[Brain metabolism studies under the treatment with pyrithioxin].
Explore the source record for details and available documents.
Adult↗
SEARCH · Search PubMed
Results for “Pyrithioxin”
Search indexed PubMed citations on genomics, clinical trials, systematic reviews and public health. Explore titles, authors and supplied subject terms, then open the PubMed record.
Quote a phrase for an exact phrase match. Source license links do not imply unrestricted reuse.
[Antineoplastic activity of drugs affecting the central nervous system against chemically induced tumors in the rat (author's transl)].
Piracetam and Pyrithioxin, drugs affecting the central nervous system, prolonged survival times in rats with the 3-MC sarcoma. Tumor remissions were observed in several male animals. We were able to achieve a high survival rate without metastasis after surgical removal of the tumors. The remission rate could be increased 6-fold when Piracetam was combined with Cyclophosphamid. In this group male and female animals reacted in the same manner. When used prophylactically, Piracetam proved to be more effective than Pyrithioxin. The effectiveness of Piracetam depended on the onset of treatment. Tumor remission was significant 28 weeks following 3-MC injection when 3-MC and Piracetam were given simultaneously. A remarkable increase of the tumor rate ensued when medication was discontinued. The tumor rate decreased to less than 50% 36 weeks following 3-MC injection if treatment was started 8 weeks following 3-MC application. The latter applied only to Piracetam and not to Pyrithioxin. In the EEG of rats the diminished amplitude induced by 3-MC could be fully compensated by 100 mg/kg Piracetam. All animals treated in this manner for 7 months remained tumor-free.
Animals↗
[Effect of suloctidil in the protection of the cerebral function].
It has been demonstrated that suloctidil [erythro-1-(4-isopropylthiophenyl)-2-n-octylaminopropanol] has a protective effect against cerebral hypoxia to elongate the survival time of mice subjected to normobaric hypoxia (96% N2 + 4% O2 gas mixture). In this study, further experiments were done to elucidate the mechanism of protection against cerebral hypoxia with a variety of experimental models. Pretreatment (30 min) with suloctidil (12.5-50 mg/kg, i.p.) increased the number of gasping in the decapitated head of mouse as a complete ischemic model. Pyrithioxine (25, 50 mg/kg, i.p.) or cinnarizine (50, 100 mg/kg, i.p.) did not increase the gasping number. In the histotoxic anoxia with KCN (4 mg/kg, i.v.) in mice, suloctidil showed 30.8% and 46.2% survival rates at the doses of 25 and 50 mg/kg, i.p., respectively. Concerning this result, it has been revealed that suloctidil did not have any methemoglobin formation liability in rats (unpublished). Pyrithioxine did not show such protection following the injection of 12.5-50 mg/kg, i.p.. Suloctidil (3.0-50 mg/kg, i.p.) and pyrithioxine (3.0, 10 mg/kg, i.p.) significantly prolonged the survival time of mice subjected to hypobaric hypoxia (210 mmHg). In this cerebral hypoxia model, suloctidil kept glucose at a significantly higher level and lactate at a lower level in the brain of mice that were administered this drug than the control group. ATP was kept at higher level after suloctidil than the control under hypobaric hypoxia. Taking these evidences together, it can be concluded that suloctidil exerts its cerebral anti-hypoxic effect through cerebral glucose metabolism coupled with oxidative phosphorylation to yield the high energy substance ATP in a variety of models tested in this study. The fact obtained in this study, together with increase in cerebral blood flow by suloctidil, may also elucidate the protective effect of suloctidil against cerebral hypoxia.
Animals↗
Carcinogenesis and the central nervous system.
Wistar rats were injected with the carcinogen 3-MC. The effect of psychoactive drugs on tumor-bearing rats was examined with respect to tumor growth, survival time, and remissions. CNS drugs were given both prophylactically and therapeutically. Psychopharmaceuticals like piracetam and pyrithioxin as well as catecholamine-agonists like imipramine had a definite antineoplastic effect. This effect was increased when combined with other CNS drugs and, in particular, the combination of piracetam with chemotherapeutic agents resulted in a high rate of remission and reduced the toxicity of chemotherapy. Surgical removal of tumors and subsequent treatment with CNS drugs led to a high rate of cure without metastasis. After tumor appearance, we found cerebral neuropathological changes as described in the paraneoplastic syndrome. The EEGs of 3-MC-injected rats showed early pathognomic changes in frequency and amplitude. Similar changes were found in animals with transplantation tumors (Walker carcinoma and Jensen sarcoma). The EEG pattern was normalized after surgical removal of Jensen sarcoma and treatment with piracetam and pyrithioxin. These EEG changes might have occurred as a result of transmitter metabolism; ie, carcinogenesis of both induced tumors and transplanted tumors was accompanied by an increase of GABA content in hypothalamus and hippocampus and a reduced concentration of monoamines or their metabolites in hypothalamus and caudate nucleus. Long-term treatment with piracetam or imipramine again arrested all these changes. More recently, we achieved good results with the combination of CNS drugs and cAMP agonists. We therefore conclude that carcinogenesis interferes with the metabolism or availability of cyclic nucleotides and transmitters that regulate their level. CNS drugs may effect a new balance resulting in tumor suppression.
