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PubMedDate not supplied

Systemic reactions with total dose infusion of iron dextran complex in obstetric patients.

Iron dextran complex (Imferon) total dose infusion (TDI) was used to treat iron deficiency anemia in 310 obstetric patients. Systemic reactions were reported for 13.5% of the group. Most (90.5%) of the severe reactions occurred during the test dose, while 66.6% recorded during or after TDI were mild. Antihistamine premedication included administration of promethazine hydrochloride to 104 patients and intramuscular and intravenous drip chlorpheniramine hydrogen maleate to 206 patients. Total systemic reactions were statistically greater with intramuscular promethazine hydrochloride than with intramuscular and intravenous chlorpheniramine maleate (p less than 0.001). On the other hand, the rates of severe reactions and reactions during the test dose were similar for both antihistamine schedules (p greater than 0.05). The incidence of all systemic reactions was the same for pregnant and postnatal women (p greater than 0.05), but severe reactions were more frequent among pregnant than postnatal patients (p less than 0.001). There were no fatalities.

Anemia, Hypochromic↗
PubMed1984

Discriminative stimulus properties of pizotifen maleate (BC105): a putative serotonin antagonist.

Rats were trained to discriminate the putative serotonin (5-HT) antagonist, pizotifen maleate (BC105), from saline using a two-lever drug discrimination paradigm. Pizotifen maleate (6 mg/kg, 14.6 mumol/kg, IP) or saline was administered 55 min prior to the operant training session. The pizotifen discriminative stimulus (DS) had a rapid onset (less than 7 min) and was of long duration. The pizotifen DS was dose dependent. The pizotifen DS did not generalize to the putative 5-HT antagonists, methiothepin, xylamidine, and cinanserin. Partial generalization was observed to methysergide and metergoline, and complete generalization to cyrproheptadine and the phenothiazine antihistamine, promethazine. The pizotifen DS failed to generalize to the antipsychotic chlorpromazine, the ethanolamine antihistamine diphenhydramine, the CNS stimulant, d-amphetamine, and the putative 5-HT agonists, LSD and quipazine. LSD and quipazine failed to antagonize the pizotifen DS. The results of this study suggest that different DS properties are associated with the different putative 5-HT antagonists and that pizotifen and cyproheptadine, in addition to their reported 5-HT antagonist properties, share a common property that is also associated with promethazine, probably involving antihistaminergic activity.

Animals↗
PubMed1981

Antagonism of reserpine rigidity without inducing sedation.

The effects of pretreatment with chlorpromazine, promethazine or SKF 7265 on the severity of reserpine-induced rigidity were evaluated using a series of behavioral responses. Chlorpromazine (10 mg/kg) reduced the severity of the syndrome, particularly the tremor, but only at doses that also produced marked sedation. SKF 7265 was more effective than chlorpromazine and produced no detectable sedation or other motor impairment. Promethazine was ineffective in protecting against the effects of reserpine. These studies demonstrate that motor and behavioral abnormalities induced by high doses of reserpine can be blocked without inducing generalized sedation. This would suggest that it is possible to separate pharmacologically the motor pathways responsible for reserpine rigidity and those responsible for sedation.

Acridines↗
PubMed1982

Stimulant actions of histamine H1 antagonists on operant behavior in the squirrel monkey.

Squirrel monkeys were studied under fixed-interval schedules of reinforcement in which the first response (lever press) after a fixed period time resulted either in the delivery of a food pellet or in the termination of stimuli associated with impending electric shock delivery. Benztropine mesylate (0.03-1.7 mg/kg), promethazine HCl (0.3-10 mg/kg), and diphenhydramine HCl (0.3-17 mg/kg) all produced marked increases in responding at intermediate doses. The increases in responding were at least as great as those observed with psychomotor stimulants, such as amphetamine, in this species under similar behavioral conditions. Benztropine was most potent and diphenhydramine was least potent in most monkeys and, in some, promethazine and diphenhydramine were about equipotent. The order of potency and the magnitude of potency differences among the drugs suggest that the behavioral effects were due to antagonist actions at histamine H1 receptors, rather than to effects on dopamine uptake or on muscarinic receptors.

