CS264691B1 - Analgesic agent - Google Patents

Abstract

The solution concerns increasing the analgesic effect by combining an analgesic with antidepressants. An analgesic preparation with an antidepressant containing dosulepin and ibuprofen or paracetamol. The combination will be suitable for chronic pain syndromes regardless of their etiology and pathogenesis. It will make life easier for people with pain in cancer.

Description

According to various estimates, 8-15% of the population suffer from chronic or periodic recurring pain whose cause remains unclear or unknown, but cannot be solved by Tilo people more or less Irvale or in frequently repeated episodes using analgesics. These are generally various mass-produced analgelic combinations (Acylcoffin, Alnagon, Dinyl, Sedolor, Veralgin, etc.). Efforts to exclude from these combinations substances with toxic side effects (phenacetin, aminophenazone) and substances where there is a risk of addiction (barbiturates, codeine) led to the introduction of a new type of combination products consisting of analgesics (paracetamol, acetylsalicylic acid) with guaifenesin, with myorelaxant and mild anxiolytic effect (Ataralgin, Guajanal, Rovenal). This innovation was an undisputed advance and the growing consumption of these combination products confirmed the results of their clinical trials demonstrating their therapeutic benefits. Nevertheless, these new drug combinations did not lead to the desirable major move away from Alnagona-type medicines, whose consumption continued to increase and the situation eventually required a radical administrative intervention, which was bound by the prescription of the drug.

Chronic or frequently recurring pains lead to the development of depressive syndromes, the symptomatology of which sometimes makes it difficult to distinguish whether the subjectively experienced and described pain is a symptom of depression rather than a manifestation of organic damage. This distinction is even more complex and difficult in the case of psychogenic pain. Some psychopathological schools also consider depression a “psychic pain”.

Although the physician's task remains to improve the diagnosis of these conditions and to find and then treat the cause, at least it is not yet possible to ignore the fact that in practice it is not always possible. This failure is contributing to the increase in the number of people who solve their difficulties by regularly using combined analgesic drugs prescribed by doctors or obtaining them without a prescription. Research in recent years has shown that these drugs are often abused as day-to-day doping and, in fact, are more stimulating than analgesic in chronic use.

The solution can be sought in two ways:

1, Improvement of the already established pathway by combining an analgesic-antipyretic with an anxiolytic by using a highly potent anxiolytic-diazepam myorelaxant, which additionally has a sedative effect, instead of a mildly active guaifenesin. The main indication area of such a combination drug will be acute pain syndromes associated with spinal pathology (discogenous syndromes, lumboischiadic syndromes, cephalgia associated with cervical spine changes, etc.), increased muscle tone and muscle spasms.

The major risk of such a drug could be drug dependence. This could be avoided by prescribing the medication and instructing physicians that it should not be given for more than 3-4 weeks. The acute pain syndromes for which this drug will be indicated will usually be managed within 5-10 days.

This disadvantage will more than be counterbalanced by a suitable potentiating effect of the analgesic-analgelics and the highly effective anxiolytic-muscle relaxants. As is well known, psychic tension also leads to an increase in muscle tone (this is clearly evident in the facial expression), which results in pain.

2. A qualitatively new approach will be the combination of an analgesic with a thymoleptic. Theoretically, it is possible to rely on the results of animal experiments here (Zábojníkové M „Kovalčík V., Jirásková M .: Interaction of Benactyzine with Analgesia and Prothiadene, Activ. Nerv. Supar. 15. 2. 135, 1973), that the effect of the analgesic was potentiated by dosulepin.

The combination of dosulepine with analgesics will be suitable for chronic algic syndromes regardless of their etiology and pathogenesis. Among other things, it will facilitate the existence of people with cancer pain, etc. Evidence of the analgesic effect of antidepressants can be found in J. Švihovec, M. Kršiak, O. Vinař: Contemporary Possibilities of Pain Pharmacotherapy. Time. medicine. čes. 125, 773-777 (1986).

In Scandinavia there is more than twice the consumption of antidepressants compared to Czechoslovakia. One of the likely explanations is that there are many more people with pain syndromes treated with antidepressants than in our country, where again we have a high consumption of analgesics. The proposed combination medicine could replace the previously used and misused products (Alnagon, Dinyl) and would contribute to reducing or even eliminating the difference in drug consumption in the Czech Republic and Scandinavia. The main benefit would be increased therapeutic efficacy and ease of drug use. Chronic algic syndromes often suffer from older people who have multiple diseases (polymorbidity) and use more types of drugs. The multiplication of this number is associated with the risk of poor compliance. Combining a thymoleptic with an analgesic in one tablet would be a significant advance.

It is often not easy to convince a patient to take an antidepressant or other drug declared as a psychopharmacone. A patient with an algic syndrome, in particular, often begins to think that the doctor thinks he is "telling" or even simulating his pain. Since, as a rule, antidepressant does not provide the expected relief immediately after the start of administration, many patients refuse to take it or, more often, do not tell the doctor that they are not taking it. An analgesic in combination with an antidepressant causes a rapid onset of action, the patient gains confidence in the drug, and at the time when the analgesic's tolerance and action may eventually occur, the antidepressant and analgesic effect of the antidepressant itself becomes effective. As a first step, a combination of analgesics with dosulepine is proposed. Dependence on this drug has not been described so far, and it is likely that patients could use the proposed combination on a long-term basis. After their effects have been tested in practice, some will be appropriate

CS 264 691 B1 from combinations can be dispensed in pharmacies without a prescription and thus medically justified to replace products of the type Alnagon.

The first step is a composition of the invention comprising a combination of 10 to 50 parts by weight of dosulepin and 250 to 500 parts by weight of ibuprofen or 300 to 550 parts by weight of paracetamol.

The composition of the invention may be formulated into conventional dosage forms such as tablets, etc.

The following examples serve to illustrate the preparation according to the invention and do not limit the scope of the invention in any way.

Claims (1)

Analgesic preparation with antidepressant, characterized in that it contains from 10 to 50 parts by weight of dosulepin optionally in the form Example 1 Dosulepin 15 mg Ibuprofen 350 mg Example 2 Dosulepin 15 mg Paracetamol 500mg Example 3 Dosulepin 40 mg Ibuprofen 400 mg INVENTION a pharmaceutically acceptable salt and 250 to 500 parts by weight of ibuprofen or 300 to 550 parts by weight of paracetamol.