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Nexium i.v.

NEXIUM® I.V.
(esomeprazole sodium)

for Injection
Rx only

DESCRIPTION
The active ingredient in NEXIUM® I.V. (esomeprazole sodium) for Injection is (S)-5-methoxy-2[[(4-methoxy-3,5-dimethyl-2-pyridinyl)-methyl]sulfinyl]-1 H-benzimidazole sodium a compound that inhibits gastric acid secretion. Esomeprazole is the S-isomer of omeprazole, which is a mixture of the S- and R- isomers. Its empirical formula is C17H18N3O3SNa with molecular weight of 367.4 g/mol (sodium salt) and 345.4 g/mol (parent compound). Esomeprazole sodium is very soluble in water and freely soluble in ethanol (95%). The structural formula is: NEXIUM I.V. for Injection is supplied as a sterile, freeze-dried, white to off-white, porous cake or powder in a 5 mL vial, intended for intravenous administration after reconstitution with 0.9% Sodium Chloride Injection, USP; Lactated Ringer’s Injection, USP or 5% Dextrose Injection, USP. NEXIUM I.V. for Injection contains esomeprazole sodium 21.3 mg or 42.5 mg equivalent to esomeprazole 20 mg or 40 mg, edetate disodium 1.5 mg and sodium hydroxide q.s. for pH adjustment. The pH of reconstituted solution of NEXIUM I.V. for Injection depends on the reconstitution volume and is in the pH range of 9 to 11. The stability of esomeprazole sodium in aqueous solution is strongly pH dependent. The rate of degradation increases with decreasing pH. CLINICAL PHARMACOLOGY
Pharmacokinetics
Absorption
The pharmacokinetic profile of NEXIUM I.V. for Injection
20 mg and 40 mg was determined in 24 healthy volunteers
for the 20 mg dose and 38 healthy volunteers for the 40 mg
dose following once daily administration of 20 mg and 40
mg of NEXIUM I.V. for Injection by constant rate over 30
minutes for five days. The results are shown in the
following table:
Pharmacokinetic Parameters of NEXIUM Following
I.V. Dosing for 5 days
Values represent the geometric mean (95% CI) Distribution Esomeprazole is 97% bound to plasma proteins. Plasma protein binding is constant over the concentration range of 2-20 µmol/L. The apparent volume of distribution at steady state in healthy volunteers is approximately 16 L. Metabolism Esomeprazole is extensively metabolized in the liver by the cytochrome P450 (CYP) enzyme system. The metabolites of esomeprazole lack antisecretory activity. The major part of esomeprazole’s metabolism is dependent upon the CYP2C19 isoenzyme, which forms the hydroxy and desmethyl metabolites. The remaining amount is dependent on CYP3A4 which forms the sulphone metabolite. CYP2C19 isoenzyme exhibits polymorphism in the metabolism of esomeprazole, since some 3% of Caucasians and 15-20% of Asians lack CYP2C19 and are termed Poor Metabolizers. At steady state, the ratio of AUC in Poor Metabolizers to AUC in the rest of the population (Extensive metabolizers) is approximately 2. Following administration of equimolar doses, the S- and R-
isomers are metabolized differently by the liver, resulting in
higher plasma levels of the S- than of the R-isomer.
Excretion
Esomeprazole is excreted as metabolites primarily in urine
but also in feces. Less than 1% of parent drug is excreted in
the urine. Esomeprazole is completely eliminated from
plasma and there is no accumulation during once daily
administration. The plasma elimination half-life of
intravenous esomeprazole is approximately 1.1 to 1.4 hours
and is prolonged with increasing dose of intravenous
esomeprazole.
Special Populations
Investigation of age, gender, race, renal, and hepatic
impairment and metabolizer status have been made
previously with oral esomeprazole. The pharmacokinetics
of esomeprazole is not expected to be affected differently
by intrinsic or extrinsic factors after intravenous
administration compared to oral administration. The same
recommendations for dose adjustment in special
populations are suggested for intravenous esomeprazole as
for oral esomeprazole.
Geriatric
In oral studies, the AUC and Cmax values were slightly
higher (25% and 18%, respectively) in the elderly as
compared to younger subjects at steady state. Dosage
adjustment based on age is not necessary.
Pediatric
The pharmacokinetics of esomeprazole have not been
studied in patients < 18 years of age.
Gender
In oral studies, the AUC and Cmax values were slightly
higher (13%) in females than in males at steady state.
Similar differences have been seen for intravenous
administration of esomeprazole. Dosage adjustment based
on gender is not necessary.
Hepatic Insufficiency
In oral studies, the steady state pharmacokinetics of
esomeprazole obtained after administration of 40 mg once
daily to 4 patients each with mild (Child Pugh A), moderate
(Child Pugh Class B), and severe (Child Pugh Class C)
liver insufficiency were compared to those obtained in 36
male and female GERD patients with normal liver function.
In patients with mild and moderate hepatic insufficiency,
the AUCs were within the range that could be expected in
patients with normal liver function. In patients with severe
hepatic insufficiency the AUCs were 2 to 3 times higher
than in the patients with normal liver function. No dosage
adjustment is recommended for patients with mild to
moderate hepatic insufficiency (Child Pugh Classes A and
B). However, in patients with severe hepatic insufficiency
(Child Pugh Class C) a dose of 20 mg once daily should not
