Subsyde-CR: Diclofenac sodium.
Subsyde-M: Diclofenac diethylamine.
Subsyde-CR: Diclofenac sodium is sodium -[2-[2,6-dichloroanilino)phenyl]-acetate, which is phenylacetic acid derivatives. Subsyde-CR is a controlled-release formulation which employs the new Diffusion Rate Controlling Membrane Technology (DRCM). Subsyde-CR is a multiple-unit formulation containing many pellets. Each pellet comprises of a core with alternate layers of drug and specially designed membrane, which controls the diffusion rate of the drug contents. After release of pellets into the stomach, entry of water into the pellets takes place by osmosis, starting from the stomach itself. This water dissolves the diclofenac until a saturated solution is formed internally. Diclofenac then diffuses through the dialyzing membrane into the surrounding lumen for absorption into the bloodstream. The dialyzing membrane ensures slow and steady release of the drug for absorption throughout its passage in the intestinal tract. This process continues layer by layer in a slow and steady manner ensuring that plasma diclofenac concentrations are maintained for 24 hrs after a single dose. When the entire drug has diffused out of the pellets, they then collapse and are excreted out.
Subsyde-M: Each tube contains diclofenac diethylamine 1.16% w/w equivalent to diclofenac sodium 1% w/w, linseed oil 3% w/w, methyl salicylate 10% w/w, menthol 5% w/w, methyl hydroxybenzoate 0.1% w/w, propyl hydroxybenzoate 0.025% w/w in a gel base (as needed).
Pharmacology: Subsyde-CR: Subsyde-CR contains the sodium salt of diclofenac, a nonsteroidal anti-inflammatory drug (NSAIDs). In pharmacologic studies, diclofenac has shown anti-inflammatory, analgesic and antipyretic effects. Inhibition of prostaglandin biosynthesis, which has been demonstrated in experiments, is considered to be fundamental to the mechanism of action of diclofenac. Prostaglandins play a major role in the pathogenesis of inflammation, pain and fever. In rheumatic diseases, diclofenac produces marked relief from signs and symptoms eg, pain at rest, pain on movement, morning stiffness and swelling of the joints as well as by an improvement in function. Subsyde-CR is particularly suitable for patients requiring a daily dosage of 100 mg.
Subsyde-M: Percutaneous anti-inflammatory analgesic.
Mode of Action: Diclofenac diethylamine is absorbed through the skin. It inhibits the enzyme cyclooxygenase and thus reduces the formation of prostaglandins. Moreover, it also decreases the arachidonic acid entering into the lipooxygenase pathway and the resultant effect is a decreased formation of leukotrienes. Prostaglandins and leukotrienes are the most powerful mediators of pain and inflammation. Subsyde-M gel thus provides a superior relief of pain, inflammation and swelling.
Pharmacokinetics: Absorption: Diclofenac is completely absorbed from the gastrointestinal tract. After administration of 100 mg Subsyde-CR, mean peak plasma concentrations of about 1.39 mcg/mL were reached at a mean of 4.38 hrs. Pharmacokinetic behaviour does not change after repeated administration of the drug. The area under the plasma concentration curve (AUC) is 18.87 mcg·hr/mL.
Distribution: More than 99% of diclofenac is reversibly bound to human plasma 2 albumin. As with other NSAIDs, diclofenac diffuses into and out of the synovial fluid. Diffusion into the joint occurs when plasma levels of diclofenac are higher than those in synovial fluid.
Metabolism and Excretion: Diclofenac is eliminated through metabolism and subsequent urinary and biliary excretion of the glucuronide and the sulphate conjugates of the metabolites. Approximately 65% of the dose is excreted in the urine and approximately 35% in the bile.
Subsyde-CR: Inflammatory and degenerative forms of rheumatism, rheumatoid arthritis, ankylosing spondylitis, osteoarthritis, spondylarthritis, painful syndromes of the vertebral column, non-articular rheumatism, painful post-traumatic and postoperative inflammation and swelling eg, following dental or orthopaedic surgery, painful and/or inflammatory conditions in gynaecology, as an adjuvant in severe painful inflammatory infections of the ear, nose or throat eg, pharyngotonsillitis, otitis. In accordance with general therapeutic principles, appropriate measures should be taken to treat the underlying disease.
Subsyde-M: Quick relief from pain, inflammation and swelling due to musculoskeletal disorders eg, sprains, strains, tendinitis, bursitis, hand, neck and shoulder pain, muscle stiffness, various types of arthritis, backache, lumbago and sciatica. Thus, it is a rapid acting topical gel with analgesic and anti-inflammatory effects.
Subsyde-CR: Adults: 1 cap daily preferably between 6-8 PM (because of circadian rhythm). Treatment should be started as soon as symptoms begin and continued for several days, depending on the symptomatology.
