Carbamazepine

Al-Rashood, Sara T.

doi:10.1016/bs.podrm.2015.11.001

Cited by 42 publications

(22 citation statements)

References 290 publications

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“…Carbamazepine is believed to induce the UGT2B7 isoform . Autoinduction of carbamazepine metabolism produces a variable t ½ ; the t ½ of the carbamazepine parent drug after multiple doses ranges from 10 to 20 hours …”

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confidence: 99%

Evaluation of the Pharmacokinetic Interaction Between the Voltage‐ and Use‐Dependent Nav1.7 Channel Blocker Vixotrigine and Carbamazepine in Healthy Volunteers

Dunbar

Versavel

Tate

et al. 2019

Clinical Pharm in Drug Dev

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Vixotrigine is a voltage-and use-dependent Nav1.7 channel blocker under investigation for the treatment of peripheral neuropathic pain conditions, including trigeminal neuralgia. Vixotrigine is metabolized primarily via uridine diphosphateglucuronosyltransferases (UGTs). Carbamazepine, a UGT and cytochrome P450 3A4 inducer, is a first-line treatment for trigeminal neuralgia. We conducted a double-blind, randomized, placebo-controlled, parallel-group, single-center phase 1 study to investigate the impact of coadministering vixotrigine and carbamazepine on their respective pharmacokinetics (PK) in healthy volunteers, the safety and tolerability of combined treatment, and PK recovery of vixotrigine following carbamazepine discontinuation. Randomly assigned treatments were carbamazepine (100 mg twice a day, days 1-3 and 200 mg twice a day, days 4-21) or placebo on days 1 to 21. All volunteers received vixotrigine 150 mg 3 times a day on days 16 to 28. At prespecified times, whole-blood samples were collected for PK assessment. Statistical analyses were performed on the log-transformed PK parameters area under the concentration-time curve within a dosing interval (AUC 0-tau ) and maximum observed concentration (C max ) for vixotrigine, carbamazepine, and metabolites. Vixotrigine AUC 0-tau and C max were reduced by 31.6% and 26.3%, respectively, when coadministered with carbamazepine compared with placebo. Seven days after carbamazepine discontinuation, vixotrigine AUC 0-tau and C max remained 24.5% and 21.4% lower compared with placebo. Carbamazepine AUC 0-tau and C max were <10% lower when coadministered with vixotrigine compared on days 15 and 21. Vixotrigine/carbamazepine coadministration was well tolerated. These results suggest that vixotrigine does not have an effect on carbamazepine PK, and although carbamazepine has an effect on the exposure of vixotrigine, the effect is not considered clinically relevant.

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confidence: 99%

Evaluation of the Pharmacokinetic Interaction Between the Voltage‐ and Use‐Dependent Nav1.7 Channel Blocker Vixotrigine and Carbamazepine in Healthy Volunteers

Dunbar

Versavel

Tate

et al. 2019

Clinical Pharm in Drug Dev

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“…Carbamazepine is a classic anticonvulsant frequently used for epilepsy treatment, psychiatric disorders and neuropathic pain (Alrashood, 2016). However, the prolonged use of CBZ is associated with side effects such as metabolic alteration and endocrine disturbance (Fumel et al., 2012; Lai et al., 2013; Orth, 1984), particularly with alterations in the thyroid function.…”

Section: Discussionmentioning

confidence: 99%

Thyroid hormones, Sertoli cell proliferation and differentiation in progenies from carbamazepine‐treated rat dams during pregnancy and lactation

et al. 2021

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Carbamazepine (CBZ) is used in the control of seizure and affective disorders, causing hypothyroidism. Thyroid hormones regulate the Sertoli cell proliferation and differentiation. Clinical aspects must be considered since epileptic fertile women need to continuously use CBZ during pregnancy and lactation. This study aimed to evaluate the effects of CBZ on testis development of rat offspring from dams treated during pregnancy/lactation. Rat dams received CBZ (20 mg kg−1 day−1) or vehicle by intra‐peritoneal route during gestation and lactation. Progenies were euthanised at 4, 14, 41, 63 and 93‐days post‐partum (dpp) for the evaluation of T3, T4 and TSH plasma total levels. Testicular cross sections were submitted to anti‐Ki67, anti‐PCNA, anti‐p27kip1 and anti‐transferrin immunolabelling for the evaluation of Sertoli cells. There was a significant reduction in p27kip1‐positive Sertoli cell numerical densities and an increase in TSH level at 14 dpp. CBZ exposure affected the volume density of transferrin‐positive immunolabelling at 63 dpp. These results suggest that CBZ may cause a dysregulation of the controller system of thyroid hormones homeostasis leading to an increase in the proliferation rate at the neonatal phase and a differentiation delay of the Sertoli cell, culminating in an altered function at late puberty. The occurrence of hypothyroidism cannot be completely discarded.

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“…Gabapentin has been shown to be effective in the treatment of this syndrome [11][12][13] . Carbamazepine is also indicated for neuropathic pain in the head and neck region 14 . Blockade of the somatic nerve or sympathetic ganglion is performed in more complex and refractory cases of the syndrome 3 .…”

Section: Discussionmentioning

confidence: 99%

Complex regional pain syndrome in the orofacial region. Case report

Santos¹,

Sales²,

Asano³

et al. 2018

Brazilian Journal of Pain

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BACKGROUND AND OBJECTIVES: The complex regional pain syndrome is characterized by presenting autonomic, sensory and motor difficult to control changes of the chronic evolution. Its pathophysiology and treatment are not fully defined, and the search for an increasingly effective treatment is a subject of medical concern. The involvement of the orofacial region has an even rarer incidence, and the literature reports only 14 cases in five decades. The objective of this report was to warn physicians and researchers about the importance of a correct diagnosis and to show the possibility of controlling this dysfunction with conservative treatment. CASE REPORT: A 68-year-old female patient, who after a facial trauma and three subsequent surgical procedures, developed orofacial complex regional pain syndrome. Several therapeutic regimens were performed, and after the last one she became completely asymptomatic: oxcarbazepine (900mg/day), morphine-controlled liberation (120mg/day), fluoxetine (40mg/day) and clonazepam (2mg/day), electrotherapy and oral rehabilitation. CONCLUSION: The diagnosis criteria for complex regional pain syndrome recommended by the International Association for the Study of Pain, revised in 2007, should be followed. The treatment of this neuropathic syndrome includes anticonvulsants, tricyclics, opioids, electrotherapy and somatic and stellate ganglion block, the latter when the pain is maintained by the sympathetic nervous system. In this report of an orofacial complex regional pain syndrome II, pain control was shown without the need for sympathetic ganglion block, which can be a warning to the medical class to a correct diagnosis and an effective and less invasive treatment.RESUMO JUSTIFICATIVA E OBJETIVOS: A síndrome complexa de dor regional se caracteriza por apresentar alterações autonômicas, sensitivas e motoras de evolução crônica de difícil controle. Sua fisiopatologia não está totalmente definida e a busca por um tratamento cada vez mais eficaz é objeto de preocupação médica. O comprometimento da região orofacial tem uma incidência ainda mais rara e a literatura relata apenas 14 casos em cinco décadas. O objetivo deste relato foi alertar médicos e pesquisadores para a importância de um diagnóstico correto e mostrar a possibilidade de controle dessa disfunção com o tratamento conservador. RELATO DO CASO: Paciente do sexo feminino, 68 anos, após trauma facial e três intervenções cirúrgicas posteriores, desenvolveu quadro de síndrome complexa de dor regional orofacial. Foram realizados vários esquemas terapêuticos, o último dos quais tornou-a completamente assintomática: oxcarbazepina (900mg/dia), morfina de liberação controlada (120mg/dia), fluoxetina (40mg/dia) e clonazepam (2mg/dia), eletroterapia e reabilitação oral. CONCLUSÃO: Os critérios de diagnóstico para a síndrome complexa de dor regional, preconizados pela International Association for the Study of Pain, revisados em 2007, devem ser seguidos. O tratamento desta síndrome neuropática inclui anticonvulsivantes, tricíclicos e opioide...

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Carbamazepine

Cited by 42 publications

References 290 publications

Evaluation of the Pharmacokinetic Interaction Between the Voltage‐ and Use‐Dependent Nav1.7 Channel Blocker Vixotrigine and Carbamazepine in Healthy Volunteers

Evaluation of the Pharmacokinetic Interaction Between the Voltage‐ and Use‐Dependent Nav1.7 Channel Blocker Vixotrigine and Carbamazepine in Healthy Volunteers

Thyroid hormones, Sertoli cell proliferation and differentiation in progenies from carbamazepine‐treated rat dams during pregnancy and lactation

Complex regional pain syndrome in the orofacial region. Case report

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