布洛芬-法莫替丁复方制剂Duexis获准
美国的一家生物制药公司Horizon制药开发了一种新片剂布洛芬（ibuprofen，800毫克）和法莫替丁（famotidine，26.6毫克）固定剂量复方片剂，适应关节炎、疼痛炎症性疾病治疗未能满足的需求。其商品名为Duexis，4月25日获得美国FDA批准。抗炎剂布洛芬会引起消化道溃疡，法莫替丁可减少造成溃疡的胃酸分泌。两项关键性研究——REDUCE-1和REDUCE-2数据显示：服用Duexis的患者较单独服用布洛芬者消化道溃疡明显减少。
许多骨关节炎和类风湿性关节炎患者因为长期使用非甾体抗炎剂引起上消化道溃疡，Duexis 为他们提供了新的选择。
DUEXIS
Manufacturer:
Horizon Pharma
Pharmacological Class:
NSAID + H2 blocker.
Active Ingredient(s):
Ibuprofen 800mg, famotidine 26.6mg; tabs.
Indication(s):
Relief of signs/symptoms of rheumatoid arthritis and osteoarthritis and to decrease the risk of developing upper gastrointestinal ulcers (eg, gastric and/or duodenal ulcer), in patients who are taking ibuprofen for those indications.
Pharmacology:
Duexis is a fixed-combination tablet of ibuprofen and famotidine.
Ibuprofen possesses analgesic and antipyretic activities. Its exact mechanism of action is not completely understood, but may be related to prostaglandin synthetase inhibition.
Famotidine is a competitive inhibitor of histamine H2-receptors. The primary pharmacologic activity of famotidine is inhibition of gastric secretion. Both the acid concentration and volume of gastric secretion are suppressed by famotidine, while changes in pepsin secretion are proportional to volume output.
Clinical Trials:
The efficacy of Duexis was evaluated in two multicenter, double-blind, active-controlled, randomized, 24-week studies in patients who were expected to require daily administration of an NSAID for at least the coming 6 months for conditions such as the following: osteoarthritis, rheumatoid arthritis, chronic low back pain, chronic regional pain syndrome, and chronic soft tissue pain. Patients were assigned randomly, in approximately a 2:1 ratio, to treatment with either Duexis or ibuprofen 800mg three times daily. A total of 1533 patients were enrolled and ranged in age from 39–80 years (median age 55 years) with 68% females.
Studies 301 and 303 compared the incidence of upper gastrointestinal (gastric and/or duodenal) ulcer formation in a total of 930 patients taking Duexis (ibuprofen and famotidine) and 452 patients taking ibuprofen only, either as a primary or secondary endpoint. In both trials, Duexis was associated with a statistically significantly reduction in the risk of developing upper gastrointestinal ulcers compared to taking ibuprofen only during the 6 month study period.
Legal Classification:
Rx
Adults:
Swallow whole. 1 tab three times daily. Use lowest effective dose for the shortest duration.
Children:
Not recommended.
Contraindication(s):
Aspirin allergy. Coronary artery bypass graft surgery. Late stage pregnancy (≥30 weeks gestation).
Warnings/Precautions:
Increased risk of serious cardiovascular or GI events. Renal impairment (CrCl <50mL/min): not recommended. Hypertension; monitor BP. Heart failure. Edema. History of ulcer disease or GI bleeding. Active peptic ulcer. Inflammatory bowel disease (eg, ulcerative colitis, Crohn’s disease). Seizures. Hepatic dysfunction. Bleeding disorders. Monitor blood, hepatic and renal function in chronic use. Discontinue if visual, rash, skin reactions, renal or liver dysfunction occurs. Asthma. Elderly. Debilitated. Labor & delivery. Pregnancy (Cat.C). Nursing mothers: not recommended.
Interaction(s):
Increased risk of GI bleed with oral corticosteroids, aspirin, warfarin-type anticoagulants (monitor), alcohol, smoking. May antagonize ACE-inhibitors, diuretics. Increases lithium levels. May increase toxicity of methotrexate. Caution with concomitant SSRIs. Delayed absorption with cholestyramine.
Adverse Reaction(s):
GI upset, constipation, upper abdominal pain, dyspepsia, headache, hemorrhage, dizziness; GI ulcer/bleed, elevated liver enzymes (discontinue if hepatotoxicity develops), blurred vision, rash/serious skin infections (discontinue if occurs), peripheral edema, anemia, hypertension, renal papillary necrosis, aseptic meningitis. See literature re: risk of cardiovascular events.
How Supplied:
Tabs—90
Last Updated:
1/10/2012