Itraconazole

(i tra ko' na zole)

PCI  / LCI Contraindicated in pregnancy and lactation

Molecule Info

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WARNING

Congestive Heart Failure, Cardiac Effects and Drug Interactions:

Itraconazole should not be administered for the treatment of onychomycosis in patients with evidence of ventricular dysfunction such as congestive heart failure (CHF) or a history of CHF. If signs or symptoms of congestive heart failure occur during administration of itraconazole capsules, discontinue administration. When itraconazole was administered intravenously to dogs and healthy human volunteers, negative inotropic effects were seen.

Drug Interactions: Co-administration of cisapride, oral midazolam, nisoldipine, felodipine, pimozide, quinidine, dofetilide, triazolam, levacetylmethadol (levomethadyl), lovastatin, simvastatin, ergot alkaloids such as dihydroergotamine, ergometrine (ergonovine), ergotamine and methylergometrine (methylergonovine) or methadone with itraconazole capsules or oral solution is contraindicated. Itraconazole, a potent cytochrome P450 3A4 isoenzyme system (CYP3A4) inhibitor, may increase plasma concentrations of drugs metabolized by this pathway. Serious cardiovascular events, including QT prolongation, torsades de pointes, ventricular tachycardia, cardiac arrest, and/or sudden death have occurred in patients using cisapride, pimozide, methadone, levacetylmethadol (levomethadyl), or quinidine, concomitantly with itraconazole and/or other CYP3A4 inhibitors.

Indication(s) & Dosage

Oral route
Oesophageal candidiasis
Adult: As oral liquid: 200 mg daily in 1 or 2 divided doses held in the mouth for 20 sec before swallowing. Double the dose in resistant infections.

candidiasis
Adult: As oral liquid: 200 mg daily in 1 or 2 divided doses held in the mouth for 20 sec before swallowing. Double the dose in resistant infections.

Prophylaxis of fungal infections in immunocompromised patients
Adult: As oral liquid: 5 mg/kg daily in 2 divided doses.

Oropharyngeal candidiasis
Adult: As capsule: 100 mg daily for 15 days.

Vulvovaginal candidiasis
Adult: As capsule: 200 mg bid for 1 day.

Pityriasis versicolor
Adult: As capsule: 200 mg daily for 7 days.

Tinea cruris
Adult: As capsule: 100 mg daily for 15 days or 200 mg daily for 7 days.

Tinea corporis
Adult: As capsule: 100 mg daily for 15 days or 200 mg daily for 7 days.

Nail fungal infections
Adult: As capsule: 200 mg daily for 3 mth. Alternatively, pulse therapy with 200 mg bid for 7 days, repeated once for fingernail infections and twice for toenail infections after drug-free intervals of 21-days.

Systemic fungal infections
Adult: As capsule: 100-200 mg once daily, increased to 200 mg bid for invasive or disseminated infections. For life-threatening infections: Loading dose of 200 mg tid for 3 days has been given. 

Primary or secondary prophylaxis of infections in neutropenic or AIDSpatients
Adult: As capsule: 200 mg daily increased to 200 mg bid if necessary.

Tinea pedis
Adult: As capsule: 100 mg daily for 30 days or 200 mg bid for 7 days

Tinea manuum
Adult: As capsule: 100 mg daily for 30 days or 200 mg bid for 7 days

Intravenous route
Systemic fungal infections
Adult: 200 mg infused bid over 1 hr for 2 days. Maintenance: 200 mg daily.

