Source:http://www4.wiwiss.fu-berlin.de/dailymed/resource/drugs/3364
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Isuprel (Injection, Solution)
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| dailymed-instance:dosage |
ISUPREL injection 1:5000 should generally be started at the
lowest recommended dose and the rate of administration gradually increased
if necessary while carefully monitoring the patient. The usual route of administration
is by intravenous infusion or bolus intravenous injection. In dire emergencies,
the drug may be administered by intracardiac injection. If time is not of
the utmost importance, initial therapy by intramuscular or subcutaneous injection
is preferred. *Subsequent dosage and method of administration depend
on the ventricular rate and the rapidity with which the cardiac pacemaker
can take over when the drug is gradually withdrawn. There
are no well-controlled studies in children to establish appropriate dosing;
however, the American Heart Association recommends an initial infusion rate
of 0.1 mcg/kg/min, with the usual range being 0.1 mcg/kg/min to 1 mcg/kg/min. Parenteral drug products should be inspected visually for
particulate matter and discoloration prior to administration, whenever solution
and container permit. Such solution should not be used.
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| dailymed-instance:descripti... |
Isoproterenol hydrochloride is 3,4-Dihydroxy-��-[(isopropylamino)methyl]
benzyl alcohol hydrochloride, a synthetic sympathomimetic amine that is structurally
related to epinephrine but acts almost exclusively on beta receptors. The
molecular formula is CHNO���HCl.
It has a molecular weight of 247.72 and the following structural formula: Isoproterenol
hydrochloride is a racemic compound. Each milliliter
of the sterile 1:5000 solution contains: The pH is adjusted between 2.5 and 4.5 with hydrochloric
acid. The sterile 1:5000 solution is nonpyrogenic and
can be administered by the intravenous, intramuscular, subcutaneous, or intracardiac
routes.
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| dailymed-instance:clinicalP... |
Isoproterenol is a potent nonselective beta-adrenergic agonist
with very low affinity for alpha-adrenergic receptors. Intravenous infusion
of isoproterenol in man lowers peripheral vascular resistance, primarily in
skeletal muscle but also in renal and mesenteric vascular beds. Diastolic
pressure falls. Renal blood flow is decreased in normotensive subjects but
is increased markedly in shock. Systolic blood pressure may remain unchanged
or rise, although mean arterial pressure typically falls. Cardiac output is
increased because of the positive inotropic and chronotropic effects of the
drug in the face of diminished peripheral vascular resistance. The cardiac
effects of isoproterenol may lead to palpitations, sinus tachycardia, and
more serious arrhythmias; large doses of isoproterenol may cause myocardial
necrosis in animals. Isoproterenol relaxes almost all
varieties of smooth muscle when the tone is high, but this action is most
pronounced on bronchial and gastrointestinal smooth muscle. It prevents or
relieves bronchoconstriction, but tolerance to this effect develops with overuse
of the drug. In man, isoproterenol causes less hyperglycemia
than does epinephrine. Isoproterenol and epinephrine are equally effective
in stimulating the release of free fatty acids and energy production. Absorption, Fate, and Excretion. Isoproterenol
is readily absorbed when given parenterally or as an aerosol. It is metabolized
primarily in the liver and other tissues by COMT. Isoproterenol is a relatively
poor substrate for MAO and is not taken up by sympathetic neurons to the same
extent as are epinephrine and norepinephrine. The duration of action of isoproterenol
may therefore be longer than that of epinephrine, but is still brief.
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| dailymed-instance:contraind... |
Use of isoproterenol hydrochloride injection is contraindicated
in patients with tachyarrhythmias; tachycardia or heart block caused by digitalis
intoxication; ventricular arrhythmias which require inotropic therapy; and
angina pectoris.
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Protect from light. Keep in opaque
container until used. Store
at controlled room temperature 20��to 25��C (68��to 77��F).
[See USP.] Do not use if the injection is
pinkish or darker than slightly yellow or contains a precipitate. HOSPIRA, INC., LAKE FOREST,
IL 60045 USA
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| dailymed-instance:precautio... |
General: Isoproterenol hydrochloride injection should generally be
started at the lowest recommended dose. This may be gradually increased if
necessary while carefully monitoring the patient. Doses sufficient to increase
the heart rate to more than 130 beats per minute may increase the likelihood
of inducing ventricular arrhythmias. Such increases in heart rate will also
tend to increase cardiac work and oxygen requirements which may adversely
affect the failing heart or the heart with a significant degree of arteriosclerosis. Particular
caution is necessary in administering isoproterenol hydrochloride injection
to patients with coronary artery disease, coronary insufficiency, diabetes,
hyperthyroidism, and sensitivity to sympathomimetic amines. Adequate
filling of the intravascular compartment by suitable volume expanders is of
primary importance in most cases of shock and should precede the administration
of vasoactive drugs. In patients with normal cardiac function, determination
of central venous pressure is a reliable guide during volume replacement.
If evidence of hypoperfusion persists after adequate volume replacement, isoproterenol
hydrochloride injection may be given. In addition to
the routine monitoring of systemic blood pressure, heart rate, urine flow,
and the electrocardiograph, the response to therapy should also be monitored
by frequent determination of the central venous pressure and blood gases.
Patients in shock should be closely observed during isoproterenol hydrochloride
injection administration. If the heart rate exceeds 110 beats per minute,
it may be advisable to decrease the infusion rate or temporarily discontinue
the infusion. Determinations of cardiac output and circulation time may also
be helpful. Appropriate measures should be taken to ensure adequate ventilation.
