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  • 1
    Electronic Resource
    Electronic Resource
    Nail incorporation kinetics of terbinafine in onychomycosis patients (1995)
    Oxford, UK : Blackwell Publishing Ltd
    Clinical and experimental dermatology 20 (1995), S. 0 
    Details
    ISSN: 1365-2230
    Source: Blackwell Publishing Journal Backfiles 1879-2005
    Topics: Medicine
    Notes: Patients with toe-nail onychomycosis were treated with terbinafine (250 mg daily, n= 20) for either 6 or 12 weeks in a randomized double-blind study. Plasma and distal nail clippings were taken before initiation of therapy and 1, 6, 12, 18, 24, 36 and 48 weeks thereafter.Analytical data of terbinafine extracted from nail clippings or plasma were obtained by high-performance liquid chromatography (HPLC). Nail extracts and isolated HPLC terbinafine peaks were analysed using a combined gas chromatography - mass spectroscopy system (GC-MS) for unequivocal identification of the drug.Terbinafine could be detected in the distal nail in the majority of the patients within 1 week of starling therapy. Maximum terbinafine levels of 0·52 and 1·01 μg;g were measured after 18 weeks in the 6- and 12-week treatment groups, respectively.While plasma levels decreased rapidly after termination of therapy terbinaiine was detected in the nails as long as 36 weeks (6 weeks treatment) and 36 weeks (12 weeks treatment) after termination of therapy at a range of 0·–0·19 μg/g. The drug concentrations measured at all time points are well above the minimum inhibitory concentration (MIC) tor dermatophytes and other fungi, These data suggest that the drug readies the nail plate rapidly and persists there for several months after cessation of active treatment.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1111/j.1365-2230.1995.tb01353.x
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  • 2
    Electronic Resource
    Electronic Resource
    Calcium-stimulated catecholamine release from .alpha.-toxin-permeabilized PC12 cells: biochemical evidence for exocytosis and its modulation by protein kinase C and G proteins (1987)
    s.l. : American Chemical Society
    Biochemistry 26 (1987), S. 7842-7848 
    Details
    ISSN: 1520-4995
    Source: ACS Legacy Archives
    Topics: Biology , Chemistry and Pharmacology
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1021/bi00398a046
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  • 3
    Electronic Resource
    Electronic Resource
    Evaluation of 6 weeks treatment of terbinafine in tinea unguium in a double-blind trial comparing 6 and 12 weeks therapy (1997)
    Oxford, UK : Blackwell Publishing Ltd
    British journal of dermatology 136 (1997), S. 0 
    Details
    ISSN: 1365-2133
    Source: Blackwell Publishing Journal Backfiles 1879-2005
    Topics: Medicine
    Notes: Terbinafine (Lamisil) has been registered throughout the world for the treatment of finger and toenail onychomycosis. The recommended duration of treatment of toenail onychomycosis based on phase III studies is 12 weeks. This study was designed to determine: (i) if patients in whom the proximal part of the toenails was not affected respond as well after 6 weeks treatment as after 12 weeks treatment; (ii) to identify factors which may allow selection of patients for shorter treatment duration; and (iii) confirm that 6 weeks therapy is sufficient in fingernail mycosis. One hundred and forty-eight patients received 250 mg terbinafine daily for either 6 or 12 weeks in a double- blinded manner, and were followed until 48 weeks after start of therapy. Cure of the nail infection was defined as negative mycological tests (mycological cure) and progressive growth of normal nail (clinical cure). Mycological cure was recorded in 43 of 72 (59.7%) in the 6-week group and 55 of 76 (72.4%) in the 12-week group. In those who completed the study per protocol in the 6-week group. 34 of 61 (55.7%) were cured mycologically corresponding to 46 of 56 (82.1%) in the 12-week group. The overall clinical and mycological cure rates for the two groups were 28 of 61 (45.9%) and 33 of 56 (58.9%), respectively. In the small number of patients with associated fingernail infection, all were improved and six of eight (75.0%) were cured after a duration of treatment of 6 weeks. A priori risk factors for failure of cure could not be identified in either group. However, shorter duration of disease prior to treatment and no involvement of the big toenail was associated with a trend toward better responses in both groups. It can be concluded from this study that, in toenail mycosis without visible matrix involvement, 6 weeks treatment of terbinafine is generally not sufficient, whereas fingernail infections respond well to this short therapy.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1046/j.1365-2133.1997.6661651.x
