Local anesthetic methods and kits

• US 6,764,678 B2
• Filed: 05/28/2002
• Issued: 07/20/2004
• Est. Priority Date: 05/12/2000
• Status: Expired due to Term

• Current Assignee: Septodont Holding
• Original Assignee: Novalar Pharmaceuticals, Inc.
• Inventors: Katz, Howard I., Weber, Eckard
• Primary Examiner(s): Tate, Christopher R.
• Assistant Examiner(s): WINSTON, RANDALL O
• Application Number:
  US10/155,171
• Publication Number:
  US 20020183356A1
• Time in Patent Office: 784 Days
• Field of Search: 424/94.62, 424/94.1, 435/810, 514/537, 514/816, 514/818, 514/304, 514/649
• US Class Current: 424/94.62
• CPC Class Codes: A61K 31/135 having aromatic rings , e.g. ketamine, nortriptyline methadone A61K31/137
• CPC Class Codes: A61K 31/165 having aromatic rings, e.g. colchicine, atenolol, progabide
• CPC Class Codes: A61K 31/24 having an amino or nitro group
• CPC Class Codes: A61K 31/415 1,2-Diazoles
• CPC Class Codes: A61K 31/44 Non condensed pyridines; Hydrogenated derivatives thereof
• CPC Class Codes: A61K 31/445 Non condensed piperidines, e.g. piperocaine
• CPC Class Codes: A61K 31/505 Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
• CPC Class Codes: A61P 23/02 Local anaesthetics
• CPC Class Codes: A61P 25/00 Drugs for disorders of the nervous system
• CPC Class Codes: A61P 25/02 for peripheral neuropathies
• CPC Class Codes: A61P 37/06 Immunosuppressants, e.g. drugs for graft rejection
• CPC Class Codes: A61P 43/00 Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
• CPC Class Codes: Y10S 435/81 Packaged device or kit

Abstract

Methods of reversing local anesthesia are disclosed. The methods comprise administering a local anesthetic and alpha adrenergic receptor agonist to induce local anesthesia followed by reversing anesthesia with a low dose of an alpha adrenergic receptor antagonist. Also disclosed are kits comprising a local anesthetic, an alpha adrenergic receptor agonist and a low dose of an alpha adrenergic receptor antagonist.

Claims

1. A method of providing local anesthesia to a mammal, comprising:

(a) administering to said mammal in need thereof an anesthetic agent and an alpha adrenergic receptor agonist to the site to be anesthetized, wherein said anesthetic agent is administered in an amount effective to provide local anesthesia and said alpha adrenergic receptor agonist is administered in an amount effective to constrict the blood vessels at the site and prolong the local anesthesia, and then

(b) administering a unit dose of a composition to said site, said unit dose comprising between about 0.00 18 mg and about 0.45 mg phentolamine mesylate or a molar equivalent of another alpha adrenergic receptor antagonist and a pharmaceutically acceptable carrier.

2. The method of claim 1, wherein said anesthetic agent and said alpha adrenergic receptor agonist are administered together in solution.

3. The method of claim 2, wherein said anesthetic agent and said alpha adrenergic receptor agonist are administered together in solution from a standard dental local anesthetic syringe.

4. The method of claim 1, wherein said anesthetic agent is selected from the group consisting of lidocaine, polocaine, etidocaine, lignocaine, xylocaine, novocaine, carbocaine, procaine, prilocaine, bupivacaine, cinchocaine, and mepivacaine.

5. The method of claim 1, wherein said alpha adrenergic receptor agonist is levonordefrin, epinephrine, or norepinephrine.

6. The method of claim 1, wherein said unit dose comprises between about 0.09 mg and about 0.45 mg phentolamine mesylate or a molar equivalent of another alpha adrenergic receptor antagonist.

7. The method of claim 1, wherein said composition is a solution formulated for administration to a mammal by injection, infiltration, or topical application.

8. The method of claim 7, wherein said solution is formulated for topical application to mucosal tissue.

9. The method of claim 8, wherein said solution is used to impregnate a wafer, pellet, or cotton ball, for application to mucosal tissue.

10. The method of claim 1, wherein said composition is a gel or a paste formulated for topical administration to a mammal.

11. The method of claim 10, wherein said composition is formulated for topical application to mucosal tissue.

12. The method of claim 1, wherein said alpha adrenergic receptor antagonist is selected from the group consisting of phentolamine, phentolamine hydrochloride, phentolamine mesylate, tolazoline, yohimbine, rauwolscine, doxazosine, labetalol, prazosine, tetrazosine and trimazosine.

13. The method of claim 12, wherein said alpha adrenergic receptor antagonist is phentolamine mesylate.

14. The method of claim 1, wherein said unit dose is present in a container that fits into a standard dental local anesthetic syringe.

15. The method of claim 14, wherein said container has a volume of between 1.6 ml and 1.8 ml.

16. The method of claim 1, wherein said unit dose comprises phentolamine mesylate, and wherein said unit dose is present in a container that fits into a standard dental local anesthetic syringe.

17. A method of providing a regional anesthetic block to a mammal, comprising:

(a) administering to said mammal in need thereof an anesthetic agent and an alpha adrenergic receptor agonist to the site to receive the anesthetic block, wherein said anesthetic agent is administered in an amount effective to provide local anesthesia and said alpha adrenergic receptor agonist is administered in an amount effective to constrict the blood vessels at the site and prolong the anesthetic block, and then

(b) administering a unit dose of a composition to said site, said unit dose comprising between about 0.0018 mg and about 0.45 mg phentolamine mesylate or a molar equivalent of another alpha adrenergic receptor antagonist and a pharmaceutically acceptable carrier.

18. The method of claim 17, wherein said site is the epidural space.

19. The method of claim 17, wherein said anesthetic agent and said alpha adrenergic receptor agonist are administered together in solution.

20. The method of claim 19, wherein said solution is administered by injection into the site.

22. The method of claim 17, wherein said alpha adrenergic receptor agonist is levonordefrin, epinephrine, or norepinephrine.

23. The method of claim 17, wherein said unit dose comprises between about 0.09 mg and about 0.45 mg phentolamine mesylate or a molar equivalent of another alpha adrenergic receptor antagonist.

24. The method of claim 17, wherein said composition is a solution formulated for administration to a mammal by injection, infiltration, or topical application.

25. The method of claim 24, wherein said solution is formulated for topical application to mucosal tissue.

26. The method of claim 25, wherein said solution is used to impregnate a wafer, pellet, or cotton ball, for application to mucosal tissue.

27. The method of claim 17, wherein said composition is a gel or a paste formulated for topical administration to a mammal.

28. The method of claim 27, wherein said composition is formulated for topical application to mucosal tissue.

29. The method of claim 17, wherein said alpha adrenergic receptor antagonist is selected from the group consisting of phentolamine, phentolamine hydrochloride, phentolamine mesylate, tolazoline, yohimbine, rauwolscine, doxazosine, labetalol, prazosine, tetrazosine and trimazosine.

30. The method of claim 29, wherein said alpha adrenergic receptor antagonist is phentolamine mesylate.

31. The method of claim 17, wherein said unit dose is present in a container having a volume of between 1.6 ml and 1.8 ml.

21. The method of claim wherein said anesthetic agent is selected from the group consisting of lidocaine, polocaine, etidocaine, lignocaine, xylocaine, novocaine, carbocaine, procaine, prilocaine, bupivacaine, cinchocaine, and mepivacaine.