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At least 955 records · Page 53Linked to original sources
PubMed1988

Lack of antihistamine properties of single dose cinnarizine in man.

A simple way to study a histamine antagonist in man is to observe the effect it has on the magnitude of the skin reaction to intradermal histamine. The aim of the present study was to evaluate the antihistamine activity of single oral doses of 75 mg cinnarizine using 75 mg diphenhydramine as control, both being compared to placebo. The study was performed with two groups of 5 healthy subjects, each group receiving one of the active treatments or placebo randomly under blind conditions. All subjects received intradermal injections on the forearm of a 0.05 ml saline solution containing 5 micrograms of histamine before and at different times after drug intake. The histamine-induced wheal area was measured and, after drug administration, the percent decrease of the wheal area was calculated. Results showed that diphenhydramine produced a significant inhibition of the histamine-induced wheal size at 1.5 h which lasted up to 4 h after drug administration, reaching maximum inhibition at 2.5 h. After cinnarizine treatment no significant decrease of the histamine-induced wheal area was observed at any time.

Adult↗
PubMedDate not supplied

Protection against fatal endotoxin shock in mice by antihistamines.

Protection against endotoxin shock by antihistamines and similar pharmacologic agents has been reported in the literature. The authors tested the validity of this form of treatment by animal experiments which were conducted in three phases. During the first phase, 10 mice each were treated intravenously with various doses of gram negative endotoxin to determine the dose of endotoxin which would kill 80% of the animals (LD80). This dose was determined to be 36 mg/kg bodyweight. During the second phase, 10 mice each were pretreated with various doses of either diphenhydramine (Benadryl) or of hydroxyzine HCI (Atarax) one hour prior to the administration of the LD80 of endotoxin. It appeared that high doses of diphenhydramine as well as of hydroxyzine were highly fatal to most animals by causing severe convulsions within 3 to 6 hours at doses of 40 or 50 mg/kg. Doses of less than 1 mg/kg appeared to have no protective effect, while doses of 2.5 and of 5 mg/kg, given one hour prior to the LD80 of endotoxin, had some protective value. In the case of diphenhydramine, 60% of the animals survived with 5 mg/kg pretreatment. Hydroxyzine hydrochloride protected 100% of the 10 animals so treated during the initial experiment and 90% during a subsequent experiment, if given 1 hour before the endotoxin. The third phase of this experiment was designed to determine the optimal time at which hydroxyzine needs to be given to protect against fatal endotoxin shock. Given 6 hours before endotoxin, hydroxyzine appeared to protect half of the animals, 1 hour prior to endotoxin, 5 mg/kg of hydroxyzine protected 90% of animals; if given simultaneously, it protected all animals. When hydroxyzine was given 1 hour after endotoxin there was a 70% survival and, if given 3 hours after endotoxin, a 40% survival.

Animals↗
PubMed1988

[The effect of metoclopramide, dexamethasone and antihistamine in the prevention of PAC chemotherapy-induced emesis].

The effect of antiemetic agents on the nausea and emesis of ovarian cancer patients treated with CDDP (45 mg/m2), ADM (45 mg/m2) and CPM (450 mg/m2) combination chemotherapy was examined in a randomized parallel study. Metoclopramide (1 mg/kg, 4 times every 2.5 hours), dexamethasone (3.8 mg, 4 times every 2.5 hours) and antihistamine (10 mg, 2 times every 5 hours) were used as antiemetic agents and these agents were gradually decreased for 5 days. The above regimen significantly suppressed the frequency and volume of vomiting on the day of the first PAC chemotherapy but showed no effect on the delayed persistent nausea during chemotherapy. The frequency and volume of vomiting on the day of chemotherapy were 1.6 times and 102 ml respectively in the antiemetic group, but 8.9 times and 352 ml, respectively, in the control group. Although this antiemetic regimen sufficiently suppressed acute drug-induced emesis during chemotherapy, delayed persistent nausea was not eliminated. We next investigated whether these combined antiemetic agents protected the quality of life of patients during maintenance chemotherapy. Our data indicated that about 2 weeks was necessary to recover health after maintenance PAC chemotherapy. These results indicated that this regimen was effective in suppressing the acute drug-induced emesis and in maintaining the quality of life following maintenance PAC chemotherapy.

