Sporax


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Brand Name


Composition and Strength: Itraconazole 100 mg

Form: Capsule

Packaging: 4C * 1 *7

Description :


Introduction

Sporax (Itraconazole) is a synthetic triazole analogue with a wide spectrum of antifungal activity.

Sporax impairs the formation of ergosterol (a vital cell membrane component in fungi) by
inhibiting fungal cytochrome P450 enzyme 14α-demethylase. Impairment of ergosterolsynthesis ultimately results in an antifungal effect.

In vitro studies demonstrate that itraconazole inhibits the growth of a broad range of fungi pathogenic for humans at concentrations usually  1 μg/ml. These include:
dermatophytes (Trichophyton spp., Microsporum spp.,);
yeasts (Candida spp., viz, C. albicans, Cryptococcus neoformans,.);
Aspergillus spp.; Histoplasma spp.; Paracoccidioides brasiliensis; Sporothrix schenckii;
Blastomyces dermatitidis; Coccidioides immitis;; Penicillium marneffei; and various other yeasts and fungi.


Indications & Dosing regimen

Vulvovaginal candidasis

-    Single day 200 mg BID or 200 mg OD for 3 days

For recurrent vaginal candidiasis:
- 200 mg OD X 3 days + 1st day of periods for 6 cycles or months
 
 Candidal balanitis
-      Single day 200 mg BID


Oral Candidiasis
 100 mg OD X 2wks
** For AIDS and Neutropenia patients:  - 200 mg OD X 2 wks

Tinea infections:
(cruris, corporis, versicolor, barbae)
-      200 mg daily X 7 days,   or 100 mg daily X 15 days
Tinea pedis, tinea manuum- 200 mg twice daily for 7 days or 100 mg once daily for 4 weeks
 
Fungal eye infections (Fungal keratitis & Candidal endophthalmitis)
            - 200 mg twice daily  X 21 days (or until infection is resolved)
 
 Onychomycosis
  • Continuous treatment : 200 mg daily for 3 months
  • Pulse treatment:

Fingernail infections: 2 pulse treatments.
Toenail infections: 3 pulse treatments.
Pulse treatments are always separated by a 3 week drug-free interval.
----     1 pulse is 200 mg bd for 1 week  --------

 
 Cutaneous Candidiasis 
100-200 mg OD for 3 wks – 7 months
 
Prophylaxis in the immune-compromised:
 -  200 mg BID until symptoms disappears and immune system recovery has occurred.
     
Blastomycosis
200 mg PO TID for 3 days; then 200 mg PO BID for 6-12 months
 
Aspergillosis
200-400 mg PO OD for 2-5 months
 
Histoplasmosis, Sporotrichosis . Paracoccidiomycosis, Chromomycosis
200 mg OD / BID ; until  disease is controlled
 
 
Precaution
Itraconazole is predominantly metabolized in the liver. In cirrhotic patients and in other cases of hepatic impairment or renal insufficiency, it is advisable to monitor the itraconazole plasma concentrations and adjust the dose when necessary.
In case of special population:

Pregnancy
-          Should not be used during pregnancy except for life-threatening cases where the potential benefit to the mother outweighs the potential harm to the fetus.

Women of childbearing potential
-          Adequate contraceptive precautions should be taken by women of childbearing potential during therapy and for one menstrual cycle after stopping therapy, as teratogenicity has been shown in laboratory animals

Lactation
-          A very small amount of itraconazole is excreted in human milk. The expected benefits of Sporax therapy should be weighed against the risks of breast feeding. In case of doubt, the patient should not breast feed.
 
Use in Children (below 12 years)
Clinical data on the use of itraconazole capsules in paediatric patients are limited. It should not be used in children unless the potential benefit outweighs the potential risks. The dose in children is usually 5 mg per kg body weight per day to maximum 200 mg per day but is reserved for exceptional circumstances.
 
Use in Elderly
As for use in children.
 
Contraindications

  • In patients with a known hypersensitivity to itraconazole other azole antifungal agents.
  • It should not be administered to treat onychomycosis in patients with evidence of cardiac conditions such as congestive heart failure (CHF) or a history of CHF.
  • Drugs like Terfenadine, astemizole, mizolastine, cisapride, quinidine, CYP3A4 metabolised HMG-CoA reductase inhibitors such as simvastatin and lovastatin, oral midazolam and triazolam should not be used during treatment with itraconazole capsules.

 
Drug Interactions
1.       Drugs affecting the metabolism of itraconazole:
Enzyme-inducing drugs such as rifampicin, rifabutin, carbamazepine, isoniazid and phenytoin significantly reduce the bioavailability of itraconazole. Monitoring of plasma concentrations of itraconazole is advised if these medicines are administered concomitantly. An increase in the dose of itraconazole may be necessary.
As itraconazole is mainly metabolised through the CYP3A4, potent inhibitors of this enzyme may increase the bioavailability of itraconazole. Examples are: ritonavir, indinavir, clarithromycin and erythromycin.
 
2.       Effect of itraconazole on the metabolism of other drugs:
 Itraconazole can inhibit the metabolism of drugs metabolised by the cytochrome 3A family. This can result in an increase and/or prolongation of their effects, including side-effects.
After stopping treatment, itraconazole plasma levels decline gradually, depending on the dose and duration of treatment. This should be taken into account when the inhibitory effect of itraconazole on co-medicated drugs is considered.
Itraconazole can inhibit the metabolism of calcium channel blockers. Therefore, caution should be used when co-administering itraconazole and calcium channel blockers.
 
Drugs whose plasma levels, effects or side-effects should be monitored:
-          Oral anticoagulants; Anti virals such as ritonavir, certain antineoplastic agents such as busulphan, docetaxel and certain Immunosuppressive agents like cyclosporine, tacrolimus
-          Few incidences of hypoglycaemia has been reported in patients concomitantly receiving azole antifungal agents and oral hypoglycaemic agents. Blood glucose concentrations should be carefully monitored when itraconazole and oral hypoglycaemic agents are co-administered.
Their dosage, if co-administered with itraconazole, should be reduced if necessary.
 

Adverse effects 
With doses of up to 400 mg/day most commonly are:
Gastrointestinal effects may include nausea, abdominal pain, diarrhea, constipation, loss of appetite and rarely, hepatotoxicity.
Other effects may include headache, dizziness and drowsiness, allergic rash, hepatitis, and hallucinations.



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