Adrenergic Agonists
Overview
Overview
Adrenergic agonists activate alpha or beta receptors directly or increase endogenous catecholamine activity indirectly. They range from emergency vasopressors to inhaled bronchodilators and centrally acting sympatholytics.
Classification
Classification
Direct agonists are grouped by alpha-1, alpha-2, beta-1, beta-2, beta-3 or mixed receptor activity. Indirect and mixed sympathomimetics increase synaptic catecholamines without being purely receptor-selective agonists.
Mechanism of action
Mechanism of action
Alpha-1 activation causes smooth-muscle contraction; central alpha-2 activation reduces sympathetic outflow. Beta-1 increases cardiac rate and force, beta-2 relaxes bronchial and uterine smooth muscle, and beta-3 relaxes detrusor during bladder filling.
Important members
Important members
Examples include phenylephrine and midodrine; clonidine, methyldopa and dexmedetomidine; dobutamine; salbutamol and formoterol; mirabegron; and mixed catecholamines such as epinephrine and norepinephrine.
Clinical uses
Clinical uses
Uses include hypotension and shock, anaphylaxis, bronchospasm, chronic obstructive airway disease, overactive bladder, sedation, ADHD, orthostatic hypotension and selected obstetric or ophthalmic indications.
Adverse effects
Adverse effects
Adverse effects include hypertension, arrhythmia, tremor, anxiety, ischaemia and hypokalaemia. Central alpha-2 agonists cause sedation, dry mouth and bradycardia, while beta-3 agonists can increase blood pressure.
Contraindications and precautions
Contraindications and precautions
Avoid indiscriminate use in severe hypertension, unstable arrhythmia or ischaemic heart disease. Long-acting beta-2 agonists in asthma should be used according to controller-therapy guidelines rather than as unsupervised monotherapy.
References
- Farzam K, Kidron A, Lakhkar AD. Adrenergic Drugs. NCBI Bookshelf. Updated 2023. SOURCE:NCBI:ADR_DRUGS:2023
- Horowitz AJ, Menice CB. Sympathomimetics. NCBI Bookshelf. Updated 2023. SOURCE:NCBI:SYMPATHOMIMETICS:2023