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Extina: Full Drug Profile

Medically reviewed by Min Clinic Staff | Updated: January 2026

Extina - General Information

Broad spectrum antifungal agent used for long periods at high doses, especially in immunosuppressed patients. [PubChem]

 

Pharmacology of Extina

Extina, like clotrimazole, fluconazole, itraconazole, and miconazole, is an imidazole antifungal agent.

 

Extina for patients

Shampoo: May be irritating to mucous membranes of the eyes and contact with this area should be avoided.

There have been reports that use of the shampoo resulted in removal of the curl from permanently waved hair.

Tablet: Patients should be instructed to report any signs and symptoms which may suggest liver dysfunction so that appropriate biochemical testing can be done. Such signs and symptoms may include unusual fatigue, anorexia, nausea and/or vomiting, jaundice, dark urine or pale stools

 

Extina Interactions

Ketoconazole is a potent inhibitor of the cytochrome P450 3A4 enzyme system. Coadministration of NIZORAL Tablets 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. The following drug interactions have been identified involving NIZORAL Tablets and other drugs metabolized by the cytochrome P450 3A4 enzyme system:

Ketoconazole tablets inhibit the metabolism of terfenadine, resulting in an increased plasma concentration of terfenadine and a delay in the elimination of its acid metabolite. The increased plasma concentration of terfenadine or its metabolite may result in prolonged QT intervals.

Pharmacokinetic data indicate that oral ketoconazole inhibits the metabolism of astemizole, resulting in elevated plasma levels of astemizole and its active metabolite desmethylastemizole which may prolong QT intervals. Coadministration of astemizole with ketoconazole tablets is therefore contraindicated.

Human pharmacokinetics data indicate that oral ketoconazole potently inhibits the metabolism of cisapride resulting in a mean eight-fold increase in AUC of cisapride. Data suggest that coadministration of oral ketoconazole and cisapride can result in prolongation of the QT interval on the ECG. Therefore concomitant administration of ketoconazole tablets with cisapride is contraindicated.

Ketoconazole tablets may alter the metabolism of cyclosporine, tacrolimus, and methylprednisolone, resulting in elevated plasma concentrations of the latter drugs. Dosage adjustment may be required if cyclosporine, tacrolimus, or methylprednisolone are given concomitantly with NIZORAL Tablets.

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

Rare cases of elevated plasma concentrations of digoxin have been reported. It is not clear whether this was due to the combination of therapy. It is, therefore, advisable to monitor digoxin concentrations in patients receiving ketoconazole.

When taken orally, imidazole compounds like ketoconazole may enhance the anticoagulant effect of coumarin-like drugs. In simultaneous treatment with imidazole drugs and coumarin drugs, the anticoagulant effect should be carefully titrated and monitored.

Because severe hypoglycemia has been reported in patients concomitantly receiving oral miconazole (an imidazole) and oral hypoglycemic agents, such a potential interaction involving the latter agents when used concomitantly with ketoconazole tablets (an imidazole) can not be ruled out.

Concomitant administration of ketoconazole tablets with phenytoin may alter the metabolism of one or both of the drugs. It is suggested to monitor both ketoconazole and phenytoin.

Concomitant administration of rifampin with ketoconazole tablets reduces the blood levels of the latter. INH (Isoniazid) is also reported to affect ketoconazole concentrations adversely. These drugs should not be given concomitantly.

After the coadministration of 200 mg oral ketoconazole twice daily and one 20 mg dose of loratadine to 11 subjects, the AUC and Cmax of loratadine averaged 302% (± 142 S.D.) and 251% (± 68 S.D.), respectively, of those obtained after co-treatment with placebo. The AUC and Cmax of descarboethoxyloratadine, an active metabolite, averaged 155% (± 27 S.D.) and 141% (± 35 S.D.), respectively. However, no related changes were noted in the QT0 on ECG taken at 2, 6, and 24 hours after the coadministration. Also, there were no clinically significant differences in adverse events when loratadine was administered with or without ketoconazole.

