Source:http://www4.wiwiss.fu-berlin.de/dailymed/resource/drugs/1375
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Brevibloc (Injection, Solution, Concentrate)
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| dailymed-instance:dosage |
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, the maintenance
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 BREVIBLOC (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
BREVIBLOC 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
BREVIBLOC 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 BREVIBLOC 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 BREVIBLOC 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 BREVIBLOC (Esmolol Hydrochloride) should be
reduced as follows: The
use of infusions of BREVIBLOC up to 24 hours has been
well documented; in addition, limited data from 24-48
hrs (N=48) indicate that BREVIBLOC 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 BREVIBLOC
(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 BREVIBLOC 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 (see above Supraventricular Tachycardia). Notes:<br/>Directions for Use
of Brevibloc Premixed Injection (10 mg/mL) and Brevibloc DOUBLE
STRENGTH Premixed Injection (20 mg/mL): This dosage
form is prediluted to 100 or 250 mL to provide a ready-to-use,
iso-osmotic solution of either 20 or 10 mg/mL esmolol
hydrochloride in sodium chloride. It is important not to
introduce additives to BREVIBLOC PREMIXED INJECTION or BREVIBLOC
DOUBLE STRENGTH PREMIXED INJECTION. See Directions
for Use of the Premixed Bag for additional
information.<br/>Directions for Use
of the Premixed Bag: Brevibloc Premixed Injection
(10 mg/mL) 250 mL IntraVia Bag Brevibloc DOUBLE STRENGTH Premixed
Injection (20 mg/mL) 100 mL IntraVia Bag BREVIBLOC
PREMIXED INJECTION (10 mg/mL) and BREVIBLOC DOUBLE STRENGTH
PREMIXED INJECTION (20 mg/mL) are provided in ready-to-use,
non-latex, non-PVC bags with two PVC ports, a medication port
and a delivery port. The medication
port is to be used solely for withdrawing an initial bolus
from the bag; the medication withdrawal port is not intended
for repeat bolus administration. The sterility of the
premixed bag cannot be assured after repeat withdrawals from
the bag. The use of aseptic technique is required when
withdrawing the bolus dose. Do not add any additional
medications to BREVIBLOC PREMIXED INJECTION. Each
bag is for single-patient use only and contains no preservative.
It is advised that once drug has been withdrawn from BREVIBLOC
PREMIXED INJECTION, the bag should be used within 24 hours, with any unused portion discarded. The
Brevibloc Premixed Injection contains Esmolol Hydrochloride at a
concentration of 10 milligrams/mL. When using a 10 milligrams/mL
concentration, a loading dose of 0.5 milligrams/kg infused over
1 minute period of time, for a 70 kg patient, is 3.5 mL. The
loading dose can be removed from the medication port of the
premixed bag. The
Brevibloc DOUBLE STRENGTH Premixed Injection contains Esmolol
Hydrochloride at a concentration of 20 milligrams/mL. When using
a 20 milligrams/mL concentration, a loading dose of
0.5 milligrams/kg infused over 1 minute period of time, for a
70 kg patient, is 1.75 mL. The loading dose can be removed from
the medication port of the premixed bag. Figure 1. Two-Port IntraVia
Bag<br/>CAUTION: Do
not use plastic containers in series connections. Such
use could result in an embolism due to residual air
being drawn from the primary container before
administration of the fluid from the secondary container
is completed.<br/>TO OPEN: Do
not remove unit from overwrap until ready to use. Do not
use if overwrap has been previously opened or damaged.
