Source:http://www4.wiwiss.fu-berlin.de/dailymed/resource/drugs/2699
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Esmolol Hydrochloride (Injection)
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Dosing Information::<br/>SUPRAVENTRICULAR TACHYCARDIA: Dosage needs to be titrated, using ventricular rate as
the guide. An
initial loading dose of 0.5 milligrams/kg (500
micrograms/kg) infused over a minute duration followed
by a maintenance infusion of 0.05 milligrams/kg/min (50
micrograms/kg/min) for the next 4 minutes is
recommended. This should give a rough guide with respect
to the responsiveness of ventricular rate. After the 4 minutes of initial maintenance infusion
(total treatment duration being 5 minutes), depending
upon the desired ventricular response, the maintenance
infusion may be continued at 0.05 mg/kg/min or increased
step-wise (e.g. 0.1 mg/kg/min, 0.15 mg/kg/min to a
maximum of 0.2 mg/kg/min) with each step being
maintained for 4 or more minutes. If
more rapid slowing of ventricular response is
imperative, the 0.5 mg/kg loading dose infused over a 1
minute period may be repeated, followed by a maintenance
infusion of 0.1 mg/kg/min for 4 minutes. Then, depending
upon ventricular rate, another (and final) loading dose
of 0.5 mg/kg/min infused over a 1 minute period may be
administered followed by a maintenance infusion of 0.15
mg/kg/min. If needed, after 4 minutes of the 0.15
mg/kg/min maintenance infusion, themaintenance infusion
may be increased to a maximum of 0.2 mg/kg/min. In
the absence of loading doses, constant infusion of a
single concentration of esmolol reaches pharmacokinetic
and pharmacodynamic steady-state in about 30 minutes.
Maintenance infusions (with or without loading doses)
may be continued for as long as 24 hours. The
following table summarizes the above and assumes that 3 loading doses (the maximum recommended) are infused over 1 minute and incremental maintenance doses are required
after each loading dose. There should be no 4th loading
dose, but the maintenance dose may be incremented one
more time. In
the treatment of supraventricular tachycardia, responses to esmolol hydrochloride usually (over 95%) occur within
the range of 50 to 200 micrograms/kg/min (0.05 to 0.2
milligrams/kg/min). The average effective dosage is
approximately 100 micrograms/kg/min (0.1
milligrams/kg/min) although dosages as low as 25
micrograms/kg/min (0.025 milligrams/kg/min) have been
adequate in some patients. Dosages as high as 300
micrograms/kg/min (0.3 milligrams/kg/min) have been
used, but these provide little added effect and increase
the rate of adverse effects, so doses greater than 200
micrograms/kg/min are not recommended. Dosage of esmolol
hydrochloride in supraventricular tachycardia must be
individualized by titration in which each step consists
of a loading dosage followed by a maintenance dosage. This specific dosage regimen has not been studied
intraoperatively and, because of the time required for
titration, may not be optimal for intraoperative use. The
safety of dosages above 300 mcg/kg/min (0.3 mg/kg/min)
has not been studied. In
the event of an adverse reaction, the dosage of esmolol
hydrochloride may be reduced or discontinued. If a local
infusion site reaction develops, an alternate infusion
site should be used and caution should be taken to
prevent extravasation. The use of butterfly needles
should be avoided. Abrupt cessation of esmolol hydrochloride in patients
has not been reported to produce the withdrawal effects
which may occur with abrupt withdrawal of beta blockers
following chronic use in coronary artery disease (CAD)
patients. However, caution should still be used in
abruptly discontinuing infusions of esmolol
hydrochloride in CAD patients. After achieving an adequate control of the heart rate
and a stable clinical status in patients with
supraventricular tachycardia, transition to alternative
antiarrhythmic agents such as propranolol, digoxin, or
verapamil, may be accomplished. A
recommended guideline for such a transition is given
below but the physician should carefully consider the
labeling instructions for the alternative agent
selected. The
dosage of esmolol hydrochloride should be reduced as
follows: The