Animals↗
PubMed1994

Biochemical mechanism of irreversible cell injury caused by free radical-initiated reactions.

Effects of oxidative stress on isolated rat ventricular myocytes were studied. Myocyte viability was determined by the ability of these cells to retain rod-shaped morphology and to exclude trypan blue. The mean life time of myocytes was quantitated using the Weibull distribution function. Superfusion with 200 microM tert-butyl hydroperoxide (t-BHP) led to a time-dependent loss of cell viability, generation of the products of lipid peroxidation, oxidation of protein and non-protein thiols, a decrease in [ATP]i and in the cellular energy charge. Dithiothreitol (DTT, 5 mM) prolonged survival of myocytes exposed to t-BHP, attenuated oxidation of protein and non-protein thiols, and preserved the energy charge. Exposure to DTT did not affect the concentration of t-BHP-generated lipid peroxidation products. Promethazine (1 microM) prevented t-BHP-induced increase in the concentration of lipid peroxidation products, but did not prevent either loss of thiols or loss of cell viability. Superfusion with N-ethylmaleimide (NEM, 5 microM) also led to loss of cell viability, with accompanying decreases in protein and non-protein thiols, ATP and energy charge without the accumulation of the products of lipid peroxidation. Superfusion with FeSO4 (400 microM) and ascorbate (1 mM), (Fe-Asc) did not result in loss of cell viability or a decrease protein thiols or the energy charge. Superfusion with Fe-Asc, did, however, lead to a slight decrease in the concentration of non-protein thiols and ATP and a large increase in the concentration of lipid peroxidation products. Accumulation of lipid peroxidation products induced by Fe-Asc was prevented by promethazine.(ABSTRACT TRUNCATED AT 250 WORDS)

Animals↗
PubMed1979

Effects of several preoperative medications on fat cell lipolysis, and activity of adipose tissue cyclic AMP phosphodiesterase.

Effects were examined of atropine, diazepam, pethidene, promethazine, scopolamine, omnopon and papaverine on basal and noradrenaline-stimulated lipolysis in rat isolated fat cells and on rat adipose tissue cyclic AMP phosphodiesterase activity. Papaverine at high concentration (1 mM) inhibited both basal and hormone-stimulated lipolysis, whereas diazepam enhanced basal lipolysis. At a 'clinical dose', omnopon increased both basal and noradrenaline-stimulated lipolysis. Adipose tissue cAMP phosphodiesterase activity was strongly inhibited by 1 mM diazepam, papaverine, promethazine and omnopon (280 microgram ml-1). Lack of enhancement of lipolysis by the established cAMP phosphodiesterase antagonist papaverine, is compatible with simultaneous inhibition also of adipose adenyl cyclase. Diazepam-stimulated lipolysis is compatible with its phosphodiesterase inhibitory activity. It is proposed that papaverine-containing omnopon may offer some survival advantages during surgical stress by facilitating a caloric supply.

3',5'-Cyclic-AMP Phosphodiesterases↗
PubMed1979

Protection of mice against endotoxin-induced liver damage by anti-inflammatory drugs.

Mice were injected with Corynebacterium parvum, which induces multiple granulomas in liver and renders animals hyper-reactive to the lethal effect of bacterial lipopolysaccharide (LPS). Such animals when challenged with LPS developed also extensive liver parenchymal cell damage as estimated by elevated blood asparate transaminase levels and a hypoglycaemia. Treatment with indomethacin, hydrocortisone, dexamethasone, promethazine, metiazinic acid and (+)-catechin ameliorated the liver damage. Hydrocortisone, dexamethasone, promethazine and metiazinic acid also reduced the mortality rate in mice challenged with LPS. Diarrhoea, accompanying the LPS-induced shock, was prevented by the drugs used. Possible agents mediating the hepatotoxic and shock effects of LPS are discussed.

Animals↗
PubMed1977

Investigations into the cardiac effects of tolazoline in guinea pig atria and ventricular strips.

