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NEOSTIGMINE METHYLSULFATE 1 mg/mL Injection

by HF Acquisition Co LLC, DBA HealthFirst · 10 POUCH in 1 CASE (51662-1557-3) / 1 CARTON in 1 POUCH (51662-1557-2) / 1 VIAL, MULTI-DOSE in 1 CARTON / 10 mL in 1 VIAL, MULTI-DOSE
NDC 51662-1557-03
🏷️ FDA NDC (as labeled) 51662-1557-3 billing pads the package segment with a zero
Rx only Generic On market Non-controlled
🗂️ Data synced Jul 24, 2026 · sources: openFDA · FDA label (DailyMed) · FDA Orange & Purple Book · First Databank · CMS NADAC, ASP, Medicare & Medicaid · RxNorm
📋 All sources & update times →

This page is curated, coded, and maintained by

Compiled from public FDA, CMS, DailyMed, NADAC, and related drug data sources. Editorial policy

🆔 Identity & classification

FDA NDC (as labeled) 51662-1557-3
Product NDC 51662-1557
11-digit billing NDC 51662155703
RxCUI 311936
UNII 98IMH7M386
Application # ANDA209933
SPL Set ID c4be8467-7b7e-551d-e053-2995a90a3045
Established class (EPC) Cholinesterase Inhibitor
Mechanism of action Cholinesterase Inhibitors
DEA schedule Non-controlled
Marketing category ANDA
Marketing status On market
FDA listing status Listed (active directory)
Marketing start 2021-06-14
Route INTRAVENOUS
Dosage form INJECTION
Substance NEOSTIGMINE METHYLSULFATE
TE code (Orange Book) AP · RLD · RS
Why two NDCs? The FDA registers this code as 51662-1557-3 — a 5-4-1 layout, and that's what's printed on the package and shown on DailyMed. For insurance claims, every NDC is standardized to a uniform 11-digit 5-4-2 format by adding a zero to the package segment → 51662-1557-03. Same drug, same package — only the format differs.
Where does this data come from?
Identifiers from the FDA openFDA NDC Directory and Structured Product Labeling; RxCUI from RxNorm (NLM); GPI from Medi-Span; GCN / HIC / AHFS / legend from First Databank.

🏷️ RxNorm drug class

This medicine belongs to the Cholinesterase Inhibitor class.

Pharmacologic class Cholinesterase Inhibitor
Drug family (ATC) Anticholinesterases, Parasympathomimetics
How it works Cholinesterase Inhibitors
Where does this data come from?
Therapeutic classes from RxNorm RxClass (U.S. National Library of Medicine) — Established Pharmacologic Class (FDA), ATC drug family (WHO) and mechanism of action, matched by this product’s RxCUI.

🏭 Manufacturer & labeler

LabelerHF Acquisition Co LLC, DBA HealthFirst
Application holderAMPHASTAR PHARMACEUTICALS INC
FDA applicationANDA209933 (ANDA)
Labeler code51662
First marketedJun 2021
Product typeHuman Prescription Drug
Portfolio333 products on file
The labeler markets the product; the application holder owns the FDA approval. They’re often the same company but can differ (e.g. a repackager or an authorized generic). A mailing address / phone appears here when the manufacturer includes it in the product’s FDA label (not all do).
Where does this data come from?
Labeler, application holder and registered establishment from the FDA openFDA NDC Directory and Drugs@FDA; address/contact from the product’s FDA label.

🩺 Clinical

📗 Our plain-language guide HelloPharmacist
  • During surgery, you may be given a muscle relaxant to keep your muscles completely still — including your breathing muscles. When the procedure is over, the care team needs those m...
  • What exactly does neostigmine methylsulfate do during or after surgery?
  • Neostigmine is given directly into a vein by the anesthesia team, so you won't feel a needle stick in the usual sense. Some people experience nausea, increased saliva, or a slow or...
  • Yes — it's important to tell your anesthesia team if you have heart disease, irregular heart rhythms, or had a recent heart attack, because neostigmine can affect your heart rate a...
📖 Read our full Neostigmine Methylsulfate guide →
Where does this data come from?
Plain-language summary from MedlinePlus (U.S. National Library of Medicine); supplement & herbal interactions and nutrient depletion data from the Natural Medicines database; our full guide is HelloPharmacist editorial content.

