• Proceedings of the Korean Society of Applied Pharmacology
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• 1996.04a
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• pp.280-280
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• 1996

carbamazepine은 대표적인 항전간제로써, 약물의 유효 혈중 농도 범위가 좁아서 TDM(Theapeutic Drug Monitoring)을 시행하는 약물이다. 그리고 이 약물은 parent drug 뿐만 아니라 대사체의 하나인 carbamazepine-10,11-epoxide 역시 carbamazepine와 동일한 효과가 있는 것으로 알려져 있어, 임상적으로 TDM 시행시에는 carbamazepine의 carbamazepine-10,11-epoxide로의 대사에 소요되는 시간과 대사 정도에 대한 자료가 필요하다. 그러나 이제껏 제시되고 있는 population parameter들이 모두 서양인에 대한 자료이므로 국내에서 이 약물을 투여하는데 있어서 인종간의 차이를 확인하지 않고서 서양인의 자료에 준하여 적용하는 것은 상당한 위험성이 따를 수도 있으므로 한국인에 있어서의 carbamazepine 대사에 관한 연구가 필요하였다. 방법 7명의 건강한 성인을 대상으로 carbamazepine 제제 400mg을 1회 경구 투여한 다음, 0, 0.5, 1, 2, 3, 4, 6, 8, 12, 24, 36, 48, 72 시간 경과시 채혈하여 정량하였다. 결과 carbamazepine의 AUC 881$\pm$233(minㆍ$\mu\textrm{g}$/$m\ell$), MRT 72.1$\pm$10.8(min), t$_{1}$2/ 40.1 $\pm$ 8.6(min), CL 6.75 $\pm$ 2.72($m\ell$/min/kg), Vdssn 484 $\pm$ 215($m\ell$/kg)의 값을 얻었다.

• The Korean Journal of Pain
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• v.26 no.1
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• pp.80-83
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• 2013

Stevens-Johnson syndrome (SJS) is a rare but life-threatening skin reaction disease and carbamazepine is one of its most common causes. We report a case of SJS secondary to carbamazepine in a patient with previous pruritus due to carbamazepine which was given for treatment of trigeminal neuralgia. We would like to caution all providers that carbamazepine readministration should be avoided in the patient with a previous history of SJS or adverse skin reaction. In addition, we strongly recommend gradual titration when initiating treatment with carbamazepine.

• Clinical and Experimental Pediatrics
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• v.51 no.4
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• pp.409-414
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• 2008

Purpose : To assess the prevalence of hyponatremia in epileptic children receiving carbamazepine or oxcarbazpine, we investigate serum sodium changes according to age, serum carbamazepine level, and daily oxcarbazepine dosage, and the prevalence of symptoms of hyponatremia. Methods : We reviewed the clinical data of the 197 children receiving carbamazepine and/or oxcarbazepine with or without antiepileptic therapy. And these were classified into the carbamazepine treated patients (group I), oxcarbazepine treated patients (group II), and carbamzepine or oxcarbazepine with other antiepileptics treated patients (group III). Potentially predictive values for development of hyponatremia were examined in each group: age, plasma level of carbamazepine and daily dosage of oxcarbazepine. We assessed the symptoms of hyponatremia. Results : The overall prevalence of hyponatremia was 20.8% (group I, II and III : 17.9%, 22.6%, and 21.8%, respectively), and the prevalence in groups II and III compared with controls (P<0.03) was significantly lower. The changes of serum sodium levels relation to age were not significantly different. The changes of serum sodium levels by increasing of serum levels of carbamazepine and dosage of oxcarbazepine were statistically significant (P<0.01). Among the 41 patients who had biochemical hyponatremia, the prevalence of hyponatremic symptoms was 17.1%. Conclusion : Hyponatremia may occur relatively more frequently with oxcarbazepine or combined other antiepileptics than carbamzepine therapy only. Age of children receiving carbamazepine or oxcarbazepine was no predictive value for occurrence of hyponatremia. The patients whose serum level were less than 125 mEq/L showed more severe clinical symptoms than any other study groups.

