Source:http://www4.wiwiss.fu-berlin.de/dailymed/resource/drugs/3268
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Enlon-Plus (Injection)
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Dosages of
ENLON-PLUS (edrophonium chloride, USP and atropine sulfate, USP)
Injection range from 0.05-0.1 mL/kg given slowly over 45 seconds to 1
minute at a point of at least 5% recovery of twitch response to
neuromuscular stimulation (95% block). The dosage delivered is 0.5-1.0
mg/kg of edrophonium chloride and 0.007-0.014 mg/kg of atropine sulfate.
A total dosage of 1.0 mg/kg of edrophonium chloride should rarely be
exceeded. Response should be monitored carefully and assisted or
controlled ventilation secured. Satisfactory reversal permits adequate
voluntary respiration and neuromuscular transmission (as tested with a
peripheralnerve stimulator). Recurarization has not been reported after
satisfactory reversal has been attained. Parenteral drug
products should be inspected visually for particulate matter and
discoloration prior to administration.
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dailymed-instance:descripti... |
ENLON-PLUS
(edrophonium chloride, USP and atropine sulfate, USP) Injection, for
intravenous use, is a sterile, nonpyrogenic, nondepolarizing
neuromuscular relaxant antagonist. ENLON-PLUS is a combination drug
containing a rapid acting acetylcholinesterase inhibitor, edrophonium
chloride, and an anticholinergic, atropine sulfate. Chemically,
edrophonium chloride is ethyl (m-hydroxyphenyl) dimethylammonium
chloride; its structural formula is: Molecular Formula:
CHClNO Molecular Weight:
201.70 Chemically,
atropine sulfate is:
endo-(��)-alpha-(hydroxymethyl)-8-methyl-8-azabicyclo [3.2.1]oct-3-yl
benzeneacetate sulfate (2:1) monohydrate. Its structural formula is: Molecular Formula:
(CHNO)��HSO��HO Molecular Weight:
694.84 ENLON-PLUS contains
in each mL of sterile solution: 5 mL Ampuls: 10 mg edrophonium chloride
and 0.14 mg atropine sulfate compounded with 2.0 mg sodium sulfite as a
preservative and buffered with sodium citrate and citric acid. The pH
range is 4.0-5.0. 15 mL Multidose Vials: 10 mg edrophonium
chloride and 0.14 mg atropine sulfate compounded with 2.0 mg sodium
sulfite and 4.5 mg phenol as a preservative and buffered with sodium
citrate and citric acid. The pH range is 4.0-5.0.
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Pharmacodynamics: ENLON-PLUS
(edrophonium chloride, USP and atropine sulfate, USP) Injection
is a combination of an anticholinesterase agent, which
antagonizes the action of nondepolarizing neuromuscular blocking
drugs, and a parasympatholytic (anticholinergic) drug, which
prevents the muscarinic effects caused by inhibition of
acetylcholine breakdown by the anticholinesterase. Edrophonium chloride antagonizes the effect of nondepolarizing neuromuscular
blocking agents primarily by inhibiting or inactivating
acetylcholinesterase. By inactivating the acetylcholinesterase
enzyme, acetylcholine is not hydrolyzed as rapidly by
acetylcholinesterase and is thereby allowed to accumulate. The
greater quantity of acetylcholine reaching the sites of
nicotinic cholinergic postjunctional receptors improves
transmission of impulses across the myoneural junction. The
concomitant, unavoidable accumulation of acetylcholine at the
sites of muscarinic cholinergic transmission occurring at the
parasympathetic, postganglionic receptors of the autonomic
nervous system, may cause bradycardia, bronchoconstriction,
increased secretions, and other parasympathomimetic side
effects. The magnitude of these muscarinic side effects can beexpected to vary from patient to patient depending upon the amount of vagal nerve activity present. Atropine sulfate
counteracts these side effects. Intravenous
edrophonium chloride in doses of 0.5 to 1.0 mg/kg promptly
antagonizes the effects of nondepolarizing muscle relaxants
reaching the maximum antagonism within 1.2 minutes. A plateau of
maximal antagonism is sustained for 70 minutes1. Intravenous
atropine sulfate has an immediate effect on heart rate which
reaches a peak in 2 to 16 minutes and lasts 170 minutes after an
average 0.02 mg/kg dose.<br/>Pharmacokinetics:<br/>Edrophonium
Chloride: Edrophonium chloride given intravenously shows first
order elimination in a two compartment open
pharmacokinetic model3. Onset of reversal of muscle
relaxant induced depression in twitch tension occurs
within three minutes. Edrophonium is primarily renally
excreted with 67% of the dose appearing in the urine4.
Hepatic metabolism and biliary excretion have also been
demonstrated in animals4,8. While infants and children
have been shown to have a reduced plasma half-life and
an increased clearance of edrophonium, doses in children
are not significantly different from adults on a mg/kg
basis although they are more variable in effect.
