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PubMedDate not supplied

[Anesthesia in magnetic resonance tomography].

Sixty patients were anesthesized for MRI. Intravenous and/or intramuscular anesthesia with ketamine, diazepam, pipolphen (promethazine) was supplemented by aminazine (chlorpromazine) or tisercin for adult patients. Spontaneous respiration was maintained, which helped avoid problems with endotracheal intubation and assisted ventilation. The method is safe, economic, and its side effects are negligible. Main features of MRI and specific anesthesiological problems associated with this method are discussed.

Adjuvants, Anesthesia↗
PubMedDate not supplied

A study of three preoperative sedative combinations.

The use of drugs as premedication for child patients to be treated in the office may provide the dentist with an adequate means of controlling the patient otherwise incapable of cooperation. Drug dosages for children cannot be determined alone on the basis of weight and age, especially when dental treatment is to be provided. Alphaprodine and promethazine; chloral hydrate and hydroxyzine pamoate; pentobarbital, meperidine, and scopolamine are three groups of balanced medication that fulfill the needs in pedodontic office procedures. The Pedi-Wrap is an important factor in treatment and control of movements unknowingly exhibited by the patient from one to six years of age. Its use should be required for the very young child patient, to prevent falls and bodily injury and to allow the doctor to execute his treatment effectively.

Adolescent↗
PubMed1975

Carbon tetrachloride induced polysome breakdown. Relative importance of lipid peroxidation and of binding to ribosomal components in the process.

In vivo, CC1-4 causes an intense polysome breakdown; CHC1-3 effect is much less intense and CH2C1-2 effect is negligible. Previous administration of either diphenyl-p-phenyelnediamine or alpha-tocopherol to the rats does not prevent CC1-4-induced polysome breakdown. Promethazine and cystamine were able to prevent to a good extent the CC1-4 induced polysome breakdown process. 14CC1-4 irreversibly binds to ribosomal proteins but not to ribosomal RNA. Several hepatocarcinogens which are effective alkylating agents and cause in vivo polysome breakdown do not induce a lipid peroxidation process.

Animals↗
PubMedDate not supplied

Prolonged inhibition of presynaptic catecholamine synthesis with alpha-methyl-para-tyrosine attenuates the circadian rhythm of human TSH secretion.

OBJECTIVE: Originating from the pituitary gland, TSH secretion is regulated predominantly by thyroid-releasing hormone (TRH) neurons located in the hypothalamus. Norepinephrine and dopamine have important effects in modulation of TSH secretion. An inhibitor of catecholamine synthesis, alpha-methyl-para-tyrosine (AMPT) has been used in several studies of the regulation of human TSH secretion. The short-term effects (<8 hours) of low doses of AMPT include stimulation of pituitary TSH secretion by selective lowering of brain dopamine levels. After prolonged administration of AMPT (>24 hours), theoretically both dopamine and norepinephrine levels are lowered significantly in the brain, although this has not been reported previously. METHODS: Nine subjects (five women and four men) received a total of five 1-g doses of AMPT or five 50-mg doses of promethazine (active placebo) over 28 hours in a randomized, double-blind, placebo-controlled crossover design in which the active and control tests were separated by 4-6 weeks. Blood samples were obtained over 24 hours (18 time points) on day 2 of each condition. RESULTS: Changes in prolactin secretion and 6-hydroxymelatonin sulfate excretion indirectly showed the effects of AMPT on dopamine and norepinephrine. The typical circadian rhythm of TSH secretion was blunted by AMPT throughout the night; at ten time points, the difference between the two groups was statistically significant (P <.01). The long-term effects of repeated doses of AMPT were inhibition of TSH secretion and significant attenuation of the circadian rhythm of TSH. Additionally, AMPT induced low norepinephrine levels, which counteracted the stimulatory effect of low dopamine levels on TSH. CONCLUSION: Through its inhibitory effect on TRH, norepinephrine appeared to be involved in the regulation of TSH.

