Rolapitant is a medication specifically developed to help prevent nausea and vomiting. It is used in adults, often alongside other medicines, as part of a regimen to manage these challenging side effects.
Understanding Rolapitant
Rolapitant is classified as a neurokinin-1 (NK-1) receptor antagonist. This means it works by selectively blocking the action of specific natural substances in the body that trigger nausea and vomiting. One such substance is Substance P, which activates NK-1 receptors primarily found in the gut and central nervous system.
When chemotherapy is administered, Substance P can be released, leading to signals that cause nausea and vomiting. By binding to the NK-1 receptor, rolapitant prevents Substance P from attaching and initiating these signals. This blockade prevents both acute and delayed nausea and vomiting associated with chemotherapy. Rolapitant also has a long half-life of about seven days, which contributes to its sustained effect after a single dose.
Primary Use of Rolapitant
Rolapitant’s primary indication is for the prevention of delayed chemotherapy-induced nausea and vomiting (CINV) in adults. CINV is a common and distressing side effect of cancer treatment. CINV can be categorized into acute, occurring within 24 hours of chemotherapy, and delayed, which develops more than 24 hours after treatment. Delayed CINV is challenging to manage.
Rolapitant helps address this by targeting the NK-1 receptor pathway, involved in delayed CINV. It is used in combination with other antiemetic medications, such as corticosteroids (e.g., dexamethasone) and 5-HT3 receptor antagonists. This multi-drug approach provides broader protection against the various mechanisms that contribute to nausea and vomiting. Rolapitant is approved for use in patients receiving highly or moderately emetogenic chemotherapy, meaning regimens likely to cause nausea and vomiting.
How Rolapitant is Taken
Rolapitant is available in oral tablet and intravenous infusion forms. For the oral form, the dosage for adults is 180 milligrams, taken as two tablets about two hours before chemotherapy. It is administered as a single dose per chemotherapy cycle and should not be taken more frequently than once every 14 days.
The medication can be taken with or without food. Follow the prescribed dosing schedule carefully, as rolapitant is part of a multi-drug regimen to optimize CINV prevention. Your healthcare provider will determine the appropriate form and dosage based on your specific chemotherapy regimen and overall health.
Potential Side Effects and Important Considerations
As with any medication, rolapitant can cause side effects. Common side effects include decreased appetite, dizziness, dyspepsia (indigestion), neutropenia, constipation, headache, hiccups, and mouth sores. These are mild and temporary.
Important considerations involve potential drug interactions. Rolapitant is a moderate inhibitor of the CYP2D6 enzyme, which metabolizes many other medications. This inhibitory effect can persist for over 28 days. Therefore, it is important to discuss all medications with your doctor to avoid potential interactions, especially with drugs that are substrates of CYP2D6, such as dextromethorphan.
While rare with rolapitant alone, there is a theoretical risk of prolonged QT interval, especially when used with other medications that can also affect heart rhythm. Rolapitant is also an inhibitor of Breast-Cancer-Resistance Protein (BCRP) and p-glycoprotein (P-gp). Contraindications include hypersensitivity to rolapitant. Patients with liver impairment, or those who are pregnant or breastfeeding, should consult their healthcare professional to discuss the potential benefits and risks before using this medication.