Details About Overdose or Poisoning Generic Salt :: Esmolol
Drug Pharmacology ::
I. Pharmacology. Esmololis a short-acting, IV, cardioselective beta-adrenergic blocker with nointrinsic sympathomimetic or membrane-depressant activity. In usualtherapeutic doses, it causes little or no bronchospasm in patients withasthma. Esmolol produces peak effects within 6–10 minutes ofadministration of an intravenous bolus. It is hydrolyzed rapidly by redblood cell esterases, with an elimination half-life of 9 minutes;therapeutic and adverse effects disappear within 30 minutes after theinfusion is discontinued.
Drug Indications ::
Rapidcontrol of supraventricular and ventricular tachyarrhythmias andhypertension, especially if caused by excessive sympathomimeticactivity (eg, stimulant drugs, hyperthyroid state).
Reversalof hypotension and tachycardia caused by excessive beta-adrenergicactivity resulting from theophylline or caffeine overdose.
Controlof ventricular tachyarrhythmias caused by excessive myocardialcatecholamine sensitivity (eg, chloral hydrate and chlorinatedhydrocarbon solvents).
Drug Contra-Indications ::
Contraindicationsinclude hypotension, bradycardia, and congestive heart failuresecondary to intrinsic cardiac disease or cardiac-depressant effects ofdrugs and toxins (eg, cyclic antidepressants and barbiturates).
Hypertensioncaused by alpha-adrenergic or generalized stimulant drugs (eg, cocaine,amphetamines), unless esmolol is coadministered with a vasodilator (eg,nitroprusside or phentolamine). Paradoxic hypertension may result froman unopposed alpha effect, although it is less likely than thatassociated with the use of a non-specific beta-adrenergic blocker(propranolol).
Drug Adverse Effects ::
IV. Adverse effects
Hypotensionand bradycardia may occur, especially in patients with intrinsiccardiac disease or cardiac-depressant drug overdose.
Bronchospasmmay occur in patients with asthma or chronic bronchospasm, but it isless likely than with propranolol or other nonselective beta blockersand is rapidly reversible after the infusion is discontinued.
Esmololmay mask physiologic responses to hypoglycemia (tremor, tachycardia,and glycogenolysis) and therefore should be used with caution inpatients with diabetes.
Use in pregnancy. FDAcategory C (indeterminate). This does not preclude its short-term usefor a seriously symptomatic patient (see Table III–1). High-doseinfusion may contribute to placental ischemia.
Drug Lab Interactions ::
Drug or laboratory interactions
Esmolol may transiently increase the serum digoxin level by 10–20%, but the clinical significance of this is unknown.
Recoveryfrom succinylcholine-induced neuromuscular blockade may be delayedslightly (5–10 minutes). Similarly, esmolol metabolism may be inhibitedby anticholinesterase agents (eg, organophosphates).
Esmolol is not compatible with sodium bicarbonate solutions.
Drug Dose Management ::
Dosage and method of administration
Dilutebefore intravenous injection to a final concentration of 10 mg/mL with5% dextrose, lactated Ringer’s injection, or saline solutions.
Giveas an intravenous infusion, starting at 0.025–0.05 mg/kg/min andincreasing as needed up to 0.2 mg/kg/min (average dose 0.1 mg/kg/min).Steady-state concentrations are reached approximately 30 minutes aftereach infusion adjustment. A loading dose of 0.5 mg/kg should be givenover 1 minute if more rapid onset of clinical effects (5–10 minutes) isdesired.
Infusionrates greater than 0.2 mg/kg/min are likely to produce excessivehypotension. At rates greater than 0.3 mg/kg/min, the beta-blockingeffects lose their beta-1 selectivity.
Drug Chemical Formulations ::
Parenteral. Esmololhydrochloride (Brevibloc), 2.5 g in 10-mL ampules (250 mg/mL), 100 mgin 10-mL vials (10 mg/mL), and 20 mg/mL (double strength) in 5-mL vialsand 100-mL bags.
The suggested minimum stocking level to treat a 70-kg adult for the first 24 hours is 2 ampules (250 mg/mL, 10 mL) or 25 vials (10 mg/mL, 10 mL).