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At least 19 recordsLinked to original sources
PubMed1975

The negative inotropic action of propanidid. influence on calcium movements in atrial tissue.

Propanidid (Epontol), a general anaesthetic agent with a particularly short action in vivo significantly depressed the contraction amplitude of guinea pig isolated atria. A steep concentration-response curve could be established. Contractile force of electrically driven atria (180/min) was reduced by approximately 50% at a propanidid concentration of 3.5 x 10-4 M in the medium. The negative inotropic effect developed rapidly (less than 10 min). At concentrations of 4.5 x 10-4 M and less propanidid hardly reduced the frequency of spontaneously beating atria. The uptake of extracellular 45 Ca by spontaneously beating atria occurred significantly more slowly in presence of propanidid (4.5 x 10-4 M ), whereas the exchangeable calcium fraction remained unchanged. Accordingly, propanidid reduced the rate of exchange of calcium so that less ionized calcium was available for excitation-contraction coupling. Propanidid (4.5 x 10-4 M) accelerated the uptake of 45Ca by isolated plasma membranes, obtained from guinea pig ventricular muscle. Moreover, the binding capacity for calcium by isolated membranes was increased in presence of propanidid. These observations imply that less ionized calcium is available for activation of the contractile system. It is concluded that the negative inotropic action of propanidid is probably due to the drug's influence on membrane function, thus bringing about an important change in cellular calcium metabolism.

Animals↗
PubMed1992

[Anesthesiologic efficacy of propanidid as a liposome dispersion. An experimental study with rats].

BACKGROUND: Propanidid, an ultra-short-acting i.v. anaesthetic agent, was widely used in the 1960s. Reports of anaphylactoid reactions in patients associated with release of histamine following administration of the drug, however, led to withdrawal of this useful anaesthetic. Since the adverse side effects of the former solution could be attributed to the solvent cremophor, attempts have recently been made to produce a propanidid solution without addition of the solvent. We report on comparative investigations employing a new liposomal solution (B. Braun, Melsungen, FRG) and the conventional cremophor preparation with regard to anaesthetic properties, haemodynamic side effects, and electroencephalographic effects (EEG). METHODS: Sprague-Dawley rats (n = 46) were implanted with venous and arterial lines and epidural EEG electrodes during chloral-hydrate anaesthesia. The following day, arterial blood pressure (ABP), heart rate (HR), and EEG were monitored in awake animals and then after induction of anaesthesia by a bolus of the respective propanidid preparation, followed by an infusion period of 15 min in six different experimental groups. Animals of groups L-60, L-90, L-120, or C-60, C-90, or C-120 groups received 60, 90, or 120 mg.100 g-1.h-1 of the liposomal (L) or cremophor (C) preparation. During anaesthesia, the corneal reflex and nociception to tail-clamping were also tested. At termination of the infusion, blood samples were drawn for determination of plasma propanidid concentrations. RESULTS: Both preparations were similarly effective in induction and maintenance of anaesthesia in a dose-dependent manner; both similarly lowered ABP and HR. The corneal reflex and nociceptive responses to tail clamping were also comparably suppressed. However, whereas the liposomal preparation was well tolerated at higher dose levels, the cremophor preparation caused considerable dose-dependent mortality of 11%, 86%, and 86% in animals in groups C-60, C-90, and C-120, respectively. Both preparations were found to induce a burst-suppression pattern in the EEG associated with clonic seizures, with a lower incidence with the liposomal preparation (22% and 50% in groups L-90 and L-120) as compared to the cremophor preparation (100% and 89% in groups C-90 and C-120). A remarkable variability in propanidid plasma concentrations was found at the end of the infusion period, although no differences were observed between both preparations. Discontinuation of infusion of propanidid resulted in rapid awakening (less than 5 min), irrespective of whether the liposomal or conventional preparation was employed. CONCLUSION: The present findings demonstrate largely identical anaesthetic potencies of a new liposomal solution as compared to the conventional cremophor preparation of propanidid. The liposomal preparation, however, was superior as far as tolerance and incidence of clonic seizures was concerned. The present findings should prompt further studies on the suitability of liposomal propanidid as a short-acting anaesthetic agent in patients.

