Bupivacaine

Bupivacaine 속성

Bupivacaine C화학적 특성, 용도, 생산

용도

Like lidocaine and mepivacaine, bupivacaine is used in infiltration, spinal, and epidural anesthesia in blocking nerve transmission. Its most distinctive property is its long-lasting action. It is used for surgical intervention in urology and in lower thoracic surgery from 3 to 5 h in length, and in abdominal surgery lasting from 45 to 60 min. It is used to block the trifacial nerve, the sacral and brachial plexuses, in resetting dislocations, in epidural anesthesia, and during Cesarian sections.

일반 설명

Bupivacaine was synthesized simultaneously with mepivacainein 1957 but was at first overlooked because of the increasedtoxicity compared with mepivacaine. When themethyl on the cyclic amine of mepivacaine is exchanged fora butyl group the lipophilicity, potency and the duration ofaction all increase. Literature reports of cardiovascular toxicity,including severe hypotension and bradycardia, areabundant in the literature.91 Bupivacaine is highly bound toplasma proteins (95%), and thus the free concentration mayremain low until all of the protein binding sites are occupied.After that point, the plasma levels of bupivacaine rise rapidlyand patients may progress to overt cardiac toxicity withoutever showing signs of CNS toxicity. The cardiotoxicity ofbupivacaine is a result of its affinity to cardiac tissues and itsability to depress electrical conduction and predispose theheart to reentry types of arrhythmias. The cardiotoxicity ofbupivacaine was found to be significantly more prominentwith the “R” isomer, or the racemic mixture, thus the “S”stereoisomer is now on the market as levobupivacaine.

Mechanism of action

Bupivacaine is a local anaesthetic containing a chiral centre and adopts dextro and laevo forms. The enantiopure l form is less cardio- and neurotoxic and has an equivalent potency to the racemic mixture; therefore levobupivacaine is often preferred to reduce the potential for toxicity. Stereoselectivity describes the differences in response at a given receptor for the different enantiomers (such as the response discussed for S(+) ketamine). The opioid and NMDA receptors also exhibit stereoselectivity.

Pharmacology

Bupivacaine is a chiral compound used clinically for 50 years, with a slower onset, greater potency and longer duration of action than lidocaine. Initial benefits of bupivacaine were sensory–motor separation and minimal tachyphylaxis, unlike repeated doses of lidocaine. However, it has greater potential for cardiac toxicity, related to its avid binding to and slow dissociation from cardiac N a+ channels. Inadvertent intravenous administration may result in systemic toxicity (see later), and it is contraindicated for intravenous regional anaesthesia.
Bupivacaine is commonly used for epidural administration in obstetrics and postoperative pain management. A hyperbaric preparation containing 80 mg ml^-1 glucose is available for spinal anaesthesia.

부작용

Common side effects of bupivacaine include:
weakness, long-lasting numbness or tingling;
feeling restless or drowsy;
tremors;
headache, blurred vision;
fast or slow heartbeats;
breathing problems;
chills or shivering;
back pain;
nausea, vomiting.

Bupivacaine 준비 용품 및 원자재

원자재

준비 용품

Bupivacaine 공급 업체

공급자	전화	이메일	국가	제품 수	이점
Jinan Jianfeng Chemical Co., Ltd	0531-88110457; +8615562555968	info@pharmachemm.com	China	246	58
Wuhan Haorong Biotechnology Co.,ltd	+8618565342920	sales@chembj.net	China	269	58
Shanghai Aosiris new Material Technology Co., LTD	+8615139564871	wrjmoon2000@163.com	China	354	58
Firsky International Trade (Wuhan) Co., Ltd	+8615387054039	admin@firsky-cn.com	China	436	58
shandong perfect biotechnology co.ltd	+86-53169958659; +8618596095638	sales@sdperfect.com	China	294	58
Xiamen Wonderful Bio Technology Co., Ltd.	+8613043004613	Sara@xmwonderfulbio.com	China	305	58
Hebei Xinsheng New Material Technology Co., LTD.	+86-16632316109	xinshengkeji@xsmaterial.com	China	1100	58
Nantong Guangyuan Chemicl Co,Ltd	+undefined17712220823	admin@guyunchem.com	China	616	58
Sigma Audley	+86-18336680971 +86-18126314766	nova@sh-teruiop.com	China	524	58
Hubei XinRunde Chemical Co., Ltd.	+8615102730682	bruce@xrdchem.cn	CHINA	566	55

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