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PubMed1970

Effects of drugs acting alone and in combination on the motor activity of intact mice.

1. When administered to intact white mice, the central depressants-diphenhydramine, promethazine, chlorpromazine, gammahydroxybutyrate, gammabutyrolactone, hyoscine, and pethidine-produced sedation in small doses, but excitement and convulsions in higher doses. When given to mice pretreated with subanaesthetic doses of phenobarbitone these drugs abolished the righting reflex both in convulsant doses (hyoscine excepted) and in non-convulsant doses. These effects are similar to the effects previously observed with local anaesthetics.2. Meprobamate, diazepam and chlorpromazine produced a loss of righting reflex both when given alone and following phenobarbitone. When given alone in higher doses, chlorpromazine induced convulsions.3. The central stimulants bemegride and picrotoxin antagonized the loss of righting reflex produced by phenobarbitone, but nikethamide, caffeine and strychnine did not alter the depressant effects of phenobarbitone.4. On the basis of these and previous studies with intact white mice a tentative classification of drugs having generalized depressant and stimulant effects on the central nervous system was proposed and discussed.

Adjuvants, Anesthesia↗

PubMed1970

Effects of general depressant drugs on the electrical responses of isolated slabs of cat's cerebral cortex.

1. In the neuronally isolated cortex of the cat, local application of diphenhydramine, promethazine, gammahydroxybutyrate, gammabutyrolactone, gamma aminobutyric acid, hyoscine and pethidine, and the intravenous injection of diazepam and meprobamate depressed or abolished the surface negative and surface positive response to direct stimulation and raised the stimulus threshold of the positive burst response. These effects were the same as previously demonstrated for general and local anaesthetics on the same preparation.2. Chlorpromazine produced a similar depression in small concentrations but caused spontaneous activity in higher concentrations.3. In contrast to local application, pethidine when given by intravenous injection in a high dose produced convulsant activity in the isolated cortical slab. The possibility was suggested that the convulsant activity was produced by a metabolite of pethidine.4. The results of this investigation suggest that the central depression produced by a number of structurally unrelated drugs is indicative of an anaesthetic-like property of these drugs.

Action Potentials↗

PubMed1982

Histamine H1-agonist potentiation of adenosine-stimulated cyclic AMP accumulation in slices of guinea-pig cerebral cortex: comparison of response and binding parameters.

1 A range of histamine analogues have been examined as potentiators of the adenosine-stimulated accumulation of cyclic adenosine 3',5'-monophosphate (cyclic AMP) in slices of guinea-pig cerebral cortex. Dose-response curves were constructed for the 6 most active compounds and characterized in terms of the IC50, the slope and the maximum response attainable relative to that of histamine. 2 Histamine, 2-thiazolylethylamine and N alpha-methylhistamine produced a maximal or near maximal response. N alpha, N alpha-dimethylhistamine and 2-methylhistamine appear to be partial agonists. 3 The response to all the agonists was practically abolished by mepyramine 1 microM, indicating that the response is mediated largely or wholly via histamine H1-receptors. 4 The relative potencies of the agonists on cyclic AMP accumulation were in general similar to relative potencies in causing contraction of intestinal smooth muscle. The biggest difference was observed with N alpha-methylhistamine. 5 The histamine analogues were also examined as inhibitors of [3H]-mepyramine binding in homogenates of guinea-pig cerebral cortex. The inhibition curves were characterized in terms of IC50, the slope and the maximum percentage inhibition. This last value was compared with the inhibition produced by promethazine 2 microM. 6 For the 6 most potent agonists, the EC50 for cyclic AMP accumulation was compared with the IC50 against [3H]-mepyramine binding, corrected for inhibition of non-receptor binding and for competition with [3H]-mepyramine. With the possible exception of 2-pyridylethylamine, the values did not differ by more than a factor of 3.

Adenosine↗

PubMed1985

Effects of H1-receptor blocking drugs on the frog sartorius neuromuscular junction.

The effects of H1-receptor blocking agents, pyrilamine, promethazine, and diphenhydramine, on the amplitude and time course of endplate potentials (e.p.ps) were studied in the sartorius muscles of frogs. H1-receptor blockers (10(-5)-10(-4) M) reduced the amplitude of e.p.ps recorded intracellularly without affecting the resting membrane potential. The acetylcholine potential was decreased by perfusion of H1-receptor blockers. However, when the muscle fibre was stimulated directly, threshold and magnitude of action potential were not affected by H1-receptor blockers. The time constant of decay of the e.p.ps recorded extracellularly was reduced by H1-receptor blockers and the decay remained exponential with a single time constant. The quantal content was not reduced by perfusion of H1-receptor blockers at a concentration of 10(-4) M. It is assumed that the major site of action of these H1-receptor blocking agents is at the postsynaptic membrane.

