[Labor analgesia with propanidid (Bayer 1420) and the diazepam-propanidid sequence. Clinical contribution].
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Anesthesia, Obstetrical↗
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[Painless labor with propanidid (on the use of propanidid by phleboclysis in labor)].
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Adolescent↗
[Propanidid anesthesia by continuous venous perfustion in minor A/Domenichini E, Mapelli A: [Propanidid anesthesia by continuous venous perfusion in minor otorhinolaryngologic surgery].
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Adult↗
The gamma-aminobutyrate/benzodiazepine receptor from pig brain. Enhancement of gamma-aminobutyrate-receptor binding by the anaesthetic propanidid.
The binding of [3H]muscimol, a gamma-aminobutyrate (GABA) receptor agonist, to a membrane preparation from pig cerebral cortex was enhanced by the anaesthetic propanidid in a concentration-dependent manner. At 0 degrees C, binding was stimulated to 220% of control values, with 50% stimulation at 60 microM-propanidid. At 37 degrees C, propanidid caused a more powerful stimulation of [3H]muscimol binding (340% of control values). Propanidid (1 mM) exerted little effect on the affinity of muscimol binding (KD approx. 10 nM), but increased the apparent number of high-affinity binding sites in the membrane by 2-fold. Enhancement of [3H]muscimol binding was observed only in the presence of Cl- ions, half-maximal activation being achieved at approx. 40 mM-Cl-. Picrotoxinin inhibited the stimulation of [3H]muscimol binding by propanidid with an IC50 (concentration causing 50% inhibition) value of approx. 25 microM. The enhancement of [3H]muscimol binding by propanidid was not additive with the enhancement produced by secobarbital. Phenobarbital inhibited the effect of propanidid and secobarbital. The GABA receptor was solubilized with Triton X-100 or with Chaps [3-[(3-cholamidopropyl)dimethylammonio]propanesulphonate]. Propanidid and secobarbital did not stimulate the binding of [3H]muscimol after solubilization with Triton X-100. However, the receptor could be solubilized by 5 mM-Chaps with retention of the stimulatory effects of propanidid and secobarbital. Unlike barbiturates, propanidid did not stimulate the binding of [3H]flunitrazepam to membranes. It is suggested that the ability to modulate the [3H]muscimol site of the GABA-receptor complex may be a common and perhaps functional characteristic of general anaesthetics.
Animals↗
[Anesthesia with propanidid in a liposomal preparation. An experimental study in swine].
BACKGROUND: Propanidid was widely used as a short-acting i.v. anaesthetic until it was withdrawn due to severe haemodynamic side effects. It was presumed that anaphylactoid reactions with massive histamine release were caused by the solvent cremophor rather than by propanidid itself. A new liposomal preparation of propanidid was examined in this animal study and compared with propanidid in cremophor solution and with propofol. METHODS: Eighteen pigs were randomly assigned to one of the following groups: Group 1 (n = 6): Propanidid in liposomal preparation (PropaLip; Braun Melsungen, Germany). Anaesthesia was induced with 60 mg/kg, followed by continuous infusion of 400 mg/kg.h. Group 2 (n = 6): Propanidid in cremophor solution (PropaCrem; Sombrevin, Gedeon Richter, Budapest) 15 mg/kg, 100 mg/kg.h. Group 3 (n = 6): Propofol (Disoprivan, Zeneca, Plankstadt, Germany) 5 mg/kg, 20 mg/kg.h. After induction and tracheal intubation, the animals were ventilated with 50% oxygen in air. Basic monitoring included noninvasive blood pressure measurements, electrocardiographic monitoring, and capnography. In a short surgical procedure, arterial and pulmonary artery catheters were placed via the right carotid artery and right internal jugular vein, respectively. As soon as the animals responded to a pain stimulus a second anaesthetic induction was performed, followed by a 60-min continuous infusion of the agent studied with invasive haemodynamic monitoring including arterial and pulmonary arterial pressures and cardiac output. Blood samples were taken for the measurement of serum levels of adrenaline, noradrenaline, cortisol, aldosterone, adrenocorticotropic hormone, and histamine. RESULTS: Intubation conditions and quality of anaesthesia were best in propofol animals, followed by PropaCrem animals. In spite of the large dose of 410 mg/kg.h, resulting in a volume load of as much as 16.4 ml/kg.h, the PropaLip animals showed evidence of poor anaesthetic quality. In group 1 we recorded the highest increases in heart rate (91 vs. 115/min), cardiac output (5.4 vs. 7.7 l/min), plasma catecholamine levels, and histamine concentrations (124-268 ng/ml). CONCLUSIONS: In our animal study, propanidid in liposomal preparation failed to show promise as a new anaesthetic agent. Our results are discussed in view of a drug targeting the cells of the reticuloendothelial system, especially the liver, where liposomes are eliminated from the blood. This may result in the transport of propanidid to one of its major places of inactivation.
