YOUR HEALTH FIRST
YOUR HEALTH FIRST
ZADOL TAB
ACECLOFENAC TABLETS 100 MG
Aceclofenac is an orally administered phenylacetic acid derivative with effects on a variety of inflammatory mediators. It is from the class of non-steroidal anti-inflammatory drug (NSAID), related to diclofenac. Through its analgesic and anti-inflammatory properties, aceclofenac provides symptomatic relief in a variety of painful conditions.
COMPOSITION
Each film coated tablet contains:
Aceclofenac BP 100mg
Excipients.........................................q.s.
PHARMACOLOGY
The mode of action of aceclofenac is largely based on the inhibition of prostaglandin synthesis. Aceclofenac is a potent inhibitor of the enzyme cyclo-oxygenase, which is involved in the production of prostaglandins.
Aceclofenac has been shown to exert effects on a variety of mediators of inflammation. The drug inhibits synthesis of the inflammatory cytokines interleukin (IL)-1ß and tumor necrosis factor and inhibits prostaglandin E (PGE ) production. Effects on 2 2 cell adhesion molecules from neutrophils have also been noted. In vitro data indicate inhibition of cyclo-oxygenase (COX)-1 and 2 by aceclofenac in whole blood assays, with selectivity for COX-2 being evident. In contrast to some other NSAIDs, aceclofenac has shown stimulatory effects on cartilage matrix synthesis,that may be linked to the ability of the drug to inhibit IL-1ß activity. In vitro data indicate stimulation by the drug of synthesis of glycosaminoglycan in osteoarthritic cartilage. There is also evidence that aceclofenac stimulates synthesis of IL-1 receptor antagonist in human articular chondrocytes subjected to inflammatory stimuli and that 4'- hydroxyaceclofenac has chondroprotective properties attributable to suppression of (IL)-1ß mediated promatrix metalloproteinase production and proteoglycan release.
In patients with osteoarthritis of the knee, aceclofenac decreases pain, reduces disease severity and improves the functional capacity of the knee. It reduces joint inflammation, pain intensity and the duration of morning stiffness in patients with rheumatoid arthritis. The duration of morning stiffness and pain intensity are reduced and spinal mobility improved, by aceclofenac in patients with ankylosing hydroxyaceclofenac. These other metabolites account for the fate of approximately 20% of each dose of aceclofenac.
Renal excretion is the main route of elimination of aceclofenac with 70 to 80% of an administered dose found in the urine, mainly as the glucuronides of aceclofenac and its metabolites. Of each dose of aceclofenac, 20% is excreted in the faeces. The plasma elimination half-life of the drug is approximately 4 hours.
INDICATION
Aceclofenac is indicated for the relief of pain and inflammation associated with rheumatoid arthritis, osteoarthritis or ankylosing spondylitis.
CONTRAINDICATIONS
Aceclofenac should not be administered to patients hypersensitive to aceclofenac or other NSAIDs, or patients with a history of aspirin or NSAID-related allergic or anaphylactic reactions or with peptic ulcers or GI bleeding, moderate or severe renal impairment.
WARNINGS
Close medical surveillance is imperative in patients with symptopms indicative of gastrointestinal disorders, with a history suggestive of gastrointestinal ulceration, with ulcerative colitis or with Crohn's disease, bleeding diathesis or haematological abnormalities.
Gastrointestinal bleeding or ulcerative perforation, haematemesis and melaena have in general more serious consequences in the elderly. They can occur at any time during treatment, with or without warning symptoms or previous history. In the rare instances, where gastrointestinal bleeding or ulceration occurs in patients receiving aceclofenac, the drug should be withdrawn. Close medical surveillance is also imperative in patients suffering from severe impairment of hepatic function.
As with other NSAIDs, allergic reactions, including anaphylactic/anaphylactoid reactions, can also occur without earlier exposure to the drug.