be exceeded (See DOSAGE AND ADMINISTRATION).
Renal Insufficiency
The pharmacokinetics of esomeprazole in patients with
renal impairment are not expected to be altered relative to
healthy volunteers as less than 1% of esomeprazole is
excreted unchanged in urine.
Pharmacodynamics
Mechanism of Action
Esomeprazole is a proton pump inhibitor that suppresses
gastric acid secretion by specific inhibition of the H+/K+-
ATPase in the gastric parietal cell. The S- and R-isomers of
omeprazole are protonated and converted in the acidic
compartment of the parietal cell forming the active
inhibitor, the achiral sulphenamide. By acting specifically
on the proton pump, esomeprazole blocks the final step in
acid production, thus reducing gastric acidity. This effect is
dose-related up to a daily dose of 20 to 40 mg and leads to
inhibition of gastric acid secretion.
Antisecretory Activity
The effect of intravenous esomeprazole on intragastric pH
was determined in two separate studies. In the first study,
20 mg of NEXIUM I.V. for Injection was administered
intravenously once daily at constant rate over 30 minutes
for 5 days. Twenty-two healthy subjects were included in
the study. In the second study, 40 mg of NEXIUM I.V. for
Injection was administered intravenously once daily at
constant rate over 30 minutes for 5 days. Thirty-eight healthy subjects were included in the study. Effect of NEXIUM I.V. for Injection on Intragastric pH on
Gastric pH was measured over a 24-hour period
Serum Gastrin Effects
In oral studies, the effect of NEXIUM on serum gastrin
concentrations was evaluated in approximately 2,700
patients in clinical trials up to 8 weeks and in over 1,300
patients for up to 6-12 months. The mean fasting gastrin
level increased in a dose-related manner. This increase
reached a plateau within two to three months of therapy and
returned to baseline levels within four weeks after
discontinuation of therapy.
Enterochromaffin-like (ECL) Cell Effects
There are no data available on the effects of intravenous
esomeprazole on ECL cells.
In 24-month carcinogenicity studies of oral omeprazole in
rats, a dose-related significant occurrence of gastric ECL
cell carcinoid tumors and ECL cell hyperplasia was
observed in both male and female animals (see
PRECAUTIONS, Carcinogenesis, Mutagenesis,
Impairment of Fertility
). Carcinoid tumors have also
been observed in rats subjected to fundectomy or long-term
treatment with other proton pump inhibitors or high doses
of H2-receptor antagonists.
Human gastric biopsy specimens have been obtained from more than 3,000 patients treated orally with omeprazole in long-term clinical trials. The incidence of ECL cell hyperplasia in these studies increased with time; however, no case of ECL cell carcinoids, dysplasia, or neoplasia has been found in these patients. In over 1,000 patients treated with NEXIUM (10, 20 or
40 mg/day) up to 6-12 months, the prevalence of ECL cell
hyperplasia increased with time and dose. No patient
developed ECL cell carcinoids, dysplasia, or neoplasia in
the gastric mucosa.
Endocrine Effects
NEXIUM had no effect on thyroid function when given in
oral doses of 20 or 40 mg for 4 weeks. Other effects of
NEXIUM on the endocrine system were assessed using
omeprazole studies. Omeprazole given in oral doses of 30
or 40 mg for 2 to 4 weeks had no effect on carbohydrate
metabolism, circulating levels of parathyroid hormone,
cortisol, estradiol, testosterone, prolactin, cholecystokinin
or secretin.
Clinical Studies
Acid Suppression in Gastroesophageal Reflux
Disease (GERD)
Four multicenter, open-label, two-period crossover studies
were conducted to compare the pharmacodynamic efficacy
of the intravenous formulation of esomeprazole (20 mg and
40 mg) to that of NEXIUM delayed-release capsules at
corresponding doses in patients with symptoms of GERD,
with or without erosive esophagitis. The patients (n=206,
18 to 72 years old; 112 female; 110 Caucasian, 50 Black,
10 Oriental, and 36 Other Race) were randomized to
receive either 20 or 40
esomeprazole once daily for 10 days (Period 1), and then were switched in Period 2 to the other formulation for 10 days, matching their respective dose level from Period 1. The intravenous formulation was administered as a 3-minute injection in two of the studies, and as a 15-minute infusion in the other two studies. Basal acid output (BAO) and maximal acid output (MAO) were determined 22-24 hours post-dose on Period 1, Day 11; on Period 2, Day 3; and on Period 2, Day 11. BAO and MAO were estimated from 1-hour continuous collections of gastric contents prior to and following (respectively) subcutaneous injection of 6.0 µg/kg of pentagastrin. In these studies, after 10 days of once daily administration, the intravenous dosage forms of NEXIUM 20 mg and 40 mg were similar to the corresponding oral dosage forms in their ability to suppress BAO and MAO in these GERD patients (see table below). There were no major changes in acid suppression when switching between intravenous and oral dosage forms. Mean (SD) BAO and MAO measured 22-24 hours post-dose
following once daily oral and intravenous administration of
esomeprazole for 10 days in GERD patients with or without a
history of erosive esophagitis
Intravenous
BAO in mmol H+/h
MAO in mmol H+/h
Administration
Intravenous Oral Intravenous Oral

