Compositions of Alpha3beta4 Receptor antagonists and opioid agonist analgesics

• US 20050026842A1
• Filed: 05/08/2004
• Published: 02/03/2005
• Est. Priority Date: 04/22/2002
• Status: Abandoned Application

• Current Assignee: David Lew Simon
• Original Assignee: David Lew Simon
• Inventors: Simon, David Lew
• Application Number:
  US10/841,408
• Publication Number:
  US 20050026842A1
• Time in Patent Office: Days
• US Class Current: 514/282
• CPC Class Codes: A61K 2300/00 Mixtures or combinations of active ingredients, wherein at least one active ingredient is fully defined in groups A61K31/00 - A61K41/00
• CPC Class Codes: A61K 31/192 having aromatic groups, e.g. sulindac, 2-aryl-propionic acids, ethacrynic acid cannabinoids A61K31/658
• CPC Class Codes: A61K 31/445 Non condensed piperidines, e.g. piperocaine
• CPC Class Codes: A61K 31/485 Morphinan derivatives, e.g. morphine, codeine
• CPC Class Codes: A61K 31/7052 having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides
• CPC Class Codes: A61K 38/33 derived from pro-opiomelanocortin, pro-enkephalin or pro-dynorphin
• CPC Class Codes: A61K 45/06 Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca

Abstract

Methods for use of pharmaceutical compositions containing an opioid agonist analgesic and an α3β4 nicotinic receptor antagonist effective to separate the brain-derived wanting of the opioid from the analgesic or anti-diarrhea effect of the opioid agonist.

Claims

1. ) A method for treating a human'"'"'s pain, diarrhea or loose stool comprising administration of a single pharmaceutical comprised of an opioid, an α

3β

4-nicotinic receptor antagonist and a pharmaceutical carrier thereof.

2. ) The method of claim 1 where the opioid is any one from the group of:

alfenanil;

allylprodine;

alphaprodine;

anileridine;

fentanyl;

sufentanil;

carfentanil;

lofentanil;

cyclazocine;

morphine;

benzylmorphine;

desomorphine;

normorphine;

dextromoramide;

benzitramide;

clonitazene;

codeine;

dihydrocodeine;

levorphanol;

oxycodone;

propoxyphene;

meperidine;

methadone;

normethadone;

meptazinol;

nicomorphine;

LAAM;

pentazocine, cyclozine, remifentanil, heroin, morphine-6-glucuronide (“

M6G”

);

nalbuphine;

buprenorphine;

butorphanol;

meptazinol;

dezocine;

diampromide;

pethidine;

hydromorphone;

diamorphine;

dihydromorphine;

dimenoxadol;

piritramide;

nicomorphine;

tilidine;

tramadol;

opium;

beta-endorphin;

met-enkaphalin;

DAGO;

delta-enkephalin;

dynorphin A;

SKF-10,047;

peptide F;

BAM12P;

Leu-enkephalin;

N-alpha-acetylmethadone;

dihydromorphine;

etorphine;

oxymorphone.

3. ) The method of claim 1 where the α

3β

4-nicotinic receptor antagonist is any one from the group of;

dextorphan;

harmaline;

ibogaine, 18-methoxycoronaridine and mecamylamine.

4. ) The method of claim 1 where the α

3β

4-nicotinic receptor antagonist is an iboga alkaloid that is not any from the group of dextorphan;

harmaline;

ibogaine, 18-methoxycoronaridine and mecamylamine.

5. ) A method for administering to a human an opioid and decreasing the illicit use of said opioid where said opioid is contained in a single pharmaceutical comprising said opioid, an α

3β

4-nicotinic receptor antagonist and a pharmaceutical carrier thereof.

6. ) The method of claim 5 where the opioid is any from the group of:

alfenanil;

allylprodine;

alphaprodine;

anileridine;

fentanyl;

sufentanil;

carfentanil;

lofentanil;

cyclazocine;

morphine;

benzylmorphine;

desomorphine;

normorphine;

dextromoramide;

benzitramide;

clonitazene;

codeine;

dihydrocodeine;

levorphanol;

oxycodone;

oxycodone;

propoxyphene;

meperidine;

methadone;

normethadone;

meptazinol;

nicomorphine;

LAAM;

pentazocine, cyclozine, remifentanil, heroin, morphine-6-glucuronide (“

M6G”

);

nalbuphine;

buprenorphine;

butorphanol;

meptazinol;

dezocine;

diampromide;

pethidine;

hydromorphone;

diamorphine;

dihydromorphine;

dimenoxadol;

piritramide;

nicomorphine;

tilidine;

tramadol;

opium;

beta-endorphin;

met-enkaphalin;

DAGO;

delta-enkephalin;

dynorphin A;

SKF-10,047;

peptide F;

BAM12P;

Leu-enkephalin;

N-alpha-acetylmethadone;

dihydromorphine;

etorphine;

oxymorphone.

7. ) The method of claim 5 where the α

3β

4-nicotinic receptor antagonist is any from the group of;

dextromethorphan, dextorphan;

harmaline;

ibogaine, 18-methoxycoronaridine and mecamylamine.

8. ) The method of claim 5 where the α

3,4-nicotinic receptor antagonist is an iboga alkaloid that is not from the group of;

dextromethorphan, dextorphan;

harmaline;

ibogaine, 18-methoxycoronaridine and mecamylamine.