Anesthesia, Intravenous↗
PubMed1976

Anaesthetic induction for Caesarean section with propanidid.

Propanidid was used for the induction of anaesthesia at Caesarean section in 50 healthy mothers. All parturients were considered to have normal placental function. Anaesthesia was maintained with nitrous oxide, oxygen, muscle relaxant and controlled ventilation. The patients were tilted laterally with a 15 degrees rubber wedge during the procedure in order to obviate the effects of aorta-caval occlusion. At the time of delivery, arterial blood was drawn from the mother and from the vessels of a double clamped section of umbilical cord, for blood-gas analysis. The results obtained are compared with those previously reported in a similar series anaesthetised with thiopentone, gas, oxygen and relaxant. Maternal blood-gas and acid-base levels were similar in the two groups at delivery. The clinical status of the infants in the present series, as judged by the modified Apgar score at 2 minutes after birth, was satisfactory. Umbilical venous and arterial pH values after propanidid were both 0-054 units (P less than 0-001) less than those following thiopentone; and average base deficits were 3-1 (Uv) and 3-9 (Ua) mEq/litre greater after propanidid (P less than 0-001). Mean oxygen levels in the umbilical cord bloods were 8-0 (Uv) and 3-5 (Ua) mmHg lower (P less than 0-001 & P less than 0-025 respectively) in the propanidid group. Derived oxygen contents was also significantly less than in the previous thiopentone series. (Ma-Uv) and (Ma-Ua) gradients were 0-053 and 0-051 pH units higher after propanidid than that following thiopentone (P less than 0-001). Mean (Ma-Uv) and (Ma-Ua) base deficits were 3-5 and 3-9 mEq/litre greater (P less than 0-001). Five patients offered definite evidence of factual recall, of whom three experienced pain. Propanidid, therefore, appeared to be associated with a greater degree of foetal acidaemia than did thiopentone. In addition, painful factual recall during surgery was encountered in 6 percent of cases. It is concluded that propanidid, although theoretically offering advantages over thiopentone to the obstetric anaesthetist, in practice, did not fulfil this promise.

Anesthesia, Intravenous↗
PubMedDate not supplied

Comparison of the immediate effects of etomidate, propanidid and thiopentone on haemodynamics, coronary bloodflow and myocardial oxygen consumption.

Since cardiovascular depression at induction is among the most common complications of anesthesia this comparative study was undertaken. Unpremedicated dogs (n = 16) were induced with 3 mg/kg piritramide i.v. and normoventilated (N2O/O2 = 2/1). In 8 animals 0.8 and 1.6 mg/kg Etomidate and 5.0 and 10.0 mg/kg thiopentone and in 8 further dogs 5.0 and 10.0 mg/kg Propanidid were tested. Equipotent doses of Thiopentone and Propanidid caused a marked myocardial depression, which was seen in a decrease in stroke volume and max dp/dt and in an increase of leftventricular end-diastolic pressure and pulmonary arterial pressure. The increased myocardial O2- cosumption mainly due to the rise in heart rate was covered after Thiopentone by an increase of coronary bloodflow (measured with a pitot-catheter) and an increase of arterio-coronaryvenous difference in oxygen. As the latter decreased after Propanidid, it appeared that Propanidid has coronary dilatory properties. The results demonstrated the uneconomic work of the heart under the influence of Thiopentone and Propanidid. In contrast to this the cardiovascular system after Etomidate remained nearly unaffected. The data of this study suggest the use of Etomidate rather than Thiopentone and Propanidid in cases of shock syndrome, heart and/or coronary insufficiency.

Anesthetics↗
PubMed1977

Negative chronotropic effect of propanidid on the SA node of the dog heart in vivo.

