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Structurally, amino esters consist of three molecular components: a lipophilic part (ester); an intermediate aliphatic chain; a hydrophilic part (amine); The chemical linkage between the lipophilic part and the intermediate chain can be of the amide-type or the ester-type, and is the general basis for the current classification of local anesthetics.
This is a list of local anesthetic agents. Not all of these drugs are still used in clinical practice and in research. Not all of these drugs are still used in clinical practice and in research. Some are primarily of historical interest.
Many local anesthetics fall into two general chemical classes, amino esters (top) and amino amides (bottom). A local anesthetic (LA) is a medication that causes absence of all sensation (including pain) in a specific body part without loss of consciousness, [1] providing local anesthesia, as opposed to a general anesthetic, which eliminates all sensation in the entire body and causes ...
This tetrameric enzyme is responsible for the metabolism of a number of substances, including amino ester local anesthetics and succinylcholine, which it hydrolyses in two stages to succinyl monocholine and choline, then to succinic acid and a second molecule of choline. Dibucaine inhibits normal butyrylcholinesterase activity, reducing the ...
Amide-linked local anesthetic agents, such as lidocaine and bupivacaine, can become "trapped" in their ionized forms on the fetal side of the placenta, so their net transfer across the placenta is increased. An ester-linked local anesthetic agent, such as 2-chloroprocaine, is rapidly metabolized, and placental transfer is limited.
Local anesthesia, in a strict sense, is anesthesia of a small part of the body such as a tooth or an area of skin. Regional anesthesia is aimed at anesthetizing a larger part of the body such as a leg or arm. Conduction anesthesia encompasses a great variety of local and regional anesthetic techniques.
Articaine is a dental amide-type local anesthetic. It is the most widely used local anesthetic in a number of European countries [2] and is available in many countries. It is the only local anaesthetic to contain a thiophene ring, meaning it can be described as 'thiophenic'; this conveys lipid solubility. [3]
About one in 3000 white North Americans is homozygous (i.e. has two copies of the abnormal gene) for the most common atypical form of the enzyme pseudocholinesterase, [12] [13] and do not hydrolyze ester anesthetics such as procaine. This results in a prolonged period of high levels of the anesthetic in the blood and increased toxicity.