Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Having -c- – wherein x is chalcogen – bonded directly to...
Reexamination Certificate
1998-07-22
2001-08-14
Spivack, Phyllis G. (Department: 1614)
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Having -c-, wherein x is chalcogen, bonded directly to...
Reexamination Certificate
active
06274591
ABSTRACT:
FIELD OF THE INVENTION
The present invention is directed at the treatment of certain side effects associated with the use of opioids as analgesics. In particular the present invention is directed at treating opioid-induced inhibition of gastrointestinal motility and constipation.
BACKGROUND OF THE INVENTION
Opioids are effective analgesics. However, their use is associated with a number of undesirable side effects. One such effect is constipation. Opioid-induced changes in gastrointestinal motility are almost universal when these drugs are used to treat pain, and at times may limit their use, leaving the patient in pain. Common treatments of bulking agents and laxatives have limited efficacy and may be associated with side effects such as electrolyte imbalances.
One treatment for opioid side effects is the use of opioid antagonists which cross the blood-brain-barrier, or which are administered directly into the central nervous system. Opioid antagonists such as naltrexone and naloxone have been administered intramuscularly or orally to treat opioid induced side effects. Naltrexone and naloxone are highly lipid soluble and rapidly diffuse across biological membranes, including the blood-brain barrier. However, naltrexone, naloxone, nalmefene, and other opioid antagonists which may reverse many opioid side effects have a narrow therapeutic window before they are observed to reverse the desired analgesic effect of the opioid being used.
Many quaternary amine opioid antagonist derivatives, such as methylnaltrexone, do not reduce the analgesic effect of opioids. These quaternary amine opioid antagonist derivatives, which have a relatively higher polarity and reduced lipid solubility when compared to the tertiary forms of the drugs, were specifically developed to not traverse the blood-brain barrier or to traverse it at a greatly reduced rate. However, high levels of MNTX in the plasma can lead to undesirable side effects such as orthostatic hypotension.
It is desirable in the treatment of many conditions to have oral medications with prolonged effects. Such oral medications are particularly desirable for the treatment of opioid-induced side effects.
It is further desirable to develop a method for the prevention of opioid-induced inhibition of gut motility and constipation which does not counteract the analgesic effects of the opioid, or risk increased levels of pain. Ideally, such a treatment has few side effects either due to low drug toxicity or because administration of small amounts are effective and/or administration results in low circulating levels of the drug.
REFERENCES:
patent: 4176186 (1979-11-01), Goldberg et al.
patent: 4311833 (1982-01-01), Namikoshi et al.
patent: 4377568 (1983-03-01), Chopra
patent: 4385078 (1983-05-01), Onda et al.
patent: 4457907 (1984-07-01), Porter
patent: 4462839 (1984-07-01), McGinley et al.
patent: 4518433 (1985-05-01), McGinley et al.
patent: 4556552 (1985-12-01), Porter et al.
patent: 4606909 (1986-08-01), Bechgaard et al.
patent: 4615885 (1986-10-01), Nakagame et al.
patent: 4670287 (1987-06-01), Tsuji
patent: 4987136 (1991-01-01), Kreek et al.
patent: 5536507 (1996-07-01), Abramowitz et al.
patent: 5567423 (1996-10-01), Ying
patent: 5591433 (1997-01-01), Michael et al.
patent: 5597564 (1997-01-01), Ying
patent: 5609871 (1997-03-01), Michael et al.
patent: 5614222 (1997-03-01), Kaplan
patent: 5626875 (1997-05-01), Rodes et al.
patent: 5629001 (1997-05-01), Michael et al.
patent: 5811451 (1998-09-01), Minoia et al.
patent: 5866164 (1999-02-01), Kuczynski et al.
patent: WO98/25613 (1995-06-01), None
patent: WO97/33566 (1997-09-01), None
Yuan, Chun Su et al.,European Journal of Pharmacology, 276:107-111, 1995.
Yuan, Chun Su et al.,Clinical Pharmacology&Therapeutics, 61:467-75, 1997.
Foss, Joseph F.,The Journal of Clinical Pharmacology, 1997;37:25-30.
Yuan, Chun Su et al.,Clinical Pharmacology&Therapeutics, 59:469-75, 1996.
Drell William
Foss Joseph F.
Moss Jonathan
Roizen Michael F.
Yuan Chun-Su
Christie Parker & Hale LLP
Spivack Phyllis G.
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