1-AdaMantanethylaMine

한글명:1-AdaMantanethylaMine

카스 번호13392-28-4

상품명:1-AdaMantanethylaMine

CBNumberCB7122907

분자식C12H21N

포뮬러 무게179.3

MOL 파일13392-28-4.mol

화학적 성질

끓는 점	248°C
밀도	1.033
인화점	99°C
저장 조건	Store at -20°C
용해도	DMSO에 용해됨
산도 계수 (pKa)	11.17±0.29(Predicted)
CAS 데이터베이스	13392-28-4(CAS DataBase Reference)
NIST	1-Adamantanemethylamine, «alpha»-methyl-(13392-28-4)

위험 및 안전 성명

위험 등급	IRRITANT
HS 번호	2902190000
유해 물질 데이터	13392-28-4(Hazardous Substances Data)

그림문자(GHS)

1-AdaMantanethylaMine 화학적 특성, 용도, 생산

용도
Rimantadine act by blocking the M2 ion channel which is required for uptake of protons into the interior of the virus to permit acid-promoted viral uncoating (decapsidation).
일반 설명
Resistant variants of influenza type A have been recoveredfrom rimantadine-treated patients.Resistance with inhibitory concentrations increased morethan 100-fold have been associated with single nucleotidechanges that lead to amino acid substitutions in the transmembranedomain of M2. rimantadineshare cross-susceptibility and resistance.
Pharmaceutical Applications
An analog of amantadine, supplied as the hydrochloride for oral administration.
Mechanism of action
Rimantadine hydrochloride (α-methyl-1-adamantanemethylamine hydrochloride) is a synthetic adamatane derivative that is structurally and pharmacologically related to amantadine. It appears to be more effective than amantadine hydrochloride against influenza A, with fewer CNS side effects. Rimantadine hydrochloride is thought to interfere with virus uncoating by inhibiting the release of specific proteins. It may act by inhibiting RT or the synthesis of virus-specific RNA, but it does not inhibit virus adsorption or penetration. It appears to produce a virustatic effect early in the virus replication. It is used widely in Russia and Europe.
Pharmacokinetics
Oral absorption: >90%
C_max 100 mg oral (every 12 h): 0.4–0.5 mg/L after 2–6 h
Plasma half-life: c. 35 h
Volume of distribution: Very large
Plasma protein binding: c. 40%
Absorption and distribution
Single- and multiple-dose pharmacokinetic studies in elderly patients and young adults are remarkably similar. The steadystate concentration in nasal mucus develops by day 5 at a concentration approximately 1.5-fold higher than plasma.
Metabolism
In contrast to amantadine, rimantadine is extensively metabolized in the liver by hydroxylation and glucuronidation.
Excretion
Less than 20% is excreted unchanged in the urine and most of the breakdown products are excreted by this route. Thus, the plasma half-life is much less affected by renal dysfunction than that of amantadine.
Clinical Use
Prophylaxis and treatment of influenza A H1N1 infections Since prolonged administration is well tolerated by elderly patients, the drug is preferable to amantadine.
부작용
Rimantadine has significantly fewer side effects than amantadine at equivalent doses, perhaps because of differences in pharmacokinetics, since with equal doses the blood levels are considerably lower. CNS side effects are not significantly higher than placebo.

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