• 제목/요약/키워드: Carbamazepine-10

검색결과 47건 처리시간 0.023초

Carbamazepine의 임상 약동학 (Clinical Pharmacokinetics of Carbamazepine)

  • 김민정;류윤미;신완균
    • 한국응용약물학회:학술대회논문집
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    • 한국응용약물학회 1996년도 춘계학술대회
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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.

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Stevens-Johnson Syndrome Induced by Carbamazepine Treatment in a Patient Who Previously Had Carbamazepine Induced Pruritus - A Case Report -

  • Bae, Hyun Min;Park, Yoo Jung;Kim, Young Hoon;Moon, Dong Eon
    • The Korean Journal of Pain
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    • 제26권1호
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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.

소아 경련 환자에서 carbamazepine과 oxcarbazepine 치료 시 환자 연령과 약물 용량과 저나트륨혈증의 연관성에 대한 연구 (The age and dose-related hyponatremia during carbamazepine and oxcarbazepine therapy in epileptic children)

  • 이규하;송준혁;차성호;정사준
    • Clinical and Experimental Pediatrics
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    • 제51권4호
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    • pp.409-414
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    • 2008
  • 목 적 : Carbamazepine은 전신 긴장간대 발작과 부분발작에 효과적으로 사용되나 부작용으로 항이뇨 작용과 저 나트륨 혈증이 유발될 수 있다. 또한 oxcarbazepine도 carbamazepine의 케톤 유도체로서 저 나트륨 혈증을 유발 할 수 있다. 이에 저자들은 carbamazepine과 oxcarbazepine을 복용한 환자의 연령, 혈중 carbamazepine 농도, oxcarbazepine의 복용량과 저 나트륨 혈증과의 관계, 저 나트륨 혈증 증상의 유병률에 대한 연구를 시행하였다. 방 법 : 경희대학교 소아청소년과 외래에서 carbamazepine을 단독 투여한 환자와 oxcarbazepine 단독 투여한 환자와 carbamazepine 또는 oxcarbazepine과 다른 항경련제를 병용한 환자 197명을 대상으로 하였다. Carbamazepine을 단독 투여한 군( I군, 67명), oxcarbazepine 단독 투여한 군( II군, 75명), carbamazepine 또는 oxcarbazepine과 다른 항경련제를 병용 투여한 군( III군, 55명)으로 구분하여서 연령과 항경련제 투여 후의 혈중 나트륨 농도를 비교하고 I군에서는 carbamazepine의 혈중 농도와 혈중 나트륨 농도를, II군에서는 oxcarbazepine의 투여 용량과 혈중 나트륨 농도 변화를 비교하였다. 각 그룹의 저 나트륨 혈증의 의한 증상(두통, 구토, 피로감, 경련, 불안, 섬망, 정신 착란)을 기록하였다. 결 과 : 전체 조사 대상의 항경련제 투여 후 저 나트륨 혈증은 41명(20.8%)에서 발견되었고 각각 I군은 12명(17.9%), II군은 17명(22.6%), III군은 12명(21.8%)에서 저 나트륨 혈증이 나타났다. II군과 III군은 항경련제 투여 전과 비교 시 유의한 차이를 보였다(P<0.03). 혈중 나트륨 농도 변화와 환자의 연령 사이에는 통계학적으로 유의한 차이는 없었다. 혈중 carbamazepine 농도 증가와 혈중 나트륨 농도의 변화, oxcarbazepine의 하루 투여량 증가에 따른 혈중 나트륨 농도의 변화 사이에는 통계학적으로 유의한 차이를 보였다(P<0.01). 혈중 농도 135 mEq/L 미만의 저 나트륨 혈증을 보인 41명의 환자 중에서 저 나트륨 혈증 증상을 보인 환자는 7명(17.1%) 였고 혈중 나트륨 농도가 120 mEq/ L 이상 125 mEq/L 이하 인 환자는 5명으로 오심과 구토, 피로감, 두통을 호소하였다. 혈중 나트륨 농도가 120 mEq/L 미만의 2명의 환자들은 반복되는 경련, 의식 혼란, 불안감, 망상 증세를 보였다. 결 론 : Carbamazepine의 단독 투여 시 보다 oxcarbazepine이나 다른 항경련제와 병용 투여 시 저 나트륨 혈증의 발생율이 높았다. 연령과 carbamazepine과 oxcarbazepine 투여 후 혈중 나트륨 농도 사이에는 별 상관 관계가 없는 반면 carbamazepine의 혈중 농도 증가와 oxcarbazepine의 투여량 증가 시 혈중 나트륨 농도가 통계학적으로 의미있게 감소하였다. 혈중 나트륨 농도가 125 mEq/L 미만인 환자에서 심한 임상 증상을 보였다.

Caffeine과 Carbamazepine: 낙동강 수계에서의 검출 및 정수처리 공정에서의 거동 (Caffeine and Carbamazepine: Detection in Nakdong River Basin and Behavior under Drinking Water Treatment Processes)

  • 손희종;염훈식;정종문;장성호;김한수
    • 한국환경과학회지
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    • 제21권7호
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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.

Effect of carbamazepine on tetrodotoxin-resistant Na+ channels in trigeminal ganglion neurons innervating to the dura

  • Han, Jin-Eon;Cho, Jin-Hwa;Nakamura, Michiko;Lee, Maan-Gee;Jang, Il-Sung
    • The Korean Journal of Physiology and Pharmacology
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    • 제22권6호
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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.

카르바마제핀 정제 용출패턴과 용출액 조성과의 상관성 (Relationship Between Dissolution Patterns of Carbamazepine Tablet and Dissolution Medium Composition)

  • 이현태;김정호;김현주;사홍기
    • Journal of Pharmaceutical Investigation
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    • 제34권3호
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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.

Effect of Neurosteroid Modulation on Global Ischaemia-Reperfusion-Induced Cerebral Injury in Mice

  • Grewal, Amarjot Kaur;Jaggi, Amteshwar Singh;Rana, Avtar Chand;Singh, Nirmal
    • The Korean Journal of Physiology and Pharmacology
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    • 제17권6호
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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.

악안면 신경통성 동통의 임상적 특징과 약물 치료 (The Clinical Characteristics and Pharmacologic Treatment of Neuralgic Pain in Maxillofacial Region)

  • Sung-Chang Chung;Sung-Woo Lee;Young-Ku Kim
    • Journal of Oral Medicine and Pain
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    • 제21권1호
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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.

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울산시 상수원수에서의 오존분해 특성 및 의약물질 분해 거동 연구 (Characteristic behaviors of ozone decomposition and oxidation of pharmaceuticals during ozonation of surface waters in Ulsan)

  • 이혜진;이홍신;이창하
    • 상하수도학회지
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    • 제27권1호
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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.