Relif - General Information
Relif is a non-steroidal anti-inflammatory drug of the arylalkanoic acid family (which includes diclofenac). Marketed under the brand name Relafen, it has been shown to have a slightly lower risk of gastrointestinal side effects than most other non-selective NSAID's.
Pharmacology of Relif
Relif is a naphthylalkanone. It is a nonsteroidal anti-inflammatory drug (NSAID) that exhibits anti-inflammatory, analgesic and antipyretic properties in pharmacologic studies. As with other nonsteroidal anti-inflammatory agents, its mode of action is not known. However, the ability to inhibit prostaglandin synthesis may be involved in the anti-inflammatory effect.
Relif for patients
Nabumetone is a non-steroidal anti-inflammatory (NSAID) medication used to relieve pain, treat fever, and decrease inflammation and swelling. It is used commonly to treat osteoarthritis and rheumatoid arthritis. This medication should not be used by those with aspirin allergies producing symptoms of difficult breathing, red itching skin. This class of medications has been associated with ulcer and bleeding in the stomach. This is often relieved by taking the medication with food. Water retention may also occur and you should report any swelling of the feet or difficulty breathing to your physician immediately. This medication can be taken with or without food, however, food often alleviates stomach irritation.
In vitro studies have shown that, because of its affinity for protein, 6MNA may displace other protein-bound drugs from their binding site. Caution should be exercised when administering nabumetone with warfarin since interactions have been seen with other NSAIDs.
Concomitant administration of an aluminum-containing antacid had no significant effect in the bioavailability of 6MNA. When administered with food or milk, there is more rapid absorption; however, the total amount of 6MNA in the plasma is unchanged.
Nabumetone is contraindicated in patients who have previously exhibited hypersensitivity to it.
Nabumetone is contraindicated in patients in whom nabumetone, aspirin or other NSAIDs induce asthma, urticaria or other allergic-type reactions. Fatal asthmatic reactions have been reported in such patients receiving NSAIDs.
Additional information about Relif
Relif Indication: For acute and chronic treatment of signs and symptoms of osteoarthritis and rheumatoid arthritis.
Mechanism Of Action: The parent compound is a prodrug, which undergoes hepatic biotransformation to the active component, 6-methoxy-2-naphthylacetic acid (6MNA), that is a potent inhibitor of prostaglandin synthesis, most likely through binding to the COX-1 and COX-2 receptors.
Drug Interactions: Alendronate Increased risk of gastric toxicity
Methotrexate The NSAID increases the effect and toxicity of methotrexate
Cyclosporine Monitor for nephrotoxicity
Anisindione The NSAID increases the anticoagulant effect
Warfarin The NSAID increases the anticoagulant effect
Acenocoumarol The NSAID increases the anticoagulant effect
Dicumarol The NSAID increases the anticoagulant effect
Food Interactions: Avoid alcohol.
Take with food.
Generic Name: Nabumetone
Synonyms: Nabumetonum [INN-Latin]; Nabumetona
Drug Category: Anti-Inflammatory Agents, Non-Steroidal; Antineoplastic Agents
Drug Type: Small Molecule; Approved
Absorption: Well absorbed from the gastrointestinal tract. Coadministration of food increases the rate of absorption and subsequent appearance of 6MNA (the active metabolite) in the plasma but does not affect the extent of conversion of nabumetone into 6MNA.
Toxicity (Overdose): The one overdose occurred in a 17-year-old female patient who had a history of abdominal pain and was hospitalized for increased abdominal pain following ingestion of 30 nabumetone tablets (15 grams total). Stools were negative for occult blood and there was no fall in serum hemoglobin concentration. The patient had no other symptoms.
Protein Binding: The active metabolite, 6MNA, is more than 99% bound to plasma proteins.
Biotransformation: Undergoes rapid biotransformation to the principal active metabolite, 6-methoxy-2-naphthylacetic acid (6MNA). Approximately 35% of a 1000 mg oral dose of nabumetone is converted to 6MNA and 50% is converted into unidentified metabolites which are subsequently excreted in the urine.
Half Life: Approximately 23 hours for the active metabolite, 6MNA. Increased in patients with renal insufficiency.
Dosage Forms of Relif: Tablet Oral
Chemical IUPAC Name: 4-(6-methoxynaphthalen-2-yl)butan-2-one
Chemical Formula: C15H16O2
Nabumetone on Wikipedia: https://en.wikipedia.org/wiki/Nabumetone
Organisms Affected: Humans and other mammals