'antitabetic' originates from the Greek-derived prefix 'anti-' (from Greek 'anti' meaning 'against') combined with 'diabetic' (from Greek 'diabētēs'), where 'diabētēs' referred to the condition now called diabetes.

'antitabetic' is a modern English medical formation combining 'anti-' + 'diabetic'. 'Diabetic' itself comes from Greek 'diabētēs' (via Late Latin 'diabetes' and Medieval Latin/French forms) and produced English 'diabetic'; 'antitabetic' was later coined to denote agents opposed to diabetes.

Initially formed to mean 'against or opposing diabetes,' the term has retained this literal medical sense and is used to describe drugs or measures that combat diabetes.