Fluconazole blocks a fungal enzyme that turns lanosterol into ergosterol, a normal sterol in the fungal cell. As ergosterol runs short, unusual sterols pile up inside the fungus. This slows or stops the fungus from growing rather than killing it outright. The matching enzyme in human cells is far less sensitive to the drug.
Nearly all of a dose is absorbed by mouth, the blood level peaks within 1 to 2 hours, and the drug reaches body fluids and tissues such as spinal fluid, saliva, and the vagina. Half of it leaves the body in about 30 hours, so it is taken once a day, and a double first dose brings levels up faster. The kidneys clear most of it unchanged, so weak kidneys let it build up. It also slows enzymes that break down many other medicines, which explains its many drug interactions, and it can lengthen the heart's QT interval and trigger a dangerous rhythm.