The positive inotropic, chronotropic and cyclic AMP producing effects of tolazoline were studied on atrial and ventricular preparations obtained from guinea pig heart. (1) The direct positive inotropic effects of tolazoline on the paced left atrial preparation from the guinea pig hearts was blocked by promethazine, but not by burimamide. Tolazoline did not elevate cyclic AMP levels in this preparation. (2) Tolazoline produced a positive chronotropic effect which was blocked by burimamide and not by promethazine and caused a 2-3 fold elevation of cyclic AMP in spontaneously beating right atria. (3) Burimamide antagonized the inotropic and cyclic AMP increasing effects of tolazoline on electrically driven ventricular strips. (4) The effects of tolazoline were unchanged by reserpine pretreatment of the guinea pigs or by prior exposure to phentolamine or propranolol. (5) These results suggest that tolazoline can activate both H1 and H2 receptors in the guinea pig heart. Furthermore the data suggests that H2 receptors are present in right atria and ventricle and that such receptors are associated with cyclic AMP. H1 receptors are present in the left atria and are not associated with the cyclic nucleotide.

Animals↗
PubMed1988

Toxicity of methylating agents in isolated hepatocytes.

To investigate the pathogenesis of hepatotoxicity by methylating agents, we exposed isolated hepatocytes to N-nitrosodimethylamine (NDMA), N-methyl-N'-nitro-N nitrosoguanidine (MNNG), N-methyl-N-nitrosourea (MNU), or methyl methanesulfonate (MMS). Although NDMA is a potent in vivo hepatotoxicant in rats, no evidence of hepatocyte injury, measured by the leakage of lactate dehydrogenase (LDH) activity into the medium, was observed following exposure to a 1-100 mM concentration of either NDMA or MNU. In contrast, exposure of hepatocytes to MMS or MNNG resulted in greater than or equal to 90% LDH release. These differences in toxicity were not related to the extent of covalent binding to hepatocytes. Following MMS or MNNG, but not MNU or NDMA exposure, a significant rise in the generation of thiobarbiturate (TBA)-reactive species was observed. When hepatocytes were exposed to the antioxidant promethazine prior to the addition of MMS or MNNG, the formation of TBA-reactive species was inhibited completely. Although promethazine blocked MNNG-mediated cell injury, the antioxidant had no effect on MMS intoxication. These data suggest that methylating agents can cause hepatotoxicity by more than a single mechanism. For MNNG, lipid peroxidation may be involved in the pathogenesis of acute hepatotoxicity.

Animals↗
PubMed1992

Effect of histamine and antagonists on electrical resistance across the blood-brain barrier in rat brain-surface microvessels.

The effect of histamine on blood-brain barrier permeability was investigated using in situ measurement of transendothelial electrical resistance in brain-surface microvessels of anaesthetized rats. Mean resistance of vessels superfused with artificial cerebrospinal fluid was 1500 omega.cm2, indicating a tight barrier with low ion permeability. The addition of 10(-4) M histamine resulted in a 75% decrease in resistance, in both arterial and venous vessels, indicating a marked increase in barrier permeability. To determine the nature of the response to histamine, rats were given presurgical intraperitoneal injections of promethazine (H1 receptor antagonist), cimetidine (H2 receptor antagonist) or indomethacin (cyclo-oxygenase inhibitor), singularly and in combinations. Cimetidine completely blocked the histamine-mediated increase in barrier permeability whereas promethazine only had a small effect and indomethacin was ineffective. In addition, cimetidine treatment resulted in a 100% increase in basal resistance in both arterial and venous vessels, suggesting endogenous histamine was acting to increase blood-brain barrier permeability. It is concluded that histamine causes an increase in blood-brain barrier permeability which is mediated via endothelial H2 receptors, and that the electrical resistance in cimetidine-treated rats most closely represents the true permeability of the blood-brain barrier.

Animals↗
PubMed1981

The role of lipid peroxidation in CCl4-induced damage to liver microsomal enzymes: comparative studies in vitro using microsomes and isolated liver cells.

The question as to whether CCl4 decreases the activities of glucose-6-phosphatase and cytochrome P-450 in liver endoplasmic reticulum mainly through its action in stimulating lipid peroxidation has been investigated using Promethazine to block lipid peroxidation. The investigation, moreover, has compared the effects of CCl4, with and without Promethazine, on isolated rat hepatocytes with corresponding effects on rat liver microsomal suspensions. Our data give no support for the view that products of lipid peroxidation are the main cause of the decrease in cytochrome P-450 observed in CCl4-intoxication. However, our present results are consistent with lipid peroxidation being a major contributory factor to the decrease in glucose-6-phosphatase activity observed in CCl4-induced liver injury.

