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At least 1,009 records · Page 56Linked to original sources
PubMed1981

The effect of histamine and H1 and H2 receptors on prolactin and luteinizing hormone release in humans: sex differences and the role of stress.

The present experiments were performed to investigate the possible role of histamine and its receptors, H1 and H2, in the control of PRL and LH release in normal adult humans of both sexes. Histamine infusion (200 microgram, iv, in 15 min) induced PRL and LH release in men; in women, histamine inhibited LH release without affecting PRL release. Two H1 antagonists, dexchlorpheniramine (10 mg, iv) and promethazine (50 mg, im), reduced PRL release in both sexes, stimulated LH release in men, and inhibited LH release in women. Cimetidine, an H2 antagonist (400 mg, iv), elicited PRL release in both sexes, more consistently in females than in males, and was without effect on LH release in either sex. These data suggest that in humans, the effect of histamine on PRL release is linked to H1 and H2 receptors, which respectively stimulate and inhibit PRL release independently of sex. The effect of histamine on LH release appears to depend on sex and to be mediated only by H1 receptors. To rule out the possibility that the effects of histamine are merely due to a nonspecific stress reaction, we have evaluated PRL and LH release in otherwise normal men and women undergoing surgery for gallstones. Surgery was accompanied by PRL release in both sexes, more evident in women, and by LH release only in men. These results indicate that the effect of histamine on PRL and LH release in humans is linked to sex and H1 and H2 receptors and is not due to stress; further studies are required to clarify the possible mechanism and site of action of histamine in modifying PRL and LH release in humans.

Adult↗
PubMed1998

Controlled trial of ketorolac in tension-type headache.

Intramuscular ketorolac 60 mg, meperidine 50 mg plus promethazine 25 mg, and normal saline were compared in acute exacerbations of tension-type headache. Forty-one subjects (30 females and 11 males) were randomized into three groups and evaluated by the McGill Short-Form Pain Questionnaire before treatment, and 0.5, 1, 2, 3, 4, 5, and 6 hours after treatment. All three groups showed a significant treatment effect that persisted for the 6 hours of evaluation. Ketorolac treatment was significantly better than placebo at 0.5 and 1 hour by the Visual Analog Scale (VAS) and Pain Rating Index, and better than meperidine at 2 hours (by the VAS). Meperidine and placebo did not differ at any time point. Ketorolac is effective in short-term treatment of tension-type headache.

Adolescent↗
PubMed1997

Psychotropic drugs and local anesthetics restore cardiolipin-inhibited mammalian DNA topoisomerase I activity.

The activity of mammalian topoisomerase I is inhibited by acidic phospholipids. We investigated the effect of psychotropic drugs and local anesthetics on cardiolipin-inhibited calf thymus DNA topoisomerase I activity. Chlorpromazine, promethazine, and imipramine, which interact with phospholipids, suppressed the inhibitory effect of cardiolipin. The present results suggest that relaxation of DNA supercoiling is involved in the cytotoxic action of these drugs.

Anesthetics, Local↗
PubMed1991

[Behavioral effects of a new antidepressant, setiptiline].

Behavioral effects of setiptiline, a new tetracyclic compound (1,2,3,4-tetrahydro-2-methyl-9H-dibenzo [3,4:6,7] cyclohepta [1,2-C] pyridine maleate), were investigated to determine its pharmacological characteristics as an antidepressant in rats and mice, as compared with amitriptyline, a tricyclic antidepressant, and promethazine, a neuroleptic possessing an antihistaminic profile. Setiptiline exerted a weak stimulatory action on ambulation, spontaneous motor-activity, observed by the open field method in rats and potentiated the stimulatory effects of methamphetamine. Setiptiline also shortened the duration of immobility in rats forced to swim and inhibited catalepsy induced by haloperidol, yawning by physostigmine, body shaking as well as head twitch by 5-hydroxytryptophan in combination with Ro4-4602 and body shaking by morphine-withdrawal in rats. On the other hand, the drug did not exhibit an antagonistic effect on the hypothermia produced by reserpine in mice. From the results, it is suggested that setiptiline seems to have antidepressive activities that are pharmacologically dissimilar to those of tricyclic antidepressants.

5-Hydroxytryptophan↗
PubMed1996

The role of histamine H1-receptors in the anticonvulsive effect of morphine against maximal electroconvulsive shock in mice.

