ESOMEPRAZOLE Drug Interactions: What You Need to Know
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Drug Interactions (FDA Label)
INTERACTIONS See Table 3 and Table 4 for clinically significant drug interactions and interactions with diagnostics with naproxen and esomeprazole magnesium.
Table
3: Clinically Significant Drug Interactions with Naproxen and Esomeprazole Magnesium – Affecting Drugs Co-Administered with N aproxen and Esomeprazole Magnesium Delayed-Release Tablets and Interactions with Diagnostics Drugs That Interfere with Hemostasis Clinical Impact : Naproxen
- Naproxen and anticoagulants such as warfarin have a synergistic effect on bleeding. The concomitant use of naproxen and anticoagulants have increased the risk of serious bleeding compared to the use of either drug alone.
- Serotonin release by platelets plays an important role in hemostasis. Case-control and cohort epidemiological studies showed that concomitant use of drugs that interfere with serotonin reuptake and an NSAID may potentiate the risk of bleeding more than an NSAID alone.
Esomeprazole
Magnesium
- Increased INR and prothrombin time in patients treated with PPIs, including esomeprazole, and warfarin concomitantly. Increases in INR and prothrombin time may lead to abnormal bleeding and even death.
- Concomitant use of esomeprazole 40 mg resulted in reduced plasma concentrations of the active metabolite of clopidogrel and a reduction in platelet inhibition [see Clinical Pharmacology (12.3) ].
- There are no adequate combination studies of a lower dose of esomeprazole or a higher dose of clopidogrel in comparison with the approved dose of clopidogrel. Intervention: Monitor patients with concomitant use of naproxen and esomeprazole magnesium delayed-release tablets with anticoagulants (e.g., warfarin), antiplatelet agents (e.g., aspirin), selective serotonin reuptake inhibitors (SSRIs), and serotonin norepinephrine reuptake inhibitors (SNRIs) for signs of bleeding [see Warnings and Precautions ( 5.14 ) ]. Clopidogrel : Avoid concomitant use of clopidogrel with naproxen and esomeprazole magnesium delayed-release tablets. Consider use of alternative anti-platelet therapy [see Warnings and Precautions ( 5.22 ) ].
Aspirin Clinical
Impact: A pharmacodynamics (PD) study has demonstrated an interaction in which lower dose naproxen (220mg/day or 220mg twice daily) interfered with the antiplatelet effect of low-dose immediate-release aspirin, with the interaction most marked during the washout period of naproxen [see Clinical Pharmacology (12.2) ]. There is reason to expect that the interaction would be present with prescription doses of naproxen or with enteric-coated low-dose aspirin; however, the peak interference with aspirin function may be later than observed in the PD study due to the longer washout period. Controlled clinical studies showed that the concomitant use of NSAIDs and analgesic doses of aspirin does not produce any greater therapeutic effect than the use of NSAIDs alone. In a clinical study, the concomitant use of an NSAID and aspirin was associated with a significantly increased incidence of GI adverse reactions as compared to use of the NSAID alone [see Warnings and Precautions (5.2) ]. Intervention : Because there may be an increased risk of cardiovascular events following discontinuation of naproxen due to the interference with the antiplatelet effect of aspirin during the washout period, for patients taking low-dose aspirin for cardioprotection who require intermittent analgesics, consider use of an NSAID that does not interfere with the antiplatelet effect of aspirin, or non-NSAID analgesics where appropriate. Concomitant use of naproxen and esomeprazole magnesium delayed-release tablets and analgesic doses of aspirin is not generally recommended because of the increased risk of bleeding [see Warnings and Precautions ( 5.12 ) ]. Naproxen and esomeprazole magnesium delayed-release tablets are not a substitute for low dose aspirin for cardiovascular protection.
Ace
Inhibitors, Angiotensin Receptor Blockers, and Beta-Blockers Clinical Impact :
- NSAIDs may diminish the antihypertensive effect of angiotensin converting enzyme (ACE) inhibitors, angiotensin receptor blockers (ARBs), or beta-blockers (including propranolol).
- In patients who are elderly, volume-depleted (including those on diuretic therapy), or have renal impairment, co-administration of an NSAID with ACE inhibitors or ARBs may result in deterioration of renal function, including possible acute renal failure. These effects are usually reversible. Intervention :
- During concomitant use of naproxen and esomeprazole magnesium delayed-release tablets and ACE-inhibitors, ARBs, or beta-blockers, monitor blood pressure to ensure that the desired blood pressure is obtained.
- During concomitant use of naproxen and esomeprazole magnesium delayed-release tablets and ACE-inhibitors or ARBs in patients who are elderly, volume-depleted or have impaired renal function, monitor for signs of worsening renal function [see Warnings and Precautions (5.6) ].
Diuretics Clinical
Impact : Clinical studies, as well as post-marketing observations, showed that NSAIDs reduced the natriuretic effect of loop diuretics (e.g., furosemide) and thiazide diuretics in some patients. This effect has been attributed to the NSAID inhibition of renal prostaglandin synthesis. Intervention : During concomitant use of naproxen and esomeprazole magnesium delayed-release tablets with diuretics, observe patients for signs of worsening renal function, in addition to assuring diuretic efficacy including antihypertensive effects [see Warnings and Precautions (5.6) ].