Administration Soln: Should be taken on an empty stomach. Take on an empty stomach & refrain from eating for at least 1 hr after intake.
Cap: Should be taken with food. Take immediately after a full meal.
Contraindications Hypersensitivity to azole antifungals; pregnancy and lactation; hepatic disease. IV: CrCl: <30 ml/min.
Special Precautions Renal insufficiency; CHF, history of CHF, COPD; monitor liver function.
Adverse Drug Reaction(s) Dyspepsia, abdominal pain, nausea, vomiting, diarrhoea; menstrual disorders; constipation, rash, pruritus, urticaria; angioedema, anaphylaxis. Increased liver enzyme values, jaundice, Stevens-Johnson syndrome, hypokalaemia.
Potentially Fatal: Liver failure; heart failure; pulmonary oedema; CV disease.
Drug Interactions Concentration increased by: clarithromycin, erythromycin, HIV protease inhibitors. Concentration decreased by: carbamazepine, phenobarbital, phenytoin, isoniazid, rifabutin, rifampin, nevirapine. Capsule absorption may be decreased by antacids, H2-receptor antagonists, proton pump inhibitors.
Potentially Fatal: Itraconazole is an inhibitor of CYP3A4 and plasma concentrations of many drugs including ciclosporin, digoxin and warfarin may be increased. Please consult detailed drug interactions before prescribing.
Food Interaction Increase in absorption rate when capsule form is taken with or just after a meal; decreased when taken as a liquid in the presence of food.
Pregnancy Category (FDA) Category C: Either studies in animals have revealed adverse effects on the foetus (teratogenic or embryocidal or other) and there are no controlled studies in women or studies in women and animals are not available. Drugs should be given only if the potential benefit justifies the potential risk to the foetus.
Storage Intravenous: Store at ≤25°C. Protect from light and freezing. Oral: Store at 15-25°C.
Pharmacology Itraconazole decreases ergosterol biosynthesis by interfering with cytochrome P450 activity. This inhibits cell membrane function of susceptible fungi including Microsporum species, Trichophyton species, Candida species,Cryptococcus neoformans, Histoplasma capsulatum, Blastomyces dermatitidis and Paracoccidiodes brasiliensis. It also has antiprotozoal activity against Leishmania major.
Absorption: Absorbed from the GIT, capsule enhanced by acidic gastric environment or when taken with food; oral liquid better absorbed during fasting state. Peak plasma concentrations are achieved after 1.5-5 hr.
Distribution: Itraconazole is extensively bound (99.8%) to plasma protein. Widely distributed in skin, sebum, pus and other tissues and organs (higher concentrations compared to plasma). Small amounts are distributed in CSF and breast milk.
Metabolism: Undergoes saturable hepatic metabolism (via cytochrome P450 isoenzyme CYP3A4); converted to hydroxyitraconazole (antifungal activity comparable to the parent drug) and other metabolites.
Excretion: Via urine or bile (as inactive metabolites), via faeces (3-18% as unchanged), stratum corneum and hair (small amounts); not removed by dialysis.
ATC Classification J02AC02 - itraconazole; Belongs to the class of systemic triazole derivative antimycotics. Used in the treatment of mycotic infections.

Brand/Product Info


Total Products : 4    
Brand Name Manufacturer/Marketer Composition Dosage Form Pack Size & Price
I-ZOL Popular Pharmaceuticals Ltd. Itraconazole INN 100mg Capsule 20's: 301.20 MRP
ICONAL Kemiko Pharmaceuticals Ltd Itraconazole INN 100mg Capsule 12's: 180.00 MRP
ITRA 100 Square Pharmaceuticals Ltd. Itraconazole 100mg Capsule 4x6's: 362.40 MRP
ITRACON Navana Pharmaceuticals Limited Itraconazole INN 100mg Capsule 12's: 180.72 MRP

Gen. MedInfo

IMPORTANT WARNING:

Itraconazole can cause congestive heart failure (condition in which the heart cannot pump enough blood through the body). inform your doctor if you have or have ever had heart failure. Your doctor may inform you not to take itraconazole. Also inform your doctor if you have or have ever had a heart attack; an irregular heartbeat; any other type of heart disease; lung, liver, or kidney disease; or any other serious health problem. If you experience any of the following symptoms, stop taking itraconazole and call your doctor immediately: shortness of breath; coughing up white or pink phlegm; weakness; excessive tiredness; fast heartbeat; swelling of the feet, ankles, or legs; waking up at night; and sudden weight gain.

Do not take cisapride, dofetilide, levomethadyl acetate, methadone, pimozide or quinidine while taking itraconazole. Taking these medications with itraconazole can cause a serious irregular heartbeat, which can lead to death.

You also should not take certain calcium channel blockers such as felodipine and nisoldipine; certain cholesterol-lowering medications (statins) such as lovastatin and simvastatin; ergot-type medications such as bromocriptine, cabergoline, dihydroergotamine, ergoloid mesylates, ergotamine, and methylergonovine; midazolam or triazolam while taking itraconazole.

Talk to your doctor about the risks of taking itraconazole.

 

Why is Itraconazole prescribed?

