Source:http://www4.wiwiss.fu-berlin.de/dailymed/resource/drugs/3296
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Fentanyl Citrate (Injection, Solution)
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| dailymed-instance:dosage |
50 mcg = 0.05 mg = 1 mL Dosage
should be individualized. Some of the factors to be considered in
determining the dose are age, body weight, physical status, underlying
pathological condition, use of other drugs, type of anesthesia to
be used and the surgical procedure involved. Dosage should be reduced
in elderly or debilitated patients (see PRECAUTIONS). Vital signs should be monitored routinely. I. Premedication���Premedication (to be appropriately
modified in the elderly, debilitated and those who have received other
depressant drugs)���50 to 100 mcg (0.05 to 0.1 mg) (1 to 2
mL) may be administered intramuscularly 30 to 60 minutes prior to
surgery. II. Adjunct to General Anesthesia���See Dosage Range Chart. III. Adjunct
to Regional Anesthesia���50 to 100 mcg (0.05 to 0.1 mg) (1
to 2 mL) may be administered intramuscularly or slowly intravenously,
over one to two minutes, when additional analgesia is required. IV. Postoperatively (recovery room)���50 to 100
mcg (0.05 to 0.1 mg) (1 to 2 mL) may be administered intramuscularly
for the control of pain, tachypnea and emergence delirium. The dose
may be repeated in one to two hours as needed. Usage in Children: For induction
and maintenance in children 2 to 12 years of age, a reduced dose as
low as 2 to 3 mcg/kg is recommended. As a General Anesthetic: When attenuation
of the responses to surgical stress is especially important, doses
of 50 to 100 mcg/kg (0.05 to 0.1 mg/kg) (1 to 2 mL/kg) may be administered
with oxygen and a muscle relaxant. This technique has been reported
to provide anesthesia without the use of additional anesthetic agents.
In certain cases, doses up to 150 mcg/kg (0.15 mg/kg) (3 mL/kg)
may be necessary to produce this anesthetic effect. It has been used
for open heart surgery and certain other major surgical procedures
in patients for whom protection of the myocardium from excess oxygen
demand is particularly indicated, and for certain complicated neurological
and orthopedic procedures. As noted above,
it is essential that qualified personnel and adequate facilities be
available for the management of respiratory depression. See WARNINGS and PRECAUTIONS for use of fentanyl with
other CNS depressants, and in patients with altered response. Parenteral drug products should be inspected visually
for particulate matter and discoloration prior to administration whenever
solution and container permit. Do not administer
unless solution is clear and container undamaged. Discard unused portion. To prevent needle-stick injuries, needles should
not be recapped, purposely bent, or broken by hand.
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| dailymed-instance:descripti... |
Fentanyl Citrate Injection, USP is a sterile, nonpyrogenic
solution of fentanyl citrate in water for injection. Fentanyl Citrate is a
potent narcotic analgesic which is administered only by the intravenous or
intramuscular routes of injection. Each milliliter
contains fentanyl (as the citrate) 50 mcg (0.05 mg). May contain sodium hydroxide
and/or hydrochloric acid for pH adjustment. pH 4.7 (4.0 to 7.5). The solution contains no bacteriostat, antimicrobial agent or added buffer
and is intended only for use as a single-dose injection. When smaller doses
are required, the unused portion should be discarded in an appropriate manner. Fentanyl Citrate, USP, a white powder which is sparingly soluble in water,
is chemically designated N-(1-phenethyl-4-piperidyl) propionanilide citrate
(1:1). The molecular formula is CHNO���CHOand
the molecular weight is 528.60. Fentanyl Citrate has the following structural
formula:
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| dailymed-instance:clinicalP... |
Fentanyl citrate is a narcotic analgesic. A dose
of 100 mcg (0.1 mg) (2 mL) is approximately equivalent in analgesic
activity to 10 mg of morphine or 75 mg of meperidine. The principal
actions of therapeutic value are analgesia and sedation. Alterations
in respiratory rate and alveolar ventilation, associated with narcotic
