Dosanac

Diclofenac sodium.

Emulsion gel: Each 100 g contains: Diclofenac diethylammonium corresponding to diclofenac sodium 1 g, in a base containing a fatty emulsion in an aqueous gel.
Injection: Each ampoule contains: Diclofenac sodium 25 mg/ml.

Pharmacology: Emulsion gel: Dosanac emulsion gel is a topically symptomatic relief of pain and inflammatory preparation. When the drug is applied locally, the active substance is absorbed through the skin. In patient with rheumatoid arthritis who had received repeated treatment with diclofenac emulsion gel, the concentrations measured in the region of the inflamed wrist both in the synovial fluid and in synovial tissue removed during surgery, proved to be higher than the plasma concentrations.
This finding confirms that diclofenac penetrates into the inflamed zone following local application.
Injection: Dosanac contains a non-steroidal compound with pronounced antirheumatic, anti-inflammatory, analgesic and antipyretic properties. When employed in high doses it also temporarily inhibits experimentally induced platelet aggregation. Inhibition of prostaglandin biosynthesis, which has been demonstrated experimentally, is regarded as having an important bearing on its mechanism of action. Prostaglandins play a major role in the causation of inflammation, pain and fever. In rheumatic diseases, the anti-inflammatory and analgesic properties of Dosanac elicit a clinical response characterised by marked relief from signs and symptoms such as pain at rest, pain on movement, morning stiffness and swelling of the joints as well as by an improvement in function. In post-traumatic and post-operative inflammatory conditions, Dosanac rapidly relieves both spontaneous pain and pain on movement and diminishes inflammatory swelling and wound edema. Dosanac has also been found to exert a pronounced analgesic effect in moderately and severely painful states of non-rheumatic origin, an effect which sets in within 15-30 minutes.
Dosanac injections are particularly suitable as initial therapy for the inflammatory and degenerative rheumatic diseases as well as for the treatment of painful conditions due to inflammation of non-rheumatic origin.

Emulsion gel: For the local relief of pain and inflammation in traumatic inflammation of the tendons, ligaments, muscles, and joints; localized forms of soft-tissue rheumatism, e.g. tendinitis; Localized painful joint diseases.
Injection: Inflammatory and degenerative forms of rheumatism: rheumatoid arthritis and ankylosing spondylitis, osteoarthrosis and spondylarthritis. Painful syndromes of the vertebral column. Renal colic, Biliary colic. Painful post-operative and post-traumatic inflammation and swelling. Non articular rheumatism. Acute attacks of gout.

Emulsion gel: Depending on the size of the painful site to be treated, apply 2-4 g gel (3-6 cm length), 3-4 times daily to the affected parts and rub in gently. It is advisable to review the treatment after 2 weeks.
Injection: For adults: The dosage is generally 1 ampoule daily, injected deep intragluteally into the upper outer quadrant. By way of exception in severe cases (e.g. of colic) two injections, separated by an interval of few hours, can be given per day (one into each buttock). Alternatively, it is possible to combine one ampoule with other dosage forms of Dosanac up to a maximum daily dosage of 150 mg.
Dosanac injection should not be given for more than a few days; if necessary, the treatment can be continued with Dosanac coated tablets.
Special populations: Established cardiovascular disease or significant cardiovascular risk factors: The use of high dose diclofenac (150 mg/day) for more than 4 weeks is contraindicated in patients with established cardiovascular disease (congestive heart failure, established ischemic heart disease, peripheral arterial disease) or uncontrolled hypertension. If diclofenac treatment is needed, patients with established cardiovascular disease, uncontrolled hypertension or significant cardiovascular risk factors (e.g. hypertension, hyperlipidemia, diabetes mellitus and smoking) should be treated only after careful consideration and at dose ≤ 100 mg daily when initial treatment with diclofenac injection continues with diclofenac tablets or suppositories for more than 4 weeks. As the cardiovascular risks of diclofenac may increase with dose and duration of exposure, diclofenac should always be prescribed at the lowest effective daily dose and for the shortest duration possible.

Emulsion gel: The low systemic absorption of topical diclofenac renders overdosage extremely unlikely.
General therapeutic measures of the kind normally adopted in order to treat poisoning with nonsteroidal anti-inflammatory drugs.

Emulsion gel: Hypersensitivity to diclofenac, acetylsalicylic acd (aspirin), and other non-steroidai anti-inflammatory drugs, as well as to isopropanol or propylene glycol.
Injection: Peptic ulcer, Hypersensitivity to the active substance. Like other non-steroidal anti-inflammatory agents Dosanac is also contraindicated in asthmatic patients in whom attacks of asthma, urticaria, or acute rhinitis are precipitated by acetylsalicylic acid or by other drugs with prostaglandin-synthetase inhibiting activity.
The use of high dose diclofenac (150 mg/day) for more than 4 weeks is contraindicated in patients with established cardiovascular disease (congestive heart failure, established ischemic heart disease, peripheral arterial disease) or uncontrolled hypertension.

