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Details for Patent: 5,849,763

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Details for Patent: 5,849,763

Title: Use of levobupivacaine as an anesthetic agent
Abstract:Levobupivacaine ((S)-1-butyl-N-(2,6-dimethylphenyl)-2-piperidinecarboxamide) is useful as an anesthetic, particularly in a patient who is CNS-compromised or predisposed to CNS side-effects. It is also useful as an anesthetic in obstetrics.
Inventor(s): Bardsley; Hazel Judith (Cambridge, GB), Gristwood; Robert William (Cambridge, GB), Richards; Andrew John McGlashan (Cambridge, GB)
Assignee: Darwin Discovery Limited (GB)
Filing Date:Oct 27, 1995
Application Number:08/549,408
Claims:1. A method of providing anesthesia, without concomitant adverse systemic side effects, in a patient, comprising administering to the patient levobupivacaine through a route where systemic exposure to said levobupivacaine occurs, wherein said levobupivacaine is present in an enantiomeric excess of at least about 90% with respect to dexbupivacaine.

2. The method, according to claim 1, wherein the side-effects are CNS side-effects.

3. The method, according to claim 1, wherein the patient is CNS-compromised or predisposed to CNS side-effects.

4. The method, according to claim 1, wherein the dosage of levobupivacaine administered is greater than the dosage of racemic bupivacaine that would result in CNS side-effects in the same patient.

5. The method, according to claim 1, wherein levobupivacaine is administered as a solution having a concentration of at least about 0.75% to about 2% w/v, measured as the free base.

6. The method, according to claim 5, wherein the concentration of levobupivacaine is in the range from about 0.75% to about 1.5% w/v.

7. The method, according to claim 6, wherein the concentration of levobupivacaine is selected from the group consisting of about 0.75%, about 1%, about 1.25%, and about 1.5% w/v.

8. The method, according to claim 5, wherein a unit dose of from about 1 to about 15 ml is administered.

9. The method, according to claim 1, wherein levobupivacaine is administered as a solution having a concentration of about 0.125% to about 0.75% w/v.

10. The method, according to claim 1, wherein levobupivacaine is administered in the form of an aqueous solution.

11. The method, according to claim 1, wherein the total dose of levobupivacaine administered to the patient is between about 2 mg to 2.5 mg per kg of patient body weight.

12. The method, according to claim 1, wherein administration of levobupivacaine is carried out for a period of at least 24 hours.

13. The method, according to claim 1, wherein administration of levobupivacaine is carried out for up to 72 hours.

14. The method, according to claim 1, wherein administration of levobupivacaine is carried out for up to a fortnight.

15. The method, according to claim 1, employing a technique selected from the group consisting of epidural block, spinal block, nerve block, field block, intercostal block, and Bier's block.

16. The method, according to claim 1, wherein the levobupivacaine is substantially free of dexbupivacaine.

17. A method of providing anesthesia in obstetrics, comprising administering to a patient levobupivacaine, wherein said levobupivacaine is present in an enantiomeric excess of at least about 90% with respect to dexbupivacaine.

18. The method, according to claim 17, wherein the patient is disposed to convulsions.

19. The method, according to claim 17, wherein the levobupivacaine is substantially free of dexbupivacaine.

20. A method of providing anesthesia, without concomitant adverse systemic side effects, in a patient, comprising administering to the patient levobupivacaine, wherein the route of administration is selected from the group consisting of epidural administration and spinal administration, and wherein said levobupivacaine is present in an enantiomeric excess of at least about 90% with respect to dexbupivacaine.
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