Esomeprazole-naproxen

Dosage Forms & Strengths

esomeprazole/naproxen

tablet

• 20mg/375mg
• 20mg/500mg

Rheumatoid Arthritis

1 tablet PO twice daily at least 30 min before meal

Osteoarthritis

1 tablet PO twice daily at least 30 min before meal

Ankylosing Spondylitis

1 tablet PO twice daily at least 30 min before meal

Dosage Modification

If a dose of omeprazole needs to be < 0 mg/day consider alternate treatment

Severe renal impairment (CrCl <30 mL/min): Use not recommended

Safety and efficacy not established

Mechanism of Action

Naproxen: NSAID that inhibits inflammatory reactions and pain by decreasing activity of cyclo-oxygenase, which is responsible for prostaglandin synthesis; has antipyretic and analgesic effects

Esomeprazole: S-isomer of omeprazole, a proton pump inhibitor; inhibits gastric acid secretion by inhibiting H+/K+-ATPase enzyme system at secretory surface of gastric parietal cells

Naproxen

Half-Life: 13-15 hr

Bioavailability: 95%

Duration: 4-7 hr

Onset: 1 hr

Distribution: 0.16 L/kg

Peak Serum Time: 1.5-3 hr; high fat meal prolongs Tmax by 10 hr

Peak Plasma Concentration: 62-96 mcg/mL Vd: 0.16 L/kg

Protein Bound: >99% albumin

Metabolism: hepatic via CYP2C9, CYP1A2; also undergoes hepatic conjugation

Clearance: 0.13 L/min/kg

Excretion: feces < 3%, urine 95%

Esomeprazole

Half-Life: 1.2-1.5 hr

Bioavailability: 90%, food decreases AUC by 33-53%

Duration: 17 hr gastric acid inhibition at steady state

Onset: 1-2 hr

Peak Plasma Time: 1-1.6 hr

Vd: 16 L

Protein Bound: 97%

Clearance: 9-16 L/hr

Excretion: Feces 20%, urine 80%

Metabolism

• Extensively by hepatic P450 enzyme: major metabolic pathway is via CYP2C19, the rest is via CYP3A4
• Slow metabolizers (3% of Caucasians and African-Americans) are deficient in CPY2C19 enzyme system, plasma concentration can be higher than those with the enzyme present
• CYP2C19 inhibitor

Esomeprazole & Naproxen may be found in some form under the following brand names:

• Vimovo

Medicines can interact with certain foods. In some cases, this may be harmful and your doctor may advise you to avoid certain foods. In the case of esomeprazole/naproxen there are no specific foods that you must exclude from your diet when receiving this medication.

Before you take esomeprazole/naproxen, tell your healthcare provider about all your medical conditions, including if you:

• have been told that you have low magnesium levels in your blood
• have liver or kidney problems
• have ulcerative colitis or Crohn’s disease (inflammatory bowel disease or IBD)
• have any other medical conditions
• are pregnant or breastfeeding

Tell your healthcare provider about all the medicines you take, including prescription and non-prescription medicines, vitamins, and herbal supplements.

Tell your doctor if you are pregnant or plan to become pregnant.

The FDA categorizes medications based on safety for use during pregnancy. Five categories - A, B, C, D, and X, are used to classify the possible risks to an unborn baby when a medication is taken during pregnancy.

Esomeprazole/naproxen falls into category C prior to 30 weeks gestation and category D starting at 30 weeks gestation. In late pregnancy, naproxen, (one component of this medication) should be avoided because it may cause harm to the unborn baby.

Tell your healthcare provider if you are breastfeeding or plan to breastfeed. Esomeprazole/naproxen can pass into your milk and may harm your baby. You should not breastfeed while taking esomeprazole/naproxen. Talk to your healthcare provider about the best way to feed your baby if you take this medication.

If you take too much esomeprazole/naproxen, tell your healthcare provider or go to the closest hospital emergency room right away. Symptoms that you have taken too much may include:

• feeling weak and tired
• dizziness
• feeling sleepy
• upper stomach-area pain or discomfort
• heartburn, indigestion, or nausea
• a change in breathing or you stop breathing
• vomiting
• bleeding
• movements of a body part that you cannot control
• coordination problems and decreased movement

If you take more esomeprazole/naproxen than your healthcare provider recommends, call your Poison Control Center at 1-800-222-1222.