Nabumetone - Uses, Dose, Side effects

Nabumetone is a non-selective COX inhibitor NSAID. It is used to reduce pain, fever, and inflammation in various inflammatory conditions.

Nabumetone Uses:

Arthritis:
- Used for relief of signs and symptoms of osteoarthritis and rheumatoid arthritis.

Nabumetone Dose in Adults

Nabumetone Dose in the treatment of Arthritis:

P/O:

Initial: 1,000 mg as a single dose; dose should be adjusted based on patient's response up to 2,000 mg/day in 1 to 2 divided doses; doses >2,000 mg/day have not been studied.

Note: Patients less than 50 kg are less likely to require doses of more than 1,000 mg per day.

Nabumetone Dose in Children

Not indicated in children.

Pregnancy Risk Factor C

Birth defects were observed in some cases following in utero NSAID treatment in certain studies. However, the data is inconsistent.
Following in utero NSAID use, nonteratogenic effects such as prenatal constriction, persistent pulmonary hypertension, oligohydramnios and necrotizing enterocolitis have been seen in the fetus/neonate.
Additionally, postnatal non-closure of ductus arteriosus may occur. This can be difficult to manage medically.
Avoid using NSAIDs in later stages of pregnancy as they can cause premature closure of ductus arteriosus.
Pregnant women can use NSAIDs to treat mild rheumatoid-arthritis flares. However, it is best to avoid NSAID use early or late in pregnancy.
Women of reproductive age who have been using NSAIDs for a long time may experience infertility. This can be reversed by stopping the drug.
The possibility of miscarriage may increase if NSAIDs are used close to the time of conception.

Nabumetone use during breastfeeding:

It is not known if breast milk contains it.
NSAIDs can be used by postpartum mothers who want to breastfeed.
However, other agents than nabumetone may be preferred (Montgomery 2012).
Women breastfeeding babies with platelet dysfunction and thrombocytopenia should avoid NSAID use (Bloor 2013, Sammaritano 2014.
According to the manufacturer breastfeeding during therapy is a decision that should be made after considering the risks to infants and the benefits to mothers.

Nabumetone Dose in Kidney Disease:

Not recommended for use in patients with advanced renal disease, but the manufacturer of nabumetone does provide some guidelines for adjustment in renal impairment:
- CrCl ≥50 mL/minute:
  - Dosage adjustment not necessary.
- CrCl 30 to 49 mL/minute:
  - Initial maximum dose: 750 mg once a day; maximum daily dose: 1,500 mg per day
- CrCl <30 mL/minute:
  - Initial maximum dose: 500 mg once a day; maximum daily dose: 1,000 mg per day
- Hemodialysis:
  - Nondialyzable
KDIGO 2012 guidelines provide the following recommendations for NSAIDs:
- eGFR 30 to <60 mL/minute/1.73 m²:
  - Temporarily discontinue in patients with intercurrent disease that increases the risk of AKI.
- eGFR <30 mL/minute/1.73 m²:
  - Avoid use.

Nabumetone Dose in Liver disease:

No dosage adjustments provided in the manufacturer’s labeling (data limited in severe impairment); use cautiously.
Prodrug activation and metabolism are hepatic function dependent and may be reduced in severe hepatic impairment.

Common Side Effects of Nabumetone:

Gastrointestinal:
- Diarrhea
- Dyspepsia
- Abdominal Pain

Less Common Side Effects Of Nabumetone:

Cardiovascular:
- Edema
Central Nervous System:
- Dizziness
- Headache
- Drowsiness
- Fatigue
- Insomnia
- Nervousness
Dermatologic:
- Pruritus
- Skin Rash
- Diaphoresis
Gastrointestinal:
- Constipation
- Flatulence
- Nausea
- Occult Blood In Stools
- Gastritis
- Stomatitis
- Vomiting
- Xerostomia
Otic:
- Tinnitus

Contraindications to Nabumetone:

Hypersensitivity to nabumetone and any component of the formulation
History of asthma, urticaria or allergic-type reactions following aspirin use or any other NSAIDs
This is used in conjunction with coronary artery bypass surgery (CABG).
Hypersensitivity to NSAIDs, active pepticule
Recurrent ulceration history or active GI inflammatory diseases
Renal function is severely impaired or deteriorating
A partial or complete syndrome of nasal polyps
Active or significant hepatic impairment
Concurrent use of other NSAIDs

