NEOSTIGMINE METHYLSULFATE

NEOSTIGMINE METHYLSULFATE- neostigmine methylsulfate injection
HF Acquisition Co LLC, DBA HealthFirst

HIGHLIGHTS OF PRESCRIBING INFORMATION


These highlights do not include all the information needed to use NEOSTIGMINE METHYLSULFATE INJECTION, USP, safely and effectively. See full prescribing information for NEOSTIGMINE METHYLSULFATE INJECTION, USP.
NEOSTIGMINE METHYLSULFATE injection,
for intravenous use
Initial U.S. Approval: 1939

INDICATIONS AND USAGE

Neostigmine Methylsulfate Injection, USP, a cholinesterase inhibitor, is indicated for the reversal of the effects of non-depolarizing neuromuscular blocking agents (NMBAs) after surgery. ( 1 )

DOSAGE AND ADMINISTRATION

Should be administered by trained healthcare providers ( 2.1)
Peripheral nerve stimulator and monitoring for twitch responses should be used to determine when Neostigmine Methylsulfate Injection, USP, should be initiated and if additional doses are needed ( 2.2)


For reversal of NMBAs with shorter half-lives, when first twitch response is substantially greater than 10% of baseline, or when a second twitch is present: 0.03 mg/kg by intravenous route ( 2.2)

For reversal of NMBAs with longer half-lives or when first twitch response is close to 10% of baseline: 0.07 mg/kg by intravenous route ( 2.2)

Maximum total dosage is 0.07 mg/kg or up to a total of 5 mg (whichever is less) ( 2.2)
An anticholinergic agent, e.g., atropine sulfate or glycopyrrolate, should be administered prior to or concomitantly with Neostigmine Methylsulfate Injection, USP ( 2.4)

DOSAGE FORMS AND STRENGTHS

Injection: 0.5 mg/mL and 1 mg/mL in 10 mL multiple-dose vials ( 3)

CONTRAINDICATIONS

Hypersensitivity to neostigmine ( 4)
Peritonitis or mechanical obstruction of the intestinal or urinary tract ( 4)

WARNINGS AND PRECAUTIONS

Bradycardia: Atropine or glycopyrrolate should be administered prior to Neostigmine Methylsulfate Injection, USP, to lessen risk of bradycardia. ( 5.1)
Serious Reactions with Coexisting Conditions: Use with caution in patients with, coronary artery disease, cardiac arrhythmias, recent acute coronary syndrome or myasthenia gravis. ( 5.2)
Neuromuscular Dysfunction: Can occur if large doses of Neostigmine Methylsulfate Injection, USP, are administered when neuromuscular blockade is minimal; reduce dose if recovery from neuromuscular blockade is nearly complete. ( 5.4)

ADVERSE REACTIONS

Most common adverse reactions during treatment: bradycardia, nausea and vomiting. ( 6)

To report SUSPECTED ADVERSE REACTIONS, contact Amphastar Pharmaceuticals, Inc., at 1-800-423-4136 or FDA at 1-800-FDA-1088 or WWW.FDA.GOV/MEDWATCH.

USE IN SPECIFIC POPULATIONS

Pregnancy: No human data and limited animal data exist. Use only if clearly needed.

Revised: 12/2017

TABLE OF CONTENTS

FULL PRESCRIBING INFORMATION: CONTENTS*
1 INDICATIONS & USAGE
2 DOSAGE & ADMINISTRATION
2.1. Important Dosage Information
2.2. Dosage in Adults
2.3. Dosage in Pediatric Patients, including Neonates
2.4. Anticholinergic (Atropine or Glycopyrrolate) Administration
3 DOSAGE FORMS & STRENGTHS
4 CONTRAINDICATIONS
5WARNINGS AND PRECAUTIONS
5.1. Bradycardia
5.2. Serious Adverse Reactions in Patients with Certain Coexisting Conditions
5.3. Hypersensitivity
5.4. Neuromuscular Dysfunction
5.5. Cholinergic Crisis
6 ADVERSE REACTIONS
6.1. Clinical Trials Experience
6.2. Post Marketing Experience
7 DRUG INTERACTIONS
8 USE IN SPECIFIC POPULATIONS
8.1. Pregnancy
8.2. Labor and Delivery
8.3. Nursing Mothers
8.4. Pediatric Use
8.5. Geriatric Use
8.6. Renal Impairment
8.7. Hepatic Impairment
10 OVERDOSAGE
11 DESCRIPTION
12 CLINICAL PHARMACOLOGY
12.1. Mechanism of Action
12.2. Pharmacodynamics
12.3. Pharmacokinetics
13 NONCLINICAL TOXICOLOGY
13.1. Carcinogenesis, Mutagenesis, Impairment of Fertility
14 CLINICAL STUDIES
16 HOW SUPPLIED

*
Sections or subsections omitted from the full prescribing information are not listed.

