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At least 991 records · Page 55Linked to original sources
PubMed1989

[Chronopharmacologic characteristics of the development of tolerance for the narcotic effect of ethanol in a hot climate].

The experiments have been carried out on rats tested by Parsolt in various time of the day in January and July. The results of investigations showed that the behaviour activity of animals was exposed to daily and season fluctuations. The tolerance development to the ethanol narcotic effect depends upon the behaviour activity of animals. During summer the increasing of ethanol toxicity was observed. In highly active rats as distinct from low active animals the real increasing of noradrenaline concentration and the decreasing of dofamine concentration were noted. Ethanol changes the correlations of blood monoamines and the behaviour activity of animals.

Animals↗
PubMed1989

[Studies on the analysis of some narcotic analgesics and CNS-stimulants].

Procedures for the separation and identification of 12 narcotic analgesics and 2 CNS-stimulants are described using GC/FID, GC/NPD and GC/MSD. The TFA and TMS derivatives were prepared by adding TFAA, MB TFA and MSTFA to the standard drugs. The mixture was heated at 70 degrees C for 30 min and chromatographed on FS capillary columns (SE-54, HP-5). Preliminary results show that all the derivatization with TFAA is better than that with MBTFA, but not much different from MSTFA derivatization. The method is reliable, fast and simple and may be used to screen these drugs and further applied to the analysis of biological fluids such as plasma and urine.

Analgesics, Opioid↗
PubMedDate not supplied

[Influence of klofelin on the analgesic and autonomotropic effects of narcotic analgesics].

In conscious rats clopheline (0.1-0.25 mg/kg), in contrast to promedol, morphine and fentanyl administered at analgesic doses, suppressed nociceptive reactions of arterial blood pressure produced by a mechanical stimulation and intracardiac infusion of bradykinin. The use of clopheline in combination with narcotic analgesics potentiated the analgesic effect and significantly inhibited nociceptive hemodynamic reactions without changing the background level of arterial blood pressure.

Analgesics↗
PubMedDate not supplied

[Influence of adrenergic-blocking agents on the pain-alleviating effect of narcotic analgesics].

The action of adrenoblocking agents on the dynamics of the pain allaying effect of narcotic analgesics, measured by the magnitude of the pain reaction threshold after irritation of the tail skin with electric current was studies in tests on mice. The beta-adreno-blocking agent (anaprillin or inderal) was found to significantly potentiate and to lengthen the action of morphine, and so did, to a lesser degree, promedol (trimeperedin) and phentanyl, while the alpha-adrenoblocking agent (phentolamine) weakened the analgesic effects of morphine and promedol, without having any essential influence on the effect of phentanyl. Phentolamine does not eliminate the potentiating effect of anapraline on the analgesic action of morphine but is capable to lessen it.

Analgesics, Opioid↗
PubMedDate not supplied

[Experimental analysis of interference between alpha-adrenergic stimulants with anti-hypertensive activity and the narcotic activity of pentobarbital].

The interactions of 3 classical alpha-adrenergic antihypertensives of prevalently central type (St 155 or clonidine St 600; BR 750 or guanabenz) with the narcotic effects of pentobarbital have been investigated in the Mus musculus. Interferences between convulsant drugs and spontaneous and coordinatory motor activity were also analysed in comparative studies.

Adrenergic alpha-Agonists↗
PubMed1978

[Spontaneous and provoked nystagmus as a criterion of the duration of effect of hypnotics and narcotics in ambulant surgery (author's transl)].

A testing of usefulness of systematic search for spontaneous and provoked nystagmus relative to the duration of effect of several hypnotics and narcotics showed in 83% positive vestibular findings in 150 non-selected, ear sound patients. Vestibular nystagmus was still detected 2 hour p.o. in 74%, 3 hours p.o. in 30% and 4 hours p.o. in 7% of cases. 78 times (52%) a convergent or divergent posture nystagmus was recorded and 47 times (31%) a vertical nystagmus. The subjective sensations of the test persons are out of proportion to the objective findings. The localisation of the pharmacotoxic lesion is discussed.

Adult↗
PubMed1979

1,6-Dimethyl-4-oxo-1,6,7,8,9,9a-hexahydro-4H-pyrido [1,2-a] pyrimidine-3-carboxamide (Chinoin-127), a potent non-narcotic analgesic and antiinflammatory agent.

