- MeSH
- Analgesics MeSH
- Anesthetics, Local administration & dosage therapeutic use MeSH
- Gabapentin administration & dosage therapeutic use MeSH
- Quality of Life MeSH
- Humans MeSH
- Lidocaine administration & dosage therapeutic use MeSH
- Neuralgia, Postherpetic * diagnosis drug therapy prevention & control MeSH
- Aged MeSH
- Transdermal Patch MeSH
- Herpes Zoster Vaccine MeSH
- Check Tag
- Humans MeSH
- Aged MeSH
- Female MeSH
- Publication type
- Case Reports MeSH
- Research Support, Non-U.S. Gov't MeSH
Na pracovišti ambulance bolesti v Českých Budějovicích se v posledních dvou letech věnujeme ošetřování akutní progrese chronických bolestí hlavy intranazální aplikací lidokainu. Jedná se o ambulantní, minimálně invazivní a pacienty dobře snášenou metodu. V poloze vleže podáváme malé množství 4% lidokainového gelu opakovaně po 3–5 minutách celkem 3–5krát nosní dírkou na postižené bolestivé polovině hlavy. Aplikátor zavádíme po znecitlivění vstupu do nosu šetrně až do kontaktu se zadní stěnou nosohltanu, pod jehož sliznicí se nachází trigeminální ganglion. Cílem ošetření je ovlivnit lokálním anestetikem ganglion sphenopalatinum a snížit vedení bolesti v povodí trigeminálního nervu z postižené poloviny hlavy a obličeje. Zákrok provádíme opakovaně třikrát týdně. Výkon často kombinujeme s podáním antineuropatické infuze. Metodu jsme vyzkoušeli u pacientů s postherpetickými bolestmi obličeje, při atakách bolestí hlavy u pacientů s roztroušenou sklerózou, u pacientů čekajících na intervenční zákrok při neuralgiích trigeminu na podkladě neurovaskulárního konfliktu. Dobrý efekt byl pozorován i u akutních postpunkčních bolestí hlavy a u migrény. Úlevu od bolesti lze pozorovat po 1–2 hodinách a trvání efektu léčby je velmi individuální: 2 dny až 4 týdny. Opakování zákroku obden a současná aplikace antineuropatické infuze nebo myorelaxační infuze potencují analgetický účinek. Ošetření bývá pacienty dobře snášeno. Při zavádění aplikátoru může dojít k poranění nosní sliznice, během aplikace je patrné slzení, necitlivost a pocit chladu pod okem a v okolí jařmového oblouku ošetřované strany. Občas se vyskytne pálení v oblasti nosohltanu ze zatékajícího lidokainového gelu, což se dá ovlivnit množstvím aplikované látky. Ze zájmu pacientů o opakování aplikace lze usuzovat na pozitivní efekt metody.
At the pain clinic in Budweis, we have been treating the acute progression of chronic headaches using intranasal lidocaine for the past two years. It is an outpatient, minimally invasive method that is well tolerated by patients. In the supine position, we administer a small amount of 4 % lidocaine gel repeatedly after 3-5 minutes a total of 3-5 times through the nostril on the affected painful half of the head. After anesthetizing the entrance to the nose, the applicator is gently inserted until it comes into contact with the back wall of the nasopharynx, under the mucosa of which the trigeminal ganglion is located. The aim of the treatment is to affect the sphenopalatine ganglion with a local anesthetic and to reduce the conduction of pain in the basin of the trigeminal nerve from the affected half of the head and face. We perform the procedure repeatedly 3 times a week. We often combine the procedure with the administration of an antineuropathic infusion. We tried the method in patients with post-herpetic facial pain, in headache attacks in patients with multiple sclerosis, in patients waiting for intervention for trigeminal neuralgia based on neurovascular conflict. A good effect was also observed in acute postpuncture headaches and migraines. The effect can be observed after 1-2 hours and the duration is very individual from 2 days to 4 weeks. Repeating the procedure every other day and simultaneous application of antineuropathic infusion or myorelaxant infusion potentiate the analgesic effect. Treatment is usually well tolerated by patients. When inserting the applicator, the nasal mucosa may be injured, during the application there is steamy lacrimation, numbness and a feeling of coldness under the eye and around the zygomatic arch of the treated side. Sometimes there is a burning sensation in the nasopharynx area from leaking lidocaine gel, which can be influenced by the amount of applied substance. The positive effect of the method can be inferred from the patients‘ interest in repeating the application.
- MeSH
- Administration, Intranasal * methods adverse effects MeSH
- Headache * etiology drug therapy classification MeSH
- Adult MeSH
- Tooth Extraction adverse effects MeSH
- Ganglia, Parasympathetic drug effects MeSH
- Middle Aged MeSH
- Humans MeSH
- Lidocaine * administration & dosage adverse effects therapeutic use MeSH
- Trigeminal Nerve physiology MeSH
- Trigeminal Neuralgia etiology drug therapy MeSH
- Check Tag
- Adult MeSH
- Middle Aged MeSH
- Humans MeSH
- Female MeSH
- Publication type
- Case Reports MeSH
- Review MeSH
- MeSH
- Gynecology * MeSH
- Humans MeSH
- Lidocaine administration & dosage therapeutic use MeSH
- Anesthesia, Local * methods MeSH
- Surveys and Questionnaires MeSH
- Check Tag
- Humans MeSH
- Female MeSH
- Geographicals
- Czech Republic MeSH
- MeSH
- Analgesics adverse effects therapeutic use MeSH
- Chronic Pain * drug therapy classification psychology MeSH
- Humans MeSH
- Lidocaine therapeutic use MeSH
- Neuralgia drug therapy MeSH
- Nociceptive Pain drug therapy MeSH
- Analgesics, Opioid therapeutic use MeSH
- Check Tag
- Humans MeSH
- Publication type
- Review MeSH
- Keywords
- Versatis,
- MeSH
- Chronic Pain drug therapy MeSH
- Drug Evaluation MeSH
- Humans MeSH
- Lidocaine * administration & dosage pharmacology therapeutic use MeSH
- Pain Management methods MeSH
- Neuralgia * drug therapy MeSH
- Neuralgia, Postherpetic * drug therapy MeSH
- Transdermal Patch MeSH
- Check Tag
- Humans MeSH
Background The effect of infarct pattern on functional outcome in acute ischemic stroke is incompletely understood. Purpose To investigate the association of qualitative and quantitative infarct variables at 24-hour follow-up noncontrast CT and diffusion-weighted MRI with 90-day clinical outcome. Materials and Methods The Safety and Efficacy of Nerinetide in Subjects Undergoing Endovascular Thrombectomy for Stroke, or ESCAPE-NA1, randomized controlled trial enrolled patients with large-vessel-occlusion stroke undergoing mechanical thrombectomy from March 1, 2017, to August 12, 2019. In this post hoc analysis of the trial, qualitative infarct variables (predominantly gray [vs gray and white] matter involvement, corticospinal tract involvement, infarct structure [scattered vs territorial]) and total infarct volume were assessed at 24-hour follow-up noncontrast CT or diffusion-weighted MRI. White and gray matter infarct volumes were assessed in patients by using follow-up diffusion-weighted MRI. Infarct variables were compared between patients with and those without good outcome, defined as a modified Rankin Scale score of 0-2 at 90 days. The association of infarct variables with good outcome was determined with use of multivariable logistic regression. Separate regression models were used to report effect size estimates with adjustment for total infarct volume. Results Qualitative infarct variables were assessed in 1026 patients (mean age ± standard deviation, 69 years ± 13; 522 men) and quantitative infarct variables were assessed in a subgroup of 358 of 1026 patients (mean age, 67 years ± 13; 190 women). Patients with gray and white matter involvement (odds ratio [OR] after multivariable adjustment, 0.19; 95% CI: 0.14, 0.25; P < .001), corticospinal tract involvement (OR after multivariable adjustment, 0.06; 95% CI: 0.04, 0.10; P < .001), and territorial infarcts (OR after multivariable adjustment, 0.22; 95% CI: 0.14, 0.32; P < .001) were less likely to achieve good outcome, independent of total infarct volume. Conclusion Infarct confinement to the gray matter, corticospinal tract sparing, and scattered infarct structure at 24-hour noncontrast CT and diffusion-weighted MRI were highly predictive of good 90-day clinical outcome, independent of total infarct volume. Clinical trial registration no. NCT02930018 © RSNA, 2021 Online supplemental material is available for this article. See also the editorial by Mossa-Basha in this issue.
- MeSH
- Arterial Occlusive Diseases diagnostic imaging pathology therapy MeSH
- Diflucortolone MeSH
- Diffusion Magnetic Resonance Imaging * MeSH
- Double-Blind Method MeSH
- Drug Combinations MeSH
- Ischemic Stroke diagnostic imaging pathology therapy MeSH
- Humans MeSH
- Lidocaine MeSH
- Neuroprotective Agents therapeutic use MeSH
- Tomography, X-Ray Computed * MeSH
- Prognosis MeSH
- Aged MeSH
- Thrombectomy MeSH
- Check Tag
- Humans MeSH
- Male MeSH
- Aged MeSH
- Female MeSH
- Publication type
- Journal Article MeSH
- Multicenter Study MeSH
- Research Support, Non-U.S. Gov't MeSH
- Randomized Controlled Trial MeSH
Despite the importance of drug release testing of parenteral depot formulations, the current in vitro methods still require ameliorations in biorelevance. We have investigated here the use of muscle tissue components to better mimic the intramuscular administration. For convenient handling, muscle tissue was used in form of a freeze-dried powder, and a reproducible process of incorporation of tested microspheres to an assembly of muscle tissue of standardized dimensions was successfully developed. Microspheres were prepared from various grades of poly(lactic-co-glycolic acid) (PLGA) or ethyl cellulose, entrapping flurbiprofen, lidocaine, or risperidone. The deposition of microspheres in the muscle tissue or addition of only isolated lipids into the medium accelerated the release rate of all model drugs from microspheres prepared from ester-terminated PLGA grades and ethyl cellulose, however, not from the acid-terminated PLGA grades. The addition of lipids into the release medium increased the solubility of all model drugs; nonetheless, also interactions of the lipids with the polymer matrix (ad- and absorption) might be responsible for the faster drug release. As the in vivo drug release from implants is also often faster than in simple buffers in vitro, these findings suggest that interactions with the tissue lipids may play an important role in these still unexplained observations.
- MeSH
- Cellulose analogs & derivatives MeSH
- Flurbiprofen administration & dosage MeSH
- Polylactic Acid-Polyglycolic Acid Copolymer MeSH
- Delayed-Action Preparations * MeSH
- Lidocaine administration & dosage MeSH
- Microspheres MeSH
- Drug Carriers MeSH
- Infusions, Parenteral * MeSH
- Excipients MeSH
- Swine MeSH
- Drug Compounding MeSH
- Risperidone administration & dosage MeSH
- Muscles metabolism MeSH
- In Vitro Techniques MeSH
- Drug Liberation MeSH
- Animals MeSH
- Check Tag
- Animals MeSH
- Publication type
- Journal Article MeSH
A simple, sensitive HPLC-MS/MS method was developed and validated for the determination of lidocaine in skin and plasma of rats. The methods were established and validated assessing lower limit of quantitation (LLOQ), linearity, intra and inter-day precision and accuracy, selectivity, recovery and matrix effect. Chromatography was done on a Gemini column embedded with C18 stationary phase (50 mm × 2.0 mm, 5 µm particle size), using a gradient with mobile phases consisting of 0.1% HCOOH in bidistilled water and 0.1% HCOOH in acetonitrile. The mass spectrometer worked with electrospray ionization in positive ion mode and selected reaction monitoring, using target ions m/z 235.10 for lidocaine and m/z 245.10 for lidocaine-d10, used as internal standard. RESULTS: The linearity of the method was in the ranges of lidocaine concentrations 10.0-200.0 ng/mL for skin homogenate (accuracy 94.1-105.5%; R2 ≥ 0.998) and 0.025-2 ng/mL for plasma (accuracy 96.2-104.8%; R2 ≥ 0.996). The intra- and inter-day precision and accuracy determined on three quality control samples (20, 75 and 170 ng/mL for skin and 0.075, 0.4 and 1.5 ng/mL for plasma) were ≤4.2% and 103.8-108.2% for skin and ≤12.4% and 95.5-101.4% for plasma. The LLOQ was 10 ng/mL in skin homogenate and 0.025 ng/mL in plasma. The applicability of the method was demonstrated by measuring lidocaine in skin and plasma after exposure to medicated patches containing 5% lidocaine.
- MeSH
- Rats MeSH
- Skin chemistry MeSH
- Lidocaine administration & dosage analysis pharmacokinetics MeSH
- Limit of Detection MeSH
- Linear Models MeSH
- Reproducibility of Results MeSH
- Drug Stability MeSH
- Tandem Mass Spectrometry methods MeSH
- Transdermal Patch * MeSH
- Chromatography, High Pressure Liquid methods MeSH
- Animals MeSH
- Check Tag
- Rats MeSH
- Male MeSH
- Animals MeSH
- Publication type
- Journal Article MeSH
The effective concentration of a drug in the blood, i.e. the concentration of a free drug in the blood, is influenced by the strength of drug binding onto plasma proteins. Besides its efficacy, these interactions subsequently influence the liberation, absorption, distribution, metabolism, excretion, and toxicological properties of the drug. It is important to not only determine the binding strength and stoichiometry, but also the binding site of a drug on the plasma protein molecule, because the co-administration of drugs with the same binding site can affect the above-mentioned concentration and as a result the pharmacological behavior of the drugs and lead to side effects caused by the change in free drug concentration, its toxicity. In this study, the binding characteristics of six drugs with human serum albumin, the most abundant protein in human plasma, were determined by capillary electrophoresis-frontal analysis, and the obtained values of binding parameters were compared with the literature data. The effect of several drugs and site markers on the binding of l-tryptophan and lidocaine to human serum albumin was investigated in subsequent displacement studies which thus demonstrated the usability of capillary electrophoresis as an automated high-throughput screening method for drug-protein binding studies.
- MeSH
- Chlorpropamide analysis pharmacology MeSH
- Diclofenac analysis pharmacology MeSH
- Electrophoresis, Capillary MeSH
- Phenylbutazone analysis pharmacology MeSH
- Flurbiprofen analysis pharmacology MeSH
- Ibuprofen analysis pharmacology MeSH
- Humans MeSH
- Lidocaine antagonists & inhibitors chemistry MeSH
- Serum Albumin, Human chemistry MeSH
- Tolbutamide analysis pharmacology MeSH
- Tryptophan antagonists & inhibitors chemistry MeSH
- Binding Sites drug effects MeSH
- Check Tag
- Humans MeSH
- Publication type
- Journal Article MeSH
