Home › NDC Lookup › Ingredients › Bupivacaine Hydrochloride › 70069-0753-01
Bupivacaine hydrochloride 5 mg/mL Injection, Solution — NDC 70069-0753-01 package photo
Label image from the product's FDA listing (DailyMed) — may show a different pack size or an older label revision.

Bupivacaine hydrochloride 5 mg/mL Injection, Solution — NDC 70069-753-01 (Billing 70069-0753-01)

by Somerset Therapeutics, LLC · 1 VIAL in 1 CARTON / 50 mL in 1 VIAL

This is a package of Bupivacaine hydrochloride 5 mg/mL Injection, Solution from Somerset Therapeutics, LLC, marketed since Nov 2023 and currently FDA-listed; retail pharmacies pay about $0.0860 per mL (NADAC). It is the main listing for this product, which comes in 3 package sizes.

NDC 70069-0753-01
🏷️ FDA NDC (as labeled) 70069-753-01 billing pads the product segment with a zero
This package
Contains50 mL in 1 vial Cost per mL$0.0860 NADAC Per package$4.30 / 50 ml Pack sizes3 compare ↓
Also priced by: Medicaid pays $0.2760/unit — full pricing hub ↓
Main listing for product 70069-753 · Also comes in: 10 vials 70069-753-10 25 vials 70069-753-25
Rx only Generic On market Non-controlled ⚠ On shortage ⇄ Compare with another NDC
🗂️ FDA directory synced Oct 1, 2026 · this listing last changed 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

⚠️
Active FDA shortage. Bupivacaine Hydrochloride Injection is currently reported in shortage by the FDA. Available Shortage details →
⚠️
Other active recalls for Bupivacaine Hydrochloride (different manufacturers) — 1 · tap to view
These affect other manufacturers’ products for the same ingredient — not necessarily the exact NDC on this page.
Class II · Apr 2, 2026 — Lack of Assurance of Sterility (Huons Co., Ltd.) · FDA recall D-0530-2026
Each entry is an official FDA enforcement report — look up any recall number in the FDA recall database ↗

Identity & classification

Regulatory identifiers FDA, NLM and CMS codes for this package

FDA NDC (as labeled) 70069-753-01
Product NDC 70069-753
11-digit billing NDC 70069075301
NCPDP billing unit ML — per mL (volume)
RxCUI 1012396, 1012404
UNII 7TQO7W3VT8
UPC 0370069753019, 0370069752012
Application # ANDA217792
SPL Set ID bcaab86f-20f0-4482-8d73-e29b36dced58
Established class (EPC) Amide Local Anesthetic
Physiologic effect Local Anesthesia
Chemical class Amides
DEA schedule Non-controlled
Marketing category ANDA
Marketing status On market
FDA listing status Listed (active directory)
Marketing start 2023-11-27
Route INFILTRATION, PERINEURAL
Dosage form INJECTION, SOLUTION
Substance BUPIVACAINE HYDROCHLORIDE
TE code (Orange Book) AP · RLD · RS

Drug-database identifiers Medi-Span GPI and First Databank GCN / HICL / AHFS classification

GPI-14 69100010102010
GCN Seq No 003359
GCN 11701
HICL code 001470
Ingredient (HICL) Bupivacaine Hcl
HIC1 code H
Therapeutic class — broad (HIC1) Nervous System (Except Autonomic)
HIC2 code H0
Therapeutic class — intermediate (HIC2) Act On Non-Autonomic Nervous System
HIC3 code H0A
Therapeutic class — specific (HIC3) Local Anesthetics
AHFS code 72:00.00.00
AHFS class Local Anesthetics
FDB label name BUPIVACAINE 0.5% VIAL
FDB brand name Bupivacaine Hcl
Legend status F — Federal legend — prescription drug or device
Quick answers
  • GSN (GCN sequence number): 003359
  • GCN: 11701
  • GPI-14 (Medi-Span): 69100010102010
  • HICL (First Databank): 001470
  • AHFS class code: 72:00.00.00
  • RxCUI (RxNorm): 1012396
Why two NDCs? The FDA registers this code as 70069-753-01 — a 5-3-2 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 product segment → 70069-0753-01. 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 Amide Local Anesthetic class.

Pharmacologic class Amide Local Anesthetic
Drug family (ATC) Amides
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.

Clinical

Label name BUPIVACAINE 0.5% VIAL Ingredient Bupivacaine Hcl
📖 What it is MedlinePlus · NLM

Bupivacaine is used to manage pain during surgery or medical procedures. Bupivacaine is in a class of medications called local anesthetics. It works by blocking nerves from sending pain signals.

Read the full MedlinePlus article ↗
📗 Our plain-language guide HelloPharmacist
  • Bupivacaine is a local anesthetic — it numbs a specific area of your body so you don't feel pain during a procedure. Your doctor or anesthesiologist injects it near the nerves that...
  • What exactly is bupivacaine and why is my doctor using it?
  • The most common ones are nausea, vomiting, constipation, dizziness, and headache. You might also notice your heart beating a little faster or your blood pressure dropping temporari...
  • What side effects should I expect after getting bupivacaine?
📖 Read our full Bupivacaine guide →

Supplement & herbal interactions

🌿 Drug–supplement interaction checker →
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.

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 mLPer package
Retail pharmacies payNADAC · weekly $0.086 $4.30 / 50 ml
Medicaid paysCMS SDUD · 12 mo $0.2760 $13.80 / 50 ml
Medicare drug plans payPart D · quarterly No Part D plan price is available for this NDC in our data.
Medicare Part B allowsASP · J0665 $0.011 / J0665 unit —
NADAC price history (per mL) — tap or hover for the price & month
Dec 2025 Jan 2026 Feb 2026 Apr 2026 $0.086 $0.079
▲ Up 10% over the last 5 months.
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.

Billing & reimbursement

FDA NDC (as labeled)70069-753-01
11-digit billing NDC70069-0753-01
Format5-3-2 as registered → padded to 5-4-2 for billing (zero added to the product segment)
HCPCS J-codeJ0665
DescriptorINJECTION, BUPIVACAINE, NOT OTHERWISE SPECIFIED, 0.5 MG
Billing units / pkg10 units
How the units are derivedThis package is 50 ML; the HCPCS unit is 0.5 MG, so one package = 10 billing units.
Medicare Part B spend (2026 (Q1))$8,142 · 24,071 claims · $0.34 per claim (all NDCs under J0665)
Crosswalk sourcePDAC NDC-HCPCS crosswalk (DME MAC / DMEPOS)
Where does this data come from?
The HCPCS J-code crosswalk comes from the CMS ASP NDC-HCPCS crosswalk and the DMEPDAC (DME MAC) NDC-HCPCS crosswalk — free public CMS data. Billing units are derived from the code’s descriptor and the package amount.

Packaging — all sizes for this product

Package NDCDescription Per unit Per pack Marketing startMarketing endStatus
70069-0753-25 70069-753-25 25 VIAL in 1 CARTON / 50 mL in 1 VIAL — — 2023-11-27 — Active
70069-0753-01 You're viewing this Main listing 1 VIAL in 1 CARTON / 50 mL in 1 VIAL $0.0860 / mL $4.30 2024-05-29 — Active
70069-0753-10 70069-753-10 10 VIAL in 1 CARTON / 50 mL in 1 VIAL — — 2024-05-30 — Active

In Medicaid, this is the most-dispensed pack of this product — about 82% of fills over the last four reported quarters. See all packs ↓

Pack size FAQ

What quantity is in this package?
This package is listed by the FDA — 1 vial in 1 carton / 50 ml in 1 vial.
What NDC number is used to bill for this package of Bupivacaine hydrochloride 5 mg/mL Injection, Solution?
Use the 11-digit billing form listed in the identifiers section of this page. Pharmacy and medical claims use the 11-digit form; the FDA label may print a shorter form of the same code.