Action Potentials↗

PubMed1989

Divalent cation dependence of the inhibition by phenothiazines of mediator release from mast cells.

1. The divalent cations calcium, strontium and barium--and in that order of decreasing effectiveness--were capable of supporting the stimulated release of histamine from rat peritoneal mast cells (RPMC). 2. The responsiveness of mast cells to stimulation in the presence of divalent cations was, in general, markedly enhanced when the cells were first depleted of their intracellular calcium stores. 3. The putative calmodulin antagonists, chlorpromazine, promethazine, thioridazine (phenothiazines) and W-7 (a naphthalene sulphonamide) all inhibited histamine release in the presence of divalent cations in both untreated cells and in RPMC depleted of their intracellular calcium. 4. Histamine release induced by antigen, compound 48/80 and ionophore A23187 was inhibited by this class of compounds most effectively in the presence of extracellular barium, less so in the presence of strontium and least so in calcium-containing media. 5. In the experimental situation where the extracellular calcium concentration was reduced (less than 1 mM), the phenothiazines inhibited the stimulated release of histamine more effectively. 6. In toto, these results suggest that strontium and barium, as well as calcium, can support histamine release from RPMC by directly interacting with an intracellular divalent cation-binding site that may be calmodulin. As a consequence, one mechanism by which the phenothiazines and W-7 may modulate the secretory response could reflect an antagonism of a divalent cation interaction at that same site, although other additional potential sites of inhibitory action are indicated, dependent on the stimulus employed for secretion.

Animals↗

PubMed1996

Effects of isoflurane on electrophysiological measurements in children with the Wolff-Parkinson-White syndrome.

This study was designed to assess the effects of isoflurane (ISO) on the electrophysiological properties of the accessory pathway, atrium, ventricle, and AV node in children with the Wolff-Parkinson-White (WPW) syndrome. The results of programmed electrical stimulation were analyzed in 51 patients (4 months to 17 years of age) with WPW. The study population was divided into two groups. Twenty-seven patients received local anesthesia and intramuscular injection of meperidine, promethazine, and chlorpromazine (MPC group). Twenty-four patients received general anesthesia with ISO inhalation (ISO group). We compared the antegrade effective refractory period of the accessory pathway (antegrade APERP), ventricular effective refractory period (VERP), atrial effective refractory period (AERP), AH interval, and cycle length of circus movement tachycardia (CMT-CL) in 12 pairs of age and sex matched patients selected from the MPC and ISO groups. Of the 12 pairs of age and sex matched patients, antegrade APERP in patients who received ISO (299 +/- 17 ms, mean +/- SEM) was significantly longer as compared with matched patients in the MPC group (262 +/- 5 ms, P < 0.025). The VERP and AERP in patients from the ISO group were significantly prolonged compared with the MPC patients (239 +/- 7 vs 210 +/- 8 ms, P < 0.025, and 228 +/- 11 vs 180 +/- 6 ms, P < 0.01, respectively). There was no significant difference in the AH interval or CMT-CL between the two subgroups. Thus, ISO prolongs the antegrade APERPs as well as the effective refractory periods of atrial and ventricular muscle in children with WPW, while the AH interval and CMT-CL appear to be unaffected. Care must be taken in interpreting measurements of the antegrade APERP made in patients under general anesthesia for RF ablation of accessory pathways.

Adjuvants, Anesthesia↗

PubMed1984

The Scandinavian multicenter photopatch study. Preliminary results.

The Scandinavian photopatch test procedure has been applied to 745 patients with suspected photodermatoses during the years 1980-1981. Our experience has been encouraging with the recording of several relevant reactions. A total of 132 positive photocontact reactions and 120 ordinary contact reactions were seen. Photocontact reactions to musk ambrette (19 cases) and PABA (19 cases) were surprisingly frequent. The next most common photocontact reactions were to promethazine (24), chlorpromazine (22 cases) and fentichlor (12). Ordinary contact reactions were observed to balsam of Peru (30), PABA (23), lichen mix (21), wood mix (14) and to perfume mix (10).

4-Aminobenzoic Acid↗

PubMed1995

Two cases of mequitazine-induced photosensitivity reactions.