INDICATIONS AND USAGE
NEXIUM I.V. for Injection is indicated for the short-term
treatment (up to 10 days) of GERD patients with a history
of erosive esophagitis as an alternative to oral therapy in
patients when therapy with NEXIUM Delayed-Release
Capsules is not possible or appropriate.
When oral therapy is possible or appropriate, intravenous
therapy with NEXIUM I.V. for Injection should be
discontinued and the therapy should be continued orally.
CONTRAINDICATIONS
NEXIUM is contraindicated in patients with known hypersensitivity to any component of the formulation or to substituted benzimidazoles. PRECAUTIONS
General
Symptomatic response to therapy with NEXIUM does not
preclude the presence of gastric malignancy.
Atrophic gastritis has been noted occasionally in gastric
corpus biopsies from patients treated long-term with
omeprazole, of which NEXIUM is an enantiomer.
Treatment with NEXIUM I.V. for Injection should be
discontinued as soon as the patient is able to resume
treatment with NEXIUM Delayed-Release Capsules.
Drug Interactions
Esomeprazole is extensively metabolized in the liver by
CYP2C19 and CYP3A4.
In vitro and in vivo studies have shown that esomeprazole is
not likely to inhibit CYPs 1A2, 2A6, 2C9, 2D6, 2E1 and
3A4. No clinically relevant interactions with drugs
metabolized by these CYP enzymes would be expected.
Drug interaction studies have shown that esomeprazole
does not have any clinically significant interactions with
phenytoin, warfarin, quinidine, clarithromycin or
amoxicillin. Post-marketing reports of changes in
prothrombin measures have been received among patients
on concomitant warfarin and esomeprazole therapy.
Increases in INR and prothrombin time may lead to
abnormal bleeding and even death. Patients treated with
proton pump inhibitors and warfarin concomitantly may
need to be monitored for increases in INR and prothrombin
time.
Esomeprazole may potentially interfere with CYP2C19, the
major esomeprazole metabolizing enzyme.
Coadministration of esomeprazole 30 mg and diazepam, a CYP2C19 substrate, resulted in a 45% decrease in clearance of diazepam. Increased plasma levels of diazepam were observed 12 hours after dosing and onwards. However, at that time, the plasma levels of diazepam were below the therapeutic interval, and thus this interaction is unlikely to be of clinical relevance. Coadministration of oral contraceptives, diazepam,
phenytoin, or quinidine did not seem to change the
pharmacokinetic profile of esomeprazole.
Concomitant administration of esomeprazole may reduce
the plasma levels of atazanavir.
Studies evaluating concomitant administration of
esomeprazole and either naproxen (non-selective NSAID)
or rofecoxib (COX-2 selective NSAID) did not identify any
clinically relevant changes in the pharmacokinetic profiles
of esomeprazole or these NSAIDs.
Esomeprazole inhibits gastric acid secretion. Therefore,
esomeprazole may interfere with the absorption of drugs
where gastric pH is an important determinant of
bioavailability (eg, ketoconazole, iron salts and digoxin).