Warnings and precautions

Anaphylactoid reactions
- Patients may experience anaphylactoid reactions even if they have not been exposed to the drug before.
- However, patients who are suffering from " Aspirin Trilogy" (bronchial asthma and aspirin intolerance, rhinitis, etc.) could be at greater risk.
- Patients with bronchospasm or rhinitis or urticaria due to nonsteroidal anti-inflammatory drugs (NSAID) and aspirin therapy are contraindicated.
Cardiovascular events: [US Boxed Warn]
- The increased risk of severe (and possibly fatal) adverse cardiovascular events due to NSAIDs, such as stroke and MI, can be caused by NSAIDs.
- There may be a risk of complications early in treatment.
- These risks may also increase as the duration of the treatment is prolonged.
- The relative risk seems to be the same in people with and without cardiovascular disease, or risk factors for it.
- However, absolute cardiovascular thrombotic events may occur earlier in treatment in patients who have had cardiovascular disease or are at higher risk.
- Exacerbation or new-onset hypertension can occur.
- NSAIDs could also affect the response to ACE inhibitors, thiazide or loop diuretics; may cause cardiovascular events. Monitor BP.
- It may cause fluid retention and sodium buildup; caution is advised for patients with edema.
- Avoid using in the event of heart failure.
- If you have a recent MI, it is best to not use this medication unless the benefits are greater than the risk of developing cardiovascular thrombotic complications.
- To reduce cardiovascular events, use the lowest effective dose for the most time. Consider alternative therapies for high-risk patients.
CNS effects
- This may cause blurred vision, drowsiness, dizziness, blurred sight, or other neurologic effects that could impair your physical or mental capabilities.
- Patients should be cautious about tasks that require mental alertness such as operating machinery or driving.
GI events: [US Boxed Warning]
- NSAIDs increase the risk of severe GI inflammation, ulceration and bleeding (may be fatal); patients older than 65 years old and those with a history peptic ulcer disease or GI bleeding are more at risk.
- These events can occur without warning and at any time during therapy.
- Patients with active GI bleeding should be avoided
- Avoid non-aspirin NSAIDs in patients who have had a history or experience of severe lower GI bleeding.
- Avoid using concurrent therapy if you have a history of GI problems. Concurrent therapy can increase the risk of GI bleeding in patients with advanced hepatic disease and/or corticosteroids.
- To reduce the risk of GI adverse reactions, use the lowest effective dose for the shortest time. Patients at high risk should consider alternate treatments.
- When used concomitantly with aspirin, a substantial increase in the risk of GI complications (eg, ulcer) occurs; concomitant gastroprotective therapy (eg, proton pump inhibitors) should be given.
Hematologic effects
- Patients with coagulation disorders and those on anticoagulants need to be closely monitored for platelet adhesion or aggregation.
- Anemia can occur. Patients on long-term NSAID therapy need to be closely monitored.
- Rarely, NSAIDs have been linked to severe blood dyscrasias, such as thrombocytopenia, agranulocytosis and aplastic anemia.
Hepatic effects
- Use has been associated with transaminase elevations; monitor any patients with abnormal liver function.
- Rare but sometimes fatal hepatic reactions have been reported with NSAIDs. If you notice any signs or symptoms of hepatic diseases or if there are systemic manifestations, stop using NSAIDs immediately.
Hyperkalemia:
- NSAIDs can increase hyperkalemia risk, especially in elderly people, diabetics, kidney disease, and concomitant usage of other agents that induce hyperkalemia (e.g. ACE-inhibitors).
- Pay attention to potassium.
Photosensitivity reactions
- Photosensitivity reactions may occur.
Effects on the renal system:
- NSAIDs can cause impairment of renal function. Dose-dependent decreases may occur in prostaglandin synthesis due to NSAIDs. This may lead to reduced renal blood flow, which may cause renal decompensation.
- Patients with impaired renal function, heart failure, hypovolemia and hepatic impairment, as well as those who take diuretics and ACE inhibitors, are at greater risk for renal toxicity.
- Before starting treatment, hydrate the patient. Monitor RFTs closely.
- Long-term NSAID treatment may cause renal papillary necrosis or other injuries.
Reactions to skin:
- NSAIDs can cause potentially fatal skin adverse reactions, including exfoliative dermatitis (SJS), Stevens-Johnson syndromes (SJS), or toxic epidermal necrolysiss (TEN).
- You should immediately stop using the product if you notice any skin reactions (or hypersensitivity).
Asthma
- Patients with asthma that is aspirin-sensitive should not use this product. Bronchospasm can be severe and possibly fatal.
- Patients with other forms or asthma should be cautious.
Bariatric surgery
- Gastric ulceration: Chronic use of oral nonselective NSAIDs after bariatric surgery should be avoided; the development of anastomotic ulcerations/perforations may occur.
- Short-term use of celecoxib or IV ketorolac is recommended as part of a multimodal pain management strategy for post-op pain.
Coronary bypass surgery for coronary artery bypass: [US Boxed Warn]
- In the case of coronary bypass graft (CABG), surgery, it is not recommended to use.
- Following CABG surgery, the risk of stroke and MI may increase.
Hepatic impairment
- Patients with hepatic impairment should be cautious; patients with advanced hepatic diseases have a greater risk of GI bleeding from NSAIDs.
- Monitor patients with abnormal LFT closely.
Renal impairment
- Patients with moderate impairment (CrCl 30-49 mL/minute), should be cautious. A dosage adjustment may also be necessary.
- Patients with advanced renal disease should be screened; closely monitor if treatment is required.