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  • 4
    Electronic Resource
    Electronic Resource
    Anti-inflammatory efficacy of low-dose cyclosporin A in psoriatic arthritis. A prospective multicentre study (1996)
    Oxford, UK : Blackwell Publishing Ltd
    British journal of dermatology 135 (1996), S. 0 
    Details
    ISSN: 1365-2133
    Source: Blackwell Publishing Journal Backfiles 1879-2005
    Topics: Medicine
    Notes: Summary Fifty-five patients with psoriatic arthritis were treated with a low dose of cyclosporin A (CyA) (mean dose 2.7 mg/kg per day) for a period of 6 months to investigate the efficacy of CyA on disease parameters. Significant improvement in the joint complaints and inflammation parameters was observed including a decrease in the number of painful (-46%) and swollen (-45%) joints, tenderness (Ritchie Index: -50%) and degree of swelling (-46%), patient's assessment of pain (-35%), the duration of morning joint stiffness (-37%), as well as a decrease in C-reactive protein (-52%). A 50% reduction of joint complaints required a total of 24 weeks, whereas a 50% reduction of skin involvement was achieved after 5–6 weeks of treatment. Four patients left the study due to adverse events: creatinine level increase in two patients, hypertension in one patient and gastroenteritis in the fourth patient. Joint scintigraphy in 18 patients indicated an improvement or stable condition in 61% of cases after a mean follow-up of approximately 8 months. The results of this prospective study show that low-dose CyA effectively improves not only skin lesions, but also joint complaints in psoriatic arthritis.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1046/j.1365-2133.1996.d01-1074.x
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  • 5
    Electronic Resource
    Electronic Resource
    Clinical relevance of the antibacterial activity of terbinafine:A contralateral comparison between 1% terbinafine cream and 0.1% gentamicin sulphate cream in pyoderma (1992)
    Oxford, UK : Blackwell Publishing Ltd
    British journal of dermatology 126 (1992), S. 0 
    Details
    ISSN: 1365-2133
    Source: Blackwell Publishing Journal Backfiles 1879-2005
    Topics: Medicine
    Notes: The antibacterial efficacy of 1% terbinafine cream and 0.1% gentamicin sulphate cream was evaluated in 33 patients with superficial staphylococcal pyoderma in a double-blind contralateral comparison. After 12 days of active treatment. Staphylococcus aureus could be grown from only one out of 33 patients using terbinafine vs no patient using gentamicin. At the end of the study, a marked improvement in clinical symptoms was observed with no significant difference between the two therapies. Despite reviewing the patients three times during the course of the study, no adverse events were reported. The results of this study demonstrate that terbinafine has clinically relevant antibacterial properties which may be useful not only in pyoderma, but also in mixed fungal/bacterial infections, such as athlete's foot.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1111/j.1365-2133.1992.tb00012.x
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  • 6
    Electronic Resource
    Electronic Resource
    Eosinophils, pruritus and psoriasis: effects of treatment with etretinate or cyclosporin-A (1998)
    Oxford, UK : Blackwell Publishing Ltd
    Journal of the European Academy of Dermatology and Venereology 11 (1998), S. 0 
    Details
    ISSN: 1468-3083
    Source: Blackwell Publishing Journal Backfiles 1879-2005
    Topics: Medicine