Adult↗
PubMed1975

Reduction of carbon tetrachloride toxicity by prior administration of a single small dose in mice and rats.

Mice were given progressively smaller doses of carbon tetrachloride (CCl4) and at intervals later the LD50 of a second dose was determined. The LD50 was greater than in previously untreated mice as soon as 10 min after the first dose, increased to a maximum between 12 and 24 h that was maintained for about 3 or 4 days, after which the LD50 returned to normal by the 7th day. The maximum LD50 reached was dependent on the first dose, but even a minute first dose, 0-004 ml/kg, had a significant effect. The same phenomenon was confirmed in rats. Administration of promethazine before doseing with CCl4 did not have this effect, nor did an ether anaesthetic.

Animals↗
PubMedDate not supplied

Mechanism of action of tricyclic drugs on Escherichia coli and Yersinia enterocolitica plasmid maintenance and replication.

Tricyclic medical compounds like many other non-antibiotics exhibit antimicrobial activities. Two chemically representative groups were tested in plasmid DNA transformation and replication to assign intracellular target sites responsible for the multiple effects in Escherichia coli and Yersinia enterocolitica cells. To analyse the mechanism of action at the molecular level, the effects of chlorpromazine, 7,8 dioxochlorpromazine, promethazine, methylene blue, imipramine, cannabidiolic acid and tetrahydrocannabidiolic acid were examined at several points in the course of transformation, in plasmid replication and on the topological state of plasmid DNA. Two possible target sites were identified, one of them involving membrane binding sites which participate in plasmid DNA replication. Drug binding at these sites interfered with the replicating plasmid DNA and membrane protein complex, preventing the proper processing of the replication that resulted in plasmid loss. The other in vivo and in vitro effect was observed on the topological state of plasmid DNA. Tricyclic drugs intefered with energy dependent gyrase activity and promoted the relaxation of plasmid DNA, causing disturbances in gene expression and in plasmid replication. The results give insight into the chemical structures connected with significant specific antimicrobial effects.

Antidepressive Agents, Tricyclic↗
PubMed1992

Specific immunotherapy stimulates the binding of histamine H2 receptor antagonist by lymphocytes.

The binding of antagonists of histamine receptors H1 (promethazine) and H2 (ranitidine) by peripheral blood lymphocytes from pollinotics was determined before and after the course of immunotherapy. We found that lymphocytes from atopic subjects showed significant decrease in the binding of H2 receptor antagonist as compared to control subjects. Specific immunotherapy induced statistically significant increase in H2 receptor antagonist binding, which correlated with the improvement of clinical symptoms.

Adolescent↗
PubMedDate not supplied

Evaluation of morphine as compared to meperidine when administered to the moderately anxious pediatric dental patient.

This investigation evaluated two narcotic regimens used to sedate pediatric dental patients who previously demonstrated uncooperative behavior. One consisted of submucosal morphine (0.15 mg/kg), and the other, oral meperidine (2.2 mg/kg); both were administered in combination with oral promethazine (1.1 mg/kg). Patients 2-7 years old were sedated with one of the two regimens and videotaped during dental treatment. If sedation was successful, the child received the other regimen at the next appointment, resulting in a total of 42 sedations in 29 children. Later, patient behavior was rated blindly by two independent observers viewing tapes of specific events during dental treatment. Fourteen of 23 (61%) patients receiving morphine and 11 of 19 (58%) patients receiving meperidine were sedated successfully. Vital signs, including pulse, respirations, blood pressure, and oxygen saturation were monitored and remained stable for both groups. ANOVA for repeated measures showed no significant differences for any vital sign in either group across time. Wilcoxon's signed rank test revealed significant improvement for the patients successfully treated in both groups when presedation behavior was compared with behavior during the events of rubber dam application, operative, restorative treatment, and exit (meperidine, P < 0.005 and morphine, P < 0.001). Improvement also was seen in the meperidine group for the event of local anesthesia (P < 0.01). Chi-square analysis showed no statistically significant differences in effectiveness or safety between the two sedative regimens.

