indication

For the treatment of patients with intermittent lameness or immobility arising from chronic occlusive arterial disease of the limbs.

pharmacology

Pentoxifylline, a synthetic dimethylxanthine derivative structurally related to theophylline and caffeine, is used in the treatment of peripheral vascular diseases and in the management of cerebrovascular insufficiency, sickle cell disease, and diabetic neuropathy.

mechanism of action

Pentoxifylline inhibits erythrocyte phosphodiesterase, resulting in an increase in erythrocyte cAMP activity. Subsequently, the erythrocyte membrane becomes more resistant to deformity. Along with erythrocyte activity, pentoxifylline also decreases blood viscosity by reducing plasma fibrinogen concentrations and increasing fibrinolytic activity. It is also a non selective adenosine receptor antagonist.

toxicity

LD₅₀=1385 mg/kg(orally in mice)

half life

0.4-0.8 hours

route of elimination

Excretion is almost totally urinary; the main biotransformation product is Metabolite V. Essentially no parent drug is found in the urine.

drug interactions

Acenocoumarol: Pentoxifylline may increase the anticoagulant effect of acenocoumarol.

Aminophylline: Pentoxifylline may increase the effect and toxicity of aminophylline.

Anisindione: Pentoxifylline may increase the anticoagulant effect of anisindione.

Dicumarol: Pentoxifylline may increase the anticoagulant effect of dicumarol.

Dyphylline: Pentoxifylline increases the effect and toxicity of theophylline

Oxtriphylline: Pentoxifylline increases the effect and toxicity of theophylline

Theophylline: Pentoxifylline increases the effect and toxicity of theophylline

Warfarin: Pentoxifylline may increase the anticoagulant effect of warfarin.