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PubMedDate not supplied

[Effects of co-administration of an antidepressant and an anxiolytic drug in the "learned helplessness" paradigm: importance of hydroxyzine].

Whereas benzodiazepines are routinely coadministered with tricyclic antidepressants, in patients undergoing treatment for depressive disorders, little information is known about the combination of benzodiazepines with other antidepressants such as specific serotonin reuptake inhibitors (SSRI's), and combination with other anxiolytic drugs. On the other hand, it is known that benzodiazepines decrease the serotoninergic transmission. The present study was undertaken to evaluate the effect of concomittant administration of anxiolytic drugs such as benzodiazepines (diazepam, lorazepam) or diphenylmethane derivative (hydroxyzine) with specific serotonin reuptake inhibitors, (fluvoxamine, fluoxetine, indalpine) on the ability of antidepressant drugs to reverse helpless behavior in this test. Our results show that: daily injection of diazepam (0.25-2 mg/kg), lorazepam (0.06-0.25 mg/kg) or hydroxyzine (8.32 mg/kg) failed to reverse the behavioral deficit in rat. In contrast fluvoxamine: 4 mg/kg/day; fluoxetine: 4 mg/kg/day; indalpine: 1 mg/kg/day significantly reverse the helpless behavior in this test; the reversal of helpless behavior by fluvoxamine or indalpine was dose-dependently antagonized by daily coadministration of diazepam or lorazepam; in contrast, the reversal of helpless behavior by fluvoxamine or fluoxetine was not modified by daily coadministration of hydroxyzine (8 mg/kg). In conclusion, it may be suggested that combined benzodiazepine-specific serotonin reuptake inhibitors, should be avoided. We suggest that anxiolytic drugs such as hydroxyzine might be better in coadministration with antidepressants, particularly with specific serotonin reuptake inhibitors.

Animals↗
PubMed2005

Effects of fexofenadine and hydroxyzine on brake reaction time during car-driving with cellular phone use.

Antihistamines are a mainstay treatment for allergic rhinitis; however, many older agents cause adverse events, including sedation and central nervous system (CNS) impairment. Research has shown sedating effects of antihistamines on driving; currently, no known study has examined whether cellular phone usage while driving further compounds impairment in individuals administered antihistamines. The aim of this study was to examine this endpoint. In a randomized, double-blind, placebo-controlled, three-way crossover study, healthy volunteers received fexofenadine HCl 120 mg, hydroxyzine HCl 30 mg and placebo. Brake reaction time (BRT) was used to examine driving performance across four conditions: driving only; driving while completing simple calculations; complex calculations; and conversing on a cellular phone. Subjective sedation assessments were also conducted. Brake reaction time with and without cellular phone usage in fexofenadine-treated subjects did not differ significantly from placebo in any condition. In contrast, hydroxyzine-treated subjects were significantly more sedated and had slower BRTs, suggesting slower hazard recognition and brake application, compared with the fexofenadine and placebo groups in all conditions. Importantly, cellular phone operation was an additive factor, increasing BRTs in hydroxyzine-treated volunteers. Fexofenadine did not impair CNS function in subjects involved in a divided attention task of driving and cellular phone operation.

Adult↗
PubMed2005

Observations of the "carry-over effect" following successful termination of chronic migraine in the adolescent with short-term dihydroergotamine, dexamethasone and hydroxyzine: a pilot study.

Chronic migraine management almost always requires daily oral preventative medication with potential adverse effects. Daily oral preventative therapy may also not be effective in terminating chronic migraine. Chronic central sensitisation caused by repetitive migraine attacks in a young person may lower the threshold for future migraine episodes leading to an intractable and debilitating disease course. The objective was to determine if short-term parenteral dihydroergotamine, dexamethasone and hydroxyzine can terminate chronic migraine and be followed by a continuous respite or conversion to a more benign episodic form without the need for daily oral preventative medication ("carry-over effect"). We treated ten patients, seven adolescents and three adults, with parenteral dihydroergotamine, dexamethasone and hydroxyzine given once a week for a maximum of three weeks. No oral preventative daily medication was administered. The setting was a private practice. Chronic migraine was terminated in all 7 adolescents. Their post-treatment course was converted to a more benign episodic migraine course and no adolescent required daily oral migraine preventative therapy for significantly long carry-over post-treatment observational periods. None of the three adult chronic migraine cases could be terminated satisfactorily as they all required daily oral preventative therapy. In the adolescent group only, this strategy terminated chronic migraine and resulted in a significant carry-over effect that appeared to favourably modify the long-term course without the need for daily pharmacological, potentially toxic, preventive therapy. Although this is a very small study, which requires confirmation by a larger controlled study, our data suggest a significant carryover effect in the young migraineur by administering short-term parenteral dihydroergotamine, dexamethasone and hydroxyzine.