Nabumetone: Drug Interaction

Risk Factor C (Monitor therapy)
5-Aminosalicylic Acid Derivatives	Nonsteroidal Anti-Inflammatory Agents may enhance the nephrotoxic effect of 5-Aminosalicylic Acid Derivatives.
Agents with Antiplatelet Properties (e.g., P2Y12 inhibitors, NSAIDs, SSRIs, etc.)	May enhance the antiplatelet effect of other Agents with Antiplatelet Properties.
Alcohol (Ethyl)	May enhance the adverse/toxic effect of Nonsteroidal Anti-Inflammatory Agents. Specifically, the risk of GI bleeding may be increased with this combination.
Aliskiren	Nonsteroidal Anti-Inflammatory Agents may diminish the antihypertensive effect of Aliskiren. Nonsteroidal Anti-Inflammatory Agents may enhance the nephrotoxic effect of Aliskiren. Management: Monitor renal function periodically in patients receiving aliskiren and any nonsteroidal anti-inflammatory agent. Patients at elevated risk of renal dysfunction include those who are elderly, are volume depleted, or have pre-existing renal dysfunction.
Aminoglycosides	Nonsteroidal Anti-Inflammatory Agents may decrease the excretion of Aminoglycosides. Data only in premature infants.
Aminolevulinic Acid (Topical)	Photosensitizing Agents may enhance the photosensitizing effect of Aminolevulinic Acid (Topical).
Angiotensin II Receptor Blockers	May enhance the adverse/toxic effect of Nonsteroidal AntiInflammatory Agents. Specifically, the combination may result in a significant decrease in renal function. Nonsteroidal Anti-Inflammatory Agents may diminish the therapeutic effect of Angiotensin II Receptor Blockers. The combination of these two agents may also significantly decrease glomerular filtration and renal function.
Angiotensin-Converting Enzyme Inhibitors	May enhance the adverse/toxic effect of Nonsteroidal Anti-Inflammatory Agents. Specifically, the combination may result in a significant decrease in renal function. Nonsteroidal Anti-Inflammatory Agents may diminish the antihypertensive effect of Angiotensin-Converting Enzyme Inhibitors.
Anticoagulants	Agents with Antiplatelet Properties may enhance the anticoagulant effect of Anticoagulants. Exceptions: Bemiparin; Enoxaparin; Heparin.
Anticoagulants	Nonsteroidal Anti-Inflammatory Agents may enhance the anticoagulant effect of Anticoagulants. Exceptions: Bemiparin; Enoxaparin; Heparin.
Beta-Blockers	Nonsteroidal Anti-Inflammatory Agents may diminish the antihypertensive effect of Beta-Blockers. Exceptions: Levobunolol; Metipranolol.
Bisphosphonate Derivatives	Nonsteroidal Anti-Inflammatory Agents may enhance the adverse/toxic effect of Bisphosphonate Derivatives. Both an increased risk of gastrointestinal ulceration and an increased risk of nephrotoxicity are of concern.
Cephalothin	Agents with Antiplatelet Properties may enhance the adverse/toxic effect of Cephalothin. Specifically, the risk for bleeding may be increased.
Collagenase (Systemic)	Agents with Antiplatelet Properties may enhance the adverse/toxic effect of Collagenase (Systemic). Specifically, the risk of injection site bruising and/or bleeding may be increased.
Corticosteroids (Systemic)	May enhance the adverse/toxic effect of Nonsteroidal AntiInflammatory Agents (Nonselective).
Dasatinib	May enhance the anticoagulant effect of Agents with Antiplatelet Properties. Management: Drugs listed as exceptions to this monograph are discussed in further detail in separate drug interaction monographs.
Deferasirox	Nonsteroidal Anti-Inflammatory Agents may enhance the adverse/toxic effect of Deferasirox. Specifically, the risk for GI ulceration/irritation or GI bleeding may be increased.
Deoxycholic Acid	Agents with Antiplatelet Properties may enhance the adverse/toxic effect of Deoxycholic Acid. Specifically, the risk for bleeding or bruising in the treatment area may be increased.
Desmopressin	Nonsteroidal Anti-Inflammatory Agents may enhance the adverse/toxic effect of Desmopressin.