PRECAUTIONS:
Aceclofenac should be given with caution to elderly patients with renal, hepatic or cardiovascular impairment and to those receiving other medication. The lowest effective dose should be used and renal function monitored regularly.
The importance of prostaglandins in maintaining renal blood flow should be taken into account in patients with impaired cardiac or renal function, those being treated with diuretics or recovering from major surgery. Effects on renal function are usually reversible on withdrawal of aceclofenac.
Caution should also be exercised in patients with history of coagulation defects and history of liver dysfunction. Renal and hepatic function and blood counts should be monitored during long term treatment. Persistently elevated hepatic enzyme levels necessitate withdrawal of aceclofenac. Aceclofenac may trigger attacks in patients with hepatic porphyria, and reversible inhibition of platelet aggregration may occur with the drug. Refrain from driving or operating machinery if there is feeling of dizziness or sleepiness whilst taking aceclofenac. Do not perform any of these actions until the effects wear off.
Usage in Pregnancy and Lactation:
The drug is not recommended in pregnant or breast feeding women.
Usage in Paediatrics:
There are no clinical data on the use of aceclofenac in children
Usage in Geriatrics:
The pharmacokinetics of aceclofenac are not altered in elderly patients, therefore it is not considered necessary to modify the dose or dose frequency.
As with other non-steroidal anti-inflammatory drugs (NSAIDs), caution should be exercised in the treatment of elderly patients, who are generally more prone to adverse reactions, and who are more likely to be suffering from impaired renal, cardiovascular or hepatic function and receiving concomitant medication.
WARNINGS
Close medical surveillance is imperative in patients with symptopms indicative of gastrointestinal disorders, with a history suggestive of gastrointestinal ulceration, with ulcerative colitis or with Crohn's disease, bleeding diathesis or haematological abnormalities.
Gastrointestinal bleeding or ulcerative perforation, haematemesis and melaena have in general more serious consequences in the elderly. They can occur at any time during treatment, with or without warning symptoms or previous history. In the rare instances, where gastrointestinal bleeding or ulceration occurs in patients receiving aceclofenac, the drug should be withdrawn.
DRUG INTERACTION
Drug interactions associated with aceclofenac are similar to those observed with other NSAIDs.
Aceclofenac may increase plasma concentrations of lithium, digoxin and methotrexate, increase the activity of anticoagulants, inhibit the activity of diuretics, enhance cyclosporin nephrotoxicity and precipitate convulsions when co-administered with quinolone antibiotics. When concomitant administration with potassium sparing diuretics is employed, serum potassium should be monitored. Futhermore, hypo or hypoglycaemia may result from the concomitant administration of aceclofenac and antidiabetic drugs, although this is rare. The coadministration of aceclofenac with other NSAIDs or corticosteroids may result in increased frequency of adverse events. Caution should be exercised if NSAIDs and methotrexate are administered within 2 – 4 hours of each other, since NSAIDs may increase methotrexate plasma levels, resulting in increased toxicity
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PRESENTATION:30 TABLETS (3 BLISTER STRIPS OF 10 TABLETS IN A MONOPACK)
STORAGE: Store below 250C in a dry place. Keep out of reach of children.
NAFDAC REG.NO.: A4-8883
Marketed by :
