Antifungals, Azole
(Systemic)
Brand Names
Some commonly used brand names are:
In the U.S.—
In Canada—
Note:
| For quick reference, the following antifungals are numbered to match the corresponding brand names. |
Category
- Antiadrenal --Ketoconazole
- Antifungal, systemic --Fluconazole ; Itraconazole; Ketoconazole
- Antineoplastic --Ketoconazole
Description
Azole antifungals are used to treat serious fungus infections that may occur in different parts of the body. These medicines may also be used for other problems as determined by your doctor.
Azole antifungals are available only with your doctor's prescription, in the following dosage forms:
Oral
- Fluconazole
- Capsules (Canada)
- Oral suspension (U.S. and Canada)
- Tablets (U.S. and Canada)
- Itraconazole
- Capsules (U.S. and Canada)
- Oral solution (U.S.)
- Ketoconazole
- Oral suspension (Canada)
- Tablets (U.S. and Canada)
Parenteral
- Fluconazole
- Injection (U.S. and Canada)
- Itraconazole
Before Using This Medicine
In deciding to use a medicine, the risks of taking the medicine must be weighed against the good it will do. This is a decision you and your doctor will make. For the azole antifungals, the following should be considered:
Allergies—Tell your doctor if you have ever had any unusual or allergic reaction to any of the azole antifungals. Also tell your health care professional if you are allergic to any other substances, such as foods, preservatives, or dyes.
Pregnancy—Studies have not been done in pregnant women. However, studies in some animals have shown that azole antifungals, taken in high doses, may cause harm to the mother and the fetus. They have caused birth defects in animals. Before taking these medicines, make sure your doctor knows if you are pregnant or if you may become pregnant.
Breast-feeding—Azole antifungals pass into breast milk. Mothers who are taking these medicines and who wish to breast-feed should discuss this with their doctors.
Children—A small number of children have been safely treated with azole antifungals. Be sure to discuss with your child's doctor the use of these medicines in children.
Older adults—Many medicines have not been studied specifically in older people. Therefore, it may not be known whether they work exactly the same way they do in younger adults or if they cause different side effects or problems in older people. There is no specific information comparing use of azole antifungals in the elderly with use in other age groups.
Other medicines—Although certain medicines should not be used together at all, in other cases two different medicines may be used together even if an interaction might occur. In these cases, your doctor may want to change the dose, or other precautions may be necessary. When you are taking azole antifungals, it is especially important that your health care professional know if you are taking any of the following:
- Acetaminophen (e.g., Tylenol) (with long-term, high-dose use) or
- Amiodarone (e.g., Cordarone) or
- Anabolic steroids (nandrolone [e.g., Anabolin], oxandrolone [e.g., Anavar], oxymetholone [e.g., Anadrol], stanozolol [e.g., Winstrol]) or
- Androgens (male hormones) or
- Antithyroid agents (medicine for overactive thyroid) or
- Carmustine (e.g., BiCNU) or
- Chloroquine (e.g., Aralen) or
- Dantrolene (e.g., Dantrium) or
- Daunorubicin (e.g., Cerubidine) or
- Disulfiram (e.g., Antabuse) or
- Divalproex (e.g., Depakote) or
- Estrogens (female hormones) or
- Etretinate (e.g., Tegison) or
- Gold salts (medicine for arthritis) or
- Hydroxychloroquine (e.g., Plaquenil) or
- Mercaptopurine (e.g., Purinethol) or
- Methotrexate (e.g., Mexate) or
- Methyldopa (e.g., Aldomet) or
- Naltrexone (e.g., Trexan) (with long-term, high-dose use) or
- Oral contraceptives (birth control pills) containing estrogen or
- Other anti-infectives by mouth or by injection (medicine for infection) or
- Phenothiazines (acetophenazine [e.g., Tindal], chlorpromazine [e.g., Thorazine], fluphenazine [e.g., Prolixin], mesoridazine [e.g., Serentil], perphenazine [e.g., Trilafon], prochlorperazine [e.g., Compazine], promazine [e.g., Sparine], promethazine [e.g., Phenergan], thioridazine [e.g., Mellaril], trifluoperazine [e.g., Stelazine], triflupromazine [e.g., Vesprin], trimeprazine [e.g., Temaril]) or
- Plicamycin (e.g., Mithracin) or
- Valproic acid (e.g., Depakene)—Use of these medicines with azole antifungals may increase the chance of side effects affecting the liver
- Alprazolam (e.g., Xanax) or
- Diazepam (e.g., Valium) or
- Midazolam (e.g., Versed) or
- Triazolam (e.g., Halcion)—Sedative effects are increased when taken with itraconazole or ketoconazole.
