Source:http://www4.wiwiss.fu-berlin.de/dailymed/resource/drugs/3931
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Bumetanide (Injection, Solution)
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dailymed-instance:dosage |
Dosage should be individualized with careful monitoring of
patient response. Parenteral
Administration: Bumetanide injection may
be administered parenterally (IV or IM) to patients in whom gastrointestinal
absorption may be impaired or in whom oral administration is not practical. Parenteral
treatment should be terminated and oral treatment instituted as soon as possible. The
usual initial dose is 0.5 mg to 1 mg intravenously or intramuscularly. Intravenous
administration should be given over a period of 1 to 2 minutes. If the response
to an initial dose is deemed insufficient, a second or third dose may be given
at intervals of 2 to 3 hours, but should not exceed a daily dosage of 10 mg. Miscibility and Parenteral Solutions: The
compatibility tests of bumetanide injection with 5% Dextrose Injection, 0.9%
Sodium Chloride Injection, and Lactated Ringer's Injection in both
glass and plasticized PVC (Viaflex) containers have shown no significant absorption
effect with either containers, nor a measurable loss of potency due to degradation
of the drug. However, solutions should be freshly prepared and used within
24 hours. Parenteral drug products should be inspected
visually for particulate matter and discoloration prior to administration
whenever solution and container permit.
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dailymed-instance:descripti... |
Bumetanide is a loop diuretic, available in 4 mL and 10 mL
vials for intravenous or intramuscular injection as a sterile solution. Each
mL contains 0.25 mg bumetanide compounded with 0.85% sodium chloride and 0.4%
ammonium acetate as buffers; 0.01% edetate disodium; 1% benzyl alcohol as
preservative, and pHadjusted to approximately 7 with sodium hydroxide. Chemically,
bumetanide is 3-(butylamino)-4-phenoxy-5-sulfamoylbenzoic acid. It is a practically
white powder, slightly soluble in water; soluble in alkaline solutions, having
a calculated molecular weight of 364.42 and a molecular formula of CHNOS.
The structural formula is as follows:
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dailymed-instance:clinicalP... |
Bumetanide is a loop diuretic with a rapid onset and short
duration of action. Pharmacological and clinical studies have shown that 1
mg bumetanide has a diuretic potency equivalent to approximately 40 mg furosemide.
The major site of bumetanide action is the ascending limb of the loop of Henle. The
mode of action has been determined through various clearance studies in both
humans and experimental animals. Bumetanide inhibits sodium reabsorption in
the ascending limb of the loop of Henle, as shown by marked reduction of free-water
clearance (HO) during hydration and tubular free-water
reabsorption (THO) during hydropenia. Reabsorption
of chloride in the ascending limb is also blocked by bumetanide, and bumetanide
is somewhat more chloruretic than natriuretic. Potassium
excretion is also increased by bumetanide, in a dose-related fashion. Bumetanide
may have an additional action in the proximal tubule. Since phosphate reabsorption
takes place largely in the proximal tubule, phosphaturia during bumetanide-induced
diuresis is indicative of this additional action. This is further supported
by the reduction in the renal clearance of bumetanide by probenecid, associated
with diminution in the natriuretic response. This proximal tubular activity
does not seem to be related to an inhibition of carbonic anhydrase. Bumetanide
does not appear to have a noticeable action on the distal tubule. Bumetanide
decreases uric acid excretion and increases serum uric acid. Diuresis starts
within minutes following an intravenous injection and reaches maximum levels
within 15 to 30 minutes. Several pharmacokinetic studies
have shown that bumetanide, administered orally or parenterally, is eliminated
rapidly in humans, with a half-life of between 1 and 1��hours. Plasma
protein-binding is in the range of 94% to 96%. Oral
administration of carbon-14 labeled bumetanide to human volunteers revealed
that 81% of the administered radioactivity was excreted in the urine, 45%
of it as unchanged drug. Urinary and biliary metabolites identified in this
study were formed by oxidation of the N-butyl side chain. Biliary excretion
of bumetanide amounted to only 2% of the administered dose. Pediatric Pharmacology: Elimination
of bumetanide appears to be considerably slower in neonatal patients compared
with adults, possibly because of immature renal and hepatobiliary function
in this population. Small phamacokinetic studies of intravenous bumetanide
in preterm and full-term neonates with respiratory disorders have reported
an apparent half-life of approximately 6 hours with a range up to 15 hours
and a serum clearance ranging from 0.2 to 1.1 mL/min/kg. In a population of
neonates receiving bumetanide for volume overload, mean serum clearance rates
were 2.17 mL/min/kg in patients less than 2 months of age and 3.8 mL/min/kg
in patients aged 2 to 6 months. Mean serum half-life of bumetanide was 2.5
hours and 1.5 hours in patients aged less than 2 months and those aged 2 to
6 months, respectively. Elimination half-life decreased considerably during
the first month of life, from a mean of approximately 6 hours at birth to
approximately 2.4 hours at 1 month of age. In preterm
neonates, mean serum concentrations following a single 0.05 mg/kg dose ranged
from 126 mcg/L at 1 hour to 57 mcg/L at 8 hours. In another study, mean serum
concentrations following a single 0.05 mg/kg dose were 338 ng/mL at 30 minutes
and 176 ng/mL after 4 hours. A single dose of 0.1 mg/kg produced mean serum
levels of 314 ng/mL at 1 hour, and 196 ng/mL at 6 hours. Mean volume
of distribution in neonates has been reported to range from 0.26 L/kg to 0.39 L/kg. The
degree of protein binding of bumetanide in cord sera from healthy neonates
was approximately 97%, suggesting the potential for bilirubin displacement.