use of infusions of esmolol hydrochloride up to 24 hours
has been well documented; in addition, limited data from
24-48 hrs (N=48) indicate that esmolol hydrochloride is
well tolerated up to 48 hours.<br/>INTRAOPERATIVE AND
POSTOPERATIVE TACHYCARDIA AND/OR HYPERTENSION: In the
intraoperative and postoperative settings it is not always
advisable to slowly titrate the dose of esmolol hydrochloride to a therapeutic effect. Therefore, two dosing options are
presented: immediate control dosing and a gradual control when
the physician has time to titrate. 1. Immediate Control For
intraoperative treatment of tachycardia and/or hypertension give
an 80 mg (approximately 1 mg/kg) bolus dose over 30 seconds
followed by a 150 mcg/kg/min infusion, if necessary. Adjust the
infusion rate as required up to 300 mcg/kg/min to maintain
desired heart rate and/or blood pressure. 2. Gradual Control For
postoperative tachycardia and hypertension, the dosing schedule
is the same as that used in supraventricular tachycardia. To
initiate treatment, administer a loading dosage infusion of 500
mcg/kg/min of esmolol hydrochloride for one minute followed by a
four-minute maintenance infusion of 50 mcg/kg/min. If an
adequate therapeutic effect is not observed within five minutes,
repeat the same loading dosage and follow with a maintenance infusion increased to 100 mcg/kg/min . Notes: 1. Higher
dosages (250-300 mcg/kg/min) may be required for adequate
control of blood pressure than those required for the treatment of atrial fibrillation, flutter and sinus tachycardia. One third
of the postoperative hypertensive patients required these higher
doses. 2.
Parenteral drug products should be inspected visually for
particulate matter and discoloration prior to administration,
whenever solution and container permit.<br/>Directions for Use
of the 10 mL Ready-to-use Vial (10 milligrams/mL): This dosage
form is prediluted to provide a ready-to-use, iso-osmotic
solution of 10 mg/mL esmolol hydrochloride in sodium chloride
recommended for esmolol hydrochloride intravenous
administration. It may be used to administer the appropriate
esmolol hydrochloride loading dosage infusions by hand-held
syringe while the maintenance infusion is being prepared. The 10 mL
Ready-to-use Vial esmolol hydrochloride at a concentration of 10
milligrams/mL. When using a 10 milligrams/mL concentration, a
loading dose of 0.5 mg/kg infused over 1 minute period of time,
for a 70 kg patient is 3.5 mL.<br/>Compatibility with
Commonly Used Intravenous Fluids: Esmolol hydrochloride was tested for compatibility with ten commonly
used intravenous fluids at a final concentration of 10 mg
Esmolol Hydrochloride per mL. Esmolol hydrochloride was found to
be compatible with the following solutions and was stable for at
least 24 hours at controlled room temperature or under
refrigeration: Esmolol
hydrochloride is NOT compatible with Sodium Bicarbonate (5%)
Injection, USP.
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Esmolol
hydrochloride is a beta-selective (cardioselective)
adrenergic receptor blocking agent with a very short duration of action
(elimination half-life is approximately 9 minutes). Esmolol
Hydrochloride is: (��)-Methyl p-
[2-hydroxy-3- (isopropylamino) propoxy] hydrocinnamate hydrochloride and
has the following structure: Esmolol
hydrochloride has the empirical formula
CHNOCl and a molecular weight
of 331.8. It has one asymmetric center and exists as an enantiomeric
pair. Esmolol
hydrochloride is a white to off-white crystalline powder. It is a
relatively hydrophilic compound which is very soluble in water and
freely soluble in alcohol. Its partition coefficient (octanol/water) at
pH 7.0 is 0.42 compared to 17.0 for propranolol.<br/>Esmolol
Hydrochloride Injection: Esmolol
Hydrochloride Injection is a clear, colorless to light yellow,
sterile, nonpyrogenic, iso-osmotic solution of esmolol
hydrochloride in sodium chloride. 100 mg, 10 mL Single Dose Vial���Each mL contains 10 mg Esmolol Hydrochloride, 5.9 mg Sodium
Chloride, USP and Water for Injection, USP; buffered with 2.8 mg
Sodium Acetate Trihydrate, USP and 0.546 mg Glacial Acetic Acid,
USP. Sodium Hydroxide and/or Hydrochloric Acid added, as
necessary to adjust pH to 5.0 (4.5-5.5).
