Background: Local anaesthetics block the peripheral nerves and are used to prevent pain, during surgical and dental procedures. The primary object of this investigation was to compare and evaluate the efficacy of 4% Articaine hydrochloride with 1:100000 adrenaline and 2% Lignocaine hydrochloride with 1:80000 adrenaline during orthodontic extraction of maxillary first premolar. Methods: This prospective randomized, double-blind study was conducted from February 2013 to September 2014 on 43 patients less than 40 years of age requiring bilateral maxillary first premolar extractions for orthodontic purposes. Each patient was randomly assigned to receive either 2% lignocaine hydrochloride or 4% articaine hydrochloride for premolar extraction of one side and another solution was administered for the premolar extraction of contralateral side spaced 1 to 3 weeks apart.In each patient, the difference in the pain levels,onset of anesthesia and duration of anesthesiawas assessed on the administration of lignocaine hydrochloride and articaine hydrochloride. Results: There was statistically no significant difference in pain levels between orthodontic extraction of maxillary first premolar between the Articaine and Lignocaine groups. (p__ampersandsigngt;0.05).The Articaine group had an earlier onset of anaesthesia after buccal infiltration and palatal infiltration as compared to the lignocaine group. The mean duration of anaesthesia was longer in the articaine group as compared to the highly significant lignocaine group. Conclusions: Articaine can be used as a suitable alternative to lignocaine in the extraction of maxillary premolars for orthodontic reasons with clinical advantages like faster time of onset, longer duration, and greater diffusing property over lignocaine.