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  • 1
    Electronic Resource
    Electronic Resource
    Pharmacology of Antidiarrheal Drugs (1983)
    Palo Alto, Calif. : Annual Reviews
    Annual Review of Pharmacology 23 (1983), S. 279-301 
    Details
    ISSN: 0362-1642
    Source: Annual Reviews Electronic Back Volume Collection 1932-2001ff
    Topics: Medicine , Chemistry and Pharmacology
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1146/annurev.pa.23.040183.001431
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  • 2
    Electronic Resource
    Electronic Resource
    Antiemetic effect of haloperidol in the dog as related to plasma level and dose (1981)
    Springer
    Psychopharmacology 75 (1981), S. 240-244 
    Details
    ISSN: 1432-2072
    Keywords: Haloperidol ; Plasma concentration ; Antiemetic effect ; Dog
    Source: Springer Online Journal Archives 1860-2000
    Topics: Medicine
    Notes: Abstract A positive and highly significant correlation was found between SC dose, plasma concentration, and antiemetic effect of haloperidol in the dog. To protect dogs from apomorphine-induced emesis, a concentration of 1 ng haloperidol/ml plasma was always sufficient, whereas protection from emesis was never obtained with plasma levels lower than 0.53 ng/ml. The elimination rate of haloperidol from plasma varied from 1.53 to 2.60 among different animals. Thus, the interindividual variability to haloperidol was surprisingly low. Antiemetic effect and plasma elimination of haloperidol were not related to body weight.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1007/BF00432431
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  • 3
    Electronic Resource
    Electronic Resource
    Bromperidol, a new butyrophenone neuroleptic: A review (1982)
    Springer
    Psychopharmacology 78 (1982), S. 1-7 
    Details
    ISSN: 1432-2072
    Keywords: Bromperidol ; Haloperidol ; Chlorpromazine ; Preclinical review ; Animal pharmacology ; Animal pharmacokinetics ; Animal biotransformation ; Animal drug safety
    Source: Springer Online Journal Archives 1860-2000
    Topics: Medicine
    Notes: Abstract This review compares and contrasts the preclinical pharmacology of bromperidol with another butyrophenone neuroleptic, haloperidol, and the phenothiazine neuroleptic chlorpromazine. Its pharmacokinetics, biotransformation, and safety in several laboratory animal species are also summarized. These preclinical data support its use as an antipsychotic agent and show that it is well absorbed following oral administration with an apparent elimination half-life of approximately 24 h, supporting a once-daily dose regimen. Animal toxicity (including acute- and multiple-dose toxicology and reproductive and mutagenicity studies) show that bromperidol is well tolerated.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1007/BF00470578
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  • 4
    Electronic Resource
    Electronic Resource
    Antiemetic specificity of dopamine antagonists (1982)
    Springer
    Psychopharmacology 78 (1982), S. 210-213 
    Details
    ISSN: 1432-2072
    Keywords: Neuroleptics ; Antiemetics ; Antiemetic specificity ; Dogs ; Rats
    Source: Springer Online Journal Archives 1860-2000
    Topics: Medicine
    Notes: Abstract Twelve antagonists of apomorphine-induced emesis in dogs were studied in different tests to evaluate their antiemetic specificity. Ten of these antagonists were neuroleptics: benzquinamide, clebopride, bromopride, prochlorperazine, haloperidol, chlorpromazine, thiethylperazine, metoclopramide, droperidol, and pimozide blocked conditioned responding in dogs and apomorphine-induced stereotyped behavior in rats. The use of these compounds as anti-emetics entails a risk of neurological side effects. Metopimazine and domperidone were devoid of neuroleptic activity. Metopimazine, however, showed potent α-adrenergic blocking activity, showed histamine H1 antagonism, and induced palpebral ptosis. Therapeutic doses of metopimazine are, therefore, likely to produce sedation and side-effects related to autonomic blockade. Domperidone showed potent antiemetic activity and, up to high doses, no other central or peripheral effects. Therefore, domperidone is the only specific antiemetic known.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1007/BF00428152
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  • 5
    Electronic Resource
    Electronic Resource
    Behavioral and 5-HT antagonist effects of ritanserin: A pure and selective antagonist of LSD discrimination in rat (1985)
    Springer
    Psychopharmacology 86 (1985), S. 45-54 
    Details
    ISSN: 1432-2072
    Keywords: 5-HT antagonist ; LSD antagonist ; Drug discrimination ; Anxiety ; 5-HTP ; Head twitch ; Conflict behavior ; Hypothermia ; Ritanserin ; Pirenperone ; Chlordiazepoxide ; Diazepam ; Rat
    Source: Springer Online Journal Archives 1860-2000
    Topics: Medicine
