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Local Anesthetics: Common Agents and Their Applications

Local Anesthetics: Common Agents and Their Applications

Local anesthetics (LAs) are commonly used for various applications in medical and dental procedures. Some of the common agents used are cocaine, lidocaine, and bupivacaine.
Cocaine is an ester of benzoic acid and methylecgogine. It is used to anesthetize and vasoconstrict locally. Currently, it is used primarily for topical applications. It is beneficial for surgeries on the upper respiratory tract, providing anesthesia and shrinking the mucosa. Cocaine in the form of cocaine hydrochloride is...

Analgesia and Pain Management

Analgesia and Pain Management

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Opioid Analgesics: Synthetic and Semisynthetic Opioids

Opioid Analgesics: Synthetic and Semisynthetic Opioids

Synthetic and semisynthetic opioids are pivotal in pain management and tackling opioid addiction. Semisynthetic opioids, including morphinans (morphine derivatives), oxycodone, oxymorphone, hydrocodone, and hydromorphone, have improved pharmacokinetic profiles compared to morphine. Additionally, heroin and 6-MAM (6-Monoacetylmorphine) show better CNS penetration than morphine due to heightened lipid solubility. Hydromorphone, a potent opioid, undergoes hepatic metabolism to form the active...

Local Anesthetics: Clinical Application as Surface, Infiltration, and Conduction Block Anesthesia

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Depending on the target organ, local anesthetics (LAs) can be administered via various routes. In surface anesthesia, LAs are applied directly to the surface of the skin or mucous membranes. It is widely used for topical skin numbing before venipuncture or minor surgical procedures. Commonly used surface local anesthetics are lidocaine or benzocaine sprays or creams. Surface anesthesia occurs within 5 minutes and lasts for about 60 minutes. One of the main disadvantages of topical anesthesia is...

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Local Anesthetics: Chemistry and Structure-Activity Relationship

Local Anesthetics: Chemistry and Structure-Activity Relationship

Local anesthetics (LAs) are drugs that induce a temporary loss of sensation in a limited body area, preventing pain. Cocaine was the first local anesthetic discovered in the late 19th century. Cocaine is a benzoic acid ester obtained from the leaves of coca shrubs and was often used for its psychotropic effects. Cocaine was first isolated in 1860 by Albert Niemann. Sigmund Freud studied the physiological actions of cocaine. Carl Koller later introduced it into clinical practice in 1884 as a...

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Related Experiment Video

Updated: Jul 9, 2026

A Modified Inflammatory Pain Model to Study the Analgesic Effect in Mice

A Modified Inflammatory Pain Model to Study the Analgesic Effect in Mice

Published on: November 15, 2024

Topical analgesics.

Gary McCleane¹

¹Rampark Pain Centre, 2 Rampark Dromore Road, Lurgan BT66 7JH, Northern Ireland, UK. gary@mccleane@freeserve.co.uk

Anesthesiology Clinics

|December 7, 2007

Summary

Topical analgesics offer a practical and effective drug delivery method, targeting peripheral receptors to minimize systemic side effects. This approach revives interest in topical drug administration for pain management.

Area of Science:

Pharmacology
Drug Delivery Systems
Pain Management

Background:

Topical administration of analgesics was historically common but declined with oral formulations.
Patients continue to find topical drug delivery practical and effective.
Recent understanding highlights peripheral mechanisms that support topical application.

Purpose of the Study:

To re-evaluate the rationale and benefits of topical analgesic administration.
To explore the potential for targeting peripheral receptors via topical application.
To assess the possibility of achieving therapeutic effects with reduced systemic side effects.

Main Methods:

Review of historical and current perspectives on drug administration routes.
Analysis of peripheral mechanisms of action for various preparations.

Related Experiment Videos

Last Updated: Jul 9, 2026

A Modified Inflammatory Pain Model to Study the Analgesic Effect in Mice

A Modified Inflammatory Pain Model to Study the Analgesic Effect in Mice

Published on: November 15, 2024

Comparison of systemic versus topical delivery for therapeutic outcomes and side effect profiles.

Main Results:

Topical application allows targeted action on peripheral receptors and neural pathways.
This route can achieve therapeutic effects without significant systemic drug concentrations.
Reduced systemic exposure minimizes the risk of systemic side effects.

Conclusions:

Topical drug delivery is a viable and effective strategy for analgesia.
Targeting peripheral mechanisms via topical application offers a favorable risk-benefit profile.
Revisiting topical administration presents opportunities for improved pain management and reduced systemic toxicity.