Faulds D, Goa KL, Benfield P, et al.
Drugs. Date of publication 1993 Jun 1;volume 45(6):953-1040.
1. Drugs. 1993 Jun;45(6):953-1040. doi: 10.2165/00003495-199345060-00007.
Cyclosporin. A review of its pharmacodynamic and pharmacokinetic properties, and
therapeutic use in immunoregulatory disorders.
Faulds D(1), Goa KL(1), Benfield P(1).
Author information:
(1)Adis International Limited, 41 Centorian Drive, Private Bag 65901, Mairangi
Bay, Auckland 10, New Zealand.
Erratum in
Drugs. 1993 Sep;46(3):377.
Drugs 1993 Sep;46(3):377.
Cyclosporin is a lipophilic cyclic polypeptide which produces calcium-dependent,
specific, reversible inhibition of transcription of interleukin-2 and several
other cytokines, most notably in T helper lymphocytes. This reduces the
production of a range of cytokines, inhibiting the activation and/or maturation
of various cell types, including those involved in cell-mediated immunity. Thus,
cyclosporin has immunosuppressive properties, and has a proven place as first
line therapy in the prophylaxis and treatment of transplant rejection.
Cyclosporin has also been evaluated in a large range of disorders where
immunoregulatory dysfunction is a suspected or proven aetiological factor, and
this is the focus of the present review. In patients with severe disease
refractory to standard treatment, oral cyclosporin is an effective therapy in
acute ocular Behçet's syndrome, endogenous uveitis, psoriasis, atopic dermatitis,
rheumatoid arthritis, active Crohn's disease and nephrotic syndrome. Concomitant
low dose corticosteroid therapy may improve response rates in some disorders. The
drug can be considered as a first line therapy in patients with moderate or
severe aplastic anaemia who are ineligible for bone marrow transplantation, with
the additional benefit of reducing platelet alloantibody titres. It may also be
of considerable therapeutic benefit in patients with primary biliary cirrhosis,
particularly those with less advanced disease. Limited evidence suggests
cyclosporin is effective in patients with intractable pyoderma gangrenosum,
polymyositis/dermatomyositis or severe, corticosteroid-dependent asthma. Indeed,
the steroid-sparing effect of cyclosporin is a significant advantage in a number
of indications. Furthermore, the drug has shown some efficacy in a wide range of
other, generally uncommon disorders in which controlled clinical trials are
lacking and/or are unlikely to be performed. Cyclosporin does not appear to be
effective in patients with allergic contact dermatitis, multiple sclerosis or
amyotrophic lateral sclerosis. It is only temporarily effective in patients with
type I (insulin-dependent) diabetes mellitus and should not be used in this
indication. To avoid relapse after control of active disease, patients should
receive cyclosporin maintenance therapy at the lowest effective dosage. However,
maintenance therapy appears to be of no benefit in patients with Crohn's disease
and cyclosporin should be discontinued in these patients once active disease is
controlled. Hypertrichosis, gingival hyperplasia, and neurological and
gastrointestinal effects are the most common adverse events in cyclosporin
recipients, but are usually mild to moderate and resolve on dosage reduction.
Changes in laboratory variables indicating renal dysfunction are relatively
common, although serious irreversible damage is rare.(ABSTRACT TRUNCATED AT 400
WORDS)
DOI: 10.2165/00003495-199345060-00007
PMID: 7691501 [Indexed for MEDLINE]
