NACOXIN

Pharmacokinetics
• Absorption: Readily absorbed from gastrointestinal tract
• Peak Plasma Concentration: About 2 to 4 hours
• Protein Binding: 99%
• Distribution: Diffuses into synovial fluid, crosses placenta and distributed into breast milk in small amount
• Metabolism: Liver via conjugation (Matabolites: 6-Desmethylnaproxen, glucuronides conjugates)
• Elimination Half-life: about 12 to 17 hours
• Excretion: Urine (95%), faeces (<5%)

Indications and Dosage
• Pain: 500 mg initially, then 250 mg q6-8 hr or 500 mg q12 hr PRN; not to exceed 1250 mg/day on day 1; subsequent daily doses should not exceed 1000 mg
• Extended release: 750-1000 mg daily; may temporarily increase to 1500 mg/day if tolerated well and clinically indicated
• Rheumatoid arthritis, osteoarthritis, Ankylosing spondylitis: 500-1000 mg/day divided q12 hr; may increase to 1500 mg/day if tolerated well for limited time
• Extended release: 750-1000 mg daily; may temporarily increase to 1500 mg/day if tolerated well and clinically indicated
• Dysmenorrhoea: 500 mg initially, then 250 mg q6-8 hr or 500 mg PO q12 hr(extended release); not to exceed 1250 mg/day on first day; subsequent doses should not exceed 1000 mg/day
• Acute Gout: 750 mg initially, followed by 250 mg q8 hr until attack subsides.
• Extended release: 1000-1500 mg daily, followed by 1000 mg daily until attack subsides
• Migraine (off-label): 750 mg initially, may give additional 250-500 mg if necessary; not to exceed 1250 mg in 24 hr

Side Effects
COMMON (3-9%): Abdominal pain, constipation, dizziness, drowsiness, headache, heartburn, nausea, edema, and dyspnea
OTHERS (1-4%): GI bleeding, GI perforation, Lightheadedness, GI ulcer, diarrhoea, stomatitis, diverticulitis, and hearing disturbances
RARE (<1%): Elevation of serum alanine aminotransferase or aspartate aminotransferase
Pregnancy Category: C

Contraindications
Absolute: Aspirin allergy, perioperative pain in setting of coronary artery bypass graft (CABG) surgery
Relative: Bleeding disorders, delayed esophageal transit, hepatic disease, peptic ulcer, renal impairment, stomatitis, late pregnancy (may cause premature closure of ductus arteriosus)

Precautions
• Use caution in congestive heart failure (CHF), hypertension, renal/hepatic impairment, or aspirin sensitive asthma
• May increase risk of aseptic meningitis, especially in patients with systemic lupus erythematosis and mixed connective tissue disorders
• Prolonged use may increase risk of adverse cardiovascular events
• May cause anaphylactoid reactions, even in patients with no prior exposure to NSAIDs
• Long-term administration of NSAIDs may result in renal papillary necrosis and other renal injury; patients at greatest risk include elderly individuals, those with impaired renal function, hypovolemia, heart failure, liver dysfunction, or salt depletion, and those taking diuretics, angiotensin-converting enzyme inhibitors, or angiotensin-receptor blockers
• May cause drowsiness, dizziness, and blurred vision
• Platelet aggregation and adhesion may be decreased; may prolong bleeding time; monitor closely patients with coagulation disorders
• May increase risk of hyperkalemia in the elderly, renal disease, or diabetics, especially when used concomitantly with drugs that increase hyperkalemia
• May cause serious skin reactions including exfoliative dermatitis, toxic epidermal syndrome, Stevens-Johnson syndrome, and toxic epidermal necrolysis; discontinue therapy at first sign of skin rash
• May cause new-onset of hypertension; monitor blood pressure closely throughout therapy
• OTC use not for children <12 years
• Withhold for at least 4-6 half-lives prior to surgery or dental procedure

Drug Interactions
• Excretion of naproxen is delayed by probeneci resulting in raised plasma concentrations of naproxen.
• Concomitant use of NSAID increases plasma concentration of lithium, methotrexate, and cardiac glycosides.
• Risk of nephrotoxicity may be increased if given with ACE inhibitors, ciclosporin, tacrolimus, or diuretics.
• Increased risk of hyperkalaemia with ACE inhibitors and some diuretics.
• Antihypertensive effects of ACE inhibitors, beta blockers, and diuretics may be reduced.
• Convulsions may occur due to an interaction with quinolones
• NSAID may increase the effect of phenytoin and sulphonylurea antidiabetics.
• Use of more than one NSAID together (including aspirin) should be avoided.
• Risk of gastrointestinal bleeding and ulceration associated with NSAIDs is increased when used with corticosteroids, the SSRIs, the SNRI venlafaxine, the antiplatelets clopidogrel and ticlopidine, iloprost, erlotinib, sibutramine

Pregnancy Category: C

Presentations
NACOXIN 250: 10 X 10’s
NACOXIN SR 500: 10 X 10’s

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