Rare cases of a disulfiram-like reaction to alcohol have been reported. These experiences have been characterized by flushing, rash, peripheral edema, nausea, and headache. Symptoms resolved within a few hours.

 

Extina Contraindications

Tablets and Shampoo

Ketoconazole is contraindicated in patients who have shown hypersensitivity to the drug or excipients of the formulation(s).

Tablets

Coadministration of terfenadine or astemizole with ketoconazole tablets is contraindicated.

Concomitant administration of NIZORAL® Tablets with oral triazolam is contraindicated.

NIZORAL is contraindicated in patients who have shown hypersensitivity to the drug.

 

Additional information about Extina

Extina Indication: For the treatment of the following systemic fungal infections: candidiasis, chronic mucocutaneous candidiasis, oral thrush, candiduria, blastomycosis, coccidioidomycosis, histoplasmosis, chromomycosis, and paracoccidioidomycosis. Mechanism Of Action: Extina interacts with 14-α demethylase, a cytochrome P-450 enzyme necessary for the conversion of lanosterol to ergosterol. This results in inhibition of ergosterol synthesis and increased fungal cellular permeability. Other mechanisms may involve the inhibition of endogenous respiration, interaction with membrane phospholipids, inhibition of yeast transformation to mycelial forms, inhibition of purine uptake, and impairment of triglyceride and/or phospholipid biosynthesis. Extina can also inhibit the synthesis of thromboxane and sterols such as aldosterone, cortisol, and testosterone. Drug Interactions: Alfentanil The imidazole increases the effect and toxicity of alfentanilAlprazolam The imidazole increases the effect of the benzodiazepineAmitriptyline The imidazole increases the effect and toxicity of the tricyclicAnisindione The imidazole increases the effect of the anticoagulantAripiprazole The imidazole increases the effect of aripiprazoleBosentan The imidazole increases the effect and toxicity of bosentanBudesonide The imidazole increases levels/effect of budesonideCarbamazepine 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 immunosuppressantDiazepam The imidazole increases the effect of the benzodiazepineDicumarol The imidazole increases the effect of the anticoagulantAcenocoumarol The imidazole increases the effect of the anticoagulantWarfarin The imidazole increases the effect of the anticoagulantEplerenone 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 imatinibImipramine The imidazole increases the effect and toxicity of the tricyclicMethylprednisolone The imidazole increases the effect and toxicity of the corticosteroidMidazolam The imidazole increases the effect of the benzodiazepineNortriptyline The imidazole increases the effect and toxicity of the tricyclicPrednisolone 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 quinidineRamelteon The imidazole increases the levels/toxicity of ramelteonRitonavir The imidazole increases the effect and toxicity of ritonavirSaquinavir The imidazole increases the effect and toxicity of saquinavirSildenafil The imidazole increases the effect and toxicity of sildenafilSirolimus The imidazole increases the effect and toxicity of sirolimusTacrolimus The imidazole increases the effect of immunosuppressantTadalafil The imidazole increases tadalafil levelsTolterodine The imidazole increases the effect and toxicity of tolterodineTriazolam The imidazole increases the effect of the benzodiazepineValdecoxib The imidazole increases the effect and toxicity of valdecoxibVardenafil The imidazole increases the effect and toxicity of vardenafilVinblastine The imidazole increases the effect and toxicity of vinblastineVincristine The imidazole increases the effect and toxicity of the antineoplasicZiprasidone Extina increases the effect and toxicity of ziprasidoneTolbutamide Extina increases the effect