Carcinogenesis, Mutagenesis,
Impairment of Fertility
The carcinogenic potential of esomeprazole was assessed
using omeprazole studies. In two 24-month oral
carcinogenicity studies in rats, omeprazole at daily doses of
1.7, 3.4, 13.8, 44.0 and 140.8 mg/kg/day (about 0.7 to 57
times the human dose of 20 mg/day expressed on a body
surface area basis) produced gastric ECL cell carcinoids in
a dose-related manner in both male and female rats; the
incidence of this effect was markedly higher in female rats,
which had higher blood levels of omeprazole. Gastric
carcinoids seldom occur in the untreated rat. In addition,
ECL cell hyperplasia was present in all treated groups of
both sexes. In one of these studies, female rats were treated
with 13.8 mg omeprazole/kg/day (about 5.6 times the
human dose on a body surface area basis) for 1 year, then
followed for an additional year without the drug. No
carcinoids were seen in these rats. An increased incidence
of treatment-related ECL cell hyperplasia was observed at
the end of 1 year (94% treated vs 10% controls). By the
second year the difference between treated and control rats
was much smaller (46% vs 26%) but still showed more
hyperplasia in the treated group. Gastric adenocarcinoma
was seen in one rat (2%). No similar tumor was seen in
male or female rats treated for 2 years. For this strain of rat
no similar tumor has been noted historically, but a finding
involving only one tumor is difficult to interpret. A
78-week oral mouse carcinogenicity study of omeprazole did not show increased tumor occurrence, but the study was not conclusive. Esomeprazole was negative in the Ames mutation test, in the in vivo rat bone marrow cell chromosome aberration test, and the in vivo mouse micronucleus test. Esomeprazole, however, was positive in the in vitro human
lymphocyte chromosome aberration test. Omeprazole was
positive in the in vitro human lymphocyte chromosome
aberration test, the in vivo mouse bone marrow cell
chromosome aberration test, and the in vivo mouse
micronucleus test.
The potential effects of esomeprazole on fertility and
reproductive performance were assessed using omeprazole
studies. Omeprazole at oral doses up to 138 mg/kg/day in
rats (about 56 times the human dose on a body surface area
basis) was found to have no effect on reproductive
performance of parental animals.
Pregnancy
Teratogenic Effects. Pregnancy Category B
Teratology studies have been performed in rats at oral
doses up to 280 mg/kg/day (about 57 times the human dose
on a body surface area basis) and in rabbits at oral doses up
to 86 mg/kg/day (about 35 times the human dose on a body
surface area basis) and have revealed no evidence of
impaired fertility or harm to the fetus due to esomeprazole.
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.
Teratology studies conducted with omeprazole in rats at
oral doses up to 138 mg/kg/day (about 56 times the human
dose on a body surface area basis) and in rabbits at doses up
to 69 mg/kg/day (about 56 times the human dose on a body
surface area basis) did not disclose any evidence for a
teratogenic potential of omeprazole. In rabbits, omeprazole
in a dose range of 6.9 to 69.1 mg/kg/day (about 5.5 to 56
times the human dose on a body surface area basis)
produced dose-related increases in embryo-lethality, fetal
resorptions, and pregnancy disruptions. In rats, dose-
related embryo/fetal toxicity and postnatal developmental
toxicity were observed in offspring resulting from parents
treated with omeprazole at 13.8 to 138.0 mg/kg/day (about
5.6 to 56 times the human doses on a body surface area
basis). There are no adequate and well-controlled studies in
pregnant women. Sporadic reports have been received of
congenital abnormalities occurring in infants born to
women who have received omeprazole during pregnancy.
Nursing Mothers
The excretion of esomeprazole in milk has not been
studied. However, omeprazole concentrations have been
measured in breast milk of a woman following oral
administration of 20 mg. Because esomeprazole is likely to
be excreted in human milk, because of the potential for
serious adverse reactions in nursing infants from
esomeprazole, and because of the potential for
tumorigenicity shown for omeprazole in rat carcinogenicity
studies, a decision should be made whether to discontinue
nursing or to discontinue the drug, taking into account the
importance of the drug to the mother.
Pediatric Use
Safety and effectiveness in pediatric patients have not been
established.
Geriatric Use
Of the total number of patients who received oral NEXIUM
in clinical trials, 1,459 were 65 to 74 years of age and 354
patients were ≥ 75 years of age.

