[Considerations on the use of betamethasone 17-valerianate in the dermatological field].
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Adolescent↗
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["Betamethasone-17-valerianate" in infantile dermatological practice].
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Betamethasone↗
[Non-steroidal anti-inflammatory agents. VI. Optically active 3-(4-biphenylyl)-3-oxybutyric, valerianic, caproic and isocaproic acids].
The synthesis of the (+/-) 3-(4-biphenylyl)-3-hydroxybutanoic, pentanoic, hexanoic and isohexanoic acids, and their resolution in to enantiomers are described. The latter were submitted to preliminary assay for antiinflammatory activity: interesting results were obtained above all for the isohexanoic acid derivative.
Animals↗
[Topical treatment of various dermatosis with difluocortolone valerianate. (ointment) Double blind comparative study].
The trial preparation, diflucortolone valerate, was tested clinically in the form of fatty ointment on 27 patients: 4 with psoriasis, 4 with neurodermatitis, 4 with contact dermatitis, 2 with actinodermatitis, 10 with eczema, 2 with cutaneous reticulosis and 1 with radiodermitis. In 89% of the cases the results were good; in 11% were they regular.
Adolescent↗
In memory of Prof. Valerian Aleksandrovich Nabokov.
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History, 20th Century↗
[Clinical experiences with the new topical steroid diflucortolone valerianate for skin diseases].
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Administration, Topical↗
Isobolographic analysis of the sedative interaction between six central nervous system depressant drugs and Valeriana edulis hydroalcoholic extract in mice.
It has been declared frequently that valerian may potentiate the effect of other central nervous system (CNS) depressant drugs, however there has been a lack of experimental data. We have evaluated the profile of the interactions between the ethanol extract of Valeriana edulis spp procera and six CNS depressant drugs using an exploratory model to test the sedative effect in mice. All the compounds tested showed a dose-dependent sedative effect with the following ED50 values: valerian 181.62, diazepam 1.21, ethanol 1938, pentobarbital 11.86, buspirone 1.04, haloperidol 0.41 and diphenhydramine 17.06 mg kg-1. An isobolographic analysis was used to evaluate the sedative interaction of the intraperitoneal co-administration of 1:1 fixed-ratio combination of equi-effective doses of valerian extract with each CNS depressant drug. The ED50 theoretical (Zadd) and experimental (Zexp) for each combination were: valerian+diazepam,Zadd=91.41 mg kg-1, Zexp=81.64 mg kg-1; valerian+ethanol, Zadd=1060.22 mg kg-1, Zexp=687.89 mg kg-1; valerian+pentobarbital, Zadd=96.74 mg kg-1, Zexp=151.83 mg kg-1; valerian+buspirone, Zadd=91.33 mg kg-1, Zexp=112.73 mg kg-1; valerian+haloperidol, Zadd=91.01 mg kg-1, Zexp=91.52 mg kg-1; valerian+diphenhydramine, Zadd=99.34 mg kg-1, Zexp=123.52 mg kg-1. Neither synergistic nor attenuate effects were found in any of the combinations evaluated. We concluded that the valerian extract did not potentiate the sedative effect of commonly prescribed CNS depressant drugs as was expected. The additive effect found through the isobolographic analysis suggested that the sedative effect of V. edulis resulted from the activation of common mechanisms of haloperidol, diazepam, buspirone, pentobarbital, diphenhydramine and ethanol.
Animals↗
Neuroprotective properties of Valeriana officinalis extracts.
Valeriana officinalis have been used in traditional medicine for its sedative, hypnotic, and anticonvulsant effects. There are several reports in the literature supporting a GABAergic mechanism of action for valerian. The rationale of the present work is based on the concept that by decreasing neuronal network excitability valerian consumption may contribute to neuroprotection. The aim of our investigation was to evaluate the neuroprotective effects of V. officinalis against the toxicity induced by amyloid beta peptide 25-35 Abeta(25-35). Cultured rat hippocampal neurons were exposed to Abeta(25-35) (25 microM) for 24-48 h, after which morphological and biochemical properties were evaluated. The neuronal injury evoked by Abeta, which includes a decrease in cell reducing capacity and associated neuronal degeneration, was prevented by valerian extract. Analysis of intracellular free calcium (Ca(2+)i) indicated that the neuroprotective mechanisms may involve the inhibition of excess influx of Ca2+ following neuronal injury. Moreover, membrane peroxidation in rat hippocampal synaptosomes was evaluated, and our data indicate that valerian extract partially inhibited ascorbate/iron-induced peroxidation. In conclusion we show evidence that the signalling pathways involving Ca(2+)i and the redox state of the cells may play a central role in the neuroprotective properties of V. officinalis extract against Abeta toxicity. The novelty of the findings of the present work, indicating neuroprotective properties of valerian against Abeta toxicity may, at the long-term, contribute to introduction of a new relevant use of valerian alcoholic extract to prevent neuronal degeneration in aging or neurodegenerative disorders.
