Lidocaine

Lidocaine	Last updated: 16/03/2023
(Also known as: lignocaine; xylestesin)

Data alerts

The following alerts are based on the data in the tables below. An absence of an alert does not imply the substance has no implications for human health, biodiversity or the environment but just that we do not have the data to form a judgement.

Environmental fate	Ecotoxicity	Human health
	Ecotoxicity Low alert: Fish acute ecotoxicity: Low; Daphnia acute ecotoxicity: Low Warning: Significant data are missing	Human health High alert: Reproduction/development effects; Neurotoxicant Warning: Significant data are missing

GENERAL INFORMATION

Description

A drug commonly used as a topical and local anesthetic

Availability status

Introduction & key dates

1943, first synthesised

Examples of species treated

Cats, Dogs, Cattle, Horses, Sheep, Pigs

Chemical structure

Isomerism

Chemical formula

C₁₄H₂₂N₂O

Canonical SMILES

CCN(CC)CC(=O)NC1=C(C=CC=C1C)C

Isomeric SMILES

No data

International Chemical Identifier key (InChIKey)

NNJVILVZKWQKPM-UHFFFAOYSA-N

International Chemical Identifier (InChI)

InChI=1S/C14H22N2O/c1-5-16(6-2)10-13(17)15-14-11(3)8-7-9-12(14)4/h7-9H,5-6,10H2,1-4H3,(H,15,17)

2D structure diagram/image available?

Yes

Cambridge Crystallographic Data Centre diagrams

Common Name	Relationship	Link
lidocaine	-

General status

Veterinary substance type

Anaesthetic, Medicinal drug

Substance groups

Unclassified substance

Minimum active substance purity

Known relevant impurities

Substance origin

Synthetic

Mode of action

Acts as a sodium channel blocker

Molecular targets

[Sodium channel protein type 10 subunit alpha, antagonist], [Sodium channel protein type 9 subunit alpha, antagonist], [Sodium channel protein type 5 subunit alpha, antagonist], [Epidermal growth factor receptor, antagonist]

CAS RN

137-58-6

EC number

205-302-8

CIPAC number

US EPA chemical code

PubChem CID

ATCvet Code

QN01BB52; QD08AE99

Therapeutic Class

Nervous system: Anaesthetic; Dermatologicals: Antiseptics & disinfectants

Controlled Drug?

Regulation 37/2010 MRL Classification

Allowed substance (Table 1: Equidae)

Molecular mass

234.34

PIN (Preferred Identification Name)

IUPAC name

2-(diethylamino)-N-(2,6-dimethylphenyl)acetamide

CAS name

N-(2,6-dimethylphenyl)-N2,N2-diethylglycinamide

Other status information

Relevant Environmental Water Quality Standards

Physical state

White to slightly yellow coloured crystalline powder

Formulations

Property

Product

Manufacturer

Authorisation Route

UK Legal Class

Example products using this active

Lignocaine and Adrenaline Solution for Injection

Norbrook Labs

UK National authorisation

Prescription only medicine to be authorised by suitably qualified person (POM-VPS)

Intubeaze 20 mg/ml Oromucosal spray

Dechra Ltd

UK National authorisation

Prescription only medicine to be authorised by a veterinarian (POM-V)

Locaine 2% w/v Solution for injection

Norbrook Labs

UK National authorisation (IC)

Prescription only medicine to be authorised by suitably qualified person (POM-VPS)

Otodex skin cream

Petlife International Ltd

UK National authorisation

Authorised veterinary medicine for general sale (AVM - GSL)

Formulation and application details

Supplied in a variety of formulations including creams and gels for topical application and solutions for injection

ENVIRONMENTAL FATE

Property

Value

Source; quality score; and other information

Interpretation

Solubility - In water at 20 °C (mg l⁻¹)

4100

High

Solubility - In organic solvents at 20 °C (mg l⁻¹)

Melting point (°C)

68.5

Boiling point (°C)

181

Degradation point (°C)

Flashpoint (°C)

Octanol-water partition coefficient at pH 7, 20 °C

2.75 X 10⁰²

Calculated

Log P

2.44

Low

Fat solubility of residues

Solubility

Data type

Density (g ml⁻¹)