Animals↗
PubMed1987

Effects of H1 blocking agents on age-related osteopenia in the mouse.

Old female B6AF1 mice were given acidified tap water, distilled water, one of five H1 blockers or chlorpheniramine (an H1 blocker) and trifluoperazine (a phenothiazine with no H1 blocking activity) in their drinking water for 5 months, and the effects of these agents on bone mineral metabolism were assessed by determining ash weights of femur, ilium and sacrum at the end of the study. In one experiment 24 h whole-body retention (WBR) of Tc 99m methylene diphosphonate (Tc 99m MDP, an indicator of bone metabolism) was measured at the beginning of the study and 40 days later. It was found that: promethazine and dimenhydrinate were the most effective of the H1 blockers in preventing age-related loss of bone mass; distilled water, chlorpheniramine, and chlorpheniramine plus trifluoperazine had no effect on the loss of bone mass; mean bone mass in the groups given meclizine and pyrilamine were greater than but not significantly different from that in the control group given acidified tap water; and only promethazine induced a significant reduction in the WBR of Tc 99m (the other H1 blockers induced small but not significant reductions).

Aging↗
PubMed1985

Sedation and the stimulus properties of antihistamines.

A group of six rats was trained to discriminate the effects of diphenhydramine (10 mg/kg; 30 min pretreatment time) and saline in a two-lever choice task using a fixed ratio schedule of water reinforcement. Stimulus control was assumed to be present when 80% or more of the first ten responses were appropriate for the treatment condition on each of five consecutive days. Diphenhydramine established stimulus control in each of the subjects. The mean number of sessions prior to the onset of criterion performance was 26 (standard error = 7). A second group of six rats was similarly trained with chlorpheniramine (10 mg/kg; 30 min pretreatment time) and saline. Four of the group reached criterion performance in a mean of 56 sessions (SE = 7). The diphenhydramine stimulus generalized completely to promethazine, azatidine, and chlorpheniramine. In rats trained with chlorpheniramine, only promethazine and azatidine substituted completely while diphenhydramine yielded intermediate results, i.e., significantly different from both training conditions. It is concluded that the relative propensity of antihistamines to induce sedation in humans is not correlated with distinctive stimulus properties in the rat.

Animals↗
PubMedDate not supplied

Relative efficacy of the proposed Space Shuttle antimotion sickness medications.

Space motion sickness has been estimated as affecting between 1/3 and 1/2 of all space flight participants. NASA has at the moment proposed a combination of promethazine and ephedrine (P/E) and one of scopolamine and dextroamphetamine (S/D), both given orally, as well as a transdermally applied scopolamine (TAS), as preventive and ameliorative measures. The reported double-blind study, tests the early phase actions and efficacy of the transdermal scopolamine (Transderm (TM)-V of ALZA Corporation) and compares these in detail to the oral medications. Motion sickness resistance was tested by standardized head movements while accelerating at 0.2 degree/sec2 to a maximum rotation of 240 degrees/sec, with an intermediate plateau of 10 min at 180 degrees/sec. To permit weighting motion sickness protection against other system influences, cardiovascular, psychological (subjective and objective), and visual parameter changes were documented for the three therapeutic modes. The relative impact of the various modalities on operational and experimental components of space missions is discussed. A comparison to intramuscularly administered promethazine (a backup therapeutic mode suggested for Space Shuttle use) is also included.

Administration, Cutaneous↗
PubMed1989

Applications in drug analysis of carbon paste electrodes modified by fatty acids.

The oxidation of promethazine as a model compound has been studied by adsorptive stripping voltammetry at carbon paste electrodes (CPE). A modification of the carbon paste matrix with fatty acids allows greater preconcentration of the molecule at the electrode surface. Several fatty acids of different chain length have been tested. The modification of the CPE with lauric acid has been successfully applied in the quantitative analysis of promethazine in standard serum samples. The influence of several parameters affecting the accumulation step has been investigated such as: pH, ionic strength, interfering ions, paste composition. The detection limit in phosphate buffer at pH 9.0 (tacc = 5 min) has been found to be 1 x 10(-10) M.

Carbon↗
PubMed1986

Histamine-induced hyperphosphatemia and hypocalcemia in the laying hen.

The effects of histamine on plasma inorganic phosphorus (Pi) and total calcium values were studied in laying hens during egg formation and in non-laying hens. Histamine induced hyperphosphatemia and slight hypocalcemia during eggshell calcification, whereas the most pronounced hypocalcemia was observed during the early stages of egg formation. The histamine-induced hyperphosphatemia was completely inhibited by cimetidine but only partly by promethazine. However, the histamine-induced hypocalcemia was totally inhibited by cimetidine and promethazine.

Animals↗
PubMed2005

Pharmacological investigation of the nociceptive response and edema induced by venom of the scorpion Tityus serrulatus.

In this study we characterized the nociceptive response and edema induced by the venom of the scorpion Tityus serrulatus in rats and mice and carried out a preliminary pharmacological investigation of the mechanisms involved in these responses. Intraplantar injection of the venom (1 or 10mug) induced edema and a marked ipsilateral nociceptive response, characterized by thermal and mechanical allodynia and paw licking behaviour. The nociceptive response was inhibited by previous intraperitoneal administration of indomethacin (4mg/kg), dipyrone (200mg/kg), cyproheptadine (10mg/kg) or morphine (5 or 10mg/kg), but not by dexamethasone (1 or 4mg/kg) or promethazine (1 or 5mg/kg). The edema was inhibited by previous treatment with promethazine (5 or 10mg/kg) or cyproheptadine (5 or 10mg/kg), but not by indomethacin (2 or 4mg/kg), dexamethasone (1 or 4mg/kg) or cromolyn (40 or 80mg/kg). Some bioactive amines, including histamine and 5-hydroxytryptamine, were found in the venom in low concentrations. In conclusion, the nociceptive response and edema induced by the venom of T. serrulatus may result from the action of multiple mediators including eicosanoids, histamine and 5-hydroxytryptamine. These results may lead to a better understanding of the host response to potent animal toxins and also give insights into a more rational pharmacological approach to alleviate the intense pain associated with the scorpion envenomation.

Analysis of Variance↗
PubMed2006

Antivenom use, premedication and early adverse reactions in the management of snake bites in rural Papua New Guinea.

OBJECTIVE: To examine antivenom use, premedication, early adverse reactions and patient outcomes after snake bite in rural Papua New Guinea. DESIGN: Retrospective chart analysis of all admissions for snake bite with documented antivenom use at 11 rural health facilities from January 1994 to June 2004. No formal protocol was followed and there was no attempt at randomisation or blinding of prophylaxis. RESULTS: Antivenom use was documented in 136/1881 (7.2%) snake bite admissions and most (121/136: 88.9%) received a single vial. CSL Polyvalent antivenom was administered to 112/136 (82.4%). One hundred and eleven patients (81.6%) happened to have been given premedication with adrenaline and/or promethazine and/or hydrocortisone. Early adverse reactions were reported in 25 patients (18.4%) including 23 treated with polyvalent antivenom. Intravenous test doses of antivenom were given to 32 patients, none of whom had a positive test result. Subsequent adverse reactions occurred in 9 of these 32 (28.1%) patients. One death may have been attributable to anaphylaxis after polyvalent antivenom. Reaction rates were significantly (p < or = 0.005) lower in adrenaline premedicated patients (7.7%) compared to patients premedicated without adrenaline (28.3%) and unpremedicated patients (28.0%). Adrenaline premedication caused no detectable changes in vital signs. The case fatality rate was 9.6% (13/136 patients). CONCLUSIONS: Polyvalent antivenom is the main treatment for envenomation in rural health centres, and early adverse reactions are common. Adrenaline premedication appears to significantly reduce acute adverse reaction rates. Premedication with promethazine and/or hydrocortisone without adrenaline did not reduce early adverse reactions.

Adolescent↗