Esmolol hydrochloride

CLINICAL USE

Beta-adrenoceptor blocker:Short-term treatment of supraventricular arrhythmias (including AF, atrial flutter, sinus tachycardia)Tachycardia and hypertension in the perioperative period

DOSE IN NORMAL RENAL FUNCTION

50–300 micrograms/kg/minute; see product literature for titration schedule

PHARMACOKINETICS

Molecular weight &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp :331.8

%Protein binding &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp :55

%Excreted unchanged in urine &nbsp &nbsp : <2

Volume of distribution (L/kg) &nbsp &nbsp &nbsp :1.9

half-life – normal/ESRD (hrs)&nbsp &nbsp &nbsp :9 minutes/unchanged

DOSE IN RENAL IMPAIRMENT

GFR (mL/MIN)

20 to 50 &nbsp &nbsp : Dose as in normal renal function

10 to 20 &nbsp &nbsp : Dose as in normal renal function

<10 &nbsp &nbsp &nbsp &nbsp &nbsp : Dose as in normal renal function

DOSE IN PATIENTS UNDERGOING RENAL REPLACEMENT THERAPIES

CAPD &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp:Dialysed. Dose as in normal renal function

HD &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp :Dialysed. Dose as in normal renal function

HDF/high flux &nbsp :Dialysed. Dose as in normal renal function

CAV/VVHD &nbsp &nbsp &nbsp:Unknown dialysability. Dose as in normal renal function

IMPORTANT DRUG INTERACTIONS

Potentially hazardous interactions with other drugs

Anaesthetics: enhanced hypotensive effect

Analgesics: NSAIDs antagonise hypotensive effect

Anti-arrhythmics: increased risk of myocardial depression and bradycardia; with amiodarone, increased risk of bradycardia and AV block and myocardial depression

Antidepressants: enhanced hypotensive effect with MAOIs

Antimalarials: increased risk of bradycardia with mefloquine

Antipsychotics: enhanced hypotensive effect with phenothiazines

Calcium-channel blockers: increased risk of bradycardia and AV block with diltiazem; severe hypotension and heart failure occasionally with nifedipine and possibly other dihydropyridines; asystole, severe hypotension and heart failure with verapamil – avoid concomitant verapamil useAntihypertensives: enhanced hypotensive effect; increased risk of withdrawal hypertension with clonidine; increased risk of first dose hypotensive effect with post-synaptic alpha-blockers

Diuretics: enhanced hypotensive effect

Moxisylyte: possible severe postural hypotension

Sympathomimetics: severe hypertension with adrenaline and noradrenaline and possibly dobutamineTropisetron: increased risk of ventricular arrhythmias – use with caution

ADMINISTRATION

Reconstition

–

Route

IV infusion

Rate of Administration

50–300 mcg/kg/minute

Comments

Incompatible with sodium bicarbonate solutionsDilute to a concentration of 10 mg/mL with sodium chloride 0.9% or glucose 5%Local irritation has occurred with infusions of 20 mg/mL

OTHER INFORMATION

Has an active renally-excreted metabolite Hyperkalaemia can occur in CKD 5 Titrate dose according to blood pressure response

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