ROLAPITANT

🔹Its a Neurokinin-1 receptor antagonist . NK-1 receptors are highly concentrated in the vomiting center of the brain and bind a neurokinin termed substance P; activation of NK-1 receptors by substance P plays a central role in eliciting chemotherapy-induced nausea and vomiting

Blocking the interaction of substance P at the NK-1 receptor, NK-1 receptor antagonists improve the management of nausea and vomiting

🔹Comes in Tablet form (90 mg)

🔹Indication: In combination with other antiemetic agents, to prevent nausea and vomiting associated with emetogenic cancer chemotherapy 

🔹Especially useful in preventing delayed phase chemotherapy induced nausea and vomiting

🔹Highly emetogenic chemotherapy

Day 1: Rolapitant 180 mg PO 1-2 hr before chemotherapy PLUS dexamethasone 20 mg PO 30 minutes before chemotherapy PLUS 5HT-3 antagonist

 

Days 2-4: Dexamethasone 8 mg PO BID

🔹Moderately emetogenic chemotherapy

Day 1: Rolapitant 180 mg PO 1-2 hr before chemotherapy PLUS dexamethasone 20 mg PO 30 minutes before chemotherapy PLUS 5HT-3 antagonist 

Days 2-4: 5HT-3 antagonist 

🔹Contraindicated with the use of thioridazine ( risk of arrhythmias due to increased thioridazine levels)

Safety not established for pediatric use and in pregnancy 

🔹SIDE EFFECTS 

Decreased appetite (9%), Neutropenia (7-9%)

Dizziness (6%)

🔹Rolapitant vs Aprepitant 

Rolapitant has been studied as a one-time dose on day 1 of chemotherapy, while aprepitant is recommended to be given on days 1 through 3. Rolapitant does not inhibit CYP 2C9 or 3A4 enzymes, whereas aprepitant induces CYP 2C9 and 3A4 and moderately inhibits 3A4.3,4 As a result, aprepitant can interfere with warfarin, hormonal contraceptives, and certain chemotherapy, among other drugs.

Ref: WHO DRUG INFORMATION, VOL 29, number 3, 2015

Medscape Reference , http://reference.medscape.com/drug/varubi-rolapitant