Prices are the latest CMS NADAC pharmacy acquisition cost per NDC; per-pack figures are per-unit × pack quantity, shown only when the pack is denominated in the same measure NADAC prices.

Therapeutic equivalents

ProductLabelerPackNADAC/unitTEStatusPrice vs. this
Bupivacaine hydrochloride 5 mg/mLthis 70069-0753-01 Somerset 1 vial $0.086 AP Availability likely —
Bupivacaine HCl 5 mg/mL 70594-0119-01 Xellia 50 ml $0.086 AP Availability likely —
bupivacaine hydrochloride 5 mg/mL 71288-0726-52 Meitheal 1 vial $0.086 — Availability likely —
Bupivacaine Hydrochloride 5 mg/mL 00143-9329-10 Hikma 10 vials — AP FDA listed —
Bupivacaine Hydrochloride 5 mg/mL 00404-9827-50 Henry 1 vial — AP FDA listed —
Sensorcaine 5 mg/mL 00404-9947-50 Henry 1 vial — AP FDA listed —
Marcaine 250 mg/50mL 00409-0525-25 Hospira, 25 vials — AP FDA listed —
Bupivacaine Hydrochloride 5 mg/mL 00409-1163-01 Hospira, 25 vials — AP FDA listed —
Bupivacaine Hydrochloride 5 mg/mL 50090-4516-00 A-S 50 ml — AP FDA listed —
Bupivacaine Hydrochloride 5 mg/mL 51662-1396-01 HF 50 ml — AP FDA listed —
BUPIVACAINE HYDROCHLORIDE injection, solution 5 mg/mL 51662-1638-03 HF 25 pouches — AP FDA listed —
Bupivacaine Hydrochloride 5 mg/mL 55150-0250-50 Eugia 25 vials — AP FDA listed —
Sensorcaine 5 mg/mL 63323-0467-57 Fresenius 25 vials — AP FDA listed —
Bupivacaine Hydrochloride 5 mg/mL 71872-7270-01 Medical 1 vial — AP FDA listed —
bupivacaine hydrochloride 5 mg/mL 72603-0287-25 Northstar 25 vials — — FDA listed —
Bupivacaine Hydrochloride 5 mg/mL 83270-0169-01 ONESOURCE 1 vial — AP FDA listed —
Bupivacaine Hydrochloride 5 mg/mL 83854-0006-01 Anthea 1 vial — 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

🏛️
2023
On the market since
Nov 2023
📍
2026
Currently FDA-listed
3 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.

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.

💡 Tap an ingredient (hover on desktop) to see what it is and why it’s used.

  • UNII QTT17582CB
    A strong acid used to adjust and maintain the proper pH level in liquid medicines, ensuring stability and preventing breakdown of active ingredients.
  • UNII 451W47IQ8X
    Sodium chloride is common table salt. It's used in medicines as a buffer to maintain proper pH, as a filler to add bulk, or to adjust the osmotic balance in liquid formulations.
  • UNII 55X04QC32I
    A strong alkaline chemical used to adjust and maintain the pH balance of liquid medicines. It helps keep the medicine stable and ensures it stays effective during storage.
  • UNII 059QF0KO0R
    Water is a liquid solvent that dissolves and mixes ingredients together in liquid medicines, syrups, and injections. It helps distribute the active drug evenly throughout the product.

4 inactive ingredients listed in the exact product block matched to this NDC.

Where does this data come from?
Data sourced from official FDA Structured Product Labeling (SPL) via DailyMed — ingredient classCode="IACT" elements from the exact product block matched by this NDC. Label-section narrative from DailyMed / the openFDA label index is shown separately when available.

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.

Manufacturer & labeler

LabelerSomerset Therapeutics, LLC
Application holderSOMERSET THERAPEUTICS LLC
FDA applicationANDA217792 (ANDA)
Labeler code70069
First marketedNov 2023
Product typeHuman Prescription Drug
Portfolio184 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.

Full prescribing information FDA SPL

The complete FDA label for this product — the official prescribing information, verbatim, section by section. Very long sections are excerpted here and marked; the full text is on DailyMed (linked in the sources below). Jump with a chip, search within the label, or expand everything.
🚨 Boxed Warning 🎯 Indications and Usage ⏱️ Dosage and Administration 💊 Dosage Forms and Strengths ⛔ Contraindications ⚠️ Warnings and Cautions 🤒 Adverse Reactions 🔄 Drug Interactions 👥 Use in Specific Populations 🤰 Pregnancy 🧒 Pediatric Use 🧓 Geriatric Use 🆘 Overdosage 🧬 Clinical Pharmacology 🧬 Mechanism of Action 📦 How Supplied / Storage and Handling 📋 Description 💬 Information for Patients 🧬 Pharmacokinetics 🧬 Pharmacodynamics 🧪 Nonclinical Toxicology 📄 Carcinogenesis, Mutagenesis, Impairment of Fertility 📄 Package Label / Principal Display Panel
🚨 Boxed Warning ~1 min read ▾

BOXED WARNING WARNING: RISK OF CARDIAC ARREST WITH USE OF BUPIVACAINE HYDROCHLORIDE INJECTION IN OBSTETRICAL ANESTHESIA There have been reports of cardiac arrest with difficult resuscitation or death during use of bupivacaine hydrochloride injection for epidural anesthesia in obstetrical patients. In most cases, this has followed use of the 0.75% (7.5 mg/mL) concentration. Resuscitation has been difficult or impossible despite apparently adequate preparation and appropriate management.

Cardiac arrest has occurred after convulsions resulting from systemic toxicity, presumably following unintentional intravascular injection. The 0.75% (7.5 mg/mL) concentration of bupivacaine hydrochloride injection is not recommended for obstetrical anesthesia and should be reserved for surgical procedures where a high degree of muscle relaxation and prolonged effect are necessary [see Warnings and Precautions (5.1)]. WARNING: RISK OF CARDIAC ARREST WITH USE OF BUPIVACAINE HYDROCHLORIDE INJECTION IN OBSTETRICAL ANESTHESIA See full prescribing information for complete boxed warning.

There have been reports of cardiac arrest with difficult resuscitation or death during use of bupivacaine hydrochloride injection for epidural anesthesia in obstetrical patients. In most cases, this has followed use of the 0.75% (7.5 mg/mL) concentration. Resuscitation has been difficult or impossible despite apparently adequate preparation and appropriate management.

Cardiac arrest has occurred after convulsions resulting from systemic toxicity, presumably following unintentional intravascular injection. The 0.75% (7.5 mg/mL) concentration of bupivacaine hydrochloride injection is not recommended for obstetrical anesthesia and should be reserved for surgical procedures where a high degree of muscle relaxation and prolonged effect are necessary (5.1).