🧪 Inactive Ingredients / Excipients

Inactive ingredients, also called excipients, are components of the drug product other than the active ingredient. They may include fillers, dyes, coatings, preservatives, flavors, or other formulation ingredients.

Loading inactive ingredients from the official FDA label in the background. No external source is being called by this page request.
Where does this data come from?
Source: official FDA Structured Product Labeling (SPL) via DailyMed and the openFDA label index. Structured IACT rows and label-wide narrative are kept separate; availability and product-level specificity depend on the submitted label.

Inactive ingredient FAQ

Are inactive ingredients the same for every manufacturer?
No. Inactive ingredients can differ by manufacturer, dosage form, strength, and package / product version.
Why might an inactive ingredient be missing?
Some SPLs do not provide a complete structured inactive-ingredient list, and older or unusual labels may only include the information in narrative text.
Can inactive ingredients matter?
Yes. They can matter for allergies, intolerances, dyes, gluten / lactose concerns, preservatives, and formulation differences — but confirm with a pharmacist or the manufacturer when it’s clinically important.

💲 Pricing

A drug doesn't have one price. Each row is a different public payment system, and none is what you'd pay at the counter — that depends on your insurance. The ⓘ on each row explains what it measures.

Price systemPer eachPer package
Retail pharmacies payNADAC · weekly Not in the retail survey — common for institutional, discontinued, or low-volume packs.
Medicaid paysCMS SDUD · 12 mo No recent Medicaid claims on file for this NDC — rare and low-volume NDCs are suppressed in the public data.
Medicare drug plans payPart D · quarterly No Part D plan price is available for this NDC in our data.
ℹ️
No price is published for this exact package yet. CMS surveys NADAC per package size, so a different pack of the same drug often has one.
Where does this data come from?
NADAC (National Average Drug Acquisition Cost) is the CMS weekly pharmacy-acquisition-cost survey — what pharmacies pay. ASP (Average Sales Price) is the CMS Medicare Part B drug-payment file, published quarterly. Medicaid pays is computed by us from CMS State Drug Utilization Data (total reimbursed ÷ units, trailing 12 months) — gross of rebates and inclusive of dispensing fees, so it reflects what Medicaid paid, not an acquisition cost. Medicare drug plans pay is the median negotiated point-of-sale unit cost across plans listing this NDC in the CMS quarterly Prescription Drug Plan pricing files, before rebates. The VA pays is the federal contract price (FSS, and the statutory Big 4 ceiling where listed) from the VA National Acquisition Center pharmaceutical price file. All are free public government data; each measures a different payer, so the figures are not directly comparable.