Animals↗
Neurochemical studies on the mechanism of action of pyritinol.
In investigations carried out in young and old rats with pyritinol (pyrithioxin, Encephabol), a substance that is frequently applied in cognitive function disturbances, besides effects on general cerebral functions, possible interactions with cholinergic transmission were determined. The following results were obtained: 1. The adenosine triphosphate (ATP) content of the blood was determined as a possible biochemical parameter of erythrocyte flexibility. After acute oral administration of 30, 100 and 300 mg/kg pyritinol, the ATP content of whole blood increased by 8%, 17% and 20% respectively compared with placebo. 2. According to the literature, brain glucose utilisation is considerably reduced at higher age. This was confirmed in old rats in the investigation presented here. Pyritinol (200 mg/kg p.o.) induced a significant increase in glucose utilisation in striatum, cortex, hypothalamus and cerebellum in 24- to 36-month-old rats. 3. The high-affinity choline uptake in striatal synaptosomes of old rats was significantly lower than that of young ones. Pyritinol (600 mg/kg p.o.) increased choline uptake in young rats as well as in old ones. 4. cGMP can serve as a postsynaptic marker for the activity of the cholinergic system. Pyritinol (200, 600, 1000 mg/kg p.o., 16-23 days) increased the cGMP level in the cortex by 25%, 42% and 71% respectively. Our results are in accordance with the recently described (Martin, 1987) elevation of cortical acetylcholine levels and facilitation of acetylcholine release under pyritinol and extend the functional relevance of these findings to the postsynaptic, cholinergically innervated cortical neurons.(ABSTRACT TRUNCATED AT 250 WORDS)
5-Hydroxytryptophan↗
Effects of various cerebral metabolic activators on glucose metabolism of brain.
The effects of various metabolic activators on the glucose metabolism of the perfused cat brain have been investigated. (1) When the perfusion is done with the blood containing cytidine monophosphate, the glucose metabolism of the brain is enhanced, as compared to the perfusion with the blood without cytidine monophosphate. There is no marked change in the cerebral metabolic rate and in the contents of intermediate metabolite of glucose in the brain. (2) Citicoline enhances the incorporation of blood glucose into the brain and its metabolism in the brain. It increases slightly the cerebral blood flow rate and decreases the accumulation of lactate in the brain. (3) Either Pyrithioxin or Meclophenoxate has no effect on the glucose metabolism of the brain nor on the cerebral metabolic rate.
Animals↗
[Animal experimental studies on the prevention of cleft palate and other malformations in the region of the head].
In fetuses of eight-week old female Swiss mice, teratogenic effects were produced by cyclophosphamid on different days of pregnancy. Frequently and combinations of malformation of a positive control group (30 mg/kg b.w. on the 11.5th day of pregnancy) were compared with "prophylaxis" groups. Pyrithioxin (Encephabol) significantly reduces the number of some malformations. The goal, i.e. to obtain normal fetuses without malformations, was not achieved, however. The best effect was obtained with 1/160 LD50 of Encephabol administered in four doses prior to Endoxan.
Abnormalities, Multiple↗
[Sulfhydryl maintenance treatment in rheumatoid polyarthritis. A series of 120 cases followed for 10 years and a study of possibilities of changing the drug].
The authors present a series of 120 cases of sero-positive rheumatoid arthritis followed for ten years and treated with D-penicillamine, gold salts and pyrithioxine used either alone or sequentially after stopping one of these treatments because of failure, intolerance or escape. This series can be broken down as follows: 13% of patients are under treatment after ten years, 27% had a favourable result with one of the three treatments for five to ten years, 59% had a poor result (less than 5 years) or no effect. However, it appeared that a failure or an escape from one of these products did not signify a failure with another product and side effects did not necessarily recur with a change of treatment.
Adult↗
Role of gastric emptying on ethanol poisoning in rats.