Subsyde-M: Puncture the nozzle seal by piercing with the piercing point of the cap. Gently squeeze the contents of the tube onto your finger. Slowly rub the gel on the intact skin around the affected area. Rub the gel until the cream disappears.
Subsyde-M gel is generally applied to the affected site 3-4 times daily. Squeeze the tube to obtain 1 inch of gel at a time and apply over the affected area. Vigorous rubbing or massaging should be avoided.
For external use only.
Subsyde-CR: In case of acute overdosage, it is recommended that the stomach be emptied by vomiting or lavage. Forced diuresis may theoretically be beneficial because the drug is excreted in the urine. In addition to supportive measures, the use of oral activated charcoal may help reduce the absorption of diclofenac.
Hypersensitivity to any of the excipients of Subsyde.
Peptic ulcer. Patients in whom attacks of asthma, urticaria or acute rhinitis have been precipitated by acetylsalicylic acid or other prostaglandin synthetase inhibitors.
Subsyde-CR: Accurate diagnosis and careful monitoring are essential in patients with gastrointestinal disorders, a history suggestive of peptic ulcer, ulcerative colitis, or Crohn's disease and in patients with severely impaired hepatic function. Particular caution is called for in patients with impaired cardiac or renal function, as well as in elderly patients. As diclofenac may increase the activity of ≥1 liver enzymes, hepatic function during prolonged treatment should be monitored.
Subsyde-M: Should be applied only to intact skin. It should not come in contact with eyes or mucous membranes.
Use in pregnancy & lactation: In 1st and 2nd trimesters, no controlled studies in pregnant women are available. Subsyde-CR should not be given during the 3rd trimester owing to the risk of premature closure of the ductus arteriosus and suppression of uterine contractility.
As with other drugs that are excreted in milk, diclofenac is not recommended for use in nursing women.
Use in children: Safety and effectiveness of diclofenac in children have not been established.
In 1st and 2nd trimesters, no controlled studies in pregnant women are available. Subsyde-CR should not be given during the 3rd trimester owing to the risk of premature closure of the ductus arteriosus and suppression of uterine contractility. As with other drugs that are excreted in milk, diclofenac is not recommended for use in nursing women.
Gastrointestinal Tract: Occasional: Epigastric pain, other gastrointestinal symptoms eg, nausea, vomiting, diarrhoea, abdominal cramps, dyspepsia, flatulence and anorexia. Rare: GI bleeding, haematemesis, melena, peptic ulcer with or without bleeding or perforation, bloody diarrhea, pancreatitis.
Central and Peripheral Nervous System: Occasional: Headache, dizziness, vertigo. Rare: Tiredness.
Skin and Subcutaneous Tissue: Occasional: Skin rash. Rare: Urticaria.
Kidneys (Isolated Cases): Acute renal failure, haematuria, proteinuria and internephritis. Occasional: Elevated serum aminotransferase values (SGOT, SGPT). Rare: Hepatitis with or without jaundice.
Blood (Isolated Cases): Thrombocytopenia, leukopenia, agranulocytosis, haemolytic anaemia, aplastic anaemia.
Hypersensitivity Reactions: Rare: Hypersensitivity reactions eg, asthma, systemic anaphylactic/anaphylactoid reactions (including hypotension).
Other Organ Systems: Rare: Oedema.
Aspirin: Concomitant administration of diclofenac and aspirin is not recommended.
Anticoagulants: Caution should be exercised while administering anticoagulants with diclofenac, since interactions of anticoagulants have been seen with other NSAIDs.
Digoxin, Methotrexate, Cyclosporine and Lithium: Patients who begin taking diclofenac or who increase their diclofenac dose while taking these drugs should be observed closely, particularly if renal function is impaired. In case of digoxin, serum levels should be monitored.
Oral Hypoglycaemics: Isolated cases have been reported of hypoglycaemic and hyperglycaemic reactions necessitating an adjustment in the dosage of antidiabetic drugs during treatment with diclofenac.
Diuretics: Concomitant treatment of diclofenac with potassium-sparing diuretics may raise serum potassium levels, which should therefore be monitored.
Subsyde-CR: Store in a cool and dry place.
Subsyde-M: Store below 25°C. Do not freeze.
M01AB05 - diclofenac ; Belongs to the class of acetic acid derivatives and related substances of non-steroidal antiinflammatory and antirheumatic products.
M02A - TOPICAL PRODUCTS FOR JOINT AND MUSCULAR PAIN ; Used in the topical treatment of joint and muscular pains.
Subsyde-CR: Cap 100 mg x 10 x 10's.
Subsyde-M: Gel 20 g.
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