Evolution of the occurrence of Tityus serrulatus (LUTZ & MELLO, 1992) in the state of Santa Catarina.

BACKGROUND: Scorpions are a leading cause of envenomation in Brazil. The species Tityus serrulatus is associated with the most severe cases, especially in children. Despite not being endemic to the state of Santa Catarina, such occurrences have increased more than 500% in the state recently. Therefore, this study aimed to analyze the occurrence of envenomation by T. serrulatus, attended by the Center for Toxicological Information and Assistance of Santa Catarina. METHODS: This was a retrospective and descriptive study of the occurrence of T. serrulatus, identified by the agency, from 2014 to 2021 in Santa Catarina, using data obtained by the BI-DATATOX system. RESULTS: A total of 112 occurrences were classified as envenomation. Of these cases, 48.2% were recorded in the Itajaí Valley region and 33% in Greater Florianópolis. Men were involved in 59.8% of these, and the most common age group was 20-39 years (39.3%). Most envenomation occurred in urban areas (89.3%) under non-occupational circumstances (83%). Stings were more frequent on the hands (50.9%). Care was sought within 1 h after the event in 75.9% of the cases, and 94.6% were classified as mild. CONCLUSIONS: Occurrence of envenomation involving T. serrulatus in Santa Catarina increased significantly during the study period. Most cases occurred in urbanized areas, which suggests that they might have been transported from other states, and it must be considered that, in the urban environment, scorpions find a large supply of food and shelter and a reduced number of specific predators, allied to parthenogenesis.

Evolution of the occurrence of Tityus serrulatus (LUTZ & MELLO, 1992) in the state of Santa Catarina

ABSTRACT Background: Scorpions are a leading cause of envenomation in Brazil. The species Tityus serrulatus is associated with the most severe cases, especially in children. Despite not being endemic to the state of Santa Catarina, such occurrences have increased more than 500% in the state recently. Therefore, this study aimed to analyze the occurrence of envenomation by T. serrulatus, attended by the Center for Toxicological Information and Assistance of Santa Catarina. Methods: This was a retrospective and descriptive study of the occurrence of T. serrulatus, identified by the agency, from 2014 to 2021 in Santa Catarina, using data obtained by the BI-DATATOX system. Results: A total of 112 occurrences were classified as envenomation. Of these cases, 48.2% were recorded in the Itajaí Valley region and 33% in Greater Florianópolis. Men were involved in 59.8% of these, and the most common age group was 20-39 years (39.3%). Most envenomation occurred in urban areas (89.3%) under non-occupational circumstances (83%). Stings were more frequent on the hands (50.9%). Care was sought within 1 h after the event in 75.9% of the cases, and 94.6% were classified as mild. Conclusions: Occurrence of envenomation involving T. serrulatus in Santa Catarina increased significantly during the study period. Most cases occurred in urbanized areas, which suggests that they might have been transported from other states, and it must be considered that, in the urban environment, scorpions find a large supply of food and shelter and a reduced number of specific predators, allied to parthenogenesis.

Population pharmacokinetics of gabapentin in patients with neuropathic pain: Lack of effect of diabetes or glycaemic control.

AIMS: Gabapentin (GBP) is widely used to treat neuropathic pain, including diabetic neuropathic pain. Our objective was to evaluate the role of diabetes and glycaemic control on GBP population pharmacokinetics. METHODS: A clinical trial was conducted in patients with neuropathic pain (n = 29) due to type 2 diabetes (n = 19) or lumbar/cervical disc herniation (n = 10). All participants were treated with a single oral dose GBP. Blood was sampled up to 24 hours after GBP administration. Data were analysed with a population approach using the stochastic approximation expectation maximization algorithm. Weight, body mass index, sex, biomarkers of renal function and diabetes, and genotypes for the main genetic polymorphisms of SLC22A2 (rs316019) and SLC22A4 (rs1050152), the genes encoding the transporters for organic cations OCT2 and OCTN1, were tested as potential covariates. RESULTS: GBP drug disposition was described by a 1-compartment model with lag-time, first-order absorption and linear elimination. The total clearance was dependent on estimated glomerular filtration rate. Population estimates (between-subject variability in percentage) for lag time, first-order absorption rate, apparent volume of distribution and total clearance were 0.316 h (10.6%), 1.12 h-1 (10.7%), 140 L (7.7%) and 14.7 L/h (6.97%), respectively. No significant association was observed with hyperglycaemia, glycated haemoglobin, diabetes diagnosis, age, sex, weight, body mass index, SLC22A2 or SLC22A4 genotypes. CONCLUSION: This population pharmacokinetics model accurately estimated GBP concentrations in patients with neuropathic pain, using estimated glomerular filtrationrate as a covariate for total clearance. The distribution and excretion processes of GBP were not affected by hyperglycaemia or diabetes.

Cetirizine Reduces Gabapentin Plasma Concentrations and Effect: Role of Renal Drug Transporters for Organic Cations.

Gabapentin (GBP) is an organic cation mainly eliminated unchanged in urine, and active drug secretion has been suggested to contribute to its renal excretion. Our objective was to evaluate the potential drug-drug interaction between GBP and cetirizine (CTZ), an inhibitor of transporters for organic cations. An open-label, 2-period, crossover, nonrandomized clinical trial was conducted in patients with neuropathic pain to evaluate the effect of CTZ on GBP pharmacokinetics. Twelve participants were treated with a single dose of 300 mg GBP (treatment A) or with 20 mg/d of CTZ for 5 days and 300 mg GBP on the last day of CTZ treatment (treatment B). Blood sampling and pain intensity evaluation were performed up to 36 hours after GBP administration. The interaction of GBP and CTZ with transporters for organic cations was studied in human embryonic kidney (HEK) cells expressing the organic cation transporters (OCTs), multidrug and toxin extrusion proteins (MATEs), and OCTN1. CTZ treatment resulted in reduced area under the concentration-time curve and peak concentration compared with treatment A. In treatment B, the lower plasma concentrations of GBP resulted in reduced pain attenuation. GBP renal clearance was similar between treatments. GBP has low apparent affinity for OCT2 (concentration of an inhibitor where the response [or binding] is reduced by half [IC50 ] 237 µmol/L) and a high apparent affinity for hMATE1 (IC50 1.1 nmol/L), hMATE2-K (IC50 39 nmol/L), and hOCTN1 (IC50 2.1 nmol/L) in HEK cells. At therapeutic concentrations, CTZ interacts with hMATE1 and OCTN1. In summary, CTZ reduced the systemic exposure to GBP and its effect on neuropathic pain attenuation. However, CTZ × GBP interaction is not mediated by the renal transporters.

Fast simultaneous quantification of gabapentin and cetirizine in cell lysates by means of HPLC-MS/MS.

A high performance liquid chromatography-tandem mass spectrometry (HPLC-MS/MS) method was successfully developed for the simultaneous detection of gabapentin (GBP) and cetirizine (CTZ) in cell lysates. Multiple reaction monitoring (MRM) transitions were found for GBP, CTZ and deuterated internal standards of both, allowing a selective and sensitive detection. Limits of detection (LODs) of 0.04 ng/mL and 0.07 ng/mL were achieved for CTZ and GBP respectively, and a linear range could be confirmed to the highest tested concentration of 50 ng/mL. Furthermore, with a total runtime of 2.5 min, this method allows a high throughput analysis. The applicability of the method was demonstrated by using it for the quantification of CTZ and GBP in cell lysates to examine the effects of renal transporters on these two analytes.