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Sporal: Full Drug Profile

Medically reviewed by Min Clinic Staff | Updated: January 2026

Sporal - General Information

One of the triazole antifungal agents that inhibits cytochrome P-450-dependent enzymes resulting in impairment of ergosterol synthesis. It has been used against histoplasmosis, blastomycosis, cryptococcal meningitis & aspergillosis. [PubChem]

 

Pharmacology of Sporal

Sporal is an imidazole/triazole type antifungal agent. Sporal is a highly selective inhibitor of fungal cytochrome P-450 sterol C-14 α-demethylation via the inhibition of the enzyme cytochrome P450 14α-demethylase. This enzyme converts lanosterol to ergosterol, and is required in fungal cell wall synthesis. The subsequent loss of normal sterols correlates with the accumulation of 14 α-methyl sterols in fungi and may be partly responsible for the fungistatic activity of fluconazole. Mammalian cell demethylation is much less sensitive to fluconazole inhibition. Sporal exhibits in vitro activity against Cryptococcus neoformans and Candida spp. Fungistatic activity has also been demonstrated in normal and immunocompromised animal models for systemic and intracranial fungal infections due to Cryptococcus neoformans and for systemic infections due to Candida albicans.

 

Sporal for patients

 

Sporal Interactions

Both itraconazole and its major metabolite, hydroxyitraconazole, are inhibitors of the cytochrome P450 3A4 enzyme system. Coadministration of Itraconazole and drugs primarily metabolized by the cytochrome P450 3A4 enzyme system may result in increased plasma concentrations of the drugs that could increase or prolong both therapeutic and adverse effects. Therefore, unless otherwise specified, appropriate dosage adjustments may be necessary.

Coadministration of terfenadine with Itraconazole has led to elevated plasma concentrations of terfenadine, resulting in rare instances of life- threatening cardiac dysrhythmias and one death.

Another oral azole antifungal, ketoconazole, inhibits the metabolism of astemizole, resulting in elevated plasma concentrations of astemizole and its active metabolite desmethylastermizole which may prolong QT intervals. In vitro data suggest that itraconazole, when compared to ketoconazole, has a less pronounced effect on the biotransformation system responsible for the metabolism of astemizole. Based on the chemical resemblance of itraconazole and ketoconazole, coadministration of astemizole with itraconazole is contraindicated.

Human pharmacokinetics data indicate that oral ketoconazole potently inhibits the metabolism of cisapride resulting in an eight-fold increase in the mean AUC of cisapride. Data suggest that coadministration of oral ketoconazole and cisapride can result in prolongation of the QT interval on the ECG. In vitro data suggest that itraconazole also markedly inhibits the biotransformation system mainly responsible for the metabolism of cisapride; therefore concomitant administration of Itraconazole with cisapride is contraindicated.

Coadministration of Itraconazole with oral midazolam or triazolam has resulted in elevated plasma concentrations of the latter two drugs. This may potentiate and prolong hypnotic and sedative effects. These agents should not be used in patients treated with Itraconazole. If midazolam is administered parenterally, special precaution is required since the sedative effect may be prolonged.

Coadministration of Itraconazole and cyclosporine, tacrolimus or digoxin has led to increased plasma concentrations of the latter three drugs. Cyclosporine, tacrolimus and digoxin concentrations should be monitored at the initiation of Itraconazole therapy and frequently thereafter, and the dose of these three drug products adjusted appropriately.

There have been rare reports of rhabdomyolysis involving renal transplant patients receiving the combination of Itraconazole, cyclosporine, and the HMG-CoA reductase inhibitors lovastatin or simvastatin. Rhabdomyolysis has been observed in patients receiving HMG-CoA reductase inhibitors administered alone (at recommended dosages) or concomitantly with immunosuppressive drugs including cyclosporine.

When Itraconazole was coadministered with phenytoin, rifampin, or H2antagonists, reduced plasma concentrations of itraconazole were reported. The physician is advised to monitor the plasma concentrations of itraconazole when any of these drugs is taken concurrently, and to increase the dose of Itraconazole if necessary. Although no studies have been conducted, concomitant administration of Itraconazole and phenytoin may alter the metabolism of phenytoin; therefore, plasma concentrations of phenytoin should also be monitored when it is given concurrently with Itraconazole.

It has been reported that Itraconazole enhances the anticoagulant effect of coumarin-like drugs. Therefore, prothrombin time should be carefully monitored in patients receiving Itraconazole and coumarin-like drugs simultaneously.

Plasma concentrations of azole antifungal agents are reduced when given concurrently with isoniazid. Itraconazole plasma concentrations should be monitored when Itraconazole and isoniazid are coadministered.

Severe hypoglycemia has been reported in patients concomitantly receiving azole antifungal agents and oral hypoglycemic agents. Blood glucose concentrations should be carefully monitored when Itraconazole and oral hypoglycemic agents are coadministered.

Tinnitus and decreased hearing have been reported in patients concomitantly receiving Itraconazole and quinidine. Edema has been reported in patients concomitantly receiving Itraconazole and dihydropyridine calcium channel blockers. Appropriate dosage adjustments may be necessary.