142 Okporo Road, Port Harcourt,Rivers State, NIGERIAKINGZY PHARMACEUTICALS LTD.
Manufactured For :(A Division of Schwitz Biotech)C/101, Satya Appartments, Near Sai Baba Temple, , AHMEDABAD - 61, GUJARAT, INDIA
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ADVERSE DRUG REACTIONS:
Aceclofenac is well tolerated, with most adverse events being minor and reversible and affecting mainly the GI system.Most common events include dyspepsia, and abdominal pain (≥ 5% incidence). Dizziness, vertigo, pruritus, rash and dermatitis have been reported with aceclofenac, but the incidence of these events is low (< 5%).Faecal blood loss was noted in similar numbers of patients receiving aceclofenac or comparator drugs. Nausea, diarrhoea, flatulence, gastritis, constipation, vomiting and ulcerative stomatitis may also occur with aceclofenac (< 5% incidence).Increases in blood urea nitrogen and blood creatinine levels have also been reported with aceclofenac treatment ( incidence < 5%). As with other NSAIDs, aceclofenac can elevate circulating levels of hepatic enzymes.Although the incidence of GI adverse events with aceclofenac was similar to those of comparator NSAIDs in individual clinical trials, withdrawal rates due to these events were significantly lower with aceclofenac than ketoprofen and tenoxicam. Costs incurred as a result of adverse event management are lower with aceclofenac than with a range of comparator NSAIDs. Althoughstatistical analyses were not consistently available, faecal bleeding and endoscopy studies in humans have indicated overall lessGI bleeding and GI mucosal damage with aceclofenac than with naproxen or diclofenac.The following adverse events (described as most frequent ≥ 5%, occasional < 5% or rare cases < 0.1%) were reported during all clinical trials:
Gastrointestinal disorders:
Most frequent: dyspepsia, abdominal pain..
Occasional: nausea, diarrhoea, flatulence, gastritis, constipation, vomiting, ulcerative stomatitis. Rare cases: pancreatitis, melaena, stomatitis.
Central and peripheral nervous system: Occasional: dizziness, vertigo,
Rare cases: paraesthesia, tremor.Psychiatric: Rare cases: depression, abnormal dreaming, somnolence, insomnia.Skin and appendages: Occasional: pruritus, rash, dermatitis Rare cases: eczemaLiver and biliary: Occasional: hepatic enzymes increasedMetabolic: Occasional: BUN increased, blood creatinine increased. Rare cases: alkaline phospahtase increased, hyperkalaemia
Cardiovascular: Rare cases: oedema (dependent), palpitation, leg cramps, flushing, purpura.Respiratory: Rare cases: dyspnoea, stridor
Blood: Rare cases: anaemia, granulocytopenia, thrombocytopeniaBody as whole, general: Rare cases: headache, fatigue, face, oedema, hot flushes, allergic reaction, weight increase.Other: Rare cases: abnormal vision, abnormal taste
DOSAGE AND ADMINISTRATION:
The usual dose of aceclofenac is 100mg given twice daily by mouth. One tablet in the morning and one in the evening.There is no evidence that the dosage of aceclofenac needs to be modified in the patients with mild renal impairment, but as with other NSAIDs caution should be exercised. There is some evidence that the dose of aceclofenac should be reduced in patients with hepatic impairment and it is suggested that an initial daily dose of 100 mg be used.Aceclofenac tablets should be swallowed whole with a sufficient quantity of liquid. When aceclofenac was administered to fasting and fed healthy volunteers only the rate and not the extent of aceclofenac absorption was affected and as such aceclofenac can be taken with food.
OVERDOSAGE:
Occasional: nausea, diarrhoea, flatulence, gastritis, constipation, vomiting, ulcerative stomatitis. Rare cases: pancreatitis, melaena, stomatitis.Central and peripheral nervous system: Occasional: dizziness, vertigo,Rare cases: paraesthesia, tremorManagement of acute poisoning with NSAIDs essentially consists of supportive and symptomatic measures.There are no human data available on the consequences of aceclofenac overdosage. The therapeutic measures to be taken are: absorption should be prevented, as soon as possible after overdosage by means of gastric lavage and treatment with activatedcharcoal; supportive and symptomatic treatment should be given for complications such as hypotension, renal failure, convulsions, gastrointestinal irritation, and respiratory depression, specific therapies such as forced diuresis, dialysis or haemoperfusion are probably of no help in eliminating NSAIDs due to their high rate of protein binding and extensive metabolism.
Manufactured by :Jay Formulation Ltd1301, Kerala GIDC, Kerala Bavla RoadDist : Ahemedabad - 382 220
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