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Indications and Dosage
Oral
Pain and inflammation associated with musculoskeletal and joint disorders Adult: Dosage is individualised depending on the severity of symptoms. Usual dose: 60 mg tid. May give up to 120 mg as a single dose for the treatment of severe symptoms. Max: 180 mg daily.
Elderly: Initiate at the lowest effective dose. |
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Renal Impairment
Severe: Contraindicated.
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Hepatic Impairment
Severe: Contraindicated.
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Administration
Should be taken with food. Take w/ or immediately after meals.
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Contraindications
Hypersensitivity to loxoprofen. History of hypersensitivity, history of or existing NSAID-induced (e.g. aspirin) asthma; severe cardiac function failure, severe blood disorders, active peptic ulcer. Severe renal and hepatic impairment. Concomitant use with other NSAIDs.
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Special Precautions
Patient with a history of peptic ulcer including peptic ulcer associated NSAID use; blood disorders; bronchial asthma; ulcerative colitis, Crohn's disease. May mask the signs and symptoms of infection. Mild to moderate renal and hepatic impairment. Elderly. Pregnancy and lactation.
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Adverse Reactions
Significant: Gastrointestinal bleeding, gastrointestinal perforation, small and/or large intestinal stenosis and/or obstruction; CHF; hypersensitivity reactions, shock, anaphylaxis; Stevens-Johnson syndrome, toxic epidermal necrolysis, erythema multiforme; agranulocytosis, haemolytic anaemia, leucopenia, thrombocytopenia, aplastic anaemia; interstitial pneumonia, asthmatic attack; acute kidney injury, nephrotic syndrome, interstitial nephritis; hepatic function disorder, jaundice, increased transaminases; aseptic meningitis; rhabdomyolysis; drowsiness.
Blood and lymphatic system disorders: Eosinophilia. Cardiac disorders: Palpitations. Gastrointestinal disorders: Constipation, heartburn, stomatitis, peptic ulcer, dyspepsia, thirst, abdominal distention, small and/or large intestine ulcer. General disorders and administration site conditions: Malaise. Nervous system disorders: Headache, numbness, dizziness, somnolence. Renal and urinary disorders: Haematuria, proteinuria, dysuria. Respiratory, thoracic and mediastinal disorders: Chest pain. |
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Monitoring Parameters
In patients receiving long-term therapy, monitor urinalysis, haematological tests, and LFTs.
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Drug Interactions
May enhance the anticoagulant effect of coumarin anticoagulants (e.g. warfarin). May increase the risk of bleeding with factor Xa inhibitor. May enhance the hypoglycaemic effect of sulfonylureas (e.g. glimepiride, tolbutamide). May enhance the convulsant effect of quinolone antimicrobial agents (e.g. levofloxacin). May increase the plasma concentration of methotrexate and lithium. May reduce the diuretic antihypertensive effect of thiazide diuretics (e.g. hydrochlorothiazide). May worsen the renal function and decrease the therapeutic effect of antihypertensive drugs (e.g. ACE inhibitors, angiotensin II receptor antagonists).
Potentially Fatal: May increase the risk of adverse effects with other NSAIDs (e.g. mefenamic acid, aspirin). |
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Food Interaction
May enhance toxic effects with alcohol.
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Lab Interference
May result in false-positive aldosterone/renin ratio (ARR).
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Action
Description:
Mechanism of Action: Loxoprofen is a propionic acid-based nonsteroidal anti-inflammatory drug (NSAID). After absorption, it is rapidly metabolised to an active metabolite (trans-alcohol form) which potently prevents prostaglandin biosynthesis by nonselective inhibition of cyclooxygenase (COX) enzymes, thus resulting in its anti-inflammatory and analgesic effects. Pharmacokinetics: Absorption: Rapidly absorbed from the gastrointestinal tract. Time to peak plasma concentration: Approx 30 minutes (loxoprofen); approx 50 minutes (active metabolite). Metabolism: Rapidly metabolised in the liver by carbonyl reductase into the trans-alcohol form (active metabolite). Excretion: Via urine (approx 50%). Elimination half-life: Approx 75 minutes. |
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Chemical Structure
 Source: National Center for Biotechnology Information. PubChem Compound Summary for CID 3965, Loxoprofen. https://pubchem.ncbi.nlm.nih.gov/compound/Loxoprofen. Accessed Jan. 31, 2024. |
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Storage
Store below 30°C.
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References
Greig, SL, Garnock-Jones, KP. Loxoprofen: A Review in Pain and Inflammation. Clinical Drug Investigation. 2016;36(9):771-781. doi: 10.1007/s40261-016-0440-9. Accessed 09/11/2023. PMID: 27444038 Paudel, S, Shrestha, A, Cho, P, et al.. Assessing Drug Interaction and Pharmacokinetics of Loxoprofen in Mice Treated with CYP3A Modulators. Pharmaceutics. 2019;11(9). doi: 10.3390/pharmaceutics11090479. Accessed 09/11/2023. PMID: 31527544 Anon. Loxoprofen. Lexicomp Online. Hudson, Ohio. Wolters Kluwer Clinical Drug Information, Inc. https://online.lexi.com. Accessed 09/11/2023. Buckingham R (ed). Loxoprofen Sodium. Martindale: The Complete Drug Reference [online]. London. Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 09/11/2023. Japrolox Tablets (Daiichi Sankyo Propharma Co., Ltd.). MIMS Thailand. http://www.mims.com/thailand. Accessed 10/11/2023. Loxotop Pap 100 mg Patch (Zuellig Pharma Sdn Bhd). National Pharmaceutical Regulatory Agency - Ministry of Health Malaysia. https://www.npra.gov.my. Accessed 09/11/2023.
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