Careful attention should be paid to acid-base balance and to the correction
of electrolyte disturbances. In cases of shock associated with bacteremia,
suitable antimicrobial therapy is, of course, imperative.<br/>Drug Interactions: Isoproterenol hydrochloride injection and epinephrine should
not be administered simultaneously because both drugs are direct cardiac stimulants
and their combined effects may induce serious arrhythmias. The drugs may,
however, be administered alternately provided a proper interval has elapsed
between doses. ISUPREL should be used with caution,
if at all, when potent inhalational anesthetics such as halothane are employed
because of potential to sensitize the myocardium to effects of sympathomimetic
amines.<br/>Carcinogenesis, Mutagenesis, Impairment of Fertility: Long-term studies in animals to evaluate the carcinogenic
potential of isoproterenol hydrochloride have not been done. Mutagenic potential
and effect on fertility have not been determined. There is no evidence from
human experience that isoproterenol hydrochloride injection may be carcinogenic
or mutagenic or that it impairs fertility.<br/>Pregnancy Category C: Animal reproduction studies have not been conducted with
isoproterenol hydrochloride. It is also not known whether isoproterenol hydrochloride
can cause fetal harm when administered to a pregnant woman or can affect reproduction
capacity. Isoproterenol hydrochloride should be given to a pregnant woman
only if clearly needed.<br/>Nursing Mothers: It is not known whether this drug is excreted in human milk.
Because many drugs are excreted in human milk, caution should be exercised
when isoproterenol hydrochloride injection is administered to a nursing woman.<br/>Pediatric Use: Safety and efficacy of isoproterenol in pediatric patients
have not been established. Intravenous infusions of
isoproterenol in refractory asthmatic children at rates of 0.05-2.7��g/kg/min
have caused clinical deterioration, myocardial necrosis, congestive heart
failure and death. The risks of cardiac toxicity appear to be increased by
some factors [acidosis, hypoxemia, coadministration of corticosteroids, coadministration
of methylxanthines (theophylline, theobromine) or aminophylline] that are
especially likely to be present in these patients. If I.V. isoproterenol is
used in children with refractory asthma, patient monitoring must include continuous
assessment of vital signs, frequent electrocardiography, and daily measurements
of cardiac enzymes, including CPK-MB.<br/>Geriatric Use: Clinical studies of Isuprel did not include sufficient numbers
of subjects aged 65 and over to determine whether they respond differently
from younger subjects in clinical circumstances. There are, however, some
data that suggest that elderly healthy or hypertensive patients are less responsive
to beta-adrenergic stimulation than are younger subjects. In general, dose
selection for elderly patients should be cautious, usually starting at the
low end of the dosing range, reflecting the greater frequency of decreased
hepatic, renal or cardiac function and of concomitant diseases or other drug
therapy.
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| dailymed-instance:overdosag... |
The acute toxicity of isoproterenol hydrochloride in animals
is much less than that of epinephrine. Excessive doses in animals or man can
cause a striking drop in blood pressure, and repeated large doses in animals
may result in cardiac enlargement and focal myocarditis. In
case of accidental overdosage as evidenced mainly by tachycardia or other
arrhythmias, palpitations, angina, hypotension, or hypertension, reduce rate
of administration or discontinue isoproterenol hydrochloride injection until
patient's condition stabilizes. Blood pressure, pulse, respiration,
and EKG should be monitored. It is not known whether
isoproterenol hydrochloride is dialyzable. The oral
LDof isoproterenol hydrochloride in mice is 3,850 mg/kg��1,190 mg/kg of pure drug in solution.
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| dailymed-instance:genericMe... |
Isoproterenol Hydrochloride
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| dailymed-instance:fullName |
Isuprel (Injection, Solution)
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| dailymed-instance:adverseRe... |
The following reactions to isoproterenol hydrochloride injection
have been reported: CNS: Nervousness, headache, dizziness, nausea, visual blurring. Cardiovascular: Tachycardia, palpitations, angina,
Adams-Stokes attacks, pulmonary edema, hypertension, hypotension, ventricular
arrhythmias, tachyarrhythmias. In a few patients, presumably
with organic disease of the AV node and its branches, isoproterenol hydrochloride
injection has been reported to precipitate Adams-Stokes seizures during normal
sinus rhythm or transient heart block. Respiratory: Dyspnea. Other: Flushing of the skin, sweating, mild tremors, weakness, pallor.
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| dailymed-instance:warning |
Isoproterenol hydrochloride injection, by increasing myocardial
oxygen requirements while decreasing effective coronary perfusion, may have
a deleterious effect on the injured or failing heart. Most experts discourage
its use as the initial agent in treating cardiogenic shock following myocardial
infarction. However, when a low arterial pressure has been elevated by other
means, isoproterenol hydrochloride injection may produce beneficial hemodynamic
and metabolic effects. In a few patients, presumably
with organic disease of the AV node and its branches, isoproterenol hydrochloride
injection has paradoxically been reported to worsen heart block or to precipitate
Adams-Stokes attacks during normal sinus rhythm or transient heart block. Contains
sodium metabisulfite, a sulfite that may cause allergic-type reactions including
anaphylactic symptoms and life-threatening or less severe asthmatic episodes
in certain susceptible people. The overall prevalence of sulfite sensitivity
in the general population is unknown and probably low. Sulfite sensitivity
is seen more frequently in asthmatic than in nonasthmatic people.
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| dailymed-instance:indicatio... |
Isoproterenol hydrochloride injection is indicated:
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| dailymed-instance:name |
Isuprel
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