A study using pooled sera from critically ill neonates found that bumetanide
at concentrations of 0.5 to 50 mcg/mL, but not 0.25 mcg/mL, caused a linear
increase in unbound bilirubin concentrations. In 56
infants aged 4 days to 6 months, bumetanide doses ranging from 0.005 mg/kg
to 0.1 mg/kg were studied for pharmacodynamic effect. Peak bumetanide
excretion rates increased linearly with increasing doses of drug. Maximal
diuretic effect was observed at a bumetanide excretion rate of about 7 mcg/kg/hr,
corresponding to doses of 0.035 to 0.040 mg/kg. Higher doses produced a higher
bumetanide excretion rate but no increase in diuretic effect. Urine flow rate
peaked during the first hour after drug administration in 80%
of patients and by 3 hours in all patients. Geriatric Pharmacology: In
a group of ten geriatric subjects between the ages of 65 and 73 years, total
bumetanide clearance was significantly lower (1.8��0.3 mL/min/kg) compared
with younger subjects (2.9��0.2 mL/min/kg) after a single
oral bumetanide 0.5 mg dose. Maximum plasma concentrations were higher in
geriatric subjects (16.9��1.8 ng/mL) compared with younger subjects
(10.3��1.5 ng/mL). Urine flow rate and total excretion of sodium and
potassium were increased less in the geriatric subjects compared with younger
subjects, although potassium excretion and fractional sodium excretion were
similar between the two age groups. Nonrenal clearance, bioavailability, and
volume of distribution were not significantly different between the two groups.
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dailymed-instance:contraind... |
Bumetanide is contraindicated in anuria. Although bumetanide
can be used to induce diuresis in renal insufficiency, any marked increase
in blood urea nitrogen or creatinine, or the development of oliguria during
therapy of patients with progressive renal disease, is an indication for discontinuation
of treatment with bumetanide. Bumetanide is also contraindicated in patients
in hepatic coma or in states of severe electrolyte depletion until the condition
is improved or corrected. Bumetanide is contraindicated in patients hypersensitive
to this drug.
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dailymed-instance:supply |
Bumetanide Injection, USP is available as: Revised: November, 2004 Store at
20 to 25��C (68 to 77��F). [See USP Controlled Room Temperature.] PROTECT
FROM LIGHT. Retain in carton until ready to use. Do
not use the injection if it is discolored or contains a precipitate. HOSPIRA, INC., LAKE FOREST, IL 60045 USA
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dailymed-instance:genericDr... | |
dailymed-instance:boxedWarn... |
WARNING: Bumetanide Injection is a potent diuretic which,
if given in excessive amounts, can lead to a profound diuresis with water
and electrolyte depletion. Therefore, careful medical supervision is required,
and dose and dosage schedule have to be adjusted to the individual patient's
needs. (See DOSAGE AND ADMINISTRATION.)
