아세트아미노펜

아세트아미노펜 속성

아세트아미노펜 MSDS

4-Acetamidophenol

아세트아미노펜 C화학적 특성, 용도, 생산

물성

백색 결정 또는 결정 성 분말.

개요

이 제품은 아세트 아닐리드 해열 진통제입니다. 시냅스 온도 조절 센터의 시냅스에서 링 옥시 다제와 선택성을 억제함으로써 말초 혈관 확장, 발한 및 해열 효과에서 프로스타글란딘의 합성, 아스피린과 유사한 해열 효과의 강도.

용도

1. 해열 진통제, 아세트아미노펜 이라는 국제 비 독점 약품. 그것은 가장 일반적으로 사용되는 비 항염증제 해열 진통제, 해열제와 유사 아스피린, 진통 효과가 약한, 아니 안티 류마티스 효과의 안티 염증, 아세트 아닐리드 약물의 최고의 품종입니다. 카르 복실 산에 특히 적합한 약물 환자는 사용할 수 없습니다. 일반적인 감기, 치통 색전증. 아세트 아미노펜은 유기 합성, 과산화수소 안정제, 사진 화학 물질의 중간체입니다.

개요

Acetaminophen differs from the nonsteroidal anti-inflammatory agents described in that it is devoid of anti-inflammatory and antirheumatic properties. It was recently shown that acetaminophen, like aspirin, inhibits cyclooxygenase action in the brain and is even stronger than aspirin. On the other hand, the mechanism of analgesic action of acetaminophen is not fully clear, since it acts poorly on peripheral cyclooxygenase.

화학적 성질

White Solid

용도

Acetaminophen is widely used as an analgesic and fever-reducing agent. Acetaminophen is designed for moderate analgesia. It is also effective like aspirin and is used in analgesia for headaches (from weak to moderate pain), myalgia, arthralgia, chronic pain, for oncological and post-operational pain, etc.

Indications

Acetaminophen (Tylenol) is an effective antipyretic and analgesic that is well tolerated at therapeutic doses. It has only weak antiinflammatory activity; thus, it is not useful in the treatment of rheumatoid arthritis and other inflammatory conditions.

World Health Organization (WHO)

Paracetamol, a widely used analgesic and antipyretic is known, in case of overdose, to cause liver damage, frequently with fatal outcome. In recommended dosages this risk does not occur. Paracetamol is listed in the WHO Model List of Essential Drugs.

일반 설명

Odorless white crystalline solid. Bitter taste. pH (saturated aqueous solution) about 6.

공기와 물의 반응

Slightly soluble in water.

반응 프로필

Acetaminophen is sensitive to light. Incompatible with strong oxidizers. 

화재위험

Flash point data for Acetaminophen are not available; however, Acetaminophen is probably combustible.

생물학적 활성

Cyclooxygenase inhibitor; may be selective for COX-3 (IC 50 values are 460, > 1000 and > 1000 μ M for canine COX-3, and murine COX-1 and COX-2 respectively). Widely used analgesic and antipyretic agent.

Mechanism of action

The mechanism of action of paracetamol is not well understood, but it may act in a similar fashion to NSAIDs, with inhibition of cyclo-oxygenase enzymes COX-1 and COX-2 to reduce the phenoxyl radical formation required for COX-1 and 2 activity and prostaglandin synthesis. I t has selectivity for inhibition of prostaglandin synthesis with low concentrations of peroxidases and arachidonic acid, but limited effect at higher concentrations and, therefore, has limited anti-inflammatory effects. Unlike opioids, paracetamol has no well-defined endogenous binding sites. I n some circumstances, it may exhibit a preferential effect on COX-2 inhibition. There is growing evidence of a central antinociceptive effect of paracetamol. It has also been found to prevent prostaglandin production at the cellular transcriptional concentration, independent of COX activity.