Anesthesia, Intravenous↗
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↗
[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↗
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↗
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↗
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↗
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↗
The effects of phenobarbital, bis-p-nitrophenyl phosphate and disulfiram on the hydrolysis of propanidid in Wistar rats.
The short-acting anesthetic propanidid was used in vivo as a model substrate in studies of phenobarbital-inducible carboxylesterases in Wistar rats. Phenobarbital shortened the duration of anesthesia produced by intravenous (25 mg/kg) or intraperitoneal (750 mg/kg) administration of propanidid which was in good agreement with the lowered plasma concentration and the shortened half-life of propanidid in phenobarbital-pretreated rats. The treatment of rats with bis-p-nitrophenyl phosphate or disulfiram with or without phenobarbital-pretreatment prolonged the sleeping time and the half-life of propanidid in plasma.
Animals↗
[Propofol versus propanidid for the conduction of suspension laryngoscopy].
Forty patients who where to undergo suspension laryngoscopy were randomly assigned to two groups, the first receiving 1 microgram . kg-1 fentanyl and a bolus of 2.5 mg . kg-1 propofol followed by 5 to 10 mg . kg-1 . h-1 propofol infusion, and the second 1 microgram . kg-1 fentanyl and 0.2 mg . kg-1 flunitrazepam with 8 mg . kg-1 propanidid in a bolus followed by 40 to 50 mg . kg-1 propanidid infusion. The following parameters were studied: length of apnoea, quality of anaesthesia, the time between stopping giving the anaesthetic and the moment when the patient opens the eyes, gives his name and date of birth, the heart rate, the systolic, diastolic and mean blood pressures, blood gases, before induction, during suspension and at stopping the infusion. Anaesthetic quality was the same for both protocols, and the variations of the haemodynamic parameters were very similar for both groups. Apnoea lasted twice as long with propofol as with the flunitrazepam-propanidid association (p less than 0.001), whereas recovery was twice as quick (p less than 0.001). This seemed to confirm that propofol is better indicated for this type of surgery than the previously used flunitrazepam-propanidid association.
Adult↗
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↗
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↗
[Propanidid as an antagonist: competitive inhibitor of neuromuscular plaque acetylcholinesterase].
Propanidid is a competitive inhibitor not only of serum cholinesterase, but of neuromuscular plaque and brain acetylcholinesterase also. The I50 of plaque acetylcholinesterase occurs at much higher concentrations of anaesthetic than for serum enzyme, this may depend on the environmental conditions under which propanidide has to act, or on acetylcholinesterase's high degree of specificity by comparison with pseudocholinesterase. Succinylcholine also inhibits serum cholinesterase but not plaque enzyme. With respect to the serum enzyme, the inhibition curve of the two drugs combined is similar to that of propanidide alone. The prolongation of apnoea observed during propanidide-induced anaesthesia, when succinylcholine is administered, does not appear to be due to diminution of serum cholinesterase activity but rather to interference of the two other drugs with neuromuscular transmission.
Animals↗
[Comparison of propofol and propanidid administered at a constant rate].
So as to compare the anaesthesia obtained using propofol with that obtained using propanidid, 40 ASA I patients, aged between 18 and 50 years, who were to undergo elective orthopaedic or plastic surgery lasting more than 60 min, were randomly divided into two equal groups, one receiving propofol (PF) and the other propanidid (PD). All the patients received 0.5 mg atropine, 100 mg pethidine and 7.5 mg droperidol (10 mg if weight greater than 60 kg) intramuscularly 45 min before induction. Patients in group PF were then given 2 mg.kg-1 propofol over 1 min and 0.9 microgram.kg-1 fentanyl over 3 min, followed by a constant rate infusion of 5 mg.kg-1.h-1 propofol and 3 micrograms.kg-1.h-1 fentanyl. For PD patients, the doses of fentanyl were identical; they were given 10.6 mg.kg-1 propanidid over 3 min for induction, and 37 mg.kg-1.h-1 for maintenance. All the patients were intubated and ventilated mechanically. The usual anaesthetic parameters were monitored at induction, during surgery, and during recovery. Consciousness was lost more quickly with propofol (p less than 0.05), but the corneal reflex returned more rapidly in group PD (p less than 0.02). The time required for a full return to normal consciousness was identical in both groups. The fall, during induction, and the increase, during recovery, of Pasys were greater in group PD (p less than 0.05 and less than 0.001 respectively). Padia and heart rate were lower in group PF after the 30th min (p less than 0.05 and less than 0.01 respectively).(ABSTRACT TRUNCATED AT 250 WORDS)
Adult↗
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↗