Dosing and uses of Daypro (oxaprozin)
Adult dosage forms and strengths
tablet
- 600mg
Osteoarthritis
Initial in mild to moderate disease: 600mg PO qDay
Usual in moderate to severe disease: 1200mg PO qDay
Maximum 1,800 mg/day or 26 mg/kg/day, whichever is lower, divided PO q12hr
Rheumatoid Arthritis
1200mg PO qDay (individualize)
Maximum 1,800 mg/day or 26 mg/kg/day, whichever is lower, divided PO q12hr
Renal Impairment
Severe renal impairment or on dialysis: 600 mg PO qDay; may increase to 1200 mg/day; monitor closely
Hepatic Impairment
Caution in patients with severe liver impairment
Administration
Take with food or 8-12 oz water to avoid GI effects
Other Information
Renal Impairment: 600 mg PO qDay
Pediatric dosage forms and strengths
tablet
- 600mg
Juvenile Rheumatoid Arthritis
<6 years
- Safety and efficacy not established
>6 years
- 22-31 kg: 600 mg PO qDay
- 32-54 kg: 900 mg PO qDay
- >55 kg: 1200 mg PO qDay
Geriatric dosage forms and strengths
Osteoarthritis
Initial in mild to moderate disease: 600mg PO qDay
Usual in moderate to severe disease: 1200mg PO qDay
Maximum 1,800 mg/day or 26 mg/kg/day, whichever is lower, divided PO q12hr
Rheumatoid Arthritis
1200mg PO qDay (individualize)
Maximum 1,800 mg/day or 26 mg/kg/day, whichever is lower, divided PO q12hr
Daypro (oxaprozin) adverse (side) effects
Common
Edema
Rash
Abdominal pain
Anorexia
Constipation
Diarrhea
Indigestion
Nausea/Vomiting
GI ulcer
Gross bleeding with perforation
Heartburn
Anemia
LFT's increased
Tinnitus
Dysuria, Increased frequency of urination
Myocardial infarction (<2%)
<1%
Hypertension (<1%)
Palpitations (<1%)
Thrombotic tendency observations
Erythema multiforme (rare)
Scaling eczema
Stevens-Johnson syndrome (rare)
Toxic epidermal necrolysis (rare)
Cerebrovascular accident
Gastrointestinal hemorrhage (<1%)
Agranulocytosis (rare)
Leukopenia (<1%)
Thrombocytopenia (<1%)
Hepatitis (rare),
Jaundice, Liver failure
Anaphylactoid reaction (<1%)
Amblyopia (<1%)
Hearing loss (<1%)
Acute renal failure (rare)
Hematuria (rare)
Interstitial nephritis (rare)
Bronchospasm
Serum sickness due to drug (rare)
Warnings
Black box warnings
Cardiovascular Risk
- NSAIDs may increase risk of serious cardiovascular thrombotic events, myocardial infarction (MI), & stroke, which can be fatal
- Risk may increase with duration of use
- Patients with risk factors for or existing cardiovascular disease may be at greater risk
- NSAIDs are contraindicated for perioperative pain in the setting of coronary artery bypass graft (CABG) surgery (increased risk of MI & stroke)
Gastrointestinal Risk
- NSAIDs increase risk of serious GI adverse events including bleeding, ulceration, & perforation of the stomach or intestines, which can be fatal
- GI adverse events may occur at any time during use & without warning symptoms
- Elderly patients are at greater risk for serious GI events
Contraindications
Absolute: ASA allergy, CABg
Relative: bleeding disorder, duodenal/gastric/peptic ulcer, stomatitis, SLE, ulcerative colitis, upper GI disease, late pregnancy (may cause premature closure of ductus arteriosus)
Cautions
Use caution in asthma (bronchial), CHF, fluid retention, cardiac disease, HTN, severe hepatic impairment, hypertension, renal impairment
Long-term administration of NSAIDs may result in renal papillary necrosis and other renal injury; patients at greatest risk include the elderly, or those with impaired renal function, hypovolemia, heart failure, liver dysfunction, salt depletion, and individuals taking diuretics, ACE inhibitors, or ARBs
Risk of HTn
Risk of renal damage on long-term use
Heart Failure (HF) risk
- NSAIDS have the potential to trigger HF by prostaglandin inhibition that leads to sodium and water retention, increased systemic vascular resistance, and blunted response to diuretics
- NSAIDS should be avoided or withdrawn whenever possible
- AHA/ACC Heart Failure Guidelines; Circulation. 2016; 134
Pregnancy and lactation
Pregnancy category: C; avoid in late pregnancy, may cause premature closure of the ductus arteriosus
The Quebec Pregnancy Registry identified 4705 women who had spontaneous abortions by 20 weeks' gestation; each case was matched to 10 control subjects (n=47,050) who had not had spontaneous abortions; exposure to nonaspirin NSAIDs during pregnancy was documented in approximately 7.5% of cases of spontaneous abortions and in approximately 2.6% of controls. (CMAJ, September 6, 2011; DOI:10.1503/cmaj.110454)
Lactation: not known whether excreted in breast milk; effect on infant unknown
Pregnancy categories
A: Generally acceptable. Controlled studies in pregnant women show no evidence of fetal risk.
B: May be acceptable. Either animal studies show no risk but human studies not available or animal studies showed minor risks and human studies done and showed no risk.
C: Use with caution if benefits outweigh risks. Animal studies show risk and human studies not available or neither animal nor human studies done.
D: Use in LIFE-THREATENING emergencies when no safer drug available. Positive evidence of human fetal risk.
X: Do not use in pregnancy. Risks involved outweigh potential benefits. Safer alternatives exist.
NA: Information not available.
Pharmacology of Daypro (oxaprozin)
Mechanism of action
Inhibits synthesis of prostaglandins in body tissues by inhibiting at least 2 cyclooxygenase isoenzymes, cyclooxygenase-1 (COX-1) and -2 (COX-2)
May inhibit chemotaxis, may alter lymphocyte activity, decrease proinflammatory cytokine activity, and may inhibit neutrophil aggregation. These effects may contribute to its anti-inflammatory activity
Pharmacokinetics
Half-Life: 44-50 hr
Protein Bound: 99%
Vd: 11-17 L/70 kg
Time to peak: 2-4hr
Metabolism: Liver (microsomal oxidation (65%); glucuronic acid conjugation (35%)
Metabolites: Ester, ether glucuronide
Excretion: Urine (65%); feces (35%)
Enzymes inhibited: Cyclooxygenase
Absorption: 95% (PO)
Dialyzable: Yes, but inefficient