Effect of propanidid on the pacemaker activity of the SA node was investigated in anesthetized dogs by injecting 30 microgram to 3 mg into the SA node artery in a single dose in a period of 4 sec. The doses of more than 100 microgram usually induced a negative chronotropic response. The injection of more than 1 mg frequently caused a sinus arrest followed by AV nodal rhythm. The initial sinus rhythm, however, was restored within 2 min after the propanidid administration. Its negative chronotropic response was not altered by pretreatment with atropine which completely blocked the action of acetylcholine. Bilateral vagotomy also did not affect the response induced by propanidid. A control solution or histamine failed to cause such a depressant effect on the SA node as observed after the propanidid injection. Thus, we conclude that propanidid supresses the SA nodal activity by a direct local action.

Animals↗
PubMed1977

The effects of propanidid on arterial pressure, pulse rate, preganglionic sympathetic activity and barostatic reflexes in the cat.

We have studied the effects of propanidid on preganglionic cervical sympathetic nervous activity, arterial pressure, pulse rate and barostatic reflexes of the cat. Normal, hypertensive, baroreceptor denervated and decerebrate animals with sectioned vagal nerves were studied. On the basis of our findings it is concluded that propanidid exerts its depressant action on the cardiovascular system directly. Central circulatory control mechanisms are essentially unaffected. The depression of arterial pressure caused by propanidid is moderated by two compensatory mechanisms: normal barostatic reflexes causing an increased sympathetic tone in response to hypotension and a vagolytic action of propanidid.

Animals↗
PubMed1975

Recovery and simulated driving after intravenous anesthesia with thiopental, methohexital, propanidid, or alphadione.

Recovery from anesthesia was assessed in a double-bind manner in 40 healthy volunteer students after intravenous anesthesia with thiopental (6.0 mg/kg), methohexital (2.0 mg/kg), propanidid (6.6 mg/kg), or alphadione (Althesin), 85 mul/kg using a driving simulator 2,4, 6, and 8 hours after injection of the drugs. Clinical recovery was faster after propanidid and methohexital than after thiopental or alphadione. Driving performances remained significantly (P less than 0.05) worse than in a control group for 6 hours after thiopental and for 8 hours after methohexital, and reaction times 8 hours after thiopental remained worse than in the control subjects. After alphadione driving skills were impaired at 6 hours only. Propanidid produced no impairment in driving skills at any time during the experiment. It is concluded that after the doses used in this study patients should not drive or operate machinery for at least 2 hours after propanidid and for at least 8 hours after alphadione. After methohexital and thiopental patients should probably not drive for 24 hours because of the severity of the disturbances at 8 hours.

Adult↗
PubMed1976

Metabolic degradation of propanidid by various tissues. Short communication.

The very short anaesthetic action of 3-methoxy-4-(N,N-diethylcarbamoyl-methoxy)-phenylacetic acid propylester (propanidid, Epantol) is due to its rapid hydrolysis in vivo. In this study, the rates of degradation of this drug under the influence of various isolated tissues have been established. The drug was hydrolysed much more rapidly by liver homogenate than by whole blood or serum. It is concluded that inactivation of propanidid in vivo occurs mainly by the liver, whereas blood esterases play an insignificant part in hydrolyzing the ester. Moreover, it was demonstrated that cardiac tissue is able to hydrolyze the drug as well. It is postulated that the inactivation of propanidid by heart muscle might partly compensate for the severe cardiodepressive action of the anaesthetic agent. A gaschromatographic determination of propanidid has been developed.

Animals↗
PubMed1975

The use of propanidid for blind nasotracheal intubation.

Blind nasotracheal intubation has been attempted in 72 patients under light general anaesthesia with propanidid in a one-dose or two-dose technique which provides conditions for up to six attempts. Nasotracheal intubation was achieved in 49 patients with a one-dose technique, and in a further 15 patients with the supplementary dose. It is suggested that this technique with propanidid is safer than other techniques using non-anasthetic respiratory stimulants with their attendant dangers, and that the success rate with propanidid is similar to that using these other techniques.

