Author: Sandin, Sonia Gallego ; Galvez-Mugica, Maria Angeles ; Novalbos, Jesus ; Santos-Ampuero, Maria Angeles ; Gilsanz, Fernando ; Garcia, Antonio Garcia ; Galiano, Alvaro ; Abad-Santos, Francisco

We evaluated the duration of sensory anesthesia after blockade of the ulnar nerve of IQB-9302, a new local amide anesthetic, compared with bupivacaine. A double-blinded, randomized, cross-over study in 12 healthy volunteers aged 18 to 35 yr was performed. Three milliliters of 0.25% IQB-9302 was administered in one wrist and bupivacaine in the other. A week later, the blocks were repeated with a concentration of 0.5%. These concentrations were chosen because they seemed to be equipotent in previous studies. The duration of sensory anesthesia was the main variable measured; secondary outcomes were motor block, time to onset, and time to recovery from block. The duration of sensory block was similar for IQB-9302 and bupivacaine at a concentration of 0.25%; median and range: 409 min (0-800 min) for IQB-9302 and 258 min (0-665 min) for bupivacaine (95% confidence interval for the difference from -47 to 545, P = 0.82, Wilcoxon's test). The results with 0.5% were: 525 min (440-735 min) and 690 min (365-1098 min), respectively (P = 0.026). There were no significant differences in the other variables measured. No important adverse reactions were seen. We conclude that IQB-9302 is an effective new local anesthetic for blockade of ulnar nerve at the concentrations tested.IMPLICATIONSIQB-9302 is a new local anesthetic that has shown a long duration of action and low cardiovascular toxicity in preclinical studies. We report the results of a phase I clinical trial to compare this new drug with bupivacaine for ulnar nerve block.

01 Feb 2001·The Journal of pharmacology and experimental therapeutics

Effects of bupivacaine and a novel local anesthetic, IQB-9302, on human cardiac K+ channels.

Article

Author: Caballero, R ; Tamargo, J ; Longobardo, M ; Delpón, E ; Valenzuela, C ; González, T

We have studied and compared the effects of bupivacaine with those induced by a new local anesthetic, IQB-9302, on human cardiac K+ channels hKv1.5, Kv2.1, Kv4.3, and HERG. Both drugs have a close chemical structure, only differing in their N-substituent (n-butyl and cyclopropylmethyl, for bupivacaine and IQB-9302, respectively). Both drugs blocked Kv2.1, Kv4.3, and HERG channels similarly. Bupivacaine inhibited these channels by 48.6 +/- 3.4, 45.4 +/- 12.4, and 43.1 +/- 9.1%, respectively, and IQB-9302 by 48.1 +/- 3.3, 36.1 +/- 3.7, and 50.3 +/- 6.6%, respectively. However, bupivacaine was 2.5 times more potent than IQB-9302 to block hKv1.5 channels (EC(50) = 8.9 +/- 1.4 versus 21.5 +/- 4.7 microM). Both drugs induced a time- and voltage-dependent block of hKv1.5 and Kv2.1 channels. Block of Kv4.3 channels induced by either drug was time- and voltage-dependent at membrane potentials coinciding with the activation of the channels. IQB-9302 produced an instantaneous block of Kv4.3 and hKv1.5 channels at the beginning of the depolarizing pulse that can be interpreted as a drug interaction with a nonconducting state. Bupivacaine and IQB-9302 induced a similar degree of block of HERG channels and induced a steep voltage-dependent decrease of the relative current. These results suggest that 1) bupivacaine and IQB-9302 block the open state of hKv1.5, Kv2.1, Kv4.3, and HERG channels; and 2) small differences at the N-substituent of these drugs do not affect the drug-induced block of Kv2.1, Kv4.3, or HERG, but specifically modify block of hKv1.5 channels.

01 Sep 2000·Regional Anesthesia and Pain Medicine

Antinociceptive and Motor-Blocking Action of Epidurally Administered IQB-9302 and Bupivacaine in the Dog

Article

Author: Gómez de Segura, I A ; De Miguel, E ; Vazquez, I

BACKGROUND AND OBJECTIVESThe aim of this study was to compare the antinociceptive and motor-blocking effects of epidurally administered IQB-9302 (C18H26N2O.HCl) and bupivacaine in the dog.METHODSTwelve adult female Beagle dogs were used. Each animal received 3 concentrations (0.25%, 0.50%, and 0.75%) of either IQB-9302 (n = 6) or bupivacaine (n = 6) by means of a chronic epidural catheter. The nocifensive and motor-blocking status were determined at regular intervals before (baseline) and after drug administration.RESULTSEpidurally administered IQB-9302 caused a more potent nocifensive and motor-blocking action than bupivacaine. The duration of complete nocifensive block was the longest with IQB-9302, whereas the duration of dermatome nocifensive block was similar for both drugs. The nocifensive to motor block ratio was significantly higher with IQB-9302.CONCLUSIONSIQB-9302 produced an anesthetic action similar to that of bupivacaine, although the former drug induced a slightly more potent nocifensive block. Nocifensive and motor block duration are very similar with IQB-9302, whereas bupivacaine induces a more prolonged motor block without nocifensive block.

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