- Amantadine (e.g., Symmetrel) or
- Antacids or
- Anticholinergics (medicine for abdominal or stomach spasms or cramps) or
- Antidepressants (medicine for depression) or
- Antidyskinetics (medicine for Parkinson's disease or other conditions affecting control of muscles) or
- Antihistamines or
- Antipsychotics (medicine for mental illness) or
- Buclizine (e.g., Bucladin) or
- Cimetidine (e.g., Tagamet) or
- Cyclizine (e.g., Marezine) or
- Cyclobenzaprine (e.g., Flexeril) or
- Disopyramide (e.g., Norpace) or
- Famotidine (e.g., Pepcid) or
- Flavoxate (e.g., Urispas) or
- Ipratropium (e.g., Atrovent) or
- Meclizine (e.g., Antivert) or
- Methylphenidate (e.g., Ritalin) or
- Nizatidine (e.g., Axid) or
- Omeprazole (e.g., Prilosec) or
- Orphenadrine (e.g., Norflex) or
- Oxybutynin (e.g., Ditropan) or
- Procainamide (e.g., Pronestyl) or
- Promethazine (e.g., Phenergan) or
- Quinidine (e.g., Quinidex) or
- Ranitidine (e.g., Zantac) or
- Sucralfate (e.g., Carafate) or
- Trimeprazine (e.g., Temaril)—Use of these medicines may decrease the effects of itraconazole and ketoconazole; these medicines should be taken at least 2 hours after itraconazole or ketoconazole
- Antidiabetic agents, oral (chlorpropamide [e.g., Diabinese], glipizide [e.g., Glucotrol], glyburide [e.g., DiaBeta, Micronase], tolbutamide [e.g., Orinase]) or
- Astemizole (e.g., Hismanal) or
- Terfenadine (e.g., Seldane)—These medicines should not be taken with fluconazole, itraconazole, or ketoconazole; these azole antifungals may increase the chance of serious side effects of astemizole or terfenadine
- Atorvastatin (e.g., Lipitor) or
- Cerivastatin (e.g., Baycol) or
- Lovastatin (e.g., Mevacor) or
- Simvastatin (e.g., Zocor)—Use of these drugs with itraconazole or ketoconazole since increased levels of these drugs can cause serious muscular disorders.
- Busulfan (e.g., Myleran) or
- Docetaxel (e.g., Taxotere) or
- Vinblastine (e.g., Velban) or
- Vincristine (e.g., Oncovin)—Metabolism of these drugs may be delayed by itraconazole.
- Felodipine (e.g., Plendil) or
- Nifedipine (e.g., Procardia) or
- Verapamil (e.g., Isoptin, Covera)—Concurrent use can cause water retention or slow the heart rate.
- Carbamazepine (e.g., Tegretol) or
- Phenobarbital (e.g., Luminal)
- Phenytoin (e.g., Dilantin)—Concurrent use with itraconazole may decrease itraconazole concentrations. Phenytoin concentrations may be increased.
- Cisapride (e.g., Propulsid)—Cisapride should not be taken with itraconazole or oral ketoconazole; these azole antifungals may increase the chance of serious side effects of cisapride
- Cyclosporine (e.g., Sandimmune, Neoral)
- Tacrolimus (e.g., Prograf)—Concomitant use may cause increased concentrations of these drugs, resulting in toxicity.
- Didanosine (e.g., ddI, Videx)—Use of didanosine with itraconazole or ketoconazole may decrease the effects of itraconazole or ketoconazole, as well as of didanosine. Itraconazole and ketoconazole should be taken at least 2 hours before or 2 hours after didanosine is given
- Digoxin (e.g., Lanoxin)—Digoxin concentrations may be increased, resulting in toxicity.
- Dofetilide (eg., Tikosyn) or
- Pimozide (e.g.,Orap) or
- Quinidine (e.g., Quinaglute, Cardioquin, Quinidex) —Pimozide, dofetilide and quinidine should not be taken with itraconazole; itraconazole may increase the chance of serious side effects of pimozide, dofetilide and quinidine.
- Indinavir (e.g., Crixivan) or
- Ritonavir (e.g., Norvir) or
- Saquinivir (e.g., Invirase)—Use of these drugs with itraconazole or ketoconazole may increase the effects of indinavir
- Isoniazid or
- Rifampin (e.g., Rifadin)—These medicines may decrease the effects of azole antifungals
- Clarithromycin (e.g., Biaxin) or
- Erythromycin (e.g., E-Mycin)—Plasma concentrations of itraconazole may be increased.
- Nevirapine (e.g., Viramune)—Plasma concentrations of itraconazole or ketoconazole may be decreased.
- Warfarin (e.g., Coumadin)—Anticoagulant effects may be increased.
Other medical problems—The presence of other medical problems may affect the use of azole antifungals. Make sure you tell your doctor if you have any other medical problems, especially:
- Congestive heart failure—Itraconazole may slow down the heart rhythm and make heart failure worse.
