Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Having -c- – wherein x is chalcogen – bonded directly to...
Patent
1996-05-23
1999-09-14
Henley, III, Raymond
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Having -c-, wherein x is chalcogen, bonded directly to...
A61K 3144
Patent
active
059523409
DESCRIPTION:
BRIEF SUMMARY
This invention relates to prevention and treatment of post-operative nausea and vomiting (PONV), and pharmaceutical compositions therefor.
PONV is an important patient problem and one that patients rate as the most distressing aspect of operative procedure, even above pain. Consequently, the need, from the patients' perspective, for an effective anti-emetic in this area is important. As a clinical problem PONV is troublesome and requires staff around to ensure that vomitus is not regurgitated, which can have very serious clinical sequela There are certain operative procedures where it is clinically important that patients do not vomit. For example, in occular surgery where intra-cranialloccular pressure can increase to the extent that stitches are ruptured and the operative procedure is set back in terms of success to a marked degree.
Thus from the point of view of patients and clinicians, the control of PONV is essential.
Financially, the control of PONV is also important. In regions such as the U.S.A., a lot of surgery is done in the day-care setting and the importance of being able to send patients home without an overnight stay is financially attractive. In other countries the popularity of day-care surgery is increasing and it may reach to over 50% in 5-10 years time.
The number of operations done per year in the Western world and Japan is in the order of 65 million. Many anaesthetists currently use prophylactic anti-emetic such as low dose metoclopramide (10 mg) pre- or peri-operatively and many use no prophylactic anti-emetics at all due to poor efficacy of current agents coupled with troublesome side-effects such as dystonic reactions and somnolence. Thus the need for a safer and efficacious antiemetic in PONV is present.
Example 6 of EP-A-200444 (Beecham Group p.l.c.) describes the preparation of the compound, granisetron (or BRL 43694 monohydrochloride) which is available in the United Kingdom as KYTRIL.sup.1 a drug for treating cytotoxic agent induced nausea and vomiting.
We have now found that granisetron is of potential use in the prevention and treatment of PONV.
Accordingly, the present invention provides the use of granisetron in the manufacture of a medicament for the treatment (including prophylaxis) of PONV.
The present invention also provides a method of treatment of (including prophylaxis) of PONV in mammals, including man, by administration of granisetron to the mammal in need thereof.
The administration of granisetron may be by way of known methods, such as oral, or parenteral administration.
An amount effective to treat the disorder hereinbefore described depends on the usual factors such as the nature and severity thereof and the weight of the mammal. However, a unit dose will normally contain 0.5 to 10 mg, for example 1 to 3 mg of granistron. A unit dose will normally be administered pre-operatively such as prior to induction of anaesthesia or peri-operatively; and/or post-operatively.
For oral or parenteral administration, it is greatly preferred that granisetron is administered in the form of a unit-dose composition, such as a unit dose oral or parenteral composition.
Such compositions are prepared by admixture and are suitably adapted for oral or parenteral administration, and as such may be in the form of tablets, capsules, oral liquid preparations, powders, granules, lozenges, reconstitutable powders, injectable and infusable solutions or suspensions or suppositories.
Tablets and capsules for oral administration are usually presented in a unit dose, and contain conventional excipients such as binding agents, fillers, diluents, tabletting agents, lubricants, disintegrants, colourants, flavourings, and wetting agents. The tablets may be coated according to well known methods in the art.
Suitable fillers for use include cellulose, mannitol, lactose and other similar agents. Suitable disintegrants include starch, polyvinylpyrrolidone and starch derivatives such as sodium starch glycollate. Suitable lubricants include, for example, magnesium stearate. Suitable pharmaceutically acc
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S. Bingham and P.D. King, (1992). In: Bianchi AL, Grelot L, Miller AD, King GL, eds. Mechanisma and control of emesis, Paris: INSERM/John Libbey Eurotext, 223, 249-250.
Buchheit K-H, Games R, Bertholet A, Buscher HH (1989). Gastroenterology, 96, A63.
P.L.R. Andrews, "Physiology of Nausea and Vomiting", British Journal of Anaesthesia, 69, No. 7(1), pp. 2-19 (1992).
Bunce et al., "The Role of 5-HT in Postoperative Nausea and Vomiting", British Journal of Anaesthesia, 69, No. 7(1), pp. 60-62 (1992).
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Davey Philip Timothy
Dott Christopher Stuart
Sanger Gareth John
Dustman Wayne J.
Henley III Raymond
King William T.
Kinzig Charles M.
SmithKline Beecham p.l.c.
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