KINZOCAP 200MG TAB

 1. QUALITATIVE AND QUANTITATIVE COMPOSITION

Each hard gelatin capsule contains :- 

Fluconazole BP 200mg 

Excipients  Q.S

2. PHARMACEUTICAL FORM

Solid Oral hard gelatin Capsule

3. CLINICAL PARTICULARS

3.1 Therapeutic indications 

Systemic mycoses:

1.  Cryptococcal infections including cryptococcal meningitis and  infections of other areas (e.g. lungs, skin). AIDS patients, as well as  patients who have undergone an organ transplant or present other causes  of immunosuppression may be treated. Fluconazole may be used for the  prevention of recurrent cryptococcal diseases in AIDS patients.

2.   Generalized candidiasis including candidaemia in clinically stable and  nonneutropenic patients, diffused and metastatic candidiasis  (infections of the peritoneum, endocardium, as well as lung and urinary  tract infections). Patients with malignant neoplasms or in intensive  care units, as well as patients receiving cytostatic or  immunosuppressive drugs or patients presenting other factors in favor of  candidiasis may also be treated with the drug. It is self-evident that  for indications 1 and 2, cultures and proper laboratory examinations  should be conducted before the initiation of the treatment (immediate  microscopic examination, biopsies, serum examinations), in order to  isolate and identify the causative factor.

3.  Deep endemic mycoses, such as coccidioidomycosis,  paracoccidioidomycosis, sporotrichosis and histoplasmosis in  immunocompetent patients.

Mucosal  candidiasis. This includes oropharyngeal and oesophageal candidiasis (as  an alternative to topical treatment), non-invasive

bronchopulmonary  candidiasis. Candiduria, chronic mucocutaneous candidiasis. Chronic  atrophic oral candidiasis (stomatitis due to dentures), as

alternative to local treatment. Patients mostly with immune system disorders can undergo a treatment with the drug.

4. Genital candidiasis:Vaginal candidiasis as an alternative to topical treatment (only as one single dose of 150mg)

a). Acute

b).  relapsing as long as the infection has been confirmed by culture  (usually of non-inflammatory cause but due to allergy or  hypersensitivity).

Candidal balanitis.

Dermatophytoses  including infections of the foot, of the thin skin layer and of the  bikini line, as well as tinea versicolor, onychomycosis and

infections  caused by CANDIDA.Note: Systemic treatment in the case of the  indications mentioned above is preferable when the infection

extends  to a large skin area or the scalp, or in patients with disorders of  defense mechanisms, unresponsive to local treatment and persistence

of the mycotic infection despite treatment.

7),  Prevention of candidiasis in patients with neutropenia and malignant  diseases that predispose to the development of such infections as a

result  of chemotherapy with cytostatic drugs or radiotherapy in cases of  marrow transplant. Caution: chronic administration of azoles increases

the  possibility of development of C. KRUSEI, ASPERGILLUS, MUCORALES,  FUSARIUM, T. GLABRATA that usually present a natural resistance to  azoles.

Therapy may be initiated  before the results of the cultures and other laboratory studies are  known. However when the results are known, therapy should be adjusted  accordingly

3.2 Posology and method of administration

As  absorption of orally administered Fluconazole is rapid and complete,  the Fluconazole daily dose is the same for both oral and intravenous  administration.

The Fluconazole  daily dose should be based on the type and severity of the mycotic  infection. Most cases of vaginal candidiasis respond therapeutically to  single dose administration.

For  infections requiring multiple dose administration, treatment should be  continued until the clinical parameters and laboratory examinations show

resolution  of the active mycotic infection. Insufficient duration of Fluconazole  treatment may result in a relapse of the active infection. Patients with

AIDS  and cryptococcal meningitis or recurrent oropharyngeal candidiasis  usually require preventative treatment to reduce the occurrence of  relapses.

1a. For  the treatment of cryptococcal meningitis and cryptococcal infections of  other body areas, the usual dose is 400mg on the first day of the  treatment followed by a dose of 200-400mg once daily. The duration of  treatment in cryptococcal infections depends on the clinical mycological

response  but usually lasts from 6 to 8 weeks in cryptococcal meningitis and 10  to 12 weeks after a negative result of the CSF culture.

1b. For  the prevention of cryptococcal meningitis relapse in patients with  AIDS, after the completion of the initial treatment it is possible to  administer fluconazole indefinitely at a daily dose of 100-200mg

2. For  the treatment of candidaemia, generalized candidiasis and other severe  candidiases, the usual dose is 400mg on the first day of the treatment,

followed  by a daily dose of 200mg. Depending on the clinical response of the  patients, the dose may be increased to 400mg daily. The treatment's

duration depends on the clinical response of the patients.

