'anticholinergic' originates from the prefix 'anti-' (from Greek 'anti' meaning 'against') combined with 'cholinergic' (itself from 'choline' + suffix '-ergic'), where 'anti-' meant 'against' and '-ergic' (from Greek 'ergon') meant 'acting on'.

'anticholinergic' was formed in the 20th century by combining 'anti-' + 'cholinergic'; 'cholinergic' derives from 'choline' (a compound named from Greek 'chole' meaning 'bile') plus the suffix '-ergic' (from Greek 'ergon'), and together they produced the modern medical term 'anticholinergic'.

Initially it denoted being 'against or opposing cholinergic action'; over time it came to refer specifically to substances or properties that block acetylcholine receptors or otherwise inhibit acetinergic (parasympathetic) activity.