1,6-Dimethyl-4-oxo-1,6,7,8,9,9a-hexahydro-4H-pyrido[1,2-a]pyrimidine-3-carbamide (Chinoin 127), a non-narcotic analgesic with potent antiinflammatory activity is described. Chinoin-127 is more potent as an analgesic in the hot plate, Randall-Selitto and writhing tests than is acetylsalicylic acid (ASA) and an effective antiphlogistic agent in a battery of tests (carrageenin, kaolin and dextran induced rat paw edema, Northover test, carrageenin induced abscess, implanted cotton pellet method, adjuvant arthritis) used for measuring antiinflammatory activity. The PG-synthesis inhibitors (indometacin, suprofen) were found to be devoid of analgesic activity, and great test-dependent variations in their antiinflammatory effect were observed. They proved to be inactive in the Northover test. Unusual grade of inhibition in the carrageenin-induced rat paw edema test was obtainable by the simultaneous administration of Chinoin 127 and indometacin.

Abscess↗
PubMed1988

[Acute poisoning with a narcotic (Tramadol) in an infant of five weeks].

Accidental rectal administration of 27 mg/kg of the narcotic analgesic Tramadol to a five-week-old infant resulted in severe cerebral depression, which had to be treated with Naloxone during 48 hours. The severity and the duration of this intoxication are not explained solely by the high dosage of Tramadol. A decreased elimination kinetics and an increased permeability of the blood-cerebrospinal fluid barrier probably also account for the pattern of the present intoxication.

Accidents↗
PubMed1988

Piroxicam and doxepin--an alternative to narcotic analgesics in managing advanced cancer pain.

To provide an effective continuum of the relief of severe carcinomatous pain with minimal side reactions, we initiated treatment with piroxicam (60 to 120 mg per day) and doxepin hydrochloride (25 to 225 mg per day). Of 30 patients presenting with severe pain of cancer of various origins, 7 continued to death with piroxicam and doxepin therapy. An additional 17 were successfully treated for 6 to 66 weeks with therapy reported here but, as disease progressed, required supplemental narcotics. The remaining six abandoned the use of piroxicam due to complications of therapy, which ranged from diarrhea to gastric perforation; serious complications were associated with patients' failure to adhere to a prescribed regimen of sucralfate. Therapy with piroxicam and doxepin proved to be safe and efficacious.

Adult↗
PubMedDate not supplied

Microsomal spectral properties and narcotic N-demethylase activity in methadone-dependent rats.

Rats were given access ad lib. to various concentrations (0.3 to 1.0 mg/ml) of methadone hydrochloride dissolved in sucrose solution. The N-demethylation of various narcotics was studied in hepatic preparations from methadone-consuming rats in order to determine if there was substrate specificity for the microsomal demethylase system. The Vmax for the N-demethylation of methadone, ethylmorphine, and meperidine was increased by 40-65%, whereas that for morphine N-demethylation was reduced to 55% of the control value. Additive or synergistic effects on microsomal cytochrome P-450 content were seen when methadone consumption was supplemented by administration of maximally inducing doses of either 3-methylcholanthrene (3-MC) or phenobarbital (PB). This suggested that there was an increase in a type of cytochrome P-450 which was independent of that induced by PB or 3-MC. The qualitative change in cytochrome P-450 reflected in the ethylisocyanide binding spectrum was also apparent after treatment with methadone, PB, or 3-MC, and the combination of methadone and PB exhibited effects that differed from PB alone. Two-substrate kinetic analysis with methadone and morphine as substrates indicated that more than one enzymic system may be involved in the N-demethylation reaction and that a common component of this N-demethylase system could not be induced with phenobarbital. However, methadone and meperidine seem to be demethylated by the same enzymic system.

Animals↗
PubMed1978

Clinical evaluation of naltrexone treatment of opiate-dependent individuals. Report of the National Research Council Committee on Clinical Evaluation of Narcotic Antagonists.

A multiclinic controlled trial of naltrexone in opiate-dependent persons led to these conclusions: (1) a narcotic antagonist is an acceptable treatment for a small number of patients undergoing treatment for opiate dependence; (2) the group most likely to be candidates for such treatment are those who are relatively opiate-free ("post-addicts") and well motivated to seek treatment; (3) although differences between patients treated with placebo and naltrexone were slight, both retention in treatment and opiate-free urine tests favored the naltrexone group; (4) adverse effects of relatively short-term treatment were slight, largely being symptoms and signs of precipitated abstinence in patients with residual dependence.

