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Lesflam 25 and 50
Each film-coated tablet contains: Diclofenac Potassium 25mg and 50mg

DESCRIPTION
Diclofenac, as the potassium salt, is a benzeneacetic acid derivative, designated chemically as 2-[(2,6- dichlorophenyl) amino] benzeneacetic acid, monopotassium salt. The structural formula is shown in Figure l.

Lesflam


R=K: Lesflam, diclofenac potassium


Diclofenac as the potassium salt, is a faintly yellowish white to light beige, virtually odorless, slightly hygroscopic crystalline powder. Molecular weight of potassium is 334.25. It is freely soluble in methanol, soluble in ethanol, and practically insoluble in chloroform and in dilute acid and soluble in water. The n-octanol / water partition coefficient is 13.4 at pH 7.4 and 1545 at pH 5.2. It has a single dissociation constant (pKa) of 4.0 0.2 at 25C in water.


:PHARMACODYNAMIC:
Lesflam is a non-steroidal anti-inflammatory agent and contains the potassium salt of diclofenac. In Lesflam the sodium ion of diclofenac sodium has been replaced by a potassium ion. The active principle is thus the same as in Voltaren. The preparation possesses pronounced analgesic, anti-inflammatory, and antipyretic properties. The fact that the active substance is quickly absorbed from the coated tablets of Lesflam makes them suitable for the treatment of acute painful and inflammatory conditions in which importance is attached to a prompt onset of effect (within 30 minutes). Inhibition of prostaglandin biosynthesis, which has been demonstrated experimentally, is regarded as having a major bearing on the drug mechanism of action. Prostaglandins play a prominent role in the causation of inflammation, pain, and fever. Lesflam like Voltaren exerts a pronounced analgesic effect in moderately and severely painful states. In post-traumatic and post-operative inflammatory conditions, Lesflam quickly relieves both spontaneous pain and pain on movement and diminished inflammatory swelling and wound oedema. In primary dysmenorrhea it is capable of relieving the pain and also reducing the extent of bleeding. At concentration corresponding to those attained in man, Lesflam in vitro does not suppress proteoglycan biosynthesis in cartilage.

PHARMACOKINETIC
Absorption
Diclofenac is rapidly and completely absorbed from the coated tablets. When the tablets are taken with a meal, the quantity of active substance absorbed is not diminished, although the speed of its absorption may possibly be reduced.

Distribution
Following ingestion of one coated tablet of 50 mg, the plasma concentrations of diclofenac attain a mean peak value of 1.2 g/mL (3.9 mol/L) after 20-60 minutes. The plasma concentrations show a linear relationship to the size of the dose. Repeated oral administration in daily doses of 50mg GA. for a week does not lead to cumulation of diclofenac in the plasma. Diclofenac becomes bound to serum proteins at a rate of 99.7%; chiefly to albumin (99.4%).

Metabolism
Roughly half of the active substance is metabolised during its first passage through the liver (<<first-pass>> effect); consequently, the areas under the concentration curves (AUCs) after an oral dose are only about one-half as large as after a parenteral dose of the same size. The biotransformation of diclofenac involves partly-glucuronidation of the intact molecule but mainly single and multiple hydroxylation followed by glucuronidation. Approx. 60% of the dose administered is excreted in the urine than 1% as unchanged substance. The remainder of the dose is eliminated as metabolites through the bile in the faeces.

No relevant age-dependent differences in the drug's absorption, metabolism, or excretion have been observed.

Elimination
The total systemic clearance of diclofenac in plasma is 26356mL/min (x SD). The terminal half-life in plasma is 1-2 hours.

 

Kinetics in special clinical situations
In patients suffering from renal impairment, no accumulation of the unchanged active substance can be inferred from the singled-dose kinetics when applying the usual dosage schedule. At a creatinine clearance of less than 10mL/min, the theoretical steady-state plasma level of metabolites is about four times higher than in normal subjects.

 

However, the metabolites are ultimately cleared through the bile.


In the presence of impaired hepatic function (chronic hepatitis, compensated cirrhosis), the kinetics and metabolism of diclofenac are the same as in patients without liver disease.