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Esmolol
hydrochloride is a beta-selective (cardioselective)
adrenergic receptor blocking agent with rapid onset, a very short
duration of action, and no significant intrinsic sympathomimetic or
membrane stabilizing activity at therapeutic dosages. Its elimination
half-life after intravenous infusion is approximately 9 minutes. Esmolol
hydrochloride inhibits the betareceptors located chiefly in
cardiac muscle, but this preferential effect is not absolute and at
higher doses it begins to inhibit betareceptors located
chiefly in the bronchial and vascular musculature.<br/>Pharmacokinetics
and Metabolism: Esmolol hydrochloride is rapidly metabolized by hydrolysis of the ester
linkage, chiefly by the esterases in the cytosol of red blood
cells and not by plasma cholinesterases or red cell membrane
acetylcholinesterase. Total body clearance in man was found to
be about 20 L/kg/hr, which is greater than cardiac output; thus
the metabolism of esmolol hydrochloride is not limited by the
rate of blood flow to metabolizing tissues such as the liver or
affected by hepatic or renal blood flow. Esmolol hydrochloride
has a rapid distribution half-life of about 2 minutes and an
elimination half-life of about 9 minutes. Using an
appropriate loading dose, steady-state blood levels of esmolol
hydrochloride for dosages from 50-300 mcg/kg/min (0.05-0.3
mg/kg/min) are obtained within five minutes. (Steady-state is
reached in about 30 minutes without the loading dose.)
Steady-state blood levels of esmolol hydrochloride increase
linearly over this dosage range and elimination kinetics are
dose-independent over this range. Steady-state blood levels are
maintained during infusion but decrease rapidly after
termination ofthe infusion. Because of its short half-life,
blood levels of esmolol hydrochloride can be rapidly altered by increasing or decreasing the infusion rate and rapidly
eliminated by discontinuing the infusion. Consistent
with the high rate of blood-based metabolism of esmolol
hydrochloride, less than 2% of the drug is excreted unchanged in
the urine. Within 24 hours of the end of infusion, approximately
73-88% of the dosage has been accounted for in the urine as the
acid metabolite of esmolol hydrochloride. Metabolism
of esmolol hydrochloride results in the formation of the
corresponding free acid and methanol. The acid metabolite has
been shown in animals to have about 1/1500th the activity of
esmolol and in normal volunteers its blood levels do not
correspond to the level of beta blockade. The acid metabolite
has an elimination half-life of about 3.7 hours and isexcreted
in the urine with a clearance approximately equivalent to the
glomerular filtration rate. Excretion of the acid metabolite is
significantly decreased in patients with renal disease, with the
elimination half-life increased to about ten-fold that of
normals, and plasma levels considerably elevated. Methanol blood levels, monitored in subjects receiving esmolol
hydrochloride for up to 6 hours at 300 mcg/kg/min (0.3
mg/kg/min) and 24 hours at 150 mcg/kg/min (0.15 mg/kg/min),
approximated endogenous levels and were less than 2% of levels
usually associated with methanol toxicity. Esmolol
hydrochloride has been shown to be 55% bound to human plasma
protein, while the acid metabolite is only 10%
bound.<br/>Pharmacodynamics: Clinical
pharmacology studies in normal volunteers have confirmed the
beta blocking activity of esmolol hydrochloride, showing
reduction in heart rate at rest and during exercise, and
attenuation of isoproterenol-induced increases in heart rate.