Antiretrovirals Clinical
Impact : The effect of esomeprazole magnesium on antiretroviral drugs is variable. The clinical importance and mechanisms behind these interactions are not always known.
- Decreased exposure of some antiretroviral drugs (e.g., rilpivirine, atazanavir, and nelfinavir) when used concomitantly with esomeprazole magnesium may reduce antiviral effect and promote the development of drug resistance [see Clinical Pharmacology (12.3) ].
- Increased exposure of other antiretroviral drugs (e.g., saquinavir) when used concomitantly with esomeprazole magnesium may increase toxicity [see Clinical Pharmacology (12.3) ].
- There are other antiretroviral drugs which do not result in clinically relevant interactions with esomeprazole magnesium. Intervention : Rilpivirine-containing products : Concomitant use with naproxen and esomeprazole magnesium delayed-release tablets is contraindicated [see Contraindications ( 4 )]. Atazanavir : See prescribing information for atazanavir for dosing information. Nelfinavir : Avoid concomitant use with naproxen and esomeprazole magnesium delayed-release tablets. Saquinavir : See the prescribing information for saquinavir for monitoring of potential saquinavir-related toxicities. Other antiretrovirals : See prescribing information of specific drugs.
Cilostazol Clinical
Impact : Increased exposure of cilostazol and one of its active metabolites (3,4-dihydro-cilostazol) when coadministered with omeprazole magnesium, the racemate of esomeprazole [see Clinical Pharmacology (12.3) ]. Intervention: Consider reducing the dose of cilostazol to 50 mg twice daily.
Digoxin Clinical
Impact : Naproxen
- The concomitant use of naproxen with digoxin has been reported to increase the serum concentration and prolong the half-life of digoxin. Esomeprazol e Magnesium
- Potential for increased exposure of digoxin [see Clinical Pharmacology (12.3) ]. Intervention : Monitor digoxin concentrations during concomitant use of naproxen and esomeprazole magnesium delayed-release tablets. Dose adjustment of digoxin may be needed to maintain therapeutic drug concentrations.
Lithium Clinical
Impact : NSAIDs have produced elevations of plasma lithium levels and reductions in renal lithium clearance. The mean minimum lithium concentration increased 15%, and the renal clearance decreased by approximately 20%. This effect has been attributed to NSAID inhibition of renal prostaglandin synthesis. Intervention : During concomitant use of naproxen and esomeprazole magnesium delayed-release tablets and lithium, monitor patients for signs of lithium toxicity.
Methotrexate Clinical
Impact : Naproxen
- Concomitant use of NSAIDs and methotrexate may increase the risk for methotrexate toxicity (e.g., neutropenia, thrombocytopenia, renal dysfunction).
Esomeprazole
Magnesium
- Concomitant use of esomeprazole magnesium with methotrexate (primarily at high dose) may elevate and prolong serum concentrations of methotrexate and/or its metabolite hydroxymethotrexate, possibly leading to methotrexate toxicities [see Warnings and Precautions ( 5.27 ) ]. Intervention: During concomitant use of naproxen and esomeprazole magnesium delayed-release tablets and methotrexate, monitor patients for methotrexate toxicity. A temporary withdrawal of naproxen and esomeprazole magnesium delayed-release tablets may be considered in some patients receiving high-dose methotrexate.
Cyclosporine Clinical
Impact : Concomitant use of naproxen and cyclosporine may increase cyclosporine’s nephrotoxicity. Intervention: During concomitant use of naproxen and esomeprazole magnesium delayed-release tablets and cyclosporine, monitor patients for signs of worsening renal function.
Tacrolimus Clinical
Impact : Concomitant use of esomeprazole magnesium and tacrolimus may increase exposure of tacrolimus Intervention : During concomitant use of naproxen and esomeprazole magnesium delayed-release tablets and tacrolimus, monitor tacrolimus whole blood concentrations. NSAIDs and Salicylates Clinical Impact : Concomitant use of naproxen with other NSAIDs or salicylates (e.g., diflunisal, salsalate) increases the risk of GI toxicity, with little or no increase in efficacy [see Warnings and Precautions (5.2) ]. Intervention: The concomitant use of naproxen and esomeprazole magnesium delayed-release tablets with other NSAIDs or salicylates is not recommended.
Pemetrexed Clinical
Impact : Concomitant use of naproxen and esomeprazole magnesium delayed-release tablets and pemetrexed may increase the risk of pemetrexed-associated myelosuppression, renal, and GI toxicity (see the pemetrexed prescribing information). Intervention: During concomitant use of naproxen and esomeprazole magnesium delayed-release tablets and pemetrexed, in patients with renal impairment whose creatinine clearance ranges from 45 to 79 mL/min, monitor for myelosuppression, renal and GI toxicity.
