Gene/Protein Disease Symptom Drug Enzyme Compound
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Query: UMLS:C0344307 (analgesia)
 28,200 document(s) hit in 31,850,051 MEDLINE articles (0.00 seconds)

213 caesarean sections and 157 hysterectomies were carried out in gilts and sows with different body weight (table I). The neuroleptic Azaperone and the hypnotic Metomidate were used for anaesthesia with different administration (table II). Local analgesia and premedication with Atropine. The duration of the anaesthesia was 45 minutes and where prolongation was necessary, Metomidate, Azaperone or barbiturates were used alone or in combinations once or more. The indications (table III) for caesarean section were retarded birth in 70 sows, dislocation of uterus in 74 sows and in 69 sows by other indications. Hysterectomy was indicated by retarded birth in 93 sows, dislocations of uterus in 40 cases and in 24 cases by other indications. In 183 operations (table IV) 1006 living piglets were delivered, and 703 were alive at discharge (70%). The chances of survival depends on the composition of the litter, in litters of piglets alive only, 76% survived at discharge; in litters consisting of both alive and stillborn 69% survived and 59% survived in litters consisting of piglets alive and post mortem piglets. The total survival of the sows was 78%, 80% after caesarean section and 76% after hysterectomy. It is pointed out that most of the patients operated were in a very late phase of birth.
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PMID:[Caesarean section in sows anesthetized with Azaperone and Metomidate (author's transl)]. 0 2

Three anaesthetic premedication regimens have been compared by double-blind controlled trial in 158 patients undergoing day-case surgery for varicose veins or hernia. Atropine plus droperidol was superior to atropine plus diazepam or atropine alone in lessening nausea and vomiting and in reducing the need for postoperative analgesia.
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PMID:Double-blind clinical trial of anaesthetic premedication for use in major day surgery. 5 98

In the rat, oxotremorine increases the threshold for vocalisation after-discharge (affective component of pain reactions) dose dependently at subtremor doses (30-67 mug/kg s.c.). Doses of 225-506 mug/kg were needed to elevate the thresholds for vocalisation and motor response. 1-Tryptophan, PCPA, alpha-methyl-p-tyrosine, 1-Dopa, pimozide and LSD-25 did not affect the antinociceptive activity of oxotremorine, while phenocybenzamine slightly increased the threshold for vocalisation. Oxotremorine did not change the endogenous brain concentrations of noradrenaline and dopamine or 5-HT but decreased that of 5-HIAA in all brain regions at the time of maximal analgesia. The decrease of 5-HIAA was still present after pretreatment with probenecid. After inhibition of tyrosine hydroxylase, oxotremorine accelerated the depletion of dopamine in telencephalic cortex during maximal antinociceptive activity and of noradrenaline in all brain regions at a time when this activity had vanished. Atropine significantly antagonized the analgesic activity of oxotremorine. It is concluded that oxotremorine antinociceptive activity in the rat is related to a cholinergic compoent, while a monoaminergic component is not directly involved.
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PMID:Antinociceptive action of oxotremorine and regional turnover of rat brain noradrenaline, dopamine and 5-HT. 23 55

The use of physostigmine electively to reverse the effects of droperidal and diazepam has permitted an optimum level of neuroleptanaesthesia in neurosurgical operations where co-operation of the patient is required during part of the procedure. The patient can be put to sleep or readily awakened to be fully co-operative depending on the needs of the surgeon. In this series of seven anaesthetics there were no side effects from the small doses of physostigmine employed. Bradycardia and salivation were not a problem. One child vomited once. Atropine was not necessary. Since a narcotic antagonist is not needed, a reasonable degree of analgesia can be maintained in these patients while they are awake. The latent time for the effect of physostigmine was two to four minutes and the effect of an intravenous dose lasted from 35 to 45 minutes. With physostigmine, these patients wake up gently as though from normal sleep. If neurological assessment is required post-operatively, drowsiness due to drugs can be reversed by giving more physostigmine and the level of consciousness can then be assessed.
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PMID:Physostigmine as an adjuvent to neuroleptanaesthesia in neurosurgical procedures. 79 61