Adult↗
PubMed1979

[Influence of narcotic analgesics, droperidol, diazepam, and flunitrazepam on the smooth muscles of small arteries (author's transl)].

In isolated segments of the rat tail artery, the influence of narcotic analgesics, their antagonists, droperidol, diazepam, and flunitrazepam on the vascular smooth muscle was investigated. The wall of this vessel consists of about 75 per cent smooth muscle fibres. For all agents studied, pressure-diameter relations were determined before and after a virtually maximum constriction which was induced with noradrenaline. The results were compared with those obtained under control conditions, i.e. prior to the addition of the drugs to the bath solution. Tested in pure Tyrode's solution, none of the agents produced a noticeable constriction or relaxation. Among the analgesics and their antagonists, morphine was the most potent in inhibiting the noradrenaline-induced constriction of the vessel (mean increase in diameter 15%). Pentazocine and levallorphan were less effective (mean increase 8%), and the administration of pethidine and naloxone was followed by even less relaxation, resulting in mean diameter increases of 4%. Piritramide and fentanyl did not show any effect. Depending on the pressure level, droperidol caused the diameter to increase 2 to 10%. Flunitrazepam brought about a marked relaxation (mean increase in diameter 15%), diazepam, however, did not influence the vessel segments. The results obtained show that the haemodynamic effects of the drugs used in this study, in particular those on the peripheral resistance, may, at least partially, be due to their direct influences on the vascular smooth muscle. The real pharmacologic mechanisms by which these effects are initiated, in most cases still remain to be investigated.

Analgesics, Opioid↗
PubMedDate not supplied

[Characteristics of the action of non-narcotic analgesics in diabetics].

Patients with diabetes mellitus were examined for the action of non-narcotic analgesics during oral cavity sanitation. All the drugs under study (amidopyrine, pyranal, baralgin, probon) taken per os increased the threshold of tactile painful sensitivity and the threshold of pain endurance in patients with diabetes mellitus to a greater degree than in normal subjects. No such differences were recorded after diazepam intake under the same conditions.

Adolescent↗
PubMed1985

Effect of narcotic premedication on scintigraphic evaluation of gallbladder perforation.

A case of gallbladder perforation is presented in which a small bile leak was demonstrated by cholescintigraphy while the patient was receiving meperidine, but not after meperidine was discontinued. The scintigrams obtained during meperidine therapy also showed a pattern of bile-duct obstruction. It is suggested that increased biliary pressure secondary to meperidine administration permitted visualization of the leak. Use of narcotic drugs may be a useful pharmacologic intervention in cases of peritonitis due to small or obscure bile leaks.

Adult↗
PubMed1979

Investigation of narcotics and antitussives using drug discrimination techniques.

Rats learned drug discriminations in a shock-escape T-maze task. They were trained to turn right in the maze following injection of a drug (D) and left when no injection (N) was given. Number of training sessions before criterion performance (STC) was used to indicate degree of discriminability of the training drug. STC decreased monotonically as dosage increased, and reached a minimum of 3 to 26 with various agonists. Most agonists were not highly discriminable. Daily maintenance injections of morphine, 200 to 600 mg/kg, increased the STC of morphine, 15 mg/kg, significantly, but complete tolerance to discriminable drug actions was not observed. After rats discriminated D vs. N, they were tested with novel drugs to determine which would elicit D choices. Most morphine-like agonists substituted for one another during substitution tests; the tested agonists included alphaprodine, codeine, fentanyl, heroin, meperidine, methadone, morphine, piminodine and propoxyphene. In a few instances, one of these agonists failed to substitute for another. Naloxone and naltrexone antagonized the discriminable effects of morphine. Cyclazocine, levallorphan, naltrexone, dextromethorphan, ethoheptazine and the narcotic agonists did not substitute for one another, suggesting that six dissimilar discriminable effects were produced by these drugs.

Analgesics, Opioid↗
PubMed1979

The effect of non-narcotic analgesic, tramadol, on cardiac contractility in dog.

The effect of a non-narcotic analgesic, tramadol, 5 mg/kg i.v. on cardiac contractility was studied in intact dog. The maximal intrinsic velocity of contraction of the ventricle, dP/dt/K P at P=O(Vmax) which is a most sensitive and reliable index of cardiac contractility, was decreased significantly 5 and 10 min after the injection, suggesting that the drug is a mild myocardial depressant at this dose and by this route.

Animals↗