analgesics, may last longer than the analgesic effect. As the dose
of narcotic is increased, the decrease in pulmonary exchange becomes
greater. Large doses may produce apnea. Fentanyl appears to have less
emetic activitythan either morphine or meperidine. Histamine assays
and skin wheal testing in man indicate that clinically significant
histamine release rarely occurs with fentanyl. Recent assays in man
show no clinically significant histamine release in dosages up to
50 mcg/kg (0.05 mg/kg) (1 mL/kg). Fentanyl preserves cardiac stability,
and blunts stress-related hormonal changes at higher doses. The pharmacokinetics of fentanyl can be described
as a three-compartment model, with a distribution time of 1.7 minutes,
redistribution of 13 minutes and a terminal elimination half-life
of 219 minutes. The volume of distribution for fentanyl is 4 L/kg. Fentanyl plasma protein binding decreases with increasing
ionization of the drug. Alterations in pH may affect its distribution
between plasma and the central nervous system. It accumulates in skeletal
muscle and fat, and is released slowly into the blood. Fentanyl, which
is primarily transformed in the liver, demonstrates a high first-pass
clearance and releases approximately 75% of an intravenous dose in
urine, mostly as metabolites with less than 10% representing the unchanged
drug. Approximately 9% of the dose is recovered in the feces, primarily
as metabolites. The onset of action of
fentanyl is almost immediate when the drug is given intravenously;
however, the maximal analgesic and respiratory depressant effect may
not be noted for several minutes. The usual duration of action of
the analgesic effect is 30 to 60 minutes after a single intravenous
dose of up to 100 mcg (0.1 mg) (2 mL). Following intramuscular administration,
the onset of action is from seven to eight minutes, and the duration
of action is one to two hours. As with longer acting narcotic analgesics,
the duration of the respiratory depressant effect of fentanyl may
be longer than the analgesic effect. The following observations have
been reported concerning altered respiratory response to COstimulation following administration of fentanyl citrate to man.
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Fentanyl Citrate Injection is contraindicated in
patients with known intolerance to the drug.
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| dailymed-instance:supply |
Fentanyl Citrate Injection, USP equivalent to 50
mcg (0.05 mg) fentanyl/mL, is supplied in single-dose glass containers
as follows: Protect from light. Retain
incarton until time of use. Store
at 20 to 25��C (68 to 77��F). [See USP Controlled Room Temperature.] April, 2006 HOSPIRA, INC., LAKE
FOREST, IL 60045 USA
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| dailymed-instance:precautio... |
General:: The initial dose of fentanyl citrate should be appropriately
reduced in elderly and debilitated patients. The effect of the initial
dose should be considered in determining incremental doses. Nitrous oxide has been reported to produce cardiovascular
depression when given with higher doses of fentanyl. Certain forms of conduction anesthesia, such as spinal anesthesia
and some peridural anesthetics, can alter respiration by blocking
intercostal nerves. Through other mechanisms (see CLINICAL PHARMACOLOGY)
fentanyl can also alter respiration. Therefore, when fentanyl is used
to supplement these forms of anesthesia, the anesthetist should be
familiar with the physiological alterations involved, and be prepared
to manage them in the patients selected for these forms of anesthesia. When a tranquilizer such as droperidol is used with fentanyl,
pulmonary arterial pressure may be decreased. This fact should be
considered by those who conduct diagnostic and surgical procedures
where interpretation of pulmonary arterial pressure measurements might
determine final management of the patient. When high dose or anesthetic
dosages of fentanyl are employed, even relatively small dosages of
diazepam may cause cardiovascular depression. When fentanyl is used with a tranquilizer such as droperidol, hypotension
can occur. If it occurs, the possibility of hypovolemia should also
be considered and managed with appropriate parenteral fluid therapy.
