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Drug interactions occur when the pharmacological effect of one drug is altered by another substance, either enhancing or diminishing its activity. The drug whose activity is altered is known as the object drug, and the substance causing the alteration is called the agent drug or the precipitant. The net effects of these interactions are mostly undesirable, leading to decreased effectiveness or increased adverse effects. In rare cases, interactions can be beneficial, such as the enhanced...
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A drug interaction occurs when the concurrent use of another drug, food, or an external substance alters the pharmacological activity of a drug. This interaction can modify the action of the original drug, affecting its effectiveness and safety.Drug–food interactions are significant as they impact drug absorption, metabolism, and excretion. For example, grapefruit juice is a well-known disruptor of drug metabolism. It inhibits the cytochrome P450 3A4 enzyme, crucial for the metabolism of...
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Drug–drug interactions can precipitate toxicity through multiple mechanisms. Absorption interactions alter how drugs enter the body, exemplified when ranitidine increases the absorption of basic drugs, while cholestyramine decreases the levels of propranolol. Protein binding interactions occur when drugs share the same binding sites on plasma proteins. Drugs like aspirin and warfarin, when bound in excess, can lead to increased free drug concentrations, enhancing the potential for...
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Cyclosporine and herbal supplement interactions.

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Many herbal extracts can alter cyclosporine (CyA) blood levels, potentially impacting its effectiveness. Patients should inform clinicians about all herbal supplement use to avoid dangerous drug interactions.

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Area of Science:

  • Pharmacology
  • Natural Products Chemistry

Background:

  • Cyclosporine (CyA) is a critical immunosuppressant with a narrow therapeutic index.
  • Its bioavailability is significantly influenced by interactions with other drugs and herbal remedies.
  • Cytochrome P-450 (CYP3A4/5) and P-glycoprotein (P-gp) are key regulators of CyA metabolism and transport.

Purpose of the Study:

  • To review known and potential interactions between commonly used herbal extracts and Cyclosporine (CyA).
  • To highlight the clinical significance of these interactions due to the widespread use of herbal supplements.
  • To inform healthcare providers and patients about the risks associated with concomitant use.

Main Methods:

  • Literature review of case reports, in vivo animal studies, and clinical observations.
  • Analysis of documented effects of various herbal extracts on CyA blood concentrations.
  • Identification of herbal products that decrease or increase CyA levels.

Main Results:

  • Herbal extracts like St. John's Wort, ginger, liquorice, scutellariae radix, and quercetin have been associated with decreased CyA concentrations.
  • Grapefruit juice, chamomile, berberine, cannabidiol, and resveratrol have been linked to increased CyA concentrations.
  • Effects of Echinacea and Serenoa repens are inconsistent, but caution is advised.

Conclusions:

  • Concomitant use of certain herbal extracts with CyA can lead to significant alterations in blood concentrations.
  • Avoiding co-administration is prudent, especially given the limited human clinical data for many herbs.
  • Clinicians must proactively inquire about and counsel patients regarding herbal supplement use before and during CyA therapy.