Source:http://www4.wiwiss.fu-berlin.de/dailymed/resource/drugs/1471
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Dipyridamole (Injection)
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The dose of
intravenous Dipyridamole Injection as an adjunct to thallium myocardial
perfusion imaging should be adjusted according to the weight of the
patient. The recommended dose is 0.142 mg/kg/min (0.57 mg/kg total)
infused over 4 minutes. Although the maximum tolerated dose has not been
determined, clinical experience suggests that a total dose beyond 60 mg
is not needed for any patient. Prior to
intravenous administration, Dipyridamole Injection should be diluted in
at least a 1:2 ratio with sodium chloride injection 0.45%, sodium
chloride injection 0.9% or dextrose injection 5% for a total volume of
approximately 20 to 50 mL. Infusion of undiluted dipyridamole may cause
local irritation. Thallium-201 should
be injected within 5 minutes following the 4-minute infusion of
dipyridamole. Do not mix
Dipyridamole Injection with other drugs in the same syringe or infusion
container. 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... |
Dipyridamole is a
coronary vasodilator described as 2,6 bis-(diethanolamino)-4,8
dipiperidino-pyrimido-(5,4-d) pyrimidine. The structural formula is: CHNOMW
504.63 Dipyridamole
Injection, USP is a sterile, odorless, pale yellow liquid which can be
diluted in sodium chloride injection or dextrose injection for
intravenous administration. Each mL contains 5 mg dipyridamole, USP, 50
mg polyethylene glycol 600 and 2 mg tartaric acid in Water for
Injection, USP. pH 2.2-3.2; hydrochloric acid added for pH
adjustment.
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In a study of 10
patients with angiographically normal or minimally stenosed (less than
25% luminal diameter narrowing) coronary vessels, Dipyridamole Injection
in a dose of 0.56 mg/kg infused over 4 minutes resulted in an average
fivefold increase in coronary blood flow velocity compared to resting
coronary flow velocity (range 3.8 to 7 times resting velocity). The mean
time to peak flow velocity was 6.5 minutes from the start of the
4-minute infusion (range 2.5 to 8.7 minutes). Cardiovascular responses
to the intravenous administration of Dipyridamole Injection when given
to patients in the supine position include a mild but significant
increase in heart rate of approximately 20% and mild but significant
decreases in both systolic and diastolic blood pressure of approximately
2-8%, with vital signs returning to baseline values in approximately 30
minutes.<br/>Mechanism of Action: Dipyridamole is a coronary vasodilator in man. The mechanism of
vasodilation has not been fully elucidated, but may result from
inhibition of uptake of adenosine, an important mediator of
coronary vasodilation. The vasodilatory effects of dipyridamole
are abolished by administration of the adenosine receptor
antagonist theophylline. How
dipyridamole-induced vasodilation leads to abnormalities in
thallium distribution and ventricular function is also uncertain
but presumably represents a���steal���phenomenon in which
relatively intact vessels dilate and sustain enhanced flow,
leaving reduced pressure and flow across areas of
hemodynamically important coronary vascular
constriction.<br/>Pharmacokinetics
and Metabolism: Plasma
dipyridamole concentrations decline in a triexponential fashion
following intravenous infusion of dipyridamole, with half-lives
averaging 3-12 minutes, 33-62 minutes and 11.6-15 hours. Two
minutes following a 0.568 mg/kg dose of Dipyridamole Injection
administered as a 4-minute infusion, the mean dipyridamole serum
concentration is 4.6��1.3 mcg/mL. The average plasma protein
binding of dipyridamole is approximately 99%, primarily to��-glycoprotein. Dipyridamole is metabolized in
the liver to the glucuronic acid conjugate and excreted with the
bile. The average total body clearance is 2.3-3.5 mL/min/kg,
with an apparent volume of distribution at steady state of 1-2.5 L/kg and a central apparent volume of 3-5 liters.
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Hypersensitivity to dipyridamole.
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Dipyridamole
Injection, USP is available in: 10 mL (50
mg/10 mL) SINGLE DOSEvial
packaged in 5s (NDC 0641-2569-44)<br/>Storage: PROTECT FROM LIGHT: Keep covered in
carton until time of use. Store between 15��-25��C (59��-77��F).