🎯 Indications and Usage 194 words ▾

1 INDICATIONS AND USAGE Bupivacaine hydrochloride injection is indicated in adults for the production of local or regional anesthesia or analgesia for surgery, dental and oral surgery procedures, diagnostic and therapeutic procedures, and for obstetrical procedures. Specific concentrations and presentations of bupivacaine hydrochloride injection are recommended for each type of block indicated to produce local or regional anesthesia or analgesia [see Dosage and Administration (2.2)]. Limitations of Use Not all blocks are indicated for use with bupivacaine hydrochloride injection given clinically significant risks associated with use [see Dosage and Administration (2.2), Contraindications (4), Warnings and Precautions (5.1, 5.4, 5.5, 5.7, 5.9)] .

Bupivacaine hydrochloride injection contains bupivacaine, an amide local anesthetic. Bupivacaine hydrochloride injection is indicated in adults for the production of local or regional anesthesia or analgesia for surgery, dental and oral surgery procedures, diagnostic and therapeutic procedures, and for obstetrical procedures. For each type of block indicated to produce local or regional anesthesia or analgesia, specific concentrations and presentations are recommended.

(1, 2.2) Limitations of Use Not all blocks are indicated for use with bupivacaine hydrochloride injection given clinically significant risks associated with use. (1, 2.2, 4, 5.1, 5.4, 5.5, 5.7, 5.9)

⏱️ Dosage and Administration ~2 min read ▾

2 DOSAGE AND ADMINISTRATION Not for intrathecal use. (2.1) Avoid use of solutions containing antimicrobial preservatives (i.e., multiple-dose vials) for epidural or caudal anesthesia. (2.1, 5.4) See full prescribing information for: Recommended concentrations and dosages of bupivacaine hydrochloride injection according to type of block.

(2.2) Additional dosage and administration information pertaining to use in epidural anesthesia, test dose for caudal and lumbar epidural blocks, use in dentistry, and use in ophthalmic surgery. (2.3, 2.4, 2.5, 2.6)

2.1Important Dosage and Administration Information Bupivacaine hydrochloride injection is not for intrathecal use. Avoid use of bupivacaine hydrochloride injection solutions containing antimicrobial preservatives (i.e., multiple-dose vials) for epidural or caudal anesthesia [see Warnings and Precautions (5.4)] . Discard unused portions of solution not containing preservatives, i.e., those supplied in single-dose vials, following initial use.

Visually inspect this product for particulate matter and discoloration prior to administration whenever solution and container permit. Bupivacaine hydrochloride injection are clear, colorless solutions. Do not administer solutions which are discolored or contain particulate matter.

Mixing or the prior or intercurrent use of any other local anesthetic with bupivacaine hydrochloride injection is not recommended because of insufficient data on the clinical use of such mixtures. Administration Precautions Bupivacaine hydrochloride injection are to be administered in carefully adjusted dosages by or under the supervision of experienced clinicians who are well versed in the diagnosis and management of dose-related toxicity and other acute emergencies which might arise from the block to be employed. Use bupivacaine hydrochloride injection only if the following are immediately available: oxygen, cardiopulmonary resuscitative equipment and drugs, and the personnel resources needed for proper management of toxic reactions and related emergencies [see Warnings and Precautions (5.2), Adverse Reactions (6), Overdosage (10)].

The toxic effects of local anesthetics are additive. Monitor for neurologic and cardiovascular effects related to local anesthetic systemic toxicity when additional local anesthetics are administered with bupivacaine hydrochloride injection [see Warnings and Precautions (5.2), Drug Interactions (7.1), Overdosage (10)]. Aspirate for blood or cerebrospinal fluid (where applicable) prior to injecting bupivacaine hydrochloride injection, both the initial dose and all subsequent doses, to avoid intravascular or intrathecal injection.

However, a negative aspiration for blood or cerebrospinal fluid does not ensure against an intravascular or intrathecal injection [see Warnings and Precautions (5.9)] . Avoid rapid injection of a large volume of bupivacaine hydrochloride injection and use fractional (incremental) doses when feasible. During major regional nerve blocks, such as those of the brachial plexus or lower extremity, the patient should have an indwelling intravenous catheter to assure adequate intravenous access.

The lowest dosage of bupivacaine hydrochloride injection that results in effective anesthesia should be used to avoid high plasma levels and serious adverse reactions. Perform careful and constant monitoring of cardiovascular and respiratory (adequacy of oxygenation and ventilation) vital signs and the patient's level of consciousness after each local anesthetic injection.

2.2Recommended Concentrations and Dosages of bupivacaine hydrochloride injection The dosage of bupivacaine hydrochloride injection administered varies with the anesthetic procedure, the area to be anesthetized, the vascularity of the tissues, the number of neuronal segments to be blocked, the depth of anesthesia and degree of muscle relaxation required, the duration of anesthesia desired, individual tolerance, and the physical condition of the patient. Admini… [Excerpted — this section continues on DailyMed.]

💊 Dosage Forms and Strengths 52 words ▾

3 DOSAGE FORMS AND STRENGTHS Bupivacaine hydrochloride injection is a clear, colorless solution available as: 0.25% (125 mg/50 mL) (2.5 mg/mL) in multiple-dose vials. 0.5% (250 mg/50 mL) (5 mg/mL) in multiple-dose vials. Bupivacaine hydrochloride injection are available in multiple concentrations. See full prescribing information for detailed description of each formulation. (3)

⛔ Contraindications 104 words ▾

4 CONTRAINDICATIONS Bupivacaine hydrochloride injection is contraindicated in: obstetrical paracervical block anesthesia. Its use in this technique has resulted in fetal bradycardia and death. intravenous regional anesthesia (Bier Block) [see Warnings and Precautions (5.7)] . patients with a known hypersensitivity to bupivacaine or to any local anesthetic agent of the amide-type or to other components of bupivacaine hydrochloride injection. Obstetrical paracervical block anesthesia.

Its use in this technique has resulted in fetal bradycardia and death. (4) Intravenous regional anesthesia (Bier Block). (4) Known hypersensitivity to bupivacaine or to any local anesthetic agent of the amide-type or to other components of bupivacaine hydrochloride injection.

(4)

⚠️ Warnings and Cautions ~2 min read ▾

5 WARNINGS AND PRECAUTIONS Dose-Related Toxicity : Monitor cardiovascular and respiratory vital signs and patient's state of consciousness after injection of bupivacaine hydrochloride injection (5.2) Methemoglobinemia : Cases of methemoglobinemia have been reported in association with local anesthetic use. See full prescribing information for more detail on managing these risks. (5.3) Chondrolysis with Intra-Articular Infusion : Intra-articular infusions of local anesthetics including bupivacaine hydrochloride injection following arthroscopic and other surgical procedures is an unapproved use, and there have been post-marketing reports of chondrolysis in patients receiving such infusions.

(5.5) Risk of Cardiac Arrest with Intravenous Regional Anesthesia Use (Bier Block) : There have been reports of cardiac arrest and death during the use of bupivacaine for intravenous regional anesthesia (Bier Block). (5.7)

5.1Risk of Cardiac Arrest with Use of bupivacaine hydrochloride injection in Obstetrical Anesthesia There have been reports of cardiac arrest with difficult resuscitation or death during use of bupivacaine hydrochloride injection for epidural anesthesia in obstetrical patients. In most cases, this has followed use of the 0.75% (7.5 mg/mL) concentration. Resuscitation has been difficult or impossible despite apparently adequate preparation and appropriate management.