Conversely, elderly subjects (>75 years old) have
a prolonged plasma half-life and a reduced clearance.
Studies have shown that in spite of these changes the
onset and duration of action is unchanged in these
patients.<br/>Atropine
Sulfate: Atropine sulfate given intravenously shows first order
elimination in a two compartment open model.
Approximately 57% of a dose of atropine appears in the
urine as unchanged drug. Tropine is the primary hepatic
metabolite of atropine and it accounts for approximately
30% of the dose. Atropine is only 14��9%
bound to plasma proteins. Atropine clearance in children under 2 years old and in the elderly is decreased in relation to normal healthy adults. T1/2��= Elimination half-life VD
= Volume of distribution Cl
= Clearance
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ENLON-PLUS
(edrophonium chloride, USP and atropine sulfate, USP) Injection is not
to be used in patients with known hypersensitivity to either of the
components, or in patients with intestinal or urinary obstruction of
mechanical type. Atropine sulfate is contraindicated in the presence of
acute glaucoma, adhesions (synechiae) between the iris and lens of the
eye, and pyloric stenosis.
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dailymed-instance:supply |
ENLON-PLUS
(edrophonium chloride, USP and atropine sulfate, USP) Injection should
be stored between 15��-26��C (59��-78��F). NDC 10019-180-05 5
mL ampuls, boxes of 10 NDC 10019-195-15 15
mL multidose vials
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General: As with any
antagonist of nondepolarizing muscle relaxants, adequate
recovery of voluntary respiration and neuromuscular transmission
must be obtained prior to the discontinuation of respiratory
assistance. Should a patient develop���anticholinesterase
insensitivity���for brief or prolonged periods, the patient
should be carefully monitored and the dosage of
anticholinesterase drugs reduced or withheld until the patient again becomes sensitive to them. Use with caution in patients
with prostatic hypertrophy and in debilitated patients with
chronic lung disease. When used
in therapeutic doses, atropine can cause dryness of the mouth.
This effect is additive when the product is administered with
other drugs that can cause dryness of the mouth. Since
atropine sulfate slows gastric emptying and gastrointestinal
motility, it may interfere with the absorption of other
medications. The effect of atropine on dryness of the mouth may
be increased if it is given with other drugs that have
anticholinergic action (tricyclic antidepressants,
antipsychotics, some antihistamines, and antiparkinsonism
drugs).<br/>Drug Interactions: ENLON-PLUS
(edrophonium chloride, USP and atropine sulfate, USP) Injection should not be administered prior to the administration of any
nondepolarizing muscle relaxants. It should be administered with
caution to patients with symptoms of myasthenic weakness who are
also on anticholinesterase drugs. Anticholinesterase overdosage
(cholinergic crisis) symptoms may mimic underdosage (myasthenic
weakness), so the use of this drug may worsen the condition of
these patients (see OVERDOSAGE section for treatment). Narcotic
analgesics, except when combined with potent inhaled
anesthetics, appear to potentiate the effect of edrophonium on
the sinus node and conduction system, increasing both the
frequency and duration of bradycardia. In patients with
cardiovascular disease, given anesthesia with narcotic and
nitrous oxide without a potent inhalational agent, there is increased risk for clinically significant bradycardia. In
patients receiving beta-adrenergic blocking agents there is
increased risk for excessive bradycardia from unopposed
parasympathetic vagal tone. Such patients should receive
atropine sulfate alone prior to ENLON-PLUS. Compared to
muscle relaxants with some vagolytic activity, muscle relaxants
with no vagolytic effects, i.e. vecuronium, may be associated with a slightly higher incidence of vagotonic effects such as
bradycardia and first-degree heart block when reversed with
ENLON-PLUS.<br/>Pregnancy Category
C: Animal
reproduction studies have not been conducted with ENLON-PLUS. It
is also not known whether ENLON-PLUS can cause fetal harm when
administered to a pregnant woman or can affect reproduction
capacity. ENLON-PLUS should be used during pregnancy only if the potential benefit justifies the potential risk to the
fetus.<br/>Labor and Delivery: The effect
of ENLON-PLUS on the mother and fetus, on the duration of labor
or delivery, in the possibility that a forceps delivery or other
intervention or resuscitation of the newborn will be necessary,
is not known. The effect of the combination drug on the later
growth, development and functional maturation of the child is
also unknown.<br/>Nursing Mothers: The safety
of ENLON-PLUS during lactation in humans has not been
established.<br/>Pediatric Use: Safety and
effectiveness in pediatric patients have not been established.
