What Is Grapefruit Effect

Grapefruit effect is a side effect of consuming grapefruit when a person is on anti-cholesterol drugs. Grapefruit and cholesterol lowering drugs can turn into a deadly combination, literally!

In order to prove this effect, studies were conducted by scientists from the University Of Michigan. Their findings revealed that grapefruit actually raises the levels of cholesterol drugs in the blood.

The result is high toxic levels of the drug in the blood, leading to a condition known as Rhabdomyolosis (rapid breakdown of muscle tissue of the skeleton).

Mechanism of Grapefruit Effect

  • The mechanism has been traced to the release of furanocumarins, a biochemical found in grapefruit, that can cause hazardous effects on interacting with anti-cholesterol medication.
  • These furanocumarins, are believed to block a certain enzyme (CYP 3A4), found in the walls of the intestine. This enzyme is critical for breaking down cholesterol drugs.
  • Thus, without this enzyme, the drug accumulates in the body leading to disastrous results.
  • Further, it also blocks another molecule, P-glycoprotein produced in the walls of the small intestine. This molecule carries the statin drugs back to the gut.
  • Finally all these effects lead to building up of statin levels and may trigger a rare but serious statin-associated complication called rhabdomyolysis.
  • Rhabdomyolosis affects muscle tissue of the skeleton that can cause temporary paralysis and acute kidney failure.
  • Another important factor is that grapefruit remains in the body for as long as 24 hours and continues to cause damage for a long time.

What are the Drugs That Cause Grapefruit Effect

  • Usually statin drugs are the class of anti-cholesterols involved in causing this effect.most common ones are: Mevacor, Zocor and Lipitor.
  • Some drugs used to control blood pressure are also known to interact with grapefruit and grapefruit juice. Procardia and Plendil are among them.
  • Certain anti-HIV drugs can also react adversely to grapefruit.

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