ACENOL 200 Tablet
197, Muyibi Street, Olodi-Apapa, Lagos. 57B, Coker Road, Ilupeju, Lagos
Tel: 234-80-34731163, 234-1-7765232
Saga Laboratories Ltd. Survey No. 198/2 & 198/3, Chachrawadi Vasna., Ta. Sanand, Dist. Ahmedabad 382210, India.
Dosage Form, Composition & NAFDAC Registration Number (NRN)
Tablet (NRN: ): Each uncoated sustained release tablet contains: Aceclofenac BP 200 mg
Pack size: Blister strips of 1 x 10 tablets
Aceclofenac is a non-steroidal agent with marked anti-inflammatory and analgesic properties. The mode of action of Aceclofenac is largely based on the inhibition of prostaglandin synthesis. Acecfenanc is a potent inhibitor of the enzyme cyclo-oxygenase, which is involved in the production of prostaglandins.
Pharmacokinetic properties After oral administration.
Aceclofenac is rapidly and completely absorbed as unchanged drug. Peak plasma concentration are reached approximately 1.25 to 3.00 hours following ingestion. Aceclofenac penetrates into the synovial fluid, where the concentrations reach approximately 57% of those in plasma. The volume of distribution is approximately 25 L. The mean (geometrical) plasma elimination half-life is 2.30 hours.
Aceclofenac is highly protein-bound (>99%). Aceclofenac circulates mainly as unchanged drug. 4’-Hydroxyaceclofenac is the main metabolite detected in plasma. Approximately two – thirds of the administered dose is excreted via the urine, mainly as hydroxymetabolites. No changes in the pharmacokinetics of Aceclofenac have been detected in the elderly.
Aceclofenac 200 mg Tablets are indicated for the relief of pain and inflammation in osteoarthritis, rheumatoid arthritis and ankylosing spondylitis.
Hypersensitivity to any of the constituents NSAIDs are contraindicated in patients who have previously shown hypersensitivity reactions (e.g. asthma, rhinitis, angioedema or urticaria) in response to ibuprofen, aspirin or other non-steroidal anti-inflammatory drugs. Severe hepatic and cardiac failure.
Moderate to severe renal failure During the last trimester of pregnancy Active or previous peptic ulcer History of upper gastrointestinal bleeding or perforation, related to previous NSAIDs therapy. Use with concomitant NSAIDs including cyclooxygenase 2 specific inhibitors is not permitted
Undesirable effects may be minimized by using the minimum effective dose for the shortest possible duration.
Elderly: The elderly have an increased frequency of adverse reactions to NSAIDs especially gastrointestinal bleeding and perforation which may be fatal.
Respiratory disorders: Caution is required if administered to patients suffering from, or with a previous history of, bronchial asthma since NSAIDs have been reported to precipate bronchospasm in such patients.
Cardiovascular, Renal and Hepatic Impairment: The administration of NSAID may cause a dose dependent reduction in prostaglandin formation and precipitate renal failure. Patients at greatest risk of this reaction are those with impaired renal function. Cardiac impairment, liver dysfunction, those taking diuretics and the elderly. Renal function should be monitored in these patients.
Effects on renal function are usually reversible on withdrawal of Aceclofenac. If abnormal liver function tests persists or worsen, clinical signs or symptoms consistent with liver disease develop or if other manifestations occur (eosinophilia, rash), Aceclofenac should be discontinued.
Hepatitis may occur without prodromal symptoms. Use of Aceclofenac in patients with hepatic porphyria may trigger an attack. Caution in patients with a history of hypertension and/or heart failure as fluid retention and oedema have been reported in association with NSAIDs therapy.
Haematological: Aceclofenac may reversibly inhibit platelet aggregation.
Long-term treatment: All patients who are receiving NSAIDs should be monitored as a precautionary measure e.g. renal function (elevation of liver enzymes may occur) and blood counts.
Interaction with other medicinal products and other forms interaction Lithium:
Aceclofenac, like many NSAIDs may increase plasma concentrations of lithium.
Cardiac Glycosides: Through their renal effects, NSAIDs may increase plasma glycosides (including digoxin) levels, exacerbate cardiac failure and reduced the glomerular filtration rate in patients receiving glycosides.
