the Dangers of Grapefruit Juice with Eszo and Mesyrel - Pharmacology

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Medication inquiries


The combination of Eszopiclone (Eszo) and Mesoridazine (Mesyrel) with grapefruit juice can pose life-threatening risks due to the potential for grapefruit juice to inhibit the cytochrome P450 3A4 enzyme.
This enzyme is responsible for the metabolism of many medications, including Eszopiclone and Mesoridazine.
When grapefruit juice is consumed, it can lead to increased blood levels of these drugs, resulting in enhanced effects and a higher risk of serious side effects, including respiratory depression and cardiac issues.
There is no specific amount of grapefruit juice that can be universally defined as dangerous, as individual responses can vary based on factors such as the person's health status, the dosage of the medications, and other concurrent medications.
Therefore, it is crucial to avoid grapefruit juice entirely when taking these medications.
If a patient with major depressive disorder were to attempt suicide using this method, inducing vomiting with milk is not recommended.
Milk does not effectively neutralize or eliminate the effects of these medications, and inducing vomiting can lead to further complications, including aspiration.
Immediate medical attention should be sought in such situations.

Ya Ya, 20~29 year old female. Ask Date: 2003/08/11

Dr. Zheng Shuwen reply Pharmacology


Hello! Grapefruit juice can affect the metabolism of Mesyrel, leading to increased concentrations of the drug in the body.
As the drug concentration rises, the relative side effects of Mesyrel may also increase.
Common side effects of Mesyrel include dizziness, headache, drowsiness, fatigue, and gastrointestinal discomfort.
There is also the potential for serotonin syndrome, characterized by clinical symptoms such as altered mental status (e.g., confusion, loss of motivation, drowsiness, coma), changes in behavior (e.g., agitation, anxiety), neuromuscular symptoms (e.g., tremors, ataxia, muscle rigidity, hyperreflexia, seizures), and autonomic instability (e.g., fever, sweating, tachycardia, nausea, vomiting, hypertension, mydriasis, diarrhea).
However, serotonin syndrome is rare, but it can be life-threatening in severe cases.
Therefore, it is advisable to avoid consuming grapefruit juice while taking this medication to minimize the risk of increased side effects and discomfort.
On the other hand, grapefruit juice does not affect Eszo, so there is no interaction between the two.
Reports indicate that consuming just one cup (200 milliliters) of grapefruit juice can delay drug metabolism, prolonging the time the drug remains in the body and potentially causing unwanted side effects, with effects lasting up to 24 hours, even if consumed a few hours before taking the medication.
Close monitoring of side effects due to the interaction between Mesyrel and grapefruit juice is necessary.
Mild cases may only require rest, while severe cases should receive symptomatic treatment.
There is no literature supporting the use of milk for inducing vomiting in this context.

Reply Date: 2003/08/11

More Info


Grapefruit juice is known to interact with various medications, including Eszopiclone (Eszo) and Mesoridazine (Mesyrel), leading to potentially dangerous consequences. The primary concern with grapefruit juice is its ability to inhibit the cytochrome P450 3A4 enzyme in the liver, which is responsible for metabolizing many drugs. When this enzyme is inhibited, the concentration of certain medications in the bloodstream can increase significantly, leading to heightened effects and side effects.


Interaction with Mesyrel and Eszo
1. Mesyrel (Mesoridazine): Grapefruit juice can increase the plasma concentration of Mesyrel, which may lead to an increase in its side effects. Common side effects of Mesyrel include dizziness, drowsiness, and gastrointestinal discomfort. More severe reactions can include serotonin syndrome, characterized by symptoms such as confusion, agitation, rapid heart rate, and muscle rigidity. In rare cases, this syndrome can be life-threatening. The consumption of grapefruit juice, even in small amounts (e.g., 200 mL), can significantly affect the metabolism of Mesyrel, potentially leading to these dangerous side effects.

2. Eszopiclone (Eszo): Fortunately, Eszopiclone does not have a significant interaction with grapefruit juice. Therefore, while caution is advised with Mesyrel, Eszo does not pose the same risk when consumed with grapefruit juice.


Risk of Life-Threatening Situations
The risk of life-threatening situations arises primarily from the interaction of grapefruit juice with Mesyrel. While there is no specific amount of grapefruit juice that can be pinpointed as the threshold for danger, even a single glass can lead to increased drug levels in the body. The effects can last up to 24 hours, meaning that consuming grapefruit juice shortly before or after taking Mesyrel can still pose risks.


Suicide Risk and Inducing Vomiting
Regarding the concern about a depressed patient potentially using this interaction as a means of self-harm, it is crucial to approach this matter with sensitivity. If someone has ingested a harmful amount of medication, inducing vomiting is not always the safest course of action. Milk is not a recommended method for inducing vomiting, especially in cases of drug overdose. Instead, it is vital to seek immediate medical attention. Healthcare professionals can provide the appropriate interventions, such as activated charcoal, which may help absorb the drug if administered shortly after ingestion.


Conclusion
In summary, the interaction between grapefruit juice and Mesyrel can lead to increased drug concentrations and heightened side effects, including severe reactions such as serotonin syndrome. While Eszopiclone does not have a significant interaction with grapefruit juice, caution should still be exercised. If there are concerns about overdose or self-harm, it is essential to seek immediate medical help rather than attempting to induce vomiting at home. Always consult with a healthcare provider regarding medication interactions and the safest practices for managing medications.

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