• Journal of Environmental Science International
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• v.21 no.7
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• pp.837-843
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• 2012

The aims of this study were to investigated the occurrence of caffeine and carbamazepine in Nakdong river basin (8 mainstreams and 2 tributaries) and the behavior of caffeine and carbamazepine under drinking water treatment processes (conventional and advanced processes). The examination results showed that caffeine was detected at all sampling sites (5.4~558.5 ng/L), but carbamazepine was detected at five sampling sites (5.1~79.4 ng/L). The highest concentration level of caffeine and carbamazepine in the mainstream and tributaries in Nakdong river were Goryeong and Jinchun-cheon, respectively. These pharmaceutical products were completely removed when they were subject to conventional plus advanced processes of drinking water treatment processes. Conventional processes of coagulation, sedimentation and sand-filtration were not effective for their removal, while advanced processes of ozonation and biological activated carbon (BAC) filtration were effective. Among these pharmaceuticals, carbamazeoine was more subject to ozonation than caffeine.

• 대한임상약리학회:학술대회논문집
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• 1996.12a
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• pp.34-34
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• 1996

• The Korean Journal of Physiology and Pharmacology
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• v.22 no.6
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• pp.649-660
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• 2018

Migraine is a neurological disorder characterized by recurrent and disabling severe headaches. Although several anticonvulsant drugs that block voltagedependent $Na^+$ channels are widely used for migraine, far less is known about the therapeutic actions of carbamazepine on migraine. In the present study, therefore, we characterized the effects of carbamazepine on tetrodotoxin-resistant (TTX-R) $Na^+$ channels in acutely isolated rat dural afferent neurons, which were identified by the fluorescent dye DiI. The TTX-R $Na^+$ currents were measured in medium-sized DiIpositive neurons using the whole-cell patch clamp technique in the voltage-clamp mode. While carbamazepine had little effect on the peak amplitude of transient $Na^+$ currents, it strongly inhibited steady-state currents of transient as well as persistent $Na^+$ currents in a concentration-dependent manner. Carbamazepine had only minor effects on the voltage-activation relationship, the voltage-inactivation relationship, and the use-dependent inhibition of TTX-R $Na^+$ channels. However, carbamazepine changed the inactivation kinetics of TTX-R $Na^+$ channels, significantly accelerating the development of inactivation and delaying the recovery from inactivation. In the current-clamp mode, carbamazepine decreased the number of action potentials without changing the action potential threshold. Given that the sensitization of dural afferent neurons by inflammatory mediators triggers acute migraine headaches and that inflammatory mediators potentiate TTX-R $Na^+$ currents, the present results suggest that carbamazepine may be useful for the treatment of migraine headaches.

• Journal of Pharmaceutical Investigation
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• v.34 no.3
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• pp.185-192
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• 2004

The objective of this study was to evaluate the effects of surfactant type and concentration upon dissolution rates of carbamazepine from an immediate-release tablet. The dissolution media used in this study were aqueous solutions containing 0.1-2% sodium lauryl sulfate, cetyltrimethylammonium bromide, or polysorbate 80. The solubility of carbamazepine in the dissolution media was determined at first. A dissolution study was then conducted by using the USP dissolution apparatus II (paddle method) with an agitation rate of 75 rpm. Aliquots of the dissolution media were taken at predetermined time intervals, and the amount of carbamazepine dissolved was measured spectrophotometrically at 285 nm. The dissolution data obtained were fitted into a biphasic exponential equation with four parameters. Excellent correlations were observed between the experimental data and the theoretical ones predicted by the equation. This equation permitted the calculation of $T_{50%}$ (the time required for dissolving 50% of carbamazepine) under various experimental conditions. Differentiation of the equation also led to the attainment of dissolution rates at dissolution time points. The addition of a surfactant to an aqueous solution led to increasing the solubility of carbamazepine by 3- to 12-folds, depending upon its type and concentration. This event also resulted in enhancing the magnitude of a sink condition during the dissolution study. As a result, the dissolution rate of carbamazepine was affected by the aqueous surfactant concentration in a proportional manner. Subsequently, $T_{50%}$ values declined rapidly, as the surfactant concentration increased. Such effects were observed in decreasing order of sodium lauryl sulfate, cetyltirmethylammonium bromide, and polysorbate 80. These results clearly demonstrated that it was possible to tailor a dissolution rate and $T_{50%}$ of carbamazepine by manipulating the type and concentration of a surfactant. Relevant information would be beneficial to setting up dissolution specifications for poorly water-soluble drug products.

• The Korean Journal of Physiology and Pharmacology
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• v.17 no.6
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• pp.485-491
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• 2013

The present study was designed to investigate the putative effect of neurosteroid modulation on global ischaemia-reperfusion-induced cerebral injury in mice. Bilateral carotid artery occlusion followed by reperfusion, produced a significant rise in cerebral infarct size along with impairment of grip strength and motor coordination in Swiss albino mice. Administration of carbamazepine (16 mg/kg, i.p.) before global cerebral ischaemia significantly attenuated cerebral infarct size and improved the motor performance. However, administration of indomethacin (100 mg/kg, i.p.) attenuated the neuroprotective effect of carbamazepine. Mexiletine (50 mg/kg, i.p.) did not produce significant neuroprotective effect. It may be concluded that the neuroprotective effect of carbamazepine may be due to increase in synthesis of neurosteroids perhaps by activating enzyme ($3{\alpha}$ HSD) as indomethacin attenuated the neuroprotective effect of carbamazepine. The sodium channel blocking effect of carbamazepine may not be involved in neuroprotection as mexiletine, a sodium channel blocker, did not produce significant neuroprotective effect.

• Journal of Oral Medicine and Pain
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• v.21 no.1
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• pp.173-182
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• 1996

This study was performed to provide the information on the clinical characteristics of the most common paroxysmal pain disorder in maxillofacial region, trigeminal neuralgia, and the effects and side effects of carbamazepine. The patients who visited Orofacial Pain Clinic, Dept. of Oral Diagnosis, Seoul National University Dental Hospital for treating paroxysmal pain were studied by history taking, clinical examination, and radiography. Sixty-two patients(male 20, female42) without any clinical and radiological abnormalities were Included. The change of pain, blood tests, and side effects were investigated periodically after administration of carbamazepine. The obtained results were as follows : 1. Almost all patient with trigeminal neuralgia were over the age of forties and it was more common in women. 2. Trigeminal neuralgia was more right sided and the involved nerve was in the order of maxillary n., mandibular n., and ophthalmic n. 3. The mean duration of suffering was 20.7 months. Eighty percent of patients had apparent trigger area. 4. The duration of pain attack was in the older of several seconds, 1 min. to 5 min., more than 10 min., and 5 min. to 10 min. The frequency of pain attack was in the order of more than 10 per day, 6-10 per day, and 1-5 per day. 5. The clinic the patients had visited for reducing neuralgic pain was in the order of dental clinic, neurology, oriental medicine, otolaryngology, and pharmacy. 6. Unnecessary dental treatments for reducing neuralgic pain were performed in 41.9% of the patients. Almosit all treatments were irreversible ones such as endodontic treatment and tooth extraction. 7. The initial mean VAS was 8.6, but it was decreased to 3.8 after 1 month, to 2.7 after 2 months. Almost all patients showed decreased pain with 200-600mg/day of carbamazepine to 6 months. 8. WBC counts, especially neutrophil counts, was decreased in 1 week after administration of carbamazepine but reached initial level after 1 month. SGOT, SGPT, and creatinine did not show any significant change. 9. Blood pressure was not changed significantly after administration of carbamazepine. 10. Almost patients did not show any apparent side effects, but drowsiness, dizziness, skin itching, constipation, and gastric irritation were occurred in some patients.

• Journal of Korean Society of Water and Wastewater
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• v.27 no.1
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• pp.39-47
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• 2013

This study demonstrates the oxidative degradation of pharmaceutical compounds during ozonation of surface waters in Ulsan. Diclofenac, carbamazepine, bezafibrate, and ibuprofen were selected as surrogate pharmaceutical compounds, and ozonation experiments were performed using raw waters collected from the Sayeon Dam and the Hoeya Dam in Ulsan. Diclofenac and carbamazepine which have high reactivity with molecular ozone showed higher removal efficiencies than bezafibrate and ibuprofen during ozonation. The addition of tert-butanol, a hydroxyl radical scavenger, increased the removal efficiencies of diclofenac and carbamazepine by increasing the ozone exposure. However, the oxidation of bezafibrate and ibuprofen was inhibited by the presence of tert-butanol due to the suppression of the exposure to hydroxyl radical. The elimination of the selected pharmaceuticals could be successfully predicted by the kinetic model base on the $R_{ct}$ concept. Depending on the experimental condition, $R_{ct}$ values were determined to be $(1.54{\sim}3.32){\times}10^{-7}$ and $(1.19{\sim}3.04){\times}10^{-7}$ for the Sayeon Dam and the Hoeya Dam waters, respectively. Relatively high $R_{ct}$ values indicate that the conversion of $O_3$ into $^{\cdot}OH$ is more pronounced for surface waters in Ulsan compared to other water sources.