YOSPRALA

Yosprala Generic Name & Formulations

Legal Class

General Description

Aspirin delayed-rel, omeprazole immediate-rel; 81mg/40mg, 325mg/40mg; delayed-rel tabs.

Pharmacological Class

Antiplatelet + proton pump inhibitor.

How Supplied

Tabs—30, 90

Manufacturer

Genus Lifesciences, Inc.

Generic Availability

Mechanism of Action

Aspirin (acetylsalicylic acid) is an inhibitor of both prostaglandin synthesis and platelet aggregation. The differences in activity between aspirin and salicylic acid are thought to be due to the acetyl group on the aspirin molecule. This acetyl group is responsible for the inactivation of cyclo-oxygenase via acetylation. Omeprazole belongs to a class of antisecretory compounds, the substituted benzimidazoles, that suppress gastric acid secretion by specific inhibition of the [H+/K+]-ATPase enzyme system at the secretory surface of the gastric parietal cell. Because this enzyme system is regarded as the acid (proton) pump within the gastric mucosa, omeprazole has been characterized as a gastric acid-pump inhibitor, in that it blocks the final step of acid production. This effect is dose related and leads to inhibition of both basal and stimulated acid secretion irrespective of the stimulus.

Yosprala Indications

Indications

Patients who require aspirin for secondary prevention of cardiovascular and cerebrovascular events and who are at risk of developing aspirin associated gastric ulcers. For separate components: see full labeling.

Limitations of Use

Not for use as initial dose of aspirin therapy during onset of acute coronary syndrome, acute MI, or before PCI. Not shown to reduce risk of GI bleeding due to aspirin. Not interchangeable with individual aspirin and omeprazole.

Yosprala Dosage and Administration

Adult

Swallow whole. Take 1 tab daily at least 1hr before a meal. Use lowest effective dose for shortest duration. Usually aspirin 81mg is acceptable; can consider the need for 325mg and refer to current guidelines.

Children

Not established.

Yosprala Contraindications

Contraindications

NSAID allergy and syndrome of asthma, rhinitis, nasal polyps. Viral infections in pediatric patients. Concomitant rilpivirine-containing drugs (due to omeprazole component).

Yosprala Boxed Warnings

Not Applicable

Yosprala Warnings/Precautions

Warnings/Precautions

Coagulation abnormalities; monitor for increased bleeding. Increased risk of serious GI adverse events (including inflammation, bleeding, ulceration, perforation). Discontinue if significant bleeding from any source, acute tubulointerstitial nephritis, severe cutaneous adverse reactions, or cutaneous/systemic lupus erythematosus develops. Gastric malignancy. Increased risk of fundic gland polyps with long-term use (esp. >1yr) or osteoporosis-related fractures (hip, wrist or spine) with long-term (>1yr) and multiple daily dose PPI therapy. Long-term therapy (>3yrs) may lead to malabsorption/deficiency of Vit. B₁₂. Monitor for hypomagnesemia during prolonged therapy. Consider monitoring magnesium, calcium levels in those with preexisting risk of hypocalcemia (eg, hypoparathyroidism). Avoid abrupt cessation. Pre-existing renal disease. Hepatic impairment or severe renal impairment (GFR <10mL/min): not recommended. Asians with unknown CYP2C19 genotype or known to be poor metabolizers: not recommended. Elderly. Labor & delivery. Pregnancy (≥30 weeks gestation: avoid). Nursing mothers: not recommended.

Yosprala Pharmacokinetics

Distribution

Plasma protein bound: ~75–90% (aspirin); ~95% (omeprazole).

Metabolism

Hepatic.

Elimination

Renal. Half-life: 0.35 hours (aspirin), 1 hour (omeprazole).

Yosprala Interactions

Interactions

See Contraindications. Concomitant St. John's wort, rifampin, atazanavir, nelfinavir, voriconazole: not recommended. Concomitant heparin, warfarin: monitor and adjust dose as needed. Avoid concomitant clopidogrel; consider alternative antiplatelet therapy. Potentiates saquinavir, hypoglycemics, acetazolamide, valproic acid, citalopram (limit to max 20mg daily), cilostazol (reduce to 50mg twice daily). May potentiate phenytoin, diazepam, tacrolimus, digoxin, methotrexate (consider temporary withdrawal if on high-doses); monitor and adjust dose as needed. May antagonize ACE inhibitors, β-blockers, diuretics, uricosurics; monitor. Increased bleeding risk with NSAIDs or chronic, heavy alcohol use. NSAIDs increase risk of renal dysfunction. Caution with drugs that may cause hypomagnesemia (eg, digoxin, diuretics); monitor. May alter absorption of pH-dependent drugs (eg, iron salts, erlotinib, dasatinib, nilotinib, ketoconazole, itraconazole, mycophenolate mofetil). Monitor drugs metabolized by CYP450 (eg, cyclosporine, disulfiram). May interfere with lab tests; discontinue ≥14 days prior to CgA level assessment and secretin stimulation test. May cause false (+) THC urine test; use alternative confirmatory method. For the 325mg/40mg tab strength: avoid concomitant ticagrelor.

Yosprala Adverse Reactions

Adverse Reactions

Gastritis, nausea, diarrhea, gastric polyps, non-cardiac chest pain; ulcers (monitor), abnormal lab tests (eg, increased liver enzymes, BUN, creatinine, hyperkalemia, proteinuria, prolonged bleeding time); possible C. diff-associated diarrhea, reversible infertility; rare: hypomagnesemia and mineral metabolism.

Yosprala Clinical Trials

See Literature

Yosprala Note