Use of creatine

Details Use of creatine Use of creatine

1999-04-19

2001-06-05

Criares, Theodore J. (Department: 1617)

Drug, bio-affecting and body treating compositions

Designated organic active ingredient containing

Radical -xh acid, or anhydride, acid halide or salt thereof...

Reexamination Certificate

active

06242490

ABSTRACT:

This invention refers to a new use of creatine, in particular in the preparation of a drug for the treatment of cardiac and/or respiratory insufficiency.
Creatine is a substance that plays an essential role in the metabolism of energy in humans and animals. A certain quantity of this vital compound is produced autonomously by our body, whereas a variable quantity is introduced through diet, basically through meat-based foods (J. B. Walker et al., in Adv. Enzymol. 1979, 50, 177-242).
It is well known that the assumption of exogenous creatine can improve the capacity to make brief and intense efforts (maximum exercise) both in normal subjects and in athletes (P. L. Greenhaff, in Clinical Science (1993), 84, 565-571; P. D. Balsom et al., in Scand. J. Med. Sci. Sports 1993, 3: 143-149).
Effects on the capacity to achieve maximum efforts have also been obtained using relatively high doses (15-20 g/die).
However, doses of this kind produce considerable collateral effects, such as gastrointestinal disorders, weight gain and water retention, representing a drawback to the prolonged use of creatine which is therefore not administered to improve the capacity of carrying out prolonged exercises (endurance) (P. D. Balsom et al., in Acta Physiol. Scand. 1993, 149, 521-523).
Moreover, the aforesaid doses, which are required to improve the capacity to perform maximum efforts, must be subdivided into several daily doses given that the administration of a single dose of more than 4-5 grams exceeds the so-called “renal threshold” and any excess substance is eliminated directly through urine without having performed any useful function at a systemic level.
The oral administration of creatine has been studied in patients suffering from cardiac insuffiency in whom it has shown a marked capacity to increase maximum effort.
Again in this case, however, the action of the substance was obtained at very high doses (15 g/die) (A. Gordon et al., in Cardiovascular Research 30 (1995) 413-418).
Owing to the aforesaid reasons, doses of this type cannot be used outside a closely contolled clinical trial performed for short periods.
It is clear that the collateral effects described earlier, which are evident in normal subjects, entail particularly high levels of risk for patients whose cardiovascular system is already damaged and/or fatigued by disease, thus representing a genuine obstacle to the administration of creatine.
Furthermore, compared to healthy subjects, the muscular energy metabolism of patients with heart and/or respiratory disorders is further damaged (B. M. Massie et al. in Circulation—vol.78, no. 2, 1988, 320-326; B. M. Massie et al., The American Journal of Cardiology, 1987, 60, 309-315) and treatment must not only take account of the general conditions, which are already critical owing to the underlying pathology, but also weigh up the negative effects of a reduced availability of energy.
Although the results of experiments in healthy subjects show that creatine doses of under 10-15 g/die are not efficacious, much lower doses (1-4 g/die) have been used as a food supplement in the diet of elderly, debilitated and/or vegetarian subjects with a marked antiasthenic effect.
Moreover, doses of this type have been much better tolerated for prolonged periods.
Surprisingly, it has now been found that creatine, administered at low doses (1-4 g/die), enables an improved efficiency of energy metabolism at a muscular level and also results in a general improvement in the exercise capacity of patients suffering from cardiac and/or respiratory insufficiency.
The subject of this invention is therefore the use of creatine in the preparation of a drug for the treatment of cardiac and/or respiratory insufficiency in which creatine is included at a dose ranging between 1 and 4 g/die.
In particular, it was surprisingly found that the use of creatine at the aforesaid doses was extremely beneficial for the preparation of a drug for the treatment of obstructive bronchopathies at an advanced stage.
The oral administration of the drug was found to be particularly well tolerated.
The drug prepared according to the method described by this invention can be realised using common pharmaceutical techniques and may include, in addition to a vehicle and/or pharmaceutically acceptable diluent, also one or more active ingredients, for example: amino acids, like arginine, valine, leucine and isoleucine, complex sugars and/or antioxidants.
The following example illustrates the invention but is in no way restrictive.


REFERENCES:
patent: 4371521 (1983-02-01), Izrael
patent: 9402127 (1994-02-01), None
patent: WO 98/00148 (1998-01-01), None
Gordon, et al., “Creatine Supplementation in Chronic Heart Failure Increases Skeletal Muscle Creatine Phosphate and Muscle Performance”Cardiovasc. Res., vol. 30, 1995, p. 413-418.
Volkov, et al., “Metabolic Correction of Psychic Disorders In Patients With Bronchial Asthma”,Allergy, vol. 51, No. Suppl. 32, 1996, p. 98.
Scattolin et al., “Diastolic Function and Creatine Phosphate: An Echographic Study”,Current Therapeutic Research, vol. 54, No. 5, 1993, p. 562-571.
Bichev, A.A., “The Effect of Exogenous Phosphocreatine on Function of Respiratory Muscles During Pulmonary Diseases”,Eur. Resp. J., vol. 7, No. S. 18, 1994, p. 343s.
Greenhaff et al. “Influence of Oral Creatine Supplementation of muscle torque during repeated Bouts Maximal Voluntary Exercise in Man”,Clinical Science, vol. 84, 1993, p. 565-571.
Balsom et al., Creatine Supplementation per se Does Not Enhance Endurance Exercis Performance:ACTA Physiol. Scand., vol. No. 149, 1993, p. 521-523.
Cafiero et al. “Efficacia della creatina fosfato nel trattamento dei pazienti con insufficienza cardiaca”,Clinical Therapeuticalvol., No. 4., 1994, p. 321-328.
Nagle, S., “Die Bedeutung von Kreatinphosphat und Adenosintripholt im Hinblick auf Energiebereitstellung, transport und-verwertung im normalen und insuffizienten Herzmusckel”,Klin. Wochenschrift, vol. 48, No. 6, 1970, p. 332-341.

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