Animals↗
Comparative cognitive and psychomotor effects of single doses of Valeriana officianalis and triazolam in healthy volunteers.
OBJECTIVES: To assess the cognitive and psychomotor effects of single oral doses of valerian in healthy volunteers in comparison with a placebo and the hypnotic agent triazolam. METHODS: In a double-blind, placebo-controlled, four-way crossover study nine healthy subjects (5 males, 4 females) received in random order valerian 500 mg, valerian 1000 mg, triazolam 0.25 mg and placebo. Doses were separated by a wash-out period of at least 1 week. Subjects were tested before each dose and at 2, 4 and 8 h after the dose of each compound using the critical flicker fusion (CFF), choice reaction time (CRT), digit symbol substitution test (DSST), symbol search test (SST), digit span test (DST) and visual analogue scales of mood. RESULTS: Repeated measures ANOVA was used to examine the changes in performance on tests over time and significant effects were further analysed using simple main effects analysis with least significant difference corrections. Statistically significant differences were only noted for the cognitive tests: SST (F(3, 8)=3.182, p<0.05) and DSST (F(3, 8)=9.688, p<0.005). In both cases the differences between groups were due to the effects of triazolam. CONCLUSION: These data confirm that at recommended therapeutic doses, triazolam has detrimental effects on cognitive processes in healthy volunteers as found in previous studies. Valerian was without effect on either cognitive or psychomotor performance in healthy volunteers at the doses used in this study. Should the hypnotic activity of valerian be confirmed in randomized double-blind trials it may be a less troublesome alternative to benzodiazepines in the treatment of insomnia.
Adult↗
Neuropharmacological profile of hydroalcohol extract of Valeriana edulis ssp. procera roots in mice.
Valerian is the common name given to the crude drug consisting of the underground organs of the species Valeriana. Valeriana edulis ssp. procera Meyer is the Mexican valerian. The aim of the present work was to elucidate the neuropharmacological profile of a hydroalcohol extract of Valeriana edulis roots at doses of 100, 300 and 1000 mg/kg in several experimental models. A dose-dependent anticonvulsant and anxiolytic-like effect of V. edulis was demonstrated. In addition, the extract decreased rotarod performance and traction force and prolonged the pentobarbital-induced sleeping time at high doses. Concomitant administration of valerian extract and pentobarbital showed a synergistic effect on motor coordination and traction force in mice. The anxiolytic-like effect of V. edulis was compared with diazepam and with diphenhydramine and doxylamine, the latter in order to consider the H(1)-antihistamine effect as another possibility to explain, at least in part, the central nervous system depressant effect of valerian. These results also underlie the medical and industrial use of this species and allowed the conclusion that the extract of V. edulis has central nervous depressant properties similar to, but with some differences to V. of ficinalis, a very well known species.
Animals↗
[Efficacy and tolerability of Baldrian versus oxazepam in non-organic and non-psychiatric insomniacs: a randomised, double-blind, clinical, comparative study].
OBJECTIVE: To show better improvement of sleep quality when treating non-organic insomniacs with extractum Valerianae radix siccum instead of oxazepam. DESIGN: Randomised, double blind, comparative study. SETTING: Out-patients of 8 general practitioners. PATIENTS: Non-organic and non-psychiatric insomniacs aged between 18 and 70 years were included into the trial. Persons with known hypersensitivity to valerian or benzodiazepines, other psychotropic drugs and various contraindications/limitations for benzodiazepines were excluded. INTERVENTION: 75 patients were randomly allocated either to the index group (2 x 300 mg extractum Valerianae radix siccum dragées LI 156) or control group (2 x 5 mg oxazepam dragées). The patients took study medication daily over a period of 28 days 30 min before going to bed. OUTCOMES: The factor sleep quality of the SF-B was defined as primary outcome. Secondary outcomes were other sleep characteristics of the SF-B, well-being (Bf-S) and anxiety (HAMA). Controls were performed before treatment as well as after 1, 2 and 4 weeks. Vital and laboratory parameters as well as unexpected events were assessed for safety and tolerability. STATISTICS: For all outcomes effect sizes between groups were calculated. For the main outcome criteria significance was tested by repeated-measures ANOVA considering all cases for which data of at least one follow-up existed (n = 70). RESULTS: Baseline characteristics were well balanced. 70% (54/75) of the patients were females, over 53% (40/75) reported insomnia for more than 1 year. Mean age was 52 +/- 12 years. In both groups sleep quality improved significantly (p <0.001), but no statistically significant difference could be found between groups (p = 0.70). Effect sizes between groups varied between 0.02 and 0.25. Five persons withdrew due to possibly adverse drug reactions (2 ( valerian, 3 ( oxazepam). No serious adverse events happened. CONCLUSIONS: The study showed no differences in the efficacy for valerian and oxazepam. Because of the more favourable adverse effect profile of valerian compared to oxazepam, this hypothesis should be analysed confirmatorily in an equivalence study.
