Disease relevance of Bethanidine

• Systemic hemodynamic effects of bethanidine in essential hypertension [1].
• In conclusion, the efficacy of bethanidine for preventing ventricular tachyarrhythmias as assessed by programmed stimulation is low [2].
• Despite protriptyline administration in 54 of 59 bethanidine trials, symptomatic hypotension occurred in 30 trials (51%) [2].
• Intravenous administration of bethanidine, meobentine or quinidine (1 to 20 mg kg-1) protected rats against these arrhythmias [3].
• Bethanidine increased ventricular fibrillation threshold in the normal dog heart from an average control value of 28.5 mA to an average peak value of 66.5 mA, an increase of 150 percent [4].

High impact information on Bethanidine

• The degree of orthostatic fall in blood pressure was greater with bethanidine than with guanethidine (P less than 0.05) [5].
• Multiclinic controlled trial of bethanidine and guanethidine in severe hypertension [5].
• In contrast to amiodarone, the IC50 values for other class III drugs (bretylium, sotalol, bethanidine, N-acetylprocainamide) were much higher than their therapeutic concentrations and bore no relation to them [6].
• The calculated structural data do not only explain the abstraction of a proton from the acceptor betanidin, but further imply that the reaction mechanism might also involve a catalytic triad, with similarities described for the serine protease family [7].
• Based on protein sequence data and RT-PCR, a full length cDNA encoding betanidin 5-O-glucosyltransferase (5-GT) was obtained from a cDNA library of Dorotheanthus bellidiformis (Burm.f.) N.E.Br [8].

Chemical compound and disease context of Bethanidine

• Like bretylium, the antifibrillatory action of bethanidine was manifested by the appearance of nonsustained ventricular fibrillation when superthreshold shocks induced episodes of ventricular fibrillation lasting from 2 to 120 seconds and converting spontaneously to sinus rhythm [4].
• A comparison and an investigation of a potential synergistic effect of labetalol and bethanidine in patients with mild hypertension [9].
• Bretylium is the only drug approved by the Food and Drug Administration specifically for the "prophylaxis and treatment of ventricular fibrillation." Unlike bretylium, which is poorly absorbed from the gut and limited to parenteral use, oral bethanidine is absorbed rapidly [10].
• In studies of ouabain-induced tachycardias and 24-h infarct-induced ventricular arrhythmias, bethanidine tends to increase heart rate and/or exacerbate the ectopic activity (due to its sympathomimetic effects), whereas meobentine tends to reduce heart rate and restore normal sinus rhythm [11].
• The combined effect of propranolol with bethanidine or methyldopa in hypertension [12].

Biological context of Bethanidine

• The urinary excretion kinetics of bethanidine during and after repetive oral dosing was also studied [13].
• Pharmacokinetics of bethanidine in hypertensive patients [13].
• Substrate specificity and sequence analysis define a polyphyletic origin of betanidin 5- and 6-O-glucosyltransferase from Dorotheanthus bellidiformis [14].
• Betanidin 6-O-glucosyltransferase (6-GT) is involved in the glycosylation of betacyanins, which replace the chromogenic anthocyanins as flower colorants in the Caryophyllales [14].
• The 6-GT cDNA was cloned from a cDNA library of Dorotheanthus bellidiformis (Burm. f.) N.E. Br., and the amino acid and nucleotide sequences were shown to be distinctly different from the corresponding betanidin 5-O-glucosyltransferase (5-GT) from the same plant species [14].

Anatomical context of Bethanidine

• This dose of bethanidine produced no effect on sinus node function, atrioventricular conduction, or atrial or ventricular refractoriness [15].
• A fluorometric method for determining bethanidine in blood plasma is described [16].
• Muscarinic receptors involved in cholinergic neurotransmission were studied in isolated innervated guinea-pig tracheas using preganglionic (nerve) and postganglionic (field) stimulation, after blocking sympathetic effects with bethanidine (5 microM) [17].
• Normal Purkinje fibers were exposed to bethanidine (10-80 mg/L) for 30-40 min [18].
• Bethanidine was found to relax vascular smooth muscle [19].

Associations of Bethanidine with other chemical compounds

• The diurnal variation of blood pressure was slightly greater with bethanidine than with guanethidine [5].
• 5-GT catalyses the transfer of glucose from UDP-glucose to the 5-hydroxyl group of the chromogenic betanidin [8].
• A comparison of the effects of bethanidine, meobentine and quinidine on the electrical activity of rat hearts in vivo and in vitro [3].
• In addition to the 5-GT and 6-GT, we isolated a UF3GT from D. bellidiformis cell cultures that preferentially accepted myricetin and quercetin, but was inactive with betanidin [20].
• Unlike bretylium, which is very poorly absorbed from the gut, bethanidine is rapidly and effectively absorbed after oral administration [4].

Gene context of Bethanidine

• In this novel method for quantifying bethanidine in plasma, after a multi-step extraction of bethanidine and internal standard from 2.0 mL of plasma, the drugs are separated on a "microbore" C18 reversed-phase column and quantified by their ultraviolet absorbance at 210 nm [21].

Analytical, diagnostic and therapeutic context of Bethanidine

• Thin-layer chromatography (TLC) and isotope dilution analysis of the urine samples indicated that only intact bethanidine was excreted [13].
• Determination of bethanidine in plasma by liquid-chromatography with a microbore reversed-phase column [21].
• Blood levels and urinary excretion rates of bethanidine were determined in three normal human subjects following oral administration of a single dose of the drug [22].
• 5. In a double-blind study in three patients with desmethylimipramine 25 mg three times daily, mianserin 20 mg three times daily did not antagonize the hypotensive action of either guanethidine or bethanidine [23].
• Myocardial bethanidine kinetics after single-dose intravenous infusion: correlation with plasma kinetics in closed-chest dogs [24].

References