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Treatment Information

Protease Inhibitors (PI's)

Protease is another enzyme that HIV needs to make copies of itself. Protease inhibitors are a class of anti-HIV drugs that work by inhibiting (slowing down or stopping) the action of protease. When this enzyme can't do its work, HIV makes defective copies of itself, which can't infect other cells.

Side Effects

The most common side effects of protease inhibitors include nausea, vomiting, diarrhea, bloating, and farting. These side effects often appear in the first days or weeks of using a protease inhibitor. They may go away on their own or they may become milder or less troublesome over time.

Haemophiliacs may experience spontaneous bleeding episodes, including bruising and bleeding into joints. It is not clear if, or how, protease inhibitors cause bleeding. Any episode of bleeding should be reported to your doctor.

With longer use, protease inhibitors may cause increased blood sugar levels and diabetes. Although the risk of developing diabetes is very low, symptoms that may be related to diabetes (increased thirst, increased urination, unexplained weight loss, fatigue, and dry, itchy skin) should be discussed with a doctor.

Dry skin, cracked lips and ingrown toenails have also been reported by people who use protease inhibitors. These symptoms are sometimes referred to as ectodermal dysplasia.

It is important that people using protease inhibitors monitor their liver function with regular blood tests.

Lipodystrophy Syndrome

Lipodystrophy syndrome is the term used to describe a range of symptoms that seem to be associated with the use of protease inhibitors. These symptoms may include physical changes in the body, such as:

  • Thickening of the waist ("protease paunch")
  • Loss of fat from face, arms, legs and buttocks.
  • Bulging or visible veins in the arms and/or legs because of the loss of subcutaneous fat.
  • Increased breast size in women (several bra sizes).
  • Development of breasts in men (gynecomastia)
  • Fat pads at the back of the neck ("buffalo hump") or around the base of the neck ("horse collar").
  • "Moon" face.

Along with these changes in appearance, there may be changes in blood tests that show:

  • Increased levels of triglycerides (fats)
  • Decreased level of high-density lipoprotein (HDL) or "good" cholesterol.
  • Increased levels of low-density lipoprotein (LDL) or "bad" cholesterol.
  • Increased levels of insulin.
  • Insulin resistance or reduced sensitivity to insulin.

The exact cause of lipodystrophy is not known, although many researchers, doctors and patients believe this syndrome is a side effect of protease inhibitors. Other researchers observed body shape changes and high blood fats long before protease inhibitors became available. They suggest that lipodystrophy syndrome may be related to HIV itself and not to antiretroviral drugs. Most likely, lipodystrophy syndrome is caused by several factors, which may include protease inhibitors, different chemicals or proteins in the body and HIV.