Information about Rolapitant
Liver safety of Rolapitant
Rolapitant therapy has not been associated with serum enzyme elevations or with instances of clinically apparent liver injury with jaundice.
Mechanism of action of Rolapitant
Rolapitant (roe la' pi tant) is a substance P/neurokinin 1 (NK-1) receptor antagonist which has potent and prolonged antiemetic activity. Rolapitant acts as a substance P antagonist blocking the neurokinin 1 (NK1) receptor, which is found in the central nervous system and induces the vomiting reflex when activated by substance P. Rolapitant has been shown to inhibit both acute and delayed nausea and vomiting associated with cancer chemotherapy and surgical procedures, and appears to act synergistically with serotonin type 3 (5-HT3) receptor blockers. Because of its delayed half-life, rolapitant is particularly potent in preventing delayed (>24 hours after chemotherapy) nausea and vomiting.
FDA approval information for Rolapitant
Rolapitant was approved for use in the United States in 2015 and current indications are in combination with other antiemetic agents in adults for prevention of delayed chemotherapy associated nausea and vomiting.
Dosage and administration for Rolapitant
Rolapitant is available as tablets of 90 mg under the brand name Varubi.
Dosage and administration for Rolapitant
The typical adult oral dose is 90 mg on day one of each emetogenic chemotherapy cycle, generally in combination with a 5-HT3 receptor blocker and dexamethasone. It has been used off label to treat postoperative nausea and vomiting.
Side effects of Rolapitant
Side effects are uncommon, but can include anorexia, headache, neutropenia and dizziness.
Antidiarrheal agents include bulk forming agents, hydroscopic agents, bile acid resins, bismuth, inhibitors of intestinal motility, non-absorbed antibiotics and hormones. Bulk forming agents include methylcellulose; hydroscopic agents include pectin and kaolin; bile acid resins are cholestyramine, colestipol and colesevalam; inhibitors of intestinal motility include opioids such as diphenoxylate and loperamide. Antibiotics include rifamycin and rifaximin which are non-absorbed and are used for travelers' diarrhea. Hormones with antidiarrheal activity include octretide and somatostatin. Most antidiarrheal agents are active locally in the small intestine and colon and are largely not absorbed. Some, however, have been implicated in rare causes of liver injury (senna, cascara, cholestyramine). Telotristat is a relatively new agent that inhibits the synthesis of serotonin and is used specifically for the diarrhea of carcinoid syndrome.
Antiemetics are a diverse group of medications that act at different points in the pathways that regulate nausea and vomiting. These include antihistamines, anticholinergic agents, phenothiazines, serotonin type 3 receptor blockers, centrally acting benzamides, cannabinoid receptor agonists, substance P antagonists and miscellaneous.
Cannabinoid Receptor Agonists
- Dronabinol, Nabilone, Tetrahydrocannabinol
- Phenothiazines [See Antipsychotic Agents]
- Chlorpromazine, Prochlorperazine
Substance P/Neurokinin 1 Receptor Antagonists
Acid peptic disease/antiulcer agents that include antacids, the histamine type 2 receptor blockers (H2 blockers), and the proton pump inhibitors (PPIs). These agents are some of the most commonly taken medications and are very well tolerated, most being available both by prescription and over-the-counter. While many of these drugs are approved for use in duodenal and gastric ulcer disease, their major use is for acid reflux and indigestion.
Cathartics, laxatives or agents for constipation include bulk forming agents, osmotic agents, stool wetting agents, nonspecific stimulants, prokinetic agents and agents that increase fluid secretion. Many of these therapies are not systemically absorbed and none are considered particularly hepatotoxic. Naldemedine and naloxegol are opioid antagonists and are used to treat the constipation associated with opioid use.
- Cascara Sagrada
- Castor Oil
- Fiber, Bran
- Magnesium Sulfate
- Naldemedine (Opioid Antagonist)
- Naloxegol (Opioid Antagonist)
- Plecanatide (for Chronic Idiopathic Constipation)
- Prucalopride (for Chronic Idiopathic Constipation)
Inflammatory bowel disease encompasses several disorders, most commonly ulcerative colitis and Crohn colitis. Agents can be classified as 5-aminosalicyclic acid (5-ASA) based agents, immunosuppressive drugs, antitumor necrosis factor agents, corticosteroids, antibiotics and miscellaneous.
5-Aminosalicyclic Acid (5-ASA) Derivatives
Tumor Necrosis Factor Antagonists
Irritable Bowel Syndrome Agents Antimuscarinics/Antispasmodics [See Anticholinergic agents