Chemical formula: C₁₆H₂₅NO₄ Molecular mass: 295.374 g/mol PubChem compound: 59768
Esmolol interacts in the following cases:
The combination of esmolol with ganglion blocking agents can enhance the hypotensive effect.
NSAIDs may decrease the hypotensive effects of beta-blockers.
The effects of esmolol may be counteracted by sympathomimetic drugs having beta- adrenergic agonist activity with concomitant administration. The dose of either agent may need to be adjusted based on patient response, or use of alternate therapeutic agents considered.
In patients with renal insufficiency caution is needed when esmolol is administered by infusion, since the acid metabolite of esmolol is excreted through the kidneys. Excretion of the acid metabolite is significantly decreased in patients with renal disease, with the elimination half-life increased to about tenfold that of normals, and plasma levels considerably elevated.
Concomitant administration of tricyclic antidepressants (such as imipramine and amitriptyline), barbiturates and phenothiazines (such as chlorpromazine), as well as other antipsychotic agents (such as clozapine) may increase the blood pressure lowering effect. Dosing of esmolol should be adjusted downward to avoid unexpected hypotension.
Concomitant use of esmolol and insulin or oral antidiabetic drugs may intensify the blood sugar lowering effect (especially non-selective beta-blockers). Beta-adrenergic blockade may prevent the appearance of signs of hypoglycemia (tachycardia), but other manifestations such as dizziness and sweating may not be masked.
When digoxin and esmolol were concomitantly administered intravenously to normal volunteers, there was a 10-20% increase in digoxin blood levels at some time points. The combination of digitalis glycosides and esmolol may increase AV conduction time. Digoxin did not affect esmolol pharmacokinetics.
Concomitant use of esmolol and Class I anti-arrhythmic agents (e.g. disopyramide quinidine) and amiodarone may have potentiating effect on atrial-conduction time and induce negative inotropic effect.
Care should always be exercised whenever esmolol is used with other antihypertensive agents or other drugs that may cause hypotension or bradycardia: the effects of esmolol may be enhanced or the side-effects of hypotension or bradycardia may be exacerbated.
Calcium antagonists such as dihydropyridine derivatives (e.g., nifedipine) may increase the risk of hypotension. In patients with cardiac insufficiency and who are being treated with a calcium antagonist, treatment with beta-blocking agents may lead to cardiac failure. Careful titration of esmolol and appropriate haemodynamic monitoring is recommended.
The use of beta-blockers with ergot derivatives may result in severe peripheral vasoconstriction and hypertension.
In situations where the patient’s volume status is uncertain or concomitant antihypertensive drugs are utilized, there may be attenuation of the reflex tachycardia and an increase of the risk of hypotension.
Continuation of beta-blockade reduces the risk of arrhythmia during induction and intubation. The anaesthesist should be informed when the patient is receiving a beta-blocking agent in addition to esmolol. The hypotensive effects of inhalation anaesthetic agents may be increased in the presence of esmolol. The dosage of either agent may be modified as needed to maintain the desired haemodynamics.
When using beta-blockers, patients at risk of anaphylactic reactions may be more reactive to allergen exposure (accidental, diagnostic, or therapeutic). Patients using beta-blockers may be unresponsive to the usual doses of epinephrine used to treat anaphylactic reactions.
Special caution must be taken when using floctafenine or amisulpride concomitantly with beta- blockers.
When intravenous morphine and esmolol interaction was studied in normal subjects, no effect on morphine blood levels was seen. The esmolol steady-state blood levels were increased by 46% in the presence of morphine, but no other pharmacokinetic parameters were changed.
Use of beta-blockers with moxonidine or alpha2-agonists (such as clonidine), increases the risk of withdrawal rebound hypertension. If clonidine or moxonidine are used in combination with a beta-blocker and both treatments have to be discontinued, the beta blocker should be discontinued first and then the clonidine or moxonidine after a few days.
Catecholamine-depleting agents, e.g., reserpine, may have an additive effect when given with beta-blocking agents. Patients treated concurrently with esmolol and a catecholamine depletor should therefore be closely observed for evidence of hypotension or marked bradycardia, which may result in vertigo, syncope or postural hypotension.
The effect of esmolol on the duration of suxamethonium chloride-induced or mivacurium-induced neuromuscular blockade has been studied in patients undergoing surgery. Esmolol did not affect the onset of neuromuscular blockade by suxamethonium chloride, but the duration of neuromuscular blockade was prolonged from 5 minutes to 8 minutes. Esmolol moderately prolonged the clinical duration (18.6%) and recovery index (6.7%) of mivacurium.
Calcium antagonists such as verapamil and to a lesser extent diltiazem have a negative influence on contractility and AV-conduction. The combination should not be given to patients with conduction abnormalities and esmolol should not be administered within 48 hours of discontinuing verapamil.
Data from an interaction study between esmolol and warfarin showed that concomitant administration of esmolol and warfarin does not alter warfarin plasma levels. Esmolol concentrations, however, were equivocally higher when given with warfarin.
Although the interactions observed in studies of warfarin, digoxin, morphine suxamethonium chloride or mivacurium are not of major clinical importance, esmolol should be titrated with caution in patients being treated concurrently with warfarin, digoxin, morphine or suxamethonium chloride or mivacurium.
