Diclofast 25 mg tablet: Pink coloured round film coated tablet with a score
on one side. Each film-coated tablet contains Diclofenac Potassium 25mg.
Diclofast 50 mg tablet: Brown coloured round film coated tablet with a score
on one side. Each film-coated tablet contains Diclofenac Potassium 50mg.
Diclofenac potassium is a nonsteroidal anti-inflammatory drug with
pronounced antirheumatic, anti-inflammatory, analgesic and antipyretic
properties. It is an inhibitor of prostaglandin biosynthesis (prostaglandin
is important in the pathogenesis of inflammation, pair. and fever) and
modulator of arachidonic acid release and uptake.
In rheumatic conditions, diclofenac is effective against chest pain, pain
on movement, morning stiffness, swelling of the joints and functional
Diclofenac potassium rapidly relieves spontaneous pain and pain on
movement and reduces inflammatory swelling and wound oedema in
post-traumatic and postoperative inflammatory conditions.
In migraine attacks, diclofenac is found to be effective in relieving the
headache and in improving the accompanying symptom of nausea.
Diclofenac potassium has also shown marked analgesic effect in moderate and
severe painful states of non-rheumatic origin.
In vitro, diclofenac potassium does not suppress proteoglycan
biosynthesis in cartilage at concentrations equivalent to the concentrations
reached in human beings.
Diclofenac potassium has a rapid onset of action and is therefore
suitable for the treatment of acute episodes of pain and inflammation. It is
also found to exert a pronounced analgesic effect in moderately and severely
Diclofenac potassium relieves the pain and reduces the extent of bleeding
in primary dysmenorrhoea.
Absorption: Diclofenac is rapidly and completely absorbed. Food
intake does not affect extent of absorption, but time taken to reach Cmax is
Distribution: Peak plasma concentration after one 50mg tablet was
1.2 ug/mL (3.9 umol/L) after 20-60 min. The plasma concentrations show a
linear relationship to the size of the dose. Administration of 50mg 3 times
daily for a week does not lead to cumulation of diclofenac in the plasma.
Diclofenac is highly bound to serum proteins (99.7%), mainly albumin
Diclofenac enters the synovial fluid, and peak concentrations are
measured 2-4 hrs after peak plasma levels have been reached. The apparent
elimination half-life from the synovial fluid is 3-6 hrs. This shows that
the concentrations in the synovial fluid are already higher than plasma
concentrations 4-6 hrs after administration, and they remain higher for up
to 12 hrs.
Metabolism: Roughly half of diclofenac potassium undergoes
first-pass metabolism; consequently, the areas under the concentration
curves (AUCs) after an oral dose are only about half as large as after a
parenteral administration of a same dose.
The biotransformation of diclofenac involves partly glucuronidation of
the intact molecule but mainly single and multiple hydroxylation followed by
Elimination: The total systemic clearance of diclofenac in plasma
is 263 ± 56 mL/min (mean value ± SD). The terminal half-life in plasma is
1-2 hrs. About 60% of the dose is excreted via the kidneys in the form of
metabolites; <1% is excreted as unchanged substance. The remainder is
eliminated as metabolites via the bile in the faeces.
Elderly: No relevant age-dependent differences have been observed
in absorption, metabolism and excretion.
Impaired renal function: No accumulation of the unchanged active
substance can be inferred from the single-dose kinetics under the usual
dosage schedule. In patients with a creatinine clearance of <10 mL/min, the
theoretical steady-state plasma levels of metabolites are about 4 times
higher than in healthy subjects. The metabolites are nevertheless ultimately
cleared via the bile.
Impaired hepatic function (chronic hepatitis, nondecompensated liver
cirrhosis): The kinetics and metabolism of diclofenac are the same as in
As short-term treatment for acute painful conditions where fast onset of
action (within 30 minutes) is desired: Post-traumatic inflammatory states (eg
due to sprains), postoperative inflammation and pain (eg following dental or
orthopaedic surgery), painful and/or inflammatory conditions in gynaecology
(eg primary dysmenorrhoea or adnexitis), painful syndromes of the vertebral
column, non-articular rheumatism, and as an adjuvant in severe painful
inflammatory infections of the ear, nose or throat (eg pharyngotonsillitis,
In keeping with general therapeutic principles, the underlying disease
should be treated with basic therapy, as appropriate.
DOSAGE AND ADMINISTRATION
Adults: 100-150mg daily.
In milder cases and for children >14 years: 75-100mg daily.
The daily dosage should be prescribed in 2-3 fractional doses.
In primary dysmenorrhea, the daily dosage is 50-150mg. A dose of 50-100mg
should be given initially and raised in the course of several menstrual
cycles up to a maximum of 200mg/day if necessary.
Treatment should be started upon appearance of the first symptoms and
depending on the symptomology, continued for a few days. The tablets should
be taken with liquid, preferably before meals.
In migraine an initial dose of 50mg should be taken at the first signs of an
attack. In cases where pain relief within 2 hours after the first dose is
not sufficient, further dose of 50mg may be taken at intervals 4-6 hours, if
needed. The total dose should not exceed 200mg in any 24 hours period.
Children: Diclofast 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.
Peptic ulcer. Hypersensitivity to diclofenac. Similar to other nonsteroidal
anti-inflammatory agents, it is contraindicated in patients whom attacks of
asthma, urticaria or acute rhinitis are precipitated by acetylsalicylic acid
or other drugs with prostaglandin synthetase-inhibiting activity.
Occasional: Epigastric pain, other gastrointestinal disorders (eg
nausea, vomiting, diarrhoea, abdominal cramps, dyspepsia, flatulence,
Rare: Gastrointestinal bleeding, haematemesis, melena, peptic ulcer
with or without bleeding or perforation, bloody diarrhoea.
Isolated cases: Lower gut disorders (eg nonspecific haemorrhagic
colitis and exacerbation of ulcerative colitis or Crohn's disease), aphthous
stomatitis, glossitis, oesophageal lesions, constipation.
Central (and Peripheral) Nervous System
Occasional: Headache, lightheadedness, vertigo.
Isolated cases: Disturbances of sensation including paraesthesia,
memory disturbances, disorientation, disturbances of vision (reduced visual
acuity, diplopia), impaired hearing, tinnitus, insomnia, irritability,
convulsions, depression, anxiety, nightmares, tremor, psychotic reactions,
taste alteration disorders.
Occasional: Rashes or skin eruptions.
Isolated cases: Bullous eruptions, eczema, erythema multiforme,
Stevens-Johnson syndrome, Lyell's syndrome (acute toxic epidermolysis),
erythroderma (exfoliative dermatitis), loss of hair, photosensitivity
reactions, purpura (including allergic purpura).
Isolated cases: Acute renal failure, haematuria, proteinuria, interstitial
nephritis, nephrotic syndrome, papillary necrosis.
Occasional: Elevation of serum aminotranferases (SGOT, SGPT),
Rare: Hepatitis with or without jaundice.
Isolated cases: Fulminant hepatitis.
Isolated cases: Thrombocytopenia, leucopenia, agranulocytosis, haemolytic
anaemia, aplastic anaemia.