Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Having -c- – wherein x is chalcogen – bonded directly to...
Patent
1994-06-28
1997-09-23
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 31445
Patent
active
056705247
DESCRIPTION:
BRIEF SUMMARY
This application is a 371 of PCT/SE94/00469 filed May 26, 1994.
1. Field of the Invention
The present invention is related to the use of a low concentration of a pharmaceutically acceptable salt of ropivacaine in the manufacture of pharmaceutical preparations for pain relief post operatively and in labour.
2. Background of the Invention
Post operative pain relief is still a problem within modern surgery. According to a newly published study about 70% of all patients treated surgically felt moderate to severe pain after the surgical treatment.
The need for qualified pain relief is greatest during the first 24 hours after the surgical treatment. The traditional method to treat the patients is to give narcotics intramuscularly or intravenously. Such treatment is often insufficient as narcotic analgetics have many negative effects. One disadvantage is depression of the breathing, which may occur even after treatment. This means that the patient must be intensively looked after by specialists.
A patient, who has been treated with morphine is tired, apathetic and is often feeling sick. The patient thus has no interest in things around him. It is thus difficult to take care of the patient and make him participate in respiratory exercises and prophylaxis for thromboses.
One method is administration epidurally, by infusion or intermittent injections of local anaesthetics. Such treatments can only be carried out on patients with epidural catheters being taken care of at an intensive care or post surgical unit by specially trained persons.
There has been a long felt need at ward level to be able to give a greater group of patients qualified pain relief by epidural infusion of e.g. local anaesthetics instead of opiates.
Normally, with local anaesthetics a good blockade of the pain is obtained. The drawback is the motor blockade in the legs, which is disturbing to the patients, who wants to give up the pain relief treatment in advance. Among other effects the motor blockade means that the patient cannot leave his bed without assistance as the legs will not bear.
Outline of the invention
According to the present invention it has surprisingly been found that the local anaesthetic agent ropivacaine, described e.g. in WO/85/00599, in form of its hydrochloride can be given to the patient in a dosage which gives pain relief with minimal effect on motor function. This is at a dosage of lower than 0.5% by weight, especially from 0.01% to 0.45% by weight. Such low dosages are normally considered to be ineffective. The normal dosage is from 0.5-2% by weight.
The local anaesthetic compound used according to the invention is in the form of its pharmaceutically acceptable salts. It is especially preferred to use ropivacaine hydrochloride.
The local anaesthetic is incorporated into a solution.
The local anaesthetic composition contains less than 0.5% by weight of the local anaesthetic compound, preferably from 0.01 up to 0.45% by weight, especially preferred 0.1-0.3% by weight.
Pharmaceutical Preparations
EXAMPLES 1-3
Solution 5 mg/ml, 3 mg/ml, 2 mg/ml
______________________________________ Examples
1 2 3
______________________________________
Ropivacaine hydrochloride
0.53 kg 0.32 kg 0.21 kg
monohydrate
Sodium hydroxide 2M to
pH 5.0-6.0
Purified water qs ad
100 kg 100 kg 100 kg
______________________________________
Ropivacaine is dissolved in the water. Sodium hydroxide is added to pH 5.0-6.0. The resulting solution is autoclaved.
The best mode of carrying out the invention known at present is to use the preparations according to Example 3.
A double blind study of sensory and motor blockade with 0.1%, 0.2%, 0.3% ropivacaine and 0.25% bupivacaine during continuous epidural infusion in healthy male volunteers.
The aim of the study was to find a low concentration of ropivacaine giving a sufficient sensory block but as little or no motor block at all during continuous epidural infusion. This study is a first step towards finding a low concentration of ropivacaine which later will be used for treatment of
REFERENCES:
"Drugs of the Future", vol. 14, No. 8, pp. 767-771 1989.
Concepcion et al., Anethesia and Analgesia, 70(1), pp. 80-85 (abstract only) 1990.
Wahedi et al. Regional-Anaesthesie, 13(3), pp. 57-65 (abstract only) 1990.
Wahedi et al., Regional-Anaesthesie, 13(3), pp. 66-72.(abstract only) 1990.
Zaric et al., Anesthesia and Analgesia, 72(4), pp. 509-515 (abstract only) 1991.
Katz et al., Biopharmaceutics & Drug Disposition, 14(7), pp. 579-588 1993.
Wood et al., Anesthesia and Analgesia, 76(6), pp. 1274-1278 1993.
Chem. Abst. No. 117:239834, Broberg et al. 1992.
Chem. Abst. No. 115:22086, Cederholm et al. 1991.
Chem. Abst. No. 111:90290, Kopacz et al. 1989.
Brockway, M.S. et al., "Comparison of Extradural Ropivacaine and Bupivacaine," British Journal of Anaesthesia 66:31-37 (1991).
Concepcion, M. et al., "A New Local Anesthetic, Ropivacaine, Its Epidural Effects in Humans," Anesth. Analg. 70:80-85 (1990).
Zaric, D. et al., "Blockade of the abdominal muscles measured by EMG during lumbar epidural analgesia with ropivacaine--a double-blind study," Acta Anaesthesiol 37:274-280 (1993).
Astra AB
Henley III Raymond
Sanzo Michael A.
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