Administration, Buccal↗
PubMed1992

Use of sedation analgesia for pediatric dentistry.

26 healthy children between the ages of 36 and 60 months (mean 35 months) who satisfied the selection criteria during a screening visit participated in this double blind study. The subjects were assigned randomly to receive either 75 mg/kg Triclofos elixir (Regimen I-21 children) or 50 mg/1kg Trichlofos elixir combined with 1 mg/kg promethazine elixir (Regimen II-22 children). All medications were given orally 45 minutes before treatment. During operative procedures all subjects received nitrous oxide/oxygen at a concentration of 35%. All the patients were restrained in a papoose board (Indigenous). The subjects were monitored for vital signs and evaluated for sedation and sleep, movement, crying and overall behaviour before, during and after the operative procedure. Regimen II was found to be superior to Regimen I with regard to behaviour management of difficult young children. However extremely apprehensive children were not good subjects for this sedation technique.

Anesthesia, Dental↗
PubMed1992

[Histamine release during induction of combination anesthesia using nalbuphine or fentanyl. Modulation of the reaction by premedication with promethazine/pethidine].

In a controlled clinical trial in patients admitted for general surgery (mainly abdominal and thyroid), histamine release following nalbuphine 1 mg/kg i.v. versus fentanyl 5 micrograms/kg i.v. was studied in the course of an otherwise routine induction with promethazine/pethidine as premedication 30 min before the opioids and alcuronium-flunitrazepam-thiopental 5 min later. Succinylcholine was given before intubation and further analgesia was obtained by repeated administration of either nalbuphine or fentanyl. Plasma histamine levels were measured by a specific fluorometric assay, heart rate and blood pressure were measured for assessing hemodynamics, and clinical signs of anaphylactoid reactions such as skin eruptions and arrhythmias were registered. RESULTS. Nalbuphine and fentanyl both released histamine with an incidence of more than 40%. In addition, nalbuphine potentiated the histamine release evoked by the sequential administration of alcuronium-flunitrazepam-thiopental in one complex of application. The incidence of histamine release in the nalbuphine group was 6/13 = 46%, in the fentanyl group only 1/11 = 9% (chi2 test, P less than 0.05). Furthermore, this study showed high histamine levels after succinylcholine and intubation in a relation to time of administration that suggested histamine release as a stress response to intubation. Finally, the incidence of histamine release after a second injection of the opioids was still 30%. A direct correlation between plasma histamine levels, hemodynamic changes, and skin reactions could not be shown. A detailed causality analysis with histamine release as a contributory determinant showed histamine release less detrimental to hemodynamic stability than the opposite, which had been expected. However, the promethazine administered 30 min before induction of anaesthesia had strong H1- and H2-receptor antagonistic activity and was given with optimum timing for H1- and H2-prophylaxis. CONCLUSION. The study demonstrated that histamine release during anaesthesia and surgery depends strongly on the time sequence of drugs and measures used. Histamine release is not predictable from studies in human volunteers alone; studies in patients have to be added. Histamine release is not always detrimental. H3-receptor-mediated effects after H1- and H2-prophylaxis may help patients to counteract the effects of a series of vasoactive drugs given during induction of anaesthesia.

Adult↗
PubMed1992

[Propofol for sedation during postoperative mechanical ventilation. A comparative study with Lytic Mixture].