Avoid freezing. 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) MLT-00098/3.0
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See WARNINGS.<br/>Drug Interactions: Oral
maintenance theophylline and other xanthine derivatives such as
caffeine may abolish the coronary vasodilatation induced by
intravenous Dipyridamole Injection administration. This could
lead to a false negative thallium imaging result (see CLINICAL
PHARMACOLOGY���Mechanism of Action). Myasthenia
gravis patients receiving therapy with cholinesterase inhibitors
may experience worsening of their disease in the presence of
dipyridamole.<br/>Carcinogenesis,
Mutagenesis, Impairment of Fertility: In studies
in which dipyridamole was administered in the feed at doses of
up to 75 mg/kg/day (9.4 timesthe
maximum recommended daily human oral dose) in mice (up to 128
weeks in males and up to 142 weeks in females) and rats (up to
111 weeks in males and females), there was no evidence of
drug-related carcinogenesis. Mutagenicity tests of dipyridamole
with bacterial and mammalian cell systems were negative. There
was no evidence of impaired fertility when dipyridamole was
administered to male and female rats at oral doses up to 500
mg/kg/day (63 times. the maximum
recommended daily human oral dose). A significant reduction in
number of corpora lutea with consequent reduction in
implantations and live fetuses was, however, observed at 1250 mg/kg/day.<br/>Pregnancy:<br/>Teratogenic
Effects���Pregnancy Category B: Reproduction studies performed in mice and rats at
daily oral doses of up to 125 mg/kg (15.6
timesthe maximum recommended daily human oral dose) and in
rabbits at daily oral doses of up to 20 mg/kg (2.5
timesthe maximum recommended daily human oral dose) have
revealed no evidence of impaired embryonic development
due to dipyridamole. There are, however, no adequate and
well-controlled studies in pregnant women. Because
animal reproduction studies are not always predictive of
human responses, this drug should be used during
pregnancy only if clearly needed.<br/>Nursing Mothers: Dipyridamole is excreted in human milk.<br/>Pediatric Use: Safety and
effectiveness in pediatric patients have not been
established.
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No cases of
overdosage in humans have been reported. It is unlikely that overdosage
will occur because of the nature of use (i.e., single intravenous
administration in controlled settings). See WARNINGS.
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Dipyridamole
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Dipyridamole (Injection)
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Adverse reaction
information concerning intravenous Dipyridamole Injection is derived
from a study of 3911 patients in which intravenous dipyridamole was used
as an adjunct to thallium myocardial perfusion imaging and from
spontaneous reports of adverse reactions and the published literature. Serious adverse
events (cardiac death, fatal and non-fatal myocardial infarction,
ventricular fibrillation, asystole, sinus node arrest, symptomatic
ventricular tachycardia, stroke, transient cerebral ischemia, seizures,
anaphylactoid reaction and bronchospasm) are described above . In a study of 3911
patients, the most frequent adverse reactions were: chest pain/angina
pectoris (19.7%), electrocardiographic changes (most commonly ST-T
changes) (15.9%), headache (12.2%) and dizziness (11.8%). Adverse reactions
occurring in greater than 1% of the patients in the study are shown in
the following table: Less common adverse
reactions occurring in 1% or less of the patients within the study
included:<br/>Cardiovascular
System: Electrocardiographic abnormalities unspecified (0.8%),
arrhythmia unspecified (0.6%), palpitation (0.3%), ventricular tachycardia , bradycardia (0.2%), myocardial infarction
, AV block (0.1%), syncope (0.1%),
orthostatic hypotension (0.1%), atrial fibrillation (0.1%),
supraventricular tachycardia(0.1%), ventricular arrhythmia
unspecified , heart block unspecified (0.03%),
cardiomyopathy (0.03%), edema (0.03%).<br/>Central and
Peripheral Nervous System: Hypothesia
(0.5%), hypertonia (0.3%), nervousness/anxiety (0.2%), tremor
(0.1%), abnormal coordination (0.03%), somnolence (0.03%),
dysphonia (0.03%), migraine (0.03%), vertigo
(0.03%).<br/>Gastrointestinal
System: Dyspepsia
(1%), dry mouth (0.8%), abdominal pain (0.7%), flatulence
(0.6%), vomiting (0.4%), eructation (0.1%), dysphagia (0.03%),
tenesmus (0.03%), appetite increase (0.03%).<br/>Respiratory System: Pharyngitis
(0.3%), bronchospasm , hyperventilation (0.1%), rhinitis (0.1%),
coughing (0.03%), pleural pain (0.03%).<br/>Other: Myalgia
(0.9%), back pain (0.6%), injection site reaction unspecified
(0.4%), diaphoresis (0.4%), asthenia (0.3%), malaise (0.3%),
arthralgia (0.3%), injection site pain (0.1%), rigor (0.1%),
earache (0.1%), tinnitus (0.1%), vision abnormalities
unspecified (0.1%), dysgeusia (0.1%), thirst (0.03%),
depersonalization (0.03%), eye pain (0.03%), renal pain (0.03%),
perineal pain (0.03%), breast pain (0.03%), intermittent
claudication (0.03%), leg cramping (0.03%). In additional
postmarketing experience, there have been rare reports of
allergic reaction including urticaria, pruritus, dermatitis and
rash.
