Table 1. Major differences in the pharmacology of clonidine and dexmedetomidine.
Clonidine | Dexmedetomidine* |
Developed in the 1960s | Developed in the 1980s |
Clinical practice: originally prescribed as a antihypertensive then as an analgesic in chronic pain (1983) | Clinical practice: tested in volunteers (1991) then used as a sedative in ICU (1999) |
Ratio α2:α1 receptor binding is 200:1 | Ratio α2:α1 receptor binding is 1600:1 |
Octanol/buffer partition coefficient: 0.8 | Octanol/buffer partition coefficient: 2.8 More lipophilic (3.5-fold) than clonidine |
Plasmatic half-life T½: 9-12 hours | Plasmatic half-life T½: 2-2.5 hours |
Protein binding: 50% | Protein binding: 94% |
*Detomidine, the racemic mixture, is widely used in veterinary medicine; dexmedetomidine is the active isomer of medetomidine. ICU, intensive care unit.