Source:http://www4.wiwiss.fu-berlin.de/dailymed/resource/drugs/4083
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Glucagon (Kit)
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General Instructions for Use::<br/>Directions for Treatment of Severe Hypoglycemia:: Severe hypoglycemia should be treated initially
with intravenous glucose, if possible.<br/>Directions for Use as a Diagnostic Aid:: Dissolve the lyophilized glucagon using the accompanying
diluting solution and use immediately. Discard any
unused portion. The doses
in the following table may be administered for relaxation of the stomach,
duodenum, and small bowel, depending on the onset and duration of effect required
for the examination. Since the stomach is less sensitive to the effect of
glucagon, 0.5 mg (0.5 units) IV or 2 mg (2 units) IM are recommended. For examination of the colon, it is recommended
that a 2 mg (2 units) dose be administered intramuscularly approximately 10 minutes
prior to the procedure. Colon relaxation and reduction of patient discomfort
may allow the radiologist to perform a more satisfactory examination.
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| dailymed-instance:descripti... |
Glucagon for Injection (rDNA origin) is a polypeptide
hormone identical to human glucagon that increases blood glucose and relaxes
smooth muscle of the gastrointestinal tract. Glucagon is synthesized in a
special non-pathogenic laboratory strain of Escherichia
coli bacteria that has been genetically altered by the addition
of the gene for glucagon. Glucagon is a single-chain
polypeptide that contains 29 amino acid residues and has a molecular weight
of 3483. The empirical formula is CHNOS.
The primary sequence of glucagon is shown below. Crystalline glucagon is a white to off-white powder. It is
relatively insoluble in water but is soluble at a pH of less than 3 or more
than 9.5. Glucagon is available for use intravenously,
intramuscularly, or subcutaneously in a kit that contains a vial of sterile
glucagon and a syringe of sterile diluent. The vial contains 1 mg (1 unit)
of glucagon and 49 mg of lactose. Hydrochloric acid may have been added during
manufacture to adjust the pH of the glucagon. One International Unit of glucagon
is equivalent to 1 mg of glucagon.The diluent syringe contains
12 mg/mL of glycerin, Water For Injection, and hydrochloric acid.
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Glucagon increases blood glucose concentration and
is used in the treatment of hypoglycemia. Glucagon acts only on liver glycogen,
converting it to glucose. Glucagon administered
through a parenteral route relaxes smooth muscle of the stomach, duodenum,
small bowel, and colon.<br/>Pharmacokinetics: Glucagon has been studied following intramuscular,
subcutaneous, and intravenous administration in adult volunteers. Administration
of the intravenous glucagon showed dose proportionality of the pharmacokinetics
between 0.25 and 2.0 mg. Calculations from a 1 mg dose showed a small volume
of distribution (mean, 0.25 L/kg) and a moderate clearance (mean, 13.5 mL/min/kg).
The half-life was short, ranging from 8 to 18 minutes. Maximum plasma concentrations of 7.9 ng/mL were achieved approximately
20 minutes after subcutaneous administration (see Figure 1A). With
intramuscular dosing, maximum plasma concentrations of 6.9 ng/mL were attained
approximately 13 minutes after dosing. Glucagon
is extensively degraded in liver, kidney, and plasma. Urinary excretion of
intact glucagon has not been measured.<br/>Pharmacodynamics: In a study of 25 volunteers, a subcutaneous dose
of 1 mg glucagon resulted in a mean peak glucose concentration of 136 mg/dL
30 minutes after injection (see Figure 1B). Similarly, following
intramuscular injection, the mean peak glucose level was 138 mg/dL, which
occurred at 26 minutes after injection. No difference in maximum blood glucose
concentration between animal-sourced and rDNA glucagon was observed after
subcutaneous and intramuscular injection.
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Glucagon is contraindicated in patients with known
hypersensitivity to it or in patients with known pheochromocytoma.
