Anaesthetic formulation

Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Having -c- – wherein x is chalcogen – bonded directly to...

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546189, A61K 31445, C07D40100

Patent

active

059325976

ABSTRACT:
A pharmaceutically-acceptable aqueous solution which is isobaric or hyperbaric, and isotonic, with respect to cerebrospinal fluid (CSF), comprises a 1-alkyl-N-(2,6-dimethylphenyl)-2-piperidinecarboxamide anesthetic agent such as bupivacaine or levobupivacaine and a saccharide. If the amount of the anesthetic agent is no more than 0.75% w/v, a salt or another additional non-saccharide is present. Accordingly, the amount of the saccharide can be kept below that which would provide isotonicity in the absence of the additional non-saccharide.

REFERENCES:
De Paula, M.L., et al. (1997) "Subarachnoid Dispersion of Local Anaesthetics: Consideration in Face of the Advent of Isobaric Bupivacaine" Rev. Bras. Anestesiol. 47(5):439-452 **Abstract No. 287549, Chemical Abstracts 127(21).
Chang, C.J., et al. (1996) "Spinal Anesthesia with 0.25% Hyperbaric Bupivacaine for Cesarean Section: Effects of volume" Br. J. Anaesth 77(2):145-149 ** Abstract No. 185717, Chemical Abstracts 125(15).
Ganem, E.M.., et al. (1996) "Neurotoxicity of Subarachnoid Hyperbaric Bupivacaine in Dogs" Reg. Anesth. 21(3):234-238 **Abstract No. 49134, Chemical Abstracts 125(5).
Hampl, K.F., et al. (1995) "Hyperosmolarity Does Not Contribute to Transient Radicular Irritation After Spinal Anesthesia with Hyperbaric 5% Lidocaine" Reg. Anesth. 20(5):363-368 **Abstract No. 307201, Chemical Abstracts 124(3).
Tetzlaff, J.E. (1995) "Influence of Baricity on the Outcome of Spinal Anesthesia with Bupivacaine for Lumbar Spine Surgery" Reg. Anesth. 20(6):533-537 **Abstract No. 278937, Chemical Abstracts 124(1).
Bigler, D., et al. (1986) "Double-Blind Evaluation of Intrathecal Hyperbaric and Glucose-Free Bupivacaine on Analgesia and Cardiovascular Function" Reg. Anesth. 11(4):151-155 **Abstract No. 107814, Chemical Abstracts 106(14).
Kytta, J. et al. (1982) "Histophathological Changes in Rabbit Spinal Cord Caused by Bupivacaine" Dep. Anesth. 5(4):85-88 **Abstract No. 46867, Chemical Abstracts 98(7).
Bannister, J. et al. (1990) "Effect of Glucose Concentration on the Intrathecal Spread of 0.5% Bupivacaine" British Journal of Anesthesia 64:232-234.
Burke, D., et al. (1998) "Intrathecal 0.5% Levobupivacaine for Lower Limb Surgery" EuroPain (Abstract).
Finucane, B.T. et al. (1980) "A Double-Blind Comparison of Etidocaine and Lidocaine for IV Regional Anesthesia" **Abstract No.
Gelman, S., Jiri J. Vitek (1980) "Thoracic Epidural Catheter Placement Under Fluoroscopic Control in Moribidly Obese Patients".
Tsai, et al. "Spinal Anesthesia with Bupivacaine for Transurethal Resection of Prostate:Effects of Specific Gravity, Volume and Dose" Ma Tsui Hsueh Tsa Chi Anaestesiologic Sinica 1989, 27 (2) 111-116, Abstract, MEDLINE acc. No. 90013942.
Wallin, G, et al "Influence of Intraperitoneal Anesthesia on Pain on the Sympathoadrenal Response to Abdominal Surgery" Acta Anaesthesiologica Scandanavica, 1988, 32 (7), 553-8.

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