Drugs
Dependent on Gastric pH for Absorption (e.g., iron salts, erlotinib, mycophenoloate mofetil, ketoconazole)
Clinical
Impact: Esomeprazole magnesium can reduce the absorption of other drugs due to its effect on reducing intragastric acidity Intervention: Mycophenolate mofetil (MMF): Co-administration of omeprazole, of which esomeprazole magnesium is an enantiomer, in healthy subjects and in transplant patients receiving MMF has been reported to reduce the exposure to the active metabolite, mycophenolic acid (MPA), possibly due to a decrease in MMF solubility at an increased gastric pH. The clinical relevance of reduced MPA exposure on organ rejection has not been established in transplant patients receiving esomeprazole and MMF. Use naproxen and esomeprazole magnesium delayed-release tablets with caution in transplant patients receiving MMF [see Clinical Pharmacology (12.3) ]. See the prescribing information for other drugs dependent on gastric pH for absorption. Interactions with Investigations of Neuroendocrine Tumors Clinical Impact : Serum chromogranin A (CgA) levels increase secondary to PPI-induced decreases in gastric acidity. The increased CgA levels may cause false positive results in diagnostic investigations for neuroendocrine tumors [see Warnings and Precautions ( 5.26 ) , Clinical Pharmacology (12.2) ]. Intervention : Temporarily stop naproxen and esomeprazole magnesium delayed-release tablets treatment at least 14 days before assessing CgA levels and consider repeating the test if initial CgA levels are high. If serial tests are performed (e.g. for monitoring), the same commercial laboratory should be used for testing, as reference ranges between tests may vary.
Diazepam Clinical
Impact: Increased exposure of diazepam [see Clinical Pharmacology (12.3) ]. Intervention: Monitor patients for increased sedation and adjust the dose of diazepam as needed.
Table
4: Clinically Significant Interactions with Esomeprazole Magnesium - Affecting Co-Administered Drugs CYP2C19 or CYP3A4 Inducers Clinical Impact : Decreased exposure of esomeprazole when used concomitantly with strong inducers [see Clinical Pharmacology (12.3) ]. Intervention: St. John’s Wort, rifampin : Avoid concomitant use with naproxen and esomeprazole magnesium delayed-release tablets [see Warnings and Precautions ( 5.25 ) ]. CYP2C19 or CYP3A4 Inhibitors Clinical Impact : Increased exposure of esomeprazole [see Clinical Pharmacology (12.3) ]. Intervention : Voriconazole : Avoid concomitant use with naproxen and esomeprazole magnesium delayed-release tablets. See full prescribing information for a list of clinically important drug interactions. ( 7 )
Contraindications
Naproxen and esomeprazole magnesium delayed-release tablets are contraindicated in the following patients:
- Known hypersensitivity (e.g., anaphylactic reactions and serious skin reactions) to naproxen, esomeprazole magnesium, substituted benzimidazoles, or to any components of the drug product, including omeprazole. Hypersensitivity reactions to esomeprazole may include anaphylaxis, anaphylactic shock, angioedema, bronchospasm, acute tubulointerstitial nephritis, and urticaria [see Warnings and Precautions ( 5.7 , 5.8 , 5.9 , 5.18 ), Adverse Reactions ( 6.2 )].
- History of asthma, urticaria, or allergic-type reactions after taking aspirin or other NSAIDs. Severe, sometimes fatal, anaphylactic reactions to NSAIDs have been reported in such patients [see Warnings and Precautions ( 5.7 , 5.8 ) ].
- In the setting of coronary artery bypass graft (CABG) surgery [see Warnings and Precautions (5.1) ].
- Proton pump inhibitors (PPIs), including esomeprazole magnesium, are contraindicated in patients receiving rilpivirine-containing products [see Drug Interactions ( 7 ) ].
- Known hypersensitivity to naproxen, esomeprazole magnesium, substituted benzimidazoles, or to any components of the drug product including omeprazole. (4 )
- History of asthma, urticaria, or other allergic-type reactions after taking aspirin or other NSAIDs. ( 4 )
- In the setting of coronary artery bypass graft (CABG) surgery. ( 4 )
- In patients receiving rilpivirine-containing products. ( 4 , 7 )
Related Warnings
AND PRECAUTIONS Hepatotoxicity: Inform patients of warning signs and symptoms of hepatotoxicity. Discontinue if abnormal liver tests persist or worsen or if clinical signs and symptoms of liver disease develop. ( 5.3 ) Hypertension: Patients taking some antihypertensive medications may have impaired response to these therapies when taking NSAIDs. Monitor blood pressure. ( 5.4 , 7 )
Heart
Failure and Edema: Avoid use of naproxen and esomeprazole magnesium delayed-release tablets in patients with severe heart failure unless benefits are expected to outweigh risk of worsening heart failure. ( 5.5 )
Renal
Toxicity: Monitor renal function in patients with renal or hepatic impairment, heart failure, dehydration, or hypovolemia. Avoid use of naproxen and esomeprazole magnesium delayed-release tablets in patients with advanced renal disease unless benefits are expected to outweigh risk of worsening renal function. ( 5.6 )
Anaphylactic