🔁 Therapeutic equivalents

ProductLabelerPackNADAC/unitTEStatusPrice vs. this
Neostigmine Methylsulfate 1 mg/mL 00548-9602-00 Amphastar 1 vial — AP FDA listed —
Neostigmine Methylsulfate 1 mg/mL 00641-6149-10 Hikma 10 vials — AP FDA listed —
Neostigmine Methylsulfate 1 mg/mL 00641-6265-10 Hikma 10 vials — AP FDA listed —
Neostigmine Methylsulfate 1 mg/mL 00641-6277-10 Hikma 10 vials — AP FDA listed —
Neostigmine Methylsulfate 1 mg/mL 14445-0414-01 Indoco 1 vial — AP FDA listed —
Neostigmine Methylsulfate 1 mg/mL 23155-0518-41 Heritage 10 vials — AP FDA listed —
Neostigmine Methylsulfate 1 mg/mL 25021-0611-10 Sagent 10 vials — AP FDA listed —
neostigmine methylsulfate 1 mg/mL 31722-0995-31 Camber 10 vials — AP FDA listed —
Neostigmine Methylsulfate 1 mg/mL 42023-0189-10 Par 10 vials — AP FDA listed —
Neostigmine 1 mg/mL 43598-0529-11 Dr.Reddy's 1 vial — AP FDA listed —
Neostigmine Methylsulfate 1 mg/mLthis 51662-1557-03 HF 10 pouches — AP FDA listed —
Neostigmine Methylsulfate 1 mg/mL 55150-0349-10 Eugia 10 vials — — FDA listed —
Neostigmine Methylsulfate 1 mg/mL 63323-0415-10 Fresenius 10 vials — AP FDA listed —
Neostigmine Methylsulfate 1 mg/mL 65145-0112-10 Caplin 10 vials — AP FDA listed —
Neostigmine Methylsulfate 1 mg/mL 65219-0811-10 Fresenius 10 vials — AP FDA listed —
Neostigmine methylsulfate 1 mg/mL 68083-0384-10 Gland 1 vial — AP FDA listed —
Neostigmine Methylsulfate 1 mg/mL 70069-0806-10 Somerset 10 vials — AP FDA listed —
Neostigmine methylsulfate 1 mg/mL 70121-1479-07 Amneal 10 vials — AP FDA listed —
Neostigmine Methylsulfate 1 mg/mL 70594-0072-02 Xellia 10 vials — AP FDA listed —
Neostigmine methylsulfate 1 mg/mL 70700-0172-22 Xiromed 1 vial — AP FDA listed —
neostigmine methylsulfate 1.02 mg/mL 71288-0501-11 Meitheal 10 vials — AP FDA listed —
Neostigmine methylsulfate 1 mg/mL 71839-0106-10 BE 10 vials — AP FDA listed —
Neostigmine Methylsulfate 1 mg/mL 71872-7016-01 Medical 1 vial — AP FDA listed —
Neostigmine Methylsulfate 1 mg/mL 71872-7143-01 Medical 1 vial — AP FDA listed —
Neostigmine 1 mg/mL 71872-7178-01 Medical 1 vial — AP FDA listed —
Neostigmine Methylsulfate 1 mg/mL 71872-7271-01 Medical 1 vial — AP FDA listed —
Neostigmine Methylsulfate 1 mg/mL 71872-7322-01 Medical 1 vial — AP FDA listed —
Neostigmine Methylsulfate 1 mg/mL 72572-0462-10 Civica, 10 vials — AP FDA listed —
Neostigmine methylsulfate 1 mg/mL 84549-0172-23 ProPharma 10 ml — AP FDA listed —
Bloxiverz 1 mg/mL 51754-1200-03 Exela 10 syringes — — FDA listed —
Neostigmine Methylsulfate 1 mg/mL 76045-0214-30 Fresenius 1 syringe — AP FDA listed —
Neostigmine Methylsulfate 1 mg/mL 43598-0945-58 Dr.Reddys 1 syringe — AP FDA listed —
Neostigmine Methylsulfate 1 mg/mL 76045-0383-30 Fresenius 1 syringe — AP FDA listed —
About this product: this is a generic version of the medicine. FDA equivalence ratings are shown when available, and other versions are listed above, least expensive first.
Where does this data come from?
Equivalents are other NDCs of the same ingredient, form and route from the openFDA NDC Directory, ranked least-expensive-first by NADAC. Therapeutic-equivalence (AB) ratings come from the FDA Orange Book; biologics use the FDA Purple Book for biosimilar & interchangeable status.

⏳ Availability & generic status

🏛️
2021
On the market since
Jun 2021
📍
2026
Currently FDA-listed
5 years listed
🔓
·
Generic on the market
this product is a generic
✅This is a generic drug

This product is an FDA-approved generic. Other versions of the same drug are listed under Therapeutic equivalents, least expensive first.

Where does this data come from?
Patents and exclusivity from the FDA Orange Book (small-molecule drugs), refreshed from public FDA data. Generic launch timing is an estimate, not a guarantee.

