'antihyperglycemic' originates from Modern English compound formation combining the prefixes 'anti-' and 'hyper-' with 'glycemic'; 'anti-' (from Greek 'anti-') meant 'against', 'hyper-' (from Greek 'hyper-') meant 'over' or 'excess', and the root 'glyc-' (from Greek 'glykys') meant 'sweet' or 'sugar'.

'antihyperglycemic' was formed in modern medical English by joining elements from Greek and Late Latin (e.g., Greek 'hyper-' + Late Latin/Neo‑Greek 'glycaemia' → English 'glycemic'), creating a descriptive compound rather than evolving from a single older English word.

Initially the elements literally signified 'against excess sugar (in the blood)'; over time the compound came to mean specifically 'having or being an agent that reduces high blood glucose' in clinical and pharmacological usage.