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Related Concept Videos

Pharmacokinetics: Drug–Drug Interactions01:25

Pharmacokinetics: Drug–Drug Interactions

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...
Combined Effects of Drugs: Antagonism01:30

Combined Effects of Drugs: Antagonism

The combined effects of drugs can result in various interactions, of which an important type is antagonism. Antagonism is a mechanism where one drug inhibits or counteracts the effects of another drug. Antagonism can occur through various means, including receptor binding, allosteric modulation, functional interaction, chemical reactions, and pharmacokinetic processes.
The most common type is receptor antagonism, where one drug acts as an antagonist to block the effects of another drug by...
Drug toxicity: Drug–Drug Interaction01:30

Drug toxicity: Drug–Drug Interaction

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...
Agonism and Antagonism: Quantification01:14

Agonism and Antagonism: Quantification

When drugs are administered, they can elicit either an agonist or antagonist effect on the body. Agonism occurs when a drug activates a specific receptor, triggering a biological response. On the other hand, antagonism happens when a drug binds to the same receptors but blocks their activation, thereby preventing a biological response.
To quantify these effects, researchers use a dose-response curve, which provides valuable information about the potency and efficacy of a drug. Potency refers to...
Drug-Receptor Interactions01:29

Drug-Receptor Interactions

Drug-receptor interaction describes the binding of receptors by drugs, but not all drug-receptor interactions result in activation and tissue response. For instance, the binding of agonists activates the receptor to generate a cellular reaction, while antagonists bind to receptors without causing their activation.
Several parameters, such as the drug's affinity for its receptor and its efficacy, which is its ability to activate the receptor, determine the drug's effect on the tissue.
Drug-Receptor Interaction: Antagonist01:28

Drug-Receptor Interaction: Antagonist

An antagonist is a drug that binds strongly to a receptor without activating it. An antagonist prevents other molecules, such as neurotransmitters or hormones, from binding to the receptor and triggering a cellular response. Such interaction effectively hinders the normal physiological processes mediated by the receptor, resulting in various pharmacological effects depending on the specific receptor targeted.
Antagonists can be classified as competitive or noncompetitive based on their...

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Drug Repurposing Hypothesis Generation Using the "RE:fine Drugs" System
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Aprepitant: drug-drug interactions in perspective.

M S Aapro1, C M Walko2

  • 1Institut Multidisciplinaire d'Oncologie, Clinique de Genolier, Genolier, Switzerland.

Annals of Oncology : Official Journal of the European Society for Medical Oncology
|May 22, 2010
PubMed
Summary

Aprepitant, an antiemetic, has potential drug-drug interactions with chemotherapy agents. However, studies show no clinically significant interactions, with management strategies available for rare cases.

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Area of Science:

  • Oncology
  • Pharmacology
  • Drug Interactions

Background:

  • Chemotherapy-induced nausea and vomiting (CINV) significantly impacts patient quality of life.
  • Aprepitant is a neurokinin-1 receptor antagonist used to prevent CINV.
  • Concerns exist regarding aprepitant's potential drug-drug interactions due to its inhibition of cytochrome P-450 3A4 (CYP3A4).

Purpose of the Study:

  • To evaluate the clinical relevance of aprepitant's drug-drug interactions with commonly used chemotherapeutic agents and antiemetics.
  • To assess the safety and efficacy of aprepitant in the context of potential interactions.

Main Methods:

  • Review of existing literature and clinical data on aprepitant and its interactions.
  • Analysis of interaction profiles with specific chemotherapeutic agents (e.g., cyclophosphamide, docetaxel, vinorelbine) and 5-HT3 antagonists (e.g., granisetron, ondansetron, palonosetron).

Main Results:

  • No clinically relevant interactions were observed between aprepitant and the evaluated chemotherapeutic agents or 5-HT3 antagonists.
  • Potential interactions with certain drugs, like warfarin, require monitoring, and corticosteroid doses may need adjustment.
  • The concern regarding negative interactions with CYP3A4-metabolized agents is largely theoretical.

Conclusions:

  • Aprepitant can be safely used for CINV prevention with minimal clinically significant drug-drug interactions.
  • Management strategies exist for identified interactions, ensuring patient safety.
  • Further investigation is needed for new agents extensively metabolized by CYP3A4.