The overwrap is a moisture barrier. The inner bag
maintains sterility of the solution. Tear overwrap at notch and remove premixed bag. Some
opacity of the plastic due to moisture absorption during
the sterilization process may be observed. This is
normal and does not affect the solution quality or
safety. The opacity will diminish gradually. Check for minute leaks by squeezing the inner bag
firmly. If leaks are found, discard solution as
sterility may be impaired. Do not use unless the
solution is clear, colorless to light yellow, and the
seal is intact. Fill out the patient information label supplied and
apply to the inner bag. Do
not introduce additives to BREVIBLOC PREMIXED INJECTION
or BREVIBLOC DOUBLE STRENGTH PREMIXED
INJECTION.<br/>PREPARATION
FOR INTRAVENOUS ADMINISTRATION: (use aseptic technique)<br/>Directions for Use
of the Ready-to-use Vials: Brevibloc Injection (10 mg/mL) 10 mL
Ready-to-use Vial Brevibloc DOUBLE STRENGTH Injection
(20 mg/mL) 5 mL Ready-to-use Vial This dosage
form is prediluted to provide a ready-to-use, iso-osmotic
solution of either 10 or 20 mg/mL esmolol hydrochloride in
sodium chloride recommended for BREVIBLOC intravenous
administration. It may be used to administer the appropriate
BREVIBLOC (Esmolol Hydrochloride) loading dosage infusions by
hand-held syringe while the maintenance infusion is being
prepared. The 10 mL
Ready-to-use Vial contains 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. The 5 mL
DOUBLE STRENGTH Ready-to-use Vial contains Esmolol Hydrochloride
at a concentration of 20 milligrams/mL. When using a 20 milligrams/mL concentration, a loading dose of 0.5 mg/kg infused
over 1 minute period of time, for a 70 kg patient is
1.75 mL.<br/>Directions for Use
of the Brevibloc Concentrate 10 mL Ampul (250 milligrams/mL): THE 2500 mg AMPUL IS NOT FOR DIRECT
INTRAVENOUS INJECTION. THIS DOSAGE FORM IS A CONCENTRATED,
POTENT DRUG WHICH MUST BE DILUTED PRIOR TO ITS INFUSION.
BREVIBLOC SHOULD NOT BE ADMIXED WITH SODIUM BICARBONATE.
BREVIBLOC SHOULD NOT BE MIXED WITH OTHER DRUGS PRIOR TO
DILUTION IN A SUITABLE INTRAVENOUS FLUID.(SeeCompatibility Section below.) Dilution: Aseptically prepare a
10 mg/mL infusion by adding two 2500 mg ampuls to a 500 mL
container or one 2500 mg ampul to a 250 mL container of a
compatible intravenous solution listed below. (Remove overage
prior to dilution as appropriate.) This yields a final
concentration of 10 mg/mL. The diluted solution is stable for at
least 24 hours at room temperature. Note: The use of esmolol
with propylene glycol has been associated with a higher
incidence of venous irritation at concentrations greater than
10 mg/mL on continued infusion. Mixed from the ampul at
concentrations of greater than 10 mg/mL BREVIBLOC has, however,
been well tolerated when administered via a central
vein.<br/>Compatibility with
Commonly Used Intravenous Fluids: BREVIBLOC
was tested for compatibility with ten commonly used intravenous
fluids at a final concentration of 10 mg Esmolol Hydrochloride
per mL. BREVIBLOC was found to be compatible with the following
solutions and was stable for at least 24 hours at controlled
room temperature or under refrigeration: BREVIBLOC
is NOT compatible with Sodium Bicarbonate (5%) Injection,
USP.
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| dailymed-instance:descripti... |
BREVIBLOC (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/>Brevibloc Premixed
Injection: BREVIBLOC
PREMIXED INJECTION is a clear, colorless to light yellow,
sterile, nonpyrogenic, iso-osmotic solution of esmolol
hydrochloride in sodium chloride. 2500 mg, 250 mL Single Use Premixed
Bag���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). The
calculated osmolarity is 312 mOsmol/L. The 250 mL bag is a
non-latex, non-PVC IntraVia bag with dual PVC ports. The
IntraVia bag is manufactured from a specially designed
multilayer plastic (PL 2408). Solutions in contact with the
plastic container leach out certain chemical compounds from the
plastic in very small amounts; however, biological testing was
supportive of the safety of the plastic container materials. SeeDOSAGE AND
ADMINISTRATION, Directions for Use of the Premixed
Bag for additional information. 2000 mg, 100 mL Single Use Premixed Bag
DOUBLE STRENGTH���Each mL contains 20 mg Esmolol
Hydrochloride, 4.1 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). The calculated osmolarity is 312 mOsmol/L. The
100 mL bag is a non-latex, non-PVC IntraVia bag with dual PVC
ports. The IntraVia bag is manufactured from a specially
designed multilayer plastic (PL 2408). Solutions in contact with
the plastic container leach out certain chemical compounds from
the plastic in very small amounts; however, biological testing
was supportive of the safety of the plastic container materials. See DOSAGE AND
ADMINISTRATION, Directions for Use of the Premixed
Bag for additional information.<br/>Brevibloc Injection: BREVIBLOC
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). 100 mg, 5 mL DOUBLE STRENGTH Single Dose
Vial���Each mL contains 20 mg Esmolol
Hydrochloride, 4.1 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).<br/>Brevibloc
Concentrate: BREVIBLOC
CONCENTRATE is a clear, colorless to light yellow, sterile,
nonpyrogenic concentrate. 2500 mg, 10 mL Ampul���Each mL
contains 250 mg Esmolol Hydrochloride in 25% Propylene Glycol,
USP, 25% Alcohol, USP and Water for Injection, USP; buffered
with 17.0 mg Sodium Acetate Trihydrate, USP, and 0.00715 mL
Glacial Acetic Acid, USP. Sodium Hydroxide and/or Hydrochloric
Acid added, as necessary, to adjust pH to 3.5-5.5. NOT FOR
DIRECT INTRAVENOUS USE - AMPUL MUST BE DILUTED PRIOR TO
INFUSION. See DOSAGE AND
ADMINISTRATION, Directions for Use of the Brevibloc
Concentrate 10 mL Ampul (250
milligrams/mL).
