Search results for "Benperidol"
showing 10 items of 10 documents
Pharmacokinetics and bioavailability of benperidol in schizophrenic patients after intravenous and two different kinds of oral application
1994
Pharmacokinetics and bioavailability of benperidol were determined in 13 schizophrenic patients after acute administration of 6 mg benperidol as an intravenous (i.v.) bolus injection, orally as liquid, and orally as tablets using a partially randomized cross-over design. Drug plasma levels were determined by high performance liquid chromatography with electrochemical detection and subjected to model independent pharmacokinetic analyses. After i.v. dosing the geometric means (mean-g) were 3.2 min for the distribution half-life, 5.80 h for the elimination half-life (t1/2 beta), 4.21 l/kg for the distribution volume, 7.50 h for the mean residence time (MRT), and 0.50 l/(h*kg) for the clearance…
Plasma levels of benperidol, prolactin, and homovanillic acid after intravenous versus two different kinds of oral application of the neuroleptic in …
2009
Plasma levels of prolactin (PRL) and the butyrophenone neuroleptic benperidol (BPD) were closely followed 0 to 48 h after acute application of 6 mg BPD as intravenous injection, orally as liquid, and orally as tablets in 12 schizophrenic patients using a partially randomized cross over design. Drug concentrations showed application specific pharmacokinetic behavior with complete elimination within 48 h. All three applications led to a biphasic PRL response with pronounced initial plasma PRL peaks returning to baseline levels within 48 h. The results suggest that after acute neuroleptic challenge BPD plasma levels as low as 2-3 ng/ml can be sufficient for complete depletion of pituitary PRL …
[123I]IBZM SPECT in patients treated with typical and atypical neuroleptics: relationship to drug plasma levels and extrapyramidal side effects
1997
[123I]Iodobenzamide (IBZM) is an iodine-labeled dopamine receptor ligand and can be used to visualize brain D2 receptors in humans with single photon emission computerized tomography (SPECT). The ratio of striatal IBZM uptake to uptake in frontal cortex (ST/FC ratio) represents a semiquantitative measure of D2 receptor binding in the striatum. Our study sample included six patients treated with haloperidol (3.0-8.0 mg/day orally; one patient with an average of 0.9 mg/day intramuscularly), five patients with benperidol (9.0-15.0 mg/day orally) and nine patients treated with clozapine (200.0-600.0 mg/day orally). Typical neuroleptics (TNs) and atypical neuroleptics (ANs) were significantly di…
Prolactin plasma levels and D2-dopamine receptor occupancy measured with IBZM-SPECT
1996
By the application of 123([123I]IBZM), an iodine-labelled dopamine D2-receptor antagonist, brain D2 receptors in humans can be visualized with single photon emission computed tomography (SPECT). The ratio of IBZM binding to striatal regions versus binding to frontal cortex (ST/FC ratio) provided a semiquantitative measurement of D2 receptor binding in the striatum. This study investigated the relationship between receptor occupancy and plasma prolactin levels in 12 male patients treated with haloperidol, benperidol or clozapine. Prolactin levels were positively correlated with D2 receptor occupancy, reflecting at least in part a comparable dopamine receptor antagonism in different dopaminer…
Why Do Chemically Similar Pharmaceutical Molecules Crystallize in Different Structures: A Case of Droperidol and Benperidol
2016
A detailed study of molecular conformation and intermolecular interactions in the experimental crystal structures and general trends observed in the Cambridge Structural Database as well as theoretical calculations were performed to identify the reason for the formation of different crystal structures of two chemically very similar pharmaceutical molecules benperidol and droperidol. The most important difference between both molecules was the weak intermolecular interactions formed by the central ring which therefore was responsible for the formation of different crystal structures. Cross-seeding experiments were performed to check the possibility for the formation of mutually isostructural…
Determination of benperidol and its reduced metabolite in human plasma by high-performance liquid chromatography and electrochemical detection.
