Pharmacodynamics<unk>  is a highly selective α2-adrenergic agonist. It possesses an α2:α1 selectivity ratio of 1620:1, making it eight times more selective for the α2-receptor than clonidine. Unlike opioids and other sedatives such as propofol,<unk>  is able to achieve its effects without causing respiratory depression.<unk>  induces sedation by decreasing activity of noradrenergic neurons in the locus ceruleus in the brain stem, thereby increasing the downstream activity of inhibitory gamma-aminobutyric acid (GABA) neurons in the ventrolateral preoptic nucleus. In contrast, other sedatives like propofol and benzodiazepines directly increase activity of gamma-aminobutyric acid neurons. Through action on this endogenous sleep-promoting pathway the sedation produced by<unk>  more closely mirrors natural sleep (specifically stage 2 non-rapid eye movement sleep), as demonstrated by EEG studies. As such,<unk>  provides less amnesia than benzodiazepines.<unk>  also has analgesic effects at the spinal cord level and other supraspinal sites. Thus, unlike other hypnotic agents like propofol,<unk>  can be used as an adjunct medication to help decrease the opioid requirements of people in pain while still providing similar analgesia. Pharmacokinetics Intravenous<unk>  exhibits linear pharmacokinetics with a rapid distribution half-life of approximately 6 minutes in healthy volunteers, and a longer and more variable distribution half-life in ICU patients. The terminal elimination half-life of intravenous<unk>  ranged 2.1 to 3.1 hours in healthy adults and 2.2 to 3.7 hours in ICU patients. Plasma protein binding of<unk>  is about 94% (mostly albumin).<unk>  is metabolized by the liver, largely by glucuronidation (34%) as well as by oxidation via CYP2A6 and other Cytochrome P450 enzymes. As such, it should be used with caution in people with liver disease. The majority of metabolized<unk>  is excreted in the urine (~95%). It can be absorbed sublingually.
Dexmedetomidine
Dezocine
Naloxone
Eptazocine
Clopenthixol
Bremazocine
Nalorphine
Ephedrine