Blood levels of esmolol hydrochloride have been shown to
correlate with extent of beta blockade. After termination of infusion, substantial recovery from beta blockade is observed in
10-20 minutes. In human
electrophysiology studies, esmolol hydrochloride produced
effects typical of a beta blocker; a decrease in the heart rate,
increase in sinus cycle length, prolongation of the sinus node
recovery time, prolongation of the AH interval during normal
sinus rhythm and during atrial pacing, and an increase in
antegrade Wenckebach cycle length. In patients
undergoing radionuclide angiography, esmolol hydrochloride, at
dosages of 200 mcg/kg/min (0.2 mg/kg/min), produced reductions
in heart rate, systolic blood pressure, rate pressure product,
left and right ventricular ejection fraction and cardiac index
at rest, which were similar in magnitude to those produced by
intravenous propranolol (4 mg). During exercise, esmolol
hydrochloride produced reductions in heart rate, rate pressure
product and cardiac index which were also similar to those
produced by propranolol, but produced a significantly larger
fall in systolic blood pressure. In patients undergoing cardiac
catheterization, the maximum therapeutic dose of 300 mcg/kg/min (0.3 mg/kg/min) of esmolol hydrochloride produced similar
effects and, in addition, there were small, clinically
insignificant increases in the left ventricular end diastolic
pressure and pulmonary capillary wedge pressure. At thirty
minutes after the discontinuation of esmolol hydrochloride
infusion, all of the hemodynamic parameters had returned to
pretreatment levels. The
relative cardioselectivity of esmolol hydrochloride was
demonstrated in 10 mildly asthmatic patients. Infusions of
esmolol hydrochloride [100, 200 and 300 mcg/kg/min (0.1, 0.2 and
0.3 mg/kg/min)] produced no significant increases in specific
airway resistance compared to placebo. At 300 mcg/kg/min (0.3
mg/kg/min), esmolol hydrochloride produced slightly enhanced
bronchomotor sensitivity to dry air stimulus. These effects were
not clinically significant, and esmolol hydrochloride was well
tolerated by all patients. Six of the patients also received
intravenous propranolol, and at a dosage of 1 mg, two
experienced significant, symptomatic bronchospasmrequiring
bronchodilator treatment. One other propranolol-treated patient
also experienced dry air-induced bronchospasm. No adverse
pulmonary effects were observed in patients with COPD who
received therapeutic dosages of esmolol hydrochloride for
treatment of supraventricular tachycardia (51 patients) or in
perioperative settings (32 patients).<br/>Supraventricular
Tachycardia: In two
multicenter, randomized, double-blind, controlled comparisons of
esmolol hydrochloride with placebo and propranolol, maintenance
doses of 50 to 300 mcg/kg/min (0.05 to 0.3 mg/kg/min) of esmolol
hydrochloride were found to be more effective than placebo and
about as effective as propranolol, 3-6 mg given by bolus
injections, in the treatment of supraventricular tachycardia,
principally atrial fibrillation and atrial flutter. The majority
of these patients developed their arrhythmias postoperatively.
About 60-70% of the patients treated with esmolol hydrochloride
had a desired therapeutic effect (either a 20% reduction in heart rate, a decrease in heart rate to less than 100 bpm, or,
rarely, conversion to NSR) and about 95% of those who responded
did so at a dosage of 200 mcg/kg/min (0.2 mg/kg/min) or less.
The average effective dosage of esmolol hydrochloride was
approximately 100-115 mcg/kg/min (0.1-0.115 mg/kg/min) in the
two studies. Other multicenter baseline-controlled studies gave
essentially similar results. In the comparison with propranolol,
about 50% of patients in both the esmolol hydrochloride and
propranolol groups were on concomitant digoxin. Response rates
were slightly higher with both beta blockers in the
digoxin-treated patients. In all
studies significant decreases of blood pressure occurred in
20-50% of patients, identified either as adverse reaction
reports by investigators, or by observation of systolic pressure
less than 90 mmHg or diastolic pressure less than 50 mmHg. The
hypotension was symptomatic (mainly diaphoresis or dizziness) in
about 12% of patients, and therapy was discontinued in about 11%
of patients, about half of whom were symptomatic. In comparison
to propranolol, hypotension was about three times as frequent
with esmolol hydrochloride, 53% vs. 17%. The hypotension was rapidly reversible with decreased infusion rate or after
discontinuation of therapy with esmolol hydrochloride. For both
esmolol hydrochloride and propranolol, hypotension was reported
less frequently in patients receiving concomitant
digoxin.
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Esmolol
hydrochloride is contraindicated in patients with sinus bradycardia,
heart block greater than first degree, cardiogenic shock or overt heart
failure .
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Esmolol
Hydrochloride Injection NDC 0641-2965-45,
100 mg - 10 mL Ready-to-use Vials, Package of 25 Store at 20��-25��C (68��-77��F). Excursions permitted
to 15��-30��C (59��-86��F). [See USP Controlled Room Temperature.]