Adolescent↗
PubMed1976

Anaesthesia for cardioversion: a comparison of diazepam, thiopentone and propanidid.

Three groups of 50 patients were anaesthetized with diazepam 0.32 mg/kg or thiopentone 3.7 mg/kg or propanidid 4.6 mg/kg for elective carfioversion. Propanidid caused more hypotension than diazepam or thiopentone. Apnoea was most frequent following thipentone and excitatory side-effects were most prominent following propanidid; the electric countershock worsened the excitatory phenomena. The success rate of conversion was higher in the diazepam group than in the other groups, but the difference was not statistically significant. Diazepam failed to produce amnesia in about 33% of the patients. Thiopentone is suitable and pleasant for cardioversion. Diazepam is recommended in poor-risk patients and in emergency situations.

Adult↗
PubMed1979

In vitro interaction of propanidid and suxamethonium with pooled human plasma cholinesterase. A kinetic study.

Human plasma cholinesterase (E.C. 3.1.1.8) was shown to be inhibited by physiological concentrations of propanidid and suxamethonium using a colourimetric assay at 25 degrees C and pH 7.2 unit with butyrylthiocholine as substrate. Propanidid inhibited the enzyme in a non-competitive manner (I50 = 2.0 mmol litre-1; apparent Km = 6.6 X 10(-4) mol litre-1) as did suxamethonium (I50 = 4.4 mmol litre-1; apparent Km = 1.6 X 10(-4) mol litre-1). Combined inhibition produced Km 3.0 X 10(-3) mol litre-1. The binding of these drugs to specific anionic sites in the vicinity of the active centre is thought to result in stereochemical changes in the enzyme. This mechanism and its relevance to the augmentation of the neuromuscular blockade produced by suxamethonium in the presence of propanidid is discussed.

Cholinesterase Inhibitors↗
PubMed1975

On the mechanism of the negative inotropic action of halothane and propanidide.

1) Halothane and propanidide reduce the contractile force of guinea pig isolated atria in a concentration-dependent manner. The approximate concentrations required to bring about a half-maximal pharmacological effect are within the same order of magnitude as the concentrations found in whole blood during general anesthesia of guinea pigs. 2) It seems most likely that the initial effect of halothane or propanidide occurs at the cell membrane. 3) Halothane and propanidide accelerate and enhance the uptake of calcium ions by the cell membrane, so that less ionized calcium will be available for excitation contraction coupling. This phenomenon readily explains the negative inotropic action of both drugs and confirms the presumption that the cell membrane is the initial site of pharmacological attack.

Animals↗
PubMed1975

Propanidid for anaesthetic induction at Caesarean section.

In 50 healthy mothers scheduled for elective Caesarean section, anaesthesia was induced with propanidid (7 mg/kg body weight). Thereafter, ventilation was controlled with nitrous oxide, oxygen and muscle relaxants. A further dose of propanidid (1 mg/kg body weight) was administered 3 minutes after the initial injection of this drug, as a means of preventing maternal awareness during equilibration with the anaesthetic gas mixture. The acid-base status of the mothers before the induction of anaesthesia, and at delivery, revealed a mild degree of respiratory alkalosis with a compensatory metabolic acidosis. Umbilical cord blood gas results indicated the presence of significant fetal acidosis, both respiratory (mean pCO2 Uv 46,3 torr (SD 11,3) and Ua 54,3 torr (SD 12,0)), and metabolic (mean base excess Uv-9 mEq/l (SD 4,2) and Ua-11,8 mEq/l, (SD 5,0)) in origin. The average umbilical cord blood oxygen tensions were Uv 25,9 torr (SD 10), and Ua 15,4 torr (SD 8,5); mean maternal to fetal base-excess gradients were Ma-Uv 4,1 mEq/l (SD 2,8) and Ma-Ua 6,5 mEq/l (SD 3,5). Five mothers (10%) offered convincing evidence of factual recall during surgery, and 3 of these were aware of pain. Nausea and vomiting occurred in 5 patients and in 4 there were clinical signs of postoperative chest infection. The degree of fetal biochemical asphyxia, and the incidence of maternal awareness during surgery, were significantly greater than previously reported when thiopentone was used for the induction of anaesthesia for Caesarean section. The results obtained are discussed, and the conclusion is drawn that propanidid for anaesthesia appears to offer no advantage over thiopentone in obstetric practice.

