Many NSAIDs have been marketed in topical formulations (mostly as gels) for application over painful muscles or joints. These preparations are being used for osteoarthritis, sprains, sports injuries, tenosinovitis, backache, spondylitis and other forms of soft tissue rheumatism.
TOPICAL NSAIDS
Many NSAIDs have been marketed
in topical formulations (mostly as gels) for application over painful muscles
or joints. These preparations are being used for osteoarthritis, sprains,
sports injuries, tenosinovitis, backache, spondylitis and other forms of soft
tissue rheumatism. It is believed that the drug would penetrate to the
subjacent tissues attaining high concentrations in the affected muscles/joints,
while maintaining low blood levels. Consequently the g.i. and other systemic
adverse effects would be minimised and first pass hepatic metabolism would also
be avoided.
While there is no
doubt about their safety, doubt has been raised about their actual efficacy
over and above a strong placebo effect of local application, massaging and that
due to presence of counter irritants like menthol, methyl salicylate, etc. in
most of them. Often they are used in addition to oral NSAID medication; the
benefit of topical application per se
is difficult to assess.
Measurement of drug
concentration attained in tissues underlying the site of application, as well
as concurrent blood levels has shown that systemic absorption from topical
NSAID preparations is slow taking ~10 times longer time to attain peak
concentration compared to oral dosing. Highest blood levels remain below 15% of
the same dose given orally. This is consistent with their lack of systemic
toxicity. Local concentrations are high upto a depth of 4–6 mm, i.e. in dermis,
but at 25 mm depth in muscles, the concentration is low and nearly the same as
in blood. Marked variation has been noted in the concentration attained in muscles
and joints depending on the type of formulation, depth and distance from site
of application and among different individuals. Reports on the clinical efficacy
of topical NSAIDs are even more variable (range 18–92% response). Better
responses have generally been obtained in short lasting musculoskeletal pain.
Contribution of the NSAID present in the formulation to the beneficial effect,
when elicited, is uncertain.
Diclofenac 1% gel : VOVERAN EMULGEL, RELAXYL GEL, DICLONAC GEL
Ibuprofen 10% gel : RIBUFEN GEL
Naproxen 10% gel : NAPROSYN GEL
Ketoprofen
2.5% gel : RHOFENID GEL
Flurbiprofen
5% gel : FROBEN GEL
Nimesulide 1% gel :
NIMULID
TRANS GEL, ZOLANDIN GEL, NIMEGESICTGEL
Piroxicam 0.5% gel :
DOLONEX
GEL, MOVON GEL, PIROX GEL, MINICAM GEL
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