Source:http://www4.wiwiss.fu-berlin.de/dailymed/resource/drugs/1752
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Robinul (Injection, Solution)
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ROBINUL
(glycopyrrolate)
Injection
is
a
synthetic
anticholinergic
agent.
Each
1 mL
contains: Glycopyrrolate,
USP
0.2 mg Water
for
Injection,
USP
q.s. Benzyl
Alcohol,
NF
0.9%
(preservative) pH
adjusted,
when
necessary,
with
hydrochloric
acid
and/or
sodium
hydroxide. For
Intramuscular
(IM)
or
Intravenous
(IV)
administration. Glycopyrrolate
is
a
quaternary
ammonium
salt
with
the
following
chemical name:
3[(cyclopentylhydroxyphenylacetyl)oxy]-1,1-dimethyl
pyrrolidinium
bromide.
The
molecular
formula
is
CHBrNOand
the
molecular
weight
is
398.33. Its
structural
formula
is
as
follows: Glycopyrrolate
occurs
as
a
white,
odorless
crystalline powder.
It
is
soluble
in
water
and
alcohol,
and
practically
insoluble
in
chloroform
and
ether. Unlike
atropine,
glycopyrrolate
is
completely
ionized
at
physiological
pH
values.
ROBINUL
(glycopyrrolate)
Injection
is
a
clear,
colorless, sterile
liquid;
pH
2.0���3.0.
The
partition
coefficient
of
glycopyrrolate
in
a
n-octanol/water
system
is
0.304
(logP=
-1.52)
at
ambient
room
temperature
(24��C).
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Known
hypersensitivity
to
glycopyrrolate
or
any
of
its
inactive
ingredients. In
addition,
in
the
management
ofpeptic
ulcer
patients,
because
of
the
longer
duration
of
therapy,
ROBINUL
Injection
may
be
contraindicated
in
patients
with
the
following
concurrent
conditions:
glaucoma;
obstructive
uropathy
(for
example,
bladder neck
obstruction
due
to
prostatic
hypertrophy);
obstructive
disease
of
the
gastrointestinal
tract
(as
in
achalasia,
pyloroduodenal
stenosis,
etc.);
paralytic
ileus,
intestinal
atonyof
the
elderly
or
debilitated
patient;
unstable
cardiovascular
status
in
acute
hemorrhage;
severe
ulcerative
colitis;
toxic
megacolon
complicating
ulcerative
colitis;
myasthenia
gravis.
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General: Investigate
any
tachycardia
before
giving
ROBINUL
Injection
since an
increase
in
the
heart
rate
may
occur. Use
with
caution
in
patients
with:
coronary
artery
disease;
congestive
heart
failure;
cardiac
arrhythmias;
hypertension;
hyperthyroidism. Use
with
caution
in
patients
with renal
disease
since
the
renal
elimination
of
glycopyrrolate
may
be
severely
impaired
in
patients
with
renal
failure.
Dosage
adjustments
may
be
necessary
(seePharmacokinetics���Renal
Impairment). Use ROBINUL
with
caution
in
the
elderly
and
in
all
patients
with
autonomic
neuropathy,
hepatic
disease,
ulcerative
colitis,
prostic
hypertrophy,
or
hiatal
hernia,
since
anticholinergic
drugs
may
aggravate
these
conditions. The
use
of anticholinergetic
drugs
in
the
treatment
of
gastric
ulcer
may
produce
a
delay
in
gastric
emptying
due
to
antral
statis.<br/>Information
for
the
Patient: Because
ROBINUL
Injection
may
produce
drowsiness
or
blurred
vision,
the
patient
should
be
cautioned
not
to
engage
in
activities
requiring
mental
alertness
and/or visual
acuity
such
as
operating
a
motor
vehicle
or
other
machinery,
or
performing
hazardous
work
while
taking
this
drug
. The
patient
also
should
be
cautioned
about the
use
of
this
drug
during
exercise
or
hot
weather
since
overheating
may
result
in
heat
stroke. The
patient
may
experience
a
possible
sensitivity
of
the
eyes
to
light.<br/>Drug
Interactions: The
concurrent
use
of
ROBINUL
Injection
with
other
anticholinergics
or
medications
with
anticholinergic activity,
such
as
phenothiazines,
antiparkinson
drugs,
or
tricyclic
antidepressants,
may
intensify
the
antimuscarinic
effects
and
may
result
in
an
increase
in
anticholinergic
side
effects. Concomitant
administration
of
ROBINUL
Injection
and
potassium
chloride
in
a
wax
matrix
may
increase
the
severity
of
potassium
chloride-induced
gastrointestinal
lesions
as
a
result
of
a
slower
gastrointestinal
transit
time.<br/>Carcinogenesis
and
Mutagenesis
and
Impairment
of
Fertility: Long-term
studies
in
animals
have
not
been
performed
to
evaluate
carcinogenic
potential.