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dailymed-instance:possibleD... | |
dailymed-instance:precautio... |
General:: Serum potassium should be measured periodically and potassium
supplements or potassium-sparing diuretics added if necessary. Periodic determinations
of other electrolytes are advised in patients treated with high doses or for
prolonged periods, particularly in those on low salt diets. Hyperuricemia
may occur; it has been asymptomatic in cases reported to date. Reversible
elevations of the BUN and creatinine may also occur, especially in association
with dehydration and particularly in patients with renal insufficiency. Bumetanide
may increase urinary calcium excretion with resultant hypocalcemia. Diuretics
have been shown to increase the urinary excretion of magnesium; this may result
in hypomagnesemia.<br/>Laboratory Tests:: Studies in normal subjects receiving bumetanide revealed
no adverse effects on glucose tolerance, plasma insulin, glucagon and growth
hormone levels, but the possibility of an effect on glucose metabolism exists.
Periodic determinations of blood sugar should be done, particularly in patients
with diabetes or suspected latent diabetes. Patients
under treatment should be observed regularly for possible occurrence of blood
dyscrasias, liver damage, or idiosyncratic reactions, which have been reported
occasionally in foreign marketing experience. The relationship of these occurrences
to bumetanide use is not certain.<br/>Drug Interactions::
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dailymed-instance:overdosag... |
Overdosage can lead to acute profound water loss, volume
and electrolyte depletion, dehydration, reduction of blood volume and circulatory
collapse with a possibility of vascular thrombosis and embolism. Electrolyte
depletion may be manifested by weakness, dizziness, mental confusion, anorexia,
lethargy, vomiting and cramps. Treatment consists of replacement of fluid
and electrolyte losses by careful monitoring of the urine and electrolyte
output and serum electrolyte levels.
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dailymed-instance:genericMe... |
Bumetanide
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dailymed-instance:fullName |
Bumetanide (Injection, Solution)
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dailymed-instance:adverseRe... |
The most frequent clinical adverse reactions considered probably
or possibly related to bumetanide are muscle cramps (seen in 1.1% of treated
patients), dizziness (1.1%), hypotension (0.8%), headache (0.6%), nausea (0.6%),
and encephalopathy (in patients with preexisting liver disease) (0.6%). One
or more of these adverse reactions have been reported in approximately 4.1%
ofbumetanide-treated patients. Less frequent clinical
adverse reactions to bumetanide are impaired hearing (0.5%), pruritus (0.4%),
electrocardiogram changes (0.4%), weakness (0.2%), hives (0.2%), abdominal
pain (0.2%), arthritic pain (0.2%), musculoskeletal pain (0.2%), rash (0.2%)
and vomiting (0.2%). One or more of these adverse reactions have been reported
in approximately 2.9% of bumetanide-treated patients. Other
clinical adverse reactions, which have each occurred in approximately 0.1%
of patients, are vertigo, chest pain, ear discomfort, fatigue, dehydration,
sweating, hyperventilation, dry mouth, upset stomach, renal failure, asterixis,
itching, nipple tenderness, diarrhea, premature ejaculation and difficulty
maintaining an erection. Laboratory abnormalities reported
have included hyperuricemia (in 18.4% of patients tested), hypochloremia (14.9%),
hypokalemia (14.7%), azotemia (10.6%), hyponatremia (9.2%), increased serum
creatinine (7.4%), hyperglycemia (6.6%), and variations in phosphorus (4.5%),
COcontent (4.3%), bicarbonate (3.1%) and calcium (2.4%). Although
manifestations of the pharmacologic action of bumetanide, these conditions
may become more pronounced by intensive therapy. Also
reported have been thrombocytopenia (0.2%) and deviations in hemoglobin (0.8%),
prothrombin time (0.8%), hematocrit (0.6%), WBC (0.3%) and differential counts
(0.1%). There have been rare spontaneous reports of thrombocytopenia from
postmarketing experience. Diuresis induced by bumetanide
may also rarely be accompanied by changes in LDH (1%), total serum bilirubin
(0.8%), serum proteins (0.7%), SGOT (0.6%), SGPT (0.5%), alkaline phosphatase
(0.4%), cholesterol (0.4%) and creatinine clearance (0.3%). Increases in urinary
glucose (0.7%) and urinary protein (0.3%) have also been seen.
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dailymed-instance:indicatio... |
Bumetanide injection is indicated for the treatment of edema
associated with congestive heart failure, hepatic and renal disease, including
the nephrotic syndrome. Almost equal diuretic response
occurs after oral and parenteral administration of bumetanide. Therefore,
if impaired gastrointestinal absorption is suspected or oral administration
is not practical, bumetanide should be given by the intramuscular or intravenous
route. Successful treatment with bumetanide following
instances of allergic reactions to furosemide suggests a lack of cross-sensitivity.
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Bumetanide
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