Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Heavy metal containing doai
Reexamination Certificate
2001-05-14
2002-09-17
Reamer, James H. (Department: 1614)
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Heavy metal containing doai
C514S262100
Reexamination Certificate
active
06451850
ABSTRACT:
SPHERE OF TECHNOLOGY
The present invention applies to medicine, more specifically, to pharmacology and it can find applications in pharmacotherapy for all kinds of diseases including decrease of organism intoxication under taking medicines.
PREVIOUS LEVEL OF TECHNOLOGY
A search for ways of strengthening of medicines action on the human organism goes on for a long time. It is connected both to insufficient therapeutic effect of the compound and to its insufficient quantity which is applied for treatment and cannot be increased owing to onset of its toxic effect as far as practically all the compounds exert an adverse effect including non-allergic negative side effect, allergic reactions, toxic effects, etc. [1]. Manifestations of non-allergic side effect include only the effects which appear under application of compounds in therapeutic doses and compose a spectrum of their pharmacological action. Thus, under application of tranquilizers quickness of mental and-physical reactions decreases, sleepiness appears; in the case of analgetics, e. g., acetylsalicylic acid, ulcerogenic action and other side effects are observed.
Side effects can be primary and secondary ones. The primary effect appears as a direct result of the present medicine influence on a certain substrate (e. g., nausea, vomiting under an irritating action of a compound on a mucous membrane of the stomach). The secondary side effect concerns unfavorable side influences (e. g. hypovitaminosis as a result of intestinal flora suppression with antibiotics) [1]. Unfavorable effects of compounds are highly diverse by their character; they have unequal expression and different duration. Side effects can be directed towards the nervous system, blood and hematogenesis, blood circulation organs, respiration, digestion, kidneys, endocrine glands, etc. Some side effects are endured relatively easily (moderate nausea, headache, etc.), other ones can be serious and even dangerous for life (liver affection, leucopenia, aplastic anemia) [1]. Negative influences exerted by medicaments also include allergic reactions, frequency of which is high enough. They appear independently from the dose of applied compound [1]. Clinical picture of allergic reactions is very different. There can appear urticaria and other skin erruptions, angioneurotic edema, serum sickness, bronchial asthma, breach of hemopoiesis, fever, hepatitis, cholestatic jaundice, anaphylactic shock, etc. [1].
Idiosyncrasy is another possible cause of unfavorable responses to compounds. Compounds cause toxic effects in doses over therapeutic ones. The last named generally manifest themselves as some serious breaches of functions of organs and systems (hearing decrease, vestibular disturbances, blindness as a result of optic nerve lesion, an expressed breach of stimulation conduction via the myocardium, liver lesion, breach of hemopoiesis, suppression of vitally important centers of medulla oblongata). The main cause of toxic effects is overdosage—occasional or deliberate exceeding of maximum permissible doses. Moreover, accumulation of toxic concentrations of compounds in the organism is possible as a result of breaches of their metabolism (e.g., under liver pathology) or under slow excretion of these (under some kidney diseases). Being prescribed during pregnancy medicaments can exert a detrimental effect on the embryo and fetus. Such effects include teratogenic impact of compounds, which causes birth of children with various anomalies [1]. Medicaments can possess mutagenous and embryotoxic properties. These properties are especially intrinsic for antitumoral agents. In the case of some compounds drug dependence can develop under repeated application. It manifests itself as irresistible yearning for application of the compounds, usually with the aim of improvement of mood or with the purpose to feel better, to get rid of suffering or unpleasant senses and feelings including ones which appear under abolition of compounds causing the drug dependence.
Psychical drug dependence and physical one are recognized. In the case of psychical drug dependence discontinuance of the drugs application (e. g., cocaine or hallucinogens) leads only to emotional discomfort. Under application of some compounds physical drug dependence can be in progress. In this case abolition of the drug causes grave condition which, in addition to acute psychical changes, manifests itself as various and often serious somatic breaches connected to functional disorder of many systems of the organism. This is the so called abstinence syndrome or deprivation phenomenon [1]. A search of ways for reduction of unfavorable effects of medicaments goes on for a long time. A big number of compounds for the specific treatment of drug poisoning, which are called antidotes and antagonists, include compounds which inactivate poisons either via chemical and physical interaction or at the sacrifice of pharmacological antagonism (at the level of physiologic systems, receptors, etc.). Thus, under intoxication with heavy metals, compounds are applied which form non-toxic complexes with the metals (e.g., unithiol, penicillamine, CaNa
2
EDTA). Antidotes are known, which react with the compound and release the substrate (e. g., oximes, which are cholinesterase reactivators; antidotes, which are applied under intoxication with methemoglobin formers, act in a similar way). Pharmacological antagonists are of considerable use under acute poisonings (atropine—under poisoning with anticholinesterase agents, naloxone—under poisoning with morphine, etc.). Pharmacological antagonists usually enter into competitory interactions with the same receptors, which interact with the compounds which caused the poisoning [1]. However, antidotes and antagonists are specific compounds characteristic for a specyfic type of intoxications and these are not applied under application of medicaments in therapeutic doses [1]. Antidotes and antagonists are not applied as complexes with medicaments.
To expand medicaments effect spectrum and promote pharmacological effect of compounds and decrease their toxicity, compounds with various composition were investigated including organogermanium ones.
Among organogermanium compounds (OGC), therapeutic effect of 2-carboxyethyl-germanium sesquioxide (O
1,5
GeCH
2
CH
2
COOH)
n
and its derivatives has been much investigated. Authors applied this compound and its derivatives as original medicaments. There exist examples of its applications in cosmetics, as a nutrition additive and as an original medicament [2]. 2-Carboxyethylgermanium sesquioxide and its derivatives have been much investigated as original anticancerogenic medicaments in clinics and found not sufficiently powerful [2].
The medicament manifested therapeutic effect in high doses, usually 100-200 mg/day, what, as it has been found later, leads to various health breaches [2]. The authors have not claimed a universal effect for expansion of the medicaments effect spectrum, strengthening of pharmacological effect of the compounds and decrease of the drug toxicity [2-11].
To promote the main pharmacological effect, medicaments are often applied on the background of various stimulants (e. g., specific antibacterial therapy on the background of immunostimulation).
Applied in therapeutic practice, immunopotentiators are the closest by their effect to the claimed compounds.
Medicaments, which stimulate (normalize) immune reactions, are applied in complex therapy of immunodeficient states, chronic infections and malignant tumors. Biogenic substances are applied as immunopotentiators (thymus preparations, interferon, BCG vaccine) and synthetic compounds (Levamisolum, sodium diethylthiocarbamate, etc.) [1].
Tactivinum (T-activin) normalize quantity and function of T-lymphocytes (in immunodeficient states), stimulates production of lymphokines, &agr;- and &bgr;-interferons, rehabilitates suppressed production of T-killers and i
Chernyshev Evgeny Andreevich
Khromova Nataliya Yurievna
Komalenkova Nina Georgievna
Kotrelev Mikhail Vladimirovich
Pavlov Konstantin Vitalevich
Greer Burns & Crain Ltd.
Reamer James H.
Soloviev Evgeny Vladimirovich
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