Propofol infusion was found to provide excellent sedation and rapid recovery in intensive care. The present study compared Propofol with lytic solution (lytic solution = mixture of 100 mg Pethidine, 50 mg Promethazine and 0.6 mg Dihydroergotamine) during 6 hours of postoperative artificial ventilation. 60 patients after major abdominal surgical procedures were studied with ethical committee approval and informed consent. Patients were randomly allocated to receive either Propofol or lytic solution. We aimed at a sedation level of stage 5 according to the Ramsey score. The mean drug dosages were 3.9 mg/kg/h of Propofol and 4.2 ml/h of lytic solution. Hemodynamic values, blood gases as well as various biochemical measures did not show any difference between the groups. At the end of the sedation period triglyceride concentrations were significantly higher in patients receiving Propofol (166 + 79 mg/dl) compared to the control group (97 + 60 mg/dl). Significant and relevant differences were found for the times of recovery after discontinuation of the sedative. These times were very short in the Propofol group. Furthermore, in view of a longer recovery time after lytic solution in this group the respiratory rate was significantly slower up to the end of the observation period. We conclude that a major advantage of Propofol in the present study was the rapid recovery after 6 hour sedation. Patients gain vigilance rapidly and sufficient spontaneous respiration within minutes. Not at least thanks to these facts patient's safety can be improved in the recovery period.

Abdomen↗
PubMedDate not supplied

Inhibition of tumor induction in tobacco by Agrobacterium tumefaciens and nodulation induced by Rhizobium meliloti in the presence of phenothiazines and structurally related compounds.

Plasmids of Agrobacterium tumefaciens and Rhizobium meliloti carrying Kanamycin resistance genes were eliminated from 1.4 to 0.2% of the growing bacterial cultures by promethazine and imipramine. As a result of plasmid elimination, the A. tumefaciens plasmidless isolate was not able to induce crown gall tumor on tobacco plants. The plasmidless R. meliloti strain failed to induce nodule formation on alfalfa plants. The efficiency of nodulation was decreased when the bacteria were grown in the presence of the drugs. The antiplasmid effects of the drugs were not prevented by opines, (nopaline and octopine) in Escherichia coli F'lac cells.

Agrobacterium tumefaciens↗
PubMed1992

[A case of neuroleptic malignant syndrome with acute renal failure].

Neuroleptic malignant syndrome is a potentially lethal side effect of neuroleptic drugs, characterized by fever, muscle rigidity, autonomic dysfunction, and altered consciousness. A 50-year-old female hospitalized three times in the past for psychiatric treatment was admitted to Umayabashi Hospital for treatment of a relapse of a schizophrenic psychosis. She had received 50 mg of chlorpromazine and one tablet of Vegetamin-A (chlorpromazine 25 mg, promethazine 12.5 mg, phenobarbital 40 mg). Approximately 24-36 hours later, the patient became febrile and lost consciousness, and eight days later, acute renal failure occurred with muscle rigidity. She was transported to Maebashi Red Cross Hospital to receive hemodialysis. On admission, the laboratory studies showed high levels of serum creatine phosphokinase, glutamic oxaloacetic transaminase, glutamic pyruvic transaminase, creatinine and blood urea nitrogen. She underwent hemodialysis for treatment of acute renal failure and recovered from it after 16 sessions of hemodialysis.

Acute Kidney Injury↗
PubMed2004

Influence of histamine and H1-receptor antagonists on ejaculated human spermatozoa: role of intrasperm Ca2+.

Histamine reduced sperm viability in a dose- and time-dependent manner, accompanied by rise in intrasperm Ca2+. Further, 2',4'-dichlorobenzamil hydrochloride (DBZ), a Na+-Ca2+ exchange inhibitor, known to elevate intrasperm Ca2+, potentiated both, elevation of intrasperm Ca2+ and spermicidal action of histamine. Pretreatment of sperm with very low doses of H1-receptor antagonists (chlorpheniramine, promethazine or diphenhydramine) prevented the histamine-induced elevation of intrasperm Ca2+ as well as its spermicidal action. However, pretreatment with famotidine, a H2-receptor antagonist did not produce such a protective action. The results strongly suggest that histamine elicits its spermicidal action via H1-receptors present on sperm cells.

Calcium↗
PubMedDate not supplied

[Phencarol--an antihistaminic preparation from the quinuclidylcarbinol group].