🔬 Reported adverse events (FAERS)

Read carefully: FAERS reports are voluntary and unverified. Counts are not incidence, do not establish causation, are subject to reporting bias, and cannot be used to compare one drug to another. Shown for signal context only. Reports for NEOSTIGMINE METHYLSULFATE — the ingredient across all brands.

Top reported reactions

Abdominal Distension26
Hypotension26
Nausea23
Cardiac Arrest21
Respiratory Failure21
Abdominal Pain20
White Blood Cell Count Increased18

Age at onset

Neonate1
Infant3
Child3
Adolescent2
Adult37
Elderly24

Reporter sex

426 reports
Male · 42%
Female · 55%
Unknown · 3%

Serious outcomes

Hospitalization165
Life-threatening102
Death53
Disabling8
Reports over time (by year) — tap or hover for the count & year
2019 2021 2023 2026 32 0
Most recent year is provisional (FAERS lags ~3 months).
Where does this data come from?
Adverse-event reports from the FDA Adverse Event Reporting System (FAERS) via openFDA. FAERS reports are voluntary and unverified — counts are not incidence and don’t establish causation.

📦 Packaging — all sizes for this product

Package NDCDescription Marketing startStatus
51662-1557-03 You're viewing this 10 POUCH in 1 CASE (51662-1557-3) / 1 CARTON in 1 POUCH (51662-1557-2) / 1 VIAL, MULTI-DOSE in 1 CARTON / 10 mL in 1 VIAL, MULTI-DOSE 2021-06-14 Active

🧭 About this NDC listing & data coverage

Finished prescription product
What data is (and isn’t) available for this NDC — tap to expand
NDC identity (package / product / labeler codes) ✓ Available
Labeler ✓ Available
Product & package description ✓ Available
Marketing category & status ✓ Available
Active ingredient / dosage form / route ✓ Available
FDA label (SPL via DailyMed) ✓ Available
Package photos — Not published for this NDC No photo available yet for this listing.
Inactive ingredients (structured) — Not published for this NDC The labeler did not submit a structured excipient list, or no SPL is available.
NADAC pharmacy acquisition price (CMS) — Not published for this NDC CMS publishes NADAC only for NDCs reported in its retail-pharmacy survey.
Orange Book / therapeutic-equivalence data ✓ Available
HCPCS J-code billing crosswalk — Not published for this NDC Most self-administered / retail products have no J-code — that is normal.
Medicaid utilization (CMS SDUD) — Not published for this NDC CMS reports utilization only for NDCs with Medicaid claims above its privacy threshold.
“Not published” reflects what the public FDA / CMS / NLM sources provide for this exact package code — it is a property of the data feeds, not a judgment about the product.

Questions about this listing

Why is there no price listed?
The pricing shown on our NDC pages comes from CMS NADAC, a voluntary survey of retail community pharmacy invoices. CMS does not publish a NADAC for every NDC — packages outside the retail survey (institutional and hospital products, bulk packages, discontinued items, and many OTC items) may never receive one. A missing price reflects the survey's scope, not this product's actual cost, and does not mean the product is free or unavailable.
Is the NDC printed on the package the same as the 11-digit billing NDC?
Yes, they identify this exact package in different formats. The FDA registers it as 51662-1557-3, which is what is printed on the packaging and shown on DailyMed. Insurance claims use a fixed 11-digit 5-4-2 format, so the short segment is padded with a leading zero: 51662-1557-03, written without dashes as 51662155703. The Identity section at the top of this page lists every form of this code.
What do the three segments of this NDC mean?
In 51662-1557-03, the first segment (51662) is the labeler code FDA assigned to HF Acquisition Co LLC, DBA HealthFirst; the middle segment (1557) identifies this specific product — its ingredient, strength, and dosage form; and the last segment (03) identifies this exact package size and type. Together they name one specific package of one specific product.
Is this package still being marketed?
Yes, per the latest FDA NDC Directory data on this page: this package is listed as actively marketed, with no marketing end date reported by HF Acquisition Co LLC, DBA HealthFirst. Listing status can change — the directory data on this page refreshes weekly.
Who lists this product with the FDA?
HF Acquisition Co LLC, DBA HealthFirst is the labeler of record for this NDC — the company under whose FDA-assigned code the package is listed. The labeler may be the manufacturer itself or a distributor marketing the product under its own code.
Do I need a prescription for this product?
This NDC is listed with FDA as a prescription product, so it is dispensed under a prescriber's order. Your pharmacist can tell you whether any over-the-counter forms of the same medication exist.
This page identifies an FDA-listed package (the NDC) and reports public regulatory and pricing data about the listing. It is reference information, not a medical recommendation — talk to your pharmacist or prescriber about your own medication.
Where does this data come from?
Listing facts (marketing category, packager status, marketing dates) from the FDA openFDA NDC Directory; label availability from DailyMed; pricing coverage from CMS NADAC; equivalence scope from the FDA Orange Book.