Repositioning the patient to improve venous return to the heart should
be considered when operative conditions permit. Care should be exercised
in moving and positioning of patients because of the possibility of
orthostatic hypotension. If volume expansion with fluids plus other
countermeasures do not correct hypotension, the administration of
pressor agents other than epinephrine should be considered. Because
of the alpha-adrenergic blocking action of droperidol, epinephrine
may paradoxically decrease the blood pressure in patients treated
with droperidol. Elevated blood pressure with
and without pre-existing hypertension has been reported following
administration of fentanyl citrate combined with droperidol. This
might be due to unexplained alterations in sympathetic activity following
large doses; however, it is also frequently attributed to anesthetic
and surgical stimulation during light anesthesia. When droperidol is used with fentanyl and the EEG is used for
postoperative monitoring, it may be found that the EEG pattern returns
to normal slowly. Vital signs should be monitored
routinely. Respiratory depression caused
by opioid analgesics can be reversed by opioid antagonists such as
naloxone. Because the duration of respiratory depression produced
by fentanyl may last longer than the duration of the opioid antagonist
action, appropriate surveillance should be maintained. As with all
potent opioids, profound analgesiais accompanied by respiratory depression
and diminished sensitivity to COstimulation which may
persist into or recur in the postoperative period. Intraoperative
hyperventilation may further alter postoperative response to CO. Appropriate postoperative monitoring should be employed
to ensure that adequate spontaneous breathing is established and maintained
in the absence of stimulation prior to discharging the patient from
the recovery area. Impaired Respiration: Fentanyl should be used with caution
in patients with chronic obstructive pulmonary disease, patients with
decreased respiratory reserve, and others with potentially compromised
respiration. In such patients, narcotics may additionally decrease
respiratory drive and increase airway resistance. During anesthesia,
this can be managed by assisted or controlled respiration. Impaired Hepatic or Renal Function: Fentanyl citrate should be administered with caution to patients
with liver and kidney dysfunction because of the importance of these
organs in the metabolism and excretion of drugs. Cardiovascular Effects: Fentanyl
may produce bradycardia, which may be treated with atropine. Fentanyl
should be used with caution in patients with cardiac bradyarrhythmias.<br/>Drug Interactions:: Other CNS depressant drugs (e.g., barbiturates, tranquilizers,
narcotics, and general anesthetics) will have additive or potentiating
effects with fentanyl. When patients have received such drugs, the
dose of fentanyl required will be less than usual. Following the administration
of fentanyl citrate, the dose of other CNS depressant drugs should
be reduced.<br/>Carcinogenesis, Mutagenesis,
Impairment of Fertility:: No carcinogenicity or mutagenicity studies have been
conducted with fentanyl citrate. Reproduction studies in rats revealed
a significant decrease in the pregnancy rate of all experimental groups.
This decrease was most pronounced in the high dosed group (1.25 mg/kg���12.5X
human dose) in which one of twenty animals became pregnant.<br/>Pregnancy���Category C:: Fentanyl citrate has been shown to impair fertility
and to have an embryocidal effect in rats when given in doses 0.3
times the upper human dose for a period of 12 days. No evidence
of teratogenic effects have been observed after administration of
fentanyl citrate to rats. There are no adequate and well-controlled
studies in pregnant women. Fentanyl should be used during pregnancy
only if the potential benefit justifies the potential risk to the
fetus.<br/>Labor and Delivery:: There are insufficient data to support the use of
fentanyl in labor and delivery. Therefore, such use is not recommended.<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 fentanyl citrate is administered to a nursing
woman.<br/>Pediatric Use:: The safety and efficacy of fentanyl citrate in children
under two years of age has not been established. Rare cases of unexplained clinically significant methemoglobinemia
have been reported in premature neonates undergoing emergency anesthesia
and surgery which included combined use of fentanyl, pancuronium and
atropine. A direct cause and effect relationship between the combined
use of these drugs and the reported cases of methemoglobinemia has
not been established.
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| dailymed-instance:overdosag... |
Manifestations: The manifestations of fentanyl overdosage are an extension of its
pharmacologic actions (see CLINICAL PHARMACOLOGY) as with other opioid
analgesics. The intravenous LDof fentanyl is 3 mg/kg
in rats, 1 mg/kg in cats, 14 mg/kg in dogs and 0.03 mg/kg in monkeys. Treatment: In the
presence of hypoventilation or apnea, oxygen should be administered
and respiration should be assisted or controlled as indicated. A patent
airway must be maintained; an oropharyngeal airway or endotracheal
tube might be indicated. If depressed respiration is associated with
muscular rigidity, an intravenous neuromuscular blocking agent might
be required to facilitate assisted or controlled respiration. The
patient should be carefully observed for 24 hours; body warmth
and adequate fluid intake should be maintained. If hypotension occurs
and is severe or persists, the possibility of hypovolemia should be
considered and managed with appropriate parenteral fluid therapy.
A specific narcotic antagonist such as nalorphine or naloxone should
be available for use as indicated to manage respiratory depression.
This does not preclude the use of more immediate countermeasures.
The duration of respiratory depression following overdosage of fentanyl
may be longer than the duration of narcotic antagonist action. Consult
the package insert of the individual narcotic antagonists for details
about use.
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Fentanyl Citrate
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Fentanyl Citrate (Injection, Solution)
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| dailymed-instance:adverseRe... |
As with other narcotic analgesics, the most common
serious adverse reactions reported to occur with fentanyl are respiratory
depression, apnea, rigidity, and bradycardia; if these remain untreated,
respiratory arrest, circulatory depression or cardiac arrest could
occur. Other adverse reactions that have been reported are hypertension,
hypotension, dizziness, blurred vision, nausea, emesis, laryngospasm,
and diaphoresis. It has been reported that
secondary rebound respiratory depression may occasionally occur postoperatively.