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| dailymed-instance:supply |
Glucagon Emergency Kit for Low Blood Sugar (Glucagon
for Injection [rDNA origin]) (MS8031):<br/>Stability and Storage:: Before
Reconstitution���Vials of Glucagon, as well as the Diluting Solution
for Glucagon, may be stored at controlled room temperature 20��to 25��C (68��to 77��F)[see
USP]. The USP defines controlled room temperature
by the following: A temperature maintained thermostatically that encompasses
the usual and customary working environment of 20��to 25��C (68��to 77��F);
that results in a mean kinetic temperature calculated to be not more than 25��C;
and that allows for excursions between 15��and 30��C (59��and 86��F) that are
experienced in pharmacies, hospitals, and warehouses. After
Reconstitution���Glucagon for Injection (rDNA origin) should be
used immediately. Discard any unused portion.
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| dailymed-instance:precautio... |
General: Glucagon is effective in treating hypoglycemia
only if sufficient liver glycogen is present. Because glucagon is of little
or no help in states of starvation, adrenal insufficiency, or chronic hypoglycemia,
hypoglycemia in these conditions should be treated with glucose.<br/>Information for Patients: Refer patients and family members to the attached
Information for the User for instructions describing the method of preparing
and injecting glucagon. Advise the patient and family members to become familiar
with the technique of preparing glucagon before an emergency arises. Instruct
patients to use 1 mg (1 unit) for adults and 1/2 the adult dose (0.5 mg) [0.5 unit]
for pediatric patients weighing less than 44 lb (20 kg). Patients and family members should be informed
of the following measures to prevent hypoglycemic reactions due to insulin: To prevent severe hypoglycemia, patients and
family members should be informed of the symptoms of mild hypoglycemia and
how to treat it appropriately. Family members
should be informed to arouse the patient as quickly as possible because prolonged
hypoglycemia may result in damage to the central nervous system. Glucagon
or intravenous glucose should awaken the patient sufficiently so that oral
carbohydrates may be taken. Patients should
be advised to inform their physician when hypoglycemic reactions occur so
that the treatment regimen may be adjusted if necessary.<br/>Laboratory Tests: Blood glucose determinations should be obtained
to follow the patient with hypoglycemia until patient is asymptomatic.<br/>Carcinogenesis, Mutagenesis, Impairment of Fertility: Because glucagon is usually given in a single
dose and has a very short half-life, no studies have been done regarding carcinogenesis.
In a series of studies examining effects on the bacterial mutagenesis (Ames)
assay, it was determined that an increase in
colony counts was related to technical difficulties in running this assay
with peptides and was not due to mutagenic activities of the glucagon. Reproduction studies have been performed in rats
at doses up to 2 mg/kg glucagon administered two times a day (up to 40 times
the human dose based on body surface area, mg/m) and have revealed
no evidence of impaired fertility.<br/>Pregnancy: Pregnancy
Category B���Reproduction studies have not been performed with recombinant
glucagon. However, studies with animal-sourced glucagon were performed in
rats at doses up to 2 mg/kg glucagon administered two times a day (up to 40 times
the human dose based on body surface area, mg/m), and have revealed
no evidence of impaired fertility or harm to the fetus due to glucagon. There
are, however, no adequate and well-controlled studies in pregnant women. Because
animal reproduction studies are not always predictive of human response, this
drug should be used during pregnancy 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 glucagon is administered to a nursing woman. If the drug
is excreted in human milk during its short half-life, it will be hydrolyzed
and absorbed like any other polypeptide. Glucagon is not active when taken
orally because it is destroyed in the gastrointestinal tract before it can
be absorbed.<br/>Pediatric Use: For the treatment of hypoglycemia: The use of
glucagon in pediatric patients has been reported to be safe and effective. For use as a diagnostic aid: Effectiveness has
not been established in pediatric patients.<br/>Geriatric Use: Clinical studies of glucagon did not include sufficient
numbers of subjects aged 65 and over to determine whether they respond differently
from younger subjects. Other reported clinical experience has not identified
differences in responses between the elderly and younger patients. In general,
dose selection for an elderly patient 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 disease or other drug
therapy.