The results from a study in which eight HIV-infected individuals were treated with zidovudine, 8 +/- 0.4 mg/kg/day, showed that the pharmacokinetics of zidovudine were not affected during concomitant administration of Itraconazole, 100 mg b.i.d.

 

Sporal Contraindications

Coadministration of terfenadine, astemizole or cisapride with Sporanox (itraconazole capsules) is contraindicated.

Concomitant administration of Sporanox with oral triazolam or with oral midazolam is contraindicated..

Sporanox should not be administered for the treatment of onychomycosis to pregnant patients or to women contemplating pregnancy.

Sporanox is contraindicated in patients who have shown hypersensitivity to the drug or its excipients. There is no information regarding cross hypersensitivity between itraconazole and other azole antifungal agents. Caution should be used in prescribing Sporanox to patients with hypersensitivity to other azoles.

 

Additional information about Sporal

Sporal Indication: For the treatment of the following fungal infections in immunocompromised and non-immunocompromised patients: pulmonary and extrapulmonary blastomycosis, histoplasmosis, aspergillosis, and onychomycosis. Mechanism Of Action: Sporal interacts with 14-α demethylase, a cytochrome P-450 enzyme necessary to convert lanosterol to ergosterol. As ergosterol is an essential component of the fungal cell membrane, inhibition of its synthesis results in increased cellular permeability causing leakage of cellular contents. Sporal may also inhibit endogenous respiration, interact with membrane phospholipids, inhibit the transformation of yeasts to mycelial forms, inhibit purine uptake, and impair triglyceride and/or phospholipid biosynthesis. Drug Interactions: Alfentanil The imidazole increases the effect and toxicity of alfentanilAlfuzosin The antifungal increases the effect of alfuzosinAlmotriptan This potent CYP3A4 inhibitor increases the effect and toxicity of the triptanAprepitant This potent CYP3A4 inhibitor increases the effect and toxicity of the triptanDarifenacin This potent CYP3A4 inhibitor slows darifenacin/solifenacin metabolismEletriptan This potent CYP3A4 inhibitor increases the effect and toxicity of the triptanDofetilide This strong CYP3A4 inhibitor increases the effect and toxicity of dofetilideErlotinib This potent CYP3A4 inhibitor increases levels/toxicity of erlotinibGefitinib This potent CYP3A4 inhibitor increases levels/toxicity of gefitinibSolifenacin This potent CYP3A4 inhibitor slows darifenacin/solifenacin metabolismTrazodone This potent CYP3A4 inhibitor increases the effect and toxicity of trazodoneAlprazolam The imidazole increases the effect of the benzodiazepineAripiprazole The imidazole increases the effect of aripiprazoleBosentan The imidazole increases the effect and toxicity of bosentanCarbamazepine The imidazole increases the effect of carbamazepineChlordiazepoxide The imidazole increases the effect of the benzodiazepineCilostazol The imidazole increases the effect of cilostazolCinacalcet The imidazole increases the effect and toxicity of cinacalcetClonazepam The imidazole increases the effect of the benzodiazepineClorazepate The imidazole increases the effect of the benzodiazepineCyclosporine The imidazole increases the effect of the immunosuppressantDiazepam The imidazole increases the effect of the benzodiazepineDigoxin Sporal increases the effect of digoxinBudesonide The imidazole increases levels/effect of budesonideEplerenone The imidazole increases the effect and toxicity of eplerenoneEstazolam The imidazole increases the effect of the benzodiazepineEverolimus The imidazole increases everolimus levels/toxicityFentanyl The imidazole increases levels/toxicity of fentanylFlurazepam The imidazole increases the effect of the benzodiazepineHalazepam The imidazole increases the effect of the benzodiazepineHaloperidol The imidazole increases the effect and toxicity of haloperidolImatinib The imidazole increases the levels of imatinibMethylprednisolone The imidazole increases the effect and toxicity of the corticosteroidMidazolam The imidazole increases the effect of the benzodiazepinePrednisolone The imidazole increases the effect and toxicity of the corticosteroidPrednisone The imidazole increases the effect and toxicity of the corticosteroidQuazepam The imidazole increases the effect of the benzodiazepineQuinidine The imidazole increases the effect and toxicity of quinidineQuinidine barbiturate The imidazole increases the effect and toxicity of quinidineRitonavir The imidazole increases the effect and toxicity of ritonavirSildenafil The imidazole increases the effect and toxicity of sildenafilSirolimus The imidazole increases the effect and toxicity of sirolimusTacrolimus The imidazole increases the effect of immunosuppressantTolterodine The imidazole increases the effect and toxicity of tolterodineTriazolam The imidazole increases the effect of the benzodiazepineVardenafil The imidazole increases the effect and toxicity of