiasis first dose of 200mg of Diflucan (fluconazole) is given on the first day then 100mg is given once daily. Similarly in case of Systemic Candida infections Diflucan (fluconazole) dose of up to 400mg is used. In case of urinary tract infections and peritonitis daily dose of up to 50 to 200mg is given. For the treatment of the acute cryptococcal meningitis the recommended daily dose is 400mg on the first day followed by the 200mg once daily. The usual recommended dose for the prophylaxis in patients undergoing bone marrow transplantation is 400mg once daily.

References

Ascher SB, Smith PB, Watt K, Benjamin DK, Cohen-Wolkowiez M, Clark RH, Benjamin DK Jr, Moran C., 2011, Antifungal Therapy and Outcomes in Infants with Invasive Candida Infections, Pediatr Infect Dis J, Dec 20. [Epub ahead of print]

Borgers M, 1980, Mechanism of action of antifungal drugs with special reference to the imidazole derivatives, Rev Inf Dis, 2:520-34.

Cordeiro Rde A, Astete-Medrano DJ, Marques FJ, Andrade HT, Perdig?o Neto LV, Tavares JL, Lima RA, Patoilo KK, Monteiro AJ, Brilhante RS, Rocha MF, Camargo ZP, Sidrim JJ., 2011, Cotrimoxazole enhances the in vitro susceptibility of Coccidioides posadasii to antifungals, Mem Inst Oswaldo Cruz, 106(8):1045-8.


Diflucan (Australian Approved Product Information), 2004, Pfizer Australia Pvt Ltd.


 

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