Studies
to
evaluate
the mutagenic
potential
of
glycopyrrolate
have
not
been
conducted.
In
reproduction
studies
in
rats,
dietary
administration
of
glycopyrrolate
resulted
in
diminished
rates
of
conception
in
a
dose-related
manner.
Other
studies
in
dogs
suggest
that
this
may be
due
to
diminished
seminal
secretion
which
is
evident
at
high
doses
of
glycopyrrolate.<br/>Pregnancy:<br/>Teratogenic
Effects���Pregnancy
Category
B.: Reproduction
studies
with
glycopyrrolate
were
performed
in
rats
at a
dietary
dose
of
approximately
65
mg/kg/day
(exposure
was
approximately
320
times
the
maximum
recommended
daily
human
dose
of
2
mg
on
a
mg/mbasis)
and
rabbits
at
intramuscular
doses
of
up
to
0.5
mg/kg/day
(exposure
was approximately
5
times
the
maximum
recommended
daily
human
dose
on
a
mg/mbasis).
These
studies
produced
no
teratogenic
effects
to
the
fetus.Because
animal
reproduction
studies
are
not
always
predictive
of
human
response,
this
drug
should
be used
during
pregnancy
only
if
clearly
needed. Single-dose
studies
in
humans
found
that
very
small
amounts
of
glycopyrrolate
passed
the
placental
barrier.<br/>Nonteratogenic
Effects: Published
literature
suggest
the
following
regarding
the
use
of
glycopyrrolate
during
pregnancy.
Unlike
atropine,
glycopyrrolate
in
normal
doses
(0.004
mg/kg)
does
not
appear
to
affect
fetal
heart
rate
or
fetal
heart
rate
variability
to
a
significant
degree.
Concentrations
of
glycopyrrolate
in
umbilical
venous
and
aterial
blood
and
in
the
amniotic
fluid
are
low
after intramuscular
administration
to
parturients.
Therefore,
glycopyrrolate
does
not
appear
to
penetrate
through
the
placental
barrier
in
significant
amounts.
In
reproduction
studies
in
rats,
dietary
administration
of
glycopyrrolate
resulted
in
diminished
rats
of
pup
survival
in a
dose-related
manner.<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
ROBINUL
Injection
is
administered
to
a
nursing
woman.
As
with
other
anticholinergics,
glycopyrrolate
may cause
suppression
of
lactation
(seeADVERSE
REACTIONS).<br/>Pediatric
Use: Due
to
its
benzyl
alcohol
content,
ROBINUL
Injection
should
not
be
used
in
neonates,
i.e.,
patients
less
than
1
month
of
age. Safety
and
effectiveness
in
pediatric
patients
below
the age
of
16
years
have
not
been
established. Safety
and
effectiveness
in
pediatric
patients
have
not
been
established
for
the
management
of
peptic
ulcer. Dysrhythmias
associated
with
the
use
of glycopyrrolate
intravenously
as
a
premedicant
or
during
anesthesia
have
been
observed
in
pediatric
patients. Infants,
patients
with
Down's
syndrome,
and
pediatric
patients
with
spastic
paralysis
or
brain
damage
may
experience
an
increased response
to
anticholinergics,
thus
increasing
the
potential
for
side
effects. A
paradoxical
reaction
characterized
by
hyperexcitability
may
occur
in
pediatric
patients
taking
large
doses
of
anticholinergics
including
ROBINUL
Injection.
Infants
and
young children
are
especially
susceptible
to
the
toxic
effects
of
anticholinergics. Benzyl
alcohol,
a
component
of
this
drug
product,
has
been
associated
with
serious
adverse
events
and
death,
particularly
in
pediatric
patients.
The���gasping
syndrome,���(characterized
by
central
nervous
system
depression,
metabolic
acidosis,
gasping
respirations,
and
high
levels
of
benzyl
alcohol
and
its
metabolites
found
in
the
blood
and
urine)
has
been
associated
with
benzyl
alcohol
dosages>99 mg/kg/day
in
neonates
and
low-birth-weight
neonates.
Additional
symptoms
may
include
gradual
neurological
deterioration,
seizures,
intracranial
hemorrhage,
hemotologic
abnormalities,
skin
breakdown,
hepatic
and
renal
failure,
hypotension,
bradycardia,
and
cardiovascular
collapse.