Cardiac arrest has occurred after convulsions resulting from systemic toxicity, presumably following unintentional intravascular injection. The 0.75% (7.5 mg/mL) concentration of bupivacaine hydrochloride injection is not recommended for obstetrical anesthesia and should be reserved for surgical procedures where a high degree of muscle relaxation and prolonged effect are necessary.

5.2Dose-Related Toxicity The safety and effectiveness of bupivacaine hydrochloride injection depend on proper dosage, correct technique, adequate precautions, and readiness for emergencies. Careful and constant monitoring of cardiovascular and respiratory (adequacy of ventilation) vital signs and the patient's state of consciousness should be performed after injection of bupivacaine hydrochloride injection solutions. Possible early warning signs of central nervous system (CNS) toxicity are restlessness, anxiety, incoherent speech, lightheadedness, numbness and tingling of the mouth and lips, metallic taste, tinnitus, dizziness, blurred vision, tremors, twitching, CNS depression, or drowsiness.

Delay in proper management of dose-related toxicity, underventilation from any cause, and/or altered sensitivity may lead to the development of acidosis, cardiac arrest, and, possibly, death. During major regional nerve blocks, such as those of the brachial plexus or lower extremity, the patient should have an indwelling intravenous catheter to assure adequate intravenous access. Use the lowest dosage of bupivacaine hydrochloride injection that results in effective anesthesia to avoid high plasma levels and serious adverse effects.

Avoid rapid injection of a large volume of bupivacaine hydrochloride injection solution and administer fractional (incremental) doses when feasible. Injection of repeated doses of bupivacaine hydrochloride injection may cause significant increases in plasma levels with each repeated dose due to slow accumulation of the drug or its metabolites, or to slow metabolic degradation. Tolerance to elevated blood levels varies with the status of the patient.

Debilitated, elderly patients and acutely ill patients should be given reduced doses commensurate with their age and physical status.

5.3Methemoglobinemia Cases of methemoglobinemia have been reported in association with local anesthetic use. Although all patients are at risk for methemoglobinemia, patients with glucose-6-phosphate dehydrogenase deficiency, congenital or idiopathic methemoglobinemia, cardiac or pulmonary compromise, infants under 6 months of age, and concurrent exposure to oxidizing agents or their meta… [Excerpted — this section continues on DailyMed.]

🤒 Adverse Reactions ~2 min read ▾

6 ADVERSE REACTIONS The following clinically significant adverse reactions have been reported and described in the Warnings and Precautions section of the labeling: Cardiac Arrest in Obstetrical Anesthesia [see Warnings and Precautions (5.1)] Dose-Related Toxicity [see Warnings and Precautions (5.2)] Methemoglobinemia [see Warnings and Precautions (5.3)] Chondrolysis with Intra-Articular Infusion [see Warnings and Precautions (5.5)] Severe, Persistent Hypertension, Cerebrovascular Accidents, and Bradycardia Due to Drug Interactions [see Warnings and Precautions (5.6)] Cardiac Arrest with Intravenous Regional Anesthesia Use [see Contraindications (4), Warnings and Precautions (5.7)] Allergic-Type Reactions [see Warnings and Precautions (5.8)] Systemic Toxicities with Unintended Intravascular or Intrathecal Injection [see Warnings and Precautions (5.9)] Respiratory Arrest Following Retrobulbar Block [see Warnings and Precautions(5.15)] The following adverse reactions from voluntary reports or clinical studies have been reported with bupivacaine or bupivacaine and epinephrine.

Because many of these reactions were 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 reactions to bupivacaine hydrochloride injection are characteristic of those associated with other amide-type local anesthetics. A major cause of adverse reactions to this group of drugs is excessive plasma levels, which may be due to overdosage, unintentional intravascular injection, or slow metabolic degradation.

The most commonly encountered acute adverse reactions that demand immediate counter-measures were related to the CNS and the cardiovascular system. These adverse reactions were generally dose-related and due to high plasma levels which may have resulted from overdosage, rapid absorption from the injection site, diminished tolerance, or from unintentional intravascular injection of the local anesthetic solution. In addition to systemic dose-related toxicity, unintentional intrathecal injection of drug during the intended performance of caudal or lumbar epidural block or nerve blocks near the vertebral column (especially in the head and neck region) has resulted in underventilation or apnea ("Total or High Spinal").

Also, hypotension due to loss of sympathetic tone and respiratory paralysis or underventilation due to cephalad extension of the motor level of anesthesia have occurred. This has led to secondary cardiac arrest when untreated. Nervous System Disorders : Adverse reactions were characterized by excitation and/or depression of the central nervous system and included restlessness, anxiety, dizziness, tinnitus, blurred vision, tremors, convulsions, drowsiness, unconsciousness, respiratory arrest, nausea, vomiting, chills, pupillary constriction.

In the practice of caudal or lumbar epidural block, unintentional penetration of the subarachnoid space by the catheter or needle has occurred. Subsequent adverse effects may have depended partially on the amount of drug administered intrathecally and the physiological and physical effects of a dural puncture. A high spinal has been characterized by paralysis of the legs, loss of consciousness, respiratory paralysis, and bradycardia.

Neurologic effects following epidural or caudal anesthesia have included spinal block of varying magnitude (including high or total spinal block); hypotension secondary to spinal block; urinary retention; fecal and urinary incontinence; loss of perineal sensation and sexual function; persistent anesthesia, paresthesia, weakness, paralysis of the lower extremities and loss of sphincter control, all of which had slow, incomplete, or no recovery; headache; backache; septic meningitis; meningismus; slowing of labor; increased incidence of forceps delivery; and cranial nerve palsies due to traction on nerves from loss of cerebrospinal fluid.

Neurologic effects… [Excerpted — this section continues on DailyMed.]

🔄 Drug Interactions ~1 min read ▾

7 DRUG INTERACTIONS Local Anesthetics : The toxic effects of local anesthetics are additive. Monitor for neurologic and cardiovascular effects when additional local anesthetics are administered. (7.1) Drugs Associated with Methemoglobinemia : Patients are at increased risk of developing methemoglobinemia when concurrently exposed to nitrates, nitrites, local anesthetics, antineoplastic agents, antibiotics, antimalarials, anticonvulsants, and other drugs.

(7.5) Potent Inhalation Anesthetics : Serious dose-related cardiac arrhythmias may occur if preparations containing a vasoconstrictor such as epinephrine are used in patients during or following the administration of potent inhalation anesthetics. (5.13, 7.6)

7.1Local Anesthetics The toxic effects of local anesthetics are additive. If coadministration of other local anesthetics with bupivacaine hydrochloride injection cannot be avoided, monitor patients for neurologic and cardiovascular effects related to local anesthetic systemic toxicity [see Dosage and Administration (2.1), Warnings and Precautions (5.2)] .

