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Through American and British English spelling differences, Drug and Sense

A wide variety of drugs are used in modern anesthetic practice. Many are rarely used outside anesthesiology, but others are used commonly in various fields of healthcare. Combinations of anesthetics are sometimes used for their synergistic and additive therapeutic effects. Adverse effects, however, may also be increased. Anesthetics are distinct from analgesics, which block only sensation of painful stimuli. Analgesics are typically used in conjunction with anesthetics to control pre-, intra-, and postoperative pain.

Local anesthetics

Ester-based

  • Procaine
  • Tetracaine (sometimes called Amethocaine)

Amide-Based

Local anesthetic agents prevent the transmission of nerve impulses without causing unconsciousness. They act by reversibly binding to fast sodium channels from within nerve fibers, thereby preventing sodium from entering the fibres, stabilising the cell membrane and preventing action potential propagation. Each of the local anesthetics has the suffix "–caine" in their names.

Local anesthetics can be either ester- or amide-based. Ester local anesthetics are generally unstable in solution and fast-acting, are rapidly metabolised by cholinesterases in the blood plasma and liver, and more commonly induce allergic reactions. Amide local anesthetics are generally heat-stable, with a long shelf life (around two years). Amides have a slower onset and longer half-life than ester anesthetics, and are usually racemic mixtures, with the exception of levobupivacaine (which is S(-) -bupivacaine) and ropivacaine (S(-)-ropivacaine). Although general rules exist for onset and duration of anesthesia between ester- or amide-based local anesthetics, these are properties are ultimately dependent on myriad factors including the lipid solubility of the agent, the concentration of the solution, and the pKa. Amides are generally used within regional and epidural or spinal techniques, due to their longer duration of action, which provides adequate analgesia for surgery, labor, and symptomatic relief. Some esters, such as benzocaine and tetracaine, are found in topical formulations to be absorbed through the skin.

Only preservative-free local anesthetic agents may be injected intrathecally.

Pethidine also has local anesthetic properties, in addition to its opioid effects.


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