Clinical Pharmacology Details


FLUCONAZOLE


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Indications & Dose:

Mucosal candidiasis, systemic candidias, cryptococcosis. Prophylaxis of fungal infections following cytotoxic chemotherapy or radiotherapy. Maintenance to prevent relapse of cryptococcal meningitis in patients with AIDS. Sporotri-chosis, histoplasmosis and vaginal candidiasis. 


DOSE



Adults
Mucosal: 50-100mg daily for 14-30 days.



Vaginal: 150mg as a single oral dose. Systemic: 400mg on first day as loading dose, then 200-400mg once daily for minimum 28 days. Crytococcal meningitis: 400mg stat as a loading dose, then 200-400mg once daily for 10-12 weeks after CSF is sterile. Prophylaxis of fungal infections (in immunocompromised/at risk patients): 50-100mg once daily. Doses may be given orally or by i.v. inf. at rate of 510ml/min. 


Children Severe life threatening infections in over 1 year: 3-6mg/kg body wt. daily. 

Contraindications:

Severe liver impair-ment, renal failure. Hypersensitivity.

Side Effects:

Nausea, abdominal discomfort, diarrhoea and flatulence, occassionally abnormalities of liver enzymes, raraly rash (discontinue treatment) angioedema, anaphylaxis and Stevens Johnson syndrome reported, fixed drug eruption also reported

Cautions:

Renal impairment, pregnancy (toxicity at high doses in animal studies) and breast feeding. Children (use only if imperative and if no alternative treatment) not recommended under 1 year, raised liver enzymes. 

Precautions:

Liver dysfunction, children less than 13 years.


Pregnancy: Use only if potential benefit justifies the possible risk to the foetus.


Breast-feeding: Not recommended. 
Old age: Use with caution. 

Interaction:

Drugs
Cimetidine: Decreased efficacy of fluconazole.


Cyclosporine: Increase in serum  cyclosporine plasma concentration.


Hydrochlorothiazide: Reduction in renal clearance of fluconazole.


Phenytoin: Efficacy of phenytoin enhanced.


Rifampicin: Efficacy of fluconazole decreased, higher dosage required.


Sulfonylurea: Efficacy of tolbutamide, glyburide and glipizide increased.


Warfarin: Potentiates the anticoagulant effect resulting in increase in prothrombin time

Warnings:

Adverse Effects:

Lactations:

Special Precautions:

Counselling:

Side Effects Or Adverse Reactions:

Patient And Carer Advice: