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Skin Testing in Drug Hypersensitivity
Published in Kirsti Kauppinen, Kristiina Alanko, Matti Hannuksela, Howard Maibach, Skin Reactions to Drugs, 2020
Tetrazepam, a benzodiazepine which structurally closely resembles diazepam, has produced positive results when tested as such and at 1% in water and petrolatum in cases of tetrazepam-induced rash59–62 and may sometimes show cross-allergy with diazepam.61 Thus, tetrazepam at 1% in petrolatum or water seems to be a useful material for patch testing.
Low Back Pain and Sciatica: Pathogenesis, Diagnosis and Nonoperative Treatment
Published in Gary W. Jay, Practical Guide to Chronic Pain Syndromes, 2016
Muscle spasmolytics or “relaxants” are traditionally used to treat painful musculoskeletal disorders, but share sedation and sometimes dizziness as common side effects; therefore, some clinicians prescribe them only at bedtime. Some muscle spasmolytics are also considered potentially addictive and have abuse potential, especially more traditional agents such as diazepam, butalbital, and phenobarbital. Examples of commonly used muscle relaxants include cyclobenzaprine, carisoprodol, methocarbamol, chlorzoxazone, and metaxalone. Benzodiazepines may be appropriate for concurrent anxiety states, and in these cases, clonazepam should be considered. Clonazepam operates via GABA-mediated mechanisms through internuncial neurons of the spinal cord to provide muscle relaxation (58). Another benzodiazepine, tetrazepam, showed strong evidence of efficacy, when compared to placebo, for improving short-term pain and moderate evidence for short-term improvement of muscle spasm, but any data for long-term use was lacking (59). A review and analysis of randomized or double-blinded controlled trials showed that muscle relaxants were effective for management of LBP, but adverse side effects limited their utility (60). A similar comprehensive meta-analysis of the effectiveness of cyclobenzaprine showed evidence to support short-term use (<4 days) citing modest benefit in early LBP, but with the same problematic side effects (61). Tizanidine is a central alpha-2-adrenoreceptor agonist that was developed for the management of spasticity due to cerebral or spinal cord injury, but also has demonstrated efficacy when compared to other muscle spasmolytics (62). Controlled clinical trials have demonstrated clinical efficacy of tizanidine, including reduced analgesic use and muscle spasm, in patients with acute neck and back pain (63, 64).
Studies of Benzodiazepine Receptors Using In Vivo Autoradiography
Published in Edythe D. London, Imaging Drug Action in the Brain, 2017
Additional ex vivo experiments have been conducted using [3H]flunitrazepam (Chang and Snyder, 1978) with a 20-min incubation period (i.e., 20 min between the intravenous injection of the radioligand and the sacrifice of the animal). CGS 8216, a benzodiazepine receptor agonist, was reported to inhibit the labeling of benzodiazepine receptors by [3H]flunitrazepam with a potency (7.0 mg/kg, p.o.) comparable to that obtained with diazepam (5.0 mg/kg, p.o.); (Czernik et al., 1982). However, this drug was a much more potent inhibitor of [3H]flunitrazepam binding in vitro (0.3 mM) when compared to diazepam (8.0 nM), suggesting important differences between results obtained ex vivo and in vitro with this antagonist. Tetrazepam is a novel benzodiazepine derivative that produces the typical benzodiazepine-like effects of ataxia and sedation at doses considerably higher than those required to produce anxiolytic and muscle relaxant effects (Keane et al., 1988a). This drug inhibited the specific binding of [3H]flunitrazepam in the mouse brain (ID50 37 mg/kg, p.o.) and kidney (ID50 38 mg/kg, p.o.), suggesting that tetrazepam has comparable affinities for the central and peripheral-type benzodiazepine receptors (Keane et al., 1988b) and also demonstrating that intravenous [3H]flunitrazepam labels both receptor types. These ex vivo data are comparable to the effects of tetrazepam on benzodiazepine receptors in vitro, although these data do not suggest the mechanisms through which this drug produces anxiolytic and muscle relaxant effects at much lower doses than required for ataxia and sedation. β-Carboline-3-carboxylic acid ethyl ester (β-CEE) has also been evaluated using this ex vivo model (Hirsch and Lydigsen, 1981). When administered intravenously (ED50 2.1 mg/kg) 10 min before the injection of [3H]flunitrazepam, β-CEE inhibited the specific binding of [3H]flunitrazepam in the same dose range as required to antagonize the effects of diazepam and to lower the convulsive dose for pentylenetetrazol (Tenen and Hirsch, 1980). Furthermore, the apparent regional specificity for β-CEE was similar ex vivo to the distribution obtained in vitro. These data suggest that a longer incubation period (20 min vs. 1 to 2 min) may be important for [3H]flunitrazepam to reach equilibrium in vivo.