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| dailymed-instance:overdosag... |
Signs and
Symptoms���If overdosage occurs, nausea, vomiting, gastric hypotonicity,
and diarrhea would be expected without causing consequential toxicity. Intravenous administration of glucagon has been shown to
have positive inotropic and chronotropic effects. A transient increase in
both blood pressure and pulse rate may occur following the administration
of glucagon. Patients taking��-blockers might be expected to have a greater
increase in both pulse and blood pressure, an increase of which will be transient
because of glucagon's short half-life. The increase in blood pressure
and pulse rate may require therapy in patients with pheochromocytoma or coronary
artery disease. When glucagon was given in
large doses to patients with cardiac disease, investigators reported a positive
inotropic effect. These investigators administered glucagon in doses of 0.5 to
16 mg/hour by continuous infusion for periods of 5 to 166 hours. Total doses
ranged from 25 to 996 mg, and a 21-month-old infant received approximately
8.25 mg in 165 hours. Side effects included nausea, vomiting, and decreasing
serum potassium concentration. Serum potassium concentration could be maintained
within normal limits with supplemental potassium. The
intravenous median lethal dose for glucagon in mice and rats is approximately
300 mg/kg and 38.6 mg/kg, respectively. Because
glucagon is a polypeptide, it would be rapidly destroyed in the gastrointestinal
tract if it were to be accidentally ingested. Treatment���To obtain up-to-date information about the treatment of overdose,
a good resource is your certified Regional Poison Control Center. Telephone
numbers of certified poison control centers are listed in the Physicians'
Desk Reference (PDR). In managing overdosage, consider the possibility
of multiple drug overdoses, interaction among drugs, and unusual drug kinetics
in your patient. In view of the extremely short
half-life of glucagon and its prompt destruction and excretion, the treatment
of overdosage is symptomatic, primarily for nausea, vomiting, and possible
hypokalemia. If the patient develops a dramatic
increase in blood pressure, 5 to 10 mg of phentolamine mesylate has been shown
to be effective in lowering blood pressure for the short time that control
would be needed. Forced diuresis, peritoneal
dialysis, hemodialysis, or charcoal hemoperfusion have not been established
as beneficial for an overdose of glucagon; it is extremely unlikely that one
of these procedures would ever be indicated.
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glucagon
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Glucagon (Kit)
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Severe adverse reactions are very rare, although nausea
and vomiting may occur occasionally. These reactions may also occur with hypoglycemia.
Generalized allergic reactions have been reported . In a
three month controlled study of 75 volunteers comparing animal-sourced glucagon
with glucagon manufactured through rDNA technology, no glucagon-specific antibodies
were detected in either treatment group.
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Glucagon should be administered cautiously to patients
with a history suggestive of insulinoma, pheochromocytoma, or both. In patients
with insulinoma, intravenous administration of glucagon may produce an initial
increase in blood glucose; however, because of glucagon's hyperglycemic
effect the insulinoma may release insulin and cause subsequent hypoglycemia.
A patient developing symptoms of hypoglycemia after a dose of glucagon should
be given glucose orally, intravenously, or by gavage, whichever is most appropriate. Exogenous glucagon also stimulates the release of
catecholamines. In the presence of pheochromocytoma, glucagon can cause the
tumor to release catecholamines, which may result in a sudden and marked increase
in blood pressure. If a patient develops a sudden increase in blood pressure,
5 to 10 mg of phentolamine mesylate may be administered intravenously in an
attempt to control the blood pressure. Generalized allergic reactions, including urticaria,
respiratory distress, and hypotension, have been reported in patients who
received glucagon by injection.
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For the treatment of hypoglycemia:: Glucagon is indicated as a treatment for severe
hypoglycemia. Because patients with type 1
diabetes may have less of an increase in blood glucose levels compared with
a stable type 2 patient, supplementary carbohydrate should be given as soon
as possible, especially to a pediatric patient.<br/>For use as a diagnostic aid:: Glucagon is indicated as a diagnostic aid in the
radiologic examination of the stomach, duodenum, small bowel, and colon when
diminished intestinal motility would be advantageous. Glucagon
is as effective for this examination as are the anticholinergic drugs. However,
the addition of the anticholinergic agent may result in increased side effects.
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Glucagon
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