Overview
Ever since its discovery and availability for sale and use in the late 1940s, lidocaine has become an exceptionally commonly used medication . In particular, lidocaine's principal mode of action in acting as a local anesthetic that numbs the sensations of tissues means the agent is indicated for facilitating local anesthesia for a large variety of surgical procedures . It ultimately elicits its numbing activity by blocking sodium channels so that the neurons of local tissues that have the medication applied on are transiently incapable of signaling the brain regarding sensations . In doing so, however, it can block or decrease muscle contractile, resulting in effects like vasodilation, hypotension, and irregular heart rate, among others . As a result, lidocaine is also considered a class Ib anti-arrhythmic agent . Nevertheless, lidocaine's local anesthetic action sees its use in many medical situations or circumstances that may benefit from its action, including the treatment of premature ejaculation . Regardless, lidocaine is currently available as a relatively non-expensive generic medication that is written for in millions of prescriptions internationally on a yearly basis. It is even included in the World Health Organization's List of Essential Medicines .
Indication
Lidocaine is an anesthetic of the amide group indicated for production of local or regional anesthesia by infiltration techniques such as percutaneous injection and intravenous regional anesthesia by peripheral nerve block techniques such as brachial plexus and intercostal and by central neural techniques such as lumbar and caudal epidural blocks .
Associated Conditions
- Acute Otitis Media (AOM)
- Anorectal discomfort
- Arrhythmia
- Back Pain Lower Back
- Bacterial Vaginosis (BV)
- Burns
- Cervical Syndrome
- Earache
- Fissure;Anal
- Haemorrhoids
- Infection
- Inflammatory Reaction caused by ear infection-not otherwise specified
- Insect Bites
- Joint Pain
- Mixed Vaginal Infections
- Multiple Myeloma (MM)
- Myringitis
- Neuritis
- Osteolysis caused by Bone Tumors
- Osteoporosis
- Otitis Externa
- Pain caused by ear infection-not otherwise specified
- Pain, Inflammatory
- Postherpetic Neuralgia
- Primary Hyperparathyroidism (PHPT)
- Rheumatic Diseases
- Rheumatic Joint Disease
- Sciatica
- Skin Irritation
- Soft Tissue Inflammation
- Sore Throat
- Sunburn
- Susceptible infections
- Trichomonas Vaginitis
- Ulcers, Leg
- Urethral Strictures
- Ventricular Arrhythmia
- Vulvovaginal Candidiasis
- Abrasions
- Anal discomfort
- Cutaneous lesions
- Gum pain
- Minor burns
- Superficial Wounds
- Susceptible Bacterial Infections
- Ulceration of the mouth
- Viral infections of the external ear canal
Research Report
Lidocaine: A Comprehensive Pharmacological Report
1. Introduction to Lidocaine
1.1. Overview and Historical Context
Lidocaine, also known by its alternative name lignocaine, stands as a cornerstone medication in modern medicine, primarily recognized for its efficacy as an amino amide-type local anesthetic and as a Class Ib antiarrhythmic agent.[1] Its discovery in 1943 by Swedish chemists Nils Löfgren and Bengt Lundqvist, and subsequent introduction to the market around 1948-1949, represented a significant advancement in pharmacology.[2] Compared to its predecessors, such as procaine (Novocain), lidocaine offered a more rapid onset of action, greater potency, and a considerably lower potential for allergic reactions, leading to its swift adoption in clinical practice.[1] The initial brand name for lidocaine was Xylocaine.[5]
The enduring clinical relevance of lidocaine, decades after its introduction, is a testament to its favorable balance of efficacy, safety (when used appropriately), and cost-effectiveness. This is particularly evident when considering its widespread use for fundamental anesthetic needs and specific cardiac arrhythmias, where newer agents have not universally surpassed its utility. This long-standing prominence is further underscored by its consistent inclusion in the World Health Organization's (WHO) List of Essential Medicines, signifying its critical role in basic healthcare systems globally.[1] As an indicator of its continued importance, lidocaine was the 262nd most commonly prescribed medication in the United States in 2022.[2] The early and extensive clinical experience gained under the Xylocaine brand likely established a strong foundation of trust and familiarity among medical practitioners, contributing to its sustained use even after the advent of generic versions.[5] This illustrates how initial market presence and robust branding can significantly influence a drug's long-term therapeutic legacy.
Clinical Trials
Title | Posted | Study ID | Phase | Status | Sponsor |
---|---|---|---|---|---|
2025/07/11 | Not Applicable | Recruiting | |||
2025/07/08 | Not Applicable | Not yet recruiting | |||
2025/07/02 | Not Applicable | Recruiting | |||
2025/06/29 | Not Applicable | Not yet recruiting | Rennes University Hospital | ||
2025/06/25 | Not Applicable | Recruiting | Harbin Medical University | ||
2025/06/24 | Phase 4 | Recruiting | |||
2025/06/10 | Not Applicable | Not yet recruiting | Medical University of Warsaw | ||
2025/05/21 | Phase 1 | Not yet recruiting | |||
2025/05/18 | Phase 3 | Recruiting | |||
2025/05/16 | Not Applicable | Recruiting |
FDA Drug Approvals
Approved Product | Manufacturer | NDC Code | Route | Strength | Effective Date |
---|---|---|---|---|---|
Medical Purchasing Solutions, LLC | 71872-7301 | INTRAVENOUS | 20 mg in 1 mL | 4/17/2023 | |
Fresenius Kabi USA, LLC | 63323-201 | INFILTRATION, PERINEURAL | 10 mg in 1 mL | 8/5/2022 | |
Bryant Ranch Prepack | 72162-2084 | TOPICAL | 50 mg in 1 g | 9/14/2023 | |
Preferred Pharmaceuticals Inc. | 68788-8129 | TOPICAL | 4.5 g in 100 g | 7/21/2023 | |
Actavis Pharma, Inc. | 0591-2070 | TOPICAL | 25 mg in 1 g | 7/31/2019 | |
A-S Medication Solutions | 50090-4538 | TOPICAL | 20 mg in 1 mL | 11/29/2016 | |
Dentsply Pharmaceutical | 66312-110 | PERIODONTAL | 25 mg in 1 g | 1/26/2024 | |
PAI Holdings, LLC | 0121-0972 | TOPICAL | 40 mg in 1 mL | 10/24/2023 | |
International Medication Systems, Limited | 76329-3011 | TOPICAL | 20 mg in 1 mL | 11/29/2016 | |
Fresenius Kabi USA, LLC | 63323-208 | INTRAVENOUS | 20 mg in 1 mL | 8/5/2022 |
EMA Drug Approvals
Approved Product | Authorization Holder | Status | Issued Date |
---|---|---|---|
Authorised | 11/15/2013 |
HSA Drug Approvals
Approved Product | Manufacturer | Approval Number | Dosage Form | Strength | Approval Date |
---|---|---|---|---|---|
Vagisil Medicated Creme | SIN10494P | CREAM | 2% w/w | 12/3/1998 | |
XYLOTIN 50 - Lidocaine Hydrochloride INJECTION USP 50MG/5ML | SIN15952P | INJECTION, SOLUTION | 50mg/5ml | 6/12/2020 | |
LIGNOCAINE INJECTION 2% (Without preservative) | SIN05673P | INJECTION | 20 mg/ml | 4/8/1991 | |
DENTINOX TEETHING GEL | SIN04042P | GEL | 0.33% w/w | 3/28/1990 | |
LYDOCAN INJECTION 2% | SIN15519P | INJECTION, SOLUTION | 200mg/10ml | 8/1/2018 | |
LIGNOCAINE HYDROCHLORIDE INJECTION BP 1% (WITHOUT PRESERVATIVE) | SIN05671P | INJECTION | 10 mg/ml | 4/8/1991 | |
XYLOCAINE JELLY 2% | SIN05684P | GEL | 20 mg/g | 4/8/1991 | |
XYLOCAINE PUMP SPRAY 10% | SIN06984P | SPRAY | 10 mg/dose | 4/27/1992 | |
XYLOCAINE OINTMENT 5% | SIN05683P | OINTMENT | 5g/100g | 4/8/1991 | |
Trachisan Forte Lozenge | SIN13276P | LOZENGE | 8mg | 5/17/2007 |
NMPA Drug Approvals
Approved Product | Company | Approval Number | Drug Type | Dosage Form | Approval Date |
---|---|---|---|---|---|
Lidocaine Hydrochloride Powder Intradermal Injection System | powder pharmaceuticals, inc. | 国药准字HJ20220012 | 化学药品 | 注射剂 | 3/1/2022 |
利多卡因气雾剂 | 国药准字H10920107 | 化学药品 | 气雾剂 | 6/19/2020 | |
Lidocaine Cataplasms | 国药准字H20180007 | 化学药品 | 贴膏剂 | 3/23/2023 | |
Lidocaine Cataplasms | 国药准字H20243065 | 化学药品 | 贴膏剂 | 1/23/2024 | |
Lidocaine Cataplasms | 国药准字HJ20240019 | 化学药品 | 贴膏剂 | 5/8/2024 | |
Lidocaine Cataplasms | 国药准字H20254079 | 化学药品 | 贴膏剂 | 5/13/2025 | |
Lidocaine Hydrochloride and Glucose Injection | 国药准字H10980209 | 化学药品 | 注射剂(注射液) | 9/27/2020 | |
Lidocaine Hydrochloride Mucilage(Ⅰ) | 国药准字H20084433 | 化学药品 | 口服溶液剂 | 7/25/2023 | |
Lidocaine Hydrochloride Mucilage(Ⅰ) | 国药准字H20065325 | 化学药品 | 胶浆剂 | 8/25/2020 | |
Lidocaine Hydrochloride Mucilage(Ⅰ) | 国药准字H13021217 | 化学药品 | 胶浆剂 | 7/21/2020 |
PPB Drug Approvals
Approved Product | Registration No. | Company | Licence No. | Strength | Registration Date |
---|---|---|---|---|---|
ZINTOIN CREAM | N/A | N/A | N/A | 5/31/1986 | |
DIFFLAM WITH ANAESTHETIC SORE THROAT LOZENGES MENTHOL & EUCALYPTUS FLAVOUR | N/A | N/A | N/A | 5/27/2022 | |
EURORECTAL OINTMENT | N/A | N/A | N/A | 2/16/1995 | |
BETOCAINE CREAM | N/A | N/A | N/A | 4/2/1990 | |
HI-VETIC A OINT | N/A | N/A | N/A | 5/18/1984 | |
MUCOCARE GEL | N/A | N/A | N/A | 11/19/2007 | |
TOOTHACHE TINCTURE | N/A | N/A | N/A | 8/13/1996 | |
AVEDIAN CREAM | N/A | N/A | N/A | 3/25/2007 | |
XYLMOL SUPPOSITORY | N/A | N/A | N/A | 6/29/2000 | |
MOUTHCIN ORAL GEL | N/A | N/A | N/A | 9/24/1999 |
TGA Drug Approvals
Approved Product | ARTG ID | Sponsor | Registration Type | Status | Registration Date |
---|---|---|---|---|---|
SM 33 ADULT FORMULA LIQUID paint bottle | 12181 | Pharmaco Australia Ltd | Medicine | A | 8/9/1991 |
HEMADERM HAEMORRHOIDAL ointment tube | 50548 | Milpharma Pty Ltd | Medicine | A | 10/13/1994 |
EMLA 5% CREAM (kit) | 12046 | Medicine | A | 8/13/1991 | |
Lignocaine Hydrochloride Injection 2% 100 mg in 5 mL | 279223 | Medicine | A | 8/16/2016 | |
STREPSILS ANAESTHETIC THROAT SPRAY bottle | 55908 | Medicine | A | 6/13/1996 | |
LMX 4 TOPICAL ANAESTHETIC CREAM lidocaine (lignocaine) 40 mg/g tubes with dressings | 208815 | Medicine | A | 4/29/2013 | |
XYLOCAINE 5% OINTMENT lidocaine (lignocaine) 50mg/g tube (Reformulation) | 215796 | Medicine | A | 10/9/2013 | |
LIDOCAINE INTAS 1% lidocaine hydrochloride 50 mg/5 mL injection ampoule | 309522 | Medicine | A | 9/20/2019 | |
LIDOCAINE ACCORD 1% lidocaine hydrochloride 50 mg/5 mL injection ampoule | 309529 | Medicine | A | 9/20/2019 | |
XYLONOR GEL tube | 20750 | Medicine | A | 10/2/1991 |
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