Itraconazole capsules are used to treat fungal infections in the lungs that can spread throughout the body. Itraconazole capsules are also used to treat fungal infections of the fingernails. Itraconazole tablets and capsules are used to treat fungal infections of the toenails. Itraconazole oral solution (liquid) is used to treat yeast infections of the mouth and throat or of the esophagus (tube that connects the throat to the stomach) . Itraconazole is in a class of antifungals called triazoles. It works by slowing the growth of fungi that cause infection.

How totraconazole be used?

Itraconazole may come as a capsule a tablet, and a solution (liquid) to take by mouth. If you are taking itraconazole to treat fungal infections in the lungs, the capsules are usually taken with a full meal one or two times a day for at least 3 months. However, if you are taking itraconazole to treat a serious fungal infection in the lungs, the capsules may be taken with a meal three times a day for the first 3 days of treatment and then taken once or twice a day with a meal for at least 3 months. If you are taking itraconazole to treat fungal infections of the toenails (including or without fingernail infections), the capsules or tablets are usually taken once a day with a full meal for 3 months. If you are taking itraconazole to treat fungal infections of the fingernails only, the capsules are usually taken twice a day with a full meal for one week, skipped for three weeks, and then taken twice a day with a meal for a week. Itraconazole solution is usually taken on an empty stomach once or twice a day for 1–4 weeks or sometimes longer. Follow the directions on your prescription label carefully, and ask your doctor to explain any part you do not understand. Take itraconazole exactly as directed. Do not take more or less of it or take it more often than prescribed by your doctor.

Your doctor may inform you to take itraconazole capsules with a cola soft drink if you have certain medical conditions or are taking any of the following medications: cimetidine ; famotidine; nizatidine; proton-pump inhibitors such as esomeprazole, lansoprazole, omeprazole (Prilosec), pantoprazole (Protonix), and rabeprazole; or ranitidine (Zantac). Follow these directions carefully.

To take itraconazole oral solution for fungal infections of the mouth or throat, swish 10 milliliters (about 2 teaspoons) of the solution in your mouth for several seconds and swallow. Repeat if necessary to take your entire dose.

Itraconazole capsules and oral solution are absorbed into the body in different ways and work to treat different conditions. Do not substitute the capsules for the liquid or the liquid for the capsules. Be sure that your pharmacist gives you the itraconazole product that your doctor prescribed.

If you are taking itraconazole to treat a nail infection, your nails will probably not look healthier until new nails grow. It can take up to 6 months to grow a new fingernail and up to 12 months to grow a new toenail, so you should not expect to see improvement during your treatment or for several months afterward. Continue to take itraconazole even if you do not see any improvement.

Continue to take itraconazole until your doctor informs you to stop even if you feel well. Do not stop taking itraconazole without talking to your doctor. If you stop taking itraconazole too soon, your infection may come back after a short time.

Other uses for Itraconazole

Itraconazole is also sometimes used to treat other types of fungal infections and to prevent fungal infections in people who have human immunodeficiency virus (HIV) or acquired immunodeficiency syndrome (AIDS). Talk to your doctor about the possible risks of using this drug for your condition.

Itraconazole may be prescribed for other uses; ask your doctor for more information.

What special precautions to follow?

Before taking itraconazole,

  • inform your doctor if you are allergic to itraconazole; other antifungal medications such as fluconazole, ketoconazole (Nizoral), or voriconazole; or any other medications. If you are taking itraconazole oral solution, inform your doctor if you are allergic to saccharin or sulfa medications.
  • inform your doctor what other prescription and nonprescription medications, vitamins, nutritional supplements and herbal products you are taking, especially alfentanil; alprazolam; anticoagulants ('blood thinners') such as warfarin; atorvastatin; buspirone; busulfan; calcium channel blockers such as amlodipine, isradipine, nifedipine, nicardipine, nimodipine, and verapamil; carbamazepine; cilostazol; clarithromycin; cyclosporine; diazepam; digoxin; disopyramide; docetaxel; eletriptan; erythromycin; fentanyl; halofantrine; HIV protease inhibitors such as indinavir, ritonavir, and saquinavir; isoniazid; medications for erectile dysfunction such as sildenafil, tadalafil, and vardenafil; midazolam; nevirapine; oral medicine for diabetes; phenobarbital; phenytoin; rifabutin; rifampin; sirolimus; steroids such as dexamethasone, budesonide, fluticasone, and methylprednisolone; tacrolimus; trimetrexate ; vinblastine; vincristine; and vinorelbine . Many other medications may also interact with itraconazole, so be sure to inform your doctor about all the medications you are taking, even those that do not appear on this list.
  • if you are taking an antacid, take it 1 hour before or 2 hours after you take itraconazole.
  • inform your doctor if you have or have ever had the conditions mentioned in the IMPORTANT WARNING section, cystic fibrosis (an inborn disease that causes problems with breathing, digestion, and reproduction), or any condition that decreases the amount of acid in your stomach.
  • inform your doctor if you are pregnant, plan to become pregnant, or are breast-feeding. You should not take itraconazole to treat nail fungus if you are pregnant or could become pregnant. You may start to take itraconazole to treat nail fungus only on the second or third day of your menstrual period when you are sure you are not pregnant. You must use effective birth control during your treatment and for 2 months afterward. If you become pregnant while taking itraconazole to treat any condition, call your doctor.