Mequitazine is a phenothiazine derivative antihistamine. We experienced 2 cases of mequitazine-induced photosensitivity reaction in patients who took mequitazine for their dermatologic problems. Case no. 1 showed features of photoallergy such as 1-month incubation period, decreased MED to UVA, strong positive photopatch test result, cross reaction to chlorpromazine, and angry back phenomenon found in allergic contact dermatitis. In addition, an immediate erythematous macule was observed on the photopatch test site of mequitazine directly after UV exposure which was similar to the immediate erythema noted in chlorpromazine photoallergy. During the follow-up period of two months, there was transiently decreased MED to UVB, which became normalized after 1 month treatment with cyclophosphamide. In case no. 2, the pathogenic mechanism seemed to be persistent light reaction preceded by systemic photoallergy, as he had taken mequitazine for 6 months, and there were strong positive photopatch test results with immediate erythema reaction, cross-reaction to promethazine, decreased MED to both UVA and UVB, and persistence of the photosensitivity over a 3-year follow-up period after discontinuation of the mequitazine. Photopatch tests to 1% mequitazine with 5 J/cm2 of UVA in 30 normal subjects were all negative, which means that 1% concentration may be appropriate for the photopatch test. Mequitazine seemed to play a part similar to chlorpromazine, and absence of mequitazine-induced photosensitivity may be due to a relatively low dosage of the drug. However, dermatologists should be cautious about a photosensitivity reaction induced by mequitazine or other phenothiazine-derivative drugs.

Chlorpromazine↗

PubMedDate not supplied

Use of dermal equivalent and skin equivalent models for identifying phototoxic compounds in vitro.

Phototoxicity inducing in vivo photoirritation, a reversible inflammatory reaction of the skin after chemical contact and UVA radiation exposure, is increasingly observed as a side effect associated with the use of both cosmetics and systemic drugs. In order to systematically screen for the phototoxic potential of new compounds, we propose two three-dimensional models suitable for in vitro testing: a dermal equivalent (DE) and a skin equivalent (SE) model. The DE model includes a collagen-glycosaminoglycans-chitosan porous matrix populated by normal human fibroblasts. The SE model is made by seeding normal human keratinocytes onto the DE, leading to a fully differentiated epidermis. The objectives of this pilot study are: 1) to compare the deleterious effects of UVA radiation on the two models and 2) to evaluate to what extent the in vitro results can predict the in vivo phototoxicity caused by well-known photoirritant compounds, included in the COLIPA validation phototoxicity reference chemical list. Dilutions of thiourea, sulisobenzone, promethazine, chlorpromazine and tetracycline were applied (20 microliters) onto DEs and SEs (n = 6) and incubated for 1 h (or 15 h) at 37 degrees C. Irradiated samples received 3 J/cm2 UVA. The 24 h post-irradiation residual cellular viability was measured using the MTT test on treated and untreated tissues and IL-1 alpha release measurement in collected SE culture media. A concordance in terms of photoirritant/non-photoirritant was obtained between the in vivo data and the in vitro results, suggesting that the DE and the SE models could be integrated, after a complete validation study, into a protocol for in vitro testing of the photoirritant potential of new molecules.

Anti-Allergic Agents↗

PubMed1982

Effect of plasma exchange and immunosuppression on Rho(D), viral, and bacterial antibody titers in Rh-immunized women.

Pharmacologic immunosuppression and plasmapheresis have both been advocated as adjunctive methods of treatment for Rh immunization, but a combined regimen of the two has not been attempted. We treated four nonpregnant, severely Rh-sensitized female volunteers with intensive plasma exchange and either promethazine 150 mg or prednisone 60 mg per day in an attempt to remove circulating anti-Rho(D) and prevent further synthesis of the antibody. Each patient received three or four exchanges. The Rho(D) antibody titer decreased by at least one dilution immediately following 11 of 14 plasma exchanges and was ultimately lowered at least two dilutions in all patients. In one case the titer was reduced from 1:512 to 1:16, and a low titer was maintained for the duration of treatment. However, this regimen could increase the risk of infection for a mother and/or infant, as evidenced by the concomitant lowering of viral and bacterial antibody titers in these women.

Antibodies, Bacterial↗

PubMed1987

Leakiness of rat brain microvessels to fluorescent probes following craniotomy.

