Amides

Information about Amides

The amide local anesthetics including lidocaine, bupivacaine and ropivacaine are commonly used for pain control during minor surgery or invasive procedures such as biopsies, small excisions or dental work.

Liver toxicity of Amides

These local anesthetics have not been linked to serum enzyme elevations, but when given as constant infusions or repeated injections have been occasionally mentioned as possible causes of clinically apparent liver injury.

Mechanism of action of Amides

Lidocaine (lye' do kane), bupivacaine (bue piv' a kane) and ropivacaine (roe piv' a kane) are commonly used local anesthetics that are chemically referred to as aminoethylamides or amide local anesthetics. Their mechanism of anesthetic action is believed to be based upon inhibition of voltage-gated sodium channels, which results in membrane stabilization and slowing of membrane depolarization and repolarization.

Local anesthetics have been shown to be effective and are used widely in preventing or reducing pain from minor surgery, incisions, biopsies, dental and obstetrical procedures and pain from wounds. They are usually given as a single injection locally into a lesion or the area of incision, but can be given as infusions for hours or for several days by epidural or wound-based catheters. Local anesthetic infusions can also be used for postoperative pain management. They have excellent tolerance and safety.

Dosage and administration for Amides

Local anesthetics have variable durations of action, and short acting versions are often given with epinephrine, which decreases the rate of absorption limiting systemic exposure and prolonging the duration of action.

FDA approval information for Amides

Lidocaine was approved for use as a local anesthetic in the 1948 originally under the commercial name Xylocaine, ropivacaine in 1990 (Naropin), and bupivacaine in 1990 (Marcaine). Other less commonly used amide anesthetics include articaine (Septocaine: 2000), mepivacaine (Carbocaine: 1960), and prilocaine (Citanest: 1965). A liposomal and longer acting preparation of bupivacaine was approved for use in controlling postsurgical pain in 2011 (Exparel).

Side effects of Amides

Side effects of the local anesthetics are usually dose related and occur mostly as a result of systemic administration or exposure. They include neurological symptoms such as drowsiness, tinnitus, dizziness and twitching as well as gastrointestinal effects such as nausea, vomiting and constipation. Cardiovascular depression can also occur and ventricular arrhythmias, especially with higher doses.

• Dailymed label info on Amides
• FDA Amides

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