INGREDIENTS:
Each capsule contains: Active ingredient: Fluconazole (I.N.N.). Inactive ingredients: monohydrate lactose, pre-gelatinized starch, anhydrous colloidal silicon dioxide, sodium laurel sulfate and magnesium stearate. The capsule contains gelatin, titanium dioxide (E-171) and quinoline (E-104).

ACTIVITY:
Loitin capsules (Fluconazole) belong to the new kind of triazole antifungal agents. It is a potent inhibitor and specially intended for the fungal synthesis of steroles. Whether Fluconazole is taken orally or intravenously, its pharmacokinetic properties are similar. When taken orally, Fluconazole is well absorbed, with plasmatic levels (and systematic bioavailability) of more than 90% over intravenous administration. Absorption when taken orally is not affected when accompanied by food. The maximum plasmatic concentrations obtained on an empty stomach are between 0.5 and 1.5 hours following the dose, with an elimination half-life of approximately 30 hours. The plasmatic concentrations are proportional to the dosage. 90% of levels in a balanced state are reached within 4-5 days following multiple doses once a day. Administering a higher dosage the first day, double the usual dose, raises plasmatic levels to 90% of the levels of the state of equilibrium by the second day. The apparent volume of distribution is close to the total of body water. Binding to plasmatic proteins is low. Fluconazole’s penetration in all of the body fluids studied is high. The levels of Fluconazole in saliva and sputum are similar to the plasmatic levels, whereas levels are reached that are above the seric concentrations in the corneal layer, in the dermis and epidermis and in eccrine perspiration. Fluconazole accumulates in the corneal layer and its concentration is measurable in fingernail samples taken 6 months after suspending treatment. In patients with fungal meningitis, the concentration of Fluconazole in the head or spine is approximately 80% of the plasmatic concentration.

Elimination is preferably renal, with 80% of the dosage appearing unmodified in urine. Fluconazole clearance is proportional to creatine clearance. There is no evidence of circulating metabolites. Its long elimination half-life makes a single administration possible in the treatment of vaginal candidiasis and balanitis caused by Candida, and once a day for the rest of mycoses where prescribed. Fluconazole is highly specific for fungal enzymes dependent on cytochrome P-450. Fluconazole does not affect plasmatic testosterone concentrations in men or steroid concentrations in women of childbearing age. Studies on interaction with antipyrine show that Fluconazole does not affect its metabolism.

RECOMMENDED FOR::

• Treating mucosal candidiasis, including orogpharingal, oesophageal, mucocutaneous and chronic atrophic oral candidiasis (associated with the use of dental prostheses).
• Dermatomycoses such as tinea pedis (athlete’s foot), tinea corporis (ringworm of the body), tinea versicolor (also called pityriasis versicolor) and Candida infections.
• It can be used to treat both ordinary hosts and patients with decreased immune function.

CONTRAINDICATIONS:
LOITIN capsules are contraindicated in patients with known hypersensitivity to this pharmaceutical product or to other related triazolic compounds.

CAUTION:
Your physician should bear in mind that hepatic problems have been produced in certain patients treated with LOITIN capsules (Fluconazole).

INTERACTIONS:
Always inform you physician of other treatments you are currently taking. Consult your physician when taking oral antidiabetic medicines containing chlorpropamide, glibenclamide, glipizide or tolbutamide, anticoagulants (warfarin), diuretics such as hydrochlorothiazide, antiepileptics such as phenytoin, contraceptives, tuberculosis treatment with rifampicin, treatment following a transplant with cyclosporin, or treatment with pharmaceutical products containing teofiline.

WARNING:
Pregnancy and breast-feeding: LOITIN capsules during pregnancy have not been proven to be harmless. Fluconazole has rarely been used by pregnant women. Adverse effects have been seen in animal fetuses but only with large doses, associated with maternal toxicity. These findings are not regarded as important in relation to the use of Fluconazole in therapeutic doses. Nonetheless, it should not be taken during pregnancy, except by patients with serious or potentially fatal infections, if and when the effect sought for using LOITIN capsules outweighs the possible risks for the fetus. Because Fluconazole concentrations in mother’s milk are similar to plasmatic concentrations, the use of LOITIN capsules is not recommended during lactation. Effects on driving capacity: Experience with LOITIN capsules (Fluconazole) has shown that treatment with this pharmaceutical product is unlikely to affect the patient’s capacity to drive or operate machinery. Children: The dosage should be modified depending on the recommendations given in DOSAGE.

DOSAGE:
When treating oropharyngeal candidiasis, the usual dosage is 50 mg daily for 7 to 14 days. If necessary, this treatment can be prolonged for longer periods in patients with a serious decrease of the immune function. In chronic atrophic oral candidiasis associated with the use of dental prostheses, the usual dosage is one 50mg LOITIN capsule, once a day for 14 days, together with local antiseptic measures. For other mucosal candidiases (except vaginal candidiasis), such as esophagitis, candiduria, mucocutaneous candidiasis, etc, the effective standard dosage is 50 mg daily, taken for 14 to 30 days. In rare, hard to treat cases of mucosal candidiasis, the dosage may be increased to 100 mg daily.

In the treatment of dermatomycosis, the usual recommended dosage is 50 mg daily for 21 to 28 days. Depending on the seriousness of the clinical pattern and the immune state of the patient, the therapeutic period can be extended. Children: A single daily dose. For the treatment of mucosal candidiasis, the recommended dosage is 3 mg/ kg/day. A shock treatment of 6 mg/kg/day can also be administered. In children with renal insufficiency, the dosage must be reduced in accordance with the following guidelines: Renal insufficiency: In the case of the administration of a single dose of LOITIN capsules, there is no need for adjustment. In treatments involving multiple doses in patients with renal problems, the normal dosage is to be used on Days 1 and 2 of treatment. Following this, the daily dosage (depending on your physician’s instructions) should be based on the following table:

Creatine clearance                Interval of administration Daily dosage (hours)
Over 40 ml/min                           24 hours (normal dosage plan)
21-40 ml/min                              48 hours or half the normal daily dosage
10-20 ml/min                              72 hours or one third of the normal daily dosage
Patients on regular renal dialysis. One dose after each dialysis session.

DIRECTIONS FOR THE CORRECT ADMINISTRATION OF THE PREPARATION:
No special attention required.

OVERDOSE:
In the event of overdose, a symptomatic treatment of the patient will be carried out, with maintenance of vital signs and gastric lavage if necessary. Fluconazole is for the most part excreted with urine. Forced diuresis most likely increases the elimination rate of the product. One 3-hr session of hemodialysis reduces plasmatic levels by approximately 50%. In the event of overdose or accidental swallowing, consult a doctor or your local toxicology office.

SIDE EFFECTS:
LOITIN capsules are generally well tolerated. The most common side effects are of a gastrointestinal nature: nausea, abdominal pain, diarrhea and flatulence. The second most frequent side effect after the gastrointestinal symptoms is exanthema. Very rare cases have been reported of anaphylaxis characterized by paleness, overall itchiness, tachycardia, and so on. Should you notice any other adverse side effect, consult your physician or pharmacist.

STORAGE:
No special storage conditions are required.

EXPIRY:
Do not use this drug after the expiry date shown on the container.

KEEP THIS AND ALL OTHER MEDICINE OUT OF THE REACH OF CHILDREN