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Serious adverse
reactions associated with the administration of intravenous Dipyridamole
Injection have included cardiac death, fatal and non-fatal myocardial
infarction, ventricular fibrillation, symptomatic ventricular
tachycardia, stroke, transient cerebral ischemia, seizures,
anaphylactoid reaction and bronchospasm. There have been reported cases
of asystole, sinus node arrest, sinus node depression and conduction
block. Patients with abnormalities of cardiac impulse
formation/conduction or severe coronary artery disease may be at
increased risk for these events. In a study of 3911
patients given intravenous dipyridamole as an adjunct to thallium
myocardial perfusion imaging, two types of serious adverse events were
reported: Although the
incidence of these serious adverse events was small (0.3%, 10 of 3911),
the potential clinical information to be gained through use of
intravenous dipyridamole thallium imaging (see INDICATIONS AND
USAGE noting the rate of false positive and false
negative results) must be weighed against the risk to the patient.
Patients with a history of unstable angina may be at a greater risk for
severe myocardial ischemia. Patients with a history of asthma may be at
a greater risk for bronchospasm during Dipyridamole Injection use. When thallium
myocardial perfusion imaging is performed with intravenous dipyridamole,
parenteral aminophylline should be readily available for relieving
adverse events such as bronchospasm or chest pain. Vital signs should be monitored during, and for 10-15 minutes following, the intravenous
infusion of dipyridamole and an electrocardiographic tracing should be
obtained using at least one chest lead. Should severe chest pain or
bronchospasm occur, parenteral aminophylline may be administered by slow
intravenous injection (50-100 mg over 30-60 seconds) in doses ranging
from 50 to 250 mg. In the case of severe hypotension, the patient should
be placed in a supine position with the head tilted down if necessary,
before administration of parenteral aminophylline. If 250 mg of
aminophylline does not relieve chest pain symptoms within a few minutes,
sublingual nitroglycerin may be administered. Ifchest pain continues
despite use of aminophylline and nitroglycerin, the possibility of
myocardial infarction should be considered. If the clinical condition of
a patient with an adverse event permits a one-minute delay in the
administration of parenteral aminophylline, thallium-201 may be injected
and allowed to circulate for one minute before the injection of
aminophylline. This will allow initial thallium perfusion imaging to be
performed before reversal of the pharmacologic effects of dipyridamole
on the coronary circulation.
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Dipyridamole
Injection is indicated as an alternative to exercise in thallium
myocardial perfusion imaging for the evaluation of coronary artery
disease in patients who cannot exercise adequately. In a study of about
1100 patients who underwent coronary arteriography and Dipyridamole
Injection assisted thallium imaging, the results of both tests were
interpreted blindly and the sensitivity and specificity of the
dipyridamole thallium study in predicting the angiographic outcome were
calculated. The sensitivity of the dipyridamole test (true positive
dipyridamole divided by the total number of patients with positive
angiography) was about 85%.The specificity (true negative divided by
the number of patients with negative angiograms) was about 50%. In a subset of
patients who had exercise thallium imaging as well as dipyridamole thallium imaging, sensitivity and specificity of the two tests were
almost identical.
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Dipyridamole
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