1 INDICATIONS & USAGE

Neostigmine Methylsulfate Injection, USP, is a cholinesterase inhibitor indicated for the reversal of the effects of nondepolarizing neuromuscular blocking agents after surgery.

2 DOSAGE & ADMINISTRATION SECTION

2.1. Important Dosage Information

Neostigmine Methylsulfate Injection, USP, should be administered by trained healthcare providers familiar with the use, actions, characteristics, and complications of neuromuscular blocking agents (NMBA) and neuromuscular block reversal agents. Doses of Neostigmine Methylsulfate Injection, USP, should be individualized, and a peripheral nerve stimulator should be used to determine the time of initiation of Neostigmine Methylsulfate Injection, USP, and should be used to determine the need for additional doses.

Neostigmine Methylsulfate Injection, USP, is for intravenous use only and should be injected slowly over a period of at least 1 minute. The Neostigmine Methylsulfate Injection, USP, dosage is weight-based [see DOSAGE AND ADMINISTRATION (2.2)].

Prior to Neostigmine Methylsulfate Injection, USP, administration and until complete recovery of normal ventilation, the patient should be well ventilated and a patent airway maintained. Satisfactory recovery should be judged by adequacy of skeletal muscle tone and respiratory measurements in addition to the response to peripheral nerve stimulation.

An anticholinergic agent, e.g., atropine sulfate or glycopyrrolate, should be administered prior to or concomitantly with Neostigmine Methylsulfate Injection, USP [see DOSAGE AND ADMINISTRATION (2.4)].

2.2. Dosage in Adults

a. Peripheral nerve stimulation devices capable of delivering a train-of-four (TOF) stimulus are essential to effectively using Neostigmine Methylsulfate Injection, USP.

b. There must be a twitch response to the first stimulus in the TOF of at least 10% of its baseline level, i.e., the response prior to NMBA administration, prior to the administration of Neostigmine Methylsulfate Injection, USP.

c. Prior to administration, visually inspect Neostigmine Methylsulfate Injection, USP, for particulate matter and discoloration.

d. Neostigmine Methylsulfate Injection, USP, should be injected slowly by intravenous route over a period of at least 1 minute.

e. A 0.03 mg/kg to 0.07 mg/kg dose of Neostigmine Methylsulfate Injection, USP, will generally achieve a TOF twitch ratio of 90% (TOF0.9) within 10 to 20 minutes of administration. Dose selection should be based on the extent of spontaneous recovery that has occurred at the time of administration, the half-life of the NMBA being reversed, and whether there is a need to rapidly reverse the NMBA.

The 0.03 mg/kg dose is recommended for:

i. Reversal of NMBAs with shorter half-lives, e.g., rocuronium, or

ii. When the first twitch response to the TOF stimulus is substantially greater than 10% of baseline or when a second twitch is present.

The 0.07 mg/kg dose is recommended for:

iii. NMBAs with longer half-lives, e.g., vecuronium and pancuronium, or

iv. When the first twitch response is relatively weak, i.e., not substantially greater than 10% of baseline or

v. There is need for more rapid recovery.

f. TOF monitoring should continue to be used to evaluate the extent of recovery of neuromuscular function and the possible need for an additional dose of Neostigmine Methylsulfate Injection, USP.

g. TOF monitoring alone should not be relied upon to determine the adequacy of reversal of neuromuscular blockade as related to a patient’s ability to adequately ventilate and maintain a patent airway following tracheal extubation.

h. Patients should continue to be monitored for adequacy of reversal from NMBAs for a period of time that would assure full recovery based on the patient’s medical condition and the pharmacokinetics of neostigmine and the NMBA used.

i. The recommended maximum total dose is 0.07 mg/kg or up to a total of 5 mg, whichever is less.

2.3. Dosage in Pediatric Patients, including Neonates

Adult guidelines should be followed when Neostigmine Methylsulfate Injection, USP, is administered to pediatric patients. Pediatric patients require Neostigmine Methylsulfate Injection, USP, doses similar to those for adult patients.

2.4. Anticholinergic (Atropine or Glycopyrrolate) Administration

An anticholinergic agent, e.g., atropine sulfate or glycopyrrolate, should be administered prior to or concomitantly with Neostigmine Methylsulfate Injection, USP. The anticholinergic agent should be administered intravenously using a separate syringe. In the presence of bradycardia, it is recommended that the anticholinergic agent be administered prior to Neostigmine Methylsulfate Injection, USP.

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