Dissociation constant pKa) at 25 °C

7.86

Vapour pressure at 20 °C (mPa)

0.144

Low volatility

Henry's law constant at 25 °C (Pa m³ mol⁻¹)

Maximum UV-vis absorption L mol⁻¹ cm⁻¹

Surface tension (mN m⁻¹)

Refractive Index

Degradation

Property

Value

Source; quality score; and other information

Interpretation

Soil degradation (days) (aerobic)

DT₅₀ (typical)

DT₅₀ (lab at 20 °C)

DT₅₀ (field)

DT₉₀ (lab at 20 °C)

DT₉₀ (field)

Note

Manure DT₅₀ (days)

Aqueous photolysis DT₅₀ (days) at pH 7

Value

Note

Aqueous hydrolysis DT₅₀ (days) at 20 °C and pH 7

Value

Note

Water-sediment DT₅₀ (days)

Water phase only DT₅₀ (days)

Soil adsorption and mobility

Property

Value

Source; quality score; and other information

Interpretation

Linear

K_d

K_oc

Notes and range

Freundlich

K_f

K_foc

¹/_n

Notes and range

pH sensitivity

Fate indices

Property

Value

Source; quality score; and other information

Interpretation

GUS leaching potential index

Bio-concentration factor

BCF (l kg⁻¹)

Low risk

Based on LogP < 3

Low risk

CT₅₀ (days)

Known soil and groundwater metabolites

None

Other known metabolites

Metabolite name and reference

Aliases

Formation medium / Rate

Estimated maximum occurrence fraction

Metabolising enzymes

monoethylglycinexylidide
Note: Pharmacologically active

MEGX

Human (Liver)

Cytochrome P450 1A2
Cytochrome P450 3A4

N,N-diethylglycine-3-hydroxy-2,6,xylidide
Note: Pharmacologically active

glycine xylidide

Human (Liver); Rat

Cytochrome P450 1A2
Cytochrome P450 3A4

4-hydroxy-2,6-dimethylaniline

Human

ECOTOXICOLOGY

Terrestrial ecotoxicology

Property

Value

Source; quality score; and other information

Interpretation

Mammals - Acute oral LD₅₀ (mg kg⁻¹)

317

Rat

Moderate

Mammals - Short term dietary NOEL

(mg kg⁻¹)

(ppm diet)

Mammals - Chronic 21d NOAEL (mg kg⁻¹ bw d⁻¹)

Birds - Acute LD₅₀ (mg kg⁻¹)

Birds - Short term dietary (LC₅₀/LD₅₀)

Birds - Chronic 21d NOEL (mg kg⁻¹ bw d⁻¹)

Earthworms - Acute 14 day LC₅₀ (mg kg⁻¹)

Earthworms - Chronic NOEC, reproduction (mg kg⁻¹)

Soil micro-organisms

Collembola

Acute LC₅₀ (mg kg⁻¹)

Chronic NOEC (mg kg⁻¹)

Non-target plants

Honeybees (Apis spp.)

Contact acute LD₅₀ (worst case from 24, 48 and 72 hour values - μg bee⁻¹)

Oral acute LD₅₀ (worst case from 24, 48 and 72 hour values - μg bee⁻¹)

Unknown mode acute LD₅₀ (worst case from 24, 48 and 72 hour values - μg bee⁻¹)

Chronic

Bumblebees (Bombus spp.)

Contact acute LD₅₀ (worst case from 24, 48 and 72 hour values - μg bee⁻¹)

Oral acute LD₅₀ (worst case from 24, 48 and 72 hour values - μg bee⁻¹)

Mason bees (Osmia spp.)

