Adult: 600 mg daily in 2-3 divided doses. Use the lowest effective dose for the shortest possible duration needed to control symptoms. Elderly: Use the lowest effective dose for the shortest possible duration of treatment.
Special Patient Group
In elderly patient with cardiac impairment: Recommended dose: Reduce to 200 mg bid.
Renal Impairment
Mild to moderate: Elderly: Recommended dose: Reduce to 200 mg bid. Severe: Contraindicated.
Hepatic Impairment
Mild to moderate: Elderly: Recommended dose: Reduce to 200 mg bid. Severe: Contraindicated.
Administration
Should be taken with food.
Contraindications
Hypersensitivity to tiaprofenic acid or other NSAIDs. Active or history of recurrent peptic ulcer or gastrointestinal haemorrhage (≥2 distinct episodes of proven ulceration or bleeding), active gastrointestinal inflammatory disease, history of gastrointestinal bleeding or perforation (related to previous NSAIDs therapy), active bladder or prostatic disease or symptoms, history of recurrent urinary tract disorder, severe heart failure; previous hypersensitivity reactions (e.g. asthma, rhinitis, angioedema, urticaria) to aspirin or other NSAIDs, existing or history of asthma. Severe renal and hepatic impairment. Pregnancy (3rd trimester). Concurrent use with other NSAIDs (including cyclooxygenase-2 selective inhibitors) and high-dose salicylates.
Special Precautions
Patient with history of ulcer (especially if complicated with haemorrhage or perforation), history of gastrointestinal disease (e.g. ulcerative colitis, Crohn’s disease); recurrent rhinosinusitis, nasal polyposis or chronic urticaria; coagulation disorder, intracranial haemorrhage, risk factors for CV disease (e.g. hyperlipidaemia, diabetes mellitus, smoking), mild to moderate CHF, uncontrolled hypertension, established ischaemic heart disease, peripheral arterial disease, cerebrovascular disease, history of hepatic insufficiency, SLE, mixed connective tissue disorders, coronavirus disease 2019 (COVID-19). Debilitated and dehydrated patients. Patient undergoing surgery or dental procedures. Not recommended in women attempting to conceive. Consider discontinuation in women who have difficulties conceiving or those undergoing investigation of infertility. Mild to moderate renal and hepatic impairment. Elderly. Pregnancy (1st-2nd trimester) and lactation.
Adverse Reactions
Significant: Bronchospasm, Na and water retention with oedema, severe cystitis or other urinary tract symptoms (e.g. bladder pain, dysuria, urinary frequency, haematuria), renal failure, arterial thrombotic events (e.g. MI, stroke), new-onset or worsening of hypertension, hyperkalaemia, blurred or diminished vision; renal papillary necrosis (prolonged use); impaired female fertility, decreased platelet adhesion and aggregation. Rarely, aseptic meningitis, potentially severe blood dyscrasias (e.g. agranulocytosis, thrombocytopenia, aplastic anaemia), jaundice. Ear and labyrinth disorders: Vertigo, tinnitus. Gastrointestinal disorders: Upper abdominal pain, nausea, vomiting, dyspepsia, diarrhoea, constipation, pancreatitis. Immune system disorders: Non-specific allergic reactions, angioedema. Investigations: Abnormal LFT. Nervous system disorders: Dizziness, headache, drowsiness. Renal and urinary disorders: Tubulointerstitial nephritis, nephrotic syndrome. Respiratory, thoracic and mediastinal disorders: Dyspnoea. Skin and subcutaneous tissue disorders: Rash, pruritus, urticaria, alopecia, photosensitivity reaction. Potentially Fatal: Gastrointestinal bleeding, ulceration or perforation; asthmatic and anaphylactoid reactions (in patients with aspirin triad), drug reaction with eosinophilia and systemic symptoms (DRESS). Rarely, exfoliative dermatitis, Stevens-Johnson syndrome, toxic epidermal necrolysis, hepatitis.
Patient Counseling Information
This drug may cause dizziness, drowsiness, fatigue and blurred vision, if affected, do not drive or operate machinery.
Monitoring Parameters
Monitor CBC, occult blood loss, LFTs (periodically), renal function (e.g. urine output, BUN, creatinine), electrolytes; response to therapy (e.g. pain, range of motion, grip strength, mobility), inflammation. Observe for weight gain, signs of oedema, bleeding or bruising; signs and symptoms of gastrointestinal effects (e.g. abdominal pain, bleeding, dyspepsia); mental confusion or disorientation. Perform ophthalmic exams periodically (prolonged use); urinalysis and urine culture (if urinary symptoms occur).
Overdosage
Symptoms: Headache, nausea, vomiting, epigastric pain, gastrointestinal bleeding, diarrhoea (rare), disorientation, excitation, drowsiness, dizziness, tinnitus, fainting, convulsion (occasional), coma; in cases of significant poisoning, acute renal failure and liver damage may occur. Management: Symptomatic and supportive treatment. Administer activated charcoal within 1 hour of ingesting a potentially toxic amount. Alternatively, gastric lavage may be performed in adults within 1 hour of ingestion. Ensure good urine output. Administer IV diazepam for frequent or prolonged convulsions. Closely monitor hepatic and renal function. Observe patient for at least 4 hours following ingestion of potentially toxic amount.
Drug Interactions
Increased risk of ulceration or bleeding with oral corticosteroids, anticoagulants (e.g. heparin, warfarin, ticlopidine, clopidogrel, dabigatran, apixaban, rivaroxaban, edoxaban), SSRIs, anti-platelet agents (e.g. aspirin), thrombolytics, nicorandil, pentoxifylline. May increase the plasma concentration of cardiac glycosides, lithium, methotrexate. Increased risk of nephrotoxicity with tacrolimus, ciclosporin, tenofovir disoproxil fumarate. Increased risk of haematological toxicity with zidovudine. May increase the risk of developing convulsion with quinolone antibiotics. May reduce the effects of antihypertensive agents (e.g. ACE inhibitors, angiotensin II receptor antagonists, β-blockers), diuretics, and mifepristone (avoid tiaprofenic acid for at least 8-12 days after mifepristone use). Decreased metabolism and elimination with probenecid. May inhibit the metabolism of sulfonylurea drugs. May decrease the elimination of aminoglycosides. Potentially Fatal: Increased risk of adverse effect (particularly upper gastrointestinal disorders) with other NSAIDs and high-dose salicylates.
Food Interaction
Delayed absorption with food.
Lab Interference
May result in false-positive aldosterone/renin ratio (ARR).
Action
Description: Tiaprofenic acid is a propionic acid derivate that has antipyretic, analgesic and anti-inflammatory properties. It acts by reversibly inhibiting cyclooxygenase-1 and 2 (COX-1 and 2) enzymes resulting in reduced formation of prostaglandin precursors. Pharmacokinetics: Absorption: Rapidly absorbed from the gastrointestinal tract. Delayed absorption with food. Time to peak plasma concentration: 30-90 minutes. Distribution: Crosses the placenta and enters breast milk. Plasma protein binding: Approx 98%. Metabolism: Metabolised into inactive metabolites (minimal). Excretion: Via urine (50% as unchanged drug, <10% as metabolites). Elimination half-life: Approx 2 hours.
Chemical Structure
Tiaprofenic acid Source: National Center for Biotechnology Information. PubChem Compound Summary for CID 5468, Tiaprofenic acid. https://pubchem.ncbi.nlm.nih.gov/compound/Tiaprofenic-acid. Accessed June 24, 2021.
Storage
Store below 25°C. Protect from light and high humidity.
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