Digoxin	Nonsteroidal Anti-Inflammatory Agents may increase the serum concentration of Digoxin.
Drospirenone	Nonsteroidal Anti-Inflammatory Agents may enhance the hyperkalemic effect of Drospirenone.
Eplerenone	Nonsteroidal Anti-Inflammatory Agents may diminish the antihypertensive effect of Eplerenone. Nonsteroidal Anti-Inflammatory Agents may enhance the hyperkalemic effect of Eplerenone.
Fat Emulsion (Fish Oil Based	May enhance the adverse/toxic effect of Agents with Antiplatelet Properties.
Felbinac	May enhance the adverse/toxic effect of Nonsteroidal Anti-Inflammatory Agents.
Glucosamine	May enhance the antiplatelet effect of Agents with Antiplatelet Properties.
Haloperidol	Nonsteroidal Anti-Inflammatory Agents may enhance the adverse/toxic effect of Haloperidol. Specifically including drowsiness and confusion.
HydrALAZINE	Nonsteroidal Anti-Inflammatory Agents may diminish the antihypertensive effect of HydrALAZINE.
Ibritumomab Tiuxetan	Agents with Antiplatelet Properties may enhance the adverse/toxic effect of Ibritumomab Tiuxetan. Both agents may contribute to impaired platelet function and an increased risk of bleeding.
Ibrutinib	May enhance the adverse/toxic effect of Agents with Antiplatelet Properties.
Inotersen	May enhance the antiplatelet effect of Agents with Antiplatelet Properties.
Limaprost	May enhance the antiplatelet effect of Agents with Antiplatelet Properties.
Multivitamins/Fluoride (with ADE)	May enhance the antiplatelet effect of Agents with Antiplatelet Properties.
Multivitamins/Minerals (with ADEK, Folate, Iron)	May enhance the antiplatelet effect of Agents with Antiplatelet Properties.
Multivitamins/Minerals (with AE, No Iron)	May enhance the antiplatelet effect of Agents with Antiplatelet Properties.
Naftazone	May enhance the antiplatelet effect of Nonsteroidal Anti-Inflammatory Agents.
Obinutuzumab	Agents with Antiplatelet Properties may enhance the adverse/toxic effect of Obinutuzumab. Specifically, the risk of serious bleeding-related events may be increased.
Omega-3 Fatty Acids	May enhance the antiplatelet effect of Agents with Antiplatelet Properties.
Pentosan Polysulfate Sodium	May enhance the adverse/toxic effect of Agents with Antiplatelet Properties. Specifically, the risk of bleeding may be increased by concurrent use of these agents.
Pentoxifylline	May enhance the antiplatelet effect of Agents with Antiplatelet Properties.
Porfimer	Photosensitizing Agents may enhance the photosensitizing effect of Porfimer.
Potassium-Sparing Diuretics	Nonsteroidal Anti-Inflammatory Agents may diminish the antihypertensive effect of Potassium-Sparing Diuretics. Nonsteroidal Anti-Inflammatory Agents may enhance the hyperkalemic effect of Potassium-Sparing Diuretics.
PRALAtrexate	Nonsteroidal Anti-Inflammatory Agents may increase the serum concentration of PRALAtrexate. More specifically, NSAIDS may decrease the renal excretion of pralatrexate. Management: Closely monitor for increased pralatrexate serum levels and/or toxicity if used concomitantly with an NSAID. Monitor for decreased pralatrexate serum levels with NSAID discontinuation.
Probenecid	May increase the serum concentration of Nonsteroidal Anti-Inflammatory Agents.
Prostacyclin Analogues	May enhance the antiplatelet effect of Agents with Antiplatelet Properties.
Prostaglandins (Ophthalmic)	Nonsteroidal Anti-Inflammatory Agents may diminish the therapeutic effect of Prostaglandins (Ophthalmic). Nonsteroidal Anti-Inflammatory Agents may also enhance the therapeutic effects of Prostaglandins (Ophthalmic).
Quinolones	Nonsteroidal Anti-Inflammatory Agents may enhance the neuroexcitatory and/or seizure-potentiating effect of Quinolones. Nonsteroidal Anti-Inflammatory Agents may increase the serum concentration of Quinolones.
