CYTOTEC / ARTHROTEC by drdoc on-line

Arthrotec is the combination of Diclofenac and Misoprostol.


Misoprostol - marketed as CYTOTEC, is a prostaglandin analogue, that has been shown to reduce incidence of peptic ulcers from anti-inflammatory drugs.  The FDA has licensed the use of cytotec for prevention of anti-inflammatory related peptic ulceration. This is the first such drug to get this approval.

The drug is now available in many countries combined with Diclofenac.

Diclofenac is an anti-inflammatory agent that has been used widely in the treatment of arthritis and inflammatory disease, but like all anti-inflammatories results in a degree of risk for the development of peptic ulceration. The combination is known as ARTHROTEC.

The combination of the diclofenac and misoprostol, does not seem to reduce the efficacy of each drug compared to when they are used apart.


Arthrotec has been used for some time in South Africa, and I find that the drug is effective and the gastrointestinal side effects regarding ulceration is reduced. The drug is still NOT absolutely guaranteed in terms of its protection against potential ulcers. In one study Arthrotec produced ulceration as seen on endoscopy in 1.5% of patients compared to 10% with piroxicam and 8.6% of naproxen patients. (Woods and Geis Arth rheum 35 suppl 9 s188).


The main side effect is still a vague gastrointestinal discomfort when starting the drug, and I find about 2 in 10 get diarrhoea. BUT this usually is mild and subsides, and only rarely do we have to withdraw the drug. The dose is 1 twice to three times daily with food. It is especially valuable in the high risk patient - previous gastric problems / the elderly.

It has become one of the most widely prescribed antiinflammatories in the UK and is on the increase here.

It is contraindicated in pregnant women or those planning pregnancy.


What is the position/role of the cyclooxygenase COX1 / COX 2 ratio's here?

Diclofenac has one of the highest selective COX2 inhibitions of the current non-steroidal anti-inflammatory drugs.
True COX 2 selective antiinflammatories are now available and offer true COX 2 specificity


Comparison of GI Event Ratings and COX2 / COX1 Ratios

NSAID

Langman [1]odds ratio(risk)

Rodriguez [2]odds ratio(risk)

Engelhardt [3]COX2/COX1ratios

Mitchell[4]COX2/COX1ratios

Ibuprofen

2.0 (1.4 - 2.8)

2.9 (1.7 - 5.0)

-

15

Diclofenac

4.2 (2.6 - 6.8)

3.9 (2.3 - 6.5)

2.2

0.7

Naproxen

9.1 (5.5 - 15.1)

3.1 (1.7 - 5.9)

-

0.6

Indomethacin

11.3 (6.3 - 20.3)

6.3 (3.3 - 12.2)

30

60

Piroxicam

13.7 (7.1 - 26.3)

18.0(8.2 - 39.6)

33

-

References:
1.Langman MJS. Anti-inflammatory drugs and the gut: Ulcerative damage and protection from cancer. Proceedings of Symposium: New Insights into Anti-inflammatory Therapy and its Benefits. Cannes, October 1994.
2. Garcia Rodriguez LA, Jick H Risk of Upper Gastrointestinal Bleeding and Perforation associated with individual non-steroidal anti-inflammatory drugs. Lancet 1994; 343: 769 - 772.
3. Engelhardt G. Bögel R, Schnitzler Chr, Utzmann R. Meloxicam: Influence on Arachidonic acid metabolism. In vitro findings - Part 1. Biochem Pharmacol 1996; 51 (1): 21 - 28
4. Mitchell JA, Akarasereenont P, Thiemermann C, et al. Selectivity of non-steroidal anti-inflammatory drugs as inhibitors of constitutive and inducible Cyclooxygenase. Proc Natl Acad Sci US 1993; 90: 11693 - 11697


In fact addition of misoprostol to Diclofenac -
Reduces the incidence of gastropathy by a further 60%

The Pharmacia Patient Partner Program


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