No overall differences in safety and efficacy were observed
between the elderly and younger individuals, and other
reported clinical experience has not identified differences in
responses between the elderly and younger patients, but
greater sensitivity of some older individuals cannot be ruled
out.
ADVERSE REACTIONS
Safety Experience with Intravenous NEXIUM
The safety of intravenous esomeprazole is based on results
from clinical trials conducted in three different populations
including patients having symptomatic GERD with or
without a history of erosive esophagitis (n=206), patients
with erosive esophagitis (n=246) and healthy subjects
(n=204). Adverse experiences occurring in >1% of patients
treated with intravenous esomeprazole (n=359) in trials
irrespective of the relationship to NEXIUM are listed below
by body system:
Skin and appendages disorders: pruritus (1.1%); Central
and peripheral nervous system disorders:
dizziness
(2.5%), headache (10.9%); Gastrointestinal system
disorders:
abdominal pain (5.8%), constipation (2.5%),
diarrhea (3.9%), dyspepsia (6.4%), flatulence (10.3%),
mouth dry (3.9%), nausea (6.4%); Respiratory system
disorders:
respiratory infection (1.1%), sinusitis (1.7%);
Body as a whole – general disorders:
AE associated with
test procedure (23.1%); and Application site disorders:
application site reaction (1.7%) (including mild focal
erythema and pruritus at IV insertion site).
Intravenous treatment with esomeprazole 20 and 40 mg
administered as an injection or as an infusion was found to
have a safety profile similar to that of oral administration of
esomeprazole 20 and 40 mg.
Safety Experience with Oral NEXIUM
The safety of oral NEXIUM was evaluated in over 15,000
patients (aged 18-84 years) in clinical trials worldwide
including over 8,500 patients in the United States and over
6,500 patients in Europe and Canada. Over 2,900 patients
were treated in long-term studies for up to 6-12 months.
The safety in the treatment of healing of erosive esophagitis
was assessed in four randomized comparative clinical trials,
which included 1,240 patients on NEXIUM 20 mg, 2,434
patients on NEXIUM 40 mg, and 3,008 patients on
omeprazole 20 mg daily. The most frequently occurring
adverse events (≥1%) in all three groups was headache (5.5,
5.0, and 3.8, respectively) and diarrhea (no difference
among the three groups). Nausea, flatulence, abdominal
pain, constipation, and dry mouth occurred at similar rates
among patients taking NEXIUM or omeprazole.
Additional adverse events that were reported as possibly or
probably related to NEXIUM with an incidence < 1% are
listed below by body system:

Body as a Whole
: abdomen enlarged, allergic reaction,
asthenia, back pain, chest pain, chest pain substernal, facial
edema, peripheral edema, hot flushes, fatigue, fever, flu-
like disorder, generalized edema, leg edema, malaise, pain,
rigors;
Cardiovascular: flushing, hypertension,
tachycardia; Endocrine: goiter; Gastrointestinal: bowel
irregularity, constipation aggravated, dyspepsia, dysphagia,
dysplasia GI, epigastric pain, eructation, esophageal
disorder, frequent stools, gastroenteritis, GI hemorrhage, GI
symptoms not otherwise specified, hiccup, melena, mouth
disorder, pharynx disorder, rectal disorder, serum gastrin
increased, tongue disorder, tongue edema, ulcerative
stomatitis, vomiting; Hearing:
Hematologic: anemia, anemia hypochromic, cervical
lymphoadenopathy, epistaxis, leukocytosis, leukopenia,
thrombocytopenia; Hepatic: bilirubinemia, hepatic function
abnormal, SGOT increased, SGPT increased;
Metabolic/Nutritional:
hyponatremia, increased alkaline phosphatase, thirst,
vitamin B12 deficiency, weight increase, weight decrease;
Musculoskeletal: arthralgia, arthritis aggravated,
arthropathy, cramps, fibromyalgia syndrome, hernia,
polymyalgia rheumatica; Nervous System/Psychiatric:
anorexia, apathy, appetite increased, confusion, depression
aggravated, dizziness, hypertonia, nervousness,
hypoesthesia, impotence, insomnia, migraine, migraine
aggravated, paresthesia, sleep disorder, somnolence,
tremor, vertigo, visual field defect; Reproductive:
dysmenorrhea, menstrual disorder, vaginitis; Respiratory:
asthma aggravated, coughing, dyspnea, larynx edema,
pharyngitis, rhinitis, sinusitis; Skin and Appendages: acne,
angioedema, dermatitis, pruritus, pruritus ani, rash, rash
erythematous, rash maculo-papular, skin inflammation,
sweating increased, urticaria; Special Senses: otitis media,
parosmia, taste loss, taste perversion; Urogenital: abnormal
urine, albuminuria, cystitis, dysuria, fungal infection,
hematuria, micturition frequency, moniliasis, genital
moniliasis, polyuria; Visual: conjunctivitis, vision
abnormal.
Endoscopic findings that were reported as adverse events
include: duodenitis, esophagitis, esophageal stricture,
esophageal ulceration, esophageal varices, gastric ulcer,
gastritis, hernia, benign polyps or nodules, Barrett’s
esophagus, and mucosal discoloration.
The incidence of treatment-related adverse events during 6-
month maintenance treatment was similar to placebo. There
were no differences in types of related adverse events seen
during maintenance treatment up to 12 months compared to
short-term treatment.
Two placebo-controlled studies were conducted in 710
patients for the treatment of symptomatic gastroesophageal
reflux disease. The most common adverse events that were
reported as possibly or probably related to NEXIUM were
diarrhea (4.3%), headache (3.8%), and abdominal pain
(3.8%).
Postmarketing Reports - There have been spontaneous
reports of adverse events with postmarketing use of
esomeprazole. These reports occurred rarely and are listed
below by body system:
Blood And Lymphatic System Disorders: agranulocytosis,
pancytopenia;
Eye Disorders: blurred vision;
Gastrointestinal Disorders: pancreatitis; Hepatobiliary
Disorders:
hepatitis with or without jaundice; Immune
System Disorders:
anaphylactic reaction/shock;
Musculoskeletal And Connective Tissue Disorders:
myalgia; Psychiatric Disorders: depression; Skin and
Subcutaneous Tissue Disorders:
alopecia, erythema
multiforme, Stevens-Johnson syndrome, toxic epidermal
necrolysis (TEN, some fatal).
Other adverse events not observed with NEXIUM, but
occurring with omeprazole can be found in the omeprazole
package insert, ADVERSE REACTIONS section.
Laboratory Events
The following potentially clinically significant laboratory
changes in clinical trials, irrespective of relationship to
NEXIUM, were reported in ≤ 1% of patients: increased
creatinine, uric acid, total bilirubin, alkaline phosphatase,
ALT, AST, hemoglobin, white blood cell count, platelets,
serum gastrin, potassium, sodium, thyroxine and thyroid
stimulating hormone (see CLINICAL
PHARMACOLOGY
, Endocrine Effects for further
information on thyroid effects). Decreases were seen in
hemoglobin, white blood cell count, platelets, potassium,
sodium, and thyroxine.