Salicylates	Agents with Antiplatelet Properties may enhance the adverse/toxic effect of Salicylates. Increased risk of bleeding may result.
Serotonin/Norepinephrine Reuptake Inhibitors	May enhance the antiplatelet effect of Nonsteroidal Anti-Inflammatory Agents (Nonselective).
Tacrolimus (Systemic)	Nonsteroidal Anti-Inflammatory Agents may enhance the nephrotoxic effect of Tacrolimus (Systemic).
Thiazide and Thiazide-Like Diuretics	May enhance the nephrotoxic effect of Nonsteroidal AntiInflammatory Agents. Nonsteroidal Anti-Inflammatory Agents may diminish the therapeutic effect of Thiazide and Thiazide-Like Diuretics.
Thrombolytic Agents	Agents with Antiplatelet Properties may enhance the anticoagulant effect of Thrombolytic Agents.
Tipranavir	May enhance the antiplatelet effect of Agents with Antiplatelet Properties.
Tolperisone	Nonsteroidal Anti-Inflammatory Agents may enhance the adverse/toxic effect of Tolperisone. Specifically, the risk of hypersensitivity reactions may be increased. Tolperisone may enhance the therapeutic effect of Nonsteroidal Anti-Inflammatory Agents.
Tricyclic Antidepressants (Tertiary Amine)	May enhance the antiplatelet effect of Nonsteroidal Anti-Inflammatory Agents (Nonselective).
Vancomycin	Nonsteroidal Anti-Inflammatory Agents may increase the serum concentration of Vancomycin.
Verteporfin	Photosensitizing Agents may enhance the photosensitizing effect of Verteporfin.
Vitamin E (Systemic	May enhance the antiplatelet effect of Agents with Antiplatelet Properties.
Risk Factor D (Consider therapy modification)
Apixaban	Nonsteroidal Anti-Inflammatory Agents (Nonselective) may enhance the adverse/toxic effect of Apixaban. Specifically, the risk of bleeding may be increased. Management: A comprehensive risk to benefit assessment should be done for all patients before any concurrent use of apixaban and nonsteroidal anti-inflammatory drugs (NSAIDs). If combined, monitor patients extra closely for signs and symptoms of bleeding.
Bemiparin	Nonsteroidal Anti-Inflammatory Agents may enhance the anticoagulant effect of Bemiparin. Management: Avoid concomitant use of bemiparin and nonsteroidal anti-inflammatory agents (NSAIDs) due to the increased risk of bleeding. If concomitant use is unavoidable, monitor closely for signs and symptoms of bleeding.
Bemiparin	Agents with Antiplatelet Properties may enhance the anticoagulant effect of Bemiparin. Management: Avoid concomitant use of bemiparin with antiplatelet agents. If concomitant use is unavoidable, monitor closely for signs and symptoms of bleeding.
Bile Acid Sequestrants	May decrease the absorption of Nonsteroidal Anti-Inflammatory Agents.
CycloSPORINE (Systemic)	Nonsteroidal Anti-Inflammatory Agents may enhance the nephrotoxic effect of CycloSPORINE (Systemic). Nonsteroidal Anti-Inflammatory Agents may increase the serum concentration of CycloSPORINE (Systemic). CycloSPORINE (Systemic) may increase the serum concentration of Nonsteroidal Anti-Inflammatory Agents. Management: Consider alternatives to nonsteroidal anti-inflammatory agents (NSAIDs). Monitor for evidence of nephrotoxicity, as well as increased serum cyclosporine concentrations and systemic effects (eg, hypertension) during concomitant therapy with NSAIDs.
Dabigatran Etexilate	Nonsteroidal Anti-Inflammatory Agents (Nonselective) may enhance the adverse/toxic effect of Dabigatran Etexilate. Specifically, the risk of bleeding may be increased. Management: A comprehensive risk to benefit assessment should be done for all patients before any concurrent use of dabigatran and nonsteroidal anti-inflammatory drugs (NSAIDs). If combined, monitor patients extra closely for signs and symptoms of bleeding.
Diclofenac (Systemic)	May enhance the adverse/toxic effect of Nonsteroidal Anti-Inflammatory Agents. Management: Seek alternatives to the combined use of diclofenac with other nonsteroidal anti-inflammatory agents (NSAIDs). Avoid the use of diclofenac/misoprostol with other NSAIDs.