7.5Drugs Associated with Methemoglobinemia Patients who are administered bupivacaine hydrochloride injection are at increased risk of developing methemoglobinemia when concurrently exposed to following drugs, which could include other local anesthetics [see Warnings and Precautions (5.3)]. Examples of Drugs Associated with Methemoglobinemia: Class Examples Nitrates/Nitrites nitric oxide, nitroglycerin, nitroprusside, nitrous oxide Local anesthetics articaine, benzocaine, bupivacaine, lidocaine, mepivacaine, prilocaine, procaine, ropivacaine, tetracaine Antineoplastic agents cyclophosphamide, flutamide, hydroxyurea, isofamide, rasburicase Antibiotics dapsone, nitrofurantoin, para-aminosalicylic acid, sulfonamides Antimalarials chloroquine, primaquine Anticonvulsants phenobarbital, phenytoin, sodium valproate Other drugs acetaminophen, metoclopramide, quinine, sulfasalazine

👥 Use in Specific Populations ~3 min read ▾

8 USE IN SPECIFIC POPULATIONS Pediatric Use : Administration of bupivacaine hydrochloride injection in pediatric patients younger than 12 years is not recommended. (8.4) Geriatric Use : Patients 65 years and over, particularly those with hypertension, may be at increased risk for developing hypotension while undergoing anesthesia with bupivacaine hydrochloride injection . (8.5) Moderate to Severe Hepatic Impairmen t: Consider increased monitoring for bupivacaine systemic toxicity.

(8.6)

8.1Pregnancy Risk Summary Bupivacaine hydrochloride injection is contraindicated for obstetrical paracervical block anesthesia. Its use in this technique has resulted in fetal bradycardia and death [see Contraindications (4), Warnings and Precautions (5.1)] . There are no available data on use of bupivacaine hydrochloride injection in pregnant women to inform a drug-associated risk of adverse developmental outcomes.

In animal studies, embryo-fetal lethality was noted when bupivacaine was administered subcutaneously to pregnant rabbits during organogenesis at clinically relevant doses. Decreased pup survival was observed in a rat pre- and post-natal developmental study (dosing from implantation through weaning) at a dose level comparable to the daily maximum recommended human dose (MRHD) on a body surface area (BSA) basis. Based on animal data, advise pregnant women of the potential risks to a fetus (see Data).

Local anesthetics rapidly cross the placenta, and when used for epidural, caudal, or pudendal block anesthesia, can cause varying degrees of maternal, fetal, and neonatal toxicity [see Clinical Pharmacology (12.3)]. The incidence and degree of toxicity depend upon the procedure performed, the type, and amount of drug used, and the technique of drug administration. Adverse reactions in the parturient, fetus, and neonate involve alterations of the CNS, peripheral vascular tone, and cardiac function.

If this drug is used during pregnancy, or if the patient becomes pregnant while taking this drug, inform the patient of the potential hazard to the fetus. The estimated background risk of major birth defects and miscarriage for the indicated populations are unknown. In the U.S. general population, the estimated background risk of major birth defects and miscarriage in clinically recognized pregnancies is 2-4% and 15-20%, respectively.

Clinical Considerations Maternal Adverse Reactions Maternal hypotension has resulted from regional anesthesia. Local anesthetics produce vasodilation by blocking sympathetic nerves. The supine position is dangerous in pregnant women at term because of aortocaval compression by the gravid uterus.

Therefore, during treatment of systemic toxicity, maternal hypotension or fetal bradycardia following regional block, the parturient should be maintained in the left lateral decubitus position if possible, or manual displacement of the uterus off the great vessels be accomplished. Elevating the patient's legs will also help prevent decreases in blood pressure. The fetal heart rate also should be monitored continuously and electronic fetal monitoring is highly advisable.

Labor or Delivery Epidural, caudal, or pudendal anesthesia may alter the forces of parturition through changes in uterine contractility or maternal expulsive efforts. Epidural anesthesia has been reported to prolong the second stage of labor by removing the parturient's reflex urge to bear down or by interfering with motor function. The use of obstetrical anesthesia may increase the need for forceps assistance.

The use of some local anesthetic drug products during labor and delivery may be followed by diminished muscle strength and tone for the first day or two of life. This has not been reported with bupivacaine. It is extremely important to avoid aortocaval compression by the gravid uterus during administration of regional block to parturients.

To do this, the patient must be maintained in the left lateral decubitus position or a blanket roll or sandbag m… [Excerpted — this section continues on DailyMed.]

🤰 Pregnancy ~3 min read ▾

8.1Pregnancy Risk Summary Bupivacaine hydrochloride injection is contraindicated for obstetrical paracervical block anesthesia. Its use in this technique has resulted in fetal bradycardia and death [see Contraindications (4), Warnings and Precautions (5.1)] . There are no available data on use of bupivacaine hydrochloride injection in pregnant women to inform a drug-associated risk of adverse developmental outcomes.

In animal studies, embryo-fetal lethality was noted when bupivacaine was administered subcutaneously to pregnant rabbits during organogenesis at clinically relevant doses. Decreased pup survival was observed in a rat pre- and post-natal developmental study (dosing from implantation through weaning) at a dose level comparable to the daily maximum recommended human dose (MRHD) on a body surface area (BSA) basis. Based on animal data, advise pregnant women of the potential risks to a fetus (see Data).

Local anesthetics rapidly cross the placenta, and when used for epidural, caudal, or pudendal block anesthesia, can cause varying degrees of maternal, fetal, and neonatal toxicity [see Clinical Pharmacology (12.3)]. The incidence and degree of toxicity depend upon the procedure performed, the type, and amount of drug used, and the technique of drug administration. Adverse reactions in the parturient, fetus, and neonate involve alterations of the CNS, peripheral vascular tone, and cardiac function.

If this drug is used during pregnancy, or if the patient becomes pregnant while taking this drug, inform the patient of the potential hazard to the fetus. The estimated background risk of major birth defects and miscarriage for the indicated populations are unknown. In the U.S. general population, the estimated background risk of major birth defects and miscarriage in clinically recognized pregnancies is 2-4% and 15-20%, respectively.

Clinical Considerations Maternal Adverse Reactions Maternal hypotension has resulted from regional anesthesia. Local anesthetics produce vasodilation by blocking sympathetic nerves. The supine position is dangerous in pregnant women at term because of aortocaval compression by the gravid uterus.

Therefore, during treatment of systemic toxicity, maternal hypotension or fetal bradycardia following regional block, the parturient should be maintained in the left lateral decubitus position if possible, or manual displacement of the uterus off the great vessels be accomplished. Elevating the patient's legs will also help prevent decreases in blood pressure. The fetal heart rate also should be monitored continuously and electronic fetal monitoring is highly advisable.

Labor or Delivery Epidural, caudal, or pudendal anesthesia may alter the forces of parturition through changes in uterine contractility or maternal expulsive efforts. Epidural anesthesia has been reported to prolong the second stage of labor by removing the parturient's reflex urge to bear down or by interfering with motor function. The use of obstetrical anesthesia may increase the need for forceps assistance.

The use of some local anesthetic drug products during labor and delivery may be followed by diminished muscle strength and tone for the first day or two of life. This has not been reported with bupivacaine. It is extremely important to avoid aortocaval compression by the gravid uterus during administration of regional block to parturients.

To do this, the patient must be maintained in the left lateral decubitus position or a blanket roll or sandbag may be placed beneath the right hip and gravid uterus displaced to the left. Data Animal Data Bupivacaine hydrochloride produced developmental toxicity when administered subcutaneously to pregnant rats and rabbits at clinically relevant doses. Bupivacaine hydrochloride was administered subcutaneously to rats at doses of 4.4, 13.3, & 40 mg/kg and to rabbits at doses of 1.3, 5.8, & 22.2 mg/kg during the period of organogenesis (implantation to closure of the hard palate).

The high doses are… [Excerpted — this section continues on DailyMed.]

