Antifungal Drugs, Systemic

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Antifungal Drugs, Systemic


Systemic antifungal drugs are medicines taken by mouth or by injection to treat deep infections caused by a fungus.


Systemic antifungal drugs are used to treat infections in various parts of the body that are caused by a fungus. A fungus is an organism that can be either one-celled or filamentous. Unlike a plant, which makes its own food, or an animal, which eats plants or other animals, a fungus survives by invading and living off other living things. Fungi thrive in moist, dark places, including some parts of the body.

Fungal infections can either be systemic, meaning that the infection is deep, or topical (dermatophytic), meaning that the infection is superficial and occurs on the skin. Additionally, yeast infections can affect the mucous membranes of the body. Fungal infections on the skin are usually treated with creams or ointments (topical antifungal drugs ). However, systemic infections, yeast infections or topical infections that do not clear up after treatment with creams or ointments may need to be treated with systemic antifungal drugs. These drugs are used, for example, to treat common fungal infections such as tinea (ringworm ), which occurs on the skin or candidiasis (a yeast infection, also known as trush), which can occur in the throat, in the vagina, or in other parts of the body. They are also used to treat other deep fungal infections such as histoplasmosis, blastomycosis, and aspergillosis, which can affect the lungs and other organs. They are sometimes used to prevent or treat fungal infections in people whose immune systems are weakened, such as bone marrow or organ transplant patients and people with AIDS.


Antifungal drugs are categorized depending on their route or site of action, their mechanism of action and their chemical nature.

Systemic antifungal drugs, such as capsofungin (Cancidas), flucytosine, fluconazole (Diflucan), itraconazole (Sporanox), ketoconazole (Nizoral), and miconazole (Monistat I.V.) are available only by prescription. They are available in tablet, capsule, liquid, and injectable forms.

Recommended dosage

The recommended dosage depends on the type of antifungal drug and the nature and extent of fungal infection being treated. Doses may also be different for different patients. The prescribing physician or the pharmacist can provide dosage information. Systemic antifungal drugs must be taken exactly as directed. Itraconazole and ketoconazole should be taken with food.

Fungal infections can take a long time to clear up, so it may be necessary to take the medication for several months, or even for a year or longer. It is very important to keep taking the medicine for as long as the physician says to take it, even if symptoms seem to improve. If the drug is stopped too soon, the symptoms may return.

Systemic antifungal drugs work best when their amount is kept constant in the body, meaning that they have to be taken regularly, at the same time every day, and without missing any doses.

Patients taking the liquid form of ketoconazole should use a specially marked medicine spoon or other medicine measuring device to make sure they take the correct amount. A regular household teaspoon may not hold the right amount of medicine. Ask the pharmacists about ways to accurately measure the dose of these drugs.


If symptoms do not improve within a few weeks, the prescribing physician should be informed.

While taking this medicine, regular medical visits should be scheduled. The physician needs to keep checking for side effects throughout the antifungal therapy.


Elixir A sweetened liquid that contains alcohol, water, and medicine.

Fetus A developing baby inside the womb.

Fungus A unicellular to filamentous organism that causes parasitic infections.

Ointment A thick substance that contains medicine and is meant to be spread on the skin, or if an ophthalmic ointment, in the eye.

Systemic A term used to describe a medicine that has effects throughout the body, as opposed to topical drugs that work on the skin. Most medicines that are taken by mouth or by injection are systemic drugs.

Some people feel drowsy or dizzy while taking systemic antifungal drugs. Anyone who takes these drugs should not drive, use machines or do anything else that might be dangerous until they have found out how the drugs affect them.

Liver problems, stomach problems and other problems may occur in people who drink alcohol while taking systemic antifungal drugs. Alcohol and prescription or nonprescription (over-the-counter) drugs that contain alcohol should be avoided while taking antifungal drugs. (Medicines that may contain alcohol include some cough syrups, tonics, and elixirs.) Alcohol should be avoided for at least a day after taking an antifungal drug.

The antifungal drug ketoconazole may make the eyes unusually sensitive to light. Wearing sunglasses and avoiding exposure to bright light may help.

Special conditions

People with certain medical conditions or who are taking certain other medicines can have problems if they take systemic antifungal drugs. Before taking these drugs, the prescribing physician should be informed about any of the following conditions:

ALLERGIES. Anyone who has had unusual reactions to systemic antifungal drugs in the past should let his or her physician know about the problem before taking the drugs again. The physician should also be told about any allergies to foods, dyes, preservatives, or other substances.

