Effects of Rolapitant Administered Intravenously or Orally on the Pharmacokinetics of Digoxin (P-glycoprotein Substrate) and Sulfasalazine (Breast Cancer Resistance Protein Substrate) in Healthy Volunteers.

Author: AroraSujata, ChristensenJennifer, HughesLorraine, KansraVikram, LuSharon, PowersDaniel, WangJing, WangXiaodong, ZhangZhi-Yi

Paper Details 
Original Abstract of the Article :
Rolapitant is a selective and long-acting neurokinin-1 receptor antagonist approved in an oral formulation in combination with other antiemetic agents for the prevention of delayed chemotherapy-induced nausea and vomiting in adults. Four open-label phase 1 studies evaluated the safety and drug-drug ...See full text at original site
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引用元:
https://doi.org/10.1002/jcph.1005

データ提供:米国国立医学図書館(NLM)

Effects of Rolapitant on the Pharmacokinetics of Digoxin and Sulfasalazine

The world of drug interactions is a complex desert landscape, where the effects of different medications can intertwine in unexpected ways. This study, like a skilled explorer, investigates the potential interactions between rolapitant, an anti-nausea medication, and two other drugs, digoxin and sulfasalazine. The researchers found that rolapitant, when administered intravenously, had no significant effect on the pharmacokinetics of either digoxin or sulfasalazine. However, oral administration of rolapitant led to increased plasma concentrations of both digoxin and sulfasalazine, suggesting a potential for drug interactions.

Oral Rolapitant's Impact on Digoxin and Sulfasalazine: A Desert of Drug Interactions

The study revealed that oral rolapitant, when co-administered with digoxin, significantly increased the peak concentration and area under the curve for digoxin in the bloodstream. Similar findings were observed for sulfasalazine, highlighting a potential for drug interactions when oral rolapitant is used in combination with these medications. This discovery is like encountering a hidden oasis in the desert, offering insights into the complex interplay of medications.

Navigating the Desert of Drug Interactions: Cautious Co-administration

The researchers concluded that while rolapitant is generally safe and well tolerated, caution should be exercised when co-administering it with drugs that are substrates for the P-glycoprotein (P-gp) and breast cancer resistance protein (BCRP) transporters. This is because increased plasma concentrations of these substrates could lead to adverse effects. This finding is like finding a treacherous sandstorm in the desert, requiring careful navigation and awareness of potential dangers.

Dr. Camel's Conclusion

This research, like a wise desert guide, reminds us of the importance of careful consideration when combining medications. While rolapitant is a valuable treatment for chemotherapy-induced nausea and vomiting, it's crucial to be aware of its potential interactions with other drugs. This study highlights the need for close monitoring of patients who are taking oral rolapitant with P-gp and BCRP substrates, ensuring their safety and well-being.
Date :
  1. Date Completed 2019-01-15
  2. Date Revised 2019-12-10
Further Info :

Pubmed ID

28906558

DOI: Digital Object Identifier

10.1002/jcph.1005

Related Literature

SNS
PICO Info
in preparation
Languages

English

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