    Notes: Background The antipsoriatic drugs cyclosporin A (CyA) and etretinate have been found to influence proinflammatory eosinophilic leukocytes and pruritus.Aim We compared the number of Wood eosinophils, concentration of serum eosinophil cationic protein (ECP), and pruritus in patients with psoriasis treated with either CyA or etretinate.Study design Patients with psoriasis vulgaris were randomly assigned to treatment for 10 weeks with either CyA (n= 21) or etretinate (n= 10). The psoriasis area-and-severity index (PASI-score) and pruritus (according to a 0–3 scale) served as clinical parameters, the blood esosinophil counts (Coulter Counter) and the serum ECP (RIA, Pharmacia) as laboratory parameters.Results After CyA treatment the PASI-score amounted to 24 ± 4%, after etretinate to 56 ± 6% of the initial values (mean ± SEM). One week after CyA treatment, esosinophils dropped from 190 ± 21 to 137 ± 16/μ (P= 0.038, Wilcoxon test), after 10 weeks to 127 ± 18/μ (P= 0.006). By contrast, under etretinate blood eosinophil counts only changed marginally. Before treatment, ECP concentrations of 15.71 ± 1.30 (CyA) and 15.3 ± 5.53 μg/1 (etretinate) were measured (normal range 3–16 /μg/1), ECP remained constant under both CyA and etretinate or tended to increase after 10 weeks; about 50% of the patients exhibited elevated ECP concentrations. Pruritus diminished more with CyA than etretinate therapy. PASI-scores and pruritus were directly proportional.Outcome We conclude that treatment of psoriasis with CyA leads to a rapid drop of blood eosinophils and that the activation state of eosinophils does not decrease after antipsoriatic treatment. Pruritus in psoriasis is coupled to disease severity. The underlying antipsoriatic mechanisms of CyA may be linked to lowering the number of blood eosinophils.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1111/j.1468-3083.1998.tb00975.x
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  • 7
    Electronic Resource
    Electronic Resource
    Direct inhibition of tyrosine hydroxylase from PC-12 cells by catechol derivatives (1986)
    Springer
    Naunyn-Schmiedeberg's archives of pharmacology 332 (1986), S. 346-350 
    Details
    ISSN: 1432-1912
    Keywords: Tyrosine hydroxylase ; Feedback inhibition ; Dopamine
    Source: Springer Online Journal Archives 1860-2000
    Topics: Medicine
    Notes: Summary Several drugs with a catechol moiety were studied for their potency to inhibit tyrosine hydroxylase (TH) from PC-12 cells in vitro. When the natural compounds tested were compared, dopamine, norepinephrine and 2(3,4-dihydroxyphenyl)-ethanol (DOPET) were most effective (IC50 between 1.4 and 3.6 μM with 0.5 μM 6(R,S)-l-erythro-5,6,7,8-tetrahydrobiopterin as cofactor). 3,4-Dihydroxyphenylalanine (DOPA; IC50: 35 μM) and 3,4-dihydroxyphenylacetic acid (DOPAC; IC50: 180 μM were less potent inhibitors. Among the synthetic drugs possessing catechol moiety, isoproterenol, (±)-2-amino-6,7-dihydroxy-1,2,3,4-tetrahydronaphthalene (6,7-ADTN) and (±)-2-dimethylamino-6,7-dihydroxy-tetrahydronaphthalene (TL-99) had the same inhibitory effects as the natural catecholamines (IC50 between 1.6 and 3.9 μM), whereas the apomorphine derivatives and 2,3,4,5-tetrahydro-1-phenyl-1 H-3-benzazepine-7,8-diol (SKF 38393) were even more potent (IC50: 0.5–0.8 μM). These results demonstrate that natural catechols and certain drugs (e.g. 6,7-ADTN, TL-99, SKF 38393) are more effective direct blockers of tyrosine hydroxylase than generally assumed provided appropriate assay conditions are used. In the case of dopamine and norepinephrine, these findings suggest a reevaluation of their role for feedback control of tyrosine hydroxylase in vivo.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1007/BF00500085
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  • 8
    Electronic Resource
    Electronic Resource
    The Role of Glucocorticoids and Prostaglandin E2 in the Recruitment of Bone Marrow Mesenchymal Cells to the Osteoblastic Lineage: Positive and Negative Effects (1996)
    Springer
    Calcified tissue international 59 (1996), S. 154-162 
    Details
    ISSN: 1432-0827
    Keywords: Key words: Glucocorticoids — Dexamethasone — Prostaglandins — Osteoblast — Bone marrow cell — Colony forming unit.
