Alpha-adrenergic agonist

Alpha-adrenergic agonists are a class of

Although complete selectivity between receptor agonism is rarely achieved, some agents have partial selectivity. NB: the inclusion of a drug in each category just indicates the activity of the drug at that receptor, not necessarily the selectivity of the drug (unless otherwise noted).

α₁ agonist

• Adrenoswitch-1 (photoswitchable partial α₁ agonist and light-controlled mydriatic)[1]
• Methoxamine
• Midodrine
• Metaraminol
• Phenylephrine^[2]
• Amidephrine^[3]
• Sdz-nvi-085 [104195-17-7].

α₂ agonist

• Clonidine (mixed alpha2-adrenergic and imidazoline-I1 receptor agonist)
• Dexmedetomidine
• Fadolmidine
• Guanfacine,^[4] (preference for alpha2A-subtype of adrenoceptor)
• Guanabenz (most selective agonist for alpha2-adrenergic as opposed to imidazoline-I1)
• Guanoxabenz (metabolite of guanabenz)
• Guanethidine (peripheral alpha2-receptor agonist)
• Xylazine(not for human use),^[5]
• Tizanidine
• Methyldopa
• Methylnorepinephrine
• Norepinephrine^[6]
• antagonist at the α_2A and α_2B subtypes.^[7][8]
• amitraz^[9]
• Detomidine^{[citation needed]}
• Lofexidine, an α_2A adrenergic receptor agonist.^[10]
• Medetomidine, an α2 adrenergic agonist.^[11]

Nonspecific agonist

Nonspecific agonists act as agonists at both alpha-1 and alpha-2 receptors.

• Xylometazoline^[12]
• Oxymetazoline^[13]
• Apraclonidine^{[citation needed]}
• Cirazoline^[14][15]
• Epinephrine^[16]

The following agents are also listed as agonists by MeSH.^[17]

• ergotamine
• etilefrine
• indanidine
• mephentermine
• metaraminol
• methoxamine
• mivazerol
• naphazoline
• norfenefrine
• octopamine
• phenylpropanolamine
• propylhexedrine
• rilmenidine
• romifidine
• synephrine
• talipexole

Clinical significance

Alpha-adrenergic agonists, more specifically the auto receptors of alpha 2 neurons, are used in the treatment of glaucoma by decreasing the production of aqueous fluid by the ciliary bodies of the eye and also by increasing uveoscleral outflow. Medications such as clonidine and dexmedetomidine target pre-synaptic auto receptors, therefore leading to an overall decrease in norepinephrine which clinically can cause effects such as sedation, analgesia, lowering of blood pressure and bradycardia. There is also low quality evidence that they can reduce shivering post operatively.^[18]

The reduction of the stress response caused by alpha 2 agonists were theorised to be beneficial peri operatively by reducing cardiac complications, however this has shown not to be clinically effective as there was no reduction in cardiac events or mortality but there was an increased incidence of hypotension and bradycardia.^[19]

Alpha-2 adrenergic agonists are sometimes prescribed alone or in combination with stimulants to treat ADHD.^[20]

See also

References