Patients should be monitored for this possibility and appropriate
countermeasures taken as necessary. When
a tranquilizer such as droperidol is used with fentanyl citrate, the
following adverse reactions can occur: chills and/or shivering, restlessness,
and postoperative hallucinatory episodes (sometimes associated with
transient periods of mental depression); extrapyramidal symptoms (dystonia,
akathisia, and oculogyric crisis) have been observed up to 24 hours
postoperatively. When they occur, extrapyramidal symptoms can usually
be controlled with anti-parkinson agents. Postoperative drowsiness
is also frequently reported following the use of droperidol.
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| dailymed-instance:warning |
FENTANYL CITRATE SHOULD BE ADMINISTERED ONLY BY PERSONS
SPECIFICALLY TRAINED IN THE USE OF INTRAVENOUS ANESTHETICS AND MANAGEMENT
OF THE RESPIRATORY EFFECTS OF POTENT OPIOIDS. AN OPIOID ANTAGONIST, RESUSCITATIVE AND INTUBATION EQUIPMENT
AND OXYGEN SHOULD BE READILY AVAILABLE. See
also discussion of narcotic antagonists in PRECAUTIONS and OVERDOSAGE. If fentanyl is administered with a tranquilizer such
as droperidol, the user should become familiar with the special properties
of each drug, particularly the widely differing duration of action.
In addition, when such a combination is used, fluids and other countermeasures
to manage hypotension should be available. As
with other potent narcotics, the respiratory depressant effect of
fentanyl may persist longer than the measured analgesic effect. The
total dose of all narcotic analgesics administered should be considered
by the practitioner before ordering narcotic analgesics during recovery
from anesthesia. It is recommended that narcotics, when required,
should be used in reduced doses initially, as low as 1/4 to 1/3 those
usually recommended. Fentanyl may cause muscle
rigidity, particularly involving the muscles of respiration. In addition,
skeletal muscle movements of various groups in the extremities, neck
and external eye have been reported during induction of anesthesia
with fentanyl; these reported movements have, on rare occasions, been
strong enough to pose patient management problems. This effect is
related to the dose and speed of injection and its incidence can be
reduced by: 1) administration of up to 1/4 of the full paralyzing
dose of a non-depolarizing neuromuscular blocking agent just prior
to administration of fentanyl citrate; 2) administration of a full
paralyzing dose of a neuromuscular blockingagent following loss of
eyelash reflex when fentanyl is used in anesthetic doses titrated
by slow intravenous infusion; or, 3) simultaneous administration of
fentanyl citrate and a full paralyzing dose of a neuromuscular blocking
agent when fentanyl citrate is used in rapidly administered anesthetic
dosages. The neuromuscular blocking agent used should be compatible
with the patient's cardiovascular status. Adequate facilities should be available for postoperative monitoring
and ventilation of patients administered anesthetic doses of fentanyl.
Where moderate or high doses are used (above 10 mcg/kg), there
must be adequate facilities for postoperative observation, and ventilation
if necessary, of patients who have received fentanyl. It is essential
that these facilities be fully equipped to handle all degrees of respiratory
depression. Fentanyl may also produce other
signs and symptoms characteristic of narcotic analgesics including
euphoria, miosis, bradycardia and bronchoconstriction. Severe and unpredictable potentiation by monoamine
oxidase (MAO) inhibitors has been reported for other narcotic analgesics.
Although this has not been reported for fentanyl, there are insufficient
data to establish that this does not occur with fentanyl. Therefore,
when fentanyl is administered to patients who have received MAO inhibitors
within 14 days, appropriate monitoring and ready availability of vasodilators
and beta-blockers for the treatment of hypertension is indicated. Head Injuries and Increased
Intracranial Pressure ���Fentanyl
should be used with caution in patients who may be particularly susceptible
to respiratory depression, such as comatose patients who may have
a head injury or brain tumor. In addition, fentanyl may obscure
the clinical course of patients with head injury.
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| dailymed-instance:indicatio... |
Fentanyl Citrate Injection is indicated: ���for analgesic action of short duration during
the anesthetic periods, premedication, induction and maintenance,
and in the immediate postoperative period (recovery room) as the need
arises. ���for use as a narcotic analgesic
supplement in general or regional anesthesia. ���for administration with a neuroleptic such as droperidol
injection as an anesthetic premedication, for the induction of anesthesia
and as an adjunct in the maintenance of general and regional anesthesia. ���for use as an anesthetic agent with oxygen
in selected high risk patients, such as those undergoing open heartsurgery or certain complicated neurological or orthopedic procedures.
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Fentanyl Citrate
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