The action of local anaesthetics on histamine release

In-vitro inhibition of the block to polyspermy of hamster eggs by tertiary amine local anaesthetics

“…The presence of high levels of Ca2+ in the medium reversed the inhibitory effects of local anaesthetics on the extrusion of cortical granules, an observation consistent with studies carried out on exocytosis in other cell systems (Kazimierczak et al, 1976;Collins & Epel, 1977). A raised external calcium concentration is known to reverse the inhibition of electrical changes in excitable cell membranes by anaesthetics (Seeman, Chen, Chan-Wong & Staiman, 1974 Local anaesthetics are also known to act by increasing membrane fluidity (Sheetz & Singer, 1974), an effect that is easily reversed by lowering the temperature (Singer, 1974).…”

“…The calcium flux across the membrane is inhibited in the presence of local anaesthetics and they are also known to disrupt the cell cytoskeleton system by displacing Ca2+ from the membranes (Seeman, 1972;Nicolson, 1976 (Austin, 1977). A wide variety of other exocytotic systems are similarly reversibly inhibited by local anaesthetics (Kazimierczak, Peret & Maslinski, 1976;Collins & Epel, 1977). The precise mechanism of inhibition is unknown.…”

Local anesthetics, mepacrine, and propranolol are antagonists of calmodulin.

“…However, these drugs can also affect a wide range of cellular processes in nonnerve tissue, such as excitation-contraction coupling in various types of muscle (1,2), exocytosis (3)(4)(5)(6), membrane transport or permeability of calcium (7), glucose (8), and anions (9), cellular adhesion (10) or aggregation (11), osmotic fragility (12), and ligand-induced Ig receptor capping (13). Several enzymatic activities are also affected by local anesthetics, notably response of adenylate cyclase to catecholamines (14), Mg2+,Ca2+-dependent ATPases ofbrain (15), sarcoplasmic reticulum (16), and erythrocytes (17), and phospholipase A2 (18).…”

Beyond a Simple Anesthetic Effect: Lidocaine in the Diagnosis and Treatment of Interstitial Cystitis/bladder Pain Syndrome

“…42 Lidocaine has been found to inhibit histamine release from challenged mast cells. 43 This action was found to be critically concentration dependent and exhibits a biphasic response: slight potentiation of histamine release occurring at 1 mM (0.027%) and complete inhibition of histamine release at 20 mM (0.5%). Subsequent investigation of this phenomenon showed that lidocaine induced a strong inhibition of activated mast cell histamine release, with increasing effect at higher pH.…”

“…44 LAs have also been shown to competitively inhibit histamine-1 receptors and the release of histamine in skin by platelet-activating factor. 43 Another possibly relevant but less-known property of these drugs is a broad-spectrum bactericidal effect that is also concentration dependent. Lidocaine has also been shown to inhibit the growth of Candida albicans and interfere with viral replication.…”