PROTECT FROM FREEZING. Avoid excessive heat. Baxter is a
registered trademark of Baxter International Inc. Manufactured by Baxter Healthcare Corporation Deerfield, IL 60015
USA For Product Inquiry
1 800 ANA DRUG (1-800-262-3784) Rev: April
2005
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General: Infusion
concentrations of 20 mg/mL were associated with more serious
venous irritation, including thrombophlebitis, than
concentrations of 10 mg/mL. Extravasation of 20 mg/mL may lead
to a serious local reaction and possible skin necrosis.
Concentrations greater than 10 mg/mL or infusion into small
veins or through a butterfly catheter should be avoided. Because the acid metabolite of esmolol hydrochloride is primarily excreted
unchanged by the kidney, esmolol hydrochloride should be
administered with caution to patients with impaired renal
function. The elimination half-life of the acid metabolite was
prolonged ten-fold and the plasma level was considerably
elevated in patients with end-stage renal disease. Care should
be taken in the intravenous administration of esmolol
hydrochloride as sloughing of the skin and necrosis have been
reported in association with infiltration and extravasation of
intravenous infusions.<br/>Drug Interactions: Catecholamine-depleting drugs, e.g., reserpine, may have an
additive effect when given with beta blocking agents. Patients
treated concurrently with esmolol hydrochloride 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. A study of
interaction between esmolol hydrochloride and warfarin showed that concomitant administration of esmolol hydrochloride and
warfarin does not alter warfarin plasma levels. Esmolol
hydrochloride concentrations were equivocally higher when given
with warfarin, but this is not likely to be clinically
important. When
digoxin and esmolol hydrochloride were concomitantly
administered intravenously to normal volunteers, there was a
10-20% increase in digoxin blood levels at some time points.
Digoxin did not affect esmolol hydrochloride pharmacokinetics.
When intravenous morphine and esmolol hydrochloride were
concomitantly administered in normal subjects, no effect on
morphine blood levels was seen, but esmolol hydrochloride
steady-state blood levels were increased by 46% in the presence
of morphine. No other pharmacokinetic parameters were changed. The effect
of esmolol hydrochloride on the duration of
succinylcholine-induced neuromuscular blockade was studied in
patients undergoing surgery. The onset of neuromuscular blockade
by succinylcholine was unaffected by esmolol hydrochloride, but
the duration of neuromuscular blockade was prolonged from 5
minutes to 8 minutes. Although
the interactions observed in these studies do not appear to be
of major clinical importance, esmolol hydrochloride should be
titrated with caution in patients being treated concurrently
with digoxin, morphine, succinylcholine or warfarin. While
taking beta blockers, patients with a history of severe
anaphylactic reaction to a variety of allergens may be more
reactive to repeated challenge, either accidental, diagnostic,
or therapeutic. Such patients may be unresponsive to the usual
doses of epinephrine used to treat allergic reaction. Caution
should be exercised when considering the use of esmolol
hydrochloride and verapamil in patients with depressed
myocardial function. Fatal cardiac arrests have occurred in
patients receiving both drugs. Additionally, esmolol
hydrochloride should not be used to control supraventricular
tachycardia in the presence of agents which are vasoconstrictive
and inotropic such as dopamine, epinephrine, and norepinephrine
because of the danger of blocking cardiac contractility when
systemic vascular resistance is high.<br/>Carcinogenesis,
Mutagenesis, Impairment of Fertility: Because of
its short term usage no carcinogenicity, mutagenicity or
reproductive performance studies have been conducted with
esmolol hydrochloride.<br/>Pregnancy Category
C: Teratogenicity studies in rats at intravenous dosages of
esmolol hydrochloride up to 3000 mcg/kg/min (3 mg/kg/min) (ten
times the maximum human maintenance dosage) for 30 minutes daily
produced no evidence of maternal toxicity, embryotoxicity or
teratogenicity, while a dosage of 10,000 mcg/kg/min (10
mg/kg/min) produced maternal toxicity and lethality. In rabbits, intravenous dosages up to 1000 mcg/kg/min (1 mg/kg/min) for 30
minutes daily produced no evidence of maternal toxicity,
embryotoxicity or teratogenicity, while 2500 mcg/kg/min (2.5
mg/kg/min) produced minimal maternal toxicity and increased
fetal resorptions. Although
there are no adequate and well-controlled studies in pregnant
women, use of esmolol in the last trimester of pregnancy or
during labor or delivery has been reported to cause fetal
bradycardia, which continued after termination of drug infusion.