Efficacy and tolerability of the antispasmodic, pridinol, in patients with muscle-pain – results of primepain, a retrospective analysis of open-label real-world data provided by the German pain E-registry
Published in Current Medical Research and Opinion, 2022
Michael A. Überall, Gerhard H. H. Müller-Schwefe, Johannes Horlemann
In Europe, the spectrum of available antispasmodics has been significantly narrowed in recent years due to several risk-benefit assessments published by the Pharmacovigilance Risk Assessment Committee (PRAC) of the European Medicines Agency (EMA) and consecutive extensions of the official product characteristic and the inclusion of new side effects (tizanidine)20, restrictions on approval (tolperisone)21, the temporary suspension (tetrazepam)22, or even withdrawal (flupirtine) of marketing authorization23. Nevertheless, certain antispasmodics – such as pridinol24, which was reapproved in Germany in 2018 and has been subsequently approved in other countries of the European Union as well – are proving very popular in daily practice, with increasing prescription numbers25.
Efficacy and safety/tolerability of pridinol: a meta-analysis of double-blind, randomized, placebo-controlled trials in adult patients with muscle pain
Published in Current Medical Research and Opinion, 2022
Michael A. Überall, Ute Essner, Gerhard H. H. Müller-Schwefe
In Europe, the spectrum of available antispasmodics has been significantly narrowed in recent years due to several risk-benefit assessments published by the Pharmacovigilance Risk Assessment Committee (PRAC) of the European Medicines Agency (EMA) and consecutive extensions of the official product characteristic and the inclusion of new side effects (tizanidine)8, restrictions on approval (tolperisone)9, the temporary suspension (tetrazepam)10, or even withdrawal of marketing authorization (flupirtine)11. This contrasts to, pridinol (PRI), a nonbenzodiazepine antispasmodic acting via cholinergic antagonism of muscarinic acetylcholine receptors (M1 subtype)12,13, which was originally discovered in the late 1950s and brought to market approval in various European and non-European countries in the 1960s. End of 2017, PRI was reauthorized in Germany to treat central and peripheral muscle spasms, torticollis, lumbago, and general muscle pain in adult patients. Subsequently and for the first time PRI has been approved by the UK, Poland, and Spain in 2020.
Psychopharmacological treatment of patients with borderline personality disorder: comparing data from routine clinical care with recommended guidelines
Published in International Journal of Psychiatry in Clinical Practice, 2019
Friedrich Riffer, Marta Farkas, Lore Streibl, Elmar Kaiser, Manuel Sprung
Overall 106 (96.4%) of the BPD patients in the present sample were prescribed at least one psychotropic medication, 37 (33.6%) were prescribed 1–2 psychotropic medications, 40 (36.4%) were prescribed 3–4 psychotropic medications and 29 (26.4%) were prescribed 5 or more psychotropic medications. The total number of psychotropic medications ranged between 1 and 9 different psychotropic drugs, with a mean of 3.44 (SD = 1.9), a median of 3 and a mode of 2. Patients were prescribed between 1 and 6 different types of psychotropic medications (i.e., FGA, SGA, mood stabilisers, TCA, SNRI/NDRI and SSRI), with a mean of 2.4 (SD = 1.3), a median and mode of 2. Table 2 depicts the categories/types of psychotropic medications and active substances (number and percentage) prescribed to BPD patients in the present sample, during in-patient treatment. The most commonly prescribed categories/types were second-generation antipsychotics (SGA) (70%), selective serotonin reuptake inhibitors (SSRIs) (49.1%) and mood stabilisers (41.8%). The most commonly prescribed single drugs were the SSRI Setraline (33.6%), the mood stabiliser Lamotrigine (31.8%), the SGA Quetiapine (29.1%), and the tricyclic antidepressant Trazodone (29.1%). Another commonly prescribed substance was the SGA Aripiprazole (13.6%), which was often prescribed together with a second SGA, such as Quetiapine or Olanzapin. Other adjunctive psychotropic medications were also common, but psychostimulants (methylphenidate) (6%) and benzodiazepines (Alprazolam, Tetrazepam) (2%) were only rarely prescribed.