A high antihistaminic activity of quinuclidyl-3-diphenylcarbinol (phencarol) has been ascertained. In pharmacological experiments phencarol is superior to dimedrol (diphenhydramine), both as concerns its antihistaminic activity and the duration of its action. Unlike dimedrol and diprazine (promethazine) it has no inhibitory effect on the central nervous system. With its clinical use phencarol is effective in treating urticaria, Quincke's edema and allergic skin reactions. The drug is well tolerated by the patients and does not produce any inhibitory or soporific action. Phencarol has an authorized permission to be used for medical purposes.

Administration, Oral↗
PubMed1992

[Anxiolysis vs. intravenous conscious sedation during maxillary fracture splinting in local anesthesia].

For the conservative treatment of mandibular fractures with arch bars under local anaesthesia we used two forms of premedication in 140 patients: 1. an analgetic sedation with pethidine 1 mg/kg body weight and promethazine 0.5 mg/kg body weight i.m. (n = 70 cases) 2. an anxiolytic sedation with midazolam 0.05-0.1 mg/kg body weight i.v. (n = 70 cases). The effect of the premedication was measured retrospectively by the mean amount of local anaesthetics used during splinting. It could be noted that the mean consumption of local anaesthetics was significantly lower in the midazolam-group than in the pethidine/promethazine-group. The postoperative subjective assessment of the operation by the patients is better under anxiolytic than under analgetic sedation, too.

Adolescent↗
PubMedDate not supplied

Synergistic interaction between proton pump inhibitors and resistance modifiers: promoting effects of antibiotics and plasmid curing.

A proton pump-deleted mutant E. coli, AG100 A, had greater sensitivity to ampicillin, tetracycline and erythromycin than the wild-type parent E. coli AG100 containing the proton pump. This antibiotic sensitivity was further increased by resistance modifiers such as the Ca2+ channel blocker (+/-) verapamil (VP) and the calmodulin antagonist promethazine (PMZ). Whereas the newly-synthesized trifluoromethyl-ketone (TF) enhanced the activity of these antibiotics against the wild-type strain, it did not enhance the activity of ampicillin against the proton pump-deleted mutant. These results suggested that TF14 had an inhibitory effect on the proton pump. Elimination of plasmids from another strain of E. coli, K12, was promoted by PMZ and 9-amino-acridine (9-AA), but not by TF14 alone. However, combinations of TF14 with either PMZ or 9-AA enhanced the plasmid elimination capacity of the latter compounds. The combination of TF14, PMZ and VP proved that the Ca2+ channel blocker was not effective by itself These results collectively suggest that TF14 inhibited the proton pump of E. coli and that it was this pump which, when inhibited by TF14, allowed more PMZ to reach its plasmid elimination target.

Aminacrine↗
PubMed1976

The effect of histamine, isoproterenol and tyramine on rat uterine cyclic AMP.

Isoproterenol (10(-4) M), histamine (10(-3) M) and tyramine (10(-3) M) elevated cyclic AMP levels in incubated rat urerine segments. Promethazine (10(-6) M) an H1-receptor antagonist was ineffective in blocking the increase in cyclic AMP due to isoproterenol, histamine and tyramine. Buriamide (10(-6) M), an H2 receptor antagonist, was effective in almost abolishing the cyclic AMP elevation due to histamine, whereas burimamide did not affect the cyclic AMP levels elevated by tyramine and only slightly reduced the isoproterenol response. Propranolol was effective in reducing or abolishing the cyclic AMP accumulation by all three agonists. The respective blockade by burimamide or propranolol was overcome by increasing the concentration of the agonists. Histamine (10(-3) M) and tyramine (10(-3) M) failed to elevate cyclic AMP in uterine segments obtained from reserpine treated rats. The data supports the hypothesis that histamine, like tyramine, has an indirect effect on the rat uterus mediated through the release of endogenous norepinephrine.

Animals↗