The FDA has approved Yosprala (aspirin and omeprazole, Aralez Pharmaceuticals) delayed-release tablets for patients requiring aspirin for secondary prevention of cardiovascular and cerebrovascular events and who are at risk of developing aspirin-associated gastric ulcers.
The FDA has approved Yosprala (aspirin and omeprazole, Aralez Pharmaceuticals) delayed-release tablets for patients requiring aspirin for secondary prevention of cardiovascular and cerebrovascular events and who are at risk of developing aspirin-associated gastric ulcers. The approval carries the limitation that it should not be used as the initial dose of aspirin therapy during the onset of acute coronary syndrome, during acute myocardial infarction, or before percutaneous coronary intervention. The limitation also states that Yosprala has not been shown to reduce the risk of gastrointestinal (GI) bleeding due to aspirin and that the medication is not interchangeable with the individual components of aspirin and omeprazole.1
PHARMACOLOGY AND PHARMACOKINETICS
Aspirin is an antiplatelet agent and omeprazole is a proton pump inhibitor (PPI).1 Utilizing the Intelli-COAT system, Yosprala first delivers imme- diate-release omeprazole to raise the gastric pH to a gastroprotective zone. The next layer is a delayed-release enteric-coated aspirin core that dissolves at a gastric pH greater than or equal to 5.5.2 Omeprazole is extensively metabolized by the cytochrome (CYP) P450 enzyme system. It inhibits CYP2C19 and can increase the systemic exposure of concurrently administered CYP2C19 substrates.1
DOSAGE AND ADMINISTRATION
Yosprala is available as 81-mg delayed-release aspirin/40-mg immediate-release omeprazole and 325-mg delayed-release aspirin/40-mg immediate-release omeprazole. It should be taken daily as 1 tablet, at least 60 minutes before a meal, and swallowed whole with liquid. Never split, chew, crush, or dissolve Yosprala.1
Yosprala was evaluated in 2 randomized double-blind clinical trials. Patients received either Yosprala 325 mg/40 mg or enteric-coated aspirin 325 mg. In each study, patients in the Yosprala arm demonstrated a significant reduction in the 6-month cumulative incidence of gastric ulcers compared with patients taking 325 mg of enteric-coated aspirin alone. Additionally, significantly fewer patients in the Yosprala arm stopped treatment due to prespecified upper-GI adverse events compared with patients in the enteric-coated aspirin arm.1,2
CONTRAINDICATIONS, WARNINGS, AND PRECAUTIONS
Yosprala is contraindicated in patients with a history of asthma, urticaria, or other allergic-type reactions after taking aspirin or nonsteroidal anti-inflammatory drugs (NSAIDs); pediatric patients with suspected viral infections; patients with a known hypersensitivity to aspirin, omeprazole, substituted benzimidazoles, or any excipient of Yosprala; or patients receiving rilpivirine-containing products.
It should be used cautiously in patients with coagulation abnormalities and GI adverse reactions. Its use should be avoided in patients with severe renal failure or hepatic impairment. Patients consuming 3 or more alcoholic drinks per day should not use Yosprala. PPI use has been associated with acute interstitial nephritis, Clostridium difficile—associated diarrhea, bone fractures, cutaneous lupus erythematosus and systemic lupus erythematosus, hypomagnesemia, and vitamin B12 deficiency. Patients with gastric symptoms during or after treatment with Yosprala should be considered for evaluation of gastric malignancy.
Yosprala may interact with diagnostic investigations for neuroendocrine tumors and should not be used in combination with clopidogrel, St. John’s wort, rifampin, or high-dose methotrexate. The higher dose of Yosprala, 325 mg/40 mg, should not be used concurrently with ticagrelor. And because NSAIDs are associated with reversible infertility, women who have difficulties conceiving should consider discontinuation of therapy. In addition, Yosprala should not be used during pregnancy after 30 weeks of gestation, as NSAIDs may cause premature closure of the fetal ductus arteriosus, or during breastfeeding.
The most common adverse reactions (≥2% incidence) are gastritis, nausea, diarrhea, gastric polyps, and noncardiac chest pain.1
Dr Holmberg earned her PharmD from the University of Connecticut and completed an ambulatory care residency at the Phoenix VA Healthcare System. Her practice has also included pediatrics and inpatient mental health. She resides in Phoenix, Arizona.
1. Yosprala [prescribing information]. Princeton, NJ: Aralez Pharmaceuticals US Inc; 2017. yospralahcp.com/files/Yosprala_Prescribing_Information.pdf. Accessed March 6, 2017.
2. Aralez announces FDA approval of Yosprala for secondary prevention of cardiovascular and cerebrovascular events in patients at risk for aspirin-associated gastric ulcers [news release]. Mississauga, Ontario, Canada; Aralez Pharmaceuticals; September 15, 2016. http://ir.aralez.com/phoenix.zhtml?c=254163&p=irol-newsArticle&ID=2202150. Accessed March 6, 2017.