Contact acute LD₅₀ (worst case from 24, 48 and 72 hour values - μg bee⁻¹)

Oral acute LD₅₀ (worst case from 24, 48 and 72 hour values - μg bee⁻¹)

Other bee species (1)

Acute LD₅₀ (worst case from 24, 48 and 72 hour values - μg insect⁻¹)

Mode of exposure

Other bee species (2)

Acute LD₅₀ (worst case from 24, 48 and 72 hour values - μg insect⁻¹)

Mode of exposure

Beneficial insects (Ladybirds)

Beneficial insects (Lacewings)

Beneficial insects (Parasitic wasps)

Beneficial insects (Predatory mites)

Beneficial insects (Ground beetles)

Aquatic ecotoxicology

Property

Value

Source; quality score; and other information

Interpretation

Fish - Acute 96 hour LC₅₀ (mg l⁻¹)

106

Danio rerio as LC0

Low

Fish - Chronic 21 day NOEC (mg l⁻¹)

Aquatic invertebrates - Acute 48 hour EC₅₀ (mg l⁻¹)

112

Daphnia magna

Low

Aquatic invertebrates - Chronic 21 day NOEC (mg l⁻¹)

Aquatic crustaceans - Acute 96 hour LC₅₀ (mg l⁻¹)

Sediment dwelling organisms - Acute 96 hour LC₅₀ (mg l⁻¹)

Sediment dwelling organisms - Chronic 28 day NOEC, static, water (mg l⁻¹)

Sediment dwelling organisms - Chronic 28 day NOEC, sediment (mg kg⁻¹)

Aquatic plants - Acute 7 day EC₅₀, biomass (mg l⁻¹)

Algae - Acute 72 hour EC₅₀, growth (mg l⁻¹)

Algae - Chronic 96 hour NOEC, growth (mg l⁻¹)

Mesocosm study data

NOEAEC mg l⁻¹

HUMAN HEALTH AND PROTECTION

General

Property

Value

Source; quality score; and other information

Interpretation

Threshold of Toxicological Concern (Cramer Class)

High (class III)

Mammals - Acute oral LD₅₀ (mg kg⁻¹)

317

Rat

Moderate

Mammals - Dermal LD₅₀ (mg kg⁻¹ body weight)

Mammals - Inhalation LC₅₀ (mg l⁻¹)

Other Mammal toxicity endpoints

Subcutaneous LD₅₀ = 335 mg kg⁻¹

Rat

Intraperitoneal LD₅₀ = 133 mg kg⁻¹

Rat

ADI - Acceptable Daily Intake (mg kg⁻¹ bw day⁻¹)

ARfD - Acute Reference Dose (mg kg⁻¹ bw day⁻¹)

AAOEL - Acute Acceptable Operator Exposure Level (mg kg⁻¹ bw day⁻¹)

AOEL - Acceptable Operator Exposure Level - Systemic (mg kg⁻¹ bw day⁻¹)

Dermal penetration studies (%)

Dangerous Substances Directive 76/464

Exposure Routes

Public

Occupational

Mammalian dose elimination route and rate

In humans & dogs, rapidly metabolised in the liver & around 75-95% eliminated in the urine as metabolites. Some is also is distributed in breast milk.

Health issues

Specific human health issues

Carcinogen

Genotoxic

Endocrine disruptor

No data found

; ; ; ;

No data found

Reproduction / development effects

Acetyl cholinesterase inhibitor

Neurotoxicant

No data found

Respiratory tract irritant

Skin irritant

Skin sensitiser

No data found

Eye irritant

Phototoxicant

No data found

General human health issues

May cause hypotension or cardiac suppression
May cause nausea and vomiting
Possible liver toxicant

Handling issues

Property

Value and interpretation

General

No information available

CLP classification 2013

WHO Classification

Not listed (Not listed)

UN Number

Waste disposal & packaging

Shelf-life, storage, stability and reactivity

TRANSLATIONS

Language

Name

English

lidocaine

French

German

Danish

Italian

xilocaina

Spanish

lidocaina

Greek

Polish

Swedish

Hungarian

Dutch

Norwegian

Record last updated:	16/03/2023
Contact:	aeru@herts.ac.uk
Please cite as:	Lewis, K.A., Tzilivakis, J., Warner, D. and Green, A. (2016) An international database for pesticide risk assessments and management. Human and Ecological Risk Assessment: An International Journal, 22(4), 1050-1064. DOI: 10.1080/10807039.2015.1133242