vardenafilVinblastine The imidazole increases the effect and toxicity of the antineoplasicVincristine The imidazole increases the effect and toxicity of the antineoplasicWarfarin The imidazole increases the effect of the anticoagulantAcenocoumarol The imidazole increases the effect of the anticoagulantDicumarol The imidazole increases the effect of the anticoagulantAnisindione The imidazole increases the effect of the anticoagulantAluminium The antacid decreases the effect of the imidazoleBismuth The antacid decreases the effect of the imidazoleCalcium The antacid decreases the effect of the imidazoleFelodipine Increases effect/toxicity of felodipineMagnesium The antacid decreases the effect of the imidazoleMagnesium oxide The antacid decreases the effect of the imidazoleLevomethadyl Acetate Sporal increases the effect/toxicity of levomethadylRisperidone Increases the level of risperidoneSucralfate Sucralfate decreases the absorption of the imidazoleSunitinib Possible increase in sunitinib levelsTerfenadine Increased risk of cardiotoxicity and arrhythmiasRifampin Rifampin decreases the effect of the imidazoleRifabutin Rifabutin decreases the effect of itraconazolePimozide Increased risk of cardiotoxicity and arrhythmiasCisapride Increased risk of cardiotoxicity and arrhythmiasAstemizole Increased risk of cardiotoxicity and arrhythmiasAtorvastatin Increased risk of myopathy/rhabdomyolysisCerivastatin Increased risk of myopathy/rhabdomyolysisLovastatin Increased risk of myopathy/rhabdomyolysisSimvastatin Increased risk of myopathy/rhabdomyolysisSimvastatin Increased risk of myopathy/rhabdomyolysisRanolazine Increased levels of ranolazine - risk of toxicityRanitidine The anti-H2 decreases the absorption of the imidazoleCimetidine The anti-H2 decreases the absorption of the imidazoleFamotidine The anti-H2 decreases the absorption of the imidazoleNizatidine The anti-H2 decreases the absorption of the imidazoleRabeprazole The proton pump inhibitor decreases the absorption of imidazoleEsomeprazole The proton pump inhibitor decreases the absorption of imidazoleLansoprazole The proton pump inhibitor decreases the absorption of imidazoleOmeprazole The proton pump inhibitor decreases the absorption of imidazolePantoprazole The proton pump inhibitor decreases the absorption of imidazolePhenytoin Phenytoin decreases the effect of itraconazoleMephenytoin Phenytoin decreases the effect of itraconazoleFosphenytoin Phenytoin decreases the effect of itraconazoleEthotoin Phenytoin decreases the effect of itraconazolePhenobarbital The barbiturate decreases the effect of itraconazoleMestranol This anti-infectious agent could decrease the effect of the oral contraceptiveBuspirone The macrolide increases the effect and toxicity of buspironeCiclesonide Increased effects/toxicity of ciclesonideCeliprolol Itaconazole increases levels/effect of celiprololClarithromycin The macrolide increases the effect and toxicity of itraconazoleJosamycin The macrolide increases the effect and toxicity of itraconazoleErythromycin The macrolide increases the effect and toxicity of itraconazoleEthinyl Estradiol This anti-infectious agent could decreases the effect of the oral contraceptiveDihydroergotamine Possible ergotism and severe ischemia with this combinationErgotamine Possible ergotism and severe ischemia with this combination Food Interactions: Avoid milk, calcium containing dairy products, iron, antacids, or aluminum salts 2 hours before or 6 hours after using antacids while on this medication.Take with food.Avoid taking with grapefruit juice.Take after a full meal. Generic Name: Itraconazole Synonyms: ITC; ITCZ; ITR; Itraconazol [Spanish]; Itraconazolum [Latin]; ITZ Drug Category: Antiprotozoals; Antifungals Drug Type: Small Molecule; Approved; Investigational Other Brand Names containing Itraconazole: Itrizole; Oriconazole; Sporal; Sporanos; Sporanox; Sporonox; Triasporn; Absorption: The absolute oral bioavailability of itraconazole is 55%, and is maximal when taken with a full meal. Toxicity (Overdose): No significant lethality was observed when itraconazole was administered orally to mice and rats at dosage levels of 320 mg/kg or to dogs at 200 mg/kg. Protein Binding: 99.8% Biotransformation: Itraconazole is extensively metabolized by the liver into a large number of metabolites, including hydroxyitraconazole, the major metabolite. The main metabolic pathways are oxidative scission of the dioxolane ring, aliphatic oxidation at the 1-methylpropyl substituent, N-dealkylation of this 1-methylpropyl substituent, oxidative degradation of the piperazine ring and triazolone scission. Half Life: 21 hours Dosage Forms of Sporal: Liquid OralCapsule Oral Chemical IUPAC Name: 2-butan-2-yl-4-[4-[4-[4-[[(2R,4S)-2-(2,4-dichlorophenyl)-2-(1,2,4-triazol-1-ylmethyl)-1,3-dioxolan-4-yl]methoxy]phenyl]piperazin-1-yl]phenyl]-1,2,4-triazol-3-one Chemical Formula: C35H38Cl2N8O4 Itraconazole on Wikipedia: https://en.wikipedia.org/wiki/Itraconazole Organisms Affected: Fungi, yeast and protozoans