🧒 Pediatric Use 57 words ▾

8.4Pediatric Use Bupivacaine hydrochloride injection is approved for use in adults. Administration of bupivacaine hydrochloride injection in pediatric patients younger than 12 years is not recommended. Continuous infusions of bupivacaine in pediatric patients have been reported to result in high systemic levels of bupivacaine and seizures; high plasma levels may also be associated with cardiovascular abnormalities.

🧓 Geriatric Use 135 words ▾

8.5Geriatric Use Patients 65 years and over, particularly those with hypertension, may be at increased risk for developing hypotension while undergoing anesthesia with bupivacaine hydrochloride injection. In clinical studies of bupivacaine, elderly patients reached the maximal spread of analgesia and maximal motor blockade more rapidly than younger adult patients. Differences in various pharmacokinetic parameters have been observed between elderly and younger adult patients [see Clinical Pharmacology (12.3)] .

This product is known to be substantially excreted by the kidney, and the risk of adverse reactions to this drug may be greater in patients with impaired renal function. Because elderly patients are more likely to have decreased renal function, care should be taken in dose selection, and it may be useful to monitor renal function. Elderly patients may require lower doses of bupivacaine hydrochloride injection.

🆘 Overdosage ~1 min read ▾

10 OVERDOSAGE Clinical Presentation Acute emergencies from use of bupivacaine hydrochloride injection are generally related to high plasma levels encountered during therapeutic use or to unintended intrathecal injection [see Warnings and Precautions (5.2, 5.9), Adverse Reactions (6)]. If not treated immediately, convulsions with simultaneous hypoxia, hypercarbia, and acidosis plus myocardial depression from the direct effects of bupivacaine may result in cardiac arrhythmias, bradycardia, asystole, ventricular fibrillation, or cardiac arrest.

Respiratory abnormalities, including apnea, may occur. Hypoventilation or apnea due to unintentional intrathecal injection of bupivacaine hydrochloride injection may produce these same signs and also lead to cardiac arrest if ventilatory support is not instituted. If cardiac arrest should occur, successful outcome may require prolonged resuscitative efforts.

Management The first step in the management of systemic toxic reactions, as well as hypoventilation or apnea due to unintentional intrathecal injection of bupivacaine hydrochloride injection, consists of immediate attention to the establishment and maintenance of a patent airway and effective assisted or controlled ventilation with 100% oxygen with a delivery system capable of permitting immediate positive airway pressure by mask. Endotracheal intubation, using drugs and techniques familiar to the clinician, may be indicated after initial administration of oxygen by mask if difficulty is encountered in the maintenance of a patent airway, or if prolonged ventilatory support (assisted or controlled) is indicated.

If necessary, use drugs to manage the convulsions. A bolus intravenous dose of a benzodiazepine will counteract CNS stimulation related to bupivacaine hydrochloride injection. Immediately after the institution of ventilatory measures, evaluate the adequacy of the circulation.

Supportive treatment of circulatory depression may require Advance Cardiac Life Support measures.

🧬 Clinical Pharmacology ~3 min read ▾

12 CLINICAL PHARMACOLOGY

12.1Mechanism of Action Bupivacaine blocks the generation and the conduction of nerve impulses, presumably by increasing the threshold for electrical excitation in the nerve, by slowing the propagation of the nerve impulse, and by reducing the rate of rise of the action potential. In general, the progression of anesthesia is related to the diameter, myelination, and conduction velocity of affected nerve fibers. Clinically, the order of loss of nerve function is as follows: (1) pain, (2) temperature, (3) touch, (4) proprioception, and (5) skeletal muscle tone.

Epinephrine is a vasoconstrictor added to bupivacaine to slow absorption into the general circulation and thus prolong maintenance of an active tissue concentration.

12.2Pharmacodynamics Systemic absorption of bupivacaine produces effects on the cardiovascular system and CNS. At blood concentrations achieved with normal therapeutic doses, changes in cardiac conduction, excitability, refractoriness, contractility, and peripheral vascular resistance are minimal. However, toxic blood concentrations depress cardiac conduction and excitability, which may lead to atrioventricular block, ventricular arrhythmias, and cardiac arrest, sometimes resulting in fatalities.

In addition, myocardial contractility is depressed and peripheral vasodilation occurs, leading to decreased cardiac output and arterial blood pressure. These cardiovascular changes are more likely to occur after unintended intravascular injection of bupivacaine [see Warnings and Precautions (5.9)] . Following systemic absorption, bupivacaine can produce CNS stimulation, CNS depression, or both.

Apparent central stimulation is manifested as restlessness, tremors, and shivering, progressing to convulsions, followed by CNS depression and coma progressing ultimately to respiratory arrest. However, bupivacaine has a primary depressant effect on the medulla and on higher centers. The depressed stage may occur without a prior excited state.

The duration of local anesthesia after administration of bupivacaine hydrochloride injection is longer than that observed after administration of other commonly used short-acting local anesthetics. There appears to be period of analgesia that persists after the resolution of the block and return of sensation. The onset of action following dental injections is usually 2 to 10 minutes and may last up to 7 hours.

The duration of anesthetic effect is prolonged by the addition of epinephrine 1:200,000.

12.3Pharmacokinetics Systemic plasma levels of bupivacaine following administration of bupivacaine hydrochloride injection do not correlate with local efficacy. Absorption The rate of systemic absorption of bupivacaine is dependent upon the total dose and concentration of drug administered, the route of administration, the vascularity of the administration site, and the presence or absence of epinephrine in the anesthetic solution. A dilute concentration of epinephrine (1:200,000) usually reduces the rate of absorption and peak plasma concentration of bupivacaine, permitting the use of moderately larger total doses and sometimes prolonging the duration of action [see Dosage and Administration (2)] .

After injection of bupivacaine hydrochloride injection for caudal, epidural, or peripheral nerve block, peak levels of bupivacaine in the blood are reached in 30 to 45 minutes, followed by a decline to insignificant levels during the next three to six hours. Distribution Bupivacaine appears to cross the placenta by passive diffusion. The rate and degree of diffusion is governed by (1) the degree of plasma protein binding, (2) the degree of ionization, and (3) the degree of lipid solubility.

Fetal/ maternal ratios of bupivacaine appear to be inversely related to the degree of plasma protein binding, because only the free, unbound drug is available for placental transfer. Bupivacaine with a high protein binding capacity (95%) has a low fetal/maternal ratio (0.2 to 0.4). The… [Excerpted — this section continues on DailyMed.]

🧬 Mechanism of Action 110 words ▾

12.1Mechanism of Action Bupivacaine blocks the generation and the conduction of nerve impulses, presumably by increasing the threshold for electrical excitation in the nerve, by slowing the propagation of the nerve impulse, and by reducing the rate of rise of the action potential. In general, the progression of anesthesia is related to the diameter, myelination, and conduction velocity of affected nerve fibers. Clinically, the order of loss of nerve function is as follows: (1) pain, (2) temperature, (3) touch, (4) proprioception, and (5) skeletal muscle tone.

Epinephrine is a vasoconstrictor added to bupivacaine to slow absorption into the general circulation and thus prolong maintenance of an active tissue concentration.