INDICATION
Lesflam is indicated as short-term treatment for the following acute conditions in cases where particular importance is attached to a prompt onset of effect (within 30 minutes):

Post-operative inflammation and pain, e.g. following dental or orthopaedic surgery
Painful and/or inflammatory conditions in gynaecology, e.g. primary dysmenorrhoea or adnexitis
Non-articular rheumatism

RECOMMENDED DOSE
Adults: As a rule, the daily dosage for adults is 100-150 mg. In milder cases, as well as for children over 14 years of age, 75-100 mg daily is usually sufficient. The daily dosage should always be prescribed in 2-3 fractional doses.
In primary dysmenorrhoea the daily dosage, which should be individually adapted, is generally 50-150 mg. Initially a dose of 50-150 mg should be given; if necessary, this can be raised in the course of several menstrual cycles up to the maximum of 200 mg daily. Treatment should be started upon appearance of the first symptoms and, depending on the symptomatology, continued for a few days. The tablets should be taken with liquid, preferably before meals.

 

Children: The dosage strengths are such that Lesflam tablets are not recommended for use in children.


After assessing the risk/benefit ratio in each individual patient, the lowest effective dose for the shortest possible duration should be used.
 

CONTRAINDICATION:
Peptic ulcer. Known hypersensitivity to the active substance. Like other non-steroidal anti-inflammatory agents, Lesflam is also contraindicated in patients in whom attacks of asthma, urticaria, or acute rhinitis are precipitated by acetylsalicylic acid or by other drngs with prostaglandin-synthetase inhibiting activity.

 


WARNINGS
Risk of GI ulceration, bleeding and perforation with NSAID
Serious GI toxicity such as bleeding, ulceration and perforation can occur at any time, with or without warning symptoms, in patients treated with NSAID therapy. Although minor upper GI problems (e.g. dyspepsia) are common, usually developing early in therapy, prescribers should remain alert for ulceration and bleeding in patients treated with NSAIDs even in the absence of previous GI tract symptoms.


Studies to date have not identified any subset of patients not at risk of developing peptic ulceration and bleeding. Patients with prior history of serious GI events and other risk factors associated with peptic ulcer disease (e.g. alcoholism, smoking, and corticosteroid therapy) are at increased risk. Elderly or debilitated patients seem to tolerate ulceration or bleeding less than other individuals and account for most spontaneous reports for fatal GI events.

 

PRECAUTION
Strict accuracy of diagnosis and close medical surveillance are imperative in patients with symptoms indicative of gastro-intestinal disease, with a case history suggestive of gastro-intestinal ulceration, with ulcerative colitis, or with Crohn's disease, as well as in patients suffering from severe impairment of hepatic function.

 

Gastro-intestinal bleeding or ulceration/ perforations generally have more serious consequences in elderly patients. This can occur at any time during the treatment, even without warning symptoms or a previous history.


In the rare instances where gastro-intestinal ulceration or bleeding occur in patients under treatment with Lesflam, the drug should be withdrawn. Owing to the importance of prostaglandin for maintaining renal blood flow, particular caution is called for in patients with impaired cardiac or renal function, in the elderly, in patients taking diuretics, and in those with extracellular volume depletion form any cause, e.g. in the peri-operative or post-operative phase of major surgical operation. Monitoring of renal functioning as a precautionary measure is recommended when using Lesflam in such cases. Discontinuation of the medication is normally followed by recovery to the pre-treatment state. In patients of advanced age, caution is indicated 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.


As with other non-steroidal anti-inflammatory drugs, elevations of one or more liver enzymes may occur with Lesflam. During prolonged treatment with Lesflam, monitoring of hepatic function is recommended as precautionary measure.


If impairment of liver function persists or worsens, if clinical signs or symptoms consistent with liver disease develop, or if other manifestation occur (e.g. eosinophilia, skin rashes, etc.) Lesflam should be withdrawn, Hepatitis may set in without prodromal symptoms. Caution is called for when using Lesflam in patients with hepatic porphyria, since the drug may trigger an attack.

 

Treatment with Lesflam in the afore-mentioned indications generally proves necessary only for a few days. But if, contrary to the recommendations for its use, Lesflam is administered over a more prolonged period it is advisable as with other highly active non-steroidal anti-inflammatory agents to perform blood counts.

 

As in the ease of other non-steroidal ants-inflammatory drugs, allergic reactions, including anaphylactic/anaphylactoid reactions, can occur, even without earlier exposure to the drug.


Discontinue Lesflam tablet immediately if rash occurs.

 

Special points to note
Patients experiencing dizziness or other central nervous disturbances should refrain from driving a vehicle or operating machines.


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