Reactions: Seek emergency help if an anaphylactic reaction occurs. ( 5.7 ) Exacerbation of Asthma Related to Aspirin Sensitivity: Naproxen and esomeprazole magnesium delayed-release tablets are contraindicated in patients with aspirin-sensitive asthma. Monitor patients with preexisting asthma (without aspirin sensitivity). ( 5.8 ) Serious or Severe Skin Reactions: Discontinue naproxen and esomeprazole magnesium delayed-release tablets at first appearance of skin rash or other signs of hypersensitivity and consider further evaluation. ( 5.9 )
Drug
Reaction with Eosinophilia and Systemic Symptoms (DRESS) : Discontinue and evaluate clinically ( 5.10 )
Fetal
Toxicity : Limit use of NSAIDs, including naproxen and esomeprazole magnesium delayed-release tablets, between about 20 weeks to 30 weeks in pregnancy due to the risk of oligohydramnios/fetal renal dysfunction. Avoid use of NSAIDs in women at about 30 weeks gestation and later in pregnancy due to the risks of oligohydramnios/fetal renal dysfunction and premature closure of the fetal ductus arteriosus ( 5.11 , 8.1 )
Hematologic
Toxicity: Monitor hemoglobin or hematocrit in patients with any signs of symptoms of anemia. ( 5.12 , 7 ) Masking of Inflammation and Fever: Potential for diminished utility of diagnostic signs in detecting infections. ( 5.13 )
Laboratory
Monitoring: Obtain CBC and chemistry profile periodically during treatment. Monitor hemoglobin periodically in patients on long-term treatment who have an initial value of 10 g or less. ( 5.14 )
Active
Bleeding: Withdraw treatment in patients who experience active and clinically significant bleeding. ( 5.15 ) Concomitant NSAID Use: Do not use naproxen and esomeprazole magnesium delayed-release tablets with other naproxen-containing products or other non-aspirin NSAIDs. ( 5.16 )
Gastric
Malignancy: In adults, symptomatic response to esomeprazole does not preclude the presence of gastric malignancy. Consider additional follow-up and diagnostic testing. ( 5.17 )
Acute Tubulointerstitial
Nephritis : Discontinue treatment and evaluate patients. ( 5.18 ) Clostridium difficile -Associated Diarrhea: PPI therapy may be associated with increased risk of Clostridium difficile associated diarrhea. ( 5.19 )
Bone
Fracture: Long-term and multiple daily dose PPI therapy may be associated with an increased risk for osteoporosis-related fractures of the hip, wrist or spine. ( 5.20 ) Cutaneous and Systemic Lupus Erythematosus: Mostly cutaneous, new onset or exacerbation of existing disease; discontinue naproxen and esomeprazole magnesium delayed-release tablets and refer to specialist for evaluation. ( 5.21 ) Interaction with Clopidogrel: Avoid concomitant use. ( 5.22 , 7 ) Cyanocobalamin (Vitamin B-12) Deficiency: Daily long-term use (e.g., longer than 3 years) may lead to malabsorption or a deficiency of cyanocobalamin. ( 5.23 ) Hypomagnesemia and Mineral Metabolism: Reported rarely with prolonged treatment with PPIs. ( 5.24 ) Interaction with St. John’s Wort or Rifampin: Avoid concomitant use. ( 5.25 , 7 ) Interactions with Diagnostic Investigations for Neuroendocrine Tumors: Increases in intragastric pH may result in hypergastrinemia, enterochromaffin-like cell hyperplasia, and increased Chromogranin A levels which may interfere with diagnostic investigations for neuroendocrine tumors. ( 5.26 ) Interaction with Methotrexate: Concomitant use with PPIs may elevate and/or prolong serum concentrations of methotrexate and/or its metabolite, possibly leading to toxicity. ( 5.27 , 7 )
Fundic Gland
Polyps: Risk increases with long-term PPI use, especially beyond one year. Use the shortest duration of therapy. ( 5.28 )
5.1 Cardiovascular Thrombotic Events Clinical trials of several COX-2 selective and nonselective NSAIDs of up to three years duration have shown an increased risk of serious cardiovascular (CV) thrombotic events, including myocardial infarction (MI), and stroke, which can be fatal. Based on available data, it is unclear that the risk for CV thrombotic events is similar for all NSAIDS. The relative increase in serious CV thrombotic events over baseline conferred by NSAID use appears to be similar in those with and without known CV disease or risk factors for CV disease. However, patients with known CV disease or risk factors had a higher absolute incidence of excess serious CV thrombotic events, due to their increased baseline rate. Some observational studies found that this increased risk of serious CV thrombotic events began as early as the first weeks of treatment. The increase in CV thrombotic risk has been observed most consistently at higher doses. To minimize the potential risk for an adverse CV event in NSAID-treated patients, use the lowest effective dose for the shortest duration possible. Physicians and patients should remain alert for the development of such events, throughout the entire treatment course, even in the absence of previous CV symptoms. Patients should be informed about the symptoms of serious CV events and the steps to take if they occur. There is no consistent evidence that concurrent use of aspirin mitigates the increased risk of serious CV thrombotic events associated with NSAID use. The concurrent use of aspirin and an NSAID, such as naproxen, increases the risk of serious gastrointestinal (GI) events <span class="opacity-50 text-xs">[see Warnings and Precautions ( 5.2 )]</span>.