📄 Full prescribing information FDA SPL

The complete FDA label for this product — the official prescribing information, verbatim, section by section. Jump with a chip, search within the label, or expand everything.
🎯 Indications and Usage ⏱️ Dosage and Administration 💊 Dosage Forms and Strengths ⛔ Contraindications ⚠️ Warnings and Cautions 🤒 Adverse Reactions 🔄 Drug Interactions 👥 Use in Specific Populations 🆘 Overdosage 🧬 Clinical Pharmacology 📦 How Supplied / Storage and Handling 📋 Description
🎯 Indications and Usage 26 words ▾

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.

⏱️ Dosage and Administration ~3 min read ▾

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 adul…

💊 Dosage Forms and Strengths 39 words ▾

3 DOSAGE FORMS & STRENGTHS Neostigmine Methylsulfate Injection, USP, is available as Injection: 0.5 mg/mL, 5 mg of neostigmine methylsulfate in 10 mL multiple- dose vials Injection: 1 mg/mL, 10 mg of neostigmine methylsulfate in 10 mL multiple-dose vials

⛔ Contraindications 49 words ▾

4 CONTRAINDICATIONS Neostigmine Methylsulfate Injection, USP, is contraindicated in patients with: known hypersensitivity to neostigmine methylsulfate (known hypersensitivity reactions have included urticaria, angioedema, erythema multiforme, generalized rash, facial swelling, peripheral edema, pyrexia, flushing, hypotension, bronchospasm, bradycardia and anaphylaxis). with peritonitis or mechanical obstruction of the intestinal or urinary tract.

⚠️ Warnings and Cautions ~1 min read ▾

5 WARNINGS AND PRECAUTIONS 5.1. Bradycardia Neostigmine has been associated with bradycardia. Atropine sulfate or glycopyrrolate should be administered prior to Neostigmine Methylsulfate Injection, USP, to lessen the risk of bradycardia [see DOSAGE AND ADMINISTRATION (2.4)].

5.2. Serious Adverse Reactions in Patients with Certain Coexisting Conditions Neostigmine Methylsulfate Injection, USP, should be used with caution in patients with coronary artery disease, cardiac arrhythmias, recent acute coronary syndrome or myasthenia gravis. Because of the known pharmacology of neostigmine methylsulfate as an acetylcholinesterase inhibitor, cardiovascular effects such as bradycardia, hypotension or dysrhythmia would be anticipated.

In patients with certain cardiovascular conditions such as coronary artery disease, cardiac arrhythmias or recent acute coronary syndrome, the risk of blood pressure and heart rate complications may be increased. Risk of these complications may also be increased in patients with myasthenia gravis. Standard antagonism with anticholinergics (e.g., atropine) is generally successful to mitigate the risk of cardiovascular complications.

5.3. Hypersensitivity Because of the possibility of hypersensitivity, atropine and medications to treat anaphylaxis should be readily available. 5.4.