Pediatric patients may have increased vagal tone. The effect of
fixed ratios of edrophonium and atropine on heart rate in such
patients has not been evaluated.<br/>Geriatric Use: Clinical
studies of ENLON-PLUS 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... |
Muscarinic symptoms
(nausea, vomiting, diarrhea, sweating, increased bronchial and salivary
secretions and bradycardia) may appear with overdosage (cholinergic
crisis) of ENLON-PLUS (edrophonium chloride, USP and atropine sulfate,
USP) Injection, but may be managed by the use of additional atropine
sulfate. Obstruction of the airway by bronchial secretions can arise and
may be managed with suction (especially if tracheostomy has been
performed). Should edrophonium
chloride overdosage occur: Appropriate
measures should be taken if convulsions occur or shock is present. Principal
manifestations of overdosage (poisoning) with atropine sulfate are
delirium, tachycardia and fever. In the treatment of atropine poisoning,
respiratory assistance and symptomatic support are indicated. Death is
usually due to paralysis of the medullary centers. In the clinical
studies performed with ENLON-PLUS, there were no reported overdoses and
therefore no clinical information is available regarding overdosing with
ENLON-PLUS.
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edrophonium chloride and atropine sulfate
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Enlon-Plus (Injection)
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dailymed-instance:adverseRe... |
Cardiovascular: Arrhythmias Frequency>10%: junctional rhythm, bradycardia,
tachycardia; Frequency 3-10%: first and second degree A-V block,
P Wave changes, atrial premature contractions; Frequency 1-3%:
third degree A-V block, ventricular premature contractions;
Frequency less than 1%: 3 second R-R interval. Of the
patients who experienced any arrhythmias, 85% had the onset
within two minutes, 74% no longer had any arrhythmias after 10
minutes. Arrhythmias related to increased vagal tone,
bradycardia, second and third degree heart block respond to
treatment with 0.2-0.4 mg of atropine I.V. (Bigeminy or
ventricular ectopy may be treated with lidocaine 50 mg I.V.). Adverse
experiences reported for anticholinesterase agents such as
edrophonium chloride, but not observed in the 235 patients
studied with ENLON-PLUS (edrophonium chloride, USP and atropine
sulfate, USP) Injection:<br/>Cardiovascular: Nonspecific
EKG changes, fall in cardiac output leading to
hypotension;<br/>Respiratory: Increased
tracheobronchial secretions, laryngospasm, bronchiolar
constriction and respiratory muscle paralysis;<br/>Neurologic: Convulsions, dysarthria, dysphonia, and dysphagia;<br/>Gastrointestinal: Nausea,
vomiting, increased peristalsis, increased gastric and
intestinal secretions, diarrhea, abdominal cramps;<br/>Musculoskeletal: Weakness
and fasciculations;<br/>Miscellaneous: Increased
urinary frequency, diaphoresis, increased lacrimation, pupillary
constriction, diplopia, and conjunctival hyperemia. Untoward
reactions to atropine sulfate generally are dose-related.
Individual tolerance varies greatly but systemic doses of 0.5 to
10 mg are likely to produce the following effects, which were
not observed in the 235 patients treated with
ENLON-PLUS:<br/>Neurologic: Speech disturbances and restlessness with
asthenia;<br/>Dermatologic: Flushed, dry skin, formation of a scarlatiniform
rash;<br/>Miscellaneous: Dryness of the nose and mouth, thirst, blurred vision,
photophobia, slight mydriasis. Atropine may produce
fever through inhibition of heat loss by
evaporation.
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dailymed-instance:warning |
ENLON-PLUS
(edrophonium chloride, USP and atropine sulfate, USP) Injection should
be used with caution in patients with bronchial asthma or cardiac
arrhythmias. Cardiac arrest has been reported to occur in digitalized
patients as well as in jaundiced subjects receiving cholinesterase
inhibitors. In patients with cardiovascular disease, given anesthesia
with narcotic and nitrous oxide without a potent inhalational agent,
there is increased risk for clinically significant bradycardia. In
patients receiving beta-adrenergic blocking agents there is increased
risk for excessive bradycardia from unopposed parasympathetic vagal
tone. Such patients should receive atropine sulfate alone prior to
ENLON-PLUS. Isolated instances of respiratory arrest have also been
reported following the administration of edrophonium chloride.
Additional atropine sulfate (1 mg) should be available for immediate use
to counteract severe cholinergic reaction which may occur in
hypersensitive individuals when ENLON-PLUS is used. ENLON-PLUS contains
sodium sulfite, 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. There is a
potential for tissue irritation by extravascular injection.
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ENLON-PLUS
(edrophonium chloride, USP and atropine sulfate, USP) Injection is
recommended as a reversal agent or antagonist of nondepolarizing neuromuscular blocking agents. It is not effective against depolarizing
neuromuscular blocking agents. It is also useful if used adjunctively in
the treatment of respiratory depression caused by curare overdosage. The appropriateness
of the specific fixed ratio of edrophonium and atropine contained in
ENLON-PLUS has not been evaluated in myasthenia gravis. Therefore,
ENLON-PLUS is not recommended for use in the differential diagnosis of
this condition.
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Enlon-Plus
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