Unlike most injectable anabolic steroids, stanozolol is not esterified and is sold as an aqueous suspension, or in oral tablet form. The drug has a high oral bioavailability, due to a C17 α-alkylation which allows the hormone to survive first-pass liver metabolism when ingested. It is because of this that stanozolol is also sold in tablet form.

Stanozolol is usually considered a safer choice for female bodybuilders in that its anabolic effects predominate over its androgenic effects, although virilization and masculinization are still very common even at low doses.

Stanozolol has been used in both animal and human patients for a number of conditions. In humans, it has been demonstrated to be successful in treating anaemia and hereditary angioedema. Veterinarians may prescribe the drug to improve muscle growth, red blood cell production, increase bone density and stimulate the appetite of debilitated or weakened animals.

In bodybuilding, stanozolol is typically "stacked" with other testosterone-based anabolic steroids. Stanozolol is preferred by many steroid users because it causes strength increases without excess weight gain, promotes increases in vascularity,^{[citation needed]} and will not convert to estrogen. It also does not cause excess water retention, and is thought to have a diuretic effect on the body.^{[citation needed]}

Stanozolol is commonly used by athletes and bodybuilders alike to lose fat while retaining lean body mass. It is usually used in a "cutting cycle", to help preserve lean body mass while metabolizing adipose, although it has not been proven conclusively that it has any special fat-burning properties.

It is presented most commonly as a 50 mg/mL injection or a 5 mg tablet. However, recently 100 mg/mL versions have become available. A common dosage can be 10–25 mg/day orally and 25–50 mg daily injected, with optimal results usually seen at 50 mg/day. It is reduced to micrometer particles in aqueous suspension and does not have a typical elimination half-life. Authentic stanozolol can easily be seen, because it will separate in its container if left undisturbed for a number of hours (the micronized crystal will fall to the bottom, and the water suspension will rise to the top). It has a white, milky color.

An alternative to stanozolol is furazabol. Furazabol's effects are virtually identical to stanozolol except that instead of having an extremely adverse effect on cholesterol values, furazabol actually improves a person's blood lipid profile (at therapeutic doses, not performance enhancing ones).^{[citation needed]} Sold under the trade name Miotolan, Furazabol is a standard treatment in Japan for hyperlipemia.