    Notes: Abstract The newly synthesized compound and putative 5-HT2 antagonist ritanserin, but not the structurally related compound R 56413, resembles pirenperone in that it acts as a pure antagonist in an LSD-saline drug discrimination assay in the rat. Ritanserin exceeded pirenperone in terms of behavioral specificity; the lowest effective dose of ritanserin in antagonizing LSD was one order of magnitude higher than that of pirenperone, but the compound depressed rate of operant responding only at doses that were about 1000-fold higher than those at which pirenperone was effective. Ritanserin exerted effects in an open field test which were reminiscent of anxiolytic drug activity in the rat; its effects were greater than those of pirenperone, R 56413 and the benzodiazepines chlordiazepoxide and diazepam. The results of experiments on antagonism of 5-HT-induced hypothermia and of the 5-HTP-induced headtwitch response fail to support the possibility that the putative anxiolytic effects of ritanserin in the rat can be ascribed simply to a pharmacologically defined action at 5-HT receptors.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1007/BF00431683
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  • 6
    Electronic Resource
    Electronic Resource
    The pharmacological profile of a specific, safe, effective and non-sedative anti-allergic, astemizole (1986)
    Springer
    Inflammation research 18 (1986), S. 141-144 
    Details
    ISSN: 1420-908X
    Source: Springer Online Journal Archives 1860-2000
    Topics: Medicine
    Notes: Abstract In the compound 48/80 lethality test in rats, which is based on the specific activation of mast cells, astemizole was selected as a potent, long-acting and orally very effective inhibitor of anaphylactoid shock. In comparison to other histamine-H1 antagonists astemizole was also a very effective inhibitor of allergic reactions in rats and dogs and remarkably free of non-specific interactions with other biological amines and normal body functions. In numerous tests no evidence of central activity was found and toxicity studies have shown astemizole to be a very safe drug despite of its long duration of action. A daily dose of 10 mg of astemizole was found clinically free of side-effects and more effective than conventional antihistamine treatment.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1007/BF01988005
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  • 7
    Electronic Resource
    Electronic Resource
    Behavioural activity of rats measured by a new method based on the piezo-electric principle (1987)
    Springer
    Psychopharmacology 93 (1987), S. 382-388 
    Details
    ISSN: 1432-2072
    Keywords: Motor activity ; Locomotion ; Behaviour ; Methods ; Haloperidol ; Apomorphine ; Amphetamine ; Rats
    Source: Springer Online Journal Archives 1860-2000
    Topics: Medicine
    Notes: Abstract Spontaneous and drug-induced (haloperidol, apomorphine, and amphetamine) motor activity of rats was measured simultaneously via two distinct and independent methods: the classical optical scanning technique and a new procedure based on the piezo-electric principle. The latter procedure measured animal-induced mechanical vibrations of a flexible cage floor which were transduced into electric signals via piezo-electricity. The piezo method appeared to be relatively more sensitive in recording the small, stereotyped motor movements induced by apomorpine (0.63–≧10 mg/kg) and high doses of amphetamine (2.5–≧20 mg/kg). The optical scanning technique, on the other hand, was more sensitive in recording horizontal displacements across the cage such as induced by low doses of amphetamine (0.31–2.5 mg/kg). Both methods showed comparable sensitivity in recording the depression of behaviour induced by haloperidol (0.04–≧1.25 mg/kg) or low doses of apomorphine (0.04–0.16 mg/kg). The piezo method may complement the optical scanning procedure, and thereby enhance the information on the extent that test compounds modify animal behaviour.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1007/BF00187261
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  • 8
    Electronic Resource
    Electronic Resource
    Differential effects of the new antipsychotic risperidone on large and small motor movements in rats: a comparison with haloperidol (1988)
    Springer
    Psychopharmacology 95 (1988), S. 493-496 
    Details
    ISSN: 1432-2072
    Keywords: Risperidone ; Haloperidol ; Antipsychotics ; Behaviour ; Activity meter ; Rats
    Source: Springer Online Journal Archives 1860-2000
    Topics: Medicine
    Notes: Abstract Risperidone, a new antipsychotic agent, was studied for its effects on spontaneous motor activity in rats in comparison with haloperidol. Motor activity was recorded via the optical scanning technique (horizontal and vertical activity) and via a recently developed technique based on the piezo-electric principle which, in contrast to optical scanning, is very sensitive to small, stationary movements (piezo activity). Risperidone and haloperidol at low doses depressed both vertical activity (ED50s: 0.062 and 0.038 mg/kg, respectively) and horizontal activity (0.18 and 0.060 mg/kg, respectively). With increase of dose, motor activity decline was significantly faster with haloperidol than with risperidone. Moreover, haloperidol also rapidly depressed piezo activity (ED50: 0.085 mg/kg) whereas risperidone depressed this component of motor behaviour at much higher doses only (ED50: 2.80 mg/kg). Visual inspection did not reveal abnormal behavioural movements following the test compounds. Risperidone, therefore, preserves normal small movements over a much larger dose interval than haloperidol; this effect may be related to its relatively low cataleptogenic activity and potentially also to a reduced EPS liability. The present results further confirm that the piezo technique may complement the optical scanning method, and thereby enhance the information on the extent that test compounds modify behaviour.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1007/BF00172961
