First-pass effect after rectal administration of thiazinamium methylsulfate.

The absorption and metabolism of the quaternary ammonium compound thiazinamium methylsulfate were studied in humans using plasma concentration data and urinary excretion measurements. After giving a dose of 150 mg in suppositories, the relative bioavailability was 5.8 +/- 3.2 (SD) % of the dose, comparable to the values obtained following oral administration. The degree of first-pass effect observed after rectal administration was comparable with that after oral administration.

Atropine versus glycopyrrolate. A study using repeated doses of suxamethonium in man.

Intermittent doses of suxamethonium have been known to result in bradycardia changes in cardiac rhythm. In order to assess the efficacy of a newer quaternary ammonium antimuscarinic, glycopyrrolate, on the cardia effects of intermittent suxamethonium, 28 patients received this drug intravenously just before induction of anesthesia. For comparison, 28 other patients were given atropine. In the atropine series, three patients developed bradycardia while none of those of the glycopyrrolate series did so. In addition, more patients had cardiac arrhythmias in the atropine group. Although no statistically significant differences were seen, clinically, glycopyrrolate seems to afford better protection against the cardiac changes resulting from intermittently administered suxamethonium.

[Clinical use of arfonad and hygronium aerosols in emergency hypotensive therapy]. / Klinicheskoe primenenie aérozolei arfonada i gigroniia pri neotlozhnoi gipotenzivnoi terapii.

During clinical testing of the administration of ganglion-blocking agents by inhalation (175 persons) it was established that drug aerosols of arfonad and hygronium possess high effectiveness, act rapidly, and are relatively safe. The inhalation method of the management of hypertensive crises may find wide use in out-patient practice, under conditions of the admission room, cardiological and resuscitation departments, as well as in obstetrics when controlled hypotension is necessary.

[Transplantability and growth of sarcoma 37 under a ganglionic blockade]. / Privivaemost' i rost sarkomy-37 v usloviiakh ganglionarnoi blokady.

The inoculation of sarcoma-37 against the background of the ganglionary blockade, provided by the intraperitoneal injection of 1 ml of pentamine, is not associated with its less take rate, but there is a manifest suppression of the tumor growth during the period up to 63 days. A preliminary ganglionary blockade completely eliminates the stimulating effect of a trauma on the tumor growth.

[Prevention of disorders of the blood acid-base equilibrium after operations on the stomach by prolonged pentamine ganglionic block]. / Preduprezhdenie narushenii kislotno-shchelochnogo sostoianiia krovi u bul'nykh posle operatsii na zheludke metodom prodlennoi ganglionarnoi blokady pentaminom.

The acid-base balance was studied in 70 patients operated for peptic ulcer. It was shown that during operation metabolic acidosis could develop and in the postoperative period there occurred metabolic alkalosis associated with hypokalemia. The continuous ganglionic blockade without a pentamine-induced hypotension performed by the proposed method was found to prevent shifts of the acid-base balance towards metabolic alkalosis in the postoperative period. The author believes that the favourable effect of the ganglionic blockade on the acid-base balance is related to the reduced hyperreaction of the sympathoadrenal system, adrenals to the operation trauma which prevents "stress" reactions of the patient.

[Clinical and biochemical evaluation of different types of anesthesia during reconstructive surgery on the abdominal aorta]. / Kliniko-biokhimicheskaia otsenka razlichnykh vidov anestezii pri rekonstruktivnykh operatsiiakh na briushnoi otdele aorty.

Reconstructive operations for occlusive injuries of the aorta and main arteries are followed by substantial changes in the clinico-biochemical indices. The investigation carried out in 100 patients has shown the degree of these changes to depend on the kind of anesthesia. The most favourable kind for the group under study was found to be the general anesthesia with sodium hydroxybutyrate.

[Functional state of the liver in patients with malignant neoplasms, operated on with the use of ganglionic blockaders and moderate hypotension]. / Funktsional'noe sostoianie pecheni u bol'nykh zlokachestvennymi novoobrazovaniiami, operirovannykh s primeneniem ganglionarnoi blokady

The functional state of the liver studied in 411 patients with malignant neoplasms undergoes the least variations under conditions of surgery with ganglionary blockade and moderate hypotension (not less than 90 mm Hg). These patients showed the best indices of protein metabolism and the status of the blood coagulation system, as well as activation of spontaneous anticoagulation. Complications in these patients were observed, but rather more rarely than in patients operated upon without using ganglionary blockade.

[Hemipelvectomy and its anesthesiological management]. / Gemipel'vektomiia i ee anesteziologicheskoe obespechenie

Based on the study of an operative course, anesthesia and immediate postoperative period in 63 patients subjected to hemipelvectomy, it is demonstrated that the danger of early complications in these cases, at present, is not great relatively, and such operations can and must be performed, if indicated. Moreover, hemipelvectomy produces a number of specific changes in the organism that should be taken into consideration in conduction of anesthesia and corrective therapy postoperatively. Ganglionary blockade seems to be an obligatory constituent of anesthesiological provision in hemipelvectomy.

[Treatment of algodystrophy. A randomized study of 95 cases with 3 treatments: Calsyn 100, Visken, Grisefuline and Penthonium]. / Thérapeutique des algodystrophies. Etude randomisée sur 95 cas de trois traitements: Calsyn 100, Visken, Griséfuline et Penthonium.

Three randomised therapeutic protocols were studied: thyrocalcitonin, beta-blockers and the combination of Grisefuline + Penthonium, in a group of 95 cases of algodystrophy (64 women, 31 men). These cases were divided into four groups: upper limb, lower limb, "recent" or "long-standing". The results were assessed after one month of treatment. A positive result was defined as being an improvement of more than 50 p. cent of the clinical subjective and objective criteria; less than that, the activity is uncertain or nil. Comparison of the results did not reveal any statistically significant difference between the three proposed treatments, whether we consider the whole group of patients or each sub-group separately (overall positive results: Calsyn 100 = 53 p. cent, Visken = 42,5 p. cent, Grisefuline + Penthonium = 53 p. cent). The important role played by rehabilitation must be stressed. It should be discontinued during the acute phase and instituted in the later phase. Cure is obtained after an average of 4-5 months of treatment. 10 patients were left with major trophic sequelae after 2 years of the disease; all involve the hand.

[Ganglionic-blockading action of bis-ammonium compounds]. / Mekhanizm ganglioblokiruiushchego deistviia bis-ammonievykh soedinenii.

The actions of bis-ammonium compounds on acetylcholine-activated channels were studied in voltage-clamped neurons of isolated superior cervical ganglion in a rabbit. The kinetics of the compound binding to open channels was estimated from shortening of the decay of fast excitatory postsynaptic current (which is determined by the rate of channels closure). The kinetics of dissociation of the compound from open channels was estimated from the kinetics of the restoration of the second response to double-pulse application of acetylcholine in presence of the blocking compound. The rate constant of bindings of the bis-ammonium compounds to open channels increased while the rate constant of dissociation decreased with membrane hyperpolarization. This voltage-dependence increased with the lengthening of the polymethylene chain in the compound and remained unchanged with the lengthening of nitrogen group radicals. The ganglion-blocking activities of the compounds as determined in the cat ganglion in situ correlated with their rate constants of binding to open channels. It was concluded that ganglion-blocking actions of bis-ammonium compounds is determined by their channel-blocking activities.