The effects of craniotomy and/or histamine treatment upon brain microvascular permeability was studied in Wistar rats. Extravasation of circulating Na-fluorescein (MW 376) and of FITC-albumin (MW 69,000) was observed through a cranial window using intravital fluorescence microscopy. Simple exposure of the pial microvessels induced formation of discrete spots of fluorescent material around venules, but not around arterioles or capillaries. The average number of leaky spots to Na-fluorescein and to FITC-albumin was 4.3 and 1.8 per 10 mm2, respectively, 35 min after exposure. Pretreatment of the rats with either indomethacin (a cyclo-oxygenase inhibitor) or promethazine (a histamine H1-receptor blocker) did not reduce the number of leaky sites, whereas pretreatment with a combination of the two drugs had a significant protective effect. Administration of histamine (10(-4) M) to the exposed brain surface for 5 min increased the number of leaky sites to Na-fluorescein and FITC-albumin 3.2 and 3.6 times, respectively. It is concluded that exposure of the brain surface induces release of histamine and cyclo-oxygenase metabolites, and that these inflammatory mediators elicit formation of leaky sites in brain venules.

Animals↗

PubMed1988

Infestation in the dog by the paralysis tick, Ixodes holocyclus. 5. Treatment.

In this study the value of drugs administered with hyperimmune serum in the treatment of advanced disease produced by Ixodes holocyclus was compared under controlled conditions. All control dogs died rapidly whereas one dog survived and 3 dogs died after receiving hyperimmune serum alone. When promethazine hydrochloride was administered with hyperimmune serum 2 dogs recovered rapidly while the remaining 2 died. Administration of dexamethasone and hyperimmune serum allowed 3 dogs to survive while administration of phenoxybenzamine hydrochloride in conjunction with hyperimmune serum allowed rapid recovery of all 4 dogs. Phenoxybenzamine hydrochloride, an alpha-adrenergic blocking drug, was chosen because of its potential to attenuate the arterial hypertension previously reported (Ilkiw et al 1988). The survival of all dogs together with the rapid return to normality indicated that this drug was beneficial in the treatment of dogs with advanced signs of tick paralysis.

Animals↗

PubMed1985

Effects of ovarian hormones on manifestation of purulent endometritis in rat uteruses infected with Escherichia coli.

To assess the influence of hormones on uterine infections, Escherichia coli was infused into uterine lumens of ovariectomized or adrenoovariectomized rats receiving exogenous administration of various doses of ovarian hormones. Large numbers of E. coli were recovered from the rat uterine lumens, irrespective of hormonal influences. The number of leukocytes in the uterine flushings, representing the magnitude of purulent inflammation, differed significantly depending upon the hormonal regimen given to each host. Purulent endometritis was induced by E. coli in ovariectomized rats receiving progesterone or corn oil (hormone vehicle). Infections were asymptomatic in rats receiving estradiol, but promethazine-treated uterine horns were susceptible to infection. When progesterone was administered along with estradiol, purulent inflammation was caused by E. coli, but the number of leukocytes in the uterine lumens was significantly less than that obtained from the rats treated with progesterone or corn oil. These effects of ovarian hormones on uterine infections were observed in adrenoovariectomized rats as well as in ovariectomized rats. It is suggested that estradiol alters the nature of endometrial epithelium and prevent manifestation of purulent endometritis; progesterone antagonizes estradiol. Adrenal hormones appear not to participate in the pathogenesis of endometritis induced by E. coli.

Adrenalectomy↗

PubMed1976

Studies on cyclic AMP in different compartments of cerebrospinal fluid.

Adenosine 3', 5'-monophosphate (cAMP) was measured in the CSF of 42 patients undergoing radiological investigation, neurosurgical procedures, or investigation of hepatic coma. The concentration of cAMP was significantly higher in ventricular CSF than in lumbar CSF. Premedication with pentobarbitone plus promethazine increased cAMP in lumbar CSF. There was no difference in cAMP concentration in lumbar CSF obtained before or after injection of air or after the administration of diazepam during lumbar pneumoencephalography. Lumbar CSF cAMP concentration was significantly increased in patients in hepatic coma. The concentration of cAMP in the lateral ventricle was not affected by general anaesthesia or by the presence of a complete block of the aqueduct of Sylvius. There was no decrease in lumbar CSF cAMP in patients with a complete stenosis of the aqueduct of Sylvius, partial blocks of CSF flow at the cervical level, or a complete block at the lower thoracic level. The concentration of cisternal CSF cAMP was similar to that of lumbar CSF. These results suggest that (1) there is a ventriculolumbar gradient in the concentration of cAMP but of insufficient magnitude to be detected by mixing of lumbar and ventricular CSF during pneumoencephalography, (2) lumbar CSF cAMP concentration is not dependent on brain as a source of this nucleotide; the source of this nucleotide may be largely derived from the spinal cord, (3) premedication may affect the concentration of cAMP in lumbar CSF cAMP, (4) the formation of cAMP is unimpaired in hepatic coma.

Adult↗

PubMed1977

Efficacy of simple sedation of pediatric computed tomography.

