Download (Nimesulide Tablets*) - Amson Vaccines and Pharma, Pvt Ltd

inflammatory disorders.
Composition:
Amsolide is available in tablet form. Each
tablet contains Nimesulide B.P 100 mg.
*Amson Specification
Pharmacodynamics:
Amsolide is a nonsteroidal anti-inflammatory
drug (NSAID) that selectively inhibits cyclooxygenase 2 the inducible form of the
enzyme found almost exclusively in
inflammatory tissues but largely devoid of
physiological activity in healthy tissues, in
which cyclo-oxygenase 1 plays important
regulating roles (particularly gastric and renal
physiological control). Most NSAIDs block
both cyclo-oxygenase 1 and cyclooxygenase 2, and as a result, they impair the
production of prostaglandins critical to gastric
mucosal protection and renal function, which
results in Clinically significant adverse
reactions especially regarding the risk of
gastrotoxicity. Amsolide is the leading
molecule of a new chemical class
Sulphonanilides, which has shown a
significant inhibitory selectivity towards
cyclooxygenase 2 without affecting cyclooxygenase 1, this results in equivalent
efficacy against pain and inflammation but
with a better safety profile, particularly at the
gastrointestinal level. The anti-inflammatory,
analgesic and antipyretic activities of
Amsolide have been demonstrated in
number of experimental models and in
numerous clinical trials. Amsolide exhibit
potency in reducing inflammation similar to or
greater than that of Indomethacin,
Diclofenac, Piroxicam and Ibuprofen, in
standard animal models such as
carrageenin-induced rat paw edema and
inflammation, ultraviolet light induced
erythema in guinea pigs and adjuvant
arthritis in rats. The analgesic potency of
Amsolide was similar to that of Ibuprofen and
less than that of Indomethacin in an acetic
acid writhing test rats and acetic acid and
acetylcholine-writhing tests in mice. Amsolide
has shown superior antipyretic potency to
Indomethacin, Ibuprofen, Aspirin and
Paracetamol (Acetaminophen) in rats with
yeast-induced fever.
Amsolide appears to exert its therapeutic
effects through a variety of mechanisms
viz.
• Selective inhibition of COX-2.
• Inhibition of superoxide anions from
stimulated polymorphs.
•
Inhibition of platelet activating factor
synthesis.
• Prevention of Bradykinin/Cytokines
stimulation of nerves.
• Scavenging of histamine release.
• Prevention of cartilage damaged by
inhibition of metalloprotease synthesis.
Pharmacokinetics:
Amsolide is rapidly & extensively absorbed
after oral administration of 50-200 mg to
healthy volunteers. Peak serum
concentration of 1.98 to 9.85 mg/L are
achieved within 1.22 to 3.17 hours. Oral
absorption of Amsolide is nearly complete.
Concomitant administration of food may
decrease the rate but not the extent of
absorption of Amsolide . Plasma binding was
high (99%) and the apparent volume of
distribution ranged from 0.19 to 0.35 L/kg.
Amsolide is extensively metabolized to
several metabolites which are excreted
mainly in the urine (70%) and in faeces
(20%).
In patients with moderately impaired renal
function (creatinine clearance 1.8 to 4.8 L/h,
(30 to 80 ml/min), in children and in elderly
volunteers, the pharmacokinetic profile of
Amsolide is not significantly altered. In
patients-with moderate renal impairment,
slight accumulation of 4-Hydroxy Nimesulide
was noted, which is its main metabolite,
however, the clinical significance of this
finding is unknown. In children, compared
with values for adult healthy volunteers, Tmax
and Tl/2 β values were similar.
Indications:
Amsolide is indicated in the treatment of
variety of painful inflammatory conditions like
Bursitis, Tendonitis, Osteoarthritis,
Rheumatoid arthritis, Post operative pain,
Sports injuries, inflammatory disorders of
E.N.T., Dental surgery and Gynecological
— Hypersensitivity to the drug,
hypersensitivity to the sulfa group,
acetyl-salicylic acid and other antiinflammatory drugs (NSAIDs).
— Gastro-intestinal hemorrhage or gastroduodenal ulcer in active phase.
—
Pregnancy & lactation.
— Severe renal insufficiency.
— Impaired liver function.
Precautions:
Symptoms/history of gastro-intestinal
disease, impaired hepatic, cardiac or renal
function, pregnancy and lactation, Porphyria,
in the elderly patients with extracellular
volume depletion from any cause. Patients
on diuretics, anti-coagulants, or antidiabetics.
If in exceptional cases prolonged treatment is
necessary, periodic monitoring of liver
function should be carried out and blood
counts are recommended.
— Must be used with caution in patients
with hemorrhagic disease.
—
In renal insufficiency the dose should
be reduced.
— Product can cause water retention
(edema), particular caution should be
adopted in the treatment of the
hypertensive patients and with reduced
cardiac functions.
Drug Interactions:
— Must be administered with caution in
patients under treatment with
anticoagulants or the drugs that inhibit
platelet aggregations.
Warnings:
— To be used exclusively in the adult
patients. Paediatric use is not
recommended.
— At this stage basic research has not
shown any embryo-fetal toxicity for
Amsolide, but the administration during
pregnancy and lactation is discouraged,
as for all new drugs.
— Drug should be administered with the
particular care in elderly patients.
Side effects:
G .I .T. : Nausea, gastralgia, pyrosis
Skin : Urticarial cutaneous eruptions.
C.N.S. : Headache, vertigo & sleepiness
others are rare like oliguria, edema,
petechias, thrombocytopenia
Hypersensitivity reactions.
Although no case has been reported for
Amsolide, however, it should be remembered
that as in case of other NSAIDs, the drug can
trigger severe hypersensitivity reactions.
Dosage & Administration:
Adults:
100 mg tablet twice in a day, dose can be
increased to 200 mg twice daily if necessary.
The dosage in the elderly patients must
carefully be established by the physician.
Caution:
To be dispensed only on the prescription of a
registered medical practitioner.
Store in a cool and dry place. Protect from
light. Keep out of the reach of children.
Presentation:
Blister pack of 3 x 10’s
— Hydantoin or sulfa drugs should not be
given during Amsolide therapy.
— Clinically important interactions
involving Amsolide have
not been described.
Manufactured by:
AMSON VACCINES & PHARMA (PVT) LTD.
154, Industrial Triangle, Islamabad, Pakistan.
ISO 9001, 14001 & 18001 Certified.
AMSON
02-04-0005C
(Nimesulide Tablets*)
Contra-indications: