API: Lidocaine Hydrochloride

What Is Lidocaine Hydrochloride and How Does It Work?

Lidocaine hydrochloride is an amide anesthetic that can be delivered topically, via injection, or by inhalation. The drug works by blocking sodium channels across the membranes of post-synaptic neurons, thereby stopping or mediating neuronal impulses and effecting local anesthetic action.1 This anesthetic property makes lidocaine hydrochloride a preferred drug to treat topical bites, burns, and rashes, and as a local surgical anesthetic when delivered intravenously. Lidocaine hydrochloride’s ability to block sodium channels can also affect the action potential of cardiac cells, making the drug suitable to treat ventricular tachycardia.

For more information, including a MSDS sheet, please see PNA’s Lidocaine Hydrochloride page.

Approved Indications

  • Topical anesthetic: Topical preparations of lidocaine hydrochloride, typically as a solution, gel, dermal patch, or ointment, can be used to treat a variety of minor burns, skin rashes, insect bites, and other irritations of the skin and mucous membranes. The drug can provide pain control and relief before surgical procedures and be used as an anesthetic lubricant for endotracheal intubation.2
  • Injection: Lidocaine hydrochloride can be used as a local anesthetic when delivered by percutaneous injection or intravenously. The drug may also be used as a nerve block.3
  • Aerosol: Delivered as a spray, lidocaine hydrochloride can also be used as a local anesthetic for the interior of the larynx and trachea.
  • Anti-arrhythmic Injection: Lidocaine hydrochloride delivered intravenously can be used in the acute management of ventricular arrhythmias due to acute myocardial infarction or cardiac surgery.4

Side Effects and Drug Interactions

Common side effects in patients taking lidocaine hydrochloride vary depending on method of delivery. For topical and spray use, side effects were limited to administration site and include5:

  • Burning or irritation of skin
  • Rash
  • Dermatitis
  • Erythema
  • Pruritus
  • Skin vesicles

Patients who suffer from severity of these common side effects should contact their pharmacist or physician right away. Patients who experience blistering or crusting of skin, cracked or scaly skin, rapid heartbeat, fever, hives or welts, hoarseness, joint pain, stiffness, or swelling, swelling of the face, eyelids, lips, tongue, throat, hands, legs, feet, or sex organs, trouble breathing or swallowing, rapid weight gain, tinnitus, numbness or tingling, blurred or double vision, burning when urinating or loss of bladder control, pain in upper stomach, or congestive heart failure symptoms should inform their physician immediately.

With lidocaine hydrochloride injections, common side effects include6:

  • Mild bruising, redness, itching, or swelling at injection site
  • Dizziness
  • Nausea
  • Numbness in area where the medicine was accidentally applied

Patients who suffer from severity of these common side effects should contact their pharmacist or physician right away. Patients who experience signs of a severe allergic reaction (including hives, difficulty breathing, swelling of the face, lips, tongue, or throat), anxiety, depression, vomiting, tinnitus, blurred vision, confusion, twitching, seizure (convulsions), rapid heart rate or breathing, feeling hot or cold, weak or shallow breathing, slow heart rate, weak pulse, or light headedness should inform their physician immediately.

Patients who are allergic to lidocaine hydrochloride should not take this drug. Topical and spray lidocaine hydrochloride have known interactions with sodium nitrite/sodium thiosulfate, prilocaine, epinephrine, and amyl nitrite. Injected lidocaine hydrochloride should not be used if patient is taking anesthetic solutions containing epinephrine or norepinephrine, monoamine oxidase inhibitors, or tricyclic antidepressants, phenothiazines, butyrophenones, vasopressor drugs, and ergot-type oxytocic drugs.

Latest News and Research

Lidocaine hydrochloride was developed in 1948 and is currently on the World Health Organization’s (WHO) List of Essential Medicines.7 This list, which is updated every two years, includes drugs that the WHO defines to “satisfy the health care needs of the majority of the population; they should therefore be available at all times in adequate amounts and in appropriate dosage forms, at a price the community can afford.”

One direction of current research is the investigation of delivering lidocaine transdermally, which would offer the ability to modulate the bioavailability of drugs for percutaneous administration while also providing the ability for exudate absorption and adherence of the patch to irregular skin surfaces in an open wound situation.8 Another method of drug delivery under study is a bioadhesive that would allow perfusion of lidocaine through oral mucosa.9 The drug is also under study for treatment of interstitial cystitis delivered through an intravesical drug delivery system. Such a device offers pain relief that is maintained for several months after the device is removed.10

Buying Guide

PNA is a recommended bulk supplier of Lidocaine Hydrochloride and other APIs. You can learn more about Lidocaine Hydrochloride here.

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Resources

Show 10 footnotes

  1. “LABEL: LIDOCAINE HYDROCHLORIDE- lidocaine hydrochloride injection, solution,” http://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?setid=44bdda18-4f41-4599-8a28-b5831a320eb1
  2. “Lidocaine Jelly,” December 1, 2015, http://www.drugs.com/pro/lidocaine-jelly.html
  3. Lidocaine Injection,” December 1, 2015, http://www.drugs.com/pro/lidocaine-injection.html
  4. “xylocaine (Lidocaine hydrochloride) injection,”  May 2008, https://dailymed.nlm.nih.gov/dailymed/archives/fdaDrugInfo.cfm?archiveid=8267
  5. “Lidocaine topical Side Effects,” December 1, 2015, http://www.drugs.com/sfx/lidocaine-topical-side-effects.html
  6. “Xylocaine,” 2016, http://www.rxlist.com/xylocaine-drug/patient-images-side-effects.htm
  7. “WHO Model Lists of Essential Medicines,” August 2015, http://www.who.int/medicines/publications/essentialmedicines/en/
  8. “Bacterial cellulose membranes applied in topical and transdermal delivery of lidocaine hydrochloride and ibuprofen: In vitro diffusion studies,” October 1, 2012, http://www.sciencedirect.com/science/article/pii/S0378517312000063
  9. “Development and Evaluation of a Bioadhesive System for Oral Mucosa Delivery of Lidocaine Hydrochloride,” August 2013, https://www.researchgate.net/profile/Cesar_Serna_Jimenez/publication/263920074_Development_and_Evaluation_of_a_Bioadhesive_System_for_Oral_Mucosa_Delivery_of_Lidocaine_Hydrochloride/links/02e7e53c51c1472eff000000.pdf
  10. “Continuous intravesical lidocaine treatment for interstitial cystitis/bladder pain syndrome: safety and efficacy of a new drug delivery device,” July 18, 2012, http://www.ncbi.nlm.nih.gov/pubmed/22814850