Administration, Oral↗
PubMedDate not supplied

A simple high-performance liquid chromatographic method for detection of hydroxyzine in human plasma after overdose.

INTRODUCTION: Hydroxyzine, a piperazine H1-receptor antagonist, is effective in generalised anxiety disorder. For toxicological purposes, a simple reversed-phase high-performance liquid chromatographic assay was developed for the detection of hydroxyzine in human plasma. METHODS: A liquid-liquid procedure was used to extract the drug from plasma in the presence of an internal standard (clothiapine). The analysis was performed on a Spherisorb S5 C(8) analytical column with UV detection. RESULTS: A linear response was observed over the concentration range 20-1500 ng/ml. A good accuracy (bias<7.3%) was achieved for all quality controls, with intraday and interday variation coefficients inferior to 8.5%. The limit of detection was 10 ng/ml, without interference of endogenous components. DISCUSSION: This rapid method (run time<13 min) is currently used for poison management involving hydroxyzine.

Adult↗
PubMed1986

Comparison of the suppressive effect of astemizole, terfenadine, and hydroxyzine on histamine-induced wheals and flares in humans.

Thirty-two healthy volunteers completed a 14-day, double-blind, noncrossover study comparing the efficacy and adverse effects of astemizole, terfenadine, and hydroxyzine. The subjects received either astemizole (load), 30 mg once daily for 1 week and then 10 mg once daily for 1 week, or astemizole (no load), 10 mg once daily for 2 weeks, or terfenadine, 60 mg twice daily for 2 weeks, or hydroxyzine, 50 mg once daily for 2 weeks. Before and on days 7 and 14 of treatment, five intradermal tests with various amounts of histamine phosphate (range 0.3 to 40 micrograms) were performed. Wheal-and-flare responses were traced, and the areas were computed by use of a graphics tablet. All four H1-receptor antagonist treatment regimens were equally effective in reducing the flare response to histamine. Astemizole (load) and hydroxyzine were significantly more effective than terfenadine and astemizole (no load) in reducing wheal size. The incidence of adverse effects, including sedation, was low overall and lowest in the astemizole (no load) and terfenadine groups, although this difference was not statistically significant.

Adult↗
PubMed1979

Suppression of histamine-induced pruritus by hydroxyzine and various neuroleptics.

This study evaluates the ability of hydroxyzine and various neuroleptics to suppress histamine-induced pruritus in ten volunteer subjects with the use of a double-blind crossover protocol. The itch threshold was determined in each volunteer by intradermal injection of gradually increasing concentrations of histamine. Volunteers were then given the study drugs and placebo at the same interval of time, under near identical conditions, and the itch threshold was determined. Thiothixene, hydroxyzine hydrochloride, chlorpromazine, thioridazine, and a lactose placebo were evaluated. Compared to other drugs, hydroxyzine alone was more effective in the suppression of histamine-induced itch. Consequently, hydrozyzine may be more effective in histamine-induced pruritus. The neuroleptic drugs used in this study do not significantly suppress histamine-induced pruritus, but they may be beneficial in nonhistamine-induced pruritus or psychogenic pruritus.

Adult↗
PubMed1992

Ketorolac versus meperidine and hydroxyzine in the treatment of acute migraine headache: a randomized, prospective, double-blind trial.

STUDY OBJECTIVE: To compare the effectiveness of IM ketorolac with that of meperidine and hydroxyzine in the treatment of acute migraine headache. DESIGN: Prospective, randomized, double-blind trial. SETTING: Urban emergency department with an annual census of 42,000 patients. PARTICIPANTS: Forty-seven adult patients with migraines enrolled on 50 visits. INTERVENTIONS: Patients were randomly assigned to receive a single injection of either 60 mg ketorolac (group 1) or 100 mg meperidine and 50 mg hydroxyzine (group 2). Pain assessment was made using both visual-analog and verbal descriptor scales. RESULTS: At 60 minutes, 15 patients (60%) from group 1 (25) and 14 patients (56%) from group 2 (25) reported a great deal of complete relief (P = .77) Sixty-minute mean pain relief scores (3.35 versus 3.37) were different (P = .76). Nine patients (36%) from group 1 and seven patients (28%) from group 2 required additional analgesia (P = .76). CONCLUSION: Ketorolac is as effective as meperidine and hydroxyzine for the treatment of acute migraine headache.