and toxicity of tolbutamideSibutramine Extina increases the levels and toxicity of sibutramineRosiglitazone Extina increases the effect of rosiglitazoneQuetiapine Extina increases the effect/toxicity of quetiapinePioglitazone Extina increases the effect of pioglitazoneGalantamine Extina increases the effect and toxicity of galantamineIndinavir Extina increases the effect of indinavirIrinotecan Extina increases the effect and toxicity of irinotecanTrazodone This strong CYP3A4 inhibitor increases the effect and toxicity of trazodoneSunitinib Possible increase in sunitinib levelsSucralfate Sucralfate decreases the absorption of the imidazoleSolifenacin This potent CYP3A4 inhibitor slows darifenacin/solifenacin metabolismAlfuzosin The antifungal increases the effect of alfuzosinAlmotriptan This potent CYP3A4 inhibitor increases the effect and toxicity of the triptanAprepitant This CYP3A4 inhibitor increases the effect and toxicity of aprepitantCiclesonide Increased effects/toxicity of ciclesonideDarifenacin This potent CYP3A4 inhibitor slows darifenacin/solifenacin metabolismDocetaxel The agent increases the serum levels and toxicity of docetaxelDofetilide This strong CYP3A4 inhibitor increases the effect and toxicity of dofetilideEletriptan This potent CYP3A4 inhibitor increases the effect and toxicity of the triptanErlotinib This CYP3A4 inhibitor increases levels/toxicity of erlotinibGefitinib This CYP3A4 inhibitor increases levels/toxicity of gefitinibIsoniazid Isoniazid decreases the effect of ketoconazoleNevirapine Nevirapine decreases the effect of ketoconazoleRifampin Rifampin dereases the effect of the imidazoleRanolazine Increased levels of ranolazine - risk of toxicityTerfenadine Increased risk of cardiotoxicity and arrhythmiasPimozide 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/rhabdomyolysisAluminium The antacid decreases the effect of the imidazoleBismuth The antacid decreases the effect of the imidazoleMagnesium The antacid decreases the effect of the imidazoleMagnesium oxide The antacid decreases the effect of the imidazoleCalcium The antacid decreases the effect of the imidazoleBuspirone The macrolide increases the effect and toxicity of buspironeCimetidine 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 imidazoleRanitidine The anti-H2 decreases the absorption of the imidazoleDihydroergotamine Possible ergotism and sever ischemia with this combinationErgotamine Possible ergotism and sever ischemia with this combinationEsomeprazole 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 imidazoleRabeprazole The proton pump inhibitor decreases the absorption of imidazoleEthinyl Estradiol This anti-infectious agent could decrease the effect of the oral contraceptiveMestranol This anti-infectious agent could decrease the effect of the oral contraceptive Food Interactions: Avoid alcohol.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. Generic Name: Ketoconazole Synonyms: Not Available Drug Category: Antifungals Drug Type: Small Molecule; Approved Other Brand Names containing Ketoconazole: Extina; Fungarest; Fungoral; Ketocanazole; Ketoconazol; Ketoconazol [Inn-Spanish]; Ketoconazole [Usan-Ban-Inn-Jan]; Ketoconazolum [Inn-Latin]; Ketoderm; Ketoisdin; Ketozole; Nizoral; Nizoral Cream; Nizoral Shampoo; Nizoral a-D; Nizoral a-D Shampoo; Orifungal; Orifungal M; Panfungol; Absorption: Moderate Toxicity (Overdose): Hepatotoxicity, LD50=86 mg/kg (orally in rat) Protein Binding: 99% (in vitro, plasma protein binding) Biotransformation: Hepatic Half Life: 2 hours Dosage Forms of Extina: Tablet OralCream TopicalShampoo Topical Chemical IUPAC Name: 1-[4-[4-[[(2S,4R)-2-(2,4-dichlorophenyl)-2-(imidazol-1-ylmethyl)-1,3-dioxolan-4-yl]methoxy]phenyl]piperazin-1-yl]ethanone Chemical Formula: C26H28Cl2N4O4 Ketoconazole on Wikipedia: https://en.wikipedia.org/wiki/Ketoconazole Organisms Affected: Fungi