- Achlorhydria (absence of stomach acid) or
- Hypochlorhydria (decreased amount of stomach acid)—Itraconazole and ketoconazole may not be absorbed from the stomach as well in patients who have low levels of or no stomach acid
- Alcohol abuse (or history of) or
- Liver disease—Alcohol abuse or liver disease may increase the chance of side effects caused by azole antifungals
- Kidney disease—The effects of fluconazole may be increased in patients with kidney disease
Proper Use of This Medicine
Ketoconazole and the capsule form of itraconazole should be taken with a fullmeal. The oral solution form of itraconazole should be taken on an empty stomach. If you have any questions about the antifungal medicine you are taking, check with your health care professional.
For patients taking the oral liquid form of fluconazole, itraconazole, or ketoconazole:
- Use a specially marked measuring spoon or other device to measure each dose accurately. The average household teaspoon may not hold the right amount of liquid.
If you have achlorhydria (absence of stomach acid) or hypochlorhydria (decreased amount of stomach acid), and you are taking itraconazole or ketoconazole, your doctor may want you to take your medicine with an acidic drink. You may dissolve your medicine in cola or seltzer water and drink the solution, or your may take your medicine with a glass of cola or seltzer water. Your doctor may suggest that you dissolve each capsule or tablet in a teaspoonful of weak hydrochloric acid solution to help you absorb the medicine better. Your health care professional can prepare the solution for you. After you dissolve the tablet in the acid solution, add this mixture to a small amount (1 or 2 teaspoonfuls) of water in a glass. Drink the mixture through a plastic or glass drinking straw. Place the straw behind your teeth, as far back in your mouth as you can. This will keep the acid from harming your teeth. Be sure to drink all the liquid to get the full dose of medicine. Next, swish around in your mouth about one-half glass of water and then swallow it. This will help wash away any acid that may remain in your mouth or on your teeth.
To help clear up your infection completely, it is very important that you keep taking this medicine for the full time of treatment , even if your symptoms begin to clear up or you begin to feel better after a few days. Since fungus infections may be very slow to clear up, you may have to continue taking this medicine every day for as long as 6 months to a year or more. Some fungus infections never clear up completely and require continuous treatment. If you stop taking this medicine too soon, your symptoms may return.
This medicine works best when there is a constant amount in the blood. To help keep the amount constant, do not miss any doses . Also, it is best to take each dose at the same time every day. If you need help in planning the best time to take your medicine, check with your health care professional.
Dosing—
The dose of azole antifungals may be different for different patients. Follow your doctor's orders or the directions on the label. The following information includes only the average doses of azole antifungals. Your dose of fluconazole may be different if you have kidney disease. If your dose is different, do not change it unless your doctor tells you to do so.
The number of capsules or tablets, or the amount of oral suspension or injection that you take depends on the strength of the medicine. Also, the number of doses you take each day, the time allowed between doses, and the length of time you take the medicine depend on the medical problem for which you are taking azole antifungals.
For fluconazole
- For fungus infections:
- For capsule dosage form:
- Adults—150 milligrams (mg) as a single dose to treat vaginal yeast infections.
- Children up to 18 years of age—Dose must be determined by your doctor.
- For oral suspension and tablet dosage forms:
- Adults and teenagers—200 to 400 mg on the first day, then 100 to 400 mg once a day for weeks or months, depending on the medical problem being treated. A vaginal yeast infection is treated with a single dose of 150 mg.
- Children 6 months of age and older—6 to 12 mg per kilogram (mg/kg) (2.7 to 5.4 mg per pound) of body weight on the first day, then 3 to 12 mg/kg (1.35 to 5.4 mg per pound) of body weight once a day for weeks or months, depending on the medical problem being treated.
- Infants and children up to 6 months of age—Dose must be determined by your doctor.
- For injection dosage form:
- Adults and teenagers—200 to 400 mg on the first day, then 100 to 400 mg once a day, injected into a vein, for weeks or months, depending on the medical problem being treated.
- Children 6 months of age and older—6 to 12 mg per kilogram (mg/kg) (2.7 to 5.4 mg per pound) of body weight on the first day, then 3 to 12 mg/kg (1.35 to 5.4 mg per pound) of body weight once a day, injected into a vein, for weeks or months, depending on the medical problem being treated.
- Infants and children up to 6 months of age—Dose must be determined by your doctor.
For itraconazole
- For fungus infections:
- For capsule dosage form:
- Adults and teenagers—200 milligrams (mg) once a day, which may be increased up to 400 mg once a day for weeks or months, depending on the medical problem being treated. Fingernail and toenail infections are treated with 200 mg one or two times a day for weeks or months.
- Children up to 16 years of age—Dose must be determined by your doctor.
- For injection dosage form:
- Adults—200 milligrams (mg) twice a day for 4 doses, then 200 mg once a day.