Acute Disease↗
PubMed1977

Comparison of i.v. diazepam and hydroxyzine as surgical premedicants.

Diazepam and hydroxyzine as i.v. surgical premedicants were compared. A double-blind randomized sequence was used employing 7.5 and 15 mg of diazepam v. 75 and 150 mg of hydroxyzine. Each group consisted of 35 patients. Anxiety relief, sedation, lack of recall and patient acceptance were the principal assessments. Diazepam was superior to hydroxyzine in all respects. No serious side-effects were noted with either drug.

Adolescent↗
PubMedDate not supplied

Another fatal case involving hydroxyzine.

Blood and tissue concentrations of hydroxyzine, an antihistamine with sedative properties, were determined in a fatal case of accidental hydroxyzine ingestion. Hydroxyzine was extracted at alkaline pH and analyzed by gas chromatography.

Female↗
PubMed1983

CSF monoamine metabolism in patients with tardive dyskinesia: effect of oxypertine and hydroxyzine pamoate.

Cerebrospinal fluid (CSF) HVA, MHPG, 5-HIAA, cAMP and cGMP concentrations were measured in schizophrenic patients with tardive dyskinesia before and after a three-week administration of oxypertine (n = 4), hydroxyzine pamoate (n = 4) or placebo (n = 4). The oxypertine administration resulted in a reduction of the CSF HVA concentration and an elevation of the MHPG and cAMP concentrations, associated with a clinical improvement in tardive dyskinesia. The hydroxyzine administration reduced the CSF 5-HIAA concentration in all the patients and the CSF HVA concentration in two of four patients with a clinical improvement. A reduction in the CSF HVA concentration associated with possible therapeutic effects of oxypertine or hydroxyzine may suggest the normalization of a hyperdopaminergic state. Discussions were held that functional disorders of not only the dopaminergic system but the norepinephrinergic and serotoninergic systems may relate to the pathogenesis of tardive dyskinesia.

Biogenic Amines↗
PubMed1990

The effects of vadocaine, dextromethorphan, diphenhydramine and hydroxyzine on the ciliary beat frequency in rats in vitro.

Mucociliary function is a major cleansing mechanism of the respiratory tract. Many drugs used in the treatment of respiratory diseases impair the ciliary beat frequency (CBF) of mucous membrane. Our aim was to study by means of a photoelectric technique, the effects of two antitussives--dextromethorphan and vadocaine--and two antihistamines--hydroxyzine and diphenhydramine--on the rat tracheal CBF in vitro. The CBF was measured from tracheal explants immersed in drug solutions. Dextromethorphan (1.0 mg/ml and 10.0 mg/ml) caused 16.9-20.8% decrease in the CBF during the 40 min. measurement period. Vadocaine (0.1 mg/ml and 0.5 mg/ml) decreased the CBF by 6.9%. Higher vadocaine concentrations caused a dose-dependent inhibitory effect so that mucociliary function stopped totally within 20 min. with 5.0 mg/ml vadocaine solution. Both diphenhydramine and hydroxyzine totally stopped the ciliary activity during 20 min. with concentrations of 2.5 mg/ml and 1.0 mg/ml. respectively. Locke-Ringer solution used as a control did not cause any change in the CBF. These results suggest that the antihistamines diphenhydramine and hydroxyzine are more ciliostatic than the antitussives dextromethorphan and vadocaine on the rat tracheal cilia in vitro. The results suggest further in vivo studies. The used photoelectric detection method proved to be suitable for evaluating drug effects on the CBF of respiratory mucosa.

Animals↗
PubMed1994

Prolonged penile erections induced by hydroxyzine: possible mechanism of action.

We describe a subject who developed prolonged penile erections on hydroxyzine. Molecular modelling showed that the hydroxyzine metabolite, norchlorcyclizine, has structural and conformational similarities to the trazodone metabolite, m-chlorophenylpiperazine. This suggests that a common pharmacological mechanism may underlie the ability of trazodone and hydroxyzine to induce erections.

Adult↗
PubMed1994

Treatment of secretory otitis media with local instillation of hydroxyzine.

The study is a preliminary single-blind, placebo- and prednisolone-controlled investigation of the treatment of 156 children with otitis media with effusion (secretory otitis media, SOM), ranging from 2 to 12 years. The protocol involved tympanotomy and placement of a ventilation tube (grommet), through which control or drug solutions were introduced. Other parameters and coexisting symptoms which could contribute to SOM were also examined. Patients were divided into 3 groups as follows: group A: control (normal saline, 2 ml); group B: prednisolone (25 mg in 2 ml); group C: hydroxyzine pamoate (10(-5) M in 2 ml). The results indicate that in those children treated with hydroxyzine, the rate of relapse was significantly reduced and so was the amount of histamine present in middle ear effusions. The effectiveness of hydroxyzine is discussed in the context of the pathophysiology of SOM, especially with respect to mast cells and their activation by allergic and nonallergic means.

