Description
Dermo
quinol
is an effective, safe, soothing, topical, non-antibiotic,
antibacterial and antifungal agent with antipruritic properties.
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Composition
| Conflu
150 |
|
|
| Each
hard gelatine capsule contains : |
|
|
| Fluconazole |
150 |
mg |
|
Approved colours used for capsules |
|
|
| Conflu200 |
|
|
| Each
hard gelatine capsule contains : |
|
|
| Fluconazole |
200 |
mg |
| Approved
colours used for capsules |
|
|
|
Actions
Azoles,
though normally fungistatic (through inhibition of ergosterol
synthesis in fungal cell membrane), can be fungicidal
at high concentrations, may be, as a result of direct
membrane damage from the binding of the azole to membrane
phospholipids. At low concentration Conflu (Fluconazole)
inhibits ergosterol synthesis (required for cell membrane
integrity) through inhibition of the enzyme
14-alfa-demethylase with the resultant elevation of lanosterol/ergosterol
ratio. At high concentration rapid fungal cell membrane
damage occurs, not dependant on lanosterol/ergosterol
ratio, to exhibit fungicidal activity. It has bioavailability
of >90% within 2 hours of administration and is resistant
to first pass metabolism. Fluconazole absorption is not
reduced by change in gastric pH, antacids or H2 blockers
(ranitidine etc.) or in neutropenic patients who experience
frequent vomiting. Cmax and tmax are not variable after
multiple dosing compared with single dose administration.
The drug distributes well into most tissues achieving
concentrations in saliva, sputum, vaginal and peritoneal
fluid after oral and i.v. administration. Tissue :
peak plasma concentration ratios in the liver, spleen,
lungs, kidneys and brain range from 0.5-0.8; the drug
freely distributes into eyes including cornea, aqueous
humor, vitreous body. However, tissue (prostate) :
serum concentration ratio is poor (0.29) indicating poor
distribution. CSF : serum concentration ratio in
normal volunteers after repeated oral/i.v. administration
is 0.52 or 0.62 respectively with higher CSF concentration
in patients with meningitis having tissue : blood
concentration ratio in the range of 0.6-0.8. The primary
route of excretion is through kidney-80% of unchanged
drug is recovered in urine and 11% as metabolites
Indications
Vaginal
candidiasis, oropharyngeal candidiasis, oesophageal candidiasis,
cryptococcal meningitis, coccidioidal meningitis, systemic
candidiasis, dermatophytosis, onychomycosis, prophylaxis
of fungal infection following cytotoxic chemotherapy or
radiotherapy.
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Precautions
& Contraindications
The drug
is to be discontinued if bullous skin lesion or erythema multiforme
develop during therapy. The drug is contraindicated in patients
with hypersensitivity to azoles. No adequate and well controlled
studies in pregnant women are available; may be used only
when the potential benefit outweigh the possible risk to the
foetus. Nursing mothers should not be given as the drug is
excreted in breast milk in concentration similar to plasma.
Safety and efficacy of fluconazole in children younger than
13 years have not been established. Use of fluconazole may
result in overgrowth of non-susceptible strains of candida
other than C.albicans. Fluconazole therapy should be discontinued
if signs and symptoms consistent with liver disease develop.
Adverse
Reactions
The
drug is generally well tolerated-nausea (3.7%), headache (1.9%),
skin rash (1.8%), abdominal pain (1.7%), vomiting (1.7%) and
diarrhoea (1.5%) are reported in most clinical trials. Dizziness
and headache have been reported in upto about 2% of the patients.
Eosinophilia has also been reported in some patients; oliguria,
hypotension, oedema, etc. are rarely reported. Hepatotoxicity
is the most concerning adverse drug reaction though serious
reactions are reported rarely. The true incidence of fluconazole
related hepatotoxicity resulting in clinical features of liver
dysfunction or discontinuation of therapy is unknown; however,
it is likely to be small. In HIV positive patients and who
are having other hepatotoxic drugs may contribute higher incidence
of hepatotoxicity with fluconazole
Drug
Interactions
Fluconazole
can alter pharmacokinetics of certain drugs undergoing hepatic
metabolism. Concomitant administration with coumarin derivatives
may cause increased prothrombin time; increased plasma concentrations
of antidiabetic agents (eg. glyburide, glipizide, tolbutamide,
etc.), cyclosporin, phenytoin may occur on concomitant administration
with fluconazole. Potential serious adverse cardiovascular
effects should be considered during concomitant administration
of astemizole/terfenadine with fluconazole.
Dose
(a)
Vaginal candidiasis : 150 mg. single
dose.
(b)
Oropharyngeal candidiasis :
200 mg. 1st day followed by 100 mg. once daily for
at least 2 weeks.
(c)
Oesophageal candidiasis : 200
mg 1st dose followed by 100 mg. once daily for 3 weeks.
(d)
Coccidioidal meningitis :
Minimal dose 400 mg. daily.
(e)
Cryptococcal meningitis (AIDS related) : 400 mg.
daily for 10 weeks.
(f)
Systemic candidiasis :Initial dose 400 mg. daily,
followed by 200-400 mg. daily.
(g)
Onychomycosis :150 mg. once weekly for
8-12 months.
(h) Dermatophytosis :150
mg. once weekly for 4-6 weeks
.
(i)
Maintenance therapy (to prevent relapse of Cryptococcal
Meningitis) :200 mg. daily.
(j)
Prophylaxis : Upto 400 mg. daily.
Packing
Conflu
150 :
Strips of 1 capsule
Conflu 200 :
Strips of 4 capsules
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