Adult↗
Effects of Valeriana officinalis extracts on [3H]flunitrazepam binding, synaptosomal [3H]GABA uptake, and hippocampal [3H]GABA release.
Extracts of Valeriana officinalis have been used in folkloric medicine for its sedative, hypnotic, tranquilizer and anticonvulsant effects, and may interact with gamma-aminobutyric acid (GABA) and/or benzodiazepine sites. At low concentrations, valerian extracts enhance [3H]flunitrazepam binding (EC50 4.13 x 10(-10) mg/ml). However, this increased [3H]flunitrazepam binding is replaced by an inhibition at higher concentrations (IC50 of 4.82 x 10(-1) mg/ml). These results are consistent with the presence of at least two different biological activities interacting with [3H]flunitrazepam binding sites. Valerian extracts also potentiate K+ or veratridine-stimulated release of radioactivity from hippocampal slices preloaded with [3H]GABA. Finally, inhibition of synaptosomal [3H]GABA uptake by valerian extracts also displays a biphasic interaction with guvacine. The results confirm that valerian extracts have effects on GABA(A) receptors, but can also interact at other presynaptic components of GABAergic neurons.
Animals↗
The induction of CYP1A2, CYP2D6 and CYP3A4 by six trade herbal products in cultured primary human hepatocytes.
The aim of this study was to evaluate the in vitro inductive potential of six commonly used trade herbal products on CYP1A2, CYP2D6 and CYP3A4 metabolic activities. Herbal components were extracted from the trade products in a way that ensured a composition equal to that present in the original product. Primary human hepatocytes and specific CYP substrates were used. Classic inducers were used as positive controls and herbal extracts were added in in vivo-relevant concentrations. Metabolites were determined by high performance liquid chromatography (HPLC). St. John's wort and common valerian were the strongest inducing herbs. In addition to induction of CYP3A4 by St. John's wort, common valerian and Ginkgo biloba increased the activity of CYP3A4 and 2D6 and CYP1A2 and 2D6, respectively. A general inhibitory potential was observed for horse chestnut, Echinacea purpurea and common sage. St. John's wort inhibited CYP3A4 metabolism at the highest applied concentration. Horse chestnut might be a herb with high inhibition potentials in vivo and should be explored further at lower concentrations. We show for the first time that G. biloba may exert opposite and biphasic effects on CYP1A2 and CYP2D6 metabolism. Induction of CYP1A2 and inhibition of CYP2D6 were found at low concentrations; the opposite was observed at high concentrations. CYP2D6 activity, regarded generally as non-inducible, was increased by exposure to common valerian (linear to dose) and G. biloba (highest concentration). An allosteric activation is suggested. From the data obtained, G. biloba, common valerian and St. John's wort are suggested as candidates for clinically significant CYP interactions in vivo.
Adult↗
Towards the industrial production of medicinal tincture by ultrasound assisted extraction.
Experiments related to the industrial production of medicinal tinctures of sage (Salvia officinalis L.) and valerian (Valeriana officinalis L.) were performed using ultrasonically assisted extraction and quality of the final tincture was evaluated by gas chromatography and dry residue determination. The constituents of the active sage compound: borneol, cineole, alpha- and beta-thujone and also the dry residue were measured. In the case of valerian extractions, the efficiency of sonicated extraction was compared with classical extraction. The course of only the dry residue was monitored. The influence of ultrasound on the quality of valerian tincture was examined by HPLC.
Chromatography, High Pressure Liquid↗
[Medicinal baths for treatment of generalized fibromyalgia].
OBJECTIVE: We studied whether whirl baths with plain water or with water containing pine oil or valerian have a different influence on pain, disturbed sleep or tender point count. METHODS: A randomized, comparative and investigator-blinded study was performed. Out-patients with generalized fibromyalgia were randomized into three treatment groups. INTERVENTIONS: Therapy consisted of either whirl bath with plain water or with the addition of pine oil or valerian. The baths were carried out 10 times, three times a week. MAIN OUTCOME MEASURES: General pain, change of pain intensity during the day, general well-being and occurrence of disturbed sleep were recorded before and after the therapy. The number of tender points was assessed by digital palpation, the pain threshold on the shinbone and the middle part of the deltoid muscle was measured by the dolorimeter of A. Fischer. The same instrument was used for recording pain threshold and pain tolerance of both trapezius muscles. The tissue compliance of these muscles was measured as well. RESULTS: 30 out of 39 patients included in the study were evaluated statistically. After treatment with valerian bath (n = 12) well-being and sleep were significantly improved and also the tender point count decreased significantly. Pine oil added to the bath water (n = 7) resulted in a significant improvement of well-being, but unfortunately also in a significant decrease of pain threshold of the shinbone and the right deltoid muscle. Whirl bath in plain water (n = 11) reduced general and maximum pain intensity significantly. CONCLUSIONS: Our cautious conclusion of this study is - with respect to the small number of treated patients - that different effects of whirl baths with or without medicinal bath oils can be detected in fibromyalgia patients. Plain water baths modify the pain intensity, medicinal baths improve well-being and sleep.