📦 How Supplied / Storage and Handling 172 words ▾

16 HOW SUPPLIED/STORAGE AND HANDLING Store at 20 °C to 25 °C (68 °F to 77 °F); excursions permitted between 15 °C to 30 °C (59 ° F to 86 °F). [See USP Controlled Room Temperature.] Bupivacaine hydrochloride injection ―Solutions of bupivacaine hydrochloride injection that do not contain epinephrine may be autoclaved. Autoclave at 15-pound pressure, 121 °C (250 °F) for 15 minutes. Protect from light.

This product is clear and colorless. Do not use the solution if it is discolored or if it contains a precipitate. Unit of Sale Concentration Each 0.25% Contains 2.5 mg bupivacaine hydrochloride per mL.

NDC 70069- 752 -01 Carton of 01 125 mg/50 mL (2.5 mg/mL) NDC 70069- 752 -01 multiple-dose vial NDC 70069- 752 -10 Carton of 10 NDC 70069- 752 -25 Carton of 25 0.5% Contains 5 mg bupivacaine hydrochloride per mL. NDC 70069- 753 -01 Carton of 01 250 mg/50 mL (5 mg/mL) NDC 70069- 753 -01 multiple-dose vial NDC 70069- 753 -10 Carton of 10 NDC 70069- 753 -25 Carton of 25

📋 Description 154 words ▾

11 DESCRIPTION Bupivacaine hydrochloride injection contains bupivacaine hydrochloride, an amide local anesthetic, as the active pharmaceutical ingredient. The route of administration for bupivacaine hydrochloride injection (without epinephrine) is by injection, for infiltration, perineural, or retrobulbar use. Multiple-dose vials contain methylparaben [see Warnings and Precautions (5.4)] .

Bupivacaine hydrochloride is 2-piperidinecarboxamide, 1-butyl- N -(2,6-dimethylphenyl)-, monohydrochloride, monohydrate. It is a white crystalline powder that is freely soluble in 96 percent ethanol, soluble in water, and slightly soluble in chloroform or acetone. It has the following structural formula: Bupivacaine hydrochloride is a clear and colorless sterile isotonic solution.

Each mL of multiple-dose vial contains 2.5 mg or 5 mg of bupivacaine hydrochloride (equivalent to 2.22 mg or 4.44 mg of bupivacaine, respectively), sodium chloride for isotonicity, sodium hydroxide or hydrochloric acid to adjust the pH between 4 and 6.5, in water for injection. For the Multiple-dose vials, each mL also contains 1 mg methylparaben as preservative. Image

💬 Information for Patients 207 words ▾

17 PATIENT COUNSELING INFORMATION Allergic-Type Reactions Assess if the patient has had allergic-type reactions to amide-type local anesthetics or to other formulation ingredients, such as the antimicrobial preservative methylparaben contained in multiple-dose vials or sulfites in epinephrine-containing solutions [see Contraindications (4), Warnings and Precautions (5.8), Adverse Reactions (6)] . Temporary Loss of Sensation and Motor Activity After Caudal or Epidural Anesthesia When appropriate, patients should be informed in advance that they may experience temporary loss of sensation and motor activity, usually in the lower half of the body, following proper administration of caudal or epidural anesthesia.

Instructions After Dental Injection of bupivacaine hydrochloride injection Advise patients receiving dental injections of bupivacaine hydrochloride injection not to chew solid foods or to test the anesthetized area by biting or probing until anesthesia has worn off (up to 7 hours) [see Warnings and Precautions (5.16)] . Methemoglobinemia Inform patients that use of local anesthetics may cause methemoglobinemia, a serious condition that must be treated promptly. Advise patients or caregivers to seek immediate medical attention if they or someone in their care experience the following signs or symptoms: pale, gray, or blue colored skin (cyanosis); headache; rapid heart rate; shortness of breath; lightheadedness; or fatigue [see Warnings and Precautions (5.3)] .

🧬 Pharmacokinetics ~3 min read ▾

12.3Pharmacokinetics Systemic plasma levels of bupivacaine following administration of bupivacaine hydrochloride injection do not correlate with local efficacy. Absorption The rate of systemic absorption of bupivacaine is dependent upon the total dose and concentration of drug administered, the route of administration, the vascularity of the administration site, and the presence or absence of epinephrine in the anesthetic solution. A dilute concentration of epinephrine (1:200,000) usually reduces the rate of absorption and peak plasma concentration of bupivacaine, permitting the use of moderately larger total doses and sometimes prolonging the duration of action [see Dosage and Administration (2)] .

After injection of bupivacaine hydrochloride injection for caudal, epidural, or peripheral nerve block, peak levels of bupivacaine in the blood are reached in 30 to 45 minutes, followed by a decline to insignificant levels during the next three to six hours. Distribution Bupivacaine appears to cross the placenta by passive diffusion. The rate and degree of diffusion is governed by (1) the degree of plasma protein binding, (2) the degree of ionization, and (3) the degree of lipid solubility.

Fetal/ maternal ratios of bupivacaine appear to be inversely related to the degree of plasma protein binding, because only the free, unbound drug is available for placental transfer. Bupivacaine with a high protein binding capacity (95%) has a low fetal/maternal ratio (0.2 to 0.4). The extent of placental transfer is also determined by the degree of ionization and lipid solubility of the drug.

Lipid soluble, nonionized drugs readily enter the fetal blood from the maternal circulation. Depending upon the route of administration, bupivacaine is distributed to some extent to all body tissues, with high concentrations found in highly perfused organs such as the liver, lungs, heart, and brain. Pharmacokinetic studies on the plasma profile of bupivacaine after direct intravenous injection (bupivacaine hydrochloride injection is not approved for intravenous use) suggest a three-compartment open model.

The first compartment is represented by the rapid intravascular distribution of the drug. The second compartment represents the equilibration of the drug throughout the highly perfused organs such as the brain, myocardium, lungs, kidneys, and liver. The third compartment represents an equilibration of the drug with poorly perfused tissues, such as muscle and fat.

Elimination The half-life of bupivacaine in adults is 2.7 hours. Metabolism Amide-type local anesthetics such as bupivacaine are metabolized primarily in the liver via conjugation with glucuronic acid. Pipecoloxylidine is the major metabolite of bupivacaine.

The elimination of drug from tissue distribution depends largely upon the availability of binding sites in the circulation to carry it to the liver where it is metabolized. Excretion The kidney is the main excretory organ for most local anesthetics and their metabolites. Urinary excretion is affected by urinary perfusion and factors affecting urinary pH.

Only 6% of bupivacaine is excreted unchanged in the urine. Specific Populations Geriatric Patients Elderly patients exhibited higher peak plasma concentrations than younger patients following administration of bupivacaine hydrochloride injection. The total plasma clearance was decreased in these patients [see Use in Specific Populations (8.5)] .

Patients with Hepatic Impairment Various pharmacokinetic parameters of the local anesthetics can be significantly altered by the presence of hepatic disease. Patients with hepatic disease, especially those with severe hepatic disease, may be more susceptible to the potential toxicities of the amide-type local anesthetics [see Use in Specific Populations (8.6)] . Patients with Renal Impairment Various pharmacokinetic parameters of the local anesthetics can be significantly altered by the presence of renal disease, factors affecting urinary pH, and ren… [Excerpted — this section continues on DailyMed.]

