DICLOFENAC-ELSaad XR 100
-
Chemical Name:
Diclofenac Sodium -
Therapeutic Category:
Anti-inflammatory drugs -
Pharmacologic Category:
Nonsteroidal anti-inflammatory drug -
Pharmaceutical Form:
Tablets -
Composition:
Diclofenac Sodium 100mg
DICLOFENAC ELSAAD
Enteric-Coated Tablets / Extended Release F.C Tablets
Diclofenac Sodium
1- COMPOSITION:
DICLOFENAC ELSAAD - 50: Each enteric-coated tablet contains 50 mg Diclofenac sodium..
DICLOFENAC ELSAAD XR 100: Each extended release F.C tablet contains 100 mg Diclofenac sodium.
2- PHARMACOLOGICAL CLASSIFICATION:
No steroidal anti-inflammatory drugs (NSAIDs).
3- PHARMACOLOGICAL PROPERTIES:
Mechanism of action/pharmacodynamics:
Diclofenac is a nonsteroidal agent with marked analgesic/anti- inflammatory properties. It is an inhibitor of prostaglandin synthetase, (cyclo-oxygenase).
In rheumatic diseases, the anti-inflammatory and analgesic properties of DICLOFENAC ELSAAD elicit a clinical response characterized by marked relief of signs and symptoms such as pain upon movement, morning stiffness, and swelling of the joints and by improvement in function.
In post-traumatic and postoperative inflammatory conditions, DICLOFENAC ELSAAD rapidly relieves both spontaneous pain and pain upon movement, and reduces inflammatory swelling and wound oedema. DICLOFENAC ELSAAD has also been found to exert a pronounced analgesic effect in moderate and severe pain of non-rheumatic origin.
4- Pharmacokinetics:
Absorption:
Diclofenac Absorption is complete but onset is delayed until passage through the stomach, which may be affected by food which delays stomach emptying. Peak plasma concentrations are reached within 2 hours, Plasma concentrations are in linear proportion to the size of the dose.
Bioavailability:
About half of the administered diclofenac is metabolised during its first passage through the liver ("first-pass" effect), the area under the concentrations curve (AUC) following oral administration is about half that following an equivalent parenteral dose.
Distribution:
The active substance is 99.7% protein bound, mainly to albumin (99.4%).
Diclofenac enters the synovial fluid, where maximum concentrations are measured 2-4 hours after the peak plasma values have been attained.
Metabolism:
Biotransformation of diclofenac takes place partly by glucuronidation of the molecule, but mainly by single and multiple hydroxylation and methoxylation, resulting in several phenolic metabolites, most of which are converted to glucuronide conjugates. Two phenolic metabolites are biologically active, but to a much lesser extent than diclofenac.
Elimination:
The total systemic clearance of diclofenac in plasma is 263 ± 56 mL/min. The half-life in plasma is 1-2 hours. About 60% of the administered dose is excreted in the urine in the form of the metabolites. Less than 1% is excreted as unchanged substance. The rest of the dose is eliminated as metabolites through the bile in the faeces.
5- INDICATIONS:
Relief of all grades of pain and inflammation in a wide range of conditions, including:
- arthritic conditions: rheumatoid arthritis, osteoarthritis, ankylosing spondylitis, acute gout,
- acute musculo-skeletal disorders such as periarthritis (for example frozen shoulder), tendinitis, tenosynovitis, bursitis,
- other painful conditions resulting from trauma, including fracture, low back pain, sprains, strains, dislocations, orthopaedic, dental and other minor surgery.
6- CONTRAINDICATIONS:
- Hypersensitivity to the active substance or any of the excipients.
- Active, gastric or intestinal ulcer, bleeding .
- Gastrointestinal bleeding or perforation, relating to previous NSAID therapy
- Last trimester of pregnancy.
- Severe hepatic, renal or cardiac failure.
- Like other non-steroidal anti-inflammatory drugs (NSAIDs), diclofenac is also contraindicated in patients in whom attacks of asthma, angioedema, urticaria or acute rhinitis are precipitated by ibuprofen, acetylsalicylic acid or other nonsteroidal anti-inflammatory drugs.
7- SIDE EFFECTS:
The most frequently reported adverse effects occurring are:
Gastrointestinal disturbances including:( abdominal pain, constipation, diarrhea, dyspepsia,
flatulence, gross bleeding, heartburn, nausea, GI ulcers and vomiting) - Abnormal renal function- anemia –dizziness- edema - elevated liver enzymes – headaches –increased bleeding time – pruritus -rashes and tinnitus.
Additional adverse experiences reported occasionally include:
- Body as a whole: fever , infection and sepsis.
- Cardiovascular System: congestive heart failure , hypertension , tachycardia and syncope.
- Digestive System: dry mouth, esophagitis ,gastric ulcer , gastritis ,gastrointestinal bleeding ,glossitis ,hematemesis ,hepatitis and jaundice.
- Hemic and Lymphatic System: ecchymosis ,eosinophilia, leukopenia ,melena, purpura ,rectal bleeding , stomatitis and thrombocytopenia.
