Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Having -c- – wherein x is chalcogen – bonded directly to...
Patent
1997-01-02
1999-06-01
Jarvis, William R. A.
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Having -c-, wherein x is chalcogen, bonded directly to...
514326, 514329, 514652, A61K 3144, A61K 31445, A61K 31135
Patent
active
059088478
DESCRIPTION:
BRIEF SUMMARY
FIELD OF THE INVENTION
The present invention is related to improvements in pain relief. More specifically the invention relates to the use of a .beta.-receptor blocker in combination with an opioid, as well as pharmaceutical compositions comprising the two active ingredients. The novel combination provides unexpected enhanced efficacy in the treatment of pain.
Background of the Invention and Prior Art
Pain is maybe the most feared and disabling consequence of illness and trauma. Pain is also the most frequent reason for patients seeking medical consultation. The human suffering has obtained significant attention among the medical community and researchers. The attention is expected to grow as the great therapeutic need is high as pain increases with the aging of a population.
Historically, opioids have been used in pain relief since the 18th century in forms for oral or injectable administration. However, the problems with opioids such as e.g. morphine, are their severe side effects which hamper their widespread use and acceptance both by physicians as well as patients. The side effects include e.g. addiction, nausea, inhibition of breathing, somnolence and dysphoria, all of which are mediated by opioid action within the brain.
Most of the side effects depend on the amount of opioid drug used. It is therefore necessary to attempt to use as low dose as possible of the opioid drug, but the problem then arises that if the dose is lowered, too much of the anaesthetic effect disappears.
In the publication by Navarro V. et al, "Synergistic effect of meperidine and propranolol in dogs", veterinaria (Mexico City) (1982). 13(4), 183-7, chemical Abstracts no. 99; 32 787, the combination of propranolol and meperidine is disclosed. However, nothing is mentioned that this combination is advantageous in the treatment of pain.
Outline of the Invention
The present invention is based on the concept of a novel combination therapy, whereby a .beta.-receptor blocker or a pharmacologically acceptable-salt thereof, and an opioid or a physiologically and pharmaceutically acceptable salt thereof, are administered simultaneously, sequentially or in form of a pharmaceutical composition comprising the two active ingredients, optionally together with a pharmaceutically acceptable carrier.
In order to obtain the advantageous effects of the present invention, the .beta.-receptor blocker and the opioid must be administered as a combination, either simultaneously or sequentially. In particular the dosage form and route of administration for each must be selected so that the therapeutic effects of each are manifest at the same time.
By the wording "simultaneous administration" is intended that the two active ingredients are given at the same time.
By the wording "sequential administration" is intended that the two active ingredients are given one after the other, i.e. first the .beta.-receptor blocker is administered, and thereafter the opioid is administered or vice versa, meaning that it does not matter in which order the two active ingredients are administered. Preferably the time interval between the administration of the .beta.-receptor blocker and the opioid, or vice versa, is not exceeding 2 hours.
Alternatively the two active ingredients may be in form of a pharmaceutical composition comprising the two active ingredients, optionally in the presence of a pharmaceutically acceptable carrier, or any additional active or inactive substances.
The .beta.-receptor blockers which can be used for the combination therapy according to the present invention include each of the known pharmaceutically useful .beta.-receptor blockers, e.g. alprenolol, propanolol, pindolol, sotalol, timolol and moreover selective .beta.-receptor blockers such as metoprolol, atenolol, betaxolol, and bisoprolol. These .beta.-receptor blockers are however only examples and should not be construed as limiting the invention in any way. Also within the scope of the invention are racemates and enantiomers of the .beta.-receptor blockers used.
The opioids useful i
REFERENCES:
patent: 4885173 (1989-12-01), Stanley et al.
Millan et al, Chemical Abstracts, vol. 124, abstract No. 194761, 1995.
Kihara et al, Chemical Abstracts, vol. 106, abstracts No. 537, 1986.
Werner et al, Derwent Drug File Abstracts, vol. 83, abstract No. 09010, 1982.
Navarro, et al., "Efecto Sinergico de la Meperidina y el Propranolol en el Perro," Veterinaria Mex 13:183-187 (1982).
STN International, File CAPlus, Accession No. 1983:432787, abstract No. 99:32787, Navarro, et al., "Synergistic Effect of Meperidine and Propranolol in Dogs," Veterinaria Mex . 13:183-187 (1982).
International Search Report for Swedish appl. No. 9503476-5 (priority appl. of PCT/SE96/01248), 1997.
Astra AB
Jarvis William R. A.
Sanzo Michael A.
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