TOLRESTAT

Description

Tolrestat is a long-acting aldose reductase inhibitor reportedly useful in the prophylaxis of diabetic neuropathy, retinopathy and cataracts.

Description

Tolrestat is an aldose reductase inhibitor (IC₅₀ = 35 nM for the bovine lens enzyme). Dietary administration of tolrestat decreases sciatic nerve galactitol accumulation in a rat model of galactosemia (ED₅₀ = 7.3 mg/kg per day) and sciatic nerve sorbitol accumulation (ED₅₀ = 4.8 mg/kg per day) in a rat model of diabetes induced by streptozotocin (STZ; ). It also decreases urinary total protein exretion in a rat model of STZ-induced diabetes when administered at a dose of 25 mg/kg per day. Topical administration of tolrestat (2 and 3% in 10 μl four times per day) decreases levels of galactitol in the lens of and inhibits cataract formation in rats fed a high-galactose diet.

Originator

American Home Products (USA)

The Uses of TOLRESTAT

Alredase (Wyeth-Ayerst).

The Uses of TOLRESTAT

Tolrestat is an aldose reductase inhibitor.

Definition

ChEBI: Tolrestat is a member of naphthalenes. It has a role as an EC 1.1.1.21 (aldehyde reductase) inhibitor.

brand name

Alredase

Biochem/physiol Actions

Tolrestat is considered to be effective in treating the consequences of diabetes including neuropathy, nephropathy, retinopathy and esophageal motility and vibration perception. Tolrestat is also believed to have lesser or no toxic effects.