What special dietary instructions to follow?

Talk to your doctor about drinking grapefruit juice while taking Itraconazole.

What to do if I forget a dose?

Take the missed dose as soon as you remember it. However, if it is almost time for the next dose, skip the missed dose and continue your regular dosing schedule. Do not take a double dose to make up for a missed one.

What side effects can Itraconazole cause?

Itraconazole may cause side effects. inform your doctor if any of these symptoms are severe or do not go away:

  • diarrhea or loose stools

  • constipation

  • gas or bloating

  • stomach pain

  • heartburn

  • unpleasant taste

  • sore or bleeding gums

  • sores in or around the mouth

  • headache

  • dizziness

  • sweating

  • muscle pain or weakness

  • joint pain

  • decreased sexual desire or ability

  • abnormal menstrual periods

  • nervousness

  • depression

  • runny nose and other cold symptoms

  • unusual dreams

  • hair loss

Some side effects can be serious. If you experience any of these symptoms, call your doctor immediately

  • increased sensitivity to sunlight

  • severe skin problems

  • blurred vision or double vision

  • ringing in the ears

  • inability to control urination or urinating much more than usual

If you experience any of the following symptoms or those listed in the IMPORTANT WARNING section, stop taking itraconazole and call your doctor immediately or get emergency medical treatment:

  • excessive tiredness

  • loss of appetite

  • nausea

  • vomiting

  • yellowing of the skin or eyes

  • dark urine

  • pale stools

  • feelings of numbness, tingling, pricking, burning, or creeping on the skin

  • difficulty hearing

  • rash

  • hives

  • itching

  • swelling of the face, throat, tongue, lips, eyes, hands, ankles, or lower legs

  • hoarseness

  • difficulty breathing or swallowing

One of the ingredients in itraconazole oral solution caused cancer in some types of laboratory animals. It is not known whether people who take itraconazole solution have an increased risk of developing cancer. Talk to your doctor about the risks of taking itraconazole solution.

What to know about storage and disposal of Itraconazole?

Keep Itraconazole in the container it came in, tightly closed, and out of reach of children. Store it at room temperature and away from excess heat, light, and moisture (not in the bathroom). Throw away any medication that is outdated or no longer needed. Talk to your pharmacist about the proper disposal of your medication.

In case of emergency/overdose

In case of overdose, consult your doctor. If the victim has collapsed or is not breathing, consult local medical emergency services.

What other information to know?

Keep all appointments with your doctor and the laboratory. Your doctor will order certain lab tests to check your response to Itraconazole.

Do not let anyone else use your medication. If you still have symptoms and need further treatment, consult your doctor.

It is important for you to keep a written list of all of the prescription and nonprescription (over-the-counter) medicines you are taking, as well as any products such as vitamins, minerals, or other dietary supplements. You should bring this list with you each time you visit a doctor or if you are admitted to a hospital. It is also important information to carry with you in case of emergencies.

Ref:  U.S. National Library of Medicine.


This information is provided for reference only and not a replacement for and should only be used in conjunction with full consultation with a registered medical practitioner. It may not contain all the available information you require and cannot substitute professional medical care, nor does it take into account all individual circumstances. Although great effort has been made to ensure content accuracy, mph-bd shall not be held responsible or liable for any claims or damages arising from the use or misuse of the information contained herein, its contents or omissions, or otherwise.

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