Morphine is known to release histamine from mast cells. It is also known that histamine receptors mediate some of morphine's effects on the central nervous system. The contribution of H1- and H2-receptors to the effect of morphine on maximal electroconvulsive shock in mice was investigated in the present experiments. Morphine showed a dose-dependent anticonvulsive effect, but produced spontaneous clonic convulsions at higher doses (100 mg/kg, i.p.). The anticonvulsive effect of morphine (1 mg/kg, i.p.) was antagonized by histamine H1-receptor antagonists, dimethindene (0.1 mg/kg, i.p.) promethazine (0.4 mg/kg, i.p.) and pheniramine (30 mg/kg, i.p.), and naloxone (10 mg/kg, i.p.), but not by the H2-receptor antagonist ranitidine (10-50 micrograms, i.c.v.). These results show that morphine has an anticonvulsive effect via histamine H1-receptors against maximal electroconvulsive shock in mice.

Animals↗
PubMed1975

Serious postextraction hemorrhage into the submandibular space: report of case.

A 47-year-old woman had a swelling in the floor of the mouth and in the submandibular area on the left side. About four hours earlier, a dentist had extracted the mandibular left second premolar and first molar. The rate and degree of the distension were alarming; the floor of the mouth was at a level with the incisal edges of the mandibular incisors. Five hours later, the floor of the mouth was elevated about 1 1/2 cm above the incisal edges of the teeth. Treatment of the patient and her unusual sensitivity to meperidine and promethazine that caused a depression into Cheyne-Stokes respiration and hypotension are described.

Blood Pressure↗
PubMed1980

Intramuscular sedation technique.

A sedative technique with meperidine hydrochloride and promethazine hydrochloride via an intramuscular injection is presented. We believe this is an excellent technique because of the safety to the patient and the ease of administration. Like any technique using potentially dangerous medications, practitioners and their staff must be familiar with and prepared for possible complications. When the technique is mastered, it will be a valuable addition for treatment of certain mentally and physically handicapped patients.

Anesthesia, Dental↗
PubMed1986

The local administration of relaxin induces changes in the microcirculation of the rat mesocaecum.

The clinical improvement of Raynaud's disease during pregnancy has been attributed to the increased relaxin (RLX) level in blood. Therefore we investigated the effect of topical porcine RLX (NIH-RXN-Pl) on the microcirculation of the mesocaecum of Wistar male rats, under direct microscope observation as judged by two observers. The hormone was applied locally to avoid systemic interferences either alone or after norepinephrine (NE) and promethazine (PM). The drugs were coded and the results were recorded independently by two observers. Porcine RLX induced rapid dilatation of the veins of the rat mesocaecum in a dose-related manner. The arteriolas and capillary flows were unchanged, while the venular flow was progressively reduced. The observed effects were sustained and disappeared with tissue wash-out. The RLX effects were reversed by addition of NE; conversely high doses of RLX were able to oppose the NE and PM vasospasm. We conclude that the local administration of RLX influences the microcirculation, possibly through an action on the smooth muscle of the venulae. The effects seems antagonistic with those of NE and PM.

Administration, Topical↗
PubMed1989

[Individual differences in PCA response in the guinea pig].

Experiments were carried out to determine the cause of individual differences in the passive cutaneous anaphylaxis (PCA) response in guinea pigs. The intensity of 4-h homologous PCA produced by anti-penicillin G serum was not markedly different among eight reactive sites on the back of a specified animal, whereas considerable individual differences were observed in the PCA response, even at a specified reactive site. PCA was significantly inhibited by an antihistaminic agent, promethazine, and the tissue histamine content was significantly reduced after PCA, suggesting histamine release as a mediator. The intensity of PCA in individual animals was highly correlated with that of the histamine-induced cutaneous reaction elicited at a site adjoining the PCA but was unrelated to skin histamine content. These results suggest that the difference in susceptibility to histamine has a considerable effect on individual differences in the PCA response in guinea pigs.

Animals↗
PubMed1977

Intraarterial analgesia in peripheral arteriography.