Acidosis↗
PubMedDate not supplied

[Use of propanidid in bioelectrical brain activation].

The purpose of the study was evaluation of propanidid as an agent activating the bioelectric activity of the brain. Examinations were carried out in 200 patients. In patients with generalized epileptic seizures a positive result of activation trial was obtained in 92,8% of the cases. In cases of focal epilepsy, temporal or not temporal, administration of propanidid revealed or increased pathological focal activity all. Activation permitted also brain tumours to be localized more precisely. In patients with cerebraal circulatory disturbances the activating effect of propanidid was observed in 82,8% of the cases. The drug is suitable for outpatient practice and for follow-up examinations.

Adolescent↗
PubMed1979

The relative potencies of thiopentone, ketamine, propanidid, alphaxalone and diazepam. A statistical study in man.

The potency of five i.v. anaesthetics (thiopentone, ketamine, alphaxalone (Althesin), propanidid and diazepam) was studied by determining the dose required to produce unconsciousness in 50% (UD50) and 95% (UD95) of patients. UD50 and UD95 were determined using the probit method. The effect of age on the anaesthetic requirement has been studied also. Relative to thiopentone, the potency was alphaxalone 9.22, diazepam 5.24, ketamine 4.37 and propanidid 1.006.

Adult↗
PubMed1978

Postanaesthetic postural stability following thiopental or propanidid anaesthesia.

Using a quantitative Romberg-test performed on a computerized force-plate-system, postural stability was tested in 39 patients before and 3 hours after general anaesthesia with either thiopental (20 patients) or propanidid (19 patients). Sway-tendencies in the sagittal and the transversal direction were recorded. Comparing pre- and postoperative test results, patients anaesthetized with thiopental had a decreased postural stability 3 hours after anaesthesia, indicated by a significantly (P less than 0.05) increased sway-tendency of 22.6% in the sagittal direction. No change occurred in sway-tendency in the transversal direction in this group. In the propanidid group no significant differences were found between pre- and postoperative test results.

Adolescent↗
PubMed1978

The effect of propanidid on systemic vascular resistance in man.

We have studied the peripheral vascular effect in man of propanidid 6 mg/kg, administered as a bolus injection during cardiopulmonary by-pass with the aorta cross-clamped and at constant perfusion flow. Ten measurements in eight patients were performed. A decrease was found in systemic vascular resistance: from 150.7 +/- 16.3 to 99.5 +/- 10.1 kPa x s/1. No venous pooling occurred. It is concluded that, in man, propanidid causes a vasodilation which must contribute to the hypotension it causes.

Anesthesia, Inhalation↗
PubMed1976

[Cardiodepressive effects due to ketamine, etomidate, methohexitone and propanidid. A clinical study by means of the systolic-time-intervals (author's transl)].

The cardiodepressive effects of ketamine (1mg/kg), etomidate (0.3mg/kg), methohexitone (1mg/kg) and propanidid (4mg/kg) have been compared by means of the systolic time intervals on patients during a steady-state halothane--N2O:02(1.1)-- anaesthesia. This anaesthesia served as a pharmacological model of reduced myocardial function, and moreover, it should block the centrally-elicited cardiac stimulation by ketamine, thus unmasking the direct negative inotropic action of this anaesthetic. Ketamine and etomidate are of lesser cardiac depressant action than methohexitone or even propanidid. Diazepam (0.2-0.25mg/kg) proved to be able to attenuate or abolish, respectively, the ketamine-induced increases of heart rate and blood pressure in normo- and hypertensive patients, and might therefore be useful for induction anaesthesia in cardiac and coronary risk patients, as proved on two patients with recent myocardial infarction.

Adult↗