Disease relevance of Dazopironium

• 1 Results from in vitro experiments on the phrenic nerve-diaphragm and the hypogastric nerve-vas deferens preparations of the guinea-pig have been used to plot log concentration-effect curves for skeletal neuromuscular and ganglion blockade, respectively, for (+)-tubocurarine, pancuronium, alcuronium, gallamine and fazadinium (AH 8165) [1].
• A supplementary biliary pathway appears to be a possible explanation for the rapid elimination of fazadinium, even in patients with renal failure [2].
• Serum concentrations of fazadinium were measured in eight patients with cirrhosis and eight patients with total biliary obstruction who underwent abdominal surgery [3].
• Fazadinium pharmacokinetics in patients with liver disease [3].
• Three cases of hypersensitivity to an anaesthetic induction with fazadinium and thiopentone are described [4].

High impact information on Dazopironium

• 2 In the anaesthetized cat, maximum neuromuscular block of tibialis anterior muscle twitches following rapid intravenous injection of fazadinium was obtained as the injection bolus passed through the muscle, indicating the fazadinium very readily crosses capillary membranes [5].
• There was a mean increase in heart rate of 5 beat min-1 during anaesthesia although the maximum values reached 200 beat min-1 in children, and 150 beat min-1 in adults who received fazadinium and 140 beat min-1 in adults who did not [6].
• The effect of atracurium or fazadinium on intra-ocular pressure. A comparative study during induction of general anaesthesia [7].
• The pharmacokinetics of fazadinium were analysed according to a two-compartment open model [8].
• Pharmacokinetics of fazadinium in patients with renal failure [2].

Chemical compound and disease context of Dazopironium

• The effects on muscle fasciculations and ease of tracheal intubation of pretreatment with fazadinium before administration of succinylcholine were evaluated in 85 patients [9].

Biological context of Dazopironium

• The effect of thiopentone and fazadinium on intraocular pressure [10].
• This rapid elimination phase of fazadinium did not correspond to an extensive biotransformation because fazadinium was excreted almost unchanged in the urine and this excretion accounted for 50% of the injected dose within 24 h [11].
• It is concluded that because of early good intubating conditions and favourable pharmacokinetics with a modest placental passage, fazadinium might be particularly useful in obstetrics [12].
• It is suggested that fazadinium may be superior to either d-tubocurarine or pancuronium in providing muscle relaxation for patients with renal failure [13].
• The administration of fazadinium was associated with a stable blood pressure and moderate sinus tachycerdia [14].

Anatomical context of Dazopironium

• Whereas autonomic blockade with tubocurarine occurred at parasympathetic and sympathetic ganglia, neuromuscular paralysing doses of gallamine, alcuronium, pancuronium and fazadinium caused blockade at vagal postganglionic sites in the heart [15].
• In cats and monkeys neuromuscular paralysis of the twitch responses of the gastrocnemius muscle by fazadinium was accompanied by impairment of the vagally induced bradycardia, but cardiovascular disturbances were small [16].

Associations of Dazopironium with other chemical compounds

• Effects of fazadinium in doses of 0.75, 1.0 and 1.25 mg/kg and pancuronium 0.1 mg/kg on respiratory functions (tidal volume, minute volume and inspiratory force) and correlation between respiratory functions and neuromuscular transmission were evaluated in 64 children aged 6 months to 12 years undergoing various types of elective surgery [17].

Analytical, diagnostic and therapeutic context of Dazopironium

• Pharmacokinetics and placental transmission of fazadinium in elective caesarean sections [12].
• Fazadinium, 1 mg/kg, was administered to 16 women undergoing general anaesthesia for casearean section or vaginal delivery with forceps [18].
• The onset of paralysis of the tetanic contractions after the intravenous injection of fazadinium (0.4 mg/kg) occurred within two minutes, but recovery was slow and about 50 minutes were needed for its completion [16].
• Pancuronium v. fazadinium. Effect on intraocular pressure during rapid endotracheal intubation [19].

References