Neuromuscular Dysfunction Large doses of Neostigmine Methylsulfate Injection, USP, administered when neuromuscular blockade is minimal can produce neuromuscular dysfunction. The dose of Neostigmine Methylsulfate Injection, USP, should be reduced if recovery from neuromuscular blockade is nearly complete. 5.5.

Cholinergic Crisis It is important to differentiate between myasthenic crisis and cholinergic crisis caused by overdosage of Neostigmine Methylsulfate Injection, USP. Both conditions result in extreme muscle weakness but require radically different treatment. [see OVERDOSAGE (10)]

🤒 Adverse Reactions 174 words ▾

6 ADVERSE REACTIONS 6.1. Clinical Trials Experience Because clinical trials are conducted under widely varying conditions, adverse reaction rates observed in the clinical trials of a drug cannot be directly compared to rates in the clinical trials of another drug and may not reflect the rates observed in practice. Adverse reactions to neostigmine methylsulfate are most often attributable to exaggerated pharmacological effects, in particular, at muscarinic receptor sites.

The use of an anticholinergic agent, e.g., atropine sulfate or glycopyrrolate, may prevent or mitigate these reactions. Quantitative adverse event data are available from trials of neostigmine methylsulfate in which 200 adult patients were exposed to the product. The following table lists the adverse reactions that occurred with an overall frequency of 1% or greater.

6.2. Post Marketing Experience The following adverse reactions have been identified during parenteral use of neostigmine methylsulfate. Because these reactions are reported voluntarily from a population of uncertain size, it is not always possible to reliably estimate their frequency or establish a causal relationship to drug exposure.

ADVERSE 1 ADVERSE 2

🔄 Drug Interactions 48 words ▾

7 DRUG INTERACTIONS The pharmacokinetic interaction between neostigmine methylsulfate and other drugs has not been studied. Neostigmine methylsulfate is metabolized by microsomal enzymes in the liver. Use with caution when using Neostigmine Methylsulfate Injection, USP, with other drugs which may alter the activity of metabolizing enzymes or transporters.

👥 Use in Specific Populations ~3 min read ▾

8 USE IN SPECIFIC POPULATIONS 8.1. Pregnancy Risk Summary There are no adequate or well-controlled studies of Neostigmine Methylsulfate Injection, USP, in pregnant women. It is not known whether Neostigmine Methylsulfate Injection, USP, can cause fetal harm when administered to a pregnant woman or can affect reproductive capacity.

The incidence of malformations in human pregnancies has not been established for neostigmine as the data are limited. All pregnancies, regardless of drug exposure, have a background risk of 2 to 4% for major birth defects, and 15 to 20% for pregnancy loss. No adverse effects were noted in rats or rabbits treated with human equivalent doses of neostigmine methylsulfate doses up to 8.1 and 13 mcg/kg/day, respectively, during organogenesis (0.1 to 0.2-times the maximum recommended human dose of 5 mg/60 kg person/day based on body surface area comparisons).

Anticholinesterase drugs, including neostigmine may cause uterine irritability and induce premature labor when administered to pregnant women near term. Neostigmine Methylsulfate Injection, USP, should be given to a pregnant woman only if clearly needed. Data Animal Data In embryofetal development studies, rats and rabbits were administered neostigmine methylsulfate at human equivalent doses (HED, on a mg/m2 basis) of 1.6, 4 and 8.1 mcg/kg/day 3.2, 8.1, and 13 mcg/kg/day, respectively, during the period of organogenesis (Gestation Days 6 through 17 for rats and Gestation Days 6 through 18 for rabbits).

There was no evidence for a teratogenic effect in rats and rabbits up to HED 8.1 and 13 mcg/kg/day, which are approximately 0.097-times and 0.16-times the MRHD of 5 mg/60 kg, respectively in the presence of minimal maternal toxicity (tremors, ataxia, and prostration). The studies resulted in exposures in the animals well below predicted exposures in humans. In a pre- and postnatal development study in rats, neostigmine methylsulfate was administered to pregnant female rats at human equivalent doses (HED) of 1.6, 4 and 8.1 mcg/kg/day from Day 6 of gestation through Day 20 of lactation, with weaning on Day 21.