Baths↗
Medicinal plants for insomnia: a review of their pharmacology, efficacy and tolerability.
A number of medicinal plants are traditionally endowed with anxiolytic or sedative properties and, in the context of this revue, both indications are considered since the former may induce a mood conducive to the latter. For any sleep-inducing drug to be effective, a tranquil ambience needs to be established a priori. Thus, physical ailments (i.e. pain), factors interfering with sleep (i.e. noise), psychological conditions causing stress, psychiatric illnesses (i.e. depression) and other drugs that interfere with sleep (i.e. caffeine) need to be controlled, if possible. Kava-kava is a well-established hypnotic drug, with a rapid onset of effect, adequate duration of action and minimal morning after-effects. However, reports of serious hepatotoxicity with this preparation have led to it being banned in most countries worldwide. On the other hand, side-effects with valerian would appear to be bland indeed. However, it's slow onset of effect (2-3 weeks) renders it unsuitable for short-term use (i.e. 'jet-lag'), but it does have profound beneficial effects on sleep architecture (augments deep sleep) that may make it particularly suitable for long-term use and for the elderly. In a personal trial (not double-blind) in stress-induced insomnia, both kava and valerian improved sleep and the ill-effects of stress, and the combination of the two was even more effective for the control of insomnia. Aromatherapy (lavender, chamomile, Ylang-Ylang) would appear to improve sleep, but how practical a form of treatment this may be remains to be determined. The only other plant drug that may have some effect on sleep is melissa, but reports are too scanty to form any opinion about this. Based on animal experiments, passion flower (passiflora) may have a sedative action, but the sedative action of hops has not been investigated in any detail. In conclusion, there is a need for longer-term controlled studies with some of these compounds (particularly valerian). Aromatherapy constitutes a tantalising possibility. In the interpretation of this review, it should be borne in mind that the evidence on which it is based is often incomplete or missing, but that is all that is available. Consequently some conjecture on the part of the author is inevitable and should be appreciated as such.
Animals↗
Beyond benzodiazepines: alternative pharmacologic agents for the treatment of insomnia.
OBJECTIVE: To review the epidemiology, etiology, and classification of insomnia and provide an overview of the pharmacologic therapy of insomnia. Novel nonbenzodiazepine hypnotics including zolpidem, zopiclone, and zaleplon, as well as nonprescription products such as valerian and melatonin, are reviewed in detail. DATA SOURCES: A MEDLINE search was performed to identify relevant clinical studies, case reports, abstracts, and review articles published between April 1992 and December 1997. Key search terms included insomnia, benzodiazepines, zolpidem, zopiclone, zaleplon, Cl 284,846, melatonin, and valerian. Additional references were obtained from the lists of review articles and textbooks. DATA EXTRACTION AND SYNTHESIS: Data concerning the safety and efficacy of the hypnotic agents were extracted from all available clinical trials and abstracts. Background information regarding insomnia, benzodiazepines, and other hypnotics was extracted from the most current literature, including review articles and textbooks. CONCLUSIONS: New developments in benzodiazepine receptor pharmacology have introduced novel nonbenzodiazepine hypnotics that provide comparable efficacy to benzodiazepines. Although they may possess theoretical advantages over benzodiazepines based on their unique pharmacologic profiles, they offer few, if any, significant advantages in terms of adverse effects. Over-the-counter agents such as valerian and melatonin may be useful in alleviating mild, short-term insomnia, but further clinical trials are required to fully evaluate their safety and efficacy.
Acetamides↗
[Phytochemicals as means to induce sleep].
Phytopharmacons are widely used in Germany. Whereas St. John's wort extracts are prescribed for the treatment of mild forms of depression and kava-kava for unspecified anxiety syndromes, hop, balm, lavender, passiflora and valerian are traditionally administered against nervousness and sleep disturbances. Controlled clinical trials are only available for valerian. However, no sleep inducing potential of valerian was observed, only a certain positive effect on daytime mood. Therefore, the mentioned phytopharmacons cannot be recommended for the treatment of sleep disturbances.
Anxiety↗