[Self-administration of intravenous drugs--a rare cause of respiratory arrest in medical practice]. / Auto-administrarea de medicamente intravenos-- cauza rara de stop respirator in practica medicala.

Respiratory arrest is a major emergency in medical practice, which implies prompt intervention from the physician assisting such case. Respiratory arrest can be classified into primary respiratory arrest, caused by airway obstruction, decreased respiratory drive, or respiratory muscle weakness and secondary respiratory arrest, as a result of circulatory insufficiency. Among important causes of respiratory arrest, acute poisonings are to remember. We present a case of respiratory arrest following intravenously self-administration of opiates in attempted suicide. Patient required rapidly orientated etiologic diagnostic, and had a favorable outcome, with complete recovery, after applying CPR protocol, as well as antidote.

[The antishock action of opiate antagonists]. / Protivoshokovoe deistvie antagonistov opiatov.

In acute experiment on 86 adult rabbits with traumatic shock modelled according to Cannon, it was established that intravenous administration of Nalorphine at the doses of 0.5 and 2 mg/kg of weight at the early period of shock contributed to prolongation of lifetime of the majority of animals. In some of them, the small doses accelerated the occurrence of lethal outcome. In administration of 0.1 mg/kg of weight of Naloxone, almost all the animals survived. At the late period of shock, the effectiveness of these preparations is insufficient.

[Respiratory depression following controlled-release morphine sulfate tablets]. / Ademhalingsdepressie na het gebruik van morfinesulfaat-tabletten met gereguleerde afgifte.

Controlled release morphine sulfate (MS Contin) is a relatively new oral preparation for the relief of chronic severe (cancer) pain. We describe a patient with severe neuralgia who experienced respiratory depression after ingestion of one single dose of morphine sulfate (20 mg). Administration of nalorphine chloride resulted in instant normalisation of respiratory function. This case illustrates respiratory depression as an adverse effect of MS Contin.

Simultaneous identification and quantification of several opiates and derivatives by capillary gas chromatography and nitrogen selective detection.

A capillary column gas chromatographic method is described for the simultaneous determination of morphine, codeine, heroin, 3- and 6-monoacetylmorphine, nalorphine, naloxone, ethylmorphine, and naltrexone. The drugs were extracted from 2 ml plasma, urine, or other biological samples, including tissue under alkaline conditions in chloroform-isopropanol-n-heptane (50:17:33, v/v), with levallorphan as an internal standard. The drugs were extracted into acid and then reextracted into chloroform after the acid had been alkalinized. After derivatization with trifluoroacetic anhydride, an aliquot was injected into a 25m capillary column equipped with a nitrogen phosphorus detector. The lower limits of detectability, extraction recovery, and the within-run and day-to-day precision of results were determined for each drug. Our results indicate that the procedure is suitable for use in overdose screening and therapeutic drug monitoring.

[Functioning of the pituitary-adrenal system during the vestibulo-vegetative syndrome and administration of dalargin and nalorphine]. / Funktsionirovanie sistemy gipofiz-kora nadpochechnikov pri vestibulovegetativnom sindrome na fone vvedeniia dalargina i nalorfina.

Changes in ACTH, cortisol, beta-endorphin have been investigated during vestibulo-vegetative syndrome (VVS) and injections of dalargin (leu-enkephalin analog) and nalorphine (agonist-antagonist of opioid receptors) in 9 volunteers with low level vestibulo-vegetative stability. Cumulative coriolis acceleration test during rotations on a special chair was used for VVS modelling. Dalargin (1-4 mg), nalorphine (5 mg) and placebo (NaCl solution) were injected intravenously 5-15 min before rotation. A significant increase in ACTH, cortisol and beta-endorphin plasma levels has been observed. Mean positive linear correlation (r greater than +0.6) between ACTH and beta-endorphin and ACTH and cortisol was noted immediately after the test only when dalargin was injected. It is suggested that in VVS there develops a hormonal conflict, i. e. an adequate hormonal release is disturbed.

[Effect of synthetic analogs of enkephalins, morphine and their antagonists on the course of experimental traumatic shock]. / Vliianie sinteticheskikh analogov énkefalinov, morfina i ikh antagonistov na techenie éksperimental'nogo travmaticheskogo shoka.

Effects of naloxone, nalorphine, thyroliberin, morphine and two analogues of enkephalins (FK 33-824 and Tyr-D-Ala-Gly-Phe(NO2)-NH2) on the course of traumatic shock were studied in experiments on rabbits. It was found that antagonists of opioid peptides aggravated the course of traumatic shock and morphine and synthetic analogues of enkephalins exerted positive effects during its treatment. Endogenous opioid peptides are suggested to play the protective role in experimental traumatic shock.