- Metabolic and Nutritional : weight change.
- Nervous System: anxiety , asthenia , depression ,drowsiness , insomnia , malaise , nervousness , somnolence and vertigo.
- Respiratory System : asthma and dyspnea .
- Skin and Appendages :alopecia , photosensitive and sweeting increased .
- Special Senses : blurred vision.
- Urogenital System: eystitis , dysuria , hematuria , interstitial nephritis , oliguria/polyuria , proteinuria and renal failure.
8- WARNINGS AND PRECAUTIONS:
- Gastrointestinal bleeding and ulceration /perforation can occur at any time during treatment, with or without warning symptoms or a previous history. They generally have more consequences in the elderly. In the rare cases where this may occur in patients receiving diclofenac, the drug should be withdrawn.
- As with other NSAID's, allergic reaction, including anaphylactic/anaphylactoid reactions, can also occur in rare cases without earlier exposure to the drug. DICLOFENAC ELSAAD may mask the signs and symptoms of infection due to its pharmacodynamics properties.
- Close medical surveillance is indicated in patients with symptoms/history of gastrointestinal diseases, impaired hepatic, cardiac, or renal function hepatic porphyria, patients being treated with diuretics, and patients with extra-cellular volume depletion.
- During prolonged treatment, periodic monitoring of liver function and blood counts is recommended.
- Like other NSAID's, DICLOFENAC ELSAAD may temporarily inhibit platelet aggregation. Patients with defects of haemostasis should be carefully monitored.
- Renal Impairment: Diclofenac is contraindication in patient with severe renal impairment , No specific studies have been carried out in patients with renal impairment , therefore no specific dose adjustment recommendations can be made. Caution is advised when administering diclofenac to patient with mild to moderate renal impairment.
- Hepatic Impairment: Diclofenac is contraindication in patient with severe hepatic impairment , No specific studies have been carried out in patients with hepatic impairment , therefore no specific dose adjustment recommendations can be made. Caution is advised when administering diclofenac to patient with mild to moderate hepatic impairment.
- Caution is indicated in the elderly on basic medical grounds. In particular, it is recommended that the lowest effective dosage be used in frail elderly patients or those with a low body weight.
9- DRUG INTERACTIONS:
- Diclofenac may raise plasma concentrations of lithium and digoxin.
- Concomitant treatment with drugs known to cause hyperkalemia like potassium-sparing diuretics, may raise serum potassium levels.
- An increased risk of hemorrhage in patients receiving diclofenac and anticoagulants or anti-platelet agents concomitantly has been reported in isolated cases although this has not been confirmed in clinical studies.
- Like other NSAIDs, concomitant use of diclofenac with diuretics and antihypertensive agents (e.g. beta-blockers, angiotensin converting enzyme (ACE) inhibitors may cause a decrease in their antihypertensive effect via inhibition of vasodilatory prostaglandin synthesis.
- Convulsions may occur due to an interaction between quinolone antibacterials and NSAIDs.
- Concomitant use of cardiac glycosides and NSAIDs in patients may exacerbate cardiac failure and increase plasma glycoside levels.
- Caution is called for when using concomitantly with methotrexate, cyclosporine, tacrolimus, potent CYP2C9 inhibitors and phenytoin.
10- DOSAGE AND METHOD OF ADMINISTRATION:
-Administer with food or milk to avoid gastric distress .
-For the relief of osteoarthritis, the recommended dosage is 100-150 mg/day in divided doses (50
mg b.i.d. or t.i.d., or XR 100mg q.i.d).
-For the relief of rheumatoid arthritis, the recommended dosage is 150-200 mg/day in divided doses
(50 mg t.i.d. or q.i.d., XR 100mg q.i.d or in rare cases b.i.d).
11- OVERDOSE:
Symptoms following acute NSAID overdoses are usually limited to lethargy, drowsiness, nausea,
vomiting, and epigastric pain, which are generally reversible with supportive care. Gastrointestinal
bleeding can occur. Hypertension, acute renal failure, respiratory depression and coma may occur,
but are rare. Anaphylactoid reactions have been reported with therapeutic ingestion of NSAIDs, and
may occur following an overdose.
Patients should be managed by symptomatic and supportive care following a NSAID overdose.
There are no specific antidotes. Emesis and/or activated charcoal (60 to 100 g in adults, 1 to 2
g/kg in children) may be indicated in patients seen within 4 hours of ingestion following a large overdose.
12- PREGNANCY AND LACTATION:
- Pregnancy category C , there are no adequate and well –control studies in pregnant woman.
In late pregnancy , as with other NSAIDs diclofenac sodium should be avoided because it may cause premature closure of the ductus arteriosus .
- it is no known whether this drug is excreted in human milk ,decision should be made whether to discontinue nursing or to discontinue the drug ,taking into account the importance of the drug to the mother.
13- PACKAGE:
DICLOFENAC ELSAAD -50: 20 Enteric-coated tablets package.
DICLOFENAC ELSAAD XR 100: 20 Extended Release F.C tablets package.
14- STORAGE:
Store at temperature below 30°C,protect from moisture.
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