Child↗
PubMed1982

The effect of clemastine and hydroxyzine on cutaneous histamine response in man.

Histamine-induced cutaneous wheals were measured in five healthy volunteers 2, 4, 8 and 24 hours after per os administration of a single dose of clemastine 1 mg and hydroxyzine 25 mg. Clemastine produced a mean wheal suppression of 9%, 18% and 6%, while hydroxyzine produced a mean wheal suppression of 49%, 73%, 82% and 77%. This experiment demonstrates the potent and long-lasting anti-H1 effect of hydroxyzine.

Adult↗
PubMedDate not supplied

A comparison of droperidol, diazepam, and hydroxyzine hydrochloride as premedication.

A double-blind comparison of the efficacy and safety of droperidol (5 mg), hydroxyzine HCl (50 mg), diazepam (5 mg), and saline placebo, given concomitantly with meperidine (50 or 75 mg) for preoperative medication, was conducted in 280 female patients scheduled for minor gynecologic procedures. Droperidol proved to significantly superior to the other study drugs in alleviating apprehension (83% of patients calm versus 54, 46, and 34% for hydroxyzine, diazepam, and placebo, respectively). Some drowsiness, occurred in 68 percent of the droperidol-treated patients versus 31, 30, and 21 percent of the other 3 groups, respectively. Global evaluations were consistent with these findings. No clinically significant changes were observed in vital signs in any of the study-drug groups. Adverse reactions were unremarkable in all groups. Significantly less nausea occurred with droperidol than with other treatments, and signficantly less vomiting occurred with droperidol or hydroxyzine. Significantly fewer patients in the droperidol group than in the diazepam group required postoperative antiemetics.

Adolescent↗
PubMed2003

A randomized, controlled, crossover trial of oral midazolam and hydroxyzine for pediatric dental sedation.

The effectiveness of oral midazolam in pediatric dentistry is controversial. This randomized, controlled, crossover, double blind clinical trial was conducted in order to study the effect of midazolam, used either alone or in association with hydroxyzine, during child dental treatment. Thirty seven dental sedation sessions were carried out on 11 ASA I uncooperative children less than five years-old. In each appointment children were randomly assigned to groups: P - placebo, M - midazolam (1.0 mg/kg), or MH - midazolam (0.75 mg/kg) plus hydroxyzine (2.0 mg/kg). Vital signs (blood pressure, breathing rate, pulse and oxygen saturation) and behavior parameters (consciousness, crying, movement, overall behavior) were evaluated every 15 minutes. Friedman and Wilcoxon statistical tests were used to compare groups and different moments in the same group. Normal values of vital signs were usually registered. Heart rate increased in groups P and M as the session went on. Group M presented less crying and movement at the first 15 minutes of treatment. Group MH caused more drowsiness at the beginning of the session. Overall behavior was better in group M than in groups P or MH. Group M produced effective sedation in 77% of the cases, and group MH did so in 30.8%. It was concluded that midazolam was effective and safe, and its association with hydroxyzine did not lead to additional advantages in pediatric dental sedation.

Administration, Oral↗
PubMed2000

[A case of drug allergy to hydroxyzine used for premedication].

A 37-year-old woman, scheduled for total knee replacement, complained of nausea and abdominal pain 30 min after pre-medication with intramuscular atropine and hydroxyzine. Hypoxemia and skin eruption all over her body was noticed in the operating room. Although hemodynamic changes were not observed, the operation was postponed. LST (lymphocyte stimulation test) showed the positive response with hydroxyzine but negative with atropine and antibiotics. This result suggests that hypersensitivity was caused by hydroxyzine in this patient.

Adult↗
PubMedDate not supplied

Changes in airway resistance following droperidol, hydroxyzine, and diazepam in normal volunteers.

The effects of droperidol, hydroxyzine, and diazepam on airway resistance (AR), functional residual capacity (FRC), and thoracic gas volume (TGV) were compared, using a CPI model-2000 body plethysmograph. Significant decreases in AR were seen following droperidol and hydroxyzine at all time intervals. A significant increase in AR also was noted 90 minutes after diazepam injection. FRC significantly decreased at 60, 90, 120, and 150 minutes following droperidol, and at 90 minutes following hydroxyzine, while no change was seen following diazepam. No significant changes in TGV were seen following administration of any of the drugs.

Adult↗