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A combination of instrumental chromatographic methods high pressure liquid chromatography in the isocratic mode and reverse phase thin-layer chromatography with densitometric ending on Russian Sorbton-RP-2 plates--is conducive to a fuller and more reliable identification of narcotic analgesics in biological fluids (blood and urine).
Morphine sulfate and methadone hydrochloride exhibit very different half-lives but are described as having an analgesic potency of one. The use of a drug like methadone may provide prolonged and constant analgesia in the perioperative setting. This double-blinded investigation used methadone and morphine intraoperatively and measured pain scores and narcotic requirements in the first 24 hours postoperatively. Thirty American Society of Anesthesiology (ASA) patients, physical status I through III, between the ages of 18 to 65 years were scheduled for orthopedic surgery and randomly assigned to receive morphine or methadone at 0.30 mg/kg. Fifteen patients received morphine and fifteen patients received methadone. There was no significant difference between the two groups in terms of age, height, weight, and ASA status. No statistically significant difference was observed among the two groups between the amount of analgesic requirements postoperatively or in the visual analogue scale pain score.
Prosidol, a new Russian narcotic analgesic, was used in various dosage forms (buccal and oral tablets, injection solution) in 113 cancer patients for the treatment of chronic pain, as a component of total anesthesia, and for postoperative analgesia. The best results were attained with the universal noninvasive dosage form, buccal tablets, used for the treatment of chronic pain in incurable patients. Analgesic properties of buccal prosidol are close to those of tramadol, the drug is well tolerated by the patients and causes no grave side effects. As a drug for postoperative analgesia prosidol was highly effective in patients after extracavitary oncologic surgery and less effective after thoracal and abdominal interventions. As a component of total anesthesia prosidol is inferior to fentanyl and approximately similar to promedol. An advantage of prosidol is its highly effective universal noninvasive dosage form, buccal tablets, which may be used for rapid analgesia in any situation.
Methamphetamine (MAP) administered in doses of 0.5 to 5 mg/kg i.p. to rats anesthetized with pentobarbital produced a shortening of the duration of loss of righting reflex. This analeptic effect of MAP was blocked by atropine but not by atropine methylbromide, indicating the central cholinergic nature of the response. This effect was also blocked by the D1 and D2 dopamine antagonists SCH 23390 (0.2 mg/kg) and raclopride (2 mg/kg), respectively. Pentobarbital decreased sodium-dependent high-affinity choline uptake (HACU) in frontal cortex and hippocampus as measured in synaptosomes from treated rats. MAP given to pentobarbital-narcotized rats restored HACU activity to nonanesthetized levels, but this restorative effect of MAP was blocked by SCH 23390 or raclopride. These data suggest that in addition to a cholinergic mechanism, the analeptic effect of MAP involves the dopamine system. alpha-Methyl-p-tyrosine, but not reserpine, pretreatment completely blocked the MAP analeptic response. In reserpinzed rats, MAP produced a markedly enhanced analeptic response. Studies of the effects of repeated administration of MAP on its analeptic activity were also undertaken in view of the well known sensitization to the locomotor and stereotypic effects of the amphetamines that occur with repeated intermittent administration. Rats pretreated daily with MAP (5 mg/kg) for 5 or 12 days showed neither tolerance nor sensitization to the analeptic effect of subsequent MAP administrations. 3H-quinuclidinyl benzilate-binding studies also showed no changes in muscarinic binding characteristics of membranes prepared from cortex or hippocampus of rats pretreated chronically with MAP. These and our earlier studies suggest that the analeptic effect of MAP is mediated via a dopaminergic-cholinergic mechanism.
Contractions caused by Slow Reacting Substance C(SRS-C) and by Arachidonic Acid hydroperoxide (AAP) in the guinea-pig ileum and by AAP in the rat fundus were studied in the presence of suprofen and of 3 reference compounds. The dose-related inhibitions were not due to antagonism of prostaglandins. Other agonists of gastrointestinal smooth muscle were not or only weakly antagonized. For the study of selective inhibition of AAP-induced contractions by non-narcotic analgesics, the rat fundus is the preferred preparation. In this model suprofen had an ED50 of 1.27 x 10(-7) M (0.033 mug/ml), being 1.5, 94 and 2, 020 times more potent than indomethacin, phenybutazone and acetylsalicylic acid, respectively. Suprofen also strongly inhibited malondialdehyde formation by guinea-pig platelets incubated with arachidonic acid. The reported effects point to inhibition by suprofen of prostaglandin biosynthesis. The antagonism of AAP-induced contractions in the rat fundus is a valuable test system for inhibitors of prostaglandin biosynthesis.
