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lidocaine 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | BioActivity |

Stem definition	Drug id	CAS RN
local anaesthetics	1579	137-58-6

Description:

Molecule	Description
Molfile Inchi Smiles Synonyms: lignocaine lidocaine xylocain dalcaine duncaine esracaine solarcaine lidocaine hydrochloride lidocaine hydrochloride anhydrous lidocaine hydrochloride hydrate lidocaine HCl	A local anesthetic and cardiac depressant used as an antiarrhythmia agent. Its actions are more intense and its effects more prolonged than those of PROCAINE but its duration of action is shorter than that of BUPIVACAINE or PRILOCAINE. Molecular weight: 234.34 Formula: C14H22N2O CLOGP: 1.95 LIPINSKI: 0 HAC: 3 HDO: 1 TPSA: 32.34 ALOGS: -2.60 ROTB: 5 Status: OFP Legend: OFP - off patent OFM - off market ONP - on patent

Molecule

Description

Molfile Inchi Smiles

Synonyms:

lignocaine
lidocaine
xylocain
dalcaine
duncaine
esracaine
solarcaine
lidocaine hydrochloride
lidocaine hydrochloride anhydrous
lidocaine hydrochloride hydrate
lidocaine HCl

A local anesthetic and cardiac depressant used as an antiarrhythmia agent. Its actions are more intense and its effects more prolonged than those of PROCAINE but its duration of action is shorter than that of BUPIVACAINE or PRILOCAINE.

Molecular weight: 234.34
Formula: C14H22N2O
CLOGP: 1.95
LIPINSKI: 0
HAC: 3
HDO: 1
TPSA: 32.34
ALOGS: -2.60
ROTB: 5

Status: OFP

Legend:
OFP - off patent
OFM - off market
ONP - on patent

Drug dosage:

Dose	Unit	Route
3	g	P

ADMET properties:

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Property	Value	Reference
EoM (Fraction excreted unchanged in urine)	8 %	Benet LZ, Broccatelli F, Oprea TI
BA (Bioavailability)	35 %	Kim MT, Sedykh A, Chakravarti SK, Saiakhov RD, Zhu H
S (Water solubility)	3.58 mg/mL	Benet LZ, Broccatelli F, Oprea TI
MRTD (Maximum Recommended Therapeutic Daily Dose)	18.29 µM/kg/day	Contrera JF, Matthews EJ, Kruhlak NL, Benz RD
CL (Clearance)	16 mL/min/kg	Lombardo F, Berellini G, Obach RS
Vd (Volume of distribution)	1.80 L/kg	Lombardo F, Berellini G, Obach RS
t_half (Half-life)	1.60 hours	Lombardo F, Berellini G, Obach RS
BDDCS (Biopharmaceutical Drug Disposition Classification System)	1	Benet LZ, Broccatelli F, Oprea TI
fu (Fraction unbound in plasma)	0.33 %	Lombardo F, Berellini G, Obach RS

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Approvals:

Date	Agency	Company	Orphan
Nov. 19, 1948	FDA	FRESENIUS KABI USA

FDA Adverse Event Reporting System (Female)

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MedDRA adverse event term	Likelihood ratio	Likelihood ratio threshold	Patients taking drug having adverse event	Patients taking drug not having adverse event	Patients not taking drug having adverse event	Patients not taking drug not having adverse event
Product adhesion issue	1104.60	9.47	377	101462	4342	63382841
Local anaesthetic systemic toxicity	566.88	9.47	154	101685	745	63386438
Product quality issue	457.27	9.47	412	101427	35453	63351730
Sinusitis	370.27	9.47	993	100846	225660	63161523
Infusion site pain	295.92	9.47	233	101606	16636	63370547
Infusion site swelling	285.02	9.47	184	101655	9586	63377597
Pemphigus	258.26	9.47	8	101831	183718	63203465
Toxic anterior segment syndrome	255.44	9.47	99	101740	1672	63385511
Contraindicated product administered	241.14	9.47	32	101807	217616	63169567
Infusion site extravasation	231.83	9.47	166	101673	10260	63376923

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FDA Adverse Event Reporting System (Male)

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MedDRA adverse event term	Likelihood ratio	Likelihood ratio threshold	Patients taking drug having adverse event	Patients taking drug not having adverse event	Patients not taking drug having adverse event	Patients not taking drug not having adverse event
Product adhesion issue	397.65	10.39	131	51445	1469	34903886
Anaphylactic shock	289.07	10.39	217	51359	15724	34889631
Methaemoglobinaemia	244.64	10.39	115	51461	3466	34901889
Anaphylactic reaction	215.74	10.39	252	51324	32049	34873306
Anaesthetic complication	197.69	10.39	71	51505	1049	34904306
Local anaesthetic systemic toxicity	180.51	10.39	49	51527	261	34905094
Cardiac arrest	148.88	10.39	392	51184	95767	34809588
Product quality issue	145.04	10.39	151	51425	16884	34888471
Sinusitis	134.97	10.39	229	51347	41173	34864182
Toxic anterior segment syndrome	126.87	10.39	52	51524	1117	34904238

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FDA Adverse Event Reporting System (Geriatric)

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MedDRA adverse event term	Likelihood ratio	Likelihood ratio threshold	Patients taking drug having adverse event	Patients taking drug not having adverse event	Patients not taking drug having adverse event	Patients not taking drug not having adverse event
Product adhesion issue	706.44	9.42	230	117573	2474	79624111
Local anaesthetic systemic toxicity	691.00	9.42	183	117620	871	79625714
Anaphylactic shock	487.32	9.42	413	117390	35583	79591002
Anaphylactic reaction	445.40	9.42	583	117220	83160	79543425
Anaesthetic complication	393.39	9.42	151	117652	2708	79623877
Toxic anterior segment syndrome	383.95	9.42	147	117656	2617	79623968
Cardiac arrest	331.99	9.42	764	117039	171332	79455253
Methaemoglobinaemia	262.54	9.42	139	117664	5418	79621167
Product quality issue	248.53	9.42	278	117525	33662	79592923
Lagophthalmos	220.84	9.42	62	117741	381	79626204

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FDA Adverse Event Reporting System (Pediatric)

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MedDRA adverse event term	Likelihood ratio	Likelihood ratio threshold	Patients taking drug having adverse event	Patients taking drug not having adverse event	Patients not taking drug having adverse event	Patients not taking drug not having adverse event
Methaemoglobinaemia	67.18	54.14	13	24	68	89687

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Pharmacologic Action:

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Source	Code	Description
ATC	C01BB01	CARDIOVASCULAR SYSTEM CARDIAC THERAPY ANTIARRHYTHMICS, CLASS I AND III Antiarrhythmics, class Ib
ATC	C05AD01	CARDIOVASCULAR SYSTEM VASOPROTECTIVES AGENTS FOR TREATMENT OF HEMORRHOIDS AND ANAL FISSURES FOR TOPICAL USE Local anesthetics
ATC	D04AB01	DERMATOLOGICALS ANTIPRURITICS, INCL. ANTIHISTAMINES, ANESTHETICS, ETC. ANTIPRURITICS, INCL. ANTIHISTAMINES, ANESTHETICS, ETC. Anesthetics for topical use
ATC	N01BB02	NERVOUS SYSTEM ANESTHETICS ANESTHETICS, LOCAL Amides
ATC	N01BB52	NERVOUS SYSTEM ANESTHETICS ANESTHETICS, LOCAL Amides
ATC	R02AD02	RESPIRATORY SYSTEM THROAT PREPARATIONS THROAT PREPARATIONS Anesthetics, local
ATC	S01HA07	SENSORY ORGANS OPHTHALMOLOGICALS LOCAL ANESTHETICS Local anesthetics
ATC	S02DA01	SENSORY ORGANS OTOLOGICALS OTHER OTOLOGICALS Analgesics and anesthetics
CHEBI has role	CHEBI:35703	Xenobiotic
CHEBI has role	CHEBI:36333	local anesthetics