Adults

3. With  regard to deep endemic mycosis, doses of 200-400mg daily for a duration  of treatment which may last 2 years may prove to be necessary.

Duration of treatment should be adapted in every case.

4. For  the treatment of oropharyngeal candidiasis, the usual dose is 50-100mg  once daily for 7-14 days. If necessary, the treatment may be continued  for a longer time span in patients with a severe disorder of the immune  system. For the treatment of atrophic oral candidiasis associated with  artificial dentures, the usual Fluconazole dose is 50mg once daily for  14 days, concurrently administered with the application of local  antiseptic measures to the dentures. For the treatment of other  candidiasis infections of the mucosa (except vaginal candidiasis, see  below), e.g. oesophagitis, non-invasive bronchopulmonary infections,  candidurea, chronic muco-cutaneous candidiasis etc., the usual  Fluconazole dose is 50-100mg daily for 14-30 days.

5. For  the treatment of vaginal candidiasis and candidal balanitis, 150mg of  Fluconazole should be administered orally as a single dose.

6. For  the treatment of skin infections including infections of the feet, of  the thin skin layer and of the bikini line, as well as tinea versicolor  and infections caused by Candida, the recommended dose is 150mg once  weekly or 50mg once daily. The duration of treatment usually extends  from 2 to

4 weeks but in particular  infection of the feet may require treatment for up to 6 weeks. For tinea  versicolor, the recommended dose is 50mg once daily for 2 to 4 weeks.

7. For  onychomycosis, the recommended dose is 150mg once weekly. Treatment  should be continued until the infected nail is replaced due to normal

nail  growth. Normally it takes about 3 to 6 months and 6 to 12 months  respectively for fingernails and toenails to grow. Of course the growth  rate may

8. For  the prevention of fungal infections in patients with an increased risk  of generalized infection e.g. patients who are expected to have severe  or

prolonged neutropenia, like  pre-marrow transplant patients, the daily recommended dose of the drug  should be 400mg and for the prevention of fungal infections in patients  with neutropenia and malignant diseases who are predisposed to the  development of such infections as a result of

chemotherapy  with cytostatic drugs of radiotherapy, the daily dose of the drug is  50-400mg once daily. Fluconazole administration should start several  days before the anticipated onset of neutropenia and continue for 7 days  after the neutrophil count is above 1000 cells per mm3.

vary  considerably from person to person and according to patient's age.  After a successful long-term treatment of chronic infections, the nails  may still show traces of infection.

Patients with renal impairment

Fluconazole  is largely eliminated in the urine in an unaltered form. In case of  administration of a single, dose of the drug its adjustment is not  necessary. When multiple doses are administered to patients with renal  impairment, a loading dose of 50 to 400 mg is administered. After the

loading dose, the daily dose (according to the indications) should be adjusted according the following table:

Creatinine clearance (ml/min)  Percent of recommended dose

>50  100%

11 - 50  50%

Patients  receiving regular dialysis 100% after each dialysis When serum  creatinine is the only measurement of renal failure, the following

equation for creatinine is applied:

Men:  Body weight (kg) x (140 - age)

72 x serum creatinine (mg / 100ml)

Women:  0.85 of the male value

3.3 CONTRAINDICATIONS

Stabilanol  should not be administered in patients with known sensitivity to  Fluconazole or to the excipients or to related azole preparations.

Co-administration  of cisapride is contra-indicated in patients receiving fluconazole.  Based on the results of a multiple dose interaction study,  co-administration of terfenadine in patients receiving fluconazole at  doses of 400 mg or more per day is contraindicated.

Special warnings and precautions for use.

General:

Fluconazole  is generally well tolerated. The most common undesirable effects  associated with the use of Fluconazole relate to the gastrointestinal

system.  They include nausea, abdominal discomfort, diarrhoea and flatulence.  Other common undesirable effects are headache and skin rashes.

Exfoliating  dermatitis, such as the Stevens-Johnson syndrome and toxic epidermic  necrolysis, especially in patients with AIDS receiving other drugs

are rarely reported.

Fluconazole  is a triazole antifungal agent. Fluconazole exerts its antifungal  effect by inhibition of sterol 14-alpha-demethylase impairing the

biosynthesis  of ergosterol, the principal sterol in the fungal cell membrane. This  damages the cell membrane, producing alterations in membrane

function and permeability.