A mixture of meperidine, chlorpromazine, and promethazine was used for sedation prior to computed tomography in pediatric patients. Diagnostic-quality scans were obtained in 88% of cases, and there were no important complications. Advantages of routine use of sedation over general anesthesia include random scheduling of adults and children, independence from the other demands placed on the anesthesia service, less need to admit these children to the hospital, and low cost.

Child, Preschool↗

PubMed1982

The choice of sedation for computed tomography in children: a prospective evaluation.

A prospective study of 582 pediatric cranial computed tomographic (CT) examinations was made in order to determine the efficacy and safety of two sedation regimens and general anesthesia. Two hundred seventy-nine outpatients were randomly given oral chloral hydrate (80 mg/kg) or an intramuscular preparation composed of atropine, meperidine, promethazine, and secobarbital (AMPS). Three hundred three inpatients were randomly administered chloral hydrate, the AMPS, or endotracheal anesthesia. Intravenous supplementation of the sedation was limited by the protocol to a maximum secobarbital dosage of 2 mg/kg. An additional retrospective analysis was made of 316 scan attempts obtained outside the study during the same period. A failed CT examination was defined as one that could not be completed or one that showed motion artifacts on two or more scan pairs after two scan pair repeats. The failure rate was 15% for the chloral hydrate group and 12% for the AMPS group. No motion artifacts were present on 94% of the completed studies. There was no mortality, but major and minor complications occurred in 3.5% of the randomized group. It was concluded that each of the methods had proved acceptably safe and effective and that measures can be taken to decrease complications and sedation failures further.

Administration, Oral↗

PubMed1985

Suppression of endotoxin-induced corticosterone secretion in rats by H1-antihistamine.

Corticosterone (CS) secretion is stimulated in rats by an intraperitoneal injection of bacterial lipopolysaccharide (LPS) or by subjecting the animals to immobilization stress. LPS injection caused a significant increase in the lung histamine level and a sharp reduction in the number of intact peritoneal mast cells. Injection of compound 48/80, a histamine liberator, provoked an increase in the histamine levels of the blood and lung and a decrease in the number of intact peritoneal mast cells with a concomitant increase in CS secretion. Administration of histamine, at a dose of 10 mg/kg, induced a marked increase in CS release. LPS-induced CS secretion was attenuated by pretreatment with an H1-antihistamine, promethazine (PMZ), whereas an H2-antihistamine, metiamide, had no effect. In contrast, PMZ was ineffective on CS release provoked by immobilization stress. These results suggest that LPS-induced CS release is mediated, in part, by histamine released in the peripheral tissues, whereas an immobilization stress-induced increase is not mediated by the amine.

Animals↗

PubMed1982

Histamine, cAMP, and activation of piglet gastric mucosa.

The involvement of cAMP as a second messenger for histamine-induced H+ secretion was studied in a physiologically active, in vitro preparation of piglet gastric mucosa. During the first 5--10 min of stimulation with either histamine or the cAMP phosphodiesterase inhibitor 3-isobutyl-1,4-methylxanthine (IBMX), increases (greater than or equal to 5-fold) in tissue cAMP content [(c-AMP]) were well correlated with the characteristic decrease in transepithelial resistance (R); these changes precede H+ secretion by several minutes. Control experiments indicate that, during these treatments, tissue [cAMP] is dominated by the [cAMP] of oxyntic cells alone; change in R and H+ are also related to activity of these cells alone. At the steady state (45 min), histamine and IBMX caused equivalent increases in H+ and decreases in R, but [cAMP] was markedly different in the two cases. With IBMX [cAMP] was elevated at least fivefold, whereas with histamine [cAMP] was less than or equal to 50% above resting levels. The tissue is also stimulated by exogenous additions of dibutyryl cAMP. A histamine-sensitive adenylate cyclase was present in isolated, purified oxyntic cells. The histamine sensitivity of the cyclase was very similar to that which the intact tissue exhibits for histamine-induced changes in H+ and R. The cyclase activity was blocked by cimetidine but not by promethazine. We conclude that during stimulation histamine activates a histamine (H2)-sensitive adenylate cyclase of oxyntic cells, and there is a rapid increase in cellular [cAMP] that is involved in activation of H+ transport and other associated changes of oxyntic cells. An active phosphodiesterase is responsible for reducing [cAMP] to a level much below the "peak" value. Other cellular factors (e.g. protein kinases and Ca2+-calmodulin) must also be involved in the maintenance of the stimulated state of oxyntic cells.

1-Methyl-3-isobutylxanthine↗