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| dailymed-instance:clinicalP... |
BREVIBLOC (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.
BREVIBLOC 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: BREVIBLOC
(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 BREVIBLOC is not limited by the rate of blood flow to metabolizing tissues such as the liver or
affected by hepatic or renal blood flow. BREVIBLOC 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 BREVIBLOC
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 BREVIBLOC 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 of the infusion. Because of
its short half-life, blood levels of BREVIBLOC can be rapidly
altered by increasing or decreasing theinfusion rate and
rapidly eliminated by discontinuing the infusion. Consistent
with the high rate of blood-based metabolism of BREVIBLOC, 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 BREVIBLOC. Metabolism
of BREVIBLOC 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 is excreted in the urine with a clearance
approximately equivalent to the glomerular filtration rate.
Excretion of the acid metabolite is significantly decreased inpatients 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 BREVIBLOC 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. BREVIBLOC
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 BREVIBLOC (Esmolol Hydrochloride),
showing reduction in heart rate at rest and during exercise, and
attenuation of isoproterenol-induced increases in heart rate.
Blood levels of BREVIBLOC 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, BREVIBLOC 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, BREVIBLOC, 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, BREVIBLOC 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
BREVIBLOC 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
BREVIBLOC infusion, all of the hemodynamic parameters had
returned to pretreatment levels. The
relative cardioselectivity of BREVIBLOC was demonstrated in 10 mildly asthmatic patients. Infusions of BREVIBLOC [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), BREVIBLOC produced
slightly enhanced bronchomotor sensitivity to dry air stimulus.
These effects were not clinically significant, and BREVIBLOC 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 bronchospasm requiring
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 BREVIBLOC 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
BREVIBLOC (Esmolol Hydrochloride) with placebo and propranolol,
maintenance doses of 50 to 300 mcg/kg/min (0.05 to
0.3 mg/kg/min) of BREVIBLOC 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
BREVIBLOC 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
BREVIBLOC 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 BREVIBLOC 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 BREVIBLOC, 53% vs. 17%. The hypotension was rapidly
reversible with decreased infusion rate or after discontinuation
of therapy with BREVIBLOC. For both BREVIBLOC and propranolol,
hypotension was reported less frequently in patients receiving
concomitant digoxin.
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BREVIBLOC (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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| dailymed-instance:supply |
BREVIBLOC PREMIXED
INJECTION NDC 10019-055-61,
2500 mg���250 mL in Ready-to-use 250 mL IntraVia Bags BREVIBLOC DOUBLE
STRENGTH PREMIXED INJECTION NDC 10019-075-87,
2000 mg���100 mL in Ready-to-use 100 mL IntraVia Bags BREVIBLOC INJECTION NDC 10019-115-01,
100 mg���10 mL Ready-to-use Vials, Package of 25 BREVIBLOC DOUBLE
STRENGTH INJECTION NDC 10019-085-01,
100 mg���5 mL Ready-to-use Vials, Package of 10 BREVIBLOC CONCENTRATE NDC 10019-025-18,
2500 mg���10 mL Ampuls for Dilution, Package of 10 Store at 25��C (77��F). Excursions permitted to
15��-30��C (59��-86��F). [See USP Controlled Room Temperature.] PROTECT
FROM FREEZING. Avoid excessive heat. Manufactured for Baxter Healthcare Corporation Deerfield, IL 60015
USA Baxter, Brevibloc,
Brevibloc Premixed and IntraVia are trademarks of Baxter International
Inc. Brevibloc (esmolol
hydrochloride) and its packaging are protected by one or more of the
following: U.S. Pat. Nos. 5,017,609; 5,849,843; 5,998,019; 6,310,094;
6,528,540; Pat. Pending. For Product Inquiry
1 800 ANA DRUG (1-800-262-3784) Revised: August
2005
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| dailymed-instance:precautio... |
General: Infusion
concentrations of 20 mg/mL were associated with more serious
venous irritation, including thrombophlebitis, than
concentrations of 10 mg/mL with BREVIBLOC CONCENTRATE,
extravasation of 20 mg/mL or higher may lead to a serious local
reaction and possible skin necrosis. Concentrations greater than
10 mg/mL or infusioninto small veins or through a butterfly
catheter should be avoided. Because the
acid metabolite of BREVIBLOC is primarily excreted unchanged by
