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University Of Nairobi
Aceclofenac is an orally administered phenyl acetic acid derivatives with effects on a variety of inflammatory mediators.
Aceclofenac contains not less than 99.0% and not more than the equivalent of 101.0 percent of 2-[[2-[2-[(2, 6-dichlorophenyl) amino] phenyl] acetyl] oxy] acetic acid.
It is a white or almost white crystalline powder. It is an effective analgesic and anti-inflammatory agent with a good tolerability profile. Through its analgesic and anti-inflammatory properties, Aceclofenac provides symptomatic relief in a variety of painful conditions. A reduction in the stimulated generation of reactive oxygen species (O2), which may play a role in joint damage, was observed after 15 days in these patients, but after 180 days. At day 180, O2 release was similar to that seen in a group of 41 healthy untreated individuals.
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 Drugs 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.
In patients with osteoarthritis of the knee, Aceclofenac decrease 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 spondylitis.
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 (79.9%). 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.
Aceclofenac may increase plasma concentrations of lithium, digoxin and methotrexate, increase the activity of anticoagulant, inhibits the activity of diuretics, enhance cyclosporin nephrotoxicity and precipitate convulsions when co-administered with quinolone antibiotics. Furthermore, hypo or hyperglycaemia may result from the concomitant administration of Aceclofenac and antidiabetic drugs, although this is rare. The co administration of Aceclofenac with other NSAIDS of corticosteroids may results in increased frequency of adverse event.
Adverse Drug Reaction
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 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.
Dosage and Administration
The usual dose of Aceclofenac is 100 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.
Serratiopeptidase is derived from bacteria belonging to the genus Serratia. The controlled fermentation of Serratia sp. secretes this enzyme in the highly selective medium. The recovery process involves various types of filtration, concentration and steps to make enzyme useful for pharmaceutical applications and finally dried to fine free flowing powder form.
Serratiopeptidase is an endopeptidase, having molecular weight of about 60 K Dalton. It absorbs strongly at 275-280 nm. Serratiopeptidase is a stronger caseionolytic agent than any other known alkaline or neutral protease.
Proteolytic enzymes (also known as proteinases or peptidases) are ubiquitous in nature, being found in animals, plants, bacteria, and fungi. Human beings produce such well known peptidases as trypsin and chymotrypsin to help digest our food, but we also generate countless others to control virtually every regulatory mechanism in our bodies. For example, various peptidases are involved in initiating blood clotting (thrombogenesis) and also in dissolving clots (fibrinolysis); in evoking an immune response and quelling it; and in both promoting and halting inflammation. The mechanism in each case is the ability of the enzyme to cut or cleave a protein target into two or more pieces, usually at very specific cleavage sites.
Mode of action:
Serratiopeptidase is a proteolytic enzyme available for clinical use more than a decade. Serratiopeptidase binds to alpha -2-macroglobulin in the blood in the ratio of 1:1, which helps to mask its antigenicity but retains its enzymatic activity and is slowly, transferred to site of inflammation. Serratiopeptidase hydrolyses bradykinin, histamine and serotonin responsible for oedematic status. Serratiopeptidase reduces swelling improves microcirculation and expectoration of sputum etc. Thus it can be concluded that Serratiopeptidase has anti-inflammatory, anti-oedemic and fibrinolytic activity and acts rapidly on localized inflammation.
Serratiopeptidase when consumed in unprotected form is destroyed by acid ion the stomach. However, enteric coated of tablet enable the enzyme to pass through the stomach unchanged and absorb in the intestine.
Serratiopeptidase 20-30mg two to three times a day.
Applications / Indications:
Trauma Surgery: In sports injuries, fractures, dislocation and Osteoarthritis etc, Serratiopeptidase reduces inflammation and helps in faster healing and repair.
Surgery: Serratiopeptidase reduces post operative Edema at injection sites. Serratiopeptidase reduces internal tissue edema and inflammation caused at post-operative handling. Reduction in edema reduces chances of rupture at tissue as well as risk of in case of plastic surgery graft rejection.
Respiratory Medicine: Serratiopeptidase breaks down complex sputum molecules into smaller peptidase of lower viscosity, helping in expectorating them more easily. Reduced viscosity of secretion helps in better antibiotic penetration to enable control over stubborn infections like bronchitis, lung abscess.
ENT: Serratiopeptidase has Mucolytic activity in sinuses, ear cavities and anti -inflammatory activity in upper respiratory tract organs help in faster resolution, better antibiotic bioavailability and faster cure rates.
Dermatology: Serratiopeptidase is used in acute painful inflamed dermatitis.
Dentistry: Serratiopeptidase helps in better control over dental infections and inflammation.
Obstetrics & Gynecology: The anti-inflammatory activity of Serratiopeptidase helps in resolution of post-partum haematomas, breast engorgements and pregnancy related thrombophlebitis.
Male Genital Infection: Serratiopeptidase restores microcirculation and augments antibiotic penetration in these organs which are known to produce poor antibiotic availability
Zyrtal SP dosage 1 tablet twice daily