Edoxaban	Nonsteroidal Anti-Inflammatory Agents (Nonselective) may enhance the adverse/toxic effect of Edoxaban. Specifically, the risk of bleeding may be increased. Management: A comprehensive risk to benefit assessment should be done for all patients before any concurrent use of edoxaban and nonsteroidal anti-inflammatory drugs (NSAIDs). If combined, monitor patients extra closely for signs and symptoms of bleeding.
Enoxaparin	Nonsteroidal Anti-Inflammatory Agents may enhance the anticoagulant effect of Enoxaparin. Management: Discontinue nonsteroidal anti-inflammatory agents (NSAIDs) prior to initiating enoxaparin whenever possible. If concomitant administration is unavoidable, monitor closely for signs and symptoms of bleeding.
Enoxaparin	Agents with Antiplatelet Properties may enhance the anticoagulant effect of Enoxaparin. Management: Discontinue antiplatelet agents prior to initiating enoxaparin whenever possible. If concomitant administration is unavoidable, monitor closely for signs and symptoms of bleeding.
Heparin	Nonsteroidal Anti-Inflammatory Agents may enhance the anticoagulant effect of Heparin. Management: Decrease the dose of heparin or nonsteroidal anti-inflammatory agents (NSAIDs) if coadministration is required.
Heparin	Agents with Antiplatelet Properties may enhance the anticoagulant effect of Heparin. Management: Decrease the dose of heparin or agents with antiplatelet properties if coadministration is required.
Herbs (Anticoagulant/Antiplatelet Properties) (eg, Alfalfa, Anise, Bilberry)	May enhance the adverse/toxic effect of Agents with Antiplatelet Properties. Bleeding may occur. Management: Avoid combination when possible. If used, monitor more closely for evidence of bleeding. Discontinue herbal products with anticoagulant or antiplatelet actions 2 weeks prior to surgical, dental, or invasive procedures.
Herbs (Anticoagulant/Antiplatelet Properties) (eg, Alfalfa, Anise, Bilberry)	May enhance the adverse/toxic effect of Nonsteroidal Anti-Inflammatory Agents. Bleeding may occur. Management: Concomitant treatment with these agents should generally be avoided. If used concomitantly, increased diligence in monitoring for adverse effects (eg, bleeding, bruising, altered mental status due to CNS bleeds) must be employed.
Lithium	Nonsteroidal Anti-Inflammatory Agents may increase the serum concentration of Lithium.
Loop Diuretics	Nonsteroidal Anti-Inflammatory Agents may diminish the diuretic effect of Loop Diuretics. Loop Diuretics may enhance the nephrotoxic effect of Nonsteroidal Anti-Inflammatory Agents. Management: Monitor for evidence of kidney injury or decreased therapeutic effects of loop diuretics with concurrent use of an NSAID. Consider avoiding concurrent use in CHF or cirrhosis. Concomitant use of bumetanide with indomethacin is not recommended.
Methotrexate	Nonsteroidal Anti-Inflammatory Agents may increase the serum concentration of Methotrexate. Management: Alternative anti-inflammatory therapy should be considered whenever possible, especially if the patient is receiving higher, antineoplastic doses of methotrexate.
Rivaroxaban	Nonsteroidal Anti-Inflammatory Agents (Nonselective) may enhance the adverse/toxic effect of Rivaroxaban. Specifically, the risk of bleeding may be increased. Management: A comprehensive risk to benefit assessment should be done for all patients before any concurrent use of rivaroxaban and nonsteroidal anti-inflammatory drugs (NSAIDs). If combined, monitor patients extra closely for signs and symptoms of bleeding.
Salicylates	Nonsteroidal Anti-Inflammatory Agents (Nonselective) may enhance the adverse/toxic effect of Salicylates. An increased risk of bleeding may be associated with use of this combination. Nonsteroidal Anti-Inflammatory Agents (Nonselective) may diminish the cardioprotective effect of Salicylates. Salicylates may decrease the serum concentration of Nonsteroidal Anti-Inflammatory Agents (Nonselective). Exceptions: Choline Magnesium Trisalicylate.