There were no adverse effects on physical development, behavior, learning ability, or fertility in the offspring occurred at HED doses up 8.1 mcg/kg/day which is 0.097-times the MRHD of 5 mg/60 kg on a mg/m2 basis in the presence of minimal maternal toxicity (tremors, ataxia, and prostration). The studies resulted in exposures in the animals well below predicted exposures in humans. 8.2.

Labor and Delivery The effect of Neostigmine Methylsulfate Injection, USP, on the mother and fetus with regard to labor, delivery, the need for forceps delivery or other intervention or resuscitation of the newborn, is not known. Cholinesterase inhibitor drugs may induce premature labor when given intravenously to pregnant women near term. 8.3.

Nursing Mothers It is not known whether neostigmine methylsulfate is excreted in human milk. Caution should be exercised when Neostigmine Methylsulfate Injection, USP, is administered to a nursing woman. 8.4.

Pediatric Use Neostigmine Methylsulfate Injection, USP, is approved for the reversal of the effects of non-depolarizing neuromuscular blocking agents after surgery in pediatric patients of all ages. Recovery of neuromuscular activity occurs more rapidly with smaller doses of cholinesterase inhibitors in infants and children than in adults. However, infants and small children may be at greater risk of complications from incomplete reversal of neuromuscular blockade due to decreased respiratory reserve.

The risks associated with incomplete reversal outweigh any risk from giving higher doses of Neostigmine Methylsulfate Injection, USP, (up to 0.07 mg/kg or up to a total of 5 mg, whichever is less). The dose of Neostigmine Methylsulfate Injection, USP, required to reverse neuromuscular blockade in children varies between 0.03 mg and 0.07 mg/kg, the same dose range shown to be effective in adults, and should be selected using…

🆘 Overdosage ~1 min read ▾

10 OVERDOSAGE Muscarinic symptoms (nausea, vomiting, diarrhea, sweating, increased bronchial and salivary secretions, and bradycardia) may appear with overdosage of Neostigmine Methylsulfate Injection, USP (cholinergic crisis), but may be managed by the use of additional atropine or glycopyrrolate. The possibility of iatrogenic overdose can be lessened by carefully monitoring the muscle twitch response to peripheral nerve stimulation. Should overdosage occur, ventilation should be supported by artificial means until the adequacy of spontaneous respiration is assured, and cardiac function should be monitored.

Overdosage of Neostigmine Methylsulfate Injection, USP, can cause cholinergic crisis, which is characterized by increasing muscle weakness, and through involvement of the muscles of respiration, may result in death. Myasthenic crisis, due to an increase in the severity of the disease, is also accompanied by extreme muscle weakness and may be difficult to distinguish from cholinergic crisis on a symptomatic basis. However, such differentiation is extremely important because increases in the dose of Neostigmine Methylsulfate Injection, USP, or other drugs in this class, in the presence of cholinergic crisis or of a refractory or “insensitive” state, could have grave consequences.

The two types of crises may be differentiated by the use of edrophonium chloride as well as by clinical judgment. Treatment of the two conditions differs radically. Whereas the presence of myasthenic crisis requires more intensive anticholinesterase therapy, cholinergic crisis calls for the prompt withdrawal of all drugs of this type.

The immediate use of atropine in cholinergic crisis is also recommended. Atropine may also be used to lessen gastrointestinal side effects or other muscarinic reactions; but such use, by masking signs of overdosage, can lead to inadvertent induction of cholinergic crisis.

🧬 Clinical Pharmacology ~1 min read ▾

12 CLINICAL PHARMACOLOGY 12.1. Mechanism of Action Neostigmine methylsulfate is a competitive cholinesterase inhibitor. By reducing the breakdown of acetylcholine, neostigmine methylsulfate induces an increase in acetylcholine in the synaptic cleft which competes for the same binding site as nondepolarizing neuromuscular blocking agents, and reverses the neuromuscular blockade.