OVERDOSAGE

The minimum lethal dose of esomeprazole sodium in rats
after bolus administration was 310 mg/kg (about 62 times
the human dose on a body surface area basis). The major
signs of acute toxicity were reduced motor activity, changes
in respiratory frequency, tremor, ataxia and intermittent
clonic convulsions.
There have been some reports of overdosage with oral
esomeprazole. Reports have been received of overdosage
with oral omeprazole in humans. Doses ranged up to 2,400
mg (120 times the usual recommended clinical dose).
Manifestations were variable, but included confusion,
drowsiness, blurred vision, tachycardia, nausea,
diaphoresis, flushing, headache, dry mouth, and other
adverse reactions similar to those seen in normal clinical
experience (see omeprazole package insert - ADVERSE
REACTIONS
). No specific antidote for esomeprazole is
known. Since esomeprazole is extensively protein bound, it
is not expected to be removed by dialysis. In the event of
overdosage, treatment should be symptomatic and
supportive.
As with the management of any overdose, the possibility of
multiple drug ingestion should be considered. For current
information on treatment of any drug overdose, a certified
Regional Poison Control Center should be contacted.
Telephone numbers are listed in the Physicians’ Desk
Reference (PDR) or local telephone book.
DOSAGE AND ADMINISTRATION
GERD with a history of Erosive Esophagitis The recommended adult dose is either 20 or 40 mg esomeprazole given once daily by intravenous injection (no less than 3 minutes) or intravenous infusion (10 to 30
minutes).
NEXIUM I.V. for Injection should not be administered
concomitantly with any other medications through the same
intravenous site and or tubing. The intravenous line should
always be flushed with either 0.9% Sodium Chloride
Injection, USP, Lactated Ringer’s Injection, USP or 5%
Dextrose Injection, USP both prior to and after
administration of NEXIUM I.V. for Injection.
Treatment with NEXIUM I.V. for Injection should be
discontinued as soon as the patient is able to resume
treatment with NEXIUM Delayed-Release Capsules.
Safety and efficacy of NEXIUM I.V. for Injection as a
treatment of GERD patients with a history of erosive
esophagitis for more than 10 days have not been
demonstrated (see INDICATIONS AND USAGE).
Special Populations
Geriatric: No dosage adjustment is necessary. (See
CLINICAL PHARMACOLOGY, Pharmacokinetics.)
Renal Insufficiency: No dosage adjustment is necessary.
(See
CLINICAL PHARMACOLOGY,
Pharmacokinetics.)
Hepatic Insufficiency: No dosage adjustment is necessary
in patients with mild to moderate liver impairment (Child
Pugh Classes A and B). For patients with severe liver
impairment (Child Pugh Class C), a dose of 20 mg of
NEXIUM should not be exceeded (See CLINICAL
PHARMACOLOGY, Pharmacokinetics.)
Gender: No dosage adjustment is necessary. (See
CLINICAL PHARMACOLOGY, Pharmacokinetics.)
Preparations for use:
Intravenous Injection (20 or 40 mg) over no less than 3
minutes

The freeze-dried powder should be reconstituted with 5 mL of 0.9% Sodium Chloride Injection, USP. Withdraw 5 mL of the reconstituted solution and administer as an intravenous injection over no less than 3 minutes. The reconstituted solution should be stored at room temperature up to 30°C (86°F) and administered within 12 hours after reconstitution. No refrigeration is required. Intravenous Infusion (20 or 40 mg) over 10 to 30 minutes A solution for intravenous infusion is prepared by first reconstituting the contents of one vial with 5 mL of 0.9% Sodium Chloride Injection, USP, Lactated Ringer’s Injection, USP or 5% Dextrose Injection, USP and further diluting the resulting solution to a final volume of 50 mL. The solution (admixture) should be administered as an intravenous infusion over a period of 10 to 30 minutes. The admixture should be stored at room temperature up to 30°C (86°F) and should be administered within the designated time period as listed in the Table below. No refrigeration is required. Diluent Administer
NEXIUM I.V. for Injection should not be administered
concomitantly with any other medications through the same
intravenous site and or tubing. The intravenous line should
always be flushed with either 0.9% Sodium Chloride
Injection, USP, Lactated Ringer’s Injection, USP or 5%
Dextrose Injection, USP both prior to and after
administration of NEXIUM I.V. for Injection.
Parenteral drug products should be inspected visually for
particulate matter and discoloration prior to administration,
whenever solution and container permit.
HOW SUPPLIED
NEXIUM I.V. for Injection is supplied as a freeze-dried powder containing 20 mg or 40 mg of esomeprazole per single-use vial. NDC 0186-6020-01 one carton containing 10 vials of
NEXIUM I.V. for Injection (each vial contains 20 mg of
esomeprazole).
NDC 0186-6040-01 one carton containing 10 vials of
NEXIUM I.V. for Injection (each vial contains 40 mg of
esomeprazole).

Storage
Store at 25°C (77°F); excursions permitted to 15°-30°C
(59°-86°F). [See USP Controlled Room Temperature].
Protect from light. Store in carton until time of use.
NEXIUM is a registered trademark of the AstraZeneca
group of companies
AstraZeneca 2005
AstraZeneca LP
Wilmington, DE 19850

Source: http://www.luminstudio.com/susanoppelt/susanoppelt/sample_launch/NEX/_pdf/nexium_iv.pdf

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