Status Post Coronary Artery Bypass
Graft (CABG)
Surgery
Two large, controlled, clinical trials of a COX-2 selective NSAID for the treatment of pain in the first 10 days to 14 days following CABG surgery found an increased incidence of myocardial infarction and stroke. NSAIDs are contraindicated in the setting of CABG [see Contraindications ( 4 )]. Post-MI Patients Observational studies conducted in the Danish National Registry have demonstrated that patients treated with NSAIDs in the post-MI period were at increased risk of reinfarction, CV-related death, and all-cause mortality beginning in the first week of treatment. In this same cohort, the incidence of death in the first year post-MI was 20 per 100-person years in NSAID-treated patients compared to 12 per 100 person years in non-NSAID exposed patients. Although the absolute rate of death declined somewhat after the first year post-MI, the increased relative risk of death in NSAID users persisted over at least the next four years after follow-up. Avoid the use of naproxen and esomeprazole magnesium delayed-release tablets in patients with a recent MI unless the benefits are expected to outweigh the risk of recurrent CV thrombotic events. If naproxen and esomeprazole magnesium delayed-release tablets are used in patients with a recent MI, monitor patients for signs of cardiac ischemia.
5.2 Gastrointestinal Bleeding, Ulceration, and Perforation NSAIDs, including naproxen, can cause serious gastrointestinal (GI) adverse events including inflammation, bleeding, ulceration, and perforation of the esophagus, stomach, small intestine, or large intestine, which can be fatal. These serious adverse events can occur at any time, with or without warning symptoms, in patients treated with NSAIDs. Only one in five patients who develop a serious upper GI adverse event on NSAID therapy is symptomatic. Upper GI ulcers, gross bleeding, or perforation caused by NSAIDs occurred in approximately 1% of patients treated for 3 months to 6 months, and in about 2% to 4% of patients treated for one year. However, even short-term NSAID therapy is not without risk.
Risk
Factors for GI Bleeding, Ulceration, and Perforation Patients with a prior history of peptic ulcer disease and/or GI bleeding who used NSAIDs had a greater than 10-fold increased risk for developing a GI bleed compared to patients without these risk factors. Other factors that increase the risk for GI bleeding in patients treated with NSAIDs include longer duration of NSAID therapy; concomitant use of oral corticosteroids, aspirin, anticoagulants, or selective serotonin reuptake inhibitors (SSRIs); smoking; use of alcohol; older age; and poor general health status. Most postmarketing reports of fatal GI events are in elderly or debilitated patients. Additionally, patients with advanced liver disease and/or coagulopathy are at increased risk for GI bleeding. Strategies to Minimize the GI Risks in NSAID-treated patients: Use the lowest effective dosage for the shortest possible duration. Avoid administration of more than one NSAID at a time. Avoid use in patients at higher risk unless benefits are expected to outweigh the increased risk of bleeding. For such as patients, as well as those with active GI bleeding, consider alternate therapies other than NSAIDs. Remain alert for signs and symptoms of GI ulceration and bleeding during NSAID therapy. If a serious GI adverse event is suspected, promptly initiate evaluation and treatment, and discontinue naproxen and esomeprazole magnesium delayed-release tablets until a serious GI adverse event is ruled out. In the setting of concomitant use of low-dose aspirin for cardiac prophylaxis, monitor patients more closely for evidence of GI bleeding [see Drug Interactions ( 7 )]. NSAIDs should be given with care to patients with a history of inflammatory bowel disease (ulcerative colitis, Crohn’s disease) as their condition may be exacerbated.
5.3 Hepatotoxicity Elevations of ALT or AST (three or more times the upper limit of the normal [ULN]) have been reported in approximately 1% of NSAID-treated patients in clinical trials. In addition, rare, and sometimes fatal, cases of severe hepatic injury, including jaundice and fatal fulminant hepatitis, liver necrosis, and hepatic failure have been reported. Elevations of ALT or AST (less than three times ULN) may occur in up to 15% of patients treated with NSAIDs including naproxen. Inform patients of the warning signs and symptoms of hepatotoxicity (e.g., nausea, fatigue, lethargy, diarrhea, pruritus, jaundice, right upper quadrant tenderness, and “flu-like” symptoms). If clinical signs and symptoms consistent with liver disease develop, or if systemic manifestations occur (e.g., eosinophilia, rash, etc.), discontinue naproxen and esomeprazole magnesium delayed-release tablets immediately, and perform a clinical evaluation of the patient. Naproxen and esomeprazole magnesium delayed-release tablets should be avoided in patients with severe hepatic impairment <span class="opacity-50 text-xs">[see Dosage and Administration ( 2 ), Use in Specific Populations ( 8.6 ), and Clinical Pharmacology ( 12.3 )]</span>.
5.4 Hypertension NSAIDs, including naproxen and esomeprazole magnesium delayed-release tablets, can lead to new onset of hypertension or worsening of preexisting hypertension, either of which may contribute to the increased incidence of CV events. Patients taking angiotensin converting enzyme (ACE) inhibitors, thiazides diuretics, or loop diuretics may have impaired response to these therapies when taking NSAIDs <span class="opacity-50 text-xs">[see Drug Interactions ( 7 )]</span>. Monitor blood pressure (BP) during the initiation of NSAID treatment and throughout the course of therapy.
