アバカビル 化學(xué)特性,用途語,生産方法
外観
白色～ほとんど白色粉末～結(jié)晶
効能
抗ウイルス薬, 逆転寫酵素阻害薬
説明
The drug is extensively metabolized via stepwise phosphorylation to 5′-mono-, di-, and triphosphate. Abacavir is well absorbed (>75%) and penetrates the CNS. The drug can be taken without regard to meals. The drug does not show any clinically significant drug–drug interactions. Abacavir has been reported to produce life-threatening hypersensitivity reactions. The major use of abacavir appears to be in combination with other nucleoside RT inhibitors. A fixed-combination product has recently been approved by the U.S. FDA consisting of 300 mg of ABC, 150 mg of 3TC, and 300 mg of ZDV (Trizivar). The combination has been shown to be superior to other combinations in reducing viral load as well as to show improvement in CD4 cell count.
使用
Abacavir is a commonly used nucleoside analogue with potent antiviral activity against HIV-1. - See more at: http://www.selleckchem.com/products/abacavir-sulfate.html#sthash.lApvcTNO.dpuf
適応癥
Abacavir (Ziagen) is a guanosine nucleoside analogue
indicated for the therapy of HIV-1 infection in adults
and children. It is used as part of a multidrug regimen
and is available in a fixed-dose combination with zidovudine
and lamivudine (Trizivir). It is also used for
postexposure HIV infection prophylaxis.
抗菌性
Abacavir has activity against HIV-1, HIV-2 and human T-cell
lymphotrophic virus type-1 (HTLV-1).
獲得抵抗性
Resistance is associated with specific changes in codons 184
with 65, 74 or 115 in the HIV reverse transcriptase codon
region.
一般的な説明
Abacavir is a nucleoside reverse transcriptase inhibitorNRTI that has been approved for use in combination therapiesfor the treatment of HIV and AIDS. Once in the tissues,it is metabolized by stepwise phosphorylation to themonophosphate, diphosphate, and triphosphate. Abacavir ishighly bioavailable (＞75%) and is effective by the oralroute. It penetrates the blood-brain barrier efficiently.Abacavir has been reported to produce life-threatening hypersensitivityreactions in some patients.
応用例（製薬）
A synthetic analog of guanine formulated for oral use.
薬物動(dòng)態(tài)學(xué)
Oral absorption: 83%
C
max 300 mg oral, twice daily: 3.0 ± 0.89 mg/L
600 mg once daily: 4.26 mg/L
Plasma half-life: 1.5 h
Volume of distribution: 0.8 L/kg
Plasma protein binding: c. 49%
Absorption
After oral administration abacavir sulfate undergoes rapid and extensive absorption unaffected by food.
Distribution
It penetrates well into the cerebrospinal fluid (CSF) and is an NRTI of choice if this characteristic is thought desirable. Good penetration into the male genital tract has been observed. The drug is secreted into human breast milk.
Metabolism
It is primarily metabolized in the liver, mainly by alcohol dehydrogenase and glucuronidation.
Excretion
Around 83% of the dose is eliminated in the urine, <2% as unchanged drug; the remainder is excreted in the feces. Dose adjustment is unnecessary in renal impairment. It can be used in moderate hepatic impairment, but is contraindicated if dysfunction is severe.
臨床応用
Treatment of HIV infection in adults and children (in combination with
other antiretroviral drugs)
副作用
Life-threatening hypersensitivity reactions occur in 5–8%
of all individuals, necessitating discontinuation of the drug.
Typically patients present within the first 6 weeks of starting
treatment with fever, rash or other symptoms that worsen
in severity with continued drug exposure. Hypersensitivity
is associated with carriage of the major histocompatibility
complex class I allele HLA-B57*01 and screening for this
allele can significantly reduce the incidence
of this effect.
Current or recent (within the preceding 6 months) use of
abacavir has been associated with a risk of myocardial infarction,
but studies have yielded conflicting data.
アバカビル 上流と下流の製品情報(bào)
原材料
準(zhǔn)備製品