Although
normal
therapeutic
doses
of this
product
deliver
amounts
of
benzyl
alcohol
that
are
substantially
lower
than
those
reported
in
association
with
the���gasping
syndrome,���the
minimum
amount
of
benzyl
alcohol
at
which
toxicity
may
occur
is
not
known.
Premature and
low-birthweight
infants,
as
well
as
patients
receiving
high
dosages,
may
be
more
likely
to
develop
toxicity.
Practitioners
administering
this
and
other
medications
containing
benzyl
alcohol
should
consider
the
combined
daily
metabolic
load
of
benzyl
alcohol
from
all
sources.<br/>Geriatric
Use: Clinical
Studies
of
ROBINUL
Injection 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
therapy.
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To
combat
peripheral
anticholinergic
effects,
a
quaternary
ammonium
anticholinesterase
such
as
neostigmine
methylsulfate
(which
does
not
cross
the
blood-brain
barrier)
may
be
given
intravenously
in
increments
of
0.25 mg
in
adults.
This
dosage
may
be repeated
every
five
to
ten
minutes
until
anticholinergic
overactivity
is
reversed
or
up
to
a
maximum
of
2.5 mg.
Proportionately
smaller
doses
should
be
used
in
pediatric
patients.
Indication
for
repetitive
doses
of
neostigmine
should
be based
on
close
monitoring
of
the
decrease
in
heart
rate
and
the
return
of
bowel
sounds. If
CNS
symptoms
(e.g.,
excitement,
restlessness,
convulsions,
psychotic
behavior)
occur,
physostigmine
(which
does
cross
the
blood���brain
barrier)
may
be
used.
Physostigmine
0.5
to
2 mg
should
be
slowly
administered
intravenously
and
repeated
as
necessary
up
to
a
total
of
5 mg
in
adults.
Proportionately
smaller
doses
should
be
used
in
pediatric
patients. To
combat
hypotension,
administer
IV
fluids
and/or
pressor
agents
along
with
supportive
care. Fever
should
be
treated
symptomatically. Following
overdosage,
a
curare-like
action
may
occur,
i.e.,
neuromuscular
blockade leading
to
muscular
weakness
and
possible
paralysis.
In
the
event
of
a
curare-like
effect
on
respiratory
muscles,
artificial
respiration
should
be
instituted
and
maintained
until
effective
respiratory
action
returns.
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glycopyrrolate
|
| dailymed-instance:fullName |
Robinul (Injection, Solution)
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| dailymed-instance:warning |
This drug
should
be
used
with
great
caution,
if
at
all,
in
patients
with
glaucoma. Exposure
to
excessive
amounts
of
benzyl
alcohol
has
been
associated
with
toxicity
(hypotension,
metabolic
acidosis),
particularly
in
neonates, and
an
increased
incidence
of
kernicterus,
particularly
in
small
preterm
infants.
There
have
been
rare
reports
of
deaths,
primarily
in
preterm
infants,
associated
with
exposure
to
excessive
amounts
of
benzyl
alcohol.
The
amount
of
benzyl
alcohol from
medications
is
usually
considered
negligible
compared
to
that
received
in
flush
solutions
containing
benzyl
alcohol.
Administration
of
high
dosages
of
medications
containing
this
preservative
must
take
into
accountthe
total
amount
of
benzyl
alcohol administered.
The
amount
of
benzyl
alcohol
at
which
toxicity
may
occur
is
not
known.
If
the
patient
requires
more
than
the
recommended
dosages
or
other
medications
containing
this
preservative,
the
practitioner
must
consider
the
daily metabolic
load
of
benzyl
alcohol
from
these
combined
sources.
(seePRECAUTIONS,
Pediatric
Use). ROBINUL
Injection
may
produce
drowsiness
or
blurred
vision.
The
patient
should
be
cautioned
regarding
activities requiring
mental
alertness
such
as
operating
a
motor
vehicle
or
other
machinery
or
performing
hazardous
work
while
taking
this
drug. In
addition,
in
the
presence
of
fever,
high
environmental
temperature
and/or
during physical
exercise,
heat
prostration
can
occur
with
use
of
anticholinergic
agents
including
glycopyrrolate
(due
to
decreased
sweating),
particularly
in
children
and
the
elderly. Diarrhea
may
be
an
early
symptom
of
incomplete
intestinal
obstruction,
especially
in
patients
with
ileostomy
or
colostomy.
In
this
instance
treatment
with
ROBINUL
Injection
would
be
inappropriate
and
possibly
harmful.
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Robinul
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