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REVIEW - MTX in RA

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Institute of Pharmacology

Polish Academy of Sciences

Pharmacological Reports

2006

" Methotrexate in rheumatoid arthritis "

Excerpt:

Folate supplementation during MTX therapy

Folic acid and folinic acid reduce some adverse

events (gastrointestinal intolerance, stomatitis, hepatotoxicity,

hyperhomocysteinaemia, alopecia) associated

with MTX, so most of rheumatologists recommended

all patients taking MTX to take them as well

even though this may be accompanied by a slight reduction

in efficacy. A very important report on folic

acid supplementation was published by et al.

[76]. The patients received placebo or 5 or 27.5 mg of

folic acid weekly. This study demonstrated that folate

intake leads to a reduction in side effects without reduced

efficacy. In a 48-week trial, Hoekstra et al. analyzed

the toxicity of MTX in patients who received either

folic acid or placebo. The addition of folate was

strongly associated with a lack of hepatotoxicity [43].

Van Ede et al. demonstrated in a randomized controlled

trial that treatment with either folate regimen

resulted in a reduction in the incidence of liver enzyme

elevations [111]. Patients receiving folate were

less likely to discontinue MTX than patients in the

placebo group, but folate supplementation was associated

with higher mean doses of MTX. Another reason

to use folic acid in MTX-treated patients is for its effectiveness

in reducing plasma homocysteine levels.

Hyperhomocysteinemia is an independent risk factor

for coronary artery disease, and premature mortality

in patients with RA is caused by accelerated atherosclerosis.

Slot demonstrated in a small study that Phomocysteine

concentrations negatively correlated

with erythrocyte folate after four weeks. P-homocysteine

and erythrocyte folate were measured before

the start of MTX treatment, after four weeks of MTX

treatment, and after further four weeks of treatment

with MTX supplemented with folic acid (15 mg per

week). The author concluded that treatment with MTX

induced a significant rise in P-homocysteine that was

neutralized by folic acid supplementation [103].

After a meta-analysis, Whittle at al. proposed that

folic acid supplements be prescribed routinely to all

patients receiving MTX for the treatment of RA. They

recommended 5 mg of oral folic acid given in the

morning following the day of MTX administration. The

folic acid dose can be increased if the side effects continue.

Folate supplements do not appear to significantly reduce

the effectiveness of MTX in the treatment of RA, so

the benefits outweights the risk [119]. In patients in whom

folic acid is not adequate, one can try using folinic acid

(initial dose: 5 mg/week) administrated 24 h after MTX.

Discussions about the necessity of folic acid supplementation

were resumed after the publication of

a post hoc analysis of two randomized, controlled

studies by Khanna et al. Nine to 21% fewer MTX treated

RA patients taking folic acid had American

College of Rheumatology (ACR) 20%, 50%, or 70%

improvement at 52 weeks compared with those who did

not receive folic acid, so some rheumatologists believe

that prophylactic prescription of folic or folinic acid

to all RApatients receiving MTX is not required [26, 52].

***************************************

Read the full article here:

http://www.if-pan.krakow.pl/pjp/pdf/2006/4_473.pdf

Not an MD

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