Pharmacokinetics

Paracetamol is absorbed rapidly from the small intestine after oral administration; peak plasma concentrations are reached after 30–60min. It may also be given rectally and intravenously (either as paracetamol or the prodrug propacetamol). It has good oral bioavailability (70%–90%); rectal absorption is more variable (bioavailability ~50%–80%) with a longer time to reach peak plasma concentration. The plasma half-life is approximately 2–3 h.
Paracetamol is metabolised by hepatic microsomal enzymes mainly to the glucuronide, sulphate and cysteine conjugates. None of these metabolites is pharmacologically active. Aminimal amount of the metabolite N-acetyl-pamino- benzoquinone imine is normally produced by cytochrome P450– mediated hydroxylation. This reactive toxic metabolite is rendered harmless by conjugation with liver glutathione, then excreted renally as mercapturic derivatives. With larger doses of paracetamol, the rate of formation of the reactive metabolite exceeds that of glutathione conjugation, and the reactive metabolite combines with hepatocellular macromolecules, resulting in cell death and potentially fatal hepatic failure. The formation of this metabolite is increased by drugs inducing cytochrome P450 enzymes, such as barbiturates or carbamazepine.

Clinical Use

Acetaminophen is weakly acidic (pKa = 9.51) and synthesized by the acetylation of p-aminophenol. It is weakly bound to plasma proteins (18–25%). Acetaminophen is indicated for use as an antipyretic/analgetic, particularly in those individuals displaying an allergy or sensitivity to aspirin. It does not possess anti-inflammatory activity, but it will produce analgesia in a wide variety of arthritic and musculoskeletal disorders. It is available in various formulations, including suppositories, tablets, capsules, granules, and solutions. The usual adult dose is 325 to 650 mg every 4 to 6 hours. Doses of greater than 2.6 g/day are not recommended for long-term therapy because of potential hepatotoxicity issues. Acetaminophen, unlike aspirin, is stable in aqueous solution, making liquid formulations readily available, a particular advantage in pediatric cases.

신진 대사 경로

Acetaminophen (APAP) is metabolized by mice, and nine metabolites are identified in the urine. The main metabolites are APAP-glucuronide and 3-cysteinyl- APAP. Hydroquinone metabolites of S-(2,5- dihydroxyphenyl)cysteine and S-(2,5-dihydroxyphenyl)- N-acetylcysteine result from the benzoquinone metabolite of APAP.

신진 대사

acetaminophen is undergoes rapid first-pass metabolism in the GI tract primarily by conjugation reactions, with the O-sulfate conjugate being the primary metabolite in children and the O-glucuronide being the primary metabolite in adults. A minor, but significant, product of both acetaminophen and phenacetin is the N-hydroxyamide produced by a CYP2E1 and CYP3A4.

Purification Methods

Recrystallise Paracetamol from water or EtOH. The 3,5-dinitrobenzamide complex gives orange crystals from hot H2O and has m 171.5o. [Beilstein 13 H 460, 13 I 159, 13 II 243, 13 III 1056, 13 IV 1091.]

아세트아미노펜 준비 용품 및 원자재

원자재

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아세트아미노펜 공급 업체

공급자	전화	이메일	국가	제품 수	이점
Hebei Miaoyin Technology Co.,Ltd	+86-17367732028 +86-17367732028	kathy@hbyinsheng.com	China	3582	58
Hubei Ipure Biology Co., Ltd	+8613367258412	ada@ipurechemical.com	China	10326	58
Hebei Guanlang Biotechnology Co., Ltd.	+86-19930503282	alice@crovellbio.com	China	8822	58
Wuhan Aoliqisi New Material Technology Co., Ltd.	+86-13545906766; +8613545906766	sales@whaop.com	China	265	58
ZHEJIANG JIUZHOU CHEM CO., LTD	+86-0576225566889 +86-13454675544	admin@jiuzhou-chem.com；jamie@jiuzhou-chem.com；alice@jiuzhou-chem.com	China	20000	58
Wuhan Haorong Biotechnology Co.,ltd	+8618565342920	sales@chembj.net	China	269	58
Hebei Mojin Biotechnology Co., Ltd	+8613288715578	sales@hbmojin.com	China	12453	58
Shanghai Affida new material science and technology center	+undefined15081010295	2691956269@qq.com	China	359	58
Hebei Yanxi Chemical Co., Ltd.	+8617531190177	peter@yan-xi.com	China	5993	58
Nanjing Deda New Material Technology Co., Ltd	+8613223293093	bella@njdeda.com	China	81	58

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