lidocaine indications/contra

Stem definitionDrug idCAS RN
local anaesthetics 1579 137-58-6

Description:

MoleculeDescription

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

Drug dosage:

DoseUnitRoute
3 g P

Approvals:

DateAgencyCompanyOrphan
Nov. 19, 1948 FDA FRESENIUS KABI USA

FDA Adverse Event Reporting System

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MedDRA adverse event termLikelihood ratioLikelihood ratio thresholdPatients taking drug having adverse eventPatients taking drug not having adverse eventPatients not taking drug having adverse eventPatients not taking drug not having adverse event
Product adhesion issue 1560.97 35.54 278 4938 1392 3379251
Product quality issue 985.26 35.54 326 4890 26409 3354234
Drug hypersensitivity 859.51 35.54 317 4899 35363 3345280
Drug ineffective 791.53 35.54 424 4792 115666 3264977
Cardiac arrest 743.74 35.54 266 4950 27053 3353590
Drug ineffective for unapproved indication 742.40 35.54 169 5047 3251 3377392
Toxicity to various agents 723.03 35.54 302 4914 46752 3333891
Methaemoglobinaemia 637.61 35.54 110 5106 432 3380211
Lagophthalmos 527.32 35.54 77 5139 55 3380588
Anaphylactic shock 493.06 35.54 135 5081 5604 3375039
Seizure 483.83 35.54 218 4998 40182 3340461
Anaesthetic complication 482.67 35.54 92 5124 693 3379950
Anaphylactic reaction 453.94 35.54 153 5063 12901 3367742
Generalised tonic-clonic seizure 435.11 35.54 132 5084 7910 3372733
Hypotension 423.61 35.54 212 5004 49302 3331341
Overdose 358.05 35.54 168 5048 33810 3346833
Bradycardia 333.71 35.54 130 5086 16539 3364104
Toxic anterior segment syndrome 324.64 35.54 62 5154 471 3380172
Respiratory arrest 260.83 35.54 98 5118 11270 3369373
Loss of consciousness 244.23 35.54 122 5094 28025 3352618
Myopathy toxic 226.45 35.54 38 5178 120 3380523
Incorrect route of drug administration 198.62 35.54 76 5140 9167 3371476
Cyanosis 195.06 35.54 64 5152 4922 3375721
Dizziness 182.38 35.54 146 5070 76366 3304277
Blood pressure decreased 181.87 35.54 80 5136 13756 3366887
Erythema 181.82 35.54 101 5115 28709 3351934
Tachycardia 181.30 35.54 94 5122 23277 3357366
Unresponsive to stimuli 176.18 35.54 67 5149 7941 3372702
Drug abuse 172.32 35.54 84 5132 18246 3362397
Arthritis bacterial 162.77 35.54 41 5175 1213 3379430

Pharmacologic Action:

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SourceCodeDescription
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 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
ATC N01BB52 NERVOUS SYSTEM
ANESTHETICS
ANESTHETICS, LOCAL
Amides
FDA EPC N0000175682 Amide Local Anesthetic
FDA Chemical/Ingredient N0000007681 Amides
FDA EPC N0000175426 Antiarrhythmic
FDA PE N0000175976 Local Anesthesia
MeSH PA D000777 Anesthetics
MeSH PA D000779 Anesthetics, Local
MeSH PA D000889 Anti-Arrhythmia Agents
CHEBI has role CHEBI:88188 drug allergen
CHEBI has role CHEBI:36333 local anaesthetic
CHEBI has role CHEBI:38070 anti-arrhythmia drug
MeSH PA D002317 Cardiovascular Agents
MeSH PA D002491 Central Nervous System Agents
MeSH PA D002492 Central Nervous System Depressants
MeSH PA D049990 Membrane Transport Modulators
MeSH PA D018373 Peripheral Nervous System Agents
MeSH PA D018689 Sensory System Agents
MeSH PA D026941 Sodium Channel Blockers
MeSH PA D061567 Voltage-Gated Sodium Channel Blockers

Drug Use (View source of the data)

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DiseaseRelationSNOMED_IDDOID
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
Local anesthetic intrathecal block indication 231249005
Skin irritation indication 367466007
Local anesthesia indication 386761002
Itching of skin indication 418363000
Local Anesthesia for Endotracheal Intubation indication
Local Anesthesia for Ophthalmologic Procedure indication
Mouth Irritation indication
Minor Skin Wound Pain indication
Regional Anesthesia for Ophthalmologic Surgery indication
Local Anesthesia for Urethral Pain indication
Prevent Minor Bacterial Skin Infection indication
Suppression of the Gag Reflex indication
Mycosis contraindication 3218000 DOID:1564
Gastritis contraindication 4556007 DOID:4029
Alcoholism contraindication 7200002
Psoriasis contraindication 9014002 DOID:8893
Bacterial septicemia contraindication 10001005
Sinus tachycardia contraindication 11092001
Measles contraindication 14189004 DOID:8622
Lowered convulsive threshold contraindication 19260006
Cirrhosis of liver contraindication 19943007 DOID:5082
Myocardial infarction contraindication 22298006 DOID:5844
Atopic dermatitis contraindication 24079001 DOID:3310
Abscess of intestine contraindication 24557004
Acute tuberculosis contraindication 25629007
Complete atrioventricular block contraindication 27885002
Shock contraindication 27942005
Hypovolemia contraindication 28560003
Parkinsonism contraindication 32798002 DOID:13548
Hyperthyroidism contraindication 34486009 DOID:7998
Gastrointestinal fistula contraindication 37831005
Hypertensive disorder contraindication 38341003 DOID:10763
Infectious disease contraindication 40733004
Gastrointestinal ulcer contraindication 40845000
Hypothyroidism contraindication 40930008 DOID:1459
Hypokalemia contraindication 43339004
Body fluid retention contraindication 43498006
Conduction disorder of the heart contraindication 44808001
Low blood pressure contraindication 45007003
Stokes-Adams syndrome contraindication 46935006
Chronic heart failure contraindication 48447003
Bradycardia contraindication 48867003
Atrial fibrillation contraindication 49436004 DOID:0060224
Disorder of cardiovascular system contraindication 49601007 DOID:1287
Sinus bradycardia contraindication 49710005
Vitamin K deficiency contraindication 52675005 DOID:11249
Nasal polyp contraindication 52756005
Acute nephropathy contraindication 58574008
Hepatic failure contraindication 59927004
Corneal opacity contraindication 64634000
Blood coagulation disorder contraindication 64779008 DOID:1247
Osteoporosis contraindication 64859006 DOID:11476
Cerebral arteriosclerosis contraindication 65312002
Psychotic disorder contraindication 69322001
Diabetes mellitus contraindication 73211009 DOID:9351
Factor II deficiency contraindication 73975000
Wolff-Parkinson-White pattern contraindication 74390002 DOID:384
Gastrointestinal hemorrhage contraindication 74474003
Thrombotic thrombocytopenic purpura contraindication 78129009 DOID:10772
Decreased respiratory function contraindication 80954004
Injury of head contraindication 82271004
Open-angle glaucoma contraindication 84494001 DOID:1067
Herpes simplex contraindication 88594005 DOID:8566
Cardiogenic shock contraindication 89138009
Kidney disease contraindication 90708001 DOID:2527
Thyrotoxicosis contraindication 90739004 DOID:7997
Hemophilia contraindication 90935002
Corneal ulcer contraindication 91514001 DOID:8463
Disorder of skin contraindication 95320005 DOID:37
Disorder of mucous membrane contraindication 95351003
Anemia due to enzyme deficiency contraindication 111577008
Magnetic resonance imaging contraindication 113091000
Open wound contraindication 125643001
Seizure disorder contraindication 128613002 DOID:1826
Bleeding contraindication 131148009
Ophthalmic herpes simplex contraindication 186542001
Angina pectoris contraindication 194828000
Primary dilated cardiomyopathy contraindication 195021004 DOID:12930
Partial atrioventricular block contraindication 195039008
Heart block contraindication 233916004
Anastomosis of intestine contraindication 235407009
Gastroesophageal reflux disease contraindication 235595009 DOID:8534
Disease of liver contraindication 235856003 DOID:409
Sepsis syndrome contraindication 238150007
Telangiectasia disorder contraindication 247479008 DOID:1272
Diverticulitis of gastrointestinal tract contraindication 271366000
Anemia contraindication 271737000 DOID:2355
Pregnancy, function contraindication 289908002
Varicella-zoster virus infection contraindication 309465005
Deficiency of cholinesterase contraindication 360607009
Adrenal cortical hypofunction contraindication 386584007 DOID:10493
Hypoxia contraindication 389086002
Angle-closure glaucoma contraindication 392291006 DOID:13550
Cardiovascular event risk contraindication 395112001
Pseudomembranous enterocolitis contraindication 397683000 DOID:0060185
Atrophoderma contraindication 399979006 DOID:2733
Peripheral vascular disease contraindication 400047006
Breastfeeding (mother) contraindication 413712001
Disorder of coronary artery contraindication 414024009
Denuded skin contraindication 418242004
Reduced Hepatic Blood Flow contraindication
Intracerebral Mass contraindication
Lidocaine Toxicity contraindication
Uncontrolled Epilepsy contraindication
Inflammatory dermatosis off-label use 703938007 DOID:2723

Acid dissociation constants calculated using MoKa v3.0.0

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Dissociation levelDissociation constantType (acidic/basic)
pKa1 13.4 acidic
pKa2 7.92 Basic

Orange Book patent data (new drug applications)

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Formulation strengthTrade nameApplicantApplication numberApproval dateTypeDose formRoutePatent numberPatent expiration datePatent use
3.5% AKTEN AKORN N022221 Oct. 7, 2008 RX GEL OPHTHALMIC 8759401 July 24, 2026 METHOD OF INDUCING TOPICAL ANESTHESIA IN THE EYE
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

Orange Book exclusivity data (new drug applications)

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Formulation strengthTrade nameApplicantApplication numberApproval dateTypeDose formRouteExclusivity dateDescription
1.8% ZTLIDO SCILEX PHARMS INC N207962 Feb. 28, 2018 RX PATCH TOPICAL Feb. 28, 2021 NEW PRODUCT

Bioactivity Summary:

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TargetClassPharosUniProtActionTypeActivity value
(-log[M])
Mechanism
action
Bioact sourceMoA source
Sodium channel protein type 2 subunit alpha Ion channel BLOCKER UNKNOWN CHEMBL
Sodium channel protein type 5 subunit alpha Ion channel BLOCKER Kd 4.80 IUPHAR CHEMBL
Sodium channel protein type 10 subunit alpha Ion channel BLOCKER UNKNOWN CHEMBL
Sodium channel protein type 4 subunit alpha Ion channel BLOCKER IC50 5.70 CHEMBL CHEMBL
Sodium channel protein type 9 subunit alpha Ion channel BLOCKER IC50 4.54 CHEMBL CHEMBL
Sodium channel protein type 3 subunit alpha Ion channel BLOCKER IC50 4.98 CHEMBL CHEMBL
Acetylcholine receptor Ion channel IC50 4.95 WOMBAT-PK
Potassium/sodium hyperpolarization-activated cyclic nucleotide-gated channel 4 Ion channel IC50 3.56 WOMBAT-PK
5-hydroxytryptamine receptor 3A Ion channel IC50 3.30 WOMBAT-PK
Sodium channel protein type X alpha subunit Unclassified BLOCKER IC50 4 IUPHAR
Sodium channel alpha subunits; brain (Types I, II, III) Ion channel IC50 4.25 CHEMBL
Sodium channel protein type 5 subunit alpha Unclassified BLOCKER IC50 4.20 IUPHAR

External reference:

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IDSource
DB00281 DRUGBANK_ID
2623 IUPHAR_LIGAND_ID
4018262 VUID
N0000146592 NUI
C0023660 UMLSCUI
D00358 KEGG_DRUG
CHEMBL79 ChEMBL_ID
3676 PUBCHEM_CID
6387 RXNORM
387480006 SNOMEDCT_US
82573000 SNOMEDCT_US
4977 MMSL
d00059 MMSL
4018262 VANDF
73102 MMSL
N0000006071 NDFRT
N0000146592 NDFRT
001350 NDDF
000626 NDDF
98PI200987 UNII
4202 INN_ID
CHEBI:6456 CHEBI
CHEMBL541521 ChEMBL_ID
CHEMBL1200409 ChEMBL_ID
73-78-9 SECONDARY_CAS_RN
D008012 MESH_DESCRIPTOR_UI
LQZ PDB_CHEM_ID

Pharmaceutical products:

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ProductCategoryIngredientsNDCFormQuantityRoute MarketingLabel
Lidocaine HUMAN OTC DRUG LABEL 1 0113-0135 AEROSOL, SPRAY 0.64 g TOPICAL OTC monograph not final 9 sections
Lidocaine and Prilocaine HUMAN PRESCRIPTION DRUG LABEL 2 0115-1468 CREAM 25 mg TOPICAL ANDA 13 sections
Lidocaine HUMAN PRESCRIPTION DRUG LABEL 1 0168-0204 OINTMENT 50 mg TOPICAL ANDA 12 sections
Lidocaine and Prilocaine HUMAN PRESCRIPTION DRUG LABEL 2 0168-0357 CREAM 25 mg TOPICAL ANDA 14 sections
Lidocaine Hydrochloride and Dextrose HUMAN PRESCRIPTION DRUG LABEL 2 0264-9594 INJECTION, SOLUTION 0.40 g INTRAVENOUS NDA 13 sections
Lidocaine Hydrochloride and Dextrose HUMAN PRESCRIPTION DRUG LABEL 2 0264-9598 INJECTION, SOLUTION 0.80 g INTRAVENOUS NDA 13 sections
PLIAGLIS HUMAN PRESCRIPTION DRUG LABEL 2 0299-6100 CREAM 70 mg TOPICAL NDA 16 sections
Lidocaine Hydrochloride and Dextrose HUMAN PRESCRIPTION DRUG LABEL 1 0338-0409 INJECTION, SOLUTION 4 mg INTRAVENOUS NDA 12 sections
Lidocaine Hydrochloride and Dextrose HUMAN PRESCRIPTION DRUG LABEL 1 0338-0411 INJECTION, SOLUTION 8 mg INTRAVENOUS NDA 12 sections
Lidocaine Hydrochloride and Dextrose HUMAN PRESCRIPTION DRUG LABEL 1 0338-9586 INJECTION 4 mg INTRAVENOUS Unapproved drug for use in drug shortage 2 sections
Lidocaine Hydrochloride and Dextrose HUMAN PRESCRIPTION DRUG LABEL 1 0338-9590 INJECTION 4 mg INTRAVENOUS Unapproved drug for use in drug shortage 2 sections
Lidocaine HUMAN PRESCRIPTION DRUG LABEL 1 0362-0221 OINTMENT 5 g TOPICAL ANDA 13 sections
Octocaine 50 HUMAN PRESCRIPTION DRUG LABEL 2 0362-9010 INJECTION, SOLUTION 20 mg SUBCUTANEOUS ANDA 12 sections
Octocaine 100 HUMAN PRESCRIPTION DRUG LABEL 2 0362-9023 INJECTION, SOLUTION 20 mg SUBCUTANEOUS ANDA 12 sections
Pain Relieving HUMAN OTC DRUG LABEL 1 0363-1112 PATCH 0.30 g TOPICAL OTC monograph not final 6 sections
Anorectal HUMAN OTC DRUG LABEL 1 0363-1114 CREAM 5 g TOPICAL OTC monograph final 6 sections
Pain and Itch Relief HUMAN OTC DRUG LABEL 1 0363-3001 CREAM 0.04 g TOPICAL OTC MONOGRAPH NOT FINAL 10 sections
Burn Relief Pain Reliever HUMAN OTC DRUG LABEL 1 0363-3107 SPRAY 0.50 g TOPICAL OTC monograph not final 6 sections
Walgreens Aloe Vera Burn Relief HUMAN OTC DRUG LABEL 1 0363-4000 GEL 0.50 g TOPICAL OTC monograph not final 7 sections
Walgreens Aloe Vera HUMAN OTC DRUG LABEL 2 0363-4003 GEL 0.50 g TOPICAL OTC monograph not final 7 sections
Walgreens HUMAN OTC DRUG LABEL 2 0363-4012 GEL 0.70 g TOPICAL OTC monograph not final 7 sections
Lidocaine HUMAN PRESCRIPTION DRUG LABEL 1 0378-9055 PATCH 140 mg CUTANEOUS ANDA 13 sections
Lidocaine-Prilocaine-Cream Base HUMAN PRESCRIPTION DRUG LABEL 2 0395-6110 CREAM 25 mg TOPICAL unapproved drug other 13 sections
Lidocaine HUMAN PRESCRIPTION DRUG LABEL 1 0440-9715 OINTMENT 50 mg TOPICAL ANDA 11 sections
LMX4 HUMAN OTC DRUG LABEL 1 0496-0882 CREAM 40 mg TOPICAL OTC monograph not final 9 sections
LMX5 HUMAN OTC DRUG LABEL 1 0496-0883 CREAM 50 mg TOPICAL OTC monograph final 8 sections
RECTICARE HUMAN OTC DRUG LABEL 1 0496-0892 CREAM 50 mg TOPICAL OTC monograph final 8 sections
Recticare Advanced HUMAN OTC DRUG LABEL 2 0496-0978 CREAM 50 mg TOPICAL OTC monograph final 8 sections
RECTICARE ADVANCED HUMAN OTC DRUG LABEL 3 0496-0979 CLOTH 50 mg TOPICAL OTC monograph final 9 sections
RECTICARE HUMAN OTC DRUG LABEL 2 0496-0980 CLOTH 50 mg TOPICAL OTC monograph final 7 sections