A pilot study involving 36 patients was undertaken to test the efficacy of combining 1% lidocaine with 60% methylglucamine iothalamate for relief of the severe burning pain often experienced during peripheral arteriography. Of 24 patients premedicated with meperidine hydrochloride and promethazine hydrochloride, 12 received lidocaine with the contrast medium and 12 did not. The remaining 12 patients were premedicated with diazepam and received lidocaine with the contrast material. By both subjective and objective criteria, those patients receiving lidocaine in the intraarterial injection of contrast medium suffered less pain. Optimum results were achieved for the lidocaine group receiving analgesic premedication. No adverse reactions attributable to the lidocaine were encountered. Subsequent to completion of the pilot study, more than 300 patients have been studied with similar impressive results of pain relief and safety.

Analgesia↗
PubMed1992

Inhibition of human and rabbit liver steroid and xenobiotic UDP-glucuronosyltransferases by tertiary amine drugs--implications for adverse drug reactions.

1. To investigate the hypothesis that disruption of glucuronidation of endogenous compounds by drugs represents a potential mechanism for pathogenesis of adverse drug reactions, the effects of a range of tertiary amine and amide drugs (many with effects on sex hormone function) on steroid hormone and xenobiotic UDP-glucuronosyltransferase activities in human and rabbit liver microsomes were studied in vitro. 2. Chlorpromazine, amitriptyline, imipramine, promethazine and cyproheptadine were consistently the most potent inhibitors of the glucuronidation of testosterone, androsterone, oestriol and 1-naphthol, the steroid activities being more susceptible to inhibition (up to 90%). 3. Carbamazepine, diphenhydramine, sulphadimethoxine, dimenhydrinate and (+/-)-chlorpheniramine had little effect on the UDPGT activities measured. 4. The structural features within this group of compounds required for inhibitory potency were the presence of a rigid tricyclic ring (e.g. phenothiazine) and either a dimethylaminopropyl or a methylpiperidine side-chain. 5. The implications of these data for involvement of disruption of the normal cellular function of glucuronidation in the pathogenesis of frequently observed adverse side-effects associated with these compounds are discussed.

Amines↗
PubMed1988

Comparison of efficacy of ginger with various antimotion sickness drugs.

UNLABELLED: Ginger and several other medications were compared with scopolamine and d-amphetamine for effectiveness in prevention of motion sickness. METHODS: Double-blind techniques were used. The subjects were given the medications two hours before they were rotated in a chair making head movements until a symptom total short of vomiting was reached. Standardized N.A.S.A. techniques were used for speed of rotation and end-point of motion sickness. RESULTS: The three doses of ginger were all at the placebo level of efficacy. Amitriptyline, ethopropazine and trihexyphenidyl increased the tolerated head movements but the increase was not statistically significant. Significant levels of protection were produced by dimenhydrinate, promethazine, scopolamine and d-amphetamine. Protection was further increased by combination of these latter drugs with d-amphetamine. Efficacy was greatest as the dose was increased. CONCLUSIONS: The medication of choice in this study was scopolamine 0.6 mg with d-amphetamine 10 mg. This combination provided good protection with acceptable side effects.

Administration, Oral↗
PubMed1996

Mechanisms of the blood pressure lowering effect of the calyx extract of Hibiscus sabdariffa in rats.

The antihypertensive effect of aqueous extracts of the calyx of Hibiscus sabdariffa (HS) has been investigated in anaesthetized rats. Hibiscus sabdariffa caused a dose-dependent decrease in mean arterial pressure (MAP) of the rats. Sectioning of the right and left vagi nerves did not have a significant effect on the fall in MAP produced by HS. Cholinergic blockade with 0.2 mgkg-1 atropine and histaminergic blockade with 1 mgkg-1 cimetidine and 15 mgkg-1 promethazine significantly attenuated the hypotensive response to HS. Pretreatment of the rats with 20 mgkg-1 HS extract did not have a significant effect on increase in blood pressure induced by bilateral carotid occlusion (48.05 +/- 6.83 mmHg vs 46.53 +/- 7.49 mmHg). The cumulative addition of HS to noradrenaline precontracted aortic rings produced dose-dependent relaxation of the rings. The maximum relaxation response was 86.96 +/- 5.20% and this was observed at the dose of 1.70 mgml-1. These findings suggest that the antihypertensive effect of the extracts of calyx of HS is not mediated through inhibition of the sympathetic nervous system but it could be mediated through acetylcholine-like and histamine-like mechanisms as well as via direct vaso-relaxant effects.