- Children—Dose must be determined by your doctor.
- For oral solution dosage form:
- Adults and teenagers—100 to 200 mg once a day for days or weeks, depending on the medical problem being treated.
- Children up to 12 years of age—Dose must be determined by your doctor.
For ketoconazole
- For fungus infections:
- For oral dosage form (oral suspension and tablets):
- Adults and teenagers—200 to 400 milligrams (mg) once a day for days or weeks, depending on the medical problem being treated.
- Children over 2 years of age—3.3 to 6.6 mg per kilogram (1.5 to 3 mg per pound) of body weight once a day for days or weeks, depending on the medical problem being treated.
- Infants and children up to 2 years of age—Dose must be determined by your doctor.
Missed dose—
If you miss a dose of this medicine, take it as soon as possible. This will help to keep a constant amount of medicine in the blood. However, if it is almost time for your next dose, skip the missed dose and go back to your regular dosing schedule. Do not double doses.
Storage—
To store this medicine:
- Keep out of the reach of children.
- Store away from heat and direct light.
- Do not store the capsule or tablet form of this medicine in the bathroom, near the kitchen sink, or in other damp places. Heat or moisture may cause the medicine to break down.
- Keep the oral liquid form of this medicine from freezing.
- Do not keep outdated medicine or medicine no longer needed. Be sure that any discarded medicine is out of the reach of children.
Precautions While Using This Medicine
It is important that your doctor check your progress at regular visits. This will allow your doctor to check for any unwanted effects.
If your symptoms do not improve within a few weeks (or months for some infections), or if they become worse, check with your doctor.
These medicines should notbe taken with astemizole (e.g., Hismanal), cisapride (e.g., Propulsid),dofetilide (e.g., Tikosyn) or terfenadine (e.g., Seldane). Doing so may increase the risk of serious side effects affecting the heart.
Liver problems may be more likely to occur if you drink alcoholic beverages while you are taking ketoconazole. Alcoholic beverages may also cause stomach pain, nausea, vomiting, headache, or flushing or redness of the face. Other alcohol-containing preparations (for example, elixirs, cough syrups, tonics) may also cause problems. These problems may occur for at least a day after you stop taking ketoconazole. Therefore, you should not drink alcoholic beverages or use alcohol-containing preparations while you are taking this medicine and for at least a day after you stop taking it.
If you are taking antacids, cimetidine (e.g., Tagamet), famotidine (e.g., Pepcid), nizatidine (e.g., Axid), omeprazole (e.g., Prilosec), or ranitidine (e.g., Zantac) while you are taking itraconazole or ketoconazole, take the other medicine at least 2 hours after you take itraconazole or ketoconazole . If you take these medicines at the same time that you take itraconazole or ketoconazole, they will keep your antifungal medicine from working properly.
Ketoconazole may cause your eyes to become more sensitive to light than they are normally. Wearing sunglasses and avoiding too much exposure to bright light may help lessen the discomfort.
Side Effects of This Medicine
Along with its needed effects, a medicine may cause some unwanted effects. Although not all of these effects may occur, if they do occur they may need medical attention.
Check with your doctor immediately if any of the following side effects occur:
-
Less common
- Fever and chills;
skin rash or itching
-
Rare
- Dark or amber urine;
fever and sore throat;
loss of appetite;
pale stools;
reddening, blistering, peeling, or loosening of skin and mucous membranes;
stomach pain;
unusual bleeding or bruising;
unusual tiredness or weakness;
yellow eyes or skin
Other side effects may occur that usually do not need medical attention. These side effects may go away during treatment as your body adjusts to the medicine. However, check with your doctor if any of the following side effects continue or are bothersome:
-
Less common
- Constipation;
diarrhea;
dizziness;
drowsiness;
headache;
nausea;
vomiting
-
Rare--for ketoconazole
- Decreased sexual ability in males;
enlargement of the breasts in males;
increased sensitivity of the eyes to light;
menstrual irregularities
Other side effects not listed above may also occur in some patients. If you notice any other effects, check with your doctor.
Additional Information
Once a medicine has been approved for marketing for a certain use, experience may show that it is also useful for other medical problems. Although these uses are not included in product labeling, azole antifungals are used in certain patients with the following medical conditions:
- Cryptococcosis
- Cushing's syndrome
- Febrile neutropenia
- Fungus infections in newborns
- Hirsutism
- Histoplasmosis
- Paronychia (infection of the tissue surrounding the nail)
- Penicillium marneffei infection
- Pneumonia caused by fungus
- Prostate cancer
- Ringworm of the beard, hand, or scalp
- Septicemia (infection of the blood) caused by fungus
- Skin infection (including leishmaniasis and sporotrichosis)
Other than the above information, there is no additional information relating to proper use, precautions, or side effects for these uses.
Developed: 11/14/1994
Revised: 06/27/2001
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