12.2. Pharmacodynamics Neostigmine methylsulfate-induced increases in acetylcholine levels results in the potentiation of both muscarinic and nicotinic cholinergic activity. The resulting elevation of acetylcholine competes with nondepolarizing neuromuscular blocking agents to reverse neuromuscular blockade.

Neostigmine methylsulfate does not readily cross the blood-brain barrier and, therefore, does not significantly affect cholinergic function in the central nervous system. 12.3. Pharmacokinetics Distribution: Following intravenous injection, the observed neostigmine methylsulfate volume of distribution is reported between 0.12 and

1.4L/kg. Protein binding of neostigmine methylsulfate to human serum albumin ranges from 15 to 25%. Metabolism: Neostigmine methylsulfate is metabolized by microsomal enzymes in the liver.

Elimination: Following intravenous injection, the reported elimination half-life of neostigmine methylsulfate is between 24 and 113 minutes. Total body clearance of neostigmine methylsulfate is reported between 1.14 and 16.7 mL/min/kg. Renal impairment: Elimination half-life of neostigmine methylsulfate was prolonged in anephric patients compared to normal subjects; elimination half-life for normal, transplant and anephric patients were 79.8 ± 48.6, 104.7 ± 64 and 181 ± 54 min (mean ± SD), respectively.

Hepatic impairment: The pharmacokinetics of neostigmine methylsulfate in patients with hepatic impairment has not been studied. Pediatrics: Elimination half-life of neostigmine methylsulfate in infants (2 to 10 months), children (1 to 6 years) and adults (29 to 48 years) were 39 ± 5 min, 48 ± 16 min, and 67 ± 8 min (mean ± SD), respectively. Observed neostigmine methylsulfate clearance for infants, children and adults were 14 ± 3, 11 ± 3 and 10 ± 2 mL/min/kg (mean ± SD), respectively.

Drug Interaction Studies: The pharmacokinetic interaction between neostigmine methylsulfate and other drugs has not been studied.

📦 How Supplied / Storage and Handling 75 words ▾

16 HOW SUPPLIED Neostigmine Methylsulfate Injection, USP, is available in the following: The vial stopper is not made with natural rubber latex. Neostigmine Methylsulfate Injection, USP, should be stored at 20° to 25°C (68° to 77°F); excursions permitted to 15° to 30°C (59° to 86°F) (see USP Controlled Room Temperature). Protect from light.

Store in carton until time of use. Rx Only Amphastar Pharmaceuticals, Inc. Rancho Cucamonga, CA 91730 USA Rev.

09/17 6996016C HOW SUPPLIED

📋 Description 134 words ▾

11 DESCRIPTION Neostigmine methylsulfate, a cholinesterase inhibitor, is (m-hydroxyphenyl) trimethylammonium methylsulfate dimethylcarbamate. The structural formula is: Neostigmine methylsulfate is a white crystalline powder and is very soluble in water and soluble in alcohol. Neostigmine Methylsulfate Injection, USP, is a sterile, nonpyrogenic solution intended for intravenous use.

Each mL of the 0.5 mg/mL strength contains neostigmine methylsulfate 0.5 mg, phenol 4.5 mg (used as preservative) and sodium acetate trihydrate 0.2 mg, in water for injection. The pH is adjusted, when necessary, with acetic acid/sodium hydroxide to a value of 5.5. Each mL of the 1 mg/mL strength contains neostigmine methylsulfate 1 mg, phenol 4.5 mg (used as preservative), and sodium acetate trihydrate 0.2 mg, in water for injection.

The pH is adjusted, when necessary, with acetic acid/sodium hydroxide to achieve a value of 5.5. DESCRIPTION

Source: FDA Structured Product Labeling, mirrored from DailyMed / openFDA. Prefer the government’s original formatting? View this label on DailyMed ↗
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