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Drug Use | Suggest Off label Use Form| |View source of the data|

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Disease	Relation	SNOMED_ID	DOID
Postherpetic neuralgia	indication	2177002
Neuralgia	indication	16269008
Urethritis	indication	31822004	DOID:1343
Premature ejaculation	indication	44001008	DOID:13709
Ventricular arrhythmia	indication	44103008
Hemorrhoids	indication	70153002	DOID:9746
Infestation by Phthirus pubis	indication	71011005	DOID:13760
Pediculosis capitis	indication	81000006	DOID:5501
Pruritus ani	indication	90446007
Infestation by Sarcoptes scabiei var hominis	indication	128869009	DOID:8295

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🐶 Veterinary Drug Use

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Species	Use	Relation
Dogs	Urinary tract infections caused by Hemolytic Staphylococcus species	Indication
Dogs	Urinary tract infections caused by Streptococcus species	Indication
Dogs	Bacterial pulmonary infections caused by Brucella bronchiseptica	Indication
Dogs	Bacterial pulmonary infections caused by Streptococcus pyogenes	Indication
Dogs	Bacterial pulmonary infections caused by Staphylococcus aureus	Indication
Dogs	Secondary bacterial infections caused by Micrococcus pyogenes var albus	Indication
Dogs	Secondary bacterial infections caused by Brucella bronchiseptica	Indication
Dogs	Secondary bacterial infections caused by Streptococcus species	Indication

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🐶 Veterinary products

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Product	Applicant	Ingredients
Aquachel 100 mg	Zoetis Inc.	2
Liquamycin Intramuscular	Zoetis Inc.	2
Tributame Euthanasia Solution	Cronus Pharma Specialities India Private Limited	3

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Acid dissociation constants calculated using MoKa v3.0.0

Dissociation level	Dissociation constant	Type (acidic/basic)
pKa1	13.4	acidic
pKa2	7.92	Basic

Orange Book patent data (new drug applications)

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Formulation strength	Trade name	Applicant	Application number	Approval date	Type	Dose form	Route	Patent number	Patent expiration date	Patent use
0.5MG	ZINGO	POWDER PHARMS	N022114	Aug. 16, 2007	RX	SYSTEM	INTRADERMAL	8540665	Oct. 22, 2029	ZINGO INTRADERMAL INJECTION SYSTEM IS A DRUG DELIVERY SYSTEM THAT IS CAPABLE OF DELIVERING FINE DRY POWDERED LIDOCAINE HYDROCHLORIDE MONOHYDRATE FOR LOCAL ANESTHETIC ACTION
0.5MG	ZINGO	POWDER PHARMS	N022114	Aug. 16, 2007	RX	SYSTEM	INTRADERMAL	9358338	April 27, 2035	ZINGO IS A POWDER INTRADERMAL SYSTEM THAT IS CAPABLE OF DELIVERING FINE DRY POWDERED LIDOCAINE HYDROCHLORIDE MONOHYDRATE FOR LOCAL ANESTHETIC ACTION
0.5MG	ZINGO	POWDER PHARMS	N022114	Aug. 16, 2007	RX	SYSTEM	INTRADERMAL	9370622	Sept. 28, 2035	ZINGO IS A POWDER INTRADERMAL SYSTEM THAT IS CAPABLE OF DELIVERING FINE DRY POWDERED LIDOCAINE HYDROCHLORIDE MONOHYDRATE FOR LOCAL ANESTHETIC ACTION
1.8%	ZTLIDO	SCILEX PHARMS	N207962	Feb. 28, 2018	RX	PATCH	TOPICAL	9925264	May 10, 2031	METHOD FOR RELIEVING THE PAIN ASSOCIATED WITH POST-HERPETIC NEURALGIA
3.5%	AKTEN	THEA PHARMA	N022221	Oct. 7, 2008	RX	GEL	OPHTHALMIC	8759401	July 24, 2026	METHOD OF INDUCING TOPICAL ANESTHESIA IN THE EYE

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Orange Book exclusivity data (new drug applications)

None

Bioactivity Summary:

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Target	Class	Pharos	UniProt	Action	Type	Activity value (-log[M])	Bioact source	MoA source
Sodium channel protein type 5 subunit alpha	Ion channel	Q14524	SCN5A_HUMAN	BLOCKER	Kd	4.80	IUPHAR	CHEMBL
Sodium channel protein type 2 subunit alpha	Ion channel	Q99250	SCN2A_HUMAN	BLOCKER			UNKNOWN	CHEMBL
Sodium channel protein type 3 subunit alpha	Ion channel	Q9NY46	SCN3A_HUMAN	BLOCKER	IC50	4.98	CHEMBL	CHEMBL
Sodium channel protein type 4 subunit alpha	Ion channel	P35499	SCN4A_HUMAN	BLOCKER	IC50	5.70	CHEMBL	CHEMBL
Sodium channel protein type 9 subunit alpha	Ion channel	Q15858	SCN9A_HUMAN	BLOCKER	IC50	4.54	CHEMBL	CHEMBL
Sodium channel protein type 10 subunit alpha	Ion channel	Q9Y5Y9	SCNAA_HUMAN	BLOCKER			UNKNOWN	CHEMBL
Potassium/sodium hyperpolarization-activated cyclic nucleotide-gated channel 4	Ion channel	Q9Y3Q4	HCN4_HUMAN		IC50	3.56	WOMBAT-PK
Acetylcholine receptor	Ion channel	P02708 P11230 Q07001	ACHA_HUMAN ACHB_HUMAN ACHD_HUMAN		IC50	4.96	WOMBAT-PK
5-hydroxytryptamine receptor 3A	Ion channel	P46098	5HT3A_HUMAN		IC50	3.30	WOMBAT-PK
Sodium channel protein type 5 subunit alpha	Ion channel		SCN5A_RAT	BLOCKER	IC50	4.20	IUPHAR

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External reference:

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ID	Source
000626	NDDF
000627	NDDF
001350	NDDF
001351	NDDF
1269131003	SNOMEDCT_US
1299236	RXNORM
14031	MMSL
2623	IUPHAR_LIGAND_ID
3676	PUBCHEM_CID
387480006	SNOMEDCT_US

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Pharmaceutical products:

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Product	Category	Ingredients	NDC	Form	Quantity	Route	Marketing	Label
ABREVARapid Pain Relief	HUMAN OTC DRUG LABEL	2	0135-0400	GEL	40 mg	TOPICAL	OTC monograph final	14 sections
basic care endure	HUMAN OTC DRUG LABEL	1	0113-7200	SPRAY	10 mg	TOPICAL	OTC monograph final	16 sections
basic care lidocaine	HUMAN OTC DRUG LABEL	1	0113-7219	PATCH	560 mg	TOPICAL	OTC monograph not final	14 sections
basic care lidocaine	HUMAN OTC DRUG LABEL	1	0113-7219	PATCH	560 mg	TOPICAL	OTC monograph not final	14 sections
basic care lidocaine	HUMAN OTC DRUG LABEL	1	0113-7700	PATCH	560 mg	TOPICAL	OTC monograph not final	14 sections
Good Sense endure	HUMAN OTC DRUG LABEL	1	0113-8000	SPRAY	10 mg	TOPICAL	OTC monograph final	16 sections
Lidocaine	HUMAN PRESCRIPTION DRUG LABEL	1	0143-9575	INJECTION, SOLUTION	20 mg	INFILTRATION	ANDA	12 sections
Lidocaine	HUMAN PRESCRIPTION DRUG LABEL	1	0143-9576	INJECTION, SOLUTION	20 mg	INFILTRATION	ANDA	12 sections
Lidocaine	HUMAN PRESCRIPTION DRUG LABEL	1	0143-9577	INJECTION, SOLUTION	10 mg	INFILTRATION	ANDA	12 sections
Lidocaine	HUMAN PRESCRIPTION DRUG LABEL	1	0143-9578	INJECTION, SOLUTION	10 mg	INFILTRATION	ANDA	12 sections

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