Animals↗
PubMedDate not supplied

In vitro released interferon-gamma in the diagnosis of drug-induced anaphylaxis.

A 17-year-old Japanese male was referred with acute urticaria and anaphylaxis after the administration of PL (salicylamide, acetaminophen, anhydrous caffeine and promethazine methylene disalicylate) and Bufferin (aspirin and dialminate) for headache and a high grade fever. The results of prick test, patch test and drug-induced lymphocyte stimulation test with PL and Bufferin were all negative. The patient's peripheral blood mononuclear cells (PBMC) were cultured with or without PL for 72 hours, and the activity of interferon-gamma (IFN-gamma) in the culture supernatant was measured with EIA. A significantly high level of IFN-gamma was detected in PBMC from the patient, but very little in those from healthy control subjects with a history of exposure to PL. This finding may indicate the presence of drug-specific IFN-gamma producing T cells in patients with an anaphylactic shock reaction to medication. Assays that measure the drug-induced IFN-gamma production may thus be a useful diagnostic tool not only for identifying delayed-type hypersensitivity (DTH) to drugs, but also for predicting anaphylactic shock reaction to drugs.

Acetaminophen↗
PubMedDate not supplied

[An experimental validation of pharmacological agents to arrest the vestibulo-autonomic syndrome (motion sickness)].

The results of development and experimental evaluation of the efficiency of pharmacological means of cupping the vestibulo-vegetative syndrome in man are presented. A model and procedure of evaluation of pharmacological cupping of the Vestibulo-vegetative syndrome are developed. The intramuscular injection of the mixture containing ephedrine, promethazine hydrochloride and strychnine (25, 50, and 1 mg, respectively) appeared most effective.

Coriolis Force↗
PubMed1976

[Current aspects of differentiation and treatment of pneumocystis carinii pneumonia (author's transl)].

There are two types of Pneumocystis carinii pneumonia. One is seen in premature and atrophic infants mainly during the 2nd to 6th month, with massive interstitial proliferation of plasmacells and acute respiratory crisis. The second typ is observed in immunodeficient children and adults with only little or no plasmacell infiltration due to the hypoimmune, hypoergic state. Pentamidine is the drug of choice in the therapy of Pneumocystis carinii pneumonia; in serious cases it will be combined with Pyrimethamine. The cocktail Hydergine + Promethazine proved good as a symptomical drug. There have been reports about recoveries in adults under the treatment with Pyrimethamamine + Sulfamethazole. This combination has been recommended as prophylaxis as well.

Age Factors↗
PubMed1976

Treatment of Pneumocystis carinii pneumonia in infancy.

Pentamidine is recommended for the therapy of Pneumocystis carinii pneumonia either alone or, in severe cases, combined with pyrimethamine. Attention is drawn to the importance of supporting symptomatic treatment, particularly with the promethazine-Hydergine cocktail, and to the possibilities for general and drug prophylaxis.

Dihydroergotoxine↗
PubMed1975

Human assay of antimotion sickness drugs.

The present study was undertaken to improve previous testing procedures, involving the use of a slow rotation room, for assessing the efficacy of antimotion sickness drugs which had validity for groups of subjects but not for each individual in the group. Three major changes were introduced: first, the use of an incremental increase in the intensity of the stressful stimuli of constant intensity; second, a systematic distribution of placebos, rather than a random distribution, in using a modified Latin-square design; third, categorizing the responses as "inconsquential," "beneficial," and "detrimental"--the range of the "placebo responses" was doubled to define the inconsequential range and response above or below were, respectively, beneficial or detrimental. Only drugs known to have antimotion sickness effectiveness were tested and the cardinal findings can be briefly summarized: 1) The group responses were similar to the data previously reported; 2) Great individual differences in response to antimotion sickness drugs were revealed, implying that individual assessments must be made for maximal benefits; 3) The fixed-dose combination of promethazine hydrochloride and ephedrine sulfate (25 mg each) proved to be outstanding as this combination of homergic drugs clearly exhibited a suprasummation effect; and 4) A few tests were conducted using larger than usual doses and the results supported previous findings that, for a maximal beneficial effect in response to a single dose, individuals may vary both with regard to the choice of drug and the amount administered.

Adult↗