Injection: Contraindicated in children under 2 years.
Cardiovascular effects: Treatment with NSAIDs, including diclofenac, particularly at high dose and in long term, may be associated with a small increased risk of serious cardiovascular thrombotic events (including myocardial infarction and stroke).
As the cardiovascular risks of diclofenac may increase with dose and duration of exposure, the lowest effective daily dose should be used for the shortest duration possible. The patient's need for symptomatic relief and response to therapy should be re-evaluated periodically, especially when initial treatment with diclofenac injection continues with diclofenac tablets or suppositories for more than 4 weeks. Patients should be advised to remain alert for the signs and symptoms or serious arteriothrombotic events (e.g. chest pain, shortness of breath, weakness, slurring of speech), which can occur without warnings. Patients should be instructed to see a physician immediately in case of such an event.

Emulsion gel: For external use only, should not be contacted with the eyes or mucous membranes. It should be applied only to intact skin surfaces, and not to skin wounds or open injuries. Severe cutaneous reactions, including Stevens-Johnson syndrome and toxic epidermal necrolysis (Lyell's syndrome) have been reported with diclofenac sodium. Patients treated with diclofenac sodium should be closely monitored for signs of hypersensitivity reactions. Discontinue diclofenac sodium if rash occurs. No dosage recommendations and indications have been established for use in pregnancy, lactation and children.
Injection: Strict accuracy of diagnosis and close medical surveillance are imperative in patients with symptoms indicative of gastrointestinal disease, with a case history suggestive of gastrointestinal ulcerative colitis, Crohn's disease, or pre-existing dyshaemopoiesis or disorders of blood coagulation, as well as in patients suffering from severe impairment of hepatic, cardiac, or renal function.
In the rare instances where peptic ulceration or gastro-intestinal bleeding occur in patients under treatment with Dosanac, the drug should be withdrawn.
In patients of advanced age, caution is indicated on basic medical grounds. During prolonged treatment with Dosanac as with other highly active non-steroidal anti-inflammatory agents blood counts and monitoring of hepatic and renal function are indicated as precautionary measures.

Injection: For general medical reasons, Dosanac should only be prescribed during pregnancy if its use is mandatory. Following oral doses of 100 mg daily, on active substance could be found in the breast milk. (Limit of detection: 10 ng/ml).
Use of NSAIDs at about 20 weeks gestation or later in pregnancy may cause foetal renal dysfunction leading to oligohydramnios and in some cases, neonatal renal impairment. These adverse outcomes are seen, on average, after days to weeks of treatment, although oligohydramnios has been infrequently reported as soon as 48 hours after NSAID initiation. Oligohydramnios is often, but not always, reversible with treatment discontinuation.

Injection: Gastrointestinal distress, occult gastrointestinal bleeding and gastric ulceration.
Cardiac disorder: Uncommon*: Myocardial infarction, cardiac failure, palpitations, chest pain.
*The frequency reflects data from long-term treatment with high dose (150 mg/day).
Description of selected adverse drug reactions: Arteriothrombotic events: Meta-analysis and pharmacoepidemiological data point towards a small increased risk of arteriothrombotic events (for example myocardial infarction) associated with the use of diclofenac, particularly at high dose (150 mg daily) and during long-term treatment.

Emulsion gel: Occasional rashes or skin eruptions. Cases of hair loss, bullous eruptions, erythema multiforme and photosensitivity reactions have been reported.

Emulsion gel: Not known.
Injection: When given concomitantly with lithium, non-steroidal antirheumatic agents raise the latter's blood concentration. Concomitant ingestion of acetylsalicylic acid has the effect of lowering the plasma concentration of diclofenac. When administered concurrently with anticoagulants or antidiabetic agents, however, Dosanac exerts no influence on their activity.

Injection: Incompatibilities: Dosanac Injections, for IM use, should not be mixed with other injectable solutions.

Emulsion gel: Protect from heat (below 25°C).
Injection: Protect from light and heat.
Shelf-life: Emulsion gel: 3 years.

Nonsteroidal Anti-Inflammatory Drugs (NSAIDs)

M02AA15 - diclofenac ; Belongs to the class of non-steroidal antiinflammatory preparations for topical use. Used in the treatment of joint and muscular pains.
M01AB05 - diclofenac ; Belongs to the class of acetic acid derivatives and related substances of non-steroidal antiinflammatory and antirheumatic products.

P, POM