5.5 Heart Failure and Edema The Coxib and traditional NSAID Trialists’ Collaboration meta-analysis of randomized controlled trials demonstrated an approximately two-fold increase in hospitalizations for heart failure in COX-2 selective treated patients and nonselective NSAID-treated patients compared to placebo-treated patients. In a Danish National Registry study of patients with heart failure, NSAID use increased the risk of MI, hospitalization for heart failure, and death. Additionally, fluid retention and edema have been observed in some patients treated with NSAIDs. Use of naproxen may blunt the CV effects of several therapeutic agents used to treat these medical conditions (e.g., diuretics, ACE inhibitors, or angiotensin receptor blockers [ARBs]) <span class="opacity-50 text-xs">[see Drug Interactions ( 7 )]</span>. Avoid the use of naproxen and esomeprazole magnesium delayed-release tablets in patients with severe heart failure unless the benefits are expected to outweigh the risk of worsening heart failure. If naproxen and esomeprazole magnesium delayed-release tablets are used in patients with severe heart failure, monitor patients for signs and symptoms of worsening heart failure.
5.6 Renal Toxicity and Hyperkalemia Renal Toxicity Long-term administration of NSAIDs has resulted in renal papillary necrosis and other renal injury. Renal toxicity has also been seen in patients in whom renal prostaglandins have a compensatory role in the maintenance of renal perfusion. In these patients, administration of an NSAID may cause a dose-dependent reduction in prostaglandin formation and, secondarily, in renal blood flow, which may precipitate overt renal decompensation. Patients at greatest risk of this reaction are those with impaired renal function, dehydration, hypovolemia, heart failure, liver dysfunction, those taking diuretics and ACE-inhibitors or ARBs, and the elderly. Discontinuation of NSAID therapy was usually followed by recovery to the pretreatment state. No information is available from controlled clinical studies regarding the use of naproxen and esomeprazole magnesium delayed-release tablets in patients with advanced renal disease. The renal effects of naproxen and esomeprazole magnesium delayed-release tablets may hasten the progression of renal dysfunction in patients with pre-existing renal disease. Correct volume status in dehydrated or hypovolemic patients prior to initiating naproxen and esomeprazole magnesium delayed-release tablets. Monitor renal function in patients with renal or hepatic impairment, heart failure, dehydration, or hypovolemia during use of naproxen and esomeprazole magnesium delayed-release tablets <span class="opacity-50 text-xs">[see Drug Interactions ( 7 )]</span> . Avoid the use of naproxen and esomeprazole magnesium delayed-release tablets in patients with advanced renal disease unless the benefits are expected to outweigh the risk of worsening renal failure. If naproxen and esomeprazole magnesium delayed-release tablets are used in patients with advanced renal disease, monitor patients for signs of worsening renal function.
Hyperkalemia
Increases in serum potassium concentration, including hyperkalemia, have been reported with use of NSAIDs, even in some patients without renal impairment. In patients with normal renal function, these effects have been attributed to a hyporeninemic-hypoaldosteronism state.
5.7 Anaphylactic Reactions Naproxen has been associated with anaphylactic reactions in patients with and without known hypersensitivity to naproxen and in patients with aspirin-sensitive asthma <span class="opacity-50 text-xs">[see Contraindications ( 4 ) and Warnings and Precautions ( 5.8 )]</span>. Seek emergency help if an anaphylactic reaction occurs.
5.8 Exacerbation of Asthma Related to Aspirin Sensitivity A subpopulation of patients with asthma may have aspirin-sensitive asthma which may include chronic rhinosinusitis complicated by nasal polyps; severe, potentially fatal bronchospasm; and/or intolerance to aspirin and other NSAIDs. Because cross-reactivity between aspirin and other NSAIDs has been reported in such aspirin-sensitive patients, naproxen and esomeprazole magnesium delayed-release tablets are contraindicated in patients with this form of aspirin sensitivity <span class="opacity-50 text-xs">[see Contraindications ( 4 )]</span> . When naproxen and esomeprazole magnesium delayed-release tablets are used in patients with preexisting asthma (without known aspirin sensitivity), monitor patients for changes in the signs and symptoms of asthma.
5.9 Serious or Severe Skin Reactions Naproxen NSAIDs, including naproxen, can cause serious skin adverse events such as exfoliative dermatitis, Stevens-Johnson syndrome (SJS), and toxic epidermal necrolysis (TEN), which can be fatal. NSAIDs can also cause fixed drug eruption (FDE). FDE may present as a more severe variant known as generalized bullous fixed drug eruption (GBFDE), which can be life-threatening. These serious events may occur without warning. Esomeprazole PPIs can cause severe cutaneous adverse reactions, including SJS, TEN, and acute generalized exanthematous pustulosis (AGEP) <span class="opacity-50 text-xs">[see Adverse Reactions ( 6.2 )]</span>. Naproxen and Esomeprazole Magnesium Delayed-Release Tablets Inform patients about the signs and symptoms of serious or severe skin reactions, and to discontinue the use of naproxen and esomeprazole magnesium delayed-release tablets at the first appearance of skin rash or any other sign of hypersensitivity and consider further evaluation. Naproxen and esomeprazole magnesium delayed-release tablets are contraindicated in patients with previous serious skin reactions to NSAIDs <span class="opacity-50 text-xs">[see Contraindications ( 4 )]</span>.