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  • 9
    Electronic Resource
    Electronic Resource
    The pharmacological and biochemical basis of neuroleptic treatment in schizophrenia (1982)
    Springer
    Pharmacy world & science 4 (1982), S. 71-78 
    Details
    ISSN: 1573-739X
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology
    Notes: Abstract In a short review some historical data are presented that underline the importance of the dopamine hypothesis in schizophrenia and the mechanism of action of neuroleptics. The assumption that neuroleptics are postsynaptic dopamine receptor blockers in certain areas of the brain is based on pharmacological, biochemical and clinical findings. New pharmacological data are presented which show that apomorphine, amphetamine, cocaine and caffeine in different ways and at different levels may exert agonist activity on the dopaminergic system in the brain. The agonist activity of these compounds, which is expressed by an increase in motility of the injected animals, can be antagonized by neuroleptics such as haloperidol. However, the higher the dose levels of the agonists, thus the higher the dopaminergic overstimulation, the higher the dose of haloperidol needed to normalize the motility. These data tend to confirm the dopamine hypothesis and may give some support for the use of individually adapted doses in the treatment of schizophrenia and mania,i.e. doses that match the dopaminergic overstimulation. Thus patients with high dopaminergic overstimulation need higher doses of neuroleptics than patients with low dopaminergic overstimulation. This could explain why some so-called ‘therapy-resistant’ patients, not responding to conventional doses, respond to high doses of neuroleptics. Adapted individualized dose levels, however, also mean low doses of neuroleptics in patients with a low dopaminergic overstimulation. It should be mentioned in this respect that chronic overblockade of the dopaminergic system (overdoses of neuroleptics) may be masked by the concomitant administration of antiparkinson agents and that chronic overblockade may induce dopaminergic hypersensitivity and lead to tardive dyskinesia. Also high doses of neuroleptics therefore should never be given to non-responders over long periods of time. Although dopamine seems to be a very important neurotransmitter involved in the mechanism of action of neuroleptics, it should be remembered that other neurotransmitters may also be of importance, since the activity of neuroleptics is not necessarily limited to dopamine receptor blockade and schizophrenia is such a complicated disease that its manifestations can hardly be explained by merely the overstimulation of postsynaptic dopamine receptors.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1007/BF01962247
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  • 10
    Electronic Resource
    Electronic Resource
    Het farmacologisch profiel van de neuroleptica (1981)
    Springer
    Pharmacy world & science 3 (1981), S. 1437-1442 
    Details
    ISSN: 1573-739X
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology
    Description / Table of Contents: Samenvatting Een vergelijkend dierfarmacologisch overzicht van de neuroleptica wordt gegeven. Verschillende onderzoekingen bij de rat en de hond worden besproken en onderling geëvalueerd. Het geheel geeft een indicatie van het te verwachten klinisch profiel van een neurolepticum, zowel wat betreft de therapeutische mogelijkheden als de bijkomende gewenste en ongewenste neveneffecten en bijwerkingen, dosering en werkingsduur.
    Notes: Abstract A survey comparing the animal pharmacology of neuroleptics is given. The tests discussed and mutually assessed are for the rat: antagonism of the effects induced by apomorphine, amphetamine, tryptamine, norepinephrine, substance 48/80 and eserine; inhibition of conditioned reactions and intracranial self-stimulation; induction of catalepsy and palpebral ptosis, delaying of oestrus and the acute toxicity. In the dog the tests performed are the antagonism of the emetic effect of apomorphine and the inhibition of conditioned reactions. Taken as a whole the results are indicative of the clinical profile to be expected for a particular neuroleptic. This profile relates to the therapeutic possibilities, as well as wanted and unwanted secondary reactions and side effects, dosage and duration of action.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1007/BF02193410
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