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Biomedical subjects

A von Schlichtegroll

Publications and source records attributed to A von Schlichtegroll.

15 recordsLinked to original sources
PubMed1986

Mefenorex (Rondimen).

Mefenorex, N-(3-chloropropyl)-alpha-methylphenethylamine, (RONDIMEN), is included in the list of centrally acting stimulants and/or hallucinogens or related compounds to be considered by a World Health Organization (WHO) Expert Committee in 1985 for possible scheduling under the Convention on Psychotropic Substances, 1971. The therapeutic efficacy of mefenorex as an adjunctive support in the treatment of obesity for limited periods of time, as well as its ability to be well tolerated, has been amply demonstrated. There have been no reports of actual abuse. There have been no reports of illicit trafficking, falsification of packages or materials, or clandestine laboratories manufacturing the compound. Data from preclinical and clinical studies do not suggest a potential for abuse similar to that of amphetamine or related compounds. Moreover, the lack of pulmonary hypertension with mefenorex has been demonstrated in both preclinical and clinical studies. There have been no reports of any public health or social problems associated with mefenorex use. The compound is a well-tolerated anorectic agent with little central stimulant activity.

Adult↗
PubMed1986

Fenetylline: new results on pharmacology, metabolism and kinetics.

In the fenetylline molecule, theophylline is covalently linked with amphetamine via an alkyl chain. The inclusion of amphetamine and results from early metabolic studies have led to speculation that fenetylline may be merely a prodrug for amphetamine and/or theophylline. Although previous studies are not consistent with this hypothesis, additional studies were conducted to comparatively evaluate the profiles of activity exhibited by fenetylline and its two postulated primary metabolites, (+/-)-amphetamine and theophylline. Investigations were also initiated using newly developed high pressure liquid chromatography (HPLC) techniques to further characterize the metabolic pattern that fenetylline undergoes and to examine the relationship between plasma pharmacokinetics and the pharmacodynamic actions of the drug. Fenetylline inhibits activity associated with amphetamine in certain test systems, an effect similar to that previously observed with fenfluramine. Only small amounts of the amphetamine theoretically available in the fenetylline molecule are released. Pharmacodynamic activity associated with fenetylline administration is more closely tied to plasma levels of the parent compound than to any (+/-)-amphetamine produced.

Amphetamines↗
PubMed1986

Fenetylline: therapeutic use, misuse and/or abuse.

Fenetylline (CAPTAGON) is included in a list of compounds to be considered by a World Health Organization (WHO) Expert Committee in April 1985 for possible international scheduling under the Convention on Psychotropic Substances, 1971. For over 23 years, this central stimulant has been used therapeutically in hyperkinetic children and other indications in place of amphetamines and other central stimulants with higher risk levels. In good correspondence with recent animal data fenetylline also shows significant qualitative and quantitative differences compared to amphetamine in man. It has few adverse side effects, a lower abuse potential and little actual abuse compared to amphetamine. Thus its benefit/risk assessment is substantially more favourable than that of other central stimulants. For proper therapeutic use of the substance, prescription status is or should be required by national authorities.

Aged↗
PubMed1985

[The pharmacologic effect of flupirtine, a structurally new analgesic].

The analgesic potency of ethyl-N-[2-amino-6-(4-fluorophenylmethylamino)pyridin-3-yl]carb ama te (flupirtine, D 9998) in mice and rats in Haffner's test, electro-pain test and Randall-Selitto test (inflammation induced pain) lies between the more potent dextromoramide and methadone and the more weakly active pethidine, dextropropoxyphene, codeine, phenacetin and paracetamol. In comparison to codeine flupirtine is up to 4 times more potent, up to 2 times more active than pethidine and 4 times more potent than dextropropoxyphene in the above-mentioned methods. With one exception of inflammation induced pain, where flupirtine shows an activity of about 1 1/2 times that of phenacetin and paracetamol, both analgesics are about 10 to nearly 30 times less active than flupirtine in other above-mentioned tests. In the hot plate test flupirtine is twice as active as codeine and approximately 10 times more active than phenacetin and paracetamol. The weakest analgesic activity of flupirtine is seen in acetic acid test where it is about half as active as codein and approximately as active as dextropropoxyphene. Nevertheless, flupirtine is up to 10 times more potent than phenacetin and paracetamol. The acetic acid test is claimed to be non-specific according to our own experience and to other authors. Flupirtine is enterally absorbed at a higher degree than the other tested centrally acting analgesics. In regard to the results of various analgesic investigations in mice and rats flupirtine can be classified as a medium to strong acting analgesic. The duration of action of flupirtine is comparable to that of codeine. Experiments with flupirtine suggest that there are some convincing criteria for a pronounced central acting component of its analgesic activity. These criteria are the strong efficacy in the hot-plate and Haffner's test, in which only centrally acting analgesics show distinct effects, and the finding that flupirtine increases the pain threshold for vocalisation in rats and mice excluding a pure reflex of the spinal cord. In current experiments concerning the mode of action flupirtine exhibits a distinct central analgesic component of action. In spite of its relatively high analgesic potency which corresponds to that of opiates flupirtine does not show any other signs of opiate properties and other potent analgesics. Thus, flupirtine does not develop tolerance in mice and rats after 19 or 17 days of daily administration.(ABSTRACT TRUNCATED AT 400 WORDS)

Aminopyridines↗
PubMed1985

[General pharmacologic studies on the analgesic flupirtine].

