Topical NSAIDs

| Home | | Pharmacology |

Chapter: Essential pharmacology : Nonsteroidal Anti-inflammatory Drugs And Antipyreticanalgesics

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.

 Preparations

 

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

 

Contact Us, Privacy Policy, Terms and Compliant, DMCA Policy and Compliant

TH 2019 - 2022 pharmacy180.com; Developed by Therithal info.