the kidney, BREVIBLOC (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 BREVIBLOC
CONCENTRATE 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 BREVIBLOC (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 BREVIBLOC and warfarin showed that
concomitant administration of BREVIBLOC and warfarin does not
alter warfarin plasma levels. BREVIBLOC concentrations were
equivocally higher when given with warfarin, but this is not
likely to be clinically important. When
digoxin and BREVIBLOC 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 BREVIBLOC pharmacokinetics. When intravenous morphine and
BREVIBLOC were concomitantly administered in normal subjects, no
effect on morphine blood levels was seen, but BREVIBLOC
steady-state blood levels were increased by 46% in the presence
of morphine. No other pharmacokinetic parameters were changed. The effect
of BREVIBLOC on the duration of succinylcholine-induced
neuromuscular blockade was studied in patients undergoing
surgery. The onset of neuromuscular blockade by succinylcholine
was unaffected by BREVIBLOC, 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, BREVIBLOC 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 BREVIBLOC and
verapamil in patients with depressed myocardial function. Fatal
cardiac arrests have occurred in patients receiving both drugs.
Additionally, BREVIBLOC 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
BREVIBLOC (Esmolol Hydrochloride).<br/>Pregnancy:<br/>Teratogenic
Effects:<br/>Nursing Mothers: It is not
known whether BREVIBLOC (Esmolol Hydrochloride) is excreted in
human milk; however, caution should be exercised when BREVIBLOC
is administered to a nursing woman.<br/>Pediatric Use: The safety
and effectiveness of BREVIBLOC (Esmolol Hydrochloride) in
pediatric patients have not been established.
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| dailymed-instance:overdosag... |
Acute Toxicity: Overdoses
of BREVIBLOC (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 BREVIBLOC have occurred due
to dilution errors. Use of BREVIBLOC PREMIXED INJECTION and
BREVIBLOC DOUBLE STRENGTH PREMIXED INJECTION may reduce the
potential for 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 BREVIBLOC resolved. Because of
its approximately 9-minute elimination half-life, the first step
in the management of toxicity should be to discontinue the
BREVIBLOC 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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| dailymed-instance:genericMe... |
esmolol hydrochloride
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| dailymed-instance:fullName |
Brevibloc (Injection, Solution, Concentrate)
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| dailymed-instance:adverseRe... |
The following
adverse reaction rates are based on use of BREVIBLOC (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 BREVIBLOC 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 BREVIBLOC
(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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| dailymed-instance:warning |
Hypotension: In clinical
trials 20-50% of patients treated with BREVIBLOC (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 timecan, in some cases, lead to cardiac failure. At the first sign
or symptom of impending cardiac failure, BREVIBLOC (Esmolol
Hydrochloride) should be withdrawn. Although withdrawal may be
sufficient because of the short elimination half-life of
BREVIBLOC, specific treatment may also be considered . The use of BREVIBLOC 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 BREVIBLOC, several cases of death
have been reported in complex clinical states where BREVIBLOC
was presumably being used to control ventricular
rate.<br/>Intraoperative and
Postoperative Tachycardia and/or Hypertension: BREVIBLOC
(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, BREVIBLOC (Esmolol Hydrochloride)
may be used with caution in patients with bronchospastic
diseases. However, since betaselectivity is not
absolute, BREVIBLOC 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: BREVIBLOC
(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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| dailymed-instance:indicatio... |
Supraventricular
Tachycardia: BREVIBLOC
(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. BREVIBLOC is also indicated
in noncompensatory sinus tachycardia where, in the physician's
judgment, the rapid heart rate requires specific intervention.
BREVIBLOC is not intended for use in chronic settings where
transfer to another agent is anticipated.<br/>Intraoperative and
Postoperative Tachycardia and/or Hypertension: BREVIBLOC
(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
BREVIBLOC to prevent such events is not recommended.
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| dailymed-instance:represent... | |
| dailymed-instance:routeOfAd... | |
| dailymed-instance:name |
Brevibloc
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