| Class | Beta blocker |
|---|---|
| Chemistry |
aryloxypropanolamine |
| Routes of administration |
Oral |
| Absorption |
90% oral bioavailability |
| Solubility |
pKa 9.5, good lipid solubility |
| Distribution |
VOD 3.5 L/kg; 30% protein bound |
| Metabolism |
50% hepatic clearance |
| Elimination |
50% renal excretion; half-life 9-12 hrs |
| Time course of action |
Clinical effects persist for longer than the half life would suggest, because they are mainly determined by drug-receptor affinity |
| Target receptor |
Highly selective β1 receptor blocker |
| Mechanism of action |
By binding to Gs-protein coupled β1 receptors, blocks cAMP synthesis |
| Clinical effects |
β1 effects: decreased heart rate, cdecreased contractility, decreased blood pressure, lower myocardial oxygen demand and increased diastolci coronary fillng, and decreased arrhythmogenicity. |
| Literature reference |
Oliver et al (2019) |
| CICM details of understanding | Not specifically listed in the CICM syllabus |
| Mentioned around Deranged Physiology | |
| Related SAQs |