5.10 Drug Reaction with Eosinophilia and Systemic Symptoms (DRESS)
Drug
Reaction with Eosinophilia and Systemic Symptoms (DRESS) has been reported in patients taking NSAIDs and PPIs such as those contained in naproxen and esomeprazole magnesium delayed-release tablets. Some of these events have been fatal or life-threatening. DRESS typically, although not exclusively, presents with fever, rash, lymphadenopathy, and/or facial swelling. Other clinical manifestations may include hepatitis, nephritis, hematological abnormalities, myocarditis, or myositis. Sometimes symptoms of DRESS may resemble an acute viral infection. Eosinophilia is often present. Because this disorder is variable in its presentation, other organ systems not noted here may be involved. It is important to note that early manifestations of hypersensitivity, such as fever or lymphadenopathy, may be present even though rash is not evident. If such signs or symptoms are present, discontinue naproxen and esomeprazole magnesium delayed-release tablets and evaluate the patient immediately [see also Warnings and Precautions ( 5.9 )] .
5.11 Fetal Toxicity Premature Closure of Fetal Ductus Arteriosus: Avoid use of NSAIDs, including naproxen and esomeprazole magnesium delayed-release tablets, in pregnant women at about 30 weeks gestation and later. NSAIDs, including naproxen and esomeprazole magnesium delayed-release tablets, increase the risk of premature closure of the fetal ductus arteriosus at approximately this gestational age.
Oligohydramnios/Neonatal
Renal Impairment: Use of NSAIDs, including naproxen and esomeprazole magnesium delayed-release tablets, at about 20 weeks gestation or later in pregnancy may cause fetal renal dysfunction leading to oligohydramnios and, in some cases, neonatal renal impairment. These adverse outcomes are seen, on average, after days to weeks of treatment, although oligohydramnios has been infrequently reported as soon as 48 hours after NSAID initiation. Oligohydramnios is often, but not always, reversible with treatment discontinuation. Complications of prolonged oligohydramnios may, for example, include limb contractures and delayed lung maturation. In some postmarketing cases of impaired neonatal renal function, invasive procedures such as exchange transfusion or dialysis were required. If NSAID treatment is necessary between about 20 weeks and 30 weeks gestation, limit naproxen and esomeprazole magnesium delayed-release tablets use to the lowest effective dose and shortest duration possible. Consider ultrasound monitoring of amniotic fluid if naproxen and esomeprazole magnesium delayed-release tablets treatment is needed in a pregnant woman. Discontinue naproxen and esomeprazole magnesium delayed-release tablets if oligohydramnios occurs and follow up according to clinical practice [see Use in Specific Populations ( 8.1 )].
5.12 Hematologic Toxicity Anemia has occurred in NSAID-treated patients. This may be due to occult or gross blood loss, fluid retention, or an incompletely described effect on erythropoiesis. If a patient treated with naproxen and esomeprazole magnesium delayed-release tablets have any signs or symptoms of anemia, monitor hemoglobin or hematocrit. NSAIDs, including naproxen and esomeprazole magnesium delayed-release tablets, may increase the risk of bleeding events. Co-morbid conditions such as coagulation disorders or concomitant use of warfarin and other anticoagulants, antiplatelet agents (e.g., aspirin), and serotonin reuptake inhibitors (SSRIs) and serotonin norepinephrine reuptake inhibitors (SNRIs) may increase the risk. Monitor these patients for signs of bleeding <span class="opacity-50 text-xs">[see Drug Interactions ( 7 )]</span>.
5.13 Masking of Inflammation and Fever The pharmacological activity of naproxen and esomeprazole magnesium delayed-release tablets in reducing inflammation, and possibly fever, may diminish the utility of diagnostic signs in detecting infections.
5.14 Laboratory Monitoring Because serious GI bleeding, hepatotoxicity, and renal injury can occur without warning symptoms or signs, consider monitoring patients on long-term NSAID treatment with a CBC and chemistry profile periodically <span class="opacity-50 text-xs">[see Warnings and Precautions ( 5.2 , 5.3 , 5.6 )]</span>. Patients with initial hemoglobin values of 10 g or less who are to receive long-term therapy should have hemoglobin values determined periodically.
5.15 Active Bleeding When active and clinically significant bleeding from any source occurs in patients receiving naproxen and esomeprazole magnesium delayed-release tablets, the treatment should be withdrawn.
5.16 Concomitant NSAID Use Naproxen and esomeprazole magnesium delayed-release tablets contain naproxen as one of its active ingredients. It should not be used with other naproxen-containing products since they all circulate in the plasma as the naproxen anion. The concomitant use of naproxen and esomeprazole magnesium delayed-release tablets with any dose of a non-aspirin NSAID should be avoided due to the potential for increased risk of adverse reactions.