The use of drugs in the treatment of patients with renal failure requires a knowledge of excretion, biotransformation and pharmacologic activity of metabolites. Narcotics, analgesics, psychotherapeutic agents, drugs affecting the heart and ciruclation, various sorbents, resins and gels, anabolic hormones and nutritional supplements are among the more frequently used drugs for patients with end-stage renal disease. Indications and dosages of these drugs must be modified for patients with renal failure, and mechanisms of their biotransformation must be studied. This combined seminar presents the participants' studies and analyses of the problems surrounding the use of these various pharmacologic agents.
Moguisteine (R,S(+/-)-2-(2-methoxyphenoxy)-methyl-3-ethoxycarbonylacetyl-1,3-t hiazolidine, CAS 119637-67-1), a new peripheral non-narcotic antitussive drug, is a racemate composed of an equimolar mixture of R(+) and S(-) enantiomers (BBR 2221 and BBR 2222, respectively). Since in some cases the use of only one enantiomer instead of a racemate may increase the efficacy and/or the tolerability of a compound, moguisteine enantiomers were submitted to toxicological evaluation. Given in a single oral (gavage) or intraperitoneal administration to mice and rats, both moguisteine enantiomers show very low general toxicity. Administered by gavage to rats and dogs for four consecutive weeks, BBR 221 and BBR 2222 are tolerated at up to the dose of 240 mg/kg/day in both sexes with no appreciable toxic changes. Finally, the mutagenicity tests show that both enantiomers are devoid of any mutagenic potential both in vitro and in vivo. Considering the overall results of the toxicological studies and comparing them with the data obtained from the previously performed studies with the racemate moguisteine, it can be affirmed that no differences can be identified between the two enantiomers and the racemate moguisteine. These findings justify the development of moguisteine as a racemate since neither enantiomer should offer any advantage over the racemate.
In mice implanted with a morphine pellet for 3 days and subsequently withdrawn for various periods of time, a single injection of morphine results in a rapid and marked sensitization of abstinent mice to naloxone-induced jumping behavior when compared to abstinent mice pretreated with saline or to placebo-withdrawn mice given a single morphine injection. Maximum sensitization of abstinent mice occurs at morphine doses of about 10 to 30 mg/kg and peaks at 0.5 to 2 hours after morphine administration. The ability of morphine to sensitize abstinent mice to naloxone declines with time after pellet removal and appears to consist of two components, one with a short T1/2 and one with a much longer T1/2. Abstinent mice are also sensitized to naloxone by levorphanol and methadone, but not by dextrorphan. It is proposed that the administration of a narcotic drug to abstinent mice uncovers a latent, pre-existing state of physical dependence and restores the responsiveness of this state to naloxone.
Five different strains of mice were investigated for their suitability to serve as models for the study of long-term effects of propoxyphene napsylate (PN) on narcotic-dependent mice. The NIH/Swiss outbred strain proved to be most suitable because of its high liability to manifest physical dependence on morphine. Following removal of subcutaneously-implanted morphine pellets from the mice, the incidence of spontaneous withdrawal jumping was used as a quantifiable criterion of physical dependence. An orally administered suspension of PN suppressed the withdrawal jumping in a dose-dependent manner. However, chronic (daily) administration of PN at doses high enough to prevent withdrawal jumping was characterized by a high degree of toxicity.
Adsorption of four 5-pyrazolone derivatives and two carboxylic acids from aqueous solutions was studied. Partition coefficients for the analyzed drugs were calculated. Good corelation between log(k1, k2) (Langmuir constants) and log (octanol-water partition coefficient) of the drugs were found. The higher log(k1k2) value the higher solubility of the non-narcotic and analgetic drugs.
During acute asphyxia in pentobarbital-narcotized cats, the elevation in plasma potassium level was parallel to that of PCO2. From the time when PO2 reached its minimum, the elevation in serum potassium was higher than that of plasma potassium. The increase of the difference between serum and plasma potassium values seems therefore to be more related to hypoxia than hypercapnia; it could be due to membrane alteration of blood cells.
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