Trospium chloride, a quaternary amine with anticholinergic properties, is used for the treatment of overactive bladder with symptoms of urge urinary incontinence, urgency and urinary frequency. The pharmacokinetics of trospium chloride have been investigated in healthy volunteers, in patients with renal and hepatic impairment, and in those with symptoms of overactive bladder, after oral, intravenous and intravesical administration. After oral administration, absorption of the hydrophilic trospium chloride is slow and incomplete. Peak plasma concentrations (Cmax) of approximately 4 ng/mL are reached 4-5 hours after administration of a 20 mg immediate-release preparation. The mean bioavailability is approximately 10% and decreases by concomitant food intake (to a mean of 26% of the fasting area under the plasma concentration-time curve [AUC]). Trospium chloride displays dose proportional increases in AUC and Cmax after a single dose within the clinically relevant dose range (20-60 mg). The mean volume of distribution is approximately 350-800 L. The drug is minimally (mean approximately 10%) metabolised to spiroalcohol by hydrolysis, is 50% plasma protein bound and does not cross the blood-brain barrier. Urinary excretion of the parent compound plays a major role in the disposition of the drug, with a mean renal clearance of 29 L/h (accounting for approximately 70% of total clearance) and a mean elimination half-life ranging from 10 to 20 hours. Elimination of the drug is slowed in patients with renal insufficiency, and population pharmacokinetic modelling has demonstrated that drug clearance is correlated with serum creatinine concentration. Thus, dose reduction is needed in patients with severe renal impairment (i.e. creatinine clearance < 30 mL/min). To date, no clinically relevant pharmacokinetic drug-drug interactions have been identified; the drug does not bind to any of the drug metabolising cytochrome P450 enzymes. The pharmacokinetics of the drug are compatible with twice-daily administration. A once-daily schedule may also be appropriate, but this regimen needs formal clinical evaluation.
Fourteen different extracts of nine vasoactive medicinal plants used in European and African phytotherapy and traditional medicine were pharmacologically tested for their possible calcium antagonistic mode of action. The criteria for the selection of plants were: use in traditional medicine in the treatment of cardiovascular diseases, 'nonspecific' spasmolytic activity (mode of action not known), natural compounds with structural similarities to already known 'calcium-antagonists' or calcium-antagonists that have been found in species of the same tribe. All plant extracts were investigated against contractions of aortic strips induced by K+-depolarization. Extracts derived from Ammi visnaga, Cuajacum officinale, Olea europaea, Peucedanum ostruthium and Ruta graveolens showed a clear activity, while Cryptolepis sanguinolenta, Leonurus cardiaca, Passiflora incarnata and Solidago gigantea showed no effect in this test. A comparison between K+-and norepinephrine-induced contractions evaluated the selectivity of the inhibition, which is demonstrated by the isolation and identification strategy for the Ca++-antagonistic principles of Olea europaea leaves and Peucedanum ostruthium rhizomes.
Isolated uterus and colon segments were taken from sennoside-pretreated female rats. They indicate a possible decrease in spontaneous contractility of both organ segments. Addition of rhein-Na, as one of the probable active metabolites of sennosides, into the bath medium of isolated colon and ileum segments of untreated rats showed a reduction in contractility at concentrations of more than 10–5 and 10–4 mol/l, respectively. Though rhein-Na in concentrations of more than 10–4 mol/l impaired acetylcholine-mediated contractures of isolated colon, the antagonism was obviously partial and noncompetitive. Isolated uteri from previously estrogen-treated rats did not show a change in the contractile behaviour up to concentrations of 10–4 mol/l rhein-Na, whereas higher concentrations induced an increase in contractions. The importance of this finding is not clear.
Planta medica 1987 8 = ppm) 7,54 (2H, m); 6,94 (1H, d); 6,41 (1H, d); 6,21 (1H, d); 4,56 -3,00 C-H der Zucker. '3C-NMR (D20, 8 = pm): 157,99 (C-2); 134,71 (C-3); 179,48 (C-4); 162,0 (C-5); 99,92 (C-6); 164,96 (C-7); 95,16 (C-8); 159,31 (C-9); 105,55 (C-10); 122,80 (C-il); 116,65 (C-12); 145,59 (C-13); 149,12 (C-14); 11707 (C-iS); 123,90 (C-16); die Obrigen Werte vergl. Tabelle I. Aus 460 mg Rohflavonoidgemisch konnten 45 mg 4 isoliert werden.Hydrolyse der Flavonoide Je 2mg 2, 3 bzw. 4 sowie Hyperosid als Vergleich wurden mit 1 ml 4prozentiger H2S04 10 mm auf 110 C erhitzt, danach wurde mit festem BaCO3 neutralisiert und das Zentrifugat mit dem gleichen Volumen Methanol verdunnt. Von diesen Losungen wurden fur die DC je 10 sI auf Kieselgel 60 F4-Platten aufgetragen und nacheinander in den Fliellmitteln: CHC13/MethanollWasser (64 + 36 + 8) und Ethylacetat/ Methanol/EssigsaurelWasser (60 + 15 + 15 + 10) entwickelt. Zur Dctektion wurde mit 0,5-proz. ThymollOsung in 5-proz. ethanolischer Schwefelsäure bespruht und unter Beobachtung Ca. 5 mm auf 120 °C erhitzt. Aus den jeweiligen Hydrolysaten liellen sich neben Quereetin (gelber Fleck an der Front) zusãtzlich nachweisen: Arabinose (violett, Rv 0,45; aus 2, 3 und 4) Xylose (blau, R 0,50; aus 4) und Galaktose (korallenrot RF 0,40; aus Hyperosid).
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