1991
An isocratic high-performance liquid chromatographic method with electrochemical detection for the quantification of benperidol and its suggested reduced metabolite TVX Q 5402 in human plasma is described. The method included a two-step solid-phase extraction on reversed-phase and cation-exchange material, followed by separation on a cyanopropyl silica gel column (5 microns; 250 mm x 4.6 mm I.D.). The eluent was 0.15 M acetate buffer (pH 4.7) containing 25% acetonitrile (w/w). Spiperone served as internal standard. The inclusion of the cation-exchange step provided sample purity higher than those achieved with other methods. After extraction of 1 ml of plasma, concentrations as low as 0.5 n…
Izvēlētu farmaceitiski aktīvo vielu cieto šķīdumu veidošanās iespējas un analīze
2018
Izvēlētu farmaceitiski aktīvo vielu cieto šķīdumu veidošanās iespējas un analīze. Saršūns K., darba vadītājs Dr. Chem. Bērziņš A. Bakalaura darbs, 76 lappuses, 43 attēli, 28 tabulas, 6 pielikumi, 55 literatūras avoti. Latviešu valodā. Bakalaura darba ietvaros ir apkopota informācija par farmaceitiski aktīvajām vielām - benperidolu un droperidolu, kā arī par barbitūrskābi un tiobarbitūrskābi, vispārīgs preparātu raksturojums, polimorfisma parādība, kristalizācijas process, cieto šķīdumu raksturojums, papildus tam arī par rentgendifraktometriju, diferenciālo skenējošo kalorimetriju, termogravimetriju un 1H-KMR spektroskopiju, kā par fizikālajām cietfāžu pētīšanas metodēm, kas tika izmantotas …
ANTI-ARRHYTHMIC EFFECT OF DEHYDROBENZPERIDOL IN DOGS
1971
SUMMARY The anti-arrhythmic activity of dehydrobenzperidol (DBP) was studied during halothane anaesthesia in dogs. Arrhythmias were provoked by single intravenous injections of catecholamines. Two groups of dogs were studied. One received norepinephrine and the odier epinephrine. The dose just sufficient to initiate arrirythmias was defined as the “threshold”. Electrocardiogram, blood pressure and heart rate were monitored. The principal findings were:— 1 The dog heart was “sensitized” to epinephrine and norepinephrine by halothane. 2 DBP did have an anti-arrhydimic action. A dose of 0.150 mg/kg roughly doubled the “threshold”. 3 DBP had significant alpha-adrenergic blocking properties. …
Templātu un neorganisku cietvielu piedevu ietekme uz izvēlētu farmaceitiski aktīvo vielu kristalizācijas produktiem
2016
Templātu un neorganisku cietvielu piedevu ietekme uz izvēlētu farmaceitiski aktīvo vielu kristalizācijas produktiem. Vainovska P. Darba vadītājs Dr. Ķīm. Bērziņš A. Bakalaura darbs, 53 lapaspuses, 44 attēli, 6 tabulas, 20 literatūras avoti, 3 pielikumi. Latviešu valodā. Darba literatūras daļā ir dota informācija par droperidolu, benperidolu, henodeoksiholskābi, polimorfismu, solvātiem, sāļiem, kokristāliem, kristalizācijas procesa ietekmējošajiem faktoriem, pulvera rentgendifraktometriju, termisko analīzi, diferenciālo skenējošo kalorimetriju un termogravimetriju. Darbā veikta droperidola, benperidola un henodeoksiholskābes kristalizācija no dažādiem šķīdinātājiem ar cietvielu neorganisko v…
Structural Characterization and Rationalization of Formation, Stability, and Transformations of Benperidol Solvates
2015
Experimental and theoretical characterization and studies of phase transitions and stability of the solvates obtained in solvate screening of the pharmaceutical compound benperidol were performed to rationalize and understand the solvate formation, stability, and phase transitions occurring during their desolvation. The solvate screening revealed that benperidol can form 11 solvates, including two sets of isostructural solvates. The analysis of the solvate crystal structures and molecular properties indicated that benperidol solvate formation is mainly driven by the complications during packing of benperidol molecules in an energetically efficient way in the absence of solvent molecules, as…