🧬 Pharmacodynamics ~1 min read ▾

12.2Pharmacodynamics Systemic absorption of bupivacaine produces effects on the cardiovascular system and CNS. At blood concentrations achieved with normal therapeutic doses, changes in cardiac conduction, excitability, refractoriness, contractility, and peripheral vascular resistance are minimal. However, toxic blood concentrations depress cardiac conduction and excitability, which may lead to atrioventricular block, ventricular arrhythmias, and cardiac arrest, sometimes resulting in fatalities.

In addition, myocardial contractility is depressed and peripheral vasodilation occurs, leading to decreased cardiac output and arterial blood pressure. These cardiovascular changes are more likely to occur after unintended intravascular injection of bupivacaine [see Warnings and Precautions (5.9)] . Following systemic absorption, bupivacaine can produce CNS stimulation, CNS depression, or both.

Apparent central stimulation is manifested as restlessness, tremors, and shivering, progressing to convulsions, followed by CNS depression and coma progressing ultimately to respiratory arrest. However, bupivacaine has a primary depressant effect on the medulla and on higher centers. The depressed stage may occur without a prior excited state.

The duration of local anesthesia after administration of bupivacaine hydrochloride injection is longer than that observed after administration of other commonly used short-acting local anesthetics. There appears to be period of analgesia that persists after the resolution of the block and return of sensation. The onset of action following dental injections is usually 2 to 10 minutes and may last up to 7 hours.

The duration of anesthetic effect is prolonged by the addition of epinephrine 1:200,000.

🧪 Nonclinical Toxicology 50 words ▾

13 NONCLINICAL TOXICOLOGY

13.1Carcinogenesis, Mutagenesis, Impairment of Fertility Carcinogenesis Long-term studies in animals to evaluate the carcinogenic potential of bupivacaine hydrochloride have not been conducted. Mutagenesis The mutagenic potential of bupivacaine hydrochloride has not been determined. Impairment of Fertility The effect of bupivacaine on fertility has not been determined.

📄 Carcinogenesis, Mutagenesis, Impairment of Fertility 47 words ▾

13.1Carcinogenesis, Mutagenesis, Impairment of Fertility Carcinogenesis Long-term studies in animals to evaluate the carcinogenic potential of bupivacaine hydrochloride have not been conducted. Mutagenesis The mutagenic potential of bupivacaine hydrochloride has not been determined. Impairment of Fertility The effect of bupivacaine on fertility has not been determined.

📄 Package Label / Principal Display Panel 56 words ▾

PACKAGE LABEL.PRINCIPAL DISPLAY PANEL Container Label (2.5 mg/mL) Carton Label (2.5 mg/mL) (25s Pack) Container Label (5 mg/mL) Carton Label (5 mg/mL) (25s Pack) Carton Label (2.5 mg/mL) (10s Pack) Carton Label (2.5 mg/mL) (1s Pack) Carton Label (5 mg/mL) (10s Pack) Carton Label (5 mg/mL) (1s Pack) Image Image Image Image image image image image

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

Medicaid utilization & spend

📍 This exact package only: Medicaid data is reported per full 11-digit NDC — labeler, product and pack size — so every number here is for this package alone, not the drug overall. Other pack sizes report separately.
💊 Pharmacy benefit only: These are Medicaid outpatient pharmacy claims, billed by NDC. They exclude the medical benefit — clinic- or hospital-administered drugs billed under HCPCS J-codes — so drugs used mostly that way (e.g. Avastin, Lucentis, Keytruda) can look low or missing here. That’s expected, not an error.
📅 Q1 2025 – Q1 2026 · 5 quarters of data
ⓘ The newest quarter is usually incomplete when first published; states restate recent quarters in later CMS releases, so the latest figures typically revise upward. State coverage-policy changes can also shift quarter-to-quarter totals.
Prescriptions last 4 qtrs
119
Units reimbursed last 4 qtrs
865
Gross reimbursed last 4 qtrs
$238.77
Avg / prescription
$2.01
Avg / unit
$0.2762
Latest quarter Q1 2026
0Rx
Medicaid pays / mL
$0.2762
gross reimbursed
vs
NADAC / mL
$0.0860
acquisition cost
=
Spread
+$0.1902
+221% vs cost
What Medicaid paid per mL (before rebates; includes the pharmacy’s dispensing fee) compared with NADAC — the average price pharmacies pay to buy the drug. A positive spread means Medicaid reimbursed more than the purchase price, before manufacturer rebates.
Fee-for-service vs managed care ⓘ
100% MCO
Fee-for-service · 0 Rx Managed care · 119 Rx
State Medicaid map
Alaska: no data reported AK Maine: no data reported ME Washington: no data reported WA Idaho: no data reported ID Montana: no data reported MT North Dakota: no data reported ND Minnesota: 315 units · 5.5 per 100k residents MN Wisconsin: no data reported WI Michigan: no data reported MI New York: no data reported NY Vermont: no data reported VT New Hampshire: no data reported NH Oregon: no data reported OR Nevada: no data reported NV Wyoming: no data reported WY South Dakota: no data reported SD Iowa: no data reported IA Illinois: no data reported IL Indiana: no data reported IN Ohio: no data reported OH Pennsylvania: no data reported PA New Jersey: no data reported NJ Massachusetts: no data reported MA California: no data reported CA Utah: no data reported UT Colorado: no data reported CO Nebraska: no data reported NE Missouri: no data reported MO Kentucky: no data reported KY West Virginia: no data reported WV Virginia: no data reported VA Maryland: no data reported MD Connecticut: no data reported CT Rhode Island: no data reported RI Arizona: no data reported AZ New Mexico: no data reported NM Kansas: no data reported KS Arkansas: no data reported AR Tennessee: no data reported TN North Carolina: 550 units · 5.1 per 100k residents NC South Carolina: no data reported SC Delaware: no data reported DE Oklahoma: no data reported OK Louisiana: no data reported LA Mississippi: no data reported MS Alabama: no data reported AL Georgia: no data reported GA D.C.: no data reported DC Hawaii: no data reported HI Texas: no data reported TX Florida: no data reported FL
Units reimbursed · per 100k residents
5.15.5
gray = no data reported ⓘ
Colors are per 100,000 residents, so big states don’t automatically dominate. Tap or hover a state for its actual totals.
Tap or hover a state
…for its Medicaid breakdown
🏆 Top states by units · per 100k residents
1 Minnesota 5.5 /100k
2 North Carolina 5.1 /100k
National units — by quarter
💵 About the dollar figures: “reimbursed” is what Medicaid paid pharmacies before confidential manufacturer rebates, so the program’s real net cost is lower than these numbers. Fee-for-service and managed-care claims are combined unless split above. Source: CMS State Drug Utilization Data; per-100k rates use 2023 Census population estimates.

Medicaid utilization by pack size

Medicaid (SDUD) totals over the four most recent reported quarters for every package size of this drug — handy when a specific package (e.g. a starter/titration pack) carries little or no Medicaid volume on its own.
1 vial this page70069-0753-01 119 Rx · $239
25 vials70069-0753-25 16 Rx
10 vials70069-0753-10 11 Rx · $2
Drug total (last 4 qtrs): 146 Rx · 8,865 units · $241 gross reimbursed
Tap a pack size to open its page. Source: CMS State Drug Utilization Data, last 4 quarters.
← 70069-0752-25 · Somerset 70069-0758-04 · Somerset →
For educational and professional reference only — not medical advice. Pricing reflects published NADAC and CMS ASP (free public data) and may differ from your acquisition cost; always verify before billing or dispensing.