9. ) A method for administering to a human an opioid and antagonizing or inhibiting dopaminergic effects that otherwise are associated with administration of said opioid, said method comprising simultaneous administration of said opioid and an α

3β

4-nicotinic receptor antagonist.

10. ) The method of claim 9 where said dopaminergic effects are associated with pleasure, reward or wanting of said opioid.

11. ) The method of claim 9 where the opioid is any from the group of:

alfenanil;

allylprodine;

alphaprodine;

anileridine;

fentanyl;

sufentanil;

carfentanil;

lofentanil;

cyclazocine;

morphine;

benzylmorphine;

desomorphine;

normorphine;

dextromoramide;

benzitramide;

clonitazene;

codeine;

dihydrocodeine;

levorphanol;

oxycodone;

propoxyphene;

meperidine;

methadone;

normethadone;

meptazinol;

nicomorphine;

LAAM;

pentazocine, cyclozine, remifentanil, heroin, morphine-6-glucuronide (“

M6G”

);

nalbuphine;

buprenorphine;

butorphanol;

meptazinol;

dezocine;

diampromide;

pethidine;

hydromorphone;

diamorphine;

dihydromorphine;

dimenoxadol;

piritramide;

nicomorphine;

tilidine;

tramadol;

opium;

beta-endorphin;

met-enkaphalin;

DAGO;

delta-enkephalin;

dynorphin A;

SKF-10,047;

peptide F;

BAM12P;

Leu-enkephalin;

N-alpha-acetylmethadone;

dihydromorphine;

etorphine;

oxymorphone.

12. ) The method of claim 9 where the α

3β

4-nicotinic receptor antagonist is any from the group of;

dextromethorphan, dextorphan;

harmaline;

ibogaine, 18-methoxycoronaridine and mecamylamine.

13. ) The method of claim 9 where the α

3β

4-nicotinic receptor antagonist is an iboga alkaloid that is not any from the group of;

dextromethorphan, dextorphan;

harmaline;

ibogaine, 18-methoxycoronaridine and mecamylamine.

14. ) A method for administering to a human an opioid and antagonizing or inhibiting dopaminergic effects that otherwise are associated with administration of said opioid, said method comprising administration of a single combination pharmaceutical comprising said opioid, an α

3β

4-nicotinic receptor antagonist and a suitable carrier thereof.

15. ) The method of claim 14 where said dopaminergic effects are associated with pleasure, reward or wanting of said opioid.

16. ) A method for treating a human'"'"'s pain, loose stool or diarrhea comprising administration of a single pharmaceutical comprised of an opioid, an α

3β

4-nicotinic receptor antagonist, a N-methyl-D-aspartate-receptor antagonist and a pharmaceutical carrier thereof.

17. ) The method of claim 16 where the N-methyl-D-aspartate-receptor antagonist is any from the group of:

d-methadone;

dextromethorphan; and

dextrophan.

18. ) A method for administering to a human an opioid and decreasing the illicit use of said opioid where said opioid is contained in a single pharmaceutical comprising said opioid, an α

3β

4-nicotinic receptor antagonist, a N-methyl-D-aspartate-receptor antagonist and a pharmaceutical carrier thereof.

19. ) The method of claim 18 where the N-methyl-D-aspartate-receptor antagonist is any from the group of:

d-methadone;

dextromethorphan; and

dextrophan.

20. ) A method for treating a human'"'"'s pain, diarrhea or loose stool comprising administration of a single pharmaceutical comprised of an opioid, an α

3β

4-nicotinic receptor antagonist, an opioid antagonist and a pharmaceutical carrier thereof.

21. ) The method of claim 20 where the opioid antagonist is any from the group of:

Naloxone;

nalmefene; and

naltrexone.

22. ) A method for administering to a human an opioid and decreasing the illicit use of said opioid where said opioid is contained in a single pharmaceutical comprising said opioid, an α

3β

4-nicotinic receptor antagonist, an opioid antagonist and a pharmaceutical carrier thereof.

23. ) The method of claim 22 where the opioid antagonist is any from the group of:

Naloxone;

nalmefene; and

naltrexone.

24. ) A method for treating a human'"'"'s pain, diarrhea or loose stool comprising administration of a single pharmaceutical comprised of an opioid, an α

3β

4-nicotinic receptor antagonist, an non-steroidal anti-inflammatory drug and a pharmaceutical carrier thereof.

25. ) The method of claim 24 where the non-steroidal anti-inflammatory drug is any from the group of:

aspirin;

ibuprofen;

naproxen;

diclofenac;

benoxaprofen;

flurbiprofen;

fenoprofen;

flubufen;

ketoprofen;

ketorolac;

indoprofen;

piroprofen;

carprofen;

oxaprozin;

pramoprofen;

muroprofen;

trioxaprofen;

suprofen;

aminoprofen;

tiaprofenic acid;

indomethacin;

sulindac;

tolmentin;

zomepirac;

toppinac;

acemetacin;

fentiazac;

clinanac;

oxpinan; and

piroxicam.

26. ) A method for treating a human'"'"'s pain comprising administration of a single pharmaceutical comprised of an opioid, an α

3β

4-nicotinic receptor antagonist, a non-opioid analgesic that is not a non-steroidal anti-inflammatory drug, and a pharmaceutical carrier thereof.

27. ) The method of claim 26 where said non-opioid analgesic is acetaminophen.