Sedative effects of medetomidine, a potent selective and specific alpha 2-adrenoceptor agonist, were evaluated in pigs using 5 different doses (30, 50, 80, 100 and 150 micrograms/kg of body weight) and compared with those of xylazine (2 mg/kg). Atropine (25 micrograms/kg) was mixed with both drugs to prevent severe bradycardia. All drugs were administered intramuscularly. Medetomidine at a dosage of 30 micrograms/kg produced more potent sedation than xylazine. The depth of sedation induced by medetomidine was dose dependent within the range from 30 to 80 micrograms/kg. At 100 or 150 micrograms/kg, the depth of sedation was mostly the similar level to that at 80 micrograms/kg but the duration was prolonged. The degree of muscle relaxation produced by medetomidine also seemed to be dose dependent from 30 to 80 micrograms/kg and was stronger than that produced by xylazine. An increase in the duration of muscle relaxation was dose dependent up to 150 micrograms/kg. No analgesic effect was produced by xylazine, however moderate analgesia was obtained by medetomidine. There were no marked changes in heart rate and respiratory rate during the observation period in pigs of any groups, however mild hypothermia after the administration of both drugs was observed. From these results, medetomidine has a significant and dose-dependent sedative effects which are much more potent than that of xylazine, and a combination of 80 micrograms/kg of medetomidine and 25 micrograms/kg of atropine is suitable for sedation with lateral recumbency and moderate muscle relaxation without notable side effects in pigs.
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PMID:Sedative effects of medetomidine in pigs. 139 Nov 73

Alpha 2-adrenergic agonists are often used for sedation and, or, analgesia in dogs, but they are often associated with bradycardia and in some animals with atrioventricular heart block. In this study, atropine or glycopyrrolate either helped to maintain the heart rates or were effective in increasing reduced heart rates of dogs treated with medetomidine. In the process, however, cardiac dysrhythmias often developed. These dysrhythmias were predominantly associated with the combined responses to the medetomidine and the anticholinergic agent because there were no significant changes in respiratory function. A reduced blood oxygen content or increased blood carbon dioxide can contribute to cardiac irritability. Atropine and glycopyrrolate were more effective in preventing bradycardia and had less undesirable side effects when they were given before the administration of medetomidine.
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PMID:Effects of anticholinergic treatment on the cardiac and respiratory systems in dogs sedated with medetomidine. 168 74

1. The effect of atropine on the nociceptive system was examined in mice and rats by use of the hot-plate, writhing and tail-flick tests. 2. Atropine dose-dependently produced analgesia, no effect and hyperalgesia. Analgesia was observed in both species with doses ranging from 1 to 100 micrograms kg-1 while hyperalgesia was obtained with 5 mg kg-1. 3. Atropine antinociception was prevented by pirenzepine (0.1 microgram per mouse, i.c.v.), dicyclomine (10 mg kg-1, i.p.), atropine-methylbromide (0.5 microgram per mouse, i.c.v.) and hemicholinium-3 (1 microgram per mouse, i.c.v.). Naloxone (1 mg kg-1, i.p.), alpha-methyl-p-tyrosine (100 mg kg-1, s.c.) and reserpine (2 mg kg-1, i.p.) were ineffective. 4. The site of atropine analgesia is in the CNS since it exerts its antinociceptive effect also when injected i.c.v. (1-10 ng per mouse). Moreover drugs which do not cross the blood-brain barrier, such as hemicholinium-3, pirenzepine and atropine methylbromide, were unable to antagonize atropine analgesia if administered i.p. 5. Atropine also in vitro, showed a biphasic action on electrically-evoked guinea-pig ileum contractions. Concentrations between 10(-14) and 10(-12) M increased electrically and nicotine-evoked contractions but did not affect acetylcholine- and oxotremorine-evoked contractions. Concentrations above 10(-9) M inhibited both electrically- and drug (acetylcholine, nicotine and oxotremorine)-evoked contractions while they were ineffective on unstimulated ileum. 6. On the basis of the above findings, amplification of cholinergic transmission by very low doses of atropine is postulated, through a selective blockade of presynaptic muscarinic autoreceptors, as the likely mechanism of action. 7. Atropine antinociception, unlike oxotremorine antinociception, was obtained without any impairment of mouse rota-rod performance. 8. The antagonism by pirenzepine and dicyclomine of oxotremorine and atropine antinociception suggests that M1 muscarinic receptor subtypes are responsible for cholinergic analgesia.
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PMID:Investigation into atropine-induced antinociception. 228 66