Diuretics: Aceclofenac, like other NSAIDs, may inhibit the activity of diuretic. Although it was not shown to affect blood pressure control when co-administered with bendroflumethiazide, interaction with other diuretics cannot be ruled out. When concomitant administration with potassium sparing diuretics is employed, serum potassium should be monitored. Diuretics can increase the risk of nephrotoxicity of NSAIDs.
Anticoagulants: Like other NSAIDs, Aceclofenac may enhance the activity of anticoagulant such as warfarin (See section 4.4- special warnings and precautions for use). Close monitoring of patients on combined anticoagulant and Aceclofenac therapy should be undertaken.
Antidiabetic agents: Clinical studies have shown that diclofenac can be given together with oral antidiabetic agents without influencing their clinical effects. However, there have been isolated reports of hypoglycaemic and hyperglycaemic effects.
Thus with Aceclofenac, consideration should be given to adjustment of the dosage of hypoglycaemic agents. Methotrexate: Caution should be exercised if NSAIDs and methotrexate are administered within 24 hours of each other, since NSAIDs may increase methotrexate plasma levels, resulting in increased toxicity.
Mifepristone: NSAIDs should not be use for 8-12 days after mifepristone administration as NSAIDs can reduce the effect of NSAIDs on renal prostaglandins.
Quinolone antimicrobials: Convulsions may occur due to an interaction between quinolones and NSAIDs. This may occur in patients with or without a previous history of epilepsy or convulsions. Therefore, caution should be exercised when considering the use of a quinolone in patients who are already receiving a NSAID.
Other analgesic including cyclooxygenase – 2 selective inhibitors:
Avoid concomitant use of two or more NSAIDs (including aspirins) as this may increase the risk of adverse effects.
Anti-hypertensive: Reduce anti-hypertensive effect.]
Corticosteroids: Increased risk of gastrointestinal ulceration or GI bleeding.
Tacrolimus: Possible increased risk of haematological toxicity when NSAIDs are given with zidovudine. There is evidence of an increased risk of haemarthroses and haematoma in HIV (+) haemophiliacs receiving concurrent treatment with zidovudine and ibuprofen.
Ritonavir: Plasma concentration of Aceclofenac possibly increased by ritonavir.
Pregnancy and Lactation
Pregnancy abnormalities have been reported in association with NSAID administration in man; however, these are low in frequency and do not appear to follow any discernible pattern. In view of the known effects of NSAIDs on the foetal cardiovascular system (risk of closure of the ductus arteriosus), use in the last trimester of pregnancy is contraindicated. The onset of labour may be delayed and the duration increased with an increased bleeding tendency in both mother and child. NSAIDs should not be used during the first two trimesters of pregnancy or labour unless the potential benefit to the patient outweighs the potential risk to the foetus.
There is no information on the secretion of Aceclofenac to breast milk; there was however, no notable transfer of radio-labelled (14C) Aceclofenac to the milk of lactating rats. In limited studies so far available, NSAIDs can appear in breast milk in very low concentration: NSAIDs should, if possible, be avoided when breast-feeding.
The majority of adverse reactions reported have been reversible and of a minor nature. The most frequent are gastro-intestinal disorders, in particular dyspepsia, abdominal pain, nausea and diarrhoea, and occasional occurrence of dizziness. Dermatological complaints including pruritus and rash and abnormal hepatic enzyme and serum creatinine levels also been reported. If serious side effects occur, Aceclofenac should be withdrawn.
Dosage & Administration
Posology and method of administration Aceclofenac tablets are supplied for oral administration and should be swallowed whole with a sufficient quantity of liquid. Aceclofenac should be taken preferably with or after food. Adults The recommended dose is 200 mg once daily.
There are no human data available on the consequence of Aceclofenac overdose.
a) Symptoms Symptoms include headache, nausea, vomiting, epigastric pain, gastrointestinal bleeding, rarely diarrhea, disorientation, excitation, coma, drowsiness, dizziness, tinnitus, fainting, occasionally convulsions. In cases of significant poisoning acute renal failure and liver damage are possible.
b) Therapeutic measure Patients should be treated symptomatically as required.
Store in a cool and dry place. Keep medicine out of reach of children