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Intracranial Pharmacotherapy and Pain Assays in Rodents
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A concise review of the basic biology and pharmacology of local analgesia

S Subramaniam1, M Tennant

  • 1Centre for Rural and Remote Oral Health, The University of Western Australia.

Australian Dental Journal
|January 19, 2006
PubMed

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Analgesia and Pain Management01:25

Analgesia and Pain Management

Pain is critical to various clinical pathologies, provoking an urgent need for effective management. Pain, whether acute or chronic, is a complex neurochemical process. Its alleviation depends on the type, with nonopioid analgesics effective for mild to moderate pain, such as musculoskeletal or inflammatory pain, while neuropathic pain responds best to anticonvulsants, tricyclic antidepressants, or serotonin/norepinephrine reuptake inhibitors. For severe acute or chronic pain, opioids may be...
Local Anesthetics: Pharmacokinetics01:13

Local Anesthetics: Pharmacokinetics

The potency and duration of action of local anesthetics (LAs) are determined by their pharmacokinetics. Pharmacokinetics describes how LAs are absorbed, distributed, metabolized, and eliminated from the body. When administered to the vascular tissues, LAs are quickly absorbed and enter the systemic circulation, reducing their localized effects. Adding vasoconstrictors such as epinephrine to LAs reduces their absorption into the systemic circulation, making them clinically effective. The...
Local Anesthetics: Differential Sensitivity of Nerve Fibers01:24

Local Anesthetics: Differential Sensitivity of Nerve Fibers

Local anesthetics (LAs) block the sodium channels of nerve trunks, sensory nerve endings, and neuromuscular junctions. Although LAs can block all kinds of nerves, the sensitivity of nerve fibers differs according to nerve types and structures. LAs are known to block myelinated fibers faster than unmyelinated ones. Also, they block pain or sensory neurons at low concentrations without affecting the motor neurons involved in muscle contractions. This helps relieve labor pain without affecting the...
Local Anesthetics: Common Agents and Their Applications01:23

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...
Local Anesthetics: Clinical Application as Epidural Anesthesia01:29

Local Anesthetics: Clinical Application as Epidural Anesthesia

Epidural anesthetics are administered in the fat-filled epidural space, the outermost part of the spinal canal. This technique is commonly employed for pain management and anesthesia during lower abdomen and pelvis surgeries or labor and delivery.
Since epidural anesthetics can be infused through an epidural catheter, all types of drugs, including short-acting ones, can be administered. Chloroprocaine and lidocaine are examples of short and long-duration anesthetics, respectively. Bupivacaine...
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Local Anesthetics: Mechanism of Action

Local anesthetics (LAs) block sensory and motor impulses by inhibiting the sodium channels on the nerve cell membranes. This induces temporary loss of sensation, relieving pain in a specific body area.
Local anesthetics are amphiphilic molecules consisting of a hydrophobic aromatic part linked to a hydrophilic group by an ester or amide linkage. They are weak bases and are usually available as salts, which increases their solubility and stability. Once administered, LAs exist in the body either...