Intraperitoneal glucose was demonstrated to significantly inhibit the absorption of ethanol ( 2 g/kg) administered orally to rats. The effect was due to slowed emptying of the stomach, verified by analysis of the stomach contents and of blood enthanol levels. The observation agrees with previous findings, according to which the rate of stomach emptying is inversely related to the blood glucose level. However, when glucose was given intravenously 15 minutes after oral administration of a lethal dose of ethanol (12.5 g/kg) no significant inhibition of ethanol absorption could be observed. Intravenous propantheline, pyrithioxine and methylene blue were also unable to prolong the survival time or to influence the lethal blood ethanol concentration (about 170 mmol/l) of the enthanol-poisoned rats.
Administration, Oral↗
[Effect of pyriditol on drug metabolism].
Pyriditol (encephabol, enerobol, pyrithioxin, etc.), a disulfide derivative of pyridoxin, exerts an inhibitory effect on hexobarbital and amphetamine metabolism i vivo and on ethylmorphine N-demethylation in vitro. In the latter case the inhibition proceeds according to the mixed type of action. Pyriditol potentiates the hypnotic action of hexobarbital and barbital as well as the effects of amphetamine stereotypy. The mechanism of the potentiating of hexobarbital and amphetamine effects is of combined character and is conditioned both by the physiological properties of pyriditol and its inhibitory effect on hexobarbital and amphetamine metabolism.
Amphetamine↗
[Clinical experience with Encephabol (author's transl)].
The author reports on a clinical study with the neuro-dynamic agent Encephabol (pyritinol, pyrithioxine) in a total of 317 patients with organic psychosyndrome of various genesis. The therapeutic effect obtained is related by the author to the mode of administration used (oral, parenteral and combined), to the dosage, and duration of treatment, and is discussed.
Administration, Oral↗
The nephrotoxic potential of drugs and chemicals. Pharmacological basis and clinical relevance.
Scores of drugs in common clinical use are capable of inflicting various degrees of damage to the kidney. Similarly, a large number of widely employed chemicals may adversely affect renal tissue as part of their toxic potential. A xenobiotic may damage the kidney by more than one mechanism. For example, NSAIDs may cause decreased renal perfusion, interstitial nephritis, primary glomerulopathy and/or altered potassium homeostasis. A large number of drugs and chemicals inflict their damage on the renal tubular cell secondary to intracellular accumulation to concentrations substantially higher than in the plasma or in other tissues. These include aminoglycosides, mercury and carbon tetrachloride and cephaloridine. Drug-induced interstitial nephritis is characterised by inflammatory lesions of the renal interstitium developed after at least 7 to 10 days of therapy. The immunological nature of this reaction is suggested by the associated fever, maculopapular rash and arthralgia observed in some of the patients. Although eosinophilia, eosinophiluria, and raised blood IgE levels are characteristic, immunoglobulins are not deposited in renal tissue, and the basic mechanism has not been elucidated. Renal biopsy demonstrates oedema and interstitial inflammatory reaction, mainly with lymphocytes, monocytes, eosinophils and plasma cells. Less frequent, vasculitis of small vessels or granulomatous reaction may develop, leading to necrotising glomerulonephritis. The drugs most commonly causing acute interstitial nephritis are methicillin, ampicillin, cephalosporins, rifampicin (rifampin), sulphonamides, phenindione and allopurinol. Other penicillins, NSAIDs, phenytoin, thiazides and frusemide (furosemide) are less frequently associated with this syndrome. Drugs and chemicals may affect renal function by pharmacologically decreasing glomerular filtration rate and/or renal blood flow. These include the NSAIDs, radiological contrast media and cyclosporin. Normal renal function depends upon an intact glomerular apparatus. Many drugs and chemicals are capable of damaging the glomerulus, causing its increased permeability to large molecules such as proteins. Several drugs including d-penicillamine, thiopronine, captopril, pyrithioxine and methimazole, are believed to exert their damage through their sulfhydryl group which bind with high affinity to glomerular structures. A variety of xenobiotics or their metabolites may be deposited in the renal tubule causing obstruction of urine flow and a secondary damage to tubular epithelium. Sulphonamides, methotrexate and ethylene glycol are good examples.(ABSTRACT TRUNCATED AT 400 WORDS)
Aminoglycosides↗
Pentoxifylline. A review of its pharmacodynamic and pharmacokinetic properties, and its therapeutic efficacy.