Adult↗
PubMed1978

[Central and peripheral interactions of the antiparkinson agent biperiden and the antihistaminic bamipin on the rat excited by pilocarpine].

Excitatory reactions elicited by pilocarpine HCl (50 mg/kg i.v. in 6 s) are used for demonstrating synergistic effects of the central anticholinergic drug biperiden (Akineton) and the antihistamine bamipine (Soventol). Scratching movements of the hind legs are used as parameter for central activity, salivation for peripheral and death for toxic drug effect, respectively. The results show distinct synergistic (central) activity of drug combinations concerning the inhibition of scratching movements. On the contrary, no intensified inhibition is found with the peripheal symptom salivation bamipine rather induces an attenuation of inhibitory effects seen after hig doses of biperiden. Furthermore, the enhanced toxicity of pilocarpine caused by bamipine in a defined dosage range is antagonized by biperiden in a dose related manner. The results of the animal experiments presented are paralleled with clinical experience.

Animals↗
PubMed1979

[Antihistamine and antiserotonin action of 2 aminotetralin derivatives].

The authors performs studies under the conditions of whole organism in vivo and on isolatid organs in vitro and examined antihistamine and antiserotonine activity of two derivatives of 2-aminotetraline, synthesized by D. Dancev and Iv. Ivanov, namely: N-(trans-e-hydroxy-1, 2, 3, 4-tetrahydro-2-naphtyl (-N-) 3-oxo-3-phenylpropyl) piperasine dichloride and N-(trans-3-hydroxy-1, 2, 3, 4-tetrahydro-2-naphtyl (-N-) 3-oxo-3-3phenyl-2-methylpropyl (piperasine dichloride) indicated respectively as P10 and P11. The experiments on isolated ileum of a guinea pig showed that the compound P11 (in concentration of 1.10(-7), 1.10(-6), and 1.10(-5) gm/ml) and P11 (in concentration of 1.10(-6) and 1.10(-5) gm/ml) inhibited the spasomogenic effect of histamine (1.10(-8) and 1.10(-7) gm/ml) as better antihistaminev effect revealed P10. Both compounds inconcentrations of 1.10(-6) and 1.10(-5) gm/ml inhibited the spasmogenic effect of serotonine (1.10(-7) gm/ml), as more significant changes occurred under the influence of the compound P11. The compound P10, administered subcutaneously in a guinea pig in a dose of 0.5 mg/kg of body weight 30 minutes before the occurrence of histamine shock, prevented its development. The same compound inhibited also the development of enterocolitis in mice, induced by serotonine (in a dose of 1 mg/kg of body weight). Both examined compounds inhibited the development of serotonine oedema of the hind paw of a rat as better effect showed the compound P11. The established facts are discussed.

2-Naphthylamine↗
PubMed1970

A second international co-operative investigation into thioacetazone side-effects. 1. The influence of a vitamin and antihistamine supplement.

As part of a large-scale international, co-operative investigation into the side-effects produced by thioacetazone employed in the treatment of tuberculosis, an evaluation has been made of a supplement incorporating vitamins and an antihistamine as a prophylactic.Over a 12-week period of treatment, the additive supplement failed to reduce the over-all frequency of side-effects or the frequency of side-effects leading to a major departure from prescribed treatment. There was also no evidence that the more serious side-effects, particularly rashes, jaundice and agranulocytosis, were reduced by the additives, although the occurrence of vomiting, which was however infrequent, was reduced.In view of this lack of appreciable benefit, as well as the higher cost and impaired keeping properties of tablets containing thioacetazone plus isoniazid when the supplement is added, the use of the supplement as a prophylactic cannot be recommended.

Adolescent↗
PubMed1980

Clinical investigation of terfenadine, a non-sedating antihistamine.