Selective Serotonin Reuptake Inhibitors	May enhance the antiplatelet effect of Nonsteroidal AntiInflammatory Agents (Nonselective). Nonsteroidal Anti-Inflammatory Agents (Nonselective) may diminish the therapeutic effect of Selective Serotonin Reuptake Inhibitors. Management: Consider alternatives to NSAIDs. Monitor for evidence of bleeding and diminished antidepressant effects. It is unclear whether COX-2-selective NSAIDs reduce risk.
Sincalide	Drugs that Affect Gallbladder Function may diminish the therapeutic effect of Sincalide. Management: Consider discontinuing drugs that may affect gallbladder motility prior to the use of sincalide to stimulate gallbladder contraction.
Sodium Phosphates	May enhance the nephrotoxic effect of Nonsteroidal Anti-Inflammatory Agents. Specifically, the risk of acute phosphate nephropathy may be enhanced. Management: Consider avoiding this combination by temporarily suspending treatment with NSAIDs, or seeking alternatives to oral sodium phosphate bowel preparation. If the combination cannot be avoided, maintain adequate hydration and monitor renal function closely.
Tenofovir Products	Nonsteroidal Anti-Inflammatory Agents may enhance the nephrotoxic effect of Tenofovir Products. Management: Seek alternatives to these combinations whenever possible. Avoid use of tenofovir with multiple NSAIDs or any NSAID given at a high dose.
Vitamin K Antagonists (eg, warfarin)	Nonsteroidal Anti-Inflammatory Agents (Nonselective) may enhance the anticoagulant effect of Vitamin K Antagonists.
Risk Factor X (Avoid combination)
Acemetacin	May enhance the adverse/toxic effect of Nonsteroidal Anti-Inflammatory Agents.
Aminolevulinic Acid (Systemic)	Photosensitizing Agents may enhance the photosensitizing effect of Aminolevulinic Acid (Systemic).
Dexibuprofen	Nonsteroidal Anti-Inflammatory Agents may enhance the adverse/toxic effect of Dexibuprofen.
Dexketoprofen	May enhance the adverse/toxic effect of Nonsteroidal Anti-Inflammatory Agents.
Floctafenine	May enhance the adverse/toxic effect of Nonsteroidal Anti-Inflammatory Agents.
Ketorolac (Nasal)	May enhance the adverse/toxic effect of Nonsteroidal Anti-Inflammatory Agents.
Ketorolac (Systemic)	May enhance the adverse/toxic effect of Nonsteroidal Anti-Inflammatory Agents.
Macimorelin	Nonsteroidal Anti-Inflammatory Agents may diminish the diagnostic effect of Macimorelin.
Mifamurtide	Nonsteroidal Anti-Inflammatory Agents may diminish the therapeutic effect of Mifamurtide.
Morniflumate	May enhance the adverse/toxic effect of Nonsteroidal Anti-Inflammatory Agents.
Nonsteroidal Anti-Inflammatory Agents (COX-2 Selective)	Nonsteroidal Anti-Inflammatory Agents may enhance the adverse/toxic effect of Nonsteroidal Anti-Inflammatory Agents (COX-2 Selective).
Omacetaxine	Nonsteroidal Anti-Inflammatory Agents may enhance the adverse/toxic effect of Omacetaxine. Specifically, the risk for bleeding-related events may be increased. Management: Avoid concurrent use of nonsteroidal antiinflammatory drugs (NSAIDs) with omacetaxine in patients with a platelet count of less than 50,000/uL.
Pelubiprofen	May enhance the adverse/toxic effect of Nonsteroidal Anti-Inflammatory Agents.
Phenylbutazone	May enhance the adverse/toxic effect of Nonsteroidal Anti-Inflammatory Agents.
Talniflumate	May enhance the adverse/toxic effect of Nonsteroidal Anti-Inflammatory Agents.
Tenoxicam	May enhance the adverse/toxic effect of Nonsteroidal Anti-Inflammatory Agents.
Urokinase	Agents with Antiplatelet Properties may enhance the anticoagulant effect of Urokinase.
Zaltoprofen	May enhance the adverse/toxic effect of Nonsteroidal Anti-Inflammatory Agents.