    Source: Springer Online Journal Archives 1860-2000
    Topics: Biology , Medicine , Physics
    Notes: Abstract. The role of glucocorticoids in bone formation presents a problem because although pharmacological doses in vivo give rise to osteoporosis, physiological concentrations are required for osteoblast (OB) differentiation in vitro. To try and rationalize this dichotomy, we investigated the effect of dexamethasone on the recruitment of OB precursors present in bone marrow. Using the CFU-f assay, we can measure (1) total colony formation; (2) the osteoblastic differentiation of the colonies defined as their ability to express alkaline phosphatase, synthesize collagen, and to calcify; and (3) colony expansion as either average colony surface area or average colony number. In control cultures and in the presence of 10−10–10−9 M dexamethasone, colony formation and total cell number was maximal, but the addition of PGE2 had no effect on colony number and very few colonies expressed the OB phenotype. In the presence of 10−8–10−7 M dexamethasone, colony numbers and total cell numbers were reduced but were increased by the addition of PGE2, the average colony cell number and surface area were relatively unchanged and a proportion of the colonies expressed APase, calcified and synthesized collagen. In cultures containing 10−6–10−5 M dexamethasone, colony numbers were further reduced but were stimulated by the addition of PGE2 and some colonies differentiated; however, colony expansion was dramatically reduced by up to 80%. These results suggest that physiological levels of glucocorticoids are necessary for OB differentiation and allow the control of OB recruitment by PGE2. High levels of glucocorticoids drastically reduce proliferation of the OB precursors leading to glucocorticoid-induced osteoporosis.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1007/s002239900102
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  • 9
    Electronic Resource
    Electronic Resource
    Depression of reserpine-induced muscular rigidity in rats after administration of lisuride into the spinal subarachnoid space (1980)
    Springer
    Naunyn-Schmiedeberg's archives of pharmacology 315 (1980), S. 177-179 
    Details
    ISSN: 1432-1912
    Keywords: Lisuride ; Reserpine-induced rigidity ; Spinal cord ; Subarachnoid space
    Source: Springer Online Journal Archives 1860-2000
    Topics: Medicine
    Notes: Summary Muscular rigidity was induced by reserpine (10 mg/kg) in rats and the tonic activity of the gastrocnemius muscle was recorded in the electromyogram. Systemic administration of lisuride, an ergoline, resulted in a dose-dependent depression of rigidity. To examine the spinal cord as a site of action for lisuride to depress reserpine-induced rigidity, a method for the chronic catheterization of the lumbar spinal subarachnoid space was used, which allowed the administration of drugs to reserpinized, intact rats without anaesthesia. Lisuride injected into the lumbar spinal subarachnoid space resulted in a longlasting depression of rigidity. These results suggest that the spinal cord is an important site of action of lisuride.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1007/BF00499261
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  • 10
    Electronic Resource
    Electronic Resource
    Inhibition of striatal tyrosine hydroxylase by low concentrations of apomorphine (1984)
    Springer
    Naunyn-Schmiedeberg's archives of pharmacology 327 (1984), S. 114-118 
    Details
    ISSN: 1432-1912
    Keywords: Apomorphine ; Dopaminergic presynaptic autoreceptor ; Tetrahydrobiopterin ; Tyrosine hydroxylase
    Source: Springer Online Journal Archives 1860-2000
    Topics: Medicine
    Notes: Summary The inhibitory effect of apomorphine on tyrosine hydroxylase (TH) was tested using enzyme preparations from rat striatum, neuroblastoma clone N1E-115 and pheochromocytoma clone PC-12. When the striatal enzyme preparation was incubated at pH 7.2 with (6R,S)-l-erythro-5,6,7,8-tetrahydrobiopterin (BH4) as cofactor (100–1,000 μmol/l), the IC50 for apomorphine was found to be in the 0.1–1 μmol/l range depending on the BH4-concentration used. Changing the incubation medium to pH 6.0 yielded an IC50 of about 2.5 μmol/l (BH4=100 μmol/l) Apomorphine was even less effective when 2-amino-4-hydroxy-6,7-dimethyl-5,6,7,8-tetrahydroteridine (100 μmol/l) was used as cofactor (IC50∼10 μmol/l). Similar results were obtained with the enzyme preparations of the two cell clones. These experiments show that, even in low concentrations, apomorphine inhibits TH directly, provided more physiological test conditions are used. The relevance of these results for the autoreceptor-mediated mechanism of the apomorphine action on catecholamine synthesis is discussed.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1007/BF00500904
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