5.17 Presence of Gastric Malignancy In adults, response to gastric symptoms with naproxen and esomeprazole magnesium delayed-release tablets does not preclude the presence of gastric malignancy. Consider additional gastrointestinal follow-up and diagnostic testing in adult patients who experience gastric symptoms during treatment with naproxen and esomeprazole magnesium delayed-release tablets or have a symptomatic relapse after completing treatment. In older patients, also consider an endoscopy.
5.18 Acute Tubulointerstitial Nephritis Acute tubulointerstitial nephritis (TIN) has been observed in patients taking PPIs and may occur at any point during PPI therapy. Patients may present with varying signs and symptoms from symptomatic hypersensitivity reactions to non-specific symptoms of decreased renal function (e.g., malaise, nausea, anorexia). In reported case series, some patients were diagnosed on biopsy and in the absence of extra-renal manifestations (e.g., fever, rash or arthralgia). Discontinue naproxen and esomeprazole magnesium delayed-release tablets and evaluate patients with suspected acute TIN <span class="opacity-50 text-xs">[see Contraindications ( 4 )]</span>.
5.19 Clostridium difficile -Associated Diarrhea Published observational studies suggest that proton pump inhibitor (PPI) therapy like naproxen and esomeprazole magnesium delayed-release tablets may be associated with an increased risk of Clostridium difficile associated diarrhea, especially in hospitalized patients. This diagnosis should be considered for diarrhea that does not improve <span class="opacity-50 text-xs">[see Adverse Reactions ( 6.2 )]</span>. Patients should use the lowest dose and shortest duration of PPI therapy appropriate to the condition being treated <span class="opacity-50 text-xs">[see Dosage and Administration ( 2 )]</span>.
5.20 Bone Fracture Several published observational studies suggest that PPI therapy may be associated with an increased risk for osteoporosis-related fractures of the hip, wrist, or spine. The risk of fracture was increased in patients who received high-dose, defined as multiple daily doses, and long-term PPI therapy (a year or longer). Patients should use the lowest dose and shortest duration of PPI therapy appropriate to the condition being treated. Patients at risk for osteoporosis-related fractures should be managed according to the established treatment guidelines <span class="opacity-50 text-xs">[see Dosage and Administration ( 2 ) , Adverse Reactions ( 6.2 )]</span>. Naproxen and esomeprazole magnesium delayed-release tablets (a combination PPI/NSAID) are approved for use twice a day and does not allow for administration of a lower daily dose of the PPI <span class="opacity-50 text-xs">[see Dosage and Administration ( 2 )]</span>.
5.21 Cutaneous and Systemic Lupus Erythematosus Cutaneous lupus erythematosus (CLE) and systemic lupus erythematosus (SLE) have been reported in patients taking PPIs, including esomeprazole. These events have occurred as both new onset and an exacerbation of existing autoimmune disease. The majority of PPI-induced lupus erythematous cases were CLE. The most common form of CLE reported in patients treated with PPIs was subacute CLE (SCLE) and occurred within weeks to years after continuous drug therapy inpatients ranging from infants to the elderly. Generally, histological findings were observed without organ involvement. SLE is less commonly reported than CLE in patients receiving PPIs. PPI associated SLE is usually milder than non-drug induced SLE. Onset of SLE typically occurred within days to years after initiating treatment primarily in patients ranging from young adults to the elderly. The majority of patients presented with rash; however, arthralgia and cytopenia were also reported. Avoid administration of PPIs for longer than medically indicated. If signs or symptoms consistent with CLE or SLE are noted in patients receiving naproxen and esomeprazole magnesium delayed-release tablets, discontinue drug and refer the patient to the appropriate specialist for evaluation. Most patients improve with discontinuation of the PPI alone in 4 to 12 weeks. Serological testing (e.g., ANA) may be positive and elevated serological test results may take longer to resolve than clinical manifestations.
5.22 Interaction with Clopidogrel Avoid concomitant use of esomeprazole with clopidogrel. Clopidogrel is a prodrug. Inhibition of platelet aggregation by clopidogrel is entirely due to an active metabolite. The metabolism of clopidogrel to its active metabolite can be impaired by use with concomitant medications, such as esomeprazole, that inhibit CYP2C19 activity. Concomitant use of clopidogrel with 40 mg esomeprazole reduces the pharmacological activity of clopidogrel. When using esomeprazole, a component of naproxen and esomeprazole magnesium delayed-release tablets, consider alternative anti-platelet therapy <span class="opacity-50 text-xs">[see Drug Interactions ( 7 ), Clinical Pharmacology ( 12.3 )]</span>.
5.23 Cyanocobalamin (Vitamin B-12)
Deficiency
Daily treatment with any acid-suppressing medications over a long period of time (e.g., longer than 3 years) may lead to malabsorption of cyanocobalamin (vitamin B-12) caused by hypo-or achlorhydria. Rare reports of cyanocobalamin deficiency occurring with acid-suppressing therapy have been reported in the literature. This diagnosis should be considered if clinical symptoms consistent with cyanocobalamin deficiency are observed.