| |
| GVFLUC 50 / 150 / 200 Capsules |
| Composition |
| GVFLUC® 50 Capsules |
|
GVFLUC® 150 Capsules |
|
| Each capsule contains |
|
Each capsule
contains |
|
| Fluconazole |
50 mg |
Fluconazole |
150 m |
| GVFLUC® 2OO Capsules |
|
GVFLUC® Powder for oral suspension |
|
| Each capsule contains |
|
Each 5 ml after
reconstitution contains |
|
| Fluconazole |
200 mg |
Fluconazole |
50 mg |
|
| Description |
Fluconazole is a
bis-triazole antifungal structurally related to imidazole-derivative
antifungals. The nitrogen of the azole ring of the triazole binds to the haem moiety of the fungal
cytochrome P 450 enzyme lanosterol 14-demethylase which halts conversion of tanosterol
Loergosterol that leads to a cascade of abnormalities in membrane permeability, membrane bound enzyme
activity and coordination of chit in synthesis. |
| Pharmacokinetics |
GVFLUC® has novel pharmacokinetic
properties like metabolic stability and relatively high water solubility which contributes to
its therapeutic efficacy. It is very well absorbed orally, with peak plasma concentrations
reached within 1 to 2 hours after administration. The bio-availability of
orally administered flueonazole is over 90% compared to I. V. administration. Peak plasma
concentration reached within 1 to 2 hours. Administration of a single oral 400 mg dose of fluconazole leads to a mean (maximum peak plasme
concentration) of 6,72 ng/ml. And after single oral doses of 50-400 mg, flueonazole
plasma concentration and AUC are dose propotionat. The
apparent volume of distribution of fluconazole approximates that of total body water. Plasma protein
binding is low (11-12%), Fluconazole circulates
mostly as free drug. Fluconazole is cleared primarily by renal excretion, with approximately 80% of the administered dose
appearing in the urine as unchanged drug. About 11% of the dose is excreted in the urine as metabolites. The elimination half life in adults with normal renal function is about 30
hours. |
| Indications |
GVFLUC® is indicated for:
- Mucosal candidiasis
- Systemic candidiasis
- Crytpococcosis
- Prevention of fungal infection
|
| Contraindications |
| Hypersensitive to fluconazole or any of its
excipients or related azole compounds. |
| Side Effects |
Fluconazole is
generally well tolerated. Commonly reported side effects are nausea, vomiting,
abdominal pain, headache, skin rash and diarrhea. Mild transient, reversible increase
in liver enzymes like ALT, AST. Alkaline phosphate and serum bilirubin,
etc. be
seen. Serious
hepatotoxicity is rarely seen. Clinical adverse reactions have been more frequently reported
in HIV
infected patients than in non-HlV infected patients, however, the patterns were
similar. In rare
cases,
anaphylaxis has been reported. |
| Dosage |
Adults
Oropharyngeal
candidiasis; 200 mg on the first day, followed by 100 mg once daily for 14 days.
Oesophageal candidiasis: 200 mg on the first day, followed by l00 mg once daily for 21 days.
Vaginal candidiasis:
150 mg single dose.
Systemic
candidiasis: 400 mg on first day, then 200-400 mg once daily.
Cryptococcal
meningitis: 400 mg loading dose, followed by 200 mg daily for 10-12 weeks after CFS becomes
culture negative.
Maintenance to prevent relapse of cryplococcal
meningitis; 100-200 mg daily.
Prophylaxis in
immunocompromised: 50-400 mg once daily started several days before onset of
neutropenia and continued for 7 days after neutrophil count > 1000
cells/mm3. |
| Children |
| Mucosal candid iasis |
Systemic
candidiasis: |
Prophylaxis in
immunocompromised: |
| < 2 weeks |
3 mg/kg every 72 hrs |
<2
weeks : |
6-12 mg/kg every 72 hrs |
< 2 weeks |
3-12 mg/kg
every 72 hrs |
| 2-4 weeks |
3 mg/kg every 48 hrs |
2-4 weeks |
6-12 mg/kg every 48 hrs |
2-4 weeks |
3-12 mg/kg
daily every 48 hrs |
| over 4 weeks |
3 mg/kg daily |
over 4 weeks |
6-l2 mg/kg daiIy |
over 4 weeks |
3-12 mg/kg daily |
|
| Overdosage |
| Fluconazole is
excreted largely
in the urine; forced diuresis would probably increase the elimination rate. A three hour
session of haemodialysis decreases plasma levels by approximately 50 percent. |
| Presentation |
GVFLUC 50 Capsules : Blister of 3 capsules
GVFLUC 150 Capsules : Blister of 1 capsule
GVELUC 200 Capsulcs :
Blister of 1 capsule
GVFLUC SUSPENSION : 35ml Bottle. |
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