Generic

Nabumetone

Indications

Nabumetone is prescribed for the treatment of osteoarthritis and rheumatoid arthritis symptoms. Before opting to take Nabumetone, carefully evaluate the potential advantages and hazards of the drug as well as other treatment choices. Use the lowest effective dose for the shortest time possible in accordance with the treatment goals of each individual patient.

Pharmacology

A naphthylalkanone is nabumetone. Is a non-selective prostaglandin G/H synthase (a.k.a. cyclooxygenase or COX) inhibitor that inhibits both prostaglandin G/H synthase 1 and 2 in the body (COX-1 and -2). Arachidonic acid is converted to prostaglandin G2 and prostaglandin G2 to prostaglandin H2 by prostaglandin G/H synthase. The precursor of several prostaglandins involved in heat, discomfort, swelling, inflammation, and platelet aggregation is prostaglandin H2. The parent molecule, 6-methoxy-2-naphthylacetic acid, is a prodrug that undergoes hepatic biotransformation to become the active agent (6MNA). NSAIDs have analgesic, antipyretic, and anti-inflammatory actions as a result of a decrease in inflammation.

Dosage & Administration

Osteoarthritis and Rheumatoid Arthritis: The recommended starting dose is 1,000 mg taken as a single dose with or without food. Some patients may obtain more symptomatic relief from 1,500 mg to 2,000 mg per day. Nabumetone can be given in either a single or twice-daily dose. Dosages greater than 2,000 mg per day have not been studied. The lowest effective dose should be used for chronic treatment.  Patients weighing under 50 kg may be less likely to require dosages beyond 1,000 mg; therefore, after observing the response to initial therapy, the dose should be adjusted to meet individual patients’ requirements.

Interaction

According to certain reports, NSAIDs may reduce the antihypertensive impact of ACE inhibitors. In patients taking NSAIDs and ACE inhibitors at the same time, this interaction should be taken into account.

Contraindications

In patients who have a known hypersensitivity to nabumetone or its excipients, nabumetone is not recommended. Patients who have had asthma, urticaria, or allergic responses after using aspirin or other NSAIDs should not be administered napumetone. In these patients, anaphylactic-like reactions to NSAIDs have been observed, which are seldom deadly. In the setting of coronary artery bypass graft (CABG) surgery, nabumetone is contraindicated for the treatment of peri-operative discomfort.

Side Effects

• Diarrhea (14%), dyspepsia (13%), stomach discomfort (12%), constipation, flatulence, nausea, positive stool guaiac, dry mouth, gastritis, stomatitis, vomiting
• Dizziness, headaches, weariness, increased perspiration, sleeplessness, anxiousness, and somnolence are all symptoms of the central nervous system.
• Pruritus, rash, dermatological
• Tinnitus is a type of hearing loss.
• Edema, Edema, Edema, Edema, Edema, Edema

Pregnancy & Lactation

Pregnancy Classification C. There was no evidence of developmental problems in rats and rabbits in reproductive trials. Animal reproductive studies, on the other hand, are not always indicative of human response. In pregnant women, there are no sufficient, well-controlled research. Nabumetone should only be used during pregnancy if the possible benefit outweighs the risk to the baby.

Nursing Mothers: It’s unclear whether this substance is secreted in human milk, although 6MNA is found in breastfeeding rats’ milk. Because many medicines are excreted in human milk and because Nabumetone can produce major side effects in nursing infants, a judgment must be made.

Precautions & Warnings

Nabumetone will not be able to replace corticosteroids or treat corticosteroid deficiency. The abrupt cessation of corticosteroids may cause the condition to worsen. If a choice is made to cease corticosteroids, patients who have been on them for a long time should have their therapy decreased slowly. Because of Nabumetone’s pharmacological efficacy in decreasing fever and inflammation, these diagnostic signals may be less useful in diagnosing complications of presumed noninfectious, painful diseases.

Therapeutic Class

Drugs for Osteoarthritis, Drugs used for Rheumatoid Arthritis

Storage Conditions

Store at 25°C, with excursions to 15-30°C allowed in a tightly sealed container; dispense in a light-resistant container.

Pharmaceutical Name

Eskayef Pharmaceuticals Ltd.