Terfenadine was evaluated for the relief of symptoms in patients with allergic pollinosis on a double-blind basis. Terfenadine 20 mg tid was as effective as Chlorpheniramine maleate 4 mg tid. Chlorpheniramine consistently showed a higher incidence of sedation than placebo. None of the terfenadein dosage schedules up to 200 mg tid caused sedation significantly different from that of placebo. Terfenadine appears to be the first antihistamine to lack significant central nervous system effects.

Benzhydryl Compounds↗
PubMedDate not supplied

[Effect of the antihistamine preparation, fencarol, and other quinuclidyldiarylcarbinols on tissue aminoxidase activity].

In experiments in vivo, the derivatives of quinuclidylarylcarbinol, possessing an antihistaminic activity, fencarol, its di(o-tolyl)- and di(o-methoxyphenyl)-derivatives activate histamine oxidative deamination by diaminoxidase of the rat lungs and increase the histamine tissue level. Quinuclidyl-3-dithienyl carbinol inhibits the activity of diaminoxidase, but decreases the histamine tissue level. On the contrary, dimedrol (diphenhydramine), pipolfen (promethazin), pyrilamine and cyproheptadin exerted no effect on the activity of diaminoxidase or the histamine tissue level. All the compounds studied did not alter oxidative deamination of the rat brain serotonin by monoamine oxidase or the serotonin content in brain tissues.

Animals↗
PubMedDate not supplied

[Effect of the antihistamine preparation, phencarol, on the central nervous system].

The new antihistaminic and antiallergic drug phencarol (quinuclidy-3-diphenylcarbinol hydrochloride) in contradistinction to dimedrol (diphenhydramine) and diprazine (promethazin) exerts no pronounced depressant effect on the central nervous system. It does not significantly influence the period of action of hypnotic drugs, the effects produced by alcohol, spontaneous motor activity, summation capacity of the central nervous system, conditioned reflexes or electroencephalogram. That phencarol possesses no marked central action may be accounted for by its low lipophilic activity and little permeability of the blood brain barrier by this drug.

Animals↗
PubMed1981

[Effect of new antihistaminic preparations on the body's immunologic reactivity].

The effect of new antihistaminic drugs, phencarol and bicarphen, on immunologic reactivity of experimental animals was studied in comparison with diphenhydramine. Phencarol and bicarphen inhibited the delayed type allergic reactions to a greater degree than diphenydramine. Unlike diphenhydramine, phencarol and bicarphen injected simultaneously with test-antigen markedly decreased the number of rosette-forming lymphocytes in the immunocompetent organs (spleen, thymus, lymph nodes). Phencarol, bicarphen and diphenhydramine produced the same inhibitory effect on the content of antibody-producing cells in the spleen of mice.

Animals↗
PubMed1981

The effects of histamine, antihistamines, isoproterenol and theophylline on the Fc and complement receptor functions of polymorphonuclear leukocytes in asthmatic children.

The effects of histamine, antihistamines, isoproterenol and theophylline on the expressions of Fc and complement (C') receptors on the polymorphonuclear leukocytes (PMN's) were studied in 40 asthmatic children. Histamine in concentrations of 10(-13) to 10(-3), isoproterenol in 10(-5) to 10(-3) and theophylline in 5 X 10(-6) to 10(-4) were all capable of causing a dose-related suppression of Fc and C' receptor functions of PMN's. Either diphenhydramine or cimetidine alone could partially block the histamine-induced suppressive effect but combination of H1 and H2 receptor antagonists were required for complete abolishment.

Adolescent↗
PubMed1981

In vivo pharmacology of astemizole, a new type of H1-antihistaminic compound.