In the present study the general pharmacological properties of ethyl-N-[2-amino-6-(4-fluor-phenylmethylamino)pyridin-3-yl]carbama te (flupirtine, D 9998), a structural new analgesic, are described. In several tests with mice flupirtine shows a centrally depressant component of action. However, regarding undesirable side effects as ataxia, inhibition of motor activity etc. this action is, with respect to the analgesic effective doses less pronounced than those of comparable analgesics, for instance phenacetin. In relatively low doses flupirtine antagonizes tremor induced by oxotremorine in mice. This activity is probably not caused by a central anticholinergic action, because other anticholinergic effects have not been observed. It should be pointed out that flupirtine antagonizes the morphine-induced tail phenomenon in mice in relatively low doses. This action obviously differentiates flupirtine from opiates. Up to high doses flupirtine does not cause catalepsia in mice, consequently its centrally depressant activity does not resemble that of reserpine and also is not comparable with those of neuroleptic agents. The corneal and pinnal reflexes are not influenced by flupirtine and the righting reflex is slightly delayed in high doses. The anticonvulsive activity of flupirtine observed in the pentetrazol shock test (mouse) after high doses probably cannot be considered to occur within the analgesic dose range. Inhibition of amphetamine toxicity in mice observed in doses near the hypnotic doses may be caused by non-specific effects. In vitro tests with isolated trachea or ileum of guinea pigs show that flupirtine possesses no or very weak antagonism against histamine-induced spasms. In spasms caused by barium chloride flupirtine shows a weak musculotropic-spasmolytic activity. Investigations on the circulatory system of dogs do not indicate any incompatibilities with flupirtine. No evidence of antiarrhythmic activity was found in rats. Flupirtine has no local anesthetic activity in mice but some weak effects on the cornea of rabbits. Like several other analgesics flupirtine shows in rats a reversible antidiuretic action including sodium and chloride retention which is of relatively short duration and is not observed in long-term studies in rats and dogs. In contrast to many stronger antiinflammatory compounds, flupirtine does not possess ulcerogenic activity in rats up to high doses. A minimal inhibition of intestinal motility (mouse) is observed only in doses higher than the analgesic effective doses.

Aminopyridines↗
PubMed1978

[Pharmacological effect of tinofedrine on cerebral and peripheral hemodynamics in the dog (author's transl)].

l-(+)-alpha-(1-[(3,3-Di-3-thienylallyl)amino]-ethyl)-benzyl alcohol hydrochloride (Tinofedrine, D 8955, Novocebrin), a new drug, synthetized in our research laboratories, has been tested in dogs with regard to the improvement of cerebral and peripheral blood flow. Direct electromagnetic flow measurement at the vertebral artery as well as 133xenon wash-out method showed a strong and long-lasting increase of cerebral and femoral blood flow following intravenous as well as oral administration. No decrease of activity was observed after repeated intravenous application. Comparative studies with several standard drugs of the same field of indication proved a remarkable superiority of tinofedrine in our experimental conditions.

Animals↗
PubMed1978

[The influence of tinofedrine on cerebral energy metabolism in normotensive, hypotensive and hypoxemic rats after carotis ligation (author's transl)].

l-(+)-alpha-(1-[(3,3-Di-3-thienylallyl)amino]-ethyl)-benzyl alcohol hydrochloride (tinofedrine hydrochloride, D 8955, Novocebrin), a new cerebrally active substance, synthetized in our research laboratories, was investigated for its action on the disturbed cerebral metabolism in rats. By variation of the arterial blood pressure (normal, 100 and 70 mmHg), and O2-concentration for the artificial ventilation of 30 or 15 vol% and carotis ligation for 15, 30 and 60 min different degrees of cerebral disturbances could be induced. The glucose concentration and energy state of the brain were used as criteria of the degree of cerebral disturbance. After intravenous injection of tinofedrine such a disturbed cerebral state could be normalized partially or completely.

Animals↗
PubMed1977

[Toxicological investigation of reproterol (author's transl)].

Only slight toxicity of 7-(3-[2-(3,5-dihydroxyphenyl-2-hydroxy-ethylamino]-propyl)-theophylline (reproterol, Bronchospasmin) was shown in the examination of acute, subacute and chronic trials on various animal species with different modes of application. Slight side-effects noted with high toxically active dosages correspond with those of other well-known beta-sympathicomimetics. No influence on the pre-,peri- and postnatal development could be proven with doses tolerated by the parent animals.

Abnormalities, Drug-Induced↗