Anti-inflammatories - the approach of drdoc on-line   

Anti-inflammatories - NSAID's

With the thousand of medications and NSAIDs available -
How does one approach the choice of agent ?
The answer is that everyone is different - and the choice has to be customized to the individual.

Nevertheless release of the COXIBs - the specific COX-2 drugs has made this a much easier task with reduced side effects. They have revolutionized the treatment of arthritis.


The Classification of NSAID's


1. CARBOXYLIC ACIDS
PHENYL ACETIC ACIDS
DICLOPHENAC
FENCLOFENAC
CARBO HETEROCYCLIC ACIDS
INDOMETHACIN
SULINDAC
TOLMETIN
SALICYLIC ACIDS
ASPIRIN
PROPRIONIC ACIDS
IBU/KETO/FENO/FLURBI PROFEN
NAPROXEN
ANTHRANILIC ACIDS
MECLOFENAMIC ACID
FLUFENAMIC ACID

2. PYRAZOLONES BUTAZONES PROPAZONES
OXICAMS
PIROXICAM
TENOXICAM
MELOXICAM

3. COXIBs
Celecoxib
Valdecoxib
Rofecoxib
Lumiracoxib
Etoricoxib


Therapy depends on :
The degree of problem.
The site of the problem.
The degree of inflammatory involvement.
It is the latter that largely determines the requirement for a medication such as a nonsteroidal anti-inflammatory drug - NSAID.


If there's no inflammation, a analgesic may only be required.
For example :
For mild discomfort - paracetamol / Acetaminophen only.
More severe pain - combination with a low dose codeine.
More severe - propoxyphene.


How do you know if there is inflammation ?


The answer to that is generally, if you have:
Stiffness. - the more the degree and in particular the morning symptom of stiffness.
Swelling - NOT BONE thickening - but soft tissue swelling.
Heat in the joints on examination.


Lets assume that you DO need a NSAID....

The answer now is so much easier since the release of specific COX - 2 drugs such as Celecoxib (Celebrex) and Valdecoxib (Bextra). However a rival drug in the same class, Rofecoxib (Vioxx) has recently been withdrawn by the MERCK corporation because of a increased association with myocardial infarction. My personal preference in the past between Celebrex and Vioxx (having been involved in doing trials on both drugs), has been Celebrex, as Vioxx has been noted to have problems of fluid retention and increased hypertension problems. Recently Vioxx was withdrawn leaving only Celebrex and Bextra available. Both are sulphur drugs and cannot be used with sulphur hypersensitivity. The FDA is re-evaluating these drugs and assessing cardiac concerns, but at this stage there is no definite evidence that they have the same risk profile as Rofecoxib.
If for whatever reason, one cannot take either Celecoxib or Valdecoxib, then one may have to resort to the older NSAIDs. It is with these agents that one has to be cautious about the potential side effects of the older drugs - especially the gastropathy and renal and platelet inhibition problems.

My preference to avoid gastropathy problems in the NSAIDS, is the combination of the NSAID, where possible, with a gastric mucosal barrier protector - prostaglandin E2 agonist called misoprostol (Cytotec). These are discussed elsewhere on the web-site.

In fact I commonly use a combination of misoprostol and diclofenac tablet, available in South Africa, and other countries as a single tablet (known as Arthrotec), but this is not yet available in the United States of America. In the USA, a standard NSAID could be taken in addition to misoprostol, separately.

There are certain contraindications to misoprostol - Especially pregnancy, and it should NOT be used in the absence of contraception, if used in patients of childbearing age groups. The use of cytoprotection reduces ulcer related problems by over 50%. It therefore becomes even more appropriate when used in high risk patients - i.e. previous ulcer, or the elderly.

Protection is NOT offered by use of H2 antagonists such as Zantac, or by Antacids. In fact these may conceal development of ulcer with NSAIDS. High dose famotidine has shown some protection. The proton pump inhibitors, such as prilosec, also do NOT offer protection. Only misoprostol is registered by the FDA for gastro-protection.


What other NSAIDS do I like...should the above be contraindicated....


Well - there are so many..........
Some people respond to some, others respond to others......
I use a small number and tend to use long acting dosage preparations......



Voltaren - diclofenac : This is available in several preparations. I tend to use the long acting preparations - especially Voltaren SR 100mg as a nocte dose ...which provides help for the morning stiffness seen in inflammatory arthritis. Other useful preparations are the 75mg preparation as a twice daily medication, or the Voltaren GT 50mg preparation used up to three times daily for adults.

Piroxicam beta cyclodextran (Brexecam) 20mg at night.
The cyclodextran is a molecular layer, around the active compound, that results in the release of the active ingredient in the small bowel, beyond the stomach. Gastroprotection is claimed by the manufacturer.

Piroxicam (Feldene) 20mg at night.

Indomethacin (indocid) long acting preparation LA 100 mg given at night.

Ketoprofen (Oruvail)200 mg given at night.

Ibuprofen (Brufen Retard- Long acting ) 2 at night

Diclofenac 100mg Long acting (Voltaren SR) at night

Meloxicam -(Mobic) 7.5mg - is a first generation NSAID which is a so called "selective Cox 2", and more gastric friendly. But I find requires a increase in dose to 15mg frequently, and have NOT personally found it to be advantageous at this time. It is NOT a specific COX 2 inhibitor drug.

Nabumetone- Relifen is also "more gastro friendly", but I haven't been too impressed with its effectiveness.

Tenoxicam (Tilcotil) 20mg at night.

The list is endless......

Generic preparations are sometimes used by myself - although I personally don't find them as effective as the original compounds-despite manufacturer claims.


What other preparations are available that I use:


1. Suppositories
The use of a nocturnal suppository - is I find very effective for the morning stiffness of inflammatory disease, such as Rheumatoid arthritis and Spondyloarthropathy.
My choice is either indomethacin, diclofenac or Tenoxicam suppositories.

2. Injectables
These are used for short term or single use only for acute problems and arthritis flares.
My choice is Diclofenac or ketoprofen or Tenoxicam

3. Poultices.
Available in South Africa, and Japan, is a anti-inflammatory poultice - This contains Flurbiprofen.
I use it for soft tissue rheumatism and localised inflammation. I find it very effective. I also use it over some joints - including the knee, ankle and low back.

4. Gels.
These are generally only mildly effective, for soft tissue rheumatism, and don't really adequately relieve deeper structures. They must be applied at least twice a day.
Choices - Methyl-salicylate gel, ketoprofen, Diclofenac, naproxen gel.

5. Combination agents.
Occasionally it is difficult to get control of symptoms, and a morning NSAID, combined with a nocturnal long acting type (of a different group), or a suppository, provides effective cover.

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drdoc on-line
Rheumatologist
Cape Town
South Africa
Feb 2000
Copyright.
Revised
Jan 2005


Original article:
Please note this reflects my personal opinion, and does not and should not be used by you without first consulting your own Doctor in this regard.