In patients with peripheral circulatory disorders (Raynaud’s disease or syndrome, intermittent claudication), beta-blockers should be used with great caution as aggravation of these disorders may occur.
Beta-blockers may increase both the sensitivity toward allergens and the seriousness of anaphylactic reactions. Patients using beta-blockers may be unresponsive to the usual doses of epinephrine used to treat anaphylactic or anaphylactoid reactions.
Patients with bronchospastic disease should, in general, not receive beta blockers. Because of its relative beta1 selectivity and titratability, esmolol should be used with caution in patients with bronchospastic diseases. However, since beta1 selectivity is not absolute, esmolol should be carefully titrated to obtain the lowest possible effective dose. In the event of bronchospasm, the infusion should be terminated immediately and a beta2-agonist should be administered if necessary.
Esmolol should be used with caution in diabetics or in case of suspected of actual hypoglycaemia. The severity of hypoglycaemia is less than the one observed with less cardio-selective beta-blockers. Beta-blockers may mask the prodromal symptoms of hypoglycaemia such as tachycardia.
However, dizziness and sweating, however, may not be affected. Concomitant use of beta-blockers and antidiabetic agents can increase the effect of the antidiabetic agents (blood glucose–lowering).
In hypovolemic patients, esmolol can attenuate reflex tachycardia and increase the risk of circulatory collapse. Therefore, esmolol should be used with caution in such patients.
Beta-blockers may increase the number and the duration of anginal attacks in patients with Prinzmetal’s angina due to unopposed alpha-receptor mediated coronary artery vasoconstriction. Non-selective beta-blockers should not be used for these patients and beta1 selective blockers should only be used with the utmost care.
Beta-blockers have been associated with the development of psoriasis or psoriasiform eruptions and with aggravation of psoriasis. Patients with a personal or family history of psoriasis should be administered beta- blockers only after careful consideration of expected benefits and risks.
There are limited amount of data from the use of esmolol in pregnant women. Studies in animals have shown reproductive toxicity.
Esmolol is not recommended in pregnancy.
There are insufficient data to determine the possible harmful effects of esmolol during pregnancy. To date, there are no indications for an increased risk on birth defects in humans. The potential risk for humans is unknown. Based on the pharmacological action, in the later period of pregnancy, side effects on the foetus and neonate (especially hypoglycemia, hypotension and bradycardia) should be taken into account.
If treatment with esmolol is considered necessary, the uteroplacental blood flow and foetal growth should be monitored. The newborn infant must be closely monitored.
Esmolol should not be used during breast-feeding.
It is not known whether esmolol/metabolites are excreted in human milk. A risk to the newborns/infants cannot be excluded.
There are no human data on the effects of esmolol on fertility.
Not relevant.
In case of undesirable effects, the dose of esmolol hydrochloride 2500 mg powder can be reduced or discontinued.
Most of the undersirable effects observed have been mild and transient. The most important one has been hypotension.
The following undesirable effects are ranked according to MedDRA System Organ Class (SOC) and to their frequency.
Note: The frequency of occurrence of adverse events is classified as follows: Very common (≥1/10), Common (≥1/100 to <1/10), Uncommon (≥1/1,000 to <1/100), Rare (≥1/10,000 to <1/1,000), Very rare (<1/10,000), Not known (cannot be estimated from the available data).
Common: Anorexia
Not known: Hyperkalemia, Metabolic acidosis
Common: Depression, Anxiety
Uncommon: Thinking abnormal
Common: Dizziness1, Somnolence, Headache, Paraesthesiae, Disturbance in attention, Confusional state, Agitation
Uncommon: Syncope, Convulsion, Speech disorder
Uncommon: Visual impairment
Uncommon: Bradycardia, Atrioventricular block, Pulmonary arterial pressure increased, Cardiac Failure, Ventricular extrasystoles, Nodal rhythm, Angina pectoris
Very rare: Sinus arrest, Asystole
Not known: Accelerated idioventricular rhythm, Coronary arteriospasm, Cardiac arrest.
Very common: Hypotension
Uncommon: Peripheral ischaemia, Pallor, Flushing
Very rare: Thrombophlebitis2
Uncommon: Dyspnoea, Pulmonary oedema, Bronchospasm, Wheezing, Nasal congestion, Rhonchi, Rales
Common: Nausea, Vomiting
Uncommon: Dysgeusia, Dyspepsia, Constipation, Dry mouth, Abdominal pain
Very common: Diaphoresis1
Uncommon: Skin discolouration2, Erythema2
Very rare: Skin necrosis2 (due to extravasation)
Not known: Psoriasis3, Angioedema, Urticaria
Uncommon: Musculoskeletal pain4
Uncommon: Urinary retention
Common: Asthenia, Fatigue, Injection site reaction, Infusion site reaction, Infusion site inflammation, Infusion site induration
Uncommon: Chills, Pyrexia, Oedema2, Pain2, Infusion site burning, Infusion site ecchymosis, Chest Pain
Not known: Infusion site phlebitis, Infusion site vesicles, Blistering2
1 Dizziness and diaphoresis are in association with symptomatic hypotension.
2 In association with Injection and Infusion site reactions.
3 Beta-blockers as a drug class can cause psoriasis in some situations, or worsen it.
4 Including midscapular pain and costochondritis.
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