ADMET-Absorption, Distribution, Metabolism, Excretion, and Toxicity

StatusFDA approved
AdministrationN/A
PharmacologyAn anti-diabetic drug used to treat type 2 diabetes mellitus and, in some countries, prediabetes.

Absorption_value2.0
Absorption (description)35% of an oral dose is absorbed as the metabolites and only 1 to 2% absorbed as the active drug.
Caco_2N/A
Bioavailability1.0

MetabollsmGastrointestinal tract. Acarbose is metabolised by intestinal digestive enzymes and by the microbial flora of the gastro-intestinal tract, where the majority of the active unchanged drug remains. The major metabolites are the 4-methylpyrogallol derivatives (sulfate, methyl and glucuronide conjugates) produced by biotransformation (mainly reduction and conjugation).
Half life2 h

ExcretionAfter intravenous administration, approximately 90% of a dose is excreted in urine, within 48 h, as the active drug (parent drug or active metabolite). After oral administration, <2% of the dose is recovered in urine as the active drug and 34% as metabolites, and approximately 50% as the unabsorbed drug in faeces (within 96 h post ingestion).
Urinary ExcretionN/A
CleranceTotal body clearance, 600 L/h.

ToxicityAcarbose is associated with hepatotoxicity and has low toxicity by ingestion, subcutaneous and intravenous routes. A 360 mg/kg body weight dose in women over a 60-day period and given intermittently in a number of separate and discrete doses can cause non-fatal toxic effects. Acarbose competitively and reversibly inhibits the α-glucosidase enzymes; glucoamylase, sucrase, maltase and isomaltase, found in the small intestine, and this delays hydrolysis of complex carbohydrates. It is unlikely to produce hypoglycaemia in overdose, but abdominal discomfort and diarrhoea may occur.
LD50 (rat)N/A
LD50 (mouse)N/A