Esmolol hydrochloride should be used during pregnancy only if
the potential benefit justifies the potential risk to the
fetus.<br/>Nursing Mothers: It is not
known whether esmolol hydrochloride is excreted in human milk;
however, caution should be exercised when esmolol hydrochloride
is administered to a nursing woman.<br/>Pediatric Use: The safety
and effectiveness of esmolol hydrochloride in pediatric patients
have not been established.
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Acute Toxicity: Overdoses
of esmolol hydrochloride can cause cardiac arrest. In addition,
overdoses can produce bradycardia, hypotension,
electromechanical dissociation and loss of consciousness. Cases
of massive accidental overdoses of esmolol hydrochloride have
occurred due to dilution errors. Some of these overdoses have
been fatal while others resulted in permanent disability. Bolus
doses in the range of 625 mg to 2.5 g (12.5-50 mg/kg) have been
fatal. Patients have recovered completely from overdoses as high
as 1.75 g given over one minute or doses of 7.5 g given over one
hour for cardiovascular surgery. The patients who survived
appear to be those whose circulation could be supported until
the effects of esmolol hydrochloride resolved. Because of
its approximately 9-minute elimination half-life, the first step
in the management of toxicity should be to discontinue the
esmolol hydrochloride infusion. Then, based on the observed
clinical effects, the following general measures should also be
considered. Bradycardia: Intravenous
administration of atropine or another anticholinergic drug. Bronchospasm: Intravenous
administration of a betastimulating agent and/or a
theophylline derivative. Cardiac Failure: Intravenous
administration of a diuretic and/or digitalis glycoside. In
shock resulting from inadequate cardiac contractility,
intravenous administration of dopamine, dobutamine,
isoproterenol, or amrinone may be considered. Symptomatic Hypotension:
Intravenous administration of fluids and/or pressor
agents.
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Esmolol Hydrochloride
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Esmolol Hydrochloride (Injection)
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The following
adverse reaction rates are based on use of esmolol hydrochloride in
clinical trials involving 369 patients with supraventricular tachycardia
and over 600 intraoperative and postoperative patients enrolled in
clinical trials. Most adverse effects observed in controlled clinical
trial settings have been mild and transient. The most important
adverse effect has been hypotension . Deaths have been reported in post-marketing
experience occurring during complex clinical states where esmolol hydrochloride was presumably being used simply to control ventricular
rate (see WARNINGS, Cardiac
Failure).<br/>Cardiovascular: Symptomatic
hypotension (diaphoresis, dizziness) occurred in 12% of
patients, and therapy was discontinued in about 11%, about half
of whom were symptomatic. Asymptomatic hypotension occurred in
about 25% of patients. Hypotension resolved during esmolol
hydrochloride infusion in 63% of these patients and within 30
minutes after discontinuation of infusion in 80% of the
remaining patients. Diaphoresis accompanied hypotension in 10%
of patients. Peripheral ischemia occurred in approximately 1% of
patients. Pallor, flushing, bradycardia (heart rate less than 50
beats per minute), chest pain, syncope, pulmonary edema and
heart block have each been reported in less than 1% of patients.
In two patients without supraventricular tachycardia but with
serious coronary artery disease (post inferior myocardial
infarction or unstable angina), severe bradycardia/sinus pause/asystole has developed, reversible in both cases with
discontinuation of treatment.<br/>Central Nervous
System: Dizziness
has occurred in 3% of patients; somnolence in 3%; confusion,
headache, and agitation in about 2%; and fatigue in about 1% of
patients. Paresthesia, asthenia, depression, abnormal thinking,
anxiety, anorexia, and lightheadedness were reported in less
than 1% of patients. Seizures were also reported in less than 1%
of patients, with one death.<br/>Respiratory: Bronchospasm, wheezing, dyspnea, nasal congestion, rhonchi, and
rales have each been reported in less than 1% of
patients.<br/>Gastrointestinal: Nausea was
reported in 7% of patients. Vomiting has occurred in about 1% of
patients. Dyspepsia, constipation, dry mouth, and abdominal
discomfort have each occurred in less than 1% of patients. Taste
perversion has also been reported.<br/>Skin (Infusion
Site): Infusion
site reactions including inflammation and induration were
reported in about 8% of patients. Edema, erythema, skin
discoloration, burning at the infusion site, thrombophlebitis,
and local skin necrosis from extravasation have each occurred in
less than 1% of patients.<br/>Miscellaneous: Each of the
following has been reported in less than 1% of patients: Urinary
retention, speech disorder, abnormal vision, midscapular pain,
rigors, and fever.