The enantiomers of the oxotremorine analog N-[4-(2-chloromethylpyrrolidine)-2-butynyl]-2-pyrrolidone (BM 130) were synthesized. The LD50 values of (+)- and (-)-BM 130 in mice (i.v.) were 10.4 +/- 1.4 and 13.5 +/- 1.9 mumol/kg, respectively. Atropine and N-methylatropine poorly protected against the lethal effects, suggesting that they were nonmuscarinic in nature. When administered i.v. to mice, (+)- and (-)-BM 130 were equipotent in producing peripheral and central muscarinic effects. ED50 values were 1.3 to 1.4, 2.8 to 3.2 and 0.20 to 0.26 mumol/kg, respectively, for salivation, tremor and analgesia (tail-flick assay). After i.p. injection, tremor was not observed and analgesic potency was reduced more than 10-fold compared to the i.v. route. The aziridinium ions [(+)- and (-)-BM 130A], formed by spontaneous cyclization of (+)- and (-)-BM 130, were virtually equipotent in eliciting contractions of the isolated guinea pig ileum and in causing salivation in mice. Their LD50 values in mice (i.v.) were 1.1 +/- 0.2 and 2.1 +/- 0.3 mumol/kg, respectively. The enantiomers of BM 130A had similar affinity for muscarinic receptors in the rat cerebral cortex as measured by competitive inhibition of (-)-[3H]N-methylscopolamine binding at 0 degrees C. The rate constants for alkylation of muscarinic receptors, obtained at 37 degrees C by measuring the decline in (-)-[3H]-3-quinuclidinyl benzilate binding to cortical homogenates that had been treated with various concentrations of (+)- and (-)-BM 130A for 20, 45 or 90 min, differed significantly for the two enantiomers.(ABSTRACT TRUNCATED AT 250 WORDS)
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PMID:Muscarinic actions and receptor binding of the enantiomers of BM 130, an alkylating analog of oxotremorine. 270 31

The pharmacological effects of N-[4-(2-bromoethylmethylamino)-2-butynyl]-2-pyrrolidone (BR 401) were compared in the mouse with those of N-[4-(2-chloroethylmethylamino)-2-butynl]-2-pyrrolidone (BM 123) and oxotremorine. BR 401 was more toxic than oxotremorine and BM 123 when administered i.v. (LD50, 0.7 mumol kg-1), but less toxic than oxotremorine when given i.p. (LD50, 39 mumol kg-1). Atropine and methylatropine (10 mumol kg-1 i.p.) increased the LD50 value of BR 401, given i.v., 75- to 100-fold. Upon i.v. administration, BR 401 was 2- to 3-fold more potent than oxotremorine and 10 to 20 times more potent than BM 123 in producing central (tremor and analgesia) and peripheral (salivation) muscarinic effects. However, after i.p. administration BR 401 was 3-fold less potent than oxotremorine in eliciting tremor and analgesia. The aziridinium ion (BR 401A), formed by cyclization of BR 401, produced salivation but no tremor. These observations suggest that BR 401 when given i.v. penetrates effectively into the central nervous system where it cyclizes rapidly to the pharmacologically active aziridinium ion. In contrast, after i.p. administration a large proportion of BR 401 will cyclize before it can reach the central nervous system. BM 123, because of its slower cyclization, enters the central nervous system effectively also by the i.p. route. Thus, central potency of 2-haloethylamines such as BR 401 and BM 123 is critically dependent not only on the rate of cyclization, but also on the route of administration. The duration of tremor induced by BR 401 and BM 123 was considerably shorter than that induced by oxotremorine.(ABSTRACT TRUNCATED AT 250 WORDS)
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PMID:Muscarinic actions of an N-methyl-N-2-bromoethylamino analog of oxotremorine (BR 401) in the mouse. 380 1

The analgesic activity of alphamethyldopa (MD) was studied in mice using the acetic acid writhing test and the hot plate method. In the writhing test, MD produced a dose-dependent analgesic effect with an ED 50 of 26.5 mg/kg. The results of the hot plate test confirmed the analgesic activity of MD. Yohimbine, but not naloxone, antagonized the analgesic effect of MD in the writhing test. Atropine antagonized MD analgesia while physostigmine potentiated it. The study suggests that MD analgesia is of the nonopioid type involving both adrenergic and cholinergic systems.
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PMID:Alphamethyldopa analgesia: its possible mechanism of action. 406 30


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