RESUMO
The pharmacokinetic behaviour and neuromuscular blockade produced by the administration of fazadinium bromide at a dose of 1 mg/kg have been studied in seven patients with end-stage renal failure. No significant differences were found in the pharmacokinetic or pharmacodynamic properties when compared with patients with normal renal function. It is suggested that fazadinium may be superior to either d-tubocurarine or pancuronium in providing muscle relaxation for patients with renal failure.
Assuntos
Falência Renal Crônica/sangue , Compostos de Piridínio/sangue , Transmissão Sináptica/efeitos dos fármacos , Adulto , Idoso , Feminino , Meia-Vida , Humanos , Falência Renal Crônica/fisiopatologia , Cinética , Masculino , Pessoa de Meia-Idade , Contração Muscular/efeitos dos fármacos , Junção Neuromuscular/fisiologia , Compostos de Piridínio/farmacologiaRESUMO
Fazadinium was administered as an intravenous bolus of 0.5 or 1 mg/kg to nine patients during neurolept-anaesthesia. Continuous recording of neuromuscular activity and serial collection of blood samples for drug assay allowed the relationship between neuromuscular blockade and plasma fazadinium concentration to be studied. Pharmacokinetic analysis demonstrated high plasma clearances (221 and 185 ml/min), and short terminal half-lives, (30 and 50 min), for the two doses of the drug. Mean plasma concentrations at 10 and 50% recovery were 1.42 and 0.88 micrograms/ml respectively, demonstrating that the potency of fazadinium is approximately half that of tubocurarine and one eighth that of pancuronium. In addition, the relationship between plasma concentration and depression of neuromuscular activity during spontaneous recovery from the relaxant is described.
Assuntos
Compostos de Piridínio/sangue , Adulto , Idoso , Feminino , Humanos , Cinética , Masculino , Pessoa de Meia-Idade , Contração Muscular/efeitos dos fármacos , Neuroleptanalgesia , Junção Neuromuscular/efeitos dos fármacos , Compostos de Piridínio/farmacologiaRESUMO
Suxamethonium was administered to patients during recovery from non-depolarising muscle relaxation. The effect of suxamethonium varied depending upon the degree of recovery from the non-depolarising block when it was administered. Early in recovery suxamethonium produced reversal of the non-depolarising block without paralysis whereas when administered later, initial recovery of the non-depolarising block was followed by paralysis. If administered after 50% recovery the predominant effect was paralysis without initial recovery. Assessment of neuromuscular blockade with train-of-four stimulation showed that the paralysis produced by suxamethonium under these circumstances, had depolarising and non-depolarising features.
Assuntos
Junção Neuromuscular/efeitos dos fármacos , Succinilcolina/farmacologia , Atropina/farmacologia , Humanos , Neostigmina/farmacologia , Junção Neuromuscular/fisiologia , Paralisia , Período Pós-Operatório , Transmissão Sináptica/efeitos dos fármacosRESUMO
A retrospective study of postoperative respiratory morbidity in 247 patients requiring renal transplantation between 1955 and 1973 showed that 7 patients required postoperative controlled ventilation for up to 6 days. The nondepolarising relaxants tubocurarine and pancuronium were used in only 65 patients, but all 7 cases of respiratory failure occurred in this group. This suggests that the use of these drugsin anephric patients is potentially hazardous so far as postoperative respiratory insufficiency is concerned.