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Hypotension: In clinical
trials 20-50% of patients treated with esmolol hydrochloride
have experienced hypotension, generally defined as systolic
pressure less than 90 mmHg and/or diastolic pressure less than
50 mmHg. About 12% of the patients have been symptomatic (mainly
diaphoresis or dizziness). Hypotension can occur at any dose but
is dose-related so that doses beyond 200 mcg/kg/min (0.2
mg/kg/min) are not recommended. Patients should be closely
monitored, especially if pretreatment blood pressure is low.
Decrease of dose or termination of infusion reverses
hypotension, usually within 30 minutes.<br/>Cardiac Failure: Sympathetic
stimulation is necessary in supporting circulatory function in
congestive heart failure, and beta blockade carries the
potential hazard of further depressing myocardial contractility
and precipitating more severe failure. Continued depression of the myocardium with beta blocking agents over a period of time
can, in some cases, lead to cardiac failure. At the first sign
or symptom of impending cardiac failure, esmolol hydrochloride
should be withdrawn. Although withdrawal may be sufficient
because of the short elimination half-life of esmolol
hydrochloride, specific treatment may also be considered . The use of esmolol hydrochloride for
control of ventricular response in patients with
supraventricular arrhythmias should be undertaken with caution
when the patient is compromised hemodynamically or is taking
other drugs that decrease any or all of the following:
peripheral resistance, myocardial filling, myocardial
contractility, or electrical impulse propagation in the
myocardium. Despite the rapid onset and offset of the effects of
esmolol hydrochloride, several cases of death have been reported
in complex clinical states where esmolol hydrochloride was
presumably being used to control ventricular rate.<br/>Intraoperative and
Postoperative Tachycardia and/or Hypertension: Esmolol
hydrochloride should not be used as the treatment for
hypertension in patients in whom the increased blood pressure is
primarily due to the vasoconstriction associated with
hypothermia.<br/>Bronchospastic
Diseases: PATIENTS
WITH BRONCHOSPASTIC DISEASES SHOULD, IN GENERAL, NOT RECEIVE
BETA BLOCKERS. Because of its relative betaselectivity and titratability, esmolol hydrochloride may be used
with caution in patients with bronchospastic diseases. However,
since betaselectivity is not absolute, esmolol
hydrochloride should be carefully titrated to obtain the lowest
possible effective dose. In the event of bronchospasm, the
infusion should be terminated immediately; a betastimulating agent may be administered if conditions warrant but
should be used with particular caution as patients already have
rapid ventricular rates.<br/>Diabetes Mellitus
and Hypoglycemia: Esmolol hydrochloride should be used with caution in diabetic patients
requiring a beta blocking agent. Beta blockers may mask
tachycardia occurring with hypoglycemia, but other
manifestations such as dizziness and sweating may not be
significantly affected.
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Supraventricular
Tachycardia: Esmolol
hydrochloride is indicated for the rapid control of ventricular
rate in patients with atrial fibrillation or atrial flutter in
perioperative, postoperative, or other emergent circumstances
where short term control of ventricular rate with a short-acting agent is desirable. Esmolol hydrochloride is also indicated in
noncompensatory sinus tachycardia where, in the physician's
judgment, the rapid heart rate requires specific intervention.
Esmolol hydrochloride is not intended for use in chronic
settings where transfer to another agent is
anticipated.<br/>Intraoperative and
Postoperative Tachycardia and/or Hypertension: Esmolol
hydrochloride is indicated for the treatment of tachycardia and
hypertension that occur during induction and tracheal
intubation, during surgery, on emergence from anesthesia, and in
the postoperative period, when in the physician's judgment such
specific intervention is considered indicated. Use of
esmolol hydrochloride to prevent such events is not
recommended.
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Esmolol Hydrochloride
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