Aceclofenac Sustained Release Tablets 200 mg
Each film-coated sustained-release tablet contains:
Aceclofenac BP 200 mg
It is a Phenylacetic acid derivative [[[2-[(2,6 Dichlorophenyl)amino]Phenyl]acetyl]oxy]acetic acid.
Non Steroidal Anti-inflammatory Drug
The mode of action of aceclofenac is largely based on the inhibition of prostaglandin synthesis. Aceclofenac is a potent inhibitor of the enzyme cyclooxygenase, which is involved in the production of prostaglandins. The drug inhibits synthesis of the inflammatory cytokines interleukin (IL)-1 and tumor necrosis factor and prostaglandin E2 (PGE2) production. Effects on cell adhesion molecular from neurophils have also been noted. In vitro data indicate inhibition of cyclooxygenase (Cox)-1 and 2 by aceclofenac in whole blood assays, with selectivity for Cox-2 being evident. Aceclofenac has shown stimulatory effects on cartilage matrix synthesis that may be linked to the ability of the drug to inhibit IL-1 activity. In vitro data indicate stimulation by the drug of synthesis of glycosaminoglycan in osteoarthritic cartilage. There is also evidence that aceclofenac stimulates the synthesis of IL-1 receptor antagonist in human articular chondrocytes subjected to inflammatory stimuli and that 4’-hydroxyacelofenac has chondroprotective properties attributable to suppression of IL-1 mediated promatrix metalloproteinase production and proteoglycan release.
Aceclofenac is rapidly and completely absorbed after oral administration, peak plasma concentrations are reached 1 to 3 hours after an oral dose. The drug is highly protein bound (7.99%). The presence of food does alter the extent of absorption of aceclofenac but the absorption rate is reduced. The plasma concentration of aceclofenac was approximately twice that in synovial fluid after multiple doses of the drug in patient with knee pain and synovial fluid effusion. Aceclofenac is metabolized to a major metabolite, 4-hydroxyaceclofenac and to a number of other metabolites including 5-hydroxyaceclofenac, 4’-hydroxydiclofenac, diclofenac and 5-hydroxydiclofenac. 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.
For the relief of pain and inflammation in both acute and chronic pain like osteoarthritis, rheumatoid arthritis, ankylosing spondylitis, dental pain, post-traumatic pain, low back pain, gynaecological pain etc.
Hypersensitive to the drugs (may precipitate attacks of asthma, bronchospasm, acute rhinitis or urticaria), GI bleeding moderate to severe renal impairment, last three months of pregnancy.
Aceclofenac is well tolerated, with most adverse events being minor and reversible and affecting mainly the GI system. Most common events include dyspepsia (7.5%), abdominal pain (6.2%), nausea (1.5%), diarrhea (1.5%), flatulence (0.8%), gastritis (0.6%), constipation (0.5%), vomiting (0.5%), ulcerative stomatitis (0.1), pancreatitis (0.1%). Although the incidence of gastro intestinal adverse events with aceclofenac was similar to those of comparator NSAIDS in individual clinical trials, withdrawal rates due to these events were significantly lower in aceclofenac than with ketoprofen and tenoxicam. Other adverse effect, which is not common such as dizziness (1%), vertigo (0.3%), and rare cases: par aesthesia and tremor.
Cautiously administer to patients with gastro-intestinal disease, history of peptic ulceration, cerebro-vascular bleeding, ulcerative colitis, Crohn’s disease, SLE, porphyria, hematopoietic-or coagulation-disorders. The dose should be reduced in patients with mild to moderate impairment of hepatic, renal or cardiac functional impairment. The use of NSAIDs may result in deterioration of renal function and fluid retention.
PREGNANCY AND LACTATION
Pregnancy: There is no information on the use of aceclofenac during pregnancy. Aceclofenac should not be administered during pregnancy unless there are compelling reasons to do so. The lowest effective dose should be administered.
Lactation: There is no information on the secretion of aceclofenac in breast milk. The use of aceclofenac should therefore be avoided during lactation unless potential benefits to the mother outweigh the possible risks to the children.
Aceclofenac may increase the plasma concentration of lithium & digoxin, concomitant use with diuretics may inhibit the activity of diuretics. Serum potassium should be monitored when used with potassium sparing diuretics. The activity of anticoagulants may be enhanced when used concomitantly with aceclofenac. Convulsion may occur due to interaction between quinolones and NSAIDs.
DOSAGE AND ADMINISTRATION
The usual dose of aceclofenac is 200 mg 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 patients with mild renal impairment, but as with other NSAIDS caution should be exercised.
Adults: 200 mg orally b.i.d. Aceclofenac can be taken before or after food.
Children: There is no clinical data on the use of aceclofenac in children.
Hepatic insufficiency: Dosage reductions are recommended in patients with hepatic impairment, with a suggested initial dosage of 100 mg/day.
OVERDOSAGE, SYMPTOMS AND ANTIDOTE
There are no human data available on the consequences of aceclofenac overdosage. The symptoms could be: Nausea, vomiting, stomach pain, dizziness, somnolence and headache. Treatment: If required, gastric lavage, charcoal in repeated doses. Antacids when necessary and other symptomatic treatment.
Store below 30°C. Keep out of reach of children.
DATE OF PUBLICATION
NAFDAC Reg. No. : B4-0219
MICRO LABS LIMITED-UNIT III
R.S. No. 63/3&4, Thiruvandar Koil,
Pondicherry-605 102. INDIA.