Monitoring parameters:

CBC
Chemistry profile
Occult blood loss
Periodic liver function test
Renal function (urine output, serum BUN and creatinine)
Signs or symptoms of GI bleeding and/or hepatic impairment
Blood pressure
Periodic ophthalmic exam with long-term therapy.

How to administer Nabumetone?

Administer with or without food

Mechanism of action of Nabumetone:

Reversible inhibition of cyclooxygenase-1 (COX-1) and 2 (COX-2), enzymes. This results in lower formation prostaglandin precursors
Antipyretic, analgesic and anti-inflammatory properties
Other proposed mechanisms not fully elucidated (and possibly contributing to the anti-inflammatory effect to varying degrees), include inhibiting chemotaxis, altering lymphocyte activity, inhibiting neutrophil aggregation/activation, and decreasing proinflammatory cytokine levels.

Absorption:

Well absorbed from GI tract

The onset of action:

Several days

Distribution:

Diffusion occurs readily into synovial fluid
V : 6MNA: 29 to 82 L

Protein binding:

6MNA: >99%

Metabolism:

It is a prodrug, rapidly metabolized in the liver to an active metabolite [6-methoxy-2naphthylacetic acid (6MNA)] and inactive metabolites
Extensive first-pass effect
~35% converted to 6MNA and 50% converted to unidentified metabolites

Half-life elimination:

6MNA: ~24 hours
The terminal half-life was increased ~50% in patients with CrCl 30 to 49 mL/minute

Time to peak, serum: 6MNA: P/O:

Adults: 2.5 to 3 hours
Elderly: 4 hours

Excretion:

6MNA: Urine (~80%) and feces (9%)

International Brands of Nabumetone:

MYLAN-Nabumetone
NU-Nabumetone
PMS-Nabumetone
TEVA-Nabumetone
Axotone
Balmox
Bumetone
Gambaran
Goflex
Labuton
Lavex
Nabone
Nabuco
Nabucox
Nabuflam
Nabugesic
Naburen
Nabuser
Nabuton
Nabutone
Nametone
No-Ton
Noac
Noracet
Relafen
Relif
Relifen
Relifex
Relisan
Relitone
Rheumaton
Rodanol
Synmeton
Tontec
Unimetone

Nabumetone Brand Names in Pakistan:

Nabumetone 500 mg Tablets
Niltisl	Genome Pharmaceuticals (Pvt) Ltd
Relifex	Glaxosmithkline

Nabumetone - Uses, Dose, Side effects

Nabumetone Uses:

Arthritis:

Nabumetone Dose in Adults

Nabumetone Dose in the treatment of Arthritis:

Nabumetone Dose in Children

Pregnancy Risk Factor C

Nabumetone use during breastfeeding:

Nabumetone Dose in Kidney Disease:

KDIGO 2012 guidelines provide the following recommendations for NSAIDs:

Nabumetone Dose in Liver disease:

Common Side Effects of Nabumetone:

Gastrointestinal:

Less Common Side Effects Of Nabumetone:

Cardiovascular:

Central Nervous System:

Dermatologic:

Gastrointestinal:

Otic:

Contraindications to Nabumetone:

Warnings and precautions

Anaphylactoid reactions

Cardiovascular events: [US Boxed Warn]

CNS effects

GI events: [US Boxed Warning]

Hematologic effects

Hepatic effects

Hyperkalemia:

Photosensitivity reactions

Effects on the renal system:

Reactions to skin:

Asthma

Bariatric surgery

Coronary bypass surgery for coronary artery bypass: [US Boxed Warn]

Hepatic impairment

Renal impairment

Monitoring parameters:

How to administer Nabumetone?

Mechanism of action of Nabumetone:

International Brands of Nabumetone:

Nabumetone Brand Names in Pakistan:

Nabumetone 500 mg Tablets

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