Indications for: ARTHROTEC 50
Osteoarthritis (OA) or rheumatoid arthritis (RA) in patients at high risk for developing NSAID-induced gastric or duodenal ulcers.
Diclofenac, as a single agent and combined with misoprostol, has been shown to be effective in the management of the signs/symptoms of osteoarthritis.
Diclofenac, as a single agent and combined with misoprostol, has been shown to be effective in the management of the signs/symptoms of rheumatoid arthritis.
Upper GI Safety
In a 12-week, randomized, double-blind, dose-response study, misoprostol 200mcg administered 4, 3 or 2 times a day, was significantly more effective than placebo in reducing the incidence of gastric ulcer in osteoarthritis and rheumatoid arthritis patients using a variety of NSAIDs. The incidence of NSAID-induced duodenal ulcer was also significantly reduced with the 2 times a day, 3 times a day, and 4 times a day dosage regimens of misoprostol compared with placebo (P <.05):
- Gastric ulcer: 6%, 3%, 3% vs 11%, respectively.
- Duodenal ulcer: 2%, 3%, 1% vs 6%, respectively.
Following 6 weeks of treatment, patients who received Arthrotec were found to have a lower incidence of endoscopically defined gastric ulcers compared with those who received diclofenac sodium in a study of 572 patients with osteoarthritis:
- Arthrotec 50 three times a day: gastric 3%; duodenal 6%
- Arthrotec 75 two times a day: gastric 4%; duodenal 3%
- Diclofenac sodium 75mg two times a day: gastric 11%; duodenal 7%
- Placebo: gastric 3%; duodenal 1%
Use lowest effective dose for shortest duration. Swallow whole; food may reduce diarrhea. ≥18yrs: OA: one Arthrotec 50 tab 3 times daily. RA: one Arthrotec 50 tab 3–4 times daily. Both: if not tolerated, may reduce to one Arthrotec 50 or one Arthrotec 75 tablet twice daily (this may be less effective in preventing ulcers). Concomitant CYP2C9 inhibitors: max Arthrotec 50 twice daily. See full labeling.
<18yrs: not established.
ARTHROTEC 50 Contraindications:
Pregnancy. Aspirin allergy. Coronary artery bypass graft surgery. Active GI bleeding.
Risk of uterine rupture, abortion, premature birth, and birth defects. Risk of serious cardiovascular and gastrointestinal events.
ARTHROTEC 50 Warnings/Precautions:
Can cause abortion, premature birth, birth defects, or uterine rupture in pregnant women. Increased risk of uterine rupture with advanced gestational age, prior uterine surgery including cesarean delivery. For women of childbearing potential: obtain negative serum pregnancy test within 2 weeks before start of therapy; begin Arthrotec therapy on 2nd or 3rd day of menstrual period; use effective contraception during therapy; give oral and written warnings on risks in pregnancy. Increased risk of serious cardiovascular events (including MI, stroke). Avoid in recent MI, severe heart failure; if necessary, monitor. Increased risk of serious GI adverse events (including inflammation, bleeding, ulceration, perforation). History of ulcer disease, GI bleeding, or inflammatory bowel disease. Hypertension; monitor BP closely. Hepatic or renal impairment. Discontinue if signs/symptoms of liver disease develop, or if abnormal LFTs persist or worsen. Dehydration. Hypovolemia. Advanced renal disease: not recommended. Hyperkalemia. Coagulation disorders. Monitor CBCs, blood chemistry, hepatic, and renal function in long-term therapy. Pre-existing asthma. May mask signs of infection or fever. Discontinue at 1st sign of rash or any other hypersensitivity. Premature closure of fetal ductus arteriosus. Elderly. Debilitated. Labor & delivery. Nursing mothers.
ARTHROTEC 50 Classification:
NSAID + prostaglandin E1 analogue.
ARTHROTEC 50 Interactions:
Avoid concomitant aspirin, salicylates (eg, diflunisal, salsalate), other NSAIDs, magnesium-containing antacids. Increased risk of GI bleed with anticoagulants, antiplatelets, oral corticosteroids, SSRIs, SNRIs, smoking, alcohol, or prolonged NSAID therapy; monitor. May antagonize, or increase risk of renal failure with diuretics (eg, loop or thiazides), ACE inhibitors, ARBs, or β-blockers; monitor closely. Potentiates digoxin; monitor levels. May potentiate lithium, methotrexate, cyclosporine; monitor for toxicity. Concomitant with pemetrexed may increase risk of pemetrexed-associated myelosuppression, renal, and GI toxicity. May be potentiated by CYP2C9 inhibitors (eg, voriconazole); see Adult. May be antagonized by CYP2C9 inducers (eg, rifampin); adjust dose. Caution with concomitant hepatotoxic drugs (eg, antibiotics, antiepileptics).
Abdominal pain, diarrhea, dyspepsia, nausea, flatulence, gastritis, vomiting, constipation, headache, dizziness, increased ALT, decreased hematocrit; cardiovascular thrombotic events, GI ulcer/bleed, hepatotoxicity, renal toxicity, hypersensitivity reactions, anemia.
Diclofenac: renal (65%), biliary (35%); half-life: ~2 hours
Misoprostol: renal (70%); half-life: ~30 minutes
Generic Drug Availability:
Arthrotec 50—60, 90; Arthrotec 75—60