Overview of drugs used in treating drug-induced dependence: a treatise interrelating existing hypotheses in order to attain maximal therapeutic benefits.

Despite the fact that we do not yet completely understand the physiology of physical dependence, many treatment modalities are available. In this overview, an attempt is made to discuss available treatments and mechanisms to possibly attain a better understanding of the complex interactions that occur between systems. An attempt is also made to understand interrelations between drug misuse and mental disorders as one aspect of the treatment process--the ultimate goal being more efficacious and safer therapy.

Antagonista-agonista de opiáceo após morfina peridural / Opiate antagonist-agonist after peridural morphine

Utilizamos antagonista agonista do opiáceo, nalorfina 10 30/microng. kg-1, no tratamento do prurido, náuseas e vômitos e retençäo urinária, quando se tornaram insuportáveis, após 2 mg de morfina peridural pós-operatória, havendo melhora dos sintomas, näo ocorrendo regressäo da analgesia espinhal

[Effect of naloxone in hypotension caused by acute blood loss in Papio hamadryas baboons]. / Effekt naloksona pri gipotonii, vyzvannoi ostroi krovopoterei u pavianov Papio Hamadryas.

Naloxone or physiological solution were injected in different doses to 11 baboons (Papio hamadryas) weighing 7-8 kg after bloodletting in a volume of 40% of the total amount of the blood. Naloxone effectively raised (in all the doses) the arterial blood pressure which dropped after bloodletting. The action of naloxone injected in small doses was more pronounced and had unique time parameters. Besides, the respiratory rate was also increased. Injection of nalorphine in a dose of 1 mg/kg produced a similar but a more demonstrable action as compared with naloxone in a dose of 1 mg/kg. A conclusion is made about the possibility of using the antagonists of opioid peptides on a clinical basis for the treatment of shock conditions. An assumption of an inconclusive role played by the subtypes of opiate receptors in the formation of shock conditions is also confirmed.

Beneficial actions of nalorphine during hemorrhagic shock in cats.

Endogenous opiates have been reported to have detrimental effects on the circulatory system during hemorrhagic shock. However, the specific opiate receptor subtype which mediates these actions has not been defined. In the present study, we have utilized the mixed agonist/antagonist, nalorphine (N-allylnormorphine), which exhibits kappa (kappa) and sigma (sigma) receptor agonism as well as mu (mu) receptor antagonism, to investigate the role of the mu receptor in hemorrhagic shock. Nalorphine (2 mg/kg) produced no significant changes in any observed experimental variable in sham-shocked animals. Shocked animals treated with nalorphine (2 mg/kg) maintained significantly higher final mean arterial blood pressures (MABP) than animals which received only vehicle (102 +/- 3.8 vs 61 +/- 6.6 mm Hg, respectively, p less than 0.001). In addition, nalorphine significantly reduced the rise in plasma MDF activity observed in untreated hemorrhaged animals (42 +/- 3.0 vs 59 +/- 4 U/ml, p less than 0.02). Our results support a significant role for the mu receptor in the deleterious actions of endogenous opioids during hemorrhagic shock.

[Effect of nalorphine and naloxone on the course of electric pain shock in rabbits]. / Vliianie nalorfina i naloksina na techenie élektrobolevogo shoka u krolikov.

Electrical stimulation of the rabbit sciatic nerve resulted in the development of shock. Injection of physiological saline (1 ml, i. v.) did not change the progressive fall of the blood pressure or depression of palpitation and respiration. The animals died 135--191 min after discontinuance of the stimulation. Injection of nalorphine (0.4 mg/kg, i. v.) or naloxone (0.1 mg/kg i. v.) greatly improved the animals' condition. The blood pressure, palpitation and respiration returned to normal in 90--120 min after the injections. No lethal cases were recorded in this group of animals. It was shown in a supplementary group of animals that naloxone did not change the reserpine-produced hypotension.

The antagonistic effect of pentazocine on fentanyl induced respiratory depression compared with nalorphine and naloxone.

The effect of pentazocine, a strong analgesic with a weak opiate antagonistic activity, on fentanyl-induced respiratory depression was studied after anaesthesia in patients undergoing gynaecological laparotomy. Pentazocine (1 mg/kg) was given intravenously at the end of operation. The postoperative respiratory depression in these patients was compared with that in patients who received strong opiate antagonists, nalorphine and naloxone, or no opiate antagonists. Respiratory depression was evaluated by measuring respiratory rate, respiratory minute volume and blood gases. The results show that pentazocine has a clear antagonistic effect on fentanyl-induced respiratory depression but the effect of 1 mg/kg is weaker and shorter than that produced by 5 mg of nalorphine or 0.4 mg of naloxone. Postoperative analgesia in patients who received pentazocine was not longer than that in patients who received no opiate antagonists at the end of the operation.