Esmolol
Esmolol. Ultra-short-acting cardioselective β1 blocker — esterase-mediated hydrolysis gives ~9 min half-life. IV-only; titratable for acute… IV half-life 0.1 h.
Ultra-short-acting cardioselective β1 blocker — esterase-mediated hydrolysis gives ~9 min half-life. IV-only; titratable for acute hypertensive emergencies, intraoperative tachycardia, AF rate control where rapid offset is needed.
PK: A HALF-LIFE THAT IS IN NO ARM OF ITS OWN CITATION. That paper compares healthy controls with two dialysis groups and reports "Mean elimination half-life (t1/2) was 7.2 minutes in control subjects compared with 7.1 and 8.0 minutes for the hemodialysis and CAPD groups" — the stored nine minutes is none of the three. It also states the clearance the pairing has to satisfy, "total body clearance for esmolol was 171.4 +/- 69.8 ... ml/min/kg for the control", which at the seventy-kilogram reference is 720 L/h against a stored assertion of 1100 — HALF AGAIN TOO FAST. Both halves now come from the control arm: the verbatim control half-life, and the volume that the verbatim control clearance implies at that rate. The abstract says the volume "did not differ significantly among the three groups" but never prints it, so that number is DERIVED and is declared as such. TWO ITEMS ARE LOGGED RATHER THAN FIXED. The dose block holds 50 to 300 with a typical of 100 MICROGRAMS, and those are the mcg/kg/MIN INFUSION RATES from this drug label — a rate, not a dose, exactly the remifentanil case, and the schema has no unit for it; as stored the model is dosing roughly three ten-thousandths of the real amount. And the active metabolite has a half-life two orders of magnitude longer than the parent, "more than 42 hours compared with only 4 hours in the control subjects", and has no record.
Pharmacokinetics
- IV — t½ 7 min · F 100% · Vd 124.6 L
Sources: PMID:2563962