Pentoxifylline (oxpentifylline) is an orally active haemorheological agent for the treatment of peripheral vascular disease, cerebrovascular disease and a number of other conditions involving a defective regional microcirculation. Pentoxifylline acts primarily by increasing red blood cell deformability, by reducing blood viscosity and by decreasing the potential for platelet aggregation and thrombus formation. Extensive open and placebo-controlled studies have shown that pentoxifylline 600 to 1200 mg/day for at least 6 weeks is associated with subjective and objective improvements in 60 to 100% of patients with peripheral vascular disease. The most commonly assessed clinical parameter, walking distance, is usually improved by about 100%, although much greater improvements have also been documented. Other parameters which have been clearly improved include lower limb rest pain, paraesthesia, muscle blood flow, cramps and leg ulcers. Pentoxifylline has produced consistently better results than placebo, and in those studies using comparative drugs, better results than nylidrin, adenosine and naftidrofuryl. In patients with cerebrovascular disorders, open studies with pentoxifylline, usually at a dosage of 600 to 1200 mg/day (300 to 600 mg/day in Japan), have shown marked overall clinical improvements in about 85% of patients. Symptomatic improvements in rehabilitation psychometric tests, neuromotor and speech deficits and other subjective symptoms have accompanied increased cerebral blood flow, particularly to ischaemic areas. Pentoxifylline would appear to be useful in most types of cerebrovascular disease including transient ischaemic attacks, sequelae of cerebral thrombosis and haemorrhage, and chronic ischaemic disorders. In patients with chronic cerebrovascular disease pentoxifylline 600 to 1200 mg/day conferred significant clinical benefit compared with placebo and in isolated studies proved to be superior to drugs such as co-dergocrine mesylate, adenosine and pyrithioxine. Preliminary studies indicate that pentoxifylline may also prove useful in vaso-occlusive crises of sickle cell disease, some hearing disorders, disorders of eye circulation, high altitude sickness and asthenozoospermia. Pentoxifylline is usually well tolerated when administered as the conventional controlled release formulation, gastrointestinal symptoms (about 3%) being the most common complaint, although these and other adverse effects have not occurred to a significantly greater extent than with placebo. Thus, pentoxifylline offers a well-tolerated and effective alternative to the treatment options available for patients with peripheral vascular disease.(ABSTRACT TRUNCATED AT 400 WORDS)
Cardiovascular Diseases↗
[Clinical observation on children with language disorder of cerebral palsy treated by acupuncture].
OBJECTIVE: To observe therapeutic effect of acupuncture on language disorder of cerebral palsy. METHODS: Ninety-eight cases of language disorder of cerebral palsy were randomly divided into an acupuncture group (n = 76) and a control group (n = 22). The acupuncture group were treated by needling main acupoints Sishenzhen, Niesanzhen, Naosanzhen, Zhisanzhen, Shesanzhen, Fengchi (GB 20) and Yamen (GV 15), and the control group by oral administration of pyrithioxine 0.1-0.2 g and gamma-aminobutyric acid, thrice each day, and intramuscular injection of 2 mL nerve growth factor, once daily. They all were treated for 4 months. RESULTS: The total effective rate was 86.8% in the acupuncture group and 59.1% in the control group with very significant difference between the two groups (P < 0.001), and early treatment in the acupuncture group had a better therapeutic effect. CONCLUSION: Acupuncture has obvious improvement action on language disorder in the children of cerebral palsy.
Acupuncture Points↗
Vasodilators in senile dementias: a review of the literature.
The rationale for the use of vasodilators in the aged has changed from the attempt to increase cerebral blood flow to the attempt to improve cerebral metabolism. Review of 102 studies of eight vasodilators showed that significantly more controlled studies claimed practical clinical benefit from drugs supposed to improve neuronal intermediary metabolism with secondary vasodilatation than from drugs supposed to have only vasodilator action (P less than .005). Studies of both classes of drugs often suffered from poor study design, inappropriate and inconsistent application of outcome measurements, as well as negative bias due to selection of severely demented subjects. Future studies should be placebo-controlled investigations of drugs with primarily metabolic action, address questions of dose and time response, consistently use appropriate outcome measurement, and concentrate on the elderly in whom cognitive improvement is possible.
Aged↗
Pathophysiological aspects concerning the treatment of the apallic syndrome.
Explore the source record for details and available documents.
Adult↗
[Stellate ganglion block under EEG control in the treatment of complicated cervical migraine (author's transl)].
Complicated migraine is regarded as a cerebrovascular syndrome of functional character. In the case of a young man with cervical migraine associated with paroxysmal neurological disorders and persisting EEG abnormalities, stellate ganglion blocks were performed under EEG control. A transient amelioration of the pathological EEG pattern was observed after each stellate ganglion block and after several treatments the EEG was normal and the migraine attacks disappeared. The pathophysiology of the effect of stellate ganglion block on cerebral blood flow is discussed.
Adult↗
Induction of auto-immune syndromes by penicillamine therapy in rheumatoid arthritis and other diseases.
Explore the source record for details and available documents.
Arthritis, Rheumatoid↗