PREGNANCY. In laboratory studies of animals, systemic antifungal drugs have caused birth defects and other problems in the mother and fetus. Studies have not been done on pregnant women, so it is not known whether these drugs cause similar effects in people. Women who are pregnant or who plan to become pregnant should check with their physicians before taking systemic antifungal drugs. Any woman who becomes pregnant while taking these drugs should let her physician know immediately.

BREASTFEEDING. Systemic antifungal drugs pass into breast milk. Women who are breastfeeding should check with their physicians before using systemic antifungal drugs.

OTHER MEDICAL CONDITIONS. People who have medical conditions that deplete stomach acid (achlorhydria) or decrease stomach acid (hypochlorhydria) should be sure to inform their physicians about their condition before they use a systemic antifungal drug. These drugs are not active in their natural form, but must be converted to the active form by an acid. If these is not enough stomach acid, the drugs will be ineffective. For people with insufficient stomach acid, it may help to take the medicine with an acidic drink, such as a cola. The patient's health care provider can suggest the best way to take the medicine.

Before using systemic antifungal drugs, people with any of these medical problems should also make sure their physicians are aware of their conditions:

  • current or past alcohol abuse
  • liver disease
  • kidney disease

USE OF CERTAIN MEDICINES. Taking systemic antifungal drugs with certain other drugs may affect the way the drugs work or may increase the chance of side effects.

Side effects


Although rare, severe allergic reactions to this medicine have been reported. Call a physician immediately if any of these symptoms develop after taking fluconazole (Diflucan):

  • hives, itching, or swelling
  • breathing or swallowing problems
  • sudden drop in blood pressure
  • diarrhea
  • abdominal pain


Ketoconazole has caused anaphylaxis (a life-threatening allergic reaction) in some people after their first dose. This is a rare reaction.

Systemic antifungal drugs in general

Systemic antifungal drugs may cause serious and possibly life-threatening liver damage. Patients who take these drugs should have liver function tests before they start taking the medicine and as often as their physician recommends while they are taking it. The physician should be notified immediately if any of these symptoms develop:

  • loss of appetite
  • nausea or vomiting
  • yellow skin or eyes
  • unusual fatigue
  • dark urine
  • pale stools

The most common minor side effects of systemic antifungal drugs are constipation, diarrhea, nausea, vomiting, headache, drowsiness, dizziness, and flushing of the face or skin. These problems usually go away as the body adjusts to the drug and do not require medical treatment. Less common side effects, such as menstrual problems in women, breast enlargement in men, and decreased sexual ability in men also may occur and do not need medical attention unless they do not improve in a reasonable amount of time.

More serious side effects are not common, but may occur. If any of the following side effects occur, check with the physician who prescribed the medicine immediately:

  • fever and chills
  • skin rash or itching
  • high blood pressure
  • pain, redness, or swelling at site of injection (for injectable miconazole)

Other rare side effects are possible. Anyone who has unusual symptoms after taking systemic antifungal drugs should get in touch with his or her physician.


Serious and possibly life-threatening side effects can result if the oral forms of itraconazole or ketoconazole or the injectable form of miconazole are taken with certain drugs. Do not take those types of systemic antifungal drugs with any of the following drugs unless the physician approves of the therapy:

  • astemizole (Hismanal)
  • cisapride (Propulsid)
  • antacids
  • theophylline-containing anti-wheezing medications

Taking an acid blocker such as cimetidine (Tagamet), famotidine (Pepcid), nizatidine (Axid), omeprazole (Prilosec), or ranitidine (Zantac) at the same time as a systemic antifungal drug may prevent the antifungal drug from working properly. For best results, take the acid blocker at least 2 hours after taking the antifungal drug.

In addition, systemic antifungal drugs may interact with many other medicines. When this happens, the effects of one or both of the drugs may change or the risk of side effects may be greater. Anyone who takes systemic antifungal drugs should inform the prescribing physician about all other prescription and nonprescription (over-the-counter) medicines he or she is taking. Among the drugs that may interact with systemic antifungal drugs are:

  • acetaminophen (Tylenol)
  • birth control pills
  • male hormones (androgens)
  • female hormones (estrogens)
  • medicine for other types of infections
  • antidepressants
  • antihistamines
  • muscle relaxants
  • medicine for diabetes, such as tolbutamide (Orinase), glyburide (DiaBeta), and glipizide (Glucotrol)
  • blood-thinning medicine, such as warfarin (Coumadin)

The list above does not include every drug that may interact with systemic antifungal drugs. Be sure to check with a physician or pharmacist before combining systemic antifungal drugs with any other medicine.