Astemizole (R 43 512), a chemically novel compound, has been studied for its in vivo histamine H1-antagonizing properties in laboratory animals. The test models used were: in rats, protection from compound 48/80-induced lethality and inhibition of histamine-induced skin reactions; in guinea-pigs, protection from histamine-induced fatality and bronchoconstriction and in dogs, inhibition of histamine-and Ascaris allergen-provoked skin oedema formation. When compared to standard antihistamines, astemizole showed a higher oral potency and a longer duration of action in all animal models studied. Astemizole's activity was highly specific: it exerted only weak antiserotonin and no anticholinergic actions. Behavioral and drug interaction studies showed that it was devoid of depressant or stimulatory effects on the central nervous system (CNS). Astemizole was very atoxic: safety margins were greater than 25,000 in rats and mice, 30,800 in guinea-pigs and greater than 2000 in dogs. The data of this study indicate that astemizole can be described as a potent, exceptionally long-acting and selective histamine H1-antagonist, free of central and toxic effects.

Animals↗
PubMed1981

The effect of the antihistaminic drugs on the central action of 5-hydroxytryptophan in mice.

Antihistaminic drugs of various chemical structure (chlorcyclizine, chloropyramine, chlorpheniramine, clemastine, diphenhydramine, mepyramine, promethazine, thenalidine) were tested on their action on the central serotonin system in mice. The test used was the antagonism to behavioral syndrome produced by D, L-5-hydroxytryptophan (5-HTP). Clemastine, promethazine and thenalidine inhibited 5-HTP-induced syndrome in doses of much lower than those inhibiting locomotor activity. Similar but weaker effect was produced by chlorcyclizine and diphenhydramine. It could be suggested that these compounds exert central antiserotonergic action. Chloropyramine and, more strongly, chlorpheniramine potentiated the action of 5-HTP; this may be due to the inhibition of serotonin uptake. Only mepyramine in these tests did not show any action on the central serotonin system.

5-Hydroxytryptophan↗
PubMed1982

Relationship between occupation of cerebral H1-receptors and sedative properties of antihistamines. Assessment in the case of terfenadine.

Alpha-[4(1,1-Dimethylethyl)phenyl]-4-(hydroxydiphenylmethyl)-1- piperidinebutanol (terfenadine, RMI 9918, Triludan, Teldane, resp.) inhibits the in vitro binding of [3H]mepyramine to H1-receptors in cerebral membranes with an apparent dissociation constant in good agreement with that found for antagonism of histamine-induced contractions of guinea pig ileum. In contrast, administration of terfenadine in therapeutic dosage does not result in the occupation of cerebral H1-receptors in the living mouse, as observed for most H1-antihistamines. A poor access of the drug to cerebral H1-receptors might account for the absence of sedative side effects.

Animals↗
PubMedDate not supplied

[Effect of the antihistaminic preparation fencarol on cardio- and hemodynamics and the energy processes in the myocardium in an infarct-like immune lesion of the heart].

Experiments were made on anesthesized dogs with closed chest to examine the effect of the Soviet antihistaminic drug phencarol on the cardio- and hemodynamics energy metabolism and microcirculatory bed of the myocardium under focal immune injury to the heart. Preliminary administration of phencarol reduced the shifts in the cardio- and hemodynamics and energy metabolism in the myocardium, characteristic for immune injury. The affected area manifested a less marked rop of the systemic arterial pressure, myocardial contractility, the content of adenyl nucleotides, glycogen and phosphorylase activity. There was a considerable decrease in size of the affected area of the left ventricular myocardium.

Animals↗
PubMed1983

The effects of diethylcarbamazine citrate, antihistamines and corticosteroid derivatives on skin reactivity to Onchocerca supernatants.

A single dose of promethazine or of betamethazone, either alone or compounded with dexchloropheniramine, was found to inhibit skin wheal formation in onchocerciasis patients challenged with Onchocerca supernatants. The mean wheal diameter developing 24 hours after drug administration ranged between 40-60% less than the original pre-treatment diameter but this effect had been abolished or was significantly less by 48 hours. Diethycarbamazinecitrate had only a 20% inhibitory effect on the wheal diameter of the skin reaction. It is concluded that antihistamines and corticosteroid derivates may interfere with the immunodiagnostic skin test for onchocerciasis based on skin reactivity to Onchocerca supernatants, unless measures are taken to ensure that these drugs are not consumed within the 48 hours preceding the skin test.

Adrenal Cortex Hormones↗