Method of treating the syndrome of coronary heart disease risk factors in humans

1 . A method of treating a human suffering from one or more conditions included within Coronary Heart Disease Risk Factor (CHDRF) syndrome, the method comprising administering, by a pharmaceutically effective mode, a drug composition comprising:

an opioidergic agent; and

an insulin secretagogue.

2 . The method of claim 1 , wherein the opioidergic agent is an opiate antagonist, an opiate having μ-agonist activity or a combination thereof.

3 . The method of claim 2 , wherein the opiate antagonist comprises a single molecular entity.

4 . The method of claim 2 , wherein the opiate antagonist comprises a combination of molecular entities.

5 . The method of claim 2 , wherein the opiate having μ-agonist activity comprises a single molecular entity.

6 . The method of claim 2 , wherein the opiate having μ-agonist activity comprises a combination of molecular entities.

7 . The method of claim 2 , wherein the drug composition comprises a peripherally acting μ-agonist.

8 . The method of claim 7 , wherein the drug composition comprises loperamide.

9 . The method of claim 2 , wherein the drug composition comprises a centrally acting μ-agonist.

10 . The method of claim 2 , wherein the drug composition further comprises an opiate having mixed μ-agonist and κ antagonist activity.

11 . The method of claim 10 , wherein the opiate having mixed μ-agonist and κ antagonist activity is buprenorphine.

12 . The method of claim 2 wherein the opioidergic agent includes at least one of the following:

i) dihydromorphine;

ii) morphine;

iii) hydromorphone;

iv) methadone;

v) fentanyl;

vi) sufentanyl;

vii) buprenorphine;

viii) demorphine;

ix) codeine;

x) ethylmorphine;

xi) etonitazene;

xii) hydrocodone;

xiii) levorphanol;

xiv) norcodeine;

xv) normophine;

xvi) (D-Ala 2 -N-Me-Phe 4 -Gly 3 -ol)-Enkephalin (DAMGO); and

xvii) oxycodone.

13 . The method of claim 2 , wherein the opioidergic agent includes at least one of the following:

i) nalmefene;

ii) naltrexone;

iii) nor-binaltorphimine;

iv) (−)-(1R,5R,9R)-5,9-diethyl-2-(3-furylmethyl)-2-hydroxy-6,7-benzomorphan (MR 2266);

v) a triethylenedioxy derivative of B-naltrexamine (TENA); and

vi) guanidylated naltrindole (GNTI).

14 . The method of claim 2 , wherein the condition included within the CHDRF Syndrome is Insulin Resistance (IR).

15 . The method of claim 2 , wherein the condition included within the CHDRF Syndrome is Beta-Cell Dysfunction.

16 . The method of claim 2 , wherein the condition included within the CHDRF Syndrome is Impaired Glucose Tolerance (IGT).

17 . The method of claim 2 , wherein the condition included within the CHDRF Syndrome is Type 2 Diabetes.

18 . The method of claim 2 , wherein the condition included within the CHDRF syndrome is overweight.

19 . The method of claim 2 , wherein the condition included within the CHDRF syndrome is obesity.

20 . The method of claim 2 , wherein the condition included within the CHDRF syndrome is dyslipidemia.

21 . The method of claim 1 , wherein the insulin secretagogue includes at least one of the following:

i. sulphonylureas;

ii. tolbutamide;

iii. chlorpropamide;

iv. glimepiride;

v. glipizide;

vi. glyburide;

vii. meglitinides;

viii. repaglinide;

ix. pramlintide;

x. morphilinoguanide;

xi. acetylcholine;

xii. muscarinic agonists;

xiii. carbachol;

xiv. bethanechol;

xv. beta-L-glucose pentaacetate;

xvi. chiro-inositol;

xvii. myo-inositol;

xviii. GIP;

xix. GLP-1; and

xx. Extendin-4.

22 . The method of claim 1 , wherein the insulin secretagogue is a non-glucose dependent insulin secretagogue, the method producing insulin release patterns capable of attaining glucose dependent, bi-phasic release characteristics with reduced likelihood of producing hypoglycemia.

23 . The method of claim 22 , wherein the insulin secretagogue is sulphonylurea.

24 . A method of treating a human suffering from one or more conditions included within Coronary Heart Disease Risk Factor (CHDRF) syndrome, the method comprising administering, by a pharmaceutically effective mode, a drug composition comprising:

an opiate antagonist; and

an insulin secretagogue.

25 . The method of claim 24 , wherein the opiate antagonist comprises a single molecular entity.

26 . The method of claim 24 , wherein the opiate antagonist comprises a combination of molecular entities.

27 . The method of claim 24 , wherein the opiate antagonist includes at least one of the following:

i) nalmefene

ii) naltrexone;

iii) nor-binaltorphimine;

iv) (−)-(1R,5R,9R)-5,9-diethyl-2-(3-furylmethyl)-2-hydroxy-6,7-benzomorphan (MR 2266);

v) a triethylenedioxy derivative of B-naltrexamine (TENA); and

vi) guanidylated naltrindole (GNTI).

28 . The method of claim 24 , wherein the condition included within the CHDRF Syndrome is Insulin Resistance.

29 . The method of claim 24 , wherein the condition included within the CHDRF Syndrome is Beta-Cell Dysfunction.

30 . The method of claim 24 , wherein the condition included within the CHDRF syndrome is Impaired Glucose Tolerance (IGT).

31 . The method of claim 24 , wherein the condition included within the CHDRF syndrome is Type 2 Diabetes.

32 . The method of claim 24 , wherein the condition included within the CHDRF syndrome is overweight.

33 . The method of claim 24 , wherein the condition included within the CHDRF syndrome is obesity.

34 . The method of claim 24 , wherein the condition included within the CHDRF syndrome is dyslipidemia.

35 . The method of claim 24 wherein the opiate antagonist has IC 50 levels for the μ, δ, and κ opiate receptors, the IC 50 levels being {(IC 50 κ/IC 50 μ)<3} and {(IC 50 κ/IC 50 δ)<3}.

36 . The method of claim 24 , wherein the insulin secretagogue includes at least one of the following:

i. sulphonylureas;

ii. tolbutamide;

iii. chlorpropamide;

iv. glimepiride;

v. glipizide;

vi. glyburide;

vii. meglitinides;

viii. repaglinide;

ix. pramlintide;

x. morphilinoguanide;

xi. acetylcholine;

xii. muscarinic agonists;

xiii. carbachol;

xiv. bethanechol;

xv. beta-L-glucose pentaacetate;

xvi. chiro-inositol;

xvii. myo-inositol;

xviii. GIP;

xix. GLP-1; and

xx. Extendin-4.

37 . The method of claim 24 , wherein the insulin secretagogue is a non-glucose dependent insulin secretagogue, the method producing insulin release patterns capable of attaining glucose dependent, bi-phasic release characteristics with reduced likelihood of producing hypoglycemia.

38 . The method of claim 37 , wherein the insulin secretagogue is sulphonylurea.

39 . A method of treating a human suffering from one or more conditions included within the Coronary Heart Disease Risk Factor (CHDRF) syndrome, the method comprising administering, by a pharmaceutically effective mode, a drug composition comprising:

an opiate agonist; and

an insulin secretagogue.

40 . The method of claim 39 , wherein the opiate agonist comprises a single molecular entity.

41 . The method of claim 39 , wherein the opiate agonist comprises a combination of molecular entities.

42 . The method of claim 39 , wherein the opiate agonist is a peripherally acting μ-agonist.

43 . The method of claim 42 , wherein the opiate agonist is loperamide.

44 . The method of claim 39 , wherein the opiate agonist is a centrally acting μ agonist.

45 . The method of claim 39 , wherein the opiate agonist includes at least one of the following:

i) dihydromorphine;

ii) morphine;

iii) hydromorphone;

iv) methadone;

v) fentanyl;

vi) sufentanyl;

vii) demorphine;

viii) codeine;

ix) ethylmorphine;

x) etonitazene;

xi) hydrocodone;

xii) levorphanol;

xiii) norcodeine;

xiv) normophine;

xv) (D-Ala 2 -N-Me-Phe 4 -Gly 3 -ol)-Enkephalin (DAMGO); and

xvi) oxycodone.

46 . The method of claim 39 , wherein the condition included within the CHDRF Syndrome is Insulin Resistance.

47 . The method of claim 39 , wherein the condition included within the CHDRF Syndrome is Beta-Cell Dysfunction.

48 . The method of claim 39 , wherein the condition included within the CHDRF syndrome is Impaired Glucose Tolerance (IGT).

49 . The method of claim 39 , wherein the condition included within the CHDRF syndrome is Type 2 Diabetes.

50 . The method of claim 39 , wherein the condition included within the CHDRF syndrome is overweight.

51 . The method of claim 39 , wherein the condition included within the CHDRF syndrome is obesity.

52 . The method of claim 39 , wherein the condition included within the CHDRF syndrome is dyslipidemia.

53 . The method of claim 39 , wherein the insulin secretagogue includes at least one of the following:

i. sulphonylureas;

ii. tolbutamide;

iii. chlorpropamide;

iv. glimepiride;

v. glipizide;

vi. glyburide;

vii. meglitinides;

viii. repaglinide;

ix. pramlintide;

x. morphilinoguanide;

xi. acetylcholine;

xii. muscarinic agonists;

xiii. carbachol;

xiv. bethanechol;

xv. beta-L-glucose pentaacetate;

xvi. chiro-inositol;

xvii. myo-inositol;

xviii. GIP;

xix. GLP-1; and

xx. Extendin-4.

54 . The method of claim 39 , wherein the insulin secretagogue is a non-glucose dependent insulin secretagogue, the method producing insulin release patterns capable of attaining glucose dependent, bi-phasic release characteristics with reduced likelihood of producing hypoglycemia.

55 . The method of claim 39 , wherein the insulin secretagogue is sulphonylurea.