Differences between Tolerance and Tachyphylaxis (Desensitization) in Pharmacology 16. Receptor Regulation Principles of Pharmacology Study Guide Not too big. Not too small. Because of their intermediate size, macrocyclic peptides combine the potency and precise targeting of an antibody or biologic therapy with the stability and ease of administration of a Histamine2 receptor antagonists: Rapid development of tachyphylaxis with repeat dosing