카르바마제핀
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카르바마제핀 속성
- 녹는점
- 191-192 °C (lit.)
- 끓는 점
- 378.73°C (rough estimate)
- 밀도
- 1.1099 (rough estimate)
- 굴절률
- 1.5906 (estimate)
- 인화점
- 9℃
- 저장 조건
- 2-8°C
- 용해도
- 45%(w/v) aq 2-히드록시프로필-β-시클로덱스트린: 가용성29mg/mL
- 산도 계수 (pKa)
- 13.94±0.20(Predicted)
- 물리적 상태
- 크리스탈
- 색상
- 거의 흰색
- 수용성
- 물에 불용성
- Merck
- 14,1781
- BCS Class
- 2
- LogP
- 2.450
- CAS 데이터베이스
- 298-46-4(CAS DataBase Reference)
안전
- 위험 및 안전 성명
- 위험 및 사전주의 사항 (GHS)
위험품 표기 | Xn,T,F | ||
---|---|---|---|
위험 카페고리 넘버 | 42/43-22-20/21/22-39/23/24/25-23/24/25-11 | ||
안전지침서 | 37-24-22-36/37/39-36-45-36/37-16 | ||
유엔번호(UN No.) | UN1230 - class 3 - PG 2 - Methanol, solution | ||
WGK 독일 | 2 | ||
RTECS 번호 | HN8225000 | ||
HS 번호 | 29339900 | ||
유해 물질 데이터 | 298-46-4(Hazardous Substances Data) | ||
독성 | LD50 orally in mice, rats: 3750, 4025 mg/kg (Stenger, Roulet) | ||
기존화학 물질 | KE-04660 |
카르바마제핀 C화학적 특성, 용도, 생산
개요
Carbamazepine is a synthetic iminostilbene derivative structurally similar to imipramine, a tricyclic antidepressant. While unrelated structurally, carbamazepine shares a similar therapeutic action with phenytoin. Carbamazepine was first discovered in 1953 by Swiss chemist Walter Schindler. Throughout the 1960s, antimuscarinic was used and marketed for trigeminal neuralgia and as an anticonvulsant. By the 1970s, it was being used as a mood stabilizer for patients with bipolar disorder.화학적 성질
White or off-white crystalline powder. Soluble in ethanol, acetone, propylene glycol, insoluble in water. Odorless and tasteless.용도
Carbamazepine (CBZ) is a first generation anticonvulsant and mood stabilizing compound that has been used as a therapeutic in the context of neuropathic pain, epilepsy, and affective disorders. It exerts its effects by blocking voltage-gated sodium channels (IC50 = 640 μM), making fewer of these channels available to subsequently open, which leads to decreased high-frequency repetitive firing of action potentials. The estimated IC50 values for inhibition of Nav1.7-, Nav1.3-, and Nav1.8-type channels by CBZ following prolonged inactivation have been reported as 406, 900, and 138 μM, respectively. CBZ can also inhibit L-type Ca2+ channels (IC50 = 974 μM) and has been shown to potentiate GABAA receptors (IC50 >3 mM).정의
ChEBI: Carbamazepine is a dibenzoazepine that is 5H-dibenzo[b,f]azepine carrying a carbamoyl substituent at the azepine nitrogen, used as an anticonvulsant. It has a role as an anticonvulsant, an EC 3.5.1.98 (histone deacetylase) inhibitor, a mitogen, a glutamate transporter activator, an antimanic drug, an analgesic, a non-narcotic analgesic, an environmental contaminant, a xenobiotic, a drug allergen and a sodium channel blocker. It is a dibenzoazepine and a member of ureas.Biological Functions
Carbamazepine has become a major drug in the treatment of seizure disorders. It has high efficacy, is well tolerated by most patients, and exhibits fewer long-term side effects than other drugs.Oral absorption of carbamazepine is quite slow and often erratic. Its half-life is reported to vary from 12 to 60 hours in humans.The development of blood level assays has markedly improved the success of therapy with this drug, since serum concentration is only partially dose related. Carbamazepine is metabolized in the liver, and there is evidence that its continued administration leads to hepatic enzyme induction. Carbamazepine- 10,11-epoxide is a pharmacologically active metabolite with significant anticonvulsant effects of its own.
일반 설명
Certified pharmaceutical secondary standards for application in quality control provide pharma laboratories and manufacturers with a convenient and cost-effective alternative to pharmacopeia primary standards.Carbamazepine is a tricyclic lipophilic compound, with mild anticholinergic activity. It is widely used as an antiepileptic drug for the treatment of simple and complex partial tonic-clonic seizures.
Mechanism of action
In animals, the profile of antiseizure properties for CBZ is similar to that of phenytoin. CBZ is effective in the maximal electroshock (MES) test (electrically induced seizure test) but is ineffective against pentylenetetrazole-induced seizures. It is not effective for absence or myoclonic seizures and, indeed, may exacerbate their onset. Like phenytoin, CBZ acts on voltage-dependent sodium channels to prevent the spread of seizures. CBZ depresses synaptic transmission in the reticular activating system, thalamus, and limbic structures. In a double-blind, crossover study in patients whose seizures were not controlled completely by combinations of AED, CBZ was equal in efficacy to phenobarbital and phenytoin in controlling seizure frequency, and side effects were minimal.Clinical Use
Carbamazepine is an effective agent for the treatment of partial seizures and generalized tonic–clonic seizures; its use is contraindicated in absence epilepsy. Carbamazepine is also useful in the treatment of trigeminal neuralgia and is an effective agent for the treatment of bipolar disorders.Drug interactions
Carbamazepine may be affected by other medicines, such as blood clot preventers and antibiotics. It may also interact with medications used to treat bipolar disorder. Some medications can decrease carbamazepine levels and others can increase carbamazepine levels. Valproate may increase carbamazepine-10,11-epoxide levels, while carbamazepine may decrease the levels of various medications including corticosteroids, clozapine, and lamotrigine. It is important to inform your doctor if you are taking any of these medicines to avoid potential interactions and to ensure carbamazepine works effectively.Taking carbamazepine with other medicines and herbal supplements
What drug-drug interactions should you be vigilant for when someone is prescribed carbamazepine
https://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?setid=c13bc0b8-7900-4ef4-98ed-e1315a08d95d
환경귀착
Carbamazepine is both an important anticonvulsant in therapeutic doses and a powerful proconvulsant in overdose. The therapeutic anticonvulsant mechanism is primarily related to blockade of presynaptic voltage-gated sodium channels. Blockade of the sodium channels is believed to inhibit the release of synaptic glutamate and possibly other neurotransmitters. Carbamazepine is also a powerful inhibitor of the muscarinic and nicotinic acetylcholine receptors, N-methyl-Daspartate (NMDA) receptors, and the central nervous system (CNS) adenosine receptors. In addition, carbamazepine is structurally related to the cyclic antidepressant imipramine and in massive overdose, it may affect cardiac sodium channels.카르바마제핀 준비 용품 및 원자재
원자재
준비 용품
카르바마제핀 공급 업체
글로벌( 729)공급 업체
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APOLLO HEALTHCARE RESOURCES | +6596580999 |
sales@apollo-healthcare.com.sg | Singapore | 400 | 58 |
Shanghai Likang New Materials Co., Limited | +86-16631818819 +86-17736933208 |
3684455296@qq.com | China | 9311 | 58 |
Hebei Chuanghai Biotechnology Co,.LTD | +86-13131129325 |
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Hong Kong Excellence Biotechnology Co., Ltd. | |
ada@sh-teruiop.com | China | 882 | 58 |
Changzhou Rokechem Technology Co., Ltd. | 18758118018 |
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Henan Bao Enluo International TradeCo.,LTD | +86-17331933971 +86-17331933971 |
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Nantong Guangyuan Chemicl Co,Ltd | +undefined17712220823 |
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Henan Fengda Chemical Co., Ltd | +86-371-86557731 +86-13613820652 |
info@fdachem.com | China | 20291 | 58 |
Sigma Audley | +86-15937194204 +86-18126314766 |
nova@sh-teruiop.com | China | 491 | 58 |
Hangzhou Hyper Chemicals Limited | +86-0086-57187702781 +8613675893055 |
info@hyper-chem.com | China | 295 | 58 |
카르바마제핀 관련 검색:
벤즈아마이드 카르바마제핀
Chlorantraniliprole
10-METHOXY CARBAMAZEPINE
10,11-DIHYDROCARBAMAZEPINE
Carbamazepine(anbromine),Carbamazepine nonbromo
3-chloroiminodibenzyl (intermediate of carbamazepine)
METHYL N-4-BOC-N-1-CBZ-2-PIPERAZINECARBOXYLATE
Iminostilbene
CARBAMAZEPINE IMPURITY A
Carbamazepine-D2
CARBAMAZEPINE 10,11-EPOXIDE,carbamazepine10,11-oxid
3-Hydroxy Carbamazepine
CARBAMAZEPINE-13C,D2
CARBAMAZEPINE-D2,15N
CARBAMAZEPINE-13C1,15N1
2-Hydroxy Carbamazepine
CARBOXAMIDE