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Rhemofenax
DESCRIPTION
RHEMOFENAX CAPSULE 25 MG: A size 2 - brown /grey capsule, with 'DUO 861'
marking.
RHEMOFENAX CAPSULE 50 MG: A size 2 - maroon / maroon capsule, with 'DUO 861'
marking.
RHEMOFENAX TABLET 25 MG : A (light) blue, 11 mm caplet with 'DUO' on one
side and scored 'DUO' on another side. RHEMOFENAX TABLET 50 MG : A blue, 11
mm caplet with 'd 861' marking on one side and scored on another side.
PHEMOFENAX 100 MG SR CAPSULE: A green I green, size 3 capsule with 'DUO 861'
marking printed on the capsule.
COMPOSITION
RHEMOFENAX CAPSULE 25 MG: Each capsule contains Diclofenac Sodium 25 mg.
RHEMOFENAX CAPSULE 50 MG: Each capsule contains Diclofenac Sodium 50 mg.
RHEMOFENAX TABLET 25 MG : Each
tablet contains Diclofenac Sodium 25 mg.
RHEMOFENAX TABLET 50 MG : Each
tablet contains Diclofenac Sodium 50 mg.
RHEMOFENAX 100 MG SR CAPSULE: Each capsule contains Diclofenac Sodium as
Diclofenac Sodium pellets 100 mg.
PHARMACODYNAMICS
Antirheumatic, anti-inflammatory, analgesic, inhibition of prostaglandin
biosynthesis, 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, the anti-inflammatory and analgesic properties of
Diclofenac Sodium elicit a clinical response characterized by marked relief
from signs and symptoms, eg. pain at rest, pain on movement, morning
stiffness and swelling of the joints, and by an improvement in function.
Diclofenac Sodium is particularly suitable for the treatment of patients
requiring a daily dosage improvement in function. Diclofenac Sodium is
particularly suitable for the treatment of patients requiring a daily dosage
of 100 mg. The fact that it allows once-daily administration facilitates
long-term treatment in particular and helps to prevent the possible dosage
errors. In vitro Diclofenac Sodium does not suppress proteoglycan
biosynthesis in cartilage at concentrations equivalent to those reached in
the human body.
PHARMACOKINETICS:
Absorption.
Tablet / capsule: As with other NSAIDs, its mode of action is not
known; however, its ability to inhibit prostaglandin synthesis may be
involved in the anti-inflammatory effect. Diclofenac is completely absorbed
after their passage through the stomach. Following ingestion of one tablet
with or after a meal, its passage through the stomach is slower than when it
is taken before a meal, but the amount of active substance absorbed remains
the same. In fasting subjects, the mean peak plasma concentration of 1.5
mcg/mL (5 mcmol/liter) is attained on average 2 hours after ingestion of one
tablet of 50 mg. Suppositories of 50 mg produce a corresponding mean peak
plasma concentration of 1.2 mcg / mL (4 mcmol/liter). The plasma
concentrations, as measured by the area under the time-concentration curve,
are in linear relation to the size of the dose.
SR capsule: Diclofenac is completely absorbed from the slow-release
capsules. Owing to slow release of the active substance, peak plasma
concentrations are lower than those attained after administration of
standard dosage forms On the other hand, measurable concentrations can still
be detected several hours after administration. Absorption begins later when
Rhemofenax SR 100 is taken with or after a meal than when it is given on an
empty stomach, but this does not influence the amount of active substance
absorbed. Mean peak plasma concentrations of 0.4 mcg I ml (1.25 µmol/L) are
reached about 5 hrs on average after administration clone slow-release
capsule.
Distribution. No accumulation in plasma occurs after repeated
oral administration if the recommended dosage intervals are observed. 99.7%
of diclofenac is bound to serum proteins mainly to albumin (99.4%).
Diclofenac enters the synovial fluid, where peak concentrations are measured
2.4 hrs after the peak plasma levels have been reached. The apparent
elimination half-life from the synovial fluid is 3-6 hrs. This means that
concentrations of active substance 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. About
half of the active substance is metabolized during its first passage through
the liver ("first pass effect"), which means that the area under the
concentration curve (AUC) is about half as large following oral or rectal
administration as it is following parenteral administration of the same
dose. Biotransformation of diclofenac takes place by glucuronidation partly
of the intact molecule, but mainly by glucuronidation after single and
multiple hydroxylation.
Elimination. The active substance is eliminated from the
plasma with a systemic clearance of 263 ± 56 mL (x t SD). The terminal
half-life is 1-2 hrs. Approximately 60% of the dose administered is excreted
via the kidneys in the form of metabolites; < 1% is excreted as unchanged
substance. The rest of the dose is eliminated in the form of metabolites
through the bile in the faeces. Kinetics in special clinical situations: No
relevant age-dependent differences in absorption, metabolism and excretion
have been observed. In patients with impaired renal function. no
accumulation of the unchanged active substance can be inferred from the
single-dose kinetics under the usual dosage schedule. At a creatinine
clearance of < 10 mL / min, the theoretic) steady-state plasma levels of
metabolites are about 4 times higher than in patients with impaired hepatic
function. The metabolites are nevertheless ultimately cleared through the
bile. In patients with impaired hepatic function (chronic hepatitis,
nondecompensated cirrhosis), the kinetics and metabolism of diclofenac are
the same as in patients without liver disease.
INDICATIONS
Inflammatory and degenerative forms of rheumatism; rheumatoid arthritis and
ankylosing spondylitis, osteoarthritis and spondylarthritis; painful
syndromes of the vertebral column; non-articular rheumatism, painful
post-traumatic and postoperative inflammation and swelling.
RECOMMENDED DOSAGE
Tablet and capsule
Adults: The initial dosage is usually 100-150 mg. In
elderly patients, particularly patients with a low body weight the initial
dosage is 75-150 mg daily.
SR Capsule
Adults: Generally, 1 cap daily. If necessary, the daily dosage can be
increased to 150 mg by giving diclofenac sodium tablets in addition. In
milder cases, where a lower dosage is sufficient, alternative dosage forms
of diclofenac sodium can be used. If symptoms are not severe during the
night or in the morning, the SR capsule should be taken preferably in the
evening. The SR capsules should not be broken or chewed. They should be
swallowed with liquid and taken preferably at mealtimes.
Children: Owing to their high active substance content, diclofenac sodium SR
capsules are not suitable 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.
CONTRAINDICATIONS
Peptic ulcer. Known hypersensitivity to the active substance. Like other
non-steroidal anti-inflammatory agents, diclofenac is contraindicated